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公开(公告)号：US5847006A
公开(公告)日：1998-12-08
申请号：US454927
申请日：1995-05-31
申请人： Sharad Magar , Graham J. Durant , Lain-Yen Hu , Stanley M. Goldin , N. Laxma Reddy , James B. Fischer , Subbarao Katragadda , Andrew Gannett Knapp , Lee David Margolin
发明人： Sharad Magar , Graham J. Durant , Lain-Yen Hu , Stanley M. Goldin , N. Laxma Reddy , James B. Fischer , Subbarao Katragadda , Andrew Gannett Knapp , Lee David Margolin
IPC分类号： C07C279/18 , A01N37/52 , C07C277/00
CPC分类号： C07C279/18 , C07C2103/20
摘要： The present invention provides N,N'-diaryl substituted guanidines having therapeutic utility. The compounds of the present invention are represented by the formula: ##STR1## wherein R and R.sup.1 represent hydrogen or other group and Ar and Ar.sup.1 represent selected aryl groups, and at least one being acenaphthyl.
摘要翻译： 本发明提供具有治疗效用的N，N'-二芳基取代的胍。 本发明的化合物由下式表示：其中R和R 1表示氢或其它基团，Ar和Ar 1表示选择的芳基，至少一个是苊基。
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公开(公告)号：US07351743B1
公开(公告)日：2008-04-01
申请号：US09637774
申请日：2000-08-11
申请人： Stanley M. Goldin , James B. Fischer , Andrew Gannett Knapp , N. Laxma Reddy , David Berlove , Graham J. Durant , Subbarao Katragadda , Lain-Yen Hu , Sharad Magar , Wenhong Fan , Elizabeth Yost , Juo Qing Guo
发明人： Stanley M. Goldin , James B. Fischer , Andrew Gannett Knapp , N. Laxma Reddy , David Berlove , Graham J. Durant , Subbarao Katragadda , Lain-Yen Hu , Sharad Magar , Wenhong Fan , Elizabeth Yost , Juo Qing Guo
IPC分类号： A61K31/155 , C07C279/18
CPC分类号： A61K31/155 , C07C279/18
摘要： The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
摘要翻译： 本发明提供治疗上有用的取代胍，以及使用或包含一种或多种此类胍的治疗方法和药物组合物。
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公开(公告)号：US06288123B1
公开(公告)日：2001-09-11
申请号：US08464103
申请日：1995-06-05
申请人： Stanley M. Goldin , James B. Fischer , Andrew Gannett Knapp , N. Laxma Reddy , David Berlove , Graham J. Durant , Subbarao Katragadda , Lain-Yen Hu , Sharad Magar , Wenhong Fan , Elizabeth Yost , Jun Qing Guo
发明人： Stanley M. Goldin , James B. Fischer , Andrew Gannett Knapp , N. Laxma Reddy , David Berlove , Graham J. Durant , Subbarao Katragadda , Lain-Yen Hu , Sharad Magar , Wenhong Fan , Elizabeth Yost , Jun Qing Guo
IPC分类号： A61K31155
CPC分类号： C07C323/43 , A61K31/155 , A61K31/405 , A61K31/445 , C07C279/04 , C07C279/18 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2603/12 , C07C2603/18 , C07C2603/20 , C07C2603/24 , C07C2603/26 , C07C2603/40 , C07C2603/74 , C07D209/08 , C07D209/90 , C07D209/92 , C07D217/06 , C07D277/62 , C07D285/10 , C07D295/215 , C07D317/58 , C07D471/04
摘要： The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
摘要翻译： 本发明提供治疗上有用的取代胍，以及使用或包含一种或多种此类胍的治疗方法和药物组合物。
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公开(公告)号：US06787569B1
公开(公告)日：2004-09-07
申请号：US09637512
申请日：2000-08-11
