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

US06291694B1 Process and intermediates useful to produce vitamin D analogs 失效
标题翻译：用于生产维生素D类似物的方法和中间体
公开(公告)号：US06291694B1
公开(公告)日：2001-09-18
申请号：US09633670
申请日：2000-08-07
申请人： Andrzej Robert Daniewski , Marek Michal Kabat , Masami Okabe , Roumen Nikolaev Radinov
发明人： Andrzej Robert Daniewski , Marek Michal Kabat , Masami Okabe , Roumen Nikolaev Radinov
IPC分类号： C07C40100
CPC分类号： C07C69/732 , C07D303/32 , C07D303/40 , C07F7/1804 , C07F7/1892
摘要： A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.
摘要翻译：用于实现以下反应的立体特异性方法：导致式2的化合物在碳1和碳3上与式1化合物具有相同的立体化学性质。因此，如果碳3在化合物中为R-构型式3的化合物中的碳原子为R构型。在上述方法中，R 1是可以是直链或支链的C 1 -C 6烷基。该方法在钯催化剂存在下使用pKa小于约9的氟化醇来进行。式1的化合物以及该方法中的新型中间体可用于制备维生素D类似物。

2. 发明授权

US06294688B1 Process useful to produce vitamin D analogs 失效
标题翻译：生产维生素D类似物的方法
公开(公告)号：US06294688B1
公开(公告)日：2001-09-25
申请号：US09633672
申请日：2000-08-07
申请人： Andrzej Robert Daniewski , Marek Michal Kabat , Masami Okabe , Roumen Nikolaev Radinov
发明人： Andrzej Robert Daniewski , Marek Michal Kabat , Masami Okabe , Roumen Nikolaev Radinov
IPC分类号： C07C6726
CPC分类号： C07C69/732 , C07D303/32 , C07D303/40 , C07F7/1804 , C07F7/1892
摘要： A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.
摘要翻译：用于实现以下反应的立体特异性方法：导致式2的化合物在碳1和碳3上与式1化合物具有相同的立体化学性质。因此，如果碳3在化合物中为R-构型式3的化合物中的碳原子为R构型。在上述方法中，R 1是可以是直链或支链的C 1 -C 6烷基。该方法在钯催化剂存在下使用pKa小于约9的氟化醇来进行。式1的化合物以及该方法中的新型中间体可用于制备维生素D类似物。

3. 发明授权

US06353123B1 Process and intermediates useful to produce vitamin D analogs 失效
标题翻译：用于生产维生素D类似物的方法和中间体
公开(公告)号：US06353123B1
公开(公告)日：2002-03-05
申请号：US09835593
申请日：2001-04-16
申请人： Andrzej Robert Daniewski , Marek Michal Kabat , Masami Okabe , Roumen Nikolaev Radinov
发明人： Andrzej Robert Daniewski , Marek Michal Kabat , Masami Okabe , Roumen Nikolaev Radinov
IPC分类号： C07D30300
CPC分类号： C07C69/732 , C07D303/32 , C07D303/40 , C07F7/1804 , C07F7/1892
摘要： A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.
摘要翻译：用于实现以下反应的立体特异性方法：导致式2的化合物在碳1和碳3上与式1化合物具有相同的立体化学性质。因此，如果碳3在化合物中为R-构型式3的化合物中的碳原子为R构型。在上述方法中，R 1是可以是直链或支链的C 1 -C 6烷基。该方法在钯催化剂存在下使用pKa小于约9的氟化醇来进行。式1的化合物以及该方法中的新型中间体可用于制备维生素D类似物。

4. 发明申请

US20070244129A1 Process for the preparation of an isopropanol solvate of a glucokinase activator 审中-公开
标题翻译：制备葡萄糖激酶活化剂的异丙醇溶剂合物的方法
公开(公告)号：US20070244129A1
公开(公告)日：2007-10-18
申请号：US11786269
申请日：2007-04-11
申请人： Andrzej Robert Daniewski , Wen Liu , Roumen Nikolaev Radinov
发明人： Andrzej Robert Daniewski , Wen Liu , Roumen Nikolaev Radinov
IPC分类号： A61K31/4965 , C07D241/20
CPC分类号： C07C315/04 , C07C2601/08 , C07D241/20 , C07D319/08 , Y02P20/55 , C07C317/44
摘要： Provided is a process for the preparation of 2(R)-(3-Chloro-4-methanesulfonyl-phenyl)-3-((R)-3-oxo-cyclopentyl)-N-pyrazin-2-yl-propionamide and its isopropanol solvate as a glucokinase activator which increases insulin secretion in the treatment of, for example, type II diabetes.
摘要翻译：提供制备2（R） - （3-氯-4-甲磺酰基 - 苯基）-3 - （（R）-3-氧代 - 环戊基）-N-吡嗪-2-基 - 丙酰胺及其制备方法异丙醇溶剂合物作为葡萄糖激酶活化剂，其在例如II型糖尿病的治疗中增加胰岛素分泌。

