-
公开(公告)号：US06841682B2
公开(公告)日：2005-01-11
申请号：US09994153
申请日：2001-11-26
申请人： Richard H. Hutchings , Haripada Khatuya , Gee-Hong Kuo , Xiaobing Li , William V. Murray , Catherine Prouty , Frank Villani , Nelson C. F. Yim , Cynthia Maryanoff
发明人： Richard H. Hutchings , Haripada Khatuya , Gee-Hong Kuo , Xiaobing Li , William V. Murray , Catherine Prouty , Frank Villani , Nelson C. F. Yim , Cynthia Maryanoff
IPC分类号： C07D295/08 , A61K31/495 , A61K31/496 , A61K31/506 , A61P13/08 , A61P43/00 , C07D211/76 , C07D213/38 , C07D261/08 , C07D263/32 , C07D263/34 , C07D277/20 , C07D277/28 , C07D277/56 , C07D295/10 , C07D295/108 , C07D295/12 , C07D295/13 , C07D333/20 , C07D333/22 , C07D333/28 , C07D401/06 , C07D409/06 , C07D413/06 , C07D417/06
CPC分类号： C07D263/34 , C07D211/76 , C07D213/38 , C07D261/08 , C07D263/32 , C07D277/28 , C07D277/56 , C07D295/108 , C07D295/13 , C07D333/20 , C07D333/22 , C07D333/28 , C07D401/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the α-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.
摘要翻译： 本发明涉及一系列含有它们的式Iph药物组合物的杂环取代的哌嗪和其制备中使用的中间体。 本发明的化合物选择性地抑制与α-1a肾上腺素能受体的结合，α受体是与良性前列腺增生有关的受体。 因此，这些化合物潜在地用于治疗这种疾病。
-
公开(公告)号：US4908475A
公开(公告)日：1990-03-13
申请号：US192736
申请日：1988-05-09
摘要： New compounds which have potent V.sub.2 -vasopressin antagonistic activity are prepared by a 1,6-cyclization using peptide bond formation. The structures of the compounds are characterized by a Pas.sup.1,6 or Tas.sup.1,6 cyclized unit. Also a chiral synthesis of the optically pure Pas intermediates is described.
摘要翻译： 通过使用肽键形成的1,6-环化制备具有有效的V2-加压素拮抗活性的新化合物。 化合物的结构由Pas1,6或Tas1,6环化单元表征。 还描述了光学纯的中间体的手性合成。
-
3.发明授权4'-Methyl-.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid vasopressin antagonists 失效4'-甲基-β-巯基-β，β-环戊基亚甲基丙酸加压素拮抗剂
公开(公告)号：US4826813A
公开(公告)日：1989-05-02
申请号：US52809
申请日：1987-05-21
CPC分类号： C07K7/16 , A61K38/00 , Y10S514/807
摘要： Vasopressin antagonists which have a 4'-methyl-.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid group have vasopressin antagonist activity without substantial agonist activity. A species of the invention is [1-(4'-methyl-.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-8-arginine]vasopressin.
-
公开(公告)号：US4760052A
公开(公告)日：1988-07-26
申请号：US43658
申请日：1987-04-28
CPC分类号： C07C403/02 , C07K7/16 , A61K38/00 , C07C2101/14 , Y10S514/807 , Y10S930/15
摘要： New compounds which have potent V.sub.2 -vasopressin antagonistic activity are prepared by a 1,6-cyclization using peptide bond formation. The structures of the compounds are characterized by a Pas.sup.1,6 or Tas.sup.1,6 cyclized unit. Also a chiral synthesis of the optically pure Pas intermediates is described.
摘要翻译： 通过使用肽键形成的1,6-环化制备具有有效的V2-加压素拮抗活性的新化合物。 化合物的结构由Pas1,6或Tas1,6环化单元表征。 还描述了光学纯的中间体的手性合成。
-
公开(公告)号：US06384035B1
公开(公告)日：2002-05-07
申请号：US09169571
申请日：1998-10-09
申请人： Richard H. Hutchings , Haripada Khatuya , Gee-Hong Kuo , Xiaobing Li , William V. Murray , Catherine Prouty , Frank Villani , Nelson C. F. Yim , Cynthia Maryanoff
发明人： Richard H. Hutchings , Haripada Khatuya , Gee-Hong Kuo , Xiaobing Li , William V. Murray , Catherine Prouty , Frank Villani , Nelson C. F. Yim , Cynthia Maryanoff
IPC分类号： A01N4300
CPC分类号： C07D263/34 , C07D211/76 , C07D213/38 , C07D261/08 , C07D263/32 , C07D277/28 , C07D277/56 , C07D295/108 , C07D295/13 , C07D333/20 , C07D333/22 , C07D333/28 , C07D401/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.
