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US 2007/0191332 A1Published application
Compounds for the treatment of inflammatory disorders
AssigneeSchering Corporation
InventorsZhaoning Zhu, Robert Mazzola, Wensheng Yu, Joseph Kozlowski
Life of this patent
Estimating the term…
Abstract
This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, wherein n, M, V, T, W, X, U, R1 and R2 are as disclosed in the present specification, and which compounds are useful for the treatment of diseases or conditions mediated by MMPs, TNF-α or combinations thereof.
Claims42
A compound represented by Formula (I):
- or a pharmaceutically acceptable salt, solvate or ester thereof, wherein:
- M, together with the two carbon atoms to which it is shown attached in formula (I) is 4-7 membered hetereocyclyl or heterocyclenyl comprising 0-3 carbonyl groups, 0-3 double bonds, and 1-3 heteroatoms selected from O, N, and S, wherein said 4-7 membered hetereocyclyl or heterocyclenyl can, in addition to the four substituents V, R2, T, and —(W)n—X—U—R1 as set forth in formula (I), be further optionally substituted with R21;
- T is selected from the group consisting of H, alkyl, R21-substituted alkyl, cycloalkyl, aryl, heteroaryl, hetereocyclyl, arylalkyl, heteroarylalkyl, —OR3, —C(O)R4, —C(O)OR3, —C(O)NR24R25, —C(O)NR24OR3, —C(O)SR3, —NR24R25, —NR25C(O)R4, —NR25C(O)OR3, —NR25C(O)NR24R25, —NR25C(O)NR24OR3, —SR3, —N(R24)S(O)2R25, —S(O)xNR24R25, —S(O)xNR25OR3, —CN, —P(O)(R24)(OR24), —P(O)(OR24)(OR24), —C(R4)(═N(OR3)), —C(O)—N(R31)CH(R32)—C(O)NR24R25 and —C(O)N(R31)CH(R32)—C(O)—NR25OR3,
- wherein each of the cycloalkyl, aryl, heteroaryl, hetereocyclyl, arylalkyl and heteroarylalkyl groups of T is unsubstituted or optionally independently substituted with one to six R20 moieties which can be the same or different, each R20 moiety being independently selected from the group of R20 moieties below;
- V is selected from the group consisting of alkyl, R21-substituted alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —OR3, —C(O)R4, —(CR23R24)n1C(O)OR3, —C(O)NR24R25, —(CR23R24)n1C(O)NR25OR3, —C(O)SR3, —C(R23)(R24)SH, —NR24R25, —NR25C(O)R4, —NR25C(O)OR3, —NR25C(O)NR24R25, —NR25C(O)NR24OR3, —SR3, —S(O)xNR24R25, —S(O)xNR25OR3, —CN, —P(O)(R25)(OR24), —P(O)(OR24)(OR24), —C(R4)(═N(OR3)), —C(O)—N(R31)CH(R32)—C(O)NR24R25 and —C(O)N(R3)CH(R32)—C(O)—NR25OR3,
- wherein each of the cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of V is unsubstituted or optionally independently substituted with one to three R20 moieties which can be the same or different, each R20 moiety being independently selected from the group of R20moieties below;
- W is selected from the group consisting of
- a covalent bond, —(C(R3)(R4))n2—, —O—, —S—, —N(R24)—, and —N(Z)-;
- X is selected from the group consisting of alkyl, cylcloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl and —C≡C—, wherein each of the alkyl, cylcloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, and heteroaryl groups of X is unsubstituted or optionally independently substituted with one to four selected R20 moieties which can be the same or different, each R20 moiety being independently selected from the group of R20 moieties below,
- U is selected from the group consisting of a covalent bond,
- —(C(R3)(R4))p—, —Y—(C(R3)(R4))q—, —(C(R3)(R4))t—Y—, —N(R3)(Z)-Q-, -Q-N(R3)(Z)- and —Y—;
- Q is selected from the group consisting of —S(O)—, —S(O)2—, —C(O)—, and —C(O)NR4—;
- Y is selected from the group consisting of —O—, —S(O)x—, —N(Z)-, —N(R4)(Z);
- —C(O)—, —OC(O)—, —C(O)N(R24)—, —N(R24)C(O)N(R25)—, —N(R24)S(O)—, —N(R24)S(O)2—, —S(O)N(R24)—, and —S(O)2N(R24)—;
- Z is selected from the group consisting of —R3, —C(O)R3, —S(O)xR3 and r25 —C(O)NR3R4;
- n is 0 to 2;
- n1 is 0 to 2;
- n2 is 1 to 2;
- p is 1 to 4;
- q is 1 to 4;
- t is 1 to 4;
- v is 1 to 3;
- x is 0 to 2;
- y is 0 to 3;
- R1 is selected from the group consisting of alkyl, R21-substituted alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —C≡CR3 and —CR3═CR4R5,
- wherein each of the alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of R1 is unsubstituted or optionally independently substituted with one to six R20 moieties which can be the same or different, each R20 moiety being independently selected from the group of R20 moieties below,
