Novel benzamide derivatives as modulators of the follicle stimulating hormone
AssigneeAddex Pharma SA
InventorsBeatrice Bonnet, Brice Campo, Luca Raveglia, Mauro Riccaboni
Life of this patent
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Abstract
The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1n are defined as in formula I; invention compounds are modulators of follicle-stimulating hormone—(“FSH”) which are useful for male and female contraception as well as other disorders modulated by FSH receptor.
Claims25
1-33. (canceled)
A compound having the formula I-A
- or a pharmaceutically acceptable salt, hydrate or solvate of such compound
- wherein:
- represents independently O—(C1-C6)alkyl, O—(C2-C6)alkynyl, O—(C2-C6)alkenyl, O—(C3-C7)cycloalkyl and O-alkylcycloalkyl;
- R2 represents independently hydrogen, OH, an optionally substituted (C1-C6)alkyl, (C2-C6)alkynyl, (C2-C6)alkenyl, (C3-C7)cycloalkyl, (C4-C10)alkylcycloalkyl, (C1-C6)heterocycloalkyl, (C1-C6)alkyl-heteroaryl, (C1-C6)alkyl-aryl or (C1-C6)alkyl-CN;
- R1 and R2 according to the above definitions can be combined to form a heterocycloalkyl ring;
- R4 is independently selected from the group consisting of hydrogen, OH, (C0-C6)alkyl-CN, (C1-C6)alkyl, (C0-C6)alkylhalo, (C3-C6)cycloalkyl, (C1-C6)alkyl-(C3-C8)cycloalkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C0-C6)alkyl-OR9, (C1-C6)alkyl-NRgR10, (C0-C6)-alkyl-NR9COR10, (C0-C6)alkyl-NR9SO2R10, (C0-C6)alkyl-NR11CONR10R9, (C0-C6)alkyl-SR9, (C0-C6)alkyl-S(═O) R9, (C0-C6)alkyl-S(═O)2R9, (C0-C6)alkyl-S(═O)2NR10R9, (C0-C6)alkyl-C(═O)—(C1-C6), (C0-C6)alkyl-C(O)—O—R9, (C0-C6)alkyl-C(═O)NR10R9, (C0-C6)alkyl-C(═NR10) R9, or (C0-C6)alkyl-C(═NOR10)R9, heterocycloalkyl, heteroaryl, heteroarylalkyl, arylalkyl or aryl;
- any of which is optionally substituted with 1-5 independent halogen, CN, (C1-C6)alkyl, O—(C0-C6)alkyl, O-alkylcycloalkyl, O(aryl), O(heteroaryl), O-(heterocycloalkyl), N(C0-C6-alkyl)2, N((C0-C6)alkyl)((C3-C7-) cycloalkyl) or N((C0-C6)alkyl)(aryl) substituents;
- R5, R6 are each independently selected from the group consisting of hydrogen, (C0-C6)alkyl-CN, (C1-C6)alkyl, (C0-C6)alkylhalo, (C3-C6)cycloalkyl, (C1-C6)alkyl-(C3-C8)cycloalkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C0-C6)alkyl-OR9, (C1-C6)alkyl-NRgR10, (C0-C6)-alkyl-NR9C0R10, (C0-C6)alkyl-NR9SO2R10, (C0-C6)alkyl-NR11CONR10R9, (C0-C6)alkyl-SR9, (C0-C6)alkyl-S(═O) R9, (C0-C6)alkyl-S(═O)2R9, (C0-C6)alkyl-S(═O)2NR10R9, (C0-C6)alkyl-C(═O)—(C1-C6), (C0-C6)alkyl-C(O)—O—R9, (C0-C6)alkyl-C(═O)NR10R9, (C0-C6)alkyl-C(═NR10) R9, or (C0-C6)alkyl-C(═NOR10)R9, heterocycloalkyl, heteroaryl, heteroarylalkyl, arylalkyl or aryl;
