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US 2026/0152487 A1Published application
Phthalazine derivatives as pyruvate kinase modulators
AssigneeSitryx Therapeutics Limited
InventorsDavid COUSIN, Oscar BARBA
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Abstract
The invention relates to compounds of formula (Ia) and to their use in treating or preventing an inflammatory disease, a disease associated with an undesirable immune response, cancer, obesity, a diabetic disease or a blood disorder: wherein RA, RB, RC and RD, X, Y1, Y2, Y3, Z1, Z2 and m are as defined herein.
Claims50
1-114. (canceled)
115:
- A compound of formula (Ia):
- wherein,
- RA is phenyl, phenyl fused to a 5-7 membered heterocyclic ring, 5-10 membered heteroaryl, or 5-6 membered heteroaryl fused to a 5-7 membered heterocyclic ring;
- wherein RA is optionally substituted on an available atom by one or more R1A, wherein each R1A is independently selected from the group consisting of halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 hydroxyalkyl, C1-6 methoxyalkyl, C1-6 haloalkyl, hydroxy, OC1-6 alkyl, OC1-6 hydroxyalkyl, OC1-6 methoxyalkyl, OC1-6 haloalkyl, cyano, NR2AR3A, C1-6 alkyl-NR2AR3A NHCOCH3, CO2H, CH2CO2H, CONR2AR3A, CH2CONR2AR3A, C3-6 cycloalkyl, oxo, and a 4 membered heterocyclic ring, wherein the 4 membered heterocyclic ring is optionally substituted by hydroxy;
- R2A and R3A are independently selected from the group consisting of H and C1-6 alkyl, or R2A and R3A together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- Y1, Y2 and Y3 are independently selected from the group consisting of CR4A and N, wherein at least two of Y1, Y2 and Y3 are CR4A;
- wherein R4A is selected from the group consisting of H, C1-3 alkyl, C2-3 alkenyl, C2-3 alkynyl, OR8A, halo, cyano, methanesulfonyl, CF3 and NR8AR9A;
- wherein R8A and R9A are independently selected from the group consisting of H and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted on an available carbon atom by one or more groups selected from halo, hydroxy, methoxy, CO2H and NR10AR11A;
- wherein R10A and R11A are independently selected from the group consisting of H and C1-6 alkyl, or R10A and R11A together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- or
- Y2 is absent and one of Y1 and Y3 is S, O or NR5A, and the remaining Y1 or Y3 is N or CR6A;
- wherein R5A is H or C1-3 alkyl;
- and
- R6A is selected from the group consisting of H, C1-3 alkyl, C2-3 alkenyl, C2-3 alkynyl, OR12A, halo, cyano, methanesulfonyl, CF3 and NR12AR13A;
- wherein R12A and R13A are independently selected from the group consisting of H and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted on an available carbon atom by one or more groups selected from halo, hydroxy, methoxy, CO2H and NR14AR15A;
- wherein R14A and R15A are independently selected from the group consisting of H and C1-6 alkyl, or R14A and R15A together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- Z1 and Z2 are independently selected from N and CH, wherein at least one of Z1 and Z2 is CH;
- RB is phenyl, phenyl fused to a 5-7 membered heterocyclic ring, 5-10 membered heteroaryl, 5-6 membered heteroaryl fused to a 5-7 membered heterocyclic ring, 5-7 membered heterocyclyl or C3-6 cycloalkyl;
- wherein RB is optionally substituted on an available atom by one or more R1B, wherein each R1B is independently selected from the group consisting of halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 hydroxyalkyl, C1-6 methoxyalkyl, C1-6 haloalkyl, hydroxy, OC1-6 alkyl, OC1-6 hydroxyalkyl, OC1-6 methoxyalkyl, OC1-6 haloalkyl, cyano, NR2BR3B, C1-6 alkyl-NR2BR3B, NHCOCH3, CO2H, CH2CO2H, CONR2BR3B, CH2CONR2BR3B, C3-6 cycloalkyl, oxo, and a 4 membered heterocyclic ring, wherein the 4 membered heterocyclic ring is optionally substituted by hydroxy;
- R2B and R3B are independently selected from the group consisting of H and C1-6 alkyl, or R2B and R3B together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- RC is H, fluoro, C1-3 alkyl, C1-2 hydroxyalkyl or C1-2 methoxyalkyl;
- RD is H or fluoro;
- m is 0 or 1;
- X is S(═O)1-2, —CH2S(═O)1-2—, S(═O)(═NH), —S(═O)2NH—, —NHS(═O)2—, CH2, —C(RE)(RF)O— or CH2NH—;
- and
- RE and RF are H, or RE and RF join to form a C3-5 heterocycloalkyl ring;
- or a pharmaceutically acceptable salt and/or solvate thereof.
24 more elements
116:
- A compound of formula (Ia) according to claim 115, which is a compound of formula (Ib):
- wherein,
- RA is phenyl, phenyl fused to a 5-7 membered heterocyclic ring, 5-10 membered heteroaryl, or 5-6 membered heteroaryl fused to a 5-7 membered heterocyclic ring;
- wherein RA is optionally substituted on an available carbon or nitrogen atom by one or more R1A wherein each R1A is independently selected from the group consisting of halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 hydroxyalkyl, C1-6 methoxyalkyl, C1-6 haloalkyl, hydroxy, OC1-6 alkyl, OC1-6 hydroxyalkyl, OC1-6 methoxyalkyl, OC1-6 haloalkyl, cyano, NR2AR3A, C1-6 alkyl-NR2AR3A NHCOCH3, CO2H, CH2CO2H, CONR2AR3A, CH2CONR2AR3A, C3-6 cycloalkyl and oxo;
- R2A and R3A are independently selected from the group consisting of H and C1-6 alkyl, or R2A and R3A together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- Y1, Y2 and Y3 are independently selected from the group consisting of CR4A and N, wherein at least two of Y1, Y2 and Y3 are CR4A;
- wherein R4A is selected from the group consisting of H, C1-3 alkyl, C2-3 alkenyl, C2-3 alkynyl, OR8A, halo, cyano, methanesulfonyl, CF3 and NR8AR9A;
- wherein R8A and R9A are independently selected from the group consisting of H and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted on an available carbon atom by one or more groups selected from halo, hydroxy, methoxy, CO2H and NR10AR11A;
- wherein R10A and R11A are independently selected from the group consisting of H and C1-6 alkyl, or R10A and R11A together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- or
- Y2 is absent and one of Y1 and Y3 is S, O or NR5A, and the remaining Y1 or Y3 is N or CR6A;
- wherein R5A is H or C1-3 alkyl;
- and
- R6A is selected from the group consisting of H, C1-3 alkyl, C2-3 alkenyl, C2-3 alkynyl, OR12A, halo, cyano, methanesulfonyl, CF3 and NR12AR13A;
- wherein R12A and R13A are independently selected from the group consisting of H and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted on an available carbon atom by one or more groups selected from halo, hydroxy, methoxy, CO2H and NR14AR15A;
- wherein R14A and R15A are independently selected from the group consisting of H and C1-6 alkyl, or R14A and R15A together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- Z1 and Z2 are independently selected from N and CH, wherein at least one of Z1 and Z2 is CH;
- RB is phenyl, phenyl fused to a 5-7 membered heterocyclic ring, 5-10 membered heteroaryl, 5-6 membered heteroaryl fused to a 5-7 membered heterocyclic ring, 5-7 membered heterocyclyl or C3-6 cycloalkyl;
- wherein RB is optionally substituted on an available carbon or nitrogen atom by one or more R1B, wherein each R1B is independently selected from the group consisting of halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 hydroxyalkyl, C1-6 methoxyalkyl, C1-6 haloalkyl, hydroxy, OC1-6 alkyl, OC1-6 hydroxyalkyl, OC1-6 methoxyalkyl, OC1-6 haloalkyl, cyano, NR2BR3B, C1-6 alkyl-NR2BR3B, NHCOCH3, CO2H, CH2CO2H, CONR2BR3B, CH2CONR2BR3B, C3-6 cycloalkyl and oxo;
- R2B and R3B are independently selected from the group consisting of H and C1-6 alkyl, or R2B and R3B together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- RC is H, fluoro, C1-3 alkyl, C1-2 hydroxyalkyl or C1-2 methoxyalkyl;
- RD is H or fluoro;
- m is 0 or 1;
- X is S(═O)1-2, —CH2S(═O)1-2—, S(═O)(═NH), —S(═O)2NH—, —NHS(═O)2—, CH2, —CH2O— or CH2NH—;
- or a pharmaceutically acceptable salt and/or solvate thereof.
