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1. 发明授权

US4153610A Process for producing 5-carboxy-2-acetylthiophene 失效
标题翻译： 5-羧基-2-乙酰基噻吩的制备方法
公开(公告)号：US4153610A
公开(公告)日：1979-05-08
申请号：US847617
申请日：1977-11-01
申请人： Toshihiko Hibino , Eiichi Murayama
发明人： Toshihiko Hibino , Eiichi Murayama
IPC分类号： C07D333/24 , C07D333/38
CPC分类号： C07D333/38 , C07D333/24
摘要： 5-Carboxy-2-acetylthiophene, which is useful as an intermediate for the production of a therapeutic agent, can be prepared in a high yield by the selective oxidation of 5-acetyl-2-thienylacetic acid or its derivative with a particularly selected oxidizing agent, i.e. permanganate.
摘要翻译：可用作制备治疗剂的中间体的5-羧基-2-乙酰基噻吩可以通过选择性氧化5-乙酰基-2-噻吩基乙酸或其衍生物，以高产率通过特别选择的氧化代理，即高锰酸盐。

2. 发明授权

US4054568A Thiazolo(5,4-f)quinoline-8-carboxylic acid derivatives 失效
标题翻译：噻唑（5,4-f）喹啉-8-羧酸衍生物
公开(公告)号：US4054568A
公开(公告)日：1977-10-18
申请号：US661455
申请日：1976-02-25
申请人： Hideo Agui , Toru Mitani , Mitsuo Nakashita , Eiichi Murayama , Kousaku Okamura , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Yasuko Eda
发明人： Hideo Agui , Toru Mitani , Mitsuo Nakashita , Eiichi Murayama , Kousaku Okamura , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Yasuko Eda
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： Thiazolo[5,4-f]quinoline-8-carboxylic acid derivatives having either the general formula (I): ##STR1## wherein R.sub.1 is a lower alkyl group, a lower alkenyl group or a benzyl group; or the general formula (III-a): ##STR2## WHEREIN R.sub.3 is a lower alkyl group and X is a halogen atom; and methods for the preparation thereof. The compounds of the general formula (I) are useful as antibacterial agents against gram-negative and gram-positive bacteria. The compounds of the general formula (III-a) are useful as antifungal agents against eumycetes and also as an intermediate in a peparation of the compounds of the general formula (I).
摘要翻译：具有通式（I）的噻唑并[5,4-f]喹啉-8-羧酸衍生物：其中R1是低级烷基，低级烯基或苄基; （III-a）：（III-a）其中R3为低级烷基，X为卤素原子; 及其制备方法。通式（I）的化合物可用作抗革兰氏阴性细菌和革兰氏阳性细菌的抗菌剂。通式（III-a）的化合物可用作抗真菌剂的抗真菌剂，也可用作通式（I）化合物的分离中的中间体。

3. 发明授权

US3954775A Thiazolo(5,4-f)quinoline-8-carboxylic acid derivatives 失效
标题翻译：噻唑（5,4-f）喹啉-8-羧酸衍生物
公开(公告)号：US3954775A
公开(公告)日：1976-05-04
申请号：US515753
申请日：1974-10-17
申请人： Hideo Agui , Toru Mitani , Mitsuo Nakashita , Eiichi Murayama , Kousaku Okamura , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Yasuko Eda
发明人： Hideo Agui , Toru Mitani , Mitsuo Nakashita , Eiichi Murayama , Kousaku Okamura , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Yasuko Eda
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： Thiazolo[5,4-f]quinoline-8-carboxylic acid derivatives having either the general formula (I): ##SPC1##wherein R.sub.1 is a lower alkyl group, a lower alkenyl group or a benzyl group; or the general formula (III-a): ##SPC2##Wherein R.sub.3 is a lower alkyl group and X is a halogen atom; and methods for the preparation thereof. The compounds of the general formula (I) are useful as antibacterial agents against gram-negative and gram-positive bacteria. The compounds of the general formula (III-a) are useful as antifungal agents against eumycetes and also as an intermediate in a preparation of the compounds of the general formula (I).
摘要翻译：具有通式（I）的噻唑并[5,4-f]喹啉-8-羧酸衍生物：

