Abstract: Various effects of photoaging or sundamage of skin including impairment of differentiation of epidermal epithelial cells and loss of collagen fibers, abnormal changes in elastic fibers and deterioration of small blood vessels in the dermis of the skin are retarded by applying topically to the epidermis in a maintenance therapy program effective amounts of retinoids including retinoid derivatives and stereoisomers thereof such that epithelial growths are substantially reduced and prevented and the skin substantially regains and maintains its firmness, turgor and elasticity. Moreover, with persistent treatment dermal blood cells and vessels increase and the epidermis and dermis thicken, resulting in improved ability of the skin to sense, resist and recover from irritation or injury. Further, hyperpigmentation, lines and wrinkles due to aging are reduced and prevented. The treatment is particularly useful for human facial skin and preferably applied in amounts insufficient to cause excessive irritation.
Abstract: An acylanilide of the formula: ##STR1## wherein R.sup.1 or R.sup.2 which may be the same or different, each is an electron-withdrawing substituent, alkylthio or phenylthio or R.sup.1 is hydrogen, alkyl or alkoxy; wherein R.sup.3 is hydrogen or halogen; wherein R.sup.4 is hydrogen or acyl wherein A is branched-chain alkylene; and wherein R.sup.5 is phenyl, substituted phenyl or naphthyl. The compounds possess progestational activity.
Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4, E.sub.4 and the slow reacting substance of anaphylaxis.As such, these compounds will be useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
Type:
Grant
Filed:
February 17, 1987
Date of Patent:
October 3, 1989
Assignee:
Merck Frosst Canada, Inc.
Inventors:
John Gillard, Joshua Rokach, Patrice C. Belanger
Abstract: This invention relates to a novel prostacyclin represented by the formula: ##STR1## [wherein R.sup.1 represents --CO.sub.2 R.sup.5 group or --CONR.sup.6 R.sup.7 group; A is(i) --CH.dbd.CH--CH.sub.2 CH.sub.2 -- or(ii) --CH.sub.2 CH.sub.2 --O--CH.sub.2 --;B represents --C.tbd.C-- group; R.sup.2 represents an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a phenyl group or a phenoxy group;R.sup.3 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.4 represents a hydrogen atom, an acyl group, a tri(1 to 7 carbon atoms)hydrocarbyl-silyl group or a group forming an acetal bond with an oxygen atom of a hydroxy group; a double bond in the substituent represented by A is E or Z, or a mixture thereof; asymmetric center in the substituent represented by R.sup.
Type:
Grant
Filed:
May 18, 1987
Date of Patent:
June 13, 1989
Assignees:
Mitsubishi Chemical Industries Limited, Sagami Chemical Research Center
Abstract: This invention provides certain diphenylmethane derivatives, their pharmaceutical formulations, and their use in treating inflammation and arthritis in mammals.
Abstract: A 6-keto-prostaglandin E.sub.1 derivative of the formula: ##STR1## (wherein R.sup.1 represents an amino acid or amino alcohol residue, R.sup.2 represents a single bond or an alkylene group of from 1 to 4 carbon atoms, R.sup.3 represents (i) an alkyl group of from 1 to 8 carbon atoms, (ii) a cycloalkyl group of from 4 to 7 carbon atoms, which may be unsubstituted or substituted by at least one alkyl group of from 1 to 8 carbon atoms or (iii) a phenyl or phenoxy group, which may be unsubstituted or substituted by chlorine, trifluoromethyl or alkyl of from 1 to 3 carbon atoms, provided that when R.sup.2 represents a single bond R.sup.3 does not represent phenoxy)cyclodextrin clathrates thereof and non-toxic salts thereof possess selective cytoprotective activity.
Abstract: A topically and systemically administered anti-inflammatory composition for human and for veterinary consumption which comprises compounds of the general formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are defined hydrocarbon attachments and Y is --OH or a phenolic ester group derived from the reaction of such --OH group with a carboxylic acid halide or anhydride.In typical compounds covered by said general formula(a) R.sub.1 is H, R.sub.2 is 5,n-octanoyl, Y is hydroxy and R.sub.3 is p-trifluoromethylphenyl;(b) R.sub.1 is H, R.sub.2 is 5,n-decanoyl, Y is hydroxy and R.sub.3 is benzothiazol-2-yl and(c) R.sub.1 is H, R.sub.2 is 5,n-decanoyl, Y is acryloyloxy and R.sub.3 is p-nitrophenyl.
