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US 8,895,313 B2Granted
Ligands for aggregated tau molecules
AssigneeWisTa Laboratories Ltd.
InventorsSteven John Kemp, Lynda Jane Storey, John Mervyn David Storey, Janet Rickard, Charles Robert Harrington, Claude Michel Wischik, Scott Clunas, Tobias Kerst Heinrich
Life of this patent
Estimating the term…
Abstract
Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.
Claims36
A compound having the formula:
- wherein
- —R— is independently selected from:
- wherein (T) indicates the point of attachment to -T;
- and (Q) indicates the point of attachment to -Q-;
- -Q- is independently selected from:
- —N═N—;
- —CH═CH—;
- —CR1═CH—;
- —CH═CR1—;
- —CR1═CR1—;
- each —R1 is independently unsubstituted saturated aliphatic C1-4-alkyl;
- —P is independently selected from:
- where the asterisk indicates the point of attachment;
- -T is independently selected from:
- where the asterisk indicates the point of attachment;
- and X is independently CH;
- —W1 is independently —WA;
- —W2 is independently —H or —WA;
- —W3 is independently —H or —WA;
- —W4 is independently —H or —WA;
- —W5 is independently —H or —WA;
- —W6 is independently —H or —WA;
- with the proviso that at least one of —W4, —W5 and —W6 is —WA;
- where —WA is independently selected from:
- —F, —Cl, —Br, —I,
- —OH, —WA1, —O—WA1,
- —NH2, —NHWA1, and —N(WA1)2;
- and —WA1 is independently selected from:
- unsubstituted saturated aliphatic C1-4-alkyl,
- —CF3,
- —CH2CH2OH, and
- —CH2CH2N(Me)2;
- -G1 is independently —H or -GA;
- -G2 is independently —H or -GA;
- where -GA is independently selected from:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, —OR2;
- —[O—CH2CH2]n—RB2, where n is 2 to 6;
- -G3 is independently —H or -GB;
- -G4 is independently —H or -GB
- where -GB is independently selected from:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, —OR2;
- —[O—CH2CH2]n—RB2, where n is 2 to 6;
- wherein:
- —P1 is independently —H or —PA;
- —P2 is independently —H or —PB;
- —P3 is independently —H or —PC;
- —P4 is independently —H or —PB;
- —P5 is independently —H or —PA;
- and wherein:
- each —PA, each —PB, and each —PC is independently:
- —F, —Cl, —Br, —I,
- —R2,
- —CF3, —OCF3,
- —OH, -L1-OH,
- —OR2, -L1-OR2, —O-L1-OR2,
- —SH, —SR2,
- —CN,
- —NO2,
- —NH2, —NHR2, —NR22, —NR3R4,
- —NHOH,
- -L1-NH2, -L1-NHR2, -L1-NR22, -L1-NR3R4,
- —O-L1-NH2, —O-L1-NHR2, —O-L1-NR22, —O-L1-NR3R4,
- —C(═O)OH, —C(═O)OR2,
- —OC(═O)R2,
- —C(═O)NH2, —C(═O)NHR2, —C(═O)NR22, —C(═O)NR3R4,
- —NHC(═O)R2, —NR2C(═O)R2,
- —C(═O)NHOR2, —C(═O)NR2OR2,
- —NHC(═O)OR2, —NR2C(═O)OR2,
- —OC(═O)NH2, —OC(═O)NHR2, —OC(═O)NR22, —OC(═O)NR3R4,
- —C(═O)R2,
- —NHC(═O)NH2, —NHC(═O)NHR2,
- —NHC(═O)NR22, —NHC(═O)NR3R4,
- —NR2C(═O)NH2, —NR2C(═O)NHR2,
- —NR2C(═O)NR22, —NR2C(═O)NR3R4,
- —NHS(═O)2R2, —NR2S(═O)2R2,
- —S(═O)2NH2, —S(═O)2NHR2, —S(═O)2NR22, —S(═O)2NR3R4,
- —S(═O)R2, —S(═O)2R2, —OS(═O)2R2, or —S(═O)2OR2
- wherein:
