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1. 发明申请

US20050192332A1 Pyrazolecarboxylic acid tricyclic derivatives, preparation and pharmaceutical compositions containing same 有权
公开(公告)号：US20050192332A1
公开(公告)日：2005-09-01
申请号：US11119074
申请日：2005-04-29
申请人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi
发明人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi
IPC分类号： A61K31/4162 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/55 , A61P1/00 , A61P1/12 , A61P3/04 , A61P3/10 , A61P13/00 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07D231/54 , C07D231/56 , C07D401/12 , C07D495/04 , C07D498/02
CPC分类号： C07D231/56 , C07D231/54 , C07D495/04
摘要： The subject of the invention is tricyclic derivatives of pyrazolecarboxylic acid of formula: in which R1 represents a C3-C15 carboxyl radical or an NR2R3 group. The invention also relates to the method for preparing the compounds of formula (I), pharmaceutical compositions containing them. The compounds of formula (I) are active on cannabinoid CB1 receptors.

2. 发明授权

US07297710B1 Derivatives of N-[(1,5-diphenyl-1H-pyrazol-3-yl)methyl]sulfonamide, their preparation and their application in therapeutics 失效
标题翻译： N - [（1,5-二苯基-1H-吡唑-3-基）甲基]磺酰胺的衍生物及其制备及其在治疗中的应用
公开(公告)号：US07297710B1
公开(公告)日：2007-11-20
申请号：US11457014
申请日：2006-07-12
申请人： Francis Barth , Christian Congy , Serge Martinez , Philippe Pointeau , Murielle Rinaldi-Carmona
发明人： Francis Barth , Christian Congy , Serge Martinez , Philippe Pointeau , Murielle Rinaldi-Carmona
IPC分类号： A61K31/415 , C07D231/10
CPC分类号： C07D213/12 , C07D213/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to compounds corresponding to the formula (I): In which R1, R2, R3, R4 and R5 are as described herein. The invention also relates to the method of preparation of said compounds and their application in therapeutics.
摘要翻译：本发明涉及对应于式（I）的化合物：其中R 1，R 2，R 3，R 3， 4和R 5 5如本文所述。本发明还涉及所述化合物的制备方法及其在治疗中的应用。

3. 发明申请

US20060135776A1 4-Cyanopyrazole-3-carboxamide derivatives, preparation, and application thereof 有权
标题翻译： 4-氰基吡唑-3-甲酰胺衍生物，其制备及应用
公开(公告)号：US20060135776A1
公开(公告)日：2006-06-22
申请号：US11315774
申请日：2005-12-22
申请人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi-Carmona
发明人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi-Carmona
IPC分类号： A61K31/454 , A61K31/4152 , C07D403/02 , C07D231/14 , C07D231/54
CPC分类号： C07D401/12 , C07D231/14
摘要： The invention relates to 4-cyanopyrazole-3-carboxamide derivatives of formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8 are as described herein. Also disclosed and claimed are the method of preparation and therapeutic application of compound of formula (I).
摘要翻译：本发明涉及式（I）的4-氰基吡唑-3-甲酰胺衍生物：其中R 1，R 2，R 3， R 4，R 5，R 6，R 7，R 8是如本文所述。还公开并要求保护的是式（I）化合物的制备和治疗应用的方法。

4. 发明授权

US07521471B2 4-cyanopyrazole-3-carboxamide derivatives, preparation and application thereof 有权
标题翻译： 4-氰基吡唑-3-甲酰胺衍生物，的制备和应用
公开(公告)号：US07521471B2
公开(公告)日：2009-04-21
申请号：US11832146
申请日：2007-08-01
申请人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi-Carmona
发明人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi-Carmona
IPC分类号： A61K31/415 , C07D231/10
CPC分类号： C07D401/12 , C07D231/14
摘要： The invention relates to 4-cyanopyrazole-3-carboxamide derivatives of formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8 are as described herein. Also disclosed and claimed are the method of preparation and therapeutic application of compound of formula (I).
摘要翻译：本发明涉及式（I）的4-氰基吡唑-3-甲酰胺衍生物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8如本文所述。还公开并要求保护的是式（I）化合物的制备和治疗应用的方法。