22 more elements
117:
- A compound of formula (Ia) according to claim 115, which is a compound of formula (I):
- wherein,
- RA is phenyl, phenyl fused to a 5-7 membered heterocyclic ring, 5-10 membered heteroaryl, or 5-6 membered heteroaryl fused to a 5-7 membered heterocyclic ring;
- wherein RA is optionally substituted on an available carbon atom by one or more R1A, wherein R1A is independently selected from the group consisting of halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 hydroxyalkyl, C1-6 methoxyalkyl, C1-6 haloalkyl, hydroxy, OC1-6 alkyl, OC1-6 hydroxyalkyl, OC1-6 methoxyalkyl, OC1-6 haloalkyl, cyano, NR2AR3A, C1-6 alkyl-NR2AR3A NHCOCH3, CO2H, CH2CO2H, CONR2AR3A, CH2CONR2AR3A, C3-6 cycloalkyl and oxo;
- R2A and R3A are independently selected from the group consisting of H and C1-6 alkyl, or R2A and R3A together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- Y1, Y2 and Y3 are independently selected from the group consisting of CR4A and N, wherein at least two of Y1, Y2 and Y3 are CR4A;
- wherein R4A is selected from the group consisting of H, C1-3 alkyl, C2-3 alkenyl, C2-3 alkynyl, OR8A, halo, cyano, methanesulfonyl, CF3 and NR8AR9A;
- wherein R8A and R9A are independently selected from the group consisting of H and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted on an available carbon atom by one or more groups selected from halo, hydroxy, methoxy, CO2H and NR10AR11A;
- wherein R10A and R11A are independently selected from the group consisting of H and C1-6 alkyl, or R10A and R11A together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- or
- Y2 is absent and one of Y1 and Y3 is S, O or NR5A, and the remaining Y1 or Y3 is N or CR6A;
- wherein R5A is H or C1-3 alkyl;
- and
- R6A is selected from the group consisting of H, C1-3 alkyl, C2-3 alkenyl, C2-3 alkynyl, OR12A, halo, cyano, methanesulfonyl, CF3 and NR12AR13A;
- wherein R12A and R13A are independently selected from the group consisting of H and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted on an available carbon atom by one or more groups selected from halo, hydroxy, methoxy, CO2H and NR14AR15A;
- wherein R14A and R15A are independently selected from the group consisting of H and C1-6 alkyl, or R14A and R15A together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- Z1 and Z2 are independently selected from N and CH, wherein at least one of Z1 and Z2 is CH;
- RB is phenyl, phenyl fused to a 5-7 membered heterocyclic ring, 5-10 membered heteroaryl, 5-6 membered heteroaryl fused to a 5-7 membered heterocyclic ring, 5-7 membered heterocyclyl or C3-6 cycloalkyl;
- wherein RB is optionally substituted on an available carbon atom by one or more R1B, wherein R1B is independently selected from the group consisting of halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 hydroxyalkyl, C1-6 methoxyalkyl, C1-6 haloalkyl, hydroxy, OC1-6 alkyl, OC1-6 hydroxyalkyl, OC1-6 methoxyalkyl, OC1-6 haloalkyl, cyano, NR2BR3B, C1-6 alkyl-NR2BR3B, NHCOCH3, CO2H, CH2CO2H, CONR2BR3B, CH2CONR2BR3B, C3-6 cycloalkyl and oxo;
- R2B and R3B are independently selected from the group consisting of H and C1-6 alkyl, or R2B and R3B together with the N atom to which they are attached combine to form a 4-7 membered heterocyclic ring which is optionally substituted on an available atom by one or more groups selected from C1-2 alkyl and oxo;
- RC is H, fluoro, C1-3 alkyl, C1-2 hydroxyalkyl or C1-2 methoxyalkyl;
- RD is H or fluoro;
- m is 0 or 1;
- X is S(═O)1-2, —CH2S(═O)1-2—, S(═O)(═NH), —S(═O)2NH—, —NHS(═O)2—, CH2, —CH2O— or CH2NH—;
- or a pharmaceutically acceptable salt and/or solvate thereof.
22 more elements
118:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RA is phenyl, phenyl fused to a 5-6 membered heterocyclic ring, 5-6 membered heteroaryl, or 5-6 membered heteroaryl fused to a 5-6 membered heterocyclic ring, and is optionally substituted on an available atom by one or more R1A.
119:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RA is phenyl optionally substituted on an available carbon atom by one or more R1A.
120:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RA is 5-10 membered heteroaryl, such as selected from the group consisting of pyrrolyl, furanyl, thienyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, triazolyl, oxazolyl, isoxazolyl, tetrazolyl, pyridinyl, pyrimidinyl, pyradizinyl, pyrazinyl, furo[3,2-b]pyridinyl, pyrazolo[1,5-a]pyridinyl, imidazo[1,2-a]pyridinyl, indolyl, indazolyl, benzofuranyl, benzimidazolyl, benzothiazolyl, benzothiophenyl, quinolinyl, isoquinolinyl and quinazolinyl;
- and is optionally substituted on an available atom by one or more R1A.
121:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein each R1A is independently selected from the group consisting of halo, C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 methoxyalkyl, C1-6 haloalkyl, hydroxy, OC1-6 alkyl, OC1-6 hydroxyalkyl, OC1-6 methoxyalkyl, OC1-6 haloalkyl, cyano, NR2AR3A NHCOCH3, CO2H, CONR2AR3A, C3-6 cycloalkyl, oxo, and a 4 membered heterocyclic ring, wherein the 4 membered heterocyclic ring is optionally substituted by hydroxy;
- and in particular is independently selected from halo, C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 methoxyalkyl, C1-6 haloalkyl, hydroxy and OC1-6 alkyl e.g. C1-6 alkyl, OC1-6 alkyl, oxo, and oxetane or azetidine either of which is optionally substituted by hydroxy.
122:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RA is unsubstituted.
123:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RB is selected from the group consisting of phenyl, phenyl fused to a 5-7 membered heterocyclic ring selected from the group consisting of 2,3-dihydrobenzofuranyl, indolinyl, 1,2,3,4-tetrahydroquinolinyl, benzo-1,4-dioxanyl, 1,3-benzodiazole and 3,4-dihydro-2H-1,4-benzoxazine, pyrrolyl, furanyl, thienyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, triazolyl, oxazolyl, isoxazolyl, tetrazolyl, pyridinyl, pyrimidinyl, pyradizinyl, pyrazinyl, furo[3,2-b]pyridinyl, pyrazolo[1,5-a]pyridinyl, imidazo[1,2-a]pyridinyl, indolyl, indazolyl, benzofuranyl, benzimidazolyl, benzothiazolyl, benzothiophenyl, quinolinyl, isoquinolinyl, quinazolinyl, pyrrolidinyl, tetrahydrofuranyl, tetrahydrothienyl, tetrahydropyranyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridone and pyridazinone;
- and is optionally substituted on an available atom by one or more R1B.
124:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RB is phenyl optionally substituted on an available carbon atom by one or more R1B.
125:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RB is 5-10 membered heteroaryl such as selected from the group consisting of pyrrolyl, furanyl, thienyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, triazolyl, oxazolyl, isoxazolyl, tetrazolyl, pyridinyl, pyrimidinyl, pyradizinyl, pyrazinyl, furo[3,2-b]pyridinyl, pyrazolo[1,5-a]pyridinyl, imidazo[1,2-a]pyridinyl, indolyl, indazolyl, benzofuranyl, benzimidazolyl, benzothiazolyl, benzothiophenyl, quinolinyl, isoquinolinyl and quinazolinyl;
- and in particular is selected from the group consisting of furanyl, thienyl, pyrazolyl, thiazolyl, isothiazolyl, isoxazolyl, pyridinyl, pyrazinyl, pyrazolo[1,5-a]pyridinyl, imidazo[1,2-a]pyridinyl and indazolyl;
- and is optionally substituted on an available atom by one or more R1B.
126:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RB is 5-6 membered heteroaryl fused to a 5-7 membered heterocyclic ring, selected group the group consisting of 2,3-dihydropyrazolo[5,1-b]oxazolyl, 2,3-dihydrofuro[2,3-b]pyridinyl, 2,3-dihydrofuro[3,2-b]pyridinyl, 2,3-dihydro-[1,4]dioxino[2,3-c]pyridinyl and 2,3-dihydro-[1,4]dioxino[2,3-b]pyridinyl;
- and is optionally substituted on an available atom (e.g. a carbon or nitrogen atom, in particular a carbon atom) by one or more R1B.
127:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein each R1B is independently selected from the group consisting of halo, C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 haloalkyl, hydroxy, OC1-6 alkyl, OC1-6 hydroxyalkyl, OC1-6 haloalkyl, cyano, NR2BR3B, CONR2BR3B, CH2CONR2BR3B, C3-6 cycloalkyl, oxo, and a 4 membered heterocyclic ring, wherein the 4 membered heterocyclic ring is optionally substituted by hydroxy;
- and in particular is independently selected from the group consisting of fluoro, chloro, methyl, ethyl, CH2OH, CH2CH2OH, CHF2, hydroxy, OCH3, OCH2CH2OH, OCHF2, cyano, NH2, CONH2, CONHCH3, CH2CONH2, cyclopropyl, oxo, and oxetane or azetidine either of which is optionally substituted by hydroxy.
128:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RB is unsubstituted.
129:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein R2B and R3B are independently selected from the group consisting of H and C1-6 alkyl.
130:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein R2B and R3B are both H.
131:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein Y1, Y2 and Y3 are independently selected from the group consisting of CR4A and N, wherein at least two of Y1, Y2 and Y3 are CR4A;
- wherein R4A is as defined in claim 1.
132:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 131, wherein Y1, Y2 and Y3 are all CR4A, wherein suitably R4A is H.
133:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein Z1 is N and Z2 is CH.
134:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RC is H, fluoro, CH3, CH2OH or CH2OCH3, and in particular is H.
135:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RD is H or fluoro, and in particular is H.
136:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein m is 0.
137:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein X is S(═O)2.
138:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein X is S(═O).
139:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein X is —CH2S(═O)1-2—.
140:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein X is S(═O)(═NH).
141:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein X is —S(═O)2NH—.
142:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein X is —NHS(═O)2—.
143:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein X is CH2.
144:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein X is —C(RE)(RF)O— and RE and RF are H or RE and RF join to form a C3-5 heterocycloalkyl ring, such as X is —CH2O—.
145:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein X is CH2NH—.
146:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein the compound of formula (Ia) is a compound of formula (IIa):
- wherein Y1, Y2 and Y3 are independently selected from the group consisting of CR4A and N, wherein at least two of Y1, Y2 and Y3 are CR4A;
- or a pharmaceutically acceptable salt and/or solvate thereof.
147:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 146, wherein the compound of formula (Ia) is a compound of formula (IIaA):
- wherein Y1, Y2 and Y3 are independently selected from the group consisting of CR4A and N, wherein at least two of Y1, Y2 and Y3 are CR4A;
- or a pharmaceutically acceptable salt and/or solvate thereof.
148:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 147, wherein the compound of formula (Ia) is a compound of formula (IIaB):
- or a pharmaceutically acceptable salt and/or solvate thereof.
149:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 148, wherein the compound of formula (Ia) is a compound of formula (IIaC):
- or a pharmaceutically acceptable salt and/or solvate thereof.
150:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 149, wherein the compound of formula (Ia) is a compound of formula (IaD):
- or a pharmaceutically acceptable salt and/or solvate thereof.
151:
- The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, selected from the group consisting of:
- 2-((1-cyclopropyl-1H-pyrazol-3-yl)methyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-(indolin-4-ylmethyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-((2-hydroxypyridin-4-yl)methyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 6-((4-methoxyphenyl)sulfonyl)-2-((1-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1-(2-hydroxyethyl)-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-((5-hydroxypyridin-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(2-methoxy-1-(6-methoxypyridin-3-yl)ethyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 3-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)picolinamide;
- 2-((1-(2-hydroxyethyl)-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1-ethyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((4-methyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 3-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)thiophene-2-carboxamide;
- 6-methoxy-3-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)picolinamide;
- 3-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)-1H-pyrazole-4-carboxamide;
- 2-((1-(2-hydroxyethyl)-4-methyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 3-((6-((4-methoxyphenyl)sulfonyl)-1-oxophthalazin-2(1H)-yl)methyl)-N-methylfuran-2-carboxamide;
- 3-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)-1H-pyrazole-4-carbonitrile;
- 2-(2-hydroxy-1-phenylethyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(2-(hydroxymethyl)benzyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((6-(2-hydroxyethoxy)pyridin-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((2-(hydroxymethyl)thiophen-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 3-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)thiophene-2-carbonitrile;
- 2-((1-(2-hydroxyethyl)-1H-pyrazol-3-yl)methyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-((5-cyclopropyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((4-(hydroxymethyl)-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydropyrazolo[5,1-b]oxazol-6-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1-(difluoromethyl)-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((2-methylthiazol-5-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((5-methoxypyridin-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(2-fluorobenzyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(2-fluoro-5-methoxybenzyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(imidazo[1,2-a]pyridin-5-ylmethyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((2,2-dimethyl-2,3-dihydrobenzofuran-5-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1-methyl-1H-indazol-5-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-2-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((6-aminopyridin-2-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1-methyl-1H-indazol-6-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(3-(difluoromethoxy)benzyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 6-((4-methoxyphenyl)sulfonyl)-2-(pyridin-3-ylmethyl)phthalazin-1(2H)-one;
- 2-(2-aminobenzyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 6-((4-methoxyphenyl)sulfonyl)-2-phenethylphthalazin-1(2H)-one;
- 2-(isoxazol-5-ylmethyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-(4-chloro-2-fluorobenzyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydrobenzofuran-5-yl)methyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-indazol-3-yl)methyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-(4-methoxybenzyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-benzyl-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 6-((4-methoxyphenyl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-(2-fluoro-3-methoxybenzyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-(2,6-difluoro-4-methoxybenzyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 6-((4-methoxyphenyl)sulfonyl)-2-((5-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((2-hydroxypyridin-4-yl)methyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-((2-hydroxypyridin-3-yl)methyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-(benzo[d][1,3]dioxol-5-ylmethyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1H-indazol-6-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((5-methoxypyridin-2-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(2-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)phenyl)acetamide;
- 2-((6-(difluoromethoxy)pyridin-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(2-(2-hydroxyethyl)benzyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((2-methyl-2,3-dihydrobenzofuran-5-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 6-(phenylsulfonyl)-2-(pyridin-3-ylmethyl)phthalazin-1(2H)-one;
- 2-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)benzamide;
- 2-(2-methoxy-1-phenylethyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 6-(phenylsulfonyl)-2-(1-(pyridin-3-yl)ethyl)phthalazin-1(2H)-one;
- 2-((1,3-dimethyl-1H-pyrazol-4-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-benzyl-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 6-((4-methoxyphenyl)sulfonyl)-2-((1-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1-cyclopropyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(1-(6-methoxypyridin-3-yl)ethyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((6-methylpyridin-2-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((4-chloro-1-methyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((2-methylthiazol-4-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(difluoro(pyridin-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(2-methoxybenzyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((5-methylisoxazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(3-methoxybenzyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(2-methoxy-1-phenylethyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1-ethyl-1H-pyrazol-5-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 3-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)benzamide;
