AU2002230836A1 - Benzylamine derivatives and their use as thrombin inhibitors - Google Patents

Benzylamine derivatives and their use as thrombin inhibitors

Info

Publication number
AU2002230836A1
AU2002230836A1 AU2002230836A AU3083602A AU2002230836A1 AU 2002230836 A1 AU2002230836 A1 AU 2002230836A1 AU 2002230836 A AU2002230836 A AU 2002230836A AU 3083602 A AU3083602 A AU 3083602A AU 2002230836 A1 AU2002230836 A1 AU 2002230836A1
Authority
AU
Australia
Prior art keywords
thrombin inhibitors
benzylamine derivatives
benzylamine
derivatives
thrombin
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.)
Abandoned
Application number
AU2002230836A
Inventor
James C. Barrow
Terry A. Lyle
Matthew M. Morrissette
Philippe G. Nantermet
Kenneth E. Rittle
Philip E Sanderson
Harold G Selnick
Donnette D. Staas
Kenneth J. Stauffer
Lekhanh O. Tran
Peter D. Williams
Catherine M. Wiscount
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.)
Merck and Co Inc
Original Assignee
Merck and Co 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 Merck and Co Inc filed Critical Merck and Co Inc
Publication of AU2002230836A1 publication Critical patent/AU2002230836A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • 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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • 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
AU2002230836A 2000-12-18 2001-12-14 Benzylamine derivatives and their use as thrombin inhibitors Abandoned AU2002230836A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US25630400P 2000-12-18 2000-12-18
US60256304 2000-12-18
US32318401P 2001-09-18 2001-09-18
US60323184 2001-09-18
PCT/US2001/048321 WO2002050056A1 (en) 2000-12-18 2001-12-14 Benzylamine derivatives and their use as thrombin inhibitors

Publications (1)

Publication Number Publication Date
AU2002230836A1 true AU2002230836A1 (en) 2002-07-01

Family

ID=26945268

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2002230836A Abandoned AU2002230836A1 (en) 2000-12-18 2001-12-14 Benzylamine derivatives and their use as thrombin inhibitors

Country Status (6)

Country Link
US (1) US6515011B2 (en)
JP (1) JP2004516286A (en)
AU (1) AU2002230836A1 (en)
CA (1) CA2431588A1 (en)
PE (1) PE20020759A1 (en)
WO (1) WO2002050056A1 (en)

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US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin inhibitors
JP2005504003A (en) 2001-02-09 2005-02-10 メルク　エンド　カムパニー　インコーポレーテッド Thrombin inhibitor
DK1485345T3 (en) 2002-03-11 2008-11-03 Curacyte Ag Urokinase Inhibitors, Their Preparation and Use
DE10301300B4 (en) 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Use of acylated 4-amidino- and 4-guanidinobenzylamines for the inhibition of plasma kallikrein
DE10342108A1 (en) 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basic substituted benzylamine analogs as coagulation factor Xa inhibitors, their preparation and use
JP4606041B2 (en) * 2004-03-05 2011-01-05 セントラル硝子株式会社 Optically active 1-aryl-2-fluoro-substituted ethylamines and process for producing the same
DE102005044319A1 (en) * 2005-09-16 2007-03-22 Curacyte Chemistry Gmbh 2- (Aminomethyl) -5-chloro-benzylamide derivatives and their use as inhibitors of coagulation factor Xa
DE102006050672A1 (en) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh New glycylglycine derivatives with a benzylsulfonylamido group and an amidino-organylamido group at the opposite chain ends, used in drugs for reducing loss of blood, e.g. in operations
JP4910148B2 (en) * 2007-03-09 2012-04-04 国立大学法人 名古屋工業大学 Method for producing optically active α-fluorobis (phenylsulfonyl) methyl adduct and method for producing optically active α-fluoromethylamine derivative
TW200911787A (en) * 2007-07-03 2009-03-16 Astrazeneca Ab New aza-bicyclohexane compounds useful as inhibitors of thrombin
EA018502B1 (en) * 2008-06-23 2013-08-30 Астразенека Аб New heterocyclic carboxamides and pharmaceutical compositions containing them
EP2230231A1 (en) * 2009-03-16 2010-09-22 Bayer CropScience AG Method for manufacturing 2,2-difluoroethylamine derivatives by imine hydrogenation
US8828474B2 (en) * 2009-09-20 2014-09-09 Medtronic Vascular, Inc. Apparatus and methods for loading a drug eluting medical device
AU2011349022B2 (en) 2010-12-21 2017-04-13 The Medicines Company (Leipzig) Gmbh Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa
WO2014025658A1 (en) * 2012-08-08 2014-02-13 Merck Sharp & Dohme Corp. Pyrrolidine thrombin inhibitors
US9469608B2 (en) 2012-11-20 2016-10-18 Merck Sharp & Dohme Corp. Thrombin inhibitors
CN103641769B (en) * 2013-12-06 2015-11-04 爱斯特（成都）生物制药有限公司 The preparation method of isoindoline hydrochloride
GB201805174D0 (en) * 2018-03-29 2018-05-16 Univ Leeds Innovations Ltd Compounds
EP3802489A4 (en) * 2018-05-29 2022-04-13 Omeros Corporation Masp-2 inhibitors and methods of use
US11584714B2 (en) 2018-05-29 2023-02-21 Omeros Corporation MASP-2 inhibitors and methods of use
CN115052862A (en) 2019-12-04 2022-09-13 奥默罗斯公司 MASP-2 inhibitors and methods of use
JP2023504543A (en) 2019-12-04 2023-02-03 オメロス コーポレーション MASP-2 inhibitors and methods of use
GB202107722D0 (en) 2021-05-28 2021-07-14 Lunac Therapeutics Ltd Factor XIIA Inhibitors

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HU192646B (en) 1984-12-21 1987-06-29 Gyogyszerkutato Intezet Process for preparing new n-alkyl-peptide aldehydes
IL77748A (en) 1985-02-04 1991-11-21 Merrell Dow Pharma Amino acid and peptide derivatives as peptidase inhibitors
US4804743A (en) 1987-01-29 1989-02-14 Warner-Lambert Copmany Proline-containing renin inhibitors
ZA897515B (en) 1988-10-07 1990-06-27 Merrell Dow Pharma Novel peptidase inhibitors
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US5688768A (en) 1991-02-19 1997-11-18 Cor Therapeutics, Inc. Recombinant thrombin receptor and related pharmaceuticals
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Also Published As

Publication number Publication date
JP2004516286A (en) 2004-06-03
WO2002050056A1 (en) 2002-06-27
PE20020759A1 (en) 2002-08-22
US20020119992A1 (en) 2002-08-29
US6515011B2 (en) 2003-02-04
CA2431588A1 (en) 2002-06-27

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