PE20081849A1 - Derivados de piperidin-4-il-propoxi-benzamida como agonistas de gpcr - Google Patents

Derivados de piperidin-4-il-propoxi-benzamida como agonistas de gpcr

Info

Publication number
PE20081849A1
PE20081849A1 PE2008000085A PE2008000085A PE20081849A1 PE 20081849 A1 PE20081849 A1 PE 20081849A1 PE 2008000085 A PE2008000085 A PE 2008000085A PE 2008000085 A PE2008000085 A PE 2008000085A PE 20081849 A1 PE20081849 A1 PE 20081849A1
Authority
PE
Peru
Prior art keywords
piperidin
propoxy
benzamide derivatives
hydroxy
alkyl
Prior art date
Application number
PE2008000085A
Other languages
English (en)
Inventor
Lisa Sarah Bertram
Matthew Colin Thor Fyfe
John Keily
Simon Andrew Swain
Revathy Perpetua Jeevaratnam
Original Assignee
Prosidion Ltd
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
Priority claimed from GB0700124A external-priority patent/GB0700124D0/en
Priority claimed from GB0708740A external-priority patent/GB0708740D0/en
Priority claimed from GB0719762A external-priority patent/GB0719762D0/en
Application filed by Prosidion Ltd filed Critical Prosidion Ltd
Publication of PE20081849A1 publication Critical patent/PE20081849A1/es

Links

Classifications

    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)

Abstract

SE REFIERE A DERIVADOS DE PIPERIDIN-4-IL-PROPOXI-BENZAMIDA DE FORMULA (I), EN DONDE UNO DE X O Y ES O Y EL OTRO ES N; R1 ES -CONHR5; R2 ES H, HALO O METILO; R3 ES H O METILO; R4 ES ALQUILO (C2-C5) Y R5 ES H, ALQUILO(C1-C3) O ALQUILO(C2-C3) SUSTITUIDO CON HIDROXI. SON SELECCIONADOS: 2-FLUORO-N-((R-2-HIDROXI-1-METILETIL)-4-{3-[1-(3-ISOPROPIL-[1,2,4]-OXADIAZOL-5-IL)PIPERIDIN-4-IL]PROPOXI}BENZAMIDA, N-((R-2-HIDROXI-1-METILETIL)-4-{3-[1-(3-ISOPROPIL-[1,2,4]OXADIAZOL-5-IL)PIPERIDIN-4-IL]PROPOXI}-2-METILBENZAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR ACOPLADO A LA PROTEINA G (GPCR) Y SON UTILES EN EL TRATAMIENTO DE LA OBESIDAD, COMO REGULADORES DE LA SACIEDAD, DEL SINDROME METABOLICO Y LA DIABETES
PE2008000085A 2007-01-04 2008-01-03 Derivados de piperidin-4-il-propoxi-benzamida como agonistas de gpcr PE20081849A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0700124A GB0700124D0 (en) 2007-01-04 2007-01-04 GPCR agonists
GB0708740A GB0708740D0 (en) 2007-05-08 2007-05-08 Gpcr agonists
GB0719762A GB0719762D0 (en) 2007-10-10 2007-10-10 GPCR agonists

Publications (1)

Publication Number Publication Date
PE20081849A1 true PE20081849A1 (es) 2009-01-26

Family

ID=39203222

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000085A PE20081849A1 (es) 2007-01-04 2008-01-03 Derivados de piperidin-4-il-propoxi-benzamida como agonistas de gpcr

Country Status (28)

