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1. 发明授权

EP1255738B1 GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 有权
标题翻译：促性腺激素释放激素受体拮抗剂和相关程序
公开(公告)号：EP1255738B1
公开(公告)日：2012-03-07
申请号：EP01910362.1
申请日：2001-01-25
申请人： NEUROCRINE BIOSCIENCES, INC.
发明人： ZHU, Yun-Fei , CHEN, Chen , TUCCI, Fabio, C. , GUO, Zhiqiang , GROSS, Timothy, D. , ROWBOTTOM, Martin , STRUTHERS, R., Scott
IPC分类号： C07D239/54 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D491/08 , C07D513/04
CPC分类号： C07D239/54 , A61K31/513 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/08 , C07D498/08 , C07D513/04
摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure of formula (I) wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

2. 发明公开

EP0977737A1 CRF ANTAGONISTIC QUINO- AND QUINAZOLINES 失效
标题翻译：喹啉和喹唑啉衍生物作为CRF拮抗剂
公开(公告)号：EP0977737A1
公开(公告)日：2000-02-09
申请号：EP98924134.4
申请日：1998-04-15
申请人： JANSSEN PHARMACEUTICA N.V. , Neurocrine Biosciences, Inc.
发明人： HUANG, Charles , WILCOXEN, Keith M. , CHEN, Chen , HADDACH, Mustapha , McCARTHY, James R.
IPC分类号： C07D215/42 , C07D215/36 , C07D215/22 , C07D215/12 , C07D401/04 , A61K31/47 , A61K31/495
CPC分类号： C07D215/233 , C07D215/12 , C07D215/36 , C07D215/42 , C07D239/94 , C07D401/04
摘要： This invention concerns compounds of formula (I), including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C¿1-6?alkyl, NR?6R7, OR6 or SR7; R2¿ is hydrogen, C¿1-6?alkyl, C1-6alkyloxy or C1-6alkylthio; R?3 is Ar1 or Het1; R4 and R5¿ are each independently selected from hydrogen, halo, C¿1-6?alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R?6¿ is hydrogen, C¿1-6?alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R?7¿ is hydrogen, C¿1-8?alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R?6¿ is C¿1-8?alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar?2CH¿2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R?6 and R7¿ taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group, optionally substituted with C¿1-6?alkyl or C1-6alkyloxyC1-6alkyl; and Ar?1 and Ar2¿ are each optionally substituted phenyl; and Het1 is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

3. 发明公开

EP0882051A1 THIOPHENOPYRIMIDINES 失效
公开(公告)号：EP0882051A1
公开(公告)日：1998-12-09
申请号：EP97904368.0
申请日：1997-01-30
申请人： JANSSEN PHARMACEUTICA N.V. , NEUROCRINE BIOSCIENCES, INC.
发明人： CHEN, Chen , WEBB, Thomas R. , McCARTHY, James R. , MORAN, Terence J.
IPC分类号： A61P5 , A61P25 , C07D495
CPC分类号： C07D495/04
摘要： This invention concerns compounds of formula (I) including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S, SO or SO2; R?1 is NR4R5 or OR5; R2¿ is C¿1-6?alkyl, C1-6alkyloxy or C1-6alkylthio; R?3¿ is hydrogen, C¿1-6?alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R?4¿ is hydrogen, C¿1-6?alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R?5¿ is C¿1-8?alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar?1CH¿2, C1-6alkyloxy-C1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6 alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of the formula: -Alk-O-CO-Ar?1; or R4 and R5¿ taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; Ar is a phenyl, substituted phenyl, pyridinyl or substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).
摘要翻译：本发明涉及式（I）化合物，包括其立体异构体及其药学上可接受的酸加成盐形式，其中X是S，SO或SO 2; R 1是NR 4 R 5或OR 5; R2是C1-6烷基，C1-6烷氧基或C1-6烷硫基; R 3是氢，C 1-6烷基，C 1-6烷基磺酰基，C 1-6烷基亚砜基或C 1-6烷硫基; （C 3-6环烷基）甲基，C 3-6环烷基，C 3-6链烯基，羟基C 1-6烷基，C 1-6烷基羰氧基C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 6为氢，C 1-6烷基， R 5是C 1-8烷基，单或二（C 3-6环烷基）甲基，Ar 1 CH 2，C 1-6烷氧基-C 1-6烷基，羟基C 1-6烷基，C 3-6链烯基，噻吩基甲基，呋喃基甲基， C1-6烷硫基C1-6烷基，吗啉基，一或二（C1-6烷基）氨基C1-6烷基，二（C1-6烷基）氨基，C1-6烷基羰基C1-6烷基，咪唑基取代的C1-6烷基; 或下式的基团：-Alk-O-CO-Ar 1; 或者R 4和R 5'与它们所连接的氮原子一起可以形成任选取代的吡咯烷基，哌啶基，高哌啶基或吗啉基; Ar是苯基，取代的苯基，吡啶基或取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物通过施用有效量的式（I）化合物治疗与CRF分泌过多相关的疾病如抑郁症，焦虑症，物质滥用的方法。

