39585-32-5Relevant academic research and scientific papers
Synthesis, biological evaluation and molecular modeling of 2-Hydroxyisoquinoline-1,3-dione analogues as inhibitors of HIV reverse transcriptase associated ribonuclease H and polymerase
Tang, Jing,Vernekar, Sanjeev Kumar V.,Chen, Yue-Lei,Miller, Lena,Huber, Andrew D.,Myshakina, Nataliya,Sarafianos, Stefan G.,Parniak, Michael A.,Wang, Zhengqiang
, p. 85 - 96 (2017/04/06)
Human immunodeficiency virus (HIV) reverse transcriptase (RT) associated ribonuclease H (RNase H) remains the only virally encoded enzymatic function not clinically validated as an antiviral target. 2-Hydroxyisoquinoline-1,3-dione (HID) is known to confer
Methods for the preparation of 6-aminoisoquinoline
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, (2018/01/21)
Described are methods for the preparation of 6-aminoisoquinoline, a useful intermediate compound in the synthesis of kinase inhibitors.
The design, synthesis and biological evaluations of C-6 or C-7 substituted 2-hydroxyisoquinoline-1,3-diones as inhibitors of hepatitis C virus
Chen, Yue-Lei,Tang, Jing,Kesler, Matthew J.,Sham, Yuk Y.,Vince, Robert,Geraghty, Robert J.,Wang, Zhengqiang
, p. 467 - 479 (2012/02/16)
C7-Substituted 2-hydroxyisoquinoline-1,3-diones inhibit the strand transfer of HIV integrase (IN) and the reverse-transcriptase-associated ribonuclease H (RNH). Hepatitis C virus (HCV) NS5B polymerase shares a similar active site fold to RNH and IN, sugge
HSP90 INHIBITOR
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Page/Page column 121, (2009/04/23)
Compounds represented by formula (1) shown below, pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising such compounds are provided.
4-(Phenylaminomethylene)isoquinoline-1,3(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4 (CDK4)
Tsou, Hwei-Ru,Otteng, Mercy,Tran, Tritin,Floyd Jr., M. Brawner,Reich, Marvin,Birnberg, Gary,Kutterer, Kristina,Ayral-Kaloustian, Semiramis,Ravi, Malini,Nilakantan, Ramaswamy,Grillo, Mary,McGinnis, John P.,Rabindran, Sridhar K.
scheme or table, p. 3507 - 3525 (2009/04/07)
The cyclin-dependent kinases (CDKs), as complexes with their respective partners, the cyclins, are critical regulators of cell cycle progression. Because aberrant regulations of CDK4/cyclin D1 lead to uncontrolled cell proliferation, a hallmark of cancer, small-molecule inhibitors of CDK4/cyclin D1 are attractive as prospective antitumor agents. The series of 4-(phenylaminomethylene)isoquinoline-1,3(2H,4H)-dione derivatives reported here represents a novel class of potent inhibitors that selectively inhibit CDK4 over CDK2 and CDK1 activities. In the headpiece of the 4-(phenylaminomethylene) isoquinoline-1,3(2H,4H)-dione, a basic amine substitutent is required on the aniline ring for the CDK4 inhibitory activity. The inhibitory activity is further enhanced when an aryl or heteroaryl substituent is introduced at the C-6 position of the isoquinoline-1,3(2H,4H)-dione core. We present here SAR data and a CDK4 mimic model that explains the binding, potency, and selectivity of our CDK4 selective inhibitors.
INHIBITORS OF CHECKPOINT KINASES
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, (2008/06/13)
The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound
Biphenyl-2-carboxylic acid-tetrahydro-isoquinolin-6-yl amide derivatives, their preparation and use as inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (ApoB) secretion
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, (2008/06/13)
Compositions comprising a lipid lowering agent selected from cholesterol biosynthesis inhibitors, bile acid sequestrants, fibrates, cholesterol absorption inhibitors, and niacin; and an inhibitor of microsomal triglyceride transfer protein for treating atherosclerosis, obesity and related diseases.
