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公开(公告)号:EP0124317B1
公开(公告)日:1990-04-11
申请号:EP84302621.2
申请日:1984-04-17
CPC分类号: C07K5/1019 , A61K38/00 , C07K5/06078 , C07K5/06086 , C07K5/0808 , C07K5/0812 , C07K5/0815 , C07K5/1016
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公开(公告)号:EP0124317A3
公开(公告)日:1987-01-14
申请号:EP84302621
申请日:1984-04-17
IPC分类号: C07C103/52 , A61K37/02
CPC分类号: C07K5/1019 , A61K38/00 , C07K5/06078 , C07K5/06086 , C07K5/0808 , C07K5/0812 , C07K5/0815 , C07K5/1016
摘要: Proline derivatives of the formulae:
wherein R 1 through R 11 have defined values, and acid- and base-addition salts thereof, and equilibrium addition compounds of the aldehyde group thereof; processes for their preparation; pharmaceutical compositions; and intermediates for preparing said proline derivatives. The proline derivatives are human leukocyte elastase inhibitors which are useful, for example, in treating pulmonary emphysema.-
公开(公告)号:EP0124317A2
公开(公告)日:1984-11-07
申请号:EP84302621.2
申请日:1984-04-17
CPC分类号: C07K5/1019 , A61K38/00 , C07K5/06078 , C07K5/06086 , C07K5/0808 , C07K5/0812 , C07K5/0815 , C07K5/1016
摘要: Proline derivatives of the formulae:
wherein R 1 through R 11 have defined values, and acid- and base-addition salts thereof, and equilibrium addition compounds of the aldehyde group thereof; processes for their preparation; pharmaceutical compositions; and intermediates for preparing said proline derivatives. The proline derivatives are human leukocyte elastase inhibitors which are useful, for example, in treating pulmonary emphysema.-
公开(公告)号:EP0276101A3
公开(公告)日:1989-11-23
申请号:EP88300343.6
申请日:1988-01-15
申请人: ICI AMERICAS INC.
CPC分类号: C07K5/06191 , A61K38/00
摘要: The invention provides a series of novel substituted peptide derivatives of the formulae la, Ib and Ic (set out hereinafter) and pharmaceutically acceptable salts thereof, in which the radicals A, R 1 , R 2 and R 4 -R 9 have the meanings defined in the following specification. The compounds of formulae la, Ib, and Ic are inhbitors of human leukocytic elastase. The invention also provides pharmaceutical compositions containing a compound of formula la, Ib or Ic, or a pharmaceutically acceptable salt thereof and processes and intermediates for the manufacture of compounds of formulae la, Ib, and Ic.
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公开(公告)号:EP0189305A3
公开(公告)日:1988-10-05
申请号:EP86300379
申请日:1986-01-20
申请人: ICI AMERICAS INC.
发明人: Bergeson, Scott Haven , Schwartz, John Anthony , Stein, Mark Morris , Wildonger, Richard Alan , Edwards, Philip Duke , Shaw, Andrew , Trainor, Diane Amy , Wolanin, Donald John
CPC分类号: C07C205/26 , A61K38/00 , C07C205/02 , C07C205/43 , C07K5/06191 , C07K5/0819 , C07K5/0827
摘要: The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae la, lb, lc set out hereinafter, and salts thereof, which are inhibitors of humanleukocyte elastase. Also described herein are pharmaceutical compositions containing apeptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.
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公开(公告)号:EP0189305B1
公开(公告)日:1992-07-29
申请号:EP86300379.4
申请日:1986-01-20
申请人: ICI AMERICAS INC.
发明人: Bergeson, Scott Haven , Schwartz, John Anthony , Stein, Mark Morris , Wildonger, Richard Alan , Edwards, Philip Duke , Shaw, Andrew , Trainor, Diane Amy , Wolanin, Donald John
CPC分类号: C07C205/26 , A61K38/00 , C07C205/02 , C07C205/43 , C07K5/06191 , C07K5/0819 , C07K5/0827
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公开(公告)号:EP0204571A3
公开(公告)日:1988-09-21
申请号:EP86304296
申请日:1986-06-05
申请人: ICI AMERICAS INC.
