JP5635991B2 - イソニコチンアミドオレキシン受容体アンタゴニスト - Google Patents

イソニコチンアミドオレキシン受容体アンタゴニスト Download PDF

Info

Publication number
JP5635991B2
JP5635991B2 JP2011534650A JP2011534650A JP5635991B2 JP 5635991 B2 JP5635991 B2 JP 5635991B2 JP 2011534650 A JP2011534650 A JP 2011534650A JP 2011534650 A JP2011534650 A JP 2011534650A JP 5635991 B2 JP5635991 B2 JP 5635991B2
Authority
JP
Japan
Prior art keywords
mmol
compound
present
alkyl
compounds
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.)
Expired - Fee Related
Application number
JP2011534650A
Other languages
English (en)
Japanese (ja)
Other versions
JP2012507538A (ja
JP2012507538A5 (enExample
Inventor
バーグマン,ジェフリー,エム.
コールマン,ポール,ジェイ.
クリスタ マターン,マミオ
クリスタ マターン,マミオ
マーサー,スワティ,ピー.
レジャー,トーマス,エス.
ローカー,アンソニー,ジェイ.
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 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 LLC filed Critical Merck Sharp and Dohme LLC
Publication of JP2012507538A publication Critical patent/JP2012507538A/ja
Publication of JP2012507538A5 publication Critical patent/JP2012507538A5/ja
Application granted granted Critical
Publication of JP5635991B2 publication Critical patent/JP5635991B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
JP2011534650A 2008-10-30 2009-10-26 イソニコチンアミドオレキシン受容体アンタゴニスト Expired - Fee Related JP5635991B2 (ja)

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 (3)

Publication Number Publication Date
JP2012507538A JP2012507538A (ja) 2012-03-29
JP2012507538A5 JP2012507538A5 (enExample) 2012-12-13
JP5635991B2 true JP5635991B2 (ja) 2014-12-03

Family

ID=41348271

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2011534650A Expired - Fee Related JP5635991B2 (ja) 2008-10-30 2009-10-26 イソニコチンアミドオレキシン受容体アンタゴニスト

Country Status (23)

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

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8003797B2 (en) 2007-08-09 2011-08-23 Merck Sharp & Dohme Corp. Pyridine carboxamide orexin receptor antagonists
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.
EP2349262B1 (en) 2008-10-30 2014-06-25 Merck Sharp & Dohme Corp. 2,5-disubstituted phenyl carboxamide orexin receptor antagonists
US8703770B2 (en) 2008-10-30 2014-04-22 Merck Sharp & Dohme Corp. Pyridazine carboxamide orexin receptor antagonists
DK3093291T3 (da) 2009-10-23 2019-07-29 Janssen Pharmaceutica Nv Disubstituerede octahy-dropyrrolo [3,4-c]pyrroler som orexinreceptormodulatorer
JP5848251B2 (ja) 2009-10-23 2016-01-27 ヤンセン ファーマシューティカ エヌ.ベー. オレキシン受容体調節因子としての縮合複素環式化合物
WO2011050200A1 (en) 2009-10-23 2011-04-28 Janssen Pharmaceutica Nv Fused heterocyclic compounds as orexin receptor modulators
WO2012110986A1 (en) * 2011-02-18 2012-08-23 Actelion Pharmaceuticals Ltd Novel pyrazole and imidazole derivatives useful as orexin antagonists
US9586962B2 (en) 2011-04-20 2017-03-07 Janssen Pharmaceutica Nv Disubstituted octahydropyrrolo [3,4-C] pyrroles as orexin receptor modulators
AR088352A1 (es) * 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
EP2811997B1 (en) 2012-02-07 2018-04-11 Eolas Therapeutics Inc. Substituted prolines/piperidines as orexin receptor antagonists
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
CN104364238A (zh) * 2012-06-15 2015-02-18 大正制药株式会社 支链烷基杂芳环衍生物
SG11201408327XA (en) * 2012-06-15 2015-02-27 Taisho Pharmaceutical Co Ltd Heteroaromatic methyl cyclic amine derivative
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
WO2015087853A1 (ja) * 2013-12-13 2015-06-18 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
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
WO2016025669A1 (en) 2014-08-13 2016-02-18 Eolas Therapeutics, Inc. Difluoropyrrolidines as orexin receptor modulators
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
PT3340971T (pt) * 2015-08-24 2024-06-05 Zogenix International Ltd Métodos de tratamento da síndrome de lennox-gastaut com utilização de fenfluramina
WO2017088759A1 (en) 2015-11-23 2017-06-01 Sunshine Lake Pharma Co., Ltd. OCTAHYDROPYRROLO [3, 4-c] PYRROLE DERIVATIVES AND USES THEREOF
PL3414241T3 (pl) 2016-02-12 2022-10-03 Astrazeneca Ab Piperydyny podstawione halo jako modulatory receptora oreksyny
IL288321B2 (en) 2016-03-10 2025-08-01 Janssen Pharmaceutica Nv Methods of treating depression using orexin-2 receptor antagonists
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

