AR088352A1 - Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina - Google Patents

Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina

Info

Publication number
AR088352A1
AR088352A1 ARP120103852A AR088352A1 AR 088352 A1 AR088352 A1 AR 088352A1 AR P120103852 A ARP120103852 A AR P120103852A AR 088352 A1 AR088352 A1 AR 088352A1
Authority
AR
Argentina
Prior art keywords
unsubstituted
substituted
alkyl
substituents selected
cycloalkyl
Prior art date
Application number
Other languages
English (en)
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 AR088352A1 publication Critical patent/AR088352A1/es

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
    • C07D401/14Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Usos de los compuestos de 2-piridil-oxi-4-nitrilo descriptos en la presente en el tratamiento o prevención de trastornos y enfermedades neurológicas y psiquiátricas en las que están implicados receptores de orexina, y composiciones farmacéuticas que comprenden estos compuestos. Reivindicación 1: Un compuesto de la fórmula (1), en la que: A se selecciona entre el grupo que consiste en fenilo, naftilo y heteroarilo; R¹ᵃ, R¹ᵇ y R¹ᶜ se seleccionan independientemente entre el grupo que consiste en: (i) hidrógeno, (ii) halógeno, (iii) hidroxilo, (iv) -(C=O)ₘ-Oₙ-alquilo C₁₋₆, donde m es 0 ó 1, n es 0 ó 1 (donde si m es 0 o n es 0, está presente un enlace) y donde el alquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R⁴, (v) -(C=O)ₘ-Oₙ-cicloalquilo C₃₋₆, donde el cicloalquilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R⁴, (vi) -(C=O)ₘ-alquenilo C₂₋₄, donde el alquenilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R⁴, (vii) -(C=O)ₘ-alquinilo C₂₋₄, donde el alquinilo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R⁴, (viii) -(C=O)ₘ-Oₙ-fenilo o -(C=O)ₘ-Oₙ-naftilo, donde el fenilo o el naftilo están sin sustituir o sustituidos con uno o más sustituyentes seleccionados entre R⁴, (ix) -(C=O)ₘ-Oₙ-heterociclo, donde el heterociclo está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R⁴, (x) -(C=O)ₘ-NR¹⁰R¹¹, donde R¹⁰ y R¹¹ se seleccionan independientemente entre el grupo que consiste en: (a) hidrógeno, (b) alquilo C₁₋₆, que está sin sustituir o sustituido con R⁴, (c) alquenilo C₃₋₆, que está sin sustituir o sustituido con R⁴, (d) alquinilo C₃₋₆, que está sin sustituir o sustituido con R⁴, (e) cicloalquilo C₃₋₆ que está sin sustituir o sustituido con R⁴, (f) fenilo, que está sin sustituir o sustituido con R¹⁴, y (g) heterociclo, que está sin sustituir o sustituido con R⁴, (xi) -S(O)₂NR¹⁰R¹¹, (xii) -S(O)q-R¹², donde q es 0, 1 ó 2 y donde R¹² se selecciona entre las definiciones de R¹⁰ y R¹¹, (xiii) -CO₂H, (xiv) -CN, y (xv) -NO₂; R³ se selecciona entre alquilo C₁₋₆ y cicloalquilo C₃₋₆, que está sin sustituir o sustituido con uno o más sustituyentes seleccionados entre R⁴; R⁴ se selecciona entre el grupo que consiste en: (i) hidroxilo, (ii) halógeno, (iii) alquilo C₁₋₆, (iv) -cicloalquilo C₃₋₆, (v) -O-alquilo C₁₋₆, (vi) -O(C=O)-alquilo C₁₋₆, (vii) -NH₂, (viii) -NH-alquilo C₁₋₆, (ix) -NO₂, (x) fenilo, (xi) heterociclo, (xii) -CO₂H, y (xiii) -CN; o una sal farmacéuticamente aceptable de los mismos.
ARP120103852 2011-10-19 2012-10-16 Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina AR088352A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161548883P 2011-10-19 2011-10-19

Publications (1)

Publication Number Publication Date
AR088352A1 true AR088352A1 (es) 2014-05-28

Family

ID=47116466

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120103852 AR088352A1 (es) 2011-10-19 2012-10-16 Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina

Country Status (11)