IPC分类号: C07C103/42 , C07K05/00 , C07C103/50 , C07C125/065 , A61K37/02 , A61K31/16 , A61K31/27 , C07D207/16
CPC分类号: C07K5/06191 , A61K38/00 , C07C271/16 , C07C271/18 , C07D207/16
摘要: The invention discloses a series of difluoroketone mono. di- and tri-peptide derivatives of the formula la, Ib and Ic:-
and salts thereof where appropriate, and wherein the radicals are defined hereafter in the specification. The derivatives are useful in inhibiting the action of human leukocyte elastase. There are also disclosed methods and intermediates for the manufacture of, and pharmaceutical compositions comprising, the said derivatives.-
公开(公告)号:EP0204571A2
公开(公告)日:1986-12-10
申请号:EP86304296.6
申请日:1986-06-05
申请人: ICI AMERICAS INC.
IPC分类号: C07C233/30 , C07K5/00 , C07C237/04 , C07C271/06 , A61K31/48 , A61K31/16 , A61K31/27 , C07D207/16
CPC分类号: C07K5/06191 , A61K38/00 , C07C271/16 , C07C271/18 , C07D207/16
摘要: The invention discloses a series of difluoroketone mono. di- and tri-peptide derivatives of the formula la, Ib and Ic:-
and salts thereof where appropriate, and wherein the radicals are defined hereafter in the specification. The derivatives are useful in inhibiting the action of human leukocyte elastase. There are also disclosed methods and intermediates for the manufacture of, and pharmaceutical compositions comprising, the said derivatives.摘要翻译: 本发明公开了一系列二氟酮单体。 式Ia,Ib和Ic的二肽和三肽衍生物: - 及其适当的盐,其中基团在下文中在说明书中定义。 该衍生物可用于抑制人类白细胞弹性蛋白酶的作用。 还公开了用于制造和包含所述衍生物的药物组合物的方法和中间体。
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公开(公告)号:EP0204571B1
公开(公告)日:1992-01-22
申请号:EP86304296.6
申请日:1986-06-05
申请人: ICI AMERICAS INC.
IPC分类号: C07C233/30 , C07K5/00 , C07C237/04 , C07C271/06 , A61K31/48 , A61K31/16 , A61K31/27 , C07D207/16
CPC分类号: C07K5/06191 , A61K38/00 , C07C271/16 , C07C271/18 , C07D207/16
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公开(公告)号:EP0276101A2
公开(公告)日:1988-07-27
申请号:EP88300343.6
申请日:1988-01-15
申请人: ICI AMERICAS INC.
CPC分类号: C07K5/06191 , A61K38/00
摘要: The invention provides a series of novel substituted peptide derivatives of the formulae la, Ib and Ic (set out hereinafter) and pharmaceutically acceptable salts thereof, in which the radicals A, R 1 , R 2 and R 4 -R 9 have the meanings defined in the following specification. The compounds of formulae la, Ib, and Ic are inhbitors of human leukocytic elastase. The invention also provides pharmaceutical compositions containing a compound of formula la, Ib or Ic, or a pharmaceutically acceptable salt thereof and processes and intermediates for the manufacture of compounds of formulae la, Ib, and Ic.
摘要翻译: 本发明提供了一系列新颖的式Ia,Ib和Ic的取代肽衍生物(下文阐述)
及其药学上可接受的盐,其中基团A,R 1,R 2和R 2, 4> -R 9具有以下说明书中定义的含义。 式Ia,Ib和Ic的化合物是人白细胞弹性蛋白酶的抑制剂。 本发明还提供含有式Ia,Ib或Ic化合物或其药学上可接受的盐的药物组合物和用于制备式Ia,Ib和Ic化合物的方法和中间体。
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