NO986090L - Phenylalanine derivatives as integrin inhibitors - Google Patents

Phenylalanine derivatives as integrin inhibitors

Info

Publication number
NO986090L
NO986090L NO986090A NO986090A NO986090L NO 986090 L NO986090 L NO 986090L NO 986090 A NO986090 A NO 986090A NO 986090 A NO986090 A NO 986090A NO 986090 L NO986090 L NO 986090L
Authority
NO
Norway
Prior art keywords
integrin inhibitors
phenylalanine derivatives
disseminated
arteriosclerosis
thrombosis
Prior art date
Application number
NO986090A
Other languages
Norwegian (no)
Other versions
NO986090D0 (en
Inventor
Beate Diefenbach
Claus Fittschen
Simon Goodman
Joachim Morz
Peter Raddatz
Matthias Wiesner
Soheila Anzali
Original Assignee
Merck Patent Gmbh
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 DE19654483A external-priority patent/DE19654483A1/en
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of NO986090L publication Critical patent/NO986090L/en
Publication of NO986090D0 publication Critical patent/NO986090D0/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic 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
    • C07D277/32Heterocyclic 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
    • C07D277/38Nitrogen atoms
    • C07D277/44Acylated amino or imino radicals
    • C07D277/46Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/01Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/06Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/14Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides 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 hydrogen atoms or to an acyclic carbon atom
    • C07C311/19Sulfonamides 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 hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
    • C07D231/38Nitrogen atoms
    • C07D231/40Acylated on said nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic 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
    • C07D233/66Heterocyclic 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
    • C07D233/88Nitrogen atoms, e.g. allantoin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; 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
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D257/00Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04Five-membered rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Forbindelser med formel (I) hvor X, Y, Z, R1, R2, R3 og R4 har betydningene angitt i krav l, med det forbehold at minst ett element valgt fra gruppen X, Y, Z må være CH2, samt deres fysiologisk ufarlige salter, kan anvendes som integrininhibitorer, særlig for profylakse og behandling av blodomløpssykdommer, ved trombose, hjerteinfarkt, koronare hjertesyk- dommer, arteriosklerose, osteoporose, ved patologiske prosesser som opp- rettholdes eller spres ved angiogenese, og ved tumorterapi.Compounds of formula (I) wherein X, Y, Z, R1, R2, R3 and R4 have the meanings set forth in claim 1, with the proviso that at least one element selected from the group X, Y, Z must be CH2, as well as their physiologically harmless salts, can be used as integrin inhibitors, in particular for the prophylaxis and treatment of circulatory disorders, in thrombosis, myocardial infarction, coronary heart disease, arteriosclerosis, osteoporosis, in pathological processes maintained or disseminated by angiogenesis, and in tumor therapy.

NO986090A 1996-06-28 1998-12-23 Phenylalanine derivatives as integrin inhibitors NO986090D0 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE19625929 1996-06-28
DE19654483A DE19654483A1 (en) 1996-06-28 1996-12-27 Phenylalanine derivatives
PCT/EP1997/003275 WO1998000395A1 (en) 1996-06-28 1997-06-23 Phenylalamine derivatives as integrin inhibitors

Publications (2)

Publication Number Publication Date
NO986090L true NO986090L (en) 1998-12-23
NO986090D0 NO986090D0 (en) 1998-12-23

Family

ID=26027004

Family Applications (1)

Application Number Title Priority Date Filing Date
NO986090A NO986090D0 (en) 1996-06-28 1998-12-23 Phenylalanine derivatives as integrin inhibitors

Country Status (10)

Country Link
EP (1) EP0907637A1 (en)
JP (1) JP2000516575A (en)
KR (1) KR20000022190A (en)
AU (1) AU3343097A (en)
CA (1) CA2259224A1 (en)
CZ (1) CZ424998A3 (en)
NO (1) NO986090D0 (en)
PL (1) PL330915A1 (en)
SK (1) SK176898A3 (en)
WO (1) WO1998000395A1 (en)

