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1. 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。

2. 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。

3. 发明授权

US4755383A Pharmaceutical composition suitable for intestinal administration 失效
标题翻译：适合肠道给药的药物组合物
公开(公告)号：US4755383A
公开(公告)日：1988-07-05
申请号：US879946
申请日：1986-06-30
申请人： Setsuro Fujii , Touru Yokoyama , Kouji Ikegaya , Nobuo Yokoo , Masahiko Nagakura
发明人： Setsuro Fujii , Touru Yokoyama , Kouji Ikegaya , Nobuo Yokoo , Masahiko Nagakura
IPC分类号： A61K31/495 , A61K38/00 , A61K38/23 , A61K38/46 , A61K38/48 , A61K38/55 , A61K39/395 , A61K45/06 , A61P43/00 , A61K37/54
CPC分类号： A61K45/06 , A61K31/495 , A61K38/005 , Y10S514/808
摘要： A pharmaceutical composition is disclosed which comprises a physiologically active substance possessing peptide bonds in its structure and being inactivable by digestive enzymes, the active substances being other than insulin, and a synthetic chymotrypsin inhibitor. The composition is particularly suitable for intestinal absorption of the active substance.

4. 发明授权

US4639435A Pharmaceutical composition suitable for intestinal administration 失效
标题翻译：适用于肠道给药的药物组合物
公开(公告)号：US4639435A
公开(公告)日：1987-01-27
申请号：US625231
申请日：1984-06-27
申请人： Setsuro Fujii , Touru Yokoyama , Kouji Ikegaya , Nobuo Yokoo , Masahiko Nagakura
发明人： Setsuro Fujii , Touru Yokoyama , Kouji Ikegaya , Nobuo Yokoo , Masahiko Nagakura
IPC分类号： A61K31/495 , A61K38/00 , A61K38/23 , A61K38/46 , A61K38/48 , A61K38/55 , A61K39/395 , A61K45/06 , A61P43/00 , A61K37/30
CPC分类号： A61K45/06 , A61K31/495 , A61K38/005 , Y10S514/808
摘要： A pharmaceutical composition is disclosed which comprises a physiologically active substance possessing peptide bonds in its structure and being inactivable by digestive enzymes, the active substance being other than insulin, and a synthetic chymotrypsin inhibitor. The composition is particularly suitable for intestinal absorption of the active substance.
摘要翻译：公开了一种药物组合物，其包含其结构中具有肽键并且通过消化酶不活动的生理活性物质，所述活性物质不是胰岛素，以及合成的胰凝乳蛋白酶抑制剂。该组合物特别适用于活性物质的肠吸收。

5. 发明授权

US4217284A Process for preparation of optically pure lactones from monoesters of cis-cyclopentenediol 失效
标题翻译：从顺式环戊烯二醇的单酯制备光学纯内酯的方法
公开(公告)号：US4217284A
公开(公告)日：1980-08-12
申请号：US920833
申请日：1978-06-30
申请人： Shun-ichi Yamada , Shiro Terashima , Masahiko Nagakura , Munehiko Nara
发明人： Shun-ichi Yamada , Shiro Terashima , Masahiko Nagakura , Munehiko Nara
IPC分类号： C07D207/16 , C07D307/935 , C07D309/12 , C07D307/93
CPC分类号： C07D307/935 , C07D207/16 , C07D309/12
摘要： A novel monoester of cis-cyclopentenediol of the following formula ##STR1## wherein ##STR2## is an optically active acyl moiety. The monoester can be prepared by reacting cis-2-cyclopentene-1,4-diol with an optically active carboxylic acid of the following formula ##STR3## wherein ##STR4## is the same as defined above, or its reactive derivative, and separating the resulting reaction product into the two individual diastereomers. Lactones can be prepared from the monoesters selectively and with commercial advantage.
摘要翻译：下式（Ⅰ）的顺式环戊烯二醇的新型单酯其中，IMAGE是光学活性酰基部分。单酯可以通过使顺式-2-环戊烯-1,4-二醇与下式的光学活性羧酸（IMA）（III）反应制备，其中＆lt; IMAGE＆gt;与上述定义相同，或其活性衍生物，并将所得反应产物分离成两种单独的非对映异构体。内酯可以选择性地从单酯制备并具有商业优势。

