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. 发明申请

WO1993009095A1 2-HETEROCYCLICETHYLAMINE DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译： 2-杂芳基胺衍生物及其作为药物的用途
公开(公告)号：WO1993009095A1
公开(公告)日：1993-05-13
申请号：PCT/GB1992001971
申请日：1992-10-28
申请人： FISONS PLC , FISONS CORPORATION , GRIFFITH, Ronald, Conrad , MURRAY, Robert, John , SCHMIESING, Richard, John
发明人： FISONS PLC , FISONS CORPORATION
IPC分类号： C07D213/38
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 C=C, S or O; Q represents a 5- or 6-membered unsaturated heterocycling ring having a nitrogen atom in the position adjacent to the point of attachment, 0-3 further heteroatoms selected from N, O and S, and substituents R?6 and R7; R1¿ represents H or C¿1-6?alkyl; R?2¿ represents H, C¿1-6?alkyl, C3-6alkenyl, C3-6alkynyl, C3-6cycloalkyl or NH2CH2CO-; in addition, R?1 and R2¿ taken together may form a C¿3-5?alkylene chain; R?3¿ represents H, C¿1-6?alkyl, C3-6alkenyl, C3-6alkynyl; R?4 and R5¿ independently represent H, OH, C¿1-6? alkoxy, C1-6 alkyl, halogen, trifluoromethyl or NR?8R9; R6 and R7¿ independently represent H, OH, C¿1-6? alkoxy, C1-6 alkyl, halogen, trifluoromethyl, C1-6 hydroxyalkyl, amidino, CONH2 or NR?8R9¿; in addition, R?6 and R7¿ may independently represent O when substituted on N; R?8 and R9¿ independently represent H or C¿1-6? alkyl; with various provisos; and pharmaceutically acceptable derivatives thereof; are useful as pharmaceuticals, in particular in the treatment of neurological disorders.

2. 发明申请

WO1992006957A1 2-PHENYL-AND 2-THIENYL-(2)-PIPERIDINE DERIVATIVES HAVING NEUROPROTECTIVE PROPERTIES 审中-公开
标题翻译：具有神经保护特性的2-苯乙烯基和2-噻吩基（2） - 哌啶衍生物
公开(公告)号：WO1992006957A1
公开(公告)日：1992-04-30
申请号：PCT/US1991007522
申请日：1991-10-11
申请人： FISONS CORPORATION , GRIFFITH, Ronald, Conrad , SCHMIESING, Richard, John , MURRAY, Robert, John
发明人： FISONS CORPORATION
IPC分类号： C07D211/12
CPC分类号： C07D409/04 , C07D211/12 , C07D211/14
摘要： Compounds of formula (I) in which R1 and R2, which may be the same or different, represent hydrogen or C1-6 alkyl, R3 and R4 independently represent one or more radicals selected from hydrogen, NH2, NO2, halogen, hydroxyl, C1-6 alkoxy or C1-6 alkyl, X represents S or a -CH=CH- group, and pharmaceutically acceptable derivatives 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.
摘要翻译：式（I）化合物，其中R 1和R 2可以相同或不同，表示氢或C 1-6烷基，R 3和R 4独立地表示一个或多个选自氢，NH 2，NO 2，卤素，羟基，C 1 -6-烷氧基或C 1-6烷基，X表示S或-CH = CH-基团，其药学上可接受的衍生物可用作药物，特别是它们具有N-甲基 - （ - ） - 天冬氨酸（NMDA）阻断性质，可用于治疗和/或预防神经障碍。

3. 发明申请

WO1993020052A1 ENANTIOMERIC 1-PHENYL-2-(2-PYRIDINYL)ETHYLAMINE FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS 审中-公开
标题翻译：用于治疗神经损伤性疾病的完美1-苯乙烯基-2-（2-吡啶基）乙酰胺
公开(公告)号：WO1993020052A1
公开(公告)日：1993-10-14
申请号：PCT/GB1993000689
申请日：1993-04-01
申请人： FISONS PLC , FISONS CORPORATION , GRIFFITH, Ronald, Conrad , MURRAY, Robert, John , BALESTRA, Michael
发明人： FISONS PLC , FISONS CORPORATION
IPC分类号： C07D213/38
CPC分类号： C07D213/38 , A61K31/44
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。

