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1. 发明申请

US20090215786A1 NOVEL CYSTEINE PROTEASE INHIBITORS AND THEIR THERAPEUTIC APPLICATIONS 有权
标题翻译：新型CYSTEINE蛋白酶抑制剂及其治疗应用
公开(公告)号：US20090215786A1
公开(公告)日：2009-08-27
申请号：US11997765
申请日：2006-07-26
申请人： Philippe Guedat , Guillaume Boissy , Catherine Borg-Capra , Frederic Colland , Laurent Daviet , Etienne Formstecher , Xavier Jacq , Jean-Christophe Rain , Remi Delansorne , Stefania Vallese , Matteo Colombo
发明人： Philippe Guedat , Guillaume Boissy , Catherine Borg-Capra , Frederic Colland , Laurent Daviet , Etienne Formstecher , Xavier Jacq , Jean-Christophe Rain , Remi Delansorne , Stefania Vallese , Matteo Colombo
IPC分类号： A61K31/498 , C07D241/36
CPC分类号： C07D241/38
摘要： The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.
摘要翻译：本发明涉及式（I）的新化合物，其制备方法及其治疗用途。

2. 发明申请

US20070032499A1 Novel cysteine protease inhibitors and their therapeutic applications 审中-公开
标题翻译：新型半胱氨酸蛋白酶抑制剂及其治疗应用
公开(公告)号：US20070032499A1
公开(公告)日：2007-02-08
申请号：US11197525
申请日：2005-08-05
申请人： Philippe Guedat , Guillaume Boissy , Catherine Borg-Capra , Frederic Colland , Laurent Daviet , Etienne Formstecher , Xavier Jacq , Jean-Christophe Rain , Rerni Delansorne , Stefania Vallese , Matteo Colombo
发明人： Philippe Guedat , Guillaume Boissy , Catherine Borg-Capra , Frederic Colland , Laurent Daviet , Etienne Formstecher , Xavier Jacq , Jean-Christophe Rain , Rerni Delansorne , Stefania Vallese , Matteo Colombo
IPC分类号： A61K31/498 , C07D241/36
CPC分类号： C07D241/38
摘要： The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.
摘要翻译：本发明涉及式（I）的新化合物，其制备方法及其治疗用途。

3. 发明授权

US08648076B2 Cysteine protease inhibitors and their therapeutic applications 有权
标题翻译：半胱氨酸蛋白酶抑制剂及其治疗应用
公开(公告)号：US08648076B2
公开(公告)日：2014-02-11
申请号：US11997765
申请日：2006-07-26
申请人： Philippe Guedat , Guillaume Boissy , Catherine Borg-Capra , Frédéric Colland , Laurent Daviet , Etienne Formstecher , Xavier Jacq , Jean-Christophe Rain , Rémi Delansorne , Stefania Vallese , Matteo Colombo
发明人： Philippe Guedat , Guillaume Boissy , Catherine Borg-Capra , Frédéric Colland , Laurent Daviet , Etienne Formstecher , Xavier Jacq , Jean-Christophe Rain , Rémi Delansorne , Stefania Vallese , Matteo Colombo
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D471/00 , C07D487/00
CPC分类号： C07D241/38
摘要： The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.
摘要翻译：本发明涉及式（I）的新化合物，其制备方法及其治疗用途。

4. 发明申请

US20070197603A1 Substituted indole ligands for the orl-1 receptor 审中-公开
标题翻译：用于orl-1受体的取代的吲哚配体
公开(公告)号：US20070197603A1
公开(公告)日：2007-08-23
申请号：US10561282
申请日：2004-07-01
申请人： Alessandra Consonni , Simone Del Sordo , Carlo Farina , Stefania Gagliardi , Silvano Ronzoni , Stefania Vallese
发明人： Alessandra Consonni , Simone Del Sordo , Carlo Farina , Stefania Gagliardi , Silvano Ronzoni , Stefania Vallese
IPC分类号： A61K31/44 , C07D401/06
CPC分类号： C07D409/14 , C07D401/06 , C07D401/14 , C07D405/14
摘要： New ligands for the ORL-1 receptor are described, useful for modulating the activity of said receptors in a patient in need thereof, and for preventing and treating illnesses dependent on the stimulation of this receptor. The new compounds conform to structural formula (I), wherein Q is a moiety of formula: and R, R0, R1, R2, R3, R4, R5, R6 are further defined in the description.
摘要翻译：描述了ORL-1受体的新配体，可用于调节有需要的患者中所述受体的活性，以及用于预防和治疗依赖于该受体刺激的疾病。新化合物符合结构式（I），其中Q是下式的部分：R 1，R 0，R 1，R 2， >，R 3，R 4，R 5，R 6，6在说明书中进一步定义。