- each of R2, R4 and R5 is the same or different and each is independently selected from the group consisting of H, halo, alkyl, R22-substituted alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —OR6, —C(O)R7, —C(O)OR6, —NR24R25, —NR24C(O)R25, —N(═C—O—NR24R25), and —NR24S(O)2R25,
- wherein each of the cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of R2, R4 and R5 is unsubstituted or optionally independently substituted with one to six alkyl, R22-substituted alkyl or R22 moieties which can be the same or different, each R22 moiety being independently selected from the group of R22 moieties below;
- each R3 is the same or different and is independently selected from the group consisting of H, alkyl, R22-substituted alkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —OR6, —C(O)R7, —C(O)OR6, —NR24R25, —NR24C(O)R25, —N(═C—O—NR24R25) and —NR24S(O)2R25, wherein
- each of the cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of R3 is unsubstituted or optionally independently substituted with one to four alkyl, R22-substituted alkyl or R22 moieties which can be the same or different, each R22 moiety being independently selected from the group of R22 moieties below;
- each R6 is independently selected from the group consisting of H, alkyl and —OCF3;
- each R7 is independently selected from the group consisting of H, alkyl, heteroaryl and —CF3;
- each R20 is independently selected from the group consisting of:
- alkyl, R21-substituted alkyl, —OR3, halo, (═O), —CN, —NO2, —NR24R25, —C(O)R3, —C(O)OR3, —C(O)NR24R25, —S(O)xNR24R25, —S(O)nR5, —CF3, —OCF3, —CF2CF3, —CH(═NOH), —C(═NOH)R3, aryl, heteroaryl, cycloalkyl, hetereocyclyl, —N(R25)S(O)xR5, —N(R25)C(O)R5, and —N(R25)C(O)NR24R25,
- wherein each of the aryl, heteroaryl, cycloalkyl and hetereocyclyl groups of R20 is unsubstituted or optionally independently substituted with one to four R22 moieties which can be the same or different, each R22 moiety being independently selected from the group of R22 moieties below,
- or two R20 groups taken together with the carbon to which both R20 groups are attached is
- R21 is one to three substituents independently selected from the group consisting of:
- —OR3, halo, —CN, —NO2, —NR24R25, —C(O)R3, —C(O)OR3, —C(O)NR24R25, —S(O)xNR24R25, —SOxR51, —CF3, —OCF3, —CF2CF3, —C(═NOH)R3, R23-substituted alkyl, aryl, heteroaryl, cycloalkyl, hetereocyclyl, —N(R25)S(O)xR5, —N(R25)C(O)R5, and —N(R25)C(O)NR24R25;
- wherein each of the aryl, heteroaryl, cycloalkyl, and hetereocyclyl groups of R21 is unsubstituted or optionally independently substituted with one to four R23 moieties which can be the same or different, each R23 moiety being independently selected from the group of R23 moieties below,
- or two R21 groups taken together with the carbon to which both R21 groups are attached is
- each R22 is independently selected from the group consisting of:
- halo, alkynyl, aryl, heteroaryl, —OR24, —(C1-C6 alkyl)-OR24, —CN, —NO2, —NR24R25, —C(O)R23, —C(O)OR23, —C(O)NR24R25, —S(O)xNR24R25, —S(O)xR23, —CF3, —OCF3, —CF2CF3, —C(═NOH)R23, —N(R24)S(O)xR25, —N(R24)C(O)R25, and —N(R24)C(O)NR24R25,
- or two R22 groups taken together with the carbon to which both R22 groups are attached is
- each R23 is independently selected from the group consisting of H, hydroxyl, halo and alkyl;
- each R24 is independently selected from the group consisting of H and alkyl;
- each R25 is independently selected from the group consisting of H, hydroxyl, alkyl, hydroxyalkyl, aryl, cycloalkyl, heteroaryl, —NR24R24—(C1 to C6 alkyl)NR24N24, —CF3 and —S(O)xR23;
- R26 is selected from the group consisting of H, alkyl, cycloalkyl, aryl, and heteroaryl;
- R27 is selected from the group consisting of H, alkyl, cycloalkyl, aryl, and heteroaryl;
- and
- each of R31 and R32 is the same or different and wherein each is independently selected from the group consisting of H, alkyl, cycloalkyl, aryl, heteroaryl, —NR24R25, —(CH2)3NH(C═NH)NH2, —CH2C(O)NH2, —CH2C(O)OH, —CH2SH, —CH2S—SCH2CH(NH2)C(O)OH, —CH2CH2C(O)OH, —CH2CH2C(O)NH2, —(CH2)4NH2, —CH2CH2CH(OH)CH2NH2, —CH2CH(CH3)2, —CH(CH3)CH2(CH3), —CH2CH2SCH3, —CH2OH, —CH(OH)(CH3),
- or R31 and R32, together with the N to which R31 is attached and the C to which R31 is attached, form a 5-membered ring which is unsubstituted or optionally independently substituted with a hydroxyl group.
