AU2001277056B2 - N-substituted indoles useful in the treatment of diabetes - Google Patents

N-substituted indoles useful in the treatment of diabetes Download PDF

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Publication number
AU2001277056B2
AU2001277056B2 AU2001277056A AU2001277056A AU2001277056B2 AU 2001277056 B2 AU2001277056 B2 AU 2001277056B2 AU 2001277056 A AU2001277056 A AU 2001277056A AU 2001277056 A AU2001277056 A AU 2001277056A AU 2001277056 B2 AU2001277056 B2 AU 2001277056B2
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AU
Australia
Prior art keywords
methyl
compound
indol
phenoxy
group
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Ceased
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AU2001277056A
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AU2001277056A1 (en
Inventor
John J. Acton Iii
Regina Marie Black
Anthony Brian Jones
Harold Blair Wood
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Merck and Co Inc
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Merck and Co Inc
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Publication of AU2001277056A1 publication Critical patent/AU2001277056A1/en
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Publication of AU2001277056B2 publication Critical patent/AU2001277056B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12Radicals substituted by oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
AU2001277056A 2000-07-25 2001-07-20 N-substituted indoles useful in the treatment of diabetes Ceased AU2001277056B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22077800P 2000-07-25 2000-07-25
US60/220,778 2000-07-25
PCT/US2001/022979 WO2002008188A1 (en) 2000-07-25 2001-07-20 N-substituted indoles useful in the treatment of diabetes

Publications (2)

Publication Number Publication Date
AU2001277056A1 AU2001277056A1 (en) 2002-05-02
AU2001277056B2 true AU2001277056B2 (en) 2005-09-29

Family

ID=22824932

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2001277056A Ceased AU2001277056B2 (en) 2000-07-25 2001-07-20 N-substituted indoles useful in the treatment of diabetes
AU7705601A Pending AU7705601A (en) 2000-07-25 2001-07-20 N-substituted indoles useful in the treatment of diabetes

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU7705601A Pending AU7705601A (en) 2000-07-25 2001-07-20 N-substituted indoles useful in the treatment of diabetes

Country Status (8)

Country Link
US (1) US6525083B2 (enExample)
EP (1) EP1305285B1 (enExample)
JP (1) JP2004513076A (enExample)
AT (1) ATE362468T1 (enExample)
AU (2) AU2001277056B2 (enExample)
CA (1) CA2415742A1 (enExample)
DE (1) DE60128475T2 (enExample)
WO (1) WO2002008188A1 (enExample)

Families Citing this family (176)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030176357A1 (en) * 1998-10-06 2003-09-18 Pospisilik Andrew J. Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels
TWI249401B (en) * 1999-04-14 2006-02-21 Takeda Chemical Industries Ltd Agent for improving ketosis
US7041691B1 (en) 1999-06-30 2006-05-09 Amgen Inc. Compounds for the modulation of PPARγ activity
US20030171399A1 (en) 2000-06-28 2003-09-11 Tularik Inc. Quinolinyl and benzothiazolyl modulators
AR030379A1 (es) * 2000-08-22 2003-08-20 Novartis Ag Combinaciones
US7166578B2 (en) 2000-08-24 2007-01-23 The Regents Of The University Of California Orally administered peptides synergize statin activity
US7148197B2 (en) * 2000-08-24 2006-12-12 The Regents Of The University Of California Orally administered small peptides synergize statin activity
US7199102B2 (en) * 2000-08-24 2007-04-03 The Regents Of The University Of California Orally administered peptides synergize statin activity
US8568766B2 (en) 2000-08-24 2013-10-29 Gattadahalli M. Anantharamaiah Peptides and peptide mimetics to treat pathologies associated with eye disease
US7144862B2 (en) * 2000-08-24 2006-12-05 The Regents Of The University Of California Orally administered peptides to ameliorate atherosclerosis
US7723303B2 (en) * 2000-08-24 2010-05-25 The Regents Of The University Of California Peptides and peptide mimetics to treat pathologies characterized by an inflammatory response
US6982251B2 (en) 2000-12-20 2006-01-03 Schering Corporation Substituted 2-azetidinones useful as hypocholesterolemic agents
ES2277890T3 (es) * 2000-12-21 2007-08-01 Sanofi-Aventis Deutschland Gmbh Nuevas difenilazetidinonas, procedimiento para su preparacion, medicamentos que contienen estos compuestos y su uso para el tratamiento de trastornos del metabolismo de lipidos.
