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1. 发明专利

BR1100967A 未知
公开(公告)号：BR1100967A
公开(公告)日：1999-10-13
申请号：BR1100967
申请日：1997-05-14
申请人： RONALD C. GRIFFITH , JAMES J. NAPIER
发明人： GRIFFITH RONALD C , NAPIER JAMES J
IPC分类号： C07C57/145 , A61K31/16 , A61K31/165 , A61K38/00 , A61P25/20 , C07C51/00 , C07C67/00 , C07C237/00 , C07C237/06 , C07C237/12 , C07K5/06 , C07C209/00 , C07C233/00 , A61K31/13
摘要： Compounds are provided of the following general structure: wherein B is hydrogen, lower alkyl (C1-C4) or methoxycarbonyl; R1 is hydrogen or methyl and where W and Q are independently selected from phenyl or 4-fluorophenyl. They are useful for providing sedative and antiepileptic activity.

2. 发明授权

US5607935A 2-heterocyclicethylamine derivatives and their use as pharmaceuticals 失效
标题翻译： 2-杂环乙胺衍生物及其作为药物的用途
公开(公告)号：US5607935A
公开(公告)日：1997-03-04
申请号：US232029
申请日：1994-08-01
申请人： Ronald C. Griffith , Richard J. Schmiesing , Robert J. Griffith
发明人： Ronald C. Griffith , Richard J. Schmiesing , Robert J. Griffith
IPC分类号： A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/54 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/30 , C07D207/00 , C07D213/36 , C07D213/38 , C07D213/40 , C07D213/61 , C07D213/73 , C07D213/81 , C07D213/89 , C07D231/12 , C07D233/54 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D241/16 , C07D249/08 , C07D261/08 , C07D263/32 , C07D277/22 , C07D285/08 , C07D401/06 , C07D405/06 , C07D409/06 , C07D417/06 , A61K31/495 , C07D241/02
CPC分类号： C07D213/40 , C07D213/38 , C07D213/61 , C07D213/73 , C07D213/81 , C07D213/89 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D241/16 , C07D401/06 , C07D405/06 , C07D409/06
摘要： Compounds of formula (I), wherein A represents CH.dbd.CH; Q represents pyrazine having substituents R.sup.6 and R.sup.7 ; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents H, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-6 cycloalkyl or NH.sub.2 CH.sub.2 CO--; R.sup.3 represents H, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.4 and R.sup.5 independently represent H, OH, C.sub.1-6 alkoxy, C.sub.1-6 alkyl, halogen, trifluoromethyl or NR.sup.8 R.sup.9 ; R.sup.6 and R.sup.7 independently represent H, OH, C.sub.1-6 alkoxy, C.sub.1-6 alkyl, halogen, trifluoromethyl, C.sub.1-6 hydroxyalkyl, amidino, CONH.sub.2 or NR.sup.8 R.sup.9 ; in addition, R.sup.6 and R.sup.7 may independently represent O when substituted on N; R.sup.8 and R.sup.9 independently represent H or C.sub.1-6 alkyl; and pharmaceutically acceptable derivatives thereof. The compounds are useful as pharmaceuticals, in particular in the treatment of neurological disorders.
摘要翻译： PCT No.PCT / GB92 / 01971 Sec。 371日期1994年8月1日 102（e）日期1994年8月1日PCT提交1992年10月28日PCT公布。公开号WO93 / 09095 日期：1993年5月13日公式（I）的化合物，其中A表示CH = CH; Q表示具有取代基R 6和R 7的吡嗪; R 1表示H或C 1-6烷基; R 2表示H，C 1-6烷基，C 3-6烯基，C 3-6炔基，C 3-6环烷基或NH 2 CH 2 CO-; R3表示H，C1-6烷基，C3-6烯基或C3-6炔基; R 4和R 5独立地表示H，OH，C 1-6烷氧基，C 1-6烷基，卤素，三氟甲基或NR 8 R 9; R6和R7独立地表示H，OH，C1-6烷氧基，C1-6烷基，卤素，三氟甲基，C1-6羟基烷基，脒基，CONH2或NR8R9; 此外，当在N上取代时，R6和R7可以独立地表示O; R8和R9独立地表示H或C1-6烷基; 及其药学上可接受的衍生物。该化合物可用作药物，特别是治疗神经障碍。

