CAVALLA, DAVID (Total 234 Patents Found)

Disclosed is a compound of the formula (I): wherein R 3 , R 6a and R 8 are the same or different and represent a C 2-8 alkyl which is unbranched or branched and unsubstituted or substituted; C 3-8 cycloalkyl which is unsubstituted or substituted; C 4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubs...
Novel compounds which are effective PDE IV inhibitors are disclosed The compounds possess similar or improved PDE IV inhibition as compared to rolipram, with improved selectivity with regard to, e.g., PDE III inhibition. Preferred compounds are 3-(3-cyclopentyloxy-4-methoxy-benzylamino)-4-hydroxymethyl pyrazole and 3-(...
Disclosed are compounds of formula (I), wherein R1, R3 and R8 are independently alkyl, aryl or aralkyl, and R2 is selected from the group consisting of S and O, R6 is selected from the group consisting of S and O, provided that R2 and R6 are not both O. The compounds are effective PDE IV inhibitors and possess improved...
The present invention comprises a method of synthesizing compounds having the formula (I): ##STR1## wherein: Z, R 1 , R 2 , R 3 , R 4 and R 8 are defined herein, which comprises the steps of (a) reacting a compound of the formula (II) ##STR2## wherein Q is a halogen, with an effective amount of a compound selec...
Disclosed are compounds having formula (I) or (II), wherein: Q3, Q6a, Q6b and Q8 are independently a bond, C1-8 alkylene, C2-8 alkenylene and C2-8 alkynylene, and R3, R6a, R6b and R8 are independently hydrogen, aryl or heteroaryl, optionally substituted by halogen, hydroxy, alkoxy, nitro, cyano and carboxy, provided th...
Novel compounds which are effective PDE IV inhibitors are disclosed. These compounds have the general structure of: ##STR1## where R 1 , R 2 , R 3 , R 4 , X 1 , X 2 and Z are described herein. The compounds possess improved PDE IV inhibition as compared to rolipram as well as with improved selectivity with regard to P...
Rolipram-based PDE IV inhibitors containing phenyl- or benzyl-substituted moieties of the formula: ##STR1## wherein X 1 and X 2 may be the same or different and each is O or S; R 1 is selected from the group consisting of hydrogen, saturated or unsaturated straight-chain or branched C 2-12 alkyl groups, cyclo...
Disclosed is a process for the preparation of a compound of Formula IV having the structure: ##STR1## wherein R 6 is N(R 6a )(R 6b ); R 3 represents a C 2-8 , alkyl which is unbranched or branched and unsubstituted or substituted; C 3-8 cycloalkyl which is unsubstituted or substituted; C 4-8 cycloalkylalkyl w...
Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram as well as with improved selectivity with regard to PDE III inhibition. In certain aspects of the invention, the compounds also demonstrate PDE V inhibition. Phar...
A compound of the formula: wherein R 3 represent a C 1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO 2 H, ═NOH, ═NOCONH 2 , or ═O; C 3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO 2 H, ═NOH, ═NOC...
Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE V inhibition. The present invention includes compounds of Formula I: wherein th...
The invention relates to compounds of the general formula (I): ##STR1## wherein R 1 and R 2 together form a C 3-5 alkylene chain and R 3 is a hydrogen atom; or R 1 and R 3 together form a C 2-4 alkylene chain and R 2 is a hydrogen atom; A-B represents the group R 4 R 5 C--CH 2 or R 4 C═CH; ...
Novel compounds which are effective PDE IV inhibitors are disclosed. The present invention is directed to compounds having the general formula I ##STR1## wherein: X is a halogen; Q is --CH 2 --CH 2 --, --CH 2 --, a single or a double bond, or --NR 1 --; R 1 is a C 3-7 monocyclic ring structure contain...
Disclosed are compounds having formula (I) or (II), wherein: Q3, Q6a, Q6b and Q8 are independently a bond, C1-8 alkylene, C2-8 alkenylene and C2-8 alkynylene, and R3, R6a, R6b and R8 are independently hydrogen, aryl or heteroaryl, optionally substituted by halogen, hydroxy, alkoxy, nitro, cyano and carboxy, provided th...
The present invention comprises a method of synthesizing compounds of formula (I): wherein Z, R 1 , R 2 , R 3 , R 4 and R 8 are as described herein; comprising the steps of. (a) reacting a compound of the formula (II) ##STR1## with an effective amount of ethyl cyanoacetate to form a compound of the formula (III...