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1. 发明申请

WO2003011293A2 GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 审中-公开
标题翻译：促性腺激素释放激素受体拮抗剂及其相关方法
公开(公告)号：WO2003011293A2
公开(公告)日：2003-02-13
申请号：PCT/US2002/024545
申请日：2002-08-02
申请人： NEUROCRINE BIOSCIENCES, INC. , CHEN, Chen , WU, Dongpei , GUO, Zhiqiang , ROWBOTTOM, Martin
发明人： CHEN, Chen , WU, Dongpei , GUO, Zhiqiang , ROWBOTTOM, Martin
IPC分类号： A61K31/4412
CPC分类号： C07D213/64 , C07D401/12
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. 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.
摘要翻译：公开了具有通式（I）的GnRH受体拮抗剂，其可用于治疗男性和女性中各种性激素相关病症。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

2. 发明申请

WO2003011839A1 1,3,5-TRIAZINE-2,4,6-TRIONES, PREPARATION AND USE AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 1,3,5-三嗪-2,4,6-TRIONES，制备和用作GONADOTROPIN-RELEASING HORMONE受体拮抗剂
公开(公告)号：WO2003011839A1
公开(公告)日：2003-02-13
申请号：PCT/US2002/024451
申请日：2002-08-01
申请人： NEUROCRINE BIOSCIENCES, INC. , GUO, Zhiqiang , WU, Dongpei , CHEN, Chen , TUCCI, Fabio, C. , REGAN, Collin
发明人： GUO, Zhiqiang , WU, Dongpei , CHEN, Chen , TUCCI, Fabio, C. , REGAN, Collin
IPC分类号： C07D251/30
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.
摘要翻译：公开了具有用于治疗男性和女性中各种性激素相关病症的功能的式I的GnRH受体拮抗剂。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

3. 发明申请

WO2005007165A1 PYRIMIDINE-2, 4-DIONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：哌嗪-2,4-二酮衍生物作为GONADOTROPIN-RELEASING HORMONE受体拮抗剂
公开(公告)号：WO2005007165A1
公开(公告)日：2005-01-27
申请号：PCT/US2004/021593
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES, INC. , GUO, Zhiqiang , CHEN, Yongsheng , WU, Dongpei , CHEN, Chen , WADE, Warren , DWIGHT, Wesley, J. , HUANG, Charles, Q. , TUCCI, Fabio, C.
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
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 R 1a , R 1b , R 1c , R 2a , R 2b , R 3 , R 4 , R 5 , R 6 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.
摘要翻译：公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。本发明的化合物具有以下结构：其中R1a，R1b，R1c，R2a，R2b，R3，R4，R5，R6和X如本文所定义，包括其立体异构体，前药和药学上可接受的盐。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

4. 发明申请

WO2005007633A1 GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 审中-公开
标题翻译：促性腺激素释放激素受体拮抗剂及其相关方法
公开(公告)号：WO2005007633A1
公开(公告)日：2005-01-27
申请号：PCT/US2004/021568
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES, INC. , HUANG, Charles, Q. , CHEN, Chen , CHEN, Yongsheng , GUO, Zhiqiang , WADE, Warren , ROWBOTTOM, Martin , RUETER, Jaimie, K.
发明人： HUANG, Charles, Q. , CHEN, Chen , CHEN, Yongsheng , GUO, Zhiqiang , WADE, Warren , ROWBOTTOM, Martin , RUETER, Jaimie, K.
IPC分类号： C07D239/54
CPC分类号： C07D239/54 , C07D403/12
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 n, R 1a , R 1b , R 1c , R 2a , R 2b , R 3 , R 4 , R 5 , R 6 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.
摘要翻译：公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。本发明的化合物具有以下结构：其中n，R1a，R1b，R1c，R2a，R2b，R3，R4，R5，R6和X如本文所定义，包括其立体异构体，前药和药学上可接受的盐。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

5. 发明申请

WO2005040109A1 LIGANDS OF MELANOCORTIN RECEPTORS AND COMPOSITIONS AND METHODS RELATED THERETO 审中-公开
标题翻译： MELANOCORTIN受体的配体及其组合物及其相关方法
公开(公告)号：WO2005040109A1
公开(公告)日：2005-05-06
申请号：PCT/US2004/035343
申请日：2004-10-22
申请人： NEUROCRINE BIOSCIENCES, INC. , CHEN, Chen , TRAN, Joe, Ahn , TUCCI, Fabio, C. , CHEN, Wei-Chuan, C., , JIANG, Wanlong , MARINKOVIC, Dragan , ARELLANO, Melissa , WHITE, Nicole
发明人： CHEN, Chen , TRAN, Joe, Ahn , TUCCI, Fabio, C. , CHEN, Wei-Chuan, C., , JIANG, Wanlong , MARINKOVIC, Dragan , ARELLANO, Melissa , WHITE, Nicole
IPC分类号： C07D207/16
CPC分类号： C04B35/632 , C07D207/16 , C07D207/277 , C07D263/24 , C07D295/185 , C07D307/24 , C07D307/33 , C07D317/32 , C07D333/38 , C07D333/48 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12
摘要： Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): (R 4 ) s (R 2 ) n N~ X 1 -X 2 (CR 1a CR lb ) q 1~ N R 1 -lm 1 O R 3 (I) including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein m, n, q, s, R 1 , R 1a , R 1b , R 2 , R 3 , R 4 , X 1 X 2 and X 3 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
摘要翻译：作为黑皮质素受体配体起作用并可用于治疗基于黑皮质素受体的疾病的化合物。该化合物具有以下结构（I）：（R4）s（R 2）n N〜X1-X2（CR1aCRlb）q 1〜N R1-lm 1 O R3（I），包括其立体异构体，前药和药学上可接受的盐其中m，n，q，s，R1，R1a，R1b，R2，R3，R4，X1 X2和X3如本文所定义。还公开了含有结构（I）化合物的药物组合物以及与其用途有关的方法。

