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. 发明申请

WO2003035618A2 MODULATORS OF PHOSPHOINOSITIDE 3-KINASE 审中-公开
标题翻译：磷酸肌醇3-激酶调节剂
公开(公告)号：WO2003035618A2
公开(公告)日：2003-05-01
申请号：PCT/US2002/034086
申请日：2002-10-24
申请人： ICONIX PHARMACEUTICALS, INC. , MELESE, Teri , PERKINS, Edward, L. , NGUYEN, Allen, T., Q. , SUN, Dongxu
发明人： MELESE, Teri , PERKINS, Edward, L. , NGUYEN, Allen, T., Q. , SUN, Dongxu
IPC分类号： C07D
CPC分类号： C07D215/22 , C07D215/38 , C07D401/12
摘要： Compounds of Formula (I) are effective modulators of PI3 kinase wherein R 1 is H, hydroxy, amino, lower alkyl, or trihalomethyl; R 2 is amino, lower alkylamino, lower acylamino, arylamino, arylacyl-amino, heteroaryl-amino, heteroaryl-acyl amino, where aryl and heteroaryl are substituted with 0-3 substituents selected from the group consisting of halo, trihalomethyl, hydroxy, lower alkyl and lower alkoxy, or a substituent of the form -(CH 2 ) n -C(=X)-R 8 , where n is 0-3 inclusive and X is O or NR 9 , where R 9 is H, lower alkyl, or R 1 and R 2 together form -CH=N-X- where X is CH, NH, O, or S, and R 8 is H, lower alkyl, lower alkoxy, aryl, aralkyl, or -(CH 2 ) m CR 10 R 11 R 12 , where m is 0-3 inclusive, and R 10 , R 11 , and R 12 are each independently H, lower alkyl, aryl, aralkyl, hydroxy, lower alkoxy, aryloxy, aralkoxy, amino, lower alkylamino, arylamino, aralkylamino, heteroaryl amino, or heteroaralkyl amino, where aryl and heteroaryl are substituted with 0-3 substituents selected from the group consisting of halo, hydroxy, and lower alkyl; R 3 is H or lower alkyl; and R 4 , R 5 , R 6 , R 7 are each independently H, halo, hydroxy, amino, nitro, lower alkyl, or lower alkoxy; and pharmaceutically acceptable salts thereof.
摘要翻译：式（I）化合物是PI3激酶的有效调节剂，其中R 1是H，羟基，氨基，低级烷基或三卤代甲基; R 2是氨基，低级烷基氨基，低级酰基氨基，芳基氨基，芳基酰基氨基，杂芳基 - 氨基，杂芳基 - 酰基氨基，其中芳基和杂芳基被0-3个取代基取代，所述取代基选自卤素，三卤代甲基，羟基，低级烷基和低级烷氧基，或 - （CH 2）n -C（= X）-R 8形式的取代基其中n为0-3（包括0和3），X为O或NR 9，其中R 9为H，低级烷基或R 1，其中X为CH，NH，O或S，并且R 8为H，低级烷基，低级烷氧基，芳基，芳烷基或 - （CH 2）m CR 12 R 11 R 12，其中m为0-3（包括0和3），并且R 10，R 11和R 12各自独立地为H，低级烷基，芳基，芳烷基，羟基，低级烷氧基，芳氧基，芳烷氧基，氨基，低级烷基氨基，芳基氨基，芳烷基氨基，杂芳基氨基或杂芳烷基氨基，其中芳基和杂芳基是取代的用选自卤素，羟基和低级烷基的0-3个取代基取代; R 3是H或低级烷基; 和R 4，R 5，R 6，R 7各自独立地为H，卤素，羟基，氨基，硝基，低级烷基或低级烷氧基; 及其药学上可接受的盐。