Country Link
US (1) US9156819B2 (es)
EP (1) EP2768823B1 (es)
JP (1) JP5947906B2 (es)
CN (1) CN103874695B (es)
AR (1) AR088352A1 (es)
AU (1) AU2012326275B2 (es)
BR (1) BR112014009486A2 (es)
CA (1) CA2852425C (es)
IN (1) IN2014CN02515A (es)
TW (1) TW201317228A (es)
WO (1) WO2013059222A1 (es)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
BR112014019426A8 (pt) 2012-02-07 2017-07-11 Eolas Therapeutics Inc Prolinas/ piperidinas substituídas como antagonistas do receptor de orexina
US9586950B2 (en) 2012-10-16 2017-03-07 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-ester-4-nitrile orexin receptor antagonists
US9546152B2 (en) * 2012-10-23 2017-01-17 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-substituted-4-nitrile orexin receptor antagonists
WO2014085208A1 (en) * 2012-11-27 2014-06-05 Merck Sharp & Dohme Corp. 2-pyridylamino-4-nitrile-piperidinyl orexin receptor antagonists
WO2014099698A1 (en) * 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-nitrile-4-substituted orexin receptor antagonists
EP2934516A4 (en) * 2012-12-20 2016-07-20 Merck Sharp & Dohme ANTAGONISTS OF 3-ESTER-4-SUBSTITUTED OREXIN RECEPTORS
US9556145B2 (en) * 2012-12-20 2017-01-31 Merck Sharp & Dohme Corp. 2-pyridyloxy-4-ester orexin receptor antagonists
TWI621618B (zh) 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途
TW201444821A (zh) * 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代之哌啶化合物及其作為食慾素受體調節劑之用途
TW201444849A (zh) 2013-03-13 2014-12-01 Janssen Pharmaceutica Nv 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途
EP2988748A1 (en) * 2013-04-23 2016-03-02 Merck Sharp & Dohme Corp. Hydroxy-substituted orexin receptor antagonists
WO2015018027A1 (en) 2013-08-08 2015-02-12 Merck Sharp & Dohme Corp. Thiazole orexin receptor antagonists
WO2015018029A1 (en) * 2013-08-08 2015-02-12 Merck Sharp & Dohme Corp. Oxazole orexin receptor antagonists
WO2015088865A1 (en) 2013-12-09 2015-06-18 Merck Sharp & Dohme Corp. 2-pyridyloxy-4-methyl orexin receptor antagonists
WO2015088864A1 (en) 2013-12-09 2015-06-18 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-ester-4-ether orexin receptor antagonists
WO2015095108A1 (en) 2013-12-18 2015-06-25 Merck Sharp & Dohme Corp. Thioether-piperidinyl orexin receptor antagonists
WO2015095441A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. 2-amino-3-ester-pyridyl orexin receptor antagonists
CA2941663C (en) * 2014-03-06 2020-02-18 Shanghai Haiyan Pharmaceutical Technology Co. Ltd Piperidine derivatives as orexin receptor antagonist
TW201613902A (en) 2014-08-13 2016-04-16 Eolas Therapeutics Inc Difluoropyrrolidines as orexin receptor modulators
WO2016040789A1 (en) 2014-09-11 2016-03-17 Janssen Pharmaceutica Nv Substituted 2-azabicycles and their use as orexin receptor modulators
WO2016065585A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Piperidine isoxazole and isothiazole orexin receptor antagonists
WO2016065587A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Pyrazole orexin receptor antagonists
WO2016065586A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Pyrazole, triazole and tetrazole orexin receptor antagonists
WO2016065583A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Oxazole orexin receptor antagonists
WO2016065584A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Piperidine oxadiazole and thiadiazole orexin receptor antagonists
WO2016083315A1 (en) * 2014-11-24 2016-06-02 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of ox1r antagonists for the treatment of inflammatory bowel diseases
US10000499B2 (en) 2014-11-26 2018-06-19 Merck Sharp & Dohme Corp. Methyl diazepane orexin receptor antagonists
US9994570B2 (en) 2014-11-26 2018-06-12 Merck Sharp & Dohme Corp. Bridged diazepane orexin receptor antagonists
WO2016086357A1 (en) 2014-12-02 2016-06-09 Merck Sharp & Dohme Corp. Methyl oxazole orexin receptor antagonists
WO2016086358A1 (en) * 2014-12-02 2016-06-09 Merck Sharp & Dohme Corp. Hydroxymethyl piperidine orexin receptor antagonists
US9987255B2 (en) 2014-12-19 2018-06-05 Merck Sharp & Dohme Corp. 5,5-bicyclic oxazole orexin receptor antagonists
US9938276B2 (en) 2014-12-19 2018-04-10 Merck Sharp & Dohme Corp. 6,5-bicyclic octahydropyrrolopyridine orexin receptor antagonists
WO2016095205A1 (en) 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Heteroaryl orexin receptor antagonists
US10011595B2 (en) 2014-12-19 2018-07-03 Merck Sharp & Dohme Corp. Ethyldiamine orexin receptor antagonists
WO2016095204A1 (en) 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Pyrrolidine orexin receptor antagonists
WO2016101119A1 (en) 2014-12-23 2016-06-30 Merck Sharp & Dohme Corp. Fused heteroaryl derivatives as orexin receptor antagonists
WO2016101118A1 (en) 2014-12-23 2016-06-30 Merck Sharp & Dohme Corp. Amidoethyl azole orexin receptor antagonists
CA3005918C (en) 2015-11-23 2023-10-17 Sunshine Lake Pharma Co., Ltd. Octahydropyrrolo[3,4-c]pyrrole derivatives and uses thereof
US10894789B2 (en) 2016-02-12 2021-01-19 Astrazeneca Ab Halo-substituted piperidines as orexin receptor modulators
WO2017194548A1 (en) 2016-05-10 2017-11-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of autoimmune inflammatory diseases
IL300063B2 (en) 2017-08-03 2024-02-01 Takeda Pharmaceuticals Co Methanesulfonamide and its use for the prevention or treatment of narcolepsy

