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51. 发明专利

CA2422589C PYRIDAZINONE AND TRIAZINONE COMPOUNDS AND USE THEREOF AS PHARMACEUTICAL PREPARATIONS 未知
公开(公告)号：CA2422589C
公开(公告)日：2011-08-09
申请号：CA2422589
申请日：2001-09-17
申请人： EISAI CO LTD
发明人： NAGATO SATOSHI , KAWANO KOKI , ITO KOICHI , NORIMINE YOSHIHIKO , UENO KOHSHI , HANADA TAKAHISA , AMINO HIROYUKI , OGO MAKOTO , HATAKEYAMA SHINJI , UENO MASATAKA , GROOM ANTHONY JOHN , RIVERS LEANNE , SMITH TERENCE
IPC分类号： C07D401/04 , A61K31/50 , A61K31/506 , A61K31/53 , A61P25/08 , A61P25/28 , C07D237/04 , C07D237/14 , C07D237/24 , C07D253/06 , C07D401/14 , C07D403/04 , C07D409/04 , C07D409/14 , C07D417/04 , C07D491/04 , C07D491/048 , C07D491/052
摘要： The present invention provides a novel compound exhibiting an excellent inhibitory action on AMPA receptor and/or kainate receptor. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. (See formula I) In the formula, A1, A2 and A3 are independent of each other and each represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a 5- to 14-membered non-aromatic heterocyclic group, a C6-14 aromatic hydrocarbon cyclic group or a 5- to 14-membered aromatic heterocyclic group, each of which may be substituted; Q represents O, S or NH; Z represents C or N; X1, X2 and X3 are independent of each other and each represents a single bond, an optionally substituted C1-6 alkylene group, an optionally substituted C2-6 alkenylene group, an optionally substituted C2-6 alkynylene group, -NH-, -O-, -NHCO-, -CONH-, -SO0-2-, etc.; R1 and R2 are independent of each other and each represents a hydrogen atom or an optionally substituted C1-6 alkyl group, or R1 and R2 may be bound together such that CR2-ZR1 forms C=C; and R3 represents a hydrogen atom or an optionally substituted C1-, alkyl group etc., or may be bound to any atom in A1 or A3 to form, together with the atom, an optionally substituted C5-8 hydrocarbon ring or an optionally substituted 5- to 8-membered heterocyclic ring.

52. 发明专利

NZ524745A Pyridazinones and triazinones and medicinal use thereof 未知
公开(公告)号：NZ524745A
公开(公告)日：2006-01-27
申请号：NZ52474501
申请日：2001-09-17
申请人： EISAI CO LTD
发明人： NAGATO SATOSHI , KAWANO KOKI , ITO KOICHI , NORIMINE YOSHIHIKO , UENO KOHSHI , HANADA TAKAHISA , AMINO HIROYUKI , OGO MAKOTO , HATAKEYAMA SHINJI , UENO MASATAKA , GROOM ANTHONY JOHN , RIVERS LEANNE , SMITH TERENCE
IPC分类号： C07D237/14 , C07D237/24 , C07D401/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D237/04 , C07D401/06 , C07D409/04 , C07D401/14 , C07D405/14 , C07D403/14 , C07D409/14 , C07D417/04 , C07D235/06 , A61K31/501 , A61K31/50 , A61K31/5025 , A61K31/506 , A61K31/53 , A61K31/5377
摘要： Disclosed are compounds of formula (I), wherein: A1, A2 and A3 are independently cycloalkyl, cycloalkenyl, non-aromatic heterocycle, aromatic hydrocarbon heterocycle, which may be substituted, Q is O, S or NH, Z is C or N, and the remaining substituents are defined herein. The compounds are used for the manufacture of medicaments for the treatment or prevention of diseases in which an AMPA receptor or kainite receptor is participated.

53. 发明专利

ZA200301537B Pyridazinones and triazinones and medicinal use thereof. 未知
公开(公告)号：ZA200301537B
公开(公告)日：2004-02-25
申请号：ZA200301537
申请日：2003-02-25
申请人： EISAI CO LTD
发明人： NAGATO SATOSHI , KAWANO KOKI , ITO KOICHI , NORIMINE YOSHIHIKO , UENO KOHSHI , HANADA TAKAHISA , AMINO HIROYUKI , OGO MAKOTO , HATAKEYAMA SHINJI , UENO MASATAKA , GROOM ANTHONY JOHN , RIVERS LEANNE , SMITH TERENCE
IPC分类号： A61K20060101 , C07D20060101 , C07D , A61K

