Nova Patents
RU2010146485A

Novel estrogen receptor ligands

Abstract

1. A compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt! ! wherein R1 is selected from the group consisting of halogen atom, cyano, nitro, ORΛ, N (RB) 2, -C (O) C1-4 alkyl, -SO2C1-4alkila, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, galogenC1 -6alkila, digalogenC1-6alkila, trigalogenC1-6alkila, galogenC2-6alkenila, digalogenC2-6alkenila, trigalogenC2-6alkenila, tsianoC1-6alkila, C1-4alkoksiC1-6alkila, C3-8 cycloalkyl, C3-8tsikloalkilC1-6alkila, phenyl, benzyl and 5-10 membered heterocyclyl, wherein said phenyl, benzyl or heterocyclyl group can either be unsubstituted or substituted with 1-3 substituents, wherein each substituent is selected from the g Rupp consisting of ORΛ, halogen atom, cyano, nitro, -C (O) C1-4 alkyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, galogenC1-6alkila, and digalogenC1-6alkila trigalogenC1-6alkila; ! R2 is selected from the group consisting of halogen atom, cyano, nitro, ORA, N (RB) 2, N (OH) 2, -C (O) C 1-4 alkyl optionally substituted with 1-3 halogens, -SO2C1-4alkila, -C (O) NH-OH, -C (NH2) = N-OH, -C (CO2H) = N-OH, -C (NH2) = NH, -C (NHC1-4alkil) = NH, -C ( O-C1-4 alkyl) = NH, -C (NH2) = N-NH2, -NH-C (NH2) = NH, -NH-C (O) NH2, -N = C (-NH-CH2CH2-NH- ), -S-CN, -SC (NH2) = NH, -SC (NH2) = N-OH, -CO2H, -CH2-CO2H, -CH (OH) CO2H, -C (O) CO2H, SO3H, CH2SO3H , C1-6alkyl, galogenC1-6alkila, digalogenC1-6alkila, trigalogenC1-6alkila, tsianoC1-6alkila, C1-4alkoksiC1-6alkila, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8tsikloalkilC1-6alkila, phenyl, benzyl and 5 -10-membered heterocyclyl, wherein said phenyl,

RU2010146485A, drawing sheet 1
Sheet 1 of 1

Term

No projected expiry on record.

