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51. 发明授权

US5130319A Pharmacologically active 2,5-dioxo-octahydro-imidazo [1,2-a]pyridines 失效
标题翻译：药理学活性的2,5-二氧代 - 吡唑并咪唑（1,2-A）吡啶
公开(公告)号：US5130319A
公开(公告)日：1992-07-14
申请号：US669806
申请日：1991-03-15
申请人： Mario Pinza , Alberto Cerri , Carlo Farina , Maria T. Riccaboni
发明人： Mario Pinza , Alberto Cerri , Carlo Farina , Maria T. Riccaboni
IPC分类号： A61K31/415 , A61K31/4166 , A61K31/435 , A61K31/55 , A61K38/00 , A61P25/00 , A61P25/18 , C07D233/32 , C07D233/36 , C07D471/04 , C07D487/04 , C07K5/078
CPC分类号： C07D471/04 , C07D233/32 , C07D487/04 , C07K5/06139 , A61K38/00
摘要： Imidazole derivatives are described which are useful in restoring learning and treating memory difficulties. A compound of the invention is 2,5-dioxohexahydro-1H-pyrrolo[1,2-a]imidazole.

52. 发明授权

US4632982A Triphenylmethyl azo and hydrazino substituted pyridazines 失效
标题翻译：三苯基甲基偶氮和肼基取代的哒嗪
公开(公告)号：US4632982A
公开(公告)日：1986-12-30
申请号：US831434
申请日：1986-02-20
申请人： Carlo Farina , Giorgio Pifferi , Mario Pinza
发明人： Carlo Farina , Giorgio Pifferi , Mario Pinza
IPC分类号： C07D237/20 , C07C107/04 , C07D237/12
CPC分类号： C07D237/20
摘要： Preparation of ethyl {6-[ethyl-(2-hydroxypropyl)amino]-3-pyridazinyl}hydrazino carboxylate is disclosed, from 3-chloro-6-hydrazinopyridazine in protected form, which is oxidized to yield the corresponding azo derivative, which is treated with ethyl-(2-hydroxypropyl)amine in the presence of strong bases, the corresponding amino derivative being subjected to reduction and deprotection, and finally acylated to yield ethyl{6-[ethyl-(2-hydroxypropyl)amino]-3-pyridazinyl}hydrazinocarboxylate.

53. 发明授权

US4575552A Process of making ethyl[6-[ethyl-(2-hydroxypropyl)amino]-3-pyridazinyl]hydrazine carboxylate 失效
标题翻译：制备乙基[6- [乙基 - （2-羟丙基）氨基] -3-哒嗪基]肼羧酸酯的方法
公开(公告)号：US4575552A
公开(公告)日：1986-03-11
申请号：US600407
申请日：1984-04-16
申请人： Carlo Farina , Giorgio Pifferi , Mario Pinza
发明人： Carlo Farina , Giorgio Pifferi , Mario Pinza
IPC分类号： C07D237/20
CPC分类号： C07D237/20
摘要： Preparation of ethyl {6-[ethyl-(2-hydroxypropyl)amino]-3-pyridazinyl} hydrazino carboxylate is disclosed from 3-chloro-6-hydrazinopyridazine in protected form, which is oxidized to yield the corresponding azo derivative, which is treated with ethyl-(2-hydroxypropyl)amine in the presence of strong bases, the corresponding amino derivative being subjected to reduction and deprotection, and finally acylated to yield ethyl {6-[ethyl-(2-hydroxypropyl)amino]-3-pyridazinyl} hydrazinocarboxylate.
摘要翻译：从保护形式的3-氯-6-肼基哒嗪公开了{6- [乙基 - （2-羟丙基）氨基] -3-哒嗪基}肼基羧酸乙酯的制备，其被氧化以产生相应的偶氮衍生物，其被处理在强碱存在下用乙基 - （2-羟丙基）胺，相应的氨基衍生物进行还原和去保护，最后酰化得到{6- [乙基 - （2-羟丙基）氨基] -3-哒嗪基 }肼基羧酸酯。

54. 发明申请

US20130123509A1 PROCESS FOR THE PREPARATION OF DIMIRACETAM 有权
标题翻译：制备DIMIRACETAM的方法
公开(公告)号：US20130123509A1
公开(公告)日：2013-05-16
申请号：US13811727
申请日：2011-07-25
申请人： Carlo Farina , Jacopo Roletto , Stefano Gobbato
发明人： Carlo Farina , Jacopo Roletto , Stefano Gobbato
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to a method of manufacture of dimiracetam (2,5-dioxohexahydro-1 H-pyrrolo[1,2-a]imidazole), characterized in that a 4-oxo-butanoic acid ester is condensed with glycinamide in a one-pot reaction with a controlled pH. The reaction may be performed in aqueous solution or in an anhydrous lower alcohol solution.
摘要翻译：本发明涉及二拉西坦（2,5-二氧代六氢-1H-吡咯并[1,2-a]咪唑）的制备方法，其特征在于4-氧代 - 丁酸酯与甘氨酰胺缩合，锅反应控制pH值。该反应可以在水溶液中或在无水低级醇溶液中进行。

55. 发明授权

US08222241B2 Use of dimiracetam in the treatment of chronic pain 有权
标题翻译：使用双拉西坦治疗慢性疼痛
公开(公告)号：US08222241B2
公开(公告)日：2012-07-17
申请号：US13166088
申请日：2011-06-22
申请人： Carlo Farina , Carla Ghelardini , Paola Petrillo
发明人： Carlo Farina , Carla Ghelardini , Paola Petrillo
IPC分类号： A61K31/44 , A61K31/40 , A61P23/00
CPC分类号： A61K31/7068 , A61K31/4188 , A61K31/555 , A61K45/06 , A61K2300/00
摘要： The use of dimiracetam in the treatment of chronic pain is disclosed. At doses higher than those previously disclosed in relation with its cognition enhancing activity (i.e. amelioration of learning and memory), dimiracetam was able to completely revert hyperalgesia or allodynia associated with several animal models of chronic pain. Dimiracetam showed high activity in iatrogenic neuropathies associated with antiviral and chemotherapeutic drug treatments and in painful conditions caused by osteoarthritis. In addition, dimiracetam was devoid of toxicity even at doses 10-fold higher than the highest therapeutic dose. The possibility of treating such debilitating pathologies with a highly effective and essentially non-toxic compound is therefore disclosed.
摘要翻译：公开了使用二拉西坦治疗慢性疼痛。在比以前公开的与其认知增强活性（即改善学习和记忆）相比更高的剂量下，二西拉坦能够完全恢复与慢性疼痛的几种动物模型相关的痛觉过敏或异常性疼痛。二西拉西坦在与抗病毒和化疗药物治疗相关的医源性神经病变以及由骨关节炎引起的疼痛状况下表现出高活性。此外，即使在比最高治疗剂量高10倍的剂量下，二西拉坦也没有毒性。因此公开了用高效和基本上无毒化合物治疗这种衰弱病态的可能性。

56. 发明申请

US20100125096A1 Acetam Derivatives for Pain Relief 有权
标题翻译：乙酰胺衍生物用于缓解疼痛
公开(公告)号：US20100125096A1
公开(公告)日：2010-05-20
申请号：US12566055
申请日：2009-09-24
申请人： Carlo Farina , Carla Ghelardini , Ruggero Fariello
发明人： Carlo Farina , Carla Ghelardini , Ruggero Fariello
IPC分类号： A61K31/4188 , A61K31/40 , A61P29/00
CPC分类号： A61K31/40 , A61K31/4188
摘要： The present invention provides a method of treatment, prevention and/or delay of progression of neuropathic pain by a specific dosing regime of acetam derivatives.
摘要翻译：本发明提供了一种通过乙酰胺衍生物的具体给药方案治疗，预防和/或延缓神经性疼痛进展的方法。

