专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 发明授权

US5109017A (2-thienyl)alkylamine derivatives having neuroprotective properties 失效
标题翻译：（2-噻吩基）烷基胺衍生物具有神经保护性质
公开(公告)号：US5109017A
公开(公告)日：1992-04-28
申请号：US589963
申请日：1990-09-26
申请人： Richard J. Schmiesing , Ronald C. Griffith , Robert J. Murray
发明人： Richard J. Schmiesing , Ronald C. Griffith , Robert J. Murray
IPC分类号： C07D333/20
CPC分类号： C07D333/20
摘要： Compounds of the formula I, ##STR1## in which: R.sub.1 represents hydrogen or C.sub.1-6 alkyl,R.sub.2 represents hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl or C.sub.3-6 cycloalkyl,R.sub.3 represents one or more radicals selected from hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen, trifluoromethyl, amino, lower alkylamino or dilower alkylamino,R.sub.4 represents one or more radicals selected from hydrogen or C.sub.1-6 alkyl,A represents an alpha-amino acid acyl group or an alkoxycarbonyl group,and pharmaceutically acceptable salts thereof are useful as pharmaceuticals, in particular they possess N-methyl-(d)-aspartate (NMDA) blocking properties and are useful in the treatment and/or prevention of neurological disorders such as stroke, cerebral ischaemia, cerebral palsy, hypoglycaemia, epilepsy, Alzheimer's disease, Huntington's chorea, Olivo-ponto-cerebellar atrophy, perinatal asphyxia and anoxia.
摘要翻译：式I的化合物，其中：R1表示氢或C1-6烷基，R2表示氢，C1-6烷基，C3-6烯基，C3-6炔基或C3-6环烷基，R3代表一个或更多的选自氢，羟基，C 1-6烷基，C 1-6烷氧基，卤素，三氟甲基，氨基，低级烷基氨基或二元烷基氨基的基团，R 4表示一个或多个选自氢或C 1-6烷基的基团，A代表α- 氨基酸酰基或烷氧基羰基及其药学上可接受的盐可用作药物，特别是它们具有N-甲基 - （ - ） - 天冬氨酸（NMDA）阻断性质，并且可用于治疗和/或预防神经障碍如中风，脑缺血，脑性麻痹，低血糖症，癫痫，阿尔茨海默病，亨廷顿氏舞蹈病，Olivo-ponto-cerebellar萎缩，围产期窒息和缺氧。

3. 发明授权

US07998986B2 Modulators of LXR 有权
标题翻译： LXR调制器
公开(公告)号：US07998986B2
公开(公告)日：2011-08-16
申请号：US10327813
申请日：2002-12-20
申请人： Christopher D. Bayne , Alan T. Johnson , Shao-Po Lu , Raju Mohan , Ronald C. Griffith
发明人： Christopher D. Bayne , Alan T. Johnson , Shao-Po Lu , Raju Mohan , Ronald C. Griffith
IPC分类号： A61K31/4412 , C07D213/64
CPC分类号： C07D401/04 , C07D213/85 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/12
摘要： Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of nuclear receptors, including liver X receptor (LXR) and orphan nuclear receptors. In certain embodiments, the compounds are N-substituted pyridones.
摘要翻译：提供了调节核受体活性的化合物，组合物和方法。特别地，提供杂环化合物用于调节核受体的活性，包括肝X受体（LXR）和孤儿核受体。在某些实施方案中，化合物是N-取代的吡啶酮。

4. 发明授权

US06897225B1 Inhibitors of αLβ2 mediated cell adhesion 失效
公开(公告)号：US06897225B1
公开(公告)日：2005-05-24
申请号：US10111110
申请日：2000-10-19
申请人： Ila Sircar , Marshall Morningstar , Paul Furth , Nicholas Smith , Bradley R. Teegarden , Ronald C. Griffith
发明人： Ila Sircar , Marshall Morningstar , Paul Furth , Nicholas Smith , Bradley R. Teegarden , Ronald C. Griffith
IPC分类号： C07D471/04 , C07D487/04 , C07D513/04 , A61K31/4188 , A61K31/4439 , A61P19/02
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to a compound of the following formula: or a pharmaceutically acceptable salt thereof. Also disclosed are compositions containing the compound and methods of preparing and using the compounds. The compounds of the invention are useful in treating αLβ2 adhesion mediated conditions in a mammal.

