公开(公告)号：EP0418065B1

公开(公告)日：1994-04-20

申请号：EP90309997.6

申请日：1990-09-12

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Fukazawa, Nobuyuki ,  Iizuka, Hajime ,  Yano, Osamu ,  Miyama, Yukio

IPC分类号： C07C235/34 ,  C07D295/18 ,  C07D213/80 ,  A61K31/16 ,  A61K31/44 ,  C07C235/36

CPC分类号： C07D213/80 ,  C07C235/34 ,  C07C235/36 ,  C07C2601/14 ,  C07C2603/74 ,  C07D295/185

公开(公告)号：EP0418065A2

公开(公告)日：1991-03-20

申请号：EP90309997.6

申请日：1990-09-12

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Fukazawa, Nobuyuki ,  Iizuka, Hajime ,  Yano, Osamu ,  Miyama, Yukio

IPC分类号： C07C235/34 ,  C07D295/18 ,  C07D213/80 ,  A61K31/16 ,  A61K31/44 ,  C07C235/36

CPC分类号： C07D213/80 ,  C07C235/34 ,  C07C235/36 ,  C07C2601/14 ,  C07C2603/74 ,  C07D295/185

摘要： Dihydrocaffeic acid derivatives are disclosed which are applicable as medicines having excellent absorbency in the case of oral administration and good concentration retention in blood.
The disclosed compounds have the function to induce the production and secretion of a nerve growth factor (NGF) in the brain tissue, and accordingly are effective as medicines for inhibiting the progression of regressive disorders of the central nervous system and for the therapeutic treatment of such disorders.

公开(公告)号：EP0295695B1

公开(公告)日：1994-06-08

申请号：EP88109678.8

申请日：1988-06-16

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Yamashita, Hiroyuki ,  Odate, Makoto ,  Iizuka, Hajime ,  Kawazura, Hiroshi ,  Shiga, Yoshio ,  Namekawa, Hiroshi

IPC分类号： C07D401/06 ,  A61K31/415 ,  C07D405/14 ,  C07D403/06 ,  C07D401/04 ,  C07D231/06 ,  A61K31/44 ,  A61K31/34 ,  A61K31/50

CPC分类号： C07D231/06 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06

公开(公告)号：EP0373512A1

公开(公告)日：1990-06-20

申请号：EP89122591.4

申请日：1989-12-07

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Kajiya, Seitaro ,  Iizuka, Hajime ,  Okumura, Kunio ,  Fujiwara, Junya ,  Ohto, Norio ,  Kawazura, Hiroshi ,  Takahashi, Yasuhiro ,  Shiga, Yoshio

IPC分类号： C07D401/06 ,  A61K31/415 ,  A61K31/44

CPC分类号： C07D401/06

摘要： The present invention relates to a novel (-)-2-­pyrazoline compound and therapeutic agents containing the same as an effective ingredient; furthermore, it relates to a method for optically resolving 1-(3-pyridylcarbonyl)-­methyl-2-pyrazoline.

摘要翻译： 本发明涉及一种新型的（ - ） - 2-吡唑啉化合物和含相同上有效成分的治疗剂; 更进一步，本发明涉及用于光学拆分1-（3-吡啶基羰基）甲基-2-吡唑啉的方法。

公开(公告)号：EP0295695A3

公开(公告)日：1990-06-06

申请号：EP88109678.8

申请日：1988-06-16

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Yamashita, Hiroyuki ,  Odate, Makoto ,  Iizuka, Hajime ,  Kawazura, Hiroshi ,  Shiga, Yoshio ,  Namekawa, Hiroshi

IPC分类号： C07D401/06 ,  A61K31/415 ,  C07D405/14 ,  C07D403/06 ,  C07D401/04 ,  C07D231/06 ,  A61K31/44 ,  A61K31/34 ,  A61K31/50

CPC分类号： C07D231/06 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06

摘要： This invention relates to new 2-pyrazoline derivatives represented by the following general formula (A):
( wherein R¹ denotes a pyridyl, a pyrazyl or an alkoxyl group; and R² stands for hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group ), and to a process for producing the same. This invention also relates to agents for treating cerebrovascular diseases containing, as active ingredients, a 2-pyrazoline derivative represented by the following general formula (G):
( wherein R³ denotes hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcabonyl, a thienylcarbonyl, a pyrazylcarbonyl, an N-substituted carbamoyl, an N-sub­stituted thiocarbamoyl, or carboxyl group; and R⁴ stands for hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group ) or a pharmaceutically acceptable salt thereof. Administration of an agent of this invention for treat­ing cerebrovascular diseases copes with cerebral edemata in the acute stage of cerebral apoplexy and regulates the whole-body and intracranial blood circulation, thereby protecting ischemic lesions and minimizing the spread of affected parts.