6. 发明申请

WO2003094918A1 SUBSTITUTED PIPERAZINE AS MELANOCORTIN RECEPTORS LIGANDS 审中-公开
标题翻译：替代哌嗪作为MELANOCORTIN受体配体
公开(公告)号：WO2003094918A1
公开(公告)日：2003-11-20
申请号：PCT/US2003/014628
申请日：2003-05-09
申请人： NEUROCRINE BIOSCIENCES, INC. , PONTILLO, Joseph , MARINKOVIC, Dragan , LANIER, Marion, C. , TRAN, Joe, Ahn , ARELLANO, Melissa , PARKER, Jessica , NELSON, Jodie , CHEN, Chen , CHEN, Caroline , JIANG, Wanglong , WHITE, Nicole , TUCCI, Fabio, C.
发明人： PONTILLO, Joseph , MARINKOVIC, Dragan , LANIER, Marion, C. , TRAN, Joe, Ahn , ARELLANO, Melissa , PARKER, Jessica , NELSON, Jodie , CHEN, Chen , CHEN, Caroline , JIANG, Wanglong , WHITE, Nicole , TUCCI, Fabio, C.
IPC分类号： A61K31/496
CPC分类号： C07D207/27 , C07D207/14 , C07D207/16 , C07D207/273 , C07D207/335 , C07D211/14 , C07D211/26 , C07D211/28 , C07D211/58 , C07D211/60 , C07D211/62 , C07D213/38 , C07D213/74 , C07D217/26 , C07D223/04 , C07D233/36 , C07D241/08 , C07D265/30 , C07D277/28 , C07D295/185 , C07D295/215 , C07D307/14 , C07D307/52 , C07D317/58 , C07D333/20 , C07D333/22 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14
摘要： Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein Ar, R 1 , R 2 , R 3a , R 3b , R 4a , R 4b , R 5 , R 7a , R 7b , q , r , X, Y 1 , Y 2 , Y 3 and Y 4 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
摘要翻译：作为黑皮质素受体配体起作用并可用于治疗基于黑皮质素受体的疾病的化合物。其中Ar，R 1，R 2，R 3a，R 3b，R 4a，R 4b，R 5，R 7a，R 7b，q，r，X，Y 1， Y2，Y3和Y4如本文所定义。还公开了含有结构（I）化合物的药物组合物以及与其用途有关的方法。

