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11. 发明授权

US08084027B2 Combinations comprising a CDK inhibitor and a growth factor antibody or anti-mitotic 有权
标题翻译：包含CDK抑制剂和生长因子抗体或抗有丝分裂的组合
公开(公告)号：US08084027B2
公开(公告)日：2011-12-27
申请号：US12278530
申请日：2007-02-02
申请人： Ciro Mercurio , Enrico Pesenti , Maria Grazia Porro , Paolo Pevarello
发明人： Ciro Mercurio , Enrico Pesenti , Maria Grazia Porro , Paolo Pevarello
IPC分类号： A61K39/395
CPC分类号： A61K39/395 , A61K31/337 , A61K31/519 , A61K39/39558 , A61K2300/00
摘要： The present invention provides a combination comprising a compound A of formula (I) as set forth in the specification or a pharmaceutically acceptable salt thereof, and an antibody inhibiting a growth factor or its receptor and/or an antimitotic agent or a derivative or prodrug thereof, useful in the treatment of tumors. The chemical name of compound A is 8-[4-(4-methyl-piperazin-1-yl)-phenylamino]-1,4,4-trimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid methylamide.
摘要翻译：本发明提供了包含本说明书中阐述的式（I）化合物A或其药学上可接受的盐和抑制生长因子或其受体的抗体和/或抗有丝分裂剂或其衍生物或前药的组合，可用于治疗肿瘤。化合物A的化学名称是8- [4-（4-甲基 - 哌嗪-1-基） - 苯基氨基] -1,4,4-三甲基-4,5-二氢-1H-吡唑并[4,3-h ]喹唑啉-3-甲酸甲基酰胺。

12. 发明授权

US07037929B1 2-amino-thiazole derivatives, process for their preparation, and their use as antitumor agents 失效
标题翻译： 2-氨基 - 噻唑衍生物，其制备方法及其作为抗肿瘤剂的用途
公开(公告)号：US07037929B1
公开(公告)日：2006-05-02
申请号：US09807962
申请日：1999-10-27
申请人： Paolo Pevarello , Raffaella Amici , Gabriella Traquandi , Manuela Villa , Anna Vulpetti , Antonella Isacchi
发明人： Paolo Pevarello , Raffaella Amici , Gabriella Traquandi , Manuela Villa , Anna Vulpetti , Antonella Isacchi
IPC分类号： A61K31/426 , A61K31/495 , C07D277/20 , C07D413/02 , C07D417/02
CPC分类号： C07D417/12 , A61K31/426 , A61K31/427 , C07D277/46
摘要： Compounds which are 2-amino-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from i) straight or branched C1–C8 alkyl, C2–C6 alkenyl or C2–C6 alkynyl; ii) C3–C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; R1 is an optionally further substituted group selected from: i) straight or branched C1–C8 alkyl or C2–C6 alkenyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain; vi) an optionally protected amino acid residue; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.
摘要翻译：作为式（I）的2-氨基-1,3-噻唑衍生物的化合物，其中R是卤素原子，硝基，任选取代的氨基，或者是任选进一步取代的选自i）直链或支链C 1 -C 8烷基，C 2 -C 6亚烯基或C 2 -C 6亚烷基， C 6 -C 6炔基; ii）C 3 -C 6环烷基; iii）在直链或支链烷基链中具有1至8个碳原子的芳基或芳基烷基; R 1是任选进一步取代的基团，其选自：i）直链或支链C 1 -C 8烷基或C 2 - / C 1 -C 6链烯基; ii）3至6元碳环或5至7元杂环; iii）芳基或芳基羰基; iv）在直链或支链烷基链中具有1至8个碳原子的芳基烷基; v）直链或支链烯基链中具有2至6个碳原子的芳基烯基; vi）任选保护的氨基酸残基; 或其药学上可接受的盐; 可用于治疗与改变的细胞依赖性激酶活性相关的细胞增殖性疾病。