US7071181B2 (en) 2001-01-26 2006-07-04 Schering Corporation Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors
BRPI0206641B8 (pt) 2001-01-26 2021-05-25 Merck Sharp & Dohme uso de um inibidor da absorção de esteróis
SK288217B6 (sk) 2001-01-26 2014-08-05 Merck Sharp & Dohme Corp. Zmes, terapeutická kombinácia, farmaceutický prostriedok a ich použitie
US7025985B2 (en) * 2001-05-28 2006-04-11 Kanebo, Ltd. Dihydroxyphenyl compounds and glucoside compounds thereof
WO2002096399A1 (fr) * 2001-05-28 2002-12-05 Kanebo, Limited Accelerateur de lipolyse, preparation dermatologique cosmetique pour reduction de masse corporelle, et composition d'aliment ou de boisson contenant cet accelerateur, et procede de reduction de masse corporelle et utilisation medicinale sur la base de l'activite de cet accelerateur
US6987123B2 (en) 2001-07-26 2006-01-17 Cadila Healthcare Limited Heterocyclic compounds, their preparation, pharmaceutical compositions containing them and their use in medicine
NZ531917A (en) 2001-09-14 2006-01-27 Japan Tobacco Inc Linked biaryl compounds
DE60216300T2 (de) 2001-09-21 2007-06-28 Schering Corp. Behandlung von xanthom mittels azetidinon-derivate als hemmer der sterol absorption
US7056906B2 (en) 2001-09-21 2006-06-06 Schering Corporation Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women
US7053080B2 (en) 2001-09-21 2006-05-30 Schering Corporation Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
US20030220374A1 (en) * 2002-01-14 2003-11-27 Pharmacia Corporation Compositions and methods of treatment involving peroxisome proliferator-activated receptor-gamma agonists and cyclooxygenase-2 selective inhibitors
AR039090A1 (es) * 2002-03-22 2005-02-09 Novartis Ag Combinacion de compuestos organicos
US6716842B2 (en) 2002-04-05 2004-04-06 Warner-Lambert Company, Llc Antidiabetic agents
AU2003225027A1 (en) * 2002-04-16 2003-11-03 Merck And Co., Inc. Combination therapy using a ppar alpha/gamma agonist
ITMI20021012A1 (it) * 2002-05-13 2003-11-13 Giovanni Scaramuzzino Combinazione di un inibitore dell'enzima hmg-coa reduttasi e di un estere nitrato
EP1388352A1 (en) * 2002-08-08 2004-02-11 Laboratoires Fournier S.A. Use of a ppar-alpha agonist to treat patients suffering from weight gain associated with a ppar-gamma agonist treatment
DK1537078T3 (da) * 2002-08-29 2010-08-02 Merck Sharp & Dohme Indoler med anti-diabetisk aktivitet
CA2495915A1 (en) * 2002-08-29 2004-03-11 Merck & Co., Inc. Indoles having anti-diabetic activity
JP4286782B2 (ja) 2002-09-12 2009-07-01 エフ.ホフマン−ラ ロシュ アーゲー 糖尿病の治療に有用な、pparアゴニストとしてのn−置換−1h−インドール−5−プロピオン酸化合物
AU2003291719A1 (en) 2002-11-06 2004-06-03 Schering Corporation Cholesterol absorptions inhibitors for the treatment of autoimmune disorders
DE10300099A1 (de) * 2003-01-07 2004-07-15 Bayer Healthcare Ag Indol-Phenylsulfonamid-Derivate
HRP20050696B1 (en) 2003-01-14 2008-10-31 Arena Pharmaceuticals Inc. 1,2,3-trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prpphylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
WO2004069158A2 (en) 2003-01-27 2004-08-19 Merck & Co., Inc. Substituted pyrazoles, compositions containing such compounds and methods of use
CN1756756A (zh) 2003-03-07 2006-04-05 先灵公司 取代的2-吖丁啶酮化合物、其制剂及其治疗高胆甾醇血症的用途
CA2517573C (en) 2003-03-07 2011-12-06 Schering Corporation Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia
ES2311806T3 (es) 2003-03-07 2009-02-16 Schering Corporation Compuesto de azetidinona sustituidos, fornulaciones y usos de los mismos para el tratamiento de hipercolesterolemia.