- 3-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)furan-2-carboxamide;
- 5-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)furan-2-carboxamide;
- 2-((5-methoxypyrazin-2-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((2-methoxypyridin-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1,4-dimethyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1,5-dimethyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-chloro-6-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)benzamide;
- 2-methoxy-6-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)benzamide;
- 4-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl)thiazole-2-carboxamide;
- 5-methyl-4-((1-oxo-6-(phenylsulfonyl)phthalazin-2(1H)-yl)methyl) isoxazole-3-carboxamide;
- 2-((1-isopropyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((5-methyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((3-methylisothiazol-5-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((2-hydroxy-6-methylpyridin-3-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 2-((2-hydroxy-4-methylpyridin-3-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 2-((5-fluoro-2-hydroxypyridin-3-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 2-((2-hydroxy-5-isopropylpyridin-3-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 2-((4-chloro-2-hydroxypyridin-3-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 2-((4-fluoro-2-hydroxypyridin-3-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 6-((4-methoxyphenyl)sulfonyl)-2-((4-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((3-hydroxypyridin-4-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 5-methoxy-2-((6-(4-methoxyphenylsulfonyl)-1-oxophthalazin-2(1H)-yl)methyl)benzamide;
- 2-((4-hydroxypyridin-3-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 6-(phenylsulfonyl)-2-(pyrazolo[1,5-a]pyridin-2-ylmethyl)phthalazin-1(2H)-one;
- 2-((2-hydroxy-6-methoxypyridin-3-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 2-((4-fluoro-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((5-fluoro-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 6-(4-methoxyphenylsulfonyl)-2-((3-(trifluoromethyl)isoxazol-5-yl)methyl)phthalazin-1(2H)-one;
- 6-(4-methoxyphenylsulfonyl)-2-((3-(trifluoromethyl)isoxazol-5-yl)methyl)phthalazin-1(2H)-one;
- 2-((3-hydroxypyridin-2-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 2-(3-aminobenzyl)-6-(quinolin-8-ylsulfonyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-(5-methylpyridin-2-ylsulfonyl)phthalazin-1(2H)-one;
- 6-(3-methoxyphenylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 3-(2-((6-methoxypyridin-3-yl)methyl)-1-oxo-1,2-dihydrophthalazin-6-ylsulfonyl)thiophene-2-carboxamide;
- 4-(2-((6-methoxypyridin-3-yl)methyl)-1-oxo-1,2-dihydrophthalazin-6-ylsulfonyl)thiophene-2-carboxamide;
- 2-(3-aminobenzyl)-6-(phenylsulfinyl)phthalazine-1(2H)-one;
- 2-(3-aminobenzyl)-6-(phenylsulfonimidoyl)phthalazin-1(2H)-one;
- 2-(3-aminobenzyl)-6-(pyridin-3-ylsulfonyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-1-oxo-N-phenyl-1,2-dihydrophthalazine-6-sulfonamide;
- 6-((1H-indazol-4-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((6-(difluoromethoxy)pyridin-3-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 3-((6-methoxypyridin-3-yl)methyl)-7-((3-phenyloxetan-3-yl)oxy)pyrido[3,4-d]pyridazin-4(3H)-one;
- 6-((2,3-dihydrobenzofuran-5-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(2,3-dihydrobenzofuran-5-sulfonimidoyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- (R)-6-(2,3-dihydrobenzofuran-5-sulfonimidoyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- (S)-6-(2,3-dihydrobenzofuran-5-sulfonimidoyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-7-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-(phenylsulfonimidoyl)phthalazin-1(2H)-one;
- R)-2-((6-methoxypyridin-3-yl)methyl)-6-(phenylsulfonimidoyl)phthalazin-1(2H)-one;
- (S)-2-((6-methoxypyridin-3-yl)methyl)-6-(phenylsulfonimidoyl)phthalazin-1(2H)-one;
- 6-(4-(difluoromethoxy)phenylsulfonimidoyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- (R)-6-(4-(difluoromethoxy)phenylsulfonimidoyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- (S)-6-(4-(difluoromethoxy)phenylsulfonimidoyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(4-methoxyphenylsulfonimidoyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- (R)-6-(4-methoxyphenylsulfonimidoyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- (S)-6-(4-methoxyphenylsulfonimidoyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-3-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-(3-aminobenzyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-(3-aminobenzyl)-6-((4-methoxyphenyl)sulfonyl)phthalazin-1(2H)-one;
- 2-(3-aminobenzyl)-6-((2,3-dihydrobenzofuran-5-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-(3-aminobenzyl)-6-(pyridin-2-ylsulfonyl)phthalazin-1(2H)-one;
- 2-(3-aminobenzyl)-6-((1-methyl-1H-pyrazol-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-(3-aminobenzyl)-6-((5-methylthiophen-2-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((4-fluorophenyl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-(3-methylisothiazol-5-ylsulfonyl)phthalazin-1(2H)-one;
- 2-(3-aminobenzyl)-6-((6-methoxypyridin-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-tosylphthalazin-1(2H)-one;
- 2-(3-aminobenzyl)-6-((2-methylthiazol-4-yl)sulfonyl)phthalazine-1(2H)-one;
- 2-(3-aminobenzyl)-6-(benzo[d][1,3]dioxol-5-ylsulfonyl)phthalazin-1(2H)-one;
- 6-(4-(difluoromethoxy)phenylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((3-chlorophenyl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((4-chlorophenyl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((3-fluorophenyl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-((1-methyl-1H-pyrazol-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-(4-methylpyridin-2-ylsulfonyl)phthalazin-1(2H)-one;
- 6-(6-methoxypyridin-2-ylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 3-(2-((6-methoxypyridin-3-yl)methyl)-1-oxo-1,2-dihydrophthalazin-6-ylsulfonyl)benzamide;
- 6-(2-fluorophenylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(2-chlorophenylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(2-methoxyphenylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(4-methoxypyridin-2-ylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((2,2-dimethyl-2,3-dihydrobenzofuran-5-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-((2-methyl-2,3-dihydrobenzofuran-5-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-(6-methylpyridin-2-ylsulfonyl)phthalazin-1(2H)-one;
- 6-(3-(difluoromethoxy)phenylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-(5-methylthiophen-2-ylsulfonyl)phthalazin-1(2H)-one;
- 6-(5-methoxypyridin-2-ylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(2-(difluoromethyl)thiazol-5-ylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-(2-methylthiazol-4-ylsulfonyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-(6-methoxypyridin-3-ylsulfonyl)phthalazin-1(2H)-one;
- 2-((6-methoxypyridin-3-yl)methyl)-6-(2-methylbenzo[d]thiazol-4-ylsulfonyl)phthalazin-1(2H)-one;
- 6-(5-methoxypyrazin-2-ylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(imidazo[1,2-a]pyridin-5-ylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(1-(difluoromethyl)-1H-pyrazol-3-ylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- (S)-6-(2,3-dihydrobenzofuran-5-sulfonimidoyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((2,3-dihydrofuro[2,3-b]pyridin-5-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(imidazo[1,2-a]pyridin-7-ylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(1,2-dimethyl-1H-imidazol-4-ylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(1,5-dimethyl-1H-pyrazol-4-ylsulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- (S)-6-(4-methoxyphenylsulfonimidoyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(1-cyclopropyl-1H-pyrazol-4-ylsulfonyl)-2-((2-hydroxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-(1-cyclopropyl-1H-pyrazol-4-ylsulfonyl)-2-((1-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-(benzofuran-5-ylsulfonyl)phthalazin-1(2H)-one;
- 2-((1-cyclopropyl-1H-pyrazol-3-yl)methyl)-6-((1-cyclopropyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-(3-(difluoromethoxy)benzyl)-6-((1-methyl-1H-pyrazol-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-(2-fluoro-5-methoxybenzyl)-6-((1-methyl-1H-pyrazol-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((2-hydroxypyridin-3-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)sulfonyl)-2-((1-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)sulfonyl)-2-((1-(2-hydroxyethyl)-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((2,3-dihydrobenzofuran-5-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((1-cyclopropyl-1H-pyrazol-3-yl)methyl)-6-((6-methoxypyridin-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)sulfonyl)-2-((1-(2-hydroxyethyl)-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)sulfonyl)phthalazine-1(2H)-one;
- 6-((2,3-dihydrobenzofuran-5-yl)sulfonyl)-2-((4-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((2,3-dihydrobenzofuran-5-yl)sulfonyl)-2-((5-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((6-(1-methyl-1H-pyrazol-3-ylsulfonyl)-1-oxophthalazin-2(1H)-yl)methyl)benzamide;
- 2-((1H-pyrazol-3-yl)methyl)-6-(pyridin-2-ylsulfonyl)phthalazin-1(2H)-one;
- 6-((4-(difluoromethoxy)phenyl)sulfonyl)-2-((1-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-((2-methyl-2,3-dihydrobenzofuran-5-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-((2-methylthiazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)sulfonyl)-2-((1-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((4-ethoxyphenyl)sulfonyl)-2-((1-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- (R)-2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-((2-methyl-2,3-dihydrobenzofuran-5-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-((4-(trifluoromethoxy)phenyl)sulfonyl)phthalazin-1(2H)-one;
