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1. 发明公开

EP1939173A1 O-substituted-dibenzyl urea- or thiourea- derivatives as trpv1 receptor antagonists 审中-公开
标题翻译： O-替代物二苄基 - 尿素 - 硫氧还原酶TRPV1-Rezeptorantagonisten
公开(公告)号：EP1939173A1
公开(公告)日：2008-07-02
申请号：EP06026533.7
申请日：2006-12-21
申请人： Pharmeste S.r.l.
发明人： Baraldi, Pier Giovanni , Borea, Pier Andrea , Geppetti, Pierangelo , Fruttarolo, Francesca , Pavani, Maria Giovanna , Trevisani, Marcello
IPC分类号： C07C275/24 , C07C335/12 , A61K31/17 , A61P29/00
CPC分类号： C07C335/12 , C07C275/24
摘要： The invention relates to compounds of formula (I)

wherein
R is halogen;
R 1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, aminomethyl, 2-aminoethyl, 3-aminopropyl, 3-amino-2-hydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxypropen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, 4-hydroxybenzyl, and 4-aminobenzyl;
R 2 is O or S;
R 3 is tert-butyl or trifluoromethyl;
n is an integer selected from 0, 1 or 2.
The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, haemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.
摘要翻译：本发明涉及其中R为卤素的式（I）化合物; R 1选自2-羟乙基，2,3-二羟丙基，3-羟丙基，2,2-二羟基乙基，3,3-二羟基丙基，氨基甲基，2-氨基乙基，3-氨基丙基，3-氨基-2-羟丙基，1 ，3-二氧戊环 - 乙基，1,3-二恶烷 - 甲基，1,3-二氧戊环 - 甲基，1,3-二恶烷 - 乙基，3-氟-2-羟丙基，3-氯-2-羟丙基，2-羟基丙基，2-羟基丙-2-基，吗啉代乙基，哌嗪基乙基，羟甲基，苄基，4-（羟甲基）苄基，4-氯苄基，4-氟苄基，4-羟基苄基和4-氨基苄基。 R 2为O或S; R 3是叔丁基或三氟甲基; n是选自0,1或2的整数。式（I）化合物可用于制备用于治疗炎性状态的药物组合物，例如慢性神经性疼痛，过度膀胱综合征，肿瘤疼痛，痔疮，炎症痛觉过敏，干预后疼痛，牙齿拔除，气道和胃肠道疾病。

2. 发明授权

EP2046752B1 VR1 VANILLOID RECEPTOR ANTAGONISTS WITH A IONONIC SUBSTRUCTURE 有权
标题翻译：具有异常子结构的VR1香草酸受体拮抗剂
公开(公告)号：EP2046752B1
公开(公告)日：2010-05-19
申请号：EP07765000.0
申请日：2007-07-02
申请人： Pharmeste S.r.l.
发明人： BARALDI, Pier, Giovanni , BOREA, Pier, Andrea , GEPPETTI, Pierangelo , PAVANI, Maria, Giovanna , FRUTTAROLO, Francesca , TREVISANI, Marcello
IPC分类号： C07D217/02 , C07D217/22 , C07D213/75 , C07C233/11 , C07C233/15 , C07C233/28
CPC分类号： C07C233/15 , C07C233/10 , C07C233/13 , C07C233/28 , C07C235/30 , C07C2601/16 , C07D213/75 , C07D217/02 , C07D217/22

3. 发明公开

EP2048133A1 Nicotinamide n-oxide derivatives as vanilloid-1 receptor modulators 审中-公开
标题翻译：烟酰胺-N-氧化物 - 衍生物调节剂（vanulidoren des Vanilloid-1-Rezeptors）
公开(公告)号：EP2048133A1
公开(公告)日：2009-04-15
申请号：EP07019421.2
申请日：2007-10-04
申请人： Pharmeste S.r.l.
发明人： Napoletano, Mauro c/o Pharmeste S.r.l , Pavani, Maria Giovanna , Fruttarolo, Francesca c/o Pharmeste S.r.l , Trevisani, Marcello
IPC分类号： C07D213/89 , C07D401/04 , A61K31/4709 , A61P29/00
CPC分类号： C07D401/04 , C07D213/89
摘要： The present invention relates to vanilloid receptor modulators of formula (I)

wherein X is selected from phenyl, naphthyl, pyridine, quinoline or isoquinoline and Y is optionally substituted phenyl or pyridyl ring, to processes for the preparation thereof and to their pharmaceutical uses for the treatment of inflammatory states.
摘要翻译：本发明涉及式（I）的香草酸受体调节剂，其中X选自苯基，萘基，吡啶，喹啉或异喹啉，Y为任选取代的苯基或吡啶环，用于其制备及其药物用途治疗炎症状态。

4. 发明公开

EP2041094A1 BIARYLCARBOXYARYLAMIDES AS VANILLOID-1 RECEPTOR MODULATORS 有权
标题翻译： BIARYLCARBOXYARYLAMIDE AS调节剂香草素-1受体
公开(公告)号：EP2041094A1
公开(公告)日：2009-04-01
申请号：EP07764992.9
申请日：2007-07-02
申请人： Pharmeste S.r.l.
发明人： BARALDI, Pier, Giovanni , BOREA, Pier, Andrea , GEPPETTI, Pierangelo , PAVANI, Maria, Giovanna , FRUTTAROLO, Francesca , TREVISANI, Marcello
IPC分类号： C07D217/00 , C07D401/04 , A61K31/47 , A61K31/4725 , A61P13/00 , A61P29/00
CPC分类号： C07D401/04 , C07D217/02
摘要： The present invention provides compounds of formula (I): wherein A and Z are as defined in the description, along with methods for preparing such derivatives and their use for the treatment of inflammatory diseases such as neuropathic pain.

5. 发明授权

EP1805138B1 SULFONAMIDO COMPOUNDS THAT ANTAGONISE THE VANILLOID TRPV1 RECEPTOR 有权
标题翻译：磺酰胺类化合物拮抗香草素TRPV1受体
公开(公告)号：EP1805138B1
公开(公告)日：2008-03-19
申请号：EP05796943.8
申请日：2005-10-18
申请人： Pharmeste S.r.l.
发明人： BARALDI, Pier Giovanni , BOREA, Pier Andrea , GEPPETTI, Pierangelo
IPC分类号： C07C335/12 , C07C335/16 , C07C311/21 , C07C311/37 , A61K31/17 , A61K31/18
CPC分类号： C07C335/18 , C07C311/47 , C07C335/12 , C07C335/16
摘要： The invention relates to sulfonamido derivatives of formula (I) wherein R 1 -R 7 are as defined in the description. Compounds (I) antagonize the 10 vanilloid receptor and can be used for the preparation of medicaments for the treatment of inflammatory states.
摘要翻译：本发明涉及式（I）的磺酰氨基衍生物，其中R 1 -R 7如说明书中所定义。化合物（I）拮抗香草素受体并可用于制备治疗炎症状态的药物。

6. 发明授权

EP2094653B1 O-SUBSTITUTED-DIBENZYL UREA-DERIVATIVES AS TRPV1 RECEPTOR ANTAGONISTS 有权
标题翻译：作为TRPV1受体拮抗剂的O-取代的二苯甲基脲衍生物
公开(公告)号：EP2094653B1
公开(公告)日：2010-09-01
申请号：EP07848984.6
申请日：2007-12-06
申请人： Pharmeste S.r.l.
发明人： BARALDI, Pier Giovanni , BOREA, Pier Andrea , GEPPETTI, Pierangelo , FRUTTAROLO, Francesca , PAVANI, Maria Giovanna , TREVISANI, Marcello
IPC分类号： C07C275/24 , A61K31/17 , A61P29/00
CPC分类号： C07C335/12 , C07C275/24

7. 发明授权

EP1758851B1 VANILLOID TRPV1 RECEPTOR ANTAGONISTS 有权
标题翻译：辣椒素TRPV1拮抗剂
公开(公告)号：EP1758851B1
公开(公告)日：2010-01-13
申请号：EP05772206.8
申请日：2005-06-16
申请人： Pharmeste S.r.l.
发明人： BARALDI, Pier, Giovanni , BOREA, Pier, Andrea , GEPPETTI, Pierangelo
IPC分类号： C07C275/24 , C07C275/36 , A61K31/17
CPC分类号： C07C335/12
摘要： The invention relates to compounds of formula (I), wherein R e R1, R2, X and n are as defined in the description, and their use for the preparation of pharmaceutical compositions for the treatment of inflammatory states.