US7459442B2 (en) 2003-03-07 2008-12-02 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
CA2522080A1 (en) * 2003-04-14 2004-10-28 The Institutes For Pharmaceutical Discovery, Llc N- (((((1,3-thiazol-2-yl) amino) carbonyl) phenyl) sulfonyl) phenylalanine derivatives and related compounds for the treatment of diabetes
US7358364B2 (en) 2003-04-30 2008-04-15 The Institute For Pharmaceutical Discovery Llc Substituted carboxylic acids
WO2004098510A2 (en) * 2003-04-30 2004-11-18 Beth Israel Deaconess Medical Center Cystic fibrosis therapy
US7981915B2 (en) * 2003-04-30 2011-07-19 Beth Israel Deaconess Medical Center Methods for modulating PPAR biological activity for the treatment of diseases caused by mutations in the CFTR gene
WO2004100895A2 (en) * 2003-05-13 2004-11-25 Pharmacia Corporation Compositions of a cyclooxygenase-2 selective inhibitor and a peroxisome proliferator activated receptor agonist for the treatment of ischemic mediated central nervous system disorders
WO2004108126A1 (en) * 2003-06-06 2004-12-16 Snowden Pharmaceuticals, Llc Fibric acid derivatives for the treatment of irritable bowel syndrome
WO2004110368A2 (en) * 2003-06-06 2004-12-23 Merck & Co., Inc. Combination therapy for the treatment of hypertension
US7132426B2 (en) 2003-07-14 2006-11-07 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
DE10335449A1 (de) * 2003-08-02 2005-02-17 Bayer Healthcare Ag Bicyclische Indolinsulfonamid-Derivate
DE10337839A1 (de) * 2003-08-18 2005-03-17 Bayer Healthcare Ag Indolin-Derivate
US7223761B2 (en) 2003-10-03 2007-05-29 Amgen Inc. Salts and polymorphs of a potent antidiabetic compound
US20050074443A1 (en) * 2003-10-03 2005-04-07 Treadwell Benjamin V. Methods of attenuating autoimmune disease and compositions useful therefor
MXPA06004642A (es) * 2003-11-05 2006-06-27 Hoffmann La Roche Derivados de heteroaril como activadores de los receptores activados de proliferadores de peroxisoma (ppar).
AU2004291262C1 (en) * 2003-11-05 2011-08-11 F. Hoffmann-La Roche Ag Phenyl derivatives as PPAR agonists
CN1875001A (zh) * 2003-11-05 2006-12-06 霍夫曼-拉罗奇有限公司 作为ppar激活剂的苯并增环化合物
WO2005056522A2 (en) 2003-12-04 2005-06-23 National Health Research Institutes Indole compounds
JP2005200419A (ja) * 2004-01-16 2005-07-28 National Health Research Inst 癌治療法
WO2005112921A2 (en) * 2004-04-26 2005-12-01 Vanderbilt University Indoleacetic acid and indenacetic acid derivatives as therapeutic agents with reduced gastrointestinal toxicity
US20080076810A1 (en) * 2004-05-28 2008-03-27 Weiguo Lui Benzoureas Having Anti-Diabetic Activity
EP2336113A1 (en) * 2004-05-29 2011-06-22 7TM Pharma A/S CRTH2 Receptor Ligands for Medical Use
ES2306165T3 (es) * 2004-06-04 2008-11-01 MERCK & CO., INC. Derivados de pirazol, composiciones que contienen dichos compuestos y procedimientos de uso.
JP2008505091A (ja) 2004-07-02 2008-02-21 メルク エンド カムパニー インコーポレーテッド 抗糖尿病活性を有するインドール
JP2008507528A (ja) 2004-07-22 2008-03-13 メルク エンド カムパニー インコーポレーテッド 置換ピラゾール、このような化合物を含有する組成物及び使用方法
AU2005266337A1 (en) 2004-07-30 2006-02-02 Laboratorios Salvat, S.A. Tyrosine derivatives as PPAR-gamma-modulators
US20060205669A1 (en) * 2004-09-16 2006-09-14 The Regents Of The University Of California G-type peptides and other agents to ameliorate atherosclerosis and other pathologies
JP2008019169A (ja) * 2004-10-25 2008-01-31 Osaka Univ 新規ppar調節剤およびそのスクリーニング方法
WO2006055708A2 (en) * 2004-11-18 2006-05-26 The Institutes For Pharmaceutical Discovery, Llc Heterocycle substituted carboxylic acids for the treatment of diabetes
RU2414236C2 (ru) 2004-12-06 2011-03-20 Зе Риджентс Оф Зи Юнивесити Оф Кэлифонье Способ улучшения структуры и/или функций артериол
DOP2006000008A (es) * 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
FR2880887B1 (fr) * 2005-01-14 2009-01-30 Merck Sante Soc Par Actions Si Derives d'hydroxyphenols, procedes pour leur preparation, compositions pharmaceutiques les contenant et applications en therapeutique
CN102584754B (zh) 2005-03-04 2016-02-03 默沙东公司 具有抗糖尿病活性的稠合芳香化合物
EA200900786A1 (ru) * 2005-04-29 2009-10-30 Зе Риджентс Оф Зи Юнивесити Оф Кэлифонье Пептид в качестве лекарственного средства и способ лечения патологий, связанных с воспалительными процессами, посредством пептида
US20080293639A1 (en) * 2005-04-29 2008-11-27 The Regents Of The University Of California Peptides and peptide mimetics to treat pathologies characterized by an inflammatory response
KR20080015802A (ko) * 2005-05-24 2008-02-20 디에스엠 아이피 어셋츠 비.브이. 염증 질환의 치료를 위한 리구스틸라이드 유도체
EP1907381A4 (en) 2005-07-06 2009-08-26 Merck & Co Inc ANTIDIABETIC OXAZOLIDE INDIONE AND THIAZOLIDE INDIONE
EP1910303A2 (en) 2005-07-26 2008-04-16 Merck & Co., Inc. Process for synthesizing a substituted pyrazole
US20070161006A1 (en) * 2006-01-10 2007-07-12 Vita Genomics, Inc. Single nucleotide polymorphisms in protein-tyrosine phosphatase receptor-type delta for the diagnosis of susceptibility to infection and asthma
PE20071221A1 (es) * 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
DE602007010420D1 (de) 2006-04-11 2010-12-23 Arena Pharm Inc Verfahren zur verwendung des gpr119-rezeptors zur identifizierung von verbindungen zur erhöhung der knochenmasse bei einer person
CA2657691A1 (en) 2006-06-19 2007-12-27 Vanderbilt University Methods and compositions for diagnostic and therapeutic targeting of cox-2
AU2007292883B2 (en) 2006-09-08 2013-09-05 Rhode Island Hospital Treatment, prevention, and reversal of alcohol-induced brain disease
KR101568799B1 (ko) 2007-01-26 2015-11-12 카네크 파마 인코포레이티드 융합된 방향족 ptp-1b 억제제
AU2008221194B2 (en) 2007-02-26 2013-06-27 Merck Canada Inc. Indole and indoline cyclopropyl amide derivatives as EP4 receptor antagonists
CA2688187C (en) 2007-05-07 2016-10-11 Merck & Co., Inc. Method of treament using fused aromatic compounds having anti-diabetic activity
