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11. 发明专利

ZA201400708B NOVEL ESTROGEN RECEPTOR LIGANDS 未知
公开(公告)号：ZA201400708B
公开(公告)日：2015-12-23
申请号：ZA201400708
申请日：2014-01-29
申请人： KAROBIO AB
发明人： NOTEBERG DANIEL , KOEHLER KONRAD , LOFSTEDT JOAKIM , GARG NEERAJ , HAGBERG LARS , KOCH EVA , KRUGER LARS , CHENG AIPING

12. 发明专利

DK2276732T3 Hidtil ukendte østrogenreceptorligander 未知
公开(公告)号：DK2276732T3
公开(公告)日：2015-08-17
申请号：DK09731606
申请日：2009-04-16
申请人： KAROBIO AB
发明人： RHÖNNSTAD PATRIK , KALLIN ELISABET , APELQVIST THERESA , CHENG AIPING , WENNERSTÃ L MATTIAS
IPC分类号： C07D209/08 , A61K31/404 , A61P3/06 , A61P5/24 , A61P13/00 , C07D209/12 , C07D209/22 , C07D209/36 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14

13. 发明专利

AU2009237657A1 Novel estrogen receptor ligands 未知
公开(公告)号：AU2009237657A1
公开(公告)日：2009-10-22
申请号：AU2009237657
申请日：2009-04-16
申请人： KAROBIO AB
发明人： APELQVIST THERESA , CHENG AIPING , KALLIN ELISABET , WENNERSTAL MATTIAS , RHONNSTAD PATRIK
IPC分类号： C07D209/08 , A61K31/404 , A61P3/06 , A61P5/24 , A61P13/00 , C07D209/12 , C07D209/22 , C07D209/36 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14
摘要： The invention provides 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. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R5 and R6 are as defined in the specification.

14. 发明专利

NO20076418L 未知
公开(公告)号：NO20076418L
公开(公告)日：2008-03-25
申请号：NO20076418
申请日：2007-12-12
申请人： KAROBIO AB
发明人： KOCH EVA KRISTINA , COLLAZO ANNA MARIA GARCIA , LOFSTEDT ANTON JOAKIM , CHENG AIPING , HANSSON TOMAS FREDRIK , ZAMARATSKI EDOUARD
IPC分类号： C07D277/64 , C07D215/20 , C07D215/233 , C07D215/38 , C07D215/48 , C07D231/56 , C07D263/56
摘要： The invention provides Compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, wherein R3, R4, G, Y, W and R5 are as defined in the specification. The invention also provides the use of such Compounds in the treatment or Prophylaxis of a condition associated with a disease or disorder associated with thyroid receptor activity.

15. 发明专利

CA2651134A1 INDOLE DERIVATIVES AND THEIR USE AS THYROID RECEPTOR LIGANDS 未知
公开(公告)号：CA2651134A1
公开(公告)日：2007-11-29
申请号：CA2651134
申请日：2007-05-24
申请人： KAROBIO AB
发明人： CHENG AIPING , HANSSON TOMAS FREDRIK , KOCH EVA KRISTINA , GARCIA COLLAZO ANA MARIA , MALM LARS JOHAN
IPC分类号： C07D209/08 , A61K31/404 , A61P5/14 , C07D209/18 , C07D209/20 , C07D405/04 , C07D413/04
摘要： The invention provides compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, (I) wherein R1, R2, R3, R4, R5, R6, Y and W are as defined in the specification. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition that may be treated with a thyroid receptor agonist or partial agonist.

16. 发明专利

HUE025471T2 Új ösztrogén receptor ligandumok 未知
公开(公告)号：HUE025471T2
公开(公告)日：2016-03-29
申请号：HUE09731606
申请日：2009-04-16
申请人： KAROBIO AB
发明人： RHOENNSTAD PATRIK , KALLIN ELISABET , APELQVIST THERESA , WENNERSTAL MATTIAS , CHENG AIPING
IPC分类号： A61P3/06 , A61P5/24 , A61P13/00

17. 发明专利

HRP20150864T1 NOVI RECEPTORSKI LIGANDI ESTROGENA 未知
公开(公告)号：HRP20150864T1
公开(公告)日：2015-09-25
申请号：HRP20150864
申请日：2015-08-12
申请人： KAROBIO AB
发明人： RHÖNNSTAD PATRIK , KALLIN ELISABET , APELQVIST THERESA , WENNERSTAL MATTIAS , CHENG AIPING
IPC分类号： C07D209/08 , A61K31/404 , A61P3/06 , A61P5/24 , A61P13/00 , C07D209/12 , C07D209/22 , C07D209/36 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14

18. 发明专利

IN2555DEN2012A "ESTROGEN RECEPTOR LIGANDS" 未知
公开(公告)号：IN2555DEN2012A
公开(公告)日：2015-08-28
申请号：IN2555DEN2012
申请日：2012-03-23
申请人： KAROBIO AB
发明人： WENNERSTAL MATTIAS , RHONNSTAD PATRIK , CHENG AIPING , GORDON SANDRA , APELQVIST THERESA , HAGBERG LARS
IPC分类号： C07D207/32
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined in the specification.

