Carboxamides (i.e., R-c(=o)-n, Wherein R Is A Radical Having Carbon Bonded Directly To The C(=o)-n Or Is Hydrogen And Wherein Any Substituent Attached To Nitrogen Will Be Referred To As E) Patents (Class 514/613)
  • Patent number: 5990170
    Abstract: The following description concerns a therapeutic method for the treatment of diseases connected with the modulation of the cannabinoid peripheral receptor, comprising administering amidic derivatives of mono and bicarboxylic acids with aminoalcohols or arninoethers selectively active on said receptor.
    Type: Grant
    Filed: September 30, 1997
    Date of Patent: November 23, 1999
    Assignee: Lifegroup S.p.A.
    Inventors: Francesco Della Valle, Alberta Leon, Gabriele Marcolongo, Silvana Lorenzi
  • Patent number: 5985910
    Abstract: The present invention relates to new 3-[4-(2-Phenyl-Indole-1-ylmethyl)-Phenyl]-Acrylamide compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, the compounds having the following general structure.
    Type: Grant
    Filed: April 14, 1997
    Date of Patent: November 16, 1999
    Assignee: American Home Products Corporation
    Inventors: Chris P. Miller, Bach D. Tran
  • Patent number: 5985926
    Abstract: There is disclosed a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans by administering an effective amount of a compound that inhibits cellular signaling through a specific phospholipid-based cellular signaling and signal amplification pathway. The invention further provides a method for preventing or delaying clinical symptoms of a group of viral diseases wherein the viral disease is mediated by host cell viral replication. The invention provides an advantage by attacking host cellular signaling mechanisms to prevent the development of drug resistance from rapidly mutating viruses.
    Type: Grant
    Filed: February 10, 1997
    Date of Patent: November 16, 1999
    Assignee: Cell Therapeutics, Inc.
    Inventors: David W. Leung, Gail E. Underiner, Jack W. Singer
  • Patent number: 5981580
    Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitrites thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: November 9, 1999
    Assignee: G. D. Searle & Co.
    Inventors: Sean T. Nugent, Richard A. Mueller
  • Patent number: 5976516
    Abstract: Described is a hair cosmetic composition comprising an amide compound having a melting point of 0 to 50.degree. C. The hair cosmetic composition according to the present invention can impart the hair with suppleness, improve the touch feeling and bring about spilt hair preventive effects. Concerning the touch feeling, in particular, the composition can impart the hair with natural feeling, more specifically, with moisturized feeling, finger passing ease, styling ease, luster and not greasy but good oily feeling, whereby the hair with healthy, moisturized and young impression can be obtained.
    Type: Grant
    Filed: November 7, 1997
    Date of Patent: November 2, 1999
    Assignee: Kao Corporation
    Inventors: Masahiko Sakai, Kumi Sugino, Yuji Hirano
  • Patent number: 5972892
    Abstract: The invention relates to a therapeutic composition for topical application containing at least one product with an irritant side effect and a substance P antagonist for reducing or even eliminating the irritant effect of this product.It also relates to the use of a substance P antagonist for the preparation of a pharmaceutical composition for topical application containing at least one product with an irritant side effect for reducing or even eliminating the irritant effect of this product.The substance P antagonist may be a peptide compound or a nitrogen-containing compound or a nitrogen-, sulphur- or oxygen-containing heterocyclic compound.
    Type: Grant
    Filed: June 15, 1998
    Date of Patent: October 26, 1999
    Assignee: L'oreal
    Inventors: Olivier De Lacharriere, Lionel Breton
  • Patent number: 5962518
    Abstract: There are described new active compound combinations of a compound of the formula (I) ##STR1## with known fungicidal active compounds, and their use for combating phytopathogenic fungi.