Family Cites Families (214)

* 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
ZA848275B (en) 1983-12-28 1985-08-28 Degussa New piridine-2-ethers or pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring
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
ATE154354T1 (de) 1991-02-11 1997-06-15 Merck Sharp & Dohme Azabicyclische verbindungen, diese enthaltende pharmazeutische zubereitungen und ihre therapeutische verwendung
US5373003A (en) 1991-03-01 1994-12-13 Pfizer Inc. 1-azabicyclo[3.2.2]nonan-3-amine derivatives
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
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
WO1996014307A1 (en) 1994-11-07 1996-05-17 Pfizer Inc. 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
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
WO1997019682A1 (en) 1995-12-01 1997-06-05 Synaptic Pharmaceutical Corporation Aryl sulfonamide and sulfamide derivatives and uses thereof
WO1997020823A2 (en) 1995-12-01 1997-06-12 Novartis Ag 2-amino quinazoline derivatives as npy receptor antagonists
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
AU1618697A (en) 1996-02-06 1997-08-28 Japan Tobacco Inc. Novel compounds and pharmaceutical use thereof
GB9606805D0 (en) 1996-03-30 1996-06-05 Glaxo Wellcome Inc Medicaments
US6043246A (en) 1996-12-03 2000-03-28 Banyu Pharmaceutical Co., Ltd. Urea derivatives
AU5410498A (en) 1996-12-12 1998-07-03 Banyu Pharmaceutical Co., Ltd. Pyrazole derivatives
US6166038A (en) 1996-12-13 2000-12-26 Banyu Pharmaceutical Co., Ltd. Aminopyrazole derivatives
AU7738198A (en) 1996-12-15 1998-07-15 Banyu Pharmaceutical Co., Ltd. Aminopyrazole derivatives
JP2001508799A (ja) 1997-01-21 2001-07-03 スミスクライン・ビーチャム・コーポレイション 新規カンナビノイド受容体モジュレータ
KR100510794B1 (ko) 1997-02-04 2005-08-31 더 보드 오브 트러스티스 오브 더 유니버시티 오브 아칸소 살진균 카르복스아미드
JP4346113B2 (ja) 1997-02-21 2009-10-21 バイエル・アクチエンゲゼルシヤフト アリールスルホンアミド及びそれらの類似体並びに神経変性疾患の治療におけるそれらの使用
AU6309698A (en) 1997-03-12 1998-09-29 Banyu Pharmaceutical Co., Ltd. Drugs containing aminopyridine derivatives as the active ingredient
JP2001516361A (ja) 1997-03-18 2001-09-25 スミスクライン・ビーチャム・コーポレイション 新規カンナビノイド受容体作動薬
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
CA2288122C (en) 1997-04-23 2006-09-26 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
AU8127998A (en) 1997-07-11 1999-02-08 Japan Tobacco Inc. Quinoline compounds and medicinal uses thereof
AR016817A1 (es) 1997-08-14 2001-08-01 Smithkline Beecham Plc Derivados de fenilurea o feniltiourea, procedimiento para su preparacion, coleccion de compuestos, compuestos intermediarios, composicion farmaceutica,metodo de tratamiento y uso de dichos compuestos para la manufactura de un medicamento
WO1999015516A1 (fr) 1997-09-25 1999-04-01 Banyu Pharmaceutical Co., Ltd. Nouveaux antagonistes des recepteurs de neuropeptides y
WO1999027965A1 (fr) 1997-11-28 1999-06-10 Banyu Pharmaceutical Co., Ltd. Agents anti-hyperlipemiques
CA2326606A1 (en) 1998-04-02 1999-10-14 Neurogen Corporation Aminoalkyl substituted 9h-pyridino[2,3-b]indole and 9h-pyrimidino[4,5-b]indole derivatives:crf1 and npy1 receptors
NZ507763A (en) 1998-04-29 2003-06-30 Ortho Mcneil Pharm Inc N-substituted aminotetralin sulphonamide derivatives useful as ligands for the neuropeptide Y Y5 receptor used in the treatment of obesity and other disorders
ES2196806T3 (es) 1998-05-08 2003-12-16 Smithkline Beecham Plc Derivados de fenilurea y de feniltiourea.
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
WO2000027845A1 (en) 1998-11-10 2000-05-18 Merck & Co., Inc. Spiro-indolines as y5 receptor antagonists
WO2000047576A1 (en) 1999-02-12 2000-08-17 Smithkline Beecham Plc Cinnamide derivatives as orexin-1 receptors antagonists