申请人： Stanley M. Goldin , James B. Fischer , Andrew Gannett Knapp , N. Laxma Reddy , David Berlove , Graham J. Durant , Subbarao Katragadda , Lain-Yen Hu , Sharad Magar , Wenhong Fan , Elizabeth Yost , Jun Qing Guo
发明人： Stanley M. Goldin , James B. Fischer , Andrew Gannett Knapp , N. Laxma Reddy , David Berlove , Graham J. Durant , Subbarao Katragadda , Lain-Yen Hu , Sharad Magar , Wenhong Fan , Elizabeth Yost , Jun Qing Guo
IPC分类号： A61K31155
CPC分类号： C07D277/62 , A61K31/155 , A61K31/405 , A61K31/445 , A61K31/50 , C07C279/18 , C07C2602/08 , C07C2602/10 , C07C2603/12 , C07C2603/18 , C07C2603/20 , C07C2603/74 , C07D209/08 , C07D209/90 , C07D209/92 , C07D217/06 , C07D285/10 , C07D295/215 , C07D317/58 , C07D471/04
摘要： The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
摘要翻译： 本发明提供治疗上有用的取代胍，以及使用或包含一种或多种此类胍的治疗方法和药物组合物。
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公开(公告)号：US06174924B1
公开(公告)日：2001-01-16
申请号：US08462013
申请日：1995-06-05
申请人： Stanley M. Goldin , James B. Fischer , Andrew Gannett Knapp , N. Laxma Reddy , David Berlove , Graham J. Durant , Subbarao Katragadda , Lain-Yen Hu , Sharad Magar , Wenhong Fan , Elizabeth Yost , Jun Qing Guo
发明人： Stanley M. Goldin , James B. Fischer , Andrew Gannett Knapp , N. Laxma Reddy , David Berlove , Graham J. Durant , Subbarao Katragadda , Lain-Yen Hu , Sharad Magar , Wenhong Fan , Elizabeth Yost , Jun Qing Guo
IPC分类号： A61K31155
CPC分类号： C07C323/43 , A61K31/155 , A61K31/405 , A61K31/445 , C07C279/04 , C07C279/18 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2603/12 , C07C2603/18 , C07C2603/20 , C07C2603/24 , C07C2603/26 , C07C2603/40 , C07C2603/74 , C07D209/08 , C07D209/90 , C07D209/92 , C07D217/06 , C07D277/62 , C07D285/10 , C07D295/215 , C07D317/58 , C07D471/04
摘要： The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
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6.发明授权Hydrazinedicarboximidamide compounds and pharmaceutical composition comprising same 失效肼酰二甲酰胺化合物和包含其的药物组合物
公开(公告)号：US5837737A
公开(公告)日：1998-11-17
申请号：US485566
申请日：1995-06-07
申请人： Stanley M. Goldin , Subbarao Katragadda , Lain-Yen Hu , N. Laxma Reddy , James B. Fischer , Andrew Gannett Knapp , Lee David Margolin
发明人： Stanley M. Goldin , Subbarao Katragadda , Lain-Yen Hu , N. Laxma Reddy , James B. Fischer , Andrew Gannett Knapp , Lee David Margolin
IPC分类号： A61K31/15 , A61K31/155 , A61K31/16 , A61K31/17 , A61K31/275 , A61K31/277 , A61K31/34 , A61K31/37 , A61K31/38 , A61K31/381 , A61K31/39 , A61K31/40 , A61K31/403 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/53 , A61K31/54 , A61K31/655 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/20 , C07C279/04 , C07C279/16 , C07C279/18 , C07C279/22 , C07C281/16 , C07C281/18 , C07D209/00 , C07D217/22 , C07D239/42 , C07D241/20 , C07D263/48 , C07D277/82 , C07D333/36 , G01N33/58 , A01N37/52 , C07C281/00