- each -L1- is independently saturated aliphatic C1-5alkylene;
- in each group —NR3R4, —R3 and —R4, taken together with the nitrogen atom to which they are attached, form a 4-, 5-, 6-, or 7-membered non-aromatic ring having exactly 1 ring heteroatom or exactly 2 ring heteroatoms, wherein one of said exactly 2 ring heteroatoms is N, and the other of said exactly 2 ring heteroatoms is independently N, O, or S;
- each —R2 is independently:
- —RA1, —RA2, —RA3, —RA4, —RA5, —RA6, —RA7, —RA8,
- LA-RA4, -LA-RA5, -LA-RA6, -LA-RA7, or -LA-RA8;
- wherein:
- each —RA1 is independently saturated aliphatic C1-6alkyl;
- each —RA2 is independently aliphatic C2-6alkenyl;
- each —RA3 is independently aliphatic C2-6alkynyl;
- each —RA4 is independently saturated C3-6cycloalkyl;
- each —RA5 is independently C3-6cycloalkenyl;
- each —RA6 is independently non-aromatic C3-7heterocyclyl;
- each —RA7 is independently C6-10-carboaryl;
- each —RA8 is independently C5-10heteroaryl;
- each -LA- is independently saturated aliphatic C1-3alkylene;
- and wherein:
- each —RA4, —RA5, —RA6, —RA7, and —RA8 is optionally substituted, for example, with one or more substituents —RB1 and/or one or more substituents —RB2, and
- each —RA1, —RA2, —RA3, and -LA- is optionally substituted, for example, with one or more substituents —RB2,
- wherein:
- each —RB1 is independently saturated aliphatic C1-4-alkyl, phenyl, or benzyl;
- each —RB2 is independently:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, -LC-OH, —O-LC-OH,
- —ORC1, -LC-ORC1, —O-LC-ORC1,
- —SH, —SRC1,
- —CN,
- —NO2,
- —NH2, —NHRC1, —NRC12, —NRC2RC3,
- -LC-NH2, -LC-NHRC1, -LC-NRC12, or -LC-NRC2RC3,
- —O-LC-NH2, —O-LC-NHRC1, —O-LC-NRC12, —O-LC-NRC2RC3,
- —C(═O)OH, —C(═O)ORC1,
- —OC(═O)RC1,
- —C(═O)RC1,
- —C(═O)NH2, —C(═O)NHRC1, —C(═O)NRC12, —C(═O)NRC2RC3,
- —NHC(═O)RC1, —NRC1C(═O)RC1,
- —NHS(═O)2RC1, —NRC1S(═O)2RC1,
- —S(═O)2NH2, —S(═O)2NHRC1, —S(═O)2NRC12, —S(═O)2NRC2RC3, or
- —S(═O)2RC1;
- wherein:
- each —RC1 is independently unsubstituted saturated aliphatic C1-4-alkyl, phenyl, or benzyl;
- each -LC- is independently unsubstituted saturated aliphatic C1-5alkylene;
- and
- in each group —NRC2RC3, —RC2 and —RC3, taken together with the nitrogen atom to which they are attached, form a 4-, 5-, 6-, or 7-membered non-aromatic ring having exactly 1 ring heteroatom or exactly 2 ring heteroatoms, wherein one of said exactly 2 ring heteroatoms is N, and the other of said exactly 2 ring heteroatoms is independently N, O, or S,
- and pharmaceutically and physiologically acceptable salts thereof,
- with the proviso that the compound is not a compound:
- (a) P-002 through P-015;
- and
- (b) where -T is:
- —R— is:
- and —P is:
- and —W4 is —H, -Q- is —CH═CH—, -G1, -G2, -G3, and -G4 are all —H, and
- (i) —P1, —P2, —P4 and —P5 are all —H, and —P3 is —RA1;
- or
- (ii) one of —P1, —P2, —P3, P4 and —P5 is —RA7, and the others of —P1, —P2, —P3, P4 and —P5 are —H.
