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1. 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。

2. 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

3. 发明专利

CY1112815T1 ΑΝΤΑΓΩΝΙΣΤΕΣ ΥΠΟΔΟΧΕΑ ΟΡΜΟΝΗΣ ΑΠΕΛΕΥΘΕΡΩΣΗΣ ΓΟΝΑΔΟΤΡΟΠΙΝΗΣ ΚΑΙ ΜΕΘΟΔΟΙ ΠΟΥ ΣΧΕΤΙΖΟΝΤΑΙ ΜΕ ΑΥΤΟΥΣ 未知
公开(公告)号：CY1112815T1
公开(公告)日：2016-02-10
申请号：CY121100499
申请日：2012-06-01
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： Ανταγωνιστέςυποδοχέα GnRΗαποκαλύπτονταιπουέχουνχρησιμότηταστηθεραπείαμιαςποικιλίαςκαταστάσεωνπουσχετίζονταιμεορμόνεςτουφύλουτόσοσεάνδρεςόσοκαισεγυναίκες. Οιενώσειςαυτήςτηςεφεύρεσηςείναιτουτύπου (Ι) όπουταΑ, Q, R1, R2, R3a, R3b, R4, R5, R6 και n είναιόπωςορίζονταιεδώ, συμπεριλαμβανομένωνστερεοϊσομερών, προφαρμάκωνκαιφαρμακευτικώςαποδεκτώναλάτωναυτών. Επίσηςαποκαλύπτονταισυνθέσειςπουπεριέχουνμιαένωσηαυτήςτηςεφεύρεσηςσεσυνδυασμόμεένανφαρμακευτικώςαποδεκτόφορέα, όπωςεπίσηςκαιμεθόδουςπουσχετίζονταιμετηχρήσηαυτώνγιαανταγωνισμόορμόνηςαπελευθέρωσηςγοναδοτροπίνηςσεέναάτομοπουχρειάζεταικάτιτέτοιο.

4. 发明专利

UY31009A1 ANTAGONISTAS DEL RECEPTOR DE LA HORMONA LIBERADORA DE GONADOTROPINA Y PROCEDIMIENTOS RELACIONADOS CON LOS MISMOS 未知
公开(公告)号：UY31009A1
公开(公告)日：2008-11-28
申请号：UY31009
申请日：2008-04-07
申请人： NEUROCRINE BIOSCIENCES INC
发明人： ASHWEEK NEIL , ROWBOTTOM MARTIN , ZHU YUN-FEI , ZHAO LIREN , WADE WARREN , SMITH NICOLE , MOREE WILLY , LOWE RICHARD , JIANG WANLONG , EWING TODD , COON TIMOTHY RICHARD , CHEN MI , BEATON GRAHAM
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/47 , A61K31/513 , A61P5/24 , C07D207/16 , C07D207/24 , C07D213/56 , C07D213/61 , C07D213/70 , C07D213/84 , C07D215/54 , C07D231/12 , C07D239/36 , C07D249/12 , C07D257/04 , C07D261/08 , C07D271/10 , C07D401/04 , C07D413/12
摘要： Antagonistas del receptor GnRH teniendo utilidad en tratamiento de diversas afecciones relacionadas con hormonas sexuales tanto en hombres como en mujeres. Dichos compuestos tienen la estructura: donde R1a, R1b, R1c, R1d, R2, R2a y A son como se definieron en este documento, incluyendo estereoisomeros, ésteres solvatos y sales farmacéuticamente aceptables de los mismos. Incluyen composiciones conteniendo un compuesto de esta invencion junto con vehículo farmacéuticamente aceptable, y aplicaciones de los mismos para antagonizar la hormona liberadora de gonadotropina en un sujeto que lo necesita.

5. 发明专利

CA2683431A1 GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 未知
公开(公告)号：CA2683431A1
公开(公告)日：2008-10-16
申请号：CA2683431
申请日：2008-04-04
申请人： NEUROCRINE BIOSCIENCES INC
发明人： MOREE WILLY , SMITH NICOLE , JIANG WANLONG , LOWE RICHARD , EWING TODD , WADE WARREN , COON TIMOTHY RICHARD , CHEN MI , BEATON GRAHAM , ZHAO LIREN , ASHWEEK NEIL , ROWBOTTOM MARTIN , ZHU YUN-FEI
IPC分类号： A61K31/435 , A61P35/00 , C07C233/88 , C07C255/57 , C07D213/56 , C07D213/61 , C07D213/70 , C07D213/84 , C07D215/14 , C07D215/54 , C07D239/36 , C07D401/12 , C07D413/12 , C07D417/12 , C07D495/02
摘要： GnRH receptor antagonists are disclosed which have utility in the treatme nt 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, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solv ates and pharmaceutically acceptable salts thereof. Also disclosed are compo sitions containing a compound of this invention in combination with a pharma ceutically acceptable carrier, as well as methods relating to the use thereo f for antagonizing gonadotropin-releasing hormone in a subject in need there of.

6. 发明专利

AU2004200664B2 Gonadotropin-releasing hormone receptor antagonists and methods relating thereto 未知
公开(公告)号：AU2004200664B2
公开(公告)日：2007-08-16
申请号：AU2004200664
申请日：2004-02-19
申请人： NEUROCRINE BIOSCIENCES INC
发明人： TUCCI FABIO C , STRUTHERS R SCOTT , GROSS TIMOTHY D , CHEN CHEN , ZHU YUN-FEI , GUO ZHIQIANG , ROWBOTTOM MARTIN
IPC分类号： C07D239/00

7. 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.

8. 发明专利

AU767585B2 Gonadotropin-releasing hormone receptor antagonists and methods relating thereto 未知
公开(公告)号：AU767585B2
公开(公告)日：2003-11-20
申请号：AU3797501
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 , 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 , C07D239/00
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 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.

9. 发明专利

HK1051042A1 GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 未知
公开(公告)号：HK1051042A1
公开(公告)日：2003-07-18
申请号：HK03103248
申请日：2003-05-07
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 , A61K31/513 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61P1/04 , A61P5/24 , A61P13/08 , A61P15/00 , A61P15/18 , A61P25/20 , A61P35/00 , A61P37/06 , C07D20060101 , 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
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 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.

10. 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.

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