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1. 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。

2. 发明授权

US06306903B1 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：US06306903B1
公开(公告)日：2001-10-23
申请号：US09582198
申请日：2000-08-29
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： A61K31275
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 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.
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。

3. 发明授权

US06303819B1 Substituted 2-benzylamino-2-phenyl-acetamide compounds 失效
标题翻译：取代的2-苄基氨基-2-苯基 - 乙酰胺化合物
公开(公告)号：US06303819B1
公开(公告)日：2001-10-16
申请号：US09581254
申请日：2000-09-11
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： C07C23305
CPC分类号： C07C237/20 , C07C2601/02
摘要： Compounds which are substituted 2-benzylamino-2-phenyl-acetamide compounds of formula (I) wherein: n is zero, 1, 2 or 3; X is —O—, —S—, —CH2— or —NH—; each of R, R1, R2 and R3, independently, is hydrogen, C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy or trifluoromethyl; each of R4 and R5, independently, is hydrogen, C1-C6 alkyl or C3-C7 cycloalkyl; or pharmaceutically acceptable salts thereof, are useful in treating conditions such as chronic or neuropathic pain.
摘要翻译：作为式（I）的取代的2-苄基氨基-2-苯基 - 乙酰胺化合物的化合物，其中：n为0,1,2或3; X为-O - ， - S - ， - CH 2 - 或-NH- R 1，R 2和R 3独立地是氢，C 1 -C 6烷基，卤素，羟基，C 1 -C 6烷氧基或三氟甲基; R 4和R 5各自独立地是氢，C 1 -C 6烷基或C 3 -C 7环烷基 ; 或其药学上可接受的盐可用于治疗诸如慢性或神经性疼痛的病症。

4. 发明申请

US20080171700A1 Use Of Secretagogue For The Teatment Of Ghrelin Deficiency 审中-公开
标题翻译：使用秘书处的Ghrelin缺乏症
公开(公告)号：US20080171700A1
公开(公告)日：2008-07-17
申请号：US11578135
申请日：2005-04-07
申请人： Henrik Nilsson , Birgitte Holst Lange , Claes Post , Tina Geritz Nielsen
发明人： Henrik Nilsson , Birgitte Holst Lange , Claes Post , Tina Geritz Nielsen
IPC分类号： A61K38/25 , A61P5/00 , A61P3/00 , A61P3/04
CPC分类号： A61K38/25
摘要： The present invention relates to the use of a growth hormone (GH) secretagogue, such as a ghrelin-like compound, for the preparation of a medicament for the prophylaxis or treatment of ghrelin deficiency, and/or undesirable symptoms associated therewith, in an individual at risk of acquiring partial or complete ghrelin deficiency resulting from a medical treatment and/or from a pathological condition. The present invention also relates to use of a secretagogue compound for the preparation of a medicament for the prophylaxis or treatment of one or more of: loss of fat mass, loss of lean body mass, weight loss, cachexia, loss of appetite, immunological dysfunction, malnutrition, disrupted sleep pattern, sleepiness, reduction in intestinal absorption and/or intestinal mobility problems in an individual suffering from, or at risk of suffering from, ghrelin deficiency. Furthermore, the present invention relates to the use of a secretagogue, such as a ghrelin-like compound, for the production of a medicament for preventing weight increase in an individual either: a) being converted from a hyperthyroidic state to euthyroid state, or b) in remission from being converted from a hyperthyroidic state to euthyroid state.
摘要翻译：本发明涉及生长激素（GH）促分泌素如生长素释放肽样化合物在个体中用于预防或治疗生长素释放肽缺乏症和/或与之相关的不良症状的药物的用途有获得由医疗和/或病理状况引起的部分或完全的生长素释放肽缺乏的风险。本发明还涉及促分泌素化合物在制备用于预防或治疗以下中的一种或多种的药物中的用途：脂肪量的损失，瘦体重的减少，体重减轻，恶病质，食欲不振，免疫功能障碍，营养不良，睡眠模式紊乱，困倦，减少肠道吸收和/或肠道运动问题，或者有遭受生长素释放肽缺乏症的个体。此外，本发明涉及促分泌素如生长素释放肽样化合物在制备用于预防个体体重增加的药物中的用途：a）从甲状腺功能亢进状态转变为甲状腺功能状态，或b ）缓解从甲状腺功能亢进状态转变为甲状腺功能状态。

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