JP2007523139A5 - - Google Patents
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- Publication number
- JP2007523139A5 JP2007523139A5 JP2006553649A JP2006553649A JP2007523139A5 JP 2007523139 A5 JP2007523139 A5 JP 2007523139A5 JP 2006553649 A JP2006553649 A JP 2006553649A JP 2006553649 A JP2006553649 A JP 2006553649A JP 2007523139 A5 JP2007523139 A5 JP 2007523139A5
- Authority
- JP
- Japan
- Prior art keywords
- base
- formula
- group
- substituted
- fluoro
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 239000002168 alkylating agent Substances 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000012442 inert solvent Substances 0.000 claims 1
Claims (1)
- 式Ｉの化合物［式中、Ｒ１はａ）１以上のフルオロによって置換されたＣ１〜３アルコキシ基または１以上のフルオロによって置換されていてもよいＣ４〜６アルコキシ基、またはｂ）式フェニル（ＣＨ２）ｐＯ−の基（式中、ｐは１、２または３であり、そしてフェニル環はＺによって表される１、２または３個の基によって置換されていてもよい）、またはｃ）Ｒ５Ｓ（Ｏ）２Ｏ基を表す］の製造のための方法であって、式ＩＩＩの化合物：
ａ）不活性溶媒中、塩基の存在下、−２５℃〜１５０℃の範囲の温度で、式Ｒ９Ｘのアルキル化剤（式中、Ｒ９は１以上のフルオロによって置換されたＣ１〜３アルキル基または１以上のフルオロによって置換されていてもよいＣ４〜６アルキル基を表し、そしてＸは脱離基を表す）；
ｂ）不活性溶媒中、塩基の存在下、−２５℃〜１５０℃の範囲の温度で、式Ｒ９Ｘのアルキル化剤（式中、Ｒ９は式フェニル（ＣＨ２）ｐＯ−の基を表し、ここでｐは１、２または３であり、フェニル環はＺによって表される１、２または３個の基によって置換されていてもよく、そしてＸは脱離基を表す）；または
ｃ）不活性溶媒中、塩基の存在下、−２５℃〜１５０℃の範囲の温度で、式Ｒ５Ｓ（Ｏ）２Ｌのスルホン化剤（式中、Ｒ５は先に定義した通りであり、Ｌは脱離基を表す）；のいずれかとそれぞれ反応させることを含む前記方法。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0403779A GB0403779D0 (en) | 2004-02-20 | 2004-02-20 | Therapeutic agents |
| GB0420780A GB0420780D0 (en) | 2004-09-18 | 2004-09-18 | Therapeutic agents |
| PCT/GB2005/000534 WO2005080343A2 (en) | 2004-02-20 | 2005-02-16 | 3-substituted 1,5-diphenylpyrazole derivatives useful as cb1 modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007523139A JP2007523139A (ja) | 2007-08-16 |
| JP2007523139A5 true JP2007523139A5 (ja) | 2008-04-03 |
| JP4208925B2 JP4208925B2 (ja) | 2009-01-14 |
Family
ID=34889139
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006553649A Expired - Fee Related JP4208925B2 (ja) | 2004-02-20 | 2005-02-16 | 治療薬 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20090149463A1 (ja) |
| EP (1) | EP1718617B1 (ja) |
| JP (1) | JP4208925B2 (ja) |
| KR (1) | KR20060131906A (ja) |
| AR (1) | AR047683A1 (ja) |
| AT (1) | ATE440085T1 (ja) |
| AU (1) | AU2005214130B2 (ja) |
| BR (1) | BRPI0507786A (ja) |
| CA (1) | CA2555331C (ja) |
| DE (1) | DE602005016082D1 (ja) |
| ES (1) | ES2329915T3 (ja) |
| HK (1) | HK1095329A1 (ja) |
| IL (1) | IL177218A0 (ja) |
| NO (1) | NO20063787L (ja) |
| RU (1) | RU2375349C2 (ja) |
| TW (1) | TW200531689A (ja) |
| UY (1) | UY28752A1 (ja) |
| WO (1) | WO2005080343A2 (ja) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008525404A (ja) * | 2004-12-23 | 2008-07-17 | アストラゼネカ アクチボラグ | 治療剤 |
| EP1743892A1 (en) * | 2005-07-15 | 2007-01-17 | Laboratorios del Dr. Esteve S.A. | Substituted pyrazoline compounds, their preparation and use as medicaments |
| GB0514738D0 (en) * | 2005-07-19 | 2005-08-24 | Astrazeneca Ab | Therapeutic agents |
| GB0516661D0 (en) * | 2005-08-13 | 2005-09-21 | Astrazeneca Ab | Therapeutic agents |
| AR056560A1 (es) | 2005-10-06 | 2007-10-10 | Astrazeneca Ab | Pirrolopiridinonas como moduladores cb1 |
| JP5069894B2 (ja) * | 2005-10-21 | 2012-11-07 | 田辺三菱製薬株式会社 | ピラゾール化合物 |
| US7872006B2 (en) | 2005-10-21 | 2011-01-18 | Mitsubishi Tanabe Pharma Corporation | Pyrazole compounds having cannabinoid receptor (CB1) antagonizing activity |
| CN101472897A (zh) * | 2006-06-20 | 2009-07-01 | 阿斯利康(瑞典)有限公司 | 治疗剂 |
| WO2007148061A1 (en) * | 2006-06-20 | 2007-12-27 | Astrazeneca Ab | Therapeutic agents |
| AU2007283113A1 (en) | 2006-08-08 | 2008-02-14 | Sanofi-Aventis | Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, processes for preparing them, medicaments comprising these compounds, and their use |
| AU2007336061B2 (en) * | 2006-12-18 | 2013-06-27 | 7Tm Pharma A/S | CB1 receptor modulators |
| US11241420B2 (en) | 2007-04-11 | 2022-02-08 | Omeros Corporation | Compositions and methods for prophylaxis and treatment of addictions |
| US20160331729A9 (en) | 2007-04-11 | 2016-11-17 | Omeros Corporation | Compositions and methods for prophylaxis and treatment of addictions |
| CN105250285B (zh) | 2007-04-11 | 2019-09-06 | 奥默罗斯公司 | 预防和治疗成瘾的组合物和方法 |
| EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| DE102008015033A1 (de) | 2008-03-17 | 2009-09-24 | Aicuris Gmbh & Co. Kg | Substituierte (Pyrazolyl-carbonyl)imidazolidinone und ihre Verwendung |
| DE102008015032A1 (de) | 2008-03-17 | 2009-09-24 | Aicuris Gmbh & Co. Kg | Substituierte Pyrazolamide und ihre Verwendung |
| UY31968A (es) | 2008-07-09 | 2010-01-29 | Sanofi Aventis | Nuevos derivados heterocíclicos, sus procesos para su preparación, y sus usos terapéuticos |
| GB0815134D0 (en) * | 2008-08-19 | 2008-09-24 | Univ Aberdeen | Therapeutic compounds and their use |
| 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 |
| DE102008062863A1 (de) | 2008-12-17 | 2010-06-24 | Aicuris Gmbh & Co. Kg | Substituierte (Thiophenyl-carbonyl)imidazolidinone und ihre Verwendung |
| DE102008062878A1 (de) | 2008-12-17 | 2010-06-24 | Aicuris Gmbh & Co. Kg | Substituierte Furancarboxamide und ihre Verwendung |
| DE102009036604A1 (de) | 2009-07-30 | 2011-02-03 | Aicuris Gmbh & Co. Kg | Substituierte Bis-Arylpyrazolamide mit terminaler primärer Amidfunktionalisierung und ihre Verwendung |
| CA2771278A1 (en) | 2009-08-26 | 2011-03-03 | Sanofi | Novel crystalline heteroaromatic fluoroglycoside hydrates, pharmaceuticals comprising these compounds and their use |
| EP2582709B1 (de) | 2010-06-18 | 2018-01-24 | Sanofi | Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen |
| 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 |
| WO2012120053A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| US8809325B2 (en) | 2011-03-08 | 2014-08-19 | Sanofi | Benzyl-oxathiazine derivatives substituted with adamantane and noradamantane, medicaments containing said compounds and use thereof |
| WO2012120058A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| US8809324B2 (en) | 2011-03-08 | 2014-08-19 | Sanofi | Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the use thereof |
| US8828994B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
