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 |
|---|---|---|---|---|
| US20080146614A1 (en) * | 2004-12-23 | 2008-06-19 | Leifeng Cheng | Therapeutic Agents |
| 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 |
| JP2009541283A (ja) * | 2006-06-20 | 2009-11-26 | アストラゼネカ アクチボラグ | 治療薬 |
| CN101472896A (zh) * | 2006-06-20 | 2009-07-01 | 阿斯利康(瑞典)有限公司 | 治疗药剂 |
| RU2009108280A (ru) | 2006-08-08 | 2010-09-20 | Санофи-Авентис (Fr) | Ариламиноарилалкилзамещенные имидазолидин-2,4-дионы, способы их получения, содержащие эти соединения лекарственные средства и их применение |
| CA2673359A1 (en) * | 2006-12-18 | 2008-06-26 | 7Tm Pharma A/S | Cb1 receptor modulators |
| ES2586433T3 (es) | 2007-04-11 | 2016-10-14 | Omeros Corporation | Composiciones y métodos para la profilaxis y el tratamiento de adicciones |
| US20160331729A9 (en) | 2007-04-11 | 2016-11-17 | Omeros Corporation | Compositions and methods for prophylaxis and treatment of addictions |
| US11241420B2 (en) | 2007-04-11 | 2022-02-08 | Omeros Corporation | Compositions and methods for prophylaxis and treatment of addictions |
| 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 |
| WO2010003624A2 (en) | 2008-07-09 | 2010-01-14 | Sanofi-Aventis | Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof |
| 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 |
| DE102008062878A1 (de) | 2008-12-17 | 2010-06-24 | Aicuris Gmbh & Co. Kg | Substituierte Furancarboxamide und ihre Verwendung |
| DE102008062863A1 (de) | 2008-12-17 | 2010-06-24 | Aicuris Gmbh & Co. Kg | Substituierte (Thiophenyl-carbonyl)imidazolidinone 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 |
| WO2011023754A1 (en) | 2009-08-26 | 2011-03-03 | Sanofi-Aventis | 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 |
| WO2012120051A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Mit adamantan- oder noradamantan substituierte benzyl-oxathiazinderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2683701B1 (de) | 2011-03-08 | 2014-12-24 | Sanofi | Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| EP2683702B1 (de) | 2011-03-08 | 2014-12-24 | Sanofi | Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2012120054A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
| US8895547B2 (en) | 2011-03-08 | 2014-11-25 | Sanofi | Substituted phenyl-oxathiazine derivatives, method for producing them, drugs containing said compounds and the 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 |
| US8901114B2 (en) | 2011-03-08 | 2014-12-02 | Sanofi | Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and 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 |
| EP2683704B1 (de) | 2011-03-08 | 2014-12-17 | Sanofi | Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes 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 |
| WO2020114813A1 (en) * | 2018-12-04 | 2020-06-11 | Basf Se | Process for preparation of 5-bromo-1,3-dichloro-2-fluoro-benzene |
| 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 |
| JP2004502642A (ja) * | 2000-02-11 | 2004-01-29 | ブリストル−マイヤーズ スクイブ カンパニー | カンナビノイドレセプターモジュレーター、それらの製造方法、および呼吸系および非呼吸系疾患の処置のためのカンナビノイドレセプターモジュレーターの使用 |
| AU2002331766A1 (en) * | 2001-08-31 | 2003-03-18 | University Of Connecticut | Novel pyrazole analogs acting on cannabinoid receptors |
| 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 |
| ES2379076T3 (es) * | 2002-12-02 | 2012-04-20 | Astellas Pharma Inc. | Derivados de pirazol útiles como inhibidores de COX-I |
-
2005
- 2005-02-16 AT AT05717730T patent/ATE440085T1/de not_active IP Right Cessation
- 2005-02-16 BR BRPI0507786-9A patent/BRPI0507786A/pt not_active IP Right Cessation
- 2005-02-16 AU AU2005214130A patent/AU2005214130B2/en not_active Ceased
- 2005-02-16 DE DE602005016082T patent/DE602005016082D1/de active Active
- 2005-02-16 WO PCT/GB2005/000534 patent/WO2005080343A2/en active Application Filing
- 2005-02-16 JP JP2006553649A patent/JP4208925B2/ja not_active Expired - Fee Related
- 2005-02-16 KR KR1020067019280A patent/KR20060131906A/ko not_active Application Discontinuation
- 2005-02-16 US US10/588,294 patent/US20090149463A1/en not_active Abandoned
- 2005-02-16 RU RU2006130683/04A patent/RU2375349C2/ru not_active IP Right Cessation
- 2005-02-16 ES ES05717730T patent/ES2329915T3/es active Active
- 2005-02-16 EP EP05717730A patent/EP1718617B1/en active Active
- 2005-02-16 CA CA2555331A patent/CA2555331C/en not_active Expired - Fee Related
- 2005-02-17 AR ARP050100566A patent/AR047683A1/es not_active Application Discontinuation
- 2005-02-17 UY UY28752A patent/UY28752A1/es unknown
- 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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