- (S)-2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-((2-methyl-2,3-dihydrobenzofuran-5-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((3-methylbenzofuran-5-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-(benzofuran-6-ylsulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-(furo[3,2-b]pyridin-5-ylsulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((2-methylbenzofuran-5-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-(furo[2,3-b]pyridin-5-ylsulfonyl)phthalazin-1(2H)-one;
- 6-((1H-indol-5-yl)sulfonyl)-2-((1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-(benzo[b]thiophen-5-ylsulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((1-cyclopropyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-6-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((2,3-dihydro-[1,4]dioxino[2,3-c]pyridin-7-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((1-methyl-1H-indol-5-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((1-cyclopropyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-(pyridin-3-ylsulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-7-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((6-methoxypyridin-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1-cyclopropyl-1H-pyrazol-3-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-(1-(2-hydroxyethyl)-1H-pyrazol-3-ylsulfonyl)-2-((2-hydroxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-3-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((1-(2-hydroxyethyl)-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 7-fluoro-2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 5-fluoro-2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 7-((2-hydroxyethyl)amino)-2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 8-fluoro-2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 7-((2-hydroxyethyl)amino)-2-((2-hydroxypyridin-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 5-((2-hydroxyethyl)amino)-2-((2-hydroxypyridin-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 3-((1-methyl-1H-pyrazol-3-yl)methyl)-7-(phenylsulfonyl)pyrido[3,4-d]pyridazin-4(3H)-one;
- 3-((1-methyl-1H-pyrazol-3-yl)methyl)-7-(phenylsulfinyl)pyrido[3,4-d]pyridazin-4(3H)-one;
- 7-((1-methyl-1H-pyrazol-3-yl)methyl)-3-(phenylsulfonyl)pyrido[2,3-d]pyridazin-8(7H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((5-fluoro-6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((3-fluoro-6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 6-(1H-pyrazol-4-ylsulfonyl)-2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-(pyridin-4-ylsulfonyl)phthalazin-1(2H)-one;
- 2-((2,4-dihydroxypyridin-3-yl)methyl)-6-(4-methoxyphenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1-cyclopropyl-1H-pyrazol-3-yl)methyl)-6-(furo[3,2-b]pyridin-5-ylsulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((5-methoxypyridin-2-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((2,3-dihydrofuro[2,3-c]pyridin-5-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1-cyclopropyl-1H-pyrazol-4-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-(pyrazin-2-ylsulfonyl)phthalazin-1(2H)-one;
- 2-(imidazo[1,2-a]pyridin-3-ylmethyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((1-methyl-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonimidoyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-7-((2-hydroxyethyl)amino)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 6-((1-(2-hydroxyethyl)-1H-pyrazol-4-yl)sulfonyl)-2-((1-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1-cyclopropyl-1H-pyrazol-3-yl)methyl)-7-((2-hydroxyethyl)amino)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 3-((1H-pyrazol-3-yl)methyl)-7-((1-methyl-1H-pyrazol-4-yl)sulfonyl)pyrido[3,4-d]pyridazin-4(3H)-one;
- 7-((1H-pyrazol-3-yl)methyl)-3-((1-methyl-1H-pyrazol-4-yl)sulfonyl)pyrido[2,3-d]pyridazin-8(7H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-7-((2-hydroxyethyl)amino)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((1-(2-hydroxyethyl)-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((6-methylpyridin-2-yl)methyl)-6-((1-(oxetan-3-yl)-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1-(2-hydroxyethyl)-1H-pyrazol-4-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1-cyclopropyl-1H-pyrazol-3-yl)methyl)-6-((1-(2-hydroxyethyl)-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1-(oxetan-3-yl)-1H-pyrazol-3-yl)methyl)-6-(phenylsulfonyl)phthalazin-1(2H)-one;
- 2-((6-(1-hydroxyethyl)pyridin-2-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((6-cyclopropylpyridin-2-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1-(azetidin-3-yl)-1H-pyrazol-4-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 6-((1-(2-aminoethyl)-1H-pyrazol-4-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- (S)-2-((6-(1-hydroxyethyl)pyridin-2-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- (R)-2-((6-(1-hydroxyethyl)pyridin-2-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1-(2-hydroxyethyl)-1H-pyrazol-3-yl)sulfonyl)-2-((6-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((1-(2-methoxyethyl)-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((2-(1-hydroxyethyl)thiazol-4-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((6-(3-hydroxyoxetan-3-yl)pyridin-2-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((2-methoxypyridin-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((1-(2-hydroxyethyl)-1H-pyrazol-3-yl)methyl)-6-((6-methoxypyridin-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((6-methoxypyridin-2-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((6-cyclopropylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((6-methylpyridin-2-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((5-methylpyridin-2-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((6-methylpyridin-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-(1H-pyrazol-4-ylsulfonyl)-2-((5-methoxy-6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((1-(2-hydroxyethyl)-1H-pyrazol-3-yl)methyl)-6-((5-methoxypyridin-2-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-(1H-pyrazol-4-ylsulfonyl)-2-((2,3-dihydrofuro[2,3-b]pyridin-5-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((6-methoxypyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((6-methylpyridin-3-yl)methyl)phthalazin-1(2H)-one;
- (R)-6-((2-(1-hydroxyethyl)thiazol-4-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- (S)-6-((2-(1-hydroxyethyl)thiazol-4-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-(furo[3,2-b]pyridin-5-ylmethyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-3-yl)sulfonyl)-2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)phthalazin-1(2H)-one;
- 7-((1H-pyrazol-4-yl)sulfonyl)-3-((5-methyl-1H-pyrazol-3-yl)methyl)pyrido[3,4-d]pyridazin-4(3H)-one;
- 6-((1H-pyrazol-5-yl)sulfonyl)-2-((3-fluoro-6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-5-yl)sulfonyl)-2-((6-cyclopropylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-5-yl)sulfonyl)-2-((5-fluoro-6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((5-methoxypyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((1-(difluoromethyl)-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((1-methyl-1H-pyrazol-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((6-cyclopropylpyridin-2-yl)methyl)-6-((1-(2-hydroxyethyl)-1H-pyrazol-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((4-chloro-1-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)-6-((1-(2-hydroxyethyl)-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((1,5-dimethyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((1-(2-hydroxyethyl)-1H-pyrazol-4-yl)sulfonyl)-2-((5-methoxypyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((5-methyl-1H-pyrazol-3-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((4-methyl-1H-pyrazol-3-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((4-chloro-5-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((1-(difluoromethyl)-1H-pyrazol-4-yl)sulfonyl)-2-((5-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((4-fluoro-1H-pyrazol-3-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((5-chloro-1H-pyrazol-3-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((3-chloro-1H-pyrazol-4-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 6-((4-chloro-1H-pyrazol-3-yl)sulfonyl)-2-((6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((2-methylthiazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((3-fluoro-5,6-dimethylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((5-fluoro-1H-pyrazol-3-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((2,3-dihydropyrazolo[5,1-b]oxazol-6-yl)methyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydropyrazolo[5,1-b]oxazol-6-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-3-yl)sulfonyl)-2-((5-methoxypyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((3-fluoro-6-methoxypyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)-6-((2-(1-hydroxyethyl)thiazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-3-yl)sulfonyl)-2-((1-(difluoromethyl)-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-3-yl)sulfonyl)-2-((3-fluoro-6-methoxypyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 2-(furo[3,2-b]pyridin-5-ylmethyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 3-((5-methyl-1H-pyrazol-3-yl)methyl)-7-((1-methyl-1H-pyrazol-4-yl)sulfonyl)pyrido[3,4-d]pyridazin-4(3H)-one;
- 6-((1H-pyrazol-3-yl)sulfonyl)-2-((4-chloro-5-methyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)-6-((1-(2-methoxyethyl)-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)-6-((1-(oxetan-3-yl)-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-3-yl)sulfonyl)-2-(furo[3,2-b]pyridin-5-ylmethyl)phthalazin-1(2H)-one;
- 2-(furo[3,2-b]pyridin-5-ylmethyl)-6-((1-methyl-1H-pyrazol-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((4-chloro-5-methyl-1H-pyrazol-3-yl)methyl)-6-((1-methyl-1H-pyrazol-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((4-chloro-1,5-dimethyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-5-yl)sulfonyl)-2-((1-cyclopropyl-1H-pyrazol-3-yl)methyl)phthalazin-1(2H)-one;