54. 发明专利

AU767849B2 Heterodiazinone derivatives 未知
公开(公告)号：AU767849B2
公开(公告)日：2003-11-27
申请号：AU2461800
申请日：2000-02-15
申请人： EISAI CO LTD
发明人： ITO KOICHI , KITAZAWA NORITAKA , NAGATO SATOSHI , KAJIWARA AKIHARU , FUKUSHIMA TATSUTO , HATAKEYAMA SHINJI , HANADA TAKAHISA , UENO MASATAKA , UENO KOHSHI , KAWANO KOKI
IPC分类号： A61K31/53 , A61K31/5395 , A61K31/549 , A61P25/00 , C07D249/12 , C07D271/10 , C07D271/113 , C07D285/16 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D253/06 , C07D273/04 , C07D285/18
摘要： The present invention provides a novel compound having an excellent 2-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor antagonistic action, particularly a therapeutic, preventing and ameliorating action useful for cerebral ischemia, cerebrospinal injuries, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's chorea, epilepsy, pain, spastic paralysis, multiple sclerosis etc. That is, the present invention provides a heterodiazinon compound represented by the following formula (I), a pharmacologically acceptable salt thereof or hydrates thereof. Wherein A represents an oxygen atom, a sulfur atom or a group represented by the formula >NR (wherein R represents hydrogen atom or a lower alkyl group); R and R are the same as or different from each other and each represents an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted aralkyl group, an optionally substituted heteroaryl alkyl group, an optionally substituted aryl alkenyl group, an optionally substituted heteroaryl alkenyl group, an optionally substituted piperidyl group, an optionally substituted piperazinyl group; a morpholinyl group, an optionally substituted lower cycloalkyl group, a tetrahydrofuranyl group, a tetrahydropyranyl group, an adamantyl group, an optionally substituted amino group or an optionally substituted amide group; and R and R are the same as or different from each other and each represents hydrogen atom, hydroxy, a halogen atom, nitrile group, nitro group, a lower alkyl group, an aryl group or a heteroaryl group, provided that the compounds represented by the following formula (II): (wherein R and R are the same as or different from each other and each represents hydrogen atom, fluorine, chlorine, bromine, iodine, a C1-C2 fluoroalkyl group, a C1-C2 chloroalkyl group, a C1-C2 bromoalkyl group, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C7-C9 aralkyl group, phenyl group, a C1-C6 alkoxy group, a C1-C6 alkylthio group, a C1-C6 alkylsulfinyl group, a C7-C9 aralkoxy group, phenoxy group, phenylthio group, phenylsulfonyl group, alkali metal carboxylate C2-C5 alkoxycarbonyl group or a group represented by the formula -N(R )R (wherein R and R are the same as or different from each other and each represents hydrogen atom or a C1-C2 alkyl group); and R and R are the same as or different from each other and each represents a C1-4 alkylsulfonyl group, nitro group, a group represented by the formula -OCHnX3-n (wherein X represents fluorine, chlorine, bromine or iodine; and n is any of integers 1 to 3) or a group having the same meanings as the definitions of R and R ) are excluded.

55. 发明专利

NO20031232D0 未知
公开(公告)号：NO20031232D0
公开(公告)日：2003-03-17
申请号：NO20031232
申请日：2003-03-17
申请人： EISAI CO LTD
发明人： NAGATO SATOSHI , KAWANO KOKI , ITO KOICHI , NORIMINE YOSHIHIKO , UENO KOHSHI , HANADA TAKAHISA , AMINO HIROYUKI , OGO MAKOTO , HATAKEYAMA SHINJI , UENO MASATAKA , GROOM ANTHONY JOHN , RIVERS LEANNE , SMITH TERENCE
IPC分类号： C07D237/14 , C07D237/24 , C07D401/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D
摘要： The present invention provides a novel compound exhibiting an excellent inhibitory action on AMPA receptor and/or kainate receptor. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, A , A and A are independent of each other and each represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a 5- to 14-membered non-aromatic heterocyclic group, a C6-14 aromatic hydrocarbon cyclic group or a 5- to 14-membered aromatic heterocyclic group, each of which may be substituted; Q represents O, S or NH; Z represents C or N; X , X and X are independent of each other and each represents a single bond, an optionally substituted C1-6 alkylene group, an optionally substituted C2-6 alkenylene group, an optionally substituted C2-6 alkynylene group, -NH-, -O-, -NHCO-, -CONH-, -SO0-2-, etc.; R and R are independent of each other and each represents a hydrogen atom or an optionally substituted C1-6 alkyl group, or R and R may be bound together such that CR -ZR forms C=C; and R represents a hydrogen atom or an optionally substituted C1-6 alkyl group etc., or may be bound to any atom in A or A to form, together with the atom, an optionally substituted C5-8 hydrocarbon ring or an optionally substituted 5- to 8-membered heterocyclic ring.

