公开(公告)号：US5397785A

公开(公告)日：1995-03-14

申请号：US115257

申请日：1993-09-02

申请人： Kunihiro Ninomiya, deceased ,  Ken-ichi Sato ,  Mamoru Sugano ,  Akihiro Tobe ,  Yasuhiro Morinaka ,  Tomoko Bessho ,  Haruko Harada

发明人： Kunihiro Ninomiya, deceased ,  Ken-ichi Sato ,  Mamoru Sugano ,  Akihiro Tobe ,  Yasuhiro Morinaka ,  Tomoko Bessho ,  Haruko Harada

IPC分类号： C07D219/10 ,  C07D221/16 ,  C07D221/20 ,  C07D221/22 ,  C07D401/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/44

CPC分类号： C07D221/20 ,  C07D219/10 ,  C07D221/16 ,  C07D221/22 ,  C07D401/12 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04

摘要： A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

摘要翻译： 公开了由下式（I）表示的新型4-酰氨基吡啶衍生物。 （I）本发明的4-酰基氨基吡啶衍生物作为治疗老年性痴呆和阿尔茨海默氏病等记忆障碍的药物是有用的，因为它具有直接激活故障胆碱能神经元的作用。

公开(公告)号：US5861411A

公开(公告)日：1999-01-19

申请号：US629901

申请日：1996-04-10

申请人： Kunihiro Ninomiya, deceased ,  Ken-ichi Saito ,  Mamoru Sugano ,  Akihiro Tobe ,  Yasuhiro Morinaka ,  Tomoko Bessho ,  Haruko Harada

发明人： Kunihiro Ninomiya, deceased ,  Ken-ichi Saito ,  Mamoru Sugano ,  Akihiro Tobe ,  Yasuhiro Morinaka ,  Tomoko Bessho ,  Haruko Harada

IPC分类号： C07D219/10 ,  C07D221/16 ,  C07D221/20 ,  C07D221/22 ,  C07D401/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/44

CPC分类号： C07D221/20 ,  C07D219/10 ,  C07D221/16 ,  C07D221/22 ,  C07D401/12 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04

摘要： A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

摘要翻译： 公开了由下式（I）表示的新型4-酰氨基吡啶衍生物。 （I）本发明的4-酰基氨基吡啶衍生物作为治疗老年性痴呆和阿尔茨海默氏病等记忆障碍的药物是有用的，因为它具有直接激活故障胆碱能神经元的作用。

公开(公告)号：US5536728A

公开(公告)日：1996-07-16

申请号：US355181

申请日：1994-12-08

申请人： Kunihiro Ninomiya, deceased ,  Ken-ichi Saito ,  Mamoru Sugano ,  Akihiro Tobe ,  Yasuhiro Morinaka ,  Tomoko Bessho ,  Haruko Harada

发明人： Kunihiro Ninomiya, deceased ,  Ken-ichi Saito ,  Mamoru Sugano ,  Akihiro Tobe ,  Yasuhiro Morinaka ,  Tomoko Bessho ,  Haruko Harada

IPC分类号： C07D219/10 ,  C07D221/16 ,  C07D221/20 ,  C07D221/22 ,  C07D401/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/44

CPC分类号： C07D221/20 ,  C07D219/10 ,  C07D221/16 ,  C07D221/22 ,  C07D401/12 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04

摘要： A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

公开(公告)号：US4977151A

公开(公告)日：1990-12-11

申请号：US501591

申请日：1990-03-29

申请人： Shinichiro Fujimori ,  Satoshi Yamazaki ,  Mamoru Sugano ,  Makoto Kawamura ,  Kunihiro Ninomiya ,  Akihiro Tobe ,  Issei Nitta

发明人： Shinichiro Fujimori ,  Satoshi Yamazaki ,  Mamoru Sugano ,  Makoto Kawamura ,  Kunihiro Ninomiya ,  Akihiro Tobe ,  Issei Nitta

IPC分类号： C07D295/12 ,  A61K31/34 ,  A61K31/343 ,  A61K31/40 ,  A61K31/415 ,  A61K31/445 ,  A61K31/495 ,  A61K31/54 ,  A61K31/5415 ,  A61P1/04 ,  C07D233/61 ,  C07D279/18 ,  C07D279/30 ,  C07D295/125 ,  C07D307/91 ,  C07D333/76 ,  C07D339/08 ,  C07D521/00

CPC分类号： C07D307/91 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D279/30 ,  C07D295/125 ,  C07D333/76 ,  C07D339/08

摘要： Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piperazino group, imidazolyl group 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.4 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or a pharmaceutically acceptable acid addition salts thereof are disclosed. They are a potent antiulcer agent.

