EA016126B1 - Антагонисты неосновного рецептора-1 меланинконцентрирующего гормона - Google Patents

Антагонисты неосновного рецептора-1 меланинконцентрирующего гормона Download PDF

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Publication number
EA016126B1
EA016126B1 EA200801165A EA200801165A EA016126B1 EA 016126 B1 EA016126 B1 EA 016126B1 EA 200801165 A EA200801165 A EA 200801165A EA 200801165 A EA200801165 A EA 200801165A EA 016126 B1 EA016126 B1 EA 016126B1
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EA
Eurasian Patent Office
Prior art keywords
nmr
group
mmol
alkyl
compound according
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EA200801165A
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English (en)
Russian (ru)
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EA200801165A1 (ru
Inventor
Уильям Н. Уошберн
Андрес С. Хернандес
Марк С. Мэнфреди
Джеффри А. Робл
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Бристол-Маерс Сквибб Компани
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Publication of EA200801165A1 publication Critical patent/EA200801165A1/xx
Publication of EA016126B1 publication Critical patent/EA016126B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P3/08Drugs 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
    • A61P5/00Drugs for disorders of the endocrine system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
EA200801165A 2005-10-26 2006-10-26 Антагонисты неосновного рецептора-1 меланинконцентрирующего гормона EA016126B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US73045305P 2005-10-26 2005-10-26
US11/586,255 US8618115B2 (en) 2005-10-26 2006-10-25 Substituted thieno[3,2-d]pyrimidinones as MCHR1 antagonists and methods for using them
PCT/US2006/041725 WO2007050726A2 (en) 2005-10-26 2006-10-26 Thienopyrimidinone derivatives as melanin concentrating hormone receptor-1 antagonists

Publications (2)

Publication Number Publication Date
EA200801165A1 EA200801165A1 (ru) 2008-10-30
EA016126B1 true EA016126B1 (ru) 2012-02-28

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA200801165A EA016126B1 (ru) 2005-10-26 2006-10-26 Антагонисты неосновного рецептора-1 меланинконцентрирующего гормона

Country Status (16)

