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公开(公告)号：EP0994848A1
公开(公告)日：2000-04-26
申请号：EP98929244.6
申请日：1998-07-01
发明人： GONZALES, Javier , SAMS, Christian , TENG, Min , LING, Anthony , GREGOR, Vlad , HONG, Yufeng , KIEL, Dan , KUKI, Atsuo , SHI, Shenghua , NAERUM, Lars , MADSEN, Peter , LAU, Jesper , PLEWE, Michael, Bruno , FENG, Jun , JOHNSON, Michael, David , TESTON, Kimberly, Ann , SIDELMANN, Ulla, Grove , KNUDSEN, Lotte, Bjerre
IPC分类号： C07C243/18 , C07D209/04 , A61K31/15 , A61K31/40
CPC分类号： C07D209/48 , C07C251/86 , C07C255/29 , C07C309/65 , C07C311/49 , C07C317/28 , C07C323/45 , C07C2601/02 , C07C2601/14 , C07D209/86 , C07D213/30 , C07D213/80 , C07D215/12 , C07D231/12 , C07D295/185 , C07D307/12 , C07D307/52 , C07D309/06 , C07D317/58
摘要： Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof. The compounds act to antagonize the action of the glucagon peptide hormone.
摘要翻译： 包含中心酰肼基序的非肽化合物及其合成方法。 该化合物用于拮抗胰高血糖素肽激素的作用。
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2.发明授权NON-PEPTIDE GnRH AGENTS, METHODS AND INTERMEDIATES FOR THEIR PREPARATION 有权非肽促性腺激素释放激素药剂油品，工艺及其生产中间体化合物
公开(公告)号：EP1105120B1
公开(公告)日：2005-03-23
申请号：EP99968010.1
申请日：1999-08-20
发明人： ANDERSON, Mark, Brian , VAZIR, Haresh, N. , LUTHIN, David, Robert , PADERES, Genevieve, DeGuzman , PATHAK, Ved, P. , CHRISTIE, Lance, Christopher , HONG, Yufeng , TOMPKINS, Eileen, Valenzuela , LI, Haitao , FAUST, James
IPC分类号： A61K31/34 , A61K31/505 , A61K31/50 , C07D405/12 , C07D307/68 , A61P5/04 , C07D409/12 , C07D417/12
CPC分类号： C07D405/12 , C07D307/68 , C07D405/14 , C07D409/12 , C07D417/12
摘要： Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
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公开(公告)号：EP0984778B1
公开(公告)日：2002-06-12
申请号：EP97939524.1
申请日：1997-08-22
IPC分类号： A61K31/34 , A61K31/35 , A61K31/415 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/47 , C07C275/26 , C07C275/28 , C07D211/08 , A61P25/22 , A61P9/12 , A61P9/10 , A61P3/10 , A61P11/08
CPC分类号： C07C279/24 , C07D213/40 , C07D307/14
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公开(公告)号：EP1137413A2
公开(公告)日：2001-10-04
申请号：EP99960663.5
申请日：1999-12-08
发明人： TRUESDALE, Larry, Kenneth , BYCHOWSKI, Richard, A. , GONZALEZ, Javier , KUKI, Atsuo , RAJAPAKSE, Ranjan, Jagath , TENG, Min , KIEL, Dan , DHANOA, Daljit, S. , HONG, Yufeng , CHOU, Tso-sheng , LING, Anthony, L. , JOHNSON, Michael, David , GREGOR, Vlad, Edward
IPC分类号： A61K31/437 , A61K31/4985 , A61K31/5377 , C07D471/04 , C07D471/12 , C07D413/14 , C07D237/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/14
摘要： Non-peptide compounds that act as antagonists of the intestinal hormone glucagon-like peptide 1 (GLP-1) have a 9H-β-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.
