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31. 发明授权

US4241070A Analgesic benzomorphan derivatives 失效
标题翻译：镇痛苯并吗啉衍生物
公开(公告)号：US4241070A
公开(公告)日：1980-12-23
申请号：US736072
申请日：1976-10-27
申请人： Junki Katsube , Hiroyuki Mizote , Shuichi Harada , Hisao Yamamoto
发明人： Junki Katsube , Hiroyuki Mizote , Shuichi Harada , Hisao Yamamoto
IPC分类号： A61K31/435 , A61P25/04 , C07D221/26 , A61K31/445
CPC分类号： C07D221/26 , Y02P20/55
摘要： 2-Substituted-2'-methyl-6,7-benzomorphan derivatives of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sub.3 is hydrogen, halogen or C.sub.1 -C.sub.3 alkyl, and pharmaceutically acceptable salts thereof, which are useful as non-addicting analgesics with sedative effects, are prepared by the reaction of a 6,7-benzomorphan derivative of the formula: ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, with a reactive derivative of an alcohol compound of the formula: ##STR3## wherein X is an optionally protected carbonyl group; and R.sub.3 is as defined above, optionally followed by the elimination of the protective group of the carbonyl group, or by the oxidation of a 6,7-benzomorphan derivative of the formula: ##STR4## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above.
摘要翻译：具有下式的2-取代的-2'-甲基-6,7-苯并吗啉衍生物：其中R 1和R 2各自为氢或C 1 -C 3烷基; 并且R3是氢，卤素或C1-C3烷基及其药学上可接受的盐，其可用作具有镇静作用的非上瘾止痛剂，通过下式的6,7-苯并吗啉衍生物的反应制备： [II]其中R1和R2如上所定义，与下式的醇化合物的反应性衍生物：其中X是任选被保护的羰基; 并且R 3如上所定义，任选地随后消除羰基的保护基，或通过下式的6,7-苯并吗啉衍生物的氧化：其中R 1，R 2和R 3是如上所述。

32. 发明授权

US4358620A 9-Formyl-9,10-dihydro-9,10-methanoanthracene 失效
标题翻译： 9-甲酰基-9,10-二氢-9,10-甲烷基蒽
公开(公告)号：US4358620A
公开(公告)日：1982-11-09
申请号：US139740
申请日：1980-04-14
申请人： Makoto Sunagawa , Hiromi Sato , Junki Katsube , Hisao Yamamoto
发明人： Makoto Sunagawa , Hiromi Sato , Junki Katsube , Hisao Yamamoto
IPC分类号： C07C47/235 , C07C47/238 , C07C47/453 , C07C57/50 , C07C61/39 , C07D295/02 , C07D295/03 , C07D295/125 , C07C47/52
CPC分类号： C07D295/03 , C07C47/235 , C07C47/238 , C07C47/453 , C07C57/50 , C07C61/39 , C07D295/125
摘要： Novel 9-aminoalkyl-methanoanthracenes of the formula: ##STR1## wherein A is C.sub.1 -C.sub.4 alkylene or C.sub.3 -C.sub.4 alkenylene and R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.6 cycloalkyl(C.sub.1 -C.sub.3)alkyl, ar(C.sub.1 -C.sub.3)alkyl or polyhalo(C.sub.2 -C.sub.4)alkyl or, when taken together with the adjacent nitrogen atom, they may form a 5 to 7-membered nitrogen-containing heterocyclic ring which may contain an additional hetero atom, and their non-toxic salts, which are useful as anti-anxiety, anti-depressant, major tranquilizer, anti-histamine and anti-allergy drugs and can be prepared through a novel key intermediate, i.e. 9-formyl-9,10-dihydro-9,10-methanoanthracene, by various methods.
摘要翻译：其中A为C 1 -C 4亚烷基或C 3 -C 4亚烯基，R 1和R 2各自为氢，C 1 -C 4烷基，C 3 -C 4烯基，C 3 -C 4炔基，C 3 -C 4炔基， C 1 -C 8环烷基（C 1 -C 3）烷基，芳（C 1 -C 3）烷基或多卤代（C 2 -C 4）烷基，或与相邻的氮原子一起形成5至7元含氮杂环，可以含有另外的杂原子及其无毒盐，其可用作抗焦虑剂，抗抑郁剂，主要镇静剂，抗组胺和抗过敏药物，并且可以通过新的关键中间体即9- 甲酰基-9,10-二氢-9,10-甲基蒽，通过各种方法。

