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1. 发明授权

KR870000370B1 PROCESSES FOR THE PRODUCTION OF (D1)-16-PHENOXY-AND 16-SUBSTITUTED PHENOXY-9-KETO PROSTATRIENOIC ACID DERIVATIVES 失效
公开(公告)号：KR870000370B1
公开(公告)日：1987-03-06
申请号：KR820003548
申请日：1982-08-06
申请人： SYNTEX INC
发明人： VAN HORN ALBERT R , GARAY GABRIEL , EDWARDS JOHN A
IPC分类号： C07C405/00 , C07C177/00
摘要： (Dl)-16-phenoxy and 16-substd. phenoxy-9-keto-prostatrienoic acid derivs. of formula (I) were prepd. by hydrolysis of 9-keto11alpha, 15alphs-bis-t-butyldimethylsilyloxy-16-phenoxy-17,18,19, 20- tetranorprosta-4,5,13-trans-trienoic acid methyl ester in the org. or in org. acids e.g. acetic, monochloroacetic, propionic acid or its mixt. for 10-24 hr and 0-35≦̸C. R is C1-4 lower-alkyl; X is H, o-,m- or p-halo(F, Cl or Br), o-, m- or p-methyl, o-,m- or p-methoxy. (I) are useful for sedatives and treatment of asthma.

2. 发明专利

JPS5513282A *D1**166PHENOXYYAND 166SUBSTITUTED PHENOXYY99KETOOPROSTATRIENIC ACID DERIVATIVE AND ITS MANUFACTURE 失效
公开(公告)号：JPS5513282A
公开(公告)日：1980-01-30
申请号：JP8511679
申请日：1979-07-06
申请人： SYNTEX INC
发明人： HORN ALBERT R VAN , GARAY GABRIEL , EDWARDS JOHN A
IPC分类号： A61K31/23 , A61K31/557 , A61K31/5575 , A61P1/04 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00

3. 发明授权

US3929824A 5(6)-Benzene ring substituted benzimidazole-2-carbamate derivatives having anthelmintic activity 失效
标题翻译： 5（6）具有驱虫活性的苯并环取代的苯并咪唑-2-氨基甲酸酯衍生物
公开(公告)号：US3929824A
公开(公告)日：1975-12-30
申请号：US52686174
申请日：1974-11-25
申请人： SYNTEX INC
发明人： BEARD COLIN C , EDWARDS JOHN A , FRIED JOHN H
IPC分类号： C07C335/38 , C07D235/32
CPC分类号： C07D235/32 , C07C335/38
摘要： R7 is lower alkyl having 1 to 4 carbon atoms or aryl, and n is 1-4; R2 is lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or aralkyl or aryl; R5 is lower alkenyl, lower alkynyl, or aralkyl; and the R1 substitution is at the 5(6)-position. These compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.

WHERE R is a lower alkyl group having 1 to 4 carbon atoms; R1 is SOR2, -SO2R2, -SCN, -SR5, -OR5 or M''(CH2)nMR7 where M and M'' are independently

This application describes further species embraced by the following generic formula:
摘要翻译：本申请描述了以下通用公式所包含的其他物种：

