PE20110852A1 - Antagonistas del receptor de orexina de isonicotinamida - Google Patents

Antagonistas del receptor de orexina de isonicotinamida

Info

Publication number
PE20110852A1
PE20110852A1 PE2011000959A PE2011000959A PE20110852A1 PE 20110852 A1 PE20110852 A1 PE 20110852A1 PE 2011000959 A PE2011000959 A PE 2011000959A PE 2011000959 A PE2011000959 A PE 2011000959A PE 20110852 A1 PE20110852 A1 PE 20110852A1
Authority
PE
Peru
Prior art keywords
halogen
phenyl
isonicotinamide
alkyl
hydroxyl
Prior art date
Application number
PE2011000959A
Other languages
English (en)
Inventor
Jeffrey M Bergman
Paul J Coleman
Mamio Christa Mattern
Swati P Mercer
Thomas S Reger
Anthony J Roecker
Original Assignee
Merck Sharp & Dohme
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 & Dohme filed Critical Merck Sharp & Dohme
Publication of PE20110852A1 publication Critical patent/PE20110852A1/es

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
    • C07D401/04—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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE ISONICOTINAMIDA DE FORMULA I DONDE: A1 ES FENILO, PIRIDILO, NAFTILO, ENTRE OTROS; A2 ES FENILO, HETEROARILO, ENTRE OTROS; A3 ES FENILO, TIAZOLILO, CICLOALQUILO C3-C6, ENTRE OTROS; R1a, R1b Y R1c SON CADA UNO H, HALOGENO, ALQUILO C1-C6 SUSTITUIDO O NO CON HALOGENO, HIDROXILO, NAFTILO O FENILO, ENTRE OTROS; R2a, R2b Y R2c SON CADA UNO H, HALOGENO, ALQUILO C1-C6 SUSTITUIDO O NO CON HALOGENO, HIDROXILO, NAFTILO O FENILO, ENTRE OTROS; R3a, R3b Y R3c SON CADA UNO H, HALOGENO, HIDROXILO, ALQUILO C1-C6. ENTRE OTROS; R4 Y R5 SON CADA UNO H, ALQUILO C1-C6 SUSTITUIDOS O NO; R6 ES H. ALQUILO C1-C6, CICLOALQUILO C3-C6 OPCIONALMENTE SUSTITUIDO. SON COMPUESTOS PREFERIDOS: N-(3,4-DIMETOXIBENCIL)-2-(3,5-DIMETILFENIL)-5-(1-METIL-1H-PIRAZOL-4-IL)ISONICOTINAMIDA; 5''-CLORO-N-[(5,6-DIMETOXIPIRIDIN-2-IL)METIL]-2,3':6',3''-TERPIRIDIN-4'-CARBOXAMIDA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DE LOS RECEPTORES DE OREXINA UTILES EN EL TRATAMIENTO DE ENFERMEDADES NEUROLOGICAS Y PSIQUIATRICAS
PE2011000959A 2008-10-30 2009-10-26 Antagonistas del receptor de orexina de isonicotinamida PE20110852A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US19778908P 2008-10-30 2008-10-30
US18057409P 2009-05-22 2009-05-22

Publications (1)

Publication Number Publication Date
PE20110852A1 true PE20110852A1 (es) 2011-11-25

Family

ID=41348271

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2011000959A PE20110852A1 (es) 2008-10-30 2009-10-26 Antagonistas del receptor de orexina de isonicotinamida

Country Status (23)

