Abstract: Hydroxylated milk glycerides having low levels of ethylenic unsaturation are disclosed. The hydroxylated milk glycerides can have enhanced resistance to rancidification and as such, are suitable for use in personal care compositions e.g., lotions, skin creams, lipsticks, eye shadow, and makeup. Personal care compositions comprising the hydroxylated milk glycerides can have enhanced properties as compared to personal care compositions which do not comprise the hydroxylated milk glycerides or alternatively comprise milk fat.
Type:
Grant
Filed:
November 19, 1996
Date of Patent:
September 22, 1998
Assignee:
Amerchol Corporation
Inventors:
Amnon Friedman, Stuart Barry Polovsky, Joseph Peter Pavlichko, Luis Sabino Moral
Abstract: A method of preventing renal failure or dysfunction caused by medical tests which utilize contrast media by administering, preferably by intravenous infusion or injection, a prostaglandin selected from PGE.sub.1, PGE.sub.2, PGI.sub.2 or an analog or pharmaceutically acceptable salt thereof and preferably in a form of a complex with .alpha.-cyclodextrin, to a patient at risk, for example, a diabetic.
Type:
Grant
Filed:
November 28, 1995
Date of Patent:
September 15, 1998
Assignee:
Schwarz Pharma, Inc.
Inventors:
Henry T. Stratton, Tammy K. Antonucci, Erwin Schollmayer
Abstract: The present quinoline derivatives and compositions having gonadotropin-releasing hormone antagonistic activity are useful as propylactics or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, uterine or cervical cancer, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; are effective as a fertility controlling agent in both sexes (e.g.
Abstract: Intercalator compounds are provided which are comprised of intercalator moieties, or substituted intercalator moieties, having one or more functionalized chains, or moieties, and which compounds provide a high affinity for binding to the DNA molecule and show reduced self-quenching, while providing superior transport kinetics. The compounds have been found to provide enhanced fluorescence when bound to a DNA molecule within a fluorescent flow cytometry environment which is about eight to ten times brighter in fluorescence than "bis" structure conventional intercalating agents and other known intercalating agents utilized in flow cytometry environment.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
September 15, 1998
Assignee:
Abbott Laboratories
Inventors:
Christopher Bieniarz, Jeffrey Bruce Huff, Denis R. Henrard
Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia, and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment or prevention a substituted or unsubstituted pyridine and pyridine (N-oxide) analogs of 4-hydroxydihydroquinolones, tetrahydroquinoline-trione-oximes and quinoxalones, tautomers and pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
September 1, 1998
Assignees:
State of Oregon, Acting by and Through the Oregon State Board of Higher Education, Acting for and on Behalf of the Oregon Health Sciences University and the University of Oregon, Cocensys, Inc.
Inventors:
John F. W. Keana, Sui Xiong Cai, Zhang-Lin Zhou, James M. Navratil
Abstract: Novel fibrinogen receptor antagonists of the formula: X--Y--Z-Aryl-A--B and the pharmaceutically acceptable salts thereof, wherein Aryl is a 5-membered aromatic ring system containing 1 or 2 heteroatoms chosen from N, O or S wherein ring atoms may be unsubstituted or substituted with R.sup.5 and wherein S may be substituted with 0, 1 or 2 oxygen atoms; and X comprises various Nitrogen substituents including aromatic or nonaromatic systems; Y comprises, for example, alkyl or alkylaminocarbonylalkyl groups and Z and A are substituents which when present are independently chosen from alkyl or alkyloxyalkyl or other groups as defined herein; B is (a) or (b). The claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating or preventing thrombus formation.
Type:
Grant
Filed:
May 31, 1995
Date of Patent:
July 28, 1998
Assignee:
Merck & Co., Inc.
Inventors:
George D. Hartman, John D. Prugh, Melissa S. Egbertson, Mark E. Duggan, William Hoffman
Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.3, R.sub.4, R.sub.11, and c are as set forth herein are described. These compounds are useful as agents for the treatment of mammals infected with herpes group virus. Certain of these compounds are useful as antitumor agents.
Type:
Grant
Filed:
August 2, 1996
Date of Patent:
July 28, 1998
Assignee:
Schering Corporation
Inventors:
Adriano Afonso, Joseph M. Kelly, Samuel Chackalamannil
Abstract: The invention relates to new intermediate compounds for preparation of new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by an unsatured bicyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds.
Type:
Grant
Filed:
August 18, 1997
Date of Patent:
July 21, 1998
Assignee:
Bayer Aktiengesellschaft
Inventors:
Uwe Petersen, Michael Ruther, Thomas Schenke, Klaus Dieter Bremm, Rainer Endermann
Abstract: The invention relates to a pharmaceutical preparation comprising a plasma protein wherein said preparation is free of infectious agents as well as essentially free of denaturation products and is obtainable by a method that encompasses the following steps:a) addition of a polyether and a chaotropic agent to a solution comprising the plasma protein, optional lyophilization of the solution;b) inactivation of infectious agents in the presence of the polyether by a physio-chemical or chemical treatment, andc) removal of the polyether and the chaotropic agent.
Type:
Grant
Filed:
June 28, 1996
Date of Patent:
June 23, 1998
Assignee:
Immuno Aktiengesellschaft
Inventors:
Johann Eibl, Friedrich Dorner, Noel Barrett
Abstract: Disclosed are intermediates for the preparation of novel aminocoumaran derivatives of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are a hydrogen atom, an acyl group, an alkoxycarbonyl group, an aliphatic group or aromatic group; R.sup.3, R.sup.4 and R.sup.5 are an optionally acylated hydroxyl, optionally substituted amino group, alkoxy group or aliphatic group, or two of R.sup.3, R.sup.4 and R.sup.5 may be linked together to form a carbocyclic group; R.sup.6 and R.sup.7 are an aliphatic group and at least one of them has a methylene group at the .alpha.-position; R.sup.8 and R.sup.9 are a hydrogen atom or an aliphatic group or aromatic group, or a salt thereof is useful for medicines for preventing and treating various diseases such as arterial sclerosis, hepatopathy, cerebrovascular diseases and the like.
Type:
Grant
Filed:
September 17, 1996
Date of Patent:
June 23, 1998
Assignee:
Takeda Chemical Industries, Ltd.
Inventors:
Tetsuya Aono, Shigenori Ohkawa, Takayuki Doi
Abstract: Polyhydroxylated and dehydrogenated metabolites of 9-amino-1,2,3,4-tetrahydro-acridine (Tacrine) in which attached to at least two of the carbon atoms numbered 1,2,3 and 4 is a hydroxyl group and to the others either hydrogen, hydroxyl or double bonded oxygen the residual valencies being occupied by hydrogen or double bonds between carbon atoms 1 and 2 and/or 3 and 4 are disclosed as being useful medicaments for enhancing memory and cognitive function in Alzheimer's disease because they have retained the anticholinesterase activity of their metabolic precursor while circumventing its hepatotoxicity. Related compounds to which this disclosure also applies include those in which the aromatic ring is substituted with lower alkyl, lower alkoxy, halogen, hydroxy, nitro, trifluoromethyl, alkyl-N-substituted carboxamides and where the 9-amino group is mono or di-substituted independently.
Abstract: This invention is concerned with polymorphic forms of the compound N-?1(R)-?(1,2-dihydro-1-methanesulfonylspiro?3H-indole-3,4'-piperdin!-1'-y l)carbonyl!-2-(phenylmethyloxy)ethyl!-2-amino-2-methylpropanamide methanesulfonate which is a growth hormone secretagogue that is useful in food animals to promote their growth thereby rendering the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, and to treat medical conditions which are improved by the anabolic effects of growth hormone. The instant polymorphic forms have advantages over the other known forms of N-?1(R)-?(1,2-dihydro-1-methanesulfonylspiro?3H-indole-3,4'-piperdin!-1'-y l)carbonyl!-2-(phenylmethyloxy)-ethyl!-2-amino-2-methylpropanamide methanesulfonate in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
Type:
Grant
Filed:
October 23, 1996
Date of Patent:
June 16, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Jerome P. Draper, Michael J. Kaufman, David C. Dubost, James A. McCauley, Jennifer L. Vandrilla, Richard J. Varsolona
Abstract: A method for the prevention and treatment of atherosclerosis and its related diseases in mammals is provided, in which an NADPH oxidase inhibitor is administered to mammals. The NADPH oxidase inhibitor prevents the production of reactive oxygen species upon exposure of endothelial cells to atherogenic LDL levels, resulting in decreased endocytosis and vascular hyperpermeability. Apocynin is a preferred NADPH oxidase inhibitor. Additionally, there is provided a diagnostic method for predicting the risk to an individual of atherosclerotic-related diseases.