Country Link
US (1) US20100022591A1 (es)
EP (2) EP2114931B1 (es)
JP (1) JP2010514829A (es)
KR (1) KR20090104092A (es)
CN (1) CN101627036A (es)
AR (1) AR064736A1 (es)
AT (1) ATE531710T1 (es)
AU (1) AU2008203673A1 (es)
BR (1) BRPI0806468A2 (es)
CA (1) CA2674093A1 (es)
CL (1) CL2008000017A1 (es)
DK (1) DK2114931T3 (es)
EA (1) EA015805B9 (es)
ES (1) ES2376015T3 (es)
HK (1) HK1135704A1 (es)
HR (1) HRP20110964T1 (es)
IL (1) IL199680A0 (es)
MA (1) MA31084B1 (es)
MX (1) MX2009007180A (es)
NZ (1) NZ578144A (es)
PE (1) PE20081849A1 (es)
PL (1) PL2114931T3 (es)
PT (1) PT2114931E (es)
RS (1) RS52168B (es)
SA (1) SA08280756B1 (es)
SI (1) SI2114931T1 (es)
TW (1) TWI380818B (es)
WO (1) WO2008081205A1 (es)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
US7501426B2 (en) 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
DE102004054054A1 (de) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
NZ556017A (en) * 2004-12-24 2009-10-30 Prosidion Ltd G-protein coupled receptor (gpr116) agonists and use thereof for treating obesity and diabetes
EP2308840A1 (en) * 2005-06-30 2011-04-13 Prosidion Limited GPCR agonists
DE102005035891A1 (de) 2005-07-30 2007-02-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
WO2007128721A1 (de) 2006-05-04 2007-11-15 Boehringer Ingelheim Internationalgmbh Polymorphe
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
CL2008000018A1 (es) * 2007-01-04 2008-08-01 Prosidion Ltd Compuestos derivados de heterociclos de nitrogeno y oxigeno, agonistas de gpcr; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la obesidad, diabetes, sindrome metabolico, hiperlipidemia, toleranci
JP2010539152A (ja) 2007-09-10 2010-12-16 プロシディオン・リミテッド 代謝障害の治療のための化合物
CN101868452B (zh) 2007-10-10 2014-08-06 诺华股份有限公司 螺环吡咯烷类与其对抗hcv和hiv感染的应用
PE20140960A1 (es) 2008-04-03 2014-08-15 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
GB0812648D0 (en) * 2008-07-10 2008-08-20 Prosidion Ltd Compounds
GB0812649D0 (en) * 2008-07-10 2008-08-20 Prosidion Ltd Compounds
GB0812642D0 (en) * 2008-07-10 2008-08-20 Prosidion Ltd Compounds
CN102137844B (zh) 2008-07-11 2013-05-22 Irm责任有限公司 作为gpr119活性调控剂的化合物和组合物
KR20190016601A (ko) 2008-08-06 2019-02-18 베링거 인겔하임 인터내셔날 게엠베하 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
RU2011113823A (ru) 2008-09-10 2012-10-20 БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГмбХ (DE) Комбинированная терапия, предназначенная для лечения диабета и связанных с ним состояний
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
US8865729B2 (en) 2008-12-23 2014-10-21 Boehringer Ingelheim International Gmbh Salt forms of a xanthine compound
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
GB0904284D0 (en) 2009-03-12 2009-04-22 Prosidion Ltd Compounds for the treatment of metabolic disorders
GB0904285D0 (en) 2009-03-12 2009-04-22 Prosidion Ltd Compounds for the treatment of metabolic disorders
GB0904287D0 (en) 2009-03-12 2009-04-22 Prosidion Ltd Compounds for the treatment of metabolic disorders
JP5467151B2 (ja) 2009-06-24 2014-04-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規化合物、医薬組成物及びそれに関する方法
US8481731B2 (en) 2009-06-24 2013-07-09 Boehringer Ingelheim International Gmbh Compounds, pharmaceutical composition and methods relating thereto