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

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008284268A1 (en) 2007-08-09 2009-02-12 Merck & Co., Inc. 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.
WO2010051237A1 (en) 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. 2,5-disubstituted phenyl carboxamide orexin receptor antagonists
AU2009308982A1 (en) 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. Pyridazine carboxamide orexin receptor antagonists
CA2778484C (en) 2009-10-23 2018-07-31 Janssen Pharmaceutica Nv Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators
EP2491034B1 (en) 2009-10-23 2013-12-18 Janssen Pharmaceutica, N.V. Fused heterocyclic compounds as orexin receptor modulators
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
CA2823877C (en) * 2011-02-18 2020-01-07 Actelion Pharmaceuticals Ltd Novel pyrazole and imidazole derivatives useful as orexin antagonists
WO2012145581A1 (en) 2011-04-20 2012-10-26 Janssen Pharmaceutica Nv Disubstituted octahy-dropyrrolo [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
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
AU2013217323A1 (en) 2012-02-07 2014-08-28 Eolas Therapeutics, Inc. Substituted prolines / piperidines as orexin receptor antagonists
RS55675B1 (sr) 2012-06-15 2017-06-30 Taisho Pharmaceutical Co Ltd Jedinjenja 1,3-oksazolidina ili 1,3-oksazinana kao antagonisti oreksinskog receptora
SG11201408316SA (en) * 2012-06-15 2015-03-30 Taisho Pharmaceutical Co Ltd Branched chain alkyl heteroaromatic ring 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
UY36272A (es) 2014-08-13 2016-02-29 Eolas Therapeutics Inc Difluoropirrolidinas como moduladores de los receptores de orexinas
US10011595B2 (en) 2014-12-19 2018-07-03 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
CA3005918C (en) 2015-11-23 2023-10-17 Sunshine Lake Pharma Co., Ltd. Octahydropyrrolo[3,4-c]pyrrole derivatives and uses thereof
TN2018000280A1 (en) 2016-02-12 2020-01-16 Astrazeneca Ab Halo-substituted piperidines as orexin receptor modulators.
CA2960253A1 (en) 2016-03-10 2017-09-10 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
GB201707499D0 (en) 2017-05-10 2017-06-21 Benevolentai Bio Ltd Orexin receptor antagonists
GB201707504D0 (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

