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1. 发明授权

US6046236A Carbocyclic sulfonamides 失效
标题翻译：碳环磺酰胺
公开(公告)号：US6046236A
公开(公告)日：2000-04-04
申请号：US848833
申请日：1997-05-05
申请人： Nobuyuki Hamanaka , Tsumoru Miyamoto
发明人： Nobuyuki Hamanaka , Tsumoru Miyamoto
IPC分类号： A61K31/557 , A61P43/00 , C07C303/38 , C07C303/40 , C07C311/07 , C07C311/10 , C07C311/11 , C07C311/12 , C07C311/13 , C07C311/14 , C07C311/19 , C07C311/20 , C07C311/27 , C07C311/29 , C07D493/08 , A01N37/12 , A01N37/44 , A61K31/24
CPC分类号： C07C311/19 , C07C311/07 , C07C311/10 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/20 , C07C311/27 , C07C311/29
摘要： (1) Prostaglandin (PG) E.sub.2 antagonist or agonist containing carbocyclic sulfonamides represented by the compound of the formula (I): ##STR1## cyclodextrin clathrates thereof, non-toxic salts thereof as active ingredient,(2) carbocyclic sulfonamides represented by the compound of the formula (II): ##STR2## cyclodextrin clathrates thereof, non-toxic salts thereof, (3) process for the preparation of the compound represented by the compound of the formula (II) described hereinbefore,(4) PGE.sub.2 antagonist or agonist containing the compound represented by the compound of the formula (II) as active ingredient.The compounds represented by the compounds of the formula (I) and (II) can be adapted to medicines which possess an inhibitory effect of uterine contraction, an analgetic action, an inhibitory effect of digestive peristalsis, a sleep-inducing effect as PGE.sub.2 antagonists, and an uterine contractile activity, a promoting effect of digestive peristalsis, a suppressive effect of gastric acid secretion, a hypotensive activity as PGE.sub.2 agonists, because they bind onto PGE.sub.2 receptor and have an activity of antagonist or agonist against the action thereof.
摘要翻译：（1）由式（I）化合物表示的前列腺素（PG）E2拮抗剂或含有碳环磺酰胺的激动剂：其环糊精包合物，其无毒性盐作为活性成分，（2）由下式表示的碳环磺酰胺（II）：其环糊精包合物，其无毒盐，（3）由上述式（II）化合物表示的化合物的制备方法，（4）PGE2拮抗剂或含有由式（II）的化合物作为活性成分。由式（I）和（II）化合物表示的化合物可适用于具有子宫收缩抑制作用，止痛作用，消化性蠕动抑制作用，睡眠诱导作用PGE2拮抗剂的药物，因为它们结合PGE2受体并且具有针对其作用的拮抗剂或激动剂的活性，因此其作为PGE2激动剂具有低血压活性，作为消化道蠕动的促进作用，胃酸分泌的抑制作用。

2. 发明授权

US5663417A Carbocyclic sulfonamides 失效
标题翻译：碳环磺酰胺
公开(公告)号：US5663417A
公开(公告)日：1997-09-02
申请号：US187008
申请日：1994-01-27
申请人： Nobuyuki Hamanaka , Tsumoru Miyamoto
发明人： Nobuyuki Hamanaka , Tsumoru Miyamoto
IPC分类号： A61K31/557 , A61P43/00 , C07C303/38 , C07C303/40 , C07C311/07 , C07C311/10 , C07C311/11 , C07C311/12 , C07C311/13 , C07C311/14 , C07C311/19 , C07C311/20 , C07C311/27 , C07C311/29 , C07D493/08 , A61K31/215 , A61K31/18 , C07C69/608
CPC分类号： C07C311/19 , C07C311/07 , C07C311/10 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/20 , C07C311/27 , C07C311/29
摘要： (1) Prostaglandin (PG) E.sub.2 antagonist or agonist containing carbocyclic sulfonamides represented by the compound of the formula (I): ##STR1## cyclodextrin clathrates thereof, non-toxic salts thereof as active ingredient, (2) carbocyclic sulfonamides represented by the compound of the formula (II): ##STR2## cyclodextrin clathrates thereof, non-toxic salts thereof, (3) process for the preparation of the compound represented by the compound of the formula (II) described hereinbefore, (4) PGE.sub.2 antagonist or agonist containing the compound represented by the compound of the formula (II) as active ingredient.The compounds represented by the compounds of the formula (I) and (II) can be adapted to medicines which possess an inhibitory effect of uterine contraction, an analgetic action, an inhibitory effect of digestive peristalsis, a sleep-inducing effect as PGE.sub.2 antagonists, and an uterine contractile activity, a promoting effect of digestive peristalsis, a suppressive effect of gastric acid secretion, a hypotensive activity as PGE.sub.2 agonists, because they bind onto PGE.sub.2 receptor and have an activity of antagonist or agonist against the action thereof.
摘要翻译：（1）由式（I）化合物表示的前列腺素（PG）E2拮抗剂或含有碳环磺酰胺的激动剂：其作为活性成分的无毒盐，（2）代表的碳环磺酰胺通式（II）的化合物：其中，式（II）的环糊精包合物，其无毒盐，（3）由上述式（II）的化合物表示的化合物的制备方法，（ 4）含有由式（II）化合物表示的化合物作为活性成分的PGE 2拮抗剂或激动剂。由式（I）和（II）化合物表示的化合物可适用于具有子宫收缩抑制作用，止痛作用，消化性蠕动抑制作用，睡眠诱导作用PGE2拮抗剂的药物，因为它们结合PGE2受体并且具有针对其作用的拮抗剂或激动剂的活性，因此其作为PGE2激动剂具有低血压活性，作为消化道蠕动的促进作用，胃酸分泌的抑制作用。

