WO1998016523A3 - Selective factor xa inhibitors - Google Patents

Selective factor xa inhibitors Download PDF

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Publication number
WO1998016523A3
WO1998016523A3 PCT/US1997/018291 US9718291W WO9816523A3 WO 1998016523 A3 WO1998016523 A3 WO 1998016523A3 US 9718291 W US9718291 W US 9718291W WO 9816523 A3 WO9816523 A3 WO 9816523A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
selective factor
compounds
factor
vitro
Prior art date
Application number
PCT/US1997/018291
Other languages
French (fr)
Other versions
WO1998016523A2 (en
WO1998016523A9 (en
Inventor
Bing-Yan Zhu
Robert M Scarborough
Original Assignee
Cor Therapeutics Inc
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 Cor Therapeutics Inc filed Critical Cor Therapeutics Inc
Priority to AU49809/97A priority Critical patent/AU720513C/en
Priority to JP51845498A priority patent/JP2001504810A/en
Priority to CA002268281A priority patent/CA2268281A1/en
Priority to EP97912697A priority patent/EP0937073A2/en
Priority claimed from US08/948,672 external-priority patent/US6262047B1/en
Publication of WO1998016523A2 publication Critical patent/WO1998016523A2/en
Publication of WO1998016523A3 publication Critical patent/WO1998016523A3/en
Publication of WO1998016523A9 publication Critical patent/WO1998016523A9/en

Links

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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders. Their formula is (I) where the meaning of the various symbols is provided in the description.
PCT/US1997/018291 1996-10-11 1997-10-10 Selective factor xa inhibitors WO1998016523A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
AU49809/97A AU720513C (en) 1996-10-11 1997-10-10 Selective factor Xa inhibitors
JP51845498A JP2001504810A (en) 1996-10-11 1997-10-10 Selective factor Xa inhibitor
CA002268281A CA2268281A1 (en) 1996-10-11 1997-10-10 Selective factor xa inhibitors
EP97912697A EP0937073A2 (en) 1996-10-11 1997-10-10 Selective factor xa inhibitors

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US73136696A 1996-10-11 1996-10-11
US3374996P 1996-10-11 1996-10-11
US08/948,672 1997-10-10
US08/948,672 US6262047B1 (en) 1996-10-11 1997-10-10 Selective factor Xa inhibitors
US08/731,366 1997-10-10
US60/033,749 1997-10-10

Publications (3)

Publication Number Publication Date
WO1998016523A2 WO1998016523A2 (en) 1998-04-23
WO1998016523A3 true WO1998016523A3 (en) 1998-06-18
WO1998016523A9 WO1998016523A9 (en) 1998-08-27

Family

ID=27364485

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1997/018291 WO1998016523A2 (en) 1996-10-11 1997-10-10 Selective factor xa inhibitors

Country Status (4)

