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1. 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。

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

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。

4. 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。

5. 发明授权

US07112676B2 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：US07112676B2
公开(公告)日：2006-09-26
申请号：US10689235
申请日：2003-10-20
申请人： Apostolos Dermatakis , Marek Michal Kabat , Kin-Chun Luk , Pamela Loreen Rossman , Sung-Sau So
发明人： Apostolos Dermatakis , Marek Michal Kabat , Kin-Chun Luk , Pamela Loreen Rossman , Sung-Sau So
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , G01N2800/52
摘要： Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and 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：公开了作为KDR和FGFR激酶的选择性抑制剂的新的嘧啶化合物，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。

6. 发明授权

US06603030B1 Process for producing phosphineoxide vitamin D precursors 失效
标题翻译：生产氧化膦维生素D前体的方法
公开(公告)号：US06603030B1
公开(公告)日：2003-08-05
申请号：US09537209
申请日：2000-03-29
申请人： Marek Michal Kabat
发明人： Marek Michal Kabat
IPC分类号： C07C40100
CPC分类号： C07F9/532 , Y02P20/55
摘要： A process for producing a compound of the formula: where Ph is phenyl, X1 and X2 are both hydrogen or X1 and X2 taken together are CH2, R1 is a protecting group, R2 is fluorine, hydrogen, or OR3, where R3 is a protecting group, and the squiggly line represents a bond that results in the adjacent double bond being in either the E or Z configuration, involves: (a) chlorinating a compound of the formula: where X1, X2, R1, R2, and the squiggly line are as above, using triphosgene in the presence of an organic base to obtain the compound of the formula: where X1, X2, R1, R2, and the squiggly line are as above; and (b) reacting the compound of formula 3 with a salt of diphenyl phosphine oxide to obtain the compound of formula 1. Each of the above steps (a) and (b) are individually useful.
摘要翻译：制备下式化合物的方法：其中Ph为苯基，X1和X2均为氢或X1和X2一起为CH2，R1为保护基，R2为氟，氢或OR3，其中R3为保护基并且波纹线表示导致相邻双键处于E或Z构型的键，其包括：（a）氯化下式的化合物：其中X1，X2，R1，R2和波峰线如上所述，在有机碱的存在下使用三光气，得到下式的化合物：其中X1，X2，R1，R2和波纹如上所述; 和（b）使式3的化合物与二苯基氧化膦的盐反应，得到式1的化合物。上述步骤（a）和（b）中的每一个可单独使用。

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