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31. 发明申请

US20070275962A1 Heterobicyclic Compounds as Pharmaceutically Active Agents 审中-公开
标题翻译：异双环化合物作为药物活性剂
公开(公告)号：US20070275962A1
公开(公告)日：2007-11-29
申请号：US10597120
申请日：2004-09-10
申请人： Anil Koul , Bert Klebl , Gerhard Muller , Andrea Missio , Wilfried Schwab , Doris Hafenbradl , Lars Neumann , Marc-Nicola Sommer , Stefan Muller , Edmund Hoppe , Achim Freisleben , Alexander Backes , Christian Hartung , Beatrice Felber , Birgit Zech , Ola Engkvist , Gyorgy Keri , Laszlo Orfi , Peter Banhegyi , Zoltan Greff , Zoltan Horvath , Zoltan Varga , Peter Marko , Janos Pato , Istvan Szabadkai , Zsolt Szekelyhid , Frigyes Waczek
发明人： Anil Koul , Bert Klebl , Gerhard Muller , Andrea Missio , Wilfried Schwab , Doris Hafenbradl , Lars Neumann , Marc-Nicola Sommer , Stefan Muller , Edmund Hoppe , Achim Freisleben , Alexander Backes , Christian Hartung , Beatrice Felber , Birgit Zech , Ola Engkvist , Gyorgy Keri , Laszlo Orfi , Peter Banhegyi , Zoltan Greff , Zoltan Horvath , Zoltan Varga , Peter Marko , Janos Pato , Istvan Szabadkai , Zsolt Szekelyhid , Frigyes Waczek
IPC分类号： C07D495/04 , A61P31/04 , C07D209/42 , C07D333/66 , C07D333/68 , C07D495/10 , C07D409/12 , C07D413/14 , C07D491/04 , C07D493/04
CPC分类号： C07D409/12 , C07D209/42 , C07D333/66 , C07D333/68 , C07D491/04 , C07D493/04 , C07D495/04 , C07D495/10
摘要： Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.
摘要翻译：描述的是杂双环化合物，例如4,5,6,7-四氢苯并[b]噻吩-3-羧酸酰胺，4,7-二氢-5H-噻吩并[2,3-c]噻喃-3-羧酸酰胺，4 ，7-二氢-5H-噻吩并[2,3-c]吡喃-3-羧酸酰胺或苯并[b]噻吩-3-羧酸酰胺及其药学上可接受的盐，这些衍生物用于预防和 /或治疗诸如感染性疾病，包括分泌细菌感染和机会性疾病，朊病毒疾病，免疫疾病，自身免疫疾病，双相和临床病症，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经变性疾病和中风，以及含有至少一种杂双环化合物和/或其药学上可接受的盐的组合物。此外，公开了用于合成杂双环化合物的反应程序。

32. 发明申请

US20090018149A1 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and methods for medical intervention against mycobacterial infections 审中-公开
标题翻译： 4,5,6,7-四氢苯并[b]噻吩衍生物和用于针对分枝杆菌感染的医疗干预的方法
公开(公告)号：US20090018149A1
公开(公告)日：2009-01-15
申请号：US10510791
申请日：2003-04-09
申请人： Andrea Missio , Gerald Bacher , Anil Koul , Axel Choidas , Peter Banhegyi , Zoltan Greff , Gyorgy Keri , Peter Marko , Laszlo Orfi , Janos Pato , Frigyes Waczek
发明人： Andrea Missio , Gerald Bacher , Anil Koul , Axel Choidas , Peter Banhegyi , Zoltan Greff , Gyorgy Keri , Peter Marko , Laszlo Orfi , Janos Pato , Frigyes Waczek
IPC分类号： A61K31/381 , A61P31/04 , A61P31/12 , C07D333/52 , C07D409/02 , G01N33/53 , A61K31/4178 , C07D495/02 , A61K31/519 , A61K31/4535
CPC分类号： C07D409/12 , C07D333/66 , C07D333/68 , C07D409/14 , C07D495/04 , C07D495/14
摘要： Described are 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of mycobacteria-induced infections and opportunistic infections, as well as compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene derivative and/or pharmaceutically acceptable salts thereof. Furthermore, the present application refers to the use of mycobacterial protein serine/threonine kinases for developing methods for detection and determination of these kinases for recognising and monitoring diseases and for controlling therapy of diseases.
摘要翻译：描述了4,5,6,7-四氢苯并[b]噻吩衍生物及其药学上可接受的盐，这些衍生物用于预防和/或治疗分枝杆菌诱导的感染和机会性感染，以及至少含有一种4,5,6,7-四氢苯并[b]噻吩衍生物和/或其药学上可接受的盐。此外，本申请是指使用分枝杆菌蛋白丝氨酸/苏氨酸激酶来开发用于检测和测定这些用于识别和监测疾病和控制疾病治疗的这些激酶的方法。

33. 发明申请

US20060142279A1 Treatment of latent tuberculosis 审中-公开
标题翻译：治疗潜伏性结核病
公开(公告)号：US20060142279A1
公开(公告)日：2006-06-29
申请号：US11296992
申请日：2005-12-08
申请人： Koenraad Marcel Andries , Anil Koul
发明人： Koenraad Marcel Andries , Anil Koul
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4709
CPC分类号： A61K31/47 , A61K31/4704
摘要： Use of a compound of formula (Ia) or (Ib) for the manufacture of a medicament for the treatment of latent tuberculosis, wherein the compound of formula (Ia) or (Ib) is a pharmaceutically acceptable salt, a quaternary amine, a N-oxide, a tautomeric form or a stereochemically isomeric form thereof wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula ;R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is zero, 1, 2, 3 or 4; R4 and R5 each independently are hydrogen, alkyl or benzyl; or R4 and R5 may be taken together including the N to which they are attached; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R6 radicals may be taken together to form a bivalent radical —CH═CH—CH═CH—; r is 1, 2, 3, 4 or 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo; or R8 and R9 together form the radical ═N—CH═CH—.
摘要翻译：式（Ia）或（Ib）化合物在制备用于治疗潜伏性结核病的药物中的用途，其中式（Ia）或（Ib）化合物是药学上可接受的盐，季胺，N 氧化物，互变异构形式或其立体化学异构体形式，其中R 1是氢，卤素，卤代烷基，氰基，羟基，Ar，Het，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，或二（Ar）烷基; p为1,2,3或4; R 2是氢，羟基，巯基，烷氧基，烷氧基烷氧基，烷硫基，一或二（烷基）氨基或式的基团; R 3是烷基，Ar，Ar - 烷基，Het或Het-烷基; q为零，1,2,3或4; R 4和R 5各自独立地是氢，烷基或苄基; 或R 4和R 5可以一起包括它们所连接的N; R 6是氢，卤素，卤代烷基，羟基，Ar，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar）或两个邻位R 6个基团可以一起形成二价基团-CH-CH-CH-CH-; r为1,2,3,4或5; R 7是氢，烷基，Ar或Het; R 8是氢或烷基; R 9是氧代; 或R 8和R 9一起形成基团-N-CH-CH-。

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