134 more elements
A compound of formula:
- wherein
- —R— is independently selected from:
- wherein (T) indicates the point of attachment to -T;
- and (Q) indicates the point of attachment to -Q-;
- -Q- is independently selected from:
- —NHC(O)—;
- —NR1C(O)—;
- each —R1 is independently unsubstituted saturated aliphatic C1-4-alkyl;
- —P is independently selected from:
- where the asterisk indicates the point of attachment;
- -T is independently selected from:
- where the asterisk indicates the point of attachment;
- and X is independently CH;
- —W1 is independently —WA;
- —W2 is independently —H or —WA;
- —W3 is independently —H or —WA;
- where —WA is independently selected from:
- —F, —Cl, —Br, —I,
- —OH, —WA1, —O—WA1,
- —NH2, —NHWA1, and —N(WA1)2;
- and —WA1 is independently selected from:
- unsubstituted saturated aliphatic C1-4-alkyl,
- —CF3,
- —CH2CH2OH, and
- —CH2CH2N(Me)2;
- -G1 is independently —H or -GA;
- -G2 is independently —H or -GA;
- where -GA is independently selected from:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, —OR2;
- —[O—CH2CH2]n—RB2, where n is 2 to 6;
- -G3 is independently —H or -GB;
- -G4 is independently —H or -GB
- where -GB is independently selected from:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, —OR2;
- —[O—CH2CH2]n—RB2, where n is 2 to 6;
- wherein:
- —P1 is independently —H or —PA;
- —P2 is independently —H or —PB;
- —P3 is independently —H or —PC;
- —P4 is independently —H or —PB;
- —P5 is independently —H or —PA;
- and wherein:
- each —PA, each —PB, and each —PC is independently:
- —F, —Cl, —Br, —I,
- —R2,
- —CF3, —OCF3,
- —OH, -L1-OH,
- —OR2, -L1-OR2, —O-L1-OR2,
- —SH, —SR2,
- —CN,
- —NO2,
- —NH2, —NHR2, —NR22, —NR3R4,
- —NHOH,
- -L1-NH2, -L1-NHR2, -L1-NR22, -L1-NR3R4,
- —O-L1-NH2, —O-L1-NHR2, —O-L1-NR22, —O-L1-NR3R4,
- —C(═O)OH, —C(═O)OR2,
- —OC(═O)R2,
- —C(═O)NH2, —C(═O)NHR2, —C(═O)NR22, —C(═O)NR3R4,
- —NHC(═O)R2, —NR2C(═O)R2,
- —C(═O)NHOR2, —C(═O)NR2OR2,
- —NHC(═O)OR2, —NR2C(═O)OR2,
- —OC(═O)NH2, —OC(═O)NHR2, —OC(═O)NR22, —OC(═O)NR3R4,
- —C(═O)R2,
- —NHC(═O)NH2, —NHC(═O)NHR2,
- —NHC(═O)NR22, —NHC(═O)NR3R4,
- —NR2C(═O)NH2, —NR2C(═O)NHR2,
- —NR2C(═O)NR22, —NR2C(═O)NR3R4,
- —NHS(═O)2R2, —NR2S(═O)2R2,
- —S(═O)2NH2, —S(═O)2NHR2, —S(═O)2NR22, —S(═O)2NR3R4,
- —S(═O)R2, —S(═O)2R2, —OS(═O)2R2, or —S(═O)2OR2
- wherein:
- each -L1- is independently saturated aliphatic C1-5alkylene;
- in each group —NR3R4, —R3 and —R4, taken together with the nitrogen atom to which they are attached, form a 4-, 5-, 6-, or 7-membered non-aromatic ring having exactly 1 ring heteroatom or exactly 2 ring heteroatoms, wherein one of said exactly 2 ring heteroatoms is N, and the other of said exactly 2 ring heteroatoms is independently N, O, or S;
- each —R2 is independently:
- —RA1, —RA2, —RA3, —RA4, —RA5, —RA6, —RA7, —RA8,
- -LA-RA4, -LA-RA5-LA-RA6, LA-RA7, or -LA-RA8;
- wherein:
- each —RA1 is independently saturated aliphatic C1-6alkyl;
- each —RA2 is independently aliphatic C2-6alkenyl;
- each —RA3 is independently aliphatic C2-6alkynyl;
- each —RA4 is independently saturated C3-6cycloalkyl;
- each —RA5 is independently C3-6cycloalkenyl;
- each —RA6 is independently non-aromatic C3-7heterocyclyl;
- each —RA7 is independently C6-10-carboaryl;
- each —RA8 is independently C5-10heteroaryl;