5. 发明授权

US06255501B1 Process for preparing antiosteoporotic agents 失效
标题翻译：制备抗骨质疏松剂的方法
公开(公告)号：US06255501B1
公开(公告)日：2001-07-03
申请号：US09548471
申请日：2000-04-13
申请人： Andrzej Robert Daniewski , Roumen Nikolaev Radinov
发明人： Andrzej Robert Daniewski , Roumen Nikolaev Radinov
IPC分类号： C07D30300
CPC分类号： C07F7/1892 , C07C401/00 , C07D303/40 , C07F7/1804 , Y02P20/55
摘要： Methods for preparing antiosteoportic agents are disclosed. Compounds useful in the methods are also disclosed.
摘要翻译：公开了制备抗结构剂的方法。也公开了可用于该方法的化合物。

6. 发明授权

US07084270B2 Pyrimido compounds having antiproliferative activity 失效
标题翻译：具有抗增殖活性的嘧啶化合物
公开(公告)号：US07084270B2
公开(公告)日：2006-08-01
申请号：US10623972
申请日：2003-07-21
申请人： Yi Chen , Andrzej Robert Daniewski , William Harris , Marek Michal Kabat , Emily Aijun Liu , Jin-Jun Liu , Kin-Chun Luk , Christophe Michoud
发明人： Yi Chen , Andrzej Robert Daniewski , William Harris , Marek Michal Kabat , Emily Aijun Liu , Jin-Jun Liu , Kin-Chun Luk , Christophe Michoud
IPC分类号： C07D487/04 , C07D25/00 , A01N43/90 , A61K31/519
CPC分类号： C07D487/04
摘要： Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR an FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.
摘要翻译：公开了新的嘧啶化合物，其是KDR和FGFR激酶的选择性抑制剂，并且对LCK具有选择性。这些化合物及其药学上可接受的盐是可用于治疗或控制实体瘤，特别是乳腺癌，结肠癌，肺癌和前列腺肿瘤的抗增殖剂。还公开了含有这些化合物的药物组合物和治疗癌症的方法。

7. 发明授权

US06284928B1 Process for preparing intermediates useful in the synthesis of vitamin D compounds 失效
标题翻译：制备可用于合成维生素D化合物的中间体的方法
公开(公告)号：US06284928B1
公开(公告)日：2001-09-04
申请号：US09501359
申请日：2000-02-10
申请人： Andrzej Robert Daniewski
发明人： Andrzej Robert Daniewski
IPC分类号： C07C4562
CPC分类号： C07C45/62 , C07C45/63 , C07C49/443 , C07C49/477
摘要： The invention relates to an improved process for preparing [(3aR,4S,7aS)4-bromooctahydro-7a-methyl-1H-indene-1,5-dione]. (S)-(+)-2,3,7,7a-tetrahydro-7a-methyl-1H-indene-1,5(6H)-dione is reduced by reaction with diisobutylaluminum hydride and hexamethylphosphoric triaminde in the presence of a catalyst of the formula R—Cu, wherein R is and R1, R2 and R3 are each, independently, selected from the group consisting of C1-7 alkyl, phenyl, phenyl substituted by at least one C1-4 alkyl group, benzyl, or benzyl substituted by at at least one C1-4 alkyl group to form a reductate. The reductate is then treated with a bromine-containing electrophile to yield (3aR,4S,7aS)4-bromooctahydro-7a-methyl-1H-indene-1,5-dione.
摘要翻译：本发明涉及制备[（3aR，4S，7aS）4-溴八氢-7a-甲基-1H-茚-1,5-二酮]的改进方法。（S） - （+） - 2,3,7,7a-四氢-7a-甲基-1H-茚-1H（6H） - 二酮在催化剂存在下与二异丁基氢化铝和六甲基磷酸三的式R-Cu，其中R是和R 1，R 2和R 3各自独立地选自C 1-7烷基，苯基，被至少一个C 1-4烷基取代的苯基，苄基或苄基取代的在至少一个C 1-4烷基上形成还原物。然后用含溴亲电子试剂处理还原物，得到（3aR，4S，7aS）4-溴八氢-7a-甲基-1H-茚-1,5-二酮。

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