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1. 发明申请

WO2003043577A3 MODULATORS OF RHO C ACTIVITY 审中-公开
公开(公告)号：WO2003043577A3
公开(公告)日：2003-05-30
申请号：PCT/US2002/037096
申请日：2002-11-19
申请人： ICONIX PHARMACEUTICALS, INC. , SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart , LEE, Ving, J.
发明人： SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart , LEE, Ving, J.
IPC分类号： A61K31/428
摘要： Compounds of formula (1) modulate the activity of Rho C, wherein n is 2 to 5, inclusive; R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and R 9 are each independently halo, lower alkyl, lower alkoxy, lower alkylamino, trifluoromethyl, nitro, lower alkylthio, or two adjacent residues form cycloalkyl, cycloalkenyl, aryl, or lower alkylenedioxy; and pharmaceutically acceptable salts thereof.

2. 发明申请

WO2003043577A2 MODULATORS OF RHO C ACTIVITY 审中-公开
标题翻译： RHO C活动调节剂
公开(公告)号：WO2003043577A2
公开(公告)日：2003-05-30
申请号：PCT/US2002/037096
申请日：2002-11-19
申请人： ICONIX PHARMACEUTICALS, INC. , SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart , LEE, Ving, J.
发明人： SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart , LEE, Ving, J.
IPC分类号： A61K
CPC分类号： C07D513/04
摘要： Compounds of formula (1) modulate the activity of Rho C, wherein n is 2 to 5, inclusive; R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and R 9 are each independently halo, lower alkyl, lower alkoxy, lower alkylamino, trifluoromethyl, nitro, lower alkylthio, or two adjacent residues form cycloalkyl, cycloalkenyl, aryl, or lower alkylenedioxy; and pharmaceutically acceptable salts thereof.
摘要翻译：式（1）化合物调节Rho C的活性，其中n为2至5，包括端值; R 1，R 2，R 3，R 4，R 5，R 5，R 5， R 6，R 7，R 8和R 9各自独立地为卤素，低级烷基，低级烷氧基低级烷基氨基，三氟甲基，硝基，低级烷硫基或两个相邻的残基形成环烷基，环烯基，芳基或低级亚烷二氧基; 及其药学上可接受的盐。

3. 发明申请

WO2003043582A3 MODULATORS OF RHO C ACTIVITY 审中-公开
公开(公告)号：WO2003043582A3
公开(公告)日：2003-05-30
申请号：PCT/US2002/037198
申请日：2002-11-19
申请人： ICONIX PHARMACEUTICALS, INC. , SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart
发明人： SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart
IPC分类号： A61K31/473
摘要： Compounds of formula (1) modulate the activily of Rho C, wherein R 1 is H, OH, or lower alkyl; R 2 , R 3 , R 4 , R 5 and R 6 are each independently H, halo, lower alkyl, OH, lower alkoxy, NH 2 , lower alkylamino, di(lower alkyl)amino, SH, lower alkylthio, NO 2 , or two residues together form a heterocyclic ring; R 7 , R 8 , R 9 and R 10 are each independently H, lower alkyl, OH, NH 2 , aryl, or aralkyl, where aryl and aralkyl are substituted with 0-3 moieties selected from the group consisting of halo, OH, NH 2 , lower alkyl, lower alkoxy, SH, lower alkylthio, and lower alkylamino; R 11 , R 12 , R 13 , R 14 , R 15 , and R 16 are each independently H, halo, lower alkyl, OH, lower alkoxy, or NO 2 ; or a pharmaceutically acceptable salt thereof.

4. 发明申请

WO2003043961A3 MODULATORS OF RHO C ACTIVITY 审中-公开
公开(公告)号：WO2003043961A3
公开(公告)日：2003-05-30
申请号：PCT/US2002/037292
申请日：2002-11-19
申请人： ICONIX PHARMACEUTICALS, INC. , SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart
发明人： SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart
IPC分类号： C07D401/06
摘要： Compounds of formula 1 modulate the activity of Rho C: (Formula I) wherein R 1 is H, lower alkyl, aralkyl, aryl-lower alkenyl, or (CH 2 ) n CH(R 7 )NR 8 R 9 , where n is 0-6 inclusive, R 7 is H, lower alkyl, aryl, or aralkyl, R 8 is H, lower alkyl, cyclo-alkyl, aryl, or aralkyl, and R 9 is R, RCO-, ROCO-, or RNHCO-, where R is lower alkyl, cycloalkyl, aryl, or aralkyl, wherein aryl and aralkyl are substituted with 0-3 substituents selected from the group consisting of lower alkyl, halo, nitro, -OH, trifluoromethyl, or lower alkoxy; R 2 is lower alkyl, aryl, aralkyl, or (CHR 10 ) m -(CO)-R 11 , wherein m is 0-4, R 10 is H or lower alkyl, and R 11 is lower alkyl, cycloalkyl, aryl, or aralkyl, wherein aryl and aralkyl are substituted with 0-3 substituents selected from the group consisting of lower alkyl, halo, nitro, -OH, trifluoromethyl, or lower alkoxy; R 3 , R 4 , R 5 and R 6 are each independtly H, lower alkyl, halo, nitro, OH, lowe alkoxy, NH 2 , lower alkylamino, di(lower alkylamino), trifluoromethyl, or SH; or a pharmaceutically acceptable salt thereof.

