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41. 发明授权

US06413985B1 Tetrahydroquinoline derivatives as glycine antagonists 失效
公开(公告)号：US06413985B1
公开(公告)日：2002-07-02
申请号：US09990513
申请日：2001-11-16
申请人： Romano Di Fabio
发明人： Romano Di Fabio
IPC分类号： A61K3147
CPC分类号： C07D401/04 , C07D401/14 , Y02P20/55
摘要： The present invention provides compounds of formula (I) or a salt or a non-toxic metabolically labile ester thereof, processes for their preparation, pharmaceutical compositions containing the same and to their use in medicine.

42. 发明授权

US06362199B1 Tetrahydroquinoline derivatives as glycine antagonists 失效
标题翻译：四氢喹啉衍生物作为甘氨酸拮抗剂
公开(公告)号：US06362199B1
公开(公告)日：2002-03-26
申请号：US09719188
申请日：2001-02-15
申请人： Romano Di Fabio
发明人： Romano Di Fabio
IPC分类号： A61K31495
CPC分类号： C07D401/04 , C07D401/14 , Y02P20/55
摘要： The present invention provides compounds of formula (I) or a salt or a non-toxic metabolically labile ester thereof, processes for their preparation, pharmaceutical compositions containing the same and to their use in medicine.
摘要翻译：本发明提供式（I）化合物或其盐或无毒的代谢不稳定酯，其制备方法，含有该化合物的药物组合物及其在医药中的用途。

43. 发明授权

US08133908B2 Heteroaryl derivatives of N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-amine 失效
标题翻译： N - {[（1S，4S，6S）-3-（2-吡啶基羰基）-3-氮杂双环[4.1.0]庚-4-基]甲基} -2-胺的杂芳基衍生物
公开(公告)号：US08133908B2
公开(公告)日：2012-03-13
申请号：US12627283
申请日：2009-11-30
申请人： Giuseppe Alvaro , David Amantini , Emiliano Castiglioni , Romano Di Fabio , Francesca Pavone
发明人： Giuseppe Alvaro , David Amantini , Emiliano Castiglioni , Romano Di Fabio , Francesca Pavone
IPC分类号： A61K31/44
CPC分类号： C07D401/06 , C07D401/14
摘要： Disclosed are N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives having the following formula: wherein m, n, Het, R1, R2 and R3 are as defined herein, and their use as orexin antagonists.
摘要翻译：公开了具有下式的N - {[（1S，4S，6S）-3-（2-吡啶基羰基）-3-氮杂双环[4.1.0]庚-4-基]甲基} -2-杂芳基胺衍生物，其中m ，n，Het，R 1，R 2和R 3如本文所定义，以及它们作为食欲素拮抗剂的用途。

44. 发明申请

US20100311734A1 Spiro Compounds Useful as Antagonists of the H1 Receptor 审中-公开
标题翻译：螺旋化合物可用作H1受体的拮抗剂
公开(公告)号：US20100311734A1
公开(公告)日：2010-12-09
申请号：US12670704
申请日：2008-07-24
申请人： Maurizio Botta , Emiliano Castiglioni , Romano Di Fabio , Raffaella Spinosa , Andrea Togninelli
发明人： Maurizio Botta , Emiliano Castiglioni , Romano Di Fabio , Raffaella Spinosa , Andrea Togninelli
IPC分类号： A61K31/5386 , C07D295/033 , C07D207/04 , C07D205/04 , C07D211/06 , C07D221/20 , C07D498/10 , C07D491/107 , A61K31/136 , A61K31/5375 , A61K31/40 , A61K31/495 , A61K31/54 , A61K31/451 , A61K31/438 , A61K31/403 , A61P25/00
CPC分类号： C07C211/42 , C07C2603/94 , C07D221/20 , C07D295/00 , C07D295/027 , C07D295/03 , C07D295/033 , C07D491/10 , C07D498/10
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.
摘要翻译：本发明提供了用于治疗中枢神经系统（CNS）的疾病和病症的式（I）化合物或其药学上可接受的盐，特别是睡眠障碍。