Type:
Grant
Filed:
November 27, 1995
Date of Patent:
June 9, 1998
Assignee:
The Research Foundation of State University of New York
Abstract: 1,2,3,4-Tetrahydro-chromeno?3,4-c!pyridin-5-ones of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.5 include hydrogen, alkyl, alkoxy, hydroxy, halo, nitro, amino, and trifluoromethyl; R.sub.4 is unsubstituted or substituted phenyl, pyridyl, or quinolinyl; and n is 0 to 4, are useful to treat psychosis in mammals, particularly schizophrenia.
Type:
Grant
Filed:
February 27, 1997
Date of Patent:
June 2, 1998
Assignee:
Warner-Lambert Company
Inventors:
David Thomas Connor, Steven Robert Miller, Paul Charles Unangst, Lawrence David Wise
Abstract: Novel 1H-imidazo?4,5-c!quinolin-4-amines are disclosed. The compounds function as antiviral agents and they are potential synthetic intermediates in the preparation of known antiviral agents and labeled known antiviral agents. Processes for the preparation of the compounds, methods for their antiviral use, and methods of inducing interferon biosynthesis, are also described.
Abstract: New compounds of the formula (A) ##STR1## a process for their preparation and their use in the manufacture of pharmaceutical preparations. The new compounds have both local anaesthetic and analgesic effect.
Abstract: Compounds selected from the series consisting of the perylenecarboximide, quinacridone, isoindoline, indigoid, azo, benzodipyrrolone, benzodifuranone, furanofuran, pyrrolo?2,5-b!pyrrole and bianthraquinone chromophores containing at least one grouping of formula ##STR1## wherein each A may be N--CN or O, with the proviso that at least one A must be N--CN, X is --N(R)--, --O-- or --S--, R is hydrogen, C.sub.1 -C.sub.18 alkyl, unsubstituted or halogen- or C.sub.1 -C.sub.4 alkyl-substituted phenyl, benzyl or phenethyl, and m and n are each independently of the other 0 or 1.Depending on the nature of their substituents, these compounds can be used as polymer-soluble dyes or as pigments for coloring high molecular weight organic material. They are distinguished by a surprisingly high solid-state fluorescence.
Type:
Grant
Filed:
March 22, 1996
Date of Patent:
May 26, 1998
Assignee:
Ciba Specialty Chemicals Corporation
Inventors:
John S. Zambounis, Zhimin Hao, Abul Iqbal
Abstract: An imidazopyridine derivative of the formula ?I!: ##STR1## wherein R.sup.1 is a lower alkyl group, R.sup.2 is a lower alkanoyl group, and R.sup.3 and R.sup.4 are each lower alkyl groups, or both combine at the end thereof to form an alkylene group having 3 to 6 carbon atoms, and a pharmaceutically acceptable salt thereof, said imidazopyridine derivatives have an excellent angiotensin II antagonistic activity and are useful for the prophylaxis or treatment of hypertension.
Abstract: This invention provides a phosphoric diester of formula (I) which is available on di-esterification of phosphoric acid with L-ascorbic acid involving its 5-hydroxyl group and tocopherol involving its hydroxyl group or a pharmacologically acceptable salt thereof. ##STR1## The compound of the invention can be used with advantage as an antioxidant (radical-scavenging) agent and a prophylactic and therapeutic agent for ischemic organ disorders (e.g. myocardial infarction, heart failure, arrhythmia, cerebral infarction, stroke (cerebral apoplexy), renal failure, etc.).