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31. 发明授权

US08669261B2 Acrylomido derivatives useful as inhibitors of the mitochondrial permeability transition 有权
标题翻译： Acrylomido衍生物可用作线粒体通透性转换的抑制剂
公开(公告)号：US08669261B2
公开(公告)日：2014-03-11
申请号：US13874081
申请日：2013-04-30
申请人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
发明人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
IPC分类号： A61K31/4965 , A61K31/445 , A61K31/4178 , A61K31/416 , A61K31/22 , A61K31/19 , A61K31/18 , A61K31/167
CPC分类号： C07C235/38 , C07C235/36 , C07C323/41 , C07C2601/04 , C07C2602/08 , C07D209/08 , C07D211/22 , C07D213/30 , C07D213/36 , C07D213/68 , C07D213/75 , C07D231/12 , C07D231/56 , C07D233/64 , C07D235/06 , C07D235/30 , C07D239/47 , C07D249/18 , C07D257/04 , C07D263/32 , C07D263/56 , C07D295/096 , C07D295/135 , C07D307/42
摘要： Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R′, R″, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
摘要翻译：可用作治疗剂的丙烯酰胺衍生物，特别是用于预防和/或治疗与线粒体通透性转换孔（MPTP）的活性相关的疾病和病症，例如以缺血/再灌注，氧化性或退行性组织损伤为特征的疾病，是在此描述。这些化合物属于结构式（I），其中R，R'，R“，W和a如说明书中所定义。本发明还涉及这些化合物的制备，以及包含它们的药物组合物。

32. 发明申请

US20070037790A1 Bicyclo-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 审中-公开
标题翻译：作为激酶抑制剂活性的双环吡唑衍生物，其制备方法和包含它们的药物组合物
公开(公告)号：US20070037790A1
公开(公告)日：2007-02-15
申请号：US10548332
申请日：2004-03-02
申请人： Francesca Abrate , Daniele Fancelli , Mario Varasi , Manuela Villa
发明人： Francesca Abrate , Daniele Fancelli , Mario Varasi , Manuela Villa
IPC分类号： A61K31/55 , A61K31/4745
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/4745 , A61K31/55
摘要： Compounds which are pyrrolo-pyrazole derivatives and pharmaceutically acceptable salts thereof, together with the process for their preparation and pharmaceutical compositions thereof are disclosed; these compounds or compositions are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders.
摘要翻译：公开了吡咯并吡唑衍生物及其药学上可接受的盐的化合物及其制备方法及其药物组合物; 这些化合物或组合物可用于治疗由改变的蛋白激酶活性如癌症，细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫疾病和神经变性疾病引起的和/或与其相关的疾病。

33. 发明授权

US06387900B1 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents 失效
标题翻译： 3（5） - 脲 - 吡唑衍生物的制备方法及其作为抗肿瘤剂的用途
公开(公告)号：US06387900B1
公开(公告)日：2002-05-14
申请号：US09372833
申请日：1999-08-12
申请人： Paolo Pevarello , Paolo Orsini , Gabriella Traquandi , Mario Varasi , Edward L. Fritzen , Martha A. Warpehoski , Betsy S. Pierce
发明人： Paolo Pevarello , Paolo Orsini , Gabriella Traquandi , Mario Varasi , Edward L. Fritzen , Martha A. Warpehoski , Betsy S. Pierce
IPC分类号： C07D23140
CPC分类号： C07D231/40 , A61K31/415 , A61K31/4155 , A61K31/4178 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/5377
摘要： 3-ureido-pyrazole derivatives represented by formula (I): where R, R1 and R2 are as described herein, or pharmnaceutically acceptable salts thereof; are useful, for example, for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
摘要翻译：由式（I）表示的3-脲基 - 吡唑衍生物：其中R，R 1和R 2如本文所述，或其药物上可接受的盐; 例如用于治疗癌症，细胞增殖性疾病，阿尔茨海默氏病，病毒感染，自身免疫性疾病或神经变性疾病是有用的。