- any of which is optionally substituted with 1-5 independent halogen, CN, (C1-C6)alkyl, O—(C0-C6)alkyl, O-alkylcycloalkyl, O(aryl), O(heteroaryl), O-(heterocycloalkyl), N(C0-C6-alkyl)2, N((C0-C6)alkyl)((C3-C7-) cycloalkyl) or N((C0-C6)alkyl)(aryl) substituents;
- G1 is independently selected from the group consisting of hydrogen, OH, (C0-C6)alkyl-CN, (C1-C6)alkyl, (C0-C6)alkylhalo, (C3-C6)cycloalkyl, (C0-C6)alkyl-(C3-C8)cycloalkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C0-C6)alkyl-OR9, (C0-C6)alkyl-NR9R10, (C0-C6)-alkyl-NR9COR10, (C0-C6)alkyl-NR9SO2R10, (C0-C6)alkyl-NR11CONR10R9, (C0-C6)alkyl-SR9, (C0-C6)alkyl-S(═O) R9, (C0-C6)alkyl-S(═O)2R9, (C0-C6)alkyl-S(═O)2NR10R9, (C0-C6)alkyl-C(═O)—(C1-C6), (C0-C6)alkyl-C(O)—O—R9, (C0-C6)alkyl-C(═O)NR10R9, (C0-C6)alkyl-C(═NR10) R9, or (C0-C6)alkyl-C(═NOR10)R9, heterocycloalkyl, heteroaryl, heteroarylalkyl, arylalkyl or aryl;
- any of which is optionally substituted with 1-5 independent halogen, CN, (C1-C6)alkyl, O—(C0-C6)alkyl, O-alkylcycloalkyl, O(aryl), O(heteroaryl), O-(heterocycloalkyl), N(C0-C6-alkyl)2, N((C0-C6)alkyl)((C3-C7-) cycloalkyl) or N((C0-C6)alkyl)(aryl) substituents, wherein optionally two substituents are combined to the intervening atoms to form a bicyclic heterocycloalkyl, aryl or heteroaryl ring;
- wherein each ring is optionally further substituted with 1-5 independent halogen, CN, (C1-C6)alkyl, O—(C0-C6)alkyl, O-alkylcycloalkyl, O(aryl), O(heteroaryl), O-arylalkyl, O-heteroarylalkyl, N((-C0-C6)alkyl)((C0-C3)arylalkyl) or N((C0-C6)alkyl)(heteroarylalkyl) groups;
- R9, R10, R11 each independently is hydrogen, (C1-C6)alkyl, (C3-C6)cycloalkyl, (C1-C6)alkyl-(C3-C8)cycloalkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, heterocycloalkyl, heteroaryl, heteroarylalkyl, arylalkyl or aryl;
- any of which is optionally substituted with 1-5 independent halogen, CN, (C1-C6)alkyl, O—(C0-C6)alkyl, O-alkylcycloalkyl, O(aryl), O(heteroaryl), N(C0-C6-alkyl)2, —N((C0-C6)alkyl)((C3-C7-)cycloalkyl) or N((C0-C6)alkyl)(aryl) substituents;
- n is an integer from 1 to 4, provided that when n>1, the G1 groups may be the same or different from each other;
- R7 and R8 represent independently an optionally substituted (C1-C4)alkyl, (C1-C6)alkylhalo, (C0-C6)alkyl-aryl, (C1-C6)alkyl-O—(C0-C6)-alkyl, (C0-C6)alkyl-heteroaryl, (C0-C6)alkyl-heterocycloalkyl, (C0-C6)alkyl-(C3-C7)cycloalkyl or R7 and R8 can together form a (C3-C6)cycloalkyl or an heterocycloalkyl group of formula:
