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81. 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。

82. 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。

83. 发明授权

US06207709B1 N-substituted-2-amino-4-phenyl-4-oxo-butanoic acid compounds having kynurenine-3-hydroxy base inhibitory activity 失效
标题翻译：具有犬尿氨酸-3-羟基抑制活性的N-取代-2-氨基-4-苯基-4-氧代 - 丁酸化合物
公开(公告)号：US06207709B1
公开(公告)日：2001-03-27
申请号：US09147722
申请日：1999-02-24
申请人： Mario Varasi , Antonio Giordani , Massimo Cini , Carmela Speciale , Alberto Bianchetti
发明人： Mario Varasi , Antonio Giordani , Massimo Cini , Carmela Speciale , Alberto Bianchetti
IPC分类号： A01N3712
CPC分类号： C07C233/47 , C07C311/06
摘要： An N-substituted-2-amino-4-phenyl-4-oxo-butanoic acid compound of the formula (I): wherein X, Y, W and R are as defined herein.
摘要翻译：式（I）的N-取代-2-氨基-4-苯基-4-氧代 - 丁酸化合物：其中X，Y，W和R如本文所定义。

84. 发明授权

US6060483A Antineurodegenerative ergoline derivatives 失效
标题翻译：抗神经变性麦角灵衍生物
公开(公告)号：US6060483A
公开(公告)日：2000-05-09
申请号：US147448
申请日：1998-12-28
申请人： Sergio Mantegani , Enzo Brambilla , Nicola Carfagna , Mario Varasi
发明人： Sergio Mantegani , Enzo Brambilla , Nicola Carfagna , Mario Varasi
IPC分类号： A61K31/48 , C07D457/02 , C07D457/10
CPC分类号： C07D457/10 , A61K31/48 , C07D457/02
摘要： The present invention provides the new use in the treatment of neurodegenerative diseases with ergoline derivatives of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or C.sub.2 -C.sub.5 alkenyl group optionally substituted with a C.sub.3 -C.sub.7 cycloalkyl, a hydroxy group or a R.sub.3 -substituted phenyl group wherein R.sub.3 is a hydroxy or a hydroxymethyl group; R.sub.2 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or a C.sub.2 -C.sub.5 alkenyl group optionally substituted with a hydroxy group, or a R.sub.3 -substituted phenyl group wherein R.sub.3 is as above defined, or with a C.sub.1 -C.sub.5 alkoxy group; the symbols--at positions 2,3 and 8, 9 independently denote a single or double chemical bond and Z represents a group (CH.sub.2).sub.n OH, wherein n is 0 or an integer from 1 to 3, or a group C(R.sub.4).sub.2 OH wherein R.sub.4 is a C.sub.1 -C.sub.5 alkyl or a phenyl group, or a pharmaceutically acceptable salt thereof. Some compounds of formula (I) are novel. Processes for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译： PCT No.PCT / EP97 / 02955 Sec。 371日期1998年12月28日第 102（e）日期1998年12月28日PCT提交1987年5月29日PCT公布。第WO98 / 00424号公报日本1998年1月8日本发明提供了用于治疗神经变性疾病的新用途，其中式（I）的麦角灵衍生物其中R 1表示氢原子或直链或支链C 1 -C 5烷基或C 2 -C 5烯基，任选被 C3-C7环烷基，羟基或R3-取代的苯基，其中R3是羟基或羟甲基; R2表示氢原子或任选被羟基取代的直链或支链C 1 -C 5烷基或C 2 -C 5烯基，或其中R 3如上所定义的R 3取代苯基，或与C 1 -C 5烷氧基 ; 位置2,3和8,9独立地表示单一或双重化学键，Z表示基团（CH 2）n OH，其中n为0或1至3的整数，或基团C（R 4）2 OH 其中R4是C1-C5烷基或苯基，或其药学上可接受的盐。一些式（I）化合物是新的。还描述了其制备方法和含有它们的药物组合物。

