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1. 发明授权

US06716856B1 4,5,6,7-tetrahydroindazole derivatives as antitumor agents 失效
标题翻译： 4,5,6,7-四氢吲唑衍生物作为抗肿瘤剂
公开(公告)号：US06716856B1
公开(公告)日：2004-04-06
申请号：US09926478
申请日：2001-11-09
申请人： Paolo Pevarello , Manuela Villa , Mario Varasi , Antonella Isacchi
发明人： Paolo Pevarello , Manuela Villa , Mario Varasi , Antonella Isacchi
IPC分类号： A01N4340
CPC分类号： C07D401/04 , C07D231/56
摘要： Compounds which are 4,5,6,7-tetrahydroindazole derivative formula (1), wherein the dotted line (x) represents a single or double bond; n is 0 or 1; R1, R2 and R3 have the meanings reported in the description; Ra, R′a, Rb, R′b, Rc, R′c have the meanings reported in the description, also comprising that Ra and Rb together and/or Ra and Rc together form a N-alkylpiperydinyl ring with 1 to 6 carbon atoms in the alkyl chain or a phenyl ring; or pharmaceutically acceptable salts thereof, are useful for treating cell proliferative disorders and Alzheimer's disease.
摘要翻译：式（1）的4,5,6,7-四氢吲唑衍生物的化合物，其中虚线（x）表示单键或双键; n为0或1; R1，R2和R3具有说明书中报道的含义; Ra，R'a，Rb，R'b，Rc，R'c具有说明书中报道的含义，也包括Ra和Rb在一起和/或Ra和Rc一起形成具有1至6个碳原子的N-烷基哌啶基烷基链中的原子或苯环; 或其药学上可接受的盐可用于治疗细胞增殖性疾病和阿尔茨海默氏病。

2. 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。

3. 发明授权

US06784198B1 Arylmethyl-carbonylamino-thiazole derivatives and their use as antitumor agents 失效
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：US06784198B1
公开(公告)日：2004-08-31
申请号：US10048474
申请日：2002-07-18
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： A61K31425
CPC分类号： A61K31/426 , C07D277/46
摘要： 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): where R, R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof are useful as, for example, 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）或（II）表示的2-氨基-1,3-噻唑衍生物：其中R，R 1，R 2和R 3在本文中定义，或其药学上可接受的盐可用作例如癌症的治疗，细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫疾病或神经变性疾病。

4. 发明授权

US6114365A Arylmethyl-carbonylamino-thiazole derivatives, process for their preparation, and their use as antitumor agents 有权
标题翻译：芳基甲基 - 羰基氨基 - 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：US6114365A
公开(公告)日：2000-09-05
申请号：US372832
申请日：1999-08-12
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： 2-amino-1,3-thiazole derivatives represented by formula (I) or (II): ##STR1## where R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein, or pharmaceutically acceptable salts thereof, are useful in, for example, 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）或（II）表示的2-氨基-1,3-噻唑衍生物：其中R，R 1，R 2和R 3如本文所定义，或其药学上可接受的盐可用于例如癌症，细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫疾病或神经变性疾病。

5. 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。

6. 发明授权

US06455559B1 Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents 失效
标题翻译：苯乙酰氨基 - 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：US06455559B1
公开(公告)日：2002-09-24
申请号：US09907943
申请日：2001-07-19
申请人： Paolo Pevarello , Paolo Orsini , Gabriella Traquandi , Maria Gabriella Brasca , Raffaella Amici , Manuela Villa , Claudia Piutti , Mario Varasi , Antonio Longo
发明人： Paolo Pevarello , Paolo Orsini , Gabriella Traquandi , Maria Gabriella Brasca , Raffaella Amici , Manuela Villa , Claudia Piutti , Mario Varasi , Antonio Longo
IPC分类号： C07D26304
CPC分类号： C07D401/12 , C07D231/40 , C07D403/12 , C07D413/12
摘要： Compounds represented by formula (I) wherein R is a C3-C5 cycloalkyl group, R1 is a hydrogen atom or a methyl group, or a pharmaceutically acceptable salt thereof; are useful in the treatment of cell proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
摘要翻译：由式（I）表示的化合物，其中R是C 3 -C 5环烷基，R 1是氢原子或甲基，或其药学上可接受的盐; 可用于治疗细胞增殖性疾病，例如，与改变的细胞周期依赖性激酶活性相关的癌症。

7. 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。

8. 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。

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

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。

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