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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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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：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：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：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：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：US4227004A
公开(公告)日：1980-10-07
申请号：US450
申请日：1979-01-02
申请人： Richard A. Wildonger
发明人： Richard A. Wildonger
IPC分类号： C07D249/04
CPC分类号： C07D249/04
摘要： Substituted 1-aralkyl-1H-v-triazoles are prepared from a suitable 1-aralkyl-1H-v-triazole by a process comprising an alkylation step and dependent on the product desired suitably followed by an oxidation step and decarboxylation step.
摘要翻译： 通过包括烷基化步骤的方法由合适的1-芳烷基-1H-v-三唑制备取代的1-芳烷基-1H-v-三唑，并依赖于所需的产物，随后进行氧化步骤和脱羧步骤。
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公开(公告)号：US4364948A
公开(公告)日：1982-12-21
申请号：US306481
申请日：1981-09-28
IPC分类号： A61K31/435 , A61P25/20 , C07D209/48 , C07D317/28 , C07D405/06 , C07D471/04 , A61K31/44
CPC分类号： C07D209/49 , C07C255/00 , C07D317/28 , C07D405/06 , C07D471/04
摘要： Certain pyrazolo[3,4-b]pyridine compounds which are useful for their activity in the central nervous system of warm-blooded animals, of the following formula (I) ##STR1## wherein R.sub.1 is lower alkyl;R.sub.a is hydrogen and R.sub.b is hydroxy or R.sub.a and R.sub.b combine to form a .dbd.O group;R.sub.5 is hydrogen or lower alkyl; andR.sub.6 is lower alkyl,and the pharmaceutically-acceptable salts thereof.
摘要翻译： 可用于其在温血动物的中枢神经系统中的活性的某些吡唑并[3,4-b]吡啶化合物，其具有下式（I）其中R 1为低级烷基; R a是氢，R b是羟基或R a和R b结合形成a = O基团; R5是氢或低级烷基; 和R6是低级烷基，及其药学上可接受的盐。
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