R Is Acyclic Patents (Class 514/625)
  • Patent number: 5683705
    Abstract: Novel sulfhydryl group-containing amides and disulfide group-containing bis-amides useful for treating or preventing an abnormal biological condition or a disease, and/or improving the texture or appearance of the skin, as well as compositions containing amides and bis-amides and methods for their use are described. Such types of abnormal biological conditions or diseases include skin atrophy, i.e., the thinning and/or general degradation of the dermis often characterized by a decrease in collagen and/or elastin as well as decreased number, size and doubling potential of fibroblast cells, and other maladies including, but are not limited to dry skin, severe dry skin, dandruff, acne, keratoses, psoriasis, eczema, skin flakiness, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, hyperkeratotic skin, inflammatory dermatoses, age-related skin changes and skin in need of cleansers.
    Type: Grant
    Filed: March 29, 1996
    Date of Patent: November 4, 1997
    Assignee: Estee Lauder, Inc.
    Inventors: Daniel H. Maes, Jules Zecchino, Althea Knight
  • Patent number: 5681852
    Abstract: The subject invention relates to desquamation compositions comprising a combination of sulfhydryl compounds and zwitterionic surfactants. The subject invention further relates to methods of desquamation in mammalian skin and treating acne in mammalian skin.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 28, 1997
    Assignee: The Procter & Gamble Company
    Inventor: Donald L. Bissett
  • Patent number: 5681859
    Abstract: A non-toxic, environmentally safe and easily employable insecticide and insect repellant is achieved by providing an aqueous composition incorporating ethanolamine based compounds, either independently or in combination with the ethanolamine based compounds being selected from both simple compounds and conjugated compounds. In one preferred embodiment, a highly effective composition is attained for safe, effective, direct topical application to humans and animals by employing between about 10% and 70% by volume of the entire composition of the ethanolamine-based compound. In alternate preferred embodiments, the insecticide is formulated for application to plants, trees, crops, and other vegetation to provide a composition which effectively controls bothersome insects, while being completely safe and non-injurious to the plant, tree, or crop, as well as to the flowers or fruit thereof.
    Type: Grant
    Filed: September 6, 1995
    Date of Patent: October 28, 1997
    Assignee: Lynn Sue James
    Inventors: Lynn Sue James, Michael A. Siedman
  • Patent number: 5679667
    Abstract: Aminoalcohols N-acyl derivatives useful in the prevention and in the treatment of mammalian pathologies induced by mast cell degranulation in consequence of peripheral nerve noxae.
    Type: Grant
    Filed: October 21, 1994
    Date of Patent: October 21, 1997
    Assignee: Lifegroup S.P.A.
    Inventors: Francesco Della Valle, Silvana Lorenzi, Federica Della Valle
  • Patent number: 5643899
    Abstract: Disorders of the skin and mucous membrane that have a disrupted or dysfunctional epidermal barrier are treated or prevented by topical application of a formulation comprising certain of the three major epidermal lipid species or their structurally similar precursors, isomers, or analogs in certain proportion ranges. This invention utilizes the following lipid species in unique combinations of two or more components: cholesterol, an acylceramide, a ceramide, and essential and nonessential fatty acids. These combinations are effective both as moisturizing agents and agents for the restoration of barrier function. Some of these combinations are further enhanced by the addition of known moisturizers such as petrolatum and glycerine.
    Type: Grant
    Filed: February 27, 1995
    Date of Patent: July 1, 1997
    Assignees: Cellegy Pharmaceuticals, Inc., The Regents of the University of California
    Inventors: Peter M. Elias, Kenneth R. Feingold, Carl R. Thornfeldt
  • Patent number: 5631297
    Abstract: Anandamides useful for the treatment of intraocular hypertension, as well as ophthalmic compositions comprising the same and a cyclodextrin, and methods of use of these compounds to treat intraocular hypertension.
    Type: Grant
    Filed: July 11, 1994
    Date of Patent: May 20, 1997
    Inventors: David W. Pate, Tomi Jarvinen, Kristiina Jarvinen, Arto Urtti
  • Patent number: 5629327
    Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis. Importantly, these compounds can be administered orally.
