公开(公告)号：US4017622A

公开(公告)日：1977-04-12

申请号：US545549

申请日：1975-01-30

申请人： Shinsaku Minami ,  Jun-Ichi Matsumoto ,  Minoru Sugita ,  Masanao Shimizu ,  Yoshiyuki Takase ,  Shinichi Nakamura

发明人： Shinsaku Minami ,  Jun-Ichi Matsumoto ,  Minoru Sugita ,  Masanao Shimizu ,  Yoshiyuki Takase ,  Shinichi Nakamura

IPC分类号： C07D215/56 ,  C07D401/04 ,  C07D471/04 ,  C07D295/10

CPC分类号： C07D401/04 ,  C07D215/56 ,  C07D471/04

摘要： Piperazine derivatives of the following formula ##STR1## wherein A and B are a carbon atom or a nitrogen atom except the case where both A and B are nitrogen atoms,R.sub.1 is hydrogen atom, an alkyl group having 1 to 4 carbon atoms, a benzyl group or acetyl group;R.sub.2 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, a benzyl group or a vinyl group; andR.sub.3 is hydrogen atom or an alkyl group having 1 to 6 carbon atoms, and pharmaceutically acceptable salts thereof.

摘要翻译： 除了A和B都是氮原子，R1是氢原子，具有1至4个碳原子的烷基，苄基以外的其中A和B是碳原子或氮原子的下式的哌嗪衍生物， 组或乙酰基; R2是氢原子，碳原子数1〜4的烷基，苄基或乙烯基; R3为氢原子或碳原子数为1〜6的烷基，及其药学上可接受的盐。

公开(公告)号：US3988456A

公开(公告)日：1976-10-26

申请号：US561336

申请日：1975-03-24

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/08 ,  A61K31/495 ,  A61P9/12 ,  A61P11/14 ,  A61P25/00 ,  A61P25/04 ,  C07D213/74 ,  C07D295/084 ,  C07D295/10

CPC分类号： C07D295/092 ,  Y10S514/849

摘要： 1,2-Diphenylethanolamine derivatives of the formula: ##SPC1##Wherein R.sub.1 and R.sub.2 are each hydrogen, a halogen, nitro, hydroxy, an alkyl or methoxy; R.sub.3 is a group of the formula: ##SPC2##Wherein R.sub.4, R.sub.5 and R.sub.6 are each hydrogen, a halogen or methoxy and n is an integer of 0 to 3, or a pyridyl; and Z is hydroxy or an acyloxy; with proviso that when R.sub.1 and/or R.sub.2 are hydroxy, Z is hydroxy, and their pharmaceutically acceptable salts, which have excellent analgesic and anti-tussive activities, and a process for the preparation thereof.

摘要翻译： 下式的1,2-二苯乙醇胺衍生物：

公开(公告)号：US3983239A

公开(公告)日：1976-09-28

申请号：US557642

申请日：1975-03-12

申请人： Yasutaka Nagai ,  Hitoshi Uno ,  Masanao Shimizu ,  Tadahiko Karasawa

发明人： Yasutaka Nagai ,  Hitoshi Uno ,  Masanao Shimizu ,  Tadahiko Karasawa

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： Hexahydro-.gamma.-carboline derivatives of the formula: ##SPC1##Wherein R.sub.1 is methyl or ethyl, and R.sub.2 is hydrogen, methyl or ethyl, with proviso that when R.sub.1 is ethyl, R.sub.2 is hydrogen, and their pharmaceutically acceptable acid addition salts, which exhibit excellent psychotropic effect, and a process for the preparation thereof.

摘要翻译： 下式的六氢-γ-咔啉衍生物：

公开(公告)号：US3957788A

公开(公告)日：1976-05-18

申请号：US541351

申请日：1975-01-15

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/02 ,  C07D295/03 ,  C07D295/096 ,  C07D295/145 ,  C07D295/08

CPC分类号： C07D295/03 ,  C07D295/096 ,  C07D295/145 ,  Y10S514/849

摘要： 1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##SPC1##Wherein X is hydroxy, methoxy, methyl or trifluoromethyl; and R is an unsubstituted monocycloalkyl group having 6 to 8 carbon atoms or 2-methoxyphenyl; provided that when X is hydroxy, R is cyclohexyl, and when X is trifluoromethyl, R is 2-methoxyphenyl,And their pharmaceutically acceptable salts, which have excellent analgesic, anti-tussive and anti-inflammatory activities, without undesirable side effect such as narcotic activity, and a process for the preparation thereof.

