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11. 发明授权

US5604245A Use of 4-amino-1-(2-pyridyl)piperidines for the preparation of a medicament for the treatment of conditions deriving from disorders of the serotoninergic systems mediated by 5-HT.sub.3 receptors 失效
标题翻译： 4-氨基-1-（2-吡啶基）哌啶用于制备用于治疗由5-HT 3受体介导的血清素能系统的病症的病症的药物的用途
公开(公告)号：US5604245A
公开(公告)日：1997-02-18
申请号：US858483
申请日：1992-03-27
申请人： G erard Le Fur , Alberto Bianchetti , Antonina Giudice , Tiziano Croci , Philippe Soubrie
发明人： G erard Le Fur , Alberto Bianchetti , Antonina Giudice , Tiziano Croci , Philippe Soubrie
IPC分类号： C07D401/04 , A61K31/44 , A61K31/4427 , A61K31/445 , A61P1/00 , A61P1/10 , A61P25/00 , A61P25/18 , A61P25/20 , A61P43/00
CPC分类号： A61K31/445 , A61K31/44
摘要： The present invention concerns the use of 4-amino-1-(2-pyridyl)piperidines of general formula (I') ##STR1## wherein R' represents hydrogen, a halogen atom, a methyl, methylthio, trifluoromethyl, trifluoromethylthio, (C.sub.1 -C.sub.3)alkoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, or phenoxy group optionally substituted with a halogen atom, a trifluoromethyl, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.3)alkylthio, or cyano group, or of a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment or prophylaxis of those conditions deriving from disorders of the serotoninergic systems wherein a serotoninergic action selectively mediated by the 5-HT.sub.3 receptors is required, e.g. affective disorders, anxiety, psychotic troubles, constipation.
摘要翻译：本发明涉及通式（I'）卤素原子的4-氨基-1-（2-吡啶基）哌啶，甲基，甲硫基，三氟甲基，三氟甲硫基，（C 1 -C 3）烷氧基，三氟甲氧基，2,2 ，（C 3 -C 3）烷基，（C 1 -C 3）烷氧基，（C 1 -C 3）烷硫基或氰基，或其药学上可接受的盐，任选被卤素原子取代的2-三氟乙氧基或苯氧基，用于制备用于治疗或预防源自5-羟色胺能系统疾病的那些病症的药物，其中需要由5-HT 3受体选择性介导的血清素能作用，例如情感障碍，焦虑症，精神障碍，便秘。

12. 发明授权

US4691019A Anorectic agent; 4-(3-trifluoromethylphenyl)-1-(2-cyanoethyl)-1,2,3,6-tetrahydropyridine 失效
标题翻译：厌食剂 4-（3-三氟甲基苯基）-1-（2-氰基乙基）-1,2,3,6-四氢吡啶
公开(公告)号：US4691019A
公开(公告)日：1987-09-01
申请号：US811490
申请日：1985-12-20
申请人： Dino Nisato , Emilio Crisafulli , Alberto Bianchetti , Paolo Carminati
发明人： Dino Nisato , Emilio Crisafulli , Alberto Bianchetti , Paolo Carminati
IPC分类号： C07D211/70 , C07D211/68
CPC分类号： C07D211/70
摘要： The invention relates to 4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridines of formula ##STR1## in which R represents a cyano, acetyl or cycloalkyl group of from 3 to 7 carbon atoms and Alk represents a straight or branched alkylene of from 1 to 4 carbon atoms, as well as to the salts thereof, having an anorectic acitivity, to a process for preparing same and to pharmaceutical compositions containing said compounds, useful in the treatment of obesity.
摘要翻译：本发明涉及式“IMAGE”的4-（3-三氟甲基苯基）-1,2,3,6-四氢吡啶，其中R表示3至7个碳原子的氰基，乙酰基或环烷基，Alk表示直链或具有1至4个碳原子的支链亚烷基，以及其具有厌食活性的盐，其制备方法和含有所述化合物的药物组合物，其可用于治疗肥胖症。

13. 发明授权

US4602024A Substituted trifluoromethylphenyltetrahydropyridines having a cyano substituent and an anorectic activity, a process for preparing same and pharmaceutical compositions 失效
标题翻译：具有氰基取代基和厌氧活性的取代的三氟甲基苯基四氢吡啶，其制备方法和药物组合物
公开(公告)号：US4602024A
公开(公告)日：1986-07-22
申请号：US630969
申请日：1984-07-16
申请人： Dino Nisato , Emilio Crisafulli , Alberto Bianchetti , Paolo Carminati
发明人： Dino Nisato , Emilio Crisafulli , Alberto Bianchetti , Paolo Carminati
IPC分类号： A61K31/445 , A61K31/451 , A61P3/04 , C07D211/70 , A61K31/44
CPC分类号： C07D211/70 , Y10S514/91
摘要： The invention relates to 4-(-3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridines of formula ##STR1## in which R represents a cyano, acetyl or cycloalkyl group of from 3 to 7 carbon atoms and Alk represents a straight or branched alkylene of from 1 to 4 carbon atoms, as well as to the salts thereof, having an anorectic activity, to a process for preparing same and to pharmaceutical compositions containing said compounds, useful in the treatment of obesity.
摘要翻译：本发明涉及式（IMAGE）的4-（ - 3-三氟甲基苯基）-1,2,3,6-四氢吡啶，其中R表示3至7个碳原子的氰基，乙酰基或环烷基，Alk表示直链或具有1至4个碳原子的支链亚烷基，以及其具有厌食活性的盐，其制备方法和含有所述化合物的药物组合物，其可用于治疗肥胖症。