4. 发明申请

WO1992005169A1 (2-THIENYL) ALKYLAMINE DERIVATIVES HAVING NEUROPROTECTIVE PROPERTIES 审中-公开
标题翻译：（2-苯乙烯）具有神经保护性质的烷基胺衍生物
公开(公告)号：WO1992005169A1
公开(公告)日：1992-04-02
申请号：PCT/US1991006951
申请日：1991-09-24
申请人： FISONS CORPORATION , GRIFFITH, Ronald, Conrad , SCHMIESING, Richard, Jon , MURRAY, Robert, John
发明人： FISONS CORPORATION
IPC分类号： C07D333/20
CPC分类号： C07D333/20
摘要： Compounds of formula (I), in which: R1 represents hydrogen or C1-6 alkyl, R2 represents hydrogen, C1-6 alkyl, C3-6 alkenyl, C3-6 alkynyl or C3-6 cycloalkyl, R3 represents one or more radicals selected from hydrogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, halogen, trifluoromethyl, amino, C1-6 alkylamino or di(C1-6 alkyl)amino, R4 represents one or more radicals selected from hydrogen or C1-6 alkyl, A represents hydrogen, C1-6 alkyl, COC(R5R6)N(R7R8) or COOC1-6 alkyl, R5 represents hydrogen, C1-6 alkyl, hydroxy-C1-2 alkyl, mercaptomethyl, (methylthio)C1-2 alkyl, carboxy-C1-2 alkyl, 2-(C1-3 alkoxy)ethyl, (aminocarbonyl)C1-2 alkyl, amino-C1-4 alkyl, 3-imidazolylmethyl, phenylmethyl or (4-hydroxyphenyl)-methyl, or in addition, R5 together with the adjacent nitrogen may represent a piperidine, pyrrolidine or a 2-pyrrolidinone ring, R6, R7 and R8 independently represent hydrogen or C1-6 alkyl, or in addition, R7 and R8 taken together with the nitrogen to which they are attached may represent a C4-5 N heterocyclic ring, and pharmaceutically acceptable acid addition salts thereof, are useful as pharmaceuticals; in particular they possess N-methyl-(D)-aspartate blocking properties and are useful in the treatment and/or prevention of neurological disorders.
摘要翻译：式（I）化合物，其中：R 1表示氢或C 1-6烷基，R 2表示氢，C 1-6烷基，C 3-6烯基，C 3-6炔基或C 3-6环烷基，R 3表示一个或多个选自由氢，羟基，C 1-6烷基，C 1-6烷氧基，卤素，三氟甲基，氨基，C 1-6烷基氨基或二（C 1-6烷基）氨基，R 4表示一个或多个选自氢或C 1-6烷基的基团， A表示氢，C 1-6烷基，COC（R 5 R 6）N（R 7 R 8）或COOC 1-6烷基，R 5表示氢，C 1-6烷基，羟基-C 1-2烷基，巯基甲基，（甲硫基） C 1-2烷基，2-（C 1-3烷氧基）乙基，（氨基羰基）C 1-2烷基，氨基-C 1-4烷基，3-咪唑基甲基，苯基甲基或（4-羟基苯基） - 甲基，与相邻的氮一起可以表示哌啶，吡咯烷或2-吡咯烷酮环，R6，R7和R8独立地表示氢或C1-6烷基，或者另外，R 7和R 8与它们所连接的氮一起可以代表C4- 5 N杂环及其药学上可接受的酸加成盐可用作药物; 特别是它们具有N-甲基（D） - 天冬氨酸阻断性质，并且可用于治疗和/或预防神经障碍。

5. 发明申请

WO1995023135A1 DIPHENYL-2-PIPERIDINONE AND -2-PYRROLIDINONE DERIVATIVES HAVING ANTI-CONVULSANT AND NEUROPROTECTIVE ACTIVITY 审中-公开
标题翻译：具有抗生素和神经保护活性的二苯基-2-哌啶酮和2,3-吡咯烷酮衍生物
公开(公告)号：WO1995023135A1
公开(公告)日：1995-08-31
申请号：PCT/GB1994000387
申请日：1994-02-28
申请人： FISONS CORPORATION , FISONS PLC , MURRAY, Robert, John , SCHMIESING, Richard, Jon
发明人： FISONS CORPORATION , FISONS PLC
IPC分类号： C07D211/76
CPC分类号： C07D207/27 , C07D211/76
摘要： Compounds of formula (I), wherein two of R , R , R and R independently represent phenyl optionally substituted by one or more groups selected from halogen, hydroxy, nitro, amino, C1-6alkyl and C1-6alkoxy; and the ramainder of R , R , R and R independently represent hydrogen or C1-6alkyl; R and R independently represent hydrogen, C1-6alkyl or C3-6cycloalkyl, or R and R together with the nitrogen atom to which they are attached form a C4-6N heterocycle; m is 1 or 2; and n is 1, 2 or 3; and pharmaceutically acceptable acid addition salt thereof; are useful in the treatment of neurodegenerative disorders, particularly epilepsy.
摘要翻译：式（I）化合物，其中R 1，R 2，R 3和R 4中的两个独立地表示任选被一个或多个选自卤素，羟基，硝基，氨基，C 1 -6-烷基和C 1-6烷氧基; R 1，R 2，R 3和R 4的分子独立地表示氢或C 1-6烷基; R 5和R 6独立地表示氢，C 1-6烷基或C 3-6环烷基，或R 5和R 6与它们所连接的氮原子一起形成C 4-6-6杂环; m为1或2; n为1,2或3; 及其药学上可接受的酸加成盐; 可用于治疗神经变性疾病，特别是癫痫。

6. 发明申请

WO1994021621A1 GUANIDINE DERIVATIVES USEFUL IN THERAPY 审中-公开
标题翻译：胍基衍生物有用于治疗
公开(公告)号：WO1994021621A1
公开(公告)日：1994-09-29
申请号：PCT/GB1994000584
申请日：1994-03-22
申请人： FISONS PLC , FISONS CORPORATION , MACDONALD, James, Edwin , GENTILE, Robert, James , MURRAY, Robert, John
发明人： FISONS PLC , FISONS CORPORATION
IPC分类号： C07D295/215
CPC分类号： C07D295/215 , C07D205/04 , C07D207/22 , C07D217/06 , C07D233/22
摘要： Guanidine derivatives of formula (I) wherein R represents hydrogen, halogen, alkyl C1 to 6, nitro, trifluoromethyl, thioalkyl C1 to 6, hydroxy, alkoxy C1 to 6, or a group selected from -NR R , -O(CH2)pQ, -O(CH2)mOQ, -(CH2)mNR R , -O(CH2)mNR R , -NHCO(CH2)mNH(CH2)nQ or -(CH2)pCONR R , or R represents the group A-CO-B-; R represents hydrogen, halogen, alkyl C1 to 6, nitro or trifluoromethyl; and R , R , R , R , n, m, p, Q, A, B and W are as defined in the specification and, are described together with processes for their manufacture and compositions containing them. Compounds of formula (I) are useful in therapy.
摘要翻译：式（I）的胍衍生物，其中R 8表示氢，卤素，C1至6的烷基，硝基，三氟甲基，硫代烷基C1至6，羟基，烷氧基C1至6，或选自-NR4R，（CH 2）m OQ， - （CH 2）m NR R 2，-O（CH 2）m NR R 2，-NHCO（CH 2）m NH （CH 2）nQ或 - （CH 2）p CONR 1 R 2或R 8表示基团A-CO-B; R 9表示氢，卤素，C 1-6的烷基，硝基或三氟甲基; 和R 1，R 2，R 4，R 5，n，m，p，Q，A，B和W如说明书中所定义，并与其制备方法和含有它们的组合物。式（I）化合物可用于治疗。

