CA2465877C - Utilisation de derives de 2-amino-4-pyridylmethyl-thiazoline comme inhibiteurs de non-synthase inductible - Google Patents

Utilisation de derives de 2-amino-4-pyridylmethyl-thiazoline comme inhibiteurs de non-synthase inductible Download PDF

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Publication number
CA2465877C
CA2465877C CA002465877A CA2465877A CA2465877C CA 2465877 C CA2465877 C CA 2465877C CA 002465877 A CA002465877 A CA 002465877A CA 2465877 A CA2465877 A CA 2465877A CA 2465877 C CA2465877 C CA 2465877C
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Canada
Prior art keywords
compound
formula
pyridin
temperature
pharmaceutically acceptable
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Expired - Fee Related
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CA002465877A
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English (en)
French (fr)
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CA2465877A1 (fr
Inventor
Eric Bacque
Antony Bigot
Jean-Christophe Carry
Serge Mignani
Baptiste Ronan
Michel Tabart
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Aventis Pharma SA
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Aventis Pharma SA
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Priority claimed from FR0114508A external-priority patent/FR2832150B1/fr
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Publication of CA2465877A1 publication Critical patent/CA2465877A1/fr
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Publication of CA2465877C publication Critical patent/CA2465877C/fr
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
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    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P25/22—Anxiolytics
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/55—Acids; Esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages

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  • Chemical Kinetics & Catalysis (AREA)
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  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA002465877A 2001-11-09 2002-11-07 Utilisation de derives de 2-amino-4-pyridylmethyl-thiazoline comme inhibiteurs de non-synthase inductible Expired - Fee Related CA2465877C (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
FR0114508A FR2832150B1 (fr) 2001-11-09 2001-11-09 Utilisation de derives de 2-amino-4-pyridylmethyl-thiazoline comme inhibiteurs de no-synthase inductible
FR01/14508 2001-11-09
US35297802P 2002-01-30 2002-01-30
US60/352,978 2002-01-30
PCT/FR2002/003808 WO2003039446A2 (fr) 2001-11-09 2002-11-07 Derives de 2-amino-4-pyridylmethyl-thiazoline et leur utilisation comme inhibiteurs de no-synthase inductible

Publications (2)

Publication Number Publication Date
CA2465877A1 CA2465877A1 (fr) 2003-05-15
CA2465877C true CA2465877C (fr) 2009-12-29

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Family Applications (1)

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CA002465877A Expired - Fee Related CA2465877C (fr) 2001-11-09 2002-11-07 Utilisation de derives de 2-amino-4-pyridylmethyl-thiazoline comme inhibiteurs de non-synthase inductible

Country Status (22)

Country Link
US (1) US6762196B2 (enExample)
EP (1) EP1450750B1 (enExample)
JP (1) JP4342309B2 (enExample)
CN (1) CN1288153C (enExample)
AT (1) ATE446295T1 (enExample)
BR (1) BR0206368A (enExample)
CA (1) CA2465877C (enExample)
CY (1) CY1110284T1 (enExample)
DE (1) DE60234117D1 (enExample)
DK (1) DK1450750T3 (enExample)
ES (1) ES2335090T3 (enExample)
HR (1) HRP20040402A2 (enExample)
HU (1) HUP0402033A2 (enExample)
IL (2) IL161843A0 (enExample)
MA (1) MA27143A1 (enExample)
MX (1) MXPA04004213A (enExample)
NO (1) NO20033131L (enExample)
PL (1) PL370267A1 (enExample)
PT (1) PT1450750E (enExample)
RU (1) RU2004117531A (enExample)
SI (1) SI1450750T1 (enExample)
WO (1) WO2003039446A2 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10240735A1 (de) * 2002-08-29 2004-03-18 Eberhard-Karls-Universität Tübingen Universitätsklinikum Verwendung von Modulatoren der NO-Signalkaskade und pharmazeutische Zusammensetzung
ES2537898T3 (es) 2005-10-25 2015-06-15 Shionogi & Co., Ltd. Derivados de aminotiazolidina y aminotetrahidrotiazepina como inhibidores de BACE 1
AU2008245082B8 (en) 2007-04-24 2012-09-13 Shionogi & Co., Ltd. Aminodihydrothiazine derivatives substituted with a cyclic group
EP2151435A4 (en) 2007-04-24 2011-09-14 Shionogi & Co PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE
US8637504B2 (en) 2008-06-13 2014-01-28 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
WO2010047372A1 (ja) 2008-10-22 2010-04-29 塩野義製薬株式会社 Bace1阻害活性を有する2-アミノピリミジン-4-オンおよび2-アミノピリジン誘導体
RU2012129168A (ru) 2009-12-11 2014-01-20 Сионоги Энд Ко. Лтд. Производные оксазина
US9018219B2 (en) 2010-10-29 2015-04-28 Shionogi & Co., Ltd. Fused aminodihydropyrimidine derivative
CA2816285A1 (en) 2010-10-29 2012-05-03 Shionogi & Co., Ltd. Naphthyridine derivative
WO2012147763A1 (ja) 2011-04-26 2012-11-01 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するbace1阻害剤
JP2016501827A (ja) 2012-10-24 2016-01-21 塩野義製薬株式会社 Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL107771A0 (en) * 1992-11-27 1994-02-27 Wellcome Found Pharmaceutical compositions containing isothiourea derivatives certain such novel compounds and their preparation
AU688811B2 (en) * 1993-10-21 1998-03-19 G.D. Searle & Co. Amidino derivatives useful as nitric oxide synthase inhibitors
WO1996014842A1 (en) * 1994-11-15 1996-05-23 Merck & Co., Inc. Substituted heterocycles as inhibitors of nitric oxide synthase
FR2810037B1 (fr) * 2000-06-09 2004-04-23 Aventis Pharma Sa Utilisation de derives de 2-aminothiazoline comme inhibiteurs de no-synthase inductible

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Publication number Publication date
PL370267A1 (en) 2005-05-16
WO2003039446A3 (fr) 2003-11-27
MXPA04004213A (es) 2004-07-08
SI1450750T1 (sl) 2010-02-26
CA2465877A1 (fr) 2003-05-15
IL161843A (en) 2011-08-31
CN1602311A (zh) 2005-03-30
NO20033131L (no) 2003-08-27
ES2335090T3 (es) 2010-03-22
HUP0402033A2 (hu) 2005-02-28
BR0206368A (pt) 2004-02-10
EP1450750B1 (fr) 2009-10-21
WO2003039446A2 (fr) 2003-05-15
ATE446295T1 (de) 2009-11-15
CY1110284T1 (el) 2015-01-14
US20030153605A1 (en) 2003-08-14
NO20033131D0 (no) 2003-07-08
CN1288153C (zh) 2006-12-06
US6762196B2 (en) 2004-07-13
HRP20040402A2 (en) 2004-10-31
PT1450750E (pt) 2010-01-18
JP2005517634A (ja) 2005-06-16
EP1450750A2 (fr) 2004-09-01
DK1450750T3 (da) 2010-03-08
JP4342309B2 (ja) 2009-10-14
DE60234117D1 (de) 2009-12-03
MA27143A1 (fr) 2005-01-03
IL161843A0 (en) 2005-11-20
RU2004117531A (ru) 2005-04-10

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Effective date: 20131107