公开(公告)号：US4003936A

公开(公告)日：1977-01-18

申请号：US202597

申请日：1971-11-26

申请人： Masaji Ohno ,  Mutsuo Kataoka ,  Norio Kawabe

发明人： Masaji Ohno ,  Mutsuo Kataoka ,  Norio Kawabe

IPC分类号： A61K31/12 ,  C07C45/62 ,  C07C45/68 ,  C07C45/74 ,  C07C49/657 ,  C07C49/697 ,  C07C49/747 ,  C07C49/753 ,  C07C49/82 ,  C07D317/54 ,  C07C49/76 ,  C07C49/80 ,  C07C49/84

CPC分类号： C07D317/54 ,  C07C205/45 ,  C07C45/62 ,  C07C45/68 ,  C07C45/74 ,  C07C49/657 ,  C07C49/697 ,  C07C49/747 ,  C07C49/753

摘要： As new compound, a series of 2-hydrocinnamoyl-1,3-cyclopentanedione derivative of the general formula: ##STR1## WHEREIN Ar stands for a mono-valent aromatic radical, for example, phenyl and 3,4-methylenedioxy-phenyl, substituted or unsubstituted, have been found to have an activity to inhibit the action of tyrosine hydroxylase and to be useful as hypotensive agent. These new compounds may be produced by condensing 2-acetyl-1,3-cyclopentanedione with an aromatic aldehyde of the formula Ar-CHO wherein Ar is as defined, according to Claisen-Schmidt condensation, followed by the hydrogenation of the condensation product obtained, or the new compounds may also be produced by reacting 2-acetyl-1,3-cyclopentanedione with an aromatic halide of the formula Ar-CH.sub.2 X wherein Ar is as defined and X is a halogen, for example, in liquid ammonia and in the presence of an alkali metal amide.

摘要翻译： 作为新化合物，通式为：其中Ar表示一价芳族基团的一系列2-氢化肉桂酰基-1,3-环戊二酮衍生物，例如苯基和3,4-亚甲二氧基 - 苯基，取代 或未取代的，已经被发现具有抑制酪氨酸羟化酶作用的活性并且可用作降压剂。 这些新化合物可以通过将2-乙酰基-1,3-环戊二酮与式Ar-CHO的芳族醛缩合制备，其中Ar如所定义，根据Claisen-Schmidt缩合，然后氢化得到的缩合产物， 或者新化合物也可以通过使2-乙酰基-1,3-环戊二酮与式Ar-CH 2 X的芳族卤化物反应来制备，其中Ar如所定义，X是卤素，例如在液氨中，并且在存在下 的碱金属酰胺。

公开(公告)号：US4061769A

公开(公告)日：1977-12-06

申请号：US672594

申请日：1976-04-01

申请人： Masaji Ohno ,  Mutsuo Kataoka

发明人： Masaji Ohno ,  Mutsuo Kataoka

IPC分类号： C07D309/36 ,  A61K31/35 ,  A61K31/36

CPC分类号： C07D309/36

摘要： New compounds of the formula ##STR1## WHEREIN Ar is selected from the group consisting of phenylethyl, furyl, methylfuryl, thienyl, pyrrolyl, naphthyl, hydroxynaphthyl, and phenyl substituted by at least one member selected from the group consisting of halogen, hydroxyl, cyano, trifluoromethyl, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, carbamoyl, amino of the formula --NR'R", alkoxycarbonyl of the formula --CO--OR' wherein R' and R" are each alkyl of 1-4 carbon atoms, and alkylenedioxy of the formula --O--R'"--O-- wherein R'" is alkylene of 1-4 carbon atoms, provided that said substituted phenyl is not 3,4-di-methoxyphenyl, and the addition salts thereof with the cation of an organic or inorganic base inhibit the enzyme activities of tyrosine hydroxylase and dopamine .beta.-hydroxylase and are useful chemotherapeutic agents in the treatment of essential hypertension.

摘要翻译： 式中新的化合物，其中Ar选自苯乙基，呋喃基，甲基呋喃基，噻吩基，吡咯基，萘基，羟基萘基和被至少一个选自卤素，羟基，氰基 ，三氟甲基，1-4个碳原子的烷基，1-4个碳原子的烷氧基，氨基甲酰基，式-NR'R“的氨基，式-CO-OR'的烷氧基羰基，其中R'和R”各自为 1-4个碳原子的烷基和式-O-R“' - O-的亚烷基二氧基，其中R”'是1-4个碳原子的亚烷基，条件是所述取代的苯基不是3,4-二 - 甲氧基苯基，其与有机或无机碱的阳离子的加成盐抑制酪氨酸羟化酶和多巴胺β-羟化酶的酶活性，并且是治疗原发性高血压的有用的化学治疗剂。

