WO1992015607A3 - Phenyl amidines derivatives useful as platelet aggregation inhibitors - Google Patents

Phenyl amidines derivatives useful as platelet aggregation inhibitors Download PDF

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Publication number
WO1992015607A3
WO1992015607A3 PCT/US1992/001531 US9201531W WO9215607A3 WO 1992015607 A3 WO1992015607 A3 WO 1992015607A3 US 9201531 W US9201531 W US 9201531W WO 9215607 A3 WO9215607 A3 WO 9215607A3
Authority
WO
WIPO (PCT)
Prior art keywords
platelet aggregation
derivatives useful
aggregation inhibitors
phenyl amidines
phenyl
Prior art date
Application number
PCT/US1992/001531
Other languages
French (fr)
Other versions
WO1992015607A2 (en
Inventor
Robert Bruce Garland
Masateru Miyano
Jeffery Alan Zablocki
Lori Ann Schretzman
Original Assignee
Searle & Co
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 Searle & Co filed Critical Searle & Co
Priority to AU16666/92A priority Critical patent/AU662142B2/en
Priority to KR1019930702646A priority patent/KR100210206B1/en
Priority to US08/090,127 priority patent/US5481021A/en
Priority to CA002099994A priority patent/CA2099994C/en
Priority to JP50875192A priority patent/JP3258659B2/en
Priority to EP92909278A priority patent/EP0574545B1/en
Priority to DE69200766T priority patent/DE69200766T2/en
Publication of WO1992015607A2 publication Critical patent/WO1992015607A2/en
Publication of WO1992015607A3 publication Critical patent/WO1992015607A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C07K5/06113—Asp- or Asn-amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds 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
    • C07C257/10—Compounds 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
    • C07C257/18—Compounds 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C07D209/16—Tryptamines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/745—Blood coagulation or fibrinolysis factors
    • C07K14/75—Fibrinogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal 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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Breeding Of Plants And Reproduction By Means Of Culturing (AREA)

Abstract

This invention relates to phenyl amidines derivatives having formula (I) or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidines derivatives.
PCT/US1992/001531 1991-03-06 1992-03-05 Phenyl amidines derivatives useful as platelet aggregation inhibitors WO1992015607A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
AU16666/92A AU662142B2 (en) 1991-03-06 1992-03-05 Phenyl amidines derivatives useful as platelet aggregation inhibitors
KR1019930702646A KR100210206B1 (en) 1991-03-06 1992-03-05 Phenylamidines derivatives useful as platelet aggregation inhibitors
US08/090,127 US5481021A (en) 1991-03-06 1992-03-05 Phenyl amidines derivatives useful as platelet aggregation inhibitors
CA002099994A CA2099994C (en) 1991-03-06 1992-03-05 Phenyl amidines derivatives useful as platelet aggregation inhibitors
JP50875192A JP3258659B2 (en) 1991-03-06 1992-03-05 Phenylamidine derivatives useful as platelet aggregation inhibitors
EP92909278A EP0574545B1 (en) 1991-03-06 1992-03-05 Phenyl amidines derivatives useful as platelet aggregation inhibitors
DE69200766T DE69200766T2 (en) 1991-03-06 1992-03-05 PHENYLAMIDE DERIVATIVES AS PLATE AGGREGATION INHIBITORS.

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US66511991A 1991-03-06 1991-03-06
US665,119 1991-03-06

Publications (2)

Publication Number Publication Date
WO1992015607A2 WO1992015607A2 (en) 1992-09-17
WO1992015607A3 true WO1992015607A3 (en) 1992-10-29

Family

ID=24668789

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1992/001531 WO1992015607A2 (en) 1991-03-06 1992-03-05 Phenyl amidines derivatives useful as platelet aggregation inhibitors

Country Status (13)

