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1. 发明授权

US06613911B2 Process for preparing arylacetylaminothiazoles 有权
标题翻译：制备芳基乙酰氨基噻唑的方法
公开(公告)号：US06613911B2
公开(公告)日：2003-09-02
申请号：US10067723
申请日：2002-02-05
申请人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Joseph E. Sundeen , Rulin Zhao
发明人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Joseph E. Sundeen , Rulin Zhao
IPC分类号： C07D41712
CPC分类号： C07D417/12 , A61K31/427 , A61K31/454 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-arylacetylaminothiazole compounds of formula I: or a pharmnaceutically acceptable salt thereof, wherein: R1, R2, R4, R5, R6, R8, R9, R12 and R13 are each independently hydrogen, alkyl, aryl or heteroaryl; R3, R7, R10 and R11 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; and X is CH or N, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention also concerns a new process for the preparation of formylarylacetates and formylarylacetic acids.
摘要翻译：本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-芳基乙酰氨基噻唑化合物的新的，有效的方法：或其药物上可接受的盐，其中：R1，R2，R4，R5，R6，R8， R9，R12和R13各自独立地为氢，烷基，芳基或杂芳基; R3，R7，R10和R11各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; 而X是CH或N，它们是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。本发明还涉及制备甲酰芳基乙酸酯和甲酰芳基乙酸的新方法。

2. 发明授权

US6107305A Use of pyrazolo [3,4-b] pyridine as cyclin dependent kinase inhibitors 有权
标题翻译：吡唑并[3,4-b]吡啶作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US6107305A
公开(公告)日：2000-08-22
申请号：US209575
申请日：1998-12-11
申请人： Raj N. Misra , S. David Kimball , David B. Rawlins , Kevin R. Webster , Isia Bursuker
发明人： Raj N. Misra , S. David Kimball , David B. Rawlins , Kevin R. Webster , Isia Bursuker
IPC分类号： A61K31/437 , A61P1/00 , A61P19/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/10 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/06 , A61P43/00 , C07D471/04 , A61K31/435
CPC分类号： C07D471/04 , A61K31/437
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof for use as inhibitors of cyclin dependent kinases, wherein:X is O, S(O).sub.m ;Y is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl;R.sub.1 is hydrogen or lower alkyl;R.sub.2 is alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, --O-alkyl, --O-aryl, --NR.sub.4 R.sub.5 ;R.sub.3 is hydrogen or lower alkyl;R.sub.4 is hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, --O-alkyl, --O-aryl;R.sub.5 is hydrogen, alkyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, cycloalkyl, alkylcycloalkyl, heterocycloalkyl, alkylheterocycloalkyl, --O-alkyl, --O-aryl; andm is 0, 1 or 2.The compounds of formula I are protein kinase inhibitors and are useful in the treatment and prevention of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, viral diseases and fungal diseases.
摘要翻译：用作细胞周期依赖性激酶抑制剂的式及其可药用盐的化合物，其中：X为O，S（O）m; Y是烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基，环烷基烷基，杂环烷基，杂环烷基烷基; R1是氢或低级烷基; R2是烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基，环烷基烷基，杂环烷基，杂环烷基烷基，-O-烷基，-O-芳基，-NR4R5; R3是氢或低级烷基; R4是氢，烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基，环烷基烷基，杂环烷基，杂环烷基烷基，-O-烷基，-O-芳基。 R5是氢，烷基，芳基，烷基芳基，杂芳基，烷基杂芳基，环烷基，烷基环烷基，杂环烷基，烷基杂环烷基，-O-烷基，-O-芳基; 并且m为0,1或2.式I化合物为蛋白激酶抑制剂，可用于治疗和预防增殖性疾病，例如癌症，炎症和关节炎。它们也可用于治疗神经变性疾病如阿尔茨海默病，心血管疾病，病毒性疾病和真菌性疾病。

3. 发明授权

US06610724B2 3-Aminopyrazole inhibitors of cyclin dependent kinases 有权
标题翻译：细胞周期蛋白依赖性激酶的3-氨基吡唑抑制剂
公开(公告)号：US06610724B2
公开(公告)日：2003-08-26
申请号：US10219844
申请日：2002-08-15
申请人： Mark E. Salvati , S. David Kimball
发明人： Mark E. Salvati , S. David Kimball
IPC分类号： A61K31415
CPC分类号： C07D413/06
摘要： The present invention describes compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, and cardiovascular disease.
摘要翻译：本发明描述了式I化合物及其药学上可接受的盐。式I化合物是蛋白激酶抑制剂，可用于治疗增殖性疾病，例如癌症，炎症和关节炎。它们也可用于治疗阿尔茨海默病和心血管疾病。