Family Cites Families (161)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3914250A (en) 1974-08-01 1975-10-21 American Home Prod 1,4-Diazepino{8 6,5,4-jk{9 carbazoles
CA1258454A (en) 1982-08-10 1989-08-15 Leo Alig Phenethanolamines
IT1159765B (it) 1982-09-28 1987-03-04 Zanussi A Spa Industrie Macchina lavabiancheria di tipo modulare
WO1990005525A1 (en) 1988-11-23 1990-05-31 Pfizer Inc. Quinuclidine derivatives as substance p antagonists
US5232929A (en) 1990-11-28 1993-08-03 Pfizer Inc. 3-aminopiperidine derivatives and related nitrogen containing heterocycles and pharmaceutical compositions and use
US5112820A (en) 1990-03-05 1992-05-12 Sterling Drug Inc. Anti-glaucoma compositions containing 2- and 3-aminomethyl-6-arylcarbonyl- or 6-phenylthio-2,3-dihydropyrrolo-(1,2,3-de)-1,4-benzoxazines and method of use thereof
US5081122A (en) 1990-03-05 1992-01-14 Sterling Drug Inc. Antiglaucoma compositions containing 4-arylcarbonyl-1-(4-morpholinyl)-lower-alkyl)-1H-indoles and method of use thereof
US5013837A (en) 1990-03-08 1991-05-07 Sterling Drug Inc. 3-Arylcarbonyl-1H-indole-containing compounds
US4973587A (en) 1990-03-08 1990-11-27 Sterling Drug Inc. 3-arylcarbonyl-1-aminoalkyl-1H-indole-containing antiglaucoma method
ATE154354T1 (de) 1991-02-11 1997-06-15 Merck Sharp & Dohme Azabicyclische verbindungen, diese enthaltende pharmazeutische zubereitungen und ihre therapeutische verwendung
EP0573522B1 (en) 1991-03-01 1994-12-14 Pfizer Inc. 1-azabicyclo[3.2.2]nonan-3-amine derivatives
CA2112397A1 (en) 1991-08-20 1993-03-04 Raymond Baker Azacyclic compounds, processes for their preparation and pharmaceutical compositions containing them
GB9211193D0 (en) 1992-05-27 1992-07-08 Merck Sharp & Dohme Therapeutic agents
FR2692575B1 (fr) 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
US5637699A (en) 1992-06-29 1997-06-10 Merck & Co., Inc. Process for preparing morpholine tachykinin receptor antagonists
US5387595A (en) 1992-08-26 1995-02-07 Merck & Co., Inc. Alicyclic compounds as tachykinin receptor antagonists
US5536716A (en) 1992-12-11 1996-07-16 Merck & Co., Inc. Spiro piperidines and homologs which promote release of growth hormone
US5292736A (en) 1993-02-26 1994-03-08 Sterling Winthrop Inc. Morpholinoalkylindenes as antiglaucoma agents
US5496833A (en) 1993-04-13 1996-03-05 Merck Sharp & Dohme Limited Piperidine tachykinin receptor antagonists
BR9509610A (pt) 1994-11-07 1997-10-28 Pfizer Ligandos específicos de neuropeptideo Y1
US5532237A (en) 1995-02-15 1996-07-02 Merck Frosst Canada, Inc. Indole derivatives with affinity for the cannabinoid receptor
US5585388A (en) 1995-04-07 1996-12-17 Sibia Neurosciences, Inc. Substituted pyridines useful as modulators of acetylcholine receptors
US6194581B1 (en) 1995-04-07 2001-02-27 Merck & Co., Inc. Substituted pyridines useful as modulators of acetylcholine receptors
US5831115A (en) 1995-04-21 1998-11-03 Abbott Laboratories Inhibitors of squalene synthase and protein farnesyltransferase
