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1. 发明申请

WO03011293A3 PYRIDINONE AND PYRIDAZINONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯烷酮和吡咯烷酮衍生物作为促性腺激素释放激素受体拮抗剂
公开(公告)号：WO03011293A3
公开(公告)日：2003-04-17
申请号：PCT/US0224545
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： A61K31/44 , A61K31/4418 , A61K31/50 , A61K31/501 , A61P1/04 , A61P5/04 , A61P5/24 , A61P13/08 , A61P15/00 , A61P15/08 , A61P25/20 , A61P35/00 , A61P37/02 , C07D213/64 , C07D401/12 , A61K31/4412 , C07D237/14
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.
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

WO0155119A3 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：WO0155119A3
公开(公告)日：2002-02-14
申请号：PCT/US0102740
申请日：2001-01-25
申请人： NEUROCRINE BIOSCIENCES INC , ZHU YUN FEI , CHEN CHEN , TUCCI FABIO C , GUO ZHIQIANG , GROSS TIMOTHY D , ROWBOTTOM MARTIN , STRUTHERS R SCOTT
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： C07D239/52 , A61K31/513 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61P1/04 , A61P5/24 , A61P13/08 , A61P15/00 , A61P15/18 , A61P25/20 , A61P35/00 , A61P37/06 , C07D239/54 , C07D239/553 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D491/08 , C07D498/18 , C07D513/04 , A61K31/505 , A61P5/04 , C07D239/60 , C07D413/12
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.
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。本发明的化合物具有式（I）的结构，其中A，Q，R 1，R 2，R 3a，R 3b，R 4，R 5，R 6和n如本文所定义，包括立体异构体，前药和其药学上可接受的盐。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。

3. 发明申请

WO0027846A3 CRF RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 审中-公开
标题翻译： CRF受体拮抗剂及其相关方法
公开(公告)号：WO0027846A3
公开(公告)日：2000-11-16
申请号：PCT/US9927054
申请日：1999-11-12
申请人： NEUROCRINE BIOSCIENCES INC , HADDACH MUSTAPHA , NELSON JODIE , DYCK BRIAN P , GUO ZHIQIANG , HUANG CHARLES Q , MCCARTHY JAMES R
发明人： HADDACH MUSTAPHA , NELSON JODIE , DYCK BRIAN P , GUO ZHIQIANG , HUANG CHARLES Q , MCCARTHY JAMES R
IPC分类号： A61K31/4985 , A61K31/551 , A61P5/02 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/24 , C07D471/16 , C07D487/16
CPC分类号： C07D471/16 , C07D487/16
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have structure (I) including stereoisomers and pharmaceutically acceptable salts thereof, wherein n , m , A, B, C, R, R1, R2 and Ar are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
摘要翻译：公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。本发明的CRF受体拮抗剂具有包括立体异构体及其药学上可接受的盐的结构（I），其中n，m，A，B，C，R，R 1，R 2 和Ar如本文所定义。还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

4. 发明申请

WO0027850A2 CRF RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 审中-公开
标题翻译： CRF受体拮抗剂及其相关方法
公开(公告)号：WO0027850A2
公开(公告)日：2000-05-18
申请号：PCT/US9926984
申请日：1999-11-12
申请人： NEUROCRINE BIOSCIENCES INC , HADDACH MUSTAPHA , GUO ZHIQIANG , MCCARTHY JAMES R
发明人： HADDACH MUSTAPHA , GUO ZHIQIANG , MCCARTHY JAMES R
IPC分类号： A61K31/4985 , A61P1/00 , A61P1/14 , A61P3/04 , A61P9/10 , A61P9/12 , A61P25/00 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/30 , A61P29/00 , A61P37/02 , A61P43/00 , C07D471/16 , C07D487/16 , A61K31/551
CPC分类号： C07D471/16 , C07D487/16
摘要： Compounds are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in warmblooded animals, including stroke. The compounds of this invention have structures (I): (a) wherein n, m, R, R1, R2, X and Ar are as defined herein, including stereoisomes and pharmaceutically acceptable salts thereof.
摘要翻译：公开了可用于治疗各种疾病的化合物，包括治疗在温血动物（包括中风）中表现出CRF过度分泌的病症。本发明的化合物具有结构（I）：（a）其中n，m，R，R 1，R 2，X和Ar如本文所定义，包括立体异构体及其药学上可接受的盐。

