PL327185A1 - Thyrosine derivatives as inhibitors of integrin-alpha v - Google Patents

Thyrosine derivatives as inhibitors of integrin-alpha v

Info

Publication number
PL327185A1
PL327185A1 PL96327185A PL32718596A PL327185A1 PL 327185 A1 PL327185 A1 PL 327185A1 PL 96327185 A PL96327185 A PL 96327185A PL 32718596 A PL32718596 A PL 32718596A PL 327185 A1 PL327185 A1 PL 327185A1
Authority
PL
Poland
Prior art keywords
thyrosine
integrin
inhibitors
alpha
derivatives
Prior art date
Application number
PL96327185A
Inventor
Beate Diefenbach
Claus Fittschen
Joachim Gante
Simon Goodman
Matthias Wiesner
Friedrich Rippmann
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
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of PL327185A1 publication Critical patent/PL327185A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • 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
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C247/00Compounds containing azido groups
    • C07C247/02Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C247/04Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being saturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • C07C271/28Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04Derivatives 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
    • C07C279/08Derivatives 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 singly-bound oxygen atoms
    • 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
PL96327185A 1995-12-23 1996-12-16 Thyrosine derivatives as inhibitors of integrin-alpha v PL327185A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19548709A DE19548709A1 (en) 1995-12-23 1995-12-23 Tyrosine derivatives
PCT/EP1996/005646 WO1997023451A1 (en) 1995-12-23 1996-12-16 Tyrosin-derivate as alpha-v-integrin inhibitors

Publications (1)

Publication Number Publication Date
PL327185A1 true PL327185A1 (en) 1998-11-23

Family

ID=7781401

Family Applications (1)

Application Number Title Priority Date Filing Date
PL96327185A PL327185A1 (en) 1995-12-23 1996-12-16 Thyrosine derivatives as inhibitors of integrin-alpha v

Country Status (14)

Country Link
EP (1) EP0879227A1 (en)
JP (1) JP2000502664A (en)
KR (1) KR19990076676A (en)
AU (1) AU1301697A (en)
BR (1) BR9612201A (en)
CA (1) CA2241149A1 (en)
CZ (1) CZ195198A3 (en)
DE (1) DE19548709A1 (en)
HU (1) HUP9903716A2 (en)
NO (1) NO982907L (en)
PL (1) PL327185A1 (en)
SK (1) SK78398A3 (en)
WO (1) WO1997023451A1 (en)
ZA (1) ZA9610725B (en)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19629816A1 (en) 1996-07-24 1998-01-29 Hoechst Ag New cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists
US5900414A (en) * 1996-08-29 1999-05-04 Merck & Co., Inc. Methods for administering integrin receptor antagonists
CA2272090A1 (en) * 1996-12-09 1998-06-18 Matthew J. Fisher Integrin antagonists
US6245809B1 (en) 1996-12-09 2001-06-12 Cor Therapeutics Inc. Integrin antagonists
US6559144B2 (en) 1997-02-13 2003-05-06 Merck Patent Gesellschaft Mit Bicyclic amino acids
DE19705450A1 (en) * 1997-02-13 1998-08-20 Merck Patent Gmbh Bicyclic aromatic amino acids
US6455550B1 (en) 1997-08-22 2002-09-24 Hoffmann-La Roche Inc. N-alkanoylphenylalanine derivatives
BR9811730B1 (en) * 1997-08-22 2014-04-08 Hoffmann La Roche N-AROYLPHENYLALANINE DERIVATIVES, USE OF THE SAME, MEDICINAL PRODUCTS CONTAINING THE SAME.
JP3727536B2 (en) * 1997-08-22 2005-12-14 エフ.ホフマン−ラ ロシュ アーゲー N-alkanoylphenylalanine derivatives
AU759449C (en) 1998-04-09 2003-10-30 Meiji Seika Pharma Co.,Ltd. Aminopiperidine derivatives as integrin alpha v beta 3 antagonists
WO2000006158A1 (en) * 1998-07-31 2000-02-10 Eli Lilly And Company Heterocyclyl sulphonamide derivatives
DE19842415A1 (en) * 1998-09-16 2000-03-23 Merck Patent Gmbh Pharmaceutical preparation for treating e.g. tumors, thrombosis or inflammation, contains cyclic pentapeptide integrin inhibitor and chemotherapeutic agent and/or angiogenesis inhibitor
US6677360B2 (en) 1998-12-16 2004-01-13 Bayer Aktiengesellschaft Biphenyl and biphenyl-analogous compounds as integrin antagonists
AU761407B2 (en) * 1998-12-16 2003-06-05 Bayer Aktiengesellschaft New biphenyl and biphenyl-analogous compounds as integrin antagonists
US6833373B1 (en) 1998-12-23 2004-12-21 G.D. Searle & Co. Method of using an integrin antagonist and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
DE60043692D1 (en) 1999-01-22 2010-03-04 Elan Pharm Inc ACYL DERIVATIVES FOR THE TREATMENT OF DISEASES RELATED TO VLA-4
AU2623900A (en) * 1999-01-22 2000-08-07 American Home Products Corporation Compounds which inhibit leukocyte adhesion mediated by vla-4
CA2359112A1 (en) 1999-01-22 2000-07-27 Elan Pharmaceuticals, Inc. 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
RU2245874C2 (en) 1999-02-18 2005-02-10 Ф.Хоффман-Ля Рош Аг Derivatives of thioamide and pharmaceutical composition
CA2361162A1 (en) 1999-03-01 2000-09-08 Elan Pharmaceuticals, Inc. Alpha-aminoacetic acid derivatives useful as alpha 4 beta 7-receptor antagonists
CA2368049A1 (en) 1999-04-13 2000-10-19 Basf Aktiengesellschaft Integrin receptor ligands
EP1209152A4 (en) 1999-08-05 2003-03-12 Meiji Seika Kaisha Omega-amino-alpha-hydroxycarboxylic acid derivatives having integrin alpha v beta 3 antagonism
DE60021521T4 (en) 1999-09-29 2006-09-21 Ortho-Mcneil Pharmaceutical, Inc. ISONIPECOTAMIDE FOR THE TREATMENT OF INTEGRIN-MEDIATED INTERFERENCE
US6531495B1 (en) 1999-10-02 2003-03-11 Aventis Pharma Deutschland Gmbh 2′-Substituted 1,1′-biphenyl-2-carboxamides, processes for their preparation, their use as medicaments, and pharmaceutical preparations comprising them
AU781747B2 (en) * 1999-10-08 2005-06-09 Meiji Seika Kaisha Ltd. 3-aminopiperidine derivatives as integrin alphavbeta3 antagonists
US20020037897A1 (en) * 2000-08-07 2002-03-28 3-Dimensional Pharmaceuticals, Inc. Tetrahydroisoquinoline-3-carboxylic acid alkoxyguanidines as integrin antagonists
US6486174B2 (en) 2000-08-07 2002-11-26 3-Dimensional Pharmaceuticals, Inc. Tetrahydroisoquinoline-3-carboxylic acid alkoxyguanidines as integrin antagonists
NZ539682A (en) 2001-01-29 2006-03-31 Dimensional Pharm Inc Substituted indoles and their use as integrin antagonists
FR2822827B1 (en) * 2001-03-28 2003-05-16 Sanofi Synthelabo NOVEL N- (ARYLSULFONYL) BETA-AMINOACIDS DERIVATIVES COMPRISING A SUBSTITUTED AMINOMETHYL GROUP, THEIR PREPARATION METHOD AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
WO2002081467A1 (en) 2001-04-09 2002-10-17 Ortho-Mcneil Pharmaceutical, Inc. Quinazoline and quinazoline-like compounds for the treatment of integrin-mediated disorders
US6872730B2 (en) 2001-04-27 2005-03-29 3-Dimensional Pharmaceuticals, Inc. Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists
WO2003008373A1 (en) * 2001-07-19 2003-01-30 Merck Patent Gmbh Tyrosine hydrazides
TWI281470B (en) 2002-05-24 2007-05-21 Elan Pharm Inc Heterocyclic compounds which inhibit leukocyte adhesion mediated by alpha4 integrins
TW200307671A (en) 2002-05-24 2003-12-16 Elan Pharm Inc Heteroaryl compounds which inhibit leukocyte adhesion mediated by α 4 integrins
JP5101512B2 (en) 2005-09-29 2012-12-19 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 Pyrimidinylamide compounds that inhibit leukocyte adhesion mediated by VLA-4
CN101273035A (en) 2005-09-29 2008-09-24 伊兰制药公司 Carbamate compounds which inhibit leukocyte adhesion mediated by VLA-4
NZ570679A (en) 2006-02-27 2011-01-28 Elan Pharm Inc Pyrimidinyl sulfonamide compounds which inhibit leukocyte adhesion mediated By VLA-4
SG175355A1 (en) 2009-04-27 2011-12-29 Elan Pharm Inc Pyridinone antagonists of alpha-4 integrins
WO2012103328A1 (en) * 2011-01-26 2012-08-02 The Methodist Hospital Research Institute Labeled, non- peptidic multivalent integrin alpha -v - beta - 3 antagonists, compositions containing them and their use

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ239846A (en) * 1990-09-27 1994-11-25 Merck & Co Inc Sulphonamide derivatives and pharmaceutical compositions thereof
IL99537A (en) * 1990-09-27 1995-11-27 Merck & Co Inc Fibrinogen receptor antagonists and pharmaceutical compositions containing them

Also Published As

Publication number Publication date
AU1301697A (en) 1997-07-17
WO1997023451A1 (en) 1997-07-03
MX9804971A (en) 1998-09-30
NO982907D0 (en) 1998-06-22
SK78398A3 (en) 1998-11-04
ZA9610725B (en) 1997-06-26
DE19548709A1 (en) 1997-07-03
BR9612201A (en) 1999-07-13
CA2241149A1 (en) 1997-07-03
NO982907L (en) 1998-06-22
CZ195198A3 (en) 1998-11-11
KR19990076676A (en) 1999-10-15
EP0879227A1 (en) 1998-11-25
JP2000502664A (en) 2000-03-07
HUP9903716A2 (en) 2000-03-28

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