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1. 发明申请

WO1997030992A1 INHIBITORS OF FARNESYL PROTEIN TRANSFERASE 审中-公开
标题翻译：番茄红素转移酶抑制剂
公开(公告)号：WO1997030992A1
公开(公告)日：1997-08-28
申请号：PCT/US1997002920
申请日：1997-02-24
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BRISTOL-MYERS SQUIBB COMPANY , DING, Charles, Z. , HUNT, John, T. , KIM, Soong-Hoon , MITT, Toomis , BHIDE, Rajeev , LEFTHERIS, Katerina
IPC分类号： C07D403/06
CPC分类号： C07D243/14 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D495/04
摘要： This invention relates to compounds that inhibit farnesyl-protein transferase and ras protein farnesylation, thereby making them useful as anti-cancer agents. The compounds are also useful in the treatment of diseases, other than cancer, associated with signal transduction pathways operating through ras and those associated with proteins other than ras that are also post-translationally modified by the enzyme farnesyl protein transferase. The compounds may also act as inhibitors of other prenyl transferases, and thus be effective in the treatment of diseases associated with other prenyl modifications of proteins.
摘要翻译：本发明涉及抑制法呢基蛋白转移酶和ras蛋白法尼基化的化合物，从而使其成为抗癌剂。所述化合物还可用于治疗与通过ras操作的信号转导途径相关的疾病以及与通过法尼基蛋白转移酶翻译后修饰的ras以外的蛋白质相关的疾病。所述化合物还可用作其它异戊二烯基转移酶的抑制剂，因此可有效治疗与蛋白质的其它异戊烯基修饰相关的疾病。

2. 发明申请

WO2004004665A3 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
公开(公告)号：WO2004004665A3
公开(公告)日：2004-01-15
申请号：PCT/US2003/022149
申请日：2003-07-02
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHENG, Peter, T., W. , CHEN, Sean , DEVASTHALE, Pratik , DING, Charles, Z. , HERPIN, Timothy, F. , WU, Shung , ZHANG, Hao , WANG, Wei , YE, Xiang-Yang
发明人： CHENG, Peter, T., W. , CHEN, Sean , DEVASTHALE, Pratik , DING, Charles, Z. , HERPIN, Timothy, F. , WU, Shung , ZHANG, Hao , WANG, Wei , YE, Xiang-Yang
IPC分类号： C07D403/06
摘要： Formula, wherein Z 1 is (CH 2 ) q or C=O; Z 2 is (CH 2 ) p or C=O; D is -CH= or C=O or (CH 2 ) m where m is 0, 1, 2 or 3; n = 0, 1 or 2; p = 1 or 2; q = 0, 1 or 2; Q is C or N; A is (CH 2 ) x where x is 1 to 5, or A is (CH 2 ) x 1 , where x 1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is -(CH 2 ) x 2 -O-(CH 2 ) x 3 - where x 2 is 0 to 5 and x 3 is 0 to 5, provided that at least one of x 2 and x 3 is other than 0; B is a bond or is (CH 2 ) x 4 where x 4 is 1 to 5; X is CH or N; X 2 is C, N, O or S; X 3 is C, N, O or S; X 4 is C, N, O or S; X 5 is C, N, O or S; X 6 is C, N, O or S; provided that at least one of X 2 , X 3 , X 4 X 5 and X 6 is N; and at least one of X 2 , X 3 , X 4 X 5 and X 6 is C. R 1 is H or alkyl; R 2 is H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; R 2a , R 2b and R 2c may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; and R 3 , E, Z and Y are as defined herein.