公开(公告)号：US4933344A

公开(公告)日：1990-06-12

申请号：US239169

申请日：1988-08-31

申请人： Shinichiro Fujimori ,  Satoshi Yamazaki ,  Mamoru Sugano ,  Makoto Kawamura ,  Kunihiro Ninomiya ,  Akihiro Tobe ,  Issei Nitta

发明人： Shinichiro Fujimori ,  Satoshi Yamazaki ,  Mamoru Sugano ,  Makoto Kawamura ,  Kunihiro Ninomiya ,  Akihiro Tobe ,  Issei Nitta

IPC分类号： C07D295/12 ,  A61K31/34 ,  A61K31/343 ,  A61K31/40 ,  A61K31/415 ,  A61K31/445 ,  A61K31/495 ,  A61K31/54 ,  A61K31/5415 ,  A61P1/04 ,  C07D233/61 ,  C07D279/18 ,  C07D279/30 ,  C07D295/125 ,  C07D307/91 ,  C07D333/76 ,  C07D339/08 ,  C07D521/00

CPC分类号： C07D307/91 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D279/30 ,  C07D295/125 ,  C07D333/76 ,  C07D339/08

摘要： Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piparazino group, imidazolyl group, 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.4 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or a pharmaceutically acceptable acid addition salts thereof are disclosed. They are a potent antiulcer agent.

公开(公告)号：US4734500A

公开(公告)日：1988-03-29

申请号：US838569

申请日：1986-03-11

申请人： Akihiro Tobe ,  Shinichiro Fujimori ,  Tomoshi Yamazaki ,  Mamoru Sugano ,  Ryoji Kikumoto ,  Issei Nitta

发明人： Akihiro Tobe ,  Shinichiro Fujimori ,  Tomoshi Yamazaki ,  Mamoru Sugano ,  Ryoji Kikumoto ,  Issei Nitta

IPC分类号： A61K31/135 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/275 ,  A61K31/495 ,  A61P1/04 ,  C07C47/11 ,  C07C67/00 ,  C07C313/00 ,  C07C317/22 ,  C07C317/32 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07D295/08 ,  C07D295/092 ,  C07D295/096 ,  C07D333/76 ,  C07D333/50

CPC分类号： C07D295/096 ,  C07D295/088 ,  C07D333/76

摘要： A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylene; Y is --(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.3 hydroxyalkyl or phenyl; or a pharmaceutically acceptable salt thereof is disclosed. The compound has anti-ulcer effect.

摘要翻译： 由通式（I）表示的新型砜化合物其中R 1是环己基，苯基; 或被选自硝基，C 1 -C 3烷基，C 1 -C 3烷氧基和卤素的基团取代的苯基; R2，R3，R4和R5分别是氢，卤素，氰基或羰基，其中R1和R2可以形成被至少一个选自硝基C1-C3烷基，C1-C3烷氧基的基团取代的邻亚苯基或邻亚苯基 和卤素; X是氧或亚甲基; Y是 - （CH 2）n - ，其中n是0或5或6的整数，或者其中m是整数1-3; R6是氢，C1-C3烷基，ω-烷基氨基烷基，其中每个烷基具有1-3个碳原子，或ω-二烷基氨基烷基，其中每个烷基具有1-3个碳原子; R7是氢或C1-C3烷基; 并且R 6和R 7可以与N或其中R 8是氢，C 1 -C 3羟基烷基或苯基形成环; 或其药学上可接受的盐。 该化合物具有抗溃疡作用。

公开(公告)号：US4985430A

公开(公告)日：1991-01-15

申请号：US279051

申请日：1988-12-02

申请人： Shuji Morita ,  Ken-Ichi Saito ,  Kunihiro Ninomiya ,  Akihiro Tobe ,  Issei Nitta ,  Mamoru Sugano

发明人： Shuji Morita ,  Ken-Ichi Saito ,  Kunihiro Ninomiya ,  Akihiro Tobe ,  Issei Nitta ,  Mamoru Sugano