- 6-((1-(difluoromethyl)-1H-pyrazol-4-yl)sulfonyl)-2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)-6-(1H-pyrazole-4-sulfonimidoyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((3,5-difluoro-6-methylpyridin-2-yl)methyl)phthalazin-1(2H)-one;
- 7-((1-(difluoromethyl)-1H-pyrazol-4-yl)sulfonyl)-3-((5-methyl-1H-pyrazol-3-yl)methyl)pyrido[3,4-d]pyridazin-4(3H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-6-yl)methyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((2-methylfuro[3,2-b]pyridin-5-yl)methyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((2-cyclopropylthiazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 7-((1H-pyrazol-4-yl)sulfonyl)-3-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)pyrido[3,4-d]pyridazin-4(3H)-one;
- 2-((4,5-dimethyl-1H-pyrazol-3-yl)methyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((4-chloro-5-methyl-1H-pyrazol-3-yl)methyl)-6-((1-(difluoromethyl)-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)-6-((2-(1-methoxyethyl)thiazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((2-(1-methoxyethyl)thiazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-(furo[3,2-b]pyridin-5-ylmethyl)-6-((2-(1-methoxyethyl)thiazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((3-fluoro-5,6-dimethylpyridin-2-yl)methyl)-6-((2-(1-methoxyethyl)thiazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 6-((1H-pyrazol-4-yl)sulfonyl)-2-((3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazin-6-yl)methyl)phthalazin-1(2H)-one;
- 6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-2-((7-methyl-2,3-dihydropyrazolo[5,1-b]oxazol-6-yl)methyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydropyrazolo[5,1-b]oxazol-6-yl)methyl)-6-((2-(1-methoxyethyl)thiazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydropyrazolo[5,1-b]oxazol-6-yl)methyl)-6-((2-methylthiazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((5-methyl-1H-pyrazol-3-yl)methyl)-6-((2-methylthiazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)-6-((5-methyl-1H-pyrazol-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)-6-((1-(2-methoxyethyl)-1H-pyrazol-3-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-((1H-pyrazol-3-yl)methyl)-6-((1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)sulfonyl)phthalazin-1(2H)-one;
- 2-[(7-methyl-2,3-dihydropyrazolo[5,1-b]oxazol-6-yl)methyl]-6-(1H-pyrazol-4-ylsulfonyl)phthalazin-1-one;
- (R)-2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)-6-(1H-pyrazole-4-sulfonimidoyl)phthalazin-1(2H)-one;
- and
- (S)-2-((2,3-dihydrofuro[3,2-b]pyridin-5-yl)methyl)-6-(1H-pyrazole-4-sulfonimidoyl)phthalazin-1(2H)-one;
- or a pharmaceutically acceptable salt and/or solvate thereof.
359 more elements
152:
- A pharmaceutical composition comprising a compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 1, and one or more pharmaceutically acceptable diluents or carriers.
153:
- A method of treating or preventing a disease, disorder or condition associated with the function of PK, in particular PKM2 and/or PKLR, which comprises administering a compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 1.
154:
- The method according to claim 153, for treating or preventing an inflammatory disease, a disease associated with an undesirable immune response, cancer, obesity, a diabetic disease or a blood disorder.
155:
- The method according to claim 154, wherein the inflammatory disease or disease associated with an undesirable immune response is, or is associated with, a disease selected from the group consisting of:
- psoriasis, asthma, chronic obstructive pulmonary disease (COPD), heart failure, myocardial infarction, angina pectoris, other atherosclerosis and/or atherothrombosis-related disorders, a mitochondrial and neurodegenerative disease, autoimmune paraneoplastic retinopathy, transplantation rejection, multiple sclerosis, transverse myelitis, ischaemia-reperfusion injury, AGE-induced genome damage, an inflammatory bowel disease, primary sclerosing cholangitis (PSC), PSC-autoimmune hepatitis overlap syndrome, non-alcoholic fatty liver disease (non-alcoholic steatohepatitis), rheumatica, granuloma annulare, cutaneous lupus erythematosus (CLE), systemic lupus erythematosus (SLE), lupus nephritis, drug-induced lupus, autoimmune myocarditis or myopericarditis, Dressler's syndrome, giant cell myocarditis, post-pericardiotomy syndrome, drug-induced hypersensitivity syndromes, eczema, sarcoidosis, erythema nodosum, acute disseminated encephalomyelitis (ADEM), neuromyelitis optica spectrum disorders, MOG (myelin oligodendrocyte glycoprotein) antibody-associated disorders, optic neuritis, CLIPPERS (chronic lymphocytic inflammation with pontine perivascular enhancement responsive to steroids), diffuse myelinoclastic sclerosis, Addison's disease, alopecia areata, ankylosing spondylitis, other spondyloarthritides, antiphospholipid antibody syndrome, autoimmune hemolytic anaemia, autoimmune hepatitis, autoimmune inner ear disease, pemphigoid, linear IgA disease, Behçet's disease, celiac disease, Chagas disease, dermatomyositis, diabetes mellitus type I, endometriosis, Goodpasture's syndrome, Graves' disease, Guillain-Barre syndrome and its subtypes, progressive inflammatory neuropathy, Hashimoto's disease, hidradenitis suppurativa, inclusion body myositis, necrotising myopathy, Kawasaki disease, IgA nephropathy, Henoch-Schonlein purpura, idiopathic thrombocytopenic purpura, thrombotic thrombocytopenic purpura (TTP), Evans' syndrome, interstitial cystitis, mixed connective tissue disease, undifferentiated connective tissue disease, morphea, myasthenia gravis, narcolepsy, neuromyotonia, pemphigus vulgaris, pernicious anaemia, psoriatic arthritis, polymyositis, primary biliary cholangitis (also known as primary biliary cirrhosis), rheumatoid arthritis, palindromic rheumatism, schizophrenia, autoimmune (meningo-)encephalitis syndromes, scleroderma, Sjogren's syndrome, stiff person syndrome, polymylagia rheumatica, giant cell arteritis (temporal arteritis), Takayasu arteritis, polyarteritis nodosa, Kawasaki disease, granulomatosis with polyangitis (GPA;
- formerly known as Wegener's granulomatosis), eosinophilic granulomatosis with polyangiitis (EGPA;
- formerly known as Churg-Strauss syndrome), microscopic polyarteritis/polyangiitis, hypocomplementaemic urticarial vasculitis, hypersensitivity vasculitis, cryoglobulinemia, thromboangiitis obliterans (Buerger's disease), vasculitis, leukocytoclastic vasculitis, vitiligo, acute disseminated encephalomyelitis, adrenoleukodystrophy, Alexander's disease, Alper's disease, balo concentric sclerosis or Marburg disease, cryptogenic organising pneumonia (formerly known as bronchiolitis obliterans organizing pneumonia), Canavan disease, central nervous system vasculitic syndrome, Charcot-Marie-Tooth disease, childhood ataxia with central nervous system hypomyelination, chronic inflammatory demyelinating polyneuropathy (CIDP), diabetic retinopathy, globoid cell leukodystrophy (Krabbe disease), graft-versus-host disease (GVHD), hepatitis C (HCV) infection or complication, herpes simplex viral infection or complication, human immunodeficiency virus (HIV) infection or complication, lichen planus, monomelic amyotrophy, fibrosis, cystic fibrosis, pulmonary arterial hypertension (PAH), lung sarcoidosis, idiopathic pulmonary fibrosis, kidney fibrosis, paediatric asthma, atopic dermatitis, allergic dermatitis, contact dermatitis, allergic rhinitis, rhinitis, sinusitis, conjunctivitis, allergic conjunctivitis, keratoconjunctivitis sicca, dry eye, xerophthalmia, glaucoma, macular oedema, diabetic macular oedema, central retinal vein occlusion (CRVO), macular degeneration, post-operative cataract inflammation, uveitis, iridocyclitis, scleritis, corneal graft and limbal cell transplant rejection, gluten sensitive enteropathy (coeliac disease), dermatitis herpetiformis, eosinophilic esophagitis, achalasia, autoimmune dysautonomia, autoimmune encephalomyelitis, autoimmune oophoritis, autoimmune orchitis, autoimmune pancreatitis, aortitis and periaortitis, autoimmune retinopathy, autoimmune urticaria, Behcet's disease, (idiopathic) Castleman's disease, Cogan's syndrome, IgG4-related disease, retroperitoneal fibrosis, juvenile idiopathic arthritis, adult-onset Still's disease, ligneous conjunctivitis, Mooren's ulcer, pityriasis lichenoides et varioliformis acuta (PLEVA, also known as Mucha-Habermann disease), multifocal motor neuropathy (MMN), paediatric acute-onset neuropsychiatric syndrome (PANS), paraneoplastic syndromes, perivenous encephalomyelitis, reflex sympathetic dystrophy, relapsing polychondritis, sperm & testicular autoimmunity, Susac's syndrome, Tolosa-Hunt syndrome, Vogt-Koyanagi-Harada Disease, anti-synthetase syndrome, autoimmune enteropathy, immune dysregulation polyendocrinopathy enteropathy X-linked (IPEX), microscopic colitis, autoimmune lymphoproliferative syndrome (ALPS), autoimmune polyendocrinopathy-candidiasis-ectodermal dystrophy syndrome (APEX), gout, pseudogout, amyloid, eosinophilic fasciitis (Shulman syndrome) progesterone hypersensitivity, Familial Mediterranean fever (FMF), tumour necrosis factor (TNF) receptor-associated periodic fever syndrome (TRAPS), hyperimmunoglobulinaemia D with periodic fever syndrome (HIDS), PAPA (pyogenic arthritis, pyoderma gangrenosum, severe cystic acne) syndrome, deficiency of interleukin-1 receptor antagonist (DIRA), deficiency of the interleukin-36-receptor antagonist (DITRA), cryopyrin-associated periodic syndromes (CAPS), NLRP12-associated autoinflammatory disorders (NLRP12AD), periodic fever aphthous stomatitis (PFAPA), chronic atypical neutrophilic dermatosis with lipodystrophy and elevated temperature (CANDLE), Majeed syndrome, Blau syndrome (also known as juvenile systemic granulomatosis), macrophage activation syndrome, chronic recurrent multifocal osteomyelitis (CRMO), familial cold autoinflammatory syndrome, mutant adenosine deaminase 2 and monogenic interferonopathies, Schnitzler syndrome;
- familial cylindromatosis, congenital B cell lymphocytosis, OTULIN-related autoinflammatory syndrome, type 2 diabetes mellitus, insulin resistance and the metabolic syndrome, atherosclerotic disorders, and renal inflammatory disorders.