- each -LA- is independently saturated aliphatic C1-3alkylene;
- and wherein:
- each —RA4, —RA5, —RA6, —RA7, and —RA8 is optionally substituted, for example, with one or more substituents —RB1 and/or one or more substituents —RB2, and
- each —RA1, —RA2, —RA3, and -LA- is optionally substituted, for example, with one or more substituents —RB2,
- wherein:
- each —RB1 is independently saturated aliphatic C1-4-alkyl, phenyl, or benzyl;
- each —RB2 is independently:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, -LC-OH, —O-LC-OH,
- —ORC1, -LC-ORC1, —O-LC-ORC1,
- —SH, —SRC1,
- —CN,
- —NO2,
- —NH2, —NHRC1, —NRC12, —NRC2RC3,
- -LC-NH2, -LC-NHRC1, -LC-NRC12, or -LC-NRC2RC3,
- —O-LC-NH2, —O-LC-NHRC1, —O-LC-NRC12, —O-LC-NRC2RC3,
- —C(═O)OH, —C(═O)ORC1,
- —OC(═O)RC1,
- —C(═O)RC1,
- —C(═O)NH2, —C(═O)NHRC1, —C(═O)NRC12, —C(═O)NRC2RC3,
- —NHC(═O)RC1, —NRC1C(═O)RC1,
- —NHS(═O)2RC1, —NRC1S(═O)2RC1,
- —S(═O)2NH2, —S(═O)2NHRC1, —S(═O)2NRC12, —S(═O)2NRC2RC3, or
- —S(═O)2RC1;
- wherein:
- each —RC1 is independently unsubstituted saturated aliphatic C1-4-alkyl, phenyl, or benzyl;
- each -LC- is independently unsubstituted saturated aliphatic C1-5alkylene;
- and
- in each group —NRC2RC3, —RC2 and —RC3, taken together with the nitrogen atom to which they are attached, form a 4-, 5-, 6-, or 7-membered non-aromatic ring having exactly 1 ring heteroatom or exactly 2 ring heteroatoms, wherein one of said exactly 2 ring heteroatoms is N, and the other of said exactly 2 ring heteroatoms is independently N, O, or S,
- and pharmaceutically and physiologically acceptable salts thereof.
117 more elements
A compound of formula:
- wherein
- —R— is independently selected from:
- wherein (T) indicates the point of attachment to -T;
- and (Q) indicates the point of attachment to -Q-;
- -Q- is independently selected from:
- —NHC(O)—;
- —NR1C(O)—;
- each —R1 is independently unsubstituted saturated aliphatic C1-4-alkyl;
- —P is independently selected from:
- where the asterisk indicates the point of attachment;
- -T is independently selected from:
- where the asterisk indicates the point of attachment;
- —W4 is independently —H or —WA;
- —W5 is independently —H or —WA;
- —W6 is independently —H or —WA;
- with the proviso that at least one of —W4, —W5 and —W6 is —WA;
- where —WA is independently selected from:
- —F, —Cl, —Br, —I,
- —OH, —WA1, —O—WA1,
- —NH2, —NHWA1, and —N(WA1)2;
- and —WA1 is independently selected from:
- unsubstituted saturated aliphatic C1-4-alkyl,
- —CF3,
- —CH2CH2OH, and
- —CH2CH2N(Me)2;
- -G1 is independently —H or -GA;
- -G2 is independently —H or -GA;
- where -GA is independently selected from:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, —OR2;
- —[O—CH2CH2]n—RB2, where n is 2 to 6;
- -G3 is independently —H or -GB;
- -G4 is independently —H or -GB
- where -GB is independently selected from:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, —OR2;
- —[O—CH2CH2]n—RB2, where n is 2 to 6;
- wherein:
- —P1 is independently —H or —PA;
- —P2 is independently —H or —PB;
- —P3 is independently —H or —PC;
- —P4 is independently —H or —PB;
- —P5 is independently —H or —PA;
- and wherein:
- each —PA, each —PB, and each —PC is independently:
- —F, —Cl, —Br, —I,
- —R2,
- —CF3, —OCF3,
- —OH, -L1-OH,
- —OR2, -L1-OR2, —O-L1-OR2,
- —SH, —SR2,
- —CN,
- —NO2,
