213262-06-7

Upstream product

• 6160-65-2 1,1'-Thiocarbonyldiimidazole 
• 198821-79-3 3-methoxy-4-(1,3-oxazol-5-yl)aniline 
• 102368-13-8 1,1'-Thiocarbonyldi-2(1H)-pyridone 
• 198821-78-2 5-(2-methoxy-4-nitrophenyl)-oxazole 
• 198821-77-1 (2-methoxy-4-nitrophenyl)methylene diacetate 

Downstream Products

• 639458-85-8 2-amino-N-(2-(2-(3-methoxy-4-oxazol-5-yl-phenylamino)-oxazol-5-yl)-benzyl)-N-methyl-acetamide 
• 267648-04-4 N-(2-Hydroxy-2-phenylethyl)-N'-[3-methoxy-4-(5-oxazolyl)phenyl]thiourea 
• 267647-89-2 (3-methoxy-4-oxazol-5-yl-phenyl)-thiourea 
• 437655-88-4 2-(acetyloxy)-N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methylacetamide 

Relevant academic research and scientific papers

A new efficient synthesis of 5-aryloxazoles from arylidene diacetates and application to the preparation of BMS-337197, a novel IMPDH inhibitor

A new method for the synthesis of 5-aryloxazoles is described. Treatment of arylidene diacetates with one equivalent of TosMIC reagent in the presence of excess of potassium carbonate in methanol afforded 5-aryloxazoles in "one-pot" in 90-94%. Heteroaryli

Compounds derived from an amine nucleus and pharmaceutical compositions comprising same

Compounds having the formula (I), are effective as inhibitors of IMPDH enzyme and/or serine protease Factor VIIa, wherein B is a monocyclic or bicyclic carbocyclic or heterocyclic ring, D is a monocyclic or bicyclic carbocyclic or heterocyclic ring except when A is a heterocyclic ring, then D is a heterocyclic ring system, R is hydrogen or C1-4alkyl, and A, R1, R2and R4are as defined in the specification.

USE OF COMPOUNDS HAVING AN AMINE NUCLEUS IN MANUFACTURE OF A MEDICAMENT USEFUL FOR TREATING FACTOR VIIA-ASSOCIATED CONDITIONS

Use of at least one compound having the formula (I), or a pharmaceutically-acceptable salt, hydrate or prodrug thereof, in the manufacture of a medicament useful for treating conditions associated with the activity of Factor VIIa is described.

Compounds derived from an amine nucleus and pharmaceutical compositions comprising same

Compounds having the formula (I), are effective as inhibitors of IMPDH enzyme and/or serine protease Factor VIIa, wherein B is a monocyclic or bicyclic carbocyclic or heterocyclic ring, D is a monocyclic or bicyclic carbocyclic or heterocyclic ring except when A is a heterocyclic ring, then D is a heterocyclic ring system, R is hydrogen or C1-4alkyl, and A, R1, R2 and R4 are as defined in the specification.

Compounds derived from an amine nucleus that are inhibitors of IMPDH enzyme

The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH mediated diseases, such as transplant rejection and autoimmune diseases.

Novel guanidine-Based inhibitors of inosine monophosphate dehydrogenase

A series of novel guanidine-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for this new series of inhibitors is given.

A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase

A series of heterocyclic replacements for the central diamide moiety of 1, a potent small molecule inhibitor of inosine monophosphate dehydrogenase (IMPDH) were explored. The synthesis and the structure-activity relationships (SARs), derived from in vitro

Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]-amino]-5-oxazolyl]phenyl]-N- methyl-4-morpholinea0cetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity

Inosine monophosphate dehydrogenase (IMPDH) is a key enzyme that is involved in the de novo synthesis of purine nucleotides. Novel 2-aminooxazoles were synthesized and tested for inhibition of IMPDH catalytic activity. Multiple analogues based on this che

Inhibitors of IMPDH enzyme

The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases.