DE60109903T2 - Verwendung eines zentralen cannabinoid-rezeptor-antagonisten für die herstelling von arzneimitteln zur erleichterung der aufgabe des tabakverbrauchs - Google Patents
Verwendung eines zentralen cannabinoid-rezeptor-antagonisten für die herstelling von arzneimitteln zur erleichterung der aufgabe des tabakverbrauchs Download PDFInfo
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- DE60109903T2 DE60109903T2 DE60109903T DE60109903T DE60109903T2 DE 60109903 T2 DE60109903 T2 DE 60109903T2 DE 60109903 T DE60109903 T DE 60109903T DE 60109903 T DE60109903 T DE 60109903T DE 60109903 T2 DE60109903 T2 DE 60109903T2
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- nicotine
- solvates
- pharmaceutically acceptable
- acceptable salts
- methylpyrazole
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- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
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- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0001682 | 2000-02-09 | ||
| FR0001682A FR2804604B1 (fr) | 2000-02-09 | 2000-02-09 | Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac |
| PCT/FR2001/000356 WO2001058450A2 (fr) | 2000-02-09 | 2001-02-07 | Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60109903D1 DE60109903D1 (de) | 2005-05-12 |
| DE60109903T2 true DE60109903T2 (de) | 2006-02-09 |
Family
ID=8846875
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60109903T Expired - Fee Related DE60109903T2 (de) | 2000-02-09 | 2001-02-07 | Verwendung eines zentralen cannabinoid-rezeptor-antagonisten für die herstelling von arzneimitteln zur erleichterung der aufgabe des tabakverbrauchs |
Country Status (32)
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US6462237B1 (en) * | 2001-06-14 | 2002-10-08 | Usv Limited | Cyclodextrin stabilized pharmaceutical compositions of bupropion hydrochloride |
| AU2002356039A1 (en) | 2001-08-13 | 2003-03-03 | Honeywell International Inc. | Methods of conducting wafer level burn-in of electronic devices |
| JP2005533748A (ja) | 2002-03-08 | 2005-11-10 | シグナル ファーマシューティカルズ，インコーポレイテッド | 増殖性障害および癌を治療、予防、または管理するための併用療法 |
| WO2003077847A2 (en) | 2002-03-12 | 2003-09-25 | Merck & Co., Inc. | Substituted amides |
| 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 |
| JP2005531520A (ja) | 2002-03-28 | 2005-10-20 | メルク エンド カムパニー インコーポレーテッド | 置換２，３−ジフェニルピリジン類 |
| WO2003086288A2 (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 |
| ATE375349T1 (de) | 2002-08-02 | 2007-10-15 | Merck & Co Inc | Substituierte furo(2,3-b)pyridin derivate |
| CA2499497A1 (en) | 2002-09-27 | 2004-04-08 | Merck & Co., Inc. | Substituted pyrimidines |
| 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 |
| WO2004058145A2 (en) | 2002-12-19 | 2004-07-15 | Merck & Co., Inc. | Substituted amides |
| US7329658B2 (en) | 2003-02-06 | 2008-02-12 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
| US7176210B2 (en) | 2003-02-10 | 2007-02-13 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US7268133B2 (en) | 2003-04-23 | 2007-09-11 | Pfizer, Inc. Patent Department | Cannabinoid receptor ligands and uses thereof |
| US20040224962A1 (en) * | 2003-05-09 | 2004-11-11 | Pfizer Inc | Pharmaceutical composition for the treatment of obesity or to facilitate or promote weight loss |
| US20040224963A1 (en) * | 2003-05-09 | 2004-11-11 | Pfizer Inc | Pharmaceutical composition for the prevention and treatment of nicotine addiction in a mammal |
| CA2526103A1 (en) * | 2003-05-20 | 2004-12-29 | Bob M. Ii Moore | Cannabinoid derivatives, methods of making, and use thereof |
| US7232823B2 (en) | 2003-06-09 | 2007-06-19 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
| CA2543882A1 (en) * | 2003-10-30 | 2005-05-19 | Merck & Co., Inc. | Aralkyl amines as cannabinoid receptor modulators |
| MX2007000491A (es) | 2004-07-12 | 2007-03-28 | Cadila Healthcare Ltd | Nuevos compuestos heterociclicos. |
| US20060025448A1 (en) | 2004-07-22 | 2006-02-02 | Cadila Healthcare Limited | Hair growth stimulators |
| ES2435790T3 (es) | 2004-12-03 | 2013-12-23 | Intervet International B.V. | Piperazinas sustituidas como antagonistas de CB1 |
| NZ569814A (en) * | 2006-01-18 | 2011-10-28 | Schering Corp | Cannibinoid receptor modulators |
| WO2007121687A1 (en) * | 2006-04-26 | 2007-11-01 | Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China | 4-methyl-1h-diaryl pyrazole derivatives and their uses as medicament |
| CN101062919B (zh) * | 2006-04-26 | 2012-08-15 | 中国人民解放军军事医学科学院毒物药物研究所 | 4-甲基-1h-二芳基吡唑衍生物及其作为药物的用途 |
| US20070287734A1 (en) * | 2006-06-09 | 2007-12-13 | Auspex Pharmaceuticals, Inc. | Preparation and utility of substituted pyrazole compounds with cannabinoid receptor activity |
| RU2477634C2 (ru) * | 2006-06-16 | 2013-03-20 | Теракос, Инк. | Лечение психологических состояний с применением антагонистов m1-мускариновых рецепторов |
| WO2008046905A1 (en) * | 2006-10-20 | 2008-04-24 | Solvay Pharmaceuticals B.V. | Micellar nanoparticles of chemical substances |
| WO2008130616A2 (en) * | 2007-04-19 | 2008-10-30 | Schering Corporation | Diaryl morpholines as cb1 modulators |
| WO2009005671A2 (en) * | 2007-06-28 | 2009-01-08 | Schering Corporation | Substituted piperazines as cb1 antagonists |
| EP2170846A2 (en) * | 2007-06-28 | 2010-04-07 | Intervet International BV | Substituted piperazines as cb1 antagonists |
| EP2095814A1 (de) * | 2008-02-26 | 2009-09-02 | Wolfgang J. Kox | Medikamentengestützter Nikotinentzug |
| WO2010018856A1 (ja) * | 2008-08-13 | 2010-02-18 | 持田製薬株式会社 | カンナビノイド受容体関連疾患の予防／改善または治療剤 |
| RU2533224C2 (ru) * | 2010-07-21 | 2014-11-20 | Мапикс Эс.Эй.Ар.Эл. | Способ лечения зависимости от психоактивных веществ, алкоголизма и табакокурения и лекарственное средство для лечения зависимости от психоактивных веществ, алкоголизма и табакокурения |
| WO2013068371A1 (en) | 2011-11-08 | 2013-05-16 | Intervet International B.V. | Soft chewable dosage form compositions of cannabinoid receptor type 1 (cb-1) antagonists |
| WO2014181357A1 (en) * | 2013-05-09 | 2014-11-13 | Council Of Scientific & Industrial Research | Novel pyrazole derivatives with silicon incorporation |
| US20200035118A1 (en) | 2018-07-27 | 2020-01-30 | Joseph Pandolfino | Methods and products to facilitate smokers switching to a tobacco heating product or e-cigarettes |
| US10897925B2 (en) | 2018-07-27 | 2021-01-26 | Joseph Pandolfino | Articles and formulations for smoking products and vaporizers |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5780051A (en) * | 1992-04-02 | 1998-07-14 | Dynagen, Inc. | Methods and articles of manufacture for nicotine cessation and monitoring nicotine use |
| 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. |
| US5596106A (en) * | 1994-07-15 | 1997-01-21 | Eli Lilly And Company | Cannabinoid receptor antagonists |
| FR2758723B1 (fr) * | 1997-01-28 | 1999-04-23 | Sanofi Sa | Utilisation des antagonistes des recepteurs aux cannabinoides centraux pour la preparation de medicaments |
| FR2765107B1 (fr) * | 1997-06-26 | 2000-03-24 | Sanofi Sa | Utilisation d'un antagoniste specifique des recepteurs 5ht2 pour la preparation de medicaments utiles dans le traitement du syndrome d'apnee du sommeil |
| FR2789079B3 (fr) | 1999-02-01 | 2001-03-02 | Sanofi Synthelabo | Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques 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 |
-
2000
- 2000-02-09 FR FR0001682A patent/FR2804604B1/fr not_active Expired - Fee Related
-
2001
- 2001-02-07 EE EEP200200439A patent/EE04836B1/xx not_active IP Right Cessation
- 2001-02-07 RU RU2002118309/15A patent/RU2257207C2/ru not_active IP Right Cessation
- 2001-02-07 IL IL15071001A patent/IL150710A0/xx not_active IP Right Cessation
- 2001-02-07 US US10/203,077 patent/US6930122B2/en not_active Expired - Fee Related
- 2001-02-07 PT PT01907722T patent/PT1257275E/pt unknown
- 2001-02-07 DE DE60109903T patent/DE60109903T2/de not_active Expired - Fee Related
- 2001-02-07 ES ES01907722T patent/ES2240416T3/es not_active Expired - Lifetime
- 2001-02-07 CZ CZ20022698A patent/CZ296685B6/cs not_active IP Right Cessation
- 2001-02-07 CN CNB018047130A patent/CN1250220C/zh not_active Expired - Fee Related
- 2001-02-07 AT AT01907722T patent/ATE292467T1/de not_active IP Right Cessation
- 2001-02-07 CA CA002397262A patent/CA2397262C/en not_active Expired - Fee Related
- 2001-02-07 HU HU0300237A patent/HU225328B1/hu not_active IP Right Cessation
- 2001-02-07 DK DK01907722T patent/DK1257275T3/da active
- 2001-02-07 WO PCT/FR2001/000356 patent/WO2001058450A2/fr not_active Ceased
- 2001-02-07 JP JP2001557560A patent/JP2003522145A/ja not_active Ceased
- 2001-02-07 PL PL358221A patent/PL201685B1/pl not_active IP Right Cessation
- 2001-02-07 BR BR0108126-8A patent/BR0108126A/pt not_active Application Discontinuation
- 2001-02-07 BG BG110386A patent/BG110386A/en unknown
- 2001-02-07 MX MXPA02007766A patent/MXPA02007766A/es active IP Right Grant
- 2001-02-07 EP EP01907722A patent/EP1257275B1/fr not_active Expired - Lifetime
- 2001-02-07 SK SK1129-2002A patent/SK284952B6/sk not_active IP Right Cessation
- 2001-02-07 AU AU35620/01A patent/AU781827B2/en not_active Ceased
- 2001-02-07 NZ NZ519924A patent/NZ519924A/en unknown
- 2001-02-07 SI SI200130365T patent/SI1257275T1/xx unknown
- 2001-02-07 RS YUP-590/02A patent/RS50404B/sr unknown
- 2001-02-09 AR ARP010100587A patent/AR028505A1/es unknown
- 2001-02-19 TW TW090102783A patent/TWI243677B/zh active
- 2001-07-02 UA UA2002075476A patent/UA72783C2/uk unknown
-
2002
- 2002-06-28 IS IS6450A patent/IS6450A/is unknown
- 2002-07-03 ZA ZA200205317A patent/ZA200205317B/en unknown
- 2002-07-23 BG BG106946A patent/BG65856B1/bg unknown
- 2002-08-08 NO NO20023765A patent/NO324521B1/no not_active IP Right Cessation
-
2005
- 2005-04-25 US US11/113,864 patent/US20050187253A1/en not_active Abandoned
-
2009
- 2009-09-18 JP JP2009217269A patent/JP2010018622A/ja not_active Withdrawn
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