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公开(公告)号：US4596789A
公开(公告)日：1986-06-24
申请号：US603408
申请日：1984-04-24
IPC分类号： A61K38/00 , C07K5/065 , C07K5/068 , C07K5/083 , C07K5/087 , C07K5/09 , C07K5/107 , C07K5/11 , A61K37/00
CPC分类号： C07K5/1019 , C07K5/06078 , C07K5/06086 , C07K5/0808 , C07K5/0812 , C07K5/0815 , C07K5/1016 , A61K38/00
摘要： Proline derivatives of the formulae: ##STR1## wherein R.sup.1 through R.sup.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.
摘要翻译： 脯氨酸衍生物如下：其中R1至R11具有定义的值，其酸和碱加成盐和平衡物的平衡（ⅰ）
（II） 加成其醛基的化合物; 其准备过程; 药物组合物; 和用于制备所述脯氨酸衍生物的中间体。 脯氨酸衍生物是人白细胞弹性蛋白酶抑制剂，其可用于例如治疗肺气肿。 -
公开(公告)号：US4691007A
公开(公告)日：1987-09-01
申请号：US806265
申请日：1985-12-06
IPC分类号： A61K38/00 , C07K5/065 , C07K5/068 , C07K5/083 , C07K5/087 , C07K5/09 , C07K5/107 , C07K5/11 , C07C103/52 , A61K37/02 , C07D207/00
CPC分类号： C07K5/1019 , C07K5/06078 , C07K5/06086 , C07K5/0808 , C07K5/0812 , C07K5/0815 , C07K5/1016 , A61K38/00
摘要： Proline derivatives of the formulae: ##STR1## wherein R.sup.1 through R.sup.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.
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公开(公告)号：US5194588A
公开(公告)日：1993-03-16
申请号：US491757
申请日：1990-03-09
IPC分类号： A61K38/00 , C07C205/02 , C07C205/26 , C07C205/43 , C07K5/06 , C07K5/08 , C07K5/093
CPC分类号： C07C205/26 , C07C205/02 , C07C205/43 , C07K5/06191 , C07K5/0819 , C07K5/0827 , A61K38/00
摘要： The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae Ia, Ib, Ic set out hereinafter, and salts thereof, which are inhibitors of human leukocyte elastase. Also described herein are pharmaceutical compositions containing a peptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.
摘要翻译： 本发明涉及作为人白细胞弹性蛋白酶抑制剂的药学上有用的三氟甲基酮取代的下式Ia，Ib和Ic的二，三和四肽衍生物及其盐。 本文还描述了含有肽衍生物的药物组合物和用于制备肽衍生物的方法和中间体。
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公开(公告)号：US5164371A
公开(公告)日：1992-11-17
申请号：US193317
申请日：1988-05-11
申请人： Philip D. Edwards , Joseph J. Lewis , Charles W. Perkins , Diane A. Trainor , Richard A. Wildonger
发明人： Philip D. Edwards , Joseph J. Lewis , Charles W. Perkins , Diane A. Trainor , Richard A. Wildonger
IPC分类号： A61K38/55 , A61K31/422 , A61K31/423 , A61K31/428 , A61P7/00 , A61P11/00 , A61P29/00 , C07D207/04 , C07D263/00 , C07D413/12 , C07D417/12 , C07K1/02 , C07K1/06 , C07K1/113 , C07K5/00 , C07K5/06 , C07K5/062 , C07K5/08 , C07K14/81 , C12N9/99
CPC分类号： C07K5/06052 , C07K5/06191
摘要： The invention provides a series of novel heterocyclic ketones of formula I ##STR1## and pharmaceutically acceptable base-addition salts thereof, in which the values of R.sup.4, L, A, X and Q have the meanings defined in the following specification. The compounds of formula I are inhibitors of human leukocytic elastase. The invention also provides pharmaceutical compositions containing a compound of formula I, or a pharmaceutically acceptable base-addition salt thereof, and processes and intermediates for the manufacture of compounds of formula I.