48 more elements
A compound represented by the structural formula (II):
- or a pharmaceutically acceptable salt, solvate or ester of said compound, wherein:
- L is aryl or heteroaryl;
- R1 is selected from the group consisting of alkyl, R21-substituted alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —C≡CR3 and —CR3═CR4R5, wherein each of the alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of R1 is unsubstituted or optionally independently substituted with one to six R20 moieties which can be the same or different, each R20 moiety being independently selected from the group of R20 moieties below,
- T is selected from the group consisting of H, alkyl, R21-substituted alkyl, cycloalkyl, aryl, heteroaryl, hetereocyclyl, arylalkyl, heteroarylalkyl, —OR3, —C(O)R4, —C(O)OR3, —C(O)NR24R25, —C(O)NR24OR3, —C(O)SR3, —NR24R25, —NR25C(O)R4, —NR25C(O)OR3, —NR25C(O)NR24R25, —NR25C(O)NR24OR3, —SR3, —N(R24)S(O)2R25, —S(O)xNR24R25, —S(O)xNR25OR3, —CN, —P(O)(R24)(OR24), —P(O)(OR24)(OR24), —C(R4)(═N(OR3)), —C(O)—N(R31)CH(R32)—C(O)NR24R25 and —C(O)N(R31)CH(R32)—C(O)—NR25OR3,
- wherein each of the cycloalkyl, aryl, heteroaryl, hetereocyclyl, arylalkyl and heteroarylalkyl groups of T is unsubstituted or optionally independently substituted with one to six R20 moieties which can be the same or different, each R20 moiety being independently selected from the group of R20 moieties below;
- G1 is O, H, alkyl, R2-substituted alkyl, —OR3, halo, —C(O)R3, —C(O)OR3, —C(O)NR24R25, —S(O)xNR24R25, —S(OxR5, —CF3, —OCF3, —CF2CF3, —C(═NOH)R3, aryl, heteroaryl, cycloalkyl, hetereocyclyl, and heteroarylalkyl,
- wherein each of the aryl, heteroaryl, cycloalkyl, hetereocyclyl and heteroarylalkyl groups of P is unsubstituted or optionally independently substituted with one to four R23 moieties which can be the same or different, each R23 moiety being independently selected from the group of R23 moieties below,
- V is selected from the group consisting of alkyl, R21-substituted alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —OR3, —C(O)R4, —(CR23R24)n1C(O)OR3, —C(O)NR24R25, —(CR23R24)n1C(O)NR25OR3, —C(O)SR3, —C(R23)(R24)SH, —NR24R25, —NR25C(O)R4, —NR25C(O)OR3, —NR25C(O)NR24R25, —NR25C(O)NR24OR3, —SR3, —S(O)xNR24R25, —S(O)xNR25OR3, —CN, —P(O)(R25)(OR24), —P(O)(OR24)(OR24), —C(R4)(═N(OR3)), —C(O)—N(R31)CH(R32)—C(O)NR24R25and —C(O)N(R31)CH(R32)—C(O)—NR25OR3,
- wherein each of the cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of V is unsubstituted or optionally independently substituted with one to three R20 moieties which can be the same or different, each R20 moiety being independently selected from the group of R20moieties below;
- n1 is 0 to 2;
- x is 0 to 2;
- each of R2, R4 and R5 is the same or different and each is independently selected from the group consisting of H, halo, alkyl, R22-substituted alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —OR6, —C(O)R7, —C(O)OR6, —NR24R25, —NR24C(O)R25, —N(═C—O—NR24R25), —NR24S(O)2R25, wherein each of the cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of R2, R4 and R5 is unsubstituted or optionally independently substituted with one to six alkyl, R22-substituted alkyl or R22 moieties which can be the same or different, each R22 moiety being independently selected from the group of R22 moieties below, or R4 and R5 taken together with the carbon to which both R4 and R5 are attached is
