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1. 发明授权

US4898876A Benzoylpiperazine esters and a process for their production 失效
标题翻译：苯甲酰哌嗪酯及其制备方法
公开(公告)号：US4898876A
公开(公告)日：1990-02-06
申请号：US796525
申请日：1985-11-12
申请人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Kazuhiro Onogi , Masahiko Nagakura
发明人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Kazuhiro Onogi , Masahiko Nagakura
IPC分类号： C07D209/48 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D237/28 , C07D241/44 , C07D261/18 , C07D295/192 , C07D307/79 , C07D307/84 , C07D307/86 , C07D311/12 , C07D311/58 , C07D311/84 , C07D317/68 , C07D319/18 , C07D333/54 , C07D333/60
CPC分类号： C07D209/48 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D237/28 , C07D241/44 , C07D261/18 , C07D295/192 , C07D307/79 , C07D307/84 , C07D307/86 , C07D311/12 , C07D311/58 , C07D311/84 , C07D317/68 , C07D319/18 , C07D333/54 , C07D333/60
摘要： A benzopylpiperazine ester of the following formula: ##STR1## wherein A represents a single bond or an alkylene group, vinylene group, --O--alkylene group or methine group, R.sub.1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenanthrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isozazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R.sub.2 represents an alkyl group, cycloalkyl group, cycloalkylalkyl group or aralkyl group, excepting the case where A is a single bond, R.sub.1 is ##STR2## and R.sub.2 is a methyl group, exhibits excellent chymotrypsin inhibitive activity.
摘要翻译：下式的苯甲酰基哌嗪酯：其中A表示单键或亚烷基，亚乙烯基，-O-亚烷基或次甲基，R 1表示可被低级烷基取代的双环碳环残基，低级烷氧基，氧代基或硝基或卤素原子，或可部分饱和; 可含有氧代基的芴残基; 亚芴基; 蒽残基; 可以被低级烷基取代的菲残基，或可以部分饱和; 可以被低级烷基或低级烷氧基取代的苯并呋喃残基或硫杂残基; 可被氧代基或苯基取代并部分饱和的苯并吡喃残基或苯并嗪残基; 邻苯二甲酰亚胺残基; 苯并二氮残基; 可以被低级烷基或苯基取代的异唑残基; 或亚烷基二氧基苯残基或呫吨残基; 除了A为单键，R 1为甲基，R 2为甲基的情况外，R 2表示烷基，环烷基，环烷基烷基或芳烷基，表现出优异的糜蛋白酶抑制活性。

