The Nitrogen Is Bonded Directly To A Ring And Is In Same Side Chain As Ester Function Patents (Class 560/43)
  • Patent number: 6159482
    Abstract: The invention relates to the use of oxamate derivatives in a composition, as agents for depigmenting and/or bleaching human skin, head hair and/or other hairs. The invention also relates to a process for depigmenting and/or bleaching the skin, head hair and/or other hairs, which includes applying a composition comprising oxamate derivatives to human skin, head hair and/or other hairs.
    Type: Grant
    Filed: August 26, 1998
    Date of Patent: December 12, 2000
    Assignee: L'Oreal
    Inventors: Remy Tuloup, Michel Philippe
  • Patent number: 6156924
    Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.
    Type: Grant
    Filed: January 6, 1999
    Date of Patent: December 5, 2000
    Assignee: Eli Lilly and Company
    Inventors: William J. Hornback, Scott C. Mauldin, John E. Munroe
  • Patent number: 6153652
    Abstract: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: November 28, 2000
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Clark N. Eid, James E. Audia
  • Patent number: 6143208
    Abstract: An optical frequency conversion element has a wave-guiding layer which consists of a .chi..sup.(2) -active ferroelectric liquid crystal. The monomeric or polymeric liquid crystal material has a periodic structure which permits the so-called quasi phase matching of a guided laser beam. The period length of the structure is equal to twice the coherence length l.sub.c =.pi./.DELTA..beta. of the material, whereby .DELTA..beta.=.beta..sub.o (2.omega.)-2.beta..sub.o (.omega.), with .omega.=angular frequency of the fundamental wave, 0=zero-order mode and .beta.=propagation constant of the mode.
    Type: Grant
    Filed: February 12, 1997
    Date of Patent: November 7, 2000
    Assignee: Rolic AG
    Inventors: Richard Buchecker, Xin Hua Chen, Jurg Fufschilling, Rolf-Peter Herr, Martin Schadt, Klaus Schmitt
  • Patent number: 6124494
    Abstract: The present invention provides compounds which inhibit. an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.
    Type: Grant
    Filed: January 6, 1999
    Date of Patent: September 26, 2000
    Assignee: Eli Lilly and Company
    Inventors: Scott C. Mauldin, John E. Munroe
  • Patent number: 6111083
    Abstract: Disperse dyes of formula ##STR1## wherein R.sub.1 is nitro or cyano, R.sub.2 is halogen, R.sub.3 is C.sub.1 -C.sub.4 alkyl, R.sub.4 and R.sub.5 are each independently of the other methyl or ethyl and R.sub.6 is hydrogen, methyl or ethyl, with the proviso that R.sub.6 is not hydrogen if R.sub.1 is cyano, R.sub.2 is halogen and R.sub.3 is methyl or isopropyl or if R.sub.1 is nitro, R.sub.2 is halogen and R.sub.3 is methyl.These dyes are suitable in particular for dyeing and printing polyester textile materials.
    Type: Grant
    Filed: April 20, 1999
    Date of Patent: August 29, 2000
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Antoine Clement, Alfons Arquint, Urs Lauk
  • Patent number: 6103922
    Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.
    Type: Grant
    Filed: January 6, 1999
    Date of Patent: August 15, 2000
    Assignee: Eli Lilly and Company
    Inventors: William J. Hornback, John E. Munroe
  • Patent number: 6103923
    Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.
    Type: Grant
    Filed: January 6, 1999
    Date of Patent: August 15, 2000
    Assignee: Eli Lilly and Company
    Inventors: Scott C. Mauldin, John E. Munroe
  • Patent number: 6100426
    Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.
    Type: Grant
    Filed: January 6, 1999
    Date of Patent: August 8, 2000
    Assignee: Eli Lilly and Company
    Inventors: Scott C. Mauldin, John E. Munroe
  • Patent number: 6096917
    Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.