5. 发明专利

JP2011079857A Gonadotropin-releasing hormone receptor antagonist and method 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：JP2011079857A
公开(公告)日：2011-04-21
申请号：JP2010274139
申请日：2010-12-08
申请人： Neurocrine Biosciences Inc , ニューロクラインバイオサイエンシーズ,インコーポレイテッド
发明人： HUANG CHARLES Q , CHEN CHEN , CHEN YONGSHENG , GUO ZHIQIANG , WADE WARREN , ROWBOTTOM MARTIN , RUETER JAIMIE K
IPC分类号： A61K31/505 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P5/06 , A61P5/24 , A61P13/08 , A61P15/00 , A61P15/08 , A61P17/14 , A61P25/20 , A61P35/00 , A61P43/00 , C07D239/54 , C07D403/06 , C07D403/12
CPC分类号： C07D239/54 , C07D403/12
摘要： PROBLEM TO BE SOLVED: To provide GnRH (gonadotropin-releasing hormone) receptor antagonists that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. SOLUTION: There are provided pharmaceutical compositions containing a compound having a structure of formula (I), stereoisomers, prodrugs or pharmaceutically acceptable salts thereof. In formula (I), n is 0 or 1; and R 1a , R 1b , R 1c , R 2a , R 2b , R 3 , R 4 , R 5 , R 6 and X represent substituents. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供可用于治疗男性和女性各种性激素相关病症的GnRH（促性腺激素释放激素）受体拮抗剂。提供了含有具有式（I）结构的化合物，立体异构体，前药或其药学上可接受的盐的药物组合物。在式（I）中，n为0或1; R＆lt; SB＆gt; 1a＆lt; /＆gt;，R＆lt; SB＆gt; 1b＆lt; / SB＆gt;，R＆lt; SB＆lt; 1＆lt; SB＆gt; R SB 3，R SB 3，R SB 5，SB SB 6，X代表取代基。版权所有（C）2011，JPO＆INPIT

6. 发明专利

JP2011088903A Pyrimidine-2,4-dione derivative as gonadotropin releasing hormone receptor antagonist 审中-公开
标题翻译：哌嗪-2,4-二酮衍生物作为甘油磷酸盐释放激素受体拮抗剂
公开(公告)号：JP2011088903A
公开(公告)日：2011-05-06
申请号：JP2010265832
申请日：2010-11-29
申请人： Neurocrine Biosciences Inc , ニューロクラインバイオサイエンシーズ,インコーポレイテッド
发明人： ZHU YUN-FEI , REGAN COLLIN , RUETER JAIMIE K , GUO ZHIQIANG , CHEN YONGSHENG , HUANG CHARLES Q
IPC分类号： C07D239/54 , A61K31/513 , A61P5/02 , A61P5/24 , A61P13/08 , A61P15/00 , A61P15/08 , A61P25/20 , A61P35/00 , A61P37/02 , A61P43/00 , C07D401/06
CPC分类号： C07D239/54 , C07D401/06
摘要： PROBLEM TO BE SOLVED: To provide a gonadotropin releasing hormone (GnRH) receptor antagonist, a method for preparing the same, a method for using the same, and a pharmaceutical composition containing the compound. SOLUTION: The GnRH receptor antagonist has utility in the treatment of a variety of sex-hormone related conditions in both men and women, and is a compound represented by structural formula (I), or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供促性腺激素释放激素（GnRH）受体拮抗剂，其制备方法，其使用方法和含有该化合物的药物组合物。解决方案：GnRH受体拮抗剂可用于治疗男性和女性各种性激素相关病症，并且是由结构式（I）表示的化合物，或立体异构体，前药或药学上可接受的盐它们。版权所有（C）2011，JPO＆INPIT