6. 发明授权

US4335247A Novel nitrosourea derivatives and process for their production 失效
标题翻译：新型亚硝基脲衍生物及其制备方法
公开(公告)号：US4335247A
公开(公告)日：1982-06-15
申请号：US237273
申请日：1981-02-23
申请人： Kichitaro Takatori , Takashi Yamaguchi , Masahiko Nagakura
发明人： Kichitaro Takatori , Takashi Yamaguchi , Masahiko Nagakura
IPC分类号： A61K31/195 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/433 , A61P35/00 , C07C67/00 , C07C239/00 , C07C275/68 , C07D209/20 , C07D285/12 , C07D285/135
CPC分类号： C07D285/135 , C07C275/68
摘要： The specification describes a nitrosourea derivative having the general formula: Cl--(CH.sub.2).sub.2 --N(NO)CO--NHR, wherein --NHR represents a 2-(1,3,4-thiadiazolyl)amino group, an amino residue of a neutral .alpha.-amino acid, or an amino residue of a neutral .alpha.-amino acid whose carboxyl group is amidated with 2-(1,3,4-thiadiazolyl)amine, or a pharmaceutically acceptable acid addition salt thereof. The above nitrosourea derivative and its salt are useful as antitumor drugs. The above nitrosourea derivative may be prepared either by nitrosating a urea derivative of the general formula: Cl--(CH.sub.2).sub.2 NHCONHR or by reacting N-(2-chloroethyl)-N-nitrosocarbamic acid or a reactive derivative thereof with an amino compound of the general formula: R--NH.sub.2.
摘要翻译：本说明书描述了具有以下通式的亚硝基脲衍生物：Cl-（CH 2）2 -N（NO）CO-NHR，其中-NHR代表2-（1,3,4-噻二唑基）氨基，氨基残基中性α-氨基酸或其羧基与2-（1,3,4-噻二唑基）胺酰胺化的中性α-氨基酸的氨基残基或其药学上可接受的酸加成盐。上述亚硝基脲衍生物及其盐可用作抗肿瘤药物。上述亚硝基脲衍生物可以通过亚硝化通式为：C 1 - （CH 2）2 NHONHR的尿素衍生物或通过N-（2-氯乙基）-N-亚硝基氨基甲酸或其反应性衍生物与通式：R-NH2。

