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1. 发明申请

WO2005084295A3 FUSED HETEROTRICYCLIC COMPOUNDS AS INHIBITORS OF 17B-HYDROXYSTEROID DEHYDROGENASE 3 审中-公开
标题翻译：作为17B-羟基脱氢酶3的抑制剂的熔融异构化合物
公开(公告)号：WO2005084295A3
公开(公告)日：2009-03-26
申请号：PCT/US2005006548
申请日：2005-02-28
申请人： SQUIBB BRISTOL MYERS CO , GAVAI ASHVINIKUMAR V , NORRIS DEREK J , HAN WEN-CHING , VITE GREGORY D , FINK BRIAN E , TOKARSKI JOHN S
发明人： GAVAI ASHVINIKUMAR V , NORRIS DEREK J , HAN WEN-CHING , VITE GREGORY D , FINK BRIAN E , TOKARSKI JOHN S
IPC分类号： A61P35/00 , A61K31/44 , A61K31/4745 , A61K31/505 , A61K31/535 , C07D267/00 , C07D281/00 , C07D487/00 , C07D487/14
CPC分类号： C07D471/04 , C07D487/04
摘要： Fused heterotricyclic compounds, methods of using such compounds in the treatment of hormone sensitive diseases such as prostate cancer, and pharmaceutical compositions containing such compounds.
摘要翻译：融合的异三环化合物，使用这些化合物治疗激素敏感性疾病如前列腺癌的方法和含有这些化合物的药物组合物。

2. 发明申请

WO2005084296A2 FUSED TRICYCLIC COMPOUNDS AS INHIBITORS OF 17BETA-HYDROXYSTEROID DEHYDROGERNASE 3 审中-公开
标题翻译：作为17BETA-羟基脱氢酶脱氢酶3的抑制剂的熔融三氯化合物
公开(公告)号：WO2005084296A2
公开(公告)日：2005-09-15
申请号：PCT/US2005006549
申请日：2005-02-28
申请人： SQUIBB BRISTOL MYERS CO , FINK BRIAN E , GAVAI ASHVINIKUMAR V , VITE GREGORY D , HAN WEN-CHING , MISRA RAJ N , XIAO HAI-YUN , NORRIS DEREK J , TOKARSKI JOHN S
发明人： FINK BRIAN E , GAVAI ASHVINIKUMAR V , VITE GREGORY D , HAN WEN-CHING , MISRA RAJ N , XIAO HAI-YUN , NORRIS DEREK J , TOKARSKI JOHN S
IPC分类号： A61K31/33 , C07D225/04
CPC分类号： C07D225/02 , C07D401/04 , C07D401/12 , C07D413/04 , C07D413/12 , C07D417/04 , C07D491/04
摘要： Fused tricyclic compounds, methods of using such compounds in the treatment of hormone sensitive diseases such as prostate cancer, and pharmaceutical compositions containing such compounds.
摘要翻译：融合的三环化合物，使用这些化合物治疗激素敏感性疾病如前列腺癌的方法和含有这些化合物的药物组合物。

3. 发明申请

WO2004054514A3 C-6 MODIFIED INDAZOLYLPYRROLOTRIAZINES 审中-公开
标题翻译： C-6改性的吲唑啉酮
公开(公告)号：WO2004054514A3
公开(公告)日：2004-10-07
申请号：PCT/US0339542
申请日：2003-12-12
申请人： SQUIBB BRISTOL MYERS CO , VITE GREGORY D , GAVAI ASHVINIKUMAR V , FINK BRIAN E , MASTALERZ HAROLD , KADOW JOHN F
发明人： VITE GREGORY D , GAVAI ASHVINIKUMAR V , FINK BRIAN E , MASTALERZ HAROLD , KADOW JOHN F
IPC分类号： A61K20060101 , A61K31/53 , A61P13/08 , A61P19/02 , A61P29/00 , A61P37/00 , C07D20060101 , C07D487/02 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐。式I化合物抑制生长因子受体如HER1，HER2和HER4的酪氨酸激酶活性，从而使其成为抗增殖剂。式I化合物还可用于治疗与通过生长因子受体操作的信号转导途径相关的其它疾病。

