Patent number: 7053216
Abstract: Compounds of formula 1 modulate the activity of Rho C: wherein R1 is H, lower alkyl, aralkyl, aryl-lower alkenyl, or —(CH2)nCH(R7)NR8R9, where n is 0–6 inclusive, R7 is H, lower alkyl, aryl, or aralkyl, R8 is H, lower alkyl, cyclo-alkyl, aryl, or aralkyl, and R9 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; R2 is lower alkyl, aryl, aralkyl, or —(CHR10)m—(CO)—R11, wherein m is 0–4, R10 is H or lower alkyl, and R11 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; R3, R4, R5, and R6, are each independently H, lower alkyl, halo, nitro, OH, lower alkoxy, NH2, lower alkylamino, di(lower alkylamino), trifluoromethyl, or SH; or a pharmaceutically acce
Type:
Grant
Filed:
November 19, 2002
Date of Patent:
May 30, 2006
Assignee:
Iconix Pharmaceuticals, Inc.
Inventors:
Dongxu Sun, Edward L. Perkins, Stuart Tugendreich
Patent number: 7049468
Abstract: Compounds of formula 1 modulate the activity of Rho C: wherein R is a direct bond, lower alkylene, —C(O)NH—, or —NHC(O)—; Ar is aryl or heteroaryl, substituted with R7, R8, R9, and R10, wherein R7, R8, and R9 are each independently H, halo, lower alkyl, OH, lower alkoxy, and R10 is H, halo, lower alkyl, OH, lower alkoxy, or forms a ring with R1; R1 is H, lower alkyl, or forms a ring with R10; R2, R3, R4, R5, and R6 are each independently H, lower alkyl, halo, nitro, OH, lower alkoxy, NH2, lower alkylamino, di(lower alkyl)amino, or two adjacent groups together form a saturated or unsaturated ring; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
November 19, 2002
Date of Patent:
May 23, 2006
Assignee:
Iconix Pharmaceuticals, Inc.
Inventors:
Dongxu Sun, Edward L. Perkins, Stuart Tugendreich
Patent number: 6908932
Abstract: Compounds of formula 1 are effective modulators of PI3 kinase: wherein R1 is H, hydroxy, amino, lower alkyl, or trihalomethyl; R2 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 —(CH2)n—C(?X)—R8, where n is 014 3 inclusive and X is O or NR9, where R9 is H, lower alkyl, or R1 and R2 together form —CH?N—X— where X is CH, NH, O, or S, and R8 is H, lower alkyl, lower alkoxy, aryl, aralkyl, or —(CH2)mCR10R11R12, where m is 0-3 inclusive, and R10, R11, and R12 are each independently H, lower alkyl, aryl, aralkyl, hydroxy, lower alkoxy, aryloxy, aralkoxy, amino, lower alkyl-amino, arylamino, aralkylamino, heteroaryl amino, or heteroaralkyl amino, where aryl and heteroaryl are substituted with 0-3 substituents selected from the group consisting of halo, hydrox
Type:
Grant
Filed:
October 24, 2002
Date of Patent:
June 21, 2005
Assignee:
Iconix Pharmaceuticals, Inc.
Inventors:
Teri Melese, Edward L. Perkins, Allen T. Q. Nguyen, Dongxu Sun
Patent number: 6894055
Abstract: Compounds of formula 1 are effective modulators of PI3 kinase: wherein X is CR9R10, O, NR11 (where R9 and R10 are each independently H, lower alkyl, lower alkoxy, or halo, and R11 is H or lower alkyl); or single bond; R1 is H, lower alkyl, aryl, aralkyl; R2 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; R3, R4, R5, R6, R7, and R8 are each independently H, lower alkyl, lower alkoxy, or halo; or a pharmaceutically acceptable salt or ester thereof.
Type:
Grant
Filed:
October 24, 2002
Date of Patent:
May 17, 2005
Assignee:
Iconix Pharmaceuticals Inc.
Inventors:
Teri Melese, Edward L. Perkins, Allen T. Q. Nguyen, Dongxu Sun
Patent number: 6800634
Abstract: Compounds of formula 1 modulate the activity of Rho C:
wherein R1 is H, OH, or lower alkyl;
R2, R3, R4, R5, and R6 are each independently H, halo, lower alkyl, OH, lower alkoxy, NH2, lower alkylamino, di(lower alkyl)amino, SH, lower alkylthio, NO2, or two residues together form a heterocyclic ring;
R7, R8, R9, and R10 are each independently H, lower alkyl, OH, NH2, aryl, or aralkyl, where aryl and aralkyl are substituted with 0-3 moieties selected from the group consisting of halo, OH, NH2, lower alkyl, lower alkoxy, SH, lower alkylthio, and lower alkylamino;
R11, R12, R13, R14, R15, and R16 are each independently H, halo, lower alkyl, OH, lower alkoxy, or NO2;
or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
November 19, 2002
Date of Patent:
October 5, 2004
Assignee:
Iconix Pharmaceuticals Inc.
Inventors:
Dongxu Sun, Edward L. Perkins, Stuart Tugendreich