3. 发明申请

WO2003106628A3 BENZODIAZEPINE INHIBITORS OF MITOCHONDIAL F¿1?F¿0? ATP HYDROLASE AND METHODS OF INHIBITING F¿1?F¿0? ATP HYDROLASE 审中-公开
公开(公告)号：WO2003106628A3
公开(公告)日：2003-12-24
申请号：PCT/US2003/018552
申请日：2003-06-13
申请人： BRISTOL-MYERS SQUIBB COMPANY , DING, Charles, Z. , HAMANN, Lawrence, G. , STEIN, Philip, D. , PUDZIANOWSKI, Andrew, T.
发明人： DING, Charles, Z. , HAMANN, Lawrence, G. , STEIN, Philip, D. , PUDZIANOWSKI, Andrew, T.
IPC分类号： A61K31/55
摘要： Compounds having the formula (I), are useful as inhibitors of mitochondrial F¿1?F¿0? ATP hydrolase, wherein R 1 , R 5 and R 7 are optional substituents, R¿2?, R¿3? and R¿4? are hydrogen, alkyl, or substituted alkyl, or comprise a bond to R, T or Y; Z and Y are selected from C(=O), -CO¿2?-, -SO¿2?-, -CH¿2?-, -CH¿2?C(=O)-, and -C(=O)C(=O)-, or Z may be absent; R and T are CH¿2?-, -C(=O)-, or -CH[(CH¿2?)¿p?(Q)]-, wherein Q is NR¿10?R¿11?, OR¿10? or CN and p is 0, 1 or 2; R¿6? is alkyl, alkenyl, substituted alkyl, substituted alkenyl, aryl, cycloalkyl, heterocyclo, or heteroaryl; R¿10? and R¿11? are hydrogen, alkyl, or substituted alkyl; and r and t are 0 or 1.

4. 发明申请

WO1998002436A1 THIADIOXOBENZODIAZEPINE INHIBITORS OF FARNESYL PROTEIN TRANSFERASE 审中-公开
标题翻译：番茄红素转移酶抑制剂
公开(公告)号：WO1998002436A1
公开(公告)日：1998-01-22
申请号：PCT/US1997011845
申请日：1997-07-08
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： BRISTOL-MYERS SQUIBB COMPANY , DING, Charles, Z.
IPC分类号： C07D417/02
CPC分类号： C07D417/06 , C07D417/14
摘要： Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by coumpounds of formulas (I) and (II) and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof wherein: r, s and t are 0 or 1; m = 0, 1, 2; p is 0, 1 or 2; X is selected from the group consisting of oxygen, hydrogen or R , R , R ; Y is selected from the group consisting of CHR , SO2, CO, CO2, O, NR , SO2NR and CONR ; R , R , R , R , R , R , R , R , R , R , R , R , R , R , R , R , R , R , R and R are selected from the group consisting of hydrogen, lower alkyl or substituted alkyl; R , R are selected from the group consisting of hydrogen, halo, nitro, cyano and U-R ; R is selected from the group consisting of hydrogen, lower alkyl, aryl, substituted alkyl or aryl; U is selected from the group consisting of sulfur, oxygen, NR , CO, SO, SO2, CO2, NR CO2, NR CONR , NR SO2, NR SO2NR , SO2NR , NR CO, CONR , PO2R and PO3R or U is absent; R , R , R , R and R are selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aralkyl, cycloalkyl, aryl, substituted aryl, heterocyclo, substituted heterocyclo; R, S and T are selected from the group consisting of CH2, CO and CH(CH2)pQ wherein Q is NR R or OR ; and A, B, C and D are carbon, oxygen, sulfur or nitrogen, with the proviso that R may be hydrogen except when U is SO, SO2, NR CO2 or NR SO2.
摘要翻译：抑制参与ras癌基因表达的酶的法呢基转移酶由式（I）和（II）及其对映体，非对映异构体及其药学上可接受的盐包括前药和溶剂合物的组合物实现，其中：r，s 和t为0或1; m = 0,1,2; p为0,1或2; X选自氧，氢或R 1，R 2，R 3; Y选自CHR 9，SO 2，CO，CO 2，O，NR 10，SO 2 NR 11和CONR 12; R 6，R 7，R 9，R 10，R 11，R 14，R 15，R 16，R 17，R 18， R 19，R 20，R 21，R 22，R 23，R 24，R 25，R 26，R 27和R 28均为选自氢，低级烷基或取代的烷基; R 4，R 5选自氢，卤素，硝基，氰基和U-R 13; R 12选自氢，低级烷基，芳基，取代的烷基或芳基; U选自硫，氧，NR 14，CO，SO，SO 2，CO 2，NR 15 CO，NR 16 CONR 17，NR 18 SO 2，NR 19， SO 2 NR 20，SO 2 NR 21，NR 22 CO，CONR 23，PO 2 R 24和PO 3 R 25或U不存在; R 1，R 2，R 3，R 8和R 13选自氢，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基，芳烷基，环烷基，芳基，取代的芳基，杂环基，取代的杂环基; R，S和T选自CH 2，CO和CH（CH 2）p Q，其中Q为NR 26 R 27或OR 28; 并且A，B，C和D是碳，氧，硫或氮，条件是R 13可以是氢，除了当U是SO，SO 2，NR 15 CO 2或NR 18 SO 2时。