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公开(公告)号：US5055450A
公开(公告)日：1991-10-08
申请号：US493025
申请日：1990-03-13
IPC分类号： A61K38/00 , C07C205/02 , C07C205/26 , C07C205/43 , C07K5/06 , C07K5/08 , C07K5/093
CPC分类号： C07K5/0819 , C07C205/02 , C07C205/26 , C07C205/43 , C07K5/06191 , C07K5/0827 , A61K38/00
摘要： The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae Ia, Ib, Ic set out hereinafter, and salts thereof, which are inhibitors of human leukocyte elastase. Also described herein are pharmaceutical compositions containing a peptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.
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公开(公告)号：US4910190A
公开(公告)日：1990-03-20
申请号：US5538
申请日：1987-01-20
申请人： Scott H. Bergeson , Philip D. Edwards , John A. Schwartz , Andrew Shaw , Mark M. Stein , Diane A. Trainor , Richard A. Wildonger , Donald J. Wolanin
发明人： Scott H. Bergeson , Philip D. Edwards , John A. Schwartz , Andrew Shaw , Mark M. Stein , Diane A. Trainor , Richard A. Wildonger , Donald J. Wolanin
IPC分类号： A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/4433 , A61K31/535 , A61K38/00 , A61K38/55 , A61P9/10 , A61P11/00 , A61P29/00 , A61P43/00 , C07C205/02 , C07C205/26 , C07C205/43 , C07D207/16 , C07D213/26 , C07D333/00 , C07D401/12 , C07D403/12 , C07D409/12 , C07K1/113 , C07K5/04 , C07K5/06 , C07K5/08 , C07K5/093 , C07K14/81 , C12N9/99
CPC分类号： C07C205/26 , C07C205/02 , C07C205/43 , C07K5/06191 , C07K5/0819 , C07K5/0827 , A61K38/00
摘要： The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae Ia, Ib, Ic set out hereinafter, and salts thereof, which are inhibitors of human leukocyte elastase. Also described herein are pharmaceutical compositions containing a peptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.
摘要翻译： 本发明涉及作为人白细胞弹性蛋白酶抑制剂的药学上有用的三氟甲基酮取代的下式Ia，Ib和Ic的二，三和四肽衍生物及其盐。 本文还描述了含有肽衍生物的药物组合物和用于制备肽衍生物的方法和中间体。
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7.发明授权Certain N(4-benzoyl-2-phenyl)-3- trifluoro-2-hydroxy-propanamide derivatives 失效某些N（4-苯甲酰基-2-苯基）-3-三氟-2-羟基 - 丙酰胺衍生物
公开(公告)号：US5482969A
公开(公告)日：1996-01-09
申请号：US212460
申请日：1994-03-11
申请人： James R. Empfield , Cyrus J. Ohnmacht , Keith Russell , Diane A. Trainor , Paul J. Warwick, Jr.
发明人： James R. Empfield , Cyrus J. Ohnmacht , Keith Russell , Diane A. Trainor , Paul J. Warwick, Jr.