Country Link
US (1) US8618115B2 (https=)
EP (2) EP1948665B1 (https=)
JP (1) JP2009513658A (https=)
KR (1) KR20080067681A (https=)
AR (1) AR056155A1 (https=)
AU (1) AU2006306140A1 (https=)
BR (1) BRPI0617945A2 (https=)
CA (1) CA2627653A1 (https=)
EA (1) EA016126B1 (https=)
GE (1) GEP20115213B (https=)
IL (1) IL190898A0 (https=)
NO (1) NO20081772L (https=)
NZ (1) NZ567659A (https=)
PE (1) PE20070532A1 (https=)
TW (1) TW200728289A (https=)
WO (1) WO2007050726A2 (https=)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7285557B2 (en) * 2001-10-15 2007-10-23 Smithkline Beecham P.L.C. Pyrimidinones as melanin concentrating hormone receptor 1
US7553836B2 (en) * 2006-02-06 2009-06-30 Bristol-Myers Squibb Company Melanin concentrating hormone receptor-1 antagonists
JP2010500300A (ja) 2006-08-08 2010-01-07 サノフィ−アベンティス アリールアミノアリール−アルキル−置換イミダゾリジン−2,4−ジオン、それらの製造法、それらの化合物を含有する薬剤、およびそれらの使用
US20080153810A1 (en) * 2006-11-15 2008-06-26 Forest Laboratories Holdings Limited Indazole derivatives useful as melanin concentrating receptor ligands
JP2010525077A (ja) * 2007-04-25 2010-07-22 ブリストル−マイヤーズ スクイブ カンパニー 非塩基性メラニン凝集ホルモン受容体−1アンタゴニスト
EP2242745A1 (de) * 2008-02-07 2010-10-27 Sanofi-Aventis Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
PE20091928A1 (es) * 2008-05-29 2009-12-31 Bristol Myers Squibb Co Tienopirimidinas hidroxisustituidas como antagonistas de receptor-1 de hormona concentradora de melanina no basicos
WO2010003624A2 (en) 2008-07-09 2010-01-14 Sanofi-Aventis Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof
CN102272135A (zh) * 2008-10-08 2011-12-07 百时美施贵宝公司 唑并吡咯酮黑色素浓集激素受体-1拮抗剂
WO2010042682A1 (en) 2008-10-08 2010-04-15 Bristol-Myers Squibb Company Azolotriazinone melanin concentrating hormone receptor-1 antagonists
WO2010068601A1 (en) 2008-12-08 2010-06-17 Sanofi-Aventis A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof
EP2405913A1 (en) 2009-03-09 2012-01-18 Bristol-Myers Squibb Company Pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
WO2010104818A1 (en) 2009-03-09 2010-09-16 Bristol-Myers Squibb Company Aza pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
MX2012001729A (es) 2009-08-26 2012-06-13 Sanofi Sa Nuevos hidratos cristalinos de fluoroglicosido heteroaromatico, productos farmaceuticos que comprenden estos compuestos, y su empleo.
EP2683705B1 (de) 2011-03-08 2015-04-22 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
EP2683699B1 (de) 2011-03-08 2015-06-24 Sanofi Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8828995B2 (en) 2011-03-08 2014-09-09 Sanofi Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
WO2012120052A1 (de) 2011-03-08 2012-09-13 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
US8871758B2 (en) 2011-03-08 2014-10-28 Sanofi Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
HUP1100241A3 (en) 2011-05-06 2013-12-30 Richter Gedeon Nyrt Oxetane substituted pyrimidones
CN103130819B (zh) * 2011-12-01 2016-01-20 中国科学院上海药物研究所 噻吩[3,2-d]并嘧啶-4-酮类化合物、其制备方法、药物组合物及用途
US20140206667A1 (en) 2012-11-14 2014-07-24 Michela Gallagher Methods and compositions for treating schizophrenia
WO2015114663A1 (en) 2014-01-30 2015-08-06 Council Of Scientific & Industrial Research Novel thieno [2,3-d]pyrimidin-4(3h)-one compounds with antimycobacterial properties
AR103297A1 (es) 2014-12-30 2017-05-03 Forma Therapeutics Inc Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 específica de ubiquitina
MA41291A (fr) 2014-12-30 2017-11-07 Forma Therapeutics Inc Dérivés de la pyrrolotriazinone et de l'imidazotriazinone en tant qu'inhibiteurs de la protéase spécifique de l'ubiquitine n° 7 (usp7) pour le traitement d'un cancer
EP3253765A1 (en) 2015-02-05 2017-12-13 Forma Therapeutics, Inc. Thienopyrimidinones as ubiquitin-specific protease 7 inhibitors
US9938300B2 (en) 2015-02-05 2018-04-10 Forma Therapeutics, Inc. Isothiazolopyrimidinones, pyrazolopyrimidinones, and pyrrolopyrimidinones as ubiquitin-specific protease 7 inhibitors
HK1248220A1 (zh) 2015-02-05 2018-10-12 Forma Therapeutics, Inc. 喹唑啉酮和偶氮喹唑啉作为泛特丁胺蛋白酶7抑制剂
EP4006038A1 (en) * 2015-12-09 2022-06-01 Cadent Therapeutics, Inc. Thienopyrimidinone nmda receptor modulators and uses thereof
SMT202000534T1 (it) 2015-12-09 2020-11-10 Cadent Therapeutics Inc Modulatori eteroaromatici del recettore nmda e loro usi
CN107216339B (zh) * 2016-03-22 2021-05-04 中国科学院上海药物研究所 一种dppiv抑制剂马来酸盐的多晶型及其制备方法
ES2975336T3 (es) 2016-12-22 2024-07-04 Novartis Ag Moduladores del receptor NMDA y usos de los mismos
BR112021001967A2 (pt) 2018-08-03 2021-04-27 Cadent Therapeutics, Inc. moduladores de receptor nmda heteroaromáticos e usos dos mesmos
KR102919209B1 (ko) 2018-08-10 2026-01-28 다이아핀 테라퓨틱스, 엘엘씨 트리-펩타이드 그리고 대사, 심장혈관 및 염증성 장애의 치료
WO2021207530A1 (en) * 2020-04-08 2021-10-14 Remix Therapeutics Inc. Compounds and methods for modulating splicing