公开(公告)号：EP0839805A1

公开(公告)日：1998-05-06

申请号：EP97308798.4

申请日：1997-11-03

申请人： MITSUI TOATSU CHEMICALS, INC.

发明人： Mita, Naruyoshi ,  Nagase, Hiroshi ,  Iizuka, Hajime ,  Oguchi, Takahisa ,  Sakai, Kazuya ,  Horikomi, Kazutoshi ,  Miwa, Takaichi ,  Takahashi, Shinji

IPC分类号： C07D207/27 ,  A61K31/495

CPC分类号： C07D207/27 ,  A61K31/496

摘要： Pyrrolidinone derivatives of general formula
wherein R 1 is hydrogen or halogen, R 2 is hydrogen,C 1-3 alkyl, C 2-3 alkenyl or C 2-3 alkynyl, and n is 2 or 3,
their pharmaceutically acceptable salts, hydrates and/or enantiomers,
are useful as sigma receptor antagonists in the treatment of among others psychosis.

摘要翻译： 通式为CHEM的吡咯烷酮衍生物，其中R 1为氢或卤素，R 2为氢，C 1-3烷基，C 2-3烯基或C 2-3炔基，n为2或3，其药学上可接受的盐，水合物 和/或对映异构体在治疗精神病中可用作σ受体拮抗剂。

公开(公告)号：EP0373512B1

公开(公告)日：1992-04-08

申请号：EP89122591.4

申请日：1989-12-07

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Kajiya, Seitaro ,  Iizuka, Hajime ,  Okumura, Kunio ,  Fujiwara, Junya ,  Ohto, Norio ,  Kawazura, Hiroshi ,  Takahashi, Yasuhiro ,  Shiga, Yoshio

IPC分类号： C07D401/06 ,  A61K31/415 ,  A61K31/44

CPC分类号： C07D401/06

公开(公告)号：EP0418065A3

公开(公告)日：1991-06-26

申请号：EP90309997.6

申请日：1990-09-12

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Fukazawa, Nobuyuki ,  Iizuka, Hajime ,  Yano, Osamu ,  Miyama, Yukio

IPC分类号： C07C235/34 ,  C07D295/18 ,  C07D213/80 ,  A61K31/16 ,  A61K31/44 ,  C07C235/36

CPC分类号： C07D213/80 ,  C07C235/34 ,  C07C235/36 ,  C07C2601/14 ,  C07C2603/74 ,  C07D295/185

摘要： Dihydrocaffeic acid derivatives are disclosed which are applicable as medicines having excellent absorbency in the case of oral administration and good concentration retention in blood. The disclosed compounds have the function to induce the production and secretion of a nerve growth factor (NGF) in the brain tissue, and accordingly are effective as medicines for inhibiting the progression of regressive disorders of the central nervous system and for the therapeutic treatment of such disorders.

摘要翻译： 公开了二氯咖啡酸衍生物，其适用于在口服给药和在血液中保持良好浓度时具有优异吸收性的药物。 所公开的化合物具有诱导脑组织中神经生长因子（NGF）的产生和分泌的功能，因此作为用于抑制中枢神经系统的退行性病症进展的药物以及用于治疗性治疗的药物是有效的 障碍。

公开(公告)号：EP0322691A1

公开(公告)日：1989-07-05

申请号：EP88121187.4

申请日：1988-12-17

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Yamashita, Hiroyuki ,  Okumura, Kunio ,  Iizuka, Hajime ,  Ohto, Norio

IPC分类号： C07D231/06 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14

CPC分类号： C07D231/06 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14

摘要： 1-Acyl-2-pyrazoline derivatives represented by the formula
where R¹ denotes a hydrogen atom, pyridyl group, pyrazinyl group, alkyl group, aryl group, or alkoxy group; and R², R³, and R⁴ independently denote a hydrogen atom, furyl group, pyridyl group, alkyl group, or aryl group, are produced by cyclizing by heating an acylhydrazone derivative represented by the formula
where R¹, R², R³, and R⁴ are defined as above, to produce compounds having useful anti-cerebral edema activity.

摘要翻译： 由式表示的1-酰基-2-吡唑啉衍生物，其中R 1表示氢原子，吡啶基，吡嗪基，烷基，芳基或烷氧基; R 2，R 3和R 4分别独立地表示氢原子，呋喃基，吡啶基，烷基或芳基，通过加热由式CHEM所代表的酰腙衍生物 >其中R 1，R 2，R 3和R 4定义如上，以产生具有有用的抗脑水肿活性的化合物。

公开(公告)号：EP0322691B1

公开(公告)日：1994-06-15

申请号：EP88121187.4

申请日：1988-12-17

申请人： MITSUI TOATSU CHEMICALS, Inc.

发明人： Yamashita, Hiroyuki ,  Okumura, Kunio ,  Iizuka, Hajime ,  Ohto, Norio

IPC分类号： C07D231/06 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14

CPC分类号： C07D231/06 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D405/14