公开(公告)号：EP1240823A4

公开(公告)日：2003-05-02

申请号：EP00970097

申请日：2000-10-26

申请人： EISAI CO LTD

发明人： INO MITSUHIRO ,  MIYAMOTO NORIMASA ,  TAKAHASHI EIKI ,  OKI TORU ,  YOSHINAGA TAKASHI ,  HATAKEYAMA SHINJI ,  NIIDOME TETSUHIRO ,  SAWADA KOHEI ,  NISHIZAWA YUKIO ,  TANAKA ISAO

IPC分类号： A61P3/10 ,  A61P9/12 ,  A61P25/04 ,  C07K14/705 ,  C12N15/85 ,  A01K67/027 ,  A61K45/00 ,  C12N15/12 ,  G01N33/15 ,  G01N33/50

CPC分类号： A01K67/0276 ,  A01K2217/05 ,  A01K2217/075 ,  A01K2227/105 ,  A01K2267/03 ,  C07K14/705 ,  C12N15/8509

摘要： A non-human animal from which functional N-calcium channel has been deleted by disrupting a gene encoding N-calcium channel; and a method of screening substances having pharmacological effects relating to blood pressure control, pain transfer, blood glucose level control, etc.

公开(公告)号：EP1254895A4

公开(公告)日：2003-01-22

申请号：EP01901413

申请日：2001-01-18

申请人： EISAI CO LTD

发明人： YAMAMOTO NOBORU ,  SUZUKI YUICHI ,  KIMURA MANAMI ,  NIIDOME TETSUHIRO ,  IIMURA YOICHI ,  TERAMOTO TETSUYUKI ,  KANEDA YOSHIHISA ,  KANEKO TOSHIHIKO ,  KURUSU NOBUYUKI ,  SHINMYO DAISUKE ,  YOSHIKAWA YUKIE ,  HATAKEYAMA SHINJI

IPC分类号： A61K31/395 ,  A61P9/10 ,  C07D207/09 ,  C07D207/14 ,  C07D207/16 ,  C07D207/32 ,  C07D207/337 ,  C07D209/14 ,  C07D209/42 ,  C07D211/22 ,  C07D211/26 ,  C07D211/32 ,  C07D211/34 ,  C07D211/46 ,  C07D211/58 ,  C07D211/64 ,  C07D213/36 ,  C07D213/38 ,  C07D213/57 ,  C07D213/74 ,  C07D215/06 ,  C07D215/12 ,  C07D215/22 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D217/22 ,  C07D235/10 ,  C07D235/14 ,  C07D235/30 ,  C07D241/04 ,  C07D243/08 ,  C07D261/08 ,  C07D263/20 ,  C07D263/32 ,  C07D263/58 ,  C07D271/06 ,  C07D277/28 ,  C07D277/42 ,  C07D277/82 ,  C07D295/14 ,  C07D295/145 ,  C07D295/185 ,  C07D295/192 ,  C07D295/215 ,  C07D307/52 ,  C07D307/54 ,  C07D307/81 ,  C07D319/20 ,  C07D333/24 ,  C07D333/28 ,  C07D333/38 ,  C07D333/60 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D405/06 ,  C07D409/00 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/08 ,  C07D417/12 ,  C07D471/10 ,  C07D487/08 ,  A61K31/36 ,  A61K31/435 ,  A61K31/495

CPC分类号： C07D207/337 ,  C07D207/09 ,  C07D207/14 ,  C07D207/16 ,  C07D209/14 ,  C07D209/42 ,  C07D211/22 ,  C07D211/26 ,  C07D211/32 ,  C07D211/34 ,  C07D211/46 ,  C07D211/58 ,  C07D211/64 ,  C07D213/36 ,  C07D213/57 ,  C07D213/74 ,  C07D215/06 ,  C07D215/12 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D217/22 ,  C07D235/14 ,  C07D235/30 ,  C07D241/04 ,  C07D243/08 ,  C07D261/08 ,  C07D263/20 ,  C07D263/32 ,  C07D263/58 ,  C07D271/06 ,  C07D277/28 ,  C07D277/42 ,  C07D277/82 ,  C07D295/145 ,  C07D295/185 ,  C07D295/192 ,  C07D295/215 ,  C07D307/52 ,  C07D307/54 ,  C07D307/81 ,  C07D319/20 ,  C07D333/24 ,  C07D333/28 ,  C07D333/38 ,  C07D333/60 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D471/10 ,  C07D487/08