34. 发明授权

US06306903B1 Alpha-aminoamide derivatives useful as analgesic agents 有权
标题翻译：用作止痛剂的α-氨基酰胺衍生物
公开(公告)号：US06306903B1
公开(公告)日：2001-10-23
申请号：US09582198
申请日：2000-08-29
申请人： Paolo Pevarello , Mario Varasi , Patricia Salvati , Claes Post
发明人： Paolo Pevarello , Mario Varasi , Patricia Salvati , Claes Post
IPC分类号： A61K31275
CPC分类号： C07C237/06 , A61K31/165 , C07C255/54
摘要： The present invention relates to novel and known alpha-aminoamide compounds, to a process for their preparation, to pharmaceutical composition containing them and to their use as therapeutic agents. In particular, the compounds of the present invention are endowed with analgesic properties and are particularly useful for the treatment and alleviation of chronic and neuropathic pain. Accordingly, one object of the present invention is to provide the use of a compound of formula (I) wherein: A is a —(CH2)m—, —(CH2)n—X— or —(CH2)v—O— group wherein m is an integer of 1 to 4, n is zero or an integer of 1 to 4, X is —S— or —NH—, and v is zero or an integer of 1 to 5; s is 1 or 2; R is a furyl, thienyl, or pyridyl ring or a phenyl ring optionally substituted by one or two substitutents independently chosen from halogen, cyano, C1-C4 alkyl, C1-C4 alkoxy and trifluoromethyl; R1 is hydrogen or C1-C4 alkyl; one of R2 and R3 is hydrogen and the other is hydrogen or C1-C4 alkyl optionally substituted by hydroxy or phenyl; or R2 and R3 taken together with the carbon atom to which they are linked form a C3-C6 cycloalkyl ring; or R2 and R3 are both methyl; R4 is hydrogen or C1-C4 alkyl.
摘要翻译：本发明涉及新的和已知的α-氨基酰胺化合物，其制备方法，含有它们的药物组合物及其作为治疗剂的用途。特别地，本发明的化合物具有止痛性质，特别是对于治疗和缓解慢性和神经性疼痛有用。因此，本发明的一个目的是提供式（I）化合物的用途，其中：A是 - （CH 2）m - ， - （CH 2）n X - 或 - （CH 2）v O-基团，其中m为1至4的整数，n为0或1至4的整数，X为-S-或-NH-，v为0或1至 5; s是1或2; R是呋喃基，噻吩基或吡啶基环或任选被一个或两个独立地选自卤素，氰基，C 1 -C 4烷基，C 1 -C 4烷氧基和三氟甲基的取代基取代的苯环; R 1是氢或C 1 -C 4烷基; R 2和R 3之一是氢，另一个是氢或任选地被H 5取代的C 1 -C 4烷基羟基或苯基; 或者R 2和R 3与它们所连接的碳原子一起形成C 3 -C 6环烷基环; 或R 2和R 3均为甲基; R 4为氢或C 1 -C 4烷基。