7. 发明申请

WO1995005363A1 AMIDINE DERIVATIVES WITH NITRIC OXIDE SYNTHETASE ACTIVITIES 审中-公开
标题翻译：具有氮氧化物合成酶活性的氨基衍生物
公开(公告)号：WO1995005363A1
公开(公告)日：1995-02-23
申请号：PCT/GB1994001767
申请日：1994-08-12
申请人： FISONS CORPORATION , FISONS PLC , GENTILE, Robert, James , MURRAY, Robert, John , MacDONALD, James, Edwin , SHAKESPEARE, William, Calvin
发明人： FISONS CORPORATION , FISONS PLC
IPC分类号： C07D207/416
CPC分类号： C07D409/12 , C07C257/14 , C07C257/18 , C07D307/68 , C07D333/38
摘要： Compounds of formula (I) wherein D represents phenyl, pyridinyl or a 5-membered heterocyclic aromatic ring containing 1 to 4 heteroatoms selected from O, S and N, which three groups are optionally substituted by one or more groups selected from alkyl C1 to 6, alkoxy C1 to 6, halogen and perfluoroalkyl C1 to 6; or perfluoroalkyl C1 to 6; R represents hydrogen, alkyl C1 to 6 or halogen; R represents a group -X(CH2)nZCONR R , -X(CH2)nNHCO(CH2)sNR R , -X(CH2)pNR R , -X(CH2)nNHCOR or -(CH2)qNHC(NH)R ; and X, Z, R , R , R , R , n, s, p and q are defined in the specification are described, together with processes for their preparation and compositions containing them. Compounds of formula (I) have nitric oxide synthetase inhibitory activity.
摘要翻译：式（I）的化合物，其中D表示苯基，吡啶基或含有1至4个选自O，S和N的杂原子的5元杂环芳环，其中3个基团任选被一个或多个选自C 1-6 ，烷氧基C1至6，卤素和全氟烷基C1至6; 或全氟烷基C1至6; R 1表示氢，C 1-6烷基或卤素; R 2表示基团-X（CH 2）n ZCONR 3 R 4，-X（CH 2）n NHCO（CH 2）s NR 3 R 4，-X（CH 2）p NR 3 R 3， 4，-X（CH 2）n NHCOR 5或 - （CH 2）q NHC（NH）R 6; 在说明书中定义的X，Z，R 3，R 4，R 5，R 6，n，s，p和q与其制备方法和含有它们的组合物。式（I）化合物具有一氧化氮合成酶抑制活性。

8. 发明申请

WO1992003420A1 SPIRO[CYCLOALKYLBENZENE-1,1'-(1',2',3',4'-TETRAHYDROISOQUINOLINES)] HAVING NEUROPROTECTIVE PROPERTIES 审中-公开
标题翻译： SPIRO [CYCLOALKYLBENZENE-1,1' - （1'，2'，3'，4'-四氢喹啉）]具有神经保护性
公开(公告)号：WO1992003420A1
公开(公告)日：1992-03-05
申请号：PCT/US1991005887
申请日：1991-08-19
申请人： FISONS CORPORATION , GRIFFITH, Ronald, Conrad , MATZ, James, Russell , NAPIER, James, Joseph
发明人： FISONS CORPORATION
IPC分类号： C07D221/20
CPC分类号： C07D221/20
摘要： Compounds of formula (I), in which R1 and R2, which may be the same or different, represent hydrogen or C1-6 alkyl, R3 and R4 independently represent one or more radicals selected from hydrogen, OH, NH2, NO2, halogen, C1-6 alkyl or C1-6 alkoxy and n is an integer from 1-2 inclusive, and pharmaceutically acceptable derivatives 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 neurodegenerative conditions.
摘要翻译：式（I）化合物，其中可以相同或不同的R 1和R 2表示氢或C 1-6烷基，R 3和R 4独立地表示一个或多个选自氢，OH，NH 2，NO 2，卤素， C 1-6烷基或C 1-6烷氧基，n是1-2的整数，其药学上可接受的衍生物可用作药物; 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/或预防神经变性疾病。