| 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 |
| 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 |
| WO2012120057A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| CN102358735B (zh) * | 2011-08-23 | 2013-09-04 | 范如霖 | 低毒性的多头分导药，带羟基或取代羟基的含氮芳环cb1受体抑制剂及其制药用途 |
| DE102011055815A1 (de) | 2011-11-29 | 2013-05-29 | Aicuris Gmbh & Co. Kg | Carboxamid-substituierte Heteroaryl-Pyrazole und ihre Verwendung |
| DE102012016908A1 (de) | 2012-08-17 | 2014-02-20 | Aicuris Gmbh & Co. Kg | Tris-(Hetero)Aryl-Pyrazole und ihre Verwendung |
| CN113166004A (zh) | 2018-12-04 | 2021-07-23 | 巴斯夫欧洲公司 | 制备5-溴-1,3-二氯-2-氟苯的方法 |
| CN113816892A (zh) * | 2021-08-27 | 2021-12-21 | 安徽鼎旺医药有限公司 | 一种醋酸巴多昔芬的合成方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2665898B1 (fr) * | 1990-08-20 | 1994-03-11 | Sanofi | Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| 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. |
| FR2732967B1 (fr) * | 1995-04-11 | 1997-07-04 | Sanofi Sa | 1-phenylpyrazole-3-carboxamides substitues, actifs sur la neurotensine, leur preparation, les compositions pharmaceutiques en contenant |
| FR2789079B3 (fr) * | 1999-02-01 | 2001-03-02 | Sanofi Synthelabo | Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant |
| WO2003020217A2 (en) * | 2001-08-31 | 2003-03-13 | University Of Connecticut | Novel pyrazole analogs acting on cannabinoid receptors |
| 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 |
| 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 |
| MXPA05005742A (es) * | 2002-12-02 | 2005-08-16 | Astellas Pharma Inc | Derivados de pirazol utiles como inhibidores de cox-i. |
-
2005
- 2005-02-16 CA CA2555331A patent/CA2555331C/en not_active Expired - Fee Related
- 2005-02-16 US US10/588,294 patent/US20090149463A1/en not_active Abandoned
- 2005-02-16 AT AT05717730T patent/ATE440085T1/de not_active IP Right Cessation
- 2005-02-16 EP EP05717730A patent/EP1718617B1/en active Active
- 2005-02-16 ES ES05717730T patent/ES2329915T3/es active Active
- 2005-02-16 WO PCT/GB2005/000534 patent/WO2005080343A2/en active Application Filing
- 2005-02-16 AU AU2005214130A patent/AU2005214130B2/en not_active Ceased
- 2005-02-16 KR KR1020067019280A patent/KR20060131906A/ko not_active Application Discontinuation
- 2005-02-16 DE DE602005016082T patent/DE602005016082D1/de active Active
- 2005-02-16 JP JP2006553649A patent/JP4208925B2/ja not_active Expired - Fee Related
- 2005-02-16 BR BRPI0507786-9A patent/BRPI0507786A/pt not_active IP Right Cessation
- 2005-02-16 RU RU2006130683/04A patent/RU2375349C2/ru not_active IP Right Cessation
- 2005-02-17 UY UY28752A patent/UY28752A1/es unknown
- 2005-02-17 AR ARP050100566A patent/AR047683A1/es not_active Application Discontinuation
- 2005-02-18 TW TW094104925A patent/TW200531689A/zh unknown
-
2006
- 2006-08-01 IL IL177218A patent/IL177218A0/en unknown
- 2006-08-24 NO NO20063787A patent/NO20063787L/no not_active Application Discontinuation
-
2007
- 2007-03-06 HK HK07102485.1A patent/HK1095329A1/xx not_active IP Right Cessation
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