ES2065182T3 - Derivados de fenilamidinas utiles como inhibidores de la agregacion de plaquetas. - Google Patents

Derivados de fenilamidinas utiles como inhibidores de la agregacion de plaquetas.

Info

Publication number
ES2065182T3
ES2065182T3 ES92909278T ES92909278T ES2065182T3 ES 2065182 T3 ES2065182 T3 ES 2065182T3 ES 92909278 T ES92909278 T ES 92909278T ES 92909278 T ES92909278 T ES 92909278T ES 2065182 T3 ES2065182 T3 ES 2065182T3
Authority
ES
Spain
Prior art keywords
derivatives
useful
platelet aggregation
phenylamidines
inhibitors
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES92909278T
Other languages
English (en)
Inventor
Robert Bruce Garland
Masateru Miyano
Jeffery Alan Zablocki
Lori Ann Schretzman
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
GD Searle LLC
Original Assignee
GD Searle LLC
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 GD Searle LLC filed Critical GD Searle LLC
Application granted granted Critical
Publication of ES2065182T3 publication Critical patent/ES2065182T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06104Dipeptides with the first amino acid being acidic
    • C07K5/06113Asp- or Asn-amino acid
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C07D209/16Tryptamines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/745Blood coagulation or fibrinolysis factors
    • C07K14/75Fibrinogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Toxicology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Indole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Breeding Of Plants And Reproduction By Means Of Culturing (AREA)

Abstract

LA INVENCION SE REFIERE A DERIVADOS DE AMIDINAS DE FENIL QUE TIENEN LA FORMULA (I) O A UNA SAL FARMACEUTICAMENTE ACEPTABLE, LOS DERIVADOS SON UTILES EN LA INHIBICION DE LA CONGREGACION DE PLAQUETAS. LA INVENCION TAMBIEN SE REFIERE A COMPOSICIONES FARMACEUTICAS TALES COMO DERIVADOS DE AMIDINAS DE FENIL.
ES92909278T 1991-03-06 1992-03-05 Derivados de fenilamidinas utiles como inhibidores de la agregacion de plaquetas. Expired - Lifetime ES2065182T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US66511991A 1991-03-06 1991-03-06

Publications (1)

Publication Number Publication Date
ES2065182T3 true ES2065182T3 (es) 1995-02-01

Family

ID=24668789

Family Applications (1)

Application Number Title Priority Date Filing Date
ES92909278T Expired - Lifetime ES2065182T3 (es) 1991-03-06 1992-03-05 Derivados de fenilamidinas utiles como inhibidores de la agregacion de plaquetas.

Country Status (13)

Country Link
US (1) US5481021A (es)
EP (2) EP0574545B1 (es)
JP (1) JP3258659B2 (es)
KR (1) KR100210206B1 (es)
AT (1) ATE114670T1 (es)
AU (1) AU662142B2 (es)
CA (1) CA2099994C (es)
DE (1) DE69200766T2 (es)
DK (1) DK0574545T3 (es)
ES (1) ES2065182T3 (es)
IE (1) IE920710A1 (es)
MX (1) MX9203551A (es)
WO (1) WO1992015607A2 (es)

Families Citing this family (37)

