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    • 1. 再颁专利
    • Alpha-aminoamide derivatives useful as analgesic agents
    • 用作止痛剂的α-氨基酰胺衍生物
    • USRE40259E1
    • 2008-04-22
    • US11359982
    • 1998-12-12
    • Paolo PevarelloMario VarasiPatricia SalvatiClaes Post
    • Paolo PevarelloMario VarasiPatricia SalvatiClaes Post
    • A61K31/275A61K31/165C07C255/50C07C233/05
    • C07C237/06A61K31/165C07C255/54
    • 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.
    • 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。
    • 2. 发明授权
    • Alpha-aminoamide derivatives useful as analgesic agents
    • 用作止痛剂的α-氨基酰胺衍生物
    • US06306903B1
    • 2001-10-23
    • US09582198
    • 2000-08-29
    • Paolo PevarelloMario VarasiPatricia SalvatiClaes Post
    • Paolo PevarelloMario VarasiPatricia SalvatiClaes Post
    • A61K31275
    • C07C237/06A61K31/165C07C255/54
    • 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.
    • 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。
    • 7. 发明授权
    • Imidazolylalkyl derivatives of imidazo�1,5-a!indol-3-one
    • 咪唑并[1,5-a]吲哚-3-酮的咪唑基烷基衍生物
    • US5874457A
    • 1999-02-23
    • US578550
    • 1996-01-24
    • Mario VarasiFranco HeidempergherCarla CacciaPatricia Salvati
    • Mario VarasiFranco HeidempergherCarla CacciaPatricia Salvati
    • A61K31/415A61K31/4188A61P1/00A61P1/08A61P1/12A61P25/06A61P25/18A61P25/22A61P25/28A61P25/36A61P43/00C07D487/04
    • C07D487/04Y02P20/55
    • Novel 5-HT.sub.3 receptor antagonist compounds having following formula (I) ##STR1## wherein n is 1, 2 or 3;each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N (R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7) N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group; and the pharmaceutically acceptable salts thereof, are disclosed.
    • PCT No.PCT / EP95 / 01651 Sec。 371日期:1996年1月24日 102(e)日期1996年1月24日PCT 1995年5月2日PCT PCT。 出版物WO95 / 32204 日期:1995年11月30日具有下式(I)的新型5-HT 3受体拮抗剂化合物其中n为1,2或3; R,R 1和R 2可以相同或不同,为氢,卤素,羟基,氰基,C 1 -C 6烷基,CF 3,C 1 -C 6烷氧基,C 1 -C 6烷硫基,甲酰基,C 2 -C 6烷酰基,羧基 ,其中R 4和R 5各自独立地为氢,C 1 -C 6烷基,甲酰基或C 2 -C 6烷酰基的C 1 -C 6烷氧羰基,硝基,-N(R 4 R 5) 或(R6R7)N-SO2基团,其中R6和R7各自独立地为氢或C1-C6烷基; R 3是式(I)的咪唑基,其中R 8和R 10各自可以相同或不同,是氢或C 1 -C 6烷基,R 9是氢,C 1 -C 6烷基或氮保护基; 及其药学上可接受的盐。
    • 9. 发明授权
    • Alpha-aminoamide derivatives useful in the treatment of cognitive disorders
    • 可用于治疗认知障碍的α-氨基酰胺衍生物
    • US08741957B2
    • 2014-06-03
    • US12304455
    • 2007-06-13
    • Patricia SalvatiStefano RossettiLuca Benatti
    • Patricia SalvatiStefano RossettiLuca Benatti
    • A61K31/165A61K31/404A61K31/085A61K31/135A61K31/341A61K31/402
    • A61K31/404A61K31/085A61K31/135A61K31/165A61K31/341A61K31/402
    • The present invention is in the field of pharmacotherapy of cognitive deficits in learning and memory by administering an α-aminoamide, particularly safinamide. Examples of disturbances in cognition that can be treated with compounds of the invention are the ones associated with disorders such as autism, dyslexia, attention deficit hyperactivity disorder, schizophrenia, obsessive compulsive disorders, psychosis, bipolar disorders, depression, Tourette's syndrome, Mild Cognitive Impairment (MCI) and disorders of learning in children, adolescents and adults, Age Associated Memory Impairment, Age Associated Cognitive Decline, Alzheimer's Disease, Parkinson's Disease, Down's Syndrome, traumatic brain injury Huntington's Disease, Progressive Supranuclear Palsy (PSP), HIV, stroke, vascular diseases, Pick's or Creutzfeldt-Jacob diseases, multiple sclerosis (MS), other white matter disorders and drug-induced cognitive worsening.
    • 本发明通过给予α-氨基酰胺,特别是safinamide,在学习和记忆中的认知缺陷的药物治疗领域。 可以用本发明化合物治疗的认知障碍的例子是与自闭症,阅读困难,注意缺陷多动障碍,精神分裂症,强迫症,精神病,双相情感障碍,抑郁症,Tourette综合征,轻度认知障碍 (MCI)和儿童,青少年和成年人学习障碍,年龄相关记忆障碍,年龄相关认知衰退,阿尔茨海默病,帕金森病,唐氏综合征,创伤性脑损伤亨廷顿病,进行性核核麻痹(PSP),艾滋病毒,中风, 血管疾病,Pick's或Creutzfeldt-Jacob疾病,多发性硬化症(MS),其他白质病症和药物诱导的认知恶化。