Z-c(=o)-o-y, Wherein Z Contains A Benzene Ring Patents (Class 514/532)
  • Patent number: 5721103
    Abstract: Novel trienoic compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 24, 1998
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Marcus F. Boehm, Lin Zhang, Youssef L. Bennani, Alex M. Nadzan
  • Patent number: 5719133
    Abstract: A dietary composition comprising, based on total caloric content of the composition,a) a carbohydrate component which comprises from 50 to 65% of the total caloric content;b) a lipid component which comprises from 20 to 35% of the total caloric content; andc) an amino acid component which comprises from 10 to 20% of the total caloric content and which comprises specified amino acids and amounts thereof is useful providing nutrition to human adolescents.
    Type: Grant
    Filed: September 21, 1994
    Date of Patent: February 17, 1998
    Assignee: Novartis Nutrition AG
    Inventors: Mary K. Schmidl, Carol J. Lowry
  • Patent number: 5719134
    Abstract: A dietary composition comprising, based on total caloric content of the composition,a) a carbohydrate component which comprises from 50 to 65% of the total caloric content;b) a lipid component which comprises from 20 to 35% of the total caloric content; andc) an amino acid component which comprises from 10 to 20% of the total caloric content and which comprises specified amino acids and amounts thereof is useful providing nutrition to human adolescents.
    Type: Grant
    Filed: September 17, 1996
    Date of Patent: February 17, 1998
    Assignee: Novartis Nutrition AG
    Inventors: Mary K. Schmidl, Carol J. Lowry
  • Patent number: 5716624
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: February 10, 1998
    Assignee: C.I.R.D. Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5710314
    Abstract: Compounds of formula I ##STR1## and possible isomers and isomeric mixtures thereof, wherein a)X is CH.sub.2 F or CHF.sub.2 ;Y is CH andZ is OMe, orb)X is CH.sub.2 F or CHF.sub.2 ;Y is a nitrogen atom andZ is OMe or NHCH.sub.3,and wherein alsom is 0, 1, 2, 3, 4 or 5 andU represents identical or different substituents selected from halogen, cyano, nitro, C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkenyloxyiminomethyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkoxyiminomethyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy and unsubstituted or substituted benzyl or represents substituents at two adjacent positions of the phenyl ring of formula I that define a fused hydrocarbon bridge so as to form a larger hydrocarbon ring having up to 14 carbon atoms, are suitable for controlling and preventing microorganisms, insects and Acarina on plants.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: January 20, 1998
    Assignee: Novartis Corporation
    Inventors: Albert Pfiffner, Stephan Trah
  • Patent number: 5705533
    Abstract: 10-thio-substituted 1,8-dihydroxy-9(10H) anthracenones, therapeutic compositions containing at least one of the 10-thio-substituted 1,8-dihydroxy-9(10H) anthracenones of the invention and methods of treating inflammatory conditions are provided.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 6, 1998
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Klaus Muller, Hsu-Shan Huang, Wolfgang Wiegrebe
  • Patent number: 5702688
    Abstract: Preventive as well as therapeutic treatment to alleviate cosmetic conditions and symptoms of dermatologic disorders with amphoteric compositions containing alpha hydroxyacids, alpha ketoacids, related compounds or polymeric forms of hydroxyacids is disclosed. The cosmetic conditions and the dermatologic disorders in which the amphoteric compositions and the polymeric compounds may be useful include dry skin, dandruff, ache, keratoses, psoriasis, eczema, pruritus, age spots, lentigines, melasmas, wrinkles, warts, blemished skin, hyperpigmented skin, kyperkeratotic skin, inflammatory dermatoses, skin changes associated with aging, and skin requiring cleansers.