3. 发明授权

US5594000A Spirofurane derivatives 失效
标题翻译：螺呋喃衍生物
公开(公告)号：US5594000A
公开(公告)日：1997-01-14
申请号：US469791
申请日：1995-06-06
申请人： Edwin S.-C. Wu , Ronald C. Griffith
发明人： Edwin S.-C. Wu , Ronald C. Griffith
IPC分类号： C07D491/10 , C07D491/107 , C07D471/10 , A61K31/445 , C07D211/44 , C07D405/06
CPC分类号： C07D491/10
摘要： Compounds of general formula I, ##STR1## wherein R.sup.1 represents hydrogen or alkyl C.sub.1-3,R.sup.2 represents hydrogen, alkyl C.sub.1-6, alkenyl C.sub.3-6 or alkynyl C.sub.3-6,n and m are integers from 1 to 3, provided that n+m=4, andone of X and Y represents CH.sub.2 and the other represents CHR.sup.3, C=CHR.sup.4 or C=NR.sup.5, in whichR.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16 and R.sup.17 are as defined in the specification,and their saltsare useful as pharmaceuticals, in particular as central muscarinic acetylcholine receptors. The compounds are therefore useful in the treatment of diseases such as presenile and senile dementia, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania and Tourette Syndrome, and also as analgesic agents for use in the treatment of severe painful conditions such as rheumatism, arthritis, and terminal illness.
摘要翻译：通式I的化合物，其中R 1表示氢或烷基C 1-3，R 2表示氢，烷基C 1-6，烯基C 3-6或炔基C 3-6，n和m是1至3的整数， n + m = 4，X和Y中的一个表示CH 2，另一个表示CHR 3，C = CHR 4或C = NR 5，其中R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11，R 12 R13，R14，R15，R16和R17如说明书中所定义，并且它们的盐可用作药物，特别是作为中毒毒蕈碱乙酰胆碱受体。因此，这些化合物可用于治疗诸如老年痴呆和老年痴呆，亨廷顿舞蹈病，迟发性运动障碍，运动过度，躁狂症和图雷特综合征等疾病，也可用作治疗严重疼痛病症如镇痛，关节炎，和末期疾病。

4. 发明授权

US5539120A Arylalkyl-amines having anticonvulsant and neuroprotective properties 失效
标题翻译：具有抗惊厥和神经保护性质的芳基烷基胺
公开(公告)号：US5539120A
公开(公告)日：1996-07-23
申请号：US399030
申请日：1995-03-06
申请人： Ronald C. Griffith , James J. Napier
发明人： Ronald C. Griffith , James J. Napier
IPC分类号： A61K31/135 , A61K31/16 , A61K31/165 , A61K31/245 , A61K31/275 , A61K31/44 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C237/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C255/58 , C07C271/12 , C07D213/38 , C07K5/06 , C07D213/02
CPC分类号： A61K31/16 , A61K31/135 , A61K31/165 , A61K31/245 , A61K31/275 , A61K31/44 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C237/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C255/58 , C07C271/12 , C07D213/38 , C07K5/06
摘要： There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano;R.sub.1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl;R.sub.2 represents hydrogen or COCH.sub.2 NH.sub.2 ;R.sub.3 represents hydrogen or C1 to 6 alkyl;in addition, when R.sub.2 represents hydrogen either one or both of Ar.sub.1 and Ar.sub.2 may also represent 2-, 3- or 4-pyridinyl and R.sub.1 may also represent trihalomethyl;or a pharmaceutically acceptable salt thereof.Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.
摘要翻译：提供治疗神经系统疾病如癫痫，中风和脑缺血的方法，其包括施用式I化合物：其中Ar1和Ar2可以相同或不同，独立地为代表苯基或被一个或多个氨基，硝基，卤素，羟基，C 1-6烷氧基，C 1-6烷基或氰基取代的苯基; R1表示氢，C1至6烷基，C1至6烷氧基羰基; R2表示氢或COCH2NH2; R 3表示氢或C 1-6烷基; 此外，当R 2表示氢时，Ar 1和Ar 2中的一个或两个也可以表示2-，3-或4-吡啶基，R 1也可以表示三卤代甲基; 或其药学上可接受的盐。一些式I的化合物是新的，并且还与含有新化合物的药物组合物一起提供。