5. 发明申请

WO2003043578A2 MODULATORS OF RHO C ACTIVITY 审中-公开
标题翻译： RHO C活性调节剂
公开(公告)号：WO2003043578A2
公开(公告)日：2003-05-30
申请号：PCT/US2002/037098
申请日：2002-11-19
申请人： ICONIX PHARMACEUTICALS, INC. , SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart
发明人： SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart
IPC分类号： A61K
CPC分类号： C07D213/75 , C07C311/16 , C07C311/17 , C07C311/29 , C07D209/08 , C07D307/52

6. 发明申请

WO2003043961A2 MODULATORS OF RHO C ACTIVITY 审中-公开
标题翻译： RHO C活动调节剂
公开(公告)号：WO2003043961A2
公开(公告)日：2003-05-30
申请号：PCT/US2002/037292
申请日：2002-11-19
申请人： ICONIX PHARMACEUTICALS, INC. , SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart
发明人： SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart
IPC分类号： C07C
CPC分类号： C07D239/91 , C07D239/90
摘要： Compounds of formula 1 modulate the activity of Rho C: (Formula I) wherein R 1 is H, lower alkyl, aralkyl, aryl-lower alkenyl, or (CH 2 ) n CH(R 7 )NR 8 R 9 , where n is 0-6 inclusive, R 7 is H, lower alkyl, aryl, or aralkyl, R 8 is H, lower alkyl, cyclo-alkyl, aryl, or aralkyl, and R 9 is R, RCO-, ROCO-, or RNHCO-, where R is lower alkyl, cycloalkyl, aryl, or aralkyl, wherein aryl and aralkyl are substituted with 0-3 substituents selected from the group consisting of lower alkyl, halo, nitro, -OH, trifluoromethyl, or lower alkoxy; R 2 is lower alkyl, aryl, aralkyl, or (CHR 10 ) m -(CO)-R 11 , wherein m is 0-4, R 10 is H or lower alkyl, and R 11 is lower alkyl, cycloalkyl, aryl, or aralkyl, wherein aryl and aralkyl are substituted with 0-3 substituents selected from the group consisting of lower alkyl, halo, nitro, -OH, trifluoromethyl, or lower alkoxy; R 3 , R 4 , R 5 and R 6 are each independtly H, lower alkyl, halo, nitro, OH, lowe alkoxy, NH 2 , lower alkylamino, di(lower alkylamino), trifluoromethyl, or SH; or a pharmaceutically acceptable salt thereof.
摘要翻译：式1的化合物调节其中R 1为H，低级烷基，芳烷基，芳基 - 低级烯基或（CH 3）2的Rho C（式I）（CH 7）2 NR 9 R 9，其中n是（CH 2） 0-6，包括R 7是H，低级烷基，芳基或芳烷基，R 8是H，低级烷基，环烷基，芳基或芳烷基，和 R 9是R，RCO-，ROCO-或RNHCO-，其中R是低级烷基，环烷基，芳基或芳烷基，其中芳基和芳烷基被0-3个选自组的取代基由低级烷基，卤素，硝基，-OH，三氟甲基或低级烷氧基组成; R 2是低级烷基，芳基，芳烷基或（CHR）10 - （CO）-R 11 - / - 其中m为0-4，R10为H或低级烷基，且R11为低级烷基，环烷基，芳基或芳烷基，其中芳基和芳烷基为被选自低级烷基，卤素，硝基，-OH，三氟甲基或低级烷氧基的0-3个取代基取代; R 3，R 4，R 5和R 6各自独立地为H，低级烷基，卤素，硝基 OH，低级烷氧基，NH 2，低级烷基氨基，二（低级烷基氨基），三氟甲基或SH; 或其药学上可接受的盐。

7. 发明申请

WO2003043582A2 MODULATORS OF RHO C ACTIVITY 审中-公开
标题翻译： RHO C活动调节剂
公开(公告)号：WO2003043582A2
公开(公告)日：2003-05-30
申请号：PCT/US2002/037198
申请日：2002-11-19
申请人： ICONIX PHARMACEUTICALS, INC. , SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart
发明人： SUN, Dongxu , PERKINS, Edward, L. , TUGENDREICH, Stuart
IPC分类号： A61K
CPC分类号： C07D221/18
摘要： Compounds of formula (1) modulate the activily of Rho C, wherein R 1 is H, OH, or lower alkyl; R 2 , R 3 , R 4 , R 5 and R 6 are each independently H, halo, lower alkyl, OH, lower alkoxy, NH 2 , lower alkylamino, di(lower alkyl)amino, SH, lower alkylthio, NO 2 , or two residues together form a heterocyclic ring; R 7 , R 8 , R 9 and R 10 are each independently H, lower alkyl, OH, NH 2 , aryl, or aralkyl, where aryl and aralkyl are substituted with 0-3 moieties selected from the group consisting of halo, OH, NH 2 , lower alkyl, lower alkoxy, SH, lower alkylthio, and lower alkylamino; R 11 , R 12 , R 13 , R 14 , R 15 , and R 16 are each independently H, halo, lower alkyl, OH, lower alkoxy, or NO 2 ; or a pharmaceutically acceptable salt thereof.
摘要翻译：式（1）的化合物调节Rho C的活性，其中R 1为H，OH或低级烷基; R 2，R 3，R 4，R 5和R 6是各自独立地为H，卤素，低级烷基，OH，低级烷氧基，NH 2，低级烷基氨基，二（低级烷基）氨基，SH，低级烷硫基，NO 2或两个残基一起形成杂环; R 7，R 8，R 9和R 10各自独立地为H，低级烷基，OH，NH 芳基或芳烷基，其中芳基和芳烷基被选自以下的0-3部分取代：卤素，OH，NH 2，低级烷基，低级烷氧基，SH，低级烷硫基和低级烷氨基; R 11，R 12，R 13，R 14，R 15，R 15，R 15，和R 16各自独立地为H，卤素，低级烷基，OH，低级烷氧基或NO 2; 或其药学上可接受的盐。

8. 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。

9. 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。

10. 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.

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