    Type: Grant
    Filed: October 7, 1993
    Date of Patent: December 30, 1997
    Assignee: Tristrata Technology, Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5700811
    Abstract: This invention is directed to compounds having the structure: ##STR1## wherein R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine or thiazoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, and n is an integer from about 4 to about 8. This invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of the compounds of the present invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: December 23, 1997
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind
  • Patent number: 5696162
    Abstract: Compounds of Formula 1 ##STR1## wherein m is 1-4; R.sub.1 -R.sub.4 independently are hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, or I; R.sub.5 is hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, I, lower alkoxy or lower thioalkoxy of 1-6 carbons; R.sub.6 is hydrogen, lower alkyl, Cl, Br, I, OR.sub.11, SR.sub.11, OCOR.sub.11, SCOR.sub.11, NH.sub.2, NHR.sub.11, N(R.sub.11).sub.2, NHCOR.sub.11 OR NR.sub.11 --COR.sub.11 ; R.sub.20 is independently hydrogen or lower alkyl; Y is an aromatic group such as phenyl or naphthyl, or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl and oxazolyl; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: December 9, 1997
    Assignee: Allergan
    Inventor: Roshantha A. Chandraratna
  • Patent number: 5691376
    Abstract: A compound of the following structure: ##STR1## wherein R.sub.8 =H: R.sub.1 =alkyl, cycloalkyl, arylalkyl, aryl;R.sub.2 =cycloalkyl, aryl, C.sub.3 -C.sub.10 alkyl;X,Y=O, S(O).sub.n, NH;Z=CO.sub.2 R.sub.3, C(O)CO.sub.2 R.sub.3, CH(OH)CO.sub.2 R.sub.3, CHFCO.sub.2 R.sub.3, CF.sub.2 CO.sub.2 R.sub.3, CONR.sub.3 R.sub.4, CONR.sub.3 OR.sub.4, CONR.sub.3 NR.sub.4 R.sub.5, 1-tetrazole, C(O)CONR.sub.3 R.sub.4, CH(OH)CONR.sub.3 R.sub.4, CF.sub.2 CONR.sub.3 R.sub.4R.sub.3, R.sub.4, R.sub.5 =hydrogen, alkyl, aryl, aryalkyl, cycloalkyl, or fluoroalkyl;halo=Cl, Br, or I;fluoroalkyl=CF.sub.3, CHF.sub.2, CH.sub.2 F, CH.sub.2 CF.sub.3, C.sub.2 F.sub.5 ;cycloalkyl=C.sub.3 -C.sub.6 cycloalkyl;arylalkyl=C.sub.1 -C.sub.4 alkyl aryl;aryl=phenyl, furanyl, thienyl, or pyridyl; andn=0-2;or pharmaceutically acceptable salts thereof, useful in the treatment of asthma, and allergic and inflammatory diseases, as well as methods of treatment and pharmaceutical compositions utilizing the same.
    Type: Grant
    Filed: October 17, 1996
    Date of Patent: November 25, 1997
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Caggiano, Joseph Prol, Jr.
  • Patent number: 5690967
    Abstract: Compositions for improved topical delivery of lactic acid comprising lactic acid and an amphoteric or pseudoamphoteric agent.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 25, 1997
    Assignee: Tristrata Technology, Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5681846
    Abstract: The present invention is directed to improved pharmaceutical compositions employing paclitaxel that are formulated to increase stability and solubility. These improved formulations are useful in long-term, multi-day continuous infusion protocols, and have the advantage of reducing the number of infusion system breaks during the entire period of drug administration. Also disclosed are kits for use in preparing paclitaxel for long-term infusion and enhanced solubility.
    Type: Grant
    Filed: March 17, 1995
    Date of Patent: October 28, 1997
    Assignee: Board of Regents, The University of Texas System
    Inventor: Lawrence A. Trissel
  • Patent number: 5681835
    Abstract: Prescribed herein are novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.
    Type: Grant
    Filed: April 25, 1994
    Date of Patent: October 28, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventor: Timothy Mark Willson
  • Patent number: 5668182
    Abstract: Various hydroxy benzaldehyde derivatives including Vanillin, a natural product derived from the vanilla bean that is commonly used as a flavoring agent, is administered by injection (i.v., i.m., s.c., and the like) or intravenous infusion in an effective dose amount to a patient in need of calming or sedation.