13. 发明申请

US20050176796A1 Tricyclic pyrazole derivatives, process for their preparation and their use as antitumor agents 审中-公开
标题翻译：三环吡唑衍生物，其制备方法及其作为抗肿瘤剂的用途
公开(公告)号：US20050176796A1
公开(公告)日：2005-08-11
申请号：US10505200
申请日：2003-02-18
申请人： Roberto D'Alessio , Alberto Bargiotti , Maria Brasca , Antonella Ermoli , Paolo Pevarello , Marcellino Tibolla
发明人： Roberto D'Alessio , Alberto Bargiotti , Maria Brasca , Antonella Ermoli , Paolo Pevarello , Marcellino Tibolla
IPC分类号： C07D231/54 , A61K31/415 , A61K31/4162 , A61K31/4439 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K31/551 , A61K45/00 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/08 , A61P13/12 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/28 , A61P31/12 , A61P35/00 , A61P35/04 , A61P37/06 , A61P43/00 , C07D403/04 , C07D403/06 , C07D413/04 , C07D471/04 , C07D471/14 , C07D471/22 , C07D487/04 , C07D487/14 , C07D495/04 , C07D498/14 , A61K31/4188
CPC分类号： C07D403/04 , A61K31/415 , C07D231/54 , C07D403/06 , C07D413/04 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D495/04
摘要： Compounds which are tricyclic pyrazole derivatives and analogues thereof, as set forth in the specification, or pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them 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：公开了如说明书中所述的三环吡唑衍生物及其类似物或其药学上可接受的盐以及包含它们的药物组合物的化合物。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。

14. 发明授权

US06863647B2 2-Ureido-thiazole derivatives, process for their preparation, and their use as antitumor agents 失效
标题翻译： 2-脲基 - 噻唑衍生物，其制备方法及其作为抗肿瘤剂的用途
公开(公告)号：US06863647B2
公开(公告)日：2005-03-08
申请号：US09830668
申请日：1999-10-27
申请人： Paolo Pevarello , Raffaella Amici , Gabriella Traquandi , Manuela Villa , Anna Vulpetti , Antonella Isacchi
发明人： Paolo Pevarello , Raffaella Amici , Gabriella Traquandi , Manuela Villa , Anna Vulpetti , Antonella Isacchi
IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/498 , A61K31/5377 , A61K31/55 , A61K31/551 , A61P9/10 , A61P11/00 , A61P13/08 , A61P13/12 , A61P17/06 , A61P19/02 , A61P25/28 , A61P31/12 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/00 , A61P43/00 , C07D277/44 , C07D277/48 , C07D277/62 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D491/10 , C07D877/48
CPC分类号： C07D277/62 , C07D277/48 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D491/10
摘要： Compounds which are 2-ureido-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group optionally further substituted, selected from: i) straight or branched C1-C6 alkyl; ii) C3-C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R1 is an optionally substituted group selected from: i) straight or branched C1-C6 alkyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R2 is hydrogen, a straight or branched C1-C6 alkyl or C2-C4 alkenyl or alkynyl group; or, taken together with the nitrogen atom so which they are bonded, R1 and R2 form a substituted or unsubstituted group selected from: i) an optionally benzocondensed or bridged 5 to 7 membered heterocycle; or ii) a 9 to 11 membered spiro-heterocyclic compound; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.
摘要翻译：作为式（I）的2-脲基-1,3-噻唑衍生物的化合物，其中R是卤素原子，硝基，任选取代的氨基，或者是任选进一步取代的基团，其选自：i）直链或支链C 1 -C 6烷基; ii）C 3 -C 6环烷基; iii）在直链或支链烷基链中具有1至6个碳原子的芳基或芳基烷基; R1是任选取代的基团，其选自：i）直链或支链C 1 -C 6烷基; ii）3至6元碳环或5至7元杂环; iii）芳基或芳基羰基; iv）在直链或支链烷基链中具有1至6个碳原子的芳基烷基; R2是氢，直链或支链C1-C6烷基或C2-C4烯基或炔基; 或者与它们所键合的氮原子一起，R1和R2形成取代或未取代的基团，其选自：i）任选苯并稠合或桥连的5至7元杂环; 或ii）9至11元螺 - 杂环化合物; 或其药学上可接受的盐; 可用于治疗与改变的细胞依赖性激酶活性相关的细胞增殖性疾病。

15. 发明授权

US06323240B1 4-phenyl-4-oxo-butanoic acid derivatives with kynurenine-3-hydroxylase inhibiting activity 失效
标题翻译：具有犬尿氨酸-3-羟化酶抑制活性的4-苯基-4-氧代 - 丁酸衍生物
公开(公告)号：US06323240B1
公开(公告)日：2001-11-27
申请号：US09068016
申请日：1998-05-01
申请人： Antonio Giordani , Paolo Pevarello , Carmela Speciale , Mario Varasi
发明人： Antonio Giordani , Paolo Pevarello , Carmela Speciale , Mario Varasi
IPC分类号： A61K31195
CPC分类号： C07C59/90 , C07C69/738 , C07C205/56
摘要： 4-phenyl-4-oxo-butanoic acid derivatives for use in the treatment of the human or animal body by therepy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enyzme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butanoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.
摘要翻译： 4-苯基-4-氧代 - 丁酸衍生物，用于通过该药物治疗人体或动物体; 特别是作为犬尿氨酸-3-羟化酶抑制剂，在预防和/或治疗需要抑制这种乙烯的神经变性疾病中。本发明还包括所选类别的上述4-苯基-4-氧代 - 丁酸衍生物，其药学上可接受的盐，其制备方法和含有它们的药物组合物。