Abstract: The present invention relates to novel specifically-substituted phenyl compounds, especially substituted di-tert-butyl phenol derivatives, which are effective as anti-inflammatory, analgesic and/or antipyretic agents. These phenyl compounds are substituted with a low molecular weight alkyl chain which terminates in a specific unsaturated functional group. These unsaturated functionalities are --C.tbd.CH, C.dbd.CH.sub.2, C.dbd.C.dbd.CH.sub.2, and aldehydes in the form of their acetals.The present invention further relates to pharmaceutical compositions which contain an anti-inflammatory agent of the present invention and a pharmaceutically-acceptable carrier.Finally, the present invention relates to methods for treating diseases characterized by inflammation, such as rheumatoid arthritis and osteoarthritis, in humans or lower animals.
Type:
Grant
Filed:
June 27, 1986
Date of Patent:
November 24, 1987
Assignee:
The Procter & Gamble Company
Inventors:
Maurice E. Loomans, Randall S. Matthews, Joseph A. Miller
Abstract: Compounds of the formula ##STR1## where n is 0 or 1,R is alkyl, phenyl or R.sub.4 -substituted phenyl,R.sub.2 and R.sub.3 are, independently, alkyl orR.sub.2 and R.sub.3 together with N is ##STR2## m is 1, 2 or 3, R.sub.1 and R.sub.4 are, independently hydrogen, halo, alkyl or alkoxy, andR.sub.5 is hydrogen or alkyl of 1 to 6 carbon atomsor their pharmaceutically acceptable salts are useful as anti-diabetic agents, in particular, as hypoglycemic agents or inhibitors of post-prandial hypoglycemia.
Abstract: This invention relates to pharmaceutical compositions containing a class of 5-phenyl-1,3-dioxoalkenyl compounds useful as inhibitors of leukotriene biosynthesis and thus useful in the treatment of conditions associated with leukotrienes. This invention also relates to the use of the 5-phenyl-1,3-dioxoalkenyl compounds in the inhibition of leukotriene biosynthesis and thus in the treatment of conditions associated with leukotrienes. This invention further relates to a novel process for the preparation of the 5-phenyl-1,3-dioxoalkenyl compounds.
Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S-- where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.
Abstract: Polyene compounds represented by the general formulae ##STR1## in which: R and R.sub.1 are each hydrogen or an alkyl group of from 1 to 5 carbon atoms;R.sub.2 is an alkyl group of from 1 to 5 carbon atoms;R.sub.3 is hydroxyl, alkoxy of from 1 to 5 carbon atoms, NH.sub.2, NHR.sub.2 or NR.sub.2 R.sub.2 and Z is a cycloalkyl, cycloalkenyl or cycloalkdienyl group substituted with from 0 to 5 alkyl groups, a keto group or a hydroxyl group or a phenyl group substituted with from 0 to 4 hydroxy, alkoxy, alkyl, aryloxy, aralkyloxy or trifluoromethyl groups or halogen atoms or combinations thereof and the pharmaceutically-acceptable salts thereof.The foregoing compounds have been found to be effective in the treatment of psoriasis, inflammatory conditions and allergic responses.
Type:
Grant
Filed:
November 2, 1984
Date of Patent:
August 13, 1985
Assignee:
USV Pharmaceutical Corp.
Inventors:
Bernard Loev, Wan-Kit Chan, Howard Jones
Abstract: Long-acting forms of theophylline for use in treating asthma comprise theophylline associated with a compound of the substituted cinnamamide type of the general formula ##STR1## wherein R is hydrogen, a hologen or an acetyl radical; R.sub.1 is hydrogen or the methyl radical; R.sub.2 is ##STR2## wherein R.sub.3 is hydrogen or the methyl radical; or R.sub.1 and R.sub.2 together with the adjacent nitrogen tom form the 2,2-dimethyl-3-oxazolidinyl group.