    Type: Grant
    Filed: August 19, 1996
    Date of Patent: September 16, 1997
    Assignee: Virginia Commonwealth University
    Inventors: Donald J. Abraham, Louis S. Harris, B. J. Meade, Albert E. Munson, Paul S. Swerdlow, Graham A. Patrick
  • Patent number: 5654331
    Abstract: Diaromatic compounds, characterised in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: August 5, 1997
    Assignee: Centre International De Recherches Dermatologiques Galderma (Cird Galderma)
    Inventor: Jean-Michel Bernardon
  • Patent number: 5654329
    Abstract: Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is 0 and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5 R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, CH.sub.2 NR.sub.5 COR.sub.7, CHO, CH(OR.sub.8).sub.2, CH(OR.sub.9 O), --COR.sub.10, CR.sub.10 (OR.sub.8).sub.2, or CR.sub.10 OR.sub.9 O, where R.sub.4 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 5, 1997
    Assignee: Allergan
    Inventors: Robert M. Burk, David F. Woodward
  • Patent number: 5646182
    Abstract: The present invention provides methods for treating autoimmune disease in humans by administering to an afflicted host pharmaceutical compositions containing a therapeutically effective amount of a combination of ##STR1## in a weight ratio ranging from about 1:1 to about 1:10 (A:B); wherein R is OH, NH.sub.2, OW, or H;X is H, F, Cl, Br, I, OH, OW, NO.sub.2, or NH.sub.2 ;Y is H, F, Cl, Br, or I;W is ##STR2## or a C.sub.1 to C.sub.12 aliphatic group; Z is an aliphatic or aromatic group of C.sub.1 to C.sub.12 ;X and Y can both vary within the compound; or pharmaceutically acceptable salts thereof.Particularly disclosed herein is a composition comprising a 1 to 4 ratio of the sodium salts of phenylacetylglutamine and phenylacetic acid, formulated in both oral and parenteral forms clinically useful in the treatment of rheumatoid arthritis, lupus erythematosus, vasculitis, insulin dependent diabetes mellitus and multiple sclerosis.
    Type: Grant
    Filed: June 15, 1992
    Date of Patent: July 8, 1997
    Inventor: Stanislaw R. Burzynski
  • Patent number: 5643949
    Abstract: Therapeutic as well as preventative measures to improve the cosmetic conditions or to alleviate the symptoms of dermatologic disorders with phenyl alpha acyloxyalkanoic acids and derivatives is disclosed. The cosmetic conditions and dermatologic disorders in humans in which the compounds may be useful include brittle or soft nails; abnormally thin skin, mucous membranes or wound; friction blisters; brittle hairs; pruritus; acne; and diseased nails, skin or mucous membranes due to natural or unnatural causes including but not limited to inflammations or infections. The phenyl alpha acyloxyalkanoic acids and derivatives include, for example, diphenyl alpha acetoxyacetic acid, phenyl alpha acetoxyacetic acid, phenyl alpha methyl alpha acetoxyacetic acid and phenyl alpha acetoxypropanoic acid. The compositions containing the active ingredients are also useful for treatment of skin, nails and hair conditions or disorders in domestic animals.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: July 1, 1997
    Assignee: Tristrata, Inc.
    Inventors: Eugene J. Van Scott, Ruey J. Yu
  • Patent number: 5616614
    Abstract: The invention relates to a compound selected from those of general formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, an optical isomer, and an addition salt thereof with a pharmaceutically-acceptable base. Medicinal product which is useful in the treatment of disorders linked to abnormal melatonin activity.
    Type: Grant
    Filed: January 25, 1995
    Date of Patent: April 1, 1997
    Assignee: Adir ET Compagnie
    Inventors: Said Yous, Daniel Lesieur, Patrick Depreux, B eatrice Guardiola-Lemaitre, G erard Adam, Pierre Renard, Daniel H. Caignard
  • Patent number: 5610188
    Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.
    Type: Grant
    Filed: December 30, 1994
    Date of Patent: March 11, 1997
    Assignee: University of Florida
    Inventors: Richard H. Hammer, Nicholas S. Bodor
  • Patent number: 5602164
    Abstract: Obesity is treated by the administration to a subject of a compound having the general formula (I): R.sub.4 --(CH.sub.2).sub.n --CO--N(R.sub.1)--CH(R.sub.2)--CO(--R.sub.3), wherein R.sub.1 represents H or CH.sub.3 ; R.sub.2 represents a side chain of a naturally occurring amino acid; R.sub.3 represents OH, OCH.sub.2 CH.sub.3 and NH.sub.2 ; n is 6-18; and R.sub.4 represents CH.sub.3 or a group having the general formula (II): R.sub.3 --CO--CH(R.sub.2)--N(R.sub.1)--CO--, wherein R.sub.1, R.sub.2 and R.sub.3 have the above meanings. The compounds of formula (I) wherein R.sub.4 is a group of formula (II), are novel compounds.