- —NH2, —NHR2, —NR22, —NR3R4,
- —NHOH,
- -L1-NH2, -L1-NHR2, -L1-NR22, -L1-NR3R4,
- —O-L1-NH2, —O-L1-NHR2, —O-L1-NR22, —O-L1-NR3R4,
- —C(═O)OH, —C(═O)OR2,
- —OC(═O)R2,
- —C(═O)NH2, —C(═O)NHR2, —C(═O)NR22, —C(═O)NR3R4,
- —NHC(═O)R2, —NR2C(═O)R2,
- —C(═O)NHOR2, —C(═O)NR2OR2,
- —NHC(═O)OR2, —NR2C(═O)OR2,
- —OC(═O)NH2, —OC(═O)NHR2, —OC(═O)NR22, —OC(═O)NR3R4,
- —C(═O)R2,
- —NHC(═O)NH2, —NHC(═O)NHR2,
- —NHC(═O)NR22, —NHC(═O)NR3R4,
- —NR2C(═O)NH2, —NR2C(═O)NHR2,
- —NR2C(═O)NR22, —NR2C(═O)NR3R4,
- —NHS(═O)2R2, —NR2S(═O)2R2,
- —S(═O)2NH2, —S(═O)2NHR2, —S(═O)2NR22, —S(═O)2NR3R4,
- —S(═O)R2, —S(═O)2R2, —OS(═O)2R2, or —S(═O)2OR2
- wherein:
- each -L1- is independently saturated aliphatic C1-5alkylene;
- in each group —NR3R4, —R3 and —R4, taken together with the nitrogen atom to which they are attached, form a 4-, 5-, 6-, or 7-membered non-aromatic ring having exactly 1 ring heteroatom or exactly 2 ring heteroatoms, wherein one of said exactly 2 ring heteroatoms is N, and the other of said exactly 2 ring heteroatoms is independently N, O, or S;
- each —R2 is independently:
- —RA1, —RA2, —RA3, —RA4, —RA5, —RA6, —RA7, —RA8,
- -LA-RA4, -LA-RA5, -LA-RA6, -LA-RA7, or -LA-RA8;
- wherein:
- each —RA1 is independently saturated aliphatic C1-6alkyl;
- each —RA2 is independently aliphatic C2-6alkenyl;
- each —RA3 is independently aliphatic C2-6alkynyl;
- each —RA4 is independently saturated C3-6cycloalkyl;
- each —RA5 is independently C3-6cycloalkenyl;
- each —RA6 is independently non-aromatic C3-7heterocyclyl;
- each —RA7 is independently C6-10-carboaryl;
- each —RA8 is independently C5-10heteroaryl;
- each -LA- is independently saturated aliphatic C1-3alkylene;
- and wherein:
- each —RA4, —RA5, —RA6, —RA7, and —RA8 is optionally substituted, for example, with one or more substituents —RB1 and/or one or more substituents —RB2, and
- each —RA1, —RA2, —RA3, and -LA- is optionally substituted, for example, with one or more substituents —RB2,
- wherein:
- each —RB1 is independently saturated aliphatic C1-4-alkyl, phenyl, or benzyl;
- each —RB2 is independently:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, -LC-OH, —O-LC-OH,
- —ORC1, -LC-ORC1, —O-LC-ORC1,
- —SH, —SRC1,
- —CN,
- —NO2,
- —NH2, —NHRC1, —NRC12, —NRC2RC3,
- -LC-NH2, -LC-NHRC1, -LC-NRC12, or -LC-NRC2RC3,
- —O-LC-NH2, —O-LC-NHRC1, —O-LC-NRC12, —O-LC-NRC2RC3,
- —C(═O)OH, —C(═O)ORC1,
- —OC(═O)RC1,
- —C(═O)RC1,
- —C(═O)NH2, —C(═O)NHRC1, —C(═O)NRC12, —C(═O)NRC2RC3,
- —NHC(═O)RC1, —NRC1C(═O)RC1,
- —NHS(═O)2RC1, —NRC1S(═O)2RC1,
- —S(═O)2NH2, —S(═O)2NHRC1, —S(═O)2NRC12, —S(═O)2NRC2RC3, or
- —S(═O)2RC1;
- wherein:
- each —RC1 is independently unsubstituted saturated aliphatic C1-4-alkyl, phenyl, or benzyl;
- each -LC- is independently unsubstituted saturated aliphatic C1-5alkylene;
- and
- in each group —NRC2RC3, —RC2 and —RC3, taken together with the nitrogen atom to which they are attached, form a 4-, 5-, 6-, or 7-membered non-aromatic ring having exactly 1 ring heteroatom or exactly 2 ring heteroatoms, wherein one of said exactly 2 ring heteroatoms is N, and the other of said exactly 2 ring heteroatoms is independently N, O, or S;
- wherein the compound contains a —F group;
- and pharmaceutically and physiologically acceptable salts thereof;
- with the proviso that the compound is not compound P-001.
