Category «Preclinical»

Synthesis of 4-Heteroaryl–Quinazoline Derivatives as Potential Anti-breast Cancer Agents

It’s only fair to share… Ethyl 2-[(6,7-dimethoxyquinazolin-4-yl)amino]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate (15b) Yield: 76%; mp: 254–256°C; IR (cm−1): 3200 (NH), 2974, 2854 (CH-aliphatic), 1656 (C=O); 1H NMR (DMSO-d6) δ ppm 1.03 (t, 3H, CH3CH2, J = 7.2 Hz), 1.21 (t, 2H, CH2, J = 6.9 Hz), 2.88 (t, 2H, CH2, J = 6.9 Hz), 3.40 (q, 2H, CH2, J = 6.9 Hz), 3.88 (s, 3H, OCH3), 3.91 (s, 3H, OCH3), 3.96 …

JNJ 54166060

It’s only fair to share… JNJ 54166060 JNJ-54166060; JNJ 54166060; JNJ54166060. (R)-(2-chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl)methanone [2-chloro-3-(trifluoromethyl)phenyl]-[(4R)-1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanone Methanone, [2-chloro-3-(trifluoromethyl)phenyl][(4R)-1-(5-fluoro-2-pyridinyl)-1,4,6,7-tetrahydro-4-methyl-5H-imidazo[4,5-c]pyridin-5-yl]- CAS 1627900-41-7 OF R ISOMER  DESIRED CAS 1627900-42-8 OF S ISOMER Chemical Formula: C20H15ClF4N4O Exact Mass: 438.0871 JNJ-54166060 is a potent P2X7 antagonist. Bioactivity data of JNJ-54166060: rP2X7 IC50=4 nM; rP2X7 IC50=115nM; HLM/RLM = 0.35/0.64, ED50 = 2.3 mg/kg in rats. JNJ-54166060 …

(3S)-3-[(2-amino-5-methoxypyrimidin-4-yl)amino]heptan-1-ol for the treatment of viral infections

It’s only fair to share… (3S)-3-[(2-amino-5-methoxypyrimidin-4-yl)amino]heptan-1-ol cas  1402802-45-2 JNJ ? WO 2012136834, WO 2014053595 for the treatment of viral infections Molecular Formula: C12H22N4O2 Molecular Weight: 254.32868 g/mol Inventors Gowan David Mc, Pierre Jean-Marie Bernard Raboisson, Werner Embrechts, Tim Hugo Maria Jonckers, Stefaan Julien Last, Serge Maria Aloysius Pieters, Jaromir Vlach,  Applicant Janssen R&D Ireland   (3S)-3-[(2-amino-5-methoxypyrimidin-4-yl)amino]heptan-1-ol Mark Hicken, …

IPI-549

It’s only fair to share… IPI-549 CAS 1693758-51-8 MF : C30H24N8O2 Molecular Weight: 528.576 (S)-2-amino-N-(1-(8-((1-methyl-1H-pyrazol-4-yl)ethynyl)-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl)ethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide 2-amino-N-[(1S)-1-[8-[2-(1-methylpyrazol-4-yl)ethynyl]-1-oxo-2-phenylisoquinolin-3-yl]ethyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide Company Infinity Pharmaceuticals Inc. Description Small molecule inhibitor of phosphoinositide 3-kinase (PI3K) gamma Molecular Target Phosphoinositide 3-kinase (PI3K) gamma Mechanism of Action Phosphoinositide 3-kinase (PI3K) gamma inhibitor Therapeutic Modality Small molecule Latest Stage of Development Phase I Standard Indication Solid …

DDD 107498

It’s only fair to share… DDD 107498, DDD 498 PATENT WO 2013153357,  US2015045354 6-Fluoro-2-[4-(morpholinomethyl)phenyl]-N-(2-pyrrolidin-1-ylethyl)quinoline-4-carboxamide 6-Fluoro-2-[4-(4-morpholinylmethyl)phenyl]-N-[2-(1-pyrrolidinyl)ethyl]-4-quinolinecarboxamide 4-Quinolinecarboxamide, 6-fluoro-2-[4-(4-morpholinylmethyl)phenyl]-N-[2-(1-pyrrolidinyl)ethyl]- CAS 1469439-69-7 CAS 1469439-71-1 SUCCINATE MF C27H31FN4O2 MW 462.559043 g/mol 6-fluoro-2-[4-(morpholin-4-ylmethyl)phenyl]-N-(2-pyrrolidin-1-ylethyl)quinoline-4-carboxamide Originator Medicines for Malaria Venture; University of Dundee Class Small molecules Mechanism of Action Protein synthesis inhibitors Highest Development Phases No development reported Malaria Most Recent Events 16 Jul 2016 No recent reports of development identified for …

PF-04745637

It’s only fair to share…   PF-04745637 cas 1917294-46-2 MW 509.00, MF C27 H32 Cl F3 N2 O2 Cyclopentanecarboxamide, 1-(4-chlorophenyl)-N-[2-[4-hydroxy-4-(trifluoromethyl)-1-piperidinyl]-3-phenylpropyl]- rac-1-(4-Chlorophenyl)-N-f2-r4-hvdroxy-4-(trifluoromethyl)piperidin-1-vn-3-phenylpropyDcyclopentanecarboxamide PRODUCT PATENT WO-2016067143-A1 Applicants: PFIZER INC. [US/US]; 235 East 42nd Street New York, New York 10017 (US) Inventors: SWAIN, Nigel Alan; (GB). PRYDE, David Cameron; (GB). RAWSON, David James; (GB). RYCKMANS, Thomas; (GB). SKERRATT, Sarah Elizabeth; (GB). …

Novel, isoform-selective inhibitor of histone deacetylase 8 (HDAC8),

It’s only fair to share… CAS 1620779-53-4 MF C22H20N4O2, MW 372.4 (S)-2-(5-(cyclopropylethynyl)-4-phenyl-1H-1,2,3-triazol-1-yl)-N-hydroxy-3-phenylpropanamide 1H-1,2,3-Triazole-1-acetamide, 5-(2-cyclopropylethynyl)-N-hydroxy-4-phenyl-α-(phenylmethyl)-, (αS)- Applicants: TRUSTEES OF BOSTON UNIVERSITY DANA-FARBER CANCER INSTITUTE, INC. Inventors: Aaron Beaty BEELER John A. PORCO, JR. Oscar J. INGHAM James E. BRADNER As histone proteins bind DNA prior to transcription, their biochemical action plays a critical role in the regulation …

AZD 2716

It’s only fair to share… AZD2716 CAS 1845753-81-2 MF C24 H23 N O3,   MW 373.44 [1,1′-Biphenyl]-3-propanoic acid, 2′-(aminocarbonyl)-α-methyl-5′-(phenylmethyl)-, (αR)- Antiplaque candidate drug AstraZeneca INNOVATOR (R)-7(AZD2716) a novel, potent secreted phospholipase A2 (sPLA2) inhibitor with excellent preclinical pharmacokinetic properties across species, clear in vivo efficacy, and minimized safety risk. Based on accumulated profiling data, (R)-7 was selected …