16. 发明授权

US6133302A 5-(3-Phenyl-3-oxo-propyl)-1H-tetrazole derivatives 失效
标题翻译： 5-（3-苯基-3-氧代 - 丙基）-1H-四唑衍生物
公开(公告)号：US6133302A
公开(公告)日：2000-10-17
申请号：US446895
申请日：1999-12-30
申请人： Paolo Pevarello , Antonio Giordani , Manuela Villa , Carmela Speciale , Mario Varasi
发明人： Paolo Pevarello , Antonio Giordani , Manuela Villa , Carmela Speciale , Mario Varasi
IPC分类号： A61K31/41 , A61P25/00 , A61P43/00 , C07D257/04
CPC分类号： C07D257/04
摘要： 5-(3-phenyl-3-oxo-propyl)-1H-tetrazole derivatives of formula (I) wherein each of R and R.sub.1, being the same or different, is hydrogen, halogen, hydroxy, trifluoromethyl, cyano, nitro, phenyl, benzyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, SOR.sub.4 or SO.sub.2 R.sub.4 wherein R.sub.4 is C.sub.1 -C.sub.6 alkyl, --N(R.sub.5 R.sub.6) in which each of R.sub.5 and R.sub.6 is, independently, hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 acyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, benzyl, phenyl; R.sub.3 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, benzyl, phenyl or a group --N(R.sub.7 R.sub.8) in which each of R.sub.7 and R.sub.8 is, independently, hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl, phenyl, or one of R.sub.7 and R.sub.8 is hydrogen and the other is COR.sub.9 wherein R.sub.9 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl or a group --N(R.sub.10 R.sub.11) in which R.sub.10 and R.sub.11 are, each independently, hydrogen or C.sub.1 -C.sub.4 alkyl or, taken together, R.sub.2 and R.sub.3 form a carbocyclic C.sub.3 -C.sub.6 ring; and pharmaceutically acceptable salts thereof have kynurenine-3-hydroxylase enzyme inhibitory activity. ##STR1##
摘要翻译： PCT No.PCT / EP98 / 04032 Sec。 371 1999年12月30日第 102（e）1999年12月30日PCT PCT。1998年6月25日PCT公布。公开号WO99 / 02506 日本1月21日，19995-（3-苯基-3-氧代 - 丙基）-1H-四唑衍生物，其中R和R 1相同或不同，为氢，卤素，羟基，三氟甲基，氰基，硝基，苯基，苄基，C1-C6烷基，C1-C6烷氧基，C1-C6烷硫基，SOR4或SO2R4，其中R4是C1-C6烷基，-N（R5R6），其中R5和R6各自独立地为氢，C 1 -C 6烷基，甲酰基或C 2 -C 6酰基; R2是氢，C1-C6烷基，C1-C6烷氧基，苄基，苯基; R3是氢，羟基，C1-C6烷基，C1-C6烷氧基，苄基，苯基或基团-N（R7R8），其中R7和R8各自独立地是氢，C1-C4烷基，苄基，苯基或 R 7和R 8中的一个是氢，另一个是COR 9，其中R 9是氢，C 1 -C 4烷基，C 1 -C 4烷氧基，苯基或基团-N（R 10 R 11），其中R 10和R 11各自独立地是氢或C1- C4烷基或一起为R2和R3形成碳环C 3 -C 6环; 及其药学上可接受的盐具有犬尿氨酸-3-羟化酶抑制活性。