    Type: Grant
    Filed: March 18, 1996
    Date of Patent: February 11, 1997
    Assignee: Senyorina Ltd.
    Inventors: Meir Shinitzky, Avner Shenfeld
  • Patent number: 5597839
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: January 28, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5591773
    Abstract: A method of inhibiting the formation of a cataract in an eye by contacting the eye with a compound having the structure: ##STR1## is described. Also described is a method of inhibiting the progression of cataract formation in an eye. Methods comprising administering a pharmaceutical composition comprising the above compound to inhibit the formation of a cataract in the eye of a subject and to inhibit progression of cataract formation in the eye of a subject are also described. The above compound also prevents diseases resulting from oxidative stress, including diseases comprising tumor formation resulting from oxidative stress, and also inhibits the progression of diseases resulting from oxidative stress. The above compound may furthermore be used to treat an HIV infection when combined in a pharmaceutical composition with a substance which inhibits HIV replication.
    Type: Grant
    Filed: March 14, 1994
    Date of Patent: January 7, 1997
    Assignees: The Trustees of Columbia University in the City of New York, New York University
    Inventors: Dezider Grunberger, Krystyna Frenkel
  • Patent number: 5571825
    Abstract: The present invention provides a method of selectively inhibiting prostaglandin G/H synthase-2 that comprises administering to a patient in need of such inhibition an inhibiting amount of a compound having the Formula I, II or III ##STR1## wherein the R groups and heterocycles are defined in the disclosure.
    Type: Grant
    Filed: March 31, 1995
    Date of Patent: November 5, 1996
    Assignee: Warner-Lambert Company
    Inventors: Diane H. Boschelli, David T. Connor, Richard D. Dyer, Sonya S. Khatana, James B. Kramer, William H. Roark
  • Patent number: 5565466
    Abstract: The invention is directed to improved methods for modulating the human sexual response by administering a vasodilator to the circulation by a route of administration that avoids the "first-pass" effect.
    Type: Grant
    Filed: August 9, 1994
    Date of Patent: October 15, 1996
    Assignee: Zonagen, Inc.
    Inventors: Diane-Marie Gioco, Adrian Zorgniotti, deceased
  • Patent number: 5559134
    Abstract: The invention relates to leukotriene-B.sub.4 antagonists of formula I ##STR1## in which n represents a whole number from 2 to 5,X represents a direct bond, 1 to 6 methylene units, an ortho-, meta- or para-substituted phenyl ring or a meta- or para-substituted pyridine ring,Y represents a bond to a hydrogen atom and simultaneously to a hydroxy group, a double-bound oxygen atom or --O--CH.sub.2 --CH.sub.2 --O--,R.sub.1 and R.sub.2 represent the radical OH, --O--(C.sub.1 -C.sub.4)--alkyl, O--(C.sub.3 -C.sub.6)--cycloalkyl, --O--(C.sub.6 -C.sub.10)--aryl, --O--(C.sub.7 -C.sub.12)--aralkyl, O--(CH.sub.2)--CO-- (C.sub.6 -C.sub.10)--aryl or the radical NHR.sub.3 with R.sub.3 meaning hydrogen, (C.sub.1 -C.sub.4)--alkyl, (C.sub.3 -C.sub.6)--cycloalkyl or (C.sub.7 -C.sub.12)--aralkyl as well as their salts with physiologically compatible bases and their cyclodextrin clathrates.