2. 发明授权

US4746737A Phenyl guanidinobenzoate derivatives which have protease inhibitory activity 失效
标题翻译：具有蛋白酶抑制活性的苯胍基苯甲酸酯衍生物
公开(公告)号：US4746737A
公开(公告)日：1988-05-24
申请号：US886046
申请日：1986-07-16
申请人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Tomio Ohta , Nobuo Yokoo , Masahiko Nagakura
发明人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Tomio Ohta , Nobuo Yokoo , Masahiko Nagakura
IPC分类号： C07C279/18 , C07D207/16 , C07D207/26 , C07D207/27 , C07D243/08 , C07D295/185 , C07D265/30
CPC分类号： C07D207/27 , C07C279/18 , C07D207/16 , C07D243/08 , C07D295/185
摘要： Novel benzoyl esters of the following formula (I), and acid addition salts thereof, ##STR1## in which R.sub.1 and R.sub.2 are the same or different and represent a hydrogen atom or a lower alkoxy group, A represents a single bond, a linear or branched lower alkylene group, a lower alkenylene group, R.sub.3 and R.sub.4 are the same or different and represent a hydrogen atom or a lower alkyl group, or R.sub.3 and R.sub.4 join together to form a lower alkylene group, R.sub.5 represents a group of the formula, --X--(CO).sub.n --Y in which X represents a single bond, a linear or branched lower alkylene group or an alkenylene group, n is 0 or 1, Y represents a hydrogen atom, a cycloalkyl group, an aryl group, a hydroxyl group, a lower alkoxy group and the like are prepared by reacting para-nitrobenzoic acid or its derivative with a compound of the general formula (III) or its derivative ##STR2## to obtain a compound of the general formula (IV) ##STR3## followed by reducing the compound of the formula (IX) ##STR4## and subjecting the compound (IX) to guanidylation reaction, or by reaction para-guanidinobenzoic derivative with compound (III) or its derivative.The benzoyl esters have strong anti-trypsin activity, anti-thrombin activity and anticoagulant activity with low toxicity and are useful as a medicine for treatment of pancreatitis and disseminated intravascular coagulation (DIC).
摘要翻译：下式（I）的新型苯甲酰基酯及其酸加成盐，其中R 1和R 2相同或不同，表示氢原子或低级烷氧基，A表示单键，直链或支链低级亚烷基，低级亚烯基，R3和R4相同或不同，表示氢原子或低级烷基，或R3和R4连接在一起形成低级亚烷基，R5表示其中X表示单键的-X-（CO）nY，直链或支链低级亚烷基或亚烯基，n为0或1，Y表示氢原子，环烷基，芳基，通过使对硝基苯甲酸或其衍生物与通式（III）的化合物或其衍生物（IMAGE）（III）反应来制备羟基，低级烷氧基等，以获得通式（III）的化合物（Ⅳ），然后还原式（Ⅸ）化合物（IX）和使化合物（IX）进行胍基化反应，或通过反应对 - 胍基苯甲酸衍生物与化合物（III）或其衍生物反应。苯甲酰酯具有很强的抗胰蛋白酶活性，抗凝血酶活性和抗凝血活性，毒性低，可用作治疗胰腺炎和弥散性血管内凝血（DIC）的药物。

3. 发明授权

US4443603A Piperazine derivatives, of aromatic acids 失效
标题翻译：哌嗪衍生物，芳香酸
公开(公告)号：US4443603A
公开(公告)日：1984-04-17
申请号：US381443
申请日：1982-05-24
申请人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Hiroshi Ishihama
发明人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Koichiro Watanabe , Hiroshi Ishihama
IPC分类号： C07D295/18 , A61K31/495 , A61P43/00 , C07D207/24 , C07D209/18 , C07D295/088 , C07D295/13 , C07D295/15 , C07D295/185 , C07D403/12 , C07D241/04
CPC分类号： C07D295/185 , C07D207/24 , C07D209/18 , C07D295/088 , C07D295/13 , C07D295/15
摘要： A piperazine derivartive represented by the following formula: ##STR1## wherein R.sub.1 : an indolyl group which may optionally be substituted by one or more lower alkyl and/or lower alkoxy groups, naphthyl group which may optionally be saturated partially with 2 or 4 hydrogen atoms, or phenyl or cyclohexyl group which may optionally be substituted by one or more lower alkyl groups;A: a single bond or alkylene group;P: a single bond or vinylene group;Q: an -O-alkylene group or -NH-alkylene group when P is a single bond, or a single bond when P is a vinylene group; andR.sub.2 : a lower alkyl, morpholino-lower alkyl, morpholino-carbonyl lower alkyl, piperidinocarbonyl lower alkyl, piperazinocarbonyl lower alkyl or lower alkylaminocarbonyl lower alkyl group, or an acid addition salt thereof is a proteolytic enzyme inhibitor.
摘要翻译：由下式表示的哌嗪衍生物：其中R 1：可任选被一个或多个低级烷基和/或低级烷氧基取代的吲哚基，可任选地被2或4个氢原子部分饱和的萘基，或可任意被一个或多个低级烷基取代的苯基或环己基; A：单键或亚烷基; P：单键或亚乙烯基; Q：当P为单键时为-O-亚烷基或-NH-亚烷基，或当P为亚乙烯基时为单键; R2为低级烷基，吗啉代低级烷基，吗啉代羰基低级烷基，哌啶子基羰基低级烷基，哌嗪基羰基低级烷基或低级烷基氨基羰基低级烷基，或其酸加成盐为蛋白水解酶抑制剂。