2 more elements
156:
- The method according to claim 155, wherein the inflammatory disease or disease associated with an undesirable immune response is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, systemic lupus erythematosus, multiple sclerosis, psoriasis, inflammatory bowel disease, atopic dermatitis, fibrosis, uveitis, cryopyrin-associated periodic syndromes, Muckle-Wells syndrome, juvenile idiopathic arthritis, chronic obstructive pulmonary disease and asthma.
157:
- The method according to claim 154, wherein cancer is selected from the group consisting of acute lymphoblastic leukaemia, adult;
- acute lymphoblastic leukaemia, childhood;
- acute myeloid leukaemia, adult;
- adrenocortical carcinoma;
- adrenocortical carcinoma, childhood;
- aids-related lymphoma;
- aids-related malignancies;
- anal cancer;
- astrocytoma, childhood cerebellar;
- astrocytoma, childhood cerebral;
- Barrett's esophagus (pre-malignant syndrome);
- bile duct cancer, extrahepatic;
- bladder cancer;
- bladder cancer, childhood;
- bone cancer, osteosarcoma/malignant fibrous histiocytoma;
- brain stem glioma, childhood;
- brain tumour, adult;
- brain tumour, brain stem glioma, childhood;
- brain tumour, cerebellar astrocytoma, childhood;
- brain tumour, cerebral astrocytoma/malignant glioma, childhood;
- brain tumour, ependymoma, childhood;
- brain tumour, medulloblastoma, childhood;
- brain tumour, supratentorial primitive neuroectodermal tumours, childhood;
- brain tumour, visual pathway and hypothalamic glioma, childhood;
- brain tumour, childhood (other);
- breast cancer;
- breast cancer and pregnancy;
- breast cancer, childhood;
- breast cancer, male;
- bronchial adenomas/carcinoids, childhood;
- carcinoid tumour, childhood;
- carcinoid tumour, gastrointestinal;
- carcinoma, adrenocortical;
- carcinoma, islet cell;
- carcinoma of unknown primary;
- central nervous system lymphoma, primary;
- cerebellar astrocytoma, childhood;
- cerebral astrocytoma/malignant glioma, childhood;
- cervical cancer;
- childhood cancers;
- chronic lymphocytic leukaemia;
- chronic myelogenous leukaemia;
- chronic myeloproliferative disorders;
- clear cell sarcoma of tendon sheaths;
- colon cancer;
- colorectal cancer;
- colorectal cancer, childhood;
- cutaneous t-cell lymphoma;
- endometrial cancer;
- ependymoma, childhood;
- epithelial cancer, ovarian;
- oesophageal cancer;
- oesophageal cancer, childhood;
- Ewing's family of tumours;
- extracranial germ cell tumour, childhood;
- extragonadal germ cell tumour;
- extrahepatic bile duct cancer;
- eye cancer, intraocular melanoma;
- eye cancer, retinoblastoma;
- gallbladder cancer;
- gastric (stomach) cancer;
- gastric (stomach) cancer, childhood;
- gastrointestinal carcinoid tumour;
- germ cell tumour, extracranial, childhood;
- germ cell tumour, extragonadal;
- germ cell tumour, ovarian;
- gestational trophoblastic tumour;
- glioma, childhood brain stem;
- glioma, childhood visual pathway and hypothalamic;
- hairy cell leukaemia;
- head and neck cancer;
- hepatocellular (liver) cancer;
- hepatocellular (liver) cancer, adult (primary);
- hepatocellular (liver) cancer, childhood (primary);
- cancer of the esophagus;
- Hodgkin's lymphoma;
- Hodgkin's lymphoma, adult;
- Hodgkin's lymphoma, childhood;
- Hodgkin's lymphoma during pregnancy;
- hypopharyngeal cancer;
- hypothalamic and visual pathway glioma, childhood;
- intraocular melanoma;
- islet cell carcinoma (endocrine pancreas);
- cancer of the endocrine system;
- Kaposi's sarcoma;
- kidney cancer;
- laryngeal cancer;
- laryngeal cancer, childhood;
- leukaemia, acute lymphoblastic, adult;
- leukaemia, acute lymphoblastic, childhood;
- leukaemia, acute myeloid, adult;
- leukaemia, acute myeloid, childhood;
- leukaemia, chronic lymphocytic;
- leukaemia, chronic myelogenous;
- leukaemia, hairy cell;
- lymphocytic lymphoma;
- lip and oral cavity cancer;
- liver cancer, adult (primary);
- liver cancer, childhood (primary);
- lung cancer;
- lung cancer, non-small cell;
- lung cancer, small cell;
- lymphoblastic leukaemia, adult acute;
- lymphoblastic leukaemia, childhood acute;
- lymphocytic leukaemia, chronic;
- lymphoma, aids-related;
- lymphoma, central nervous system (primary);
- lymphoma, cutaneous t-cell;
- lymphoma, Hodgkin's, adult;
- lymphoma, Hodgkin's, childhood;
- lymphoma, Hodgkin's during pregnancy;
- lymphoma, non-Hodgkin's, adult;
- lymphoma, non-Hodgkin's, childhood;
- lymphoma, non-Hodgkin's during pregnancy;
- lymphoma, primary central nervous system;
- macroglobulinemia, Waldenstrom's;
- male breast cancer;
- malignant mesothelioma, adult;
- malignant mesothelioma, childhood;
- malignant thymoma;
- medulloblastoma, childhood;
- melanoma;
- melanoma, intraocular;
- Merkel cell carcinoma;
- mesothelioma, malignant;
- metastatic squamous neck cancer with occult primary;
- multiple endocrine neoplasia syndrome, childhood;
- multiple myeloma/plasma cell neoplasm;
- mycosis fungoides;
- myelodysplastic syndromes;
- myelogenous leukaemia, chronic;
- myeloid leukaemia, childhood acute;
- myeloma, multiple;
- myeloproliferative disorders, chronic;
- nasal cavity and paranasal sinus cancer;
- nasopharyngeal cancer;
- nasopharyngeal cancer, childhood;
- neoplastic cutaneous disease;
- neuroblastoma;
- non-Hodgkin's lymphoma, adult;
- non-Hodgkin's lymphoma, childhood;
- non-Hodgkin's lymphoma during pregnancy;
- non-small cell lung cancer;
- neoplasms of the central nervous system;
- oat-cell cancer;
- oral cancer, childhood;
- oral cavity and lip cancer;
- oropharyngeal cancer;
- osteosarcoma/malignant fibrous histiocytoma of bone;
- ovarian cancer;
- ovarian cancer, childhood;
- ovarian epithelial cancer;
- ovarian germ cell tumour;
- ovarian low malignant potential tumour;
- pediatric malignancy;
- pancreatic cancer;
- pancreatic cancer, childhood;
- pancreatic cancer, islet cell;
- paranasal sinus and nasal cavity cancer;
- parathyroid cancer;
- penile cancer;
- pheochromocytoma;
- pineal and supratentorial primitive neuroectodermal tumours, childhood;
- pituitary tumour;
- plasma cell neoplasm/multiple myeloma;
- pleuropulmonary blastoma;
- pregnancy and breast cancer;
- pregnancy and Hodgkin's lymphoma;
- pregnancy and non-Hodgkin's lymphoma;
- primary central nervous system lymphoma;
- primary liver cancer, adult;
- primary liver cancer, childhood;
- prostate cancer (particularly hormone-refractory);