5. 发明申请

US20080070962A1 DERIVATIVES OF N-[(1,5-DIPHENYL-1H-PYRAZOL-3-YL)METHYL] SULFONAMIDE, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS 失效
标题翻译： N - [（1,5-二苯基-1H-吡唑-3-基）甲基]磺酰胺的衍生物及其在治疗中的应用
公开(公告)号：US20080070962A1
公开(公告)日：2008-03-20
申请号：US11859010
申请日：2007-09-21
申请人： Francis Barth , Christian Congy , Serge Martinez , Philippe Pointeau , Murielle Rinaldi-Carmona
发明人： Francis Barth , Christian Congy , Serge Martinez , Philippe Pointeau , Murielle Rinaldi-Carmona
IPC分类号： A61K31/40 , A61K31/41 , A61K31/415 , A61P43/00
CPC分类号： C07D213/12 , C07D213/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to compounds corresponding to the formula (I): In which R1, R2, R3, R4 and R5 are as described herein. The invention also relates to the method of preparation of said compounds and their application in therapeutics.
摘要翻译：本发明涉及对应于式（I）的化合物：其中R 1，R 2，R 3，R 3， 4和R 5 5如本文所述。本发明还涉及所述化合物的制备方法及其在治疗中的应用。

6. 发明授权

US06906080B1 Pyrazolecarboxylic acid tricyclic derivatives, preparation and pharmaceutical compositions containing same 有权
标题翻译：吡唑羧酸三环衍生物，制剂和含有它们的药物组合物
公开(公告)号：US06906080B1
公开(公告)日：2005-06-14
申请号：US10111765
申请日：2000-11-02
申请人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi
发明人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi
IPC分类号： A61K31/4162 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/55 , A61P1/00 , A61P1/12 , A61P3/04 , A61P3/10 , A61P13/00 , A61P15/00 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07D231/54 , C07D231/56 , C07D401/12 , C07D495/04
CPC分类号： C07D231/56 , C07D231/54 , C07D495/04
摘要： The subject of the invention is tricyclic derivatives of pyrazolecarboxylic acid of formula: in which R1 represents a C3-C15 carboxyl radical or an NR2R3 group. The invention also relates to the method for preparing the compounds of formula (I), pharmaceutical compositions containing them. The compounds of formula (I) are active on cannabinoid CB1 receptors.
摘要翻译：本发明的主题是下式的吡唑羧酸的三环衍生物：其中R 1代表C 3 -C 15羧基或 NR 2 R 3 N 3基团。本发明还涉及制备式（I）化合物的方法，含有它们的药物组合物。式（I）化合物在大麻素CB 1受体上是有活性的。

7. 发明授权

US5624941A Pyrazole derivatives, method of preparing them and pharmaceutical compositions in which they are present 失效
标题翻译：吡唑衍生物，其制备方法和它们存在的药物组合物
公开(公告)号：US5624941A
公开(公告)日：1997-04-29
申请号：US348881
申请日：1994-11-29
申请人： Francis Barth , Pierre Casellas , Christian Congy , Serge Martinez , Murielle Rinaldi , Gilles Anne-Archard
发明人： Francis Barth , Pierre Casellas , Christian Congy , Serge Martinez , Murielle Rinaldi , Gilles Anne-Archard
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/4402 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/5375 , A61K31/553 , A61P1/08 , A61P9/00 , A61P9/10 , A61P11/06 , A61P11/08 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/28 , A61P27/02 , A61P27/06 , A61P37/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D20060101 , C07D231/12 , C07D231/14 , C07D231/38 , C07D231/40 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D493/08
CPC分类号： C07D231/12 , C07D231/14 , C07D231/40 , C07D401/12 , C07D403/12 , C07D405/12 , C07D493/08
摘要： The present invention relates to compounds of the formula: ##STR1## These compounds are useful in pharmaceuticals in which cannabis is known to be involved.
摘要翻译：本发明涉及下式的化合物：（I）这些化合物可用于已知涉及大麻的药物中。

8. 发明授权

US08088797B2 Substituted N-(4-cyano-1H-pyrazol-3-yl)methylamine derivatives, preparation thereof and therapeutic use thereof 失效
标题翻译：取代的N-（4-氰基-1H-吡唑-3-基）甲胺衍生物，其制备及其治疗用途
公开(公告)号：US08088797B2
公开(公告)日：2012-01-03
申请号：US12490735
申请日：2009-06-24
申请人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi-Carmona , Martine Vernhet
发明人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi-Carmona , Martine Vernhet
IPC分类号： A01N43/40
CPC分类号： C07D231/14 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to compounds corresponding to formula (I): Wherein X, R1, R2, R3 and R4 are as defined herein. The invention further relates to preparation and therapeutic use of these compounds.
摘要翻译：本发明涉及对应于式（I）的化合物：其中X，R 1，R 2，R 3和R 4如本文所定义。本发明还涉及这些化合物的制备和治疗用途。

