专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US09102698B2 Process for the synthesis of IB-MECA 有权
标题翻译：合成IB-MECA的方法
公开(公告)号：US09102698B2
公开(公告)日：2015-08-11
申请号：US12450094
申请日：2008-03-13
申请人： Paul Bruzinski , Xuejun Liu , Cameron Gibb , Pedro E. HErnandez-Abad
发明人： Paul Bruzinski , Xuejun Liu , Cameron Gibb , Pedro E. HErnandez-Abad
IPC分类号： C07H19/16 , C07H1/00
CPC分类号： C07H19/16 , C07H1/00 , Y02P20/55
摘要： The present disclosure provides a method for the synthesis of IB-MECA. More specifically, the present disclosure provides a simple and high yield method for Good Manufacturing Production (GMP) of IB-MECA. The method involves the reaction of 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine; reaction of the diol protected 6-halopurine with a nucleophile (e.g. methylamine); substitution of the halogen group with iodobenzylamine and removal of the diol protecting group.
摘要翻译：本公开提供了用于合成IB-MECA的方法。更具体地，本公开提供了IB-MECA的良好制造生产（GMP）的简单且高产率的方法。该方法涉及6-卤代嘌呤-9-核糖苷与二醇保护试剂的反应; 用二醇保护试剂氧化二醇保护的6-卤嘌呤-9-核糖苷中的伯醇; 二醇中的伯醇的氧化被保护的6-卤代嘌呤; 二醇保护的6-卤代嘌呤与亲核试剂（如甲胺）的反应; 用碘苄胺取代卤素基团并除去二醇保护基团。

2. 发明授权

US08334266B2 Process for and intermediates in the preparation of canfosfamide and its salts 有权
标题翻译：用于制备卡非司酮及其盐的方法和中间体
公开(公告)号：US08334266B2
公开(公告)日：2012-12-18
申请号：US13429065
申请日：2012-03-23
申请人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
发明人： William A. Boulanger , Steven J. Collier , Stephen A. Eastham , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Hans J. Kjaersgaard , Harold Meckler , Robert E. Polomski , Steven R. Schow , Pavel E. Zhichkin
IPC分类号： A61K38/07 , C07K38/06
CPC分类号： C07K5/0205 , A61K38/00 , C07F9/2408 , C07F9/2458 , C07K5/0215 , C07K5/0606 , C07K5/06191
摘要： A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.
摘要翻译：一种在制备头孢噻吩及其盐的过程和中间体。一些中间体具有抗癌活性。

3. 发明授权

US5817807A Antiviral compounds 失效
标题翻译：抗病毒化合物
公开(公告)号：US5817807A
公开(公告)日：1998-10-06
申请号：US659500
申请日：1996-06-06
申请人： Gary J. Bridger , Sreenivasan Padmanabhan , Renato T. Skerlj , Pedro E. Hernandez-Abad , Milind P. Sant
发明人： Gary J. Bridger , Sreenivasan Padmanabhan , Renato T. Skerlj , Pedro E. Hernandez-Abad , Milind P. Sant
IPC分类号： C07D487/08 , A61K31/395 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/495 , A61K31/505 , A61P31/12 , C07D255/02 , C07D257/02 , C07D259/00 , C07D401/12 , C07D403/12 , C07D409/12 , A61K31/33 , C07D257/00
CPC分类号： C07D401/12 , C07D255/02 , C07D257/02 , C07D259/00 , C07D403/12 , C07D409/12
摘要： Macrocyclic compounds having 1, 4, 8, 11-tetraazacyclotetradecanyl group, show good selectivity against HIV-1 and HIV-2, in in vitro tests are disclosed.
摘要翻译：在体外试验中公开了具有1,4,8,11-四氮杂环十四烷基的大环化合物对HIV-1和HIV-2具有良好的选择性。