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DE19705450A1 (en) * 1997-02-13 1998-08-20 Merck Patent Gmbh Bicyclic aromatic amino acids
US6197794B1 (en) 1998-01-08 2001-03-06 Celltech Therapeutics Limited Phenylalanine derivatives
US6313119B1 (en) 1998-01-23 2001-11-06 Adventis Pharma Deutschland Gmbh Sulfonamide derivatives as inhibitors of bone resorption and as inhibitors of cell adhesion
US6329372B1 (en) 1998-01-27 2001-12-11 Celltech Therapeutics Limited Phenylalanine derivatives
JP2002504534A (en) * 1998-02-26 2002-02-12 セルテック・セラピューティクス・リミテッド Phenylalanine derivatives as inhibitors of α4 integrin
GB9805655D0 (en) 1998-03-16 1998-05-13 Celltech Therapeutics Ltd Chemical compounds
US6521626B1 (en) 1998-03-24 2003-02-18 Celltech R&D Limited Thiocarboxamide derivatives
GB9811159D0 (en) 1998-05-22 1998-07-22 Celltech Therapeutics Ltd Chemical compounds
GB9811969D0 (en) 1998-06-03 1998-07-29 Celltech Therapeutics Ltd Chemical compounds
GB9812088D0 (en) * 1998-06-05 1998-08-05 Celltech Therapeutics Ltd Chemical compounds
GB9814414D0 (en) 1998-07-03 1998-09-02 Celltech Therapeutics Ltd Chemical compounds
GB9821061D0 (en) 1998-09-28 1998-11-18 Celltech Therapeutics Ltd Chemical compounds
GB9821222D0 (en) 1998-09-30 1998-11-25 Celltech Therapeutics Ltd Chemical compounds
GB9825652D0 (en) 1998-11-23 1999-01-13 Celltech Therapeutics Ltd Chemical compounds
GB9826174D0 (en) * 1998-11-30 1999-01-20 Celltech Therapeutics Ltd Chemical compounds
US6677360B2 (en) 1998-12-16 2004-01-13 Bayer Aktiengesellschaft Biphenyl and biphenyl-analogous compounds as integrin antagonists
KR20010086112A (en) * 1998-12-16 2001-09-07 빌프리더 하이더 New Biphenyl and Biphenyl-analogous Compounds as Integrin Antagonists
US6291503B1 (en) 1999-01-15 2001-09-18 Bayer Aktiengesellschaft β-phenylalanine derivatives as integrin antagonists
DK1144388T3 (en) 1999-01-22 2010-05-25 Elan Pharm Inc Acyl derivatives that treat VLA-4-related disorders
CN1336921A (en) 1999-01-22 2002-02-20 依兰制药公司 Fused ring heteroaryl and heterocyclic compounds which inhibit leukocyte adhesion mediated by VLA-4
US6436904B1 (en) 1999-01-25 2002-08-20 Elan Pharmaceuticals, Inc. Compounds which inhibit leukocyte adhesion mediated by VLA-4
US6344484B1 (en) 1999-02-12 2002-02-05 3-Dimensional Pharmaceuticals, Inc. Tyrosine alkoxyguanidines as integrin inhibitors
EP1028114A1 (en) * 1999-02-13 2000-08-16 Aventis Pharma Deutschland GmbH Novel guanidine derivatives as inhibitors of cell adhesion
JP2002538135A (en) 1999-03-01 2002-11-12 エラン ファーマシューティカルズ,インコーポレイテッド α-aminoacetic acid derivatives useful as α4β7 receptor antagonists
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Also Published As

Publication number Publication date
PL330915A1 (en) 1999-06-07
CA2259224A1 (en) 1998-01-08
EP0907637A1 (en) 1999-04-14
WO1998000395A1 (en) 1998-01-08
CZ424998A3 (en) 1999-03-17
NO986090D0 (en) 1998-12-23
AU3343097A (en) 1998-01-21
JP2000516575A (en) 2000-12-12
SK176898A3 (en) 1999-05-07
KR20000022190A (en) 2000-04-25

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