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21. 发明授权

US06867208B2 Vitronectin receptor antagonists, their preparation and their use 有权
标题翻译： Vitronectin受体拮抗剂，其制备及其应用
公开(公告)号：US06867208B2
公开(公告)日：2005-03-15
申请号：US10142975
申请日：2002-05-13
申请人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Jochen Knolle , Jean-Marie Ruxer , Denis Carniato , Jean-Michel Lefrancois , Thomas Richard Gadek , Robert McDowell
发明人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Jochen Knolle , Jean-Marie Ruxer , Denis Carniato , Jean-Michel Lefrancois , Thomas Richard Gadek , Robert McDowell
IPC分类号： C07D239/00 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/33 , A61K31/395 , A61K31/415 , A61K31/4184 , A61K31/47 , A61K31/472 , A61K31/55 , A61K38/04 , A61P9/00 , A61P19/08 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C279/20 , C07C279/24 , C07C311/64 , C07C313/30 , C07C327/00 , C07D217/24 , C07D233/04 , C07D235/16 , C07D243/06 , C07D253/06 , C07D253/08 , C07D263/52 , C07D267/08 , C07D277/60 , C07D471/02 , C07D471/04 , C07D487/04 , C07K5/04 , A61K31/437
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the formula I A—B—D—E—F—G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
摘要翻译：本发明涉及式Iin的化合物，其中A，B，D，E，F和G具有专利权利要求中给出的含义，其制备和用作药物。本发明的化合物用作玻连蛋白受体拮抗剂和骨吸收抑制剂。

22. 发明授权

US6100428A Nickel promoted guanylation of amines with isothioureas and thioureas 失效
标题翻译：镍促进胺与异硫脲和硫脲的胍基化
公开(公告)号：US6100428A
公开(公告)日：2000-08-08
申请号：US412844
申请日：1999-10-06
申请人： Laxminarayan Bhat , Gunda I. Georg
发明人： Laxminarayan Bhat , Gunda I. Georg
IPC分类号： C07C277/08 , C07C279/18 , C07C279/24 , C07C311/64 , C07D295/215 , C07D295/26 , C07C279/16 , C07C271/20 , C07C303/40
CPC分类号： C07D295/215 , C07C277/08 , C07C311/64 , C07D295/26 , C07C2101/02 , C07C2101/14 , Y02P20/55
摘要： An improved method for guanylating amines is provided. Broadly, the amines are reacted with a guanylating agent in the presence of a nickel catalyst. Preferably, the nickel catalyst comprises nickel in the zero oxidation state. Suitable nickel(0) catalysts are derived from nickel-boride alloys, nickel-phosphide alloys, aluminum-nickel alloys, nickel on kieselguhr, and nickel on silica/alumina catalysts. Preferred guanylating agents are thioureas and isothioureas. In one embodiment, protecting groups are selectively attached to the guanylating agents to yield particular substituted guanidines. The preferred protecting groups are Boc groups, Cbz groups, and arylsulfonyl groups. The reactions are particularly well suited for guanylating primary and secondary amines. The methods of the invention can be carried out under ambient conditions to provide high yields of the corresponding guanidines, with the nickel catalyst being essentially completely recoverable for reuse.
摘要翻译：提供了一种改进的脒基化胺的方法。广泛地，胺与脒基化剂在镍催化剂存在下反应。优选地，镍催化剂包括处于零氧化状态的镍。合适的镍（0）催化剂衍生自镍 - 硼化物合金，镍 - 磷化物合金，铝 - 镍合金，硅藻土上的镍和二氧化硅/氧化铝催化剂上的镍。优选的脒基化剂是硫脲和异硫脲。在一个实施方案中，保护基选择性连接到脒基化剂以产生特定的取代的胍。优选的保护基是Boc基团，Cbz基团和芳基磺酰基。反应特别适用于脒基化的伯胺和仲胺。本发明的方法可以在环境条件下进行以提供高产率的相应的胍，镍催化剂基本上完全可回收再利用。

