公开(公告)号：US4602009A

公开(公告)日：1986-07-22

申请号：US645100

申请日：1984-08-28

申请人： Issei Nitta ,  Akira Maruyama ,  Kenichiro Nakao ,  Motoyoshi Miyake ,  Hiroaki Ueno

发明人： Issei Nitta ,  Akira Maruyama ,  Kenichiro Nakao ,  Motoyoshi Miyake ,  Hiroaki Ueno

IPC分类号： A61K31/57 ,  A61P5/38 ,  C07J5/00 ,  C07J7/00 ,  C07J21/00 ,  C07J31/00 ,  A61K31/56

CPC分类号： C07J5/0053 ,  C07J21/00 ,  C07J31/006 ,  C07J5/0076 ,  C07J7/0085

摘要： Novel corticoid 17.alpha.-alkoxycarbonyl carboxylate derivatives are disclosed. These derivatives have strong topical anti-inflammatory activity and extremely weak systemic adverse reactions and are useful for the treatment of acute and chronic eczema, eczema seborrhoicorum, contact dermatitis, atopic dermatitis, asthma, etc.

摘要翻译： 公开了新型皮质激素17α-烷氧基羰基羧酸酯衍生物。 这些衍生物具有强烈的局部抗炎活性和非常弱的全身不良反应，可用于治疗急性和慢性湿疹，皮脂溢性湿疹，接触性皮炎，特应性皮炎，哮喘等。

公开(公告)号：US4585766A

公开(公告)日：1986-04-29

申请号：US645099

申请日：1984-08-28

申请人： Issei Nitta ,  Kenichiro Nakao ,  Motoyoshi Miyake ,  Akira Maruyama ,  Junko Takashima

发明人： Issei Nitta ,  Kenichiro Nakao ,  Motoyoshi Miyake ,  Akira Maruyama ,  Junko Takashima

IPC分类号： A61K8/63 ,  A61K31/57 ,  A61P17/00 ,  A61P29/00 ,  C07J5/00 ,  C07J7/00 ,  C07J21/00 ,  C07J31/00

CPC分类号： C07J5/0076 ,  C07J21/00 ,  C07J31/006 ,  C07J5/0053 ,  C07J7/0085

摘要： Novel 6-oxygenated corticoid 17.alpha.-carbonates are disclosed. These compounds have strong topical anti-inflammatory activity which are accompanied by extremely weak systemic adverse reaction. The present compounds are useful for the treatment of acute and chronic eczema, eczema seborrhoicorum, contact dermatitis, atopic dermatitis, asthma, etc.

摘要翻译： 公开了新型6-氧合的皮质激素17α-碳酸酯。 这些化合物具有强的局部抗炎活性，伴随着非常弱的全身不良反应。 本发明化合物可用于治疗急性和慢性湿疹，湿疹湿疹，接触性皮炎，特应性皮炎，哮喘等。

公开(公告)号：US4716161A

公开(公告)日：1987-12-29

申请号：US719456

申请日：1985-04-03

申请人： Harukazu Fukami ,  Ryoji Kikumoto ,  Kenichiro Nakao ,  Issei Nitta ,  Shinya Inoue

发明人： Harukazu Fukami ,  Ryoji Kikumoto ,  Kenichiro Nakao ,  Issei Nitta ,  Shinya Inoue

IPC分类号： C07D239/96 ,  C07D285/32 ,  C07D491/04 ,  C07D491/056 ,  C07D513/04 ,  A61K31/54 ,  C07D417/06

CPC分类号： C07D491/04 ,  C07D239/96 ,  C07D285/32 ,  C07D513/04

摘要： A phenylpiperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or alkoxy group having 1 to 3 carbon atoms, orR.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together with carbon atoms to which they are attached form --O(CH.sub.2).sub.m O-- wherein m is an integer of 1 to 3, oreither R.sup.1 or R.sup.2 is amine residue selected from the group consisting of --NH.sub.2 , --NHSO.sub.2 CH.sub.3, --NHCOCH.sub.3 and --NHCONH.sub.2 and the other is hydrogen or alkoxy group of 1 to 3 carbon atoms and R.sup.3 is hydrogen;R.sup.4 and R.sup.5 are independently hydrogen or alkyl group of 1 to 3 carbon atoms;Y is --CO-- or --SO.sub.2 -- provided that at least one of R.sup.1 and R.sup.2 is not hydrogen when Y is --CO--; andn is an integer of 2 to 4.An acid addition salt of the phenylpiperazine derivative having the general formula [I] is included in the present invention. The phenylpiperazine derivative as well as its acid addition salt according to the present invention have the ability to reduce the blood pressure.