4. 发明授权

US4620005A 1-isopropyl-4[(4-tetrahydro-1-naphthoyloxy phenyl)(alkylene)-carbonyl(oxymethlcarbonyl)]piperazines having chymotrypsin-inhibitory activity 失效
标题翻译：具有胰凝乳蛋白酶抑制活性的1-异丙基-4 [（4-四氢-1-萘氧基苯基）（亚烷基） - 羰基（羟甲羰基）]哌嗪
公开(公告)号：US4620005A
公开(公告)日：1986-10-28
申请号：US787714
申请日：1985-10-17
申请人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Hisashi Kunieda , Koichiro Watanabe , Hiroshi Ishihama
发明人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Hisashi Kunieda , Koichiro Watanabe , Hiroshi Ishihama
IPC分类号： C07D295/10 , A61K31/495 , A61P1/00 , A61P43/00 , C07D295/108 , C07D295/12 , C07D295/13 , C07D295/18 , C07D295/185 , C07D241/04
CPC分类号： C07D295/185 , C07D295/108 , C07D295/13
摘要： Phenyl tetrahydronaphthylcarboxylate of the formula: ##STR1## wherein A is a direct bond, or a lower alkylene, vinylene or imino group; B is a direct bond, a lower alkylene or --NH-lower alkylene group, or an --OCH.sub.2 CO-- residual group; and R is a lower alkyl group, with the proviso that A and B are not direct bonds simultaneously, and A, B and R are not a lower alkylene group, a direct bond and a methyl group, respectively, at the same time, are effectively useful as chymotrypsin inhibitors.
摘要翻译：下式的四氢萘基羧酸苯酯：其中A是直接键，或低级亚烷基，亚乙烯基或亚氨基; B是直接键，低级亚烷基或-NH-低级亚烷基或-OCH 2 CO-残基; 并且R是低级烷基，条件是A和B不是同时是直接键，并且A，B和R不分别是低级亚烷基，直接键和甲基，同时是有效用作糜蛋白酶抑制剂。

5. 发明授权

US4605739A Benzoyl indolecarboxylates 失效
标题翻译：苯甲酰基吲哚羧酸盐
公开(公告)号：US4605739A
公开(公告)日：1986-08-12
申请号：US608957
申请日：1984-05-10
申请人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Hisashi Kunieda , Koichiro Watanabe , Hiroshi Ishihama
发明人： Setsuro Fujii , Eizou Hattori , Mitsuteru Hirata , Hisashi Kunieda , Koichiro Watanabe , Hiroshi Ishihama
IPC分类号： A61K31/495 , A61P1/00 , C07D207/12 , C07D209/42 , C07D403/12
CPC分类号： C07D209/42 , C07D207/12
摘要： Benzoyl indolecarboxylates of the formula: ##STR1## where R.sup.1 is hydrogen, halogen, lower alkyl or lower alkoxy; R.sup.2 is hydrogen, lower alkyl, acetyl or benzoyl; R.sup.3 is hydrogen or lower alkyl; and A is a direct bond, or lower alkylene or vinylene substituted at the 2-, 3- or 5-position of the indole nucleus, are effective agents as chymotrypsin inhibitors.
摘要翻译：下式的苯甲酰基吲哚羧酸盐：其中R 1是氢，卤素，低级烷基或低级烷氧基; R2是氢，低级烷基，乙酰基或苯甲酰基; R3是氢或低级烷基; 并且A是直接键合，或在吲哚核的2-，3-或5-位取代的低级亚烷基或亚乙烯基，作为糜蛋白酶抑制剂是有效的试剂。

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