公开(公告)号：US3948928A

公开(公告)日：1976-04-06

申请号：US340195

申请日：1973-03-12

申请人： Haruki Nishimura ,  Masanao Shimizu ,  Hitoshi Uno ,  Tetsuo Hirooka ,  Yoshinobu Masuda ,  Mikio Kurokawa

发明人： Haruki Nishimura ,  Masanao Shimizu ,  Hitoshi Uno ,  Tetsuo Hirooka ,  Yoshinobu Masuda ,  Mikio Kurokawa

IPC分类号： A61K31/42 ,  C07D261/20

CPC分类号： A61K31/42 ,  C07D261/20

摘要： 3-Substituted-1,2-benzisoxazole derivative of the following formula: ##SPC1##Wherein R.sub.1 is hydrogen, hydroxy, nitro, alkyl, alkoxy, halogen or amino; R.sub.2 is hydroxyamino, amino, hydrazino, mono- or di- alkyl substituted amino, aralkylamino, acyloxyamino, morpholino, piperazine which is unsubstituted or substituted with alkyl, aralkyl or aryl at 4 position, or pyrrolidino, or R.sub.2 may combine with imino group and form together with the adjacent carbon atom a heterocyclic ring such as imidazoline or tetrahydropyrimidine; and n is an integer of 0 to 3, and its pharmaceutically acceptable acid addition salt, and preparation thereof. The present compounds show valuable pharmacological properties, such as anti-reserpine activity, central nervous depressing activity, anti-hypertensive activity and l-dopa potentiating activity.

摘要翻译： 3-取代的1,2-苯并异恶唑衍生物：

公开(公告)号：US3981999A

公开(公告)日：1976-09-21

申请号：US513824

申请日：1974-10-10

申请人： Masanao Shimizu ,  Yoshiyuki Takase ,  Kaoru Kouno

发明人： Masanao Shimizu ,  Yoshiyuki Takase ,  Kaoru Kouno

IPC分类号： A01K61/00 ,  A23K1/16 ,  A61K31/495 ,  A61K31/505 ,  A61P31/04 ,  C07D215/56 ,  C07D471/04

CPC分类号： C07D215/56 ,  A23K20/116 ,  A61K31/495 ,  C07D471/04

摘要： Pyrimidine compositions or their non-toxic acid-addition salts are used for preventing and treating infectious diseases of fish caused by pathogenic microorganisms.

摘要翻译： 嘧啶组合物或其无毒酸加成盐用于预防和治疗由病原微生物引起的鱼传染病。

公开(公告)号：US4162316A

公开(公告)日：1979-07-24

申请号：US821918

申请日：1977-08-04

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/02 ,  C07D295/03 ,  C07D295/096 ,  C07D241/04 ,  A61K31/495

CPC分类号： C07D295/03 ,  C07D295/096

摘要： 1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##STR1## wherein X is 2- or 3-hydroxy, 2-methoxy, 3-methyl, 3-alkoxy having 1 to 4 carbon atoms, or 2- or 3-alkanoyloxy having 2 to 5 carbon atoms; R is allyl, 3-hydroxyisoamyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, propyl, an unsubstituted monocycloalkyl having 5 to 8 carbon atoms, 2-chlorophenyl, or a phenyl substituted by hydroxy or methoxy; with proviso that when X is a substituent at position 2, R is cyclohexyl and when X is 3-methyl, R is 2-methoxyphenyl or an unsubstituted monocycloalkyl having 6 to 8 carbon atoms, and their pharmaceutically acceptable salts, and the preparation thereof, and analgesic or antitussive compositions containing the same as the essentially active ingredient.

公开(公告)号：US3985875A

公开(公告)日：1976-10-12

申请号：US537601

申请日：1974-12-30

申请人： Kouji Hayashi ,  Masahisa Hashimoto ,  Kiyoshi Nakamura ,  Masanao Shimizu ,  Naonobu Hatano ,  Kunihiko Takeyama

发明人： Kouji Hayashi ,  Masahisa Hashimoto ,  Kiyoshi Nakamura ,  Masanao Shimizu ,  Naonobu Hatano ,  Kunihiko Takeyama

IPC分类号： C07F9/09 ,  A01N9/36

CPC分类号： C07F9/091 ,  Y02P20/55 ,  Y10S530/86

摘要： New .omega.-(N-acylamino)alkylphosphoryl ethanolamines and their pharmaceutically acceptable acid addition salts have superior renin-inhibitory activities, antihypertensive activities and cholesterol-lowering activities. The .omega.-(N-acylamino)alkylphosphoryl ethanolamines are prepared by (1) reacting an .omega.-(N-acylamino) alkanol with a 2-(N-substituted amino)ethyl phosphate or its derivative, hydrolyzing the resulting product or splitting off the phosphoric acid-protective group of the resulting product thereby to form an .omega.-(N-acylamino) alkyl 2-(N-substituted amino) ethyl phosphate, and splitting off the amino-protective groups of the resulting phosphate, or (2) reacting an .omega.-(N-acylamino) alkanol with a phosphorus oxyhalide, reacting the resulting .omega.-(N-acylamino)alkyl dichlorophosphate with a 2-(N-substituted amino) ethanol, hydrolyzing the reaction product to form an .omega.-(N-acylamino) alkyl 2-(N-substituted)ethyl phosphate, and splitting off the amino-protective groups of said phosphate.

