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1. 发明专利

CA2386942A1 GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 未知
公开(公告)号：CA2386942A1
公开(公告)日：2001-04-26
申请号：CA2386942
申请日：2000-10-16
申请人： NEUROCRINE BIOSCIENCES INC
发明人： CHEN CHEN , GAO YINGHONG , GROSS TIMOTHY D , CONNORS PATRICK J JR , ZHU YUN-FEI , GUO ZHIQIANG
IPC分类号： C07D471/04 , A61K31/519 , A61P1/00 , A61P5/02 , A61P5/04 , A61P15/00 , A61P17/00 , A61P35/00 , A61P43/00 , C07D487/04 , A61K31/505
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 structure (I): wherein Ar, A, B, Q, R1, R2, R3a, R3b, R6, R7 and m are as defined herein, including stereoisomers, prodrugs and pharmaceutical 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. 发明申请

WO2006133339A3 MONOAMINE RE-UPTAKE INHIBITORS AND METHODS RELATING THERETO 审中-公开
标题翻译：单体重新吸收抑制剂及其相关方法
公开(公告)号：WO2006133339A3
公开(公告)日：2007-03-22
申请号：PCT/US2006022227
申请日：2006-06-07
申请人： NEUROCRINE BIOSCIENCES INC , PONTILLO JOSEPH , GAO YINGHONG , WADE WARREN S , WU DONGPEI , ECCLES WENDY K
发明人： PONTILLO JOSEPH , GAO YINGHONG , WADE WARREN S , WU DONGPEI , ECCLES WENDY K
IPC分类号： C07C323/32 , A61K31/138 , A61K31/353 , A61K31/5386 , A61P25/00 , C07C215/42 , C07C217/74 , C07D265/34 , C07D311/22 , C07D317/64 , C07D333/54
CPC分类号： C07C215/42 , C07C217/74 , C07C323/32 , C07C2602/08 , C07D265/34 , C07D317/64 , C07D333/54
摘要： Monoamine re-uptake inhibitors and more specifically serotonin and noradrenaline re-uptake inhibitors are disclosed that have utility in the treatment of disorders of the central or peripheral nervous system in both men and women. The compounds of this invention have the structure (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , m, n, W, X, Y, and Z are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts, esters and solvates 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 inhibiting monoamine re-uptake in a subject in need thereof.
摘要翻译：公开了单胺再吸收抑制剂，更具体地说，可用于治疗男性和女性中枢性或周围神经系统疾病的5-羟色胺和去甲肾上腺素再摄取抑制剂。本发明的化合物具有结构（I），其中R 1，R 2，R 3，R 4， R 5，R 6，m，n，W，X，Y和Z如本文所定义，包括立体异构体，前药和药学上可接受的盐，酯和溶剂化物。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抑制单胺再摄取的方法。

3. 发明专利

AU4845700A Imidazo- and pyrrolo(1,2-a)pyrimid-4-ones as gonadotropin-releasing hormone receptor antagonists 未知
公开(公告)号：AU4845700A
公开(公告)日：2000-12-05
申请号：AU4845700
申请日：2000-05-12
申请人： NEUROCRINE BIOSCIENCES INC
发明人： ZHU YUN-FEI , WILCOXEN KEITH M , STRUTHERS R SCOTT , CHEN CHEN , CONNORS PATRICK JR , GAO YINGHONG , TUCCI FABIO C
IPC分类号： A61K31/519 , A61P1/00 , A61P13/08 , A61P15/00 , A61P15/02 , A61P15/12 , A61P17/00 , A61P25/20 , A61P35/00 , A61P37/02 , C07D487/04 , A61K31/505
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 structure (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein Ar, B, R1, R2, R3a, R3b, R4, R5, R6 and m are as defined herein.

4. 发明专利

DE60022769T2 未知
公开(公告)号：DE60022769T2
公开(公告)日：2006-07-06
申请号：DE60022769
申请日：2000-10-16
申请人： NEUROCRINE BIOSCIENCES INC
发明人： ZHU YUN-FEI , GROSS D , GAO YINGHONG , CONNORS J , GUO ZHIQIANG , CHEN CHEN
IPC分类号： C07D471/04 , C07D487/04 , A61K31/505 , A61K31/519 , A61P1/00 , A61P5/02 , A61P5/04 , A61P15/00 , A61P17/00 , A61P35/00 , A61P43/00
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 structure (I): wherein Ar, A, B, Q, R1, R2, R3a, R3b, R6, R7 and m are as defined herein, including stereoisomers, prodrugs and pharmaceutical 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.

