NO982907L - Tyrosine derivatives as <alfa> -v integrin inhibitors - Google Patents

Tyrosine derivatives as <alfa> -v integrin inhibitors

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Publication number
NO982907L
NO982907L NO982907A NO982907A NO982907L NO 982907 L NO982907 L NO 982907L NO 982907 A NO982907 A NO 982907A NO 982907 A NO982907 A NO 982907A NO 982907 L NO982907 L NO 982907L
Authority
NO
Norway
Prior art keywords
integrin inhibitors
tyrosine derivatives
alfa
atoms
independently
Prior art date
Application number
NO982907A
Other languages
Norwegian (no)
Other versions
NO982907D0 (en
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 NO982907L publication Critical patent/NO982907L/en
Publication of NO982907D0 publication Critical patent/NO982907D0/en

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    • 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
    • C07D211/36—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 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C247/00—Compounds containing azido groups
    • C07C247/02—Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C247/04—Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26—Esters 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
    • C07C271/28—Esters 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
    • 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
    • C07C279/08—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 singly-bound oxygen atoms
    • 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
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides 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
    • C07C311/06—Sulfonamides 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
    • 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
    • C07C311/14—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of rings other than 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
    • C07C311/16—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 hydrogen atoms or to an acyclic carbon atom
    • C07C311/19—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 hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Diabetes (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)

Abstract

Tyrosinderivater som a-v-integrininhibitorer Forbindelser med formel (I) hvor X er alkylen med 1-6 C-atomer eller l,4-piperidyl; Y mangler eller er O, CONH eller -C=C-; R1 er H, CN, N3, NH2, H2N-C(=NH) eller H2N-C(=NH)-NH, idet de primære aminogruppene også kan være forsynt med vanlige aminobeskyt- telsesgrupper; R2, R3 er uavhengig av hverandre H, A, A-S02-, Ar-S02-, kamfer-10-S02-, COOA eller en vanlig aminobeskyttelsesgruppe; A, R4 er uavhengig av hverandre H eller alkyl med 1-10 C-atomer; og Ar er usubsti- tuert eller en gang med CH3 substituert fenyl eller benzyl, samt deres fysio- logisk akseptable salter, kan anvendes som av-integrininhibitorer, særlig for behandling av tumorsykdommer, osteo- poroser, osteolytiske sykdommer samt til undertrykkelse av angiogenese.Tyrosine derivatives as α-v integrin inhibitors Compounds of formula (I) wherein X is alkylene having 1-6 C atoms or 1,4-piperidyl; Y is missing or is O, CONH or -C = C-; R1 is H, CN, N3, NH2, H2N-C (= NH) or H2N-C (= NH) -NH, the primary amino groups also being provided with conventional amino protecting groups; R2, R3 are independently H, A, A-SO2-, Ar-SO2-, camphor-10-SO2-, COOA or a common amino protecting group; A, R4 are independently H or alkyl of 1-10 C atoms; and Ar is unsubstituted or once with CH 3 substituted phenyl or benzyl, as well as their physiologically acceptable salts, can be used as de-integrin inhibitors, especially for the treatment of tumor diseases, osteoporoses, osteolytic diseases and for suppression of angiogenesis.

NO982907A 1995-12-23 1998-06-22 Tyrosine derivatives as <alfa> -v integrin inhibitors NO982907D0 (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 (2)

Publication Number Publication Date
NO982907L true NO982907L (en) 1998-06-22
NO982907D0 NO982907D0 (en) 1998-06-22

Family

ID=7781401

Family Applications (1)

Application Number Title Priority Date Filing Date
NO982907A NO982907D0 (en) 1995-12-23 1998-06-22 Tyrosine derivatives as <alfa> -v integrin inhibitors

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) NO982907D0 (en)
PL (1) PL327185A1 (en)
SK (1) SK78398A3 (en)
WO (1) WO1997023451A1 (en)
ZA (1) ZA9610725B (en)