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
MX18467A (es) 1988-11-23 1993-07-01 Pfizer Agentes terapeuticos de quinuclidinas
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
US4973587A (en) 1990-03-08 1990-11-27 Sterling Drug Inc. 3-arylcarbonyl-1-aminoalkyl-1H-indole-containing antiglaucoma method
US5013837A (en) 1990-03-08 1991-05-07 Sterling Drug Inc. 3-Arylcarbonyl-1H-indole-containing compounds
US5242930A (en) 1991-02-11 1993-09-07 Merck Sharp & Dohme Ltd. Azabicyclic compounds, pharmaceutical compositions containing them and their use in therapy
ATE115581T1 (de) 1991-03-01 1994-12-15 Pfizer 1-azabicyclo(3.2.2>nonan-3-aminderivate.
US5459270A (en) 1991-08-20 1995-10-17 Merck Sharp & Dohme Limited 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
US5578593A (en) 1992-12-11 1996-11-26 Merck & Co., Inc. Spiro piperidines and homologs 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
KR970707101A (ko) 1994-11-07 1997-12-01 스피겔 알렌 제이 치환된 벤질아민 유도체; 신규한 부류의 신경펩타이드 y1 특이적 리간드(certain substituted benzylamine derivatives; a new class of neuropeptide y1 specific ligands)
US5532237A (en) 1995-02-15 1996-07-02 Merck Frosst Canada, Inc. Indole derivatives with affinity for the cannabinoid receptor
US6194581B1 (en) * 1995-04-07 2001-02-27 Merck & Co., Inc. Substituted pyridines useful as modulators of acetylcholine receptors
US5585388A (en) * 1995-04-07 1996-12-17 Sibia Neurosciences, 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
FR2741621B1 (fr) 1995-11-23 1998-02-13 Sanofi Sa Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant
AU7692696A (en) 1995-12-01 1997-06-27 Novartis Ag Heteroaryl derivatives
AU7626496A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Heteroaryl compounds
AU7692896A (en) 1995-12-01 1997-06-27 Novartis Ag Quinazolin-2,4-diazirines as NPY receptor antagonist
AU7692996A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Receptor antagonists
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
AU1856997A (en) 1996-02-02 1997-08-22 Merck & Co., Inc. Method for raising hdl cholesterol levels
EP0887340A4 (en) 1996-02-06 2000-03-29 Japan Tobacco Inc CHEMICAL COMPOUNDS AND THEIR PHARMACEUTICAL USE
GB9606805D0 (en) 1996-03-30 1996-06-05 Glaxo Wellcome Inc Medicaments
AU5135998A (en) 1996-12-03 1998-06-29 Banyu Pharmaceutical Co., Ltd. Novel urea derivatives
DE69719544T2 (de) 1996-12-12 2003-11-06 Banyu Pharmaceutical Co., Ltd. Pyrazolderivate
WO1998025908A1 (fr) 1996-12-13 1998-06-18 Banyu Pharmaceutical Co., Ltd. Nouveaux derives d'aminopyrazole
EP0945440B1 (en) 1996-12-16 2004-05-26 Banyu Pharmaceutical Co., Ltd. Aminopyrazole derivatives
DE69822449T2 (de) 1997-01-21 2005-01-27 Smithkline Beecham Corp. Neue cannabinoidrezeptor-modulatoren
AU5932098A (en) 1997-02-04 1998-08-25 E.I. Du Pont De Nemours And Company Fungicidal carboxamides
HU228509B1 (en) 1997-02-21 2013-03-28 Bayer Ip Gmbh Aryl sulfonamides and analogues thereof and their use in the treatment of neurodegenerative diseases
WO1998040356A1 (fr) 1997-03-12 1998-09-17 Banyu Pharmaceutical Co., Ltd. Medicaments contenant des derives d'aminopyridine comme ingredient actif
CA2283797A1 (en) 1997-03-18 1998-09-24 Paul Elliot Bender Novel 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
WO1998047505A1 (fr) 1997-04-23 1998-10-29 Banyu Pharmaceutical Co., Ltd. Antagoniste de recepteur de neuropeptide y
US6001836A (en) 1997-05-28 1999-12-14 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: cyanoguanidine derivatives
WO1999002499A1 (fr) 1997-07-11 1999-01-21 Japan Tobacco Inc. Composes quinoline et utilisations de ceux-ci en medecine
AU9185598A (en) 1997-09-25 1999-04-12 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
AU1262199A (en) 1997-11-28 1999-06-16 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
EP1068207A1 (en) 1998-04-02 2001-01-17 Neurogen Corporation AMINOALKYL SUBSTITUTED 9H-PYRIDINO 2,3-b]INDOLE AND 9H-PYRIMIDINO 4,5-b]INDOLE DERIVATIVES
EP1076644B1 (en) 1998-04-29 2004-06-23 Ortho-McNeil Pharmaceutical, Inc. N-substituted aminotetralins as ligands for the neuropeptide y y5 receptor useful in the treatment of obesity and other disorders
US6329395B1 (en) 1998-06-08 2001-12-11 Schering Corporation Neuropeptide Y5 receptor antagonists
DE19837627A1 (de) 1998-08-19 2000-02-24 Bayer Ag Neue Aminosäureester von Arylsulfonamiden und Analoga