119 more elements
A compound of formula:
- wherein
- —R— is independently selected from:
- wherein (T) indicates the point of attachment to -T;
- and (Q) indicates the point of attachment to -Q-;
- -Q- is independently selected from:
- —NHC(O)—;
- —NR1C(O)—;
- —N═N—;
- —CH═CH—;
- —CR1═CH—;
- —CH═CR1—;
- —CR1═CR1—;
- each —R1 is independently unsubstituted saturated aliphatic C1-4-alkyl;
- —P is independently selected from:
- where the asterisk indicates the point of attachment;
- -T is independently selected from:
- where the asterisk indicates the point of attachment;
- and X is independently N;
- —W1 is independently H or —WA;
- where —WA is independently selected from:
- —F, —Cl, —Br, —I,
- —OH, —WA1, —O—WA1,
- —NH2, —NHWA1, and —N(WA1)2;
- and —WA1 is independently selected from:
- unsubstituted saturated aliphatic C1-4-alkyl,
- —CF3,
- —CH2CH2OH, and
- —CH2CH2N(Me)2;
- -G1 is independently —H or -GA;
- -G2 is independently —H or -GA;
- where -GA is independently selected from:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, —OR2;
- —[O—CH2CH2]n—RB2, where n is 2 to 6;
- -G3 is independently —H or -GB;
- -G4 is independently —H or -GB
- where -GB is independently selected from:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, —OR2;
- —[O—CH2CH2]n—RB2, where n is 2 to 6;
- wherein:
- —P1 is independently —H or —PA;
- —P2 is independently —H or —PB;
- —P3 is independently —H or —PC;
- —P4 is independently —H or —PB;
- —P5 is independently —H or —PA;
- and wherein:
- each —PA, each —PB, and each —PC is independently:
- —F, —Cl, —Br, —I,
- —R2,
- —CF3, —OCF3,
- —OH, -L1-OH,
- —OR2, -L1-OR2, —O-L1-OR2,
- —SH, —SR2,
- —CN,
- —NO2,
- —NH2, —NHR2, —NR22, —NR3R4,
- —NHOH,
- -L1-NH2, -L1-NHR2, -L1-NR22, -L1-NR3R4,
- —O-L1-NH2, —O-L1-NHR2, —O-L1-NR22, —O-L1-NR3R4,
- —C(═O)OH, —C(═O)OR2,
- —OC(═O)R2,
- —C(═O)NH2, —C(═O)NHR2, —C(═O)NR22, —C(═O)NR3R4,
- —NHC(═O)R2, —NR2C(═O)R2,
- —C(═O)NHOR2, —C(═O)NR2OR2,
- —NHC(═O)OR2, —NR2C(═O)OR2,
- —OC(═O)NH2, —OC(═O)NHR2, —OC(═O)NR22, —OC(═O)NR3R4,
- —C(═O)R2,
- —NHC(═O)NH2, —NHC(═O)NHR2,
- —NHC(═O)NR22, —NHC(═O)NR3R4,
- —NR2C(═O)NH2, —NR2C(═O)NHR2,
- —NR2C(═O)NR22, —NR2C(═O)NR3R4,
- —NHS(═O)2R2, —NR2S(═O)2R2,
- —S(═O)2NH2, —S(═O)2NHR2, —S(═O)2NR22, —S(═O)2NR3R4,
- —S(═O)R2, —S(═O)2R2, —OS(═O)2R2, or —S(═O)2OR2
- wherein:
- each -L1- is independently saturated aliphatic C1-5alkylene;
