公开(公告)号：US5401760A

公开(公告)日：1995-03-28

申请号：US8365

申请日：1993-01-22

申请人： Masaaki Toda ,  Shuichi Ohuchida ,  Hiroyuki Ohno

发明人： Masaaki Toda ,  Shuichi Ohuchida ,  Hiroyuki Ohno

IPC分类号： C07D207/08 ,  C07D277/04 ,  C07D405/04 ,  C07D417/06 ,  A61K31/40

CPC分类号： C07D207/08 ,  C07D277/04 ,  C07D405/04 ,  C07D417/06

摘要： Heterocyclic compounds of the general formula: ##STR1## R represents a general formula:G--E--D--B--A--G represents a carbocyclic or heterocyclic ring which is unsubstituted or substituted, L represents a group of general formula:--CO--COR.sup.2--CO--CH.sub.2 --COR.sup.2--CO--CF.sub.2 --COR.sup.2--CO--CO--NR.sup.5 R.sup.6or--CO--CH.sub.2 --CO--NR.sup.5 R.sup.6and non-toxic salt or hydrate thereof possess an inhibitory activity on propyl endopeptidase, and therefore usefull for prevention and/or treatment of amnesia.

摘要翻译： 具有以下通式的杂环化合物：（I）R表示通式：GEDBA-G表示未取代或取代的碳环或杂环，L表示通式-CO-COR 2 -CO-CH 2 -COR2 -CO-CF2-COR2 -CO-CO-NR5R6或-CO-CH2-CO-NR5R6及其无毒盐或水合物对丙基内肽酶具有抑制活性，因此可用于预防和/或治疗健忘症 。

公开(公告)号：US5266709A

公开(公告)日：1993-11-30

申请号：US936285

申请日：1992-08-28

申请人： Shuichi Ohuchida ,  Masaaki Toda ,  Tsumoru Miyamoto

发明人： Shuichi Ohuchida ,  Masaaki Toda ,  Tsumoru Miyamoto

IPC分类号： C07D311/72 ,  C07D311/92 ,  C07D311/04

CPC分类号： C07D311/92 ,  C07D311/72

摘要： Benzopyran derivatives of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof possess the inhibitory activity on Maillard reaction and an antioxidizing effect, and therefore, are useful for the prevention and treatment of several diabetic complications, diseases induced by aging and several diseases caused by formation of peroxidized fat.

摘要翻译： 具有下式的苯并吡喃衍生物及其药学上可接受的酸加成盐对美拉德反应具有抑制活性和抗氧化作用，因此可用于预防和治疗几种糖尿病并发症，由 老化和由过氧化脂肪形成引起的几种疾病。

公开(公告)号：US5212191A

公开(公告)日：1993-05-18

申请号：US700299

申请日：1991-05-15

申请人： Masaaki Toda ,  Shuichi Ohuchida ,  Hiroyuki Ohno

发明人： Masaaki Toda ,  Shuichi Ohuchida ,  Hiroyuki Ohno

IPC分类号： C07D207/08 ,  C07D277/04 ,  C07D405/04 ,  C07D417/06

CPC分类号： C07D207/08 ,  C07D277/04 ,  C07D405/04 ,  C07D417/06

摘要： Heterocyclic compounds of the general formula: ##STR1## wherein, Z represents sulfur atom, R represents a general formula:G--E--D--B--A--L represents a group of the general formula: ##STR2## R.sup.3 represents alkyl group of from 1 to 6 carbon atom(s), phenyl group.

摘要翻译： 具有以下通式的杂环化合物：其中Z表示硫原子，R表示通式：GEDBA-L表示通式为CH（OR 3）2的基团，R 3表示 1至6个碳原子，苯基。

公开(公告)号：US4983624A

公开(公告)日：1991-01-08

申请号：US139231

申请日：1987-12-29

申请人： Masaaki Toda ,  Shuichi Ohuchida ,  Hiroyuki Ohno

发明人： Masaaki Toda ,  Shuichi Ohuchida ,  Hiroyuki Ohno

IPC分类号： C07D207/08

CPC分类号： C07D207/08

摘要： A novel prolinal derivative of general formula: ##STR1## [whereinA represents a group of the general formula: ##STR2## (wherein one of R.sup.1 and R.sup.2 represents hydrogen atom and the other represents alkyl group of from 2 to 5 carbon atoms, alkoxy group of from 1 to 5 carbon atom(s), phenyl group, benzyl group, cycloalkyl group of from 4 to 6 carbon atoms or (cycloalkyl group of from 4 to 6 carbon atoms) - methyl group or R.sup.1 and R.sup.2 each represents, same or different, alkyl group of from 1 to 4 carbon atom(s).)or a group of the general formula: ##STR3## (wherein m represents an integer of from 3 to 6.) n represents an integer of from 3 to 10.D represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of halogen atom, nitro group, trifluoromethyl group, alkyl or akloxy group of from 1 to 4 carbon atom(s).]possess inhibitory activity on prolyl endopeptidase, and therefore be useful for treating and/or preventing agent for amnesia.