7. 发明授权

US4216225A Methylmethioninesulfonium compounds, process for their preparation, and pharmaceutical compositions containing them 失效
标题翻译：甲基亚氨基锍化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US4216225A
公开(公告)日：1980-08-05
申请号：US906567
申请日：1978-05-16
申请人： Masami Shiratsuchi , Kiyoshi Kawamura , Hisashi Kunieda , Naoki Machida , Toshihiro Akashi , Masahiko Nagakura
发明人： Masami Shiratsuchi , Kiyoshi Kawamura , Hisashi Kunieda , Naoki Machida , Toshihiro Akashi , Masahiko Nagakura
IPC分类号： A61K31/195 , A61K31/16 , A61K31/22 , A61P1/04 , C07C67/00 , C07C325/00 , C07C381/12 , C07D213/82 , A61K31/55 , A61K31/215
CPC分类号： C07D213/82
摘要： Methylmethioninesulfonium compounds of the formula ##STR1## wherein X.crclbar. represents an anion;R.sup.1 represents a hydrogen atom or an acyl group of the formula -COR.sup.3 in which R.sup.3 represents an alkyl group with 1 to 20 carbon atoms, the group --CH.sub.2).sub.2 COOH or the group ##STR2## in which Z represents a direct bond or a methylene or vinylene linkage, Y represents C or N, R.sup.4 represents a member selected from the class consisting of a hydrogen atom, lower alkyl groups, lower alkoxy groups, di-lower-alkylamino groups and a sulfamoyl group, n is a number of 1 to 3, and two or more R.sup.4 groups may be identical or different; andR.sup.2 represents the group --COOR.sup.5 in which R.sup.5 represents a hydrogen atom, an alkyl group with 1 to 5 carbon atoms or a metal- or metal complex-forming moiety, or the group ##STR3## in which R.sup.6 groups may be identical or different, and each represent a hydrogen atom or an alkyl group with 1 to 5 carbon atoms, with the proviso that when R.sup.1 represents a hydrogen atom, R.sup.2 is not --COOH; when R.sup.1 represents a hydrogen atom and R.sup.2 represents --CONH.sub.2, X.crclbar. is not Cl.crclbar.; and when R.sup.1 is --COCH.sub.3 and R.sup.2 is --COOCH.sub.3, X.crclbar. is not I.crclbar..The compounds can be easily prepared from methionine as a starting material by a combination of known unit reactions such as methylsulfonium-forming reaction, acylation, amidation, esterification and metal salt-forming reaction. These compounds are especially useful for treating ulcers.
摘要翻译：其中X（ - ）表示阴离子的式“IMAGE”的甲基甲硫氨onium化合物; R 1表示氢原子或式-COR 3的酰基，其中R 3表示具有1至20个碳原子的烷基，基团-CH 2）2 COOH或其中Z表示直接键或基团亚甲基或亚乙烯基，Y表示C或N，R4表示选自氢原子，低级烷基，低级烷氧基，二低级烷基氨基和氨磺酰基的成员，n为1 至3个，并且两个或更多个R 4基团可以相同或不同; 并且R 2表示其中R 5表示氢原子，具有1至5个碳原子的烷基或金属或金属络合物形成部分的基团-COOR 5或其中R6基团可以相同或不同的基团并且各自表示氢原子或具有1至5个碳原子的烷基，条件是当R 1表示氢原子时，R 2不是-COOH; 当R 1表示氢原子且R 2表示-CONH 2时，X（ - ）不是Cl（ - ）; 当R1是-COCH3且R2是-COOCH3时，X（ - ）不是I（ - ）。通过已知的单元反应如甲基锍形成反应，酰化，酰胺化，酯化和金属盐形成反应的组合，可以容易地从甲硫氨酸作为原料制备化合物。这些化合物特别适用于治疗溃疡。

8. 发明授权

US4394382A Dihydrobenzopyran compounds and pharmaceutical composition comprising said compounds 失效
标题翻译：二氢苯并吡喃化合物和包含所述化合物的药物组合物
公开(公告)号：US4394382A
公开(公告)日：1983-07-19
申请号：US271927
申请日：1981-06-09
申请人： Masami Shiratsuchi , Noboru Shimizu , Hiromichi Shigyo , Yoshinori Kyotani , Hisashi Kunieda , Kiyoshi Kawamura , Seiichi Sato , Toshihiro Akashi , Masahiko Nagakura , Naotoshi Sawada , Yasumi Uchida
发明人： Masami Shiratsuchi , Noboru Shimizu , Hiromichi Shigyo , Yoshinori Kyotani , Hisashi Kunieda , Kiyoshi Kawamura , Seiichi Sato , Toshihiro Akashi , Masahiko Nagakura , Naotoshi Sawada , Yasumi Uchida
IPC分类号： C07D311/04 , A61K31/353 , A61P9/02 , A61P9/04 , A61P21/02 , C07D311/22 , C07D311/58 , C07D311/64 , C07D311/66 , A61K31/35
CPC分类号： C07D311/22 , C07D311/58 , C07D311/64 , C07D311/66 , Y10S514/821
摘要： A benzopyran compound represented by the following ##STR1## wherein A represents a direct bond or the bond --CH.sub.2 --O--,R.sub.1 represents a member selected from the group consisting of a C.sub.3 -C.sub.5 alkyl group, a hydroxy-(C.sub.3 -C.sub.5 alkyl) group, a lower alkylamino-lower alkyl group, a nitrato-(C.sub.3 -C.sub.5 alkyl) group and a phenyl-(C.sub.1 -C.sub.5) alkyl group, provided that the phenyl may be substituted by a lower alkoxy group, R.sub.2 represents a member selected from the group consisting of hydrogen, halogen, OH, NO.sub.2, a carbamoyl group, a lower alkyl group, a lower alkoxy group, a lower alkyleneoxy group and acetyl group,R.sub.3 represents hydrogen or NO.sub.2,B represents a direct bond, a C.sub.1 -C.sub.7 alkylene group, a --O-lower alkylene group or a --CONH-lower alkylene group, andn represents 1 or 2;and an acid addition salt thereof and a pharmaceutical composition comprising aforesaid compound.
摘要翻译：由下式（I）表示的苯并吡喃化合物，其中A表示直接键或键-CH2-O-，R1表示选自C3-C5烷基，羟基 - （C3 -C 5烷基）基，低级烷基氨基 - 低级烷基，硝基 - （C 3 -C 5烷基）基和苯基 - （C 1 -C 5）烷基，条件是苯基可以被低级烷氧基取代，R 2 表示选自氢，卤素，OH，NO 2，氨基甲酰基，低级烷基，低级烷氧基，低级亚烷基氧基和乙酰基的成员，R 3表示氢或NO 2，B表示直接键，C 1 -C 7亚烷基，-O-低级亚烷基或-CONH-低级亚烷基，n表示1或2; 及其酸加成盐和包含上述化合物的药物组合物。

9. 发明授权

US4382142A Thiadiazole derivatives and process for preparing same 失效
标题翻译：噻二唑衍生物及其制备方法
公开(公告)号：US4382142A
公开(公告)日：1983-05-03
申请号：US203152
申请日：1980-11-03
申请人： Kichitaro Takatori , Takashi Yamaguchi , Masahiko Nagakura
发明人： Kichitaro Takatori , Takashi Yamaguchi , Masahiko Nagakura
IPC分类号： C07D285/12 , A61K31/41 , A61K31/433 , A61P35/00 , A61P35/02 , C07D285/135 , A61K31/425
CPC分类号： C07D285/135
摘要： A compound represented by the formula, ##STR1## wherein R.sub.1 represents a hydrogen atom, and R.sub.2 represents a lower alkyl group, an aryl group, an aralkyl group, a lower alkylthio lower alkyl group, a lower alkyl group substituted by a carboxyl or hydroxyl group, or a 3-indolymethyl group, or wherein R.sub.1 and R.sub.2 define in combination an alkylene group, or a pharmaceutically acceptable acid addition salt thereof, is an anti-tumor agent for leukemia and malignant tumors.
摘要翻译：由式表示的化合物，其中R1表示氢原子，R2表示低级烷基，芳基，芳烷基，低级烷硫基低级烷基，被羧基或羟基取代的低级烷基基团或3-取代的甲基，或其中R1和R2组合形成亚烷基或其药学上可接受的酸加成盐是白血病和恶性肿瘤的抗肿瘤剂。

10. 发明授权

US4170596A Novel monoesters of cis-cyclopentenediol, process for preparation thereof, and process for preparation of lactones from the monoesters 失效
标题翻译：顺式环戊烯二醇的新型单酯，其制备方法，以及由单酯制备内酯的方法
公开(公告)号：US4170596A
公开(公告)日：1979-10-09
申请号：US839356
申请日：1977-10-04
申请人： Shun-Ichi Yamada , Shiro Terashima , Masahiko Nagakura , Munehiko Nara
发明人： Shun-Ichi Yamada , Shiro Terashima , Masahiko Nagakura , Munehiko Nara
IPC分类号： C07D207/16 , C07D307/935 , C07D309/12 , C07D207/12 , C07C149/40
CPC分类号： C07D307/935 , C07D207/16 , C07D309/12
摘要： A novel monoester of cis-cyclopentenediol of the following formula ##STR1## wherein ##STR2## is an optically active acyl moiety. The monoester can be prepared by reacting cis-2-cyclopentene-1,4-diol with an optically active carboxylic acid of the following formula ##STR3## wherein ##STR4## is the same as defined above, or its reactive derivative, and separating the resulting reaction product into the two individual diastereomers. Lactones can be prepared from the monoesters selectively and with commercial advantage.
摘要翻译：下式（Ⅰ）的顺式环戊烯二醇的新型单酯其中，IMAGE是光学活性酰基部分。单酯可以通过使顺式-2-环戊烯-1,4-二醇与下式的光学活性羧酸（IMA）（III）反应制备，其中＆lt; IMAGE＆gt;与上述定义相同，或其活性衍生物，并将所得反应产物分离成两种单独的非对映异构体。内酯可以选择性地从单酯制备并具有商业优势。

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