公开(公告)号：US4981860A

公开(公告)日：1991-01-01

申请号：US470244

申请日：1990-01-25

申请人： Susumu Tsushima ,  Muneo Takatani ,  Kohei Nishikawa

发明人： Susumu Tsushima ,  Muneo Takatani ,  Kohei Nishikawa

IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61P7/02 ,  A61P9/00 ,  A61P13/02 ,  A61P15/00 ,  A61P29/00 ,  A61P37/00 ,  A61P37/08 ,  C07D401/12

CPC分类号： C07D401/12

摘要： Novel compound of the formula: ##STR1## is useful as a platelet activating factor antagonist and is so stable that it is advantageously used as drugs.

公开(公告)号：US4962113A

公开(公告)日：1990-10-09

申请号：US224352

申请日：1988-07-26

申请人： Susumu Tsushima ,  Muneo Takatani ,  Kohei Nishikawa

发明人： Susumu Tsushima ,  Muneo Takatani ,  Kohei Nishikawa

IPC分类号： C07D215/36 ,  A61K31/44 ,  A61K31/4425 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/495 ,  A61P7/02 ,  A61P9/02 ,  A61P11/08 ,  A61P43/00 ,  C07D213/71 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D213/83 ,  C07D215/48 ,  C07D215/54 ,  C07D401/12 ,  C07D405/12

CPC分类号： C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D215/48 ,  C07D401/12 ,  C07D405/12

摘要： Novel pyridinium derivatives represented by the formula (I): ##STR1## wherein ##STR2## is an optionally substituted pyridinium ring; R.sup.1 is a lower alkyl group or aralkyl group;R.sup.7 and R.sup.10 are independently hydrogen, a lower alkyl group, aryl group or aralkyl group;l is 0 or 1;R.sup.5 is a phenylene group or an alkylene group which may be substituted;R.sup.11 is an alkyl group or aryl group;X is a group of the formula: --CH.sub.2 OCH.sub.2 -- or a group of the formula: ##STR3## wherein R.sup.6 is hydrogen, a lower alkyl or a lower alkoxy, and m is an integer of 0 to 3;U is a group of the formula: ##STR4## wherein R.sup.4 is hydrogen, a lower alkyl group, aryl group or aralkyl group;Y and Z are independently a divalent chain group consisting of one to six members which is selected from the class consisting of groups of the formulae: ##STR5## wherein R is hydrogen, a lower alkyl group, acyl group or aryl group and at least one of which is a group of the formula: ##STR6## with the proviso that R may be the same or different from each other, or may form a ring together when two or more groups of the formula: ##STR7## are present, that R may be bonded to R.sup.4 when Y contains a group of the formula: ##STR8## and that R may be bonded to R.sup.11 when Z contains a group of the formula: ##STR9## and W.sup..crclbar. is a counter anion; are useful as a platelet activating factor antagonist.

公开(公告)号：US5025005A

公开(公告)日：1991-06-18

申请号：US556280

申请日：1990-07-23

申请人： Hiroaki Nomura ,  Kohei Nishikawa ,  Susumu Tsushima

发明人： Hiroaki Nomura ,  Kohei Nishikawa ,  Susumu Tsushima

IPC分类号： A61K31/23 ,  C07C271/06 ,  C07C271/12 ,  C07C271/14 ,  C07C271/16 ,  C07C271/20 ,  C07C271/22 ,  C07C271/64 ,  C07C271/66 ,  C07C275/50 ,  C07C275/60 ,  C07D207/09 ,  C07D209/48 ,  C07D211/56 ,  C07D213/40 ,  C07D213/75 ,  C07D233/72 ,  C07D239/54 ,  C07D277/22 ,  C07D277/28 ,  C07D295/088 ,  C07D295/13 ,  C07D295/205 ,  C07D295/215 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D417/06 ,  C07D417/12 ,  C07D521/00

CPC分类号： C07D209/48 ,  C07C271/12 ,  C07C271/14 ,  C07C271/16 ,  C07C271/20 ,  C07C271/22 ,  C07C271/64 ,  C07C271/66 ,  C07C275/50 ,  C07C275/60 ,  C07C309/00 ,  C07D207/09 ,  C07D211/56 ,  C07D213/40 ,  C07D213/75 ,  C07D231/12 ,  C07D233/56 ,  C07D233/72 ,  C07D239/54 ,  C07D249/08 ,  C07D277/22 ,  C07D277/28 ,  C07D295/088 ,  C07D295/13 ,  C07D295/205 ,  C07D295/215 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D417/06 ,  C07D417/12

摘要： Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.