WO2011019538A1 (en) 2009-08-13 2011-02-17 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
AU2010323068B2 (en) 2009-11-27 2015-09-03 Boehringer Ingelheim International Gmbh Treatment of genotyped diabetic patients with DPP-IV inhibitors such as linagliptin
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
JP2013522279A (ja) 2010-03-18 2013-06-13 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 糖尿病及び関連状態の治療で用いるgpr119作動薬とddp−iv阻害薬リナグリプチンの組合せ
GB201006167D0 (en) 2010-04-14 2010-05-26 Prosidion Ltd Compounds for the treatment of metabolic disorders
GB201006166D0 (en) 2010-04-14 2010-05-26 Prosidion Ltd Compounds for the treatment of metabolic disorders
ITMI20100770A1 (it) 2010-05-03 2011-11-04 Dipharma Francis Srl Procedimento per la preparazione di 3-(4-piridinil)-propanolo e suoi intermedi
CN102946875A (zh) 2010-05-05 2013-02-27 贝林格尔.英格海姆国际有限公司 组合疗法
TW201209054A (en) 2010-05-28 2012-03-01 Prosidion Ltd Novel compounds
ITMI20100984A1 (it) 2010-05-31 2011-12-01 Dipharma Francis Srl Procedimento per la preparazione di ossadiazoli
WO2011157827A1 (de) 2010-06-18 2011-12-22 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
MX2012014247A (es) 2010-06-24 2013-01-18 Boehringer Ingelheim Int Terapia para la diabetes.
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
AR083904A1 (es) 2010-11-18 2013-04-10 Prosidion Ltd Derivados de 1,4-pirrolidinas disustituidos y 3-il-aminas y sus usos en el tratamiento de desordenes metabolicos
GB201114389D0 (en) 2011-08-22 2011-10-05 Prosidion Ltd Novel compounds
WO2012138845A1 (en) * 2011-04-08 2012-10-11 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment
EA031618B1 (ru) 2011-06-09 2019-01-31 Ризен Фармасьютикалз Са Соединения-модуляторы gpr-119
WO2012173917A1 (en) 2011-06-16 2012-12-20 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment
MX366629B (es) 2011-07-15 2019-07-17 Boehringer Ingelheim Int Quinazolinas sustituidas, su preparación y su uso en composiciones farmacéuticas.
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2760855B1 (en) 2011-09-30 2017-03-15 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds, compositions containing such compounds as well as their use in treating type-2 diabetes
EP2771000B1 (en) 2011-10-24 2016-05-04 Merck Sharp & Dohme Corp. Substituted piperidinyl compounds useful as gpr119 agonists
EP2780337B1 (en) 2011-11-15 2017-12-20 Merck Sharp & Dohme Corp. Substituted cyclopropyl compounds useful as gpr119 agonists
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
JP6224084B2 (ja) 2012-05-14 2017-11-01 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 糸球体上皮細胞関連障害及び/又はネフローゼ症候群の治療に用いるdpp−4阻害薬としてのキサンチン誘導体
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
WO2015128453A1 (en) 2014-02-28 2015-09-03 Boehringer Ingelheim International Gmbh Medical use of a dpp-4 inhibitor
KR101726819B1 (ko) 2014-10-27 2017-04-13 동아에스티 주식회사 Gpr119 작용 활성을 갖는 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 약제학적 조성물
US10155000B2 (en) 2016-06-10 2018-12-18 Boehringer Ingelheim International Gmbh Medical use of pharmaceutical combination or composition
EP3421455B1 (en) * 2017-06-29 2019-03-27 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Improved process for the preparation of chiral 3-amino-piperidins, useful intermediates for the preparation of tofacitinib

