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21. 发明授权

US09012634B2 Antibacterial piperidinyl substituted 3,4-dihydro-1H-[1,8]naphthyridinones 有权
标题翻译：抗菌哌啶基取代的3,4-二氢-1H- [1,8]萘啶酮
公开(公告)号：US09012634B2
公开(公告)日：2015-04-21
申请号：US14237851
申请日：2012-08-10
申请人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans
发明人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans
IPC分类号： A61K31/4375 , C07D515/04 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention is related to novel compounds of formula (I) that inhibit the activity of the Fab1 enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
摘要翻译：本发明涉及抑制Fab1酶活性的新型式（I）化合物，因此可用于治疗细菌感染。它还涉及包含这些化合物的药物组合物和用于制备这些化合物的化学方法。

22. 发明授权

US08906923B2 Antibacterial cyclopenta[c]pyrrole substituted 3,4-dihydro-1H-[1,8]naphthyridinones 有权
公开(公告)号：US08906923B2
公开(公告)日：2014-12-09
申请号：US14237862
申请日：2012-08-10
申请人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans , Eric Pierre Alexandre Arnoult
发明人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans , Eric Pierre Alexandre Arnoult
IPC分类号： C07D471/00 , C07D487/00 , C07D471/02 , A61K31/50 , A61K31/495 , A61K31/44
CPC分类号： C07D471/04 , C07D487/04 , C07D519/00
摘要： The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.

23. 发明申请

US20140171451A1 Antibacterial cyclopenta[c]pyrrole substituted 3,4-dihydro-1H-[1,8]naphthyridinones 有权
标题翻译：抗菌环戊二烯并[c]吡咯取代的3,4-二氢-1H- [1,8]萘啶酮
公开(公告)号：US20140171451A1
公开(公告)日：2014-06-19
申请号：US14237862
申请日：2012-08-10
申请人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans , Eric Pierre Alexandre Arnoult
发明人： Jerôme Emile Georges Guillemont , David Francis Alain Lançois , Magali Madeleine Simone Motte , Anil Koul , Wendy Mia Albert Balemans , Eric Pierre Alexandre Arnoult
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04 , C07D519/00
摘要： The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
摘要翻译：本发明涉及抑制因此可用于治疗细菌感染的FabI酶的活性的式（I）化合物。它还涉及包含这些化合物的药物组合物和用于制备这些化合物的化学方法。

24. 发明申请

US20080207687A1 Quinoline Derivatives as Antibacterial Agents 有权
公开(公告)号：US20080207687A1
公开(公告)日：2008-08-28
申请号：US11997173
申请日：2006-07-31
申请人： Jerome Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier , David Francis Alain Lancois , Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Leo Jacobus Jozef Backx , Lieven Meerpoel
发明人： Jerome Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier , David Francis Alain Lancois , Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Leo Jacobus Jozef Backx , Lieven Meerpoel
IPC分类号： A61K31/47 , A61P31/04 , C07D215/227
CPC分类号： C07D215/227 , A61K31/47
摘要： Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (I) a pharmaceutically acceptable acid or base addition salt, a quaternary amine, a stereochemically isomeric form, a tautomeric form or a N-oxide 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 to 3; s is 0 to 4; R2 is hydrogen; halo; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 0 to 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 together with the phenyl ring to which they are attached a naphthyl; r is 1 to 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen, alkyl, hydroxyl, aminocarbonyl, mono- or di(alkyl)aminocarbonyl, Ar, Het, alkyl substituted with one or two Het, alkyl substituted with one or two Ar, Het-C(═O)— or Ar—C(═O)—; provided that when the R3 bearing radical is placed in position 3 of the quinoline moiety; R7 is placed in position 4 and R2 is placed in position 2 and represents hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula then s is 1 to 4.