8. 发明公开

EP1889837A1 VR1 vanilloid receptor antagonists with a iononic substructure 审中-公开
标题翻译： VR1 Vanilloidrezeptorantagonisten mit jononischen Substrukturen
公开(公告)号：EP1889837A1
公开(公告)日：2008-02-20
申请号：EP06014299.9
申请日：2006-07-10
申请人： Pharmeste S.r.l.
发明人： Baraldi, Pier Giovanni , Borea, Pier Andrea , Geppetti, Pierangelo , Pavani, Maria Giovanna , Fruttarolo, Francesca , Trevisani, Marcello
IPC分类号： C07D217/02 , C07D217/22 , C07D213/75 , C07C233/11 , C07C233/15 , C07C233/28
CPC分类号： C07C233/15 , C07C233/10 , C07C233/13 , C07C233/28 , C07C235/30 , C07C2601/16 , C07D213/75 , C07D217/02 , C07D217/22
摘要： The invention provides compounds of formula (I):

wherein Y, R, n and X are as defined in the description,
a process for their preparation and pharmaceutical compositions containing them. The compounds of formula (I) inhibit the Transient Receptor Potential Vanilloid 1 (TRPV1), which plays a pivotal role in the development of post-inflammatory analgesia, therefore they can be used as analgesic and anti-inflammatory drugs.
摘要翻译：本发明提供式（I）化合物：其中Y，R，n和X如说明书中所定义，其制备方法和含有它们的药物组合物。式（I）化合物抑制瞬时受体电位香草酸1（TRPV1），其在炎性镇痛的发展中起关键作用，因此它们可以用作镇痛和抗炎药物。

9. 发明授权

EP2041094B1 BIARYLCARBOXYARYLAMIDES AS VANILLOID-1 RECEPTOR MODULATORS 有权
标题翻译： BIARYLCARBOXYARYLAMIDE AS调节剂香草素-1受体
公开(公告)号：EP2041094B1
公开(公告)日：2011-06-29
申请号：EP07764992.9
申请日：2007-07-02
申请人： Pharmeste S.r.l.
发明人： BARALDI, Pier, Giovanni , BOREA, Pier, Andrea , GEPPETTI, Pierangelo , PAVANI, Maria, Giovanna , FRUTTAROLO, Francesca , TREVISANI, Marcello
IPC分类号： C07D217/00 , C07D401/04 , A61K31/47 , A61K31/4725 , A61P13/00 , A61P29/00
CPC分类号： C07D401/04 , C07D217/02
摘要： The present invention provides compounds of formula (I): wherein A and Z are as defined in the description, along with methods for preparing such derivatives and their use for the treatment of inflammatory diseases such as neuropathic pain.

10. 发明公开

EP2094653A1 O-SUBSTITUTED-DIBENZYL UREA-DERIVATIVES AS TRPV1 RECEPTOR ANTAGONISTS 有权
标题翻译：作为TRPV1受体拮抗剂的O-取代的二苯甲基脲衍生物
公开(公告)号：EP2094653A1
公开(公告)日：2009-09-02
申请号：EP07848984.6
申请日：2007-12-06
申请人： Pharmeste S.r.l.
发明人： BARALDI, Pier Giovanni , BOREA, Pier Andrea , GEPPETTI, Pierangelo , FRUTTAROLO, Francesca , PAVANI, Maria Giovanna , TREVISANI, Marcello
IPC分类号： C07C275/24 , A61K31/17 , A61P29/00
CPC分类号： C07C335/12 , C07C275/24
摘要： The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane- ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro- 2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. R2 is te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, haemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.
摘要翻译：本发明涉及式（I）的化合物，其中R选自卤素，烷基，烷氧基，芳基和杂芳基; R1选自2-羟乙基，2,3-二羟基丙基，3-羟基丙基，2,2-二羟基乙基，3,3-二羟基丙基，1,3-二氧戊环 - 乙基，1,3-二恶烷 - 甲基，二氧戊环 - 甲基，1,3-二氧六环 - 乙基，3-氟-2-羟丙基，3-羧基-2-羟基丙基，3-氯-2-羟丙基，2-羟丙基，2-羟基丙烯-2-基，吗啉代乙基，哌嗪基乙基，羟甲基，苄基，4-（羟甲基）苄基，4-氯苄基，4-氟苄基和4-羟基苄基。 R2是叔丁基或三氟甲基; R 3独立地选自氢，羧基，氰基，烷基或羟烷基。式（I）化合物可用于制备用于治疗炎症状态的药物组合物，所述炎症状态例如慢性神经性疼痛，过度活跃的膀胱综合征，肿瘤疼痛，痔疮，炎性痛觉过敏，介入后疼痛，拔牙，气道和胃肠疾病。

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