IPC分类号： A61K31/165 , A61K31/275 , A61K31/44 , A61K31/4409 , A61P13/02 , A61P15/00 , C07C233/75 , C07C235/16 , C07C255/49 , C07C255/60 , C07C317/40 , C07D213/71 , C07D237/14 , C07D237/18 , C07D237/20 , C07D239/34 , C07D239/38 , C07D239/42 , C07D241/18 , C07D241/20 , C07C51/255 , A61K31/16 , C07C233/01 , C07C237/20
CPC分类号： C07C235/16 , C07C255/60 , C07C317/40 , C07D213/71
摘要： Compounds of formula I: ##STR1## wherein, ring C, A-B, R.sup.1, n, R.sup.2, and R.sup.3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
摘要翻译： 式I化合物：其中环C，A-B，R 1，n，R 2和R 3具有本说明书中给出的任何含义，其药学上可接受的盐可用于治疗尿失禁。 还公开了药物组合物，制备式I化合物和中间体的方法。
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公开(公告)号：US4880780A
公开(公告)日：1989-11-14
申请号：US58079
申请日：1987-06-04
申请人： Diane A. Trainor , Mark M. Stein
发明人： Diane A. Trainor , Mark M. Stein
IPC分类号： C07K14/81 , A61K31/16 , A61K31/27 , A61K31/48 , A61K38/00 , A61K38/55 , A61P43/00 , C07C67/00 , C07C233/30 , C07C233/31 , C07C233/45 , C07C233/47 , C07C237/04 , C07C237/06 , C07C239/00 , C07C269/00 , C07C271/06 , C07C271/16 , C07C271/18 , C07C275/04 , C07C301/00 , C07C303/02 , C07C303/40 , C07C311/00 , C07D207/16 , C07D233/60 , C07K1/113 , C07K5/00 , C07K5/06
CPC分类号： C07K5/06191 , C07C271/16 , C07C271/18 , C07D207/16 , A61K38/00
摘要： The invention discloses a series of difluoroketone, mono- di- and tri-peptide derivatives of formula Ia, Ib and Ic:______________________________________ (Formula set out on pages following Examples) Ia (Formula set out on pages following Examples) Ib (Formula set out on pages following Examples) 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式Ia，Ib和Ic的二氟酮，一 - 和三 - 肽衍生物： - （在实施例之后的页面上列出的配方）Ia-（在实施例之后的页面上列出的配方）Ib-（式 列于以下实施例的页面）Ic-及其盐，并且其中基团在下文在说明书中定义。 该衍生物可用于抑制人白细胞弹性蛋白酶的作用。 还公开了用于制备所述衍生物的方法和中间体以及包含所述衍生物的药物组合物。
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公开(公告)号：US5550136A
公开(公告)日：1996-08-27
申请号：US374053
申请日：1995-01-19
IPC分类号： A61K31/445 , A61K31/4427 , A61K31/4465 , A61K31/454 , A61K31/4545 , A61P25/18 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/36 , C07D401/06 , C07D417/06 , A61K34/445
CPC分类号： C07D401/06 , C07D211/22 , C07D211/32 , C07D417/06
摘要： Compounds of formula I ##STR1## wherein X and Y are H or halo; R.sup.2 is: [structures Ia, Ib or Ic;] ##STR2## R.sup.3 is selected from unsubstituted or substituted alkyl, aryl or heteroaryl groups;R.sup.4 is selected from H or (C1-6)alkyl,and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disoders such as psychoses; pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropschiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective mount of a compound of formula I, or a pharmaceutically acceptable salt thereof.
摘要翻译： 式I的化合物其中X和Y是H或卤素; R 2是：[未取代或取代的烷基，芳基或杂芳基]中选择的结构：[结构Ia，Ib或Ic;]
R4选自H或（C 1-6）烷基及其药学上可接受的盐，可用于治疗精神病学等神经精神病学解码器; 包含式I化合物和药学上可接受的稀释剂或载体的药物组合物; 以及治疗神经精神障碍的方法，其包括向需要这种治疗的哺乳动物（包括人）施用有效装载式I化合物或其药学上可接受的盐。 -
公开(公告)号：US5484792A
公开(公告)日：1996-01-16
申请号：US193346
申请日：1994-02-08
IPC分类号： A61K31/435 , A61K31/473 , A61P13/02 , A61P13/06 , A61P13/10 , A61P15/00 , C07D20060101 , C07D219/06 , C07D401/04 , C07D405/04 , C07D409/04 , C07D409/14 , A61K31/425
CPC分类号： C07D401/04 , C07D219/06 , C07D405/04 , C07D409/04
摘要： Compounds of general formula I, ##STR1## and pharmaceutically acceptable salts thereof, in which R.sup.1 has any of the meanings given in the specification, pharmaceutical compositions comprising them and their use in the treatment of urinary incontinence.
摘要翻译： 通式Ⅰ的化合物及其药学上可接受的盐，其中R1具有本说明书中给出的任何含义，包含它们的药物组合物及其在治疗尿失禁中的用途。
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