摘要翻译： 新的ω-（N-酰基氨基）烷基磷酰基乙醇胺及其药学上可接受的酸加成盐具有优异的肾素抑制活性，降压活性和降胆固醇活性。 ω-（N-酰氨基）烷基磷酰基乙醇胺通过以下步骤制备：（1）使ω-（N-酰氨基）链烷醇与2-（N-取代氨基）乙基磷酸酯或其衍生物反应，水解得到的产物或将 得到产物的磷酸保护基，从而形成2-（N-取代氨基）乙基磷酸的ω-（N-酰基氨基）烷基酯，并分离得到的磷酸酯的氨基保护基，或（2）使 将具有卤代磷酸酯的ω-（N-酰基氨基）链烷醇与所得的ω-（N-酰基氨基）烷基二氯磷酸酯与2-（N-取代的氨基）乙醇反应，水解反应产物以形成ω-（N- 酰基氨基）烷基2-（N-取代）乙基磷酸酯，并分离出所述磷酸酯的氨基保护基团。

公开(公告)号：US4080453A

公开(公告)日：1978-03-21

申请号：US663158

申请日：1976-03-02

申请人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

发明人： Haruki Nishimura ,  Hitoshi Uno ,  Kagayaki Natsuka ,  Noriaki Shimokawa ,  Masanao Shimizu ,  Hideo Nakamura

IPC分类号： C07D295/02 ,  C07D295/03 ,  C07D295/096 ,  C07D295/14 ,  A61K31/495

CPC分类号： C07D295/03 ,  C07D295/096

摘要： 1-Substituted-4-(1,2-diphenylethyl)piperazine derivatives of the formula: ##STR1## wherein X is 2- or 3-hydroxy, 2-methoxy, 3-methyl, 3-alkoxy having 1 to 4 carbon atoms, or 2- or 3-alkanoyloxy having 2 to 5 carbon atoms; R is allyl, 3-hydroxyisoamyl, 3-methyl-2-butenyl, 3-methyl-3-butenyl, propyl, an unsubstituted monocycloalkyl having 5 to 8 carbon atoms, 2-chlorophenyl, or a phenyl substituted by hydroxy or methoxy; with proviso that when X is a substituent at position 2, R is cyclohexyl and when X is 3-methyl, R is 2-methoxyphenyl or an unsubstituted monocycloalkyl having 6 to 8 carbon atoms, and their pharmaceutically acceptable salts, and the preparation thereof, and analgesic or antitussive compositions containing the same as the essentially active ingredient.

摘要翻译： 1-取代的4-（1,2-二苯基乙基）哌嗪衍生物，其结构式如下：其中X是2-或3-羟基，2-甲氧基，3-甲基，具有1至4个碳原子的3-烷氧基， 或具有2至5个碳原子的2-或3-烷酰氧基; R是烯丙基，3-羟基异戊基，3-甲基-2-丁烯基，3-甲基-3-丁烯基，丙基，未取代的具有5-8个碳原子的单环烷基，2-氯苯基或被羟基或甲氧基取代的苯基; 条件是当X是位置2的取代基时，R是环己基，当X是3-甲基时，R是2-甲氧基苯基或未取代的具有6-8个碳原子的单环烷基及其药学上可接受的盐及其制备方法， 以及含有与基本上活性成分相同的镇痛或镇咳药物。

公开(公告)号：US4029780A

公开(公告)日：1977-06-14

申请号：US626042

申请日：1975-10-28

申请人： Haruki Nishimura ,  Masanao Shimizu ,  Naonobu Hatano ,  Katsuyoshi Nakatsuzi ,  Hiroaki Kinugasa ,  Hiroko Kon

发明人： Haruki Nishimura ,  Masanao Shimizu ,  Naonobu Hatano ,  Katsuyoshi Nakatsuzi ,  Hiroaki Kinugasa ,  Hiroko Kon

IPC分类号： C07D417/04 ,  C07D285/24 ,  A61K31/54

CPC分类号： C07D417/04

摘要： A compound of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group, and R.sub.2 represents a hydrogen or halogen atom or a trifluoromethyl group,And its pharmaceutically acceptable salt. The compound is prepared by reacting the corresponding 1,2,4-benzothiadiazine 1,1-dioxide with a piperazine compound or alkylating 1,2,4-benzothiadiazine 1,1-dioxide whose corresponding 3-position is substituted by a piperazinyl group. The above compound has superior antihypertensive activity separated from diuretic, antidiuretic and hyperglycemic activities, and is free from side-effects.

摘要翻译： 式IMA的化合物，其中R 1表示氢原子或低级烷基，R 2表示氢或卤素原子或三氟甲基，以及其药学上可接受的盐。 该化合物通过相应的1,2,4-苯并噻二嗪1,1-二氧化物与相应的3-位被哌嗪基取代的哌嗪化合物或烷基化的1,2,4-苯并噻二嗪1,1-二氧化物反应来制备。 上述化合物具有从利尿，抗利尿和高血糖活性中分离的优异的抗高血压活性，并且没有副作用。