AU2910600A (en) 1999-02-12 2000-08-29 Smithkline Beecham Plc Phenyl urea and phenyl thiourea derivatives
EP1150977B1 (en) 1999-02-12 2004-08-25 SmithKline Beecham plc Phenyl urea and phenyl thiourea derivatives as orexin receptor antagonists
US6340683B1 (en) 1999-04-22 2002-01-22 Synaptic Pharmaceutical Corporation Selective NPY (Y5) antagonists (triazines)
WO2000064880A1 (en) 1999-04-22 2000-11-02 Synaptic Pharmaceutical Corporation 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.
US6291476B1 (en) 1999-05-12 2001-09-18 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
NZ516782A (en) 1999-07-28 2004-12-24 Ortho Mcneil Pharm 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
EP1219294A4 (en) 1999-09-20 2005-01-26 ANTAGONISTS OF THE MELANIN CONCENTRATING HORMON
EP1218336A2 (en) 1999-09-20 2002-07-03 Takeda Chemical Industries, Ltd. 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
WO2001023387A2 (en) 1999-09-30 2001-04-05 Neurogen Corporation CERTAIN ALKYLENE DIAMINE-SUBSTITUTED PYRAZOLO[1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES
AU7737900A (en) 1999-09-30 2001-04-30 Neurogen Corporation Amino substituted pyrazolo(1,5,-a)-1,5-pyrimidines and pyrazolo(1,5-a)-1,3,5-triazines
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
ES2243337T3 (es) 1999-12-16 2005-12-01 Schering Corporation Imidazoles sustituidos antagonistas del receptor y5 del neuropeptido y.
MXPA02007036A (es) 2000-01-20 2002-12-13 Eisai Co Ltd Compuesto de piperidina novedoso y composicion farmaceutica del mismo.
WO2001056592A1 (en) 2000-02-01 2001-08-09 Novo Nordisk A/S Use of compounds for the regulation of food intake
WO2001058869A2 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
CA2400659A1 (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
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
FR2805818B1 (fr) 2000-03-03 2002-04-26 Aventis Pharma Sa Derives d'azetidine, leur preparation et les compositions pharmaceutiques les contenant
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
EP1132389A1 (en) 2000-03-06 2001-09-12 Vernalis Research Limited New aza-indolyl derivatives for the treatment of obesity
MXPA02008797A (es) 2000-03-14 2005-09-08 Actelion Pharmaceuticals Ltd Derivados de 1,2,3,4-tetrahidroisoquinolina.
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
US6444675B2 (en) 2000-05-10 2002-09-03 Bristol-Myers Squibb Company 4-alkyl and 4-cycloalkyl derivatives of dihydropyridine NPY antagonists
US6432960B2 (en) 2000-05-10 2002-08-13 Bristol-Myers Squibb Company Squarate derivatives of dihydropyridine NPY antagonists
WO2001085173A1 (en) 2000-05-10 2001-11-15 Bristol-Myers Squibb Company Alkylamine derivatives of dihydropyridine npy antagonists
AU5959201A (en) 2000-05-11 2001-11-20 Bristol Myers Squibb Co Tetrahydroisoquinoline analogs useful as growth hormone secretagogues
JPWO2001085693A1 (ja) 2000-05-11 2004-01-08 萬有製薬株式会社 N−アシルテトラヒドロイソキノリン誘導体
WO2001087834A1 (fr) 2000-05-16 2001-11-22 Takeda Chemical Industries, Ltd. Antagoniste de l'hormone de concentration de la melanine
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
DE60110066T2 (de) 2000-06-16 2006-02-02 Smithkline Beecham P.L.C., Brentford Piperidine zur verwendung als orexinrezeptorantagonisten
EP1299362A4 (en) 2000-07-05 2004-11-03 Synaptic Pharma Corp SELECTIVE RECEPTOR ANTAGONISTS OF MELANINE CONCENTRATING HORMON-1 (MCH1) AND THEIR USE
AU2001279294A1 (en) 2000-07-06 2002-01-21 Neurogen Corporation Melanin concentrating hormone receptor ligands
WO2002008250A2 (en) 2000-07-24 2002-01-31 Ardana Bioscience Limited Ghrelin antagonists
EP1325008B1 (en) 2000-07-31 2005-10-05 F. Hoffmann-La Roche Ag Piperazine derivatives