5. 发明专利

AT305008T 未知
公开(公告)号：AT305008T
公开(公告)日：2005-10-15
申请号：AT00973591
申请日：2000-10-16
申请人： NEUROCRINE BIOSCIENCES INC
发明人： ZHU YUN-FEI , GROSS TIMOTHY D , GAO YINGHONG , CONNORS PATRICK J JR , GUO ZHIQIANG , CHEN CHEN
IPC分类号： C07D471/04 , A61K31/519 , A61P1/00 , A61P5/02 , A61P5/04 , A61P15/00 , A61P17/00 , A61P35/00 , A61P43/00 , C07D487/04 , A61K31/505
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 structure (I): wherein Ar, A, B, Q, R1, R2, R3a, R3b, R6, R7 and m are as defined herein, including stereoisomers, prodrugs and pharmaceutical 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.

6. 发明专利

NZ515460A Imidazo- and pyrrolo[1,2-A]pyrimid-4-ones as gonadotropin-releasing hormone receptor antagonists 未知
公开(公告)号：NZ515460A
公开(公告)日：2004-06-25
申请号：NZ51546000
申请日：2000-05-12
申请人： NEUROCRINE BIOSCIENCES INC
发明人： ZHU YUN-FEI , WILCOXEN KEITH M , STRUTHERS R SCOTT , CHEN CHEN , CONNORS PATRICK , GAO YINGHONG , TUCCI FABIO C
IPC分类号： A61K31/519 , A61P1/00 , A61P13/08 , A61P15/00 , A61P15/02 , A61P15/12 , A61P17/00 , A61P25/20 , A61P35/00 , A61P37/02 , C07D487/04 , A61K31/505
摘要： Gonadotrophin releasing hormone (GnRH) receptor antagonists of formula (I) wherein: m is an integer from 1 to 6; R1 is H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, aryl(CR3cR3d)n, substituted aryl(CR3cR3d)n, heteroaryl(CR3cR3d)n or substituted heteroaryl(CR3cR3d)n; R2 is H, alkyl or substituted alkyl; or R1 and R2 together with the N atom to which they are attached form a heterocycle ring or a substituted heterocycle ring; R3a, R3b, R3c and R3d are the same or different and independently H, alkyl, substituted alkyl, hydroxy, alkoxy, thioalkyl, amino, alkylamino, dialkylamino, cyano, halogen, -C(=O)OR7 or -C(=O)NR7R8; or R3a-3d together with the C atom to which they are attached form a carbocyclic ring or substituted carbocyclic ring; or R3a and R1 taken together with the C and N atom respectively to which they are attached form a heterocyclic ring or substituted heterocyclic ring; R4 is H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituterd arylalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl or substituted heteroarylalkyl; R5 is H, halogen, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, thioalkyl, or mono- or di-alkylamine; R6 is H, alkyl, substituted alkyl, aryl, substituted aryl, hetercycle, substituted heterocycle, -OR7, -SR7, -SOR7, -SO2R7, -OSO2R7, -SO2OR7, -SO2NR7R8, -NR9SO2R7, -C(=O0R7, -C(=O)OR7, -OC(=O)R7, -NR7R8 -C(=O)NR7R8, -OC(=O)NR7R8, -NR9C(=O)R7, -NR9C(=O)NR7R8, NR8C(=O)NR7 or -C(OH)R7R8; B and Ar are: B is N or CR10 when Ar is heteroaryl or substituted heteroaryl and R10 is H; or B is CR10 when Ar is aryl, substituted aryl, heteroaryl, or substituted heteroaryl and R10 is halogen, cyano, nitro, amino, mono- or di- alkylamino or alkyl. Also covered is the use of said compounds in the preparation of medicaments for the treatment of a sex-hormone related condition, wherein said condition is cancer, benign prostatic hypertrophy or myoma of the uterus.

7. 发明专利

HK1047437A1 Gonadotropin releasing hormone receptor antagonists and their related methods of use. 未知
公开(公告)号：HK1047437A1
公开(公告)日：2003-02-21
申请号：HK02109095
申请日：2002-12-16
申请人： NEUROCRINE BIOSCIENCES INC
发明人： ZHU YUN-FEI , GROSS TIMOTHY D , GAO YINGHONG , CONNORS PATRICK J JR , GUO ZHIQIANG , CHEN CHEN
IPC分类号： C07D471/04 , A61K31/519 , A61P1/00 , A61P5/02 , A61P5/04 , A61P15/00 , A61P17/00 , A61P35/00 , A61P43/00 , C07D487/04 , C07D , A61K , A61P
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 structure (I): wherein Ar, A, B, Q, R1, R2, R3a, R3b, R6, R7 and m are as defined herein, including stereoisomers, prodrugs and pharmaceutical 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.