4. 发明授权

US4759880A Alkanoarachidonic acids 失效
标题翻译：藻糖酸
公开(公告)号：US4759880A
公开(公告)日：1988-07-26
申请号：US655196
申请日：1984-09-27
申请人： Kyriacos C. Nicolaou , Nicos A. Petasis , Wen-Sen Li , Tamara Ladduwahetty , Jared L. Randall , Stephen E. Webber , Pedro E. Hernandez
发明人： Kyriacos C. Nicolaou , Nicos A. Petasis , Wen-Sen Li , Tamara Ladduwahetty , Jared L. Randall , Stephen E. Webber , Pedro E. Hernandez
IPC分类号： C07C47/225 , C07C47/45 , C07C57/26 , C07C57/52 , C07C61/35 , C07C62/16 , C11C1/00 , A61K31/045 , C07C33/05 , C07C47/21
CPC分类号： C07C57/26 , C07C47/225 , C07C47/45 , C07C57/52 , C07C61/35 , C07C62/16
摘要： A series of alkanoarachidonic acids have been prepared as modulators of the arachidonic acid cascade to increase the production of biologically desirable compounds and minimize the production of biologically undesirable compounds. Examples of desirable compounds in this respect comprise postaglandins and thromboxanes whereas undesirable compounds comprise the mono- and polyhydroxyarachidonic acids and leukotrienes. The alkanoarachidonic acids and their intermediates are of the general formula: ##STR1## and at least one of X, Y, and Z is lower alkano and is hydrogen when not lower alkano; the esters and salts of the acids are also prepared. The acids, esters and salts may be used as anti-anaphylaxis or anti-thrombosis agents.
摘要翻译：已经制备了一系列链烷二糖酸作为花生四烯酸级联的调节剂，以增加生物需要的化合物的产生并使生物学不需要的化合物的产生最小化。所需化合物在这方面的实例包括Postaglandin和血栓素，而不希望的化合物包括单羟基和多羟基花生四烯酸和白三烯。链烷二酸及其中间体具有以下通式：其中R 1 =低级烷基（低级烷基）（低级亚烷基）OH（低级亚烷基）CHO CHO，其中R 2 = COO（低级烷基）（低级烷基）亚烷基）OH（低级亚烷基）CHO CHO其中R3 = COO（低级烷基）（低级亚烷基）OH（低级亚烷基）CHO CHO，X，Y和Z中的至少一个为低级烷基，当不为低级烷还制备了酸的酯和盐。酸，酯和盐可用作抗过敏反应或抗血栓形成剂。

5. 发明授权

US5792444A Labeled chemotactic peptides to image focal sites of infection or inflammation 失效
标题翻译：标记趋化肽以影像感染或炎症的焦点
公开(公告)号：US5792444A
公开(公告)日：1998-08-11
申请号：US140000
申请日：1993-10-22
申请人： Alan J. Fischman , Howard F. Solomon , Claudia K. Derian , Gary J. Bridger , John D. Higgins, III , Scott K. Larsen , Pedro E. Hernandez , Robert H. Rubin , H. William Strauss , Anthony J. Fuccello , Daniel J. Kroon
发明人： Alan J. Fischman , Howard F. Solomon , Claudia K. Derian , Gary J. Bridger , John D. Higgins, III , Scott K. Larsen , Pedro E. Hernandez , Robert H. Rubin , H. William Strauss , Anthony J. Fuccello , Daniel J. Kroon
IPC分类号： A61K38/00 , A61K38/06 , A61K49/00 , A61K51/00 , A61K51/08 , A61P29/00 , A61P31/00 , C07K20060101 , C07K5/083 , C07K5/103 , C07K7/06
CPC分类号： C07K7/06 , A61K51/08 , A61K51/088 , C07K5/081 , C07K5/101 , C07K5/1013 , A61K2123/00 , A61K38/00 , Y02P20/55
摘要： The invention relates to a method of detecting a site of infection or inflammation, and a method for treating such infection or inflammation, in an individual by administering to the individual a diagnostically or therapeutically effective amount of detectably labeled, therapeutic, or therapeutically-conjugated, chemotactic peptide that accumulates substantially at the infected or inflamed site, said chemotactic peptide having the general structure X--Y--Leu--Phe--�Z!.sub.n --W wherein: X is an amino protecting group, Y is an amino acid residue, Z is a spacer sequence, n is 0 or 1, and W is a labeling or attachment substituent.
摘要翻译：本发明涉及通过向个体施用诊断或治疗有效量的可检测标记的，治疗性的或治疗上缀合的，可检测地标记的，治疗性的或治疗上缀合的，在个体中检测感染或炎症部位的方法和治疗这种感染或炎症的方法，所述趋化肽基本上在感染或发炎部位积累，所述趋化肽具有通式X-Y-Leu-Phe- [Z] n -W其中：X为氨基保护基，Y为氨基酸残基，Z为间隔序列，n为0或1，W为标记或连接取代基。