CN1474810A (zh) 2000-09-14 2004-02-11 ���鹫˾ 取代脲,神经肽yy5受体拮抗剂
ATE270280T1 (de) 2000-10-13 2004-07-15 Lilly Co Eli Substituierte dipeptide zur förderung der sekretion von wachstumshormon
MXPA03003246A (es) 2000-10-16 2003-06-06 Hoffmann La Roche Derivados de indolina y su uso como ligandos del receptor 5-ht2.
WO2002036596A2 (en) 2000-11-03 2002-05-10 Wyeth CYCLOALKYL[b][1,4]DIAZEPINO[6,7,1-hi]INDOLES AND DERIVATIVES
NZ525700A (en) 2000-11-20 2004-12-24 Biovitrum Ab Piperazinylpyrazine compounds as agonist or antagonist of serotonin 5HT-2 receptor
CA2449899C (en) 2000-11-20 2010-04-06 Biovitrum Ab Piperazinylpyrazines compounds as antagonists of serotonin 5-ht2 receptor
DE60108420T2 (de) 2000-11-28 2005-12-22 Smithkline Beecham P.L.C., Brentford Morpholinderivate als antagonisten an orexinrezeptoren
BR0116113A (pt) 2000-12-12 2004-08-03 Neurogen Corp Espiro[isobenzofuran-1,4'-piperidin]-3-onas e 3h-espiroisoben-zofuran-1,4'-piperidinas
GB0030710D0 (en) 2000-12-15 2001-01-31 Hoffmann La Roche Piperazine derivatives
AU2002234056B2 (en) 2000-12-21 2005-04-07 Schering Corporation Heteroaryl urea neuropeptide Y Y5 receptor antagonists
HUP0302582A2 (hu) 2000-12-22 2003-12-29 Schering Corp. Piperidin MCH antagonisták, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk elhízás kezelésére
WO2002051232A2 (en) 2000-12-27 2002-07-04 Actelion Pharmaceuticals Ltd. Novel benzazepines and related heterocyclic derivatives
WO2002051844A1 (en) 2000-12-27 2002-07-04 F. Hoffmann-La Roche Ag Indole derivatives and their use as 5-ht2b and 5-ht2c receptor ligands
PE20021002A1 (es) 2001-02-02 2002-12-06 Takeda Chemical Industries Ltd Compuestos heterociclicos condensados
IL157456A0 (en) 2001-03-21 2004-03-28 Pharmacopeia Inc Pharmacopeia 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
DE60202270T2 (de) 2001-03-22 2005-05-19 Solvay Pharmaceuticals B.V. 4,5-dihydro-1h-pyrazolderivate mit cb1-antagonistischer wirkung
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
MXPA03009353A (es) 2001-04-12 2004-02-12 Pharmacopeia Inc Aril y biaril piperidinas utilizadas como antagonistas de mch.
US7432270B2 (en) 2001-05-05 2008-10-07 Smithkline Beecham P.L.C. N-aroyl cyclic amines
US20040192673A1 (en) 2001-05-05 2004-09-30 Pascale Gaillard N-aroyl cyclic amine derivatives as orexin receptor antagonists
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
DE60209348T2 (de) 2001-06-20 2006-10-12 Merck & Co., Inc. Dipeptidylpeptidase-hemmer zur behandlung von diabetes
AU2002344820B2 (en) 2001-06-20 2006-12-14 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
DE60223920T2 (de) 2001-06-27 2008-11-13 Smithkline Beecham Corp. Pyrrolidine als dipeptidyl-peptidase-inhibitoren
ES2291477T3 (es) 2001-06-27 2008-03-01 Smithkline Beecham Corporation Fluoropirrolidinas como inhibidores de dipeptidil peptidasa.
EP1406873B1 (en) 2001-06-27 2007-09-26 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
EP1399469A2 (en) 2001-06-27 2004-03-24 Probiodrug AG Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis
DE60212968T2 (de) 2001-06-28 2007-02-01 Smithkline Beecham P.L.C., Brentford N-aroyl-(cyclisches amin)-derivate als orexinrezeptor antagonisten
GB0115862D0 (en) 2001-06-28 2001-08-22 Smithkline Beecham Plc Compounds
WO2003004496A1 (en) 2001-07-03 2003-01-16 Novo Nordisk A/S Dpp-iv-inhibiting purine derivatives for the treatment of diabetes
MXPA03011886A (es) 2001-07-05 2005-03-07 Lundbeck & Co As H Piperidinias anilinicas sustituidas como antagonistas selectivos de mch.
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
MXPA04001144A (es) 2001-08-07 2004-07-08 Banyu Pharma Co Ltd Compuestos espiro.
GB0124463D0 (en) 2001-10-11 2001-12-05 Smithkline Beecham Plc Compounds
GB0126292D0 (en) 2001-11-01 2002-01-02 Smithkline Beecham Plc Compounds
GB0127145D0 (en) 2001-11-10 2002-01-02 Smithkline Beecham Compounds
GB0130335D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
GB0130341D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
GB0130393D0 (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
TWI283241B (en) 2002-05-29 2007-07-01 Tanabe Seiyaku Co Novel piperidine compound
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
EP1521583B1 (en) 2002-07-09 2007-01-10 Actelion Pharmaceuticals Ltd. 7,8,9,10-tetrahydro-6h-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2h-pyrrolo (2,1-b)-quinazolinone derivatives
ATE344261T1 (de) 2002-09-18 2006-11-15 Glaxo Group Ltd Cyclische n-aroylamine als orexinrezeptorantagonisten
US6869966B2 (en) 2002-09-30 2005-03-22 Banyu Pharmaceutical Co., Ltd. N-substituted-2-oxodihydropyridine derivatives
WO2004033445A1 (en) 2002-10-08 2004-04-22 Merck Frosst Canada & Co. 4-amino-azepan-3-one compounds as cathepsin k inhibitors useful in the treatment of osteoporosis
RU2334735C2 (ru) 2002-10-11 2008-09-27 Актелион Фармасьютиклз Лтд. Производные сульфониламиноуксусной кислоты и их применение в качестве антагонистов рецепторов орексина
GB0225884D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
GB0225938D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
MY134457A (en) 2002-11-22 2007-12-31 Merck & Co Inc Substituted amides
US6951882B2 (en) 2002-12-12 2005-10-04 Janssen Pharmaceutica N.V. Substituted 4-phenyl-[1,3]-dioxanes
JO2397B1 (en) 2002-12-20 2007-06-17 ميرك شارب اند دوم كوربوريشن Terazol derivatives as beta-hydroxy steroid dihydrogenase-1 inhibitors
CL2004000553A1 (es) 2003-03-20 2005-02-04 Actelion Pharmaceuticals Ltd Uso de compuestos derivados de guanidina como antagonistas del receptor de neuropeptido ff; compuestos derivados de guanidina; procedimientos de preparacion; y composicion farmaceutica que los comprende.
KR20050114242A (ko) 2003-03-26 2005-12-05 액테리온 파마슈티칼 리미티드 오렉신 수용체 길항제로서 이용되는테트라하이드로이소퀴놀릴 아세트아마이드 유도체
JO2355B1 (en) 2003-04-15 2006-12-12 ميرك شارب اند دوم كوربوريشن Hereditary calcitonin polypeptide receptor antagonists
DE602004011204T2 (de) 2003-04-28 2008-12-24 Actelion Pharmaceuticals Ltd. Quinoxalin-3-on-verdindungen als orexin-rezeptor antagonisten.
US7485732B2 (en) 2003-06-11 2009-02-03 Merck & Co., Inc. Substituted 3-alkyl and 3-alkenyl azetidine derivatives
HUP0304101A3 (en) 2003-12-22 2008-10-28 Sanofi Aventis Pyrazole derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates
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
EP1751111B1 (en) 2004-03-01 2014-12-31 Actelion Pharmaceuticals Ltd. Substituted 1,2,3,4-tetrahydroisoquinoline derivatives
WO2006067224A2 (en) 2004-12-23 2006-06-29 Biovitrum Ab (Publ) Spiro-benzodioxole and spiro-benzodioxane compounds as orexin receptor antagonists
DE102004062544A1 (de) 2004-12-24 2006-07-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Pyrrolidinone, deren Herstellung und deren Verewendung als Arzneimittel
AU2006235302A1 (en) 2005-04-12 2006-10-19 Merck & Co., Inc. Amidopropoxyphenyl orexin receptor antagonists
CA2606288A1 (en) * 2005-04-18 2006-10-26 Neurogen Corporation Subtituted heteroaryl cb1 antagonists
US20090215742A1 (en) 2005-05-03 2009-08-27 Pfizer, Inc. Amide resorcinol compounds
WO2006127550A1 (en) 2005-05-23 2006-11-30 Merck & Co., Inc. Proline bis-amide orexin receptor antagonists
CA2617324A1 (en) 2005-08-04 2007-02-15 Merck & Co., Inc. Aminoethane sulfonamide orexin receptor antagonists
JP2009506061A (ja) 2005-08-26 2009-02-12 メルク エンド カムパニー インコーポレーテッド ジアザスピロデカンオレキシン受容体拮抗薬