- each R3 is the same or different and is independently selected from the group consisting of H, alkyl, R22-substituted alkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —OR6, —C(O)R7, —C(O)OR6, —NR24R25, —NR24C(O)R25, —N(═C—O—NR24R25) and —NR24S(O)2R25, wherein each of the cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of R3 is unsubstituted or optionally independently substituted with one to four alkyl, R22-substituted alkyl or R22 moieties which can be the same or different, each R22 moiety being independently selected from the group of R22 moieties below;
- each R6 is independently selected from the group consisting of H, alkyl and —OCF3;
- each R7 is independently selected from the group consisting of H, alkyl, heteroaryl and —CF3;
- each R20 is independently selected from the group consisting of:
- alkyl, R21-substituted alkyl, —OR3, halo, —CN, —NO2, —NR24R25, —C(O)R3, —C(O)OR3, —C(O)NR24R25, —S(O)xNR24R25, —S(O)xR5, —CF3, —OCF3, —CF2CF3, —C(═NOH)R3, aryl, heteroaryl, cycloalkyl, hetereocyclyl, —N(R25)S(O)xR5, —N(R25)C(O)R5, and —N(R25)C(O)NR24R25,
- wherein each of the aryl, heteroaryl, cycloalkyl and hetereocyclyl groups of R20 is unsubstituted or optionally independently substituted with one to four R22 moieties which can be the same or different, each R22 moiety being independently selected from the group of R23 moieties below,
- or two R20 groups taken together with the carbon to which both R20 groups are attached is
- R21 is one to three substituents independently selected from the group consisting of:
- —OR3, halo, —CN, —NO2, —NR24R25, —C(O)R3, —C(O)OR3, —C(O)NR24R25, —S(O)xNR24R25, —SOxR5, —CF3, —OCF3, —CF2CF3, —C(═NOH)R3, R23-substituted alkyl, aryl, heteroaryl, cycloalkyl, hetereocyclyl, —N(R25)S(O)xR5, —N(R25)C(O)R5, and —N(R25)C(O)NR24R25;
- wherein each of the aryl, heteroaryl, cycloalkyl, and hetereocyclyl groups of R21 is unsubstituted or optionally independently substituted with one to four R23 moieties which can be the same or different, each R23 moiety being independently selected from the group of R23 moieties below,
- or two R21 groups taken together with the carbon to which both R21 groups are attached is
- each R22 is independently selected from the group consisting of:
- halo, alkynyl, aryl, heteroaryl, —OR24, —(C1-C6 alkyl)-OR24, —CN, —NO2, —NR24R25, —C(O)R23, (O)OR23, —C(O)NR24R25, —S(O)xNR24R25, —S(O)xR23, —CF3, —OCF3, —CF2CF3, —C(═NOH)R23, —N(R24)S(O)xR25, —N(R24)C(O)R25, and —N(R24)C(O)NR24R25,
- or two R22 groups taken together with the carbon to which both R22 groups are attached is
- each R23 is independently selected from the group consisting of H, hydroxyl, halo and alkyl;
- each R24 is independently selected from the group consisting of H and alkyl;
- each R25 is independently selected from the group consisting of H, hydroxyl, alkyl, hydroxyalkyl, aryl, cycloalkyl, heteroaryl, —NR24R24, —(C1 to C6 alkyl)NR24N24, —CF3 and —S(O)xR23;
- each of R31 and R32 is the same or different and wherein each is independently selected from the group consisting of H, alkyl, cycloalkyl, aryl, heteroaryl, —NR24R25, —(CH2)3NH(C═NH)NH2, —CH2C(O)NH2, —CH2C(O)OH, —CH2SH, —CH2S—SCH2CH(NH2)C(O)OH, —CH2CH2C(O)OH, —CH2CH2C(O)NH2, —(CH2)4NH2, —CH2CH2CH(OH)CH2NH2, —CH2CH(CH3)2, —CH(CH3)CH2(CH3), —CH2CH2SCH3, —CH2OH, —CH(OH)(CH3),
- or R31 and R32, together with the N to which R31 is attached and the C to which R31 is attached, form a 5-membered ring which is unsubstituted or optionally independently substituted with a hydroxyl group.