4. 发明授权

US06482842B2 3-aminopyrazole inhibitors of cyclin dependent kinases 有权
标题翻译：细胞周期蛋白依赖性激酶的3-氨基吡唑抑制剂
公开(公告)号：US06482842B2
公开(公告)日：2002-11-19
申请号：US09777273
申请日：2001-02-06
申请人： Mark E. Salvati , S. David Kimball
发明人： Mark E. Salvati , S. David Kimball
IPC分类号： A61K314155
CPC分类号： C07D413/06
摘要： The present invention describes compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, and cardiovascular disease.
摘要翻译：本发明描述了式I化合物及其药学上可接受的盐。式I化合物是蛋白激酶抑制剂，可用于治疗增殖性疾病，例如癌症，炎症和关节炎。它们也可用于治疗阿尔茨海默病和心血管疾病。

5. 发明授权

US06414156B2 Process for preparing azacycloalkanoylaminothiazoles 有权
标题翻译：制备氮杂环烷酰氨基噻唑的方法
公开(公告)号：US06414156B2
公开(公告)日：2002-07-02
申请号：US09746060
申请日：2000-12-22
申请人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xiao , Rulin Zhao
发明人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xiao , Rulin Zhao
IPC分类号： C07D41714
CPC分类号： C07D417/12 , A61K31/427 , A61K31/454 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.
摘要翻译：本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R是烷基，芳基或杂芳基; R 1，R 2，R 3， R4和R5各自独立地为氢，烷基，芳基或杂芳基; R6和R7各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; R8为氢，烷基，芳基，杂芳基，CONR9R10，COR11或COOR12; R9，R10，R11和R12各自独立地为氢，烷基或芳基; m等于0至5; 和等于0至5，这是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。本发明还涉及新的关键中间体化合物，式III'的季铵盐和式IX的2-恶唑基烷基衍生物。

6. 发明授权

US06407124B1 Carbon substituted aminothiazole inhibitors of cyclin dependent kinases 有权
标题翻译：细胞周期蛋白依赖性激酶的碳取代的氨基噻唑抑制剂
公开(公告)号：US06407124B1
公开(公告)日：2002-06-18
申请号：US09329616
申请日：1999-06-10
申请人： David B. Rawlins , S. David Kimball , Kyoung S. Kim , Raj N. Misra , Kevin R. Webster
发明人： David B. Rawlins , S. David Kimball , Kyoung S. Kim , Raj N. Misra , Kevin R. Webster
IPC分类号： A61K314439
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/46 , C07D417/04 , C07D417/06 , C07D417/14
摘要： Compounds of the formula and pharmaceutically acceptable salts thereof are provided.
摘要翻译：提供式及其药用盐的化合物

7. 发明授权

US06534531B2 Methods for preventing and treating alopecia induced by chemotherapy or radiotherapy 有权
标题翻译：预防和治疗化疗或放疗引起的脱发的方法
公开(公告)号：US06534531B2
公开(公告)日：2003-03-18
申请号：US09842595
申请日：2001-04-26
申请人： S. David Kimball , Kevin R. Webster , David K. Bol
发明人： S. David Kimball , Kevin R. Webster , David K. Bol
IPC分类号： A61K31425
CPC分类号： C07D417/12 , A61K31/427 , A61K31/454 , C07D417/14
摘要： The invention provides a method for preventing or treating alopecia induced by chemotherapy or radiotherapy by administering to a mammalian specie in need thereof a therapeutically effective amount of a compound of formula I or II or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了一种预防或治疗由化学疗法或放射治疗引起的脱发的方法，其通过向有需要的哺乳动物物种施用治疗有效量的式I或II化合物或其药学上可接受的盐。