7. 发明专利

JP2011088902A Pyrimidine-2,4-dione derivative as gonadotropin releasing hormone receptor antagonist 有权
标题翻译：哌嗪-2,4-二酮衍生物作为甘油磷酸盐释放激素受体拮抗剂
公开(公告)号：JP2011088902A
公开(公告)日：2011-05-06
申请号：JP2010265830
申请日：2010-11-29
申请人： Neurocrine Biosciences Inc , ニューロクラインバイオサイエンシーズ,インコーポレイテッド
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： C07D239/54 , A61K31/513 , A61P1/04 , A61P5/02 , A61P15/00 , A61P15/08 , A61P17/14 , A61P25/20 , A61P35/00 , A61P37/02 , A61P43/00 , C07D403/12 , C07D405/04
CPC分类号： C07D239/54 , C07D239/52 , C07D403/12 , C07D405/04
摘要： PROBLEM TO BE SOLVED: To provide a GnRH receptor antagonist. SOLUTION: The GnRH receptor antagonist has utility in the treatment of a variety of sex-hormone related conditions in both men and women, and is represented by the following formula, wherein R 1a , R 1b , R 1c , R 2a , R 2b , R 3 , R 4 , R 5 , R 6 , and X each indicate a 1-6C alkanediyl substituted with one to three 1-6C alkyl groups. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供GnRH受体拮抗剂。解决方案：GnRH受体拮抗剂可用于治疗男性和女性各种性激素相关病症，并由下式表示，其中R <1> ，R < R b，R b，R b，R b，R SB 2，R SB 2，R SB 3， SB> 4 ，R SB 5，R SB 6，X各自表示被一至三个1-6C烷基取代的1-6C烷二基。版权所有（C）2011，JPO＆INPIT

8. 发明专利

CY1108656T1 ΠΑΡΑΓΩΓΑ ΤΗΣ ΠΥΡΙΜΙΔΙΝΟ-2,4-ΔΙΟΝΗΣ ΩΣ ΑΝΤΑΓΩΝΙΣΤΕΣ ΤΩΝ ΥΠΟΔΟΧΕΩΝ ΤΗΣ ΕΚΛΥΟΥΣΑΣ ΓΟΝΑΔΟΤΡΟΠΙΝΕΣ ΟΡΜΟΝΗΣ 未知
公开(公告)号：CY1108656T1
公开(公告)日：2014-04-09
申请号：CY081101424
申请日：2008-12-09
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 , A61P5/02 , C07D239/54 , C07D401/12 , C07D403/12 , C07D405/04
摘要： Οιανταγωνιστέςτωνυποδοχέωντης GnRH αποκαλύπτεταιότιέχουνχρησιμότηταστηνθεραπείαμίαςποικιλίαςπαθήσεων, οιοποίεςσχετίζονταιμετηνγεννητικήορμόνη, σεαμφότερουςτουςάνδρεςκαιτιςγυναίκες. Οιενώσειςαυτήςτηςευρεσιτεχνίαςέχουντηνδομή: όπου R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 καιΧ είναιόπωςορίζονταιεδώ, περιλαμβάνονταςταστερεοϊσομερή, τοπροφάρμακακαιταφαρμακευτικάαποδεκτάάλατααυτών. Επίσης, αποκαλύπτονταιοισυνθέσεις, οιοποίεςπεριέχουνμίαένωσηαυτήςτηςευρεσιτεχνίαςσεσυνδυασμόμεένανφαρμακευτικάαποδεκτόφορέα, καθώςκαιτιςμεθόδουςπουσχετίζονταιμετηνχρήσηαυτώνγιατονανταγωνισμότηςεκλυτικήςορμόνηςτωνγοναδοτροπινώνσευποκείμενοπουτηνχρειάζεται.

