公开(公告)号：US3940403A

公开(公告)日：1976-02-24

申请号：US360065

申请日：1973-05-14

申请人： Ryozo Maeda ,  Katsumi Hirose

发明人： Ryozo Maeda ,  Katsumi Hirose

IPC分类号： C07D213/64 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/455 ,  A61P25/04 ,  A61P29/00 ,  C07D213/28 ,  C07D213/55 ,  C07D213/63 ,  C07D213/643 ,  C07D213/65 ,  C07D213/68 ,  C07D213/69 ,  C07D213/70 ,  C07D213/78 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D213/84 ,  C07D213/85 ,  C07D213/89 ,  C07D215/22 ,  C07D215/227 ,  C07D215/36 ,  C07D215/60 ,  C07D217/24

CPC分类号： C07D213/643 ,  C07D213/63 ,  C07D213/70 ,  C07D213/78 ,  C07D213/81 ,  C07D213/82 ,  C07D213/84 ,  C07D213/85 ,  C07D213/89 ,  C07D215/227 ,  C07D215/36 ,  C07D215/60 ,  C07D217/24 ,  Y10S514/916

摘要： Substituted acetic acid derivatives represented by the formula: ##SPC1##Wherein X, X', X", Y, Y' and Y" each represents a hydrogen atom, an alkyl group of 1 to 8 carbon atoms, an alkoxy group of 1 to 8 carbon atoms, a hydroxy group, an acyl group, an acylamino group, an acyloxy group, an amino group, a cyano group, a nitro group, an alkoxycarbonyl group of 2 to 9 carbon atoms, an alkoxycarbonylalkyl group of 3 to 10 carbon atoms, an alkoxycarbonylamino group of 2 to 9 carbon atoms, a trifluoromethyl group, a halogen atom, a carboxy group, or a carbamoyl group, two of X, X' and X", or two of Y, Y' and Y" are optionally combined to form an alicyclic ring of 5 to 7 carbon atoms or a benzene ring, A represents an oxygen atom or a sulfur atom, R and R.sub.1 each represents a hydrogen atom or a lower alkyl group of 1 to 4 carbon atoms and Q represents the optional presence of an oxygen atom, or their alkali metal or alkali earth metal salts, being useful as anti-inflammatory, anti-rheumatic, analgesic or anti-pyretic agents, are prepared essentially by the Arndt-Eistert reaction.

公开(公告)号：US4077968A

公开(公告)日：1978-03-07

申请号：US730965

申请日：1976-10-08

申请人： Ryozo Maeda ,  Katsumi Hirose

发明人： Ryozo Maeda ,  Katsumi Hirose

IPC分类号： C07D277/32 ,  C07D277/34 ,  C07D277/36 ,  C07D277/42 ,  C07D277/56 ,  A61K31/38

CPC分类号： C07D277/34 ,  C07D277/32 ,  C07D277/36 ,  C07D277/42 ,  C07D277/56 ,  Y10S514/825 ,  Y10S514/87

摘要： Thiazole derivatives represented by the general formula: ##STR1## wherein A is oxygen, sulfur, imino, or NR.sub.3, wherein R.sub.3 is C.sub.1-5 alkyl, C.sub.2-5 alkenyl, C.sub.3-5 alkynyl, C.sub.3-6 cycloalkyl-C.sub.1-3 alkyl or C.sub.7-8 aralkyl; R.sub.1 is hydrogen, C.sub.1-5 alkyl, C.sub.2-5 alkenyl, C.sub.3-5 alkynyl, C.sub.3-6 cycloalkyl-C.sub.1-3 alkyl or C.sub.7-8 aralkyl; R.sub.2 is hydroxy, C.sub.1-5 alkoxy or OM, wherein M is alkali metal, or one equivalent of alkaline earth metal, cupric or aluminum cation; n is an integer of 0 or 1; X.sub.1 and X.sub.2 are independently hydrogen or C.sub.1-5 alkyl; Y.sub.1 and Y.sub.2 are independently hydrogen, halogen, C.sub.1-5 alkyl, C.sub.1-5 alkoxy or trifluoromethyl; and the group ##STR2## is linked to one of the meta or para positions of the benzene ring A, n is not 0 when A is imino and --CH.sub.2 --COR.sub.2 does not substitute the thiazole ring when A is imino, being useful as anti-inflammatory, anti-rheumatic, analgesic or anti-lipemia agents.