56. 发明专利

CA2412172A1 1,2-DIHYDROPYRIDINE COMPOUNDS, MANUFACTURING METHOD THEREOF AND USE THEREOF 未知
公开(公告)号：CA2412172A1
公开(公告)日：2002-12-06
申请号：CA2412172
申请日：2001-06-08
申请人： EISAI CO LTD
发明人： UENO KOHSHI , HANADA TAKAHISA , RIVERS LEANNE , KAWANO KOKI , ITO KOICHI , SMITH TERENCE , NORIMINE YOSHIHIKO , OGO MAKOTO , AMINO HIROYUKI , NAGATO SATOSHI , GROOM ANTHONY JOHN , NAKA HIROYUKI , UENO MASATAKA , HATAKEYAMA SHINJI , URAWA YOSHIO
IPC分类号： A61K20060101 , A61P20060101 , A61P1/08 , A61P9/10 , A61P13/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D213/64 , C07D213/65 , C07D213/69 , C07D213/70 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/81 , C07D213/84 , C07D213/89 , C07D401/04 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D471/06 , C07F7/18 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/5377 , C07D213/71 , C07D213/82
摘要： Provided are novel compounds exhibiting excellent inhibitory activities against AMPA receptor and/or kainite receptor, specifically compounds of the general formula (I), salts of the same, or hydrates of both, wherein Q is NH , O, or S; and R1, R2, R3, R4 and R5 are each independently hydrogen, halogeno , C1-6 alkyl, or a group of the general formula: -X-A (wherein X is a single bond, optionally substituted C1-6 alkylene, or the like; and A is, e.g., a C 6- 14 aromatic carbocyclic group or a 5- to 14-membered aromatic heterocyclic group, any of which may be optionally substituted).

57. 发明专利

DE69528485D1 未知
公开(公告)号：DE69528485D1
公开(公告)日：2002-11-14
申请号：DE69528485
申请日：1995-03-22
申请人： EISAI CO LTD
发明人： AKASAKA KOZO , YONAGA MASAHIRO , KAJIWARA AKIHARU , HIGURASHI KUNIZO , UENO KOHSHI , NAGATO SATOSHI , KOMATSU MAKOTO , KITAZAWA NORITAKA , UENO MASATAKA , YAMANISHI YOSHIHARU , MACHIDA YOSHIMASA , KOMATSU YUKI , SHIMOMURA NAOYUKI , MINAMI NORIO , SHIMIZU TOSHIKAZU , NAGAOKA ATSUSHI
IPC分类号： C07D295/03 , A61K31/495 , A61P25/18 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/50 , C07D213/70 , C07D295/02 , C07D295/04 , C07D295/073 , C07D295/088 , C07D295/096 , C07D295/112 , C07D295/135 , C07D295/155 , C07D295/205 , C07D295/26 , C07D307/14 , C07D307/52 , C07D319/06 , C07D339/08 , C07F7/18 , C07D213/36 , C07D295/20 , C07D295/06
摘要： A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R represents a hydrogen atom, a halogen atom, a hydroxyl group, an amino group, a lower alkyl group, a halogenated lower alkyl group, a lower alkoxy group, a halogenated lower alkoxy group, a lower alkoxyalkyl group, a lower alkoxyalkoxy group, an aryl group, an aralkyl group, a heteroaryl group, a heteroarylalkyl group, a halogenated heteroarylalkyl group, a cyano lower alkyl group, a hydroxy lower alkyl group, an amino lower alkyl group, a lower alkoxycarbonyl group, an aryloxycarbonyl group, a cyano group, a formyl group, a lower acyl group, an aralkylcarbonyl group, a cycloether group, an alkenyl group, an alkynyl group, a lower alkylsulfinyl group, a lower alkylsulfonyl group, a lower alkylaminosulfonyl group, an arylaminosulfonyl group, a lower alkylsulfonylamino group, a halogenated lower alkylsulfonylamino group or an arylsulfonylamino group; R and R may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a halogenated lower alkyl group, a lower alkoxy group, a halogenated lower alkoxy group or a cyano group; R represents a hydrogen atom or a halogen atom; R represents a hydrogen atom, a lower alkyl group, a halogenated lower alkyl group, a hydroxy lower alkyl group, a lower alkoxycarbonyl group or an aryloxycarbonyl group; and n is 0 or an integer of 1 to 3, which exhibits dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis.