4. 发明授权

US4082913A Phenoxyalicyclic carboxylic acid derivatives 失效
标题翻译：羟基乙酰氧基酸衍生物
公开(公告)号：US4082913A
公开(公告)日：1978-04-04
申请号：US365277
申请日：1973-05-30
申请人： Yoshio Suzuki , Masayoshi Minai , Noritaka Hamma , Eiichi Murayama , Shunji Aono
发明人： Yoshio Suzuki , Masayoshi Minai , Noritaka Hamma , Eiichi Murayama , Shunji Aono
IPC分类号： C07C62/08 , A61K20060101 , A61K31/19 , A61K31/215 , A61P9/10 , A61P29/00 , C07C20060101 , C07C51/00 , C07C61/00 , C07C61/06 , C07C61/08 , C07C61/12 , C07C62/34 , C07C63/00 , C07C67/00 , C07C69/66 , C07C69/74 , C07C69/757 , C07C69/76
CPC分类号： C07C51/367 , Y10S514/824
摘要： Novel anti-atherosclerosis agents having the formula, ##STR1## wherein R is hydrogen or lower alkyl, n and m each signify an integer of 4 - 6, and A is hydrogen or a group of the formula, ##STR2## WHEREIN R and m have the same meanings as defined above. These compounds are produced, for example, by reacting a bisphenolic compound of the formula, ##STR3## with chloroform and a ketone compound of the formula, ##STR4## in the presence of an alkali. Alternatively, they are produced by reacting the bisphenolic compound with .alpha.-halogeno- or .alpha.-hydroxycarboxylic acid derivative of the formula, ##STR5## wherein R and m have the same meanings as defined above, and X is halogen or hydroxyl.

5. 发明授权

US4008265A Novel bisphenoxy carboxylic acid derivatives and their salts 失效
公开(公告)号：US4008265A
公开(公告)日：1977-02-15
申请号：US491033
申请日：1974-07-23
申请人： Yoshio Suzuki , Masayoshi Minai , Noritaka Hamma , Eiichi Murayama , Shunji Aono
发明人： Yoshio Suzuki , Masayoshi Minai , Noritaka Hamma , Eiichi Murayama , Shunji Aono
IPC分类号： C07D211/46 , C07D213/30 , C07D213/75 , C07D295/185 , C07C69/66
CPC分类号： C07D213/30 , C07D211/46 , C07D213/75 , C07D295/185 , Y10S514/824
摘要： Bisphenoxy carboxylic acid derivatives useful as an antiarteriosclerosis agent with good absorbability and low toxicity, which are novel compounds represented by the general formula, ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atoms or lower alkyl groups and A represents ##STR2## (wherein in case R.sub.3 is a hydrogen atom, R.sub.4 represents an amino-lower-alkyl group, an N-lower-alkylaminoalkyl group, a heterocyclic group, or a heterocyclic group-substituted alkyl group; or R.sub.3 and R.sub.4 may join through an intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent) or ##STR3## (wherein R.sub.5 represents a hydrogen atom, a hydroxyalkyl group or a derivative thereof, and R.sub.6 represents a hydroxyalkyl group or a heterocyclic group; or R.sub.5 and R.sub.6 may join to form a cyclic group, or may join through another intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent), are prepared by reacting a bisphenoxy acid represented by the general formula, ##STR4## wherein R.sub.1 and R.sub.2 have the same meanings as defined above, or a reactive derivative thereof with a hetero atom-containing alcohol compound represented by the general formula, ##STR5## wherein R.sub.3 and R.sub.4 have the same meanings as defined above, an amine derivative represented by the general formula, ##STR6## wherein R.sub.5 and R.sub.6 have the same meanings as defined above, or a salt thereof. Alternatively, the bisphenoxy carboxylic acid derivatives represented by the said general formula (I), wherein A is ##STR7## R.sub.5 is hydrogen and R.sub.6 is a hydroxyalkyl group, are prepared by heating a bisphenoxy acid derivative represented by the general formula, ##STR8## wherein R.sub.1 and R.sub.2 have the same meanings as defined above and X represents an alkylene chain.