- X2 is independently selected from the group consisting of CH2, O, S, SO2;
- M is independently selected from the group of consisting of a bond, an optionally substituted (C1-C6)alkyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C2-C6)alkenyl, (C1-C6)alkyl-O—(C0-C6)alkyl, (C0-C6)alkyl-S(═O)2NR12—(C0-C6)alkyl, (C0-C6)alkyl-NR12—S(═O)2—(C0-C6)alkyl, (C0-C6)alkyl-C(═O)—NR12-(C0-C6)alkyl, (C0-C6)alkyl-NR12C(═O)—(C0-C6)alkyl, (C0-C6)alkyl-NR12—C(═O)—O—(C0-C6)alkyl, (C0-C6)alkyl-O—C(═O)—NR12—(C0-C6)alkyl or (C0-C6)alkyl-NR12—C(═O)—NR13—(C0-C6)alkyl substituents;
- wherein optionally two substituents are combined with the intervening atoms to form a cycloalkyl or heterocycloalkyl ring;
- R12 and R13 are each independently selected from the group consisting of hydrogen, an optionally substituted (C1-C6)alkyl;
- Q represents independently H, an optionally substituted (C1-C6)alkyl, (C0-C6)alkyl-CN, (C1-C6)alkylhalo, (C3-C7)cycloalkyl, (C3-C7) heterocycloalkyl or one of the following aryl or heteroaryl:
- G2 groups are each independently selected from the group consisting of hydrogen, halogen, CN, OH, nitro, an optionally substituted (C1-C6)alkyl, (C1-C6)alkylhalo, (C2-C6)alkynyl, (C2-C6)alkenyl, O—(C1-C6)alkyl, O—(C1-C6)alkylhalo, O—(C3-C6)alkynyl, O—(C3-C6)alkenyl, O—(C2-C6)alkyl-OR14, O—(C3-C7)cycloalkyl, O—(C1-C6)alkyl-heteroaryl, O—(C1-C6)alkyl-aryl, (C0-C6)alkyl-OR14, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, O—(C3-C7)cycloalkyl-(C1-C6)alkyl, O-heteroaryl, heteroaryl, (C1-C6)alkyl-heteroaryl, aryl, O-aryl, (C1-C6)alkyl-aryl, (C1-C6)alkylhalo-OR17, (C3-C6)alkynyl-OR17, (C3-C6)alkenyl-OR17, (C0-C6)alkyl-S—R17, O—(C2-C6)alkyl-S—R17, (C0-C6)alkyl-S(═O)—R17, O—(C2-C6)alkyl-S(═O)—R17, (C0-C6)alkyl-S(═O)2—R17, O—(C1-C6)alkyl-S(═O)2—R17, (C0-C6)alkyl-NR17R18, O—(C2-C6)alkyl-NR17R18, (C0-C6)alkyl-S(═O)2NR17R18, (C0-C6)alkyl-NR17—S(═O)2R18, O—(C1-C6)alkyl-S(═O)2NR17R18, O—(C2-C6)alkyl-NR17—S(═O)2R18, (C0-C6)alkyl-C(═O)—NR17R18, (C0-C6)alkyl-NR17C(═O)—R18, O—(C1-C6)alkyl-C(═O)—NR17R18, O—(C2-C6)alkyl-NR17C(═O)—R18, (C0-C6)alkyl-OC(═O)—R17, (C0-C6)alkyl-C(═O)—OR17, O—(C2-C6)alkyl-OC(═O)—R17, O—(C1-C6)alkyl-C(═O)—OR17, (C0-C6)alkyl-C(═O)—R17, O—(C1-C6)alkyl-C(═O)—R17, (C0-C6)alkyl-NR17—C(═O)—OR18, (C0-C6)alkyl-O—C(═O)—NR17R18 or (C0-C6)alkyl-NR17—C(═O)—NR18R19 substituents;
- wherein optionally two substituents are combined to the intervening atoms to form a bicyclic aryl, cycloalkyl, heterocycloalkyl or heteroaryl ring;
- wherein each ring is optionally further substituted with 1-5 independent hydrogen, halogen, CN, OH, nitro, an optionally substituted (C1-C6)alkyl, (C1-C6)alkylhalo, (C2-C6)alkynyl, (C2-C6)alkenyl, O—(C1-C6)alkyl, O—(C1-C6)alkylhalo, O—(C3-C6)alkynyl, O—(C3-C6)alkenyl, O—(C3-C7)cycloalkyl, O—(C1-C6)alkyl-heteroaryl, O—(C1-C6)alkylaryl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, O—(C3-C7)cycloalkyl-(C1-C6)alkyl, O-heteroaryl, heteroaryl, (C1-C6)alkyl-heteroaryl, aryl, O-aryl;
- p is an integer that is selected from the group consisting of 1, 2, 3, 4 and 5 provided that when p>1, the G2 groups may be the same or different from each other;
- R16, R17, R18, R19, R20 and R21 are each independently selected from the group consisting of hydrogen, an optionally substituted (C1-C6)alkyl, (C1-C6)alkylhalo, (C1-C6)alkyl-CN, (C1-C6)alkyl-O—(C0-C6)alkyl, (C1-C6)alkyl-N((C0-C6)alkyl)2, (C1-C6)alkyl-C(═O)—O—(C0-C6)alkyl, (C1-C6)alkyl-heterocycloalkyl, (C2-C6)alkynyl, (C2-C6)alkenyl, (C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, heteroaryl, (C1-C6)alkyl-heteroaryl, aryl;
- Z1, Z2, Z3 and Z4 are each independently selected from the group consisting of bond, —C═, —C═C—, —C(═O)—, —C(═S)—, —C—, —O—, —N═, —N— or —S— which may further be substituted by G2p groups;
- B1, B2 and B3 are each selected independently from —C— or —N— which may further be substituted by one G2p group;
- Any N or S bearing ring may be in its N-oxide, S-oxide or S-dioxide form;
- And wherein the compound of formula I-A includes both possible stereoisomers and includes not only racemic compounds but the individual enantiomers as well;
- With the following provisos:
- When R7 and R8 are each independently selected from an optionally substituted (C1-C4)alkyl, or can together form a (C3-C6)cycloalkyl or an heterocycloalkyl group of formula
- and Gin are hydrogens, then
- can not be
- If R7 and R8 all represent CH3 at the same time, then M-Q may not represent CH3;
- R7 and R8 may not represent at the same time (C0-C6)alkyl-aryl, (C0-C6)alkyl-heteroaryl;
- When n>1, G1n groups may not represent at the same time OH;
- If R7, R8 and M represent at the same time an optionally substituted (C1-C4)alkyl, then Q can not be H;
- If R7, R8 represent
- then compounds of the following list are excluded:
- 3,4-dimethoxy-N-[4-[1-[[(4-methoxyphenyl)amino]carbonyl]cyclopentyl]phenyl]-benzamide
- N-[4-(1-cyanocyclopentyl)phenyl]-3,4-dimethoxy-benzamide.
A compound according to claim 1, which can exist as optical isomers, wherein said compound is either the racemic mixture or one or both of the individual optical isomers.
