ATE77083T1 - Benzamide protease-inhibitoren. - Google Patents

Benzamide protease-inhibitoren.

Info

Publication number
ATE77083T1
ATE77083T1 AT89305142T AT89305142T ATE77083T1 AT E77083 T1 ATE77083 T1 AT E77083T1 AT 89305142 T AT89305142 T AT 89305142T AT 89305142 T AT89305142 T AT 89305142T AT E77083 T1 ATE77083 T1 AT E77083T1
Authority
AT
Austria
Prior art keywords
benzamide
protease inhibitors
het
chem
integer
Prior art date
Application number
AT89305142T
Other languages
English (en)
Inventor
Anton Franz Josef Fliri
Rodney Caughren Schnur
Original Assignee
Pfizer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer filed Critical Pfizer
Application granted granted Critical
Publication of ATE77083T1 publication Critical patent/ATE77083T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/40—Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C07D215/40—Nitrogen atoms attached in position 8
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/14—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/54—Nitrogen and either oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
AT89305142T 1988-05-24 1989-05-22 Benzamide protease-inhibitoren. ATE77083T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/197,927 US4874864A (en) 1988-05-24 1988-05-24 Benzamide protease inhibitors
EP89305142A EP0343894B1 (de) 1988-05-24 1989-05-22 Benzamide Protease-Inhibitoren

Publications (1)

Publication Number Publication Date
ATE77083T1 true ATE77083T1 (de) 1992-06-15

Family

ID=22731305

Family Applications (1)

Application Number Title Priority Date Filing Date
AT89305142T ATE77083T1 (de) 1988-05-24 1989-05-22 Benzamide protease-inhibitoren.

Country Status (19)

Country Link
US (1) US4874864A (de)
EP (1) EP0343894B1 (de)
JP (1) JPH0667905B2 (de)
KR (1) KR910004207B1 (de)
AT (1) ATE77083T1 (de)
AU (1) AU602294B2 (de)
DE (1) DE68901746T2 (de)
DK (1) DK249089A (de)
ES (1) ES2032229T3 (de)
FI (1) FI91254C (de)
GR (1) GR3005072T3 (de)
HU (1) HU201314B (de)
IE (1) IE61151B1 (de)
IL (1) IL90336A (de)
MY (1) MY104021A (de)
NO (1) NO173867C (de)
NZ (1) NZ229235A (de)
PT (1) PT90623B (de)
ZA (1) ZA893865B (de)

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JPH05201981A (ja) * 1991-08-06 1993-08-10 Ichikawa Gosei Kagaku Kk ２−アミノ−３−ニトロ−５−ハロゲノピリジン類の製造方法
US5726192A (en) * 1992-12-29 1998-03-10 Smithkline Beecham Corporation Platelet aggregation inhibiting compounds
FR2703995B1 (fr) * 1993-04-16 1995-07-21 Sanofi Elf 5-acylamino 1,2,4-thiadiazoles, leur preparation et compositions pharmaceutiques en contenant.
WO1995002586A1 (fr) * 1993-07-14 1995-01-26 Taisho Pharmaceutical Co., Ltd. Derive de 5-acetylthiazoline oxime
MX9605196A (es) * 1994-04-29 1997-12-31 Sanofi Winthrop Inc Halometilamidas como inhibidores de la proteasa il-1b.
CA2230209A1 (en) 1995-08-30 1997-03-06 G.D. Searle & Co. Meta-guanidine, urea, thiourea or azacyclic amino benzoic acid derivatives as integrin antagonists
US6100423A (en) * 1995-08-30 2000-08-08 G. D. Searle & Co. Amino benzenepropanoic acid compounds and derivatives thereof
AU727708B2 (en) * 1996-06-20 2000-12-21 Board Of Regents, The University Of Texas System Compounds and methods for providing pharmacologically active preparations and uses thereof
US6028087A (en) * 1998-01-21 2000-02-22 Smithkline Beecham Corporation Platelet aggregation inhibiting compounds
US6162791A (en) * 1998-03-02 2000-12-19 Apotex Inc. Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes
FR2783519B1 (fr) * 1998-09-23 2003-01-24 Sod Conseils Rech Applic Nouveaux derives d'amidines, leur preparation, leur application a titre de medicaments et les compositions pharmaceutiques les contenant
DZ3415A1 (fr) 2000-08-31 2002-03-07 Chiron Corp Guanidinobenzamides comme mc4-r agonistes.
DE60216747T2 (de) * 2001-04-09 2007-10-04 Novartis Vaccines and Diagnostics, Inc., Emeryville Guanidinoverbindungen als melanocortin-4-rezeptor (mc4-r) agonisten
ATE511840T1 (de) * 2001-10-09 2011-06-15 Amgen Inc Imidazolderivate als entzündungshemmende mittel
US20030207814A1 (en) * 2002-02-04 2003-11-06 Chiron Corporation Novel guanidinyl derivatives
US20050124652A1 (en) * 2002-02-04 2005-06-09 Rustum Boyce Guanidino compounds
US20030195187A1 (en) * 2002-02-04 2003-10-16 Chiron Corporation Guanidino compounds
US20070004743A1 (en) * 2002-02-25 2007-01-04 Xiao Linda L Intranasal administration of mc4-r agonists
US7034033B2 (en) * 2002-05-23 2006-04-25 Chiron Corporation Substituted quinazolinone compounds
WO2004014905A1 (en) * 2002-08-08 2004-02-19 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted benzimidazole compounds
DE10314761A1 (de) * 2003-03-31 2004-10-14 Basf Ag Als Katalysator für die Hydrocyanierung von olefinisch ungesättigten Verbindungen geeignetes System
AU2004249120B2 (en) * 2003-05-23 2008-07-24 Glaxosmithkline Guanidino-substituted quinazolinone compounds as MC4-R agonists
EP1686996A4 (de) * 2003-11-19 2008-11-12 Novartis Vaccines & Diagnostic Chinazolinon-verbindungen mit verringerter bioakkumulation
AU2008299781B2 (en) * 2007-08-03 2013-11-14 Romark Laboratories L.C. Alkylsulfonyl-substituted thiazolide compounds
CN102803203B (zh) 2009-05-12 2016-05-11 罗马克实验室有限公司 卤代烷基杂芳基苯甲酰胺化合物
CN108042535A (zh) 2009-06-26 2018-05-18 罗马克实验室有限公司 用于治疗流感的化合物和方法
KR20130108543A (ko) 2010-08-05 2013-10-04 암젠 인코포레이션 역형성 림프종 키나제를 억제하는 벤즈이미다졸 및 아자벤즈이미다졸 화합물

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Also Published As

Publication number Publication date
AU3509789A (en) 1989-11-30
NZ229235A (en) 1990-06-26
MY104021A (en) 1993-10-30
KR910004207B1 (ko) 1991-06-24
NO892058D0 (no) 1989-05-23
NO892058L (no) 1989-11-27
KR890017237A (ko) 1989-12-15
DE68901746D1 (de) 1992-07-16
US4874864A (en) 1989-10-17
AU602294B2 (en) 1990-10-04
FI91254C (fi) 1994-06-10
HU201314B (en) 1990-10-28
JPH0217177A (ja) 1990-01-22
NO173867C (no) 1994-02-16
FI91254B (fi) 1994-02-28
PT90623B (pt) 1994-10-31
DE68901746T2 (de) 1992-12-17
HUT49860A (en) 1989-11-28
ZA893865B (en) 1991-01-30
IE891668L (en) 1989-11-24
FI892497A (fi) 1989-11-25
IE61151B1 (en) 1994-10-05
ES2032229T3 (es) 1993-01-16
EP0343894A1 (de) 1989-11-29
EP0343894B1 (de) 1992-06-10
DK249089D0 (da) 1989-05-23
GR3005072T3 (de) 1993-05-24
JPH0667905B2 (ja) 1994-08-31
NO173867B (no) 1993-11-08
FI892497A0 (fi) 1989-05-23
IL90336A (en) 1993-01-31
DK249089A (da) 1989-11-27
PT90623A (pt) 1989-11-30

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