3. 发明授权

US5508450A Benzopyran derivatives 失效
标题翻译：苯并吡喃衍生物
公开(公告)号：US5508450A
公开(公告)日：1996-04-16
申请号：US316332
申请日：1994-09-30
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 which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, coronary heart disease, peripheral circulatory insufficiency or failure, cerebrovascular hindrance, neurogenous diabetes, nephropathy, arteriosclerosis, arthrosclerosis, cataracts and retinopathy. Further, the derivatives may also be used in the treatment and/or prevention of diseases induced by aging and in the treatment and/or prevention of diseases caused by the formation of peroxidized fat.
摘要翻译：本文描述了对美拉德反应具有抑制作用以及抗氧化作用的苯并吡喃衍生物。这些衍生物可用于治疗和/或预防糖尿病并发症，例如冠心病，周围循环功能不全或失败，脑血管障碍，神经源性糖尿病，肾病，动脉硬化，关节动脉硬化，白内障和视网膜病变。此外，衍生物还可以用于治疗和/或预防由老化引起的疾病和治疗和/或预防由形成过氧化脂肪引起的疾病。

4. 发明授权

US5384414A Benzopyran derivatives 失效
标题翻译：苯并吡喃衍生物
公开(公告)号：US5384414A
公开(公告)日：1995-01-24
申请号：US107576
申请日：1993-08-18
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## wherein R.sup.1a is hydrogen, C1-4 alkyl or C1-4 alkoxy; or two R.sup.1a taken together with 7th- and 8th-carbon to which they are attached form a C6 carbocyclic ring;R.sup.2a is hydrogen, C1-4 alkyl or C1-4 alkoxy;R.sup.3a is hydrogen, C2-4 acyl or benzoyl;na is 1-3;Ya is C1-7 alkylene, C2-7 alkenylene or C2-7 alkynylene;Ma isi) bond orii) a group of the formula: --Da--Ba--;Da isi) --O-- orii) --S--;Ba isi) C1-4 alkylene orii) a group of the formula: ##STR2## Za is i) bond,ii) --OCO--,iii) CONR.sup.9a --,iv) --COO--,v) --NR.sup.9a CO--,vi) --O-- orvii) --NH--CO--NH--;Wa is a group of the formula: --W1a--Aa--W2 a--;Aa isi) bond orii) a group of the formula: --Ea-- .circle.Ga --;Ea isi) bond,ii) --O-- oriii) --S--; .circle.Ga is C4-10 carbocyclic or heterocyclic ring; or C4-10 carbocyclic or heterocyclic ring substituted by one to three C1-4 alkyl, C1-4 alkoxy, halogen, a group of the formula: --COOR.sup.7a, trihalomethyl or acetamido;W1a and W2a each, independently, isi) bondii) C1-4 alkylene,iii) C2-4 alkenylene oriv ) C2-4 alkynylene;R.sup.4a is hydrogen or C1-4 alkyl;R.sup.5a is hydrogen, C1-4 alkyl or amino;R.sup.6a is hydrogen, C1-4 alkyl, C1-4 alkoxy, halogen, a group of the formula: --COOR.sup.8a, trihalomethyl or acetoamido;R.sup.7a is hydrogen or C1-4 alkyl;R.sup.8a is hydrogen or C1-4 alkyl;R.sup.9a is hydrogen, C1-4 alkyl or benzyl; with a proviso, and the pharmaceutically acceptable acid addition salts thereof possess the inhibitory activity on Maillard reaction and an antioxidizing effect.