US5739106A (en) 1995-06-07 1998-04-14 Rink; Timothy J. Appetite regulating compositions
WO2008109437A2 (en) 2007-03-02 2008-09-12 Northwestern University Compositions and treatments for seizure-related disorders
FR2741621B1 (fr) 1995-11-23 1998-02-13 Sanofi Sa Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant
WO1997020821A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl derivatives
AU7692996A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Receptor antagonists
WO1997020822A1 (en) 1995-12-01 1997-06-12 Novartis Ag Quinazolin-2,4-diazirines as npy receptor antagonist
WO1997020820A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl compounds
WO1997019682A1 (en) 1995-12-01 1997-06-05 Synaptic Pharmaceutical Corporation Aryl sulfonamide and sulfamide derivatives and uses thereof
TW432073B (en) 1995-12-28 2001-05-01 Pfizer Pyrazolopyridine compounds
WO1997028149A1 (en) 1996-02-02 1997-08-07 Merck & Co., Inc. Method for raising hdl cholesterol levels
WO1997029079A1 (en) 1996-02-06 1997-08-14 Japan Tobacco Inc. Novel compounds and pharmaceutical use thereof
GB9606805D0 (en) 1996-03-30 1996-06-05 Glaxo Wellcome Inc Medicaments
CA2273102A1 (en) 1996-12-03 1998-06-11 Banyu Pharmaceutical Co., Ltd. Urea derivatives
CA2274592C (en) 1996-12-12 2007-03-13 Banyu Pharmaceutical Co., Ltd. Pyrazole derivatives
DE69720038T2 (de) 1996-12-13 2003-08-28 Banyu Pharmaceutical Co., Ltd. Aminopyrazolderivate
DE69729315T2 (de) 1996-12-16 2005-06-23 Banyu Pharmaceutical Co., Ltd. Aminopyrazolderivate
ES2213892T3 (es) 1997-01-21 2004-09-01 Smithkline Beecham Corporation Nuevos moduladores del receptor de canabinoides.
CN1246845A (zh) 1997-02-04 2000-03-08 纳幕尔杜邦公司 杀菌的羧酰胺
RU2203272C2 (ru) 1997-02-21 2003-04-27 Байер Акциенгезелльшафт Замещенные бициклические соединения, исходные и промежуточные продукты для их получения и фармацевтическая композиция на их основе
WO1998040356A1 (en) 1997-03-12 1998-09-17 Banyu Pharmaceutical Co., Ltd. Drugs containing aminopyridine derivatives as the active ingredient
US5948777A (en) 1997-03-18 1999-09-07 Smithkline Beecham Corporation Cannabinoid receptor agonists
FR2761265B1 (fr) 1997-03-28 1999-07-02 Sanofi Sa Composition pharmaceutique pour l'administration orale d'un derive du n-piperidino-3-pyrazolecarboxamide, de ses sels et de leurs solvates
FR2761266B1 (fr) 1997-03-28 1999-07-02 Sanofi Sa Composition pharmaceutique formee par granulation humide pour l'administration orale d'un derive du n-piperidino-3- pyrazolecarboxamide, de ses sels et de leurs solvates
AU7079498A (en) 1997-04-23 1998-11-13 Banyu Pharmaceutical Co., Ltd. Neuropeptide y receptor antagonist
US6001836A (en) 1997-05-28 1999-12-14 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: cyanoguanidine derivatives
KR20010021696A (ko) 1997-07-11 2001-03-15 미즈노 마사루 퀴놀린 화합물 및 그의 의약용도
WO1999015516A1 (en) 1997-09-25 1999-04-01 Banyu Pharmaceutical Co., Ltd. Novel neuropeptide y receptor antagonists
US6362009B1 (en) 1997-11-21 2002-03-26 Merck & Co., Inc. Solid phase synthesis of heterocycles