HN1998000027A (es) 1998-08-19 1999-06-02 Bayer Ip Gmbh Arilsulfonamidas y analagos
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
US6191160B1 (en) 1998-11-10 2001-02-20 Merck & Co., Inc. Spiro-indolines as Y5 receptor antagonists
IL144851A0 (en) * 1999-02-24 2002-06-30 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)
EP1816127A1 (en) 1999-04-22 2007-08-08 H. Lundbeck A/S Triazine derivatives for use as selective npy (y5) antagonists
MXPA01011321A (es) 1999-05-05 2003-08-01 Johnson & Johnson Neuropeptidos y ligandos de receptores 3a, 4, 5, 9b-tetrahidro-1h-benz(e)indol-2-il amino derivados utiles en el tratamiento de obesidad y otros trastornos.
EP1177188B1 (en) 1999-05-12 2005-10-12 Ortho-McNeil Pharmaceutical, Inc. Pyrazole carboxamides useful for the treatment of obesity and other disorders
CA2380866A1 (en) 1999-06-30 2001-01-11 Synaptic Pharmaceutical Corporation 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
EP1493742A1 (en) 1999-07-28 2005-01-05 Ortho-Mcneil Pharmaceutical, Inc. Amine and amide derivatives as ligands for the neuropeptide Y Y5 receptor useful in the treatment of obesity and other disorders
TWI279402B (en) 1999-08-20 2007-04-21 Banyu Pharma Co Ltd Spiro compounds having NPY antagonistic activities and agents containing the same
US6462053B1 (en) 1999-08-20 2002-10-08 Banyu Pharmaceutical Co., Ltd. Spiro compounds
CA2386474A1 (en) 1999-09-20 2001-03-29 Takeda Chemical Industries, Ltd. Melanin concentrating hormone antagonist
WO2001021169A1 (fr) 1999-09-20 2001-03-29 Takeda Chemical Industries, Ltd. Antagonistes de l'hormone de concentration de la melanine
US6414002B1 (en) 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
CZ20021067A3 (cs) 1999-09-30 2002-11-13 Neurogen Corporation Určité alkylendiaminové substituované pyrazolo[1,5-a]- 1,5-pyrimidiny a pyrazolo[1,5-a]-1,3,5-triaziny
JP2003510327A (ja) 1999-09-30 2003-03-18 ニューロジェン・コーポレーション 特定のアルキレンジアミンで置換された複素環
US6476038B1 (en) 1999-09-30 2002-11-05 Neurogen Corporation Amino substituted pyrazolo[1,5,-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines
TR200201568T2 (tr) 1999-12-16 2002-10-21 Schering Corporation İkame edilmiş imidazol nöropeptid Y Y5 reseptörü antagonistleri.
WO2001056592A1 (en) 2000-02-01 2001-08-09 Novo Nordisk A/S Use of compounds for the regulation of food intake
AU2001234958A1 (en) 2000-02-11 2001-08-20 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators for treating respiratory and non-respiratory diseases
DE60109756T2 (de) 2000-02-22 2005-08-25 Banyu Pharmaceutical Co., Ltd. Imidazolin-verbindungen
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
AU2001263021A1 (en) 2000-05-10 2001-11-20 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
MXPA02010452A (es) 2000-05-11 2003-06-06 Bristol Myers Squibb Co Analogos de tetrahidroisoquinolina utiles como secretagogos de la hormona del crecimiento.
CA2408913A1 (en) 2000-05-16 2001-11-22 Takeda Chemical Industries, 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
CA2384041A1 (en) 2000-07-05 2002-01-24 Synaptic Pharmaceuticals Corporation Selective melanin concentrating hormone-1 (mch1) receptor antagonists and uses thereof
US6569861B2 (en) 2000-07-06 2003-05-27 Neurogen Corporation Melanin concentrating hormone receptor ligands
AU2001283938A1 (en) 2000-07-24 2002-02-05 Ardana Bioscience Limited Ghrelin antagonists
ES2250459T3 (es) 2000-07-31 2006-04-16 F. Hoffmann-La Roche Ag Derivados de piperazina.
JP2004509108A (ja) 2000-09-14 2004-03-25 シェーリング　コーポレイション 置換尿素神経ペプチドｙｙ５受容体アンタゴニスト
TR200402046T4 (tr) 2000-10-13 2004-10-21 Eli Lilly And Company Büyüme hormonu salgılanmasını uyarıcı maddeler olarak ikameli dipeptitler.
EP1328515B1 (en) 2000-10-16 2008-08-06 F. Hoffmann-La Roche AG Indoline derivatives and their use as 5-ht2 receptor ligands
WO2002036596A2 (en) 2000-11-03 2002-05-10 Wyeth CYCLOALKYL[b][1,4]DIAZEPINO[6,7,1-hi]INDOLES AND DERIVATIVES
CN1227237C (zh) 2000-11-20 2005-11-16 比奥维特罗姆股份公司 作为五羟色胺5－ht2受体拮抗剂的哌嗪基吡嗪化合物
NZ525700A (en) 2000-11-20 2004-12-24 Biovitrum Ab Piperazinylpyrazine compounds as agonist or antagonist of serotonin 5HT-2 receptor
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
EP1343503B1 (en) 2000-12-21 2008-11-12 Schering Corporation Heteroaryl urea neuropeptide y y5 receptor antagonists
ATE302185T1 (de) 2000-12-22 2005-09-15 Schering Corp Piperidin mch antagonisten und ihre verwendung in der behandlung von obesität
