N-ethyl-N-[3-(3-cyanopyrazolo[1,5-a]pyrimidine-7-yl)phenyl]acetamide (Zaleplon) can be produced by condensing 3-(N-acetyl-N-ethyl-amino)-.beta.-oxo-phenylpropanal sodium salt with 3-amino-4-cyanopyrazole. Said sodium salt can be produced by first treating 3-acetylamino-acetophenone with an alkali metal hydroxide, in particular with powdered potassium hydroxide and then with an ethylating reagent, in particular ethyl bromide and the N-(3-acetylphenyl)-N-ethyl-acetamide that is obtained is reacted...

A process of preparing a compound of the formula (I) ##STR00001## wherein B is chosen from OH, NH.sub.2, NHR, H or halogen; D is chosen from OH, NH.sub.2, NHR, H halogen or SCH.sub.3; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof, which comprises ...

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical co...

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical co...

The present application is directed to a compound of Formula (I) as defined herein which are useful as kinase inhibitors.

Disclosed are novel crystalline 2-(1-isopropoxycarbonyloxy-2-methylpropyl)- -7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine and a pharmaceutical composition comprising the same.

The invention provides a compound of the formula: ##STR00001## wherein A is selected from N, CH and CR; R is selected from halogen, optionally substituted alkyl, aralkyl and aryl, OH, NH.sub.2, NHR.sup.1, NR.sup.1R.sup.2 and SR.sup.3; R.sup.1, R.sup.2 and R.sup.3 are each optionally substituted alkyl, aralkyl or aryl groups; B is selected from NH.sub.2 and NHR.sup.4; R.sup.4 is an optionally substituted alkyl, aralkyl or aryl group; X is selected from H, OH and halogen; Z is selected from H, Q, ...

The present invention relates to 5-aminomethylpyrazolo[4,3-d]pyrimidines of the general formula (I) ##STR00001## in which the radicals R.sup.1 to R.sup.6 have the meaning indicated in the text. The compounds show phosphodiesterase V inhibition and can be employed for the treatment of conditions of the cardiovascular system and for the treatment of potency disorders.

The invention relates to a method for the production of 2-phenyl-substituted imidazotriazinones of general formula (I), comprising the reaction of compounds of formula (II) with compounds of formula (III) and subsequent reaction with iodine or bromine, then with a metal cyanide and reaction with an acid.

The invention relates to a process for the preparation of zaleplon (N-[3(3-cyanopyrazolo[1,5-a]pyrim-idin-7-yl)phenyl]-N-ethyl-accramide) in the reaction of 3-dimethylamino-1-(3-N-ethyl-N-acetylamirnophenyl)-2-propen-1-one with 3-aminopyrazole-4-carbonitrile, which comprises carrying out said reaction in an aqueous solution of formic acid at formic acid concentrations in the range of 20 80% (w/w). Zaleplon is useful as an anxiolytic, a sedactive and a skeletal muscle relaxant.