6. 发明授权

US4092324A Diheterocyclic esters of 4-(1,1-bis-(phenoxy-propionic or -butoyric acid)-cyclohexane).alpha.-methyl substituted 失效
标题翻译： 4-（1,1-双 - （苯氧基 - 丙酸） - 环己烷）（60-甲基取代的）的二杂环酯
公开(公告)号：US4092324A
公开(公告)日：1978-05-30
申请号：US716666
申请日：1976-08-23
申请人： Yoshio Suzuki , Masayoshi Minai , Noritaka Hamma , Eiichi Murayama , Shunji Aono
发明人： Yoshio Suzuki , Masayoshi Minai , Noritaka Hamma , Eiichi Murayama , Shunji Aono
IPC分类号： C07D211/46 , C07D213/30 , C07D213/75 , C07D213/55
CPC分类号： C07D213/30 , C07D211/46 , C07D213/75
摘要： Bisphenoxy carboxylic acid derivatives useful as an antiarteriosclerosis agent with good absorbability and low toxicity, which are novel compounds represented by the general formula, ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atoms or lower alkyl groups and A preresents ##STR2## (wherein in case R.sub.3 is a hydrogen atom, R.sub.4 represents an amino-lower-alkyl group, an N-lower-alkylaminoalkyl group, a heterocyclic group, or a heterocyclic group-substituted alkyl group; or R.sub.3 and R.sub.4 may join through an intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent) or ##STR3## (wherein R.sub.5 represents a hydrogen atom, a hydroxyalkyl group or a derivative thereof, and R.sub.6 represents a hydroxyalkyl group or a heterocyclic group; or R.sub.5 and R.sub.6 may join to form a cyclic group, or may join through another intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent).
摘要翻译：作为具有良好吸收性和低毒性的抗动脉硬化剂的双苯氧基羧酸衍生物，它们是由通式表示的新化合物，其中R 1和R 2表示氢原子或低级烷基，并且A表示（其中，在R 3为氢原子的情况下，R 4表示氨基 - 低级烷基，N-低级烷基氨基烷基，杂环基或杂环基取代的烷基;或者，R 3和R 4可以通过中间杂原子原子形成杂环基，如果所述杂原子是氮原子，则该氮原子可以具有作为取代基的低级烷基）或者其中R5表示氢原子，羟烷基或其衍生物，和 R6表示羟基烷基或杂环基;或者R5和R6可以连接形成环状基团，或者可以通过另一个中间杂原子连接形成杂环基，如果所述杂原子是氮原子，该氮原子可以具有低级烷基作为取代基）。

7. 发明授权

US3970694A Cycloalkyl phenoxy carboxylic acid derivatives 失效
标题翻译：环烷基苯氧基羧酸衍生物
公开(公告)号：US3970694A
公开(公告)日：1976-07-20
申请号：US484063
申请日：1974-06-28
申请人： Masayoshi Minai , Yoshio Suzuki , Noritaka Hamma , Eiichi Murayama , Shunji Aono
发明人： Masayoshi Minai , Yoshio Suzuki , Noritaka Hamma , Eiichi Murayama , Shunji Aono
IPC分类号： A61K31/19 , A61K31/215 , A61K31/22 , A61P3/06 , A61P9/10 , C07C51/00 , C07C59/125 , C07C59/68 , C07C59/70 , C07C67/00 , C07C69/712 , C07C63/33
CPC分类号： C07C59/70 , C07C59/68 , C07C69/712 , Y10S514/824
摘要： Novel compounds having the formula, ##SPC1##Wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen or a C.sub.1 -C.sub.4 alkyl; n is an integer of 4-6; and Y is hydrogen or a group of the formula ##EQU1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above. These compounds are produced, for example, by reacting a bisphenolic compound of the formula, ##SPC2##With chloroform and a ketone compound of the formula,R.sub.1 -- CO -- R.sub.2in the presence of an alkali. Alternatively, they are produced by reacting the bisphenolic compound with .alpha.-halogeno- or .alpha.-hydroxycarboxylic acid derivative of the formula, ##EQU2## wherein R.sub.1, R.sub.2, and R.sub.3 are as defined above, and X is a halogen or hydroxyl. The novel compounds are anti-atherosclerosis agents useful for lowering elevated levels of cholesterol or lipids.
摘要翻译：具有式WHEREIN R1，R2和R3的新型化合物各自独立地为氢或C1-C4烷基; n为4-6的整数; 并且Y是氢或式R1R2 ANGLE -C-COOR3的基团，其中R1，R2和R3如上定义。

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