公开(公告)号：US4576933A

公开(公告)日：1986-03-18

申请号：US490224

申请日：1983-04-29

申请人： Susumu Tsushima ,  Kohei Nishikawa

发明人： Susumu Tsushima ,  Kohei Nishikawa

IPC分类号： A61K31/685 ,  A61P9/12 ,  C07C43/178 ,  C07D295/205 ,  C07D319/06 ,  C07F9/09 ,  C07F9/10 ,  C07F9/58 ,  C07F9/6509 ,  C07F9/6533 ,  C07F9/6539 ,  A61K31/42 ,  A61K31/425 ,  A61K31/44

CPC分类号： C07D295/205 ,  C07C43/1785 ,  C07D319/06 ,  C07F9/091 ,  C07F9/10 ,  C07F9/581 ,  C07F9/650958 ,  C07F9/6533 ,  C07F9/6539

摘要： Glycerol derivatives, inclusive of salts thereof, of the formula ##STR1## wherein R.sup.1 is alkyl or alkylcarbamoyl containing 10 to 30 carbon atoms, R.sup.2 and R.sup.3 are independently hydrogen, C.sub.1-6 alkyl or, taken together with the adjacent nitrogen atom, form cyclic amino, and ##STR2## represents cyclic ammonio, and of the formula ##STR3## wherein R.sup.1 is as defined above, R.sup.2' and R.sup.3' are C.sub.1-6 alkyl or, taken together with the adjacent nitrogen atom, form cyclic amino and R.sup.4', R.sup.5' and R.sup.6' are independently hydrogen or C.sub.1-6 alkyl, are useful as antihypertensive agents.

摘要翻译： 其中R1是烷基或含10-30个碳原子的烷基氨基甲酰基的甘油衍生物，包括它们的盐，其中R 1和R 3独立地是氢，C 1-6烷基或与相邻的氮原子一起形成环状 氨基，＆lt; IMAGE＆gt;表示环状铵，并且其中R 1如上所定义，R 1和R 3'为C 1-6烷基，或与相邻氮原子一起形成环状氨基和R4' ，R5'和R6'独立地为氢或C1-6烷基，可用作抗高血压剂。

公开(公告)号：US4737518A

公开(公告)日：1988-04-12

申请号：US906310

申请日：1986-09-12

申请人： Hiroaki Nomura ,  Kohei Nishikawa ,  Susumu Tsushima ,  Yoshio Kozai

发明人： Hiroaki Nomura ,  Kohei Nishikawa ,  Susumu Tsushima ,  Yoshio Kozai

IPC分类号： A61K31/23 ,  C07C271/06 ,  C07C271/12 ,  C07C271/14 ,  C07C271/16 ,  C07C271/20 ,  C07C271/22 ,  C07C271/64 ,  C07C271/66 ,  C07C275/50 ,  C07C275/60 ,  C07D207/09 ,  C07D209/48 ,  C07D211/56 ,  C07D213/40 ,  C07D213/75 ,  C07D233/72 ,  C07D239/54 ,  C07D277/22 ,  C07D277/28 ,  C07D295/088 ,  C07D295/13 ,  C07D295/205 ,  C07D295/215 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D417/06 ,  C07D417/12 ,  C07D521/00 ,  C07C125/065 ,  A61K31/325

CPC分类号： C07D209/48 ,  C07C271/12 ,  C07C271/14 ,  C07C271/16 ,  C07C271/20 ,  C07C271/22 ,  C07C271/64 ,  C07C271/66 ,  C07C275/50 ,  C07C275/60 ,  C07C309/00 ,  C07D207/09 ,  C07D211/56 ,  C07D213/40 ,  C07D213/75 ,  C07D231/12 ,  C07D233/56 ,  C07D233/72 ,  C07D239/54 ,  C07D249/08 ,  C07D277/22 ,  C07D277/28 ,  C07D295/088 ,  C07D295/13 ,  C07D295/205 ,  C07D295/215 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D417/06 ,  C07D417/12

摘要： Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.