14. 发明授权

US5786508A 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：US5786508A
公开(公告)日：1998-07-28
申请号：US411656
申请日：1995-04-06
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： C07C229/36 , A61K31/195 , C07C239/36
CPC分类号： C07C229/36 , C07C2101/14
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, and R.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, either as a single isomer or as a mixture of isomers, and the pharmaceutically acceptable salts thereof.
摘要翻译： PCT No.PCT / US94 / 07804 Sec。 371日期：1995年4月6日 102（e）日期1995年4月6日PCT 1994年7月15日PCT公布。公开号WO95 / 04714 日期1995年2月16日本发明涉及用作治疗与作为犬尿氨酸转氨酶（KAT）酶抑制剂的化合物的脑老化过程和围产期脑疾病相关的认知障碍的用途。本发明还提供作为新化合物的选择类别的作为式（IA）化合物的KAT抑制剂，其中R是卤素，C 1 -C 6烷基，C 5 -C 7环烷基，苯基-C 1 -C 4烷基， C 1 -C 6烷氧基，C 6 -C 10芳氧基，苯基-C 1 -C 4烷氧基或三氟甲基，R 1是羟基，C 1 -C 6烷氧基，氨基，单-C 1 -C 6烷基氨基，二-C 1 -C 6烷基氨基，羟基氨基，C 1 -C 4 烷氧基氨基或苄氧基氨基，条件是：（ⅰ）当R 1为羟基，同时R为卤素时，该卤素不为氟; 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，作为单一异构体或作为异构体的混合物，以及其药学上可接受的盐。

15. 发明授权

US4472408A Substituted trifluoromethylphenyltetrahydropyridines having an anorectic activity 失效
标题翻译：具有厌氧活性的取代的三氟甲基苯基四氢吡啶
公开(公告)号：US4472408A
公开(公告)日：1984-09-18
申请号：US354522
申请日：1982-03-03
申请人： Dino Nisato , Emilio Crisafulli , Alberto Bianchetti , Paolo Carminati
发明人： Dino Nisato , Emilio Crisafulli , Alberto Bianchetti , Paolo Carminati
IPC分类号： A61K31/445 , A61K31/451 , A61P3/04 , C07D211/70 , A61K31/44 , C07D211/68
CPC分类号： C07D211/70 , Y10S514/91
摘要： The invention relates to 4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridines of formula ##STR1## in which R represents a cyano, acetyl or cycloalkyl group of from 3 to 7 carbon atoms and Alk represents a straight or branched alkylene of from 1 to 4 carbon atoms, as well as to the salts thereof, having an anorectic activity, to a process for preparing same and to pharmaceutical compositions containing said compounds, useful in the treatment of obesity.
摘要翻译：本发明涉及式“IMAGE”的4-（3-三氟甲基苯基）-1,2,3,6-四氢吡啶，其中R表示3至7个碳原子的氰基，乙酰基或环烷基，Alk表示直链或具有1至4个碳原子的支链亚烷基，以及其具有厌食活性的盐，其制备方法和含有所述化合物的药物组合物，其可用于治疗肥胖症。

16. 发明授权

US4181740A Indolyl acetic acid derivative 失效
标题翻译：吲哚乙酸衍生物
公开(公告)号：US4181740A
公开(公告)日：1980-01-01
申请号：US796607
申请日：1977-05-13
申请人： Silvia Tricerri Zumin , Alberto Bianchetti
发明人： Silvia Tricerri Zumin , Alberto Bianchetti
IPC分类号： A01H1/02 , A01H3/04 , A01N43/58 , A01N47/22 , A61K31/403 , A61K31/404 , A61K31/405 , A61P25/04 , A61P29/00 , C07D209/26 , C07D237/14 , C07D237/24 , C07D209/04
CPC分类号： A01H1/02 , A01N43/58 , A01N47/22 , C07D209/26 , C07D237/24
摘要： The present invention provides 1-(p-azidobenzoyl)-5-methoxy-2-methyl-3-indolylacetic acid and its pharmaceutically acceptable salts and esters and processes of preparation.
摘要翻译：本发明提供1-（对叠氮苯甲酰基）-5-甲氧基-2-甲基-3-吲哚乙酸及其药学上可接受的盐和酯及其制备方法。

17. 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。

18. 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。

19. 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。

20. 发明授权

US5270341A Method of treatment or prophylaxis of depression and stress 失效
标题翻译：治疗或预防抑郁症和压力的方法
公开(公告)号：US5270341A
公开(公告)日：1993-12-14
申请号：US804580
申请日：1991-12-04
申请人： Peter-Eugene Keane , Alberto Bianchetti , Jacques Simiand , Tiziano Croci
发明人： Peter-Eugene Keane , Alberto Bianchetti , Jacques Simiand , Tiziano Croci
IPC分类号： A61K31/19 , A61K31/195 , A61K31/215 , A61P25/24 , A61P25/26 , C07C217/84 , A61K31/24
CPC分类号： A61K31/215
摘要： The invention concerns a method of treatment and prophylaxis of depression and stress by means of a phenylethanolaminotetralin of formula (I) ##STR1## wherein A is a (C.sub.1 -C.sub.4)alkylene radical and R represents a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl group, or a pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及一种通过式（I）的苯乙醇氨基四氢化萘治疗和预防抑郁和应激的方法，其中A是（C 1 -C 4）亚烷基，R代表氢原子或（C1 -C 4）烷基，或其药学上可接受的盐。

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