    Type: Grant
    Filed: October 1, 1997
    Date of Patent: October 5, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Stenzel, Wilhelm Brandes, Stefan Dutzmann, Bernd-Wieland Kruger, Karl-Heinz Kuck, Rolf Pontzen, Thomas Seitz, Atsumi Kamochi, Ikuya Saitoh
  • Patent number: 5958439
    Abstract: A composition containing, as active ingredient, one or more water soluble plant protection active materials and further containing an effective amount of one or more polyalkoxylated amidoamines of average formula (1) or (2), wherein all R.sup.1, which are the same or different, are a straight or branched C.sub.2 -C.sub.22 alkyl or alkenyl hydrocarbon group, cycloalkyl or alkylaryl, all R.sup.2, which are the same or different, are hydrogen or a C.sub.1 -C.sub.4 alkyl radical, and p, q, r, s and t, which are the same or different, are integers that can be zero, such that p+q is 1-20 and r+s+t is 1-20. Applications of said composition as a herbicide, a fungicide or a fertilizer are also described.
    Type: Grant
    Filed: January 30, 1998
    Date of Patent: September 28, 1999
    Assignee: Rhodia Chimie
    Inventor: Isabelle Gubelmann
  • Patent number: 5952377
    Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: September 14, 1999
    Assignee: G. D. Searle & Co.
    Inventors: Sean T. Nugent, Richard A. Mueller
  • Patent number: 5952386
    Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: September 14, 1999
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
  • Patent number: 5929110
    Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof.These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure ##STR1## in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L-Ala, L-Ile, L-Phe, L-Trp, L-Thr or an amide such as NHCH.sub.2 C.sub.6 H.sub.5 or NH(CH.sub.2).sub.2 C.sub.6 H.sub.5.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: July 27, 1999
    Assignee: G. D. Searle & Co.
    Inventors: Sean T. Nugent, Richard A. Mueller
  • Patent number: 5929119
    Abstract: A composition which is suitable for controlling fungal pests, comprising conventional additives and an effective amount of a p-hydroxyaniline derivative of the general formula I ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted bicycloalkyl, unsubstituted or substituted bicycloalkenyl;R.sup.2 and R.sup.3 independently of one another are halogen, alkyl, haloalkyl, alkoxy or haloalkoxy,and a liquid or solid carrier, its use, the use of the compounds I for controlling fungal pests, and the use of the compounds I for the preparation of the compositions.
    Type: Grant
    Filed: August 11, 1997
    Date of Patent: July 27, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Oliver Wagner, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5929117
    Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.
    Type: Grant
    Filed: August 11, 1997
    Date of Patent: July 27, 1999
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire
  • Patent number: 5925367
    Abstract: A composition for controlling harmful insects and representatives of the order Acarina, containing as biologically active components a) a substance that modifies the behavior of the pests and b) at least one pesticidally active compound, wherein the biologically active components are contained in a flowable or viscous non-hardening matrix that is resistant to water and weather, is protected against light and is suitable for distribution in the form of droplets or droplet-like units or spots that adhere to a substrate, by means of which matrix the behavior-modifying substance is protected against UV radiation and from which it is slowly released in a biologically effective amount over a prolonged period, and wherein the pesticidally active compound can be taken up in a pesticidally effective amount from the surface of the droplets or droplet-like units or spots by the pests to be controlled; as well as a method of controlling the said pests, especially plant-destructive insects.
    Type: Grant
    Filed: January 19, 1995
    Date of Patent: July 20, 1999
    Assignee: Ciba-Geigy Corporation
    Inventors: Max Angst, Fran.cedilla.ois Gugumus, Gunther Rist, Manfred Vogt, Jean Rody
  • Patent number: 5925674
    Abstract: This invention relates to cycloalkylcarboxanilides of the formula ##STR1## which are used to combat pests.
    Type: Grant
    Filed: October 26, 1995
    Date of Patent: July 20, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Krueger, Klaus Sasse, Thomas Schenke, Michael Negele, Heinz-Wilhelm Dehne
  • Patent number: 5922762
    Abstract: There are described new active compound combinations of a compound of the formula (I) ##STR1## with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.
    Type: Grant
    Filed: May 1, 1997
    Date of Patent: July 13, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wilhelm Brandes, Heinz-Wilhelm Dehne, Stefan Dutzmann, Karl-Heinz Kuck, Bernd-Wieland Kruger
  • Patent number: 5919958
    Abstract: The present invention deals with the composition of matter and the utilization of certain novel amido amine salts of meadowfoam amido propyl dimethyl amine. These materials are useful in personal care applications.
    Type: Grant
    Filed: May 1, 1998
    Date of Patent: July 6, 1999
    Assignee: Fan Tech Ltd
    Inventor: Anthony J. O'Lenick, Jr.