WO1999027965A1 (en) 1997-11-28 1999-06-10 Banyu Pharmaceutical Co., Ltd. Antihyperlipemic agents
US6174901B1 (en) 1998-12-18 2001-01-16 Amgen Inc. Substituted pyridine and pyridazine compounds and methods of use
JP2002510688A (ja) 1998-04-02 2002-04-09 ニューロゲン コーポレイション アミノアルキル置換9H−ピリジノ[2,3−b]インドールおよび9H−ピリミジノ[4,5−b]インドール誘導体
CN1289475C (zh) 1998-04-29 2006-12-13 奥索-麦克尼尔药品公司 在肥胖症和其它病症的治疗中用作神经肽yy5受体配体的n-取代的氨基1,2,3,4-四氢化萘
US6329395B1 (en) 1998-06-08 2001-12-11 Schering Corporation Neuropeptide Y5 receptor antagonists
HN1998000027A (es) 1998-08-19 1999-06-02 Bayer Ip Gmbh Arilsulfonamidas y analagos
DE19837627A1 (de) 1998-08-19 2000-02-24 Bayer Ag Neue Aminosäureester von Arylsulfonamiden und Analoga
US6358951B1 (en) 1998-08-21 2002-03-19 Pfizer Inc. Growth hormone secretagogues
US6337332B1 (en) 1998-09-17 2002-01-08 Pfizer Inc. Neuropeptide Y receptor antagonists
JP2002529464A (ja) 1998-11-10 2002-09-10 メルク エンド カムパニー インコーポレーテッド Y5受容体拮抗薬としてのスピロインドリン類
PL350428A1 (en) * 1999-02-24 2002-12-16 Hoffmann La Roche 3-phenylpyridine derivatives and their use as nk-1 receptor antagonists
US6340683B1 (en) 1999-04-22 2002-01-22 Synaptic Pharmaceutical Corporation Selective NPY (Y5) antagonists (triazines)
ATE361917T1 (de) 1999-04-22 2007-06-15 Lundbeck & Co As H Selektive npy(y5)-antagonisten
HK1041263A1 (zh) 1999-05-05 2002-07-05 Ortho-Mcneil Pharmaceutical, Inc. 可用於治疗肥胖和其他疾病的3a,4,5,9b-四氢-1h-苯并[e]吲-2-基胺衍生的神经肽y受体配体
CA2373510A1 (en) 1999-05-12 2000-11-23 Ortho-Mcneil Pharmaceutical, Inc. Pyrazole carboxamides useful for the treatment of obesity and other disorders
AU773892B2 (en) 1999-06-30 2004-06-10 H. Lundbeck A/S Selective NPY (Y5) antagonists
WO2001007409A1 (en) 1999-07-23 2001-02-01 Astrazeneca Uk Limited Carbazole derivatives and their use as neuropeptide y5 receptor ligands
ES2250170T3 (es) 1999-07-28 2006-04-16 Ortho-Mcneil Pharmaceutical, Inc. Derivados de aminas y de amidas utilizados como ligando para el receptor y5 del neuropeptido y, util en el tratamiento de la obesidad y otros trantornos.
US6462053B1 (en) 1999-08-20 2002-10-08 Banyu Pharmaceutical Co., Ltd. Spiro compounds
TWI279402B (en) 1999-08-20 2007-04-21 Banyu Pharma Co Ltd Spiro compounds having NPY antagonistic activities and agents containing the same
WO2001021169A1 (en) 1999-09-20 2001-03-29 Takeda Chemical Industries, Ltd. Mch antagonists
US7115750B1 (en) 1999-09-20 2006-10-03 Takeda Pharmaceutical Company Limited Melanin concentrating hormone antagonist
US6414002B1 (en) 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
IL148903A0 (en) 1999-09-30 2002-09-12 Neurogen Corp Certain alkylene diamine-substituted heterocycles
US6372743B1 (en) 1999-09-30 2002-04-16 Neurogen Corporation Certain alkylene diamine-substituted pyrazlo (1,5-a)-1,5-pyrimidines and pyrazolo (1,5-a) 1,3,5-triazines
WO2001023388A2 (en) 1999-09-30 2001-04-05 Neurogen Corporation AMINO SUBSTITUTED PYRAZOLO[1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES
CZ20022100A3 (cs) 1999-12-16 2002-09-11 Schering Corporation Substituované imidazolové deriváty a farmaceutický prostředek
WO2001056592A1 (en) 2000-02-01 2001-08-09 Novo Nordisk A/S Use of compounds for the regulation of food intake
EP1254115A2 (en) 2000-02-11 2002-11-06 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators for treating respiratory and non-respiratory diseases
WO2001062738A1 (en) 2000-02-22 2001-08-30 Banyu Pharmaceutical Co., Ltd. Novel imidazoline compounds
US6531478B2 (en) 2000-02-24 2003-03-11 Cheryl P. Kordik Amino pyrazole derivatives useful for the treatment of obesity and other disorders
FR2805817B1 (fr) 2000-03-03 2002-04-26 Aventis Pharma Sa Compositions pharmaceutiques contenant des derives d'azetidine, les nouveaux derives d'azetidine et leur preparation
FR2805818B1 (fr) 2000-03-03 2002-04-26 Aventis Pharma Sa Derives d'azetidine, leur preparation et les compositions pharmaceutiques les contenant
FR2805810B1 (fr) 2000-03-03 2002-04-26 Aventis Pharma Sa Compositions pharmaceutiques contenant des derives de 3- amino-azetidine, les nouveaux derives et leur preparation
EP1132389A1 (en) 2000-03-06 2001-09-12 Vernalis Research Limited New aza-indolyl derivatives for the treatment of obesity
EP1142886A1 (en) 2000-04-07 2001-10-10 Aventis Pharma Deutschland GmbH Percyquinnin, a process for its production and its use as a pharmaceutical
US6930185B2 (en) 2000-04-28 2005-08-16 Takeda Chemical Industries, Ltd. Melanin-concentrating hormone antagonist
GB0010757D0 (en) 2000-05-05 2000-06-28 Astrazeneca Ab Chemical compounds
GB0011013D0 (en) 2000-05-09 2000-06-28 Astrazeneca Ab Chemical compounds
WO2001085173A1 (en) 2000-05-10 2001-11-15 Bristol-Myers Squibb Company Alkylamine derivatives of dihydropyridine npy antagonists
US6432960B2 (en) 2000-05-10 2002-08-13 Bristol-Myers Squibb Company Squarate derivatives of dihydropyridine NPY antagonists
US6444675B2 (en) 2000-05-10 2002-09-03 Bristol-Myers Squibb Company 4-alkyl and 4-cycloalkyl derivatives of dihydropyridine NPY antagonists
CA2408486A1 (en) 2000-05-11 2001-11-15 Bristol-Myers Squibb Company Tetrahydroisoquinoline analogs useful as growth hormone secretagogues
US7229986B2 (en) 2000-05-16 2007-06-12 Takeda Pharmaceutical Company Ltd. Melanin-concentrating hormone antagonist
EP1286697A2 (en) 2000-05-17 2003-03-05 Eli Lilly And Company Method for selectively inhibiting ghrelin action
US6391881B2 (en) 2000-05-19 2002-05-21 Bristol-Myers Squibb Company Thiourea derivatives of dihydropyridine NPY antagonists
SE0001899D0 (sv) 2000-05-22 2000-05-22 Pharmacia & Upjohn Ab New compounds
JP2004504303A (ja) 2000-07-05 2004-02-12 シナプティック・ファーマスーティカル・コーポレーション 選択的メラニン凝集ホルモン−1(mch1)受容体アンタゴニストおよびその使用
US6569861B2 (en) 2000-07-06 2003-05-27 Neurogen Corporation Melanin concentrating hormone receptor ligands
US20020187938A1 (en) 2000-07-24 2002-12-12 Romano Deghenghi Ghrelin antagonists
CN1277828C (zh) 2000-07-31 2006-10-04 霍夫曼-拉罗奇有限公司 哌嗪衍生物
EP1322628A2 (en) 2000-09-14 2003-07-02 Schering Corporation Substituted urea neuropeptide y y5 receptor antagonists