    Type: Grant
    Filed: January 6, 1999
    Date of Patent: August 1, 2000
    Assignee: Eli Lilly and Company
    Inventors: William J. Hornback, Scott C. Mauldin, John E. Munroe
  • Patent number: 6075049
    Abstract: Phenylcarbamates of the formula I ##STR1## where the substituents and the index have the following meanings: R is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2;R.sup.1 is alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, and, in the event that X is NR.sup.a, additionally hydrogen;X is a direct bond, O or NR.sup.a ;R.sup.a is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl;R.sup.2 is hydrogen,substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, alkylcarbonyl or alkoxycarbonyl;R.sup.3 and R.sup.4 independently of one another are hydrogen, cyano, nitro, hydroxyl, amino, halogen, hetaryloxy, hetarylthio, hetarylamino or N-hetaryl-N-alkylamino, andR.sup.5 is one of the groups mentioned under R.sup.3 or a group CR.sup.d .dbd.NOR.sup.e ;processes and intermediates for their preparation, and their use.
    Type: Grant
    Filed: April 23, 1998
    Date of Patent: June 13, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Muller, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Klaus Oberdorf, Franz Rohl, Norbert Gotz, Michael Rack, Ruth Muller, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
  • Patent number: 6063815
    Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein Y is ##STR2## R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl mono-, di- or tri-substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy;R.sup.3 and R.sup.4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, hydroxyalkanoyl of 1-6 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, aminoalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, alkylsulfanyl of 1-6 carbon atoms, nitrile, nitro, amino, --NHSO.sub.2 CF.sub.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: May 16, 2000
    Assignee: American Home Products Corporation
    Inventor: Paul J. Dollings
  • Patent number: 6054457
    Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: December 9, 1997
    Date of Patent: April 25, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
  • Patent number: 6039773
    Abstract: A polyamine-containing polyalkyl aromatic ester having the formula: ##STR1## or a fuel-soluble salt thereof; wherein R.sub.1 is a polyamine moiety having about 2 to about 12 amine nitrogen atoms and about 2 to about 40 carbon atoms, wherein the polyamine moiety is connected to the aromatic ring through one of its amine nitrogen atoms and R.sub.2 is a polyalkyl group having an average molecular weight in the range of about 450 to 5000.The polyamine-containing polyalkyl aromatic esters of the present invention are useful as fuel additives for the prevention and control of engine deposits.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: March 21, 2000
    Assignee: Chevron Chemical Company LLC
    Inventor: Richard E. Cherpeck
  • Patent number: 6034266
    Abstract: The present invention refers to novel gem-difluoro compounds of formula: ##STR1## wherein: R.sub.1 can be hydrogen, acyl or acyl substituted; R.sub.2 is hydrogen, lower alkyl, lower alkyl substituted, nitro, halogen, methylenedioxy, trifluoromethyl or OR';Y is oxygen, sulfur or NR";R.sub.3 is hydrogen, lower alkyl, lower alkyl substituted, phenyl, aryl group substituted or metal selected of the group consisting of sodium, potassium, clcium, magnesium, zinc or aluminum;R' and R" are hydrogen, lower alkyl, lower alkyl substituted, phenyl or aryl substituted; and(a) in the group C.sub.1 -C.sub.
    Type: Grant
    Filed: September 17, 1996
    Date of Patent: March 7, 2000
    Assignee: Fundacao Oswaldo Cruz-Fiocruz
    Inventors: Nubia Boechat, Angelo Da Cunha Pinto
  • Patent number: 6028093
    Abstract: Fungicidal mixtures, comprisinga) a carbamate of the formula I ##STR1## where T is CH or N, n is 0, 1 or 2 and R is halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -haloalkyl, it being possible for the radicals R to be different when n is 2, and/orb) an oxime ether of the formula II, ##STR2## where the substituents have the following meanings: X is oxygen or amino;Y is CH or N;Z is oxygen, sulfur, amino or C.sub.1 -C.sub.4 -alkylaminoR' is C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -haloalkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -haloalkynyl, C.sub.3 -C.sub.6 -cycloalkyl-methyl, or is benzyl which can be partially or fully halogenated and/or can have attached to it one to three of the following radicals: cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy and C.sub.1 -C.sub.4 -alkylthio; andc) a carbamate of the formula III(CH.sub.3).sub.2 N--CH.sub.2 CH.sub.2 CH.sub.