  • Patent number: 5914349
    Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 22, 1999
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Sasson Cohen, Yaacov Herzig, Ruth Levy, Mitchell Shirvan, Jeff Sterling, Alex Veinberg, Moussa B. H. Youdim, John P. M. Finberg
  • Patent number: 5907049
    Abstract: The present invention deals with the composition of matter and the utilization of certain amine oxides of meadowfoam amido propyl dimethyl amine. These materials are useful in personal care applications.
    Type: Grant
    Filed: May 11, 1998
    Date of Patent: May 25, 1999
    Assignee: Fan Tech LTD
    Inventor: Anthony J. O'Lenick, Jr.
  • Patent number: 5900432
    Abstract: Compounds of formula I: ##STR1## wherein, ring C, A--B, R.sup.1, n, R.sup.2, and R.sup.3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
    Type: Grant
    Filed: October 12, 1995
    Date of Patent: May 4, 1999
    Assignee: Zeneca Limited
    Inventors: James Roy Empfield, Cyrus John Ohnmacht, Keith Russell, Diane Amy Trainor, Paul James Warwick, Jr.
  • Patent number: 5889058
    Abstract: Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof.
    Type: Grant
    Filed: November 3, 1994
    Date of Patent: March 30, 1999
    Assignee: Celltech Limited
    Inventors: John Robert Porter, Thomas Andrew Millican, John Richard Morphy, Nigel Robert Arnold Beeley
  • Patent number: 5883106
    Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, and C.sub.1-4 alkyl; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino and C.sub.1-4 alkyl; R.sup.1 and R.sup.2 are each C.sub.
    Type: Grant
    Filed: February 6, 1998
    Date of Patent: March 16, 1999
    Assignee: Pfizer Inc.
    Inventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
  • Patent number: 5877220
    Abstract: The present invention provides amide-based oligomeric cationic lipids. The present invention further provides compositions of these amide-based cationic lipids with anionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions and a kit for preparing the same.
    Type: Grant
    Filed: March 6, 1997
    Date of Patent: March 2, 1999
    Assignee: Genta, Incorporated
    Inventors: David Aaron Schwartz, Brian Patrick Dwyer, William J. Daily, Kumar Srinivasan, Bob Dale Brown
  • Patent number: 5874459
    Abstract: Disclosed is a method of inhibiting anandamide amidase in an individual or animal and novel inhibitors of anandamide amidase. The disclosed method and novel compounds can be used to reduce pain in an individual or animal suffering from pain, reducing nausea in an individual undergoing chemotherapy, for example cancer chemotherapy, suppressing appetite in an individual, reducing intraocular pressure in the eye of an individual or animal suffering from glaucoma and suppressing the immune system in an individual with an organ transplant.
    Type: Grant
    Filed: November 12, 1997
    Date of Patent: February 23, 1999
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Sonyan Lin, William Adam Hill
  • Patent number: 5874444
    Abstract: Inhibition of the enzyme poly (ADP-ribose) polymerase can delay the onset of senescence and inhibitors of the enzyme can be used to treat diseases caused or exacerbated by cellular senescence.
    Type: Grant
    Filed: August 27, 1996
    Date of Patent: February 23, 1999
    Assignee: Geron Corporation
    Inventor: Michael David West
  • Patent number: 5869453
    Abstract: The present invention provides cytotoxic Epstein-Barr virus T-cell epitopes. The epitopes are selected from the group consisting of QAKWRLQTL, RYSIFFDY, HLAAQGMAY, YPLHEQHGM, SVRDRLARL, AVLLHEESM, VSFIEFVGW, FRKAQIQGL, PYLFWLAAI, TVFYNIPPMPL, PGDQLPGFSDGRACPV, VEITPYKPTW, and variants thereof. In addition, the present invention provides compositions including these epitopes for use in inducing CTL's in a subject.
