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1. 发明申请

WO2005007164A1 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促性腺激素释放激素受体拮抗剂
公开(公告)号：WO2005007164A1
公开(公告)日：2005-01-27
申请号：PCT/US2004/021569
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES, INC. , ZHU, Yun-Fei , REGAN, Collin , RUETER, Jaimie, K. , GUO, Zhiqiang , CHEN, Yongsheng , HUANG, Charles, Q.
发明人： ZHU, Yun-Fei , REGAN, Collin , RUETER, Jaimie, K. , GUO, Zhiqiang , CHEN, Yongsheng , HUANG, Charles, Q.
IPC分类号： A61K31/513
CPC分类号： C07D239/54 , 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 formula (I) 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.
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结构式（I），其中R 1a，R 1b，R 2a，R 2b，R 3，R 4，R 5，R 6，R 7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。

2. 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。

3. 发明申请

WO2005113516A1 URACIL-TYPE GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATED THERETO 审中-公开
标题翻译：尿嘧啶型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：WO2005113516A1
公开(公告)日：2005-12-01
申请号：PCT/US2005/016906
申请日：2005-05-13
申请人： NEUROCRINE BIOSCIENCES, INC. , ZHU, Yun-Fei , GOU, Zhiqiang , CHEN, Mi , ZHAO, Liren
发明人： ZHU, Yun-Fei , GOU, Zhiqiang , CHEN, Mi , ZHAO, Liren
IPC分类号： C07D239/54
CPC分类号： C07D239/54 , C07D403/12
摘要： Compounds having utility as GnRH receptor antagonists and for treatment of a variety of sex-hormone related conditions in both men and women. Such compounds have the following structure (I): (I) wherein R 1a , R 1b , R 1c , R 2a , R 2b , R 3 , R 4 , R 5 , R 6 , R 7 , n and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of structure (I) 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：具有用作GnRH受体拮抗剂并用于治疗男性和女性中各种性激素相关病症的化合物。这些化合物具有以下结构（I）：（I）其中R 1a，R 1b，R 1c，R 2a，R 2b，R 3，R 4，R 5，R 6，R 7，n和X如本文所定义，包括立体异构体，前药和药学上可接受的盐它们。还公开了含有结构（I）的化合物与药学上可接受的载体的组合物的组合物，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

WO2008124610A1 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：WO2008124610A1
公开(公告)日：2008-10-16
申请号：PCT/US2008/059438
申请日：2008-04-04
申请人： NEUROCRINE BIOSCIENCES, INC. , BEATON, Graham , CHEN, Mi , COON, Timothy, Richard , EWING, Todd , JIANG, Wanlong , LOWE, Richard , MOREE, Willy , SMITH, Nicole , WADE, Warren , ZHAO, Liren , ZHU, Yun-Fei , ROWBOTTOM, Martin , ASHWEEK, Neil
发明人： BEATON, Graham , CHEN, Mi , COON, Timothy, Richard , EWING, Todd , JIANG, Wanlong , LOWE, Richard , MOREE, Willy , SMITH, Nicole , WADE, Warren , ZHAO, Liren , ZHU, Yun-Fei , ROWBOTTOM, Martin , ASHWEEK, Neil
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
CPC分类号： C07D495/04 , C07C233/88 , C07C235/42 , C07C255/57 , C07D213/56 , C07D213/58 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/81 , C07D213/84 , C07D213/89 , C07D215/14 , C07D215/54 , C07D239/36 , C07D401/04 , C07D401/12 , C07D413/12 , C07D417/12
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. The compounds of this invention have the structure, wherein R 1a , R 1b , R 1c , R 1d , R 2 , R 2a , and A 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 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以下结构，其中R 1a 1a，R 1b，R 1c，R 1d， R 2，R 2a和A如本文所定义，包括其立体异构体，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.

6. 发明授权

EP2155194B1 GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 无效转让
标题翻译：促性腺激素释放激素受体的拮抗剂及任何相关手续
公开(公告)号：EP2155194B1
公开(公告)日：2015-01-21
申请号：EP08745136.5
申请日：2008-04-04
申请人： NEUROCRINE BIOSCIENCES, INC.
发明人： BEATON, Graham , CHEN, Mi , COON, Timothy, Richard , EWING, Todd , JIANG, Wanlong , LOWE, Richard , MOREE, Willy , HARRIOTT, Nicole , WADE, Warren , ZHAO, Liren , ZHU, Yun-Fei , ROWBOTTOM, Martin , ASHWEEK, Neil
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
CPC分类号： C07D495/04 , C07C233/88 , C07C235/42 , C07C255/57 , C07D213/56 , C07D213/58 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/81 , C07D213/84 , C07D213/89 , C07D215/14 , C07D215/54 , C07D239/36 , C07D401/04 , C07D401/12 , C07D413/12 , C07D417/12
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. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A 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 for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