6. 发明申请

US20100087636A1 PROCESS FOR THE SYNTHESIS OF IB-MECA 有权
标题翻译：合成IB-MECA的方法
公开(公告)号：US20100087636A1
公开(公告)日：2010-04-08
申请号：US12450094
申请日：2008-03-13
申请人： Paul Bruzinski , Xuejun Liu , Cameron Gibb , Pedro E. Hernandez-Abad
发明人： Paul Bruzinski , Xuejun Liu , Cameron Gibb , Pedro E. Hernandez-Abad
IPC分类号： C07H19/16 , C07H1/00
CPC分类号： C07H19/16 , C07H1/00 , Y02P20/55
摘要： The present disclosure provides a method for the synthesis of IB-MECA. More specifically, the present disclosure provides a simple and high yield method for Good Manufacturing Production (GMP) of IB-MECA. The method involves the reaction of 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine; reaction of the diol protected 6-halopurine with a nucleophile (e.g. methylamine); substitution of the halogen group with iodobenzylamine and removal of the diol protecting group.
摘要翻译：本公开提供了用于合成IB-MECA的方法。更具体地，本公开提供了IB-MECA的良好制造生产（GMP）的简单且高产率的方法。该方法涉及6-卤代嘌呤-9-核糖苷与二醇保护试剂的反应; 用二醇保护试剂氧化二醇保护的6-卤嘌呤-9-核糖苷中的伯醇; 二醇中的伯醇的氧化被保护的6-卤代嘌呤; 二醇保护的6-卤代嘌呤与亲核试剂（如甲胺）的反应; 用碘苄胺取代卤素基团并除去二醇保护基团。

7. 发明授权

US08198247B2 Process for and intermediates in the preparation of canfosfamide and its salts 失效
公开(公告)号：US08198247B2
公开(公告)日：2012-06-12
申请号：US11018391
申请日：2004-12-21
申请人： William A. Boulanger , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Harold Meckler , Steven R. Schow , Pavel E. Zhichkin
发明人： William A. Boulanger , Dennis L. Edie , Ronan Y. Guevel , Pedro E. Hernandez Abad , R. Jason Herr , Harold Meckler , Steven R. Schow , Pavel E. Zhichkin
IPC分类号： A61K38/14
CPC分类号： C07K5/0205 , A61K38/00 , C07F9/2408 , C07F9/2458 , C07K5/0215 , C07K5/0606 , C07K5/06191
摘要： A process for and intermediates in the preparation of canfosfamide and its salts. Some of the intermediates have anticancer activity.

8. 发明授权

US06239277B1 Process for preparing piperazine-substituted aliphatic carboxylates 失效
标题翻译：制备哌嗪取代的脂肪族羧酸盐的方法
公开(公告)号：US06239277B1
公开(公告)日：2001-05-29
申请号：US09421514
申请日：1999-10-20
申请人： Pedro E. Hernandez , David John Fairfax , Erik T. Michalson
发明人： Pedro E. Hernandez , David John Fairfax , Erik T. Michalson
IPC分类号： C07D29510
CPC分类号： C07D295/088
摘要： A process is disclosed for the preparation of a piperazine-substituted aliphatic carboxylate having the formula where m and n are individually an integer of from 1 to 6, R and R′ are the same or different and are hydrogen, C1 to C6 alkyl or aryl or heteroaryl that is unsubstituted or is substituted with at least one substituent that is halo, C1 to C6 alkyl or C1 to C6 alkoxy and R″ is C3 to C12 branched alkyl or an organic or inorganic cation. The process comprises treating a solution comprising a compound of the formula wherein m, R and R′ are as defined above and an aliphatic ester of the formula X—(CH2)n—O—CH2—CO(O)R″ where X is a leaving group and n and R″ are as defined above, with an effective amount of a base for a time and at a temperature sufficient to form a piperazine-substituted aliphatic carboxylate. Hydrolysis of the carboxylate with acid produces a piperazine-substituted aliphatic carboxylic acid or the acid salt thereof.
摘要翻译：公开了制备具有式m和n分别为1至6的整数的哌嗪取代的脂族羧酸酯的方法，R和R'相同或不同，为氢，C 1至C 6烷基或芳基或未被取代或被至少一个为卤素，C 1至C 6烷基或C 1至C 6烷氧基的取代基取代的杂芳基，R“为C 3至C 12支链烷基或有机或无机阳离子。该方法包括处理包含糠醛的化合物的溶液，R和R'如上所定义，并且所述式的脂族酯是离去基团，n和R“如上定义，并且有效量碱处理一段时间并在足以形成哌嗪取代的脂族羧酸酯的温度下进行。羧酸酯与酸的水解产生哌嗪取代的脂族羧酸或其酸式盐。