摘要翻译：下式的苯并吡喃衍生物：其中R 1a是氢，C 1-4烷基或C 1-4烷氧基; 或两个R 1a与它们所连接的第七和第八碳一起形成C6碳环; R 2a是氢，C 1-4烷基或C 1-4烷氧基; R3a是氢，C2-4酰基或苯甲酰基; na是1-3; Ya是C 1-7亚烷基，C 2-7亚烯基或C 2-7亚炔基; Ma是i）键或ii）下式的基团：-Da-Ba-; Da为i）-O-或ii）-S-; b）i）C1-4亚烷基或ii）下式的基团：Za是i）键，ii）-OCO-，iii）CONR9a - ，iv）-COO-，v）-NR9aCO-，vi ）-O-或vii）-NH-CO-NH-; Wa是下列基团：-W1a-Aa-W2a-; Aa是i）键或ii）下式的基团：-Ea-＆Cir＆Ga - ; Ea为i）键，ii）-O-或iii）-S-; ＆cir＆Ga是C4-10碳环或杂环; 或被一至三个C 1-4烷基取代的C 4-10碳环或杂环，C 1-4烷氧基，卤素，下式基团：-COOR 7 a，三卤代甲基或乙酰氨基; W1a和W2a各自独立地是i）键合ii）C 1-4亚烷基，iii）C 2-4亚烯基或iv）C 2-4亚炔基; R4a是氢或C1-4烷基; R5a是氢，C1-4烷基或氨基; R 6a是氢，C 1-4烷基，C 1-4烷氧基，卤素，下式基团：-COOR 8 a，三卤甲基或乙酰胺基; R 7a是氢或C 1-4烷基; R 8a是氢或C 1-4烷基; R9a是氢，C1-4烷基或苄基; 并且其药学上可接受的酸加成盐具有对美拉德反应的抑制活性和抗氧化作用。

5. 发明授权

US5169957A Benzopyran derivatives 失效
标题翻译：苯并吡喃衍生物
公开(公告)号：US5169957A
公开(公告)日：1992-12-08
申请号：US736321
申请日：1991-07-26
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
CPC分类号： C07D311/72 , C07D311/92
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。

6. 发明授权

US5614555A Amidinophenol derivatives 失效
标题翻译：脒基苯酚衍生物
公开(公告)号：US5614555A
公开(公告)日：1997-03-25
申请号：US464206
申请日：1995-06-05
申请人： Hisao Nakai , Masanori Kawamura , Tsumoru Miyamoto
发明人： Hisao Nakai , Masanori Kawamura , Tsumoru Miyamoto
IPC分类号： C07D295/18 , A61K31/235 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/495 , A61P29/00 , A61P37/08 , A61P43/00 , C07C257/18 , C07C323/59 , C07C323/62 , C07C323/63 , C07D205/04 , C07D207/08 , C07D207/16 , C07D209/20 , C07D223/04 , C07D295/185 , C07D295/192 , A61K31/165 , A61K31/24 , C07C229/36 , C07C271/18
CPC分类号： C07D295/185 , C07C257/18 , C07C323/59 , C07C323/62 , C07D207/16 , C07D209/20 , C07D295/192 , C07C2101/02 , C07C2101/04 , C07C2101/10 , C07C2101/14
摘要： Amidinophenol derivatives of the formula (I) ##STR1## wherein the various symbols are as defined herein; which have inhibitory activities on PLA.sub.2 and on various proteases such as trypsin, plasmin, thrombin, kallikrein, especially trypsin, and are useful for the prevention and/or the treatment of various inflammatory diseases, allergic diseases, disseminated intravascular coagulation, pancreatitis, severity in pancreatitis and multiple organ failure.
摘要翻译：式（I）的脒基苯酚衍生物其中各种符号如本文所定义; 其对PLA2和胰蛋白酶，纤溶酶，凝血酶，激肽释放酶，特别是胰蛋白酶等各种蛋白酶具有抑制活性，可用于预防和/或治疗各种炎性疾病，过敏性疾病，弥散性血管内凝血，胰腺炎，严重程度胰腺炎和多器官衰竭。