4. 发明授权

US3897441A Certain thiazole-carboxamides and acylamino-thiazoles 失效
标题翻译：某些噻唑 - 甲酰胺和酰氨基 - 噻唑
公开(公告)号：US3897441A
公开(公告)日：1975-07-29
申请号：US45117974
申请日：1974-03-14
申请人： SYNTEX INC
发明人： EDWARDS JOHN A
IPC分类号： A61K31/425 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/54 , C07D277/56 , C07D277/58 , C07D417/12 , C07D91/32 , C07D91/34
CPC分类号： A61K31/425 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40 , C07D277/46 , C07D277/48 , C07D277/54 , C07D277/56 , C07D277/58 , C07D417/12
摘要： 1-Amino-3-(4- or 5-substituted thiazol-2-oxy)-2-propanol and/or substituted amino derivatives thereof; 3-(4- or 5-substituted thiazol-2-oxy)-1,2-epoxypropane and 5-(4- or 5-substituted thiazol-2-oxymethylene)-oxazolidine and/or N- and/or 2-substituted oxazolidine derivatives thereof, and methods of making such compounds. The compounds are characterized by an aminocarbonyl or carbonylamino type substituent at the 5- or 4-position on the thiazole ring. The above 1-amino-3-(4- or 5-substituted thiazol2-oxy)-2-propanol and derivatives exhibit cardiovascular activity and are useful in the treatment of abnormal heart conditions in mammals. The 3-(4- or 5-substituted thiazol-2-oxy)-1,2epoxypropanes are useful as intermediates for the aforementioned cardiovascular agents. The 5-(4- or 5-substituted thiazol-2oxymethylene)-oxazolidine and derivatives are intermediates for the aforementioned cardiovascular agents and further exhibit cardiovascular activity and thus are useful in the treatment of abnormal heart conditions in mammals. The 1-amino-3-(4- or 5substituted thiazol-2-oxy)-2-propanol and derivatives can be prepared by base or acid hydrolysis of the corresponding 5-(4- or 5-aminocarbonylthiazol-2-oxymethylene)-oxazolidine or derivative; or by treatment of the corresponding 3-(4- or 5-substituted thiazol-2-oxy)-2,3-epoxypropane or derivative with the desired amine or amine derivative.
摘要翻译： 1-氨基-3-（4-或5-取代的噻唑-2-氧）-2-丙醇和/或其取代的氨基衍生物; 3-（4-或5-取代的噻唑-2-氧）-1,2-环氧丙烷和5-（4-或5-取代的硫杂-2-甲醛） - 恶唑烷和/或N-和/或2 - 取代的恶唑烷衍生物，以及制备这些化合物的方法。该化合物的特征在于噻唑环上5-或4-位上的氨基羰基或羰基氨基取代基。上述1-氨基-3-（4-或5-取代的噻唑-2-氧基）-2-丙醇及其衍生物具有心血管活性，可用于治疗哺乳动物异常心脏病。 3-（4-或5-取代的噻唑-2-氧）-1,2-环氧丙烷可用作上述心血管药物的中间体。 5-（4-或5-取代的噻唑-2-甲醛）恶唑烷及其衍生物是上述心血管药物的中间体，并且进一步显示心血管活性，因此可用于治疗哺乳动物的异常心脏病。 1-氨基-3-（4-或5-取代的噻唑-2-氧基）-2-丙醇及其衍生物可以通过相应的5-（4-或5-氨基羰基噻唑-2-甲醛） - 恶唑烷或其衍生物; 或通过用所需的胺或胺衍生物处理相应的3-（4-或5-取代的噻唑-2-氧）-2,3-环氧丙烷或衍生物。

5. 发明授权

US3929821A 5 (6)-Benzene ring substituted benzimidazole-2-carbamate derivatives 失效
标题翻译： 5（6） - 苯环取代的苯并咪唑-2-氨基甲酸酯衍生物
公开(公告)号：US3929821A
公开(公告)日：1975-12-30
申请号：US41796373
申请日：1973-11-21
申请人： SYNTEX INC
发明人： BEARD COLIN C , EDWARDS JOHN A , FRIED JOHN H
IPC分类号： A01N47/18 , A61K31/415 , A61K31/4184 , A61P31/04 , A61P31/10 , A61P33/00 , A61P33/10 , C07C335/38 , C07D235/32 , C07D235/02
CPC分类号： C07C335/38 , C07D235/32
摘要： R7 is lower alkyl having 1 to 4 carbon atoms or aryl, and n is 1-4; R2 is lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or aralkyl or aryl; and R5 is lower alkenyl, lower alkynyl, or aralkyl. The R1 substitution is at the 5(6)-position. The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.

WHERE R is a lower alkyl group having 1 to 4 carbon atoms; R1 is -SOR2, -SO2R2, -SCN, -SR5, -OR5 or M'' (CH2)nMR7 where M and M'' are independently

Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula:
摘要翻译：由下式表示的苯环取代的苯并咪唑-2-氨基甲酸酯衍生物：

6. 发明授权

US3929823A 5(6)-Benzene ring substituted benzimidazole-2-carbamate derivatives having anthelmintic activity 失效
公开(公告)号：US3929823A
公开(公告)日：1975-12-30
申请号：US51813074
申请日：1974-10-25
申请人： SYNTEX INC
发明人： BEARD COLIN C , EDWARDS JOHN A , FRIED JOHN H
IPC分类号： A23K1/16 , C07C335/38 , C07D235/32
CPC分类号： C07D235/32 , C07C335/38
摘要： Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula:

WHERE R is a lower alkyl having one to 4 carbon atoms; M is O or S; and R1 is an alkyl group having 1 to 6 carbon atoms and is substituted with one or more halo or cyano radicals. The R1Msubstitution is at the 5(6)-position. The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.