5. 发明申请

WO2004004655A3 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
公开(公告)号：WO2004004655A3
公开(公告)日：2004-01-15
申请号：PCT/US2003/021331
申请日：2003-07-08
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHENG, Peter, T., W. , CHEN, Sean , DING, Charles, Z. , HERPIN, Timothy, F.
发明人： CHENG, Peter, T., W. , CHEN, Sean , DING, Charles, Z. , HERPIN, Timothy, F.
IPC分类号： A61K31/41
摘要： Compounds are provided which are useful as antidiabetic agents and antiobesity agents and have the structure (I) wherein m is 0, 1 or 2; n is 0, 1 or 2; Q is C or N; A is (CH 2 )x where x is 1 to 5, or A is (CH 2 )x1 where x 1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is -(CH 2 )x 2 -O-(CH 2 )x 3 - where x 2 is 0 to 5 and x 3 is 0 to 5, provided that at least one of x 2 and x 3 is other than 0; B is a bond or is (CH 2 )x 4 where x 4 is 1 to 5; X is CH or N; X 2 is C, N, O or S; X 3 is C, N, O or S; X 4 is C, N, O or S; X 5 is C, N, O or S; X 6 is C, N, O or S; provided that at least one of X 2 , X 3 , X 4 X 5 and X 6 is N; and at least one of X 2 , X 3 , X 4 , X 5 and X 6 is C, and specifically excluding the structure (II) where X 2 = N, X 3 = C, X 4 = O or S, Z = o or a bond; R 1 is H or alkyl; R 2 is H, alkyl, alkoxy, halogen, amino or substituted amino or cyano; R 2a , R 2b and R 2c may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino or substituted amino or cyano; and R 3 and Y are as defined herein, which compounds are useful in treating diabetes and obesity.

6. 发明公开

EP1027042A1 INHIBITORS OF FARNESYL PROTEIN TRANSFERASE 审中-公开
标题翻译：法尼蛋白转移酶抑制剂
公开(公告)号：EP1027042A1
公开(公告)日：2000-08-16
申请号：EP98948279.9
申请日：1998-09-16
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： DING, Charles, Z. , HUNT, John, T. , LEFTHERIS, Katerina , BHIDE, Rajeev, S.
IPC分类号： A61K31/33 , A61K31/495 , A61K31/50 , A61K31/53 , A61K31/535 , A61K31/54 , A61K31/55 , C07D237/26 , C07D239/70 , C07D241/36 , C07D243/12
CPC分类号： C07D401/06 , C07D243/14 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/06
摘要： Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of formulas (I), (II), their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof inhibit farnesyl protein transferase which is an enzyme involved in ras oncogene expression.
摘要翻译：式（I），（II）化合物，它们的对映异构体，非对映异构体及其药学上可接受的盐，前药和溶剂合物抑制作为参与ras致癌基因表达的酶的法尼基转移酶抑制法呢基蛋白转移酶，涉及ras致癌基因表达的酶。