公开(公告)号：US3963756A

公开(公告)日：1976-06-15

申请号：US363559

申请日：1973-05-24

申请人： Masaji Ohno ,  Mutsuo Kataoka

发明人： Masaji Ohno ,  Mutsuo Kataoka

IPC分类号： A61K31/35 ,  A61K31/351 ,  A61K31/36 ,  A61P9/12 ,  A61P43/00 ,  C07D309/36 ,  C07D309/30

CPC分类号： C07D309/36

摘要： New compounds of the formula ##SPC1##Wherein Ar is selected from the group consisting of phenylethyl, furyl, methylfuryl, thienyl, pyrrolyl, naphthyl, hydroxynaphthyl, and phenyl substituted by at least one member selected from the group consisting of halogen, hydroxyl, cyano, trifluoromethyl, akyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, carbamoyl, amino of the formula --NR'R", alkoxycarbonyl of the formula --CO--OR' wherein R'and R"are each alkyl of 1-4 carbon atoms, and alkylenedioxy of the formula --O--R '"--O-- wherein R'" is alkylene of 1-4 carbon atoms, provided that said substituted phenyl is not 3,4-di-methoxyphenyl, and the addition salts thereof with the cation of an organic or inorganic base inhibit the enzyme activities of tyrosine hydroxylase and dopamine .beta.-hydroxylase and are useful chemotherapeutic agents in the treatment of essential hypertension.

摘要翻译： 新的式WHEREIN Ar化合物选自苯乙基，呋喃基，甲基呋喃基，噻吩基，吡咯基，萘基，羟基萘基和被至少一种选自卤素，羟基，氰基，三氟甲基， 1-4个碳原子的烷基，1-4个碳原子的烷氧基，氨基甲酰基，式-NR'R“的氨基，式-CO-OR'的烷氧基羰基，其中R'和R”各为1的烷基 -4个碳原子和亚烷基二氧基，其中R“是1-4个碳原子的亚烷基，条件是所述取代的苯基不是3,4-二甲氧基苯基，并且加成 其与有机或无机碱的阳离子的盐抑制酪氨酸羟化酶和多巴胺β-羟化酶的酶活性，并且是治疗原发性高血压的有用的化学治疗剂。

公开(公告)号：US4065475A

公开(公告)日：1977-12-27

申请号：US688920

申请日：1976-05-21

申请人： Kazuo Hosoi ,  Norio Kawabe ,  Masaji Ohno

发明人： Kazuo Hosoi ,  Norio Kawabe ,  Masaji Ohno

IPC分类号： C07D303/48 ,  C07D301/12

CPC分类号： C07D303/48

摘要： High purity cis-epoxysuccinic acid and salts thereof are economically and systematically prepared by contacting an aqueous solution, obtained by reacting a maleic acid salt and hydrogen peroxide in the presence of a tungstate or molybdate catalyst under a specified condition, with a strongly basic Type II anion exchange resin.

摘要翻译： 在特定条件下，在钨酸盐或钼酸盐催化剂存在下，通过使马来酸盐和过氧化氢反应得到的水溶液与强碱性II型相接触，经济地和系统地制备高纯度顺式 - 环氧琥珀酸及其盐 阴离子交换树脂。

公开(公告)号：US4980347A

公开(公告)日：1990-12-25

申请号：US337573

申请日：1989-04-13

申请人： Masaji Ohno ,  Masato Mutoh ,  Go Hata ,  Keiichi Matsunaga ,  Satoshi Hanada

发明人： Masaji Ohno ,  Masato Mutoh ,  Go Hata ,  Keiichi Matsunaga ,  Satoshi Hanada

IPC分类号： C07F15/00

CPC分类号： C07F15/0093

摘要： A platinum complex represented by the formula: ##STR1## where X is ##STR2## wherein R.sup.1 is a (C1-18) alkyl group, a (C1-18)alkenyl group or a group --Z--R.sup.4 in which Z is --CH.dbd.CH-- or a (C1-5)alkylene group, and R.sup.4 is a phenyl group, a hydroxyphenyl group, a (C7-12)alkoxyphenyl group, a halogenophenyl group, a nitrophenyl group, or (C8-13)alkoxycarbonylphenyl group, a cyclohexyl group having a (C1-5)alkyl substituent, ##STR3## R.sup.2 is hydrogen or a (C1-18)alkyl group, R.sup.3 is hydrogen or a (C1-3) alkyl group, R.sup.2 and R.sup.3 are linked together to form a (C2-7)alkylene group; the dotted line indicates that the bond may be either a single bond or a double bond; the chain line indicates a conjugated system; the 1,2-diaminocyclohexane moiety has a cis-, trans-l- or trans-d-configuration; and Y is an anion. This platinum complex is useful in the treatment of tumors.