US20080319221A1 (en) * 2007-06-22 2008-12-25 Bernd Junker Esters of Pentahydroxyhexylcarbamoyl Alkanoic Acids
US20080319218A1 (en) * 2007-06-22 2008-12-25 Andreas Haubrich Processes for Making and Using Benzyl Pentahydroxyhexylcarbamoylundecanoate
JP2010537638A (ja) 2007-08-28 2010-12-09 ユーエービー リサーチ ファウンデーション 合成アポリポ蛋白質e模倣ポリペプチドおよび使用方法
AU2008296478B9 (en) 2007-08-28 2015-03-19 The Uab Research Foundation Synthetic apolipoprotein E mimicking polypeptides and methods of use
FR2921366B1 (fr) * 2007-09-26 2009-12-04 Servier Lab Nouveaux derives heterocycliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE102007054497B3 (de) * 2007-11-13 2009-07-23 Sanofi-Aventis Deutschland Gmbh Neue kristalline Diphenylazetidinonhydrate und Verfahren zu deren Herstellung
EP2146210A1 (en) * 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
JO2870B1 (en) 2008-11-13 2015-03-15 ميرك شارب اند دوهم كورب Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes
WO2010056717A1 (en) 2008-11-17 2010-05-20 Merck Sharp & Dohme Corp. Substituted bicyclic amines for the treatment of diabetes
TW201028414A (en) 2009-01-16 2010-08-01 Merck Sharp & Dohme Oxadiazole beta carboline derivatives as antidiabetic compounds
JP2012515781A (ja) 2009-01-23 2012-07-12 シェーリング コーポレイション 架橋および縮合複素環式抗糖尿病化合物
AU2010206789A1 (en) 2009-01-23 2011-07-28 Merck Sharp & Dohme Corp. Bridged and fused antidiabetic compounds
EP2393810A1 (en) 2009-02-05 2011-12-14 Schering Corporation Phthalazine-containing antidiabetic compounds
CA2768577A1 (en) 2009-07-23 2011-01-27 Schering Corporation Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
WO2011019538A1 (en) 2009-08-13 2011-02-17 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
EP2473047B1 (en) 2009-09-02 2014-08-13 Merck Sharp & Dohme Corp. Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
CA2785790A1 (en) 2010-01-15 2011-07-21 Merck Sharp & Dohme Corp. Oxadiazole beta carboline derivatives as antidiabetic compounds
WO2011103256A1 (en) 2010-02-22 2011-08-25 Merck Sharp & Dohme Corp. Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
EP2563764B1 (en) 2010-04-26 2015-02-25 Merck Sharp & Dohme Corp. Novel spiropiperidine prolylcarboxypeptidase inhibitors
US9365539B2 (en) 2010-05-11 2016-06-14 Merck Sharp & Dohme Corp. Prolylcarboxypeptidase inhibitors
US8980929B2 (en) 2010-05-21 2015-03-17 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
EP2579873A4 (en) 2010-06-11 2013-11-27 Merck Sharp & Dohme NOVEL PROLYLCARBOXYPEPTIDASE HEMMER
EP2605658B1 (en) 2010-08-18 2016-03-23 Merck Sharp & Dohme Corp. Spiroxazolidinone compounds
MX2013003184A (es) 2010-09-22 2013-06-07 Arena Pharm Inc Moduladores del receptor gpr119 y el tratamiento de transtornos relacionados con el mismo.
US9108920B2 (en) 2010-10-29 2015-08-18 Merck Sharp & Dohme Corp. Diazeniumdiolate heterocyclic derivatives
MX351305B (es) 2011-01-20 2017-10-09 Merck Sharp & Dohme Antagonistas del receptor de mineralocorticoides.