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AU646838B2 (en) * 1990-03-09 1994-03-10 F. Hoffmann-La Roche Ag Acetic acid derivatives
US5736122A (en) * 1991-02-08 1998-04-07 Diatide, Inc. Technetium-99m labeled peptides for thrombus imaging
US5645815A (en) 1991-02-08 1997-07-08 Diatide, Inc. Radiolabled compounds for thrombus imaging
US6019958A (en) * 1991-02-08 2000-02-01 Diatide, Inc. Technetium-99m labeled peptides for imaging inflammation
US5830856A (en) * 1991-02-08 1998-11-03 Diatide, Inc. Radiolabeled compounds for thrombus imaging
EP0570493B1 (en) * 1991-02-08 2000-01-05 Diatide, Inc. TECHNETIUM-99m LABELED POLYPEPTIDES FOR IMAGING
AU661659B2 (en) * 1991-04-11 1995-08-03 Rhone-Poulenc Rorer International (Holdings) Inc. Anti-thrombotic peptide and pseudopeptide derivatives
DE69213546T2 (de) * 1991-05-13 1997-02-27 Fujisawa Pharmaceutical Co Neue Peptid-Verbindungen und Verfahren zur Herstellung davon
US5239113A (en) * 1991-10-15 1993-08-24 Monsanto Company Substituted β-amino acid derivatives useful as platelet aggregation inhibitors and intermediates thereof
US5424334A (en) * 1991-12-19 1995-06-13 G. D. Searle & Co. Peptide mimetic compounds useful as platelet aggregation inhibitors
US5264457A (en) * 1992-02-14 1993-11-23 G. D. Searle & Co. Phenyl amidines sulfonamides useful as platelet aggregation inhibitors
TW223629B (es) * 1992-03-06 1994-05-11 Hoffmann La Roche
DE4212304A1 (de) * 1992-04-13 1993-10-14 Cassella Ag Asparaginsäurederivate, ihre Herstellung und Verwendung
AU687080B2 (en) * 1993-04-08 1998-02-19 Cis Bio International Radiolabeled compounds for thrombus imaging
US5968476A (en) * 1992-05-21 1999-10-19 Diatide, Inc. Technetium-99m labeled peptides for thrombus imaging
US5354738A (en) * 1992-09-04 1994-10-11 G. D. Searle & Co. Platelet aggregation inhibitors
US5314902A (en) * 1993-01-27 1994-05-24 Monsanto Company Urea derivatives useful as platelet aggregation inhibitors
US5409939A (en) * 1993-02-12 1995-04-25 G. D. Searle & Co. Phenyl amidine thio derivatives useful as platelet aggregation inhibitors
WO1994021602A1 (en) * 1993-03-15 1994-09-29 G.D. Searle & Co. Urea derivatives useful as platelet aggregation inhibitors
TW394760B (en) * 1993-09-07 2000-06-21 Hoffmann La Roche Novel Carboxamides, process for their preparation and pharmaceutical composition containing the same
ATE188611T1 (de) * 1993-11-19 2000-01-15 Searle & Co Transdermale zusammensetzung von n-(n-(5-(4- (aminoiminomethyl)phenyl-1-oxopentyl)-l-alpha- aspartyl)-l-phenylalanin oder deren esterderivaten und ihre pharmazeutischverwendbaren salze
US5563158A (en) * 1993-12-28 1996-10-08 The Dupont Merck Pharmaceutical Company Aromatic compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
US6387880B1 (en) * 1994-10-24 2002-05-14 G.D. Searle & Co. Transdermal N-[N-[5-[4-(aminoiminomethly)phenyl]-1-oxopentyl]-L-α-aspartyl]-L-phenylalainine or its esters and their pharmaceutically acceptable salts
JP3874455B2 (ja) * 1996-06-27 2007-01-31 新日本製鐵株式会社 フィブリノーゲン受容体拮抗物質およびそれを有効成分とする医薬製剤
US5811398A (en) * 1995-04-11 1998-09-22 G. D. Searle & Co. Platelet aggregation inhibitors containing C-terminal aminergic side chain amino acid residues
US5942544A (en) * 1996-02-22 1999-08-24 Dupont Pharmaceuticals Company α-branched anilines, toluenes, and analogs thereof as factor Xa inhibitors
EP0892780B1 (en) * 1996-02-22 2002-11-20 Bristol-Myers Squibb Pharma Company M-AMIDINO PHENYL ANALOGS AS FACTOR Xa INHIBITORS
AU3474997A (en) * 1996-06-10 1998-01-07 G.D. Searle & Co. Radiopharmaceutical compositions capable of localizing at sites of thrombus
RU2142939C1 (ru) * 1996-10-28 1999-12-20 Эл Джи Кемикал Лтд. Избирательно действующие ингибиторы тромбина и фармацевтическая композиция на их основе
US5872122A (en) * 1997-10-16 1999-02-16 Monsanto Company Pyrimidinylamidino β-amino acid derivatives useful as inhibitors of platelet aggregation
WO1999024407A1 (en) * 1997-11-10 1999-05-20 Array Biopharma, Inc. Compounds which inhibit tryptase activity
US6037365A (en) * 1998-09-25 2000-03-14 G.D. Searle & Co. Aminobenzamidinosuccinyl lactone derivatives useful as inhibitors of platelet aggregation
US6362216B1 (en) 1998-10-27 2002-03-26 Array Biopharma Inc. Compounds which inhibit tryptase activity
ATE518874T1 (de) * 1999-11-15 2011-08-15 Oncothyreon Inc Synthetische lipid-a analogen und verwendungen davon
CA2445160A1 (en) * 2001-04-24 2002-10-31 Aryx Therapeutics Coumarin derivatives to be used as anticoagulants
JP3964417B2 (ja) 2004-09-27 2007-08-22 国立大学法人金沢大学 インドール誘導体を有効成分とするα2受容体遮断剤及び血管拡張剤
AU2010319927B2 (en) 2009-10-29 2015-01-22 Janssen Pharmaceutica Nv Alkynyl derivatives useful as DPP-1 inhibitors