7. 发明授权

US3929822A 1,5(6)-Disubstituted benzizimidazole-2-carbamate derivatives having anthelmintic activity 失效
标题翻译： 1,5（6）具有驱虫活性的二取代的苯并咪唑-2-氨基甲酸酯衍生物
公开(公告)号：US3929822A
公开(公告)日：1975-12-30
申请号：US47386574
申请日：1974-05-28
申请人： SYNTEX INC
发明人： BEARD COLIN C , EDWARDS JOHN A , FRIED JOHN H
IPC分类号： C07C335/38 , C07D235/32
CPC分类号： C07C335/38 , C07D235/32
摘要： WHERE R is lower alkyl having 1 to 4 carbon atoms; R1 is -SOR2, -SR5, -OR5 or M''(CH2)nMR7; R2 is lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or aralkyl or aryl; R5 is lower alkenyl, lower alkynyl or aralkyl; R7 is lower alkyl having 1 to 4 carbon atoms or aryl; M and M'' are independently N IS 1-4; AND R8 is phenyl, benzyl, phenethyl, or lower alkyl having 1 to 12 carbon atoms optionally substituted with a -COOR group where R is lower alkyl having 1 to 4 carbon atoms; The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.

This application relates to 1,5(6)-disubstituted benzimidazole2-carbamate derivatives represented by the following formula:
摘要翻译：本申请涉及由下式表示的1,5（6） - 二取代的苯并咪唑-2-氨基甲酸酯衍生物：

8. 发明授权

US3897442A Thiazole cardiovascular agents 失效
标题翻译：噻唑心血管药
公开(公告)号：US3897442A
公开(公告)日：1975-07-29
申请号：US45119574
申请日：1974-03-14
申请人： SYNTEX INC
发明人： EDWARDS JOHN A
IPC分类号： C07D277/20 , C07D277/34 , C07D277/56 , C07D417/12 , C07F1/02 , C07D91/32
CPC分类号： C07F1/02 , C07D277/34 , C07D277/56
摘要： 1-( Beta -(Aminocarbonylphenoxyl)-ethylamino)-3-(thiazol-2-oxy)2-propanol and/or substituted amino derivatives thereof, and methods of making such compounds. The above compounds and their salts exhibit cardiovascular activity and are useful in the treatment of abnormal heart conditions in mammals. The compounds and derivatives can be prepared by treating 3-(thiazol-2-oxy)1,2-epoxypropane with the desired substituted amine.

9. 发明授权

US3896139A Process for preparing 3-(4-or-5-azidocarbonylthiazol-2-oxy)-propanediol-1,2-acetonides 失效
标题翻译：制备3-（4-还原-5-叠氮基硼烷-2-氧）丙酰基-1,2-乙酸酯的方法
公开(公告)号：US3896139A
公开(公告)日：1975-07-22
申请号：US45119474
申请日：1974-03-14
申请人： SYNTEX INC
发明人： BERKOZ BELIG M , EDWARDS JOHN A , FRIED JOHN H
IPC分类号： C07D277/20 , C07D277/34 , C07D277/56 , C07D417/12 , C07F1/02 , C07D91/32
CPC分类号： C07F1/02 , C07D277/34 , C07D277/56
摘要： Processes for preparing 3-(4- or 5-substituted thiazol-2-oxy)propanediol 1,2-acetonides. The processes are characterized by the steps of treating the desired lithium salt of 3-(4- or 5carboxy-thiazol-2-oxy)-propanediol 1,2-acetonide with an alkyl chloroformate to yield the corresponding 4''-or 5''alkylcarbonyldioxycarbonyl derivative which is then reacted with an alkali metal azide to yield the corresponding 3-(4- or 5azidocarbonylthiazol-2-oxy)-propanediol 1,2-acetonide. The azidocarbonyl derivative can be readily rearranged to the isocyanato derivative which is an intermediate for cardiovascular agents useful for the treatment of mammals.
摘要翻译： 1- [β-（氨基羰基苯氧基） - 乙基氨基] -3-（噻唑-2-氧基）-2-丙醇和/或其取代的氨基衍生物，以及制备这些化合物的方法。上述化合物及其盐具有心血管活性，可用于治疗哺乳动物异常心脏病。化合物和衍生物可以通过用所需的取代胺处理3-（噻唑-2-氧）-1,2-环氧丙烷来制备。

10. 发明专利

DK157753C 未知
公开(公告)号：DK157753C
公开(公告)日：1990-07-09
申请号：DK288879
申请日：1979-07-09
申请人： SYNTEX INC
发明人： HORN ALBERT R VAN , GARAY GABRIEL , EDWARDS JOHN A
IPC分类号： A61K31/23 , A61K31/557 , A61K31/5575 , A61P1/04 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00
摘要： Novel 16-phenoxy and 16-(o, m or p)-substituted phenoxy derivatives of (dl)-9-keto-11 alpha ,15 alpha -dihydroxy-17,18,19,20-tetranorprosta-4,5,13-trans-trienoic acid, the pharmaceutically acceptable, non-toxic lower alkyl esters and salts thereof and processes for the production of such compounds. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals where prostaglandins are indicated. They are particularly useful as inhibitors of gastric acid secretion; and as agents for the control of asthmatic attack, because of their bronchodilating activity.

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