7. 发明授权

US5055598A Benzopyran derivatives 失效
标题翻译： BENZOPYRAN衍生物
公开(公告)号：US5055598A
公开(公告)日：1991-10-08
申请号：US491876
申请日：1990-03-12
申请人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
发明人： Shuichi Ohuchida , Masaaki Toda , Tsumoru Miyamoto
IPC分类号： A61K31/00 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/355 , A61P3/00 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/02 , A61P15/00 , A61P25/18 , A61P27/02 , A61P35/00 , A61P43/00 , C07D311/72 , C07D311/92 , C07D405/06
CPC分类号： C07D311/92 , C07D311/72
摘要： Benzopyran derivatives of the formula: ##STR1## wherein the variables are defined in the specification 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.

8. 发明授权

US5013734A Novel esters of phenylalkanoic acid 失效
标题翻译：苯基链烷酸的新型酯
公开(公告)号：US5013734A
公开(公告)日：1991-05-07
申请号：US521962
申请日：1990-05-11
申请人： Sadahiko Iguchi , Masanori Kawamura , Tsumoru Miyamoto
发明人： Sadahiko Iguchi , Masanori Kawamura , Tsumoru Miyamoto
IPC分类号： A61K31/44 , A61K31/443 , A61K31/495 , A61K31/535 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07D317/24 , C07D317/72 , C07D405/12
CPC分类号： C07D317/72 , C07D317/24
摘要： The esters of phenylalkanoic acid of the formula: ##STR1## wherein R.sup.1 is 4-10 membered, saturated or unsaturated, mono- or bi-cyclic hetero ring containing as hetero atoms:(i) one or two nitrogen,(ii) two or three of nitrogen and sulfur in total, or(iii) one or two sulfur;R.sup.2 is hydrogen; orR.sup.1 and R.sup.2, taken together with a nitrogen to which they are attached, form 4-7 membered, saturated or unsaturated, mono-cyclic hetero ring containing as hetero atoms:(i) one or two nitrogen, or(ii) two or three of nitrogen and oxygen in total, the aforementioned hetero rings, represented by R.sup.1 or formed by R.sup.1 and R.sup.2, taken together with a nitrogen to which they are attached, may be substituted by one substituent selected from C1-4 alkyl and C2-5 acyl;R.sup.3 each, independently, is hydrogen or C1-4 alkyl;R.sup.4 is hydrogen, halogen, trihalomethyl, C1-4 alkyl, C1-4 alkoxy, C2-5 acyl, cyano, nitro or nitroxy;R.sup.5 each, independently, is hydrogen, C1-4 alkyl or phenyl; or the two R.sup.5 's, taken together with a carbon to which they are attached, form cyclopentane or cyclohexane;and the pharmaceutically acceptable acid addition salts thereof, have .beta..sub.1 -adrenergic receptor blocking activity, and therefore, are useful for the prevention of and/or in the treatment of cardiovascular diseases such as angina pectoris, myocardial infarction, congestive heart failure, hypertension, arrhythmia, etc.