摘要翻译： 本发明涉及一系列含有它们的式Iph药物组合物的杂环取代的哌嗪和其制备中使用的中间体。 本发明的化合物选择性地抑制与α-1a肾上腺素能受体的结合，α受体是与良性前列腺增生有关的受体。 因此，这些化合物潜在地用于治疗这种疾病。
-
公开(公告)号：US4108854A
公开(公告)日：1978-08-22
申请号：US714723
申请日：1976-08-16
IPC分类号： C07D207/32 , C07D207/337 , C07D209/20 , C07D307/54 , C07D473/00
CPC分类号： C07D207/337 , C07D209/20 , C07D307/54 , C07D473/00
摘要： A new process is disclosed for the preparation of N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines by reaction of an .alpha.-ester or ether of an N-acylglycine ester or acid with an aromatic or heteroaromatic compound. Also disclosed are new intermediates for preparing N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines.
摘要翻译： 公开了通过N-酰基甘氨酸酯或酸与芳族或杂芳族化合物的α-酯或醚的反应制备N-酰基-α-芳族和N-酰基-α-杂芳香族甘氨酸的新方法。 还公开了用于制备N-酰基-α-芳族和N-酰基-α-异芳香族甘氨酸的新中间体。
-
公开(公告)号：US3997584A
公开(公告)日：1976-12-14
申请号：US619266
申请日：1975-10-03
IPC分类号： C07D207/32 , C07D207/337 , C07D209/20 , C07D307/54 , C07D473/00 , C07C155/02
CPC分类号： C07D207/337 , C07D209/20 , C07D307/54 , C07D473/00
摘要： A new process is disclosed for the preparation of N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines by reaction of an .alpha.-ester or ether of an N-acylglycine ester or acid with an aromatic or heteroaromatic compound. Also disclosed are new intermediates for preparing N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines.
摘要翻译： 公开了通过N-酰基甘氨酸酯或酸与芳族或杂芳族化合物的α-酯或醚的反应制备N-酰基-α-芳族和N-酰基-α-杂芳香族甘氨酸的新方法。 还公开了用于制备N-酰基-α-芳族和N-酰基-α-异芳香族甘氨酸的新中间体。
-
公开(公告)号：US4810778A
公开(公告)日：1989-03-07
申请号：US191673
申请日：1988-05-09
CPC分类号： C07K7/16 , A61K38/00 , Y10S930/15
摘要： New compounds which have potent V.sub.2 -vasopressin antagonistic activity are prepared by a 1,6-cyclization using peptide bond formation. The structures of the compounds are characterized by the Pas.sup.1,6 or Tas.sup.1,6 cyclized unit. Also a chiral synthesis of the optically pure Pas intermediates is described.
摘要翻译： 通过使用肽键形成的1,6-环化制备具有有效的V2-加压素拮抗活性的新化合物。 化合物的结构由Pas1,6或Tas1,6环化单元表征。 还描述了光学纯的中间体的手性合成。
-
公开(公告)号：US3994954A
公开(公告)日：1976-11-30
申请号：US589962
申请日：1975-06-24
IPC分类号： C07D207/32 , C07D207/337 , C07D209/20 , C07D307/54 , C07D473/00 , C07C155/02
CPC分类号： C07D207/337 , C07D209/20 , C07D307/54 , C07D473/00
摘要： A new process is disclosed for the preparation of N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines by reaction of an .alpha.-ester or ether of an N-acylglycine ester or acid with an aromatic or heteroaromatic compound. Also disclosed are new intermediates for preparing N-acyl-.alpha.-aromatic and N-acyl-.alpha.-heteroaromatic glycines.
-
-
-
-
-
-
-
-
搜索结果
9 条记录 (耗时 0.016 秒)