17. 发明授权

US6048896A 4-phenyl-4-oxo-2-butenoic acid derivatives with kynurenine-3-hydroxylase inhibiting activity 失效
标题翻译：具有犬尿氨酸-3-羟化酶抑制活性的4-苯基-4-氧代-2-丁烯酸衍生物
公开(公告)号：US6048896A
公开(公告)日：2000-04-11
申请号：US68103
申请日：1998-05-04
申请人： Antonio Giordani , Paolo Pevarello , Carmela Speciale , Mario Varasi
发明人： Antonio Giordani , Paolo Pevarello , Carmela Speciale , Mario Varasi
IPC分类号： C07C59/185 , A61K31/00 , A61K31/19 , A61K31/192 , A61P5/36 , A61P25/28 , A61P27/00 , A61P27/02 , A61P43/00 , C07C59/205 , C07C59/21 , C07C59/215 , C07C59/88 , C07C69/738 , C07C205/56 , A01N37/10 , C07C69/76
CPC分类号： C07C205/56 , C07C59/88 , C07C69/738
摘要： 4-Phenyl-4-oxo-butenoic acid derivatives for use in the treatment of the human or animal body by therapy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enzyme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butenoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.
摘要翻译： PCT No.PCT / EP96 / 04517 371日期：1998年5月4日 102（e）日期1998年5月4日PCT提交1996年10月16日PCT公布。公开号WO97 / 17316 PCT 日期：19974年5月15日 - 苯基-4-氧代 - 丁烯酸衍生物，用于治疗人体或动物体; 特别是作为犬尿氨酸-3-羟化酶抑制剂，在预防和/或治疗需要抑制这种酶的神经变性疾病中。本发明还包括所选类别的上述4-苯基-4-氧代 - 丁烯酸衍生物，其药学上可接受的盐，其制备方法和含有它们的药物组合物。

18. 发明授权

US5945454A 2-(4-substituted)-benzylamino-2-methyl-propanamide derivatives 失效
标题翻译： 2-（4-取代） - 苄基氨基-2-甲基 - 丙酰胺衍生物
公开(公告)号：US5945454A
公开(公告)日：1999-08-31
申请号：US981492
申请日：1998-01-08
申请人： Paolo Pevarello , Raffaella Amici , Mario Varasi , Alberto Bonsignori , Patricia Salvati
发明人： Paolo Pevarello , Raffaella Amici , Mario Varasi , Alberto Bonsignori , Patricia Salvati
IPC分类号： A61K31/00 , A61K31/16 , A61K31/165 , A61P25/16 , A61P25/20 , A61P25/24 , C07C231/12 , C07C237/06 , C07C321/30 , C07C323/32 , C07C323/36 , C07C233/05
CPC分类号： C07C237/06 , C07C323/36
摘要： Novel 2(4-substituted)-benzylamino-2-methyl-propanamides compounds, having CNS activity, of general formula (I) wherein: n is zero, 1, 2 or 3; X is --O--, --S--, --CH.sub.2 -- or --NH--; each of R and R.sub.1 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, C.sub.1 -C.sub.4 alkoxy or trifluoromethyl; each of R.sub.2, R.sub.3 and R.sub.4 independently is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.7 cycloalkyl; and the pharmacetically acceptable salts thereof, are disclosed. ##STR1##
摘要翻译： PCT No.PCT / EP96 / 02961 Sec。 371日期1998年1月8日 102（e）1998年1月8日PCT PCT 1996年7月5日PCT公布。出版物WO97 / 05102 PCT 日期1997年2月13日具有通式（I）的CNS活性的新型2（4-取代） - 苄基氨基-2-甲基 - 丙酰胺化合物，其中：n为0,1,2或3; X是-O - ， - S - ， - CH 2 - 或-NH-; R和R 1各自独立地是氢，C 1 -C 6烷基，卤素，羟基，C 1 -C 4烷氧基或三氟甲基; R2，R3和R4各自独立地为氢，C1-C6烷基或C3-C7环烷基; 及其药物可接受的盐。

19. 发明授权

US5502079A N-phenylalkyl substituted .alpha.-amino carboxamide derivatives and process for their preparation 失效
公开(公告)号：US5502079A
公开(公告)日：1996-03-26
申请号：US343853
申请日：1994-11-17
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 , A61K31/165
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.

20. 发明授权

US08557857B2 Substituted pyrrolo-pyrazole derivatives as kinase inhibitors 有权
公开(公告)号：US08557857B2
公开(公告)日：2013-10-15
申请号：US12181772
申请日：2008-07-29
申请人： Maria Gabriella Brasca , Raffaella Amici , Daniele Fancelli , Marcella Nesi , Paolo Orsini , Fabrizio Orzi , Patrick Roussel , Anna Vulpetti , Paolo Pevarello
发明人： Maria Gabriella Brasca , Raffaella Amici , Daniele Fancelli , Marcella Nesi , Paolo Orsini , Fabrizio Orzi , Patrick Roussel , Anna Vulpetti , Paolo Pevarello
IPC分类号： A61K31/4162 , C07D487/02
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , A61N5/10
摘要： Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.

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