9. 发明授权

US5622984A Amidinophenol derivatives 失效
公开(公告)号：US5622984A
公开(公告)日：1997-04-22
申请号：US396784
申请日：1995-03-01
申请人： Hisao Nakai , Masanori Kawamura , Tsumoru Miyamoto
发明人： Hisao Nakai , Masanori Kawamura , Tsumoru Miyamoto
IPC分类号： C07D295/18 , A61K31/235 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/495 , A61P29/00 , A61P37/08 , A61P43/00 , C07C257/18 , C07C323/59 , C07C323/62 , C07C323/63 , C07D205/04 , C07D207/08 , C07D207/16 , C07D209/20 , C07D223/04 , C07D295/185 , C07D295/192
CPC分类号： C07D295/185 , C07C257/18 , C07C323/59 , C07C323/62 , C07D207/16 , C07D209/20 , C07D295/192 , C07C2101/02 , C07C2101/04 , C07C2101/10 , C07C2101/14
摘要： Amidinophenol derivatives of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are (i) H, (ii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO.sub.2, (vii) benzoyl, (viii) COOR.sup.4 (in which R.sup.4 is C1-3 alkyl); A is bond, C1-4 alkylene, --C(R.sup.5).dbd.C(R.sup.6)--(in which R.sup.5 and R.sup.6 are H or C1-4 alkyl; R.sup.3 is (i) CON(R.sup.7)(R.sup.8), (ii) CON(R.sup.9)--CH(R.sup.7)(R.sup.8) or (iii) ##STR2## in which R.sup.7 and R.sup.8 are (1) H,(2) phenyl, (3) C7-10 phenylalkyl, (4) phenyl or C7-10 phenylalkyl substituted by 1 or 2 C1-4 alkyl, halogen or R.sup.11 --COOR.sup.12 (in which R.sup.11 is bond, C1-8 alkylene, C2-8 alkenylene, C2-8 alkynylene; R.sup.12 is H, C1-4 alkyl, C7-10 phenylalkyl, phenyl, allyl, propargyl), (5) C1-10 alkyl, (6) C2-10 alkenyl having 1 to 3 double bonds, (7) C2-10 alkynyl having 1 or 2 triple bonds, (8) R.sup.11a --COXR.sup.12 (in which R.sup.11a is (a) bond, (b) C1-8 alkylene, (c) C2-8 alkylene in which 1 or 2 carbon atoms in the main chain are replaced by sulfur, or sulfur and phenylene, (d) C2-8 alkenylene, (e) C4-8 alkenylene in which 1 or 2 carbon atoms in the main chain are replaced by sulfur, or sulfur and phenylene, (f) C2-8 alkynylene, (g) C4-8 alkynylene in which 1 or 2 carbon atoms in the main chain are replaced by sulfur, or sulfur and phenylene; X is --O-- or --NH--), (9) C1-4 alkyl substituted by a 7-14 membered, bi- or tri-cyclic hetero ring containing one N atom, (10) C3-7 cycloalkyl); R.sup.9 is (1) H, (2) C1-8 alkyl, (3) C7-10 phenylalkyl, (4) C2-10 alkenyl having 1 to 3 double bonds, (5) C2-10 alkynyl having 1 or 2 triple bonds, (6) R.sup.11 --COOR.sup.12, (7) C3-7 cycloalkyl; ##STR3## is 4-7 membered, mono-cyclic hetero ring containing 1 or 2 N atom; R.sup.10 is H, C7-10 phenylalkyl or COOR.sup.13 (in which R.sup.13 is H, C1-4 alkyl or C7-10 phenylalkyl)); with the proviso that (i) both R.sup.7 and R.sup.8 do not represent hydrogen at the same time, and (ii) when at least one group in R.sup.7, R.sup.8 and R.sup.9 represents the group containing t-butyl ester, the other groups do not represent the group containing carboxy; or an acid-addition salt thereof, have inhibitory activities on PLA.sub.2 and on various proteases such as trypsin, plasmin, thrombin, kallikrein, especially trypsin, and are useful for the prevention and/or the treatment of various inflammatory diseases, allergic diseases, disseminated intravascular coagulation, pancreatitis, severity in pancreatitis and multiple organ failure.

10. 发明授权

US5494662A Stimulator for bone formation 失效
标题翻译：用于骨形成的刺激器
公开(公告)号：US5494662A
公开(公告)日：1996-02-27
申请号：US49503
申请日：1993-04-21
申请人： Ueno Kohji , Teruaki Katayama , Tsumoru Miyamoto
发明人： Ueno Kohji , Teruaki Katayama , Tsumoru Miyamoto
IPC分类号： A61K38/20 , A61K48/00 , C07K2/00 , C07K4/00
CPC分类号： A61K38/2026
摘要： A stimulator for bone formation containing human interleukin 4 or an analogue thereof as an active ingredient. This stimulator is useful for the prevention and treatment of, for example, osteoporosis, osteogenesis imperfecta, injured bone and abnormality of dental and the improvement of metabolic abnormality of bone.
摘要翻译：用于骨形成的刺激剂，其含有人白细胞介素4或其类似物作为活性成分。该刺激剂可用于预防和治疗例如骨质疏松症，成骨不全，骨骼损伤和牙齿异常以及骨代谢异常的改善。

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