AR055203A1 (es) * 2005-08-31 2007-08-08 Otsuka Pharma Co Ltd Derivados de benzotiofeno con propiedades antipsicoticas
CA2629192A1 (en) 2005-11-22 2007-05-31 Merck & Co., Inc. Indole orexin receptor antagonists
CA2647678A1 (en) 2006-03-29 2007-11-08 Merck & Co., Inc. Diazepan orexin receptor antagonists
US20090105318A1 (en) 2006-03-29 2009-04-23 Coleman Paul J Amidoethylthioether Orexin Receptor Antagonists
WO2007116374A1 (en) 2006-04-11 2007-10-18 Actelion Pharmaceuticals Ltd Novel sulfonamide compounds
WO2007122591A2 (en) 2006-04-26 2007-11-01 Actelion Pharmaceuticals Ltd Pyrazolo-tetrahydro pyridine derivatives as orexin receptor antagonists
EP2049110B1 (en) 2006-07-14 2014-08-20 Merck Sharp & Dohme Corp. Bridged diazepan orexin receptor antagonists
JP5479893B2 (ja) 2006-07-14 2014-04-23 メルク・シャープ・アンド・ドーム・コーポレーション 置換ジアゼパンオレキシン受容体アンタゴニスト
EP2049526A2 (en) 2006-07-14 2009-04-22 Merck & Co., Inc. 2-substituted proline bis-amide orexin receptor antagonists
DE602007012910D1 (de) 2006-08-15 2011-04-14 Actelion Pharmaceuticals Ltd Azetidinverbindungen als orexin-rezeptor-antagonisten
JP2010502587A (ja) 2006-08-28 2010-01-28 アクテリオン ファーマシューティカルズ リミテッド オレキシン受容体アンタゴニストとしての1,4,5,6,7,8−ヘキサヒドロ−1,2,5−トリアザ−アズレン誘導体
CA2662612A1 (en) 2006-09-29 2008-04-03 Actelion Pharmaceuticals Ltd 3-aza-bicyclo[3.1.0]hexane derivatives
ES2357992T3 (es) 2006-12-01 2011-05-04 Actelion Pharmaceuticals Ltd. Derivados de 3-heteroaril(amino o amido)-1-(bifenil o feniltiazolil)carbonilpiperidina como inhibidores del receptor de orexina.
PE20081229A1 (es) 2006-12-01 2008-08-28 Merck & Co Inc Antagonistas de receptor de orexina de diazepam sustituido
US8410142B2 (en) * 2007-03-02 2013-04-02 Merck Sharp & Dohme Corp. Bipyridine carboxamide orexin receptor antagonists
MY148544A (en) * 2007-05-23 2013-04-30 Merck Sharp & Dohme Pyridyl piperidine orexin receptor antagonists
WO2009020642A1 (en) * 2007-08-09 2009-02-12 Merck & Co., Inc. Pyridine carboxamide orexin receptor antagonists
CN101903372B (zh) * 2007-12-21 2014-06-18 弗·哈夫曼-拉罗切有限公司 作为食欲肽受体拮抗剂的杂芳基衍生物
UY31603A1 (es) * 2008-01-23 2009-08-31 Derivados de ftalazinona
CN102015645B (zh) * 2008-04-30 2012-11-14 埃科特莱茵药品有限公司 哌啶和吡咯烷化合物
CA2724648A1 (en) 2008-05-22 2009-11-26 Merck Sharp & Dohme Corp. Process for the preparation of an orexin receptor antagonist
WO2010048012A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,5-disubstituted piperidine orexin receptor antagonists
EP2348846B1 (en) 2008-10-21 2013-08-28 Merck Sharp & Dohme Corp. Disubstituted azepan orexin receptor antagonists
CA2739917A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,5-disubstituted morpholine orexin receptor antagonists
CA2740190A1 (en) * 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,3-disubstituted piperidine orexin receptor antagonists
JP2012506374A (ja) 2008-10-21 2012-03-15 メルク・シャープ・エンド・ドーム・コーポレイション 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
WO2010048014A1 (en) * 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,4-disubstituted pyrrolidine orexin receptor antagonists
JP5635991B2 (ja) * 2008-10-30 2014-12-03 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. イソニコチンアミドオレキシン受容体アンタゴニスト
CA2741648A1 (en) * 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. 2,5-disubstituted phenyl carboxamide orexin receptor antagonists
GB0823467D0 (en) 2008-12-23 2009-01-28 Glaxo Group Ltd Novel Compounds
US20120149723A1 (en) 2009-08-24 2012-06-14 Romano Di Fabio 5-methyl-piperidine derivatives as orexin receptor antagonists for the treatment of sleep disorder
US9546152B2 (en) * 2012-10-23 2017-01-17 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-substituted-4-nitrile orexin receptor antagonists