33. 发明授权

US4073933A Novel bicycloheptene derivatives 失效
标题翻译：新型双环庚烯衍生物
公开(公告)号：US4073933A
公开(公告)日：1978-02-14
申请号：US697152
申请日：1976-06-17
申请人： Hiromi Shimomura , Akihiko Sugie , Junki Katsube , Hisao Yamamoto
发明人： Hiromi Shimomura , Akihiko Sugie , Junki Katsube , Hisao Yamamoto
IPC分类号： C07C405/00 , C07D309/12 , C07D311/94 , C07C177/00 , C07C61/38 , C07C69/74
CPC分类号： C07C405/0091 , C07C405/00 , C07D309/12 , C07D311/94 , Y10S514/925
摘要： Novel bicycloheptene compounds of the formula: ##STR1## wherein A is C.sub.2 -C.sub.4 alkylene; X and B are each ethylene or vinylene; R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.4 -C.sub.8 alkoxyalkyl, C.sub.5 -C.sub.7 cycloalkyl, C.sub.5 -C.sub.8 cycloalkylalkyl, aryl, C.sub.7 -C.sub.10 arylalkyl, C.sub.7 -C.sub.10 aryloxyalkyl; R.sub.2 is hydrogen, or C.sub.1 -C.sub.4 alkyl; and Z is carboxyl, C.sub.2 -C.sub.5 alkoxycarbonyl or C.sub.1 -C.sub.5 carbamoyl, and its non-toxic salts, which are useful as antiulcers, gastric secretion inhibitors, central nervous system regulators, and labor inducing agents.
摘要翻译：下式的新型双环庚烯化合物：其中A是C 2 -C 4亚烷基; X和B各自为亚乙烯基或亚乙烯基; R1是氢，C1-C8烷基，C4-C8烷氧基烷基，C5-C7环烷基，C5-C8环烷基烷基，芳基，C7-C10芳基烷基，C7-C10芳氧基烷基; R2是氢或C1-C4烷基; Z为羧基，C 2 -C 5烷氧基羰基或C 1 -C 5氨基甲酰基及其无毒盐，其可用作抗溃疡剂，胃分泌抑制剂，中枢神经系统调节剂和劳动诱导剂。

34. 发明授权

US4125731A Novel indan derivatives 失效
标题翻译：新的indan衍生物
公开(公告)号：US4125731A
公开(公告)日：1978-11-14
申请号：US748539
申请日：1976-12-08
申请人： Akihiko Sugie , Hiromi Shimomura , Junki Katsube , Hisao Yamamoto
发明人： Akihiko Sugie , Hiromi Shimomura , Junki Katsube , Hisao Yamamoto
IPC分类号： C07C17/32 , C07C33/38 , C07C405/00 , C07D307/93 , C07D309/12 , C07C69/76
CPC分类号： C07D309/12 , C07C17/32 , C07C33/38 , C07C405/00 , C07D307/93 , C07C2102/08 , Y10S514/927
摘要： Novel indan compounds of the formula ##STR1## wherein A and X are each ethylene or vinylene; B is C.sub.2-4 alkylene; R and R.sub.2 are each hydrogen or C.sub.1-4 alkyl; R.sub.1 is C.sub.1-8 alkyl;
摘要翻译：式IMA的新型茚满化合物，其中A和X各自为亚乙烯基或亚乙烯基; B是C 2-4亚烷基; R和R 2各自为氢或C 1-4烷基; R1是C1-8烷基; 及其无毒盐，其可用作抗溃疡剂，胃分泌物抑制剂和假体。

35. 发明授权

US4085210A Novel morpholine derivatives and the treatment of mental depression 失效
标题翻译：新型吗啉衍生物和精神抑郁症的治疗
公开(公告)号：US4085210A
公开(公告)日：1978-04-18
申请号：US646908
申请日：1976-01-06
申请人： Junki Katsube , Atsuyuki Kojima , Makoto Sunagawa , Yoshinori Takashima , Yoshito Kameno , Hisao Yamamoto
发明人： Junki Katsube , Atsuyuki Kojima , Makoto Sunagawa , Yoshinori Takashima , Yoshito Kameno , Hisao Yamamoto
IPC分类号： C07D265/30 , C07D267/10 , C07D409/06 , A61K31/535 , C07D405/06
CPC分类号： C07D265/30 , C07D267/10
摘要： Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4)alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D --E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.
摘要翻译：式中：R1代表氢或C1-C4烷基，R2代表氢，C1-C4烷基，C3-C5烯基，C3-C5炔基，芳基 - （C1-C4）烷基，（C3 -C 6）环烷基（C 1 -C 4）烷基，多卤代（C 2 -C 4）烷基或羟基（C 2 -C 4）烷基，A表示直链或支链C 2 -C 4亚烷基，B表示选自-CH 2 -CH 2 - ， - CH = CH-， -CH 2 -O-，-CH 2 -S-，-S-和-O-，> D-E-代表选自下组的三价基团：CH -CH 2 - 和> C = CH-且C 1和C 2各自表示任选被一个或多个选自卤素，C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的1,2-亚苯基，它们的无毒盐，其可用作抗抑郁药并且可以通过各种方法制备。