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003033476A1 (en) * 2001-10-15 2003-04-24 Smithkline Beecham Plc Pyrimidinones as melanin concentrating hormone receptor 1
WO2004092181A1 (en) * 2003-04-11 2004-10-28 Smithkline Beecham Corporation Heterocyclic mchr1 antagonists
WO2005023782A1 (ja) * 2003-09-05 2005-03-17 Sankyo Company, Limited 置換された縮環ピリミジン-4(3h)-オン化合物
WO2005042541A1 (en) * 2003-10-23 2005-05-12 Glaxo Group Limited 3-(4-aminophenyl) thienopyrimid-4-one derivatives as mch r1 antagonists for the treatment of obesity, diabetes, depression and anxiety

Family Cites Families (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3674836A (en) 1968-05-21 1972-07-04 Parke Davis & Co 2,2-dimethyl-{11 -aryloxy-alkanoic acids and salts and esters thereof
US4027009A (en) 1973-06-11 1977-05-31 Merck & Co., Inc. Compositions and methods for depressing blood serum cholesterol
JPS5612114B2 (https=) 1974-06-07 1981-03-18
JPS5432794A (en) 1977-08-18 1979-03-10 Omron Tateisi Electronics Co Manufacturing method of terminal rack
NO154918C (no) 1977-08-27 1987-01-14 Bayer Ag Analogifremgangsmaate til fremstilling av terapeutisk aktive derivater av 3,4,5-trihydroksypiperidin.
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
DE2951135A1 (de) 1979-12-19 1981-06-25 Hoechst Ag, 6230 Frankfurt Sulfonylharnstoffe, verfahren zu ihrer herstellung, pharmazeutische praeparate auf basis dieser verbindungen und ihre verwendung
MX7065E (es) 1980-06-06 1987-04-10 Sankyo Co Un procedimiento microbiologico para preparar derivados de ml-236b
US4450171A (en) 1980-08-05 1984-05-22 Merck & Co., Inc. Antihypercholesterolemic compounds
US4448784A (en) 1982-04-12 1984-05-15 Hoechst-Roussel Pharmaceuticals, Inc. 1-(Aminoalkylphenyl and aminoalkylbenzyl)-indoles and indolines and analgesic method of use thereof
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
US4499289A (en) 1982-12-03 1985-02-12 G. D. Searle & Co. Octahydronapthalenes
CA1327360C (en) 1983-11-14 1994-03-01 William F. Hoffman Oxo-analogs of mevinolin-like antihypercholesterolemic agents
US4613610A (en) 1984-06-22 1986-09-23 Sandoz Pharmaceuticals Corp. Cholesterol biosynthesis inhibiting pyrazole analogs of mevalonolactone and its derivatives
US4686237A (en) 1984-07-24 1987-08-11 Sandoz Pharmaceuticals Corp. Erythro-(E)-7-[3'-C1-3 alkyl-1'-(3",5"-dimethylphenyl)naphth-2'-yl]-3,5-dihydroxyhept-6-enoic acids and derivatives thereof
US4647576A (en) 1984-09-24 1987-03-03 Warner-Lambert Company Trans-6-[2-(substitutedpyrrol-1-yl)alkyl]-pyran-2-one inhibitors of cholesterol synthesis
EP0216785B1 (en) 1984-12-04 1991-01-30 Sandoz Ag Indene analogs of mevalonolactone and derivatives thereof
US4668794A (en) 1985-05-22 1987-05-26 Sandoz Pharm. Corp. Intermediate imidazole acrolein analogs
HUT48208A (en) 1985-10-25 1989-05-29 Sandoz Ag Process for producing heterocyclic analogues of mevalolactone derivatives and pharmaceutical compositions comprising such compounds
DE3543999A1 (de) 1985-12-13 1987-06-19 Bayer Ag Hochreine acarbose
FR2596393B1 (fr) 1986-04-01 1988-06-03 Sanofi Sa Derives de l'acide hydroxy-3 dihydroxyoxophosphorio-4 butanoique, leur procede de preparation, leur application comme medicament et les compositions les renfermant
US4681893A (en) 1986-05-30 1987-07-21 Warner-Lambert Company Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
FI89493C (fi) 1987-05-22 1993-10-11 Squibb & Sons Inc Foerfarande foer framstaellning av terapeutiskt aktiva, fosforhaltiga inhibitorer av hmg-coa-reduktas och vid foerfarandet anvaendbar ny mellanprodukt