35. 发明授权

US06303819B1 Substituted 2-benzylamino-2-phenyl-acetamide compounds 失效
标题翻译：取代的2-苄基氨基-2-苯基 - 乙酰胺化合物
公开(公告)号：US06303819B1
公开(公告)日：2001-10-16
申请号：US09581254
申请日：2000-09-11
申请人： Paolo Pevarello , Mario Varasi , Patricia Salvati , Claes Post
发明人： Paolo Pevarello , Mario Varasi , Patricia Salvati , Claes Post
IPC分类号： C07C23305
CPC分类号： C07C237/20 , C07C2601/02
摘要： Compounds which are substituted 2-benzylamino-2-phenyl-acetamide compounds of formula (I) wherein: n is zero, 1, 2 or 3; X is —O—, —S—, —CH2— or —NH—; each of R, R1, R2 and R3, independently, is hydrogen, C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy or trifluoromethyl; each of R4 and R5, independently, is hydrogen, C1-C6 alkyl or C3-C7 cycloalkyl; or pharmaceutically acceptable salts thereof, are useful in treating conditions such as chronic or neuropathic pain.
摘要翻译：作为式（I）的取代的2-苄基氨基-2-苯基 - 乙酰胺化合物的化合物，其中：n为0,1,2或3; X为-O - ， - S - ， - CH 2 - 或-NH- R 1，R 2和R 3独立地是氢，C 1 -C 6烷基，卤素，羟基，C 1 -C 6烷氧基或三氟甲基; R 4和R 5各自独立地是氢，C 1 -C 6烷基或C 3 -C 7环烷基 ; 或其药学上可接受的盐可用于治疗诸如慢性或神经性疼痛的病症。

36. 发明授权

US5449692A Substituted (arylalkylaminobenzyl) aminopropionamide derivatives and process for their preparation 失效
标题翻译：取代的（芳基烷基氨基苄基）氨基丙酰胺衍生物及其制备方法
公开(公告)号：US5449692A
公开(公告)日：1995-09-12
申请号：US215694
申请日：1994-03-22
申请人： Mario Varasi , Philippe Dostert , Paolo Pevarello , Alberto Bonsignori
发明人： Mario Varasi , Philippe Dostert , Paolo Pevarello , Alberto Bonsignori
IPC分类号： A61K31/165 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07C231/10 , C07C237/06 , C07C233/05
CPC分类号： C07C237/06
摘要： The invention provides new compounds of formula (I) ##STR1## wherein n is an integer of 1 to 4; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R2 is hydrogen or C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable salts thereof; and wherein when, at the same time, R is hydrogen, R.sub.1 is hydrogen or halogen and n is one, then R.sub.2 is other than hydrogen or methyl; and of formula (IA) ##STR2## wherein R.sub.3 is halogen, and a pharmaceutical acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.
摘要翻译：本发明提供新的式（I）化合物其中n为1至4的整数; R和R 1可以相同或不同，为氢，卤素，三氟甲基或C 1 -C 4烷氧基; R2是氢或C1-C4烷基; 及其药学上可接受的盐; 并且其中当R同时为氢时，R 1为氢或卤素且n为1，则R 2为氢或甲基; 和式（IA）其中R 3是卤素的式（IA）及其药学上可接受的盐，其在中枢神经系统（CNS）上是有活性的，可用于治疗作为抗癫痫药，抗帕金森病，神经保护，抗抑郁药，抗痉挛药和催眠药。

37. 发明授权

US5236957A N-phenylalkyl substituted .alpha.-amino carboxamide derivatives and process for their preparation 失效
标题翻译：取代（α-氨基）氨基甲酰胺衍生物及其制备方法
公开(公告)号：US5236957A
公开(公告)日：1993-08-17
申请号：US646596
申请日：1991-01-25
申请人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
发明人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
IPC分类号： C07C237/06 , A61K31/16 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07C231/02 , C07C231/10 , C07C323/63 , C07D213/30 , C07D307/42 , C07D307/58 , C07D333/16 , C07D333/32
CPC分类号： C07D213/30 , C07C237/06 , C07C323/63 , C07D307/58 , C07D333/32
摘要： N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.