9. 发明申请

US20100041709A1 SUBSTITUTED N-(4-CYANO-1H-PYRAZOL-3-YL)METHYLAMINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 失效
标题翻译：取代的N-（4-氰基-1H-吡唑-3-基）甲基胺衍生物，其制备方法及其治疗方法
公开(公告)号：US20100041709A1
公开(公告)日：2010-02-18
申请号：US12490735
申请日：2009-06-24
申请人： Francis BARTH , Christian Congy , Serge Martinez , Murielle Rinaldi-Carmona , Martine Vernhet
发明人： Francis BARTH , Christian Congy , Serge Martinez , Murielle Rinaldi-Carmona , Martine Vernhet
IPC分类号： A61K31/415 , C07D231/14 , C07D401/12 , C07D403/12 , A61K31/4439 , A61K31/4155 , A61P3/00 , A61P3/04 , A61P3/10 , A61P25/00 , A61P1/00 , A61P1/04 , A61P1/16 , A61P37/00 , A61P25/28 , A61P25/16 , A61P25/34
CPC分类号： C07D231/14 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to compounds corresponding to formula (I): Wherein X, R1, R2, R3 and R4 are as defined herein. The invention further relates to preparation and therapeutic use of these compounds.
摘要翻译：本发明涉及对应于式（I）的化合物：其中X，R 1，R 2，R 3和R 4如本文所定义。本发明还涉及这些化合物的制备和治疗用途。

10. 发明授权

US6028084A Pyrazole derivatives, method for preparing same, and pharmaceutical compositions containing said derivatives 失效
标题翻译：吡唑衍生物，其制备方法和含有所述衍生物的药物组合物
公开(公告)号：US6028084A
公开(公告)日：2000-02-22
申请号：US068869
申请日：1998-05-19
申请人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi
发明人： Francis Barth , Christian Congy , Serge Martinez , Murielle Rinaldi
IPC分类号： A61K31/00 , A61K31/415 , A61K31/445 , A61K31/4453 , A61P25/00 , A61P43/00 , C07D231/14 , C07D401/12
CPC分类号： C07D231/14
摘要： Compounds of formula (I), wherein R.sub.1 is fluorine, hydroxy, (C.sub.1-5) alkoxy, (C.sub.1-5) alkylthio, hydroxy(C.sub.1-5)alkoxy, a -NR.sub.10 R.sub.11, group, cyano, (C.sub.1-5) alkyl-sulphonyl or (C.sub.1-5) alkylsulphinyl; R.sub.2 and R.sub.3 are each (C,.sub.4) alkyl or, taken together with the nitrogen atom to which they are attached, form a saturated or unsaturated 5- to 10-membered heterocyclic radical optionally substituted one or more times by (C.sub.1-3) alkyl or (C.sub.1-3) alkoxy; each of R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 is independently hydrogen, halogen or trifluoromethyl, and when R.sub.1 is fluorine, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and/or R.sub.9 may also be fluoromethyl; with the proviso that at least one of substituents R.sub.4 or R.sub.7. is other than hydrogen; each of R.sub.10 and R.sub.11 is independently hydrogen or (C.sub.1-5) alkyl, or R.sub.10 and R.sub.11, taken together with the nitrogen atom to which they are attached, form a heterocyclic radical selected from pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or piperazin-1-yl optionally substituted by (C.sub.1-4) alkyl; a method for preparing same, and pharmaceutical compositions containing said compounds, are disclosed. Said compounds have very high affinity for central cannabinoid receptors. ##STR1##
摘要翻译： PCT No.PCT / FR96 / 01847 Sec。 371日期1998年5月19日 102（e）日期1998年5月19日PCT 1996年11月21日PCT PCT。第WO97 / 19063号公报日期：1997年5月29日，式（I）的化合物，其中R 1为氟，羟基，（C 1-5）烷氧基，（C 1-5）烷硫基，羟基（C 1-5）烷氧基，-NR 10 R 11基，氰基，（C 1 -5）烷基磺酰基或（C 1-5）烷基亚磺酰基; R 2和R 3各自为（C 1-4）烷基，或与它们所连接的氮原子一起形成任选被（C 1-3）取代一次或多次的饱和或不饱和的5至10元杂环基，烷基或（C 1-3）烷氧基; R4，R5，R6，R7，R8和R9各自独立地是氢，卤素或三氟甲基，当R1是氟时，R4，R5，R6，R7，R8和/或R9也可以是氟甲基; 条件是至少一个取代基R4或R7。不是氢; R 10和R 11各自独立地为氢或（C 1-5）烷基，或者R 10和R 11与它们所连接的氮原子一起形成选自吡咯烷-1-基，哌啶-1-基，任选被（C 1-4）烷基取代的吗啉-4-基或哌嗪-1-基; 公开了其制备方法和含有所述化合物的药物组合物。所述化合物对中枢大麻素受体具有非常高的亲和力。

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