ZA200503378B - Purine compounds and uses thereof as cannabinoid receptor ligands - Google Patents
Purine compounds and uses thereof as cannabinoid receptor ligands Download PDFInfo
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- ZA200503378B ZA200503378B ZA200503378A ZA200503378A ZA200503378B ZA 200503378 B ZA200503378 B ZA 200503378B ZA 200503378 A ZA200503378 A ZA 200503378A ZA 200503378 A ZA200503378 A ZA 200503378A ZA 200503378 B ZA200503378 B ZA 200503378B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- alkylamino
- partially
- fully saturated
- aryl
- Prior art date
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| US20050026983A1 (en) * | 2003-07-30 | 2005-02-03 | Pfizer Inc | Imidazole compounds and uses thereof |
| US20050043327A1 (en) * | 2003-08-21 | 2005-02-24 | Pfizer Inc | Pharmaceutical composition for the prevention and treatment of addiction in a mammal |
| US7151097B2 (en) * | 2003-11-07 | 2006-12-19 | Pfizer Inc. | Bicyclic pyrazolyl and imidazolyl compounds and uses thereof |
| US7649002B2 (en) | 2004-02-04 | 2010-01-19 | Pfizer Inc | (3,5-dimethylpiperidin-1yl)(4-phenylpyrrolidin-3-yl)methanone derivatives as MCR4 agonists |
| US20060025448A1 (en) | 2004-07-22 | 2006-02-02 | Cadila Healthcare Limited | Hair growth stimulators |
| US20080097097A1 (en) * | 2004-10-22 | 2008-04-24 | Ragan John A | Process for Preparing Purine Compounds |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| AR051596A1 (es) * | 2004-10-26 | 2007-01-24 | Irm Llc | Compuestos heterociclicos condensados nitrogenados como inhibidores de la actividad del receptor canabinoide 1; composiciones farmaceuticas que los contienen y su empleo en la preparacion de medicamentos para el tratamiento de trastornos alimentarios |
| AU2005305675B2 (en) | 2004-11-16 | 2012-12-13 | Gw Pharma Limited | New use for cannabinoid |
| GB0425248D0 (en) * | 2004-11-16 | 2004-12-15 | Gw Pharma Ltd | New use for cannabinoid |
| PA8660701A1 (es) | 2005-02-04 | 2006-09-22 | Pfizer Prod Inc | Agonistas de pyy y sus usos |
| CA2605479A1 (en) * | 2005-04-20 | 2006-10-26 | Pfizer Products Inc. | Acylaminobicyclic heteroaromatic compounds and uses thereof |
| CA2609783A1 (en) * | 2005-05-27 | 2006-12-07 | Pfizer Products Inc. | Combination of a cannabinoid-1- receptor-antagonist and a microsomal triglyceride transfer protein inhibitor for treating obesity or mainataining weight loss |
| CA2613235A1 (en) | 2005-06-30 | 2007-01-11 | Prosidion Limited | Gpcr agonists |
| US7741317B2 (en) | 2005-10-21 | 2010-06-22 | Bristol-Myers Squibb Company | LXR modulators |
| US7888376B2 (en) | 2005-11-23 | 2011-02-15 | Bristol-Myers Squibb Company | Heterocyclic CETP inhibitors |
| ES2562428T3 (es) | 2005-12-15 | 2016-03-04 | Rigel Pharmaceuticals, Inc. | Inhibidores de cinasa y sus usos |
| EP1962863A4 (en) * | 2005-12-22 | 2010-11-24 | Conforma Therapeutics Corp | ORALLY ACTIVE PURINE INHIBITORS OF THERMAL SHOCK PROTEIN 90 |
| US20080027087A1 (en) * | 2006-02-21 | 2008-01-31 | Ampla Pharmaceuticals, Inc. | CB1 antagonists and inverse agonists |
| WO2007096763A2 (en) | 2006-02-23 | 2007-08-30 | Pfizer Limited | Melanocortin type 4 receptor agonist piperidinoylpyrrolidines |