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5.发明公开
公开(公告)号：EP1105120A2
公开(公告)日：2001-06-13
申请号：EP99968010.1
申请日：1999-08-20
发明人： ANDERSON, Mark, Brian , VAZIR, Haresh, N. , LUTHIN, David, Robert , PADERES, Genevieve, DeGuzman , PATHAK, Ved, P. , CHRISTIE, Lance, Christopher , HONG, Yufeng , TOMPKINS, Eileen, Valenzuela , LI, Haitao , FAUST, James
IPC分类号： A61K31/34 , A61K31/505 , A61K31/50 , C07D405/12 , C07D307/68 , A61P5/04
CPC分类号： C07D405/12 , C07D307/68 , C07D405/14 , C07D409/12 , C07D417/12
摘要： Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
摘要翻译： 描述了能够抑制促性腺激素释放激素作用的非肽GnRH剂。 这些化合物及其药学上可接受的盐，多聚体，前体药物和活性代谢物适用于治疗哺乳动物生殖疾病和类固醇激素依赖性肿瘤以及调节生育力，其中指示促性腺激素释放的抑制。 还描述了合成用于其制备的化合物和中间体的方法。
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公开(公告)号：EP1068178A1
公开(公告)日：2001-01-17
申请号：EP99909706.6
申请日：1999-03-01
IPC分类号： C07C279/12 , A61K31/155 , C07D307/77 , C07D405/12 , C07D409/12 , C07D213/82 , C07D319/18 , C07D333/70 , C07D317/68 , C07D261/18 , C07D237/24 , C07D209/42
CPC分类号： C07D213/82 , C07C279/12 , C07D207/34 , C07D209/42 , C07D215/12 , C07D231/14 , C07D231/16 , C07D261/10 , C07D307/00 , C07D307/68 , C07D307/71 , C07D307/91 , C07D317/68 , C07D319/18 , C07D333/38 , C07D333/70 , C07D405/12 , C07D409/12
摘要： Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of general formula (I), where X1, X2, Y, and Z are defined variables. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
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公开(公告)号：EP1137413B1
公开(公告)日：2005-02-02
申请号：EP99960663.5
申请日：1999-12-08
发明人： TRUESDALE, Larry, Kenneth , BYCHOWSKI, Richard, A. , GONZALEZ, Javier , KUKI, Atsuo , RAJAPAKSE, Ranjan, Jagath , TENG, Min , KIEL, Dan , DHANOA, Daljit, S. , HONG, Yufeng , CHOU, Tso-sheng , LING, Anthony, L. , JOHNSON, Michael, David , GREGOR, Vlad, Edward
IPC分类号： A61K31/437 , A61K31/4985 , A61K31/5377 , C07D471/04 , C07D471/12 , C07D413/14 , C07D237/00 , A61K31/435
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/14
摘要： Non-peptide compounds that act as antagonists of the intestinal hormone glucagon-like peptide 1 (GLP-1) have a 9H-β-carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.
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8.发明公开NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USES, AND PROCESSES FOR PREPARING THEM 审中-公开非肽GnRH一剂，药物组合物及使用及其制造方法FOR THEIR
公开(公告)号：EP1401427A2
公开(公告)日：2004-03-31
申请号：EP02739712.4
申请日：2002-06-05
发明人： SUN, Eric, T. , ANDERSON, Mark, B. , ANDERES, Kenna, Lynn , CHRISTIE, Lance, Christopher , DO, Quyen-Quyen, Thuy , FENG, Jun , GOETZEN, Thomas , HONG, Yufeng , KRAYNOV, Eugenia, Anatolievna , LI, Haitao , LUTHIN, David, Robert , PADERES, Genevieve, D. , PATHAK, Ved, P. , RAJAPAKSE, Ranjan, Jagath , SHACKELFORD, Scott , TOMPKINS, Eileen, Valenzuela , TRUESDALE, Larry, Kenneth , VAZIR, Haresh
IPC分类号： A61K31/341 , A61K31/443 , A61K31/497 , C07D307/58 , C07D405/10
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D307/68 , C07D405/12 , C07D405/14 , C07D407/12 , C07D471/04
摘要： Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
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