AU2002228007B2 (en) 2000-12-27 2007-06-21 F. Hoffmann-La Roche Ag Indole derivatives and their use as 5-HT2b and 5-HT2c receptor ligands
HUP0400058A2 (hu) 2001-02-02 2004-04-28 Takeda Chemical Industries, Ltd. Kondenzált heterogyűrűs vegyületek, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
US6900329B2 (en) 2001-03-21 2005-05-31 Schering Corporation MCH antagonists and their use in the treatment of obesity
EP1370520A1 (en) 2001-03-21 2003-12-17 Pharmacopeia, Inc. Aryl and biaryl compounds having mch modulatory activity
RU2281941C2 (ru) 2001-03-22 2006-08-20 Солвей Фармасьютикалс Б.В. Производные 4,5-дигидро-1h-пиразола, обладающие cb1-антагонистической активностью
MXPA03009353A (es) 2001-04-12 2004-02-12 Pharmacopeia Inc Aril y biaril piperidinas utilizadas como antagonistas de mch.
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
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
KR20040012851A (ko) 2001-05-22 2004-02-11 뉴로젠 코포레이션 멜라닌 농축성 호르몬 수용체 리간드: 치환된1-벤질-4-아릴 피페라진 유사체
WO2002094825A1 (fr) 2001-05-22 2002-11-28 Banyu Pharmaceutical Co., Ltd. Nouveau derive de spiropiperidine
CA2450475A1 (en) 2001-06-20 2003-01-03 Linda Brockunier Dipeptidyl peptidase inhibitors for the treatment of diabetes
WO2003000180A2 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
RU2003105463A (ru) 2001-06-27 2004-11-27 Пробиодруг Аг (De) Пептидные структуры, пригодные для конкурентного модулирования катализа, осуществляемого дипептидилпептидазой iv
ATE380175T1 (de) 2001-06-27 2007-12-15 Smithkline Beecham Corp Pyrrolidine als dipeptidyl peptidase inhibitoren
DE60221983T2 (de) 2001-06-27 2008-05-15 Smithkline Beecham Corp. Fluorpyrrolidine als dipeptidyl-peptidase inhibitoren
AU2002322344C1 (en) 2001-06-27 2006-02-16 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
ATE388951T1 (de) 2001-07-03 2008-03-15 Novo Nordisk As Dpp-iv-inhibierende purin-derivative zur behandlung von diabetes
JP2004536104A (ja) 2001-07-05 2004-12-02 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 Ｍｃｈ選択的アンタゴニストとしての置換されたアニリン−ピペリジン誘導体
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
CN1538956A (zh) 2001-08-07 2004-10-20 ������ҩ��ʽ���� 螺环化合物
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
RU2006100298A (ru) 2003-06-11 2006-05-10 Мерк энд Ко., Инк. (US) Замещенные производные 3-алкил-и 3-алкенилазетидинов
JP4795022B2 (ja) * 2003-09-30 2011-10-19 エーザイ・アール・アンド・ディー・マネジメント株式会社 ヘテロ環化合物を含有する新規な抗真菌剤
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
CN1933838A (zh) 2004-02-12 2007-03-21 默克公司 作为代谢型谷氨酸受体－5调节剂的联吡啶酰胺
CA2603345C (en) * 2005-04-01 2017-05-02 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
US20090088452A1 (en) * 2005-11-22 2009-04-02 Coleman Paul J Indole Orexin Receptor Antagonists
CA2679817A1 (en) * 2007-03-02 2008-09-12 Merck & Co., Inc. Bipyridine carboxamide orexin receptor antagonists
US20080214301A1 (en) 2007-03-02 2008-09-04 Wildtangent, Inc. In-game advertisements
CA2679917A1 (en) 2007-03-02 2008-09-12 Northwestern University Compositions and treatments for seizure-related disorders
KR101167773B1 (ko) * 2007-08-03 2012-07-24 에프. 호프만-라 로슈 아게 Ｔａａｒ１ 리간드로서의 피리딘카복스아마이드 및 벤즈아마이드 유도체
AU2008284268A1 (en) 2007-08-09 2009-02-12 Merck & Co., Inc. 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.
AU2009308982A1 (en) * 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. Pyridazine carboxamide orexin receptor antagonists
WO2010051237A1 (en) * 2008-10-30 2010-05-06 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
EP2350010A1 (en) 2011-08-03
TN2011000171A1 (en) 2012-12-17
IL212436A0 (en) 2011-06-30
CA2741644A1 (en) 2010-05-06
CR20110228A (es) 2011-06-24
ZA201103156B (en) 2012-01-25
DOP2011000120A (es) 2011-10-15
MX2011004551A (es) 2011-05-25
JP5635991B2 (ja) 2014-12-03
NI201100084A (es) 2011-11-03
BRPI0919876A2 (pt) 2015-08-18
EA201170624A1 (ru) 2011-12-30
KR20110071101A (ko) 2011-06-28
CO6361994A2 (es) 2012-01-20
CN102272103B (zh) 2015-10-21
JP2012507538A (ja) 2012-03-29
AU2009308980B2 (en) 2013-02-28
MA32804B1 (fr) 2011-11-01
KR101320245B1 (ko) 2013-10-30
WO2010051236A1 (en) 2010-05-06
CN102272103A (zh) 2011-12-07
BRPI0919876A8 (pt) 2016-02-10
CL2011000976A1 (es) 2012-02-24
ECSP11011019A (es) 2011-05-31
NZ592544A (en) 2013-01-25
US20110201591A1 (en) 2011-08-18
AU2009308980A1 (en) 2010-05-06
CA2741644C (en) 2013-05-07
US8592457B2 (en) 2013-11-26
EP2350010B1 (en) 2014-03-26