58. 发明专利

NZ337651A 1,4-substituted cyclic amine derivatives, preparation and use as seretonin antagonists 未知
公开(公告)号：NZ337651A
公开(公告)日：2002-04-26
申请号：NZ33765198
申请日：1998-03-31
申请人： EISAI CO LTD
发明人： KITAZAWA NORITAKA , UENO KOHSHI , TAKAHASHI KEIKO , KIMURA TEIJI , SASAKI ATSUSHI , KAWANO KOKI , OKABE TADAHSI , KOMATSU MAKOTO , MATSUNAGA MANABU , KUBOTA ATSUHIKO
IPC分类号： C07D211/22 , A61K31/135 , A61P21/02 , C07D211/26 , C07D211/74 , C07D217/02 , C07D217/04 , C07D221/04 , C07D295/08 , C07D295/10 , C07D295/18 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D417/14 , C07D491/04 , C07D491/056 , C07D513/04 , C07D521/00 , A61K31/535 , A61K31/40 , C07D295/12 , A61K31/47 , A61K31/55 , C07D471/04 , C07D409/14 , A61K31/445 , A61K31/435 , A61K31/495
摘要： A 1,4-substituted cyclic amine derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof is disclosed, wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R1, R2, R3, R4 and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.

59. 发明专利

AU9022901A Pyridazinones and triazinones and medicinal use thereof 未知
公开(公告)号：AU9022901A
公开(公告)日：2002-03-26
申请号：AU9022901
申请日：2001-09-17
申请人： EISAI CO LTD
发明人： NAGATO SATOSHI , KAWANO KOKI , ITO KOICHI , NORIMINE YOSHIHIKO , UENO KOHSHI , HANADA TAKAHISA , AMINO HIROYUKI , OGO MAKOTO , HATAKEYAMA SHINJI , UENO MASATAKA , GROOM ANTHONY JOHN , RIVERS LEANNE , SMITH TERENCE
IPC分类号： C07D237/14 , C07D237/24 , C07D401/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D237/04 , C07D401/06 , C07D409/04 , C07D401/14 , C07D405/14 , C07D403/14 , C07D409/14 , C07D417/04 , C07D253/06 , A61K31/501 , A61K31/50 , A61K31/5025 , A61K31/506 , A61K31/53 , A61K31/5377
摘要： The present invention provides a novel compound exhibiting an excellent inhibitory action on AMPA receptor and/or kainate receptor. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, A , A and A are independent of each other and each represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a 5- to 14-membered non-aromatic heterocyclic group, a C6-14 aromatic hydrocarbon cyclic group or a 5- to 14-membered aromatic heterocyclic group, each of which may be substituted; Q represents O, S or NH; Z represents C or N; X , X and X are independent of each other and each represents a single bond, an optionally substituted C1-6 alkylene group, an optionally substituted C2-6 alkenylene group, an optionally substituted C2-6 alkynylene group, -NH-, -O-, -NHCO-, -CONH-, -SO0-2-, etc.; R and R are independent of each other and each represents a hydrogen atom or an optionally substituted C1-6 alkyl group, or R and R may be bound together such that CR -ZR forms C=C; and R represents a hydrogen atom or an optionally substituted C1-6 alkyl group etc., or may be bound to any atom in A or A to form, together with the atom, an optionally substituted C5-8 hydrocarbon ring or an optionally substituted 5- to 8-membered heterocyclic ring.

60. 发明专利

HK1026700A1 1,4-Substituted cyclic amine derivatives or dihydroindole derivatives and medicament thereof. 未知
公开(公告)号：HK1026700A1
公开(公告)日：2000-12-22
申请号：HK00105871
申请日：2000-09-19
申请人： EISAI CO LTD
发明人： KITAZAWA NORITAKA , UENO KOHSHI , TAKAHASHI KEIKO , KIMURA TEIJI , SASAKI ATSUSHI , KAWANO KOKI , OKABE TADASHI , KOMATSU MAKOTO , MATSUNAGA MANABU , KUBOTA ATSUHIKO
IPC分类号： C07D211/22 , A61K31/135 , A61P21/02 , C07D211/26 , C07D211/74 , C07D217/02 , C07D217/04 , C07D221/04 , C07D295/08 , C07D295/10 , C07D295/18 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D417/14 , C07D491/04 , C07D491/056 , C07D513/04 , C07D521/00 , C07D , A61K
摘要： A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: (wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R , R , R , R and R represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3.) The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.

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