IPC分类号： C07D219/10 ,  C07D219/12 ,  C07D221/16 ,  C07D401/12 ,  C07D471/04 ,  C07D471/18 ,  C07D491/04 ,  C07D491/052 ,  C07D491/10 ,  C07D495/04 ,  C07D495/14 ,  C07D495/22

CPC分类号： C07D401/12 ,  C07D219/10 ,  C07D219/12 ,  C07D221/16 ,  C07D471/04 ,  C07D491/04 ,  C07D491/10 ,  C07D495/04 ,  C07D495/14

摘要： There are disclosed a 9-acylamino-tetrahydroacridine derivative represented by the following formula (I): ##STR1## wherein R ##STR2## are as defined in the specification, its optical antipode or pharmaceutically acceptable acid addition salt thereof and a memory enhancing agent containing the same as an active ingredient.

公开(公告)号：US4814507A

公开(公告)日：1989-03-21

申请号：US95766

申请日：1987-09-14

申请人： Akihiro Tobe ,  Shinichiro Fujimori ,  Tomoshi Yamazaki ,  Mamoru Sugano ,  Ryoji Kikumoto ,  Issei Nitta

发明人： Akihiro Tobe ,  Shinichiro Fujimori ,  Tomoshi Yamazaki ,  Mamoru Sugano ,  Ryoji Kikumoto ,  Issei Nitta

IPC分类号： A61K31/135 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/275 ,  A61K31/495 ,  A61P1/04 ,  C07C47/11 ,  C07C67/00 ,  C07C313/00 ,  C07C317/22 ,  C07C317/32 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07D295/08 ,  C07D295/092 ,  C07D295/096 ,  C07D333/76 ,  C07C87/28 ,  C07C147/00

CPC分类号： C07D295/096 ,  C07D295/088 ,  C07D333/76

摘要： A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylkene; Y is -(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.3 hydroxyalkyl or phenyl; or a pharmaceutically acceptable salt thereof is disclosed. The compound has anti-ulcer effect.

公开(公告)号：US4684651A

公开(公告)日：1987-08-04

申请号：US352716

申请日：1982-02-26

申请人： Ryoji Kikumoto ,  Harukazu Fukami ,  Kenichiro Nakao ,  Mamoru Sugano

发明人： Ryoji Kikumoto ,  Harukazu Fukami ,  Kenichiro Nakao ,  Mamoru Sugano

IPC分类号： C07D317/58 ,  C07D317/66 ,  C07D319/18 ,  C07D321/10 ,  A61K31/495 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14

CPC分类号： C07D317/66 ,  C07D317/58 ,  C07D319/18 ,  C07D321/10

摘要： Alkylenedioxybenzene derivatives are prepared and found to be useful as pharmaceutical agents, particularly as hypotensives.

摘要翻译： 制备了亚烷基二氧基苯衍生物，发现其可用作药剂，特别是作为低渗剂。

公开(公告)号：US4143040A

公开(公告)日：1979-03-06

申请号：US853424

申请日：1977-11-21

申请人： Tadashi Oohama ,  Ryozo Yamaguchi ,  Mamoru Sugano

发明人： Tadashi Oohama ,  Ryozo Yamaguchi ,  Mamoru Sugano

IPC分类号： C07J1/00 ,  C07J21/00 ,  C07J75/00 ,  C07J17/00

CPC分类号： C07J21/008 ,  C07J1/0081

摘要： 17-Ketals of 3-alkoxyestra-2,5(10)-dien-17-ones are prepared by reacting 17-ketals of 3-alkoxyestra-1,3,5(10)-trien-17-ones with sodium or potassium, liquid ammonia and a tertiary alcohol in the presence of an alicyclic hydrocarbon and/or an aliphatic hydrocarbon, and a solvent selected from the group consisting of tetrahydrofuran, dioxane and tetrahydropyran.Yield and selectivity of this reaction are improved by using the 17-ketal of the 3-alkoxyestra-1,3,5(10)-trien-17-one, sodium or potassium, liquid ammonia and the solvent in such proportions that the 17-ketal of the 3-alkoxyestra-1,3,5(10)-trien-17-one is substantially dissolved in the reaction system and that two liquid phases are formed, the lower phase being colored.