849833-55-2

Upstream product

• 107-12-0 propiononitrile 

Downstream Products

• 721952-76-7 3-{3-[4-(3-ethyl-1,2,4-oxadiazol-5-yl)-1-piperidinyl]propyl}-5,5-bis(4-fluorophenyl)-2-methyl-3,5-dihydro-4H-imidazol-4-one 
• 50737-34-3 5-chloromethyl-3-ethyl-[1,2,4]oxadiazole 
• 1596358-16-5 3-ethyl-5-(4'-nitrophenyl)-1,2,4-oxadiazole 
• 1046536-29-1 C₁₈H₃₁N₃O₄ 
• 22354-96-7 3-ethyl-5-phenyl-1,2,4-oxadiazole 
• 1035263-85-4 4-[(4-Chlorophenyl)methyl]-2-({(2R)-1-[2-(3-ethyl-1,2,4-oxadiazol-5-yl)ethyl]-2-pyrrolidinyl}methyl)pyrido[3,4-d]pyridazin-1(2H)-one 
• 1204315-98-9 4-{3-[1-(3-ethyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]propoxy}-2-methyl-benzoic acid methyl ester 
• 1163127-01-2 1-((3-ethyl-[1,2,4]oxadiazol-5-yl)(phenyl)methyl)-4-(2-fluoro-4-nitrophenyl)piperazine 
• 1163248-70-1 5-(4-bromo-3-fluorophenyl)-3-ethyl-[1,2,4]oxadiazole 

Relevant academic research and scientific papers

Optimization of Novel 1-Methyl-1 H-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber's Pole Worm

A phenotypic screen of a diverse library of small molecules for inhibition of the development of larvae of the parasitic nematode Haemonchus contortus led to the identification of a 1-methyl-1H-pyrazole-5-carboxamide derivative with an IC50 of 0.29 μM. Medicinal chemistry optimization targeted modifications on the left-hand side (LHS), middle section, and right-hand side (RHS) of the scaffold in order to elucidate the structure-activity relationship (SAR). Strong SAR allowed for the iterative and directed assembly of a focus set of 64 analogues, from which compound 60 was identified as the most potent compound, inhibiting the development of the fourth larval (L4) stage with an IC50 of 0.01 μM. In contrast, only 18% inhibition of the mammary epithelial cell line MCF10A viability was observed, even at concentrations as high as 50 μM.

Synthesis and methemoglobinemia-inducing properties of benzocaine isosteres designed as humane rodenticides

A number of isosteres (oxadiazoles, thiadiazoles, tetrazoles and diazines) of benzocaine were prepared and evaluated for their capacity to induce methemoglobinemia - with a view to their possible application as humane pest control agents. It was found that an optimal lipophilicity for the formation of methemoglobin (metHb) in vitro existed within each series, with 1,2,4-oxadiazole 3 (metHb% = 61.0 ± 3.6) and 1,3,4-oxadiazole 10 (metHb% = 52.4 ± 0.9) demonstrating the greatest activity. Of the 5 candidates (compounds 3, 10, 11, 13 and 23) evaluated in vivo, failure to induce a lethal end-point at doses of 120 mg/kg was observed in all cases. Inadequate metabolic stability, particularly towards hepatic enzymes such as the CYPs, was postulated as one reason for their failure.

FUSED HETEROCYCLIC COMPOUND

The present invention relates to a fused heterocyclic compound having the Formula 1, which is useful as a platelet aggregation inhibitor, a method for preparing the same, and a pharmaceutical composition for inhibiting platelet aggregation comprising the same.

CYCLOAMINO DERIVATIVES AS GPR119 ANTAGONISTS

Therapeutic compounds are disclosed having the general formula (I) that are useful for the treatment of metabolic disorders, including type II diabetes. The compounds have activity as agonists of GPR119. Compounds having the stereochemistry of formula (la) may also demonstrate DPP-IV inhibitory activity.

FUSED HETEROCYCLIC RING COMPOUND

A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: wherein P: substituted 6-membered aromatic ring, Q: (substituted) 6-membered aromatic ring, A1: CR4aR4b, NR4c, O, S, SO or SO2 {R4a-4c: H etc.}, L1: (substituted) C1-5 alkylene, L2: a bond or (substituted) C1-3 alkylene, L3-4: (substituted) C1-3 alkylene, R1: H, X, CN, (substituted) hydrocarbon, (substituted) heterocycle or (substituted) OH, or (substituted) 4- to 8-membered (heterocyclic) ring together with A1, R2: H, CN, (substituted) hydrocarbon, and R3a: -COSRA1, (substituted) 5- or 6-membered aromatic ring {RA1: (substituted) hydrocarbon or (substituted) heterocycle}.

THIAZOLYL-DIHYDRO-CYCLOPENTAPYRAZOLE

Disclosed are compounds of general formula (I), wherein the groups R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures

THIAZOLYL-DIHYDRO-CHINAZOLINE

Disclosed are compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.

THIAZOLYL-DIHYDRO-INDAZOLE

Disclosed are compounds of general formula (I), wherein the groups R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-indazoles and the use thereof as pharmaceutical compositions.

2-ACYLAMINOTHIAZOLE DERIVATIVES

The Invention relates to compounds of the formula I, wherein the variables are as defined in the claims, for use as a medicament. The compounds are A2A-receptor legends and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.

INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE

Compounds of formula (I) in free or salt form, wherein R1, R2, R3, and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinos