Abstract: Novel aroyl-substituted benzofuran and benzothiophene acetic and proprionic acids are disclosed herein. These compounds are useful as analgesic, anti-inflammatory, and antipyretic agents.
Abstract: Peptides which promote the release of growth hormone by the pituitary gland or which inhibit the release of growth hormone by growth hormone releasing factor and which have an N,N'-dialkyl substituted guanidino amino acyl residue at position 1 or 2 are disclosed herein.
Abstract: Process and novel intermediates for preparing 9-(1,3-dihydroxy-2-propoxymethyl)guanine and 2,6-diamino-9-(1,3-dihydroxy-2-propoxymethyl)purine and certain esters thereof. The present process and intermediates reduce the number of reaction steps to prepare these compounds as compared to prior processes. The products are useful as antiviral agents.
Type:
Grant
Filed:
February 23, 1984
Date of Patent:
November 4, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Julien P. H. Verheyden, John C. Martin, Daniel P. C. McGee
Abstract: Compounds useful as antiviral agents are defined by the following formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 and R.sup.2 are both --C(O)R.sup.7 wherein R.sup.7 is 1-adamantyl;R.sup.3 is amino;(a) R.sup.6 is hydrogen or amino and R.sup.4 together with R.sup.5 is a bond; or(b) R.sup.5 together with R.sup.6 is a keto group and R.sup.4 is hydrogen.
Abstract: Compounds useful as antiviral agents are defined by the following formula: ##STR1## wherein R.sup.1 is hydrogen, --C(Y)OR.sup.7 or --C(O)NHR.sup.7 wherein R.sup.7 is alkyl of one to twelve carbon atoms, alkenyl of two to twelve carbon atoms, cyclopentyl, cyclohexyl, phenyl or benzyl;R.sup.2 is --C(Y)OR.sup.7 or --C(O)NHR.sup.7 wherein R.sup.7 is as defined above;Y is oxygen or sulfur;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are as defined above or --NHC(O)R.sup.8 wherein R.sup.8 is as defined above and R.sup.4 together with R.sup.5 is a bond; or(b) R.sup.5 together with R.
Abstract: Novel 4-substituted-5-hydroxymethyl-1,2-cyclopentanediols or 1-cyclopentanol substituted at the 3-position by various heterocyclic groups are useful as antiviral agents.
Type:
Grant
Filed:
April 30, 1985
Date of Patent:
August 12, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Julien P. H. Verheyden, John C. Martin, G. V. Bindu Madhaven, Daniel P. C. McGee, Ernest J. Prisbe
Abstract: The compounds 9-(1,3-dihydroxy-2-propoxymethyl)guanine and the pharmaceutically acceptable salts thereof are useful as antiviral agents. The compound 1,3-dibenzyloxy-2-acetyloxy-methoxypropane is useful as an intermediate for the preparation of 9-(1,3-dihydroxy-2-propoxymethyl)guanine.
Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy, lower alkylthio, optionally substituted phenoxy or optionally substituted phenylthio,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2; andW is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl.
Type:
Grant
Filed:
December 22, 1983
Date of Patent:
June 3, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Gordon H. Jones, Michael C. Venuti, John M. Young
Abstract: An improved process for preparing the cyclic phosphate ester of substituted 9-(1,3-dihydroxy-2-propoxymethyl)purines which are useful as antiviral agents.
Abstract: This invention relates to compounds of the formula: ##STR1## wherein A is biphenyl unsubstituted or substituted on one or both rings with one or more halo, lower alkyl, lower alkoxy or trifluoromethyl substituents; Z is ethylene unsubstituted or substituted with a single lower alkyl substituent or propylene unsubstituted or substituted with one or two lower alkyl substituents; and the pharmaceutically acceptable acid addition salts thereof. These compounds have anticonvulsant activity.
Abstract: 1-Monophosphate esters, 1,3-bisphosphate esters and cyclic phosphate esters of 9-(1,3-dihydroxy-2-propoxymethyl)guanine are useful as antiviral agents.
