1239465-20-3

Upstream product

• 54716-02-8 ethyl (E)-3-(1-pyrrolidino)-2-butenoate 
• 5775-76-8 valeraldoxime 

Downstream Products

• 1254962-95-2 6-[(3-butyl-5-methyl-isoxazol-4-ylmethyl)-amino]-nicotinic acid methyl ester 
• 1254966-38-5 5-[3-butyl-5-(1,2-dihydroxy-2-phenyl-ethyl)-isoxazol-4-ylmethoxy]-2-methyl-2H-pyrazole-3-carboxylic acid methyl ester 
• 1246924-89-9 [3-Butyl-5-([E]-styryl)-isoxazol-4-yl]-methanol 
• 1246924-88-8 3-butyl-5-([E]-styryl)-isoxazole-4-carboxylic acid 

Relevant academic research and scientific papers

ISOXAZOLE-ISOXAZOLES AND ISOXAZOLE-ISOTHIAZOLES

The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.

ISOXAZOLES / O-PYRIDINES WITH ETHYL AND ETHENYL LINKER

The present invention is concerned with novel isoxazole-pyridines of formula I wherein R1, R2, R3 and L are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the

ISOXAZOLE DERIVATIVES

The present invention is concerned with novel isoxazole derivatives of formula (I), wherein X, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A α5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as medicaments.

ISOXAZOLE-PYRIDAZINE DERIVATIVES

The present invention is concerned with isoxazole-pyridazine derivatives of Formula (I), having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.

ISOXAZOLE-PYRAZOLE DERIVATIVES

The present invention is concerned with isoxazole-pyrazole derivatives of formula I, having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.

ISOXAZOLE-PYRIDINE DERIVATIVES AS GABA MODULATORS

The present invention is concerned with novel isoxazole derivatives of formula (I) wherein X, R1, R2, R3 and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A α5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula (I), pharmaceutical compositions containing them and their use as medicaments.

PHARMACEUTICAL FORMULATION FOR TREATING CARDIOVASCULAR DISEASE

The present invention provides a pharmaceutical formulation comprising: an early release portion comprising as a pharmaceutical active ingredient a statin-based hypolipidic agent, an isomer thereof, or a pharmaceutically acceptable salt thereof; and a slow release portion comprising as a pharmaceutical active ingredient a dihydropyridine-based calcium channel blocking agent, an isomer thereof, or a pharmaceutically acceptable salt thereof. When compared with a single formulation of each of the drugs or a simple combination formulation of the drugs, the pharmaceutical formulation according to the present invention comprising an early release portion comprising a statin-based hypolipidic agent and a slow release portion comprising a dihydropyridine-based calcium channel blocking agent is pharmaceutically, scientifically, and economically very useful in preventing or treating cardiovascular disease, pulmonary heart disease, pulmonary disease, or kidney disease of patients who have a metabolic syndrome, insulin resistance, diabetes, or prediabetes. The formulation of the present invention is effective in preventing antagonistic and side effects between the drugs by making the dissolution rate of the statin-based hypolipidic agent different from that of the dihydropyridine-based calcium channel blocking agent, and in facilitating patient compliance in taking the drugs by administering the two different drugs simultaneously.