8. 发明专利

AU1208901A Gonadotropin-releasing hormone receptor antagonists and methods relating thereto 未知
公开(公告)号：AU1208901A
公开(公告)日：2001-04-30
申请号：AU1208901
申请日：2000-10-16
申请人： NEUROCRINE BIOSCIENCES INC
发明人： ZHU YUN-FEI , GROSS TIMOTHY D , GAO YINGHONG , CONNORS PATRICK J JR , GUO ZHIQIANG , CHEN CHEN
IPC分类号： C07D471/04 , A61K31/519 , A61P1/00 , A61P5/02 , A61P5/04 , A61P15/00 , A61P17/00 , A61P35/00 , A61P43/00 , C07D487/04 , A61K31/505
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 structure (I): wherein Ar, A, B, Q, R1, R2, R3a, R3b, R6, R7 and m are as defined herein, including stereoisomers, prodrugs and pharmaceutical 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. 发明专利

ES2249302T3 ANTAGONISTAS DEL RECEPTOR DE LA HORMONA LIBERADORA DE GONADOTROPINA Y SUS METODOS DE USO RELACIONADOS. 未知
公开(公告)号：ES2249302T3
公开(公告)日：2006-04-01
申请号：ES00973591
申请日：2000-10-16
申请人： NEUROCRINE BIOSCIENCES INC
发明人： ZHU YUN-FEI , GROSS TIMOTHY D , GAO YINGHONG , CONNORS PATRICK J JR , GUO ZHIQIANG , CHEN CHEN
IPC分类号： C07D471/04 , A61K31/519 , A61P1/00 , A61P5/02 , A61P5/04 , A61P15/00 , A61P17/00 , A61P35/00 , A61P43/00 , C07D487/04 , A61K31/505
摘要： Un compuesto y sus estereoisómeros y sus sales farmacéuticamente aceptables, donde: A se selecciona independientemente entre N o CR4; B se selecciona independientemente entre N o CR5; Q es un enlace directo o -(CR8aR8b)r-Z-(CR10aR10b)s-; m, r y s son iguales o diferentes y se seleccionan de un número entero de 0 a 6; Z es un enlace directo o -O-, -S-, ¿NR9-, -SO-, -SO2-, - OSO2-, -SO2O-, -SO2NR9-, -NR9SO2-, -CO-, -COO-, -OCO-, - CONR9-, -NR9CO-, -NR9CONR9a, -OCONR9- o -NR9COO-; R1 es hidrógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, -C(R1a(=NR1b), o - C(NR1aR1c)(=NR1b); R2 es hidrógeno, alquilo o alquilo sustituido; o R1 y R2 considerados junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico o un anillo heterocíclico sustituido; R3a y R3b se seleccionan independientemente entre hidrógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, heterociclo, heterocicloalquilo, hidroxi, alcoxi, alquiltio, alquilamino, CONR14R15, o - COOR14; o R3a y R3b considerados junto con el átomo de carbono al que están unidos forman un anillo homocíclico de 3-6 miembros, un anillo homocíclico sustituido, un anillo heterocíclico o un anillo heterocíclico sustituido; o R3a y R3b considerados juntos forman =NR3c.

10. 发明专利

DE60022769D1 未知
公开(公告)号：DE60022769D1
公开(公告)日：2006-02-02
申请号：DE60022769
申请日：2000-10-16
申请人： NEUROCRINE BIOSCIENCES INC
发明人： ZHU YUN-FEI , GROSS D , GAO YINGHONG , CONNORS J , GUO ZHIQIANG , CHEN CHEN
IPC分类号： C07D471/04 , A61K31/505 , A61K31/519 , A61P1/00 , A61P5/02 , A61P5/04 , A61P15/00 , A61P17/00 , A61P35/00 , A61P43/00 , C07D487/04
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 structure (I): wherein Ar, A, B, Q, R1, R2, R3a, R3b, R6, R7 and m are as defined herein, including stereoisomers, prodrugs and pharmaceutical 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.

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