4. 发明申请

WO2007140297A2 AZIRIDINYL-EPOTHILONE COMPOUNDS 审中-公开
标题翻译：亚胺基 - 丙烯酸酯化合物
公开(公告)号：WO2007140297A2
公开(公告)日：2007-12-06
申请号：PCT/US2007069736
申请日：2007-05-25
申请人： SQUIBB BRISTOL MYERS CO , VITE GREGORY D , LEE FRANCIS Y , LEAMON CHRISTOPHER P , VLAHOV IONTCHO R
发明人： VITE GREGORY D , LEE FRANCIS Y , LEAMON CHRISTOPHER P , VLAHOV IONTCHO R
IPC分类号： C07D491/04 , A61K31/396 , A61K31/427 , A61P35/00
CPC分类号： C07D491/04 , A61K47/551 , A61K47/65
摘要： The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having Formula (X), wherein K is -O-, -S-, or -NR7-; A is -(CR 8 R 9 )-(CH 2 )m-Z- wherein Z is - (CHR 10 )-, -C(=O)-, -C(=O)-C(=O)-, -OC(=O>, -N(R 11 )O=O)-, -SO 2 -, or - N(R 11 )SO 2 -; B 1 is hydroxyl or cyano and R 1 is hydrogen or B 1 and R 1 are taken together to form a double bond; R 2 , R 3 , and R 5 are, independently, hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; or R 2 and R 3 may be taken together with the carbon to which they are attached to form an optionally substituted cycloalkyl; R 4 is hydrogen, alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, or substituted aryl; R 6 is hydrogen, alkyl or substituted alkyl; R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are independently hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, or substituted heteroaryl; and R 13 is aryl, substituted aryl, heteroaryl or substituted heteroaryl.
摘要翻译：本发明涉及本文进一步描述的吖丙啶基埃坡霉素化合物和/或其药学上可接受的盐和/或溶剂化物，其具有式（X），其中K是-O - ， - S - 或-NR 7 - ; A是 - （CH 2 CH 2）mZ-，其中Z是 - （CHR 10 N / -C（= O） - ， - OC（= O）， - N（R 11）O = O） - ，-SO 2 - 或 - N（R 11）SO 2 - ; B 1是羟基或氰基，R 1是氢或B 1和R 1一起形成双重键 R 2，R 3和R 5独立地是氢，烷基，取代的烷基，芳基或取代的芳基; 或R 2和R 3可以与它们所连接的碳一起形成任选取代的环烷基; R 4是氢，烷基，烯基，取代的烷基，取代的烯基，芳基或取代的芳基; R 6是氢，烷基或取代的烷基; R 7，R 8，R 9，R 10，R 11和R 11和 R 12独立地是氢，烷基，取代的烷基，环烷基，取代的环烷基，芳基，取代的芳基，杂环烷基，取代的杂环烷基，杂芳基或取代的杂芳基; R 13是芳基，取代的芳基，杂芳基或取代的杂芳基。

5. 发明申请

WO0173103A2 PREPARATION OF EPOTHILONE INTERMEDIATES 审中-公开
标题翻译： EPOTHILONE中间体的制备
公开(公告)号：WO0173103A2
公开(公告)日：2001-10-04
申请号：PCT/US0109620
申请日：2001-03-23
申请人： SQUIBB BRISTOL MYERS CO , VITE GREGORY D , KIM SOONG HOON , HOEEFLE GERHARD
发明人： VITE GREGORY D , KIM SOONG-HOON , HOEEFLE GERHARD
IPC分类号： C07D277/30 , C12P17/14 , C07D277/00
CPC分类号： C12P17/14 , C07D277/30
摘要： The present invention relates to a process for the preparation of intermediates useful in the synthesis of epothilone analogs by initially enzymatically degrading certain epothilone compounds to form ring-open structures containing a carboxyl group which is esterified, the hydroxyl groups on the moiety protected and the resulting compound oxidized by, e.g. ozone, to form a first intermediate. The first intermediate can be reacted with a thiphenylphosphine adduct to yield a compound containing an ester group at position 1 which is subsequently hydrolyzed to form a second intermediate.
摘要翻译：本发明涉及用于制备用于合成埃坡霉素类似物的中间体的方法，该方法通过最初酶促降解某些埃坡霉素化合物以形成含羧基的开环结构，所述羧基被酯化，保护部分上的羟基被保护，化合物被氧化，例如臭氧，形成第一中间体。可以将第一中间体与二苯基膦加合物反应，得到在1位含有酯基的化合物，随后将其水解形成第二中间体。

6. 发明申请

WO9902514A3 EPOTHILONE DERIVATIVES 审中-公开
标题翻译： EPOTHILONE衍生物
公开(公告)号：WO9902514A3
公开(公告)日：2001-05-10
申请号：PCT/US9812550
申请日：1998-06-16
申请人： SQUIBB BRISTOL MYERS CO
发明人： VITE GREGORY D , BORZILLERI ROBERT M , KIM SOONG-HOON , JOHNSON JAMES A
IPC分类号： C07D491/044 , A61K31/335 , A61K31/395 , A61K31/427 , A61P19/00 , A61P35/00 , A61P43/00 , C07D225/00 , C07D273/00 , C07D277/26 , C07D313/00 , C07D417/06 , C07D417/08 , C07D491/04 , C07D493/04 , C07D498/04
CPC分类号： C07D491/044 , C07D417/06 , C07D491/04 , C07D493/04
摘要： The present invention relates to compounds of formula (V).
摘要翻译：本发明涉及式（Ⅴ）化合物。

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