28 more elements
A compound represented by the structural formula (III):
- or a pharmaceutically acceptable salt, solvate or ester of said compound, wherein:
- L is aryl or heteroaryl;
- R1 is selected from the group consisting of alkyl, R21-substituted alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —C≡CR3 and —CR3═CR4R5, wherein each of the alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of R1 is unsubstituted or optionally independently substituted with one to six R20 moieties which can be the same or different, each R20 moiety being independently selected from the group of R20 moieties below,
- T is selected from the group consisting of H, alkyl, R21-substituted alkyl, cycloalkyl, aryl, heteroaryl, hetereocyclyl, arylalkyl, heteroarylalkyl, —OR3, —C(O)R4, —C(O)OR3, —C(O)NR24R25, —C(O)NR24OR3, —C(O)SR3, —NR24R25, —NR25C(O)R4, —NR25C(O)OR3, —NR25C(O)NR24R25, —NR25C(O)NR24OR3, —SR3, —N(R24)S(O)2R25, —S(O)xNR24R25, —S(O)xNR25OR3, —CN, —P(O)(R24)(OR24), —P(O)(OR24)(OR24), —C(R4)(═N(OR3)), —C(O)—N(R31)CH(R32)—C(O)NR24R25 and —C(O)N(R31)CH(R32)—C(O)—NR25OR3,
- wherein each of the cycloalkyl, aryl, heteroaryl, hetereocyclyl, arylalkyl and heteroarylalkyl groups of T is unsubstituted or optionally independently substituted with one to six R20 moieties which can be the same or different, each R20 moiety being independently selected from the group of R20 moieties below;
- G2 is H, alkyl, R21 -substituted alkyl, —OR3, halo, —C(O)R3, —C(O)OR3, —C(O)NR24R25, —S(O)xNR24R25, —S(O)xR5, —CF3, —OCF3, —CF2CF3, —C(═NOH)R3, aryl, heteroaryl, cycloalkyl, hetereocyclyl, and heteroarylalkyl,
- wherein each of the aryl, heteroaryl, cycloalkyl, hetereocyclyl and heteroarylalkyl groups of Q is unsubstituted or optionally independently substituted with one to four R23 moieties which can be the same or different, each R23 moiety being independently selected from the group of R23 moieties below,
- V is selected from the group consisting of alkyl, R21-substituted alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —OR3, —C(O)R4, —(CR23R24)n1C(O)OR3, —C(O)NR24R25, —(CR23R24)n1C(O)NR25OR3, —C(O)SR3, —C(R23)(R24)SH, —NR24R25, —NR25C(O)R4, —NR25C(O)OR3, —NR25C(O)NR24R25, —NR25C(O)NR24OR3, —SR3, —S(O)xNR24R25, —S(O)xNR25OR3, —CN, —P(O)(R25)(OR24), —P(O)(OR24)(OR24), —C(R4)(═N(OR3)), —C(O)—N(R31)CH(R32)—C(O)NR24R25 and —C(O)N(R3)CH(R32)—C(O)—NR25OR3,
- wherein each of the cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of V is unsubstituted or optionally independently substituted with one to three R20 moieties which can be the same or different, each R20 moiety being independently selected from the group of R20moieties below;
- n1 is 0 to 2;
- x is 0 to 2;
- each of R2, R4 and R5 is the same or different and each is independently selected from the group consisting of H, halo, alkyl, R22-substituted alkyl, cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —OR6, —C(O)R7, —C(O)OR6, —NR24R25, —NR24C(O)R25, —N(═C—O—NR24R25), —NR24S(O)2R25, wherein each of the cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of R2, R4 and R5 is unsubstituted or optionally independently substituted with one to six alkyl, R22-substituted alkyl or R22 moieties which can be the same or different, each R22 moiety being independently selected from the group of R22 moieties below,
- or R4 and R5taken together with the carbon to which both R4 and R5 are attached is
