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53 条记录 (耗时 0.03 秒)

    Substituted (arylalkoxybenzyl)aminopropanamide derivatives and process for their preparation
    4.
    发明授权
    Substituted (arylalkoxybenzyl)aminopropanamide derivatives and process for their preparation 失效
    取代（芳基烷氧基苄基）氨基丙酰胺衍生物及其制备方法

    公开(公告)号：US5446066A

    公开(公告)日：1995-08-29

    申请号：US215628

    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 ,  C07C231/10 ,  C07C237/00 ,  C07C237/06 ,  C07C233/04

    CPC分类号： C07C237/00

    摘要： The invention provides new compounds of formula (I) ##STR1## wherein, subject to a proviso, n is zero or an integer of 1 to 3; 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; R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted by hydroxy; each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof; and of formula (IA) ##STR2## wherein R.sub.5 is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy, or a pharmaceutically 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，条件是n为0或1〜3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是氢或任选被羟基取代的C 1 -C 4烷基; R 3和R 4各自独立地是氢或C 1 -C 4烷基; 或其药学上可接受的盐; 和式（IA）的化合物（IA）其中R5是氢，卤素，三氟甲基或C1-C4烷氧基，或其药学上可接受的盐，其在中枢神经系统（CNS）上是有活性的并且可以用于治疗 作为抗癫痫药，抗帕金森综合征，神经保护药，抗抑郁药，抗痉挛药和催眠药。

    Substituted (arylalkylaminobenzyl) aminopropionamide derivatives and process for their preparation
    5.
    发明授权
    Substituted (arylalkylaminobenzyl) aminopropionamide derivatives and process for their preparation 失效
    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。

    Alpha-aminoamide derivatives useful as analgesic agents
    7.
    再颁专利
    Alpha-aminoamide derivatives useful as analgesic agents 有权
    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。

    Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
    9.
    发明授权
    Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention 失效
    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。