Country Link
EP (1) EP0937073A2 (en)
JP (1) JP2001504810A (en)
CA (1) CA2268281A1 (en)
WO (1) WO1998016523A2 (en)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
AU6896298A (en) 1997-04-14 1998-11-11 Cor Therapeutics, Inc. Selective factor xa inhibitors
EP0975625A1 (en) 1997-04-14 2000-02-02 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
JP2002514214A (en) 1997-04-14 2002-05-14 シーオーアール セラピューティクス インコーポレイテッド Selective factor Xa inhibitor
EP0975659A1 (en) * 1997-04-14 2000-02-02 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
EP0994894A1 (en) * 1997-08-11 2000-04-26 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
AU753842B2 (en) * 1997-08-11 2002-10-31 Millennium Pharmaceuticals, Inc. Selective factor Xa inhibitors
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
CA2300478A1 (en) * 1997-08-11 1999-02-18 Cor Therapeutics, Inc. Selective factor xa inhibitors
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
HRP990246A2 (en) 1998-08-07 2000-06-30 Du Pont Pharm Co Succinoylamino benzodiazepines as inhibitors of a beta protein production
NZ509241A (en) 1998-08-07 2003-08-29 Du Pont Pharm Co Succinoylamino lactams as inhibitors of alpha-beta protein production
AU778005B2 (en) 1998-12-24 2004-11-11 Bristol-Myers Squibb Pharma Company Succinoylamino benzodiazepines as inhibitors of Abeta protein production
US6262080B1 (en) 1998-12-31 2001-07-17 Avantis Pharmaceuticals Inc. 3-(thio-substitutedamido)-lactams useful as inhibitors of matrix metalloproteinase
US6344450B1 (en) 1999-02-09 2002-02-05 Bristol-Myers Squibb Company Lactam compounds and their use as inhibitors of serine proteases and method
WO2000047207A1 (en) 1999-02-09 2000-08-17 Bristol-Myers Squibb Company LACTAM INHIBITORS OF FXa AND METHOD
CA2361919A1 (en) * 1999-02-09 2000-08-17 Bristol-Myers Squibb Company Lactam inhibitors of fxa and method
US6503902B2 (en) 1999-09-13 2003-01-07 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of a β protein production
DK1212300T3 (en) 1999-09-13 2004-03-15 Dimensional Pharm Inc Azacyclolol alkanone serine protease inhibitors
US6960576B2 (en) 1999-09-13 2005-11-01 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production
AU7997700A (en) 1999-10-08 2001-04-23 Du Pont Pharmaceuticals Company Amino lactam sulfonamides as inhibitors of abeta protein production
US6525044B2 (en) 2000-02-17 2003-02-25 Bristol-Myers Squibb Company Succinoylamino carbocycles and heterocycles as inhibitors of a-β protein production
US6495540B2 (en) 2000-03-28 2002-12-17 Bristol - Myers Squibb Pharma Company Lactams as inhibitors of A-β protein production
US6713476B2 (en) 2000-04-03 2004-03-30 Dupont Pharmaceuticals Company Substituted cycloalkyls as inhibitors of a beta protein production
EP1268433A1 (en) 2000-04-03 2003-01-02 Bristol-Myers Squibb Pharma Company Cyclic lactams as inhibitors of a-beta-protein production
AU2001257006A1 (en) 2000-04-11 2001-10-23 Du Pont Pharmaceuticals Company Substituted lactams as inhibitors of abeta protein production
BR0106717A (en) 2000-06-01 2002-04-16 Bristol Myers Squibb Pharma Co Compounds, pharmaceutical composition and uses of innovative lactam compounds
US6511973B2 (en) 2000-08-02 2003-01-28 Bristol-Myers Squibb Co. Lactam inhibitors of FXa and method
JP2004518688A (en) 2001-01-30 2004-06-24 ブリストル−マイヤーズ　スクイブ　カンパニー Factor Xa inhibitor sulfonamide lactam and method thereof
GB0114005D0 (en) 2001-06-08 2001-08-01 Glaxo Group Ltd Chemical compounds
GB0114004D0 (en) * 2001-06-08 2001-08-01 Glaxo Group Ltd Chemical compounds
GB0127568D0 (en) 2001-11-16 2002-01-09 Glaxo Group Ltd Chemical compounds
ES2543588T3 (en) 2002-12-03 2015-08-20 Pharmacyclics Llc 2- (2-Hydroxybiphenyl-3-yl) -1H-benzoimidazol-5-carboxamidine derivatives as inhibitors of factor VIIa
GB0228533D0 (en) * 2002-12-06 2003-01-15 Glaxo Group Ltd Crystalline form
MX2011013016A (en) 2009-06-05 2012-04-20 Link Medicine Corp Aminopyrrolidinone derivatives and uses thereof.
JP2023509452A (en) 2020-01-03 2023-03-08 バーグ エルエルシー Polycyclic Amides as UBE2K Modulators to Treat Cancer

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997017363A1 (en) * 1995-11-03 1997-05-15 Akzo Nobel N.V. Thrombin inhibitors
WO1997030073A1 (en) * 1996-02-13 1997-08-21 Akzo Nobel N.V. Serine protease inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997017363A1 (en) * 1995-11-03 1997-05-15 Akzo Nobel N.V. Thrombin inhibitors
WO1997030073A1 (en) * 1996-02-13 1997-08-21 Akzo Nobel N.V. Serine protease inhibitors

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BIOORG. MED. CHEM. LETT., vol. 3, no. 4, 1993, pages 773 - 778 *
CHEMICAL ABSTRACTS, vol. 120, no. 11, 14 March 1994, Columbus, Ohio, US; abstract no. 135101a, J W SKILES ET AL.: "Elastase inhibitors containing conformationally restricted lactams as P3-P2 dipeptide replacements" page 1113; XP002056972 *

Also Published As

Publication number Publication date
EP0937073A2 (en) 1999-08-25
WO1998016523A2 (en) 1998-04-23
CA2268281A1 (en) 1998-04-23
AU720513B2 (en) 2000-06-01
JP2001504810A (en) 2001-04-10
AU4980997A (en) 1998-05-11

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