A compound according to claim 1, wherein said compound is selected from:
- Pyrazolo[1,5-a]pyridine-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- Benzo[b]thiophene-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-[4-(Cyano-dimethyl-methyl)-3-ethyl-phenyl]-3,4-dimethoxy-benzamide
- 5-Fluoro-1H-indole-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 6-Fluoro-1H-benzoimidazole-2-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-[4-(Cyano-dimethyl-methyl)-3-thiophen-2-yl-phenyl]-3,4-dimethoxy-benzamide
- 6-Fluoro-imidazo[1,2-a]pyridine-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-(4-{2-[2-(5-Fluoro-indol-1-yl)-acetylamino]-1,1-dimethyl-ethyl}-phenyl)-3,4-dimethoxy-benzamide
- 1H-Pyrrolo[2,3-b]pyridine-5-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-[4-(2-Acetylamino-1,1-dimethyl-ethyl)-3-ethyl-phenyl]-3,4-dimethoxy-benzamide
- 3H-Imidazo[4,5-b]pyridine-6-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-2-ethyl-phenyl]-2-methyl-propyl}-amide
- 5-Fluoro-1H-pyrrolo[2,3-c]pyridine-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-[4-(2-Benzoylamino-1,1-dimethyl-ethyl)-phenyl]-3,4-dimethoxy-benzamide
- Furan-2-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-{4-[1,1-Dimethyl-2-(3-phenyl-propionylamino)-ethyl]-phenyl}-3,4-dimethoxy-benzamide
- 1-Methyl-1H-indazole-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- Thiophene-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- Pyridine-2-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 1H-Indazole-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-[4-(Cyano-dimethyl-methyl)-3-methyl-phenyl]-3,4-dimethoxy-benzamide
- N-[4-(Cyano-dimethyl-methyl)-3-trifluoromethyl-phenyl]-3,4-dimethoxy-benzamide
- 1H-Indole-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 1H-Indazole-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-2-methyl-phenyl]-2-methyl-propyl}-amide
- 1-Methyl-1H-Indazole-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-2-methyl-phenyl]-2-methyl-propyl}-amide
- 1H-Indazole-3-carboxylic acid {2-[2-chloro-4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-[3,5-Dichloro-4-(cyano-dimethyl-methyl)-phenyl]-3,4-dimethoxy-benzamide
- 1-Methyl-1H-indazole-3-carboxylic acid {2-[2-chloro-4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-{4-[2-(2-1H-Indol-3-yl-acetylamino)-1,1-dimethyl-ethyl]-phenyl
- N-[4-(Cyano-dimethyl-methyl)-3-pyridin-3-yl-phenyl]-3,4-dimethoxy-benzamide
- 1H-Indole-5-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 1H-Benzoimidazole-5-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- Imidazo[1,2-a]pyridine-3-carboxylic acid {3-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-3-methyl-butyl}-amide
- 3H-Imidazo[4,5-c]pyridine-2-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 5-Fluoro-1H-pyrrolo[2,3-b]pyridine-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 3H-Imidazo[4,5-b]pyridine-2-carboxylic acid {3-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-3-methyl-butyl}-amide
- 5-Fluoro-1-(2-methoxy-ethyl)-1H-indole-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 7-Fluoro-1H-pyrrolo[2,3-c]pyridine-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 3H-Imidazo[4,5-b]pyridine-6-carboxylic acid {3-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-3-methyl-butyl}-amide
- 5-Chloro-1H-pyrrolo[2,3-c]pyridine-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 1H-Pyrrolo[2,3-b]pyridine-5-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- Imidazo[1,2-a]pyridine-3-carboxylic acid {2-[3-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- and pharmaceutically acceptable salts thereof.