85. 发明授权

US5968955A Disubstituted piperidine derivatives as neuroprotective agents 失效
标题翻译：二取代哌啶衍生物作为神经保护剂
公开(公告)号：US5968955A
公开(公告)日：1999-10-19
申请号：US43906
申请日：1998-03-31
申请人： Sergio Mantegani , Tiziano Bandiera , Manuela Villa , Mario Varasi , Carmela Speciale
发明人： Sergio Mantegani , Tiziano Bandiera , Manuela Villa , Mario Varasi , Carmela Speciale
IPC分类号： A61K31/00 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61P25/00 , A61P25/04 , C07D413/06
CPC分类号： C07D413/06
摘要： A Disubstituted piperidine compounds of formula (I), wherein R.sub.1 is hydrogen; bromo; chloro; a linear or branched C.sub.1 -C.sub.5 alkyl group; a linear or branched C.sub.1 -C.sub.5 alkoxy group; or an optionally substituted phenyl group; R.sub.2 is hydrogen, a linear or branched C.sub.1 -C.sub.5 alkyl group or an optionally substituted phenyl group; X is CH.sub.2, C.dbd.O, CHOH or C.dbd.NOH; R.sub.3 is hydrogen or a linear or branched C.sub.1 -C.sub.5 alkyl group; Y is a (CH.sub.2).sub.n group in which n is an integer from 0 to 4, CHOH, C.dbd.O or CH-A wherein A is an optionally substituted phenyl group; A is an optionally substituted phenyl group; W is hydrogen or hydroxy; stereoisomers thereof and their pharmaceutically acceptable salts. The compounds possess selective neuroprotective activity and are useful in the treatment of an acute or a degenerative CNS disease. A process is described for preparing the compounds and pharmaceutical compositions containing them.
摘要翻译： PCT No.PCT / EP95 / 04075第 371日期1998年3月31日 102（e）1998年3月31日PCT PCT 1996年9月16日PCT公布。公开号WO97 / 13769 日期1997年4月17日A式（I）的二取代哌啶化合物，其中R 1是氢; 溴氯直链或支链C 1 -C 5烷基; 直链或支链C 1 -C 5烷氧基; 或任选取代的苯基; R2是氢，直链或支链C1-C5烷基或任意取代的苯基; X是CH 2，C = O，CHOH或C = NOH; R3是氢或直链或支链C1-C5烷基; Y为（CH 2）n基团，其中n为0至4的整数，CHOH，C = O或CH-A，其中A为任选取代的苯基; A是任选取代的苯基; W是氢或羟基; 其立体异构体及其药学上可接受的盐。该化合物具有选择性神经保护活性，可用于治疗急性或退行性CNS疾病。描述了制备含有它们的化合物和药物组合物的方法。

86. 发明授权

US5708030A Substituted kynurenines and process for their preparation 失效
标题翻译：替代的犬尿苷及其制备方法
公开(公告)号：US5708030A
公开(公告)日：1998-01-13
申请号：US463895
申请日：1995-06-05
申请人： Robert Schwarcz , Mario Varasi , Arturo Della Torre , Carmela Speciale , Alberto Bianchetti
发明人： Robert Schwarcz , Mario Varasi , Arturo Della Torre , Carmela Speciale , Alberto Bianchetti
IPC分类号： A61K31/00 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/216 , C07C229/36 , C07C233/43 , C07C233/44 , C07C235/10 , A61K31/12 , A61K31/44 , A61K33/18
CPC分类号： C07C229/36 , A61K31/00 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/216 , C07C2101/08
摘要： The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).
摘要翻译：本发明涉及用于治疗与脑衰老过程相关的认知障碍和围产期脑疾病的化合物的用途，所述化合物作为犬尿氨酸转氨酶（KAT）酶的抑制剂。

87. 发明授权

US5519055A Substituted kynurenines and process for their preparation 失效
标题翻译：替代的犬尿苷及其制备方法
公开(公告)号：US5519055A
公开(公告)日：1996-05-21
申请号：US102843
申请日：1993-08-06
申请人： Robert Schwarcz , Mario Varasi , Arturo Della Torre , Carmela Speciale , Alberto Bianchetti
发明人： Robert Schwarcz , Mario Varasi , Arturo Della Torre , Carmela Speciale , Alberto Bianchetti
IPC分类号： A61K31/00 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/216 , C07C229/36 , C07C233/43 , C07C233/44 , C07C235/10 , A61K31/24 , C07C229/00
CPC分类号： C07C229/36 , A61K31/00 , A61K31/165 , A61K31/195 , A61K31/198 , A61K31/215 , A61K31/216 , C07C2101/08
摘要： The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, andR.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, mono-C.sub.1 -C.sub.6 alkylamino, di-C.sub.1 -C.sub.6 alkylamino, hydroxylamino, C.sub.1 -C.sub.4 alkoxyamino or benzyloxyamino; with the provisos that(i) when R.sub.1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and(ii) when R.sub.1 is hydroxy and, at the same time, R is C.sub.1 -C.sub.6 alkyl, then this C.sub.1 -C.sub.6 alkyl is not methyl, and the pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及用于治疗与脑衰老过程相关的认知障碍和围产期脑疾病的化合物的用途，所述化合物作为犬尿氨酸转氨酶（KAT）酶的抑制剂。本发明还提供作为新化合物的选定类别的KAT抑制剂，其是式（IA）化合物其中R是卤素，C 1 -C 6烷基，C 5 -C 7环烷基，苯基-C 1 -C 6烷基， C4烷基，C1-C6烷氧基，C6-C10芳氧基，苯基-C1-C4烷氧基或三氟甲基，R1为羟基，C1-C6烷氧基，氨基，单C1-C6烷基氨基，二C1-C6烷基氨基， C1-C4烷氧基氨基或苄氧基氨基; 条件是（i）当R 1是羟基，同时R是卤素时，该卤素不是氟; 和（ii）当R 1是羟基，并且同时R是C 1 -C 6烷基时，则该C 1 -C 6烷基不是甲基，及其药学上可接受的盐。