9. 发明专利

ES2383954T3 Antagonistas del receptor de la hormona liberadora de ganodotropina y métodos relacionados con ellos 未知
公开(公告)号：ES2383954T3
公开(公告)日：2012-06-27
申请号：ES01910362
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： C07D239/52 , C07D239/54 , A61K31/513 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61P1/04 , A61P5/24 , A61P13/08 , A61P15/00 , A61P15/18 , A61P25/20 , A61P35/00 , A61P37/06 , C07D239/553 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D491/08 , C07D498/18 , C07D513/04
摘要： Un compuesto que tiene la siguiente estructura: o uno de sus estereoisómeros, profármacos o sales farmacéuticamente aceptables, en donde: Q es un enlace directo; A es O, S o NR7; n es 2, 3 ó 4; R1 y R2 son iguales o diferentes y son, de modo independiente, hidrógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo, heterocicloalquilo sustituido, -C (R1a) (>=NR1b) o -C (NR1aR1c) (>=NR1b); o R1 y R2, tomados juntos con el átomo de nitrógeno al que están unidos, forman un anillo heterocíclico o un anillo heterocíclico sustituido; R3a y R3b son iguales o diferentes y, en cada aparición, son, de modo independiente, hidrógeno, alquilo, alquilo sustituido, alcoxi, alquiltio, alquilamino, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo, heterocicloalquilo sustituido, -COOR14 o -CONR14R15; o R3a y R3b, tomados juntos con el átomo de carbono al que están unidos, forman un anillo homocíclico, anillo homocíclico sustituido, anillo heterocíclico o anillo heterocíclico sustituido; o R3a y R3b, tomados juntos, forman >=NR3c; o R3a y el carbono al que está unido tomados juntos con R1 y el nitrógeno al que está unido forman un anillo heterocíclico o anillo heterocíclico sustituido; R4 es arilo sustituido o heterociclo; R5 es hidrógeno, halógeno, alquilo inferior, alquilo inferior sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, alcoxi, alquiltio, alquilamino, ciano o nitro; R6 es alquilo superior, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo o heteroarilalquilo sustituido; R7 es hidrógeno, -SO2R11, ciano, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, heteroarilo, heteroarilo sustituido, heteroarilalquilo o heteroarilalquilo sustituido; y R1a, R1b, R1c, R3c, R8a, R8b, R9, R9a, R10a, R10b, R11, R12, R13, R14 y R15 son iguales o diferentes y, en cada aparición, son, de modo independiente, hidrógeno, acilo, alquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo o heterocicloalquilo sustituido; o R1a y R1b, R8a y R8b, R10a y R10b, R12 y R13 o R14 y R15 tomados juntos con el átomo o los átomos a los que están unidos forman un anillo homocíclico, anillo homocíclico sustituido, anillo heterocíclico o anillo heterocíclico sustituido, en donde "alquilo" es un hidrocarburo alifático de cadena lineal o ramificada, no cíclico o cíclico, insaturado o saturado que contiene de 1 a 10 átomos de carbono, en donde alquilo consiste en 1 a 10 átomos de carbono, alquilo inferior consiste en 1 a 6 átomos de carbono y alquilo superior consiste en 2 a 10 átomos de carbono, en donde la forma de profármaco consiste en acetato, formato y benzoato derivados de alcohol y grupos funcionales de amina de compuestos de la estructura (I) y grupos funconales de ésteres de ácido carboxílico, en donde el término "sustituido" tal como se usa en la presente implica cualquiera de los grupos anteriores en donde al menos un átomo de hidrógeno está reemplazado con un sustituyente y en el caso del sustituyente ceto ("-C (>=O) 5 "), dos átomos de hidrógeno están reemplazados, en donde los sustituyentes están seleccionados de halógeno, hidroxi, ciano, nitro, amino, alquilamino, dialquilamino, alquilo, alcoxi, alquiltio, haloalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclo y heterocicloalquilo, así como -NRaRb, -NRaC (>=O) Rb, NRaC (>=O) NRaNRb, -NRaC (>=O) ORb, -NRaSO2Rb, -C (>=O) Ra, -C (>=O) ORa, -C (>=O) NRaRb, -OC (>=O) NRaRb, -ORa, -SRa, - SORa, -S (>=O) 2Ra, -OS (>=O) 2Ra y -S (>=O) 2ORa, en donde los sustituyentes anteriores también pueden estar sustituidos con uno o varios de los sustituyentes anteriores y en donde Ra y Rb pueden ser iguales o diferentes y son, de modo independiente, hidrógeno, alquilo, haloalquilo, alquilo sustituido, arilo, arilo sustituido, arilalquilo, arilalquilo sustituido, heterociclo, heterociclo sustituido, heterocicloalquilo o heterocicloalquilo sustituido.

10. 发明专利

AU2004257636B2 Pyrimidine-2,4-dione derivatives as gonadotropin-releasing hormone receptor antagonists 未知
公开(公告)号：AU2004257636B2
公开(公告)日：2011-01-06
申请号：AU2004257636
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES INC
发明人： HUANG CHARLES Q , RUETER JAIMIE K , CHEN YONGSHENG , REGAN COLLIN , ZHU YUN-FEI , GUO ZHIQIANG
IPC分类号： C07D239/54 , A61K31/495 , A61P5/02 , C07D401/06
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 2a , R 2b , R 3 , R 4 , R 5 , R 6 , R 7 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.

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