4. 发明公开

EP2445878A1 NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO 审中-公开
标题翻译：新化合物的药物组合以及任何相关方法
公开(公告)号：EP2445878A1
公开(公告)日：2012-05-02
申请号：EP10728189.1
申请日：2010-06-23
申请人： Boehringer Ingelheim International GmbH , NEUROCRINE BIOSCIENCES, INC.
发明人： DYCK, Brian , TRAN, Joe A. , TAMIYA, Junko , JOVIC, Florence , VICKERS, Troy , CHEN, Chen , HARRIOTT, Nicole , COON, Timothy , ASHWEEK, Neil J.
IPC分类号： C07D211/68 , C07D401/10 , C07D401/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/10 , A61K31/15 , A61P7/12
CPC分类号： C07D211/72 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D495/04
摘要： New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R
1 , R
2 , R
3 , n, p, q, and Ar are as defined herein, including stereoisomers, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.

5. 发明公开

EP1412338A1 1,3,5-TRIAZINE-2,4,6-TRIONES, PREPARATION AND USE AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 有权
标题翻译： 1,3,5-三嗪-2,4,6-三酮，生产和应用促性腺激素释放激素受体的拮抗剂
公开(公告)号：EP1412338A1
公开(公告)日：2004-04-28
申请号：EP02759239.3
申请日：2002-08-02
申请人： Neurocrine Biosciences, Inc.
发明人： GUO, Zhiqiang , WU, Dongpei , CHEN, Chen , TUCCI, Fabio, C. , REGAN, Collin
IPC分类号： C07D251/30 , C07D401/12 , C07D417/04 , C07D417/14 , C07D403/06 , C07D409/06 , C07D401/06 , C07D417/10 , A61P15/08 , A61K31/53
CPC分类号： C07D401/12 , C07D251/34 , C07D403/06 , C07D403/12 , C07D409/06 , C07D417/04 , C07D417/10 , C07D417/14
摘要： GnRH receptor antagonists of formula I are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

6. 发明公开

EP1411941A2 PYRIDINONE AND PYRIDAZINONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡啶酮和哒嗪酮衍生物作为促性腺激素释放激素受体的拮抗剂
公开(公告)号：EP1411941A2
公开(公告)日：2004-04-28
申请号：EP02756905.2
申请日：2002-08-02
申请人： Neurocrine Biosciences, Inc.
发明人： CHEN, Chen , WU, Dongpei , GUO, Zhiqiang , ROWBOTTOM, Martin
IPC分类号： A61K31/4412 , A61K31/50 , C07D213/64 , C07D237/14 , C07D401/12 , A61P5/04
CPC分类号： C07D213/64 , C07D401/12
摘要： GnRH receptor antagonists are disclosed having general formula (I), which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

7. 发明公开

EP2445901A1 NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO 审中-公开
标题翻译：新化合物的药物组合和任何相关程序
公开(公告)号：EP2445901A1
公开(公告)日：2012-05-02
申请号：EP10725783.4
申请日：2010-06-23
申请人： Boehringer Ingelheim International GmbH , NEUROCRINE BIOSCIENCES, INC.
发明人： TRAN, Joe, A. , CHEN, Chen
IPC分类号： C07D401/14 , C07D403/14 , C07D471/04 , A61K31/506 , A61P3/10
CPC分类号： C07D471/04 , C07D401/14 , C07D403/14
摘要： New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X
1 , X
2 , X
3 , X
4 , Y
1 , Y
2 , A, R
1 , R
2 , R
3 , R
4 , m, n, p, and q are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof in a patient in need thereof.