- in each group —NR3R4, —R3 and —R4, taken together with the nitrogen atom to which they are attached, form a 4-, 5-, 6-, or 7-membered non-aromatic ring having exactly 1 ring heteroatom or exactly 2 ring heteroatoms, wherein one of said exactly 2 ring heteroatoms is N, and the other of said exactly 2 ring heteroatoms is independently N, O, or S;
- each —R2 is independently:
- —RA1, —RA2, —RA3, —RA4, —RA5, —RA6, —RA7, —RA8,
- -LA-RA4, -LA-RA5, -LA-RA6, -LA-RA7, or -LA-RA8;
- wherein:
- each —RA1 is independently saturated aliphatic C1-6alkyl;
- each —RA2 is independently aliphatic C2-6alkenyl;
- each —RA3 is independently aliphatic C2-6alkynyl;
- each —RA4 is independently saturated C3-6cycloalkyl;
- each —RA5 is independently C3-6cycloalkenyl;
- each —RA6 is independently non-aromatic C3-7heterocyclyl;
- each —RA7 is independently C6-10-carboaryl;
- each —RA8 is independently C5-10heteroaryl;
- each -LA- is independently saturated aliphatic C1-3alkylene;
- and wherein:
- each —RA4, —RA5, —RA6, —RA7, and RA8 is optionally substituted, for example, with one or more substituents —RB1 and/or one or more substituents —RB2, and
- each —RA1, —RA2, —RA3, and -LA- is optionally substituted, for example, with one or more substituents —RB2,
- wherein:
- each —RB1 is independently saturated aliphatic C1-4-alkyl, phenyl, or benzyl;
- each —RB2 is independently:
- —F, —Cl, —Br, —I,
- —CF3, —OCF3,
- —OH, -LC-OH, —O-LC-OH,
- —ORC1, -LC-ORC1, —O-LC-ORC1,
- —SH, —SRC1,
- —CN,
- —NO2,
- —NH2, —NHRC1, —NRC12, —NRC2RC3,
- -LC-NH2, -LC-NHRC1, -LC-NRC12, or -LC-NRC2RC3,
- —O-LC-NH2, —O-LC-NHRC1, —O-LC-NRC12, —O-LC-NRC2RC3,
- —C(═O)OH, —C(═O)ORC1,
- —OC(═O)RC1,
- —C(═O)RC1,
- —C(═O)NH2, —C(═O)NHRC1, —C(═O)NRC12, —C(═O)NRC2RC3,
- —NHC(═O)RC1, —NRC1C(═O)RC1,
- —NHS(═O)2RC1, —NRC1S(═O)2RC1,
- —S(═O)2NH2, —S(═O)2NHRC1, —S(═O)2NRC12, —S(═O)2NRC2RC3, or
- —S(═O)2RC1;
- wherein:
- each —RC1 is independently unsubstituted saturated aliphatic C1-4-alkyl, phenyl, or benzyl;
- and
- each -LC- is independently unsubstituted saturated aliphatic C1-5alkylene;
- and
- in each group —NRC2RC3, —RC2 and —RC3, taken together with the nitrogen atom to which they are attached, form a 4-, 5-, 6-, or 7-membered non-aromatic ring having exactly 1 ring heteroatom or exactly 2 ring heteroatoms, wherein one of said exactly 2 ring heteroatoms is N, and the other of said exactly 2 ring heteroatoms is independently N, O, or S,
- and pharmaceutically and physiologically acceptable salts thereof.
121 more elements
Dependencies are inferred from the claim text.