9. 发明申请

WO1990015804A1 NOVEL SPIROFURANE DERIVATIVES 审中-公开
标题翻译：新型螺旋体衍生物
公开(公告)号：WO1990015804A1
公开(公告)日：1990-12-27
申请号：PCT/US1990003351
申请日：1990-06-20
申请人： FISONS CORPORATION , WU, Edwin, Schen-Chou , GRIFFITH, Ronald, Conrad
发明人： FISONS CORPORATION
IPC分类号： C07D491/107
CPC分类号： C07D491/10
摘要： Compounds of general formula (I), wherein R1 represents hydrogen or alkyl C¿1-3; R?2 represents hydrogen, alkyl C¿1-6?, alkenyl C3-6 or alkynyl C3-6; n and m are integers from 1 to 3, provided that n + m = 4, and one of X and Y represents CH2 and the other represents CHR?3, C=CHR4¿ or C=NR5, in which R?3, R4, R5, R6, R7, R8, R9, R10, R11 and R12¿ are as defined in the specification, and their salts are 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.

10. 发明申请

WO1994013678A1 SPIROFURANONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE DISORDERS 审中-公开
标题翻译：螺旋体衍生物及其在治疗神经损伤性疾病中的应用
公开(公告)号：WO1994013678A1
公开(公告)日：1994-06-23
申请号：PCT/GB1993002500
申请日：1993-12-06
申请人： FISONS PLC , FISONS CORPORATION , KOVER, Alexander , LOCH, James, III , MULLEN, George , WU, Edwin, Shen-Chou
发明人： FISONS PLC , FISONS CORPORATION
IPC分类号： C07D491/107
CPC分类号： C07D491/10
摘要： Compounds of formula (I), wherein ring A is a ring of formula (AI) or (AII) (in which the spiro atom is indicated by *), R represents H or alkyl C1-6; R represents -(CH2)n-OR , -(CH2)m-C(O)R , fluoroalkyl C1-6, cyanoalkyl C1-6 or alkyl C1-6 substituted with a 4-7 membered optionally unsaturated heterocyclic ring; R represents H, alkyl C1-6 (optionally substituted with alkoxy C1-6), cycloalkyl C4-7, a 4-7 membered optionally unsaturated heterocyclic ring, phenyl (optionally substituted with halogen, hydroxy or alkyl C1-6), or benzyl (optionally substituted with halogen, hydroxy or alkyl C1-6); R represents OR , NR R , N(OR )R or alkyl C1-6; R represents H, alkenyl C2-6, alkynyl C2-6 or alkyl C1-6) optionally substituted with phenyl); R and R independently represent H or alkyl C1-6; R represents H or alkyl C1-6; n is 2-5; m is 1-5; p is 1 or 2; and pharmaceutically acceptable salts thereof; are useful in the treatment of neurodegenerative disorders.
摘要翻译：式（I）化合物，其中环A是式（A1）或（AII）的环（其中螺原子由*表示），R 1表示H或烷基C1-6; R 2表示 - （CH 2）n -OR 3， - （CH 2）m C（O）R 4，氟烷基C 1-6，氰基烷基C 1-6或被4-7元任选的不饱和杂环; R 3表示H，烷基C 1-6（任选被烷氧基C 1-6取代），环烷基C4-7，4-7元任意性不饱和杂环，苯基（任选被卤素，羟基或C 1-6烷基取代）或苄基（任选被卤素，羟基或C 1-6烷基取代）; R 4表示OR 5，NR 6 R 7，N（OR 6）R 7或C 1-6烷基; R 5表示任选被苯基取代的H，烯基C 2-6，炔基C 2-6或烷基C 1-6）; R 6和R 7独立地表示H或烷基C 1-6; R 8表示H或烷基C 1-6; n为2-5; m为1-5; p为1或2; 及其药学上可接受的盐; 可用于治疗神经变性疾病。

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