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

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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
ES2141102T3 (en) * 1991-02-08 2000-03-16 Diatide Inc POLYPEPTIDES MARKED WITH TECNETIO-99M FOR THE GENERATION OF IMAGES.
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
WO1992018117A1 (en) * 1991-04-11 1992-10-29 Rhone-Poulenc Rorer International (Holdings), Inc. Anti-thrombotic peptide and pseudopeptide derivatives
ES2091359T3 (en) * 1991-05-13 1996-11-01 Fujisawa Pharmaceutical Co NEW PEPTIDIC COMPOUND AND A PROCEDURE FOR ITS PREPARATION.
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 (en) * 1992-03-06 1994-05-11 Hoffmann La Roche
DE4212304A1 (en) * 1992-04-13 1993-10-14 Cassella Ag Aspartic acid derivatives, their preparation and use
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
US5614539A (en) * 1993-03-15 1997-03-25 G. D. Searle & Co. Urea compounds which are useful as platelet aggregation inhibitors
ES2179076T3 (en) * 1993-04-08 2003-01-16 Diatide Inc RADIOLOGICALLY MARKED COMPOUNDS TO PLAY THROMBES IN PICTURES.
TW394760B (en) * 1993-09-07 2000-06-21 Hoffmann La Roche Novel Carboxamides, process for their preparation and pharmaceutical composition containing the same
EP0729362B1 (en) * 1993-11-19 2000-01-12 G.D. SEARLE & CO. TRANSDERMAL COMPOSITION OF N- N- 5- 4-(AMINOIMINOMETHYL)PHENYL]-1-OXOPENTYL]-L-alpha-ASPARTYL]-L-PHENYLALANINE OR ITS ESTERS AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS
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 (en) * 1996-06-27 2007-01-31 新日本製鐵株式会社 Fibrinogen receptor antagonist and pharmaceutical preparation containing the same as an active ingredient
US5811398A (en) * 1995-04-11 1998-09-22 G. D. Searle & Co. Platelet aggregation inhibitors containing C-terminal aminergic side chain amino acid residues
DK0892780T3 (en) * 1996-02-22 2003-03-03 Bristol Myers Squibb Pharma Co m-Amidinophenyl analogues as factor Xa inhibitors
US5942544A (en) * 1996-02-22 1999-08-24 Dupont Pharmaceuticals Company α-branched anilines, toluenes, and analogs thereof as factor Xa inhibitors
JP2001504801A (en) * 1996-06-10 2001-04-10 ジー．ディー．サール アンド カンパニー Radiopharmaceutical composition localizable to thrombus site
US5872122A (en) * 1997-10-16 1999-02-16 Monsanto Company Pyrimidinylamidino β-amino acid derivatives useful as inhibitors of platelet aggregation
AU1208999A (en) * 1997-11-10 1999-05-31 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
JP2003514824A (en) 1999-11-15 2003-04-22 ビオミラ，インコーポレーテッド Synthetic lipid-A analogs and uses thereof
AU2002256361B2 (en) * 2001-04-24 2008-01-24 Arxy Therapeutics Coumarin derivatives to be used as anticoagulants
JP3964417B2 (en) 2004-09-27 2007-08-22 国立大学法人金沢大学 Α2 receptor blocker and vasodilator containing indole derivative as active ingredient
JP5815542B2 (en) 2009-10-29 2015-11-17 ヤンセン ファーマシューティカ エヌ．ベー． Alkynyl derivatives useful as DPP-1 inhibitors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0384362A2 (en) * 1989-02-23 1990-08-29 F. Hoffmann-La Roche Ag Glycinderivatives

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US4578079A (en) * 1982-08-04 1986-03-25 La Jolla Cancer Research Foundation Tetrapeptide
US4589881A (en) * 1982-08-04 1986-05-20 La Jolla Cancer Research Foundation Polypeptide
US4661111A (en) * 1982-08-04 1987-04-28 La Jolla Cancer Research Foundation Polypeptide
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US4683291A (en) * 1985-10-28 1987-07-28 Scripps Clinic And Research Foundation Platelet binding inhibitors
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NZ223148A (en) * 1987-01-16 1989-10-27 Merrell Dow Pharma Peptide derivatives having peptidase inhibition activity
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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
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Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
EP0384362A2 (en) * 1989-02-23 1990-08-29 F. Hoffmann-La Roche Ag Glycinderivatives

Also Published As

Publication number Publication date
WO1992015607A2 (en) 1992-09-17
DE69200766D1 (en) 1995-01-12
KR100210206B1 (en) 1999-07-15
EP0502536B1 (en) 1996-10-09
JP3258659B2 (en) 2002-02-18
DE69200766T2 (en) 1995-05-04
AU662142B2 (en) 1995-08-24
CA2099994C (en) 2003-05-20
IE920710A1 (en) 1992-09-09
EP0574545B1 (en) 1994-11-30
EP0574545A1 (en) 1993-12-22
ES2065182T3 (en) 1995-02-01
EP0502536A1 (en) 1992-09-09
US5481021A (en) 1996-01-02
MX9203551A (en) 1992-09-01
AU1666692A (en) 1992-10-06
CA2099994A1 (en) 1992-09-07
ATE114670T1 (en) 1994-12-15
DK0574545T3 (en) 1995-01-30
JPH06505497A (en) 1994-06-23

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