    Type: Grant
    Filed: March 23, 1995
    Date of Patent: September 24, 1996
    Assignee: Schering Aktiengesellschaft
    Inventors: Bernd Buchmann, Werner Skuballa, Josef Heindl, Wolfgang Fr ohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5508275
    Abstract: Lipid-selective antioxidants of the formula I(A).sub.a (L)(X).sub.a, (I),in whichA=an antioxidative component,L=a bridging member,X=a lipophilic componenta and a'=independently of one another the numbers 1 or 2.The compounds are used for the protection of lipid-containing substances against oxidation and in pharmaceuticals for the prophylaxis and treatment of diseases in which bioradicals are involved, in particular of coronary, circulatory and vascular diseases.
    Type: Grant
    Filed: March 15, 1994
    Date of Patent: April 16, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Klaus-Ulrich Weithmann, Gunther Wess, Dirk Seiffge
  • Patent number: 5504111
    Abstract: This invention relates to methods for treating Adult Respiratory Distress Syndrome (ARDS) which involves the administration of 2,3-alkylcarbonyloxybenzoic acid and salts thereof wherein the alkyl group has 2-18 carbon atoms.
    Type: Grant
    Filed: December 30, 1994
    Date of Patent: April 2, 1996
    Assignee: Medichem Research, Inc.
    Inventors: Michael T. Flavin, Deanna J. Nelson, Julian F. Borgia, deceased, Gary Jesmok
  • Patent number: 5502061
    Abstract: The present invention provides HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
    Type: Grant
    Filed: September 26, 1994
    Date of Patent: March 26, 1996
    Assignee: Eli Lilly and Company
    Inventors: Kwan Y. Hui, Charles D. Jones, Louis N. Jungheim, Pamela A. Pennington
  • Patent number: 5492917
    Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: February 20, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Ralph A. Rivero, Peter D. Williams, Daniel F. Veber
  • Patent number: 5482970
    Abstract: Novel compositions comprising an antiandrogenic compound of the formula ##STR1## wherein R is COR.sub.1 wherein R.sub.1 is loweralkyl and a vehicle comprising a metabolism modulator and a polar organic solvent, and a method of controlling the membrane permeation and metabolism of the compound thereof are disclosed.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: January 9, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Kwon H. Kim, Barry Koplowitz, Norman L. Henderson
  • Patent number: 5472970
    Abstract: Allylaminoesters of the formula (I): ##STR1## in which: R.sub.1 is H or low-molecular-weight alkyl,R.sub.2 is low-molecular-weight alkyl, cycloalkyl, or low-molecular-weight phenylcycloalkyl, pyridyl or phenyl, low-molecular-weight phenylalkyl, low-molecular-weight diphenylalkyl, low-molecular-weight phenylalkenyl, in which the phenyl cycle may be mono-, di- or trisubstituted by chlorine atoms, low-molecular-weight alkyl radicals, low-molecular-weight alkoxy, or trifluoromethyl, acetamide or acetyloxy radicals, their racemic forms, their (S) enantiomers and their addition salts. Also, antiallergic drugs containing the same.
    Type: Grant
    Filed: September 19, 1994
    Date of Patent: December 5, 1995
    Assignee: Institut de Recherche Jouveinal S.A.
    Inventors: Alain P. Calvet, Agnes G. Grouhel, Jean-Louis Junien
  • Patent number: 5457128
    Abstract: Disclosed is a topical preparation for healing wounds of the skin, which can demonstrate remarkable effects of the treatment of wounds of the skin, such as an ulcer of the skin, traumatogenic wounds caused by the abrasion of the skin, traumatogenic wounds caused by the defect of the skin, an ulcer of the crus, zoster, and so on. The topical preparation contains at least one pharmaceutically effective compound selected from gefarnate, and sofalcone.
    Type: Grant
    Filed: November 29, 1993
    Date of Patent: October 10, 1995
    Assignee: Dott Limited Company
    Inventor: Akira Yanagawa
  • Patent number: 5451205
    Abstract: A method for facilitating autologous blood use by a patient facing a loss of blood, comprising the steps of removing and preferably storing a portion of the patient's blood, intravenously administering a biocompatible liquid in sufficient quantity to substantially maintain the patient's hemodynamic stability, wherein the liquid comprises an effective oxygen-delivery enhancing amount of a biocompatible synthetic oxygen carrier, after which the patient undergoes a loss of blood, and then readministering blood to the patient, preferably the stored blood. In one embodiment, the biocompatible liquid further comprises a hemodiluent and the hemodiluent is administered separately from the oxygen carrier.