5. 发明授权

US5430044A Arylalkyl-amines and -amides having anticonvulsant and neuroprotective properties 失效
标题翻译：具有抗惊厥和神经保护性质的芳基烷基胺和酰胺
公开(公告)号：US5430044A
公开(公告)日：1995-07-04
申请号：US915489
申请日：1992-07-16
申请人： Ronald C. Griffith , James J. Napier
发明人： Ronald C. Griffith , James J. Napier
IPC分类号： A61K31/135 , A61K31/16 , A61K31/165 , A61K31/245 , A61K31/275 , A61K31/44 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C237/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C255/58 , C07C271/12 , C07D213/38 , C07K5/06
CPC分类号： A61K31/16 , A61K31/135 , A61K31/165 , A61K31/245 , A61K31/275 , A61K31/44 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C237/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C255/58 , C07C271/12 , C07D213/38 , C07K5/06
摘要： There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano;R.sub.1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl;R.sub.2 represents hydrogen or COCH.sub.2 NH.sub.2 ;R.sub.3 represents hydrogen or C1 to 6 alkyl;in addition, when R.sub.2 represents hydrogen either one or both of Ar.sub.1 and Ar.sub.2 may also represent 2-, 3- or 4-pyridinyl and R.sub.1 may also represent trihalomethyl;or a pharmaceutically acceptable salt thereof.Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.
摘要翻译：提供治疗神经系统疾病如癫痫，中风和脑缺血的方法，其包括施用式I化合物：其中Ar1和Ar2可以相同或不同，独立地为代表苯基或被一个或多个氨基，硝基，卤素，羟基，C 1-6烷氧基，C 1-6烷基或氰基取代的苯基; R1表示氢，C1至6烷基，C1至6烷氧基羰基; R2表示氢或COCH2NH2; R 3表示氢或C 1-6烷基; 此外，当R 2表示氢时，Ar 1和Ar 2中的一个或两个也可以表示2-，3-或4-吡啶基，R 1也可以表示三卤代甲基; 或其药学上可接受的盐。一些式I的化合物是新的，并且还与含有新化合物的药物组合物一起提供。

6. 发明授权

US5331007A Arylalkyl-amines and -amides having anticonvulsant and neuroprotective properties 失效
标题翻译：具有抗惊厥和神经保护性质的芳基烷基胺和酰胺
公开(公告)号：US5331007A
公开(公告)日：1994-07-19
申请号：US918158
申请日：1992-07-20
申请人： Ronald C. Griffith , James J. Napier
发明人： Ronald C. Griffith , James J. Napier
IPC分类号： A61K31/135 , A61K31/16 , A61K31/165 , A61K31/245 , A61K31/275 , A61K31/44 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C237/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C255/58 , C07C271/12 , C07K5/06 , A01N31/34 , A01N37/12 , A01N37/18
CPC分类号： A61K31/135 , A61K31/16 , A61K31/165 , A61K31/245 , A61K31/275 , A61K31/44 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C237/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C255/58 , C07C271/12 , C07K5/06
摘要： There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano;R.sub.1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl;R.sub.2 represents hydrogen or COCH.sub.2 NH.sub.2 ;R.sub.3 represents hydrogen or C1 to 6 alkyl;in addition, when R.sub.2 represents hydrogen either one or both of Ar.sub.1 and Ar.sub.2 may also represent 2-, 3- or 4-pyridinyl and R.sub.1 may also represent trihalomethyl;or a pharmaceutically acceptable salt thereof.Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.
摘要翻译：提供治疗神经系统疾病如癫痫，中风和脑缺血的方法，其包括施用式I化合物：其中Ar1和Ar2可以相同或不同，独立地为代表苯基或被一个或多个氨基，硝基，卤素，羟基，C 1-6烷氧基，C 1-6烷基或氰基取代的苯基; R1表示氢，C1至6烷基，C1至6烷氧基羰基; R2表示氢或COCH2NH2; R 3表示氢或C 1-6烷基; 此外，当R 2表示氢时，Ar 1和Ar 2中的一个或两个也可以表示2-，3-或4-吡啶基，R 1也可以表示三卤代甲基; 或其药学上可接受的盐。一些式I的化合物是新的，并且还与含有新化合物的药物组合物一起提供。

7. 发明授权

US4912222A Antihistamines related to cyproheptadine 失效
标题翻译：抗组胺药与赛庚啶相关
公开(公告)号：US4912222A
公开(公告)日：1990-03-27
申请号：US207840
申请日：1988-06-17
申请人： Ronald C. Griffith , James J. Napier
发明人： Ronald C. Griffith , James J. Napier
IPC分类号： C07D211/14 , C07D211/22 , C07D211/70 , C07D313/12 , C07D405/04
CPC分类号： C07D405/04 , C07D211/14 , C07D211/22 , C07D211/70 , C07D313/12
摘要： 4-Dibenzocycloheptenyl, 4-dibenzocycloheptyl, and 4-dibenzoxepinylpiperidine compounds possessing antihistaminic activity.
摘要翻译： 4-二苯并环庚烯基，4-二苯并环庚基和具有抗组胺活性的4-二苯并氧杂环丁基哌啶化合物。