25. 发明申请

US20080227775A1 Quinoline Derivatives as Antibacterial Agents 有权
标题翻译：喹啉衍生物作为抗菌剂
公开(公告)号：US20080227775A1
公开(公告)日：2008-09-18
申请号：US11997015
申请日：2006-07-31
申请人： Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Jerome Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier
发明人： Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Jerome Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier
IPC分类号： A61K31/5355 , C07D413/08 , A61P31/04
CPC分类号： C07D413/06 , A61K31/4709 , C07D413/14 , Y02A50/473
摘要： Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of Formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a quaternary amine thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide 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, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; R4 is hydrogen, alkyl or benzyl; R5 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R5 radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1, 2, 3, 4 or 5; R6 is hydrogen, alkyl, Ar or Het; R7 is hydrogen or alkyl; R5 is oxo; or R7 and R5 together form the radical —CH═CH—N═; Z is CH2 or C(═O).
摘要翻译：使用化合物制造用于治疗细菌感染的药物，只要细菌感染不是分枝杆菌感染，所述化合物是式（Ia）或（Ib）的化合物，其药学上可接受的酸或碱加成其盐，其季胺，其立体化学异构形式，其互变异构形式或其N-氧化物形式，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，芳烷基或二（Ar）烷基; p为1,2,3或4; R 2是氢，羟基，硫代，烷氧基，烷氧基烷氧基，烷硫基，一或二（烷基）氨基或式R 3的基团是烷基，Ar，Ar- 烷基，Het或Het-烷基; R 4是氢，烷基或苄基; R 5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）烷基; 或两个邻位R 5个基团可以与它们所连接的苯环一起形成萘基; r为1,2,3,4或5; R 6是氢，烷基，Ar或Het; R 7是氢或烷基; R 5是氧代; 或R 7和R 5一起形成基团-CH-CH-N-; Z是CH 2或C（-O）。

26. 发明申请

US20110166179A1 ANTIBACTERIAL QUINOLINE DERIVATIVES 审中-公开
标题翻译：抗生素喹啉衍生物
公开(公告)号：US20110166179A1
公开(公告)日：2011-07-07
申请号：US12516396
申请日：2007-12-04
申请人： Jérôme Emile Georges Guillemont , Koenraad Jozef Lodewijk Andries , Anil Koul
发明人： Jérôme Emile Georges Guillemont , Koenraad Jozef Lodewijk Andries , Anil Koul
IPC分类号： A61K31/47 , C07D215/227 , A61K31/4709 , A61P31/04
CPC分类号： C07D401/04 , C07D215/14 , C07D413/04 , C07D417/04
摘要： The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvateas thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
摘要翻译：本发明涉及根据通式（Ia）或式（Ib）的新的取代喹啉衍生物：包括其任何立体化学异构形式，其N-氧化物，其药学上可接受的盐或溶剂化物。所要求保护的化合物可用于治疗细菌感染。还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的要求保护的化合物的组合物，所要求保护的化合物或组合物在制备用于治疗细菌感染的药物中的用途和制备所要求的化合物。

27. 发明申请

US20080255116A1 Quinoline Derivatives as Antibacterial Agents 有权
标题翻译：喹啉衍生物作为抗菌剂
公开(公告)号：US20080255116A1
公开(公告)日：2008-10-16
申请号：US11997182
申请日：2006-07-31
申请人： Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Jerome Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier , David Francis Alain Lancois
发明人： Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Jerome Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier , David Francis Alain Lancois
IPC分类号： A61K31/4709 , C07D215/20 , C07D405/02 , C07D401/04 , C07D413/04 , A61P31/04 , A61K31/5377 , A61K31/496 , A61K31/4704
CPC分类号： C07D215/227 , A61K31/47 , Y02A50/473
摘要： Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of Formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a quaternary amine thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide 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 or 3; R2 is hydrogen; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is zero, 1, 2, 3 or 4; X is a direct bond or CH2; 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 or a radical of formula R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo; or R8 and R9 together form the radical —CH═CH—N═;
摘要翻译：使用化合物制造用于治疗细菌感染的药物，只要细菌感染不是分枝杆菌感染，所述化合物是式（Ia）或（Ib）的化合物，其药学上可接受的酸或碱加成其盐，其季胺，其立体化学异构形式，其互变异构形式或其N-氧化物形式，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，芳烷基或二（Ar）烷基; p为1,2或3; R 2是氢; 烷基; 羟基; 巯基任选取代的烷氧基; 烷氧基烷氧基; 烷硫基单或二（烷基）氨基，其中烷基可任选被取代; Ar; Het或式R 3的基团是烷基，Ar，Ar-烷基，Het或Het-烷基; q为零，1,2,3或4; X是直接键或CH 2 N 2; 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是氢或式R 7的基团是氢，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-CH-CH-N-;

28. 发明申请

US20060281741A1 Quinoline derivatives as antibacterial agents 有权
公开(公告)号：US20060281741A1
公开(公告)日：2006-12-14
申请号：US11296918
申请日：2005-12-08
申请人： Koenraad Jozef Marcel Andries , Anil Koul , Jerome Guillemont , Elisabeth Therese Pasquier
发明人： Koenraad Jozef Marcel Andries , Anil Koul , Jerome Guillemont , Elisabeth Therese Pasquier
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/506 , A61K31/501 , A61K31/497 , A61K31/53 , A61K31/4709 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D215/227 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/541 , C07D215/36 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/06 , Y02A50/473
摘要： The present invention relates to the use of a compound for the manufacture of a medicament for the treatment of a bacterial infection, said compound being a compound of formula a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, polyhaloC1-6alkyl, C1-6alkyl, Ar or Het; p is an integer equal to 1 or 2; R2 is C1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy or C1-6alkylthio; R3 is Ar, Het or Het1; R4 and R5 each independently are hydrogen, C1-6alkyl or benzyl; or R4 and R5 together and including the N to which they are attached may form a radical selected from the group of pyrrolidinyl, 2-pyrrolinyl, 3-pyrrolinyl, pyrrolyl, imidazolidinyl, pyrazolidinyl, 2-imidazolinyl, 2-pyrazolinyl, imidazolyl, pyrazolyl, triazolyl, piperidinyl, pyridinyl, piperazinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, morpholinyl and thiomorpholinyl, each of said rings may optionally be substituted with C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, hydroxyC1-6alkyl, C1-6alkyloxy, amino, mono- or di(C1-6alkyl)amino, C1-6alkylthio, C1-6alkyloxyC1-6alkyl, C1-6alkylthioC1-6alkyl or pyrimidinyl; R6 is hydrogen, halo, polyhaloC1-6alkyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio; or two vicinal R6 radicals may be taken together to form a bivalent radical of formula —CH═CH—CH═CH—; r is an integer equal to 1 or 2; R7 is hydrogen, C1-6alkyl, Ar, Het or Het1; provided that the bacterial infection is other than a Mycobacterial infection.

29. 发明申请

US20090298842A1 Novel therapeutic targets for the treatment of mycobacterial infections and compounds useful therefor 审中-公开
标题翻译：用于治疗分枝杆菌感染的新型治疗靶点和有用的化合物
公开(公告)号：US20090298842A1
公开(公告)日：2009-12-03
申请号：US12462236
申请日：2009-08-01
申请人： János Pató , György Kéri , László Örfi , Frigyes Wáczek , Zoltán Horváth , Péter Banhegyi , Istaván Szabadkai , Jenö Marosfalvi , Bálint Hegymegi-barakonyi , Zsolt Székélyhidi , Zoltán Greff , Axel Choidas , Gerald Bacher , Andrea Missio , Anil Koul
发明人： János Pató , György Kéri , László Örfi , Frigyes Wáczek , Zoltán Horváth , Péter Banhegyi , Istaván Szabadkai , Jenö Marosfalvi , Bálint Hegymegi-barakonyi , Zsolt Székélyhidi , Zoltán Greff , Axel Choidas , Gerald Bacher , Andrea Missio , Anil Koul
IPC分类号： A61K31/498 , C12Q1/48 , C07D241/36 , C07D333/00 , A61K31/38
CPC分类号： C07D241/38
摘要： Described herein is the discovery that certain mycobacterial serine/threonine protein kinases, particularly protein kinase G (PknG), are effective therapeutic targets for the treatment of mycobacterial infections. Furthermore, the present application refers to the use of mycobacterial serine/threonine protein kinases for developing methods for detection and determination of these kinases for recognizing and monitoring diseases and for controlling therapy of diseases. Additionally disclosed are novel 4,5,6,7-tetrahydrobenzo[b]thiophene compounds, benzo(g)quinoxaline compounds, and pharmaceutically acceptable salts thereof, and methods of using such compounds and salts thereof for the prophylaxis and/or treatment of virally and/or bacterially induced infections, particularly mycobacteria-induced infections, including opportunistic infections, as well as pharmaceutical compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene compound and/or benzo(g)quinoxaline compound and/or pharmaceutically acceptable salts thereof in a pharmaceutically acceptable carrier.
摘要翻译：本文描述的是某些分枝杆菌丝氨酸/苏氨酸蛋白激酶，特别是蛋白激酶G（PknG）是用于治疗分枝杆菌感染的有效治疗靶标的发现。此外，本申请涉及使用分枝杆菌丝氨酸/苏氨酸蛋白激酶来开发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。另外公开了新的4,5,6,7-四氢苯并[b]噻吩化合物，苯并（g）喹喔啉化合物及其药学上可接受的盐，以及使用这些化合物和其盐来预防和/或治疗病毒的方法和/或细菌诱导的感染，特别是分枝杆菌诱导的感染，包括机会性感染，以及含有至少一种4,5,6,7-四氢苯并[b]噻吩化合物和/或苯并（g）喹喔啉化合物的药物组合物，以及 /或其药学上可接受的盐在药学上可接受的载体中。

30. 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。

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