摘要： Novel compounds exhibiting excellent calcium antagonism, particularly neuroselective calcium antagonism, namely, compounds of the general formula (I), salts of the same, or hydrates of both wherein Ar is a group derived from an optionally substituted 5- to 14-membered aromatic ring, or the like; the ring A is one member selected from among piperazine, homopiperazine, piperidine and so on; the ring B is an optionally substituted C3-14 hydrocarbon ring or the like; E is a single bond, -CO-, or the like; X is a single bond, oxygen, or the like; R1 is hydrogen, halogeno, hydroxyl, or the like; and D?1, D2, W1 and W2¿ are each independently a single bond or optionally substituted C¿1-6? alkylene.

公开(公告)号：EP1300396A4

公开(公告)日：2005-06-15

申请号：EP01936920

申请日：2001-06-08

申请人： EISAI CO LTD

发明人： NAGATO SATOSHI ,  UENO KOHSHI ,  KAWANO KOKI ,  NORIMINE YOSHIHIKO ,  ITO KOICHI ,  HANADA TAKAHISA ,  UENO MASATAKA ,  AMINO HIROYUKI ,  OGO MAKOTO ,  HATAKEYAMA SHINJI ,  URAWA YOSHIO ,  NAKA HIROYUKI ,  GROOM ANTHONY JOHN ,  RIVERS LEANNE ,  SMITH TERENCE

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 ,  C07D213/71 ,  A61K31/44

CPC分类号： C07F7/1856 ,  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

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 R?1, R2, R3, R4 and R5¿ are each independently hydrogen, halogeno, C¿1-6? 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 C6-14 aromatic carbocyclic group or a 5- to 14-membered aromatic heterocyclic group, any of which may be optionally substituted).

公开(公告)号：EP1153922A4

公开(公告)日：2002-05-15

申请号：EP00902953

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

CPC分类号： C07D271/113 ,  A61K31/53 ,  A61K31/5395 ,  A61K31/549 ,  C07D249/12 ,  C07D285/16 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14

摘要： Heterodiazinone derivatives represented by general formula (1 ), pharmacologically acceptable salts of the same, or hydrates of both, exhibiting 2-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonism wherein A is O, S or NR3 (wherein R3 is hydrogen or lower alkyl); R?1 and R2¿ are each independently optionally substituted (hetero)aryl or the like; and R?4 and R5¿ are each independently hydrogen, hydroxyl, halogeno, cyano, nitro, lower alkyl, (hetero)aryl, or the like.

摘要翻译： 由通式（1）表示的异二嗪酮衍生物，其药理学上可接受的盐或两者的水合物显示2-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体拮抗作用，其中A是O，S 或NR 3（其中R 3是氢或低级烷基）; R 1和R 2'各自独立地为任选取代的（杂）芳基等; R 4和R 5各自独立地为氢，羟基，卤素，氰基，硝基，低级烷基，（杂）芳基等。

公开(公告)号：EP1319659A4

公开(公告)日：2005-08-10

申请号：EP01970120

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 ,  A61K31/50 ,  A61P25/00 ,  C07D401/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14

CPC分类号： C07D237/24 ,  C07D237/14 ,  C07D401/04 ,  C07D491/04

摘要： Provided are novel compounds exhibiting excellent inhibitory activities against AMPA receptor and/or kainate receptor, i.e., compounds of the general formula (I), salts thereof, or hydrates of both wherein A?1, A2 and A3¿ are each independently C¿3-8? cycloalkyl, C3-8 cycloalkenyl, a 5- to 14-membered nonoaromatic heterocyclic group, a C6-14 aromatic carbocyclic group, or a 5- to 14-membered aromatic heterocyclic group, any of which may be substituted; Q is O, S, or NH; Z is C or N; X?1, X2 and X3¿ are each independently a single bond, optionally substituted C¿1-6? alkylene, optionally substituted C2-6 alkenylene, optionally substituted C2-6 alkynylene, -NH-, -O-, -NHCO-, -CONH-, -SO0-2-, or the like; R?1 and R2¿ are each independently hydrogen or optionally substituted C¿1-6? alkyl, or alternatively R?1 and R2¿ may be united in such a way that CR2-ZR1 forms C=C; and R3 is hydrogen, optionally substituted C¿1-6? alkyl, or the like, or alternatively R?3¿ may unite with any atom on the ring A1 or A3 to form together with the atom an optionally substituted C¿5-8? carbocycle or an optionally substituted 5- to 8-membered heterocycle.

公开(公告)号：EP1099692A4

公开(公告)日：2002-05-15

申请号：EP99931461

申请日：1999-07-21

申请人： EISAI CO LTD

发明人： YAMAMOTO NOBORU ,  KOMATSU MAKOTO ,  SUZUKI YUICHI ,  KAWANO KOKI ,  KIMURA TEIJI ,  ITO KOICHI ,  NAGATO SATOSHI ,  NORIMINE YOSHIHIKO ,  NIIDOME TETSUHIRO ,  TERAMOTO TETSUYUKI ,  IIMURA YOICHI ,  HATAKEYAMA SHINJI

IPC分类号： C07D295/08 ,  A61K31/496 ,  A61P9/10 ,  A61P25/28 ,  C07D213/57 ,  C07D213/64 ,  C07D215/20 ,  C07D217/02 ,  C07D233/54 ,  C07D233/58 ,  C07D239/34 ,  C07D239/80 ,  C07D317/64 ,  C07D333/24 ,  C07D333/38 ,  C07D401/12 ,  C07D403/12 ,  C07D213/30 ,  A61K31/495 ,  C07D243/08 ,  C07D295/12 ,  C07D295/14 ,  C07D333/16

CPC分类号： C07D213/64 ,  C07D213/57 ,  C07D215/20 ,  C07D217/02 ,  C07D233/54 ,  C07D239/34 ,  C07D239/80 ,  C07D295/15 ,  C07D317/64 ,  C07D333/24 ,  C07D333/38

摘要： N,N-substituted cyclic amine derivatives represented by general formula (VIII) or pharmacologically acceptable salts thereof: wherein A represents aryl, etc.; E represents -CO- or -CHOH-; G represents oxygen, etc.; J represents optionally substituted aryl; R1 represents lower alkyl, etc.; Alk represents linear or branched lower alkylene; n, v, w, x and y independently represent each 0 or 1; and p represents 2 or 3. These compounds or salts thereof are efficacious in treating diseases against which calcium antagonism is efficacious. These diseases include cerebrovascular disorder at the acute stage, cerebral stroke, cerebral infarction, head injury, cerebral nerve cell death, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, brain circulatory disturbance, brain function disturbance, pain, convulsion, schizophrenia, hemicrania, epilepsy, circular psychosis, nerve degeneration diseases, brain ischemia, AIDS, complex dementia, edema, anxiety and diabetic nephropathy.

摘要翻译： 由通式（VIII）表示的N，N-取代的环胺衍生物或其药理学上可接受的盐：其中A表示芳基等; E表示-CO-或-CHOH-; G代表氧气等; J表示任选取代的芳基; R 1表示低级烷基等; Alk表示直链或支链低级亚烷基; n，v，w，x和y独立地表示0或1; 并且p表示2或3.这些化合物或其盐在治疗有效钙拮抗作用的疾病中是有效的。 这些疾病包括急性期的脑血管障碍，脑中风，脑梗塞，头部损伤，脑神经细胞死亡，阿尔茨海默病，帕金森病，肌萎缩性侧索硬化，亨廷顿病，脑循环障碍，脑功能紊乱，疼痛，惊厥，精神分裂症 ，hemicrania，癫痫，圆形精神病，神经变性疾病，脑缺血，艾滋病，复杂性痴呆，水肿，焦虑和糖尿病肾病。