公开(公告)号：US4857537A

公开(公告)日：1989-08-15

申请号：US159073

申请日：1988-02-23

申请人： Masaaki Toda ,  Shuichi Ohuchida ,  Hiroyuki Ohno

发明人： Masaaki Toda ,  Shuichi Ohuchida ,  Hiroyuki Ohno

IPC分类号： C07D277/04 ,  C07D417/06

CPC分类号： C07D417/06 ,  C07D277/04

摘要： A novel thiazolidine derivative of general formula: ##STR1## [wherein R represents a group of general formula:G-E-D-B-A-(wherein A represents single bond, alkylene group of from 1 to 6 carbon atom(s), alkylene group of from 2 to 6 carbon atoms, a group of general formula: ##STR2## or saturated hydrocarbon ring of from 4 to 7 carbon atoms or single heterocyclic ring.Y represents alkylene group of from 1 to 4 carbon atom(s) or alkenylene group of from 2 to 4 carbon atoms.B represents single bond or alkylene group of from 1 to 6 carbon atom(s).D represents single bond, oxygen atom, carbonyl group or a group of general formula: ##STR3## R.sup.1 represents hydrogen atom, alkyl group of from 1 to 4 carbon atom(s), phenyl group or benzyl group.E represents single bond, alkylene group of from 1 to 8 carbon atom(s) or alkylene group of from 1 to 8 carbon atom(s) substituted by phenyl group or benzyl group.G represents carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three of alkyl group of from 1 to 6 carbon atom(s), alkoxy group of from 1 to 6 carbon atom(s), halogen atom, trifluoromethyl group or nitro group.)With the proviso that, A and B do not represent mono-bonds at the same time.]possess inhibitory activity on prolyl endopeptidase, and therefore be useful for treating and/or preventing agent for amnesia.

公开(公告)号：US4234597A

公开(公告)日：1980-11-18

申请号：US20339

申请日：1979-03-14

申请人： Masaki Hayashi ,  Shuichi Ohuchida ,  Yoshinobu Arai

发明人： Masaki Hayashi ,  Shuichi Ohuchida ,  Yoshinobu Arai

IPC分类号： C07D209/94 ,  A61K31/557 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07C405/00 ,  C07D209/52 ,  A61K31/40

CPC分类号： C07C405/00 ,  C07C405/0041 ,  C07D209/52

摘要： Prostaglandin I.sub.2 analogues of the formula: ##STR1## [wherein R.sup.1 represents hydrogen, alkyl of 1 to 12 carbon atoms, aralkyl of 7 to 12 carbon atoms, cycloalkyl of 4 to 7 carbon atoms optionally substituted by alkyl of 1 to 4 carbon atoms, phenyl optionally substituted by chlorine, trifluoromethyl, alkyl of 1 to 4 carbon atoms or phenyl, or represents a group --C.sub.p H.sub.2p COOR.sup.5, --C.sub.q H.sub.2q OR.sup.6 or ##STR2## (wherein R.sup.5, R.sup.7 and R.sup.8 represent alkyl of 1 to 4 carbon atoms, R.sup.6 represents hydrogen or alkyl of 1 to 4 carbon atoms, p represents an integer of from 1 to 12, and q represents an integer of from 2 to 12), R.sup.2, R.sup.3 and R.sup.4, represent hydrogen or alkyl of 1 to 8 carbon atoms, B represents a single bond, or alkylene of 1 to 4 carbon atoms, n represents 3, 4, 5 or 6, and the symbol represents a single or double bond] and, when appropriate, non-toxic salts, including acid addition salts, thereof are new compounds possessing pharmacological properties typical of the prostaglandins.

摘要翻译： 具有下式的前列腺素I2类似物：其中R 1表示氢，1至12个碳原子的烷基，7至12个碳原子的芳烷基，4至7个碳原子的环烷基，任选被1至4个碳原子的烷基取代 任选被氯，三氟甲基，1-4个碳原子的烷基或苯基取代的苯基，或代表基团-CpH2pCOOR5，-CqH2qOR6或者其中R5，R7和R8代表1-4个碳原子的烷基，R6代表 氢或1〜4个碳原子的烷基，p表示1〜12的整数，q表示2〜12的整数），R2，R3和R4表示氢或碳原子数为1〜8的烷基，B 表示单键，或1〜4个碳原子的亚烷基，n表示3,4,5或6，符号表示单键或双键]，适当时包括无毒盐，包括其酸加成盐 是具有典型的前列腺素的药理学特性的新化合物。