88. 发明授权

US5449692A Substituted (arylalkylaminobenzyl) aminopropionamide derivatives and process for their preparation 失效
标题翻译：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。

89. 发明授权

US5236957A N-phenylalkyl substituted .alpha.-amino carboxamide derivatives and process for their preparation 失效
标题翻译：取代（α-氨基）氨基甲酰胺衍生物及其制备方法
公开(公告)号：US5236957A
公开(公告)日：1993-08-17
申请号：US646596
申请日：1991-01-25
申请人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
发明人： Philippe Dostert , Paolo Pevarello , Franco Heidempergher , Mario Varasi , Alberto Bonsignori , Romeo Roncucci
IPC分类号： C07C237/06 , A61K31/16 , A61K31/33 , A61K31/34 , A61K31/341 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07C231/02 , C07C231/10 , C07C323/63 , C07D213/30 , C07D307/42 , C07D307/58 , C07D333/16 , C07D333/32
CPC分类号： C07D213/30 , C07C237/06 , C07C323/63 , C07D307/58 , C07D333/32
摘要： N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.

90. 发明授权

US5229383A Piperazine-substituted 1,4-benzoxazine derivatives and their use in treating disorders of the central nervous system 失效
标题翻译：哌嗪取代的1,4-苯并恶嗪衍生物及其在治疗中枢神经系统疾病中的应用
公开(公告)号：US5229383A
公开(公告)日：1993-07-20
申请号：US748221
申请日：1991-08-20
申请人： Mario Varasi , Piero Melloni , Maria A. Cervini , Alberto Bonsignori , Roberto Commisso
发明人： Mario Varasi , Piero Melloni , Maria A. Cervini , Alberto Bonsignori , Roberto Commisso
IPC分类号： C07D265/36 , C07D279/16 , C07D471/10
CPC分类号： C07D471/10 , C07D265/36 , C07D279/16
摘要： The present invention relates to compounds having the following formula (I) ##STR1## wherein X represents --O-- or --S--;each of R and R.sub.1, independently, is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, amino, nitro or trihalo-C.sub.1 -C.sub.6 alkyl;each of R.sub.2 and R.sub.3, independently, is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or phenyl-C.sub.1 -C.sub.6 alkyl; or R.sub.2 and R.sub.3, taken together with the nitrogen atom to which they are linked, form an unsubstituted or substituted, 6-membered, saturated, heteromonocyclic ring optionally containing a further heteroatom chosen from oxygen, sulphur and nitrogen;each of R.sub.4 and R.sub.5, independently, is hydrogen, halogen, nitro, amino or trihalo-C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful in therapy as major tranquilizers e.g., in the management of psychotic disorders.
摘要翻译：本发明涉及具有下式（I）的化合物：其中X表示-O-或-S-; R和R 1各自独立地是氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，氨基，硝基或三卤代-C 1 -C 6烷基; R 2和R 3各自独立地是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或苯基-C 1 -C 6烷基; 或R 2和R 3与它们所连接的氮原子一起形成任选含有另外选自氧，硫和氮的杂原子的未取代或取代的6元饱和的杂单环; R 4和R 5各自独立地是氢，卤素，硝基，氨基或三卤代-C 1 -C 6烷基; 及其药学上可接受的盐。本发明的化合物可用于作为主要镇静剂的治疗，例如在精神病性障碍的治疗中。

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