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1. 发明申请

WO2007017758A3 NOVEL CYSTEINE PROTEASE INHIBITORS AND THEIR THERAPEUTIC APPLICATIONS 审中-公开
公开(公告)号：WO2007017758A3
公开(公告)日：2007-02-15
申请号：PCT/IB2006/002637
申请日：2006-07-26
申请人： HYBRIGENICS SA , GUEDAT, Philippe , BOISSY, Guillaume , BORG-CAPRA, Catherine , COLLAND, Frédéric , DAVIET, Laurent , FORMSTECHER, Etienne , JACQ, Xavier , RAIN, Jean-Christophe , DELANSORNE, Rémi , VALLESE, Stefania , COLOMBO, Matteo
发明人： GUEDAT, Philippe , BOISSY, Guillaume , BORG-CAPRA, Catherine , COLLAND, Frédéric , DAVIET, Laurent , FORMSTECHER, Etienne , JACQ, Xavier , RAIN, Jean-Christophe , DELANSORNE, Rémi , VALLESE, Stefania , COLOMBO, Matteo
IPC分类号： C07D241/38 , A61K31/495 , A61P35/00 , A61P25/28 , A61P9/00 , A61P31/00
摘要： The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.

2. 发明申请

WO2009149188A1 COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS 审中-公开
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：WO2009149188A1
公开(公告)日：2009-12-10
申请号：PCT/US2009/046136
申请日：2009-06-03
申请人： INTERMUNE, INC. , KOSSEN, Karl , SEIWERT, Scott, D. , SEREBRYANY, Vladimir , RUHRMUND, Donald , BEIGELMAN, Leonid , RAVEGLIA, Luca, Francesco Mario , VALLESE, Stefania , BIANCHI, Ivana , HU, Tao
发明人： KOSSEN, Karl , SEIWERT, Scott, D. , SEREBRYANY, Vladimir , RUHRMUND, Donald , BEIGELMAN, Leonid , RAVEGLIA, Luca, Francesco Mario , VALLESE, Stefania , BIANCHI, Ivana , HU, Tao
IPC分类号： A61K31/44 , C07D213/22
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。

3. 发明申请

WO2007017758A2 NOVEL CYSTEINE PROTEASE INHIBITORS AND THEIR THERAPEUTIC APPLICATIONS 审中-公开
标题翻译：新型CYSTEINE蛋白酶抑制剂及其治疗应用
公开(公告)号：WO2007017758A2
公开(公告)日：2007-02-15
申请号：PCT/IB2006002637
申请日：2006-07-26
申请人： HYBRIGENICS SA , GUEDAT PHILIPPE , BOISSY GUILLAUME , BORG-CAPRA CATHERINE , COLLAND FREDERIC , DAVIET LAURENT , FORMSTECHER ETIENNE , JACQ XAVIER , RAIN JEAN-CHRISTOPHE , DELANSORNE REMI , VALLESE STEFANIA , COLOMBO MATTEO
发明人： GUEDAT PHILIPPE , BOISSY GUILLAUME , BORG-CAPRA CATHERINE , COLLAND FREDERIC , DAVIET LAURENT , FORMSTECHER ETIENNE , JACQ XAVIER , RAIN JEAN-CHRISTOPHE , DELANSORNE REMI , VALLESE STEFANIA , COLOMBO MATTEO
IPC分类号： C07D241/38 , A61K31/495 , A61P25/28 , A61P35/00
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

WO2008052078A2 BENZOXATHIINE AND BENZOXATHIOLE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：苯并吖庚因和苯并氧杂环庚二烯衍生物及其用途
公开(公告)号：WO2008052078A2
公开(公告)日：2008-05-02
申请号：PCT/US2007/082425
申请日：2007-10-24
申请人： WYETH , STACK, Gary, Paul , LUONI, Giovanna , BIANCHI, Ivana , VALLESE, Stefania
发明人： STACK, Gary, Paul , LUONI, Giovanna , BIANCHI, Ivana , VALLESE, Stefania
IPC分类号： C07D327/04 , C07D327/06 , A61K31/381 , A61K31/39 , A61P25/04 , A61P25/06 , A61P25/14 , A61P25/28
CPC分类号： C07D327/04 , C07D327/06
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of R 1 , R 2 , R 3 , R 4 , 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 3， R 4，y，n，m，p和Ar如本文的类别和亚类中所定义和描述，它们是脑5-羟色胺2C亚型的激动剂或部分激动剂受体。这些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。

5. 发明申请

WO2005040138A1 SUBSTITUTED BENZYLAMINOALKYLENE HETEROCYCLES 审中-公开
标题翻译：取代的苯甲酰氨基烯烃杂环化合物
公开(公告)号：WO2005040138A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011104
申请日：2004-10-05
申请人： NEWRON PHARMACEUTICALS S.P.A. , SALVATI, Patricia , CACCIA, Carla , MELLONI, Piero , RESTIVO, Alessandra , SABIDO DAVID, Cibele , VALLESE, Stefania
发明人： SALVATI, Patricia , CACCIA, Carla , MELLONI, Piero , RESTIVO, Alessandra , SABIDO DAVID, Cibele , VALLESE, Stefania
IPC分类号： C07D261/02
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 NR 7 group; R 1 is C 3 -C 8 alkyl, or C 1 -C 8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C 1 -C 6 alkyl, hydroxyl, C 1 -C 6 alkoxy; R 2 , R 3 are independently hydrogen, C 1 -C 6 alkyl, halogen, trifluoromethyl, hydroxy or C 1 -C 6 alkoxy; R 4 is hydrogen, C 1 -C 8 alkyl; R 5 , R 6 are independently hydrogen, C 1 -C 3 alkyl, optionally substituted by hydroxy or phenyl; R 7 is hydrogen or straight or branched C 1 -C 3 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 C 1 -C 6 alkyl, halogen, hydroxyl or C 1 -C 6 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; R 2，R 3独立地是氢，C 1 -C 6烷基，卤素，三氟甲基，羟基或C 1 -C 6烷氧基; R 4是氢，C 1 -C 8烷基; R 5，R 6独立地是氢，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抑制剂具有活性，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。

6. 发明申请

WO2008052078A3 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：WO2008052078A3
公开(公告)日：2008-06-19
申请号：PCT/US2007082425
申请日：2007-10-24
申请人： WYETH CORP , STACK GARY PAUL , LUONI GIOVANNA , BIANCHI IVANA , VALLESE STEFANIA
发明人： STACK GARY PAUL , LUONI GIOVANNA , BIANCHI IVANA , VALLESE STEFANIA
IPC分类号： C07D327/04 , A61K31/381 , A61K31/39 , A61P25/04 , A61P25/06 , A61P25/14 , A61P25/28 , C07D327/06
CPC分类号： C07D327/04 , C07D327/06
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of R 1 , R 2 , R 3 , R 4 , 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 2， y，n，m，p和Ar定义如下，并且在本文的类别和亚类中描述，其是脑5-羟色胺受体的2C亚型的激动剂或部分激动剂。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

WO2005005411A1 SUBSTITUTED INDOLE LIGANDS FOR THE ORL-1 RECEPTOR 审中-公开
标题翻译：替代ORL-1受体的替代配体
公开(公告)号：WO2005005411A1
公开(公告)日：2005-01-20
申请号：PCT/EP2004/007294
申请日：2004-07-01
申请人： GLAXOSMITHKLINE S.P.A. , CONSONNI, Alessandra , DEL SORDO, Simone , FARINA, Carlo , GAGLIARDI, Stefania , RONZONI, Silvano , VALLESE, Stefania
发明人： CONSONNI, Alessandra , DEL SORDO, Simone , FARINA, Carlo , GAGLIARDI, Stefania , RONZONI, Silvano , VALLESE, Stefania
IPC分类号： 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 (II) and R, R 0 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 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是式（II）的部分，R 1，R 2，R 1，R 2，R 3，R 4，R 4， <5>，R 6在说明书中进一步限定。

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