8. 发明授权

US4647674A Bis-(dibenzo[b,d]pyranyloxy) propanes 失效
标题翻译：双（二苯并[b，d]吡喃氧基）丙烷
公开(公告)号：US4647674A
公开(公告)日：1987-03-03
申请号：US784979
申请日：1985-10-07
申请人： Ronald C. Griffith
发明人： Ronald C. Griffith
IPC分类号： A61K31/365 , A61P9/00 , A61P25/04 , A61P25/20 , C07D311/80 , C07D407/00
CPC分类号： C07D311/80
摘要： Dibenzopyrone derivatives which possess depressant and/or antihypoxia activity are 1,3-bis(dibenzo[b,d]pyranyloxy propanes having the formula (1): ##STR1## where R and R.sup.1 independently represent hydrogen or methyl; where A is ##STR2## and where X represents single substitution with oxygen or substitution with hydrogen and a second group taken to be hydrogen, hydroxyl, amino, C.sub.1 -C.sub.4 alkylamino or an acyloxy radical ##STR3## where B represents C.sub.1 -C.sub.15 alkyl, --CH.sub.2 CH.sub.2 COOH, or (dimethylamino)phenyl. Also included are pharmaceutically acceptable salt forms of the compounds.These compounds are useful as sedatives and/or for the protection of warm blooded animals from the effects of oxygen deprivation.
摘要翻译：具有抑制和/或抗缺氧活性的二苯并吡喃衍生物是具有式（1）的1,3-双（二苯并[b，d]吡喃氧基丙烷：其中R和R 1独立地表示氢或甲基;其中A是其中X表示用氧取代或用氢取代，第二组取代为氢，羟基，氨基，C 1 -C 4烷基氨基或酰氧基，其中B表示C 1 -C 15烷基，-CH 2 CH 2 COOH或（二甲基氨基）苯基，还包括化合物的药学上可接受的盐形式，这些化合物可用作镇静剂和/或用于保护温血动物免受氧气剥夺的影响。

9. 发明申请

US20080247992A1 NITROGEN-CONTAINING HETEROARYL DERIVATIVES 审中-公开
标题翻译：含氮含量衍生物
公开(公告)号：US20080247992A1
公开(公告)日：2008-10-09
申请号：US11923568
申请日：2007-10-24
申请人： Christopher D. Roberts , Dong-Fang Shi , Ronald C. Griffith
发明人： Christopher D. Roberts , Dong-Fang Shi , Ronald C. Griffith
IPC分类号： A61K31/4439 , C07D235/18 , C07D401/04 , A61K38/22 , A61K31/7056 , A61K38/21 , A61K31/4164 , A61P31/12
CPC分类号： C07D235/18 , C07D401/14 , C07D403/12
摘要： Disclosed are compounds, compositions and methods for treating Flaviviridae family virus infections.
摘要翻译：公开了用于治疗黄病毒科家族病毒感染的化合物，组合物和方法。

10. 发明授权

US5455259A Compounds for the treatment of neurodegenerative disorders 失效
标题翻译：用于治疗神经变性疾病的化合物
公开(公告)号：US5455259A
公开(公告)日：1995-10-03
申请号：US221076
申请日：1994-03-31
申请人： Ronald C. Griffith , Robert J. Murray , Michael Balestra , Donald Mathisen
发明人： Ronald C. Griffith , Robert J. Murray , Michael Balestra , Donald Mathisen
IPC分类号： A61K31/135 , A61K31/16 , A61K31/165 , A61K31/245 , A61K31/275 , A61K31/44 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C237/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C255/58 , C07C271/12 , C07D213/38 , C07K5/06 , C07D213/36
CPC分类号： A61K31/16 , A61K31/135 , A61K31/165 , A61K31/245 , A61K31/275 , A61K31/44 , C07C211/27 , C07C211/29 , C07C215/52 , C07C217/60 , C07C237/00 , C07C237/06 , C07C237/08 , C07C237/10 , C07C255/58 , C07C271/12 , C07D213/38 , C07K5/06
摘要： (S)-.alpha.-phenyl-2-pyridineethanamine, and its pharmaceutically acceptable derivatives, are useful in the treatment of neurodegenerative disorders, and exhibit linear pharmacokinetics.
摘要翻译：（S）-α-苯基-2-吡啶乙胺及其药学上可接受的衍生物可用于治疗神经变性疾病，并呈现线性药代动力学。

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