摘要翻译： 式（IMAGE）的新型脂质衍生物[其中R1是烷基或烷基氨基甲酰基; R2是氢，可被取代的羟基，可被取代的或环状的氨基; R3是可以被取代的化学结合或亚烷基; R4是氢，烷基或芳烷基; X和Y独立地为O，S或可被取代的亚氨基，Y为亚氨基时，Y与X或R 4表示的亚氨基一起形成环; Z为亚氨基或可被取代的含氮杂环基]及其盐对血小板活化因子具有抑制活性，可用作各种循环系统疾病和过敏性疾病的预防或治疗剂，并且作为抗肿瘤药物 。

公开(公告)号：US4650791A

公开(公告)日：1987-03-17

申请号：US689730

申请日：1985-01-08

申请人： Hiroaki Nomura ,  Kohei Nishikawa ,  Susumu Tsushima

发明人： Hiroaki Nomura ,  Kohei Nishikawa ,  Susumu Tsushima

IPC分类号： A61K31/685 ,  C07D207/40 ,  C07D207/404 ,  C07D207/44 ,  C07D207/448 ,  C07D209/48 ,  C07F9/10 ,  C07F9/553 ,  C07F9/572 ,  C07F9/6558 ,  A61K31/50 ,  A61K31/425 ,  A61K31/44 ,  A61K31/535

CPC分类号： C07D207/404 ,  C07C309/00 ,  C07D207/448 ,  C07D209/48 ,  C07F9/5537 ,  C07F9/65583

摘要： A novel phospholipid of the formula: ##STR1## wherein R.sup.1 is an alkyl group of 10 to 24 carbon atoms, R.sup.2 is a cyclic imide group and A.sup.+ is a cyclic ammonio group and a salt thereof have platelet activating factor inhibiting activity and are useful for prevention and treatment of circulatory disorders and allergic bronchial asthma.

摘要翻译： 一种下式的新型磷脂：其中R1为10-24个碳原子的烷基，R2为环状酰亚胺基，A +为环状铵基，其盐为血小板活化因子抑制活性，可用于 预防和治疗循环系统疾病和过敏性支气管哮喘。

公开(公告)号：US4582824A

公开(公告)日：1986-04-15

申请号：US614024

申请日：1984-05-25

申请人： Kohei Nishikawa ,  Susumu Tsushima ,  Hiroaki Nomura

发明人： Kohei Nishikawa ,  Susumu Tsushima ,  Hiroaki Nomura

IPC分类号： A61K31/685 ,  A61P9/00 ,  C07F9/10 ,  C07F9/58 ,  C07F9/62 ,  C07F9/6539

CPC分类号： C07F9/10 ,  C07F9/581 ,  C07F9/62 ,  C07F9/6539

摘要： Compounds of the formula ##STR1## wherein R.sup.1 is a C.sub.10-24 alkyl group, R.sup.2 is a C.sub.1-4 alkyl group or a phenyl-C.sub.1-3 alkyl group and A.sup.+ is a heterocyclic group containing a quaternized nitrogen, and physiologically acceptable salts thereof have platelet activating factor inhibiting activity and are useful in the prevention and treatment of various circulatory diseases or allergic diseases.

摘要翻译： PCT No.PCT / JP83 / 00289 Sec。 371日期1984年5月25日第 102（e）日期1984年5月25日PCT申请日1983年8月31日。式的化合物，其中R 1是C 10-24烷基，R 2是C 1-4烷基或苯基-C 1-3烷基 A +是含有季铵化氮的杂环基，其生理上可接受的盐具有血小板活化因子抑制活性，可用于预防和治疗各种循环系统疾病或过敏性疾病。