    Type: Grant
    Filed: October 21, 1998
    Date of Patent: February 22, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Muller, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Klaus Schelberger, Maria Scherer, Dietrich Mappes, Joachim Leyendecker, Herbert Bayer, Ruth Muller
  • Patent number: 5990341
    Abstract: A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)amino(alkyl or substituted alkyl) methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.
    Type: Grant
    Filed: December 24, 1996
    Date of Patent: November 23, 1999
    Assignee: Emory University
    Inventors: Dennis C. Liotta, Bharat Ramkrishna Lagu
  • Patent number: 5977173
    Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.
    Type: Grant
    Filed: September 4, 1998
    Date of Patent: November 2, 1999
    Inventors: John August Wos, Mitchell Anthony deLong, Jack S. Amburgey, Jr., Biswanath De, Haiyan George Dai, Yili Wang
  • Patent number: 5973189
    Abstract: Compounds have the formula (I), ##STR1## in which R stands for straight-chain or branched (C.sub.1 -C.sub.20) alkyl, phenyl or CH.sub.2 phenyl, the alkyl group or phenyl group being optionally substituted by halogen, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, and R.sup.1, R.sup.2, R.sup.3, R.sup.4 independently represent hydrogen, halogen, OH, NO.sub.2, (C.sub.1 -C.sub.6) alkoxy, (C.sub.1 -C.sub.6) alkyl or halogen-substituted (C.sub.1 -C.sub.6)-alkyl. Also disclosed is a process for preparing these compounds.
    Type: Grant
    Filed: July 16, 1998
    Date of Patent: October 26, 1999
    Assignee: Clariant GmbH
    Inventors: Theodor Papenfuhs, Ralf Pfirmann, Doris Neumann-Grimm, Stefan Krause
  • Patent number: 5965614
    Abstract: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: November 21, 1997
    Date of Patent: October 12, 1999
    Assignee: Athena Neurosciences, Inc.
    Inventors: James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Jon K. Reel, Eugene D. Thorsett, Celia A. Whitesitt
  • Patent number: 5959120
    Abstract: The present invention provides an acetate ester compound of formula (III), ##STR1## a process for synthesizing compound (III), and a process for using that compound to prepare a pyrazolone compound, where the substituent definitions are as defined in the Summary of the Invention.
    Type: Grant
    Filed: June 12, 1997
    Date of Patent: September 28, 1999
    Assignee: Eastman Kodak Company
    Inventors: Jared B. Mooberry, Thomas E. Gompf, Brian H. Johnston
  • 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: 5945556
    Abstract: A process for preparing N-carboxymethylene-4-chloroanthranilic acid, and its dialkyl esters. The invention relates to a process for preparing N-carboxymethylene-4-chloroanthranilic acid and its dialkyl esters, which comprises reacting 2,4-dichlorobenzoic acid in the presence of a base, of a solvent and of a catalyst with glycine to give N-carboxymethylene-4-chloroanthranilic acid and, where appropriate, reacting the latter in the presence of a base and of a solvent with a dialkyl sulfate, dialkyl carbonate or alkyl halide to give the dialkyl ester.