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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
US6245809B1 (en) 1996-12-09 2001-06-12 Cor Therapeutics Inc. Integrin antagonists
DE69720062D1 (en) * 1996-12-09 2003-04-24 Lilly Co Eli 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
CN100369888C (en) * 1997-08-22 2008-02-20 霍夫曼-拉罗奇有限公司 N-alkanoylphenylalanine derivatives
DK1005446T3 (en) * 1997-08-22 2004-06-07 Hoffmann La Roche N-aroylphenylalanine derivatives
US6455550B1 (en) 1997-08-22 2002-09-24 Hoffmann-La Roche Inc. N-alkanoylphenylalanine derivatives
KR20010042587A (en) 1998-04-09 2001-05-25 기따자또 이찌로 AMINOPIPERIDINE DERIVATIVES AS INTEGRIN αvβ3 ANTAGONISTS
DE69917278T2 (en) * 1998-07-31 2005-05-19 Eli Lilly And Co., Indianapolis 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
EP1140809B1 (en) * 1998-12-16 2005-08-31 Bayer HealthCare AG New biphenyl and biphenyl-analogous compounds as integrin antagonists
US6677360B2 (en) 1998-12-16 2004-01-13 Bayer Aktiengesellschaft 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
CA2359115C (en) 1999-01-22 2011-06-21 Elan Pharmaceuticals, Inc. Acyl derivatives which treat vla-4 related disorders
AU2623900A (en) * 1999-01-22 2000-08-07 American Home Products Corporation Compounds which inhibit leukocyte adhesion mediated by vla-4
JP2002535316A (en) 1999-01-22 2002-10-22 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 Fused-ring heteroaryl and heterocyclic compounds that 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
CZ20012980A3 (en) 1999-02-18 2002-04-17 F. Hoffmann-La Roche Ag Thioamide derivatives
AU3246600A (en) 1999-03-01 2000-09-21 Elan Pharmaceuticals, Inc. Alpha-aminoacetic acid derivatives useful as alpha 4 beta 7 receptor antagonists
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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
CA2386821A1 (en) * 1999-10-08 2001-04-19 Kazuyuki Fujishima 3-aminopiperidine derivatives as integrin .alpha.v.beta.3 antagonists
US6486174B2 (en) 2000-08-07 2002-11-26 3-Dimensional Pharmaceuticals, Inc. Tetrahydroisoquinoline-3-carboxylic acid alkoxyguanidines as integrin antagonists
US20020037897A1 (en) * 2000-08-07 2002-03-28 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
JP2004529918A (en) 2001-04-09 2004-09-30 オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド Quinazoline and quinazoline analogs for the treatment of integrin-derived diseases
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TW200307671A (en) 2002-05-24 2003-12-16 Elan Pharm Inc Heteroaryl compounds which inhibit leukocyte adhesion mediated by α 4 integrins
EP1940827B1 (en) 2005-09-29 2011-03-16 Elan Pharmaceuticals Inc. Carbamate compounds which inhibit leukocyte adhesion mediated by vla-4
NZ567270A (en) 2005-09-29 2011-06-30 Elan Pharm Inc Pyrimidinyl amide 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
SG10201401836RA (en) 2009-04-27 2014-10-30 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

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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
BR9612201A (en) 1999-07-13
KR19990076676A (en) 1999-10-15
DE19548709A1 (en) 1997-07-03
HUP9903716A2 (en) 2000-03-28
EP0879227A1 (en) 1998-11-25
ZA9610725B (en) 1997-06-26
AU1301697A (en) 1997-07-17
JP2000502664A (en) 2000-03-07
CZ195198A3 (en) 1998-11-11
WO1997023451A1 (en) 1997-07-03
CA2241149A1 (en) 1997-07-03
NO982907D0 (en) 1998-06-22
PL327185A1 (en) 1998-11-23
MX9804971A (en) 1998-09-30
SK78398A3 (en) 1998-11-04

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