45. 发明申请

US20100286151A1 1-OXA-3-Azaspiro[4,5]Decan--2-One Derivatives For The Treatment Of Eating Disorders 审中-公开
标题翻译： 1-OXA-3-Azaspiro [4,5] Decan-2-One衍生物治疗饮食失调
公开(公告)号：US20100286151A1
公开(公告)日：2010-11-11
申请号：US12524080
申请日：2008-01-30
申请人： Jonathan Bentley , Matteo Biagetti , Romano Di Fabio , Thorsten Genski , Sebastien Guery , Silvia Rosalia Kopf , Colin philip Leslie , Angelica Mazzali , Sergio Melotto , Domenica Antonia Pizzi , Fabio Maria Sabbatini , Catia Seri
发明人： Jonathan Bentley , Matteo Biagetti , Romano Di Fabio , Thorsten Genski , Sebastien Guery , Silvia Rosalia Kopf , Colin philip Leslie , Angelica Mazzali , Sergio Melotto , Domenica Antonia Pizzi , Fabio Maria Sabbatini , Catia Seri
IPC分类号： A61K31/423 , C07D417/14 , A61K31/4439 , A61K31/505 , C07D413/14 , A61K31/501 , A61K31/444 , A61K31/497 , A61K31/433 , C07D471/04 , A61K31/437 , C07D487/04 , A61K31/4985 , C07D413/12 , A61P3/04 , A61P3/00
CPC分类号： C07D413/14
摘要： The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; Z1 is H, C1-C4 alkyl or F; Z is CH2, CH(C1-C4 alkyl), C(C1-C4 alkyl)2 or a bond; A is a 5 membered heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, Cl C4 haloalkoxy, cyano; B is hydrogen or is a 5-6 membered heteroaryl, or phenyl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; being A and B linked via any atom; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基; 其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; Z 1是H，C 1 -C 4烷基或F; Z是CH 2，CH（C 1 -C 4烷基），C（C 1 -C 4烷基）2或键; A是5元杂芳基，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; B是氢或是5-6元杂芳基或苯基，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 是通过任何原子连接的A和B; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。

46. 发明申请

US20080114049A1 CHEMICAL COMPOUNDS 失效
标题翻译：化学化合物
公开(公告)号：US20080114049A1
公开(公告)日：2008-05-15
申请号：US11851459
申请日：2007-09-07
申请人： Romano Di Fabio
发明人： Romano Di Fabio
IPC分类号： A61K31/403 , C07D209/02
CPC分类号： C07D221/04
摘要： The present invention relates to (1S,6R)-6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane, pharmaceutically acceptable salts, prodrugs or solvates thereof; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.
摘要翻译：本发明涉及（1S，6R）-6-（3,4-二氯苯基）-1 - [（甲氧基）甲基] -3-氮杂双环[4.1.0]庚烷，其药学上可接受的盐，前药或溶剂合物; 再摄入抑制剂，作为5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE），再摄取抑制剂，它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的应用。

47. 发明申请

US20070099914A1 Piperidine Derivatives 有权
标题翻译：哌啶衍生物
公开(公告)号：US20070099914A1
公开(公告)日：2007-05-03
申请号：US11608853
申请日：2006-12-11
申请人： Giuseppe Alvaro , Romano Di Fabio , Maria Tranquillini , Simone Spada
发明人： Giuseppe Alvaro , Romano Di Fabio , Maria Tranquillini , Simone Spada
IPC分类号： A61K31/5383 , A61K31/498
CPC分类号： C07D487/04 , A61K31/445
摘要： The present invention relates to methods for treatment of inflammatory diseases of the bladder.
摘要翻译：本发明涉及治疗膀胱炎性疾病的方法。

