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1. 发明申请

US20120258949A1 SPIROCYCLIC DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 有权
标题翻译：螺旋体脱乙酰酶抑制剂的螺环衍生物
公开(公告)号：US20120258949A1
公开(公告)日：2012-10-11
申请号：US13446861
申请日：2012-04-13
申请人： Mario Varasi , Florian Thaler , Raffaella Amici , Agnese Abate , Maria Carmela Fulco , Saverio Minucci , Ciro Mercurio
发明人： Mario Varasi , Florian Thaler , Raffaella Amici , Agnese Abate , Maria Carmela Fulco , Saverio Minucci , Ciro Mercurio
IPC分类号： A61K31/407 , A61K31/438 , A61K31/55 , A61K31/397 , C07D498/10 , A61K31/537 , A61P35/00 , A61P25/00 , A61P29/00 , A61P31/00 , A61P11/00 , A61P37/00 , A61P9/00 , A61P21/00 , A61P17/06 , C07D491/107
CPC分类号： A61K31/397 , A61K31/407 , A61K31/438 , A61K31/537 , A61K31/55 , C07D491/107 , C07D498/10
摘要： This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C═R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
摘要翻译：本发明涉及根据通式（I）的新的组蛋白脱乙酰酶抑制剂，其中：m和n独立地为0或1至4的整数; p为0或1至3的整数，条件是当p为零时，n和m不能同时为1; R是氢; 任选被C 3 -C 8环烷基，C 6 -C 10芳基或杂（C 2 -C 9）芳基取代的C 1 -C 6烷基; （CO）R2; （SO2）R3; C3-C8环烷基; C6-C10芳基; 或杂（C 2 -C 9）芳基; R1是卤素，C1-C6烷基，C1-C6卤代烷基，C1-C6烷氧基，C1-C6卤代烷氧基; Y是CH 2或NR 4; Z为C = R5; R2，R3，R4和R5如说明书中进一步定义; 及其药学上可接受的盐。

2. 发明授权

US08173659B2 Substituted pyrazolo[4,3-C]pyridine derivatives active as kinase inhibitors 有权
标题翻译：作为激酶抑制剂活性的取代的吡唑并[4,3-C]吡啶衍生物
公开(公告)号：US08173659B2
公开(公告)日：2012-05-08
申请号：US13085889
申请日：2011-04-13
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 , 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。

3. 发明授权

US07531531B2 Method of treating diseases associated with altered kinase activity with bicyclo-pyrazoles 有权
标题翻译：用双环吡唑治疗与改变的激酶活性有关的疾病的方法
公开(公告)号：US07531531B2
公开(公告)日：2009-05-12
申请号：US11784980
申请日：2007-04-10
申请人： Daniele Fancelli , Valeria Pittalà , Mario Varasi
发明人： Daniele Fancelli , Valeria Pittalà , Mario Varasi
IPC分类号： A61K31/55 , A61K31/501 , A61K31/437 , A61K31/426
CPC分类号： C07D487/04 , C07D471/04 , C40B40/00
摘要： Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.
摘要翻译：如本文所定义的式（I）的双 - 吡唑化合物可用于治疗与失调的蛋白激酶相关的疾病。

4. 再颁专利

USRE40259E1 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：USRE40259E1
公开(公告)日：2008-04-22
申请号：US11359982
申请日：1998-12-12
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： A61K31/275 , A61K31/165 , C07C255/50 , C07C233/05
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 substituents 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特性，特别可用于治疗和缓解慢性和神经性疼痛。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）n - ， - （ CH 2 - （CH 2）n -X - 或 - （CH 2）2 -O - ，其中m是 1〜4的整数，n为0或1〜4的整数，X为-S-或-NH-，v为0或1〜5的整数。 s为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烷基的取代基取代的苯环，C C 1 -C 4烷氧基和三氟甲基; R 1是氢或C 1 -C 4烷基; R 2和R 3中的一个是氢，另一个是氢或任选地是C 1 -C 4 - 被羟基或苯基取代; 或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是氢或C 1 -C 4烷基。

5. 发明授权

US07141568B2 Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 有权
公开(公告)号：US07141568B2
公开(公告)日：2006-11-28
申请号：US10882493
申请日：2004-07-01
申请人： Daniele Fancelli , Barbara Forte , Jürgen Moll , Mario Varasi , Paola Vianello
发明人： Daniele Fancelli , Barbara Forte , Jürgen Moll , Mario Varasi , Paola Vianello
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , C07D413/14 , C07D403/14 , C07D211/18
CPC分类号： C07D487/04
摘要： Pyrrolo[3,4-c]pyrazole 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 disregulated protein kinase activity, like cancer.