| EP3421471B1 (en) | 2006-04-25 | 2021-05-26 | Astex Therapeutics Limited | Purine and deazapurine derivatives as pharmaceutical compounds |
| WO2008044111A1 (en) * | 2006-10-13 | 2008-04-17 | Pfizer Products Inc. | Pharmaceutical formulation tablet |
| WO2008059335A1 (en) | 2006-11-13 | 2008-05-22 | Pfizer Products Inc. | Diaryl, dipyridinyl and aryl-pyridinyl derivatives and uses thereof |
| ES2382009T3 (es) | 2006-12-01 | 2012-06-04 | Bristol-Myers Squibb Company | Derivados de N-((3-bencil)-2,2-(bis-fenil-)-propan-1-amina como inhibidores de CETP para el tratamiento de aterosclerosis y enfermedades cardiovasculares |
| GB0700122D0 (en) | 2007-01-04 | 2007-02-14 | Prosidion Ltd | GPCR agonists |
| PT2114933E (pt) | 2007-01-04 | 2011-12-20 | Prosidion Ltd | Agonistas do gpcr de piperidina |
| WO2008081208A1 (en) | 2007-01-04 | 2008-07-10 | Prosidion Limited | Piperidine gpcr agonists |
| AR064736A1 (es) | 2007-01-04 | 2009-04-22 | Prosidion Ltd | Agonistas de gpcr |
| AR064735A1 (es) | 2007-01-04 | 2009-04-22 | Prosidion Ltd | Agonistas de gpcr y composicion farmaceutica en base al compuesto |
| US20080220104A1 (en) * | 2007-03-08 | 2008-09-11 | Cappello John V | Compositions for producing satiety |
| RU2681081C2 (ru) | 2007-10-05 | 2019-03-04 | Верастэм, Инк. | Пиримидинзамещенные производные пурина, фармацевтическая композиция на их основе, способ ингибирования протеинкиназ, способ лечения или профилактики заболеваний, чувствительных к ингибированию протеинкиназ, и способ лечения пролиферативных заболеваний |
| GB0720389D0 (en) | 2007-10-18 | 2008-11-12 | Prosidion Ltd | G-Protein Coupled Receptor Agonists |
| GB0720390D0 (en) | 2007-10-18 | 2007-11-28 | Prosidion Ltd | G-Protein coupled receptor agonists |
| CN101925599A (zh) * | 2007-11-21 | 2010-12-22 | 雅培制药有限公司 | 作为烟碱性乙酰胆碱受体活性调节剂的联芳基取代的氮杂双环烷衍生物 |
| SG176464A1 (en) | 2008-05-09 | 2011-12-29 | Agency Science Tech & Res | Diagnosis and treatment of kawasaki disease |
| KR101280786B1 (ko) | 2008-08-06 | 2013-07-05 | 화이자 리미티드 | 멜라노코르틴 4 작용제로서 다이아제핀 및 다이아조칸 화합물 |
| WO2010019762A1 (en) * | 2008-08-13 | 2010-02-18 | Jenrin Discovery | Purine compounds as cannabinoid receptor blockers |
| KR101686685B1 (ko) | 2008-10-31 | 2016-12-14 | 제넨테크, 인크. | 피라졸로피리미딘 ｊａｋ 억제제 화합물 및 방법 |
| UA104010C2 (en) * | 2008-12-18 | 2013-12-25 | Эли Лилли Энд Компани | Purine compounds |
| EP2246335A1 (de) * | 2009-02-17 | 2010-11-03 | Bayer CropScience AG | Aminopyrimidinamide als Schädlingsbekämpfungsmittel |
| RU2506264C2 (ru) | 2009-04-03 | 2014-02-10 | Вэрастэм, Инк. | Пиримидин-замещенные пуриновые соединения в качестве ингибиторов киназы (или киназ) |
| UA110324C2 (en) | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| KR101414012B1 (ko) | 2009-11-13 | 2014-07-01 | 주식회사 녹십자 | 아릴피페라진-함유 퓨린 유도체 및 그의 용도 |
| MX2012010265A (es) * | 2010-03-17 | 2012-10-01 | Hoffmann La Roche | Compuestos de imidazopiridina, composiciones y metodos de uso. |
| AR080711A1 (es) | 2010-03-31 | 2012-05-02 | Lilly Co Eli | Compuesto de piperazin-purina composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para el tratamiento o prevencion del dolor |
| MX2012011164A (es) * | 2010-03-31 | 2012-11-12 | Lilly Co Eli | Compuesto de purina usados como agonistas de cb2. |
| JP2013528598A (ja) | 2010-05-11 | 2013-07-11 | ファイザー・インク | ミネラルコルチコイド受容体拮抗薬としてのモルホリン化合物 |
| WO2012035039A1 (en) | 2010-09-15 | 2012-03-22 | F. Hoffmann-La Roche Ag | Azabenzothiazole compounds, compositions and methods of use |
| EP2619198A1 (en) | 2010-09-22 | 2013-07-31 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| CN103313987A (zh) | 2010-11-19 | 2013-09-18 | 弗·哈夫曼-拉罗切有限公司 | 吡唑并吡啶化合物、吡唑并吡啶化合物以及它们作为tyk2抑制剂的用途 |
| JP2014526538A (ja) * | 2011-09-20 | 2014-10-06 | エフ．ホフマン−ラ ロシュ アーゲー | イミダゾピリジン化合物、組成物及び使用方法 |
| CZ305750B6 (cs) * | 2012-01-26 | 2016-03-02 | Ústav Organické Chemie A Biochemie Akademie Věd Čr, V.V.I. | Způsob výroby N-9 substituovaných analogů purinu |
| JP6215237B2 (ja) * | 2012-02-17 | 2017-10-18 | リサーチ・トライアングル・インスティチュート | 末梢限定的ジフェニルプリン誘導体 |
| RU2485939C1 (ru) * | 2012-06-19 | 2013-06-27 | Станислав Анатольевич Кедик | Офтальмологический препарат в виде глазных капель, содержащий дисульфирам и таурин |
| MX2015014757A (es) | 2013-05-02 | 2016-03-11 | Hoffmann La Roche | Derivados de purina como agonistas del receptor de cannabinoides 2 (cb2). |
| WO2015121136A1 (de) | 2014-02-17 | 2015-08-20 | Bayer Cropscience Ag | 2-(het)aryl-substituierte kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| CN109970743B (zh) | 2014-05-23 | 2022-03-04 | 豪夫迈·罗氏有限公司 | 为jak抑制剂的5-氯-2-二氟甲氧基苯基吡唑并嘧啶化合物 |
| EP4445956A2 (en) | 2015-01-06 | 2024-10-16 | Arena Pharmaceuticals, Inc. | Compound for use in treating conditions related to the s1p1 receptor |
| CN104581617A (zh) * | 2015-01-22 | 2015-04-29 | 小米科技有限责任公司 | 无线通信方法和智能设备 |
| WO2016209809A1 (en) | 2015-06-22 | 2016-12-29 | Arena Pharmaceuticals, Inc. | Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid(compound1) for use in sipi receptor-associated disorders |
| WO2018119076A1 (en) | 2016-12-21 | 2018-06-28 | Research Triangle Institute | Diaryl purine derivatives with improved bioavailability |
| WO2018151873A1 (en) | 2017-02-16 | 2018-08-23 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of primary biliary cholangitis |
| TW201902896A (zh) | 2017-05-22 | 2019-01-16 | 瑞士商赫孚孟拉羅股份公司 | 治療化合物及組合物及其使用方法 |
| WO2020148760A1 (en) * | 2019-01-15 | 2020-07-23 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Cb1r receptor blockers with acyclic backbones |
Family Cites Families (76)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3018378A (en) * | 1954-09-20 | 1962-01-23 | North American Aviation Inc | Radiant energy scanning system |
| US3016378A (en) | 1959-07-01 | 1962-01-09 | Thomae Gmbh Dr K | Amino-substituted purine derivatives |
| GB1165283A (en) | 1967-01-17 | 1969-09-24 | Science Union & Cie | New Purine Derivatives and processes for prepararing them |
| AT321295B (de) | 1971-11-11 | 1975-03-25 | Thomae Gmbh Dr K | Verfahren zur Herstellung von neuen Thiazolo[5,4-d]-pyrimidin-Derivaten und ihren Salzen |
| CH653021A5 (fr) | 1981-04-24 | 1985-12-13 | Delalande Sa | Derives piperidino, piperazino et homopiperazino, n-substitues par un groupe heterocyclique aromatique, leur procede de preparation et composition therapeutique les contenant. |
| JPS60260579A (ja) | 1984-01-13 | 1985-12-23 | Yoshitomi Pharmaceut Ind Ltd | プリン誘導体 |
| GB8613591D0 (en) | 1986-06-04 | 1986-07-09 | Roussel Lab Ltd | Chemical compounds |
| ES2037739T3 (es) | 1986-10-22 | 1993-07-01 | Ciba-Geigy Ag | Derivados del acido 1,5-difenilpirazol-3-carboxilico para la proteccion de plantas de cultivo. |
| AU611437B2 (en) | 1987-05-29 | 1991-06-13 | Ortho Pharmaceutical Corporation | Pharmacologically active 2- and 3-substituted (1',5'-diaryl-3-pyrazolyl)-n-hydroxypropanamides and method for synthesizing the same |
| US5057517A (en) | 1987-07-20 | 1991-10-15 | Merck & Co., Inc. | Piperazinyl derivatives of purines and isosteres thereof as hypoglycemic agents |
| PH27357A (en) | 1989-09-22 | 1993-06-21 | Fujisawa Pharmaceutical Co | Pyrazole derivatives and pharmaceutical compositions comprising the same |
| FR2665898B1 (fr) | 1990-08-20 | 1994-03-11 | Sanofi | Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| US5256398A (en) | 1990-11-08 | 1993-10-26 | Whitby Research, Inc. | Composition for determining viability of tissue |
| FR2692575B1 (fr) | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| FR2714057B1 (fr) | 1993-12-17 | 1996-03-08 | Sanofi Elf | Nouveaux dérivés du 3-pyrazolecarboxamide, procédé pour leur préparation et compositions pharmaceutiques les contenant. |
| US5596106A (en) | 1994-07-15 | 1997-01-21 | Eli Lilly And Company | Cannabinoid receptor antagonists |
| FR2741621B1 (fr) | 1995-11-23 | 1998-02-13 | Sanofi Sa | Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant |
| FR2742148B1 (fr) | 1995-12-08 | 1999-10-22 | Sanofi Sa | Nouveaux derives du pyrazole-3-carboxamide, procede pour leur preparation et compositions pharmaceutiques les contenant |
| DE69717453T2 (de) | 1996-06-06 | 2003-07-10 | Otsuka Pharmaceutical Factory, Inc. | Amid derivate |
| DE69822449T2 (de) | 1997-01-21 | 2005-01-27 | Smithkline Beecham Corp. | Neue cannabinoidrezeptor-modulatoren |
| FR2758723B1 (fr) | 1997-01-28 | 1999-04-23 | Sanofi Sa | Utilisation des antagonistes des recepteurs aux cannabinoides centraux pour la preparation de medicaments |
| AU6452098A (en) | 1997-03-07 | 1998-09-22 | Metabasis Therapeutics, Inc. | Novel purine inhibitors of fructose-1,6-bisphosphatase |
| 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 |
| JP3990061B2 (ja) * | 1998-01-05 | 2007-10-10 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | プリン誘導体および糖尿病の予防・治療剤としてのアデノシンａ２受容体拮抗剤 |
| CA2315736A1 (en) | 1998-01-05 | 1999-07-15 | Eisai Co., Ltd. | Purine compounds and adenosine a2 receptor antagonist as preventive or therapeutic for diabetes mellitus |
| KR100652994B1 (ko) | 1998-09-11 | 2006-11-30 | 아방티 파르마 소시에테 아노님 | 아제티딘 유도체, 이의 제조방법 및 이를 함유하는 약제 |
| FR2783246B1 (fr) | 1998-09-11 | 2000-11-17 | Aventis Pharma Sa | Derives d'azetidine, leur preparation et les medicaments les contenant |
| FR2789079B3 (fr) | 1999-02-01 | 2001-03-02 | Sanofi Synthelabo | Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant |
| KR100694684B1 (ko) * | 1999-07-02 | 2007-03-13 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 축합 이미다졸 화합물 및 당뇨병 치료약 |
| FR2799124B1 (fr) | 1999-10-01 | 2004-08-13 | Sanofi Synthelabo | Utilisation des antagonistes des recepteurs aux cannabinoides centraux pour la preparation de medicaments |
| CA2387892A1 (en) | 1999-10-18 | 2001-04-26 | University Of Connecticut | Pyrazole derivatives as cannabinoid receptor antagonists |
| MXPA02005101A (es) | 1999-10-18 | 2003-09-25 | Alexipharma Inc | Derivados de indol canabimimeticos. |
| FR2800375B1 (fr) | 1999-11-03 | 2004-07-23 | Sanofi Synthelabo | Derives tricycliques d'acide pyrazolecarboxylique, leur preparation, les compositions pharmaceutiques en contenant |
| FR2800372B1 (fr) | 1999-11-03 | 2001-12-07 | Sanofi Synthelabo | Derives tricycliques d'acide 1-benzylpyrazole-3- carboxylique, leur preparation, les medicaments en contenant |
| FR2804604B1 (fr) | 2000-02-09 | 2005-05-27 | Sanofi Synthelabo | Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac |
| CA2399791A1 (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 |
| US6355631B1 (en) | 2000-03-03 | 2002-03-12 | Aventis Pharma S.A. | Pharmaceutical compositions containing azetidine derivatives, novel azetidine derivatives and their preparation |
| US6566356B2 (en) | 2000-03-03 | 2003-05-20 | Aventis Pharma S.A. | Pharmaceutical compositions containing 3-aminoazetidine derivatives, novel derivatives and their preparation |
| US6479479B2 (en) | 2000-03-03 | 2002-11-12 | Aventis Pharma S.A. | Azetidine derivatives, their preparation and pharmaceutical compositions containing them |
| DZ3335A1 (fr) | 2000-03-23 | 2001-09-27 | Solvay Pharm Bv | Derives de 4,5-dihydro-1h-pyrazole ayant une activite antagoniste de cb1 |
| FR2809621B1 (fr) | 2000-05-12 | 2002-09-06 | Sanofi Synthelabo | Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles comme antidiarrheiques |
| US20020019421A1 (en) | 2000-07-05 | 2002-02-14 | Roni Biberman | Compositions and therapy for substance addiction |
| US20020091114A1 (en) | 2000-10-04 | 2002-07-11 | Odile Piot-Grosjean | Combination of a CB1 receptor antagonist and of sibutramine, the pharmaceutical compositions comprising them and their use in the treatment of obesity |
| CA2432148C (en) | 2000-12-28 | 2011-01-18 | Ono Pharmaceutical Co., Ltd. | Tri-heterocyclic compounds and a pharmaceutical comprising them as an active ingredient |
| CA2422708C (en) | 2001-03-22 | 2010-10-26 | Solvay Pharmaceuticals B.V. | 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity |
| ITMI20011483A1 (it) | 2001-07-11 | 2003-01-11 | Res & Innovation Soc Coop A R | Uso di composti come antagonisti funzionali ai recettori centrali deicannabinoidi |
| WO2003007887A2 (en) | 2001-07-20 | 2003-01-30 | Merck & Co., Inc. | Substituted imidazoles as cannabinoid receptor modulators |
| 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 |
| 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 |
| AU2002331766A1 (en) | 2001-08-31 | 2003-03-18 | University Of Connecticut | Novel pyrazole analogs acting on cannabinoid receptors |
| IL160081A0 (en) | 2001-09-21 | 2004-06-20 | Solvay Pharm Bv | Novel 4,5-dihydro-1h-pyrazole derivatives having 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 |
| MXPA03009439A (es) | 2001-09-21 | 2004-02-12 | Solvay Pharm Bv | Derivados de 4,5-dihidro-1h-pirazol que tienen una potente actividad antagonistica de cb1. |
| US6509367B1 (en) | 2001-09-22 | 2003-01-21 | Virginia Commonwealth University | Pyrazole cannabinoid agonist and antagonists |
| US7071207B2 (en) | 2001-09-24 | 2006-07-04 | Bayer Pharmaceuticals Corporation | Preparation and use of 1,5,6,7-tetrahydropyrrolo[3,2-c]pyridine derivatives for treatment of obesity |
| MXPA04002438A (es) | 2001-09-24 | 2004-06-29 | Bayer Pharmaceuticals Corp | Preparacion y uso de derivados de pirroll para el tratamiento de la obesidad. |
| AR036608A1 (es) | 2001-09-24 | 2004-09-22 | Bayer Corp | Derivados de imidazol, composiciones farmaceuticas y el uso de dichos derivados para la fabricacion de un medicamento para el tratamiento de la obesidad |
| SE0104332D0 (sv) | 2001-12-19 | 2001-12-19 | Astrazeneca Ab | Therapeutic agents |
| SE0104330D0 (sv) | 2001-12-19 | 2001-12-19 | Astrazeneca Ab | Therapeutic agents |
| US20030139386A1 (en) | 2001-12-21 | 2003-07-24 | Sophie Cote | Pharmaceutical compositions based on azetidine derivatives |
| WO2003075660A1 (en) | 2002-03-06 | 2003-09-18 | Merck & Co., Inc. | Method of treatment or prevention of obesity |
| EP1496838B1 (en) | 2002-03-12 | 2010-11-03 | Merck Sharp & Dohme Corp. | 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 |
| WO2003082190A2 (en) | 2002-03-26 | 2003-10-09 | Merck & Co., Inc. | Spirocyclic amides as cannabinoid receptor modulators |
| ES2192494B1 (es) | 2002-03-27 | 2005-02-16 | Consejo Superior De Investigaciones Cientificas | Derivados de 1,2,4-triazol con propiedades cannabinoides. |
| FR2837706A1 (fr) | 2002-03-28 | 2003-10-03 | Sanofi Synthelabo | Utilisation d'un antagoniste des recepteurs aux cannabinoides cb1 pour la preparation de medicaments utiles pour traiter les dysfonctionnements sexuels et/ou ameliorer les performances sexuelles |
| WO2003082191A2 (en) | 2002-03-28 | 2003-10-09 | Merck & Co., Inc. | Substituted 2,3-diphenyl pyridines |
| WO2003087037A1 (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 |
| CA2481313A1 (en) | 2002-04-12 | 2003-10-23 | 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 |
| ATE365740T1 (de) | 2002-05-10 | 2007-07-15 | Smithkline Beecham Corp | Substituierte pyrazolopyrimidine |
| BR0314872A (pt) | 2002-10-18 | 2005-08-02 | Pfizer Prod Inc | Ligandos do receptor canabinóide e usos dos mesmos |
| US7129239B2 (en) * | 2002-10-28 | 2006-10-31 | Pfizer Inc. | Purine compounds and uses thereof |
| US20050043327A1 (en) * | 2003-08-21 | 2005-02-24 | Pfizer Inc | Pharmaceutical composition for the prevention and treatment of addiction in a mammal |
| US20080097097A1 (en) * | 2004-10-22 | 2008-04-24 | Ragan John A | Process for Preparing Purine Compounds |
-
2003
- 2003-10-20 US US10/689,381 patent/US7129239B2/en not_active Expired - Fee Related
- 2003-10-21 NZ NZ539589A patent/NZ539589A/en not_active IP Right Cessation
- 2003-10-21 EP EP03751149A patent/EP1558615B8/en not_active Expired - Lifetime
- 2003-10-21 RS YUP-2005/0306A patent/RS20050306A/sr unknown
- 2003-10-21 CN CNB2003801022192A patent/CN100439369C/zh not_active Expired - Fee Related
- 2003-10-21 CN CNA2006101625782A patent/CN1955181A/zh active Pending
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