    Type: Grant
    Filed: December 15, 1993
    Date of Patent: May 13, 1997
    Assignee: Childrens Hospital Medical Center Corp.
    Inventor: Robert D'Amato
  • Patent number: 5622927
    Abstract: The invention relates to a pharmaceutical composition for treating the symptoms of vulvitis and vulvovaginitis which comprises folic acid, panthenol and/or allantoin, protein hydrolysate or casein hydrolysate, lactose or dextrose, lactic acid, magnesium sulfate and sodium chloride or ammonium chloride in the form of suppositories, ointments, solutions or sprays and a method of use thereof.
    Type: Grant
    Filed: August 16, 1995
    Date of Patent: April 22, 1997
    Assignee: Vepex KFT.
    Inventors: Gy orgy Hangay, G aborn e Olah, Edit T okos, Gy orgy V amos
  • Patent number: 5622992
    Abstract: The present invention relates to topical aromatic releasing compositions containing one or more volatile aromatic compounds selected from the group consisting of 3-1-menthoxy propane-1,2-diol, N-substituted-p-menthane-3-carboxamides and acyclic carboxamides and mixtures thereof. In further embodiments, these compositions are also useful for providing relief from nasal symptoms.
    Type: Grant
    Filed: March 7, 1996
    Date of Patent: April 22, 1997
    Assignee: The Procter & Gamble Company
    Inventor: William F. Beck
  • Patent number: 5621008
    Abstract: Disclosed is the novel use of N-acyl-N,N',N'-ethylenediaminetriacetic acids and N-acyl-N,N',N'-(ethylenedioxy) diethylenedinitrilotriacetic acids as active ingredients in preventative as well as therapeutic topical compositions to promote exfoliation and alleviate symptoms of skin conditions caused by abnormal keratinization.
    Type: Grant
    Filed: October 27, 1995
    Date of Patent: April 15, 1997
    Assignee: Avon Products, Inc.
    Inventor: Dmitri Ptchelintsev
  • Patent number: 5614558
    Abstract: A non-toxic, environmentally safe and easily employable insecticide and insect repellant is achieved by providing an aqueous composition incorporating ethanolamine based compounds, either independently or in combination with the ethanolamine based compounds being selected from both simple compounds and conjugated compounds. In one preferred embodiment, a highly effective composition is attained for safe, effective, direct topical application to humans and animals by employing between about 10% and 70% by volume of the entire composition of the ethanolamine-based compound. In alternate preferred embodiments, the insecticide is formulated for application to plants, trees, crops, and other vegetation to provide a composition which effectively controls bothersome insects, while being completely safe and non-injurious to the plant, tree, or crop, as well as to the flowers or fruit thereof.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: March 25, 1997
    Assignee: Lynn Sue James
    Inventors: Lynn S. James, Michael A. Siedman
  • Patent number: 5612382
    Abstract: A pharmaceutical composition for transdermally delivering pharmaceutically active ingredients through skin or mucosal tissues. The composition comprises pharmaceutically active ingredients in admixture with a pharmaceutically acceptable carrier that is a hydroxy alkyl amide. The composition exhibits an improved ability to control the rate of delivery of the pharmaceutically active ingredients into the body.
    Type: Grant
    Filed: July 15, 1994
    Date of Patent: March 18, 1997
    Assignee: Frances B. Fike
    Inventor: Elmer A. Fike
  • Patent number: 5612380
    Abstract: Sleep may be induced by administration of fatty acid primary amides, including cis-9,10-octadecenoamide. Furthermore, sleep deprivation may be assayed by analyzing cerebrospinal fluid with respect to the presence of fatty acid primary amides, including cis-9,10-octadecenoamide. The presence of cis-9,10-octadecenoamide in cerebrospinal fluid is correlated with comparative sleep deprivation.
    Type: Grant
    Filed: January 5, 1995
    Date of Patent: March 18, 1997
    Assignee: The Scripps Research Institute
    Inventors: Richard A. Lerner, Dale Boger, Ben Cravatt, Gary E. Siuzdak, Steven J. Henriksen
  • Patent number: 5612061
    Abstract: A composition for the treatment of premenstrual syndrome comprising an effective amount of calcium, magnesium, an analgesic and a diuretic sufficient to reduce the symptoms of premenstrual syndrome.