8. 发明公开

EP1646389A1 PYRIMIDINE-2,4-DIONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 有权转让
标题翻译：嘧啶-2,4-二酮衍生物促性腺激素释放激素受体拮抗剂
公开(公告)号：EP1646389A1
公开(公告)日：2006-04-19
申请号：EP04777603.4
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES, INC.
发明人： GUO, Zhiqiang , CHEN, Yongsheng , WU, Dongpei , CHEN, Chen , WADE, Warren , DWIGHT, Wesley, J. , HUANG, Charles, Q. , TUCCI, Fabio, C.
IPC分类号： A61K31/513 , C07D239/54 , C07D401/12 , C07D405/04 , A61P5/02
CPC分类号： C07D239/54 , C07D239/52 , C07D403/12 , C07D405/04
摘要： GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

9. 发明授权

EP1412338B1 1,3,5-TRIAZINE-2,4,6-TRIONES, PREPARATION AND USE AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 有权
标题翻译： 1,3,5-三嗪-2,4,6-三酮，生产和应用促性腺激素释放激素受体的拮抗剂
公开(公告)号：EP1412338B1
公开(公告)日：2006-01-18
申请号：EP02759239.3
申请日：2002-08-02
申请人： NEUROCRINE BIOSCIENCES, INC.
发明人： GUO, Zhiqiang , WU, Dongpei , CHEN, Chen , TUCCI, Fabio, C. , REGAN, Collin
IPC分类号： C07D251/30 , C07D401/12 , C07D417/04 , C07D417/14 , C07D403/06 , C07D409/06 , C07D401/06 , C07D417/10 , A61P15/08 , A61K31/53
CPC分类号： C07D401/12 , C07D251/34 , C07D403/06 , C07D403/12 , C07D409/06 , C07D417/04 , C07D417/10 , C07D417/14
摘要： GnRH receptor antagonists of formula I are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

10. 发明公开

EP1465867A1 LIGANDS OF MELANOCORTIN RECEPTORS AND COMPOSITIONS AND METHODS RELATED THERETO 审中-公开
标题翻译： MELANDOCORTINREZEPTOREN和配体任何相关组合物和方法
公开(公告)号：EP1465867A1
公开(公告)日：2004-10-13
申请号：EP02800985.0
申请日：2002-10-09
申请人： Neurocrine Biosciences, Inc.
发明人： DYCK, Brian, P. , GOODFELLOW, Val , PHILLIPS, Teresa , PARKER, Jessica , ZHANG, Xiaohu , CHEN, Chen , TRAN, Joe, Anh , PONTILLO, Joseph , TUCCI, Fabio, C.
IPC分类号： C07D209/42 , C07D209/44 , C07D211/60 , C07D213/38 , C07D213/81 , C07D213/82 , C07D215/54 , C07D217/26 , C07D277/28 , C07D295/18 , C07D307/68 , C07D333/20 , C07D401/12 , C07D487/08
CPC分类号： C07D213/81 , A61K38/00 , C07D209/42 , C07D209/44 , C07D211/60 , C07D213/38 , C07D213/82 , C07D215/54 , C07D217/26 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/28 , C07D295/185 , C07D307/68 , C07D333/20 , C07D333/24 , C07D333/38 , C07D401/12 , C07D403/12 , C07D405/14 , C07D409/14 , C07D487/08 , C07K5/06139 , C07K5/06191
摘要： Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders, and may be used to treat disorders or illnesses including eiating disorders, cachexia, obesity, diabetes, metabolic disorders, inflammation, pain, skin disorders; skin and hair coloration, male and female sexual dysfuntion, erectile dysfunction, dry eye acne and/or Cushing's disease. The compounds have the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein A, m, n R1, R2, R3a, R3b, R4, R5, R6, W1, W2, W3, W4, Y1, Y2, Y3 and Y4 area defined herin. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.

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