285139-04-0

Upstream product

• 50-01-1 guanidine hydrochloride 
• 27514-08-5 N-(4-oxocyclohexyl)acetamide 
• 90978-87-3 trans-4-(acetylamino)cyclohexyl acetate 
• 27489-60-7 N-((trans)-4-hydroxycyclohexyl)acetamide 
• 27489-62-9 trans-4-hydroxycyclohexylamine 

Relevant academic research and scientific papers

POTENT SMALL MOLECULE INHIBITORS OF AUTOPHAGY, AND METHODS OF USE THEREOF

Certain aspects of the invention relate to small molecule autophagy inhibitors, and their use for treatment and prevention of cancers and acute pancreatitis. Medicinal chemistry studies led to small molecular autophagy inhibitors with improved potency and selectivity.

Thrombin inhibitors

The invention relates to compounds of formula I D—CO—B—A-Het and pharmaceutically acceptable salts thereof where substituents in description have the specified meanings. The compounds are used as thrombin inhibitors.

Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics

The design, synthesis and biological activity of non-covalent thrombin inhibitors incorporating 4,5,6,7-tetrahydroindazole, 2-methyl-4,5,6,7-tetrahydroindazole, 4,5,6,7-tetrahydroisoindole, 5,6,7,8-tetrahydroquinazoline and 5,6,7,8-tetrahydroquinazolin-2-amine as novel, partially saturated, heterobicyclic P1-arginine side-chain mimetics is described. The binding mode of the most potent candidate in the series co-crystallized with human α-thrombin, which exhibited an in vitro Ki of 140 nM and more that 478-fold selectivity against trypsin, is discussed.

Synthesis of 2-amino-7,8-dihydro-6(5H)-quinazolinone, 2,4-diamino-7,8- dihydro-6(5H)-quinazolinone, 5,6,7,8-tetrahydro-2,6-quinazolinediamine and 5,6,7,8-tetrahydro-2,4,6-quinazolinetriamine derivatives

N-(2-Amino-5,6,7,8-tetrahydro-6-quinazolinyl)acetamide (9) and N-(2,4- diamino-5,6,7,8-tetrahydro-6-quinazolinyl)acetamide (6) were synthesized from N-(4-oxocyclohexyl)acetamide (5) as novel peptidomimetic building blocks. With similar purpose, N-(6-oxo-5,6,7,8-tetrahydro-2-quinazolinyl)acetamide (18) and N-[2-(acetylamino)-6-oxo-5,6,7,8-tetrahydro-4-quinazolinyl]acetamide (14) were prepared from cyclohexane-1,4-dione monoethylene ketal (11).