- chronic or acute leukemia;
- solid tumors of childhood;
- hypereosinophilia;
- rectal cancer;
- renal cell (kidney) cancer;
- renal cell cancer, childhood;
- renal pelvis and ureter, transitional cell cancer;
- retinoblastoma;
- rhabdomyosarcoma, childhood;
- salivary gland cancer;
- salivary gland cancer, childhood;
- sarcoma, Ewing's family of tumours;
- sarcoma, Kaposi's;
- sarcoma (osteosarcoma)/malignant fibrous histiocytoma of bone;
- sarcoma, rhabdomyosarcoma, childhood;
- sarcomas of soft tissues;
- sarcoma, soft tissue, adult;
- sarcoma, soft tissue, childhood;
- Sezary syndrome;
- skin cancer;
- skin cancer, childhood;
- skin cancer (melanoma);
- skin carcinoma, Merkel cell;
- small cell lung cancer;
- dermatofibrosarcoma protuberans;
- small intestine cancer;
- soft tissue sarcoma, adult;
- soft tissue sarcoma, childhood;
- cancer of the head and neck;
- squamous neck cancer with occult primary, metastatic;
- stomach (gastric) cancer;
- stomach (gastric) cancer, childhood;
- supratentorial primitive neuroectodermal tumours, childhood;
- t-cell lymphoma, cutaneous;
- testicular cancer;
- thymoma, childhood;
- thymoma, malignant;
- thyroid cancer;
- thyroid cancer, childhood;
- transitional cell cancer of the renal pelvis and ureter;
- trophoblastic tumour, gestational;
- unknown primary site, cancer of, childhood;
- unusual cancers of childhood;
- ureter and renal pelvis, transitional cell cancer;
- urethral cancer;
- cancer of the ureter;
- cancer of the penis;
- gynecologic tumors;
- uterine cancer;
- uterine sarcoma;
- carcinoma of the fallopian tubes;
- carcinoma of the endometrium;
- vaginal cancer;
- carcinoma of the vagina;
- carcinoma of the vulva;
- visual pathway and hypothalamic glioma, childhood;
- vulvar cancer;
- Waldenstrom's macro globulinemia;
- and Wilms' tumour.
229 more elements
158:
- The method according to claim 155, for use in combination with a further therapeutic agent selected from the group consisting of a corticosteroid (glucocorticoid), retinoid, anthralin, vitamin D analogue, calcineurin inhibitors, phototherapy or photochemotherapy or other form of ultraviolet light irradiation therapy, ciclosporine, a thiopurine, methotrexate, an anti-TNFα agent, phosphodiesterase-4 (PDE4) inhibitors, anti-IL-17 agent, anti-IL12/IL-23 agent, anti-IL-23 agent, JAK (Janus Kinase) inhibitor, plasma exchange, intravenous immune globulin (IVIG), cyclophosphamide, anti-CD20 B cell depleting agent, anthracycline analogue, cladribine, sphingosine 1-phosphate receptor modulator or sphingosine analogue, interferon beta preparation, glatiramer, anti-CD3 therapy, anti-CD52 targeting agent, leflunomide, teriflunomide, gold compound, laquinimod, potassium channel blocker, mycophenolic acid, mycophenolate mofetil, purine analogue, mTOR (mechanistic target of rapamycin) pathway inhibitor, anti-thymocyte globulin (ATG), IL-2 receptor (CD25) inhibitor, anti-IL-6 receptor or anti-IL-6 agent, Bruton's tyrosine kinase (BTK) inhibitor, tyrosine kinase inhibitor, ursodeoxycholic acid, hydroxychloroquine, chloroquine, B cell activating factor (BAFF, also known as BlyS, B lymphocyte stimulator) inhibitor, other B cell targeted therapy including a fusion protein targeting both APRIL (A Proliferation-Inducing Ligand) and BlyS, PI3K inhibitor including pan-inhibitor or one targeting the p110δ and/or p110γ containing isoforms, an interferon α receptor inhibitor, T cell co-stimulation blocker, thalidomide and its derivatives, dapsone, clofazimine, a leukotriene antagonist, theophylline, anti-IgE therapy, an anti-IL-5 agent, a long-acting muscarinic agent, a PDE4 inhibitor, riluzole, a free radical scavenger, a proteasome inhibitor, a complement cascade inhibitor including one directed against C5, immunoadsor, antithymocyte globulin, 5-aminosalicylates and their derivatives, an anti-integrin agent including one targeting α4β1 and/or α4β7 integrins, an anti-CD11-α agent, a non-steroidal anti-inflammatory drug (NSAID) including a salicylate, a propionic acid, an acetic acid, an oxicam, a fenamate, a selective or relatively selective COX-2 inhibitor, colchicine, an IL-4 receptor inhibitor, topical/contact immunotherapy, anti-IL-1 receptor therapy, IL-1β inhibitor, IL-1 neutralising therapy, chlorambucil, a specific antibiotic with immunomodulatory properties and/or ability to modulate NRF2, anti-androgenic therapy, pentoxifylline, ursodeoxycholic acid, obeticholic acid, fibrate, a cystic fibrosis transmembrane conductance regulator (CFTR) modulator, a VEGF (vascular endothelial growth factor) inhibitor, pirfenidone and mizoribine.
159:
- A process for preparing a compound of formula (Ia) as described in claim 115, or a salt, such as a pharmaceutically acceptable salt and/or solvate thereof, which comprises reacting a compound of formula (IIa-S):
- or a salt thereof;
- with a compound of formula (IIIa-S):
- wherein RA, RB, RC, RD Y1, Y2, Y3, Z1, Z2, X and m are defined according to claim 1, and LG2 is a leaving group such as halo, OMs or OTs.
1 more element
160:
- A compound selected from the group consisting of:
- a compound of formula (IIa-S):
- or a salt and/or solvate thereof;
- wherein RA Y1, Y2, Y3, Z1, Z2 and X are defined according to claim 1;
- a compound of formula (IVa):
- or a salt and/or solvate thereof;
- wherein Y1, Y2, Y3, Z1 and Z2 are defined in claim 1, and LG is a leaving group such as halo, OMs or OTs;
- a compound of formula (Va):
- or a salt and/or solvate thereof;
- wherein RA Y1, Y2, Y3, Z1, and Z2 are defined in claim 1;
- a compound of formula (VIa):
- or a salt and/or solvate thereof;
- wherein RB, RC, RD, m, Y1, Y2, Y3, Z1 and Z2 are defined in claim 1 and LG1 is a leaving group such as halo, OMs or OTs;
- and
- a compound of formula (VIIa):
- or a salt and/or solvate thereof;
- wherein RA, RB, RC, RD, m, Y1, Y2, Y3, Z1 and Z2 are defined in claim 1.
14 more elements
161:
- The compound or a pharmaceutically acceptable salt and/or solvate thereof according to claim 115 which is a pharmaceutically acceptable salt of the compound of formula (Ia).
162:
- The compound or a pharmaceutically acceptable salt and/or solvate thereof according to claim 115 which is the compound of formula (Ia).
The compound, pharmaceutically acceptable salt and/or solvate thereof according to claim 115, wherein RC is H and RD is H.
Dependencies are inferred from the claim text.