6. 发明申请

US20050004120A1 Arylmethyl-carbonylamino-thiazole derivatives and their use as antitumor agents 审中-公开
标题翻译：芳基甲基 - 羰基氨基 - 噻唑衍生物及其作为抗肿瘤剂的用途
公开(公告)号：US20050004120A1
公开(公告)日：2005-01-06
申请号：US10902326
申请日：2004-07-29
申请人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
发明人： Paolo Pevarello , Raffaella Amici , Manuela Villa , Barbara Salom , Anna Vulpetti , Mario Varasi
IPC分类号： C07D277/20 , A61K20060101 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/5377 , A61P20060101 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/08 , A61P19/02 , A61P25/28 , A61P31/12 , A61P35/00 , A61P37/02 , C07D20060101 , C07D277/04 , C07D277/46 , C07D401/00 , C07D417/12 , C07D417/14
CPC分类号： A61K31/426 , C07D277/46
摘要： A method of modulating apoptosis or treating diseases associated with protein kinases by administering to a mammal in need thereof of an effective amount of 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): where R, R1, R2 and R3 are as defined herein, or pharmaceutically acceptable salts thereof.
摘要翻译：通过向有需要的哺乳动物施用有效量的由式（I）或（II）表示的2-氨基-1,3-噻唑衍生物来调节凋亡或治疗与蛋白激酶相关的疾病的方法：其中R，R 1 ，R2和R3如本文所定义，或其药学上可接受的盐。

7. 发明授权

US06414013B1 Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention 失效
标题翻译：噻吩化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US06414013B1
公开(公告)日：2002-07-02
申请号：US09596550
申请日：2000-06-19
申请人： Daniele Fancelli , Paolo Pevarello , Mario Varasi
发明人： Daniele Fancelli , Paolo Pevarello , Mario Varasi
IPC分类号： A61K3138
CPC分类号： C07D409/12 , C07D333/38 , C07D333/68 , C07D413/12 , C07D473/00 , C07D495/04
摘要： Compounds which are 3-aminocarbonyl-2-carboxamido-thiophene derivatives of formula (I): wherein R1 and R2 are, independently from each other, hydrogen, halogen or an optionally substituted group selected from aryl, straight or branched C1-C6 alkyl or aryl C1-C6 alkyl; or, taken together with the thiophene bond to which they are linked, R1 and R2 form a —(CH2)m—(NR4)n—(CH2)p— group wherein m and p are, each independently, an integer form 1 to 3, n is 0 or 1 and m+n+p is an integer from 3 to 5; and R4 is hydrogen or an optionally substituted straight or branched C1-C6 alkyl group; R3 is a group, optionally further substituted, selected from: i) straight or branched C1-C8 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C2-C6 alkylcarbonyl; ii) aryl; iii) 3 to 7 membered carbocycle; iv) 5 to 7 membered heterocycle with from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulphur; or a pharmaceutically acceptable salt thereof; are useful in the treatment of diseases associated with an altered protein kinase activity such as cancer, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders.
摘要翻译：作为式（I）的3-氨基羰基-2-甲酰氨基 - 噻吩衍生物的化合物：其中R 1和R 2彼此独立地为氢，卤素或任选取代的基团，其选自芳基，直链或支链C 1 -C 6烷基或芳基C1-C6烷基; 或者与它们所连接的噻吩键一起，R 1和R 2形成 - （CH 2）m - （NR 4）n - （CH 2）p - 基团，其中m和p各自独立地是1〜 3，n为0或1，m + n + p为3〜5的整数，且R 4为氢或任选取代的直链或支链C 1 -C 6烷基; R 3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烯基，C 2 -C 6炔基或C 2 -C 6烷基羰基; ii）芳基; iii）3至7元碳环; iv）具有1至3个选自氮，氧和硫的杂原子的5至7元杂环; 或其药学上可接受的盐; 可用于治疗与改变的蛋白激酶活性如癌症，阿尔茨海默病，病毒感染，自身免疫疾病和神经变性疾病相关的疾病。