23. 发明授权

US6072075A Guanidinylation reagents 失效
公开(公告)号：US6072075A
公开(公告)日：2000-06-06
申请号：US861942
申请日：1997-05-22
申请人： Murray Goodman , Konrad Feichtinger , Todd T. Romoff
发明人： Murray Goodman , Konrad Feichtinger , Todd T. Romoff
IPC分类号： C07C279/14 , C07C279/24 , C07C311/64 , C07K1/00 , C07K1/06 , C07C277/08
CPC分类号： C07C279/14 , C07C279/24 , C07C311/64 , C07K1/006 , C07K1/064 , Y02P20/55
摘要： Trisubstituted N-protected guanidines and methods for use as guanidinylating reagents to yield N-protected guanidine derivatives.

24. 发明授权

US5013723A New thymopentin retro-inverso analogs and fragments thereof, a process of preparation of the new compounds and the intermediates obtained therein 失效
标题翻译：新的胸腺五肽逆转型类似物及其片段，新化合物及其中获得的中间体的制备方法
公开(公告)号：US5013723A
公开(公告)日：1991-05-07
申请号：US168237
申请日：1988-03-15
申请人： Alessandro Sisto , Antonio Verdini
发明人： Alessandro Sisto , Antonio Verdini
IPC分类号： A61K38/00 , A61P37/00 , C07C67/00 , C07C239/00 , C07C279/12 , C07C301/00 , C07C311/64 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/08
CPC分类号： C07K5/0212
摘要： New retro-inverso analogs of thymopentin (TP5) and of its tripeptide fragment (TP5.sup.1-3) of general formula (I) ##STR1## are described wherein R is hydrogen or an acyl radical, and R.sup.1 is --OR.sup.2 or ##STR2## wherein R.sup.2 is hydrogen or a hydrocarbyl radical, and the corresponding pharmaceutically acceptable acid- or base-addition salts.The new compounds are enzyme-resistant immunomodulatory peptides.

25. 发明授权

US4877895A Glycine and .beta. alanine derivatives as sweetening agents 失效
标题翻译：甘氨酸和β丙氨酸衍生物作为甜味剂
公开(公告)号：US4877895A
公开(公告)日：1989-10-31
申请号：US836071
申请日：1986-03-04
申请人： Claude Nofre , Jean M. Tinti , Farroudja O. Chatzopoulos
发明人： Claude Nofre , Jean M. Tinti , Farroudja O. Chatzopoulos
IPC分类号： A23L27/30 , A23L27/40 , A61K31/18 , C07C255/58 , C07C255/61 , C07C279/18 , C07C279/28 , C07C311/37 , C07C311/64 , C07C317/36
CPC分类号： C07C255/00 , A23L27/30 , C07C279/18 , C07C279/28 , C07C311/64
摘要： Sweetening agents, characterized in that they conform to the following formula: ##STR1## wherein: A is an imino (.dbd.N--), iminium (.dbd.N.sup.+
摘要翻译：其特征在于它们符合以下分子式：其中：A是亚氨基（= N-），亚胺（= N +），亚甲基（= C））基团，亚胺基团可以是由生理学上可接受的阴离子盐化; m和n的数目等于1或2; B：当n = 1时，代表H，CN，OCH3，NO2，SO2R，SOR，SO2NHR，SO2NR2，其中R是具有至多10个碳原子的烷基，环烷基或芳基; 当n = 2时，表示H，CN，OCH 3; X：表示CN，NO 2，当B为H时，CN，OCH 3; 表示CN，NO2，COCH3，CHO，Cl，CF3，F，H，当B为NO2，SO2R，SOR，SO2NHR，SO2NR2时; M是氢原子或生理上可接受的有机或无机阳离子。