36. 发明授权

US4418079A Conjugated ketone compounds in preventing platelet thrombosis 失效
标题翻译：共轭酮化合物预防血小板血栓形成
公开(公告)号：US4418079A
公开(公告)日：1983-11-29
申请号：US335522
申请日：1981-12-29
申请人： Atsuyuki Kojima , Tsunemasa Irie , Shuichi Harada , Yoshito Kameno , Junki Katsube , Hisao Yamamoto
发明人： Atsuyuki Kojima , Tsunemasa Irie , Shuichi Harada , Yoshito Kameno , Junki Katsube , Hisao Yamamoto
IPC分类号： C07C29/42 , C07D209/44 , C07D295/108 , C07D307/52 , C07D317/58 , C07D333/22 , A61K27/00 , A61K31/135 , A61K31/34 , A61K31/36 , A61K31/38 , A61K31/40 , A61K31/44 , A61K31/445
CPC分类号： C07D295/108 , C07C29/42 , C07D209/44 , C07D307/52 , C07D317/58 , C07D333/22
摘要： Conjugated ketone compounds of the formula: ##STR1## wherein Ar is naphthyl, furyl, thienyl, or phenyl optionally bearing one or more substituents selected from the group consisting of chlorine, bromine, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, trifluoromethyl and methylenedioxy, R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.7 -C.sub.8 aralkyl or adamantyl, R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.5 alkenyl or C.sub.3 -C.sub.6 cycloalkyl, or when R.sub.1 and R.sub.2 are taken together with the nitrogen atom to which they are attached, they form a heterocyclic amino group containing up to 8 carbon atoms, A is straight or branched C.sub.1 -C.sub.3 alkylene, N-[4-(p-chlorophenyl)-4-oxo-2-trans-butenyl]morpholine and N-[4-(p-methoxyphenyl)-4-oxo-2-trans-butenyl]piperidine being excluded, and their non-toxic salts, which are useful as blood platelet anti-aggregative agents.
摘要翻译：具有下式的共轭酮化合物：其中Ar是萘基，呋喃基，噻吩基或任选具有一个或多个选自氯，溴，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4 烷基硫基，三氟甲基和亚甲二氧基，R 1是C 1 -C 6烷基，C 3 -C 5烯基，C 3 -C 6环烷基，C 7 -C 8芳烷基或金刚烷基，R 2是C 1 -C 6烷基，C 3 -C 5链烯基或C 3 -C 6环烷基，并且R 2与它们所连接的氮原子一起形成含有至多8个碳原子的杂环氨基，A是直链或支链C1-C3亚烷基，N- [4-（对氯苯基）-4 - 氧代-2-反式 - 丁烯基]吗啉和N- [4-（对甲氧基苯基）-4-氧代-2-反式 - 丁烯基]哌啶，以及它们的无毒盐，其可用作血小板抗体聚集代理。

37. 发明授权

US4224344A Organic tricyclic compounds 失效
标题翻译：有机三环化合物
公开(公告)号：US4224344A
公开(公告)日：1980-09-23
申请号：US639974
申请日：1975-12-11
申请人： Makoto Sunagawa , Hiromi Sato , Junki Katsube , Hisao Yamamoto
发明人： Makoto Sunagawa , Hiromi Sato , Junki Katsube , Hisao Yamamoto
IPC分类号： C07C47/235 , C07C47/238 , C07C47/453 , C07C57/50 , C07C61/39 , C07D295/02 , C07D295/03 , C07D295/125 , C07C87/28 , A01N9/24
CPC分类号： C07D295/03 , C07C47/235 , C07C47/238 , C07C47/453 , C07C57/50 , C07C61/39 , C07D295/125
摘要： Novel 9-aminoalkyl-methanoanthracenes of the formula: ##STR1## wherein A is C.sub.1 -C.sub.4 alkylene or C.sub.3 -C.sub.4 alkenylene and R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.6 cycloalkyl(C.sub.1 -C.sub.3)alkyl, ar(C.sub.1 -C.sub.3)alkyl or polyhalo(C.sub.2 -C.sub.4)alkyl or, when taken together with the adjacent nitrogen atom, they may form a 5 to 7-membered nitrogen-containing heterocyclic ring which may contain an additional hetero atom, and their non-toxic salts, which are useful as anti-anxiety, anti-depressant, major tranquilizer, anti-histamine and anti-allergy drugs and can be prepared through a novel key intermediate, i.e., 9-formyl-9,10-dihydro-9,10-methanoanthracene, by various methods.
摘要翻译：其中A为C 1 -C 4亚烷基或C 3 -C 4亚烯基，R 1和R 2各自为氢，C 1 -C 4烷基，C 3 -C 4烯基，C 3 -C 4炔基，C 3 -C 4炔基， C 1 -C 8环烷基（C 1 -C 3）烷基，芳（C 1 -C 3）烷基或多卤代（C 2 -C 4）烷基，或与相邻的氮原子一起形成5至7元含氮杂环，可以含有另外的杂原子及其无毒盐，它们可用作抗焦虑剂，抗抑郁剂，主要镇静剂，抗组胺和抗过敏药物，可以通过一种新的关键中间体即9 - 甲酰基-9,10-二氢-9,10-甲烷基蒽。