2. 发明申请

WO2003034997A2 MODULATORS OF PHOSPHOINOSITIDE 3-KINASE 审中-公开
标题翻译：磷酸三辛酯3激酶的调节剂
公开(公告)号：WO2003034997A2
公开(公告)日：2003-05-01
申请号：PCT/US2002/034054
申请日：2002-10-24
申请人： ICONIX PHARMACEUTICALS, INC. , MELESE, Teri , PERKINS, Edward, L. , NGUYEN, Allen, T., Q. , SUN, Dongxu
发明人： MELESE, Teri , PERKINS, Edward, L. , NGUYEN, Allen, T., Q. , SUN, Dongxu
IPC分类号： A61K
CPC分类号： C07D495/14
摘要： Compounds of formula 1 are effective modulators of P13 kinase: wherein X is CR 9, R 10 , 0, NR 11 (where R 9 and R 1O are each independently H, lower alkyl, lower alkoxy, or halo, and R 11 is H or lower alkyl); or single bond; R 1 is H, lower alkyl, aryl, aralkyl; R 2 is H, lower alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, lower alkoxy, amino, lower alkylamino, lower acylamino, arylamino, arylacyl-amino, heteroaryl-amino, heteroaryl-acyl amino, thio, lower alkylthio, arylthio, or aralkyl-thio, where aryl and heteroaryl are substituted with 0-3 substituents selected from the group consisting of halo, trihalomethyl, hydroxy, lower alkyl and lower alkoxy; R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are each independently H, lower alkyl, lower alkoxy, or halo; or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：式1的化合物是P13激酶的有效调节剂：其中X是CR 9，R 11，R 11，其中R sb R 9和R 11各自独立地为H，低级烷基，低级烷氧基或卤素，R 11为H或低级烷基）。或单键; R 1是H，低级烷基，芳基，芳烷基; R 2是H，低级烷基，芳基，芳烷基，杂芳基，杂芳基 - 烷基，低级烷氧基，氨基，低级烷基氨基，低级酰基氨基，芳基氨基，芳酰基 - 氨基，杂芳基 - 氨基，杂芳基 - 酰基氨基其中芳基和杂芳基被0-3个选自卤素，三卤代甲基，羟基，低级烷基和低级烷氧基的取代基所取代; R 3，R 4，R 4，R 6，R 7，R 7和R 7，和 R 8各自独立地为H，低级烷基，低级烷氧基或卤素; 或其药学上可接受的盐或酯。

3. 发明申请

WO2003035618A3 MODULATORS OF PHOSPHOINOSITIDE 3-KINASE 审中-公开
公开(公告)号：WO2003035618A3
公开(公告)日：2003-05-01
申请号：PCT/US2002/034086
申请日：2002-10-24
申请人： ICONIX PHARMACEUTICALS, INC. , MELESE, Teri , PERKINS, Edward, L. , NGUYEN, Allen, T., Q. , SUN, Dongxu
发明人： MELESE, Teri , PERKINS, Edward, L. , NGUYEN, Allen, T., Q. , SUN, Dongxu
IPC分类号： A61K31/47
摘要： Compounds of Formula (I) are effective modulators of PI3 kinase wherein R 1 is H, hydroxy, amino, lower alkyl, or trihalomethyl; R 2 is amino, lower alkylamino, lower acylamino, arylamino, arylacyl-amino, heteroaryl-amino, heteroaryl-acyl amino, where aryl and heteroaryl are substituted with 0-3 substituents selected from the group consisting of halo, trihalomethyl, hydroxy, lower alkyl and lower alkoxy, or a substituent of the form -(CH 2 ) n -C(=X)-R 8 , where n is 0-3 inclusive and X is O or NR 9 , where R 9 is H, lower alkyl, or R 1 and R 2 together form -CH=N-X- where X is CH, NH, O, or S, and R 8 is H, lower alkyl, lower alkoxy, aryl, aralkyl, or -(CH 2 ) m CR 10 R 11 R 12 , where m is 0-3 inclusive, and R 10 , R 11 , and R 12 are each independently H, lower alkyl, aryl, aralkyl, hydroxy, lower alkoxy, aryloxy, aralkoxy, amino, lower alkylamino, arylamino, aralkylamino, heteroaryl amino, or heteroaralkyl amino, where aryl and heteroaryl are substituted with 0-3 substituents selected from the group consisting of halo, hydroxy, and lower alkyl; R 3 is H or lower alkyl; and R 4 , R 5 , R 6 , R 7 are each independently H, halo, hydroxy, amino, nitro, lower alkyl, or lower alkoxy; and pharmaceutically acceptable salts thereof.