Similar Documents

Publication Publication Date Title
PE20110852A1 (es) Antagonistas del receptor de orexina de isonicotinamida
PE20081229A1 (es) Antagonistas de receptor de orexina de diazepam sustituido
PE20050874A1 (es) Compuestos de bencimidazolona que tienen actividad agonista del receptor 5-ht4
PE20110028A1 (es) Derivados de isoxazol y su uso como potenciadores de los receptores metabotropicos de glutamato
PE20121506A1 (es) Compuestos triazolopiridinas como inhibidores de c-met
PE20070002A1 (es) Compuestos derivados de heteroaril como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa tipo i
NO20076418L (no) Heterocyclic compounds as agonists for the thyroid receptor
PE20060312A1 (es) Derivados de tetrahidronaftiridina como ligandos del receptor h3 de histamina
PE20070016A1 (es) Compuestos heterociclicos n-enlazados como antagonistas del receptor p2y1
PE20090237A1 (es) Derivados de sulfonamidas como inhibidores de los canales de sodio
PE20121050A1 (es) Compuestos de n-(1-(4-(1h-pirazol-5-il)ftalazin-1-il)piperidin-4-il)-benzamida sustituidos como antagonistas de la trayectoria hedgehog
PE20141281A1 (es) Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a
CO5700757A2 (es) Derivados de (3-oxo-3,4-dihidro-quinoxalin-2-il-amino)-benzamida y compuesto relacionado, como inhibidores de glucogeno fosforilasa para el tratamiento de la diabetes y obesidad
AR061644A1 (es) Derivados de benzofurano
PE20070528A1 (es) Compuestos heterociclicos como ligandos del receptor vaniloide del subtipo 1
AR056536A1 (es) Compuestos de 2-amino-5- [4-(difluormetoxi)fenil]-5-fenilimidazolona como inhibidores de la beta secretasa (bace)
PE20141375A1 (es) Activadores de glucoquinasa
AR079327A1 (es) Derivados de 2-amino-5,5-difluor -5,6-dihidro-4h-(1,3) oxazin-4-il) fenil)-amida
AR077935A1 (es) Derivados de 3-amino-5 fenil-5,6-dihidro-2h-(1,4)oxazina
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
PE20071001A1 (es) Derivados de 1-(azolin-2-il)-amino-1-fenil-2-hetaril-etano con actividad pesticida
PE20090622A1 (es) Nuevos derivados de bencimidazol sustituido
PE20081467A1 (es) Compuestos de benzoil amino heterociclico como mediadores de glucoquinasas (glk)
AR070467A1 (es) Inhibidores de quinasa de pirrolopirazina
PE20120031A1 (es) Compuestos aril metil benzoquinazolinona como moduladores alostericos positivos del receptor m1

Legal Events

Date Code Title Description
FD Application declared void or lapsed