Patents Represented by Attorney, Agent or Law Firm Brian Lewis
  • Patent number: 4792561
    Abstract: The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein:X is chosen from the group consisting of: ##STR2## and a covalent bond in which R.sup.1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R.sup.2 is H or OH, or R.sup.1 and R.sup.2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene;R.sup.3 is H or alkyl having 1-6 carbon atoms, R.sup.4 is H and R.sup.3 and R.sup.4 are either cis or trans to each other, or R.sup.3 and R.sup.4 taken together represent a covalent bond;n is an integer from 0-3;Het is 1-imidazolyl or 3-pyridyl; and the dotted line represents an optional covalent bond.
    Type: Grant
    Filed: May 29, 1986
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Keith A. M. Walker, John J. Bruno, Gregory R. Martinez
  • Patent number: 4791108
    Abstract: Compounds of formulas (1) and (2): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenendioxy or ethylene-1,2-dioxy, andR is lower alkyl, optionally substituted phenyl, --(CH.sub.2).sub.m OR.sup.1 or --NR.sup.1 R.sup.2 wherein m is an integer of 1 to 6 and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or --NR.sup.1 R.sup.2 taken together is a heterocycle of the formula: ##STR2## wherein A is --CH.sub.2 --, --NR.sup.1 -- or oxygen, or a pharmaceutically acceptable salt thereof, are useful as .alpha..sub.2 -blockers, especially as antidepressants.
    Type: Grant
    Filed: April 13, 1987
    Date of Patent: December 13, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Robin D. Clark
  • Patent number: 4786652
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy,R.sup.2 is the same as R.sup.1, or R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl,R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X is the same and is either --C(O)OR.sup.4 or --C(O)NR.sup.5 R.sup.6,whereinR.sup.4 is alkyl, phenyl or benzyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl, cycloalkyl or phenyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: November 22, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti
  • Patent number: 4766127
    Abstract: The invention concerns a method of inhibiting thromboxane synthetase with a compound of the formula: ##STR1## or a pharmaceutically acceptable salt or ester thereof, in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclinthromboxane levels.
    Type: Grant
    Filed: February 10, 1987
    Date of Patent: August 23, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gregory R. Martinez, John J. Bruno
  • Patent number: 4761420
    Abstract: Compound of formula 1 are calcium entry antagonists useful for treating hypertension, congestive heart failure, angina, and vasospastic disorders: ##STR1## wherein n is an integer from 1 to 4;R.sub.1 and R.sub.2 are lower alkyl;R.sub.3 is lower alkyl or alkoxyalkyl;A is alkylene of two to eight carbon atoms;X.sub.1 and X.sub.2 are each independently --NO.sub.2, --CF.sub.3, CH.sub.3 O--, --CN, --H, lower alkyl or halo;Y is --O--, --S--, --S(O)--, or --S(O).sub.2 --; andR is H, lower alkyl, cycloalkyl, alkoxyalkyl, cycloalkyloxy-alkyl, alkoxycycloalkyl, acyl, or saturated or unsaturated 5- or 6-membered heterocyclyl optionally substituted with lower alkyl or alkoxy, wherein the heteroatom is one oxygen atom.
    Type: Grant
    Filed: June 13, 1986
    Date of Patent: August 2, 1988
    Assignee: Laboratoires Syntex S.A.
    Inventor: Gilles Genain
  • Patent number: 4758587
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X and Y are different and are either R.sup.4 or --C(O)W whereinR.sup.4 is lower alkyl or optionally substituted phenyl-lower-alkyl;W is --OR.sup.5 or --NR.sup.6 R.sup.7,whereinR.sup.5 is alkyl, optionally substituted phenyl or optionally substituted benzyl; andR.sup.6 and R.sup.7 are independently hydrogen, lower alkyl, cycloalkyl or optionally substituted phenyl.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: July 19, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti
  • Patent number: 4735966
    Abstract: Compounds useful in treating cardiovascular disorders such as thrombosis, hypertension and atherosclerosis are depicted in formulas (1), (2) and (3): ##STR1## wherein: A is --C.tbd.C--, trans --HC.dbd.CH--, --CH.sub.2 CH.sub.2 -- or --CH.dbd.CHCH.sub.2 --;X is lower alkoxy, hydroxy, or (2,2,2)-trifluoroethoxy;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);is an integer of 2-4;R.sub.1 is --CH.sub.2 OH, --CHO, --CO.sub.2 R or --CO.sub.2 H, and the olefin formed by the R.sub.1 (CH.sub.2).sub.n CH.dbd. moiety is either (E) or (Z);R.sub.2 is hydrogen or methyl, or optionally --CH.dbd.CH.sub.2 when A is --CH.dbd.CHCH.sub.2 --; andR.sub.3 is linear or branched alkyl, alkenyl or alkynyl having 5-10 carbon atoms, ##STR2## --(CH.sub.2).sub.m -phenyl or CH.sub.
    Type: Grant
    Filed: August 25, 1986
    Date of Patent: April 5, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Helen Y. Wu, Walter Kurz
  • Patent number: 4713382
    Abstract: Compounds having the formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the definitions given herein, are useful as antiarrhythmic agents.
    Type: Grant
    Filed: May 30, 1985
    Date of Patent: December 15, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Jean-Claude Pascal
  • Patent number: 4670465
    Abstract: Long chain unsaturated hydrocarbon derivatives, having from 13 to 21 carbon atoms, which are substituted at the 1-position by a phenoxy, phenylthio or a phenyl that bear a carboxylic acid group at the ortho, meta or para positions, and up to 4 carbon-carbon triple bonds, methods of preparing them, and pharmaceutical preparations containing them. These compounds are useful as lipoxygenase inhibitors, and therefore as antiinflammatory agents.
    Type: Grant
    Filed: May 21, 1986
    Date of Patent: June 2, 1987
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Angel Guzman, Joseph M. Muchowski