- each R3 is the same or different and is independently selected from the group consisting of H, alkyl, R22-substituted alkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl, heteroaryl, —OR6, —C(O)R7, —C(O)OR6, —NR24R25, —NR24C(O)R25, —N(═C—O—NR24R25) and —NR24S(O)2R25, wherein each of the cycloalkyl, hetereocyclyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl groups of R3 is unsubstituted or optionally independently substituted with one to four alkyl, R22-substituted alkyl or R22 moieties which can be the same or different, each R22 moiety being independently selected from the group of R22 moieties below;
- each R6 is independently selected from the group consisting of H, alkyl and —OCF3;
- each R7 is independently selected from the group consisting of H, alkyl, heteroaryl and —CF3;
- each R20 is independently selected from the group consisting of:
- alkyl, R2-substituted alkyl, —OR3, halo, —CN, —NO2, —NR24R25, —C(O)R3, —C(O)OR3, —C(O)NR24R25, —S(O)xNR24R25, —S(O)xR5, —CF3, —OCF3, —CF2CF3, —C(═NOH)R3, aryl, heteroaryl, cycloalkyl, hetereocyclyl, —N(R25)S(O)xR5, —N(R25)C(O)R5, and —N(R25)C(O)NR24R25,
- wherein each of the aryl, heteroaryl, cycloalkyl and hetereocyclyl groups of R20 is unsubstituted or optionally independently substituted with one to four R22 moieties which can be the same or different, each R22 moiety being independently selected from the group of R23 moieties below,
- or two R20 groups taken together with the carbon to which both R20 groups are attached is
- R21 is one to three substituents independently selected from the group consisting of:
- —OR3, halo, —CN, —NO2, —NR24R25, —C(O)R3, —C(O)OR3, —C(O)NR24R25, —S(O)xNR24R25, —SOxR5, —CF3, —OCF3, —CF2CF3, —C(═NOH)R3, R23-substituted alkyl, aryl, heteroaryl, cycloalkyl, hetereocyclyl, —N(R25)S(O)xR5, —N(R25)C(O)R5, and —N(R25)C(O)NR24R25;
- wherein each of the aryl, heteroaryl, cycloalkyl, and hetereocyclyl groups of R21 is unsubstituted or optionally independently substituted with one to four R23 moieties which can be the same or different, each R23 moiety being independently selected from the group of R23 moieties below,
- or two R21 groups taken together with the carbon to which both R21 groups are attached is
- each R22 is independently selected from the group consisting of:
- halo, alkynyl, aryl, heteroaryl, —OR24, —(C1-C6 alkyl)-OR24, —CN, —NO2, —NR24R25, —C(O)R23, —C(O)OR23, —C(O)NR24R25, —S(O)xNR24R25, —S(O)xR23, —CF3, —OCF3, —CF2CF3, —C(═NOH)R23, —N(R24)S(O)xR25, —N(R24)C(O)R25, and —N(R24)C(O)NR24R25,
- or two R22 groups taken together with the carbon to which both R22 groups are attached is
- each R23 is independently selected from the group consisting of H, hydroxyl, halo and alkyl;
- each R24 is independently selected from the group consisting of H and alkyl;
- each R25 is independently selected from the group consisting of H, hydroxyl, alkyl, hydroxyalkyl, aryl, cycloalkyl, heteroaryl, —NR24R24, —(C1 to C6 alkyl)NR24N24, —CF3 and —S(O)xR23;
- each of R31 and R32 is the same or different and wherein each is independently selected from the group consisting of H, alkyl, cycloalkyl, aryl, heteroaryl, —NR24R25, —(CH2)3NH(C═NH)NH2, —CH2C(O)NH2, —CH2C(O)OH, —CH2SH, —CH2S—SCH2CH(NH2)C(O)OH, —CH2CH2C(O)OH, —CH2CH2C(O)NH2, —(CH2)4NH2, —CH2CH2CH(OH)CH2NH2, —CH2CH(CH3)2, —CH(CH3)CH2(CH3), —CH2CH2SCH3, —CH2OH, —CH(OH)(CH3),
- or R31 and R32, together with the N to which R31 is attached and the C to which R31 is attached, form a 5-membered ring which is unsubstituted or optionally independently substituted with a hydroxyl group.
29 more elements
Dependencies are inferred from the claim text.