US4759923A (en) 1987-06-25 1988-07-26 Hercules Incorporated Process for lowering serum cholesterol using poly(diallylmethylamine) derivatives
JP2569746B2 (ja) 1987-08-20 1997-01-08 日産化学工業株式会社 キノリン系メバロノラクトン類
US4871721A (en) 1988-01-11 1989-10-03 E. R. Squibb & Sons, Inc. Phosphorus-containing squalene synthetase inhibitors
US4924024A (en) 1988-01-11 1990-05-08 E. R. Squibb & Sons, Inc. Phosphorus-containing squalene synthetase inhibitors, new intermediates and method
NO177005C (no) 1988-01-20 1995-07-05 Bayer Ag Analogifremgangsmåte for fremstilling av substituerte pyridiner, samt mellomprodukter til bruk ved fremstillingen
US5506219A (en) 1988-08-29 1996-04-09 E. R. Squibb & Sons, Inc. Pyridine anchors for HMG-CoA reductase inhibitors
US5753675A (en) 1989-03-03 1998-05-19 Novartis Pharmaceuticals Corporation Quinoline analogs of mevalonolactone and derivatives thereof
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
US5177080A (en) 1990-12-14 1993-01-05 Bayer Aktiengesellschaft Substituted pyridyl-dihydroxy-heptenoic acid and its salts
JP2648897B2 (ja) 1991-07-01 1997-09-03 塩野義製薬株式会社 ピリミジン誘導体
DE4129603A1 (de) 1991-09-06 1993-03-11 Thomae Gmbh Dr K Kondensierte 5-gliedrige heterocyclen, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
GB9209628D0 (en) 1992-05-05 1992-06-17 Smithkline Beecham Plc Compounds
US5470845A (en) 1992-10-28 1995-11-28 Bristol-Myers Squibb Company Methods of using α-phosphonosulfonate squalene synthetase inhibitors including the treatment of atherosclerosis and hypercholesterolemia
LT3300B (en) 1992-12-23 1995-06-26 Schering Corp Combination of a cholesterol biosynhtesis inhibitor and a beta- lactam cholesterol absorbtion inhibitor
US5594016A (en) 1992-12-28 1997-01-14 Mitsubishi Chemical Corporation Naphthalene derivatives
US5662934A (en) 1993-01-05 1997-09-02 Najarian; Thomas Compositions and methods for lowering cholesterol while maintaining antioxidant levels
ES2133158T3 (es) 1993-01-19 1999-09-01 Warner Lambert Co Formulacion ci-981 oral, estable y proceso de preparacion del mismo.
EP0733048A1 (en) 1993-12-07 1996-09-25 Smithkline Beecham Plc Heterocyclic biphenylylamides useful as 5ht1d antagonists
US5776983A (en) 1993-12-21 1998-07-07 Bristol-Myers Squibb Company Catecholamine surrogates useful as β3 agonists
US5488064A (en) 1994-05-02 1996-01-30 Bristol-Myers Squibb Company Benzo 1,3 dioxole derivatives
US5385929A (en) 1994-05-04 1995-01-31 Warner-Lambert Company [(Hydroxyphenylamino) carbonyl] pyrroles
US5612359A (en) 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
US5491134A (en) 1994-09-16 1996-02-13 Bristol-Myers Squibb Company Sulfonic, phosphonic or phosphiniic acid β3 agonist derivatives
US5541204A (en) 1994-12-02 1996-07-30 Bristol-Myers Squibb Company Aryloxypropanolamine β 3 adrenergic agonists
US5698527A (en) 1995-08-08 1997-12-16 Merck & Co., Inc. Steroidal glycosides as antihyperlipidemic agents
AU717743B2 (en) 1995-12-13 2000-03-30 Regents Of The University Of California, The Nuclear receptor ligands and ligand binding domains
IL117702A0 (en) 1996-03-28 1996-07-23 Tel Aviv Medical Center Resear Drug for hyperlipoproteinemia
US5770615A (en) 1996-04-04 1998-06-23 Bristol-Myers Squibb Company Catecholamine surrogates useful as β3 agonists
DE19622222A1 (de) 1996-06-03 1997-12-04 Hoechst Ag Verwendung von Inhibitoren des zellulären Na·+·/H·+·-Exchangers (NHE) zur Herstellung eines Medikament zur Normalisierung der Serumlipide
US6537987B1 (en) 1996-06-20 2003-03-25 Pfizer Inc. 4,1-benzoxazepines or 4,1-benzothiazepines and their use as squalene synthetase inhibitors
