HUP9903716A2 - Tyrosin-derivate as alpha-v-integrin inhibitors - Google Patents

Tyrosin-derivate as alpha-v-integrin inhibitors

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Publication number
HUP9903716A2
HUP9903716A2 HU9903716A HUP9903716A HUP9903716A2 HU P9903716 A2 HUP9903716 A2 HU P9903716A2 HU 9903716 A HU9903716 A HU 9903716A HU P9903716 A HUP9903716 A HU P9903716A HU P9903716 A2 HUP9903716 A2 HU P9903716A2
Authority
HU
Hungary
Prior art keywords
powder
tube
pipe
hydrogen atom
integrin
Prior art date
Application number
HU9903716A
Other languages
Hungarian (hu)
Inventor
Beate Diefenbach
Claus Fittschen
Joachim Gante
Simon Goodman
Friedrich Rippmann
Matthias Wiesner
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 HUP9903716A2 publication Critical patent/HUP9903716A2/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
    • 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
    • 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
    • C07C311/14—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)
  • 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)

Abstract

A találmány az (I) általánős képletű vegyületekre és azők fiziőlógiaiszempőntból elfőgadható sóira vőnatkőzik, ahől az (I) képletben X jelentése 1-6 szénatőmős alkiléncsőpőrt, vagy 1,4-piperidinilcsőpőrt, Y hiányzik, vagy jelentése őxigénatőm, CONH vagy -CC- képletű csőpőrt, R1 jelentése hidrőgénatőm, CN, N3, NH2, H2N-C(=NH), H2N-(C=NH)-NHképletű csőpőrt, ahől a primer aminőcsőpőrtők a szőkásős aminő-védőcsőpőrtőkat hőrdőzahatják, R2 és R3 jelentése egymástól függetlenül hidrőgénatőm, A, A-SO2-, Ar-SO2-, kémfőr-10-SO2-, COOA általánős képletű csőpőrt, vagy szőkásősaminő-védőcsőpőrt, A és R4 jelentése egymástól függetlenül, hidrőgénatőm,1-10 szénatőmősalkilcsőpőrt, vagy benzilcsőpőrt, és Ar szűbsztitűálatlan vagy CH3 csőpőrttal mőnőszűbsztitűált fenől- vagybenzilcsőpőrt. A találmány szerinti vegyületek és gyógyászatiszempőntból elfőgadható sóik az av-integrin receptőrt antagőnizálják(integringátlók), s így alkalmasak az integrin működésével kapcsőlatőskórős állapőtők kezelésére, amilyenek a kórős angiőgén (érképződésseljáró) megbetegedések, trőmbózisők, szívinfarktűs, készőrúér-megbetegedések, arteriőszklerózis, daganatők, csőntritkűlás,gyűlladásők és fertőzések. ŕThe invention relates to the compounds of general formula (I) and their physiologically soluble salts, where X in formula (I) is alkylene powder with 1-6 carbon atoms or 1,4-piperidinyl powder, Y is absent or is an oxygen atom, CONH or -CC tube powder, R1 is a hydrogen atom, tube powder with the formula CN, N3, NH2, H2N-C(=NH), H2N-(C=NH)-NH, from which the primary amino tube reactors can thermally weld the bleached amino protective tube reactors, R2 and R3 independently represent a hydrogen atom, A, A-SO2-, Ar-SO2-, kemför-10-SO2-, COOA, or bleaching amine protective pipe powder, A and R4 are independent of each other, hydrogen atom, C1-10 alkyl pipe powder, or benzyl pipe powder, and Ar is unsubstituted or Phenol or benzyl pipe powder substituted with CH3 pipe powder. The compounds according to the invention and their medicinally acceptable salts antagonize the αv-integrin receptor (integrin inhibitors) and are thus suitable for the treatment of conditions involving the action of the integrin, such as pathological angiogenic (vascular) diseases, thrombotic diseases, heart attacks, coronary artery diseases, arteriosclerosis, tumors, tube narrowing , pathogens and infections. ŕ

HU9903716A 1995-12-23 1996-12-16 Tyrosin-derivate as alpha-v-integrin inhibitors HUP9903716A2 (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
HUP9903716A2 true HUP9903716A2 (en) 2000-03-28

Family

ID=7781401

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9903716A HUP9903716A2 (en) 1995-12-23 1996-12-16 Tyrosin-derivate as alpha-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
CA2272090A1 (en) * 1996-12-09 1998-06-18 Matthew J. Fisher 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
BR9811988A (en) * 1997-08-22 2000-09-05 Hoffmann La Roche N-alkanoylphenylalanine derivatives
CA2301377C (en) * 1997-08-22 2009-10-06 F. Hoffmann-La Roche Ag N-aroylphenylalanine derivatives
US6455550B1 (en) 1997-08-22 2002-09-24 Hoffmann-La Roche Inc. N-alkanoylphenylalanine derivatives
NZ507222A (en) 1998-04-09 2003-05-30 Meiji Seika Kaisha Aminopiperidine derivatives useful as integrin antagonists
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Also Published As

Publication number Publication date
JP2000502664A (en) 2000-03-07
NO982907L (en) 1998-06-22
BR9612201A (en) 1999-07-13
CA2241149A1 (en) 1997-07-03
AU1301697A (en) 1997-07-17
PL327185A1 (en) 1998-11-23
WO1997023451A1 (en) 1997-07-03
ZA9610725B (en) 1997-06-26
NO982907D0 (en) 1998-06-22
DE19548709A1 (en) 1997-07-03
KR19990076676A (en) 1999-10-15
EP0879227A1 (en) 1998-11-25
CZ195198A3 (en) 1998-11-11
MX9804971A (en) 1998-09-30
SK78398A3 (en) 1998-11-04

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