    Type: Grant
    Filed: January 27, 1997
    Date of Patent: February 9, 1999
    Assignee: The Council of the Queensland Institute of Medical Research
    Inventors: Denis James Moss, Scott Renton Burrows, Rajiv Khanna, Beverley Mavis Kerr, Jacqueline Margaret Burrows, Andreas Suhrbier
  • Patent number: 5861520
    Abstract: The present invention provides a compound which is a glycolipid analog having a novel structure represented by the formula (1): ##STR1## wherein Z represents an imino group, an oxygen atom or a sulfur atom; m is an integer of from 3 to 12; and n is an integer of from 4 to 22; and shows a potent activity of inhibiting glycosidase and has potential physiological activities, for example, antiviral activity. The invention also provides a glycosidase inhibitor which comprises said glycolipid analog as an active ingredient.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: January 19, 1999
    Assignee: Seikagaku Kogyo Kabushiki Kaisha (Seikagaku Corporation)
    Inventors: Seiichiro Ogawa, Hidetoshi Tsunoda, Jinichi Inokuchi
  • Patent number: 5859054
    Abstract: Pharmacologically active leukotriene-B.sub.4 derivatives of general formula I, ##STR1## are described, in whichR.sub.1 represents CH.sub.2 OH, CH.sub.3, CF.sub.3, COOR.sub.4, CONR.sub.5 R.sub.6, orR.sub.2 represents H or an organic acid radical with 1-15 C atoms,R.sub.3 symbolizes H; C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl optionally substituted singly or multiply; C.sub.6 -C.sub.10 aryl radicals, independently of one another, optionally substituted singly or multiply by halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy; or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom,R.sub.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 cycloalkyl; C.sub.6 -C.sub.10 aryl radicals optionally substituted by 1-3 halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy; CH.sub.2 --CO--(C.sub.6 -C.sub.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: January 12, 1999
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Buchmann, Josef Heindl, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5856354
    Abstract: The invention concerns tachykinin antagonists. The compounds are neopeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.
    Type: Grant
    Filed: October 17, 1997
    Date of Patent: January 5, 1999
    Assignee: Warner-Lambert Company
    Inventors: David Christopher Horwell, William Howson, Martyn Clive Pritchard, Edward Roberts, David Charles Rees
  • Patent number: 5856537
    Abstract: Inhibitors of oleamide hydrolase, responsible for the hydrolysis of an endogenous sleep-inducing lipid (1, cis-9-octadecenamide) were designed and synthesized. The most potent inhibitors possess an electrophilic carbonyl group capable of reversibly forming a (thio) hemiacetal or (thio) hemiketal to mimic the transition state of a serine or cysteine protease catalyzed reaction. In particular, the tight binding .alpha.-keto ethyl ester 8 (1.4 nM) and the trifluoromethyl ketone inhibitor 12 (1.2 nM) were found to have exceptional inhibitory activity. In addition to the inhibitory activity, some of the inhibitors displayed agonist activity which resulted in the induction of sleep in laboratory animals.
    Type: Grant
    Filed: June 26, 1996
    Date of Patent: January 5, 1999
    Assignee: The Scripps Research Institute
    Inventors: Richard A. Lerner, Chi-Huey Wong, Dale L. Boger, Steven J. Henriksen
  • Patent number: 5849728
    Abstract: The subject invention relates to desquamation compositions comprising a combination of salicylic acid and certain zwitterionic surfactants. The subject invention further relates to methods of desquamation in mammalian skin and treating acne in mammalian skin.
    Type: Grant
    Filed: May 15, 1997
    Date of Patent: December 15, 1998
    Assignee: The Procter & Gamble Company
    Inventor: Donald L. Bissett
  • Patent number: 5846958
    Abstract: The present invention relates to methods of stimulating the growth of hematopoietic progenitor cells. In particular, it relates to the use of thiols and related compounds in stimulating the growth of hematopoietic progenitor cells in vitro and in vivo. Furthermore, the present invention relates to methods of using these compounds for the treatment of marrow failure states and immunodeficient conditions, including but not limited to myelodysplastic syndromes and acquired immunodeficiency syndrome.
    Type: Grant
    Filed: February 17, 1995
    Date of Patent: December 8, 1998
    Assignees: U.S. Bioscience, Inc., Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Robert L. Capizzi, Alan F. List
  • Patent number: 5834517
    Abstract: The present invention deals with a process for cleaning and conditioning hair and skin which comprises the contacting of hair or skin woth an effective concentration of certain novel meadowfoam derived sulfosuccinates. These materials are useful as cosmetic ingredients as additives to shampoo systems where outstanding liquidity, resistance to oxidation, and minimal odor variation are required.