    Type: Grant
    Filed: October 14, 1994
    Date of Patent: March 18, 1997
    Inventor: Simon W. Rabkin
  • Patent number: 5610194
    Abstract: Insect repellent compositions are provided comprising mixtures of:(a) from about 5 to about 95%, by weight, of an N-alkyl neoalkanamide having the formula: ##STR1## wherein R.sub.1 R.sub.2, and R.sub.3 are alkyl groups and the sum of the carbon atoms therein is from 6 to 12, and wherein R.sub.4 is either a hydrogen atom or an alkyl group having one to two carbon atoms, and wherein R.sub.5 is methyl, ethyl, or propyl; and(b) from about 5 to about 95%, by weight, of N,N-diethyl-meta-toluamide (DEET).Preferred repellent composition comprise mixtures of N-methyl neodecanamide (MNDA) and DEET which provide synergistic repellency effects against a variety of insects including cockroaches, silverfish, mosquitoes, flies and ants. The repellent compositions may be applied directly to surfaces to be treated or they may be incorporated in detergent compositions such as laundry detergents, floor and wall cleaners, rug cleaners and shampoos, hair shampoos and liquid and bar soaps.
    Type: Grant
    Filed: June 10, 1996
    Date of Patent: March 11, 1997
    Assignee: Colgate-Palmolive Company
    Inventors: Thomas G. Polefka, Pallassana Ramachandran, Robert J. Steltenkamp, Thomas F. Connors, Kevin M. Kinscherf
  • Patent number: 5602277
    Abstract: A compound of the Formula (I): ##STR1## or pharmaceutically-suitable salts or prodrug forms thereof, wherein: n is 0-1;m is 0;p is 0-1;R.sup.1 is --CO.sub.2 H;R.sup.2 is selected from the group consisting of H, --OH, and --NH.sub.2 ;R.sup.3 is H;R.sup.4 is --C(O)NHR.sup.8 ;R.sup.5 is --NHC(R.sup.6)NH.sub.2R.sup.6 is selected from the group consisting of .dbd.NH, .dbd.NOH, .dbd.NCN, .dbd.O, and .dbd.S; andR.sup.8 is selected from the group consisting of C.sub.1 -C.sub.4 linear or branched alkyl substituted with 0-3 halogens on each carbon.
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: February 11, 1997
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand, David A. Walsh
  • Patent number: 5597840
    Abstract: An agrochemical microemulsion composition for injection into trees, and the use of said composition for preventing and treating damage to trees from disease and pests or regulating tree growth. The composition includes a nonpolar agrochemical active ingredient, a water-miscible solvent, and an emulsifying agent. When the composition is diluted in water, the particle size of the active ingredient is between about 0.01 and about 0.1 microns.
    Type: Grant
    Filed: July 7, 1994
    Date of Patent: January 28, 1997
    Assignee: Ciba-Geigy Corporation
    Inventor: Carolyn E. Moore
  • Patent number: 5596019
    Abstract: Certain N-acyl-cycloalkylamine derivatives are useful as melatonergic agents.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 21, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ronald J. Mattson, Daniel J. Keavy, Michael F. Parker, Graham Johnson
  • Patent number: 5589178
    Abstract: Cosmetic or dermatological compositions containing at least one anti-aging active agent having an irritant effect, a cosmetically or dermatologically acceptable medium, and in addition, as an agent mollifying the irritant effect, a ceramide of the following formula (I): ##STR1## R.sub.1 is a saturated or unsaturated, linear or branched C.sub.10 to C.sub.26 alkyl group;R.sub.2 is a saturated or unsaturated, linear or branched C.sub.12 to C.sub.32 alkyl group;R.sub.3 is H or --CO--CHOH--R.sub.2 ; andn is 0 or 1.