摘要翻译： 由以下通式表示的噻唑衍生物：其中A是氧，硫，亚氨基或NR 3，其中R 3是C 1-5烷基，C 2-5烯基，C 3-5炔基，C 3-6环烷基-C 1-3烷基 或C7-8芳烷基; R 1是氢，C 1-5烷基，C 2-5烯基，C 3-5炔基，C 3-6环烷基-C 1-3烷基或C 7-8芳烷基; R2是羟基，C1-5烷氧基或OM，其中M是碱金属，或1当量碱土金属，铜或铝阳离子; n为0或1的整数; X 1和X 2独立地是氢或C 1-5烷基; Y1和Y2独立地是氢，卤素，C1-5烷基，C1-5烷氧基或三氟甲基; 并且组与苯环A的间位或对位相连，当A为亚氨基时，n不为0，当A为亚氨基时，-CH2-COR2不取代噻唑环，可用作抗 炎性，抗风湿，镇痛或抗血脂代谢。

公开(公告)号：US4025528A

公开(公告)日：1977-05-24

申请号：US596244

申请日：1975-07-16

申请人： Ryozo Maeda ,  Katsumi Hirose

发明人： Ryozo Maeda ,  Katsumi Hirose

IPC分类号： C07D277/32 ,  C07D277/34 ,  C07D277/36 ,  C07D277/42 ,  C07D277/56 ,  C07D277/54

CPC分类号： C07D277/34 ,  C07D277/32 ,  C07D277/36 ,  C07D277/42 ,  C07D277/56

摘要： Thiazole derivatives represented by the general formula: ##STR1## wherein A is oxygen, sulfur, imino, or NR.sub.3, wherein R.sub.3 is C.sub.1.sub.-5 alkyl, C.sub.2.sub.-5 alkenyl, C.sub.3.sub.-5 alkynyl, C.sub.3.sub.-6 cycloalkyl-C.sub.1.sub.-3 alkyl or C.sub.7.sub.-8 aralkyl; R.sub.1 is hydrogen, C.sub.1.sub.-5 alkyl, C.sub.2.sub.-5 alkenyl, C.sub.3.sub.-5 alkynyl, C.sub.3.sub.-6 cycloalkyl-C.sub.1.sub.-3 alkyl or C.sub.7.sub.- 8 aralkyl; R.sub.2 is hydroxy, C.sub.1.sub.-5 alkoxy or OM, wherein M is alkali metal, or one equivalent of alkaline earth metal, cupric or aluminum cation; n is an integer of 0 or 1; X.sub.1 and X.sub.2 are independently hydrogen or C.sub.1.sub.-5 alkyl; Y.sub.1 and Y.sub.2 are independently hydrogen, halogen, C.sub.1.sub.-5 alkyl, C.sub.1.sub.-5 alkoxy or trifluoromethyl; and the group ##STR2## is linked to one of the meta or para positions of the benzene ring A, n is not 0 when A is imino and --CH.sub.2 --COR.sub.2 does not substitute the thiazole ring when A is imino, being useful as anti-inflammatory, anti-rheumatic, analgesic or anti-lipemia agents.

摘要翻译： 由以下通式表示的噻唑衍生物：其中A是氧，硫，亚氨基或NR 3，其中R 3是C 1-5烷基，C 2-5烯基，C 3-5炔基，C 3-6环烷基-C 1-3烷基 或C7-8芳烷基; R1是氢，C1-5烷基，C2-5烯基，C3-5炔基，C3-6环烷基C1-3烷基或C7-8芳烷基; R2是羟基，C1-5烷氧基或OM，其中M是碱金属，或1当量碱土金属，铜或铝阳离子; n为0或1的整数; X 1和X 2独立地是氢或C 1-5烷基; Y1和Y2独立地为氢，卤素，C1-5烷基，C1-5烷氧基或三氟甲基; 并且组与苯环A的间位或对位相连，当A为亚氨基时，n不为0，当A为亚氨基时，-CH2-COR2不取代噻唑环，可用作抗 炎性，抗风湿，镇痛或抗血脂代谢。