7. 发明公开

EP1411945A1 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-ON及其作为拮抗剂的促性腺激素释放激素
公开(公告)号：EP1411945A1
公开(公告)日：2004-04-28
申请号：EP02756927.6
申请日：2002-08-02
申请人： Neurocrine Biosciences, Inc.
发明人： TUCCI, Fabio, C. , CONNORS, Patrick, J. , ZHU, Yun-Fei , CHEN, Chen
IPC分类号： A61K31/45 , A61K31/443 , A61K31/444 , A61K31/4439 , A61K31/4436 , C07D213/68 , C07D401/12 , C07D405/12 , C07D453/02 , C07D487/04 , C07D409/12 , C07D213/69 , C07D409/04 , A61P5/04
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; R1 and R2 are the same or different and independently hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycle, substituted heterocycle, heterocyclealkyl, susbstituted heterocyclealkyl, -C(R8)(=NR9) or -C(NR10R11)(=NR9); or R1 and R2 taken together with the nitrogen atom to which they are attached form a heterocycle or a substituted heterocycle; R3a and R3b 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, -COOR12 or -CONR10R11; or R3ab and R3b taken together with the carbon atom to which they are attached form a homocycle, substituted homocycle, heterocycle or substituted heterocycle; or R3a and the carbon to which it is attached taken together with R1 and the nitrogen to which it is attached form a heterocycle or substituted heterocycle; R4 is hydrogen, alkyl or substituted alkyl; R5 is arylalkyl, substituted arylalkyl, heteroarylalkyl or substituted heteroalalkyl; R6 is aryl, substituted aryl, heteroaryl or substituted heteroaryl; R7 is hydrogen, alkyl or substituted alkyl; R8, R9, R10 and R11 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 R12 is hydrogen, alkyl or substituted alkyl.

8. 发明公开

EP2155194A1 GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 无效转让
标题翻译：促性腺激素释放激素受体的拮抗剂及任何相关手续
公开(公告)号：EP2155194A1
公开(公告)日：2010-02-24
申请号：EP08745136.5
申请日：2008-04-04
申请人： NEUROCRINE BIOSCIENCES, INC.
发明人： BEATON, Graham , CHEN, Mi , COON, Timothy, Richard , EWING, Todd , JIANG, Wanlong , LOWE, Richard , MOREE, Willy , SMITH, Nicole , WADE, Warren , ZHAO, Liren , ZHU, Yun-Fei , ROWBOTTOM, Martin , ASHWEEK, Neil
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
CPC分类号： C07D495/04 , C07C233/88 , C07C235/42 , C07C255/57 , C07D213/56 , C07D213/58 , C07D213/61 , C07D213/64 , C07D213/70 , C07D213/81 , C07D213/84 , C07D213/89 , C07D215/14 , C07D215/54 , C07D239/36 , C07D401/04 , C07D401/12 , C07D413/12 , C07D417/12
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. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A 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 for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

9. 发明公开

EP1660091A1 PYRIMIDINE-2,4-DIONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS 有权
标题翻译：作为促性腺激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物
公开(公告)号：EP1660091A1
公开(公告)日：2006-05-31
申请号：EP04777596.0
申请日：2004-07-06
申请人： NEUROCRINE BIOSCIENCES, INC.
发明人： ZHU, Yun-Fei , REGAN, Collin , RUETER, Jaimie, K. , GUO, Zhiqiang , CHEN, Yongsheng , HUANG, Charles, Q.
IPC分类号： A61K31/513 , C07D239/54 , C07D401/06 , A61P5/02
CPC分类号： C07D239/54 , 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 formula (I) wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 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GnRH受体拮抗剂，其可用于治疗男性和女性的各种与性激素有关的病症。本发明化合物具有结构式（I）其中R 1a，R 1b，R 2a，R 2b，R 3，R 4，R 5，R 6，R 7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以及药学上可接受的载体的组合物，以及涉及其在需要其的受试者中用于拮抗促性腺激素释放激素的方法。

10. 发明授权

EP1220857B1 GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONISTS AND THEIR RELATED METHODS OF USE 有权
标题翻译：促性腺激素释放激素受体拮抗剂和相关的应用
公开(公告)号：EP1220857B1
公开(公告)日：2005-09-21
申请号：EP00973591.1
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： C07D487/04 , A61K31/505 , A61P5/02
CPC分类号： 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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