CPC分类号： C07C281/16 , A61K31/155 , A61K31/17 , A61K31/275 , A61K31/277 , A61K31/34 , A61K31/37 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/655 , C07C279/16 , C07C2101/14 , C07C2103/20 , C07C2103/74
摘要： Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
摘要翻译： 公开了神经递质释放的调节剂，包括取代的胍，N“ - 氨基胍和N，N'N”，N“ - 四取代肼二甲酰亚胺酰胺及其药物组合物。 还公开了涉及使用这种神经递质释放调节剂来治疗或预防以释放过量或不适当水平的神经递质为特征的病理生理学病症的方法。 还公开了选择性抑制谷氨酸释放的化合物的筛选测定。 还公开了阻断哺乳动物神经细胞中电压敏感的钠和钙通道的方法。
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公开(公告)号：US5686495A
公开(公告)日：1997-11-11
申请号：US466031
申请日：1995-06-06
申请人： Stanley M. Goldin , Subbarao Katragadda , Lain-Yen Hu , N. Laxma Reddy , James B. Fischer , Andrew Gannett Knapp , Lee David Margolin
发明人： Stanley M. Goldin , Subbarao Katragadda , Lain-Yen Hu , N. Laxma Reddy , James B. Fischer , Andrew Gannett Knapp , Lee David Margolin
IPC分类号： A61K31/15 , A61K31/155 , A61K31/16 , A61K31/17 , A61K31/275 , A61K31/277 , A61K31/34 , A61K31/37 , A61K31/38 , A61K31/381 , A61K31/39 , A61K31/40 , A61K31/403 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/53 , A61K31/54 , A61K31/655 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/20 , C07C279/04 , C07C279/16 , C07C279/18 , C07C279/22 , C07C281/16 , C07C281/18 , C07D209/00 , C07D217/22 , C07D239/42 , C07D241/20 , C07D263/48 , C07D277/82 , C07D333/36 , G01N33/58
CPC分类号： C07C281/16 , A61K31/155 , A61K31/17 , A61K31/275 , A61K31/277 , A61K31/34 , A61K31/37 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/655 , C07C279/16 , C07C2101/14 , C07C2103/20 , C07C2103/74
摘要： Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
摘要翻译： 公开了神经递质释放的调节剂，包括取代的胍，N“ - 氨基胍和N，N'N”，N“ - 四取代肼二甲酰亚胺酰胺及其药物组合物。 还公开了涉及使用这种神经递质释放调节剂来治疗或预防以释放过量或不适当水平的神经递质为特征的病理生理学病症的方法。 还公开了选择性抑制谷氨酸释放的化合物的筛选测定。 还公开了阻断哺乳动物神经细胞中电压敏感的钠和钙通道的方法。
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公开(公告)号：US6071969A
公开(公告)日：2000-06-06
申请号：US461700
申请日：1995-06-05
申请人： Stanley M. Goldin , Subbarao Katragadda , Lain-Yen Hu , N. Laxma Reddy , James B. Fischer , Andrew Gannett Knapp , Lee David Margolin
发明人： Stanley M. Goldin , Subbarao Katragadda , Lain-Yen Hu , N. Laxma Reddy , James B. Fischer , Andrew Gannett Knapp , Lee David Margolin
IPC分类号： A61K31/15 , A61K31/155 , A61K31/16 , A61K31/17 , A61K31/275 , A61K31/277 , A61K31/34 , A61K31/37 , A61K31/38 , A61K31/381 , A61K31/39 , A61K31/40 , A61K31/403 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/53 , A61K31/54 , A61K31/655 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/20 , C07C279/04 , C07C279/16 , C07C279/18 , C07C279/22 , C07C281/16 , C07C281/18 , C07D209/00 , C07D217/22 , C07D239/42 , C07D241/20 , C07D263/48 , C07D277/82 , C07D333/36 , G01N33/58
CPC分类号： C07C281/16 , A61K31/155 , A61K31/17 , A61K31/275 , A61K31/277 , A61K31/34 , A61K31/37 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/655 , C07C279/16 , C07C2101/14 , C07C2103/20 , C07C2103/74
摘要： Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