5. 发明授权

US5605916A 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：US5605916A
公开(公告)日：1997-02-25
申请号：US398850
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 , C07D213/73
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

US4351847A Antiviral alpha, alpha-dialkyl adamantylethylamines 失效
标题翻译：抗病毒α，α-二烷基金刚烷乙胺
公开(公告)号：US4351847A
公开(公告)日：1982-09-28
申请号：US277777
申请日：1981-06-26
申请人： Ronald C. Griffith , Clyde R. Kinsolving
发明人： Ronald C. Griffith , Clyde R. Kinsolving
IPC分类号： A61K31/13 , A61P31/12 , A61P31/22
CPC分类号： A61K31/13 , Y10S514/934
摘要： Warm-blooded animals are treated by administering to the animal a dosage, effective to prevent or to alleviate the symptoms of herpes virus, type II, of a compound of the formula I or its acid salt: ##STR1## wherein R.sub.1 and R.sub.2 are selected from the class consisting of H and --CH.sub.3 ; and at least one pharmaceutically acceptable carrier, wherein the compound is 0.01 to 95% by weight of the composition.
摘要翻译：通过向动物施用有效预防或减轻II型化合物或其酸式盐的疱疹病毒II型症状的剂量来治疗温血动物：其中R1和 R2选自H和-CH 3; 和至少一种药学上可接受的载体，其中所述化合物为所述组合物的0.01至95重量％。

7. 发明授权

US5075317A Spirofurane derivatives 失效
标题翻译：螺旋体衍生物
公开(公告)号：US5075317A
公开(公告)日：1991-12-24
申请号：US369324
申请日：1989-06-21
申请人： Edwin S. Wu , Ronald C. Griffith
发明人： Edwin S. Wu , Ronald C. Griffith
IPC分类号： A61K31/44 , A61P25/18 , A61P25/28 , C07D491/10 , C07D491/107
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 or alkyl C.sub.1-6,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.dbd.O, C.dbd.CHR.sup.4 or C.dbd.NR.sup.5, in whichR.sup.3, R.sup.4 and R.sup.5 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表示氢或烷基C 1-6，n和m是1至3的整数，条件是n + m = 4，并且其中之一 X和Y表示CH 2，另一个表示CHR 3，C = O，C = CHR 4或C = NR 5，其中R 3，R 4和R 5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。

8. 发明授权

US4873241A 2-amino-N-(2-phenylindan-2-yl)acetamides useful as anti-epileptics 失效
标题翻译：可用作抗癫痫药的2-氨基-N-（2-苯基茚满-2-基）乙酰胺
公开(公告)号：US4873241A
公开(公告)日：1989-10-10
申请号：US265087
申请日：1988-10-31
申请人： James J. Napier , Ronald C. Griffith
发明人： James J. Napier , Ronald C. Griffith
IPC分类号： C07C237/04 , C07D295/15
CPC分类号： C07D295/15 , C07C237/04 , C07C2102/08
摘要： 2-Amino-N-(2-phenylindan-2-yl)acetamides of the following formula are provided ##STR1## wherein, a=0 to 3,R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen and methyl,R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sub.5 is selected from hydrogen, C.sub.1 -C.sub.4 alkyl, cyclopropyl and (aminomethyl)carbonyl, orR.sub.4 and R.sub.5 taken together with the nitrogen atom to which they are attached from a heterocyclic ring selected from pyrrolidinyl, piperidinyl and morpholinyl, orR.sub.3 and R.sub.4 taken together with the carbon atom and nitrogen atom to which they are respectively attached form a heterocyclic ring selected from pyrrolidinyl and piperidinyl, andR.sub.6 is selected from hydrogen, halogen, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl, C.sub.1 -C.sub.4 alkyl and combinations thereof.The compounds have antiepileptic or antihypoxia activity.
摘要翻译：提供下式的2-氨基-N-（2-苯基茚基-2-基）乙酰胺：其中a = 0至3，R 1，R 2和R 3独立地选自氢和甲基，R 4 是氢或C 1 -C 4烷基，R 5选自氢，C 1 -C 4烷基，环丙基和（氨基甲基）羰基，或者R 4和R 5与它们所连接的氮原子一起选自吡咯烷基，哌啶基和吗啉基，或者R 3和R 4与它们分别连接的碳原子和氮原子一起形成选自吡咯烷基和哌啶基的杂环，R 6选自氢，卤素，C 1 -C 4烷氧基，三氟甲基， C4烷基及其组合。该化合物具有抗癫痫或抗低氧活性。