CA2419388A1 (en) 2000-10-13 2002-04-25 Eli Lilly And Company Substituted dipeptides as growth hormone secretagogues
AU2002221670B2 (en) 2000-10-16 2006-11-02 F. Hoffmann-La Roche Ag Indoline derivatives and their use as 5-HT2 receptor ligands
AU2002227170A1 (en) 2000-11-03 2002-05-15 Wyeth Cycloalkyl(b)(1,4)diazepino(6,7,1-hi)indoles and derivatives
ATE470662T1 (de) 2000-11-20 2010-06-15 Biovitrum Ab Publ Piperazinylpyrazinverbindungen als agonisten oder antagonisten am serotonin-5ht-2-rezeptor
DE60139021D1 (de) 2000-11-20 2009-07-30 Biovitrum Ab Publ Piperazinylpyrazinverbindungen als antagonisten des serotonin-5-ht2-rezeptors
ES2249384T3 (es) 2000-12-12 2006-04-01 Neurogen Corporation Espiro(isobenzofuran-1,4'-piperadin)-3-onas y 3h-espirobenzofuran-1,4-piperidinas.
GB0030710D0 (en) 2000-12-15 2001-01-31 Hoffmann La Roche Piperazine derivatives
NZ526174A (en) 2000-12-21 2004-12-24 Schering Corp Heteroaryl urea neuropeptide Y Y5 receptor antagonists
MXPA03005744A (es) 2000-12-22 2003-09-05 Schering Corp Antagonistas de piperidina mch y su uso en el tratamiento de obesidad.
CA2432085C (en) 2000-12-27 2009-02-24 F. Hoffmann-La Roche Ag Indole derivatives and their use as 5-ht2b and 5-ht2c receptor ligands
MXPA03006918A (es) 2001-02-02 2004-05-24 Takeda Chemical Industries Ltd Compuestos heterociclicos fusionados.
US7034056B2 (en) 2001-03-21 2006-04-25 Pharmacopeia Drug Discovery, Inc. Aryl and biaryl compounds having MCH modulatory activity
US6900329B2 (en) 2001-03-21 2005-05-31 Schering Corporation MCH antagonists and their use in the treatment of obesity
SI1373216T1 (en) 2001-03-22 2005-06-30 Solvay Pharmaceuticals B.V. 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
JP4280073B2 (ja) 2001-04-12 2009-06-17 ファーマコペイア ドラッグ ディスカバリー, インコーポレイテッド Mchアンタゴニストとして使用されるアリールピペリジンおよびビアリールピペリジン
FR2824825B1 (fr) 2001-05-15 2005-05-06 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2002094825A1 (en) 2001-05-22 2002-11-28 Banyu Pharmaceutical Co., Ltd. Novel spiropiperidine derivative
US6953801B2 (en) 2001-05-22 2005-10-11 Neurogen Corporation Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues
WO2003000180A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
US7253172B2 (en) 2001-06-20 2007-08-07 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
ATE370943T1 (de) 2001-06-27 2007-09-15 Smithkline Beecham Corp Fluoropyrrolidine als dipeptidyl-peptidase inhibitoren
JP4300108B2 (ja) 2001-06-27 2009-07-22 スミスクライン ビーチャム コーポレーション ジペプチジルペプチダーゼ阻害剤としてのピロリジン類
CN1990468A (zh) 2001-06-27 2007-07-04 史密丝克莱恩比彻姆公司 作为二肽酶抑制剂的氟代吡咯烷
CA2419888A1 (en) 2001-06-27 2003-01-09 Probiodrug Ag Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis
EP1404675B1 (en) 2001-07-03 2008-03-12 Novo Nordisk A/S Dpp-iv-inhibiting purine derivatives for the treatment of diabetes
PL366624A1 (en) 2001-07-05 2005-02-07 Synaptic Pharmaceutical Corporation Substituted anilinic piperidines as mch selective antagonists