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4578079A (en) * 1982-08-04 1986-03-25 La Jolla Cancer Research Foundation Tetrapeptide
US4661111A (en) * 1982-08-04 1987-04-28 La Jolla Cancer Research Foundation Polypeptide
US4517686A (en) * 1982-08-04 1985-05-21 La Jolla Cancer Research Foundation Polypeptide
US4614517A (en) * 1982-08-04 1986-09-30 La Jolla Cancer Research Foundation Tetrapeptide
US4589881A (en) * 1982-08-04 1986-05-20 La Jolla Cancer Research Foundation Polypeptide
US4683291A (en) * 1985-10-28 1987-07-28 Scripps Clinic And Research Foundation Platelet binding inhibitors
ES2052595T3 (es) * 1986-12-15 1994-07-16 Inst Nat Sante Rech Med Nuevos derivados peptidicos y su aplicacion en especial en terapeutica.
NZ223148A (en) * 1987-01-16 1989-10-27 Merrell Dow Pharma Peptide derivatives having peptidase inhibition activity
FR2617170B1 (fr) * 1987-06-25 1989-12-22 Inst Nat Sante Rech Med Nouveaux derives peptidiques et leur application notamment en therapeutique
US4857508A (en) * 1987-12-03 1989-08-15 Monsanto Company Novel platelet-aggregation inhibitor peptide derivatives
US4879313A (en) * 1988-07-20 1989-11-07 Mosanto Company Novel platelet-aggregation inhibitors
US5039805A (en) * 1988-12-08 1991-08-13 Hoffmann-La Roche Inc. Novel benzoic and phenylacetic acid derivatives
US5084466A (en) * 1989-01-31 1992-01-28 Hoffmann-La Roche Inc. Novel carboxamide pyridine compounds which have useful pharmaceutical utility
CA2008116C (en) * 1989-02-23 2001-11-20 Thomas Weller Glycine derivatives
CA2021951A1 (en) * 1989-07-28 1991-01-29 Ruth F. Nutt Fibrinogen receptor antagonists

Also Published As

Publication number Publication date
EP0502536A1 (en) 1992-09-09
DE69200766D1 (en) 1995-01-12
JP3258659B2 (ja) 2002-02-18
EP0574545A1 (en) 1993-12-22
WO1992015607A2 (en) 1992-09-17
AU662142B2 (en) 1995-08-24
DK0574545T3 (da) 1995-01-30
DE69200766T2 (de) 1995-05-04
MX9203551A (es) 1992-09-01
EP0502536B1 (en) 1996-10-09
CA2099994C (en) 2003-05-20
KR100210206B1 (ko) 1999-07-15
EP0574545B1 (en) 1994-11-30
IE920710A1 (en) 1992-09-09
AU1666692A (en) 1992-10-06
WO1992015607A3 (en) 1992-10-29
CA2099994A1 (en) 1992-09-07
ATE114670T1 (de) 1994-12-15
JPH06505497A (ja) 1994-06-23
US5481021A (en) 1996-01-02

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