Abstract: Compounds useful as antiviral agents are defined by the following formula: ##STR1## wherein R.sup.1 is hydrogen, --C(Y)OR.sup.7 or --C(O)NHR.sup.7 wherein R.sup.7 is alkyl of one to twelve carbon atoms, alkenyl of two to twelve carbon atoms, cyclopentyl, cyclohexyl, phenyl or benzyl;R.sup.2 is --C(Y)OR.sup.7 or --C(O)NHR.sup.7 wherein R.sup.7 is as defined above;Y is oxygen or sulfur;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are as defined above or --NHC(O)R.sup.8 wherein R.sup.8 is as defined above and R.sup.4 together with R.sup.5 is a bond; or(b) R.sup.5 together with R.
Abstract: Devices, of suitable form and size for insertion into the vagina of a female mammal, composed of a polymeric material which has, incorporated in it, a 1-substituted imidazole spermicide and a pharmaceutically acceptable chelating agent, and which release effective amounts of said spermicide while in place in the vaginal cavity, are useful as contraceptives.
Abstract: New compounds of the formula ##STR1## wherein: R.sup.1 is cycloalkyl of five to seven carbon atoms optionally substituted with one or more lower alkyl groups;R.sup.2 is alkyl of two to twelve carbon atoms, cycloalkyl of five to seven carbon atoms, or cycloalkylalkyl of six to ten carbon atoms wherein the cycloalkyl group may be optionally substituted with one or more lower alkyl groups;R.sup.3 is hydrogen or lower alkyl;a is 0, 1, 2 or 3; andb is 1, 2 or 3;and the pharmaceutically acceptable acid addition salts thereof are useful as spermicidal and spermatostatic agents.
Abstract: A compound useful as antifungal, antibacterial and antiprotozoal agents and as spermicides have the formula ##STR1## and the acid addition salts thereof wherein Z is oxygen or sulfur;m is 0, 1, 2 or 3;n is 1, 2 or 3;R.sup.1 is hydrogen; alkyl; cycloalkyl; cycloalkyl-lower-alkyl; optionally substituted phenyl; phenyl-lower-alkyl; monocyclic heteroaromatic ring; monocyclic heteroaromatic-lower-alkyl; naphthyl; or naphthyl-lower-alkyl.A and B are independently hydrogen, halo, lower alkyl or lower alkoxy and either one of A or B may be nitro, amino or alkanoylamino;Q is (a) NR.sup.2 R.sup.3 or (b) NR.sup.4 C(X)YR.sup.5 whereinX is oxygen or sulfur;Y is oxygen, sulfur, NR.sup.6 or a bond;R.sup.2 is hydrogen; alkyl; cycloalkyl; cycloalkyl-lower-alkyl; optionally substituted phenyl or optionally substituted phenyl-lower-alkyl;R.sup.3 is hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together with N is a five or six membered optionally substituted ring;R.sup.4 and R.sup.6 are independently hydrogen or lower alkyl;R.
Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are lower alkoxy or lower alkylthio;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, halo, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and n is 0, 1 or 2; andW is alkyl of one to seven carbon atoms.
Type:
Grant
Filed:
October 27, 1982
Date of Patent:
August 21, 1984
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Gordon H. Jones, Michael C. Venuti, Young, John M.
Abstract: Psoriasis in mammals is relieved by topically administering naphthoquinones of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are lower alkoxy; andR.sup.3 is halo or cyano.
Abstract: 1-Substituted imidazole derivatives exhibit spermatostatic and spermatocidal activity and are useful for contraceptive purposes both in male and female mammals.
Type:
Grant
Filed:
July 19, 1982
Date of Patent:
March 27, 1984
Assignee:
SYNTEX (U.S.A.) Inc.
Inventors:
Duane W. Hallesy, Richard E. Jones, Brian H. Vickery, Keith A. M. Walker