HUP9802764A2 - Guanidino-proteáz-inhibitorok - Google Patents

Guanidino-proteáz-inhibitorok

Info

Publication number
HUP9802764A2
HUP9802764A2 HU9802764A HUP9802764A HUP9802764A2 HU P9802764 A2 HUP9802764 A2 HU P9802764A2 HU 9802764 A HU9802764 A HU 9802764A HU P9802764 A HUP9802764 A HU P9802764A HU P9802764 A2 HUP9802764 A2 HU P9802764A2
Authority
HU
Hungary
Prior art keywords
alkyl
aryl
pipe powder
compounds
general formula
Prior art date
Application number
HU9802764A
Other languages
English (en)
Inventor
Roger F. Bone
Carl R. Illig
Tianbao Lu
Richard M. Soll
Nalin L. Subasinghe
Bruce E. Tomczuk
Original Assignee
3-Dimensional Pharmaceuticals, Inc.
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
Priority claimed from US08/698,401 external-priority patent/US5792769A/en
Application filed by 3-Dimensional Pharmaceuticals, Inc. filed Critical 3-Dimensional Pharmaceuticals, Inc.
Publication of HUP9802764A2 publication Critical patent/HUP9802764A2/hu
Publication of HUP9802764A3 publication Critical patent/HUP9802764A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/215—Radicals derived from nitrogen analogues of carbonic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/12—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/73—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/21—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms

Abstract

A találmány (I) általánős képletű vegyületekre vőnatkőzik - ahől aképletben a szűbsztitűensek főbb jelentései a következők: R1 jelentése alkilcsőpőrt, ciklőalkilcsőpőrt, arilcsőpőrt vagyheterőarilcsőpőrt, Z jelentése -NR10SO2-, -SO2NR10-, -OSO2-, -SO2O- vagy -CONR10- képletűcsőpőrt, ahől R10 jelentése hidrőgénatőm, alkilcsőpőrt, alkil-őxi-alkil-csőpőrt vagy arilcsőpőrt; R2, R3 és R4 jelentése hidrőgénatőm, alkilcsőpőrt, ciklőalkilcsőpőrt vagyarilcsőpőrt; Ra, Rb és Rc jelentése hidrőgénatőm, alkilcsőpőrt, hidrőxilcsőpőrt vagyalkőxicsőpőrt; Y jelentése -O-, -S- vagy kővalens kötés; W jelentése N vagy CR10; R7 és R8 jelentése hidrőgénatőm, alkilcsőpőrt, arilcsőpőrt vagy karbőxi-alkil-csőpőrt; m jelentése 0-tól 8-ig terjedő egész szám; és n jelentése 0-tól 4-ig terjedő egész szám. A (I) általánős képletű vegyületek számős prőteőlitikűs enzimetgátőlnak. A találmány az (I) általánős képletű vegyületek előállítására isvőnatkőzik. ŕ
HU9802764A 1995-09-29 1996-09-27 Guanidino protease inhibitors HUP9802764A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US53693995A 1995-09-29 1995-09-29
US08/698,401 US5792769A (en) 1995-09-29 1996-08-15 Guanidino protease inhibitors

Publications (2)

Publication Number Publication Date
HUP9802764A2 true HUP9802764A2 (hu) 1999-03-29
HUP9802764A3 HUP9802764A3 (en) 2000-03-28

Family

ID=27065321

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9802764A HUP9802764A3 (en) 1995-09-29 1996-09-27 Guanidino protease inhibitors

Country Status (15)

Country Link
EP (1) EP0859607B1 (hu)
JP (1) JPH11512722A (hu)
AT (1) ATE229800T1 (hu)
AU (1) AU714292C (hu)
BR (1) BR9610876A (hu)
CA (1) CA2233344A1 (hu)
CZ (1) CZ92298A3 (hu)
DE (1) DE69625505T2 (hu)
ES (1) ES2191109T3 (hu)
HU (1) HUP9802764A3 (hu)
IL (1) IL123802A0 (hu)
NO (1) NO981393L (hu)
NZ (1) NZ319474A (hu)
PL (1) PL325954A1 (hu)
WO (1) WO1997011693A1 (hu)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR19990076817A (ko) 1995-12-29 1999-10-15 3-디멘져널 파마슈티칼즈 인코오포레이티드 아미디노 프로테아제 억제제
SE9602646D0 (sv) 1996-07-04 1996-07-04 Astra Ab Pharmaceutically-useful compounds
TW499412B (en) 1996-11-26 2002-08-21 Dimensional Pharm Inc Aminoguanidines and alkoxyguanidines as protease inhibitors
JP2002510313A (ja) * 1997-06-26 2002-04-02 イーライ・リリー・アンド・カンパニー 抗血栓物質
DE69919349T2 (de) * 1998-03-23 2005-01-13 Aventis Pharmaceuticals Inc. Piperidinyl- und n-amidinopiperidinyl-derivate
US6344486B1 (en) 1998-04-03 2002-02-05 3-Dimensional Pharmaceuticals, Inc. Benzamide and sulfonamide substituted aminoguanidines and alkoxyguanidines as protease inhibitors
ATE461210T1 (de) 1998-06-11 2010-04-15 Ortho Mcneil Pharm Inc Pyrazine protease inhibitore
US6858598B1 (en) 1998-12-23 2005-02-22 G. D. Searle & Co. Method of using a matrix metalloproteinase inhibitor and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
CA2415932A1 (en) 2000-07-17 2002-01-24 3-Dimensional Pharmaceuticals, Inc. Cyclic oxyguanidine pyrazinones as protease inhibitors
CA2417914A1 (en) 2000-08-04 2002-02-14 3-Dimensional Pharmaceuticals, Inc. Cyclic oxyguanidine protease inhibitors
US6486174B2 (en) 2000-08-07 2002-11-26 3-Dimensional Pharmaceuticals, Inc. Tetrahydroisoquinoline-3-carboxylic acid alkoxyguanidines as integrin antagonists
UA75093C2 (en) 2000-10-06 2006-03-15 Dimensional Pharm Inc Aminopyridinyl-,aminoguanidinyl-, and alkoxyguanidinesubstituted phenylsubstituted phenylacetamides as protease inhibitors
DK1569912T3 (en) 2002-12-03 2015-06-29 Pharmacyclics Inc 2- (2-hydroxybiphenyl-3-yl) -1h-benzoimidazole-5-carboxamidine derivatives as factor VIIa inhibitors.

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3577432A (en) * 1968-12-23 1971-05-04 Robins Co Inc A H 1-substituted-3-phenoxypyrrolidines
JPS537436B2 (hu) * 1974-04-16 1978-03-17
US4433152A (en) * 1981-05-25 1984-02-21 Nippon Chemiphar Co., Ltd. Amidinopiperidine derivatives
TW201303B (hu) * 1990-07-05 1993-03-01 Hoffmann La Roche

Also Published As

Publication number Publication date
EP0859607A1 (en) 1998-08-26
IL123802A0 (en) 1998-10-30
EP0859607B1 (en) 2002-12-18
HUP9802764A3 (en) 2000-03-28
NO981393D0 (no) 1998-03-27
AU7201296A (en) 1997-04-17
BR9610876A (pt) 1999-07-13
NO981393L (no) 1998-05-25
CZ92298A3 (cs) 1998-07-15
AU714292C (en) 2001-11-01
AU714292B2 (en) 1999-12-23
CA2233344A1 (en) 1997-04-03
JPH11512722A (ja) 1999-11-02
WO1997011693A1 (en) 1997-04-03
EP0859607A4 (en) 1999-05-06
DE69625505T2 (de) 2003-11-13
DE69625505D1 (de) 2003-01-30
NZ319474A (en) 2000-01-28
PL325954A1 (en) 1998-08-17
ATE229800T1 (de) 2003-01-15
ES2191109T3 (es) 2003-09-01

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