9. 发明授权

US5350837A Complexes with .sup.99m Tc suitable for radiolabelling monoclonal antibodies or other macro molecules 失效
标题翻译：与99mTc的复合物适用于放射性标记单克隆抗体或其他大分子
公开(公告)号：US5350837A
公开(公告)日：1994-09-27
申请号：US55312
申请日：1993-05-03
申请人： Gary J. Bridger , Pedro E. Hernandez , John D. Higgins, III , Scott K. Larsen
发明人： Gary J. Bridger , Pedro E. Hernandez , John D. Higgins, III , Scott K. Larsen
IPC分类号： G01N33/534 , A61K51/04 , A61K51/10 , C07C227/00 , C07C229/08 , C07C229/12 , C07C229/76 , C07F13/00
CPC分类号： C07F13/005 , A61K51/0476 , A61K51/0478 , A61K51/1093 , C07C229/12 , A61K2123/00
摘要： The ligand L, (R.sup.3)(R.sup.4)(R.sup.5)C--N(R)--C(R.sup.1)(R.sup.2)--(CH.sub.2).sub.n --COOH L where R is hydrogen, hydroxy, alkyl, hydroxyalkyl, or alkylcarboxy, or R and R.sup.1 together may form a mono-, di-, tri-, or tetra-methylene radical, or R and R.sup.3 together may form a mono-, di-, tri-, or tetra-methylene radical, and R.sup.1 and R.sub.2 may be the same or different and are selected from hydrogen, hydroxy, alkyl, hydroxyalkyl, carboxy, alkylcarboxy, alkylamine, alkylthiol, aryl or R.sup.1 and R.sup.2 together may form a tetra- or penta-methylene radical, and R.sup.3 and R.sup.4 and R.sup.5 may be the same or different and are selected from hydrogen, hydroxy, alkyl, hydroxyalkyl, carboxy, alkylcarboxy, provided that at least one of R.sup.3, R.sup.4 and R.sup.5 is hydroxyalkyl, and n is equal to 0, 1 or 2, for example tricine, form useful complexes with .sup.99m Tc, for radiolabelling macromolecules such as monoclonal antibodies.
摘要翻译：配体L，（R3）（R4）（R5）CN（R）-C（R1）（R2） - （CH2）n-COOHL其中R是氢，羟基，烷基，羟基烷基或烷基羧基，或R和 R1一起可以形成单 - ，二 - ，三 - 或四 - 亚甲基，或者R和R 3一起可以形成单 - ，二 - ，三 - 或四 - 亚甲基，R1和R2可以是相同或不同，选自氢，羟基，烷基，羟基烷基，羧基，烷基羧基，烷基胺，烷基硫醇，芳基或R 1和R 2一起可以形成四或五亚甲基，R3和R4和R5可以相同或不同的，并且选自氢，羟基，烷基，羟基烷基，羧基，烷基羧基，条件是R 3，R 4和R 5中的至少一个是羟烷基，n等于0,1或2，例如三羟甲基，形成有用的络合物具有99mTc，用于放射性标记大分子如单克隆抗体。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式