JO3350B1 (ar) 2011-03-07 2019-03-13 Merck Sharp & Dohme مشتقات حلقية غير متجانسة محتوية على مجموعات أمينو أولية ومركبات داي أزينيومديولات
WO2012138845A1 (en) 2011-04-08 2012-10-11 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
EP2697203B1 (en) 2011-04-13 2017-05-24 Merck Sharp & Dohme Corporation Mineralocorticoid receptor antagonists
WO2012151114A1 (en) 2011-05-02 2012-11-08 Merck Sharp & Dohme Corp. Diazeniumdiolate cyclohexyl derivatives
JP2014518890A (ja) 2011-06-02 2014-08-07 インターベット インターナショナル ベー. フェー. イミダゾール誘導体
US9006228B2 (en) 2011-06-16 2015-04-14 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment
WO2012178142A1 (en) * 2011-06-23 2012-12-27 Metabolic Solutions Development Company, Llc Ppar-sparing compounds and combinations fort the treatment of diabetes and other metabolic diseases
US9422266B2 (en) 2011-09-30 2016-08-23 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
WO2013055606A1 (en) 2011-10-13 2013-04-18 Merck Sharp & Dohme Corp. Mineralocorticoid receptor antagonists
EP3078374B1 (en) 2011-10-17 2019-06-19 Vanderbilt University Indomethacin analogs for the treatment of castrate-resistant prostate cancer
WO2013062838A1 (en) 2011-10-24 2013-05-02 Merck Sharp & Dohme Corp. Substituted piperidinyl compounds useful as gpr119 agonists
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
WO2013068328A1 (en) 2011-11-07 2013-05-16 Intervet International B.V. Bicyclo [2.2.2] octan-1-ylcarboxylic acid compounds as dgat-1 inhibitors
WO2013068439A1 (en) 2011-11-09 2013-05-16 Intervet International B.V. 4-amino-5-oxo-7,8-dihydropyrimido[5, 4 -f] [1, 4] oxazepine compounds as dgat1 inhibitors
EP2780337B1 (en) 2011-11-15 2017-12-20 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds useful as gpr119 agonists
WO2013122920A1 (en) 2012-02-17 2013-08-22 Merck Sharp & Dohme Corp. Dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2013155600A1 (en) 2012-04-16 2013-10-24 Kaneq Pharma Fused aromatic phosphonate derivatives as precursors to ptp-1b inhibitors
US9315508B2 (en) 2012-07-23 2016-04-19 Merck Sharp & Dohme Corp. Treating diabetes with dipeptidyl peptidase-IV inhibitors
US9453038B2 (en) 2012-12-17 2016-09-27 Merck Sharp & Dohme Corp. Glucokinase activator compounds, compositions containing such compounds, and methods of treatment
US9717714B2 (en) 2012-12-19 2017-08-01 Merck Sharp & Dohme Corp. Spirocyclic CETP inhibitors
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
WO2015089809A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Antidiabetic substituted heteroaryl compounds
EP3097101B1 (en) 2014-01-24 2020-12-23 Merck Sharp & Dohme Corp. Isoquinoline derivatives as mgat2 inhibitors
WO2015176267A1 (en) 2014-05-22 2015-11-26 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
US10011572B2 (en) 2014-07-29 2018-07-03 Merck Sharp & Dohme Corp. Monocyclic isoxazolines as inhibitors of cholesterol ester transfer protein
CA2954475C (en) 2014-07-31 2023-05-16 Uab Research Foundation Apoe mimetic peptides and higher potency to clear plasma cholesterol
WO2016022446A1 (en) 2014-08-08 2016-02-11 Merck Sharp & Dohme Corp. [5,6]-fused bicyclic antidiabetic compounds
WO2016022742A1 (en) 2014-08-08 2016-02-11 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
US10662171B2 (en) 2014-08-08 2020-05-26 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
MX382408B (es) 2014-10-24 2025-03-13 Merck Sharp & Dohme Llc Coagonistas de los receptores de glucagón y de glp-1.