8. 发明授权

US06316451B1 Heterocyclyl anthracyclinone derivatives 失效
标题翻译：杂环蒽环类衍生物
公开(公告)号：US06316451B1
公开(公告)日：2001-11-13
申请号：US09623859
申请日：2000-09-26
申请人： Sergio Mantegani , Gabriella Traquandi , Tiziano Bandiera , Jacqueline Lansen , Mario Varasi
发明人： Sergio Mantegani , Gabriella Traquandi , Tiziano Bandiera , Jacqueline Lansen , Mario Varasi
IPC分类号： C07D27742
CPC分类号： C07D417/04 , C07D233/88 , C07D277/40 , C07D277/42
摘要： A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy, R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.
摘要翻译：式（1）的化合物，其中R 1是氢，羟基，式OR 5的基团，其中R 5是C 1 -C 6烷基，C 2 -C 6烯基或C 3 -C 8环烷基，卤素，可被未被取代或被C1单或二取代的氨基 C 6烷基，C 2 -C 6烯基，芳烷基，酰基或三氟乙酰基; R 2是氢，羟基，NR 6 R 7基团，其中R 6和R 7独立地表示氢，任选取代的C 1 -C 6烷基，C 2 -C 6烯基，C 3 -C 8环烷基或与氮原子一起代表任选取代的C 3 -C 8 杂环 R3是氢，羟基，R4是2-取代的噻唑基或咪唑基系统及其药学上可接受的盐，可用于治疗淀粉样变性。还描述了制备方法和药物组合物。

9. 发明授权

US06218418B1 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents 失效
标题翻译： 3（5） - 氨基 - 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：US06218418B1
公开(公告)日：2001-04-17
申请号：US09667603
申请日：2000-09-22
申请人： Paolo Pevarello , Paolo Orsini , Gabriella Traquandi , Mario Varasi , Edward L. Fritzen , Martha A. Warpehoski , Betsy S. Pierce , Maria Gabriella Brasca
发明人： Paolo Pevarello , Paolo Orsini , Gabriella Traquandi , Mario Varasi , Edward L. Fritzen , Martha A. Warpehoski , Betsy S. Pierce , Maria Gabriella Brasca
IPC分类号： A61K31415
CPC分类号： C07D403/12 , A61K31/415 , A61K31/4155 , A61K45/06 , C07D231/16 , C07D231/40 , C07D405/12 , C07D409/12
摘要： Compounds which are 3-amino-pyrazole derivatives represented by formula (I): where R is a C3-C6 cycloalkyl group, which may optionally be substituted by a straight or branched C1-C6 alkyl group, and R1 is a straight or branched C1-C6 alkyl group or a C2-C4 alkenyl, cycloalkyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl and arylalkenyl, which may be optionally substituted; or a pharmaceutically acceptable salt thereof. The compounds are useful 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-氨基 - 吡唑衍生物的化合物：其中R是可以被直链或支链C1-C6烷基取代的C3-C6环烷基，R1是直链或支链C1-C6 烷基或C 2 -C 4烯基，环烷基，芳基，芳基烷基，芳基羰基，芳氧基烷基和芳基烯基，其可以任选被取代; 或其药学上可接受的盐。该化合物可用于治疗癌症，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。

10. 发明授权

US5973006A Fluoro-substituted benzoylpropionic acid derivatives 失效
标题翻译：氟取代的苯甲酰基丙酸衍生物
公开(公告)号：US5973006A
公开(公告)日：1999-10-26
申请号：US51486
申请日：1998-04-20
申请人： Mario Varasi , Antonio Giordani , Carmela Speciale , Massimo Cini , Alberto Bianchetti
发明人： Mario Varasi , Antonio Giordani , Carmela Speciale , Massimo Cini , Alberto Bianchetti
IPC分类号： A61K31/00 , A61K31/165 , A61K31/195 , A61K31/197 , A61K31/22 , A61P5/36 , A61P25/08 , A61P25/16 , A61P25/28 , C07C227/12 , C07C229/36 , C07C237/20 , C07C259/06 , A01N37/12 , A01N37/18 , C07C229/28 , C07C233/05
CPC分类号： C07C259/06 , C07C229/36 , C07C237/20
摘要： A fluoro-substituted benzoylpropionic acid compound of formula (I) either as a single optical isomer or as a mixture of optical isomers ##STR1## wherein R is hydroxy, amino, hydroxylamine, --OR', --NHR', N(R').sub.2 or --NHOR' in which R' is C.sub.1 -C.sub.6 alkyl or benzyl;or a pharmaceutically acceptable salt thereof.
摘要翻译： PCT No.PCT / EP96 / 04321 Sec。 371日期：1998年4月20日 102（e）1998年4月20日PCT PCT 1996年10月4日PCT公布。第WO97 / 15550号公报日期：1997年5月1日一种式（I）的氟取代的苯甲酰基丙酸化合物作为单一光学异构体或作为光学异构体的混合物，其中R是羟基，氨基，羟胺，-OR'，-NHR'，N（R' ）2或-NHOR'，其中R'是C 1 -C 6烷基或苄基; 或其药学上可接受的盐。

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