    Type: Grant
    Filed: June 3, 1994
    Date of Patent: September 19, 1995
    Assignee: Alliance Pharmaceutical Corp.
    Inventors: Duane J. Roth, Peter E. Keipert, Nicholas S. Faithfull, Thomas F. Zuck, Jean G. Riess
  • Patent number: 5446067
    Abstract: Oxime ethers of the formula ##STR1## wherein m, G, R, R.sup.1, X, Y, and Z are as defined herein and fungicides containing these compounds.
    Type: Grant
    Filed: July 12, 1994
    Date of Patent: August 29, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Remy Benoit, Hubert Sauter, Reinhard Kirstgen, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5439925
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: August 8, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, Willliam R. Pilgrim
  • Patent number: 5434186
    Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: July 18, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff
  • Patent number: 5434180
    Abstract: The present invention relates to new polycyclic aromatic derivatives, to processes for their preparation and to their use in therapeutic and cosmetic formulations.
    Type: Grant
    Filed: March 27, 1992
    Date of Patent: July 18, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (CIRD Galderma)
    Inventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
  • Patent number: 5420160
    Abstract: There are described new 1-alkoxyhexatriene-2-carboxylates of the formula (I) ##STR1## in which R represents substituted phenyl,and a plurality of processes for their preparation.The new 1-alkoxyhexytriene-2-carboxylates are used as pesticides.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: May 30, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Gayer, Peter Gerdes, Heinz-Wilhelm Dehne, Stefan Dutzmann
  • Patent number: 5416068
    Abstract: .alpha.-Phenylacrylic acid derivatives I ##STR1## n=1; y=1;R.sup.1 =methylR.sup.2 =methyl, ethyl or methoxymethylR.sup.3 =H;R.sup.4 is 2,5-dimethylphenyl, 2,5-dichloropehnyl, 2-methyl-5-chlorophenyl, 2,4-dimethylphenyl, 2-chloro-5-methylphenyl, 2,3,5-trimethylphenyl or 2-methyl-5-isopropylphenyl.W=oxygen;A is --O--, --S--, --OCH.sub.2 --, --SCH.sub.2 --, --CH.dbd.CH--, --CO--OCH.sub.2 -- or --N(CH.sub.3) --CH.sub.2 --; methods for their preparation, agents containing them for combating injurious fungi and pests, and their use.
    Type: Grant
    Filed: January 3, 1994
    Date of Patent: May 16, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Wassilios Grammenos, Reinharad Kirstgen, Klaus Oberdorf, Hubert Sauter, Franz Roehl, Rainer Otter, Eberhard Ammermann, Gisela Lorenz, Uwe Kardorff, Christoph Kuenast
  • Patent number: 5393764
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents O, S, or CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl and R.sup.6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or R is (CH.
    Type: Grant
    Filed: August 25, 1993
    Date of Patent: February 28, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5389619
    Abstract: Compounds of the formula I ##STR1## where n, W, X, Y, Z, R.sup.1, R.sup.2, and R.sup.3 are as defined herein exhibit fungicidal, insecticidal, and acaracidal activity.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: February 14, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Doetzer, Hubert Sauter, Horst Wingert, Reinhard Kirstgen, Albrecht Harreus, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5387594
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: August 4, 1992
    Date of Patent: February 7, 1995
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5380883
    Abstract: A compound of the formula ##STR1##
    Type: Grant
    Filed: April 12, 1993
    Date of Patent: January 10, 1995
    Assignee: Roussel-Uclaf
    Inventors: Marc Benoit, Sylvain Laugraud, Jean-Louis Brayer
  • Patent number: 5356931
    Abstract: Alpha-Arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; n is 0 or 1;m is 0, 1, 2, 3 or 4;R.sup.1 is cyano, cyanato, thiocyanato, nitro, hydroxyl, carboxyl, haloalkyl, haloalkoxy, unsubstituted or substituted cycloalkyl, cycloalkenyl, cycloalkadienyl, alkenyl, alkynyl or amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, unsubstituted or substituted benzyloxycarbonyl, benzoyl, phenylalkyl, phenylalkoxy or phenoxyalkyl,or R.sup.1 together with one of the radicals R.sup.2 forms an unsubstituted or substituted 1,3-butadiene-1,4-diyl group or an unsubstituted or substituted chain consisting of carbon members and an oxygen member, andR.sup.2 is halogen, unsubstituted or substituted alkyl, alkoxy, alkenyloxy, alkynyloxy, alkadienyloxy, benzyloxy or benzylthio, are used for controlling pests.