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
AU2002319627A1 (en) 2001-07-20 2003-03-03 Merck And Co., Inc. Substituted imidazoles as cannabinoid receptor modulators
BRPI0104510B8 (pt) 2001-07-27 2021-05-25 Embrapa Pesquisa Agropecuaria peptídeos antibióticos da família das phylloseptinas isolados da secreção da pele de phylloseptina hypocondrialis e composição antimicrobiana relacionada
IL160139A0 (en) 2001-08-07 2004-06-20 Banyu Pharma Co Ltd Spiro compounds
GB0126292D0 (en) 2001-11-01 2002-01-02 Smithkline Beecham Plc Compounds
GB0130341D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
JP2005320249A (ja) 2002-05-01 2005-11-17 Banyu Pharmaceut Co Ltd 2−アミノピラジン誘導体の製造方法
AR040241A1 (es) 2002-06-10 2005-03-23 Merck & Co Inc Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia
US7105526B2 (en) 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
US6869966B2 (en) 2002-09-30 2005-03-22 Banyu Pharmaceutical Co., Ltd. N-substituted-2-oxodihydropyridine derivatives
US20040116479A1 (en) 2002-10-04 2004-06-17 Fortuna Haviv Method of inhibiting angiogenesis
MY134457A (en) 2002-11-22 2007-12-31 Merck & Co Inc Substituted amides
JO2397B1 (en) 2002-12-20 2007-06-17 ميرك شارب اند دوم كوربوريشن Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors
AU2004252109B2 (en) 2003-06-11 2010-04-08 Merck Sharp & Dohme Corp. Substituted 3-alkyl and 3-alkenyl azetidine derivatives
EP1669348A4 (en) 2003-09-30 2009-03-11 Eisai R&D Man Co Ltd NEW ANTIPILIC AGENT CONTAINING A HETEROCYCLIC COMPOUND
HUP0400405A3 (en) 2004-02-10 2009-03-30 Sanofi Synthelabo Pyrimidine derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates
EP1715867A4 (en) 2004-02-12 2009-04-15 Merck & Co Inc BIPYRIDYLAMIDE AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
WO2006103120A2 (en) 2005-04-01 2006-10-05 Insa Rouen New heterocyclic compounds, their preparation and their use as medicaments, in particular as anti-alzheimer agents
CA2603766A1 (en) 2005-04-12 2006-10-19 Merck & Co., Inc. Amidopropoxyphenyl orexin receptor antagonists
WO2007011760A2 (en) 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin
JP2009516742A (ja) * 2005-11-22 2009-04-23 メルク エンド カムパニー インコーポレーテッド インドールオレキシン受容体アンタゴニスト
US20080214301A1 (en) 2007-03-02 2008-09-04 Wildtangent, Inc. In-game advertisements
US8410142B2 (en) 2007-03-02 2013-04-02 Merck Sharp & Dohme Corp. Bipyridine carboxamide orexin receptor antagonists
JP5341084B2 (ja) 2007-08-03 2013-11-13 エフ.ホフマン−ラ ロシュ アーゲー Taar1リガンドとしてのピリジンカルボキシアミド及びベンズアミド誘導体
US8003797B2 (en) 2007-08-09 2011-08-23 Merck Sharp & Dohme Corp. Pyridine carboxamide orexin receptor antagonists
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.
US8703770B2 (en) 2008-10-30 2014-04-22 Merck Sharp & Dohme Corp. Pyridazine carboxamide orexin receptor antagonists
EP2349262B1 (en) * 2008-10-30 2014-06-25 Merck Sharp & Dohme Corp. 2,5-disubstituted phenyl carboxamide orexin receptor antagonists
EP2438041A4 (en) 2009-06-01 2012-11-21 Merck Sharp & Dohme PYRAZINE-carboxamide-orexin receptor Antagonist