48. 发明授权

US5962496A Indole derivatives as NMDA antagonists 失效
标题翻译：吲哚衍生物作为NMDA拮抗剂
公开(公告)号：US5962496A
公开(公告)日：1999-10-05
申请号：US86522
申请日：1998-05-29
申请人： Alfredo Cugola , Romano Di Fabio , Giorgio Pentassuglia
发明人： Alfredo Cugola , Romano Di Fabio , Giorgio Pentassuglia
IPC分类号： A61K31/395 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/475 , A61K31/50 , A61P25/00 , A61P43/00 , C07D401/06 , C07D401/14 , C07D403/06 , C07D413/06 , C07D413/14 , C07D231/04
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D413/06 , Y02P20/55
摘要： This invention relates to compounds of formula ##STR1## or a salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.2 or COR.sub.2 wherein R.sub.2 represents hydroxy, methoxy, amino, alkylamino, or dialkylamino; m is zero or an integer 1 or 2;R.sub.1 represents a cycloalkyl, bridged cycloalkyl, heteroaryl, bridged heterocyclic or optionally substituted phenyl or fused bicyclic carbocylic group;A represents a C.sub.1-4 alkylene chain or the chain (CH.sub.2).sub.p Y(CH.sub.2).sub.q wherein Y is O, S(O)n or NR.sub.3 and which chains may be substituted by one or two groups selected from C.sub.1-6 alkyl optionally substituted by hydroxy, amino, alkylamino or dialkylamino, or which chains may be substituted by the group=O;R.sub.3 represents hydrogen, alkyl or a nitrogen protecting group;n is zero or an integer from 1 to 2;p is zero or an integer from 1 to 3;q is zero or an integer from 1 to 3 with the proviso that the sum of p+q is 1, 2 or 3, which are antagonists of excitatory amino acids, to processes for the preparation and to other use in medicine.
摘要翻译：本发明涉及式或其盐或其代谢不稳定酯的化合物，其中R表示选自卤素，烷基，烷氧基，氨基，烷基氨基，二烷基氨基，羟基，三氟甲基，三氟甲氧基，硝基，氰基，SO 2 R 2或COR 2的基团，其中R 2 表示羟基，甲氧基，氨基，烷基氨基或二烷基氨基; m为零或整数1或2; R 1表示环烷基，桥连环烷基，杂芳基，桥连杂环或任选取代的苯基或稠合双环碳酰基; A表示C 1-4亚烷基链或链（CH 2）p Y（CH 2）q，其中Y是O，S（O）n或NR 3，哪些链可以被选自任选被羟基取代的C 1-6烷基中的一个或两个基团取代，氨基，烷基氨基或二烷基氨基，或哪些链可以被基团= O取代; R3表示氢，烷基或氮保护基; n为0或1至2的整数; p为0或1至3的整数; q为0或1至3的整数，条件是p + q的和为1,2或3，它们是兴奋性氨基酸的拮抗剂，用于制备和在医药中的其它用途。

49. 发明授权

US5047433A N-alkyl derivatives of 2-amino-6,7-dimethoxy tetraline and pharmaceutical compositions having antihypertensive activity containing same 失效
标题翻译： 2-氨基-6,7-二甲氧基四氢萘的N-烷基衍生物和含有其的抗高血压活性的药物组合物
公开(公告)号：US5047433A
公开(公告)日：1991-09-10
申请号：US135335
申请日：1987-12-21
申请人： Mauro Marzi , Maria O. Tinti , Romano Di Fabio , Domenico Misiti
发明人： Mauro Marzi , Maria O. Tinti , Romano Di Fabio , Domenico Misiti
IPC分类号： C07C217/74 , A61K31/13 , A61K31/135 , A61P9/12 , C07C67/00 , C07C213/00 , C07C213/02
CPC分类号： A61K31/13
摘要： N-alkyl derivatives of 2-amino-6,7-dimethoxy tetraline having general formula (I) ##STR1## wherein R is selected from hydrogen, ethyl, n-propyl and methyl cyclopropyl;R.sub.1 is selected from hydrogen, hydroxy and --OR.sub.3 wherein R.sub.3 is selected from methyl, ethyl and n-propyl; andR.sub.2 is selected from hydrogen, methyl, hydroxy, trifluoromethyl, fluoro and methoxy,are endowed with potent antihypertensive activity.

50. 发明申请

US20120149723A1 5-METHYL-PIPERIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS FOR THE TREATMENT OF SLEEP DISORDER 审中-公开
标题翻译： 5-甲基哌啶衍生物作为治疗睡眠障碍的OREXIN受体拮抗剂
公开(公告)号：US20120149723A1
公开(公告)日：2012-06-14
申请号：US13391694
申请日：2010-08-16
申请人： Romano Di Fabio
发明人： Romano Di Fabio
IPC分类号： A61K31/506 , A61K31/4545 , A61P25/24 , A61P25/20 , A61P25/22 , A61P25/30 , A61P3/00 , C07D401/14 , A61P25/00
CPC分类号： C07D401/14
摘要： This invention relates to heteroaryloxy 5-methyl substituted piperidine derivatives and their use as pharmaceuticals.
摘要翻译：本发明涉及杂芳氧基-5-甲基取代的哌啶衍生物及其作为药物的用途。

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