9. 发明授权

US4871872A 2-[(2-aminoacetyl)amino]acetamide derivatives 失效
标题翻译： 2 - [（2-氨基乙酰基）氨基]乙酰胺衍生物
公开(公告)号：US4871872A
公开(公告)日：1989-10-03
申请号：US145866
申请日：1988-01-20
申请人： Ronald C. Griffith
发明人： Ronald C. Griffith
IPC分类号： A61K38/00 , C07C237/06 , C07C237/20 , C07K5/06
CPC分类号： C07K5/06026 , C07C237/06 , C07C237/20 , A61K38/00 , C07C2101/02
摘要： Compounds are provided of the following general structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are hydrogen or methyl and where R.sub.5 and R.sub.6 are independently selected from hydrogen or fluorine.These are useful for providing antiepileptic activity.
摘要翻译：化合物由以下一般结构提供：其中R 1，R 2，R 3和R 4是氢或甲基，其中R 5和R 6独立地选自氢或氟。这些可用于提供抗癫痫活动。

10. 发明授权

US4766131A 2-amino (or hydroxy) phenethyl-1,2,3,4-tetrahydroisoquinolines as analgesics 失效
标题翻译： 2-氨基（或羟基）苯乙基-1,2,3,4-四氢异喹啉作为止痛剂
公开(公告)号：US4766131A
公开(公告)日：1988-08-23
申请号：US948449
申请日：1986-12-30
申请人： Thomas A. Davidson , Ronald C. Griffith
发明人： Thomas A. Davidson , Ronald C. Griffith
IPC分类号： C07D217/02 , C07D217/04 , C07D217/06 , A61K31/47 , C07D217/18
CPC分类号： C07D217/04 , C07D217/02 , C07D217/06
摘要： Analgesic 1,2,3,4-tetrahydroisoquinolines of the formula (1) ##STR1## wherein R.sub.1 and R.sub.2 respectively are hydrogen, hydroxy or alkoxy of 1 to 4 carbon atoms, R.sub.3 and R.sub.4 respectively are hydrogen or alkyl of 1 to 4 carbon atoms, and R.sub.5 is hydroxy, nitro or ##STR2## wherein R.sub.6 and R.sub.7 respectively are hydrogen, alkyl of 1 to 4 carbon atoms or RCO-- wherein R is hydrogen or alkyl of 1 to 4 carbon atoms; pharmaceutically acceptable addition salts thereof with non-toxic acids; analgesic compositions thereof in an inert, pharmaceutical carrier; and methods of preparation from corresponding R.sub.1, R.sub.2, R.sub.3 and R.sub.4 -substituted tetrahydroisoquinolines.
摘要翻译：式（1）的镇痛性1,2,3,4-四氢异喹啉其中R1和R2分别是氢，1-4个碳原子的羟基或烷氧基，R3和R4分别是氢或1的烷基 4个碳原子，R5是羟基，硝基或者其中R6和R7分别是氢，1-4个碳原子的烷基或RCO-，其中R是氢或1-4个碳原子的烷基; 其药学上可接受的加成盐与无毒酸; 其镇痛组合物在惰性药物载体中; 和由相应的R1，R2，R3和R4取代的四氢异喹啉制备的方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式