8. 发明授权

US06897321B2 Process for preparing azacycloalkanoylaminothiazoles (LD 137e) 有权
标题翻译：制备氮杂环烷酰氨基噻唑的方法（LD 137e）
公开(公告)号：US06897321B2
公开(公告)日：2005-05-24
申请号：US10639272
申请日：2003-08-12
申请人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xia , Rulin Zhao
发明人： Bang-Chi Chen , Kyoung S. Kim , S. David Kimball , Raj N. Misra , Mark E. Salvati , Joseph E. Sundeen , Hai-Yun Xia , Rulin Zhao
IPC分类号： C07D487/18 , A61K20060101 , A61K31/427 , A61K31/454 , A61P20060101 , C07D20060101 , C07D263/32 , C07D417/12 , C07D417/14 , C07D521/00 , C07D263/30
CPC分类号： C07D417/12 , A61K31/427 , A61K31/454 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要： The present invention relates to new, efficient processes for the preparation of 5-(-2-oxyazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or a pharmaceutically acceptable salt thereof, wherein: R is alkyl, aryl or heteroaryl; R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl; R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy; R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9, R10, COR11 or COOR12; R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl; m equals 0 to 5; and n equals 0 to 5, which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III′ and a 2-oxazolylalkyl derivative of formula IX.
摘要翻译：本发明涉及制备式I的5-（ - 2-氧杂唑基烷硫基）-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R是烷基，芳基或杂芳基; R 1，R 2，R 3，R 4和R 5均为各自独立地为氢，烷基，芳基或杂芳基; R 6和R 7各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; R 8是氢，烷基，芳基，杂芳基，CONR 9，R 10，COR 11或COOR， SUP> 12 R 9，R 10，R 11和R 12各自独立地为氢，烷基或芳基; m等于0到5; 且n等于0至5，这是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。本发明还涉及新的关键中间体化合物，式III'的季铵盐和式IX的2-恶唑基烷基衍生物。

9. 发明授权

US06262096B1 Aminothiazole inhibitors of cyclin dependent kinases 有权
标题翻译：细胞周期蛋白依赖性激酶的氨基噻唑抑制剂
公开(公告)号：US06262096B1
公开(公告)日：2001-07-17
申请号：US09464511
申请日：1999-12-15
申请人： Kyoung S. Kim , S. David Kimball , Zhen-wei Cai , David B. Rawlins , Raj N. Misra , Michael A. Poss , Kevin R. Webster , John T. Hunt , Wen-Ching Han
发明人： Kyoung S. Kim , S. David Kimball , Zhen-wei Cai , David B. Rawlins , Raj N. Misra , Michael A. Poss , Kevin R. Webster , John T. Hunt , Wen-Ching Han
IPC分类号： A61K31425
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D417/12 , C07D417/14
摘要： Compounds of the formula and pharmaceutically acceptable salts thereof. R1 and R2 are independently hydrogen, fluorine or alkyl; R3 is aryl or heteroaryl R4 is alkyl, cycloalkyl, aryl, cycloalkylalkyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl; m is an integer of 0 to 2; and n is an integer of 1 to 3. The compounds of formula I are protein kinase inhibitors and are useful in the treatment and prevention of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, cardiovascular diseases, viral diseases and fungal diseases.
摘要翻译： R 1和R 2独立地是氢，氟或烷基; R 3是芳基或杂芳基R 4是烷基，环烷基，芳基，环烷基烷基，芳基烷基，杂芳基，杂芳基烷基，杂环烷基，杂环烷基烷基; m是整数0 到2; andn是1至3的整数。式I化合物是蛋白激酶抑制剂，可用于治疗和预防增殖性疾病，例如癌症，炎症和关节炎。它们也可用于治疗神经变性疾病如阿尔茨海默病，心血管疾病，病毒性疾病和真菌性疾病。

10. 发明授权

US06214852B1 N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases 有权
标题翻译：细胞周期蛋白依赖性激酶N- [5 - [[[5-烷基-2-恶唑基]甲基]硫基] -2-噻唑基] - 甲酰胺抑制剂
公开(公告)号：US06214852B1
公开(公告)日：2001-04-10
申请号：US09616629
申请日：2000-07-26
申请人： Kyoung S. Kim , S. David Kimball
发明人： Kyoung S. Kim , S. David Kimball
IPC分类号： A61K31425
CPC分类号： C07D417/12 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要： The present invention describes compounds of formula I and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. The formula I compounds are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example, cancer, inflammation and arthritis. They may also be useful in the treatment of Alzheimer's disease, chemotherapy-induced alopecia, and cardiovascular disease.
摘要翻译：本发明描述了式I化合物及其对映体，非对映异构体及其药学上可接受的盐。式I化合物是蛋白激酶抑制剂，可用于治疗增殖性疾病，例如癌症，炎症和关节炎。它们也可用于治疗阿尔茨海默病，化学疗法诱发的脱发和心血管疾病。

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