5. 发明授权

US08304413B2 Compounds and methods for treating inflammatory and fibrotic disorders 有权
标题翻译：用于治疗炎性和纤维化疾病的化合物和方法
公开(公告)号：US08304413B2
公开(公告)日：2012-11-06
申请号：US12477715
申请日：2009-06-03
申请人： Karl Kossen , Scott D. Seiwert , Vladimir Serebryany , Donald Ruhrmund , Leonid Beigelman , Luca Francesco Mario Raveglia , Stefania Vallese , Ivana Bianchi , Tao Hu
发明人： Karl Kossen , Scott D. Seiwert , Vladimir Serebryany , Donald Ruhrmund , Leonid Beigelman , Luca Francesco Mario Raveglia , Stefania Vallese , Ivana Bianchi , Tao Hu
IPC分类号： A61K31/50 , A61K31/497 , A61K31/437 , A61K31/44
CPC分类号： C07D213/63 , C07D213/22 , C07D213/64 , C07D213/69 , C07D213/71 , C07D213/85 , C07D237/14 , C07D239/36 , C07D239/54 , C07D241/18 , C07D251/10 , C07D401/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
摘要翻译：公开了用于治疗炎症和纤维化疾病的化合物和方法，包括用活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中活性化合物表现出低的抑制p38MAPK的能力; 并且其中所述接触以对所述化合物抑制p38MAPK的抑制浓度低的SAPK调节浓度进行。还公开了吡非尼酮的衍生物和类似物，其可用于调节应激活化蛋白激酶（SAPK）系统。

6. 发明申请

US20100160411A1 BENZOXATHIINE AND BENZOXATHIOLE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：苯甲酸和苯并恶唑衍生物及其用途
公开(公告)号：US20100160411A1
公开(公告)日：2010-06-24
申请号：US12446904
申请日：2007-10-24
申请人： Gary Paul Stack , Ivana Bianchi , Stefania Vallese , Giovanna Luoni
发明人： Gary Paul Stack , Ivana Bianchi , Stefania Vallese , Giovanna Luoni
IPC分类号： A61K31/39 , C07D327/06 , C07D327/04 , A61P25/18 , A61P25/00 , A61P15/00 , A61P13/10 , A61P25/24 , A61P25/16 , A61P25/08 , A61P25/22 , A61P25/30 , A61P25/06
CPC分类号： C07D327/04 , C07D327/06
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of R1, R2, R3, R4, y, n, m, p, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
摘要翻译：提供式（I）化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，Y，n，m，p和Ar各自如本文中所定义和描述，其为激动剂或部分激动剂的2C亚型脑血清素受体。化合物和含有这些化合物的组合物可用于治疗各种中枢神经系统疾病如精神分裂症。

7. 发明申请

US20070135496A1 Substituted benzylaminoalkylene heterocycles 有权
公开(公告)号：US20070135496A1
公开(公告)日：2007-06-14
申请号：US10575627
申请日：2004-10-05
申请人： Patricia Salvati , Carla Caccia , Piero Melloni , Alessandra Restivo , Cibele Sabido David , Stefania Vallese
发明人： Patricia Salvati , Carla Caccia , Piero Melloni , Alessandra Restivo , Cibele Sabido David , Stefania Vallese
IPC分类号： A61K31/44 , A61K31/421 , A61K31/42 , A61K31/4172 , A61K31/381 , A61K31/35 , A61K31/343 , A61K31/34
CPC分类号： C07D261/02 , A61K31/341 , A61K31/422 , A61K31/426 , C07D213/38 , C07D233/64 , C07D235/14 , C07D249/08 , C07D261/08 , C07D263/32 , C07D277/28 , C07D307/14 , C07D307/38 , C07D307/52 , C07D307/81 , C07D309/04 , C07D319/12 , C07D333/20
摘要： This invention is related to compounds of general formula (I) wherein X is oxygen or sulphur or a NR7 group; R1 is C3-C8 alkyl, or C1-C8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C1-C6 alkyl, hydroxyl, C1-C6 alkoxy; R2, R3 are independently hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, hydroxy or C1-C6 alkoxy; R4 is hydrogen, C1-C8 alkyl; R5, R6 are independently hydrogen, C1-C3 alkyl, optionally substituted by hydroxy or phenyl; R7 is hydrogen or straight or branched C1-C3 alkyl; Het is a five to seven membered, saturated or unsaturated heteromonocyclic or an eight to ten membered, saturated or unsaturated heterobicyclic group, containing one or more heteroatoms chosen independently from nitrogen, oxygen and sulphur, said mono- or bicyclic groups being optionally substituted by C1-C6alkyl, halogen, hydroxyl or C1-C6 alkoxy; and the pharmaceutically acceptable salts or prodrug thereof, that are active as sodium and/or calcium channel modulators and/or as selective MAO-B inhibitors and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.

8. 发明申请

US20090318455A1 COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS 有权
标题翻译：用于治疗炎症和纤维性疾病的化合物和方法
公开(公告)号：US20090318455A1
公开(公告)日：2009-12-24
申请号：US12477715
申请日：2009-06-03
申请人： Karl Kossen , Scott D. Seiwert , Vladimir Serebryany , Donald Ruhrmund , Leonid Beigelman , Luca F. Raveglia , Stefania Vallese , Ivana Bianchi , Tao Hu
发明人： Karl Kossen , Scott D. Seiwert , Vladimir Serebryany , Donald Ruhrmund , Leonid Beigelman , Luca F. Raveglia , Stefania Vallese , Ivana Bianchi , Tao Hu
IPC分类号： A61K31/50 , A61K31/497 , A61K31/437 , A61K31/44 , C07D237/02 , C07D241/02 , C07D471/02 , C07D213/63
CPC分类号： C07D213/63 , C07D213/22 , C07D213/64 , C07D213/69 , C07D213/71 , C07D213/85 , C07D237/14 , C07D239/36 , C07D239/54 , C07D241/18 , C07D251/10 , C07D401/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
摘要翻译：公开了用于治疗炎症和纤维化疾病的化合物和方法，包括用活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中活性化合物表现出低的抑制p38MAPK的能力; 并且其中所述接触以对所述化合物抑制p38MAPK的抑制浓度低的SAPK调节浓度进行。还公开了吡非尼酮的衍生物和类似物，其可用于调节应激活化蛋白激酶（SAPK）系统。

9. 发明授权

US07649005B2 Substituted benzylaminoalkylene heterocycles 有权
标题翻译：取代的苄基氨基亚烷基杂环
公开(公告)号：US07649005B2
公开(公告)日：2010-01-19
申请号：US10575627
申请日：2004-10-05
申请人： Patricia Salvati , Carla Caccia , Piero Melloni , Alessandra Restivo , Cibele Sabido David , Stefania Vallese
发明人： Patricia Salvati , Carla Caccia , Piero Melloni , Alessandra Restivo , Cibele Sabido David , Stefania Vallese
IPC分类号： A61K31/44 , C07D213/02
CPC分类号： C07D261/02 , A61K31/341 , A61K31/422 , A61K31/426 , C07D213/38 , C07D233/64 , C07D235/14 , C07D249/08 , C07D261/08 , C07D263/32 , C07D277/28 , C07D307/14 , C07D307/38 , C07D307/52 , C07D307/81 , C07D309/04 , C07D319/12 , C07D333/20
摘要： This invention is related to compounds of general formula (I) wherein X is oxygen or sulphur or a NR7 group; R1 is C3-C8 alkyl, or C1-C8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C1-C6 alkyl, hydroxyl, C1-C6 alkoxy; R2, R3 are independently hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, hydroxy or C1-C6 alkoxy; R4 is hydrogen, C1-C8 alkyl; R5, R6 are independently hydrogen, C1-C3 alkyl, optionally substituted by hydroxy or phenyl; R7 is hydrogen or straight or branched C1-C3 alkyl; Het is a five to seven membered, saturated or unsaturated heteromonocyclic or an eight to ten membered, saturated or unsaturated heterobicyclic group, containing one or more heteroatoms chosen independently from nitrogen, oxygen and sulphur, said mono- or bicyclic groups being optionally substituted by C1-C6alkyl, halogen, hydroxyl or C1-C6 alkoxy; and the pharmaceutically acceptable salts or prodrug thereof, that are active as sodium and/or calcium channel modulators and/or as selective MAO-B inhibitors and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
摘要翻译：本发明涉及通式（I）的化合物，其中X是氧或硫或NR 7基团; R 1是C 3 -C 8烷基或被苯氧基或苯基取代的C 1 -C 8烷基，苯氧基或苯基任选被一个或多个氟，氯，三氟甲基，C 1 -C 6烷基，羟基，C 1 -C 6烷氧基取代; R2，R3独立地是氢，C1-C6烷基，卤素，三氟甲基，羟基或C1-C6烷氧基; R4是氢，C1-C8烷基; R5，R6独立地为氢，任选被羟基或苯基取代的C 1 -C 3烷基; R 7是氢或直链或支链C 1 -C 3烷基; Het是五至七元饱和或不饱和杂单环或八至十元饱和或不饱和杂双环基团，其含有一个或多个独立地选自氮，氧和硫的杂原子，所述单 - 或双环基团任选被C 1 -C 1-6烷基，卤素，羟基或C 1 -C 6烷氧基; 其作为钠和/或钙通道调节剂和/或作为选择性MAO-B抑制剂是有活性的，因此可用于预防，缓解和治愈广泛范围的病症，包括但不限于神经，精神，心血管，炎症，眼科，泌尿，代谢和胃肠疾病，其中上述机制已被描述为发挥病理作用。

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