摘要翻译： 由下式表示的铂络合物：其中X为，其中R1为（C1-18）烷基，（C1-18）烯基或-Z-R4基团，其中Z 是-CH = CH-或（C1-5）亚烷基，R4是苯基，羟基苯基，（C7-12）烷氧基苯基，卤代苯基，硝基苯基或（C8-13） 烷氧基羰基苯基，具有（C1-5）烷基取代基的环己基，R2是氢或（C1-18）烷基，R3是氢或（C1-3）烷基，R2和R3连接 一起形成（C2-7）亚烷基; 虚线表示该键可以是单键或双键; 链线表示共轭系统; 1,2-二氨基环己烷部分具有顺式，反式-1-或反式-d构型; Y为阴离子。 该铂络合物可用于治疗肿瘤。

公开(公告)号：US4912100A

公开(公告)日：1990-03-27

申请号：US108074

申请日：1987-10-13

申请人： Masaji Ohno ,  Masato Mutoh ,  Hisao Kondo ,  Keiichi Matsunaga

发明人： Masaji Ohno ,  Masato Mutoh ,  Hisao Kondo ,  Keiichi Matsunaga

IPC分类号： C07F15/00

CPC分类号： C07F15/0093

摘要： A platinum complex represented by the formula: ##STR1## wherein R.sup.1 is a (Cl-18) alkyl group, a (Cl-18)-alkenyl group or a group ----X--R.sup.5 in which X is --CH.dbd.CH-- or a (Cl-5)alkylene group, and R.sup.5 is a phenyl group, a hydroxyphenyl group, a (C7-12) alkoxyphenyl group, a halogenophenyl group, a nitrophenyl group, or (C8-13)alkoxycarbonylphenyl group, a cyclohexyl group having a (Cl--5)alkyl substituent, ##STR2## R.sup.2 is a (Cl-18 alkyl group, R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 are linked together to form a (C2-7)alkylene group, R.sup.4 is OH or NO.sub.3 ; the dotted line indicates that the bond may be either a single bond or a double bond; the chain line indicates a conjugated system; n is a number of from 1 to 2, and the 1,2-diaminocyclohexane moiety has a cis-, trans-l- or trans-d-configuration. This platinum complex is useful in the treatment of tumors.

公开(公告)号：US08501977B2

公开(公告)日：2013-08-06

申请号：US13060906

申请日：2009-08-25

申请人： Hisae Arai ,  Masaji Ohno ,  Hisao Kondo ,  Ikuko Arai

发明人： Hisae Arai ,  Masaji Ohno ,  Hisao Kondo ,  Ikuko Arai

IPC分类号： C07F15/00 ,  A61K31/28

CPC分类号： C07C55/07 ,  C07C61/04 ,  C07C211/38 ,  C07C2602/50 ,  C07F15/0093

摘要： A new platinum complex which has strong antitumor activity and has effect with smaller doses and a pharmaceutical composition containing the same are provided. A spiro[4,4]nonane-1,6-diamineplatinum(II) complex which is represented by a following general formula (A). (In the formula, X and Y are same or different, and X and Y represent halogen atoms respectively, or X and Y cooperatively represent a divalent residue which is described by a formula (Z).) The platinum complex has a strong antitumor activity and is efficacious as a therapeutic agent for malignant tumors.

摘要翻译： 提供了具有强抗肿瘤活性并具有较小剂量效果的新型铂络合物和含有该铂络合物的药物组合物。 由以下通式（A）表示的螺[4,4]壬烷-1,6-二氨基铂（II）络合物。 （式中X和Y相同或不同，X和Y分别表示卤素原子，或X和Y表示二价残基，由式（Z）表示）。铂络合物具有强的抗肿瘤活性 并且作为恶性肿瘤的治疗剂是有效的。

公开(公告)号：US4452897A

公开(公告)日：1984-06-05

申请号：US388475

申请日：1982-06-14

申请人： Hamao Umezawa ,  Masaji Ohno ,  Hirokazu Kotani ,  Toshinori Miyabe ,  Akira Obayashi ,  Osamu Tanabe

发明人： Hamao Umezawa ,  Masaji Ohno ,  Hirokazu Kotani ,  Toshinori Miyabe ,  Akira Obayashi ,  Osamu Tanabe

IPC分类号： C12P13/04 ,  C07B20/00 ,  C12R1/20

CPC分类号： C12P13/04 ,  Y10S435/85

摘要： The present invention provides a process for preparing a optically active .beta.-(S)-aminoglutaric acid monoalkyl ester of the formula: ##STR1## wherein R is a lower alkyl group having 1 to 4 carbon atoms, which comprises subjecting a .beta.-N-protected aminoglutaric acid dialkyl ester of the formula: ##STR2## wherein each R is as defined above and A is an easily removable protecting group, to an action of an enzyme produced by a microorganism belonging to the genera Flavobacterium, Achromobacter, Xanthomonas, Alcaligenes, Serratia, Gluconobacter, Chromobacterium and Acetobacter, to selectively hydrolyze only one of the two ester groups, and then removing the protecting group.