    Type: Grant
    Filed: January 4, 1993
    Date of Patent: October 18, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Kirstgen, Rainer Otter, Christoph Kuenast, Uwe Kardorff, Wolfgang Steglich, Gunda Bertram
  • Patent number: 5352693
    Abstract: A solid composition comprising a dispersion of at least one alkyl ester of p-hydroxybenzoic acid in a hydroxymethyl-substituted dimethylhydantoin, its method of preparation, and its use as a preservative in shampoos, lotions, and cosmetics.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: October 4, 1994
    Assignee: Lonza Inc.
    Inventor: Thomas E. Farina
  • Patent number: 5349112
    Abstract: Novel cyclic anti-tumor promoter compounds and therapeutic compositions are disclosed, along with method for their production and use as anti-cancer and cancer-prevention agents.
    Type: Grant
    Filed: November 26, 1993
    Date of Patent: September 20, 1994
    Assignee: University of Hawaii
    Inventor: Marcus A. Tius
  • Patent number: 5342835
    Abstract: Compounds of formula ##STR1## in which: CYCLE surrounded by a semicircle represents, with the two carbon atoms to which the semicircle is linked, a carbon-containing, optionally heterocyclic, ring containing at least one ethylenic or aromatic bond between the two carbon atoms which carry the --C(Z).dbd.Y group and the phenyl group, Y is oxygen or sulphur, Z is NR.sub.1 R.sub.2, R.sub.1 and R.sub.2, each represents optionally substituted alkyl, alkoxy or cycloalkyl; alkenyl or alkynyl; or --NR.sub.1 R.sub.2 represents saturated or unsaturated heterocyclyl;R.sub.3, R.sub.4 and R.sub.5, each represents a hydrogen or halogen atom (at least one of R.sub.3, R.sub.4 and R.sub.5 being other than hydrogen or halogen); optionally substituted amino; optionally halogenated hydroxylated alkyl, alkoxy, alkylalkoxy or alkylthio; or R.sub.3 and R.sub.4 (in the 3- and 4-positions) can together form a single divalent radical with 3 or 4 members containing 1 or 2 non-adjacent oxygen atoms; are useful as agricultural fungicides.
    Type: Grant
    Filed: January 3, 1992
    Date of Patent: August 30, 1994
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Regis Pepin, Christian Schmitz, Guy-Bernard Lacroix, Philippe Dellis, Christine Veyrat
  • Patent number: 5334607
    Abstract: Antimycotics containing a compound of the formula ##STR1## where .dbd.Y is .dbd.CH--OCH.sub.3, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3, .dbd.CH--SCH.sub.3 or .dbd.N--OCH.sub.3, and X is oxygen, or X may also be NH if Y is .dbd.N--OCH.sub.3,Z is halogen, nitro, cyano, unsubstituted or substituted organic radicals, OR.sup.12, SR.sup.13, SOR.sup.14, SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22 R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--N.dbd.CR.sup.27 R.sup.28 andU, V, W can be hydrogen or one of the meanings given for Z, or where two of Z, U, V and W in adjacent positions on the phenyl ring can form an unsubstituted or substituted five- or six-membered, aromatic or aliphatic ring which may contain one to three hetero atoms (N, S, O), and R.sup.12 to R.sup.26 are identical or different and are hydrogen, unsubstituted or substituted organic radicals,are used for controlling mycoses.
    Type: Grant
    Filed: May 28, 1992
    Date of Patent: August 2, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Hubert Sauter, Gisela Lorenz, Gerd Steiner, Bernd Janssen, Timm Anke, Wolfgang Steglich
  • Patent number: RE34805
    Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: December 6, 1994
    Assignee: Centre International de Recherches Dermatologiques (CIRD)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon