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：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：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：US4775758A

公开(公告)日：1988-10-04

申请号：US924129

申请日：1986-10-28

申请人： Shoshichi Nojima ,  Hiroaki Nomura ,  Susumu Tsushima

发明人： Shoshichi Nojima ,  Hiroaki Nomura ,  Susumu Tsushima

IPC分类号： A01N57/12 ,  A01N57/16 ,  A61K31/685 ,  A61P35/00 ,  C07C43/13 ,  C07C43/164 ,  C07F9/10 ,  C07F9/58 ,  C07F9/6539 ,  C07F9/65

CPC分类号： C07F9/10 ,  A01N57/12 ,  A01N57/16 ,  C07C43/135 ,  C07C43/164 ,  C07F9/581 ,  C07F9/6539

摘要： Novel phospholipids, inclusive of salts thereof, of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently an aliphatic hydrocarbon residue containing 1 to 20 carbon atoms, with the numbers of the carbon atoms for both totalling 8 to 30, andR.sup.3, R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-6 alkyl, or ##STR2## represents a cyclic ammonio group, exhibit inhibitory activity against multiplication or tumor cells and antifungal activity.

摘要翻译： 新颖的磷脂，包括其盐，其中R 1和R 2独立地是含有1至20个碳原子的脂族烃残基，其中碳原子数合计为8-30，R3，R4和 R5独立地是氢或C1-6烷基，或者“IMAGE”表示环状氨基，对增殖或肿瘤细胞表现出抑制活性和抗真菌活性。

公开(公告)号：US4166178A

公开(公告)日：1979-08-28

申请号：US897157

申请日：1978-04-17

申请人： Susumu Tsushima ,  Michiyuki Sendai ,  Mitsuru Shiraishi ,  Norichika Matsumoto

发明人： Susumu Tsushima ,  Michiyuki Sendai ,  Mitsuru Shiraishi ,  Norichika Matsumoto

IPC分类号： A61K31/545 ,  C07D501/20 ,  C07D501/26

CPC分类号： C07D501/18 ,  C07D501/26

摘要： Novel 3-acyloxymethyl-cephem compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen or an acyl group; X is a divalent group consisting of a carbon chain having 2 to 3 carbon atoms and a carbonyl or sulfonyl group at one terminal end thereof, said divalent group being either substituted or unsubstituted on the carbon chain; and Z is an organic acid residue, and salts thereof were found to be useful as starting materials for preparing cephalosporins of the formula: ##STR2## wherein R.sup.2 stands for a residue of a nucleophilic compound and R.sup.1 has the same meaning as above.

公开(公告)号：US4068072A

公开(公告)日：1978-01-10

申请号：US701731

申请日：1976-06-30

申请人： Susumu Tsushima ,  Norichika Matsumoto ,  Mitsuo Numata

发明人： Susumu Tsushima ,  Norichika Matsumoto ,  Mitsuo Numata

IPC分类号： C07D499/10 ,  C07D499/00 ,  C07D499/04 ,  C07D499/21 ,  C07D499/42 ,  C07D501/04 ,  C07D501/18 ,  C07D501/02

CPC分类号： C07D499/00

摘要： A derivative of 6-aminopenicillanic acid or 7-aminocephalosporanic acid is produced by a process which comprises chlorinating or brominating a 6-thioacylaminopenicillanic acid or 7-thioacylaminocephalosporanic acid compound to obtain a corresponding iminothiohalide compound, and then solvolyzing the iminothiohalide compound. The process is novel and industrially feasible for producing the amino compound, which is not accompanied by "reconversion reaction".

摘要翻译： 6-氨基青霉烷酸或7-氨基头孢烷酸的衍生物是通过将6-硫代酰基氨基青霉烷酸或7-硫代酰基氨基头孢烷酸化合物氯化或溴化得到相应的亚氨基硫鎓化合物，然后使亚氨基硫代化合物溶解的方法制备的。 该方法在生产氨基化合物方面是新颖的和工业上可行的，其不伴随“再转化反应”。