7. 发明申请

WO2003013528A1 SUBSTITUTED PYRIDIN-4-ONES AND THEIR USE AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS. 审中-公开
标题翻译：取代的吡啶-4-酮及其作为促性腺激素释放激素受体拮抗剂的用途。
公开(公告)号：WO2003013528A1
公开(公告)日：2003-02-20
申请号：PCT/US2002/024643
申请日：2002-08-02
申请人： NEUROCRINE BIOSCIENCES, INC. , TUCCI, Fabio, C. , CONNORS, Patrick, J. , ZHU, Yun-Fei , CHEN, Chen
发明人： TUCCI, Fabio, C. , CONNORS, Patrick, J. , ZHU, Yun-Fei , CHEN, Chen
IPC分类号： A61K31/45
CPC分类号： C07D213/69 , C07D211/86 , C07D213/68 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/04 , C07D409/14 , C07D453/02 , C07D453/06 , C07D473/24
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, including stereosomers, prodrugs and pharmaceutically acceptable salts thereof, wherein: A is O or a bond; n is 1, 2, 3 or 4; R 1 and R 2 are the same or different and independently hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycle, substituted heterocycle, heterocyclealkyl, susbstituted heterocyclealkyl, -C(R 8 )(=NR 9 ) or -C(NR 10 R 11 )(=NR 9 ); or R 1 and R 2 taken together with the nitrogen atom to which they are attached form a heterocycle or a substituted heterocycle; R 3a and R 3b are the same or different and, at each occurrence, independently hydrogen, alkyl, substituted alkyl, alkoxy, alkylthio, alkylamino, aryl, substituted aryl, arylakyl, substituted arylalkyl, heterocycle, substituted heterocycle, heterocyclealkyl, substituted heterocyclealkyl, -COOR 12 or -CONR 10 R 11 ; or R 3ab and R 3b taken together with the carbon atom to which they are attached form a homocycle, substituted homocycle, heterocycle or substituted heterocycle; or R 3a and the carbon to which it is attached taken together with R 1 and the nitrogen to which it is attached form a heterocycle or substituted heterocycle; R 4 is hydrogen, alkyl or substituted alkyl; R 5 is arylalkyl, substituted arylalkyl, heteroarylalkyl or substituted heteroalalkyl; R 6 is aryl, substituted aryl, heteroaryl or substituted heteroaryl; R 7 is hydrogen, alkyl or substituted alkyl; R 8 , R 9 , R 10 and R 11 are the same or different and, at each occurrence, independently hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycle, substituted heterocycle, heterocyclealkyl or substituted heterocyclealkyl, and R 12 is hydrogen, alkyl or substituted alkyl.
摘要翻译：公开了式（I）的GnRH受体拮抗剂，其可用于治疗男性和女性中各种性激素相关病症。还公开了含有本发明化合物与药学上可接受的载体的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的用途的方法，包括立体异构体，前药和药学上可接受的盐，其中：A为O或键; n为1,2,3或4; R 1和R 2相同或不同，并且独立地是氢，烷基，取代的烷基，芳基，取代的芳基，芳基烷基，取代的芳基烷基，杂环，取代的杂环，杂环烷基，取代的杂环烷基，-C（R 8）（= NR 9） NR 10 R 11）（= NR 9）; 或者R 1和R 2与它们所连接的氮原子一起形成杂环或取代的杂环; R3a和R3b相同或不同，并且在每次出现时独立地为氢，烷基，取代的烷基，烷氧基，烷硫基，烷基氨基，芳基，取代的芳基，芳基烷基，取代的芳基烷基，杂环，取代的杂环，杂环烷基，取代的杂环烷基，-COOR12 或-CONR10R11; 或者R3ab和R3b与它们所连接的碳原子一起形成同质环，取代的杂环，杂环或取代的杂环; 或R 3a，并且其连接的碳与R 1一起并且与其连接的氮形成杂环或取代的杂环; R4是氢，烷基或取代的烷基; R5是芳基烷基，取代的芳基烷基，杂芳基烷基或取代的杂芳烷基; R6是芳基，取代的芳基，杂芳基或取代的杂芳基; R7是氢，烷基或取代的烷基; R8，R9，R10和R11相同或不同，并且在每次出现时独立地为氢，烷基，取代的烷基，芳基，取代的芳基，芳基烷基，取代的芳基烷基，杂环，取代的杂环，杂环烷基或取代的杂环烷基，R12为氢，烷基或取代的烷基。

8. 发明申请

WO2010149685A1 NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO 审中-公开
标题翻译：新化合物，药物组合物及其相关方法
公开(公告)号：WO2010149685A1
公开(公告)日：2010-12-29
申请号：PCT/EP2010/058874
申请日：2010-06-23
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , NEUROCRINE BIOSCIENCES, INC. , TRAN, Joe, A. , CHEN, Chen
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.
摘要翻译：公开了可用于治疗患者中各种代谢相关病症的新化合物。本发明的化合物具有结构（I）：其中X1，X2，X3，X4，Y1，Y2，A，R1，R2，R3，R4，m，n，p和q如本文所定义，包括立体异构体，酯，溶剂化物和药学上可接受的盐。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及与其在有需要的患者中的用途有关的方法。

9. 发明申请

WO2003011870A1 GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：促性腺激素释放激素受体拮抗剂
公开(公告)号：WO2003011870A1
公开(公告)日：2003-02-13
申请号：PCT/US2002/024493
申请日：2002-08-02
申请人： NEUROCRINE BIOSCIENCES, INC. , PONTILLO, Joseph , CHEN, Chen
发明人： PONTILLO, Joseph , CHEN, Chen
IPC分类号： C07D498/04
CPC分类号： 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. 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.
摘要翻译：公开了GnRH受体拮抗剂，其可用于治疗男性和女性中各种性激素相关病症。还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

10. 发明申请

WO2010149684A1 NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO 审中-公开
标题翻译：新化合物，药物组合物及其相关方法
公开(公告)号：WO2010149684A1
公开(公告)日：2010-12-29
申请号：PCT/EP2010/058873
申请日：2010-06-23
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , NEUROCRINE BIOSCIENCES, INC. , DYCK, Brian , TRAN, Joe A. , TAMIYA, Junko , JOVIC, Florence , VICKERS, Troy , CHEN, Chen , HARRIOTT, Nicole , COON, Timothy , ASHWEEK, Neil J.
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.
摘要翻译：公开了可用于治疗患者中各种代谢相关病症的新化合物。本发明的化合物具有结构（I）：其中R 1，R 2，R 3，n，p，q和Ar如本文所定义，包括其立体异构体，溶剂化物和药学上可接受的盐。还公开了包含本发明化合物的药物组合物以及与其在有需要的患者中的用途有关的方法。

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