  1. Priority
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25 claims: 4 independent, 21 dependent

  1. 1
    A compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt 1. Соединение формулы (I) или его фармацевтически приемлемый сложный эфир, амид, карбамат, сольват или соль, включая соль такого сложного эфира, амида или карбамата и сольват такого сложного эфира, амида, карбамата или соли where R1 is selected from the group consisting of halogen atom, cyano, nitro, ORL., N (RB)2, -C (O) C1-4alkyl, -SO2C1-4alkyl, C1-6alkyl, C2-6alkenyl, C2-6alkynylaniline, galogenC1-6alkyl digalogenC1-6alkyl trigalogenC1-6alkyl, haloC2-6alkenyl digalogenC2-6alkenyl trigalogenC2-6alkenyl tsianoC1-6alkyl, C1-4alkoksiC1-6alkyl, C3-8cycloalkyl, C3-8tsikloalkilC1-6alkyl, phenyl, benzyl and 5-10 membered heterocyclyl, wherein said phenyl, benzyl or heterocyclyl group can either be unsubstituted or substituted with 1-3 substituents, wherein each substituent is selected from the group consisting of ORL., Halogen, cyano, nitro, -C (O) C1-4alkyl, C1-6alkyl, C2-6alkenyl, C2-6alkynylaniline, galogenC1-6alkyl digalogenC1-6alkyl and trigalogenC1-6alkyl;R2 is selected from the group consisting of halogen atom, cyano, nitro, ORA, N (RB)2, N (OH)2, -C (O) C1-4alkyl optionally substituted with 1-3 halogen atoms, -SO2C1-4алкила, -C (O) NH-OH, -C (NH2)=N-OH, -C(CO2H)=N-OH, -C(NH2) = NH, -C (NHC1-4алкил)=NH, -C(O-C1-4алкил) = NH, -C (NH2)=N-NH2, -NH-C (NH2) = NH, -NH-C (O) NH2, -N=C(-NH-CH2CH2-NH-), -S-CN, -S-C(NH2)=NH, -S-C(NH2)=N-OH, -CO2H, -CH2-CO2H, -CH(OH)CO2H, -C(O)CO2H, SO3H, CH2SO3H, C1-6alkyl, haloC1-6alkyl digalogenC1-6alkyl trigalogenC1-6alkyl tsianoC1-6alkyl, C1-4alkoksiC1-6alkyl, C2-6alkenyl, C2-6alkynylaniline, C3-8cycloalkyl, C3-8tsikloalkilC1-6alkyl, phenyl, benzyl and 5-10 membered heterocyclyl, wherein said phenyl, benzyl or heterocyclyl group can either be unsubstituted or substituted with 1-3 substituents, wherein each substituent is selected from the group consisting of ORL., Halogen, cyano, nitro, C1-6alkyl, C2-6alkenyl, C2-6alkynylaniline, galogenC1-6alkyl digalogenC1-6alkyl and trigalogenC1-6alkyl;with the proviso that if one of R1 and R2 It represents a halogen atom, the other must be a group other than a halogen atom;each of R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen, ORA, Halogen, cyano, nitro, C1-6alkyl, C2-6alkenyl, C2-6alkynylaniline, galogenC1-6alkyl digalogenC1-6alkyl and trigalogenC1-6alkyl;each RA are independently selected from the group consisting of hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynylaniline, C3-8cycloalkyl, C3-8tsikloalkilC1-6alkyl, C6-10арила и C6-10arilC1-6alkyl, each of which is optionally substituted by 1-3 halogen atoms;and each RB are independently selected from the group consisting of hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynylaniline, C3-8cycloalkyl, C3-8tsikloalkilC1-6alkyl, C6-10арила и C6-10arilC1-6alkyl, each of which is optionally substituted by 1-3 halogen atoms;with the proviso that the compound of formula (I) does not represent 4- [3- (4,5-Digidro-1H-imidazol-2-yl) -2- (3,5-dimethylisoxazol-4-yl) indol-1-yl] phenol;1- (4-Gidroksifyenil) 2 (4-myetilimidazol-1-exposed) -1H-indole-3-karbonitril;1- (4-Gidroksifenil) -2- (1H-pyrazol-3-yl) -1H-indole-3-carbonitrile;1- (3-Chloro-4-gidroksifenil) -2- (1-methyl-1H-pyrazol-4-yl) -1H-indole-3-carbonitrile;1- (4-Hydroxyphenyl) -2-prop-1-ynyl-1H-indole-3-carboxylic acid amide;or 1- (4-Hydroxyphenyl) -2-thiazol-2-yl-1H-indole-3-carboxylic acid.
  2. 19
    6. Соединение по п.5, где R1 выбирают из группы, состоящей из ORA, N(RB)2, -C(O)C1-4алкила, C1-4алкила, C2-4алкенила, C2-4алкинила, фенила и 5-6-членного гетероциклила, где упомянутые фенильная или гетероциклильная группы могут быть либо незамещенными, либо замещенными 1-3 заместителями, выбранными из атома галогена, циано, C1-4алкила, -C(O)C1-4алкила и ORA, где RA представляет собой атом водорода или C1-4алкил. 19. A pharmaceutical composition which comprises a compound according to any one of claims 1-18 together with a pharmaceutically acceptable carrier.
  3. 20
    7. Соединение по п.1, где R2 выбирают из группы, состоящей из атома галогена, ORA, N(RB)2, -C(O)C1-4алкила, необязательно замещенного 1-3 атомами галогена, -C(NH2)=N-OH, -CO2H, -CH2-CO2H, C1-6алкила, C2-6алкенила, C2-6алкинила, галогенC1-4алкила, дигалогенC1-4алкила, тригалогенC1-4алкила, галогенC2-4алкенила, дигалогенC2-4алкенила, тригалогенC2-4алкенила, фенила и 5-6-членного гетероциклила, где упомянутые фенильная или гетероциклильная группы могут быть либо незамещенными, либо замещенными 1-3 заместителями, выбранными из группы, состоящей из ORΛ, атома галогена, циано, -C(O)C1-4алкила, C1-4алкила, C2-4алкенила, C2-4алкинила, галогенC1-4алкила, дигалогенC1-4алкила и тригалогенC1-4алкила. 20. A compound according to any one of claims 1-18 for use as a medicament.
  4. 23
    10. Соединение по п.9, где каждую из R3, R4, R5 и R6 независимо выбирают из группы, состоящей из атома водорода, OH, атома галогена, циано, метила и трифторметила. 23. Use of a compound according to any one of claims 1-18 for the manufacture of a medicament for the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
Independent claims4