752244-29-4

Upstream product

• 16000-13-8 2,6-dimethyl-2,3-dihydro-pyranone 
• 1004-36-0 2,6-dimethylpyrone 
• 64-17-5 ethanol 
• 190912-17-5 (R)-2-methyl-2,3-dihydro-4H-pyran-4-one 
• 676-58-4 methylmagnesium chloride 
• 869293-25-4 (R)-5-((tert-butyldimethylsilyl)oxy)hex-1-en-3-one 
• 33747-09-0 (2R,4S,6S)-2,6-dimethyltetrahydro-2H-pyran-4-ol 
• 155206-70-5 (4E)-4-Ethoxyhepta-4,6-dien-2-ol 
• 122222-69-9 5-t-butoxycarbonyl-2,6-dimethyl-2,3-dihydro-4H-pyran-4-one 

Downstream Products

• 677028-16-9 4-(2'-hydroxy-1'R-phenylethyl)-2R,7S-dimethyl[1,4]oxazepan-5-one 
• 10341-27-2 (+/-)-cis-2,7-dimethyl[1,4]oxazepan-5-one 
• 1141822-61-8 (1R,2S,5R)-8-phenylmenthyl (2R,4S,7S)-4-benzyl-2,7-dimethyl-5-oxooxepane-4-carboxylate 
• 1620450-76-1 C₁₈H₂₃NO₅ 

Relevant academic research and scientific papers

Optimization of Orally Bioavailable PI3KδInhibitors and Identification of Vps34 as a Key Selectivity Target

Optimization of a lead series of PI3Kδinhibitors based on a dihydroisobenzofuran core led to the identification of potent, orally bioavailable compound 19. Selectivity profiling of compound 19 showed similar potency for class III PI3K, Vps34, and PI3Kδ, and compound 19 was not well-tolerated in a 7-day rat toxicity study. Structure-based design led to an improvement in selectivity for PI3Kδover Vps34 and, a focus on oral phramacokinetics properties resulted in the discovery of compound 41, which showed improved toxicological outcomes at similar exposure levels to compound 19.

INHIBITOR OF BTK AND MUTANTS THEREOF

The disclosure includes compounds of Formula (I) (1) wherein Q0, Q1, Q2, Q3, Q4, Z, W, i, j, m, n, Warhead, R0, R1, R3, R4, R5, R6, and R7, are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.

Discovery of MK-6169, a Potent Pan-Genotype Hepatitis C Virus NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Substitutions

We describe the discovery of MK-6169, a potent and pan-genotype hepatitis C virus NS5A inhibitor with optimized activity against common resistance-associated substitutions. SAR studies around the combination of changes to both the valine and aminal carbon region of elbasvir led to the discovery of a series of compounds with substantially improved potency against common resistance-associated substitutions in the major genotypes, as well as good pharmacokinetics in both rat and dog. Through further optimization of key leads from this effort, MK-6169 (21) was discovered as a preclinical candidate for further development.

PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS

The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

A Scalable Synthesis of (R,R)-2,6-Dimethyldihydro-2H-pyran-4(3H)-one

A scalable synthesis of (R,R)-2,6-dimethyldihydro-2H-pyran-4(3H)-one is reported. Key to this strategy is the Ti(OiPr)4-catalyzed Kulinkovich cyclopropanation of silyl protected (R)-ethyl 3-hydroxybutanoate, and subsequent oxidative fragmentati

HETEROCYCLE-SUBSTITUED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES

The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A', R 2 R 3, R 4 and R are as defined herein. The present i

THIAZOLYL-SUBSTITUED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES

The present invention relates to novel Thiazolyl-Substituted Tetracyclic Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, A', R2R3, R4 and R5 are as defined herein. The present

THIOPHENE-SUBSTITUTED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES

Thiophene-substituted tetracyclic compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein A, A', R2, R3, R4 and R5 are as defined herein. The compositions comprising at least one thiophene-substituted tetracyclic compound, and methods of using the thiophene-substituted tetracyclic compounds for treating or preventing HCV infection in a patient are also provided.

APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES

Disclosed herein are compounds that inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases using the compounds.

PHENYL-HETEROARYL AMINE COMPOUNDS AND THEIR USES

The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I, and pharmaceutical compositions comprising such compounds