26. 发明授权

US4304780A Aminoalkylthiophene derivatives as histamine H.sub.2 -antagonists 失效
标题翻译：氨基烷基噻吩衍生物作为组胺H2拮抗剂
公开(公告)号：US4304780A
公开(公告)日：1981-12-08
申请号：US157195
申请日：1980-06-06
申请人： Michael Martin-Smith , Barry Price , John Bradshaw , John W. Clitherow
发明人： Michael Martin-Smith , Barry Price , John Bradshaw , John W. Clitherow
IPC分类号： A61K31/34 , A61K31/341 , A61K31/345 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/495 , A61K31/505 , A61P1/04 , C07C67/00 , C07C209/00 , C07C209/60 , C07C211/29 , C07C217/48 , C07C261/04 , C07C275/32 , C07C301/00 , C07C303/36 , C07C303/40 , C07C311/64 , C07C313/00 , C07C323/29 , C07C323/44 , C07C323/47 , C07C323/48 , C07C325/00 , C07C335/08 , C07D209/48 , C07D213/32 , C07D295/096 , C07D307/28 , C07D307/38 , C07D307/52 , C07D333/20 , C07D405/12 , C07D409/12 , A61K31/445 , A61K31/44 , C07D409/14
CPC分类号： C07D209/48 , C07D213/32 , C07D295/096 , C07D307/52 , C07D333/20 , Y10S514/826 , Y10S514/887 , Y10S514/925 , Y10S514/926 , Y10S514/927
摘要： The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof,in which Y represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl;R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.4 represents hydrogen or lower alkyl; Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5-positions, or a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1- and 3- or 1- and 4-positions;X represents --CH.sub.2 --, --O-- or --S--;n represents zero, 1 or 2;m represents 2, 3 or 4;Alk represents a straight chain alkylene group of 1 to 3 carbon atoms;(except that n is not zero when X is oxygen and Q is a furan or thiophen ring system)q represents 2, 3 or 4 or can additionally represent zero or 1 when E is a --CH.sub.2 --group;p represents zero, 1 or 2;E represents --CH.sub.2 --, --O-- or --S--; andZ represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring which may be optionally substituted by one or more groups or Z represents ##STR3## where Q' represents any of the rings defined for Q; Alk' represents any of the groups defined for Alk; and R.sub.5 and R.sub.6, which may be the same or different, each represent any of the groups defined for R.sub.1 and R.sub.2 ;(except that p is not zero when E is oxygen and Q' or Z is a furan or thiophen ring system)The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

27. 发明授权

US2390734A Disulphanilylguanidine and process of preparing same 失效
标题翻译：二磺酰基胍及其制备方法
公开(公告)号：US2390734A
公开(公告)日：1945-12-11
申请号：US53602144
申请日：1944-05-17
申请人： AMERICAN CYANAMID CO
发明人： PIERCE ALAN E
IPC分类号： C07C311/64
CPC分类号： C07C311/64

28. 发明授权

US2359912A Sulphanilamide derivatives 失效
标题翻译：磺胺衍生物
公开(公告)号：US2359912A
公开(公告)日：1944-10-10
申请号：US47082342
申请日：1942-12-31
申请人： ICI LTD
发明人： ERNEST HAWORTH , LESLIE ROSE FRANCIS
IPC分类号： C07C311/64
CPC分类号： C07C311/64

29. 发明授权

US2301000A Sulphanilyl alkyl guanidine and process for making it 失效
标题翻译：磺酰基烷基胍及其制备方法
公开(公告)号：US2301000A
公开(公告)日：1942-11-03
申请号：US38917241
申请日：1941-04-18
申请人： AMERICAN CYANAMID CO
发明人： STANLEY WINNEK PHILIP
IPC分类号： C07C311/64
CPC分类号： C07C311/64

30. 发明授权

US2229784A P-nitrobenzene sulphonyl guanidine and process for making it 失效
标题翻译：对硝基苯磺酰胍及其制备方法
公开(公告)号：US2229784A
公开(公告)日：1941-01-28
申请号：US35749940
申请日：1940-09-19
申请人： AMERICAN CYANAMID CO
发明人： STANLEY WINNEK PHILIP
IPC分类号： C07C311/64
CPC分类号： C07C311/64

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