7. 发明公开

EP1531810A2 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 有权
标题翻译：取代的杂环衍生物作为预防糖尿病剂和肥胖程序
公开(公告)号：EP1531810A2
公开(公告)日：2005-05-25
申请号：EP03763345.0
申请日：2003-07-08
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： CHENG, Peter, T., W. , CHEN, Sean , DING, Charles, Z. , HERPIN, Timothy, F.
IPC分类号： A61K31/41 , A61K31/42 , A61K31/50 , A61K31/52 , A61K31/435
CPC分类号： C07D233/64 , C07D249/06 , C07D263/32 , C07D271/06 , C07D413/12
摘要： Compounds are provided which are useful as antidiabetic agents and antiobesity agents and have the structure (I) wherein m is 0, 1 or 2; n is 0, 1 or 2; Q is C or N; A is (CH2)x where x is 1 to 5, or A is (CH2)x1 where x1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is -(CH2)x2-O-(CH2)x3- where x2 is 0 to 5 and x3 is 0 to 5, provided that at least one of x2 and x3 is other than 0; B is a bond or is (CH2)x4 where x4 is 1 to 5; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; provided that at least one of X2, X3, X4 X5 and X6 is N; and at least one of X2, X3, X4, X5 and X6 is C, and specifically excluding the structure (II) where X2 = N, X3 = C, X4 = O or S, Z = o or a bond; R1 is H or alkyl; R2 is H, alkyl, alkoxy, halogen, amino or substituted amino or cyano; R2a, R2b and R2c may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino or substituted amino or cyano; and R3 and Y are as defined herein, which compounds are useful in treating diabetes and obesity.

8. 发明授权

EP1531810B1 SUBSTITUTED HETEROCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 有权
标题翻译：取代的杂环衍生物作为预防糖尿病剂和肥胖程序
公开(公告)号：EP1531810B1
公开(公告)日：2012-02-01
申请号：EP03763345.0
申请日：2003-07-08
申请人： Bristol-Myers Squibb Company
发明人： CHENG, Peter, T., W. , CHEN, Sean , DING, Charles, Z. , HERPIN, Timothy, F.
IPC分类号： A61K31/41 , A61K31/42 , A61K31/50 , A61K31/52 , A61K31/435 , C07D249/06 , C07D263/32 , C07D233/64 , C07D271/06 , C07D413/12 , A61P3/10
CPC分类号： C07D233/64 , C07D249/06 , C07D263/32 , C07D271/06 , C07D413/12
摘要： Compounds are provided which are useful as antidiabetic agents and antiobesity agents and have the structure (I) wherein m is 0, 1 or 2; n is 0, 1 or 2; Q is C or N; A is (CH2)x where x is 1 to 5, or A is (CH2)x1 where x1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is -(CH2)x2-O-(CH2)x3- where x2 is 0 to 5 and x3 is 0 to 5, provided that at least one of x2 and x3 is other than 0; B is a bond or is (CH2)x4 where x4 is 1 to 5; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; provided that at least one of X2, X3, X4 X5 and X6 is N; and at least one of X2, X3, X4, X5 and X6 is C, and specifically excluding the structure (II) where X2 = N, X3 = C, X4 = O or S, Z = o or a bond; R1 is H or alkyl; R2 is H, alkyl, alkoxy, halogen, amino or substituted amino or cyano; R2a, R2b and R2c may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino or substituted amino or cyano; and R3 and Y are as defined herein, which compounds are useful in treating diabetes and obesity.

9. 发明公开

EP1656368A2 SUBSTITUTED HERTOCYCLIC DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD 审中-公开
标题翻译： AS抗糖尿病和手段对抗肥胖合适的取代的杂环衍生物方法
公开(公告)号：EP1656368A2
公开(公告)日：2006-05-17
申请号：EP03763485.4
申请日：2003-07-02
申请人： Bristol-Myers Squibb Company
发明人： CHENG, Peter, T. W. , CHEN, Sean , DEVASTHALE, Pratik , DING, Charles, Z. , HERPIN, Timothy, F. , WU, Shung , ZHANG, Hao , WANG, Wei , YE, Xiang-Yang
IPC分类号： C07D403/06 , C07D403/08 , C07D403/10 , C07D403/14 , C07D413/12 , C07D413/14 , A61K31/422 , A61K31/397 , A61P35/00
CPC分类号： C07D413/12 , C07D413/14
摘要： Formula, wherein Z1 is (CH2)q or C=O; Z2 is (CH2)p or C=O; D is -CH= or C=O or (CH2)m where m is 0, 1, 2 or 3; n = 0, 1 or 2; p = 1 or 2; q = 0, 1 or 2; Q is C or N; A is (CH2)x where x is 1 to 5, or A is (CH2)x1, where x1 is 1 to 5 with an alkenyl bond or an alkynyl bond embedded anywhere in the chain, or A is -(CH2)x2-O-(CH2)x3 - where x2 is 0 to 5 and x3 is 0 to 5, provided that at least one of x2 and x3 is other than 0; B is a bond or is (CH2)x4 where x4 is 1 to 5; X is CH or N; X2 is C, N, O or S; X3 is C, N, O or S; X4 is C, N, O or S; X5 is C, N, O or S; X6 is C, N, O or S; provided that at least one of X2, X3, X4 X5 and X6 is N; and at least one of X2, X3, X4 X5 and X6 is C. R1 is H or alkyl; R2 is H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; R2a, R2b and R2c may be the same or different and are selected from H, alkyl, alkoxy, halogen, amino, substituted amino or cyano; and R3, E, Z and Y are as defined herein.

10. 发明公开

EP0918771A1 THIADIOXOBENZODIAZEPINE INHIBITORS OF FARNESYL PROTEIN TRANSFERASE 失效
标题翻译： THIADIOXOBENZODIAZEPIN抑制剂法尼基蛋白转移
公开(公告)号：EP0918771A1
公开(公告)日：1999-06-02
申请号：EP97936043.0
申请日：1997-07-08
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： DING, Charles, Z.
IPC分类号： A61K31 , A61P9 , A61P13 , A61P17 , A61P19 , A61P25 , A61P31 , A61P35 , A61P37 , A61P43 , C07D417
CPC分类号： C07D417/06 , C07D417/14
摘要： Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by coumpounds of formulas (I) and (II) and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof wherein: r, s and t are 0 or 1; m = 0, 1, 2; p is 0, 1 or 2; X is selected from the group consisting of oxygen, hydrogen or R?1, R2, R3¿; Y is selected from the group consisting of CHR9, SO2, CO, CO2, O, NR10, SO2NR11 and CONR?12; R6, R7, R9, R10, R11, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27 and R28¿ are selected from the group consisting of hydrogen, lower alkyl or substituted alkyl; R4, R5 are selected from the group consisting of hydrogen, halo, nitro, cyano and U-R13; R12 is selected from the group consisting of hydrogen, lower alkyl, aryl, substituted alkyl or aryl; U is selected from the group consisting of sulfur, oxygen, NR14, CO, SO, SO¿2?, CO2, NR?15CO¿2, NR?16CONR17, NR18SO¿2, NR19SO2NR20, SO2NR?21, NR22¿CO, CONR23, PO2R24 and PO¿3R?25 or U is absent; R?1, R2, R3, R8 and R13¿ are selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aralkyl, cycloalkyl, aryl, substituted aryl, heterocyclo, substituted heterocyclo; R, S and T are selected from the group consisting of CH¿2?, CO and CH(CH2)pQ wherein Q is NR?26R27 or OR28¿; and A, B, C and D are carbon, oxygen, sulfur or nitrogen, with the proviso that R13 may be hydrogen except when U is SO, SO¿2?, NR?15CO¿2 or NR18SO2.

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