AU2009308980B2 - Isonicotinamide orexin receptor antagonists - Google Patents

Isonicotinamide orexin receptor antagonists Download PDF

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Publication number
AU2009308980B2
AU2009308980B2 AU2009308980A AU2009308980A AU2009308980B2 AU 2009308980 B2 AU2009308980 B2 AU 2009308980B2 AU 2009308980 A AU2009308980 A AU 2009308980A AU 2009308980 A AU2009308980 A AU 2009308980A AU 2009308980 B2 AU2009308980 B2 AU 2009308980B2
Authority
AU
Australia
Prior art keywords
methyl
carboxamide
bipyridine
present
mmol
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.)
Ceased
Application number
AU2009308980A
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English (en)
Other versions
AU2009308980A1 (en
Inventor
Jeffrey M. Bergman
Paul J. Coleman
Mamio Christa Mattern
Swati P. Mercer
Thomas S. Reger
Anthony J. Roecker
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 Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme Ltd
Merck Sharp and Dohme 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 Merck Sharp and Dohme Ltd, Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme Ltd
Publication of AU2009308980A1 publication Critical patent/AU2009308980A1/en
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Alteration of Name(s) of Applicant(s) under S113 Assignors: MERCK SHARP & DOHME CORP.
Application granted granted Critical
Publication of AU2009308980B2 publication Critical patent/AU2009308980B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D417/14—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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Anesthesiology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
AU2009308980A 2008-10-30 2009-10-26 Isonicotinamide orexin receptor antagonists Ceased AU2009308980B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US19778908P 2008-10-30 2008-10-30
US61/197,789 2008-10-30
US18057409P 2009-05-22 2009-05-22
US61/180,574 2009-05-22
PCT/US2009/061987 WO2010051236A1 (en) 2008-10-30 2009-10-26 Isonicotinamide orexin receptor antagonists

Publications (2)

Publication Number Publication Date
AU2009308980A1 AU2009308980A1 (en) 2010-05-06
AU2009308980B2 true AU2009308980B2 (en) 2013-02-28

Family

ID=41348271

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2009308980A Ceased AU2009308980B2 (en) 2008-10-30 2009-10-26 Isonicotinamide orexin receptor antagonists

Country Status (23)

Country Link
US (1) US8592457B2 (OSRAM)
EP (1) EP2350010B1 (OSRAM)
JP (1) JP5635991B2 (OSRAM)
KR (1) KR101320245B1 (OSRAM)
CN (1) CN102272103B (OSRAM)
AU (1) AU2009308980B2 (OSRAM)
BR (1) BRPI0919876A8 (OSRAM)
CA (1) CA2741644C (OSRAM)
CL (1) CL2011000976A1 (OSRAM)
CO (1) CO6361994A2 (OSRAM)
CR (1) CR20110228A (OSRAM)
DO (1) DOP2011000120A (OSRAM)
EA (1) EA201170624A1 (OSRAM)
EC (1) ECSP11011019A (OSRAM)
IL (1) IL212436A0 (OSRAM)
MA (1) MA32804B1 (OSRAM)
MX (1) MX2011004551A (OSRAM)
NI (1) NI201100084A (OSRAM)
NZ (1) NZ592544A (OSRAM)
PE (1) PE20110852A1 (OSRAM)
TN (1) TN2011000171A1 (OSRAM)
WO (1) WO2010051236A1 (OSRAM)
ZA (1) ZA201103156B (OSRAM)

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AR072899A1 (es) 2008-08-07 2010-09-29 Merck Sharp & Dohme Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad.
WO2010051238A1 (en) 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. Pyridazine carboxamide orexin receptor antagonists
CA2741648A1 (en) 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. 2,5-disubstituted phenyl carboxamide orexin receptor antagonists
US8653263B2 (en) 2009-10-23 2014-02-18 Janssen Pharmaceutica Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators
US8680275B2 (en) 2009-10-23 2014-03-25 Janssen Pharmaceutica Nv Fused heterocyclic compounds as orexin receptor modulators
US9062044B2 (en) 2009-10-23 2015-06-23 Janssen Pharmaceutica Nv Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators
JP5987005B2 (ja) * 2011-02-18 2016-09-06 アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ オレキシン拮抗薬として有用な新規なピラゾール及びイミダゾール誘導体
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US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
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JP5907310B2 (ja) * 2013-12-13 2016-04-26 大正製薬株式会社 オキサジナン化合物の結晶形及びその製造方法
JP5930010B2 (ja) * 2013-12-13 2016-06-08 大正製薬株式会社 ヘテロ芳香環メチル環状アミン誘導体を含有する医薬
EP2915811A1 (en) * 2014-03-04 2015-09-09 Centre Régional de Lutte contre le Cancer - Centre François Baclesse MCL-1 modulating compounds for cancer treatment
UY36272A (es) 2014-08-13 2016-02-29 Eolas Therapeutics Inc Difluoropirrolidinas como moduladores de los receptores de orexinas
WO2016100161A1 (en) * 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Ethyldiamine orexin receptor antagonists
WO2016101118A1 (en) * 2014-12-23 2016-06-30 Merck Sharp & Dohme Corp. Amidoethyl azole orexin receptor antagonists
HUE066912T2 (hu) * 2015-08-24 2024-09-28 Zogenix International Ltd Lennox-Gastaut szindróma kezelési eljárása fenfluramin alkalmazásával
CN106749269B (zh) 2015-11-23 2019-01-04 广东东阳光药业有限公司 八氢吡咯并[3,4-c]吡咯衍生物及其用途
TWI710557B (zh) 2016-02-12 2020-11-21 美商伊歐拉斯治療學公司 作為食慾素受體調節劑之經鹵素取代之六氫吡啶
BR112018067906A2 (pt) 2016-03-10 2019-01-29 Janssen Pharmaceutica Nv métodos de tratamento de depressão usando antagonistas do receptor de orexina-2
GB201702174D0 (en) 2017-02-09 2017-03-29 Benevolentai Bio Ltd Orexin receptor antagonists
GB201707504D0 (en) 2017-05-10 2017-06-21 Benevolentai Bio Ltd Orexin receptor antagonists
GB201707499D0 (en) 2017-05-10 2017-06-21 Benevolentai Bio Ltd Orexin receptor antagonists
CN109280027A (zh) * 2018-12-13 2019-01-29 康化（上海）新药研发有限公司 一种5,6-二甲氧基-2-吡啶甲酸的合成方法
CN116600803A (zh) * 2020-11-02 2023-08-15 默沙东有限责任公司 大环脲食欲素受体激动剂

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