摘要翻译： 公开了神经递质释放的调节剂，包括取代的胍，N“ - 氨基胍和N，N'N”，N“ - 四取代肼二甲酰亚胺酰胺及其药物组合物。 还公开了涉及使用这种神经递质释放调节剂来治疗或预防以释放过量或不适当水平的神经递质为特征的病理生理学病症的方法。 还公开了选择性抑制谷氨酸释放的化合物的筛选测定。 还公开了阻断哺乳动物神经细胞中电压敏感的钠和钙通道的方法。
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公开(公告)号：US5677348A
公开(公告)日：1997-10-14
申请号：US462834
申请日：1995-06-05
申请人： Stanley M. Goldin , Subbarao Katragadda , Lain-Yen Hu , N. Laxma Reddy , James B. Fischer , Andrew Gannett Knapp , Lee David Margolin
发明人： Stanley M. Goldin , Subbarao Katragadda , Lain-Yen Hu , N. Laxma Reddy , James B. Fischer , Andrew Gannett Knapp , Lee David Margolin
IPC分类号： A61K31/15 , A61K31/155 , A61K31/16 , A61K31/17 , A61K31/275 , A61K31/277 , A61K31/34 , A61K31/37 , A61K31/38 , A61K31/381 , A61K31/39 , A61K31/40 , A61K31/403 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/53 , A61K31/54 , A61K31/655 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/20 , C07C279/04 , C07C279/16 , C07C279/18 , C07C279/22 , C07C281/16 , C07C281/18 , C07D209/00 , C07D217/22 , C07D239/42 , C07D241/20 , C07D263/48 , C07D277/82 , C07D333/36 , G01N33/58
CPC分类号： C07C281/16 , A61K31/155 , A61K31/17 , A61K31/275 , A61K31/277 , A61K31/34 , A61K31/37 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/655 , C07C279/16 , C07C2101/14 , C07C2103/20 , C07C2103/74
摘要： Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
摘要翻译： 公开了神经递质释放的调节剂，包括取代的胍，N“ - 氨基胍和N，N'N”，N“ - 四取代肼二甲酰亚胺酰胺及其药物组合物。 还公开了涉及使用这种神经递质释放调节剂来治疗或预防以释放过量或不适当水平的神经递质为特征的病理生理学病症的方法。 还公开了选择性抑制谷氨酸释放的化合物的筛选测定。 还公开了阻断哺乳动物神经细胞中电压敏感的钠和钙通道的方法。
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公开(公告)号：US5670519A
公开(公告)日：1997-09-23
申请号：US463420
申请日：1995-06-05
申请人： Stanley M. Goldin , Subbarao Katragadda , Lain-Yen Hu , N. Laxma Reddy , James B. Fischer , Andrew Gannett Knapp , Lee David Margolin
发明人： Stanley M. Goldin , Subbarao Katragadda , Lain-Yen Hu , N. Laxma Reddy , James B. Fischer , Andrew Gannett Knapp , Lee David Margolin
IPC分类号： A61K31/15 , A61K31/155 , A61K31/16 , A61K31/17 , A61K31/275 , A61K31/277 , A61K31/34 , A61K31/37 , A61K31/38 , A61K31/381 , A61K31/39 , A61K31/40 , A61K31/403 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/53 , A61K31/54 , A61K31/655 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/20 , C07C279/04 , C07C279/16 , C07C279/18 , C07C279/22 , C07C281/16 , C07C281/18 , C07D209/00 , C07D217/22 , C07D239/42 , C07D241/20 , C07D263/48 , C07D277/82 , C07D333/36 , G01N33/58 , A61K31/395 , A61K31/36
CPC分类号： C07C281/16 , A61K31/155 , A61K31/17 , A61K31/275 , A61K31/277 , A61K31/34 , A61K31/37 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/655 , C07C279/16 , C07C2101/14 , C07C2103/20 , C07C2103/74
摘要： Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.
摘要翻译： 公开了神经递质释放的调节剂，包括取代的胍，N“ - 氨基胍和N，N'N”，N“ - 四取代肼二甲酰亚胺酰胺及其药物组合物。 还公开了涉及使用这种神经递质释放调节剂来治疗或预防以释放过量或不适当水平的神经递质为特征的病理生理学病症的方法。 还公开了选择性抑制谷氨酸释放的化合物的筛选测定。 还公开了阻断哺乳动物神经细胞中电压敏感的钠和钙通道的方法。
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