A compound according to claim 1 wherein said compound is selected from:
- 1-Acetyl-1H-indole-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 1-Methyl-1H-indole-2-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 5-Methyl-1H-pyrazole-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 3H-Imidazo[4,5-b]pyridine-2-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-[4-(Cyano-dimethyl-methyl)-3-(1-methyl-1H-pyrazol-4-yl)-phenyl]-3,4-dimethoxy-benzamide
- 2-Methyl-1H-benzoimidazole-5-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 1,3-Dimethyl-2-oxo-2,3-dihydro-1H-benzoimidazole-5-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 1H-Pyrrolo[2,3-c]pyridine-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- Imidazo[1,2-a]pyrimidine-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-(4-(4-acetamido-2-methylbutan-2-yl)-3-(pyridin-3-yl)phenyl)-3,4-dimethoxybenzamide
- 1-Methyl-1H-indazole-3-carboxylic acid {1-[3-(3,4-dimethoxy-benzoylamino)-phenyl]-cyclopentylmethyl}-amide
- N-[4-Chloro-3-(cyano-dimethyl-methyl)-phenyl]-3,4-dimethoxy-benzamide
- N-[4-(Cyano-dimethyl-methyl)-3-pyrimidin-5-yl-phenyl]-3,4-dimethoxy-benzamide
- N-[4-(Cyano-dimethyl-methyl)-3-pyridin-2-yl-phenyl]-3,4-dimethoxy-benzamide
- N-[4-(Cyano-dimethyl-methyl)-3-morpholin-4-yl-phenyl]-3,4-dimethoxy-benzamide
- 1,2-Dimethyl-1H-benzoimidazole-5-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- Imidazo[1,2-a]pyrimidine-2-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 3H-Imidazo[4,5-b]pyridine-6-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- N-[4-(2-Acetylamino-1,1-dimethyl-ethyl)-3-pyridin-3-yl-phenyl]-3,4-dimethoxy-benzamide
- Imidazo[1,2-a]pyridine-6-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- 1-(3-Dimethylamino-propyl)-5-fluoro-1H-indole-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-2-methyl-propyl}-amide
- Imidazo[1,2-a]pyridine-3-carboxylic acid {2-[4-(3,4-dimethoxy-benzoylamino)-phenyl]-3-hydroxy-2-methyl-propyl}-amide
- and pharmaceutically acceptable salts thereof.
A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier and/or excipient.
A method in treating or preventing a condition in a mammal, including a human, the treatment or prevention of which is affected or facilitated by the effect of FSH receptor negative allosteric modulators, the method comprising:
- administering a compound of claim 1 to the mammal in need thereof.
A method to provide female or male contraception, the method comprising:
- administering a compound according to claim 1 to a female or male in need thereof.
A method to treat or prevent disorders selected from the group consisting of uterine fibroids, endometriosis, polycystic ovarian disease, dysfunctional uterine bleeding, hormono-dependent cancer, prostate cancer, uterine cancer, breast cancer and ovarian cancer;
- or osteoporosis, the method comprising:
- administering a compound of claim 1 to a subject suffering from or susceptible to a disorder selected from the group consisting of uterine fibroids, endometriosis, polycystic ovarian disease, dysfunctional uterine bleeding, hormono-dependent cancer, prostate cancer, uterine cancer, breast cancer and ovarian cancer;
- or osteoporosis.
A method to treat or prevent disorders selected from the group consisting of uterine fibroids, endometriosis, polycystic ovarian disease, dysfunctional uterine bleeding, hormono-dependent cancer, prostate cancer, uterine cancer, breast cancer and ovarian cancer;
- or osteoporosis, the method comprising:
- administering a compound of claim 1 to a subject suffering from or susceptible to a disorder selected from the group consisting of uterine fibroids, endometriosis, polycystic ovarian disease, dysfunctional uterine bleeding, hormono-dependent cancer, prostate cancer, uterine cancer, breast cancer and ovarian cancer;
- or osteoporosis.
A method for fertility control in a mammal including men or women, the method comprising:
- administering a compound of claim 1 to a mammal including men or women in need thereof.
A method for treating or preventing uterine fibroids, endometriosis, polycystic ovarian disease, and/or dysfunctional uterine bleeding, the method comprising:
- administering a compound of claim 1 to a subject suffering from or susceptible to uterine fibroids, endometriosis, polycystic ovarian disease, and/or dysfunctional uterine bleeding.
A method to treat hormono-dependent cancer, prostate cancer, uterine cancer, breast cancer and/or ovarian cancer, the method comprising:
- administering a compound of claim 1 to a subject suffering from or susceptible to hormono-dependent cancer, prostate cancer, uterine cancer, breast cancer and/or ovarian cancer.
A method for treating or preventing osteoporosis, the method comprising:
- administering a compound of claim 1 to a subject suffering from or susceptible to osteoporosis.
A method for preparing a tracer for imaging FSH receptors, comprising:
- using a compound of claim 1 to prepare a tracer for imaging a FSH receptor.
Dependencies are inferred from the claim text.