Apo B-secretion/MTP inhibitory amides
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, (2008/06/13)
PCT No. PCT/IB97/01368 Sec. 371 Date Apr. 20, 1999 Sec. 102(e) Date Apr. 20, 1999 PCT Filed Nov. 3, 1997 PCT Pub. No. WO98/23593 PCT Pub. Date Jun. 4, 1998This invention is directed to compounds of formula (I) or the stereoisomers, pharmaceutically accept
Apo B-secretion/MTP inhibitor hydrochloride salt
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, (2008/06/13)
A hydrochloride salt of an Apo B secretion/MTP inhibitor, methods of making the salt, methods of using the salt and pharmaceutical compositions containing the salt are disclosed.
Biphenyl-2-carboxylic acid-tetrahydro-isoquinolin-6-yl amide derivatives, their preparation and their use as inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (Apo B) secretion
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, (2008/06/13)
Compounds of formula (I), STR1 wherin X is CH2, CO, CS or SO2 ; Y is selected from: a direct link, aliphatic hydrocarbylene radicals having up to 20 carbon atoms, which radical may be mono-substituted by hydroxy, (C1 -C10)alkoxy, (C1 -C10)acyl, (C1 -C10)acyloxy, or (C6 -C10)aryl, NH, and O, provided that if X is CH2,Y is a direct link; Z is selected from the following groups: (1) H, halo, cyano, (2) hydroxy, (C1 -C10)alkoxy, (C1 -C10)a1kylthio, (C1 -C10)acyl, thiophenylcaronyl (C1 -C10)alkoxycarbonyl, (3) (C1 -C10)aklkyammo, di(C1 -C10)alylamino, (C6 -C10)aryl(C1 -C10)alkylamino, provided that Y is not O or NH, (4) unsubstituted vinyl, (C6 -C10)aryl, (C3 -C8)cycloalkyl and fused benz derivatives thereof, (C7 -C10)polycycloalkyl, (C4 -C8)cycloalkenyl, (C7 -C10)polycycloalkenyl, (5) (C6 -C10)aryloxy, (C6 -C10)aryltio, (C6 -C10)aryl(C1 -C10)alkoxy, (C6 -C10)aryl(C1 -C10)alkylthio, (C3 -C8)cycloalkyloxy, (C4 -C8)cycloalkenyloxy, (6) heterocyclyl sclected from the group consisting of monocyclic radicals and fused polycycuic radicals, wherein said radicals contain a total of from 5 to 14 ring atoms, wherein said radicals contain a total of from 1 to 4 ring heteroatoms independently selocted from oxygen, nitrogen, and sulfur, and wherein the individual rings of said radicals may be independendy satated, partally unsaturated, or aromatic, provided that if X is CH2, Z is H or is selected from groups (4) and (6), wherein, when Z contains one or more rings, said rings may each independently bear 0 to 4 substituents independently selected from halo, hydroxy, cyano, nitro, oxo, thioxo, aminosulfonyl, phenyl phenoxy, phenylthio, halophenylthio, benzyl, benzyloxy, (C1 -C10)alkyl, (C1 -C10)alkoxy, (C1 -C10)alkoxycarbonyl, (C1 -C10)althyltio, (C1 -C10)altylamino, (C1 -C10)alkylaminocarbonyl, di(C1 -C10)alkylamino, di(C1 -C10)alkylaminocarbonyl, di(C1 -C10)alkyo(C1 -C10)alkoxy, (C1 -C3)perfluoroalkyl, (C1 -C3)perfluoroalkoxy, (C1 -C10)acyl, (C1 -C10)acyloxy, (C1 -C10)acyloxy(C1 -C10)alkyl, and pyrrolidinyl; and pharmaceutically acceptable salts thereof.