HRP970330B1 (en) 1996-07-08 2004-06-30 Bayer Ag Cycloalkano pyridines
US6482821B2 (en) 1996-12-20 2002-11-19 Hoechst Aktiengellschaft Vitronectin receptor antagonists, their preparation and their use
DE19653647A1 (de) 1996-12-20 1998-06-25 Hoechst Ag Vitronectin - Rezeptorantagonisten, deren Herstellung sowie deren Verwendung
DE19653645A1 (de) 1996-12-20 1998-06-25 Hoechst Ag Vitronectin - Rezeptorantagonisten, deren Herstellung sowie deren Verwendung
TW536540B (en) 1997-01-30 2003-06-11 Bristol Myers Squibb Co Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe
BR9809598A (pt) 1997-05-08 2000-07-04 Agrevo Uk Ltd Uso de compostos, e, composto.
GB9713739D0 (en) 1997-06-27 1997-09-03 Karobio Ab Thyroid receptor ligands
CN1255386C (zh) 1997-10-08 2006-05-10 三共株式会社 有取代稠合杂环化合物
WO2000001389A1 (en) 1998-07-06 2000-01-13 Bristol-Myers Squibb Co. Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists
WO2000015201A2 (en) 1998-09-10 2000-03-23 Forbes Medi-Tech Inc. Compositions comprising one or more phytosterols, phytostanols or mixtures of both and one or more alpha, beta, delta, or gamma tocotrienols or derivatives thereof and use of the compositions in treating or preventing cardiovascular disease, its underlying conditions and other disorders
US6147089A (en) 1998-09-17 2000-11-14 Pfizer Inc. Annulated 4-carboxyamino-2-methyl-1,2,3,4,-tetrahydroquinolines
BR9915687A (pt) 1998-11-25 2001-12-04 Nutri Pharma As Composição compreendendo proteìna de soja,fibras de dieta e um composto fitoestrogênio eseu uso na prevenção e/ou tratamento de doençascardiovasculares
AU2157400A (en) 1998-12-23 2000-07-31 G.D. Searle & Co. Combinations of cholesteryl ester transfer protein inhibitors and hmg coa reductase inhibitors for cardiovascular indications
GB9828442D0 (en) 1998-12-24 1999-02-17 Karobio Ab Novel thyroid receptor ligands and method II
CA2362549A1 (en) 1999-02-24 2000-08-31 John Hopkins University Compositions and methods for modulating serum cholesterol
AU5031200A (en) 1999-05-28 2000-12-18 Vertex Pharmaceuticals Incorporated Method for preparing 5-substituted oxazoles
US6414002B1 (en) 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
MXPA03000923A (es) 2000-07-31 2003-06-09 Smithkline Beecham Plc Compuestos de carboxamida y su uso como antagonistas de un receptor 11cby humano.
WO2002101146A1 (fr) 2001-05-11 2002-12-19 Arina Nakayama Papier lumineux et son procede de production et d'utilisation
US7183415B2 (en) 2001-10-25 2007-02-27 Takeda Pharmaceutical Company Limited Quinoline compound
CN1747949A (zh) 2002-12-20 2006-03-15 法马西亚公司 无环吡唑化合物
WO2005047293A1 (en) 2003-11-07 2005-05-26 Neurocrine Biosciences, Inc. Melanin-concentrating hormone receptor antagonists and compositions and methods related thereto
US20050256124A1 (en) 2004-04-15 2005-11-17 Neurocrine Biosciences, Inc. Melanin-concentrating hormone receptor antagonists and compositions and methods related thereto
RU2266906C1 (ru) 2004-04-29 2005-12-27 Общество с ограниченной ответственностью "Исследовательский Институт Химического Разнообразия" (ООО "Исследовательский Институт Химического Разнообразия") Анелированные карбамоилазагетероциклы, способы их получения (варианты), фармацевтическая композиция, фокусированная библиотека
US7745447B2 (en) 2005-10-26 2010-06-29 Bristol-Myers Squibb Company Substituted thieno[3,2-D]pyrimidines as non-basic melanin concentrating hormone receptor-1 antagonists
US7553836B2 (en) 2006-02-06 2009-06-30 Bristol-Myers Squibb Company Melanin concentrating hormone receptor-1 antagonists