Also Published As

Publication number Publication date
IL212436A0 (en) 2011-06-30
CN102272103A (zh) 2011-12-07
MX2011004551A (es) 2011-05-25
NI201100084A (es) 2011-11-03
CA2741644C (en) 2013-05-07
EA201170624A1 (ru) 2011-12-30
ECSP11011019A (es) 2011-05-31
CL2011000976A1 (es) 2012-02-24
KR101320245B1 (ko) 2013-10-30
ZA201103156B (en) 2012-01-25
JP2012507538A (ja) 2012-03-29
WO2010051236A1 (en) 2010-05-06
CO6361994A2 (es) 2012-01-20
CN102272103B (zh) 2015-10-21
EP2350010B1 (en) 2014-03-26
KR20110071101A (ko) 2011-06-28
US20110201591A1 (en) 2011-08-18
CA2741644A1 (en) 2010-05-06
EP2350010A1 (en) 2011-08-03
CR20110228A (es) 2011-06-24
TN2011000171A1 (en) 2012-12-17
AU2009308980A1 (en) 2010-05-06
MA32804B1 (fr) 2011-11-01
NZ592544A (en) 2013-01-25
DOP2011000120A (es) 2011-10-15
BRPI0919876A2 (pt) 2015-08-18
US8592457B2 (en) 2013-11-26
PE20110852A1 (es) 2011-11-25
AU2009308980B2 (en) 2013-02-28
BRPI0919876A8 (pt) 2016-02-10

Similar Documents

Publication Publication Date Title
JP5635991B2 (ja) イソニコチンアミドオレキシン受容体アンタゴニスト
JP5947906B2 (ja) 2−ピリジルオキシ−4−ニトリルオレキシン受容体アンタゴニスト
US8003797B2 (en) Pyridine carboxamide orexin receptor antagonists
US8349872B2 (en) Tripyridyl carboxamide orexin receptor antagonists
JP5639564B2 (ja) ピリジルピペリジン・オレキシン受容体アンタゴニスト
EP2349267B1 (en) Pyridazine carboxamide orexin receptor antagonists
EP2349262B1 (en) 2,5-disubstituted phenyl carboxamide orexin receptor antagonists
JP5479893B2 (ja) 置換ジアゼパンオレキシン受容体アンタゴニスト
US20120065205A1 (en) Pyrazine carboxamide orexin receptor antagonists
JP2012506377A (ja) 2,4−二置換フェニルカルボキサミド・オレキシン受容体アンタゴニスト
JP2012506376A (ja) 2,5−二置換モルホリンオレキシン受容体アンタゴニスト
JP2012506378A (ja) 2,3−二置換フェニルカルボキサミド・オレキシン受容体アンタゴニスト
JP2012506375A (ja) 2,5−二置換ピペリジンオレキシン受容体アンタゴニスト
JP2010520206A (ja) ビピリジンカルボキサミドオレキシン受容体アンタゴニスト
JP2010528007A (ja) シクロプロピルピロリジンオレキシン受容体アンタゴニスト
JP2012506379A (ja) 二置換アゼパンオレキシン受容体アンタゴニスト
JP2012506374A (ja) 2,5−二置換ピペリジンオレキシン受容体アンタゴニスト
US20120101106A1 (en) Tetrahydronapthyridine Orexin Receptor Antagonists

Legal Events

Date Code Title Description
RD03 Notification of appointment of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7423

Effective date: 20120308

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20121024

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20121024

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A712

Effective date: 20130223

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20140212

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20140213

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140508

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140515

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140808

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20140930

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20141017

LAPS Cancellation because of no payment of annual fees