Also Published As

Publication number Publication date
US20130102619A1 (en) 2013-04-25
JP5947906B2 (ja) 2016-07-06
AU2012326275B2 (en) 2016-12-01
WO2013059222A1 (en) 2013-04-25
CA2852425C (en) 2019-11-12
AU2012326275A1 (en) 2014-04-17
CN103874695A (zh) 2014-06-18
IN2014CN02515A (es) 2015-07-31
EP2768823B1 (en) 2017-09-06
US9156819B2 (en) 2015-10-13
CN103874695B (zh) 2017-12-15
BR112014009486A2 (pt) 2017-05-09
CA2852425A1 (en) 2013-04-25
JP2014532624A (ja) 2014-12-08
EP2768823A1 (en) 2014-08-27
TW201317228A (zh) 2013-05-01

Similar Documents

Publication Publication Date Title
AR088352A1 (es) Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
AR090292A1 (es) Compuestos basados en pirazolo[1,5-a]pirimidina, composiciones que los comprenden y metodos que los utilizan
AR082111A1 (es) Furopiridinas o tienopiridinas condensadas, composiciones farmaceuticas que las contienen utiles para tratar trastornos psicoticos y del sistema nervioso central, y metodo de preparacion de las mismas
AR092108A1 (es) Piridazina 1,4 disustituida, analogos de la misma y metodos para tratar las enfermedades relacionadas con deficiencia del smn
AR089682A1 (es) Compuestos de piridazina-amida
AR080057A1 (es) Piridinas disustituidas como anticancerigenos
AR094313A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR090220A1 (es) Inhibidores de serina/treonina cinasa
DOP2010000272A (es) Nuevos derivados de carbazol inhibidores de hsp90, composiciones que los contienen y utilizacion
AR088535A1 (es) Derivados de amidas de aminoacidos sustituidos con n-urea como moduladores de receptor formil peptido del receptor del tipo 1 (fprl-1)
AR086357A1 (es) Derivados de indazol sustituidos activos como inhibidores de quinasas
DOP2014000121A (es) Derivados de betulina
AR087760A1 (es) Heterociclilaminas como inhibidores de pi3k
AR091424A1 (es) Compuestos triciclicos sustituidos como inhibidores de receptores del factor de crecimiento del fibroplasto (fgfr)
AR077695A1 (es) Derivados de pirimidina como inhibidores del factor ixa
AR094262A1 (es) Compuestos antivirales para el tratamiento de la hepatitis c
EA201490272A1 (ru) Новые 4-пиперидинильные соединения для применения в качестве ингибиторов танкиразы
AR087628A1 (es) Inhibidores de pde10 de pirimidina
BR112012018865A2 (pt) naftiridinas substituídas e seu uso como inibidores de quinase syk
AR070130A1 (es) Compuestos moduladores de beta-amiloide, un proceso para su obtencion, el uso del compuesto para la fabricacion de un medicamento y dicho medicamento
AR087915A1 (es) N-(3-(2-amino-6,6-difluor-4,4a,5,6,7,7a-hexahidro-ciclopenta-[e][1,3]oxazin-4-il)-fenil)-amidas como inhibidores de la bace1
AR085088A1 (es) Inhibidores de histona desacetilasa y composiciones farmaceuticas que los contienen
AR060535A1 (es) Pirido-piridazinonas y ftalazinonas como antagonistas duales de los receptores h1 y h3 de histamina
CO6341610A2 (es) Compuesto heterociclilo aromatico que contiene nitrogeno.
AR102217A1 (es) Derivados de benzotiofenilo sustituidos como agonistas de gpr40 para el tratamiento de la diabetes tipo ii

Legal Events

Date Code Title Description
FA Abandonment or withdrawal