TW201625635A (zh) 2014-11-21 2016-07-16 默沙東藥廠 作為可溶性鳥苷酸環化酶活化劑之三唑并吡基衍生物
US11007175B2 (en) 2015-01-06 2021-05-18 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
US10245264B2 (en) 2015-05-27 2019-04-02 Merck Sharp & Dohme Corp. Substituted imidazo[1,2-a]pyrazines as soluble guanylate cyclase activators
WO2016191335A1 (en) 2015-05-28 2016-12-01 Merck Sharp & Dohme Corp. Imidazo-pyrazinyl derivatives useful as soluble guanylate cyclase activators
BR112017027656B1 (pt) 2015-06-22 2023-12-05 Arena Pharmaceuticals, Inc. Hábito cristalino de placa livre de sal de l-arginina de ácido (r)-2-(7-(4- ciclopentil-3-(trifluorometil)benzilóxi)- 1,2,3,4-tetra-hidrociclo-penta[b]indol-3- il)acético, composição farmacêutica que o compreende, seus usos e método de preparação do mesmo
US20180230166A1 (en) 2015-07-13 2018-08-16 Merck Sharp & Dohme Corp. Bicyclic heterocycles as inhibitors of cholesterol ester transfer protein
EP3359191A4 (en) 2015-10-05 2019-05-29 Merck Sharp & Dohme Corp. ANTIBODY PEPTIDE CONJUGATES WITH AGONISTEACTIVITY ON GLUCAGON RECEPTORS AND GLUCAGON-LIKE PEPTIDE-1
WO2017095724A1 (en) 2015-11-30 2017-06-08 Merck Sharp & Dohme Corp. Aryl sulfonamides as blt1 antagonists
WO2017095725A1 (en) 2015-11-30 2017-06-08 Merck Sharp & Dohme Corp. Aryl sulfonamides as blt1 antagonists
WO2017107052A1 (en) 2015-12-22 2017-06-29 Merck Sharp & Dohme Corp. Soluble guanylate cyclase stimulators
WO2017197555A1 (en) 2016-05-16 2017-11-23 Merck Sharp & Dohme Corp. Fused pyrazine derivatives useful as soluble guanylate cyclase stimulators
WO2017201683A1 (en) 2016-05-25 2017-11-30 Merck Sharp & Dohme Corp. Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists
WO2018034917A1 (en) 2016-08-15 2018-02-22 Merck Sharp & Dohme Corp. Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease
WO2018034918A1 (en) 2016-08-15 2018-02-22 Merck Sharp & Dohme Corp. Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease
WO2018057409A1 (en) 2016-09-20 2018-03-29 Merck Sharp & Dohme Corp. Substituted 1-methyl-1,2,3,4-tetrahydroisoquinoline molecules as pcsk9 allosteric binders
MX2019005679A (es) 2016-11-18 2019-08-14 Merck Sharp & Dohme Derivados de indol de utilidad como inhibidores de diacilglicerido o-aciltransferasa 2.
US11104690B2 (en) 2016-11-18 2021-08-31 Merck Sharp & Dohme Corp. Indazole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
WO2018107415A1 (en) 2016-12-15 2018-06-21 Merck Sharp & Dohme Corp. Hydroxy isoxazole compounds useful as gpr120 agonists
CA3053418A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
BR112020024762A2 (pt) 2018-06-06 2021-03-23 Arena Pharmaceuticals, Inc. métodos de tratamento de condições relacionadas ao receptor s1p1
JOP20190150A1 (ar) 2018-06-21 2019-12-21 Merck Sharp & Dohme مركبات مناهضة لـ pcsk9
EP3946324B1 (en) 2019-04-04 2025-07-30 Merck Sharp & Dohme LLC Inhibitors of histone deacetylase-3 useful for the treatment of cancer, inflammation, neurodegeneration diseases and diabetes
US20220281886A1 (en) 2019-05-22 2022-09-08 Merck Sharp Dohme Corp. Natriuretic peptide receptor a agonists useful for the treatment of cardiometabolic diseases, kidney disease and diabetes
EP3972590A4 (en) 2019-05-22 2023-06-14 Merck Sharp & Dohme LLC NATRIURETIC PEPTIDE RECEPTOR A AGONISTS USED TO TREAT CARDIOMETABOLIC DISEASES, KIDNEY DISEASES AND DIABETES
WO2021041770A1 (en) 2019-08-30 2021-03-04 Merck Sharp & Dohme Corp. Pcsk9 antagonist compounds
EP3842061A1 (en) 2019-12-23 2021-06-30 Merck Sharp & Dohme Corp. Stapled triazole co-agonists of the glucagon and glp-1 receptors
EP3842449A1 (en) 2019-12-23 2021-06-30 Merck Sharp & Dohme Corp. Stapled olefin co-agonists of the glucagon and glp-1 receptors
EP3842060A1 (en) 2019-12-23 2021-06-30 Merck Sharp & Dohme Corp. Stapled lactam co-agonists of the glucagon and glp-1 receptors
US11787810B2 (en) 2020-05-18 2023-10-17 Merck Sharp & Dohme Llc Diacylglyceride O-acyltransferase 2 inhibitors
US12410159B2 (en) 2020-10-08 2025-09-09 Merck Sharp & Dohme Llc Preparation of oxindole derivatives as novel diacylglyceride O-acyltransferase 2 inhibitors
IL310851A (en) 2021-08-19 2024-04-01 Merck Sharp & Dohme Llc Compounds for the treatment of diseases associated with PCSK9 activity
CA3259207A1 (en) 2022-06-15 2023-12-21 Merck Sharp & Dohme Llc CYCLIC PEPTIDES TO TRAPP INTERLEUKIN-1 BETA
CN120500483A (zh) 2022-12-02 2025-08-15 默沙东有限责任公司 作为新型二酰基甘油o-酰基转移酶2抑制剂的稠合唑衍生物的制备
US20250152658A1 (en) 2023-11-14 2025-05-15 Merck Sharp & Dohme Llc Cyclic peptide for trapping interleukin-1 beta
WO2025128805A1 (en) 2023-12-15 2025-06-19 Merck Sharp & Dohme Llc A cyclic peptide il-1beta trap for the treatment of atherosclerosis and inflammatory disorders

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3564009A (en) 1966-01-13 1971-02-16 Sumitomo Chemical Co Process for producing 1-acylindole derivatives
CH605742A5 (en) 1973-11-29 1978-10-13 Crc Ricerca Chim 1-Benzoyl-2-methyl-indole derivs.
WO1990005721A1 (en) 1988-11-14 1990-05-31 The Upjohn Company Alpha-amino-indole-3-acetic acids useful as anti-diabetic, anti-obesity and anti-atherosclerotic agents
JPH0764841B2 (ja) 1990-10-03 1995-07-12 ファイザー製薬株式会社 インドール誘導体およびその用途
WO1993005020A1 (en) 1991-09-06 1993-03-18 Merck & Co., Inc. Indoles as inhibitors of hiv reverse transcriptase
US5527819A (en) 1991-09-06 1996-06-18 Merck & Co., Inc. Inhibitors of HIV reverse transcriptase
CZ236494A3 (en) 1992-04-03 1994-12-15 Upjohn Co Pharmaceutically active bicyclic-heterocyclic amines
ZA939516B (en) * 1992-12-22 1994-06-06 Smithkline Beecham Corp Endothelin receptor antagonists
US5686481A (en) * 1993-12-21 1997-11-11 Smithkline Beecham Corporation Endothelin receptor antagonists
MX9700693A (es) 1994-07-26 1997-04-30 Pfizer Derivados del 4-indol.
HUT76923A (hu) 1994-07-27 1998-01-28 Sankyo Company Limited Muszkarinreceptorokra alloszterikus hatást kifejtő heterociklusos vegyületek
US5532237A (en) 1995-02-15 1996-07-02 Merck Frosst Canada, Inc. Indole derivatives with affinity for the cannabinoid receptor
EP0768311B1 (en) * 1995-03-09 2003-08-06 Kyowa Hakko Kogyo Co., Ltd. Pyrrolocarbazole derivatives
FR2735774B1 (fr) 1995-06-21 1997-09-12 Sanofi Sa Utilisation de composes agonistes du recepteur cb2 humain pour la preparation de medicaments immunomodulateurs, nouveaux composes agonistes du recepteur cb2 et les compositions pharmaceutiques les contenant
WO1998008818A1 (en) 1996-08-26 1998-03-05 Genetics Institute, Inc. Inhibitors of phospholipase enzymes
CA2322162A1 (en) * 1998-02-25 1999-09-02 Genetics Institute, Llc Inhibitors of phospholipase enzymes
EP1062216A1 (en) 1998-02-25 2000-12-27 Genetics Institute, Inc. Inhibitors of phospholipase a2
IL137718A0 (en) 1998-02-25 2001-10-31 Genetics Inst Inhibitors of phospholipase enzymes
PL349192A1 (en) * 1998-12-18 2002-07-01 Axys Pharmaceuticals Protease inhibitors

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