19. 发明专利

ES2543599T3 Nuevos ligandos de receptor de estrógeno 未知
公开(公告)号：ES2543599T3
公开(公告)日：2015-08-20
申请号：ES09731606
申请日：2009-04-16
申请人： KAROBIO AB
发明人： RHÖNNSTAD PATRIK , KALLIN ELISABET , APELQVIST THERESA , WENNERSTÅL MATTIAS , CHENG AIPING
IPC分类号： C07D209/08 , A61K31/404 , A61P3/06 , A61P5/24 , A61P13/00 , C07D209/12 , C07D209/22 , C07D209/36 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14
摘要： Un compuesto de fórmula (I) o un éster, amida, carbamato, solvato o sal farmacéuticamente aceptable del mismo, incluyendo una sal de tal éster, amida o carbamato, y un solvato de tal éster, amida, carbamato o sal,**Fórmula** en la que R1 es seleccionado entre el grupo que consiste en halógeno, ciano, nitro, ORA, N(RB)2, -C(O)alquilo C1-4, - SO2alquilo C1-4, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6, trihaloalquilo C1-6, haloalquenilo C2-6, dihaloalquenilo C2-6, trihaloalquenilo C2-6, cianoalquilo C1-6, alcoxi C1-4-alquilo C1-6, cicloalquilo C3- 8, cicloalquil C3-8-alquilo C1-6, fenilo, bencilo, y heterociclilo de 5-10 miembros, en el que dicho grupo fenilo, bencilo o heterociclilo puede estar sin sustituir o sustituido con 1 a 3 sustituyentes, estando cada sustituyente seleccionado entre el grupo que consiste en ORA, halógeno, ciano, nitro, -C(O)alquilo C1-4, alquilo C1-6, alquenilo C2-6, alquinilo C2- 6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1-6; R2 es seleccionado entre el grupo que consiste en halógeno, ciano, nitro, ORA, N(RB)2, N(OH)2, -C(O)alquilo C1-4 opcionalmente sustituido con 1 a 3 halógenos, -SO2alquilo C1-4, -C(O)NH-OH, -C(NH2)>=N-OH, -C(CO2H)>=N-OH, - C(NH2)>=NH, -C(NHalquilo C1-4)>=NH, -C(O-alquilo C1-4)>=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, alquilo C1-6, haloalquilo C1-6, dihaloalquilo C1-6, trihaloalquilo C1-6, cianoalquilo C1-6, alcoxi C1-4-alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-6, fenilo, bencilo y heterociclilo de 5-10 miembros en la que dicho grupo fenilo, bencilo o heterociclilo puede estar sin sustituir o sustituido con 1 a 3 sustituyentes, estando cada sustituyente seleccionado entre el grupo que consiste en ORA, halógeno, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1-6; con la condición de que si uno de R1 y R2 representa halógeno, el otro debe representar un grupo distinto de halógeno; cada uno de R3, R4, R5 y R6 es seleccionado independientemente entre el grupo que consiste en hidrógeno, ORA, halógeno, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1- 6; cada RA es seleccionado independientemente entre el grupo que consiste en hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-6, arilo C6-10 y aril C6-10-alquilo C1-6, cada uno opcionalmente sustituido con 1 a 3 átomos de halógeno; y cada RB es seleccionado independientemente entre el grupo que consiste en hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-6, arilo C6-10 y aril C6-10-alquilo C1-6, cada uno opcionalmente sustituido con 1 a 3 átomos de halógeno; con la condición de que el compuesto de fórmula (I) no sea 4-[3-(4,5-Dihidro-1H-imidazol-2-il)-2-(3,5-dimetil-isoxazol- 4-il)-indol-1-il]-fenol; 1-(4-Hidroxi-fenil)-2-(4-metil-imidazol-1-il)-1H-indolo-3-carbonitrilo; 1-(4-Hidroxi-fenil)-2-(1Hpirazol- 3-il)-1H-indolo-3-carbonitrilo; 1-(3-Cloro-4-hidroxi-fenil)-2-(1-metil-1H-pirazol-4-il)-1H-indolo-3-carbonitrilo; amida del ácido 1-(4-Hidroxi-fenil)-2-prop-1-inil-1H-indolo-3-carboxílico; o ácido 1-(4-Hidroxi-fenil)-2-tiazol-2-il-1H35 indolo-3-carboxílico.

20. 发明专利

NZ620935A Novel estrogen receptor ligands 未知
公开(公告)号：NZ620935A
公开(公告)日：2015-06-26
申请号：NZ62093512
申请日：2012-08-02
申请人： KAROBIO AB
发明人： CHENG AIPING , GARG NEERAJ , KRÜGER LARS , LÖFSTEDT JOAKIM , KOCH EVA , KOEHLER KONRAD , HAGBERG LARS , NÖTEBERG DANIEL
IPC分类号： C07D213/58 , C07D215/12 , C07D217/14 , C07D231/12 , C07D233/64 , C07D235/16 , C07D261/08 , C07D277/30 , C07D277/34 , C07D307/54 , C07D307/68 , C07D307/87 , C07D317/60 , C07D333/20 , C07D409/10
摘要： Disclosed are biphenyl and terphenyl compounds of formula (I), wherein the substituents are as defined in the specification. Also disclosed is the use of compounds of formula (I) for treating as estrogen receptor ligands that are preferably selective for the estrogen receptor &bgr; isoform. The compounds are useful for the treatment of diseases related to the estrogen receptor such as depressive disorders, anxiety disorders, Alzheimer’s disease, cognitive disorders, osteoporosis, elevated blood triglyceride levels, atherosclerosis, endometriosis, urinary incontinence, autoimmune disease, and cancer of the lung, colon, breast, uterus and prostate. Examples of a compound of formula (I) are: 2-(3 ,5-dimethylisoxazol-4-yl)-N’,4’-dihydroxy-5-methyl-[1,1’-biphenyl]-3 -carboximidamide 2”-ethyl-N’,4-dihydroxy-5’-propyl-[1,1’:2’,1”-terphenyl]-3’-carboximidamide 2-(2,4-dimethylfuran-3-yl)-4’-hydroxy-5-propyl-[1,1’-biphenyl]-3-carbonitrile

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