Family Cites Families (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3576810A (en) * 1968-06-20 1971-04-27 Robins Co Inc A H 1-substituted-3-(-4)-aroylpiperidines
US5252586A (en) * 1990-09-28 1993-10-12 The Du Pont Merck Pharmaceutical Company Ether derivatives of alkyl piperidines and pyrrolidines as antipsychotic agents
FR2713225B1 (fr) 1993-12-02 1996-03-01 Sanofi Sa N-pipéridino-3-pyrazolecarboxamide substitué.
FR2692575B1 (fr) 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
DE4222565A1 (de) * 1992-07-09 1994-01-13 Hoechst Ag Meta-substituierte Sechsringaromaten zur Verwendung in Flüssigkristallmischungen
US6100042A (en) * 1993-03-31 2000-08-08 Cadus Pharmaceutical Corporation Yeast cells engineered to produce pheromone system protein surrogates, and uses therefor
DE4311967A1 (de) * 1993-04-10 1994-10-13 Hoechst Ag Smektische Flüssigkristallmischung
DE4311968A1 (de) * 1993-04-10 1994-10-20 Hoechst Ag Smektische Flüssigkristallmischung
US5338738A (en) * 1993-04-19 1994-08-16 Bristol-Myers Squibb Company Cerebral function enhancers: acyclic amide derivatives of pyrimidinylpiperidines
FR2705346B1 (fr) * 1993-05-18 1995-08-11 Union Pharma Scient Appl Nouveaux dérivés de pipéridinyl thio indole, leurs procédés de préparation, compositions pharmaceutiques les contenant, utiles notamment comme antalgiques .
ES2140543T3 (es) 1993-08-13 2000-03-01 Zeneca Ltd Derivados de tia- y oxadiazol y su uso como fungicidas o insecticidas.
EP0858457A1 (de) * 1995-10-20 1998-08-19 Dr. Karl Thomae GmbH 5-gliedrige heterocyclen, diese verbindungen enthaltende arzneimittel und deren verwendung sowie verfahren zu ihrer herstellung
EP0934941A1 (en) * 1996-08-09 1999-08-11 Eisai Co., Ltd. Benzopiperidine derivatives
GB9719496D0 (en) 1997-09-13 1997-11-19 Glaxo Group Ltd G protien chimeras
CA2343046A1 (en) 1998-09-01 2000-03-09 Basf Aktiengesellschaft Enhanced functional expression of g protein-coupled receptors
US6221660B1 (en) * 1999-02-22 2001-04-24 Synaptic Pharmaceutical Corporation DNA encoding SNORF25 receptor
AU2001292255A1 (en) * 2000-11-21 2002-06-03 Mitsubishi Chemical Corporation Process for producing 2-(4-pyridyl)ethanethiol
FR2829027A1 (fr) 2001-08-29 2003-03-07 Aventis Pharma Sa Association avec un antagoniste du recepteur cb1, les compositions pharmaceutiques les contenant et leur utilisation pour le traitement de la maladie de parkinson
FR2829028B1 (fr) 2001-08-29 2004-12-17 Aventis Pharma Sa Association d'un antagoniste du recepteur cb1 et d'un produit qui active la neurotransmission dopaminergique dans le cerveau, les compositions pharmaceutiques les contenant et leur utilisation pour le traitement de la maladie de
JP2005507875A (ja) 2001-08-31 2005-03-24 ユニバーシティ オブ コネチカット カンナビノイド受容体に作用する新規なピラゾール類似体
NZ528280A (en) 2001-09-21 2005-11-25 Solvay Pharmaceuticals B 4,5-dihydro-1H-pyrazole derivatives having potent CB1-antagonistic activity
TWI231757B (en) 2001-09-21 2005-05-01 Solvay Pharm Bv 1H-Imidazole derivatives having CB1 agonistic, CB1 partial agonistic or CB1-antagonistic activity