    Type: Grant
    Filed: May 1, 1997
    Date of Patent: November 10, 1998
    Assignee: Fan Tech Ltd.
    Inventor: Anthony J. O'Lenick, Jr.
  • Patent number: 5830869
    Abstract: The present invention provides novel thiadiazole amide derivatives represented by formula I ##STR1## The compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, predominantly stromelysins, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthritis, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis, periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, inflammation and other diseases related to connective tissue degradation.
    Type: Grant
    Filed: June 18, 1997
    Date of Patent: November 3, 1998
    Inventors: Mark Allen Mitchell, Heinrich Josef Schostarez, Linda Louise Maggiora, Thomas J. Lindberg
  • Patent number: 5827852
    Abstract: Pharmaceutical composition suitable for coating comprising a composition for oral administration in unit dosage form wherein said composition has been coated with from about 0.01% to about 10% by weight of the composition with a volatile aromatic compound 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.
    Type: Grant
    Filed: September 16, 1994
    Date of Patent: October 27, 1998
    Assignee: The Procter & Gamble Company
    Inventors: Carmelita Macklin Russell, Allen I. Dines, James Grigg Upson
  • Patent number: 5827891
    Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 27, 1998
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
  • Patent number: 5824650
    Abstract: The invention relates to a therapeutic composition for topical application containing at least one product with an irritant side effect and a substance P antagonist for reducing or even eliminating the irritant effect of this product.It also relates to the use of a substance P antagonist for the preparation of a pharmaceutical composition for topical application containing at least one product with an irritant side effect for reducing or even eliminating the irritant effect of this product.The substance P antagonist may be a peptide compound or a nitrogen-containing compound or a nitrogen-, sulphur- or oxygen-containing heterocyclic compound.
    Type: Grant
    Filed: December 19, 1995
    Date of Patent: October 20, 1998
    Assignee: L'Oreal
    Inventors: Olivier De Lacharriere, Lionel Breton
  • Patent number: 5792776
    Abstract: Disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF and/or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 27, 1994
    Date of Patent: August 11, 1998
    Assignee: Cytomed, Inc.,
    Inventors: Tesfaye Biftu, Ralph Scannell, Xiong Cai, Sajjat Hussoin
  • Patent number: 5783593
    Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: April 29, 1996
    Date of Patent: July 21, 1998
    Assignee: Abbott Laboratories
    Inventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
  • Patent number: 5760023
    Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.
    Type: Grant
    Filed: July 14, 1997
    Date of Patent: June 2, 1998
    Assignee: Adolor Corporation
    Inventors: John J. Farrar, An-Chih Chang, Virendra Kumar, Wei Yuan Zhang, Alan Cowan
  • Patent number: 5760085
    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: September 12, 1996
    Date of Patent: June 2, 1998
    Assignee: The Procter & Gamble Company
    Inventors: William Fletcher Beck, Sekhar Mitra
  • Patent number: 5756547
    Abstract: Bucillamine and N-2,2-dimethyl-3-mercaptopropionyl)-L-cysteine or related compounds can be used to prevent damage to living tissue from the formation or presence of reactive oxygen species. These reactive oxygen species are formed when tissue is first rendered hypoxic due to interruption of blood flow and then reoxygenated by restoration of blood flow. In particular, the invention is directed to the administration of bucillamine and N-2,2-dimethyl-3-mercaptopropionyl)-L-cysteine prior to or coincidental with reperfusion to prevent damage to myocardium from formation of reactive oxygen species. Also presented are application of these compounds to similar ischemia-related cell injury in other organs.
    Type: Grant
    Filed: May 23, 1997
    Date of Patent: May 26, 1998
    Assignee: Regents of the University of Colorado
    Inventor: Lawrence D. Horwitz
  • Patent number: 5753704
    Abstract: Disclosed are certain novel polyunsaturated dioic acids having between 8 and 16 carbon atoms (inclusive), excluding those compounds in the group consisting of: 2,5 octadienedioic acid; 1,7 octadienedioic acid; 2,4,6 octatrienedioic acid; and 1,3,5,7 nonatetraenedioic acid; 2,5,8 decatrienedioic acid; 3,6 dodecadienedioic acid; 3,13 hexadecadienedioic acid. Also disclosed are pharmaceutical or cosmetic compositions comprising unsaturated dioic acids and certain of their derivatives. Also disclosed are methods of treating human skin and a method of preparing unsaturated dioic acids.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: May 19, 1998
    Assignee: Unichema Chemie B.V.