    Type: Grant
    Filed: December 30, 1994
    Date of Patent: December 31, 1996
    Assignee: L'Oreal
    Inventors: Lucien Aubert, Francoise Gagnebien-Cabanne
  • Patent number: 5567831
    Abstract: This invention discloses compounds useful as non-steroidal sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R.sub.1 is selected from the group consisting of hydrogen and a lower alkyl group, (b) R.sub.2 is selected from the group consisting of H and a lower alkyl group, (c) m is an integer from 0 to 4, and (d) n is an integer from 5 to 14. R.sub.1 is selected from the group consisting of H and C.sub.1 -C.sub.6 alkyl and R.sub.2 is selected from the group consisting of H and C.sub.1 -C.sub.6 alkyl. The invention also discloses methods of treating a patient prophylactically to provide protection as an estrogen depleting agent for estrogen dependent illnesses and treating a patient therapeutically for estrogen dependent diseases. A method of making the non-steroidal sulfatase inhibitors is also disclosed.
    Type: Grant
    Filed: August 16, 1995
    Date of Patent: October 22, 1996
    Assignee: Duguesne University of the Holy Ghost
    Inventor: Pui-Kai Li
  • Patent number: 5567735
    Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 22, 1996
    Assignee: Imperial Chemical Industries PLC
    Inventors: Keith Russell, Cyrus J. Ohnmacht, Keith H. Gibson
  • Patent number: 5554642
    Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description,its optical isomers and its addition salts thereof with a pharmaceuticaliy-accepable acid or base,and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: September 10, 1996
    Assignee: Adir et Compagnie
    Inventors: Michel Langlois, Pierre Renard, G erard Adam
  • Patent number: 5547984
    Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a heterocycle, a phenylalkyl, a phenylalkoxy, naphthyl, cycloalkyl, alkoxyalkyl, alkyl, haloalkyl or alkenyl group; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2)alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyl, dithiocarbamoyl, hydroxy, azide, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 20, 1996
    Assignee: Rohm and Haas Company
    Inventor: Ashok K. Sharma
  • Patent number: 5541228
    Abstract: New melatonergic agents are phenyl alkanyl or phenyl alkyl substituted carboxamides and ureas of Formula I: ##STR1## wherein: R.sub.1 =C.sub.1-3 alkyl, allyl, C.sub.3-6 cycloalkyl substituted C.sub.1-4 alkyl;R.sub.2 =hydrogen, halogen or C.sub.1-4 alkoxy;R.sub.3 =hydrogen or C.sub.1-4 alkyl;R.sub.4 =C.sub.1-4 alkyl, C.sub.1-4 alkyl substituted amino, carboxylic acid substitutedC.sub.1-4 alkyl or C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl, or straight or branched chain C.sub.2-4 alkenyl;A=a linear C.sub.2-4 alkanediyl or alkenediyl chain, provided that A not be --CH.sub.2 CH.sub.2 -- when X is a bond; andX=a covalent bond or oxygen.
    Type: Grant
    Filed: March 8, 1995
    Date of Patent: July 30, 1996
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Katherine S, Takaki, George N. Karageorge, Daniel J. Keavy, Michael F. Parker, Brett T. Watson
  • Patent number: 5538986
    Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.
    Type: Grant
    Filed: December 6, 1993
    Date of Patent: July 23, 1996
    Assignee: Schering Corporation
    Inventors: Pauline C. Ting, Daniel M. Solomon, Richard J. Friary, Frank J. Villani, John J. Piwinski, Joe F. Lee, Dhiru B. Vashi
  • Patent number: 5523320
    Abstract: N-methyldeacetylcolchiceinamide derivatives represented by the formula ##STR1## wherein R denotes a residue obtained by removing COOH from a C.sub.3 -C.sub.7 sugar carboxylic acid, and hydroxyl groups present in the residue may properly be protected with a protecting group for a hydroxyl group.The N-methyldeacetylcolchiceinamide derivatives have less toxicity and strong effect for inhibiting proliferation of tumor cells, and are expected to be used as a carcinostatic.
    Type: Grant
    Filed: January 3, 1995
    Date of Patent: June 4, 1996
    Assignee: Ohgen Research Laboratories, Ltd.