MXPA04002583A (es) 2001-09-21 2004-06-18 Solvay Pharm Bv Derivados de 4,5-dihidro-1h-pirazol novedosos que tienen actividad antagonistica del canabinoide (cb1).
FR2831883B1 (fr) 2001-11-08 2004-07-23 Sanofi Synthelabo Forme polymorphe du rimonabant, son procede de preparation et les compositions pharmaceutiques en contenant
SE0104332D0 (sv) 2001-12-19 2001-12-19 Astrazeneca Ab Therapeutic agents
SE0104330D0 (sv) 2001-12-19 2001-12-19 Astrazeneca Ab Therapeutic agents
FR2833842B1 (fr) 2001-12-21 2004-02-13 Aventis Pharma Sa Compositions pharmaceutiques a base de derives d'azetidine
WO2003063781A2 (en) 2002-01-29 2003-08-07 Merck & Co., Inc. Substituted imidazoles as cannabinoid receptor modulators
US20050171161A1 (en) 2002-03-06 2005-08-04 Fong Tung M. Method of treatment or prevention of obesity
NZ534757A (en) 2002-03-12 2006-07-28 Merck & Co Inc Substituted amides
AR038966A1 (es) 2002-03-18 2005-02-02 Solvay Pharm Bv Derivados de tiazol que tienen actividad antagonista, agonista o agonista parcial de cb1
JP2005528366A (ja) 2002-03-26 2005-09-22 メルク エンド カムパニー インコーポレーテッド カンナビノイド受容体モジュレータとしてのスピロ環式アミド
ES2192494B1 (es) 2002-03-27 2005-02-16 Consejo Superior De Investigaciones Cientificas Derivados de 1,2,4-triazol con propiedades cannabinoides.
US7271266B2 (en) 2002-03-28 2007-09-18 Merck & Co., Inc. Substituted 2,3-diphenyl pyridines
CA2480856A1 (en) 2002-04-05 2003-10-23 Merck & Co., Inc. Substituted aryl amides
FR2838439B1 (fr) 2002-04-11 2005-05-20 Sanofi Synthelabo Derives de terphenyle, leur preparation, les compositions pharmaceutqiues en contenant
FR2838438A1 (fr) 2002-04-11 2003-10-17 Sanofi Synthelabo Derives de diphenylpyridine,leur preparation, les compositions pharmaceutiques en contenant
US7667053B2 (en) 2002-04-12 2010-02-23 Merck & Co., Inc. Bicyclic amides
US6825209B2 (en) 2002-04-15 2004-11-30 Research Triangle Institute Compounds having unique CB1 receptor binding selectivity and methods for their production and use
CN100486973C (zh) 2002-07-29 2009-05-13 霍夫曼-拉罗奇有限公司 新苯并间二氧杂环戊烯类
ATE375349T1 (de) 2002-08-02 2007-10-15 Merck & Co Inc Substituierte furo(2,3-b)pyridin derivate
AU2003296895A1 (en) 2002-08-20 2004-05-04 The Regents Of The University Of California Combination therapy for controlling appetites
US7319110B2 (en) 2002-09-19 2008-01-15 Solvay Pharmaceuticals B.V. 1H-1,2,4-triazole-3-carboxamide derivatives having cannabinoid-CB1 receptor agonistic, partial agonistic, inverse agonistic or antagonistic activity
EP1546115A4 (en) 2002-09-27 2010-08-04 Merck Sharp & Dohme SUBSTITUTED PYRIMIDINES
MXPA05004115A (es) 2002-10-18 2005-06-22 Pfizer Prod Inc Ligandos del receptor cannabionoide y usos de los mismos.
US7129239B2 (en) 2002-10-28 2006-10-31 Pfizer Inc. Purine compounds and uses thereof
US7247628B2 (en) 2002-12-12 2007-07-24 Pfizer, Inc. Cannabinoid receptor ligands and uses thereof
CA2510785C (en) 2002-12-19 2013-04-09 Merck & Co., Inc. Substituted amides
GB0230087D0 (en) 2002-12-24 2003-01-29 Astrazeneca Ab Therapeutic agents
MXPA05007115A (es) 2003-01-02 2005-11-16 Hoffmann La Roche Nuevos agonistas inversos del receptor cb 1.
EP1583742B1 (en) 2003-01-02 2009-12-02 F. Hoffmann-La Roche Ag Cb 1 receptour inverse agonists
US7329658B2 (en) 2003-02-06 2008-02-12 Pfizer Inc Cannabinoid receptor ligands and uses thereof
KR20050100686A (ko) 2003-02-13 2005-10-19 사노피-아벤티스 도이칠란트 게엠베하 질소-치환된헥사하이드로피라지노[1,2-a]피리미딘-4,7-디온 유도체,이의 제조방법 및 의약으로서의 이의 용도
CA2515735A1 (en) 2003-02-13 2004-08-26 Aventis Pharma Deutschland Gmbh Substituted hexahydropyrazino(1,2-a)pyrimidin-4,7-dion derivatives, method for the production and use thereof as medicaments
US20040167188A1 (en) * 2003-02-14 2004-08-26 Zhili Xin Protein-tyrosine phosphatase inhibitors and uses thereof
US7169797B2 (en) * 2003-02-14 2007-01-30 Abbott Laboratories Protein-tyrosine phosphatase inhibitors and uses thereof
WO2004078261A1 (en) 2003-03-07 2004-09-16 The University Court Of The University Of Aberdeen Cannabinoid receptor inverse agonists and neutral antagonists as therapeutic agents for the treatment of bone disorders
US7232823B2 (en) 2003-06-09 2007-06-19 Pfizer, Inc. Cannabinoid receptor ligands and uses thereof
AR045496A1 (es) * 2003-08-29 2005-11-02 Schering Corp Analolgos de benzimidazolpiperidinas 2- substiyuidas como antagonistas de los receptores de la hormona que concentra melanina selectivos para el tratamiento de la obesidad y trastornos relacionados
JP4958560B2 (ja) 2003-12-24 2012-06-20 プロシディオン・リミテッド Gpcr受容体作動薬としてのヘテロ環誘導体
WO2006067532A1 (en) 2004-12-24 2006-06-29 Prosidion Ltd G-protein coupled receptor agonists
NZ556017A (en) * 2004-12-24 2009-10-30 Prosidion Ltd G-protein coupled receptor (gpr116) agonists and use thereof for treating obesity and diabetes
GB0428514D0 (en) 2004-12-31 2005-02-09 Prosidion Ltd Compounds
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
EP1907383A1 (en) 2005-06-30 2008-04-09 Prosidion Limited Gpcr agonists
US20090221644A1 (en) 2005-06-30 2009-09-03 Stuart Edward Bradley Gpcr Agonists
EP2308840A1 (en) * 2005-06-30 2011-04-13 Prosidion Limited GPCR agonists
JP2008545010A (ja) 2005-06-30 2008-12-11 プロシディオン・リミテッド Gタンパク質共役受容体アゴニスト
EP2013201B1 (en) * 2006-04-06 2012-07-25 Prosidion Limited Heterocyclic gpcr agonists
KR20090097184A (ko) * 2006-12-06 2009-09-15 스미스클라인 비참 코포레이션 비시클릭 화합물 및 항당뇨병제로서의 용도
CL2008000018A1 (es) * 2007-01-04 2008-08-01 Prosidion Ltd Compuestos derivados de heterociclos de nitrogeno y oxigeno, agonistas de gpcr; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la obesidad, diabetes, sindrome metabolico, hiperlipidemia, toleranci
EP2114936A1 (en) * 2007-01-04 2009-11-11 Prosidion Limited Piperidine gpcr agonists
EP2114933B1 (en) * 2007-01-04 2011-09-07 Prosidion Ltd Piperidine gpcr agonists

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EA015805B9 (ru) 2012-03-30
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KR20090104092A (ko) 2009-10-05
HRP20110964T1 (hr) 2012-01-31
SI2114931T1 (sl) 2012-02-29
PT2114931E (pt) 2012-01-12
RS52168B (en) 2012-08-31
ES2376015T3 (es) 2012-03-08
CA2674093A1 (en) 2008-07-10
EA200900796A1 (ru) 2010-02-26
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BRPI0806468A2 (pt) 2011-09-27
IL199680A0 (en) 2010-04-15
EP2114931B1 (en) 2011-11-02
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