    Inventors: Nigel Lindner, John Casey
  • Patent number: 5750559
    Abstract: The antireactive-antiasthmatic effect of inhaled loop diuretics is potentiated by the use of a combination of a loop diuretic and a non-steroidal anti-inflammatory drug as an inhalant for combating asthma. The use of a cyclooxygenase inhibitor as the non-steroidal anti-inflammatory drug is preferred, particularly preferred is the use of furosemide as the loop diuretic. Especially advantageous is the use of piretanide as the loop diuretic. Particularly preferred is the use of acetylsalicylic acid as the non-steroidal anti-inflammatory drug.The most remarkable finding of this invention is the excellent and steady protective effect afforded by the combination of the two drugs in the patients with late asthmatic reactions between the seventh and eighth hour, when the effect of treatment with either drug alone appeared to be progressively decreasing.
    Type: Grant
    Filed: August 5, 1994
    Date of Patent: May 12, 1998
    Assignee: Sebastiano Bianco
    Inventor: Sebastiano Bianco
  • Patent number: 5744453
    Abstract: The present invention relates to methods of preventing or treating an infection or disease caused by an infectious agent. The present invention also relates to the augmentation of the efficacy of existing anti-infective agents by the co-administration of the compounds described herein.
    Type: Grant
    Filed: January 5, 1996
    Date of Patent: April 28, 1998
    Inventors: Clifford S. Mintz, Natan A. Kogan, Ramesh Kakarla, Helena R. Axelrod, Michael J. Sofia
  • Patent number: 5712312
    Abstract: The invention relates to a compound selected from these of formula (I): ##STR1## in which R.sub.7, R.sub.8, Y, n and A are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.
    Type: Grant
    Filed: April 12, 1996
    Date of Patent: January 27, 1998
    Assignee: Adir et Compagnie
    Inventors: Michel Langlois, Monique Mathe-Allainmat, Philippe Delagrange, Pierre Renard, Beatrice Guardiola
  • Patent number: 5703129
    Abstract: A series of 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives of Formula I have been synthesized. ##STR1## As inhibitors of the production of .beta.-amyloid protein from .beta.-amyloid precursor protein, these compounds are expected to be effective in treating patients suffering from or susceptible to conditions or disorders linked to brain accumulation of .beta.-amyloid protein; e.g., Alzheimer's Disease and Down's Syndrome.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: December 30, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kevin Felsenstein, David W. Smith, Michael A. Poss, Prasad Chaturvedula, Charles P. Sloan
  • Patent number: 5693630
    Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.
    Type: Grant
    Filed: October 26, 1994
    Date of Patent: December 2, 1997
    Assignee: Astra Aktiebolag
    Inventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
  • Patent number: 5688819
    Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.
    Type: Grant
    Filed: February 22, 1996
    Date of Patent: November 18, 1997
    Assignee: Allergan
    Inventors: David F. Woodward, Steven W. Andrews, Robert M. Burk, Michael E. Garst
  • Patent number: 5684049
    Abstract: A compound for use as a medicine having the formula ##STR1## a pharmaceutically acceptable acid addition salt form or a stereochemically isomeric form thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-6 alkyl or C.sub.3-6 cyclo-alkyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom bearing said R.sup.1 and R.sup.2 may form a pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl or 4-C.sub.1-4 alkylpiperazinyl group; X is O or S; R.sup.3 is hydrogen or C.sub.1-6 alkyl; R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, nitro, trifluoromethyl, cyano, aminomethyl, carboxyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl-carbonyl, aminocarbonyl, or hydroxy; R.sup.7 is hydrogen or halo; and R.sup.8, R.sup.9 and R.sup.10 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.
    Type: Grant
    Filed: March 27, 1995
    Date of Patent: November 4, 1997
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges Henri Van Daele, Marc Gustaaf Verdonck, Jean-Paul Rene Bosmans, Paul Adriaan Janssen