    Inventor: Kiyoshi Akiyama
  • Patent number: 5482965
    Abstract: A method and compositions for enhancing absorption of topically administered physiologically active agents through the skin and mucous membranes of humans and animals in a transdermal device or formulation for local or systemic use, comprising a therapeutically effective amount of a pharmaceutically active agent and a non-toxic, effective amount of penetration enhancing agent of the formula I or a physiologically acceptable salt thereof: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein.
    Type: Grant
    Filed: September 3, 1993
    Date of Patent: January 9, 1996
    Inventor: Vithal J. Rajadhyaksha
  • Patent number: 5474757
    Abstract: A method of preventing acetaminophen (APAP)-induced hepatotoxicity utilizing diallyl sulfide (DAS) and diallyl sulfone (DASO.sub.2) is disclosed. DAS and DASO.sub.2 are prepared as an oral dosage form or injected. In a preferred embodiment, diallyl sulfone is added to a dosage form of acetaminophen in an amount effective to prevent the metabolism of said unit dose of acetaminophen into its hepatotoxic metabolites. In certain preferred embodiments, the above formulations further include an effective amount of N-acetylcysteine to detoxify hepatotoxic metabolites of acetaminophen.
    Type: Grant
    Filed: October 16, 1992
    Date of Patent: December 12, 1995
    Assignee: Rutgers University
    Inventor: Chung S. Yang
  • Patent number: 5466712
    Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants ##STR1##
    Type: Grant
    Filed: November 4, 1994
    Date of Patent: November 14, 1995
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth
  • Patent number: 5464872
    Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: November 7, 1995
    Assignee: Adir et Compagnie
    Inventors: Michel Langlois, Pierre Renard, Gerard Adam
  • Patent number: 5464867
    Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: November 16, 1994
    Date of Patent: November 7, 1995
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
  • Patent number: 5446027
    Abstract: Amino derivatives represented by the following general formula (1): ##STR1## and external skin care preparations containing such an amide derivative, are useful for preventing or curing skin roughness. Intermediates useful for the preparation of such amides are also disclosed.
    Type: Grant
    Filed: November 2, 1993
    Date of Patent: August 29, 1995
    Assignee: Kao Corporation
    Inventors: Taketoshi Fujimori, Yukihiro Ohashi, Akira Kawamata
  • Patent number: 5436273
    Abstract: Propargylamine derivatives having the general formula: ##STR1## wherein R is a hydrogen atom, an unsubstituted phenyl group or a phenyl group substituted with halogen, trifluoromethyl, loweralkoxy, nitro, cyano, amido or N,N-diloweralkylamido, R.sub.1, R.sub.2 or R.sub.3 are the same or different and each represent a hydrogen atom or a loweralkyl group, R.sub.4 is a hydrogen atom or a loweralkyl, benzyl, phenethyl or furyl group, or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form a piperidinyl group, and their pharmaceutically acceptable acid addition salts, have been found to be useful in the treatment of anxiety, psychotic states and aggressive behavior in affected animals.
    Type: Grant
    Filed: November 26, 1993
    Date of Patent: July 25, 1995
    Assignee: Lowchol Scientific, Inc.
    Inventors: Romano Salvador, David Z. Simon, Louis Leonard
  • Patent number: 5434190
    Abstract: N-monosubstituted neoalkanamides of 11 to 14 carbon atoms wherein the substituent on the amide nitrogen is cyclic (aromatic or cycloaliphatic, such as aryl or cycloalkyl) and of at least five carbon atoms, have been discovered to be insect repellent, providing that any aromatic substituent is unsubstituted at the ortho position and that when the neoalkanoyl moiety is pivaloyl the total number of carbon atoms in the N-cyclic neoalkanamide is at least 12. Such neoalkanamides are useful as repellents against cockroaches, including American, German and Oriental cockroaches, and are also effective against mosquitoes (both Anopheles and Aedes), black flies and carpenter ants, and to some extent against deer ticks. They may be applied to areas, locations and items which are desirably to be kept free of such insects, with applications being direct or of solutions or emulsions thereof, preferably by spraying, or in detergent compositions or other products to be applied to such areas, etc.
    Type: Grant
    Filed: October 11, 1994
    Date of Patent: July 18, 1995
    Assignee: Colgate-Palmolive Co.