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003033476A1 (en) * 2001-10-15 2003-04-24 Smithkline Beecham Plc Pyrimidinones as melanin concentrating hormone receptor 1
WO2004092181A1 (en) * 2003-04-11 2004-10-28 Smithkline Beecham Corporation Heterocyclic mchr1 antagonists
WO2005023782A1 (ja) * 2003-09-05 2005-03-17 Sankyo Company, Limited 置換された縮環ピリミジン-4(3h)-オン化合物
WO2005042541A1 (en) * 2003-10-23 2005-05-12 Glaxo Group Limited 3-(4-aminophenyl) thienopyrimid-4-one derivatives as mch r1 antagonists for the treatment of obesity, diabetes, depression and anxiety

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CARPENTER ET AL.: "Novel benzimidazole-based MCH R1 antagonists", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 16, no. 19, 1 October 2006 (2006-10-01), pages 4994-5000, XP005611681, ISSN: 0960-894X, page 4997; table 1; compounds 24-29, page 4998; table 2; compounds 26-35, page 4998; table 3; compounds 36-47, page 4999; table 4 *
DATABASE WPI Week 200525, Derwent Publications Ltd., London, GB; AN 2005-242113, XP002427719 & WO 2005/023782 A1 (SANKYO CO LTD), 17 March 2005 (2005-03-17), page 95; compounds 9-138, abstract *
HERTZOG ET AL.: "The discovery and optimization of pyrimidinone-containing MCH R1 antagonists", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 16, no. 18, 15 September 2006 (2006-09-15), pages 4723-4727, XP005594946, ISSN: 0960-894X, page 4724; table 1; compounds 7A-7S *
WARSHAKOON ET AL.: "Design and synthesis of substituted quinolines as novel and selective melanin concentrating hormone antagonists as anti-obesity agents", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 16, no. 19, 1 October 2006 (2006-10-01), pages 5207-5211, XP005611723, ISSN: 0960-894X, page 5210; table 2; compounds 18A-18G *

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WO2007050726A2 (en) 2007-05-03
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BRPI0617945A2 (pt) 2011-08-09
EA200801165A1 (ru) 2008-10-30
EP1948665A2 (en) 2008-07-30
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US20070093509A1 (en) 2007-04-26

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