4. 发明申请

WO2003034997A3 MODULATORS OF PHOSPHOINOSITIDE 3-KINASE 审中-公开
公开(公告)号：WO2003034997A3
公开(公告)日：2003-05-01
申请号：PCT/US2002/034054
申请日：2002-10-24
申请人： ICONIX PHARMACEUTICALS, INC. , MELESE, Teri , PERKINS, Edward, L. , NGUYEN, Allen, T., Q. , SUN, Dongxu
发明人： MELESE, Teri , PERKINS, Edward, L. , NGUYEN, Allen, T., Q. , SUN, Dongxu
IPC分类号： C07D519/00
摘要： Compounds of formula 1 are effective modulators of P13 kinase: wherein X is CR 9, R 10 , 0, NR 11 (where R 9 and R 1O are each independently H, lower alkyl, lower alkoxy, or halo, and R 11 is H or lower alkyl); or single bond; R 1 is H, lower alkyl, aryl, aralkyl; R 2 is H, lower alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, lower alkoxy, amino, lower alkylamino, lower acylamino, arylamino, arylacyl-amino, heteroaryl-amino, heteroaryl-acyl amino, thio, lower alkylthio, arylthio, or aralkyl-thio, where aryl and heteroaryl are substituted with 0-3 substituents selected from the group consisting of halo, trihalomethyl, hydroxy, lower alkyl and lower alkoxy; R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are each independently H, lower alkyl, lower alkoxy, or halo; or a pharmaceutically acceptable salt or ester thereof.

5. 发明申请

WO0244157A3 PARB INHIBITORS 审中-公开
标题翻译： PARB抑制剂
公开(公告)号：WO0244157A3
公开(公告)日：2002-12-27
申请号：PCT/US0146811
申请日：2001-12-03
申请人： ICONIX PHARM INC , MELESE TERI , PERKINS EDWARD L , YEH ELAINE , SUN DONXU
发明人： MELESE TERI , PERKINS EDWARD L , YEH ELAINE , SUN DONXU
IPC分类号： A61P35/00 , C07D237/32 , A61K31/50 , C07D217/24 , C07D239/90 , C07D279/08 , C07D401/06 , C07D401/12 , C07D409/04
CPC分类号： C07D237/32
摘要： Compounds of formula 1, 2, and 3 where A1 is C(R4)or N; A2 is C(R5) or S; R1 is H, lower alkyl, halo, or a carbonyl; R2 is H, lower alkyl, acyl, or forms a double bond with an adjacent ring atom; R3 is H, lower alkyl, halo, aryl, aralkyl, acyl, lower alkenyl, or a radical or the form (CH2)nC(O)-Ra, where Ra is lower alkyl, OH, NH2, lower alkoxy, lower aklylamino, di(lower alkyl)amino, aryl, or heterocyclyl, or forms a double bond with an adjacent ring atom; R4 is H, lower alkyl, or forms a double bond with an adjacent ring atom, R5 is H, lower alkyl, OH, halo, lower alkoxy, lower alkyl-thio, aryl-thio, or heterocyclyl-thio; R6 and R7 are each independently H, lower alkyl, OH, lower alkoxy, halo, nitro, amino, thio, acyl, lower alkylamino, acyloxy, acylamino, sulfinyl, sulfonyl, alkylsulfinyl, alkylsulfonyl, arylsulfonyl, aryl, heterocyclyl, aralkyl, or heterocyclyl-alkyl; R10 is H, lower alkyl, lower alkenyl, aryl, heterocyclyl, aryl-lower alkyl, or heterocyclyl-lower alkyl; and R11, R12, and R13 are each independently halo, nitro, OH, NH2, or lower alkyl, and pharmaceutically acceptable salts thereof, are effective modulators of PARP enzymes.
摘要翻译：式1，式2和式3的化合物，其中A1是C（R4）或N; A2是C（R5）或S; R1是H，低级烷基，卤素或羰基; R2是H，低级烷基，酰基或与相邻的环原子形成双键; R3是H，低级烷基，卤素，芳基，芳烷基，酰基，低级链烯基或基团或形式（CH2）nC（O）-Ra，其中Ra是低级烷基，OH，NH2，低级烷氧基，低级烷基氨基，二（低级烷基）氨基，芳基或杂环基，或与相邻的环原子形成双键; R4是H，低级烷基或与相邻的环原子形成双键，R5是H，低级烷基，OH，卤素，低级烷氧基，低级烷基 - 硫基，芳基 - 硫基或杂环基 - 低级烷基，OH，低级烷氧基，卤素，硝基，氨基，硫代，酰基，低级烷基氨基，酰氧基，酰基氨基，亚磺酰基，磺酰基，烷基亚磺酰基，烷基磺酰基，芳基磺酰基，芳基，杂环基，芳烷基或杂环基 - 烷基; R10为H，低级烷基，低级链烯基，芳基，杂环基，芳基 - 低级烷基或杂环基 - 低级烷基; 和R 11，R 12和R 13各自独立地为卤素，硝基，OH，NH 2或低级烷基，及其药学上可接受的盐是PARP酶的有效调节剂。

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