摘要翻译： 本发明提供了制备下式的光学活性β-（S） - 氨基戊二酸单烷基酯的方法：其中R是具有1至4个碳原子的低级烷基，其包括使β N-保护的下式的化合物的氨基戊二酸二烷基酯：其中每个R如上定义并且A是容易除去的保护基团，涉及由属于黄杆菌属的微生物产生的酶的作用， 无色杆菌，黄单胞菌属，产碱杆菌属，沙雷氏菌属，葡萄糖酸杆菌属，色杆菌属和醋杆菌属，仅选择性地水解两个酯基中的一个，然后除去保护基团。

公开(公告)号：US20110152555A1

公开(公告)日：2011-06-23

申请号：US13060906

申请日：2009-08-25

申请人： Hisae Arai ,  Masaji Ohno ,  Hisao Kondo ,  Ikuko Arai

发明人： Hisae Arai ,  Masaji Ohno ,  Hisao Kondo ,  Ikuko Arai

IPC分类号： C07F15/00

CPC分类号： C07C55/07 ,  C07C61/04 ,  C07C211/38 ,  C07C2602/50 ,  C07F15/0093

摘要： A new platinum complex which has strong antitumor activity and has effect with smaller doses and a pharmaceutical composition containing the same are provided. A spiro[4,4]nonane-1,6-diamineplatinum(II) complex which is represented by a following general formula (A). (In the formula, X and Y are same or different, and X and Y represent halogen atoms respectively, or X and Y cooperatively represent a divalent residue which is described by a formula (Z).) The platinum complex has a strong antitumor activity and is efficacious as a therapeutic agent for malignant tumors.

摘要翻译： 提供了具有强抗肿瘤活性并具有较小剂量效果的新型铂络合物和含有该铂络合物的药物组合物。 由以下通式（A）表示的螺[4,4]壬烷-1,6-二氨基铂（II）络合物。 （式中X和Y相同或不同，X和Y分别表示卤素原子，或X和Y表示二价残基，由式（Z）表示）。铂络合物具有强的抗肿瘤活性 并且作为恶性肿瘤的治疗剂是有效的。

公开(公告)号：US4415657A

公开(公告)日：1983-11-15

申请号：US328696

申请日：1981-12-08

申请人： Hamao Umezawa ,  Masaji Ohno ,  Junzo Hasegawa ,  Shigeki Hamaguchi ,  Masahiro Ogura ,  Hajime Kawaharada ,  Kiyoshi Watanabe

发明人： Hamao Umezawa ,  Masaji Ohno ,  Junzo Hasegawa ,  Shigeki Hamaguchi ,  Masahiro Ogura ,  Hajime Kawaharada ,  Kiyoshi Watanabe

IPC分类号： C12P13/04 ,  C07B19/02 ,  C12P7/62

CPC分类号： C12P13/04 ,  Y10S435/83 ,  Y10S435/832 ,  Y10S435/84 ,  Y10S435/843 ,  Y10S435/859 ,  Y10S435/872 ,  Y10S435/874 ,  Y10S435/882 ,  Y10S435/885 ,  Y10S435/911 ,  Y10S435/912 ,  Y10S435/913 ,  Y10S435/921 ,  Y10S435/929 ,  Y10S435/931 ,  Y10S435/932 ,  Y10S435/933 ,  Y10S435/938 ,  Y10S435/939

摘要： A process is disclosed in which an optically active monoalkyl ester of .beta.-(S)-aminoglutaric acid is prepared by subjecting a dialkyl ester of .beta.-protected aminoglutaric acid to the action of a culture broth, cells, or treated cells of a microorganism capable of stereoselectively hydrolyzing only one of the ester groups in the above-mentioned dialkyl ester to produce an optically active monoalkyl ester of .beta.-protected (S)-aminoglutaric acid, and then removing the amino-protecting group from the product. An optically active monoalkyl ester of .beta.-(S)-aminoglutaric acid is useful as a starting material for synthesizing .beta.-lactam antibiotics of carbapenem type such as thienamycin.

摘要翻译： 公开了一种方法，其中β-（S） - 氨基戊二酸的光学活性单烷基酯通过使β-受保护的氨基戊二酸的二烷基酯经受培养液，细胞或能够处理的微生物的处理细胞的作用 立体选择性地水解上述二烷基酯中的一个酯基，得到β-保护（S） - 氨基戊二酸的光学活性单烷基酯，然后从产物中除去氨基保护基。 β-（S） - 氨基戊二酸的光学活性单烷基酯可用作合成碳青霉烯类的β-内酰胺抗生素如噻吩霉素的起始原料。