57. 发明申请

US20100062077A1 PYRROLO[1,2-A]IMIDAZOLEDIONE EFFECTIVE IN THE TREATMENT OF PERIPHERAL NEUROTOXICITY INDUCED BY CHEMOTHERAPEUTIC AGENTS 失效
标题翻译：治疗由化疗药物引起的外周神经毒性的PYRROLO [1,2-A]咪达拉灭有效
公开(公告)号：US20100062077A1
公开(公告)日：2010-03-11
申请号：US12312575
申请日：2007-11-14
申请人： Carlo Farina , Carla Ghelardini , Paola Petrillo
发明人： Carlo Farina , Carla Ghelardini , Paola Petrillo
IPC分类号： A61K31/4188 , A61K33/24 , A61K31/4745 , A61P25/02
CPC分类号： A61K31/4188 , C07D487/04
摘要： The use of a compound of formula (I), is disclosed in treating and/or preventing 5 chemotherapy-induced peripheral neurotoxicity (CIPN). The invention includes pharmaceutical compositions wherein the compound of formula (I) is present in a mixture with anticancer agents. An improved anticancer treatment with reduced CIPN-related side effects is also provided.
摘要翻译：公开了式（I）化合物在治疗和/或预防5种化学疗法诱发的周围神经毒性（CIPN）中的应用。本发明包括其中式（I）化合物与抗癌剂混合存在的药物组合物。还提供了具有减少的CIPN相关副作用的改进的抗癌治疗。

58. 发明授权

US07482458B2 Quinoline derivatives 失效
标题翻译：喹啉衍生物
公开(公告)号：US07482458B2
公开(公告)日：2009-01-27
申请号：US11385461
申请日：2006-03-21
申请人： Carlo Farina , Giuseppe Arnaldo Maria Giardina , Mario Grugni , Luca Francesco Raveglia
发明人： Carlo Farina , Giuseppe Arnaldo Maria Giardina , Mario Grugni , Luca Francesco Raveglia
IPC分类号： C07D215/38 , C07D215/44 , A61K31/47
CPC分类号： C04B35/632 , A61K31/00 , A61K31/4709 , C07D215/52 , C07D221/18 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D417/04
摘要： NK3 receptor antagonists of formula (I): are useful in treating inter alia pulmonary disorders, CNS disorders and neurodegenerative disorders.
摘要翻译：式（I）的NK3受体拮抗剂：可用于治疗肺功能紊乱，中枢神经系统疾病和神经变性疾病。

59. 发明申请

US20080317857A1 V-Atpase Inhibitors of Use in the Treatment of Septic Shock 审中-公开
标题翻译： V-Atpase抑制剂用于治疗脓毒性休克
公开(公告)号：US20080317857A1
公开(公告)日：2008-12-25
申请号：US12091740
申请日：2006-10-27
申请人： Carlo Farina , Gabriela Constantin , Carlo Laudanna , Paola Misiano
发明人： Carlo Farina , Gabriela Constantin , Carlo Laudanna , Paola Misiano
IPC分类号： A61K9/28 , A61K31/7048 , A61K38/02 , A61K31/4015
CPC分类号： A61K31/4166 , A61K31/365 , A61K31/4015 , A61K31/7048
摘要： The use of vacuolar ATPase inhibitors in the prevention and/or treatment of septic shock is herein described. Vacuolar ATPase inhibitors are selected among products of natural, semi-synthetic or synthetic origin.
摘要翻译：本文描述了液泡ATP酶抑制剂在预防和/或治疗败血性休克中的用途。真空ATP酶抑制剂选自天然，半合成或合成来源的产品。

60. 发明申请

US20070161647A1 QUINOLINE-4-CARBOXAMIDE DERIVATIVES AS NK-3 and NK-2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：喹啉-4-羧酰胺衍生物作为NK-3和NK-2受体拮抗剂
公开(公告)号：US20070161647A1
公开(公告)日：2007-07-12
申请号：US11685380
申请日：2007-03-13
申请人： Carlo Farina , Stefania Gagliardi , Giuseppe Giardina , Marisa Martinelli
发明人： Carlo Farina , Stefania Gagliardi , Giuseppe Giardina , Marisa Martinelli
IPC分类号： A61K31/496 , A61K31/4747 , C07D403/02 , C07D471/10
CPC分类号： C07D215/50 , C07D215/16 , C07D215/52 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D409/14 , C07D417/06 , C07D487/04
摘要： A compound of formula (I) as detailed in the specification or a pharmaceutically acceptable salt or solvate thereof, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.
摘要翻译：说明书或其药学上可接受的盐或溶剂合物中详述的式（I）化合物，制备这些化合物的方法，包含这些化合物的药物组合物以及这些化合物在医药中的用途。

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