摘要翻译： 根据本发明的苯基哌嗪衍生物具有以下通式[I]：其中R 1，R 2和R 3独立地是氢或具有1至3个碳原子的烷氧基，或者R 1和R 2或R 2和R 3 与其连接的碳原子一起形成-O（CH 2）m O-，其中m是1至3的整数，或者R 1或R 2是选自-NH 2，-NHSO 2 CH 3，-NHCOCH 3和 -NHCONH 2，另一个是1或3个碳原子的氢或烷氧基，R 3是氢; R4和R5独立地是氢或1〜3个碳原子的烷基; Y是-CO-或-SO 2 - ，条件是当Y是-CO-时，R 1和R 2中的至少一个不是氢; n为2〜4的整数。本发明包括具有通式[I]的苯基哌嗪衍生物的酸加成盐。 根据本发明的苯基哌嗪衍生物及其酸加成盐具有降低血压的能力。

公开(公告)号：US4613598A

公开(公告)日：1986-09-23

申请号：US708641

申请日：1985-03-06

申请人： Harukazu Fukami ,  Shinya Inoue ,  Issei Nitta ,  Kenichiro Nakao ,  Ryoji Kikumoto

发明人： Harukazu Fukami ,  Shinya Inoue ,  Issei Nitta ,  Kenichiro Nakao ,  Ryoji Kikumoto

IPC分类号： C07D213/74 ,  C07D265/36 ,  C07D267/14 ,  C07D279/16 ,  C07D295/084 ,  C07D295/108 ,  C07D417/12 ,  A61K31/55 ,  C07D417/10

CPC分类号： C07D295/108 ,  C07D213/74 ,  C07D265/36 ,  C07D267/14 ,  C07D279/16 ,  C07D295/092 ,  C07D417/12

摘要： A piperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1 is --OH, --OR.sup.3, --SR.sup.3, --SOR.sup.3 or --SO.sub.2 R.sup.3 wherein R.sup.3 is alkyl group having 1 to 3 carbon atoms;R.sup.2 is --SO.sub.2 NH.sub.2, --SO.sub.2 NHR.sup.4, --SO.sub.2 NR.sup.4 R.sup.5, --COOH, --COOR.sup.4, --CONH.sub.2, --CONHR.sup.4, --CONR.sup.4 R.sup.5, --NHCONH.sub.2, --NHCSNH.sub.2, --NHCONHR.sup.4, --NHCOR.sup.4 or --NHSO.sub.2 R.sup.4 wherein R.sup.4 and R.sup.5 are independently alkyl group having 1 to 3 carbon atoms; orR.sup.1 and R.sup.2 together with carbon atoms to which they are attached form ##STR2## Z is --CO-- or --CH(OH)--; Ar is pyridyl or substituted or unsubstituted phenyl; andn is an integer of 3 to 5.An acid addition salt of the piperazine derivative having the above formula [I] is included in the present invention. The piperazine derivative as well as its acid addition salt according to the present invention have the ability to reduce the blood pressure.

摘要翻译： 根据本发明的哌嗪衍生物具有以下通式[I]：其中R 1是-OH，-OR 3，-SR 3，-SOR 3或-SO 2 R 3，其中R 3是具有1至3个碳原子的烷基 原子 R2是-SO2NH2，-SO2NHR4，-SO2NR4R5，-COOH，-COOR4，-CONH2，-CONHR4，-CONR4R5，-NHCONH2，-NHCSNH2，-NHCONHR4，-NHCOR4或-NHSO2R4，其中R4和R5独立地为具有1 至3个碳原子; 或R 1和R 2与它们所连接的碳原子一起形成Z是-CO-或-CH（OH） - ; Ar为吡啶基或取代或未取代的苯基; n为3〜5的整数。上述式[I]的哌嗪衍生物的酸加成盐包括在本发明中。 根据本发明的哌嗪衍生物及其酸加成盐具有降低血压的能力。

公开(公告)号：US4585591A

公开(公告)日：1986-04-29

申请号：US325026

申请日：1981-11-25

申请人： Issei Nitta ,  Shinichiro Fujimori ,  Toshio Haruyama ,  Shinya Inoue

发明人： Issei Nitta ,  Shinichiro Fujimori ,  Toshio Haruyama ,  Shinya Inoue

IPC分类号： C07J7/00 ,  C07J13/00 ,  C07J31/00 ,  C07J41/00 ,  C07J1/00

CPC分类号： C07J41/0038 ,  C07J13/005 ,  C07J31/006 ,  C07J7/0005 ,  C07J7/0045

摘要： This is disclosed novel intermediates, i.e. 17.beta.-ethynylsteroids, which are useful for the preparation of corticoids such as hydrocortisone and prednisolone, and a process for preparing the same.

摘要翻译： 公开了可用于制备皮质激素例如氢化可的松和泼尼松龙的新型中间体，即17β-乙炔基甾类化合物及其制备方法。

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：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：US4213902A

公开(公告)日：1980-07-22

申请号：US8173

申请日：1979-01-31

申请人： Hiromi Okushima ,  Issei Nitta ,  Rikizo Furuya

发明人： Hiromi Okushima ,  Issei Nitta ,  Rikizo Furuya

IPC分类号： A61K31/57 ,  A61P7/10 ,  C07J31/00 ,  C07J19/00

CPC分类号： C07J31/003

摘要： A steroidal 7.alpha.-acylthio-4-en-3-one is produced by adding a thiocarboxylic acid to a steroidal 4,6-dien-3-one in the presence of a strong acid in a neutral organic solvent.

摘要翻译： 通过在强酸的存在下在中性有机溶剂中将硫代羧酸加入甾族4,6-二烯-3-酮来制备甾族7α-酰基硫代-4-烯-3-酮。

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。