    Inventor: Robert J. Steltenkamp
  • Patent number: 5434189
    Abstract: N-lower alkyl neoalkanamides of 1 to 2 carbon atoms in the lower alkyl thereof, and of 12 to 14 carbon atoms in the noalkanoyl group, e.g., N-methyl- and N-ethyl neotridecanamides, are new compounds which have insect repellent properties, being especially effective against cockroaches, e.g., the German and American cockroaches. However, they are also useful as repellents for other insects, including mosquitoes, moths, flies, fleas, ants, and lice. Additionally, they may repel arachnids, such as spiders, ticks and mites. The new neoalkanamides may be synthesized easily, as by reacting a primary lower alkyl amine with a neoalkanoyl halide, e.g., by reacting methyl amine or ethyl amine with neotridecanoyl chloride.
    Type: Grant
    Filed: January 25, 1994
    Date of Patent: July 18, 1995
    Assignee: Colgate-Palmolive Co.
    Inventor: Robert J. Steltenkamp
  • Patent number: 5416118
    Abstract: Novel bicyclic amides of the formula ##STR1## wherein Ar.sup.1 and Ar.sup.2 are phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl, wherein R.sup.2 is 1 to 3 substituents independently selected from the group consisting of halogeno, hydroxy, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino and lower dialkylamino;X, Y and Z are --CH.sub.2 --, --CH(alkyl)--, --C(alkyl).sub.2 --, --NH--, --N(alkyl)--, --O-- or --SO.sub.r, wherein r is 0, 1 or 2, and m, n and p are 0 or 1;R.sup.1 is an alkyl chain of 1 to 25 carbon atoms; an alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain --O--, --SO.sub.r, phenylene, R.sup.2 -substituted phenylene, heteroarylene or R.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: May 16, 1995
    Assignee: Schering Corporation
    Inventors: John W. Clader, Thomas Fevig, Wayne Vaccaro, Joel G. Berger
  • Patent number: 5414017
    Abstract: Compounds of the formula ##STR1## wherein m is zero or 1; n is zero, 1 or 2; p is zero or 1 to 6 provided that m and p are not both zero; R.sub.3 is hydrogen, acyl, or benzyl; and R.sub.1 is hydrogen, alkyl, phenyl, substituted phenyl, phenyl-alkylene, heterocyclic-alkylene, etc. These compounds are useful as cardiovascular agents.
    Type: Grant
    Filed: March 26, 1993
    Date of Patent: May 9, 1995
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Norma G. Delaney, George C. Rovnyak, Melanie J. Loots
  • Patent number: 5411989
    Abstract: The invention concerns nitric acid esters of cyclohexanol of formula I ##STR1## in which A signifies a valency bond or a C.sub.1 -C.sub.6 -alkylene chain and B the group --NR.sup.1 --CO--Z, --NR.sup.1 --SO.sub.2 --Z or --CO--NR.sup.2 --Z, whereby R.sup.1 signifies hydrogen or a C.sub.1 -C.sub.6 -alkyl alkyl group R.sup.2 hydrogen, a hydroxyl, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group and Z signifies hydrogen a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group which may optionally be substituted for the case that B is an --NR.sup.1 --CO--Z group, Z can also signify a C.sub.1 -C.sub.6 -alkoxy group.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: May 2, 1995
    Assignee: Boehringer Mannheim, GmbH
    Inventors: Helmut Michel, Wolfgang Bartsch
  • Patent number: 5391578
    Abstract: N-lower alkyl neoalkanamides are liquid state isomeric mixtures. Such new compounds are mixtures of isomeric secondary amides which have insect repellent properties, being especially effective against German cockroaches. They may be applied directly to surfaces to be treated and have been found to be sufficiently substantive to such surfaces so as to impart insect repelling properties thereto.
    Type: Grant
    Filed: May 15, 1992
    Date of Patent: February 21, 1995
    Assignee: Colgate-Palmolive Co.
    Inventor: Robert J. Steltenkamp
  • Patent number: 5369030
    Abstract: The present invention provides methods and pharmaceutical preparations of N-acyl-phenylaminoalcohol analogs for inducing differentiation of cells. Compositions having the formula ##STR1## wherein R.sub.1 is H, NO.sub.2, OH, chlorine, bromine or fluorine;R.sub.2 is H, OH or methoxy;R.sub.3 is H or OH; andm is from about 10 to about 14are administered to cells of a mammal that are capable of undergoing differentiation in amounts effective to induce differentiation of the cells. The invention also provides methods and pharmaceutical preparations for altering the phenotype of cells and for treating diseases characterized by hyperproliferation of cells.
    Type: Grant
    Filed: September 11, 1992
    Date of Patent: November 29, 1994
    Assignee: Duke University
    Inventors: Yusuf A. Hannun, Alicja Bielawska
  • Patent number: 5346887
    Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, (alpha, alpha) -dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is substituted hydroxyalkylamino.
    Type: Grant
    Filed: April 23, 1991
    Date of Patent: September 13, 1994
    Assignee: Abbott Laboratories
    Inventors: Herman H. Stein, Jacob J. Plattner, Steven R. Crowley
  • Patent number: 5336271
    Abstract: A method for increasing the proportion of a crystalline organic compound which remains amorphous and suppressing recrystallization in which a crystalline organic compound and a hydrophilic polymer substance are fixed onto a surface of core particles by means of impacts applied in a high velocity gas stream. The solubility and stability of the resulting composite product, such as a drug for internal use, can be improved.
    Type: Grant
    Filed: March 20, 1992
    Date of Patent: August 9, 1994
    Assignee: Nara Machinery Co., Ltd.
    Inventors: Takafumi Ishizaka, Yuji Kikuchi, Masumi Koishi
  • Patent number: 5318994
    Abstract: Compounds of the formula: ##STR1## in which: A represents ##STR2## R represents linear or branched lower alkyl, R.sub.1 represents hydrogen or linear or branched lower alkyl, andR.sub.2 represents aryl or lower arylalkyl or aryl or lower arylalkyl substituted by lower alkyl, lower alkoxy, trifluoromethyl, or halogen, aryl means phenyl or naphthyl, as well as optical isomers, epimers and diastereoisomers and addition salts thereof with a pharmaceutically-acceptable acid, lower alkyl and lower alkoxy having 1 to 6 carbon atoms inclusive, andmedicaments containing the same which are useful for the treatment of disorders of the melatoninergic system.
    Type: Grant
    Filed: November 3, 1992
    Date of Patent: June 7, 1994
    Assignee: Adir et Compagnie
    Inventors: Jean Andrieux, Raymond Houssin, Said Yous, Beatrice Guardiola, Daniel Lesieur
  • Patent number: 5302609
    Abstract: The present invention is a novel method for the treatment of renal hypertrophy and hyperplasia associated with diabetic nephropathy. The method of the present invention generally comprises the administration to the diabetic patient of a compound which inhibits glycosphingolipid synthesis, more particularly, an inhibitor of GlcCer synthase or 3-ketodihydrosphingosine synthase.
    Type: Grant
    Filed: December 16, 1992
    Date of Patent: April 12, 1994
    Assignee: The Regents of the University of Michigan
    Inventors: James A. Shayman, Norman S. Radin
  • Patent number: 5284872
    Abstract: New organic nitrate compounds, formed by condensing a nitrato alkanoic acid with a sulfur-containing amino acid or peptide followed by the reaction of the resulting product with an amino acid, N-acylamino acid, peptide or an N-acyl peptide to produce a thio ester thereof, which prevent nitrate tolerance or overcome existing tolerance and which are useful for the treatment of cardiac diseases including circulatory diseases, coronary dilation, high blood pressure, cardiac insufficiency and for dilating the peripheral vessels.
    Type: Grant
    Filed: April 5, 1991
    Date of Patent: February 8, 1994
    Assignee: Schwarz Pharma AG
    Inventors: Klaus Sandrock, Eike Noack, Edgar Fritschi, Ralf Kanzler, Martin Feelisch
  • Patent number: 5281611
    Abstract: An euthanasia solution based upon gamma-hydroxybutramide and a cardiotoxic amount of a compound selected from chloroquine and quinacrine is described. The composition provides effective euthanasia without unwanted side effects.
    Type: Grant
    Filed: December 19, 1990
    Date of Patent: January 25, 1994
    Assignee: Board of Trustees operating Michigan State University
    Inventors: Donald C. Sawyer, Theodore M. Brody, Marlee A. Langham
  • Patent number: 5270310
    Abstract: The present invention provides methods for inhibiting protein kinase C which comprise contacting protein kinase C with an inhibitory amount of a compound having the formula ##STR1## wherein R.sub.1 is C.sub.8 through C.sub.15 alkyl; R.sub.2 is H, C.sub.1 through C.sub.10 alkyl, or benzyl; R.sub.3 is N-heterocyclic, N-alkylheterocyclic, quaternized N-heterocyclic, NR.sub.4 R.sub.5 or N.sup.+ R.sub.4 R.sub.5 R.sub.6 X.sup.- ; R.sub.4, R.sub.5 and R.sub.6 are independently C.sub.1 through C.sub.10 alkyl; n is 2, 3, 4, or 5; and X is an anion. The invention also provides novel compounds having the formula ##STR2## wherein R.sub.1 is C.sub.8 through C.sub.15 alkyl; R.sub.2 is H, C.sub.1 through C.sub.10 alkyl, or benzyl; R.sub.3 is N-heterocyclic, N-alkylheterocyclic or quaternized N-heterocyclic; and n is 2, 3, 4, or 5.
    Type: Grant
    Filed: December 13, 1991
    Date of Patent: December 14, 1993
    Assignees: Sphinx Pharmaceuticals Corporation, Duke University
    Inventors: Robert M. Bell, Robert J. Fogelsong, Jeffrey B. Nichols
  • Patent number: 5262436
    Abstract: Mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
    Type: Grant
    Filed: August 6, 1991
    Date of Patent: November 16, 1993
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 5258408
    Abstract: N-lower alkyl neoalkanamides (N-lower alkyl trialkylacetamides of certain types) of 1 to 4 carbon atoms in the lower alkyl thereof and of 5 to 14 carbon atoms in the neoalkanoyl (or trialkylacetyl) group, e.g., N-methyl- and N-ethyl neodecanamides and N-methyl and N-ethyl neotridecanamides, are new compounds, secondary amides which have insect repellent properties, being especially effective against cockroaches, e.g., the German cockroach. However, they are also useful as repellents for other insects, including American cockroaches, mosquitoes, flies, fleas, ants, and lice. Additionally, they may repel arachnids, such as spiders, ticks and mites. The new neoalkanamides may be synthesized easily, as by reacting a primary lower alkyl amine with a neoalkanoyl halide, e.g. by reacting methyl amine or ethyl amine with neodecanoyl chloride. The most effective of the described amides for insect repellency are normally liquid and are sufficiently volatile to be detectable in air by insects.
    Type: Grant
    Filed: April 15, 1991
    Date of Patent: November 2, 1993
    Assignee: Colgate-Palmolive Company
    Inventor: Robert J. Steltenkamp
  • Patent number: 5256697
    Abstract: A method for administering pyruvate is disclosed which comprises administering a therapeutically effective amount of a pyruvate precursor to a mammal in the form of pyruvamide or a pyruvyl-amino acid. The pyruvyl-amino acid is preferably selected from the group comprising pyruvyl-glycine, pyruvyl-alanine, pyruvyl-leucine, pyruvyl-valine, pyruvyl-isoleucine, pyruvyl-phenylalanine, pyruvyl-proline and pyruvyl-sarcosine, and their amides and esters as well as their salts. Associated with the administration of a pyruvate precursor to a mammal in accordance with this invention are improved insulin resistance, lower fasting insulin levels, and reduced fat gain. Novel methods of synthesizing several pyruvate precursors are also disclosed.
    Type: Grant
    Filed: April 16, 1992
    Date of Patent: October 26, 1993
    Assignee: Abbott Laboratories
    Inventors: Robert H. Miller, Nickki L. Parlet, Kent L. Cipollo, Madhup K. Dhaon, John A. Houbion, Edwin O. Lundell