公开(公告)号：US4018785A

公开(公告)日：1977-04-19

申请号：US637479

申请日：1975-12-03

申请人： Ryozo Maeda ,  Katsumi Hirose

发明人： Ryozo Maeda ,  Katsumi Hirose

IPC分类号： F23G5/14 ,  B04C9/00 ,  C07D277/42 ,  F23G5/16 ,  F23J15/00 ,  C07D277/38

CPC分类号： C07D277/42 ,  Y10S514/916

摘要： Thiazoline derivatives represented by the general formula: ##STR1## wherein X.sub.1 represents hydrogen or methyl; Y.sub.1 and Y.sub.2 each represents hydrogen, halogen, C.sub.1.sub.-3 alkyl, C.sub.1.sub.-3 alkoxy or trifluoromethyl; R.sub.1 represents hydrogen, methyl, or ethyl; R.sub.2 represents C.sub.1.sub.-3 alkyl or C.sub.3.sub.-5 alkenyl and Z represents hydrogen, carboxy or carboxy ester group and its esters and pharmaceutically acceptable salts, synthesized by quaternization and acid-elimination reaction being useful as anti-inflammatory, anti-rheumatic, analgesic and anti-pyretic agents.

摘要翻译： 由以下通式表示的噻唑啉衍生物：其中X1表示氢或甲基; Y1和Y2各自表示氢，卤素，C1-3烷基，C1-3烷氧基或三氟甲基; R1代表氢，甲基或乙基; R2表示C1-3烷基或C3-5烯基，Z表示氢，羧基或羧基酯基，其酯和药学上可接受的盐，通过季铵化和酸消除反应合成，可用作抗炎，抗风湿，止痛和抗炎 抗热解剂。

公开(公告)号：US3994908A

公开(公告)日：1976-11-30

申请号：US635253

申请日：1975-11-25

申请人： Ryozo Maeda ,  Katsumi Hirose

发明人： Ryozo Maeda ,  Katsumi Hirose

IPC分类号： C07D213/64 ,  C07D213/70 ,  C07D213/78 ,  C07D213/81 ,  C07D213/82 ,  C07D213/84 ,  C07D213/85 ,  C07D213/89 ,  C07D217/24 ,  C07D213/55

CPC分类号： C07D213/78 ,  C07D213/64 ,  C07D213/70 ,  C07D213/81 ,  C07D213/82 ,  C07D213/84 ,  C07D213/85 ,  C07D213/89 ,  C07D217/24 ,  Y10S514/916

摘要： Substituted acetic acid derivatives represented by the formula: ##SPC1##Wherein X, X', X", Y, Y' and Y" each represents a hydrogen atom, an alkyl group of 1 to 8 carbon atoms, an alkoxy group of 1 to 8 carbon atoms, a hydroxy group, an acyl group, an acylamino group, an acyloxy group, an amino group, a cyano group, a nitro group, an alkoxycarbonyl group of 2 to 9 carbon atoms, an alkoxycarbonylalkyl group of 3 to 10 carbon atoms, an alkoxycarbonylamino group of 2 to 9 carbon atoms, a trifluoromethyl group, a halogen atom, a carboxy group, or a carbamoyl group, two of X, X' and X", or two of Y, Y' and Y" are optionally combined to form an alicyclic ring of 5 to 7 carbon atoms or a benzene ring, A represents an oxygen atom or a sulfur atom, R and R.sub.1 each represents a hydrogen atom or a lower alkyl group of 1 to 4 carbon atoms and Q represents the optional presence of an oxygen atom, or their alkali metal or alkali earth metal salts, being useful as anti-inflammatory, anti-rheumatic, analgesic or anti-pyretic agents, are prepared essentially by the Arndt-Eistert reaction.

摘要翻译： 由下式表示的取代的乙酸衍生物：