38. 发明授权

US4169146A Novel morpholine derivatives and treating depression therewith 失效
标题翻译：新型吗啉衍生物和治疗抑郁症
公开(公告)号：US4169146A
公开(公告)日：1979-09-25
申请号：US811944
申请日：1977-06-30
申请人： Junki Katsube , Atsuyuki Kojima , Makoto Sunagawa , Yoshinori Takashima , Yoshito Kameno , Hisao Yamamoto
发明人： Junki Katsube , Atsuyuki Kojima , Makoto Sunagawa , Yoshinori Takashima , Yoshito Kameno , Hisao Yamamoto
IPC分类号： C07D265/30 , C07D267/10 , A61K27/00
CPC分类号： C07D265/30 , C07D267/10
摘要： Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4) alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D--E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.
摘要翻译：式中：R1代表氢或C1-C4烷基，R2代表氢，C1-C4烷基，C3-C5烯基，C3-C5炔基，芳基 - （C1-C4）烷基，（C3 -C 6）环烷基（C 1 -C 4）烷基，多卤代（C 2 -C 4）烷基或羟基（C 2 -C 4）烷基，A表示直链或支链C 2 -C 4亚烷基，B表示选自-CH 2 -CH 2 - ， - CH = CH-， -CH 2 -O-，-CH 2 -S-，-S-和-O-，> DE-表示选自下组的三价基团：CH-CH 2 - 和> C = CH-和C1和C2各自表示任选被一个或多个选自卤素，C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的1,2-亚苯基及其无毒盐，其可用作抗抑郁药并且可以通过各种方法制备。

39. 发明授权

US4045560A 2-Morpholine containing methano or ethano anthracene compounds 失效
标题翻译：含有甲醇或乙炔蒽化合物的2-吗啉
公开(公告)号：US4045560A
公开(公告)日：1977-08-30
申请号：US703128
申请日：1976-07-07
申请人： Makoto Sunagawa , Hiromi Sato , Junki Katsube , Hisao Yamamoto
发明人： Makoto Sunagawa , Hiromi Sato , Junki Katsube , Hisao Yamamoto
IPC分类号： C07C1/22 , C07C47/453 , C07C57/50 , C07D265/30 , C07D265/32 , C07D303/04 , A61K31/535
CPC分类号： C07D265/30 , C07C1/22 , C07C47/453 , C07C57/50 , C07D265/32 , C07D303/04
摘要： Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, aryl(C.sub.1 -C.sub.4)alkyl or (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl and n represents 1 or 2, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.
摘要翻译：下式的新型吗啉化合物：其中R1代表氢，C1-C4烷基，C3-C5烯基，芳基（C1-C4）烷基或（C3-C6）环烷基（C1-C4）烷基，n表示1或 2及其无毒盐，其可用作抗抑郁药并且可以通过各种方法制备。

40. 发明授权

US3953446A Process for preparing quinazolines 失效
标题翻译：制备喹唑啉的方法
公开(公告)号：US3953446A
公开(公告)日：1976-04-27
申请号：US494885
申请日：1974-08-05
申请人： Kikuo Ishizumi , Kazuo Mori , Michihiro Yamamoto , Masao Koshiba , Shigeho Inaba , Hisao Yamamoto
发明人： Kikuo Ishizumi , Kazuo Mori , Michihiro Yamamoto , Masao Koshiba , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D239/82 , C07D209/10 , C07D209/42 , C07D401/06 , C07D405/06 , C07D409/06 , C07D405/04
CPC分类号： C07C247/00 , C07D209/42
摘要： Quinazoline derivatives which have anti-inflammatory, antiviral, uricosuric activities are prepared by reacting an indole-2-carbonylazide derivative with an oxidizing agent under mild conditions.
摘要翻译：具有抗炎，抗病毒，尿酸营养活性的喹唑啉衍生物通过在温和条件下使吲哚-2-羰基叠氮化物衍生物与氧化剂反应来制备。

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