公开(公告)号：US06686383B2

公开(公告)日：2004-02-03

申请号：US10227537

申请日：2002-08-26

申请人： Kohei Nishikawa ,  Yumiko Shibouta ,  Keiji Kubo

发明人： Kohei Nishikawa ,  Yumiko Shibouta ,  Keiji Kubo

IPC分类号： A61K3141

CPC分类号： A61K31/4184 ,  A61K31/415 ,  A61K31/4245 ,  Y02A50/395

摘要： This invention relates to methods for the prophylaxis or treatment of diabetic nephropathy comprising, administering as an active ingredient, a compound, or salt thereof, of formula (I) wherein R1 stands for H or lower alkyl; R2 stands for an optionally esterified carboxyl group; R3 stands for a group actually or potentially capable of forming an anion; X shows that the phenylene and phenyl groups bind to each other directly or through a spacer having an atomic chain length of two or less; n stands for 1 or 2; ring A stands for a benzene ring; Y stands for a bond, —O—, —S(O)m— wherein m stands for 0, 1 or 2, or —N(R4)— wherein R4 stands for H or an optionally substituted alkyl group).

摘要翻译： 本发明涉及预防或治疗糖尿病性肾病的方法，包括给予其中R 1代表H或低级烷基的式（Ⅰ）化合物或其盐作为活性成分; R 2代表任选酯化的羧基; R 3代表实际上或潜在地能够形成阴离子的基团; X表示亚苯基和苯基直接或通过原子链长度为2或更小的间隔物彼此结合; n代表1或2; 环A代表苯环; Y代表键，-O - ， - S（O）m-，其中m代表0,1或2或-N（R 4） - ，其中R 4代表H或任选取代的烷基 组）。

公开(公告)号：US06469037B2

公开(公告)日：2002-10-22

申请号：US09977476

申请日：2001-10-16

申请人： Kohei Nishikawa ,  Yumiko Shibouta ,  Keiji Kubo

发明人： Kohei Nishikawa ,  Yumiko Shibouta ,  Keiji Kubo

IPC分类号： A61K3141

CPC分类号： A61K31/4184 ,  A61K31/415 ,  A61K31/4245 ,  Y02A50/395

摘要： This invention relates to methods for lowering urinary total protein comprising, administering as an active ingredient, a compound or salt thereof represented by general formula (I) wherein R1 stands for H or alkyl; R2 stands for an optionally esterified carboxyl group; R3 stands for a group actually or potentially capable of forming an anion; X shows that the phenylene and phenyl groups bind to each other directly or through a spacer having an atomic chain length of two or less; n stands for 1 or 2; ring A stands for a benzene ring having an optional substituent in addition to R2; Y stands for a bond, —O—, —S(O)m— wherein m stands for 0, 1 or 2, or —N(R4)— wherein R4 stands for H or an optionally substituted alkyl group.

摘要翻译： 本发明涉及降低尿总蛋白的方法，其包括给予作为活性成分的由通式（I）表示的化合物或其盐，其中R1代表H或烷基; R2代表任选酯化的羧基; R3代表实际上或潜在能够形成阴离子的组; X表示亚苯基和苯基直接或通过原子链长度为2或更小的间隔物彼此结合; n代表1或2; 环A代表除R2之外具有任选取代基的苯环; Y代表键，-O - ， - S（O）m-，其中m代表0,1或2或-N（R4） - ，其中R4代表H或任选取代的烷基。

公开(公告)号：US5705517A

公开(公告)日：1998-01-06

申请号：US131667

申请日：1993-10-05

申请人： Takehiko Naka ,  Kohei Nishikawa

发明人： Takehiko Naka ,  Kohei Nishikawa

IPC分类号： A61K31/415 ,  C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/10 ,  C07D405/14 ,  A61K31/41 ,  C07D235/06

CPC分类号： C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/10 ,  C07D405/14

摘要： Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R' is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.

摘要翻译： 式（I）的苯并咪唑衍生物：其中环A是可以任选地含有取代基的R'基团的苯环; R'是氢或任选取代的烃残基; R2是能够形成阴离子或可转换的基团的基团; X是亚苯基和苯基之间的原子长度为2以下的直接键或间隔物; R'是羧基，其酯，其酰胺或能够形成阴离子或可转化成阴离子的基团; Y是-O - ， - S（O）m - 或-N（R4） - ，其中m是0,1或2的整数，R4是氢或任选取代的烷基; n为1或2的整数; 和其药学上可接受的盐具有有效的血管紧张素II拮抗活性和抗高血压活性，因此可用作治疗循环系统疾病如高血压疾病，心脏病（例如高血压，心力衰竭，心肌梗塞等），中风 ，脑中风，肾炎等