38. 发明申请

US20130245019A1 ACRYLOMIDO DERIVATIVES USEFUL AS INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION 有权
标题翻译：丙烯酰胺衍生物有助于作为MITOCHENDRIAL渗透性转换的抑制剂
公开(公告)号：US20130245019A1
公开(公告)日：2013-09-19
申请号：US13874081
申请日：2013-04-30
申请人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
发明人： Daniele Fancelli , Mario Varasi , Simon Plyte , Marco Ballarini , Anna Cappa , Giacomo Carenzi , Saverio Minucci , Gilles Pain , Manuela Villa
IPC分类号： C07C235/38 , C07D213/36 , C07D209/08 , C07D233/64 , C07D263/32 , C07C323/41 , C07D235/30 , C07D263/56 , C07D235/06 , C07D231/56 , C07D249/18 , C07D213/68 , C07D211/22 , C07D239/47 , C07D295/135 , C07D295/096 , C07D213/30
CPC分类号： C07C235/38 , C07C235/36 , C07C323/41 , C07C2601/04 , C07C2602/08 , C07D209/08 , C07D211/22 , C07D213/30 , C07D213/36 , C07D213/68 , C07D213/75 , C07D231/12 , C07D231/56 , C07D233/64 , C07D235/06 , C07D235/30 , C07D239/47 , C07D249/18 , C07D257/04 , C07D263/32 , C07D263/56 , C07D295/096 , C07D295/135 , C07D307/42
摘要： Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R′, R″, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
摘要翻译：可用作治疗剂的丙烯酰胺衍生物，特别是用于预防和/或治疗与线粒体通透性转换孔（MPTP）的活性相关的疾病和病症，例如以缺血/再灌注，氧化性或退行性组织损伤为特征的疾病，是在此描述。这些化合物属于结构式（I），其中R，R'，R“，W和a如说明书中所定义。本发明还涉及这些化合物的制备，以及包含它们的药物组合物。

39. 发明申请

US20090023745A1 Substituted Pyrazolo[4,3-c]Pyridine Derivatives Active as Kinase Inhibitors 有权
标题翻译：取代的吡唑并[4,3-c]吡啶衍生物作为激酶抑制剂
公开(公告)号：US20090023745A1
公开(公告)日：2009-01-22
申请号：US12096979
申请日：2006-12-06
申请人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
发明人： Tiziano Bandiera , Andrea Lombardi Borgia , Paolo Polucci , Manuela Villa , Marcella Nesi , Mauro Angiolini , Mario Varasi
IPC分类号： A61K31/496 , C07D471/04 , C07K14/71 , A61P35/00 , A61K31/437
CPC分类号： C07D471/04
摘要： Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.
摘要翻译：公开了如本说明书中定义的式（I）的吡唑并[4,3-c]吡啶衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病如癌症。

40. 发明申请

US20060135508A1 Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 审中-公开
标题翻译：作为激酶抑制剂活性的双环吡唑，其制备方法和包含它们的药物组合物
公开(公告)号：US20060135508A1
公开(公告)日：2006-06-22
申请号：US10522253
申请日：2003-07-16
申请人： Manuela Villa , Francesca Abrate , Daniele Fancelli , Mario Varasi , Anna Vulpetti
发明人： Manuela Villa , Francesca Abrate , Daniele Fancelli , Mario Varasi , Anna Vulpetti
IPC分类号： A61K31/55 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号： C07D487/04 , A61K31/415 , A61K45/06 , C07D471/04 , A61K2300/00
摘要： The present invention provides a method for treating diseases caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof an effective amount of a pyrrolo-pyrazole or pyrazolo-azepine. The invention also provides specific pyrrolo-pyrazoles and pyrazolo-azepines, useful intermediates, a library comprising at least two of them, a process for their preparation and the pharmaceutical compositions containing them, which are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.
摘要翻译：本发明提供了治疗由变化的蛋白激酶活性引起和/或与其相关的疾病的方法，其包括向有需要的哺乳动物施用有效量的吡咯并吡唑或吡唑并氮。本发明还提供特定的吡咯并吡唑和吡唑并氮杂，有用的中间体，包含其中至少两个的文库，其制备方法和含有它们的药物组合物，其可用于治疗由和/或与改变的蛋白激酶活性如癌症，细胞增殖性病症，病毒感染，自身免疫疾病和神经变性疾病有关。

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