    Type: Grant
    Filed: April 14, 1998
    Date of Patent: August 31, 1999
    Assignee: Clariant GmbH
    Inventors: Theodor Papenfuhs, Ralf Pfirmann, Stefan Krause, Doris Neumann-Grimm
  • Patent number: 5945448
    Abstract: The present invention relates to a composition for treating or preventing brain edemas which comprises containing an endothelin antagonist as an active ingredient, for example, the compound of the following formula (I): ##STR1## or pharmaceutically acceptable salts or hydrates thereof, bosentan, cyclo?D-aspartyl-L-?3-(4-phenylpiperazin-1-ylcarbonyl)!-alanyl-L-aspartyl- D-?2-(2-thienyl)!glycyl-L-leucyl-D-tryptophyl!disodium or cyclo ?D-Asp-L-Pro-D-Val-L-Leu-D-Trp!.Furthermore, the present invention provides a method for treating or preventing brain edemas, which comprises administering an effective amount of an endothelin antagonist and use of an endothelin antagonist for the manufacture of a medicament for treating or preventing brain edemas.An endothelin antagonist exhibits an inhibitory effect, on all brain edemas regardless of the onset mechanism and thus is highly useful in the treatment or prevention of brain edemas.
    Type: Grant
    Filed: October 10, 1997
    Date of Patent: August 31, 1999
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuyoshi Ninomiya, Yoshiyuki Matsuo
  • Patent number: 5939579
    Abstract: Disperse dyes of formula wherein R is nitro or cyano, R.sub.1 is halogen, R.sub.2 is C.sub.1 -C.sub.4 alkyl which is unsubstituted or substituted by C.sub.1 -C.sub.3 alkoxy, halogen, cyano or phenyl, R.sub.3 is C.sub.1 -C.sub.4 alkyl, R.sub.4 is methyl or ethyl, R.sub.5 is hydrogen, methyl or ethyl, and R.sub.6 is methyl or ethyl, with the proviso that R.sub.5 is not hydrogen if R is nitro, R.sub.1 is halogen and R.sub.2 is C.sub.1 -C.sub.4 alkyl.These dyes are particularly suitable for dyeing and printing textile materials consisting of polyester fibres.
    Type: Grant
    Filed: July 6, 1998
    Date of Patent: August 17, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Paul Herzig, Antoine Clement, Alfons Arquint
  • Patent number: 5922887
    Abstract: A compound, or solvate or salt thereof, of formula (I) ##STR1## in which, R.sub.1 and R.sub.2, are, independently hydrogen, linear or branched C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkenyl, or C.sub.3-6 alkenyl, or together form a C.sub.3-7 alkyl;R.sub.3 and R.sub.4 are, independently, hydrogen, linear or branched C.sub.1-6 alkyl, or R.sub.4 is oxygen forming with the carbon atom to which is attached a C.dbd.O group;R.sub.5 is hydrogen, hydroxy, or C.sub.1-3 alkoxy;R.sub.6 is halogen, NH.sub.2 or a para or meta --COR-8 group, in which R.sub.8 is C.sub.1-8 -alkyl, C.sub.1-8 -alkoxy or NR.sub.9 R.sub.10, wherein R.sub.9 and R.sub.10, are, independently, hydrogen, straight or branched C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl or phenyl; or R.sub.6 is a para or meta group ##STR2## in which R.sub.11 and R .sub.12 are, independently, hydrogen or straight or branched C .sub.1-6 and,R.sub.7 is hydrogen, or straight or branched C.sub.1-8 alkyl; is provided.
    Type: Grant
    Filed: November 18, 1997
    Date of Patent: July 13, 1999
    Assignee: SmithKline Beecham SpA
    Inventors: Giulio Dondio, Silvano Ronzoni
  • Patent number: 5919969
    Abstract: The invention provides a method of synthesis of a image-dye forming coupler of formula (I) ##STR1## wherein X is a substituent linked to the coupler by an atom of oxygen, sulfur or nitrogen R.sup.1 is an alkyl or aryl group, R.sup.2 is a hydrogen atom or an alkyl group; R.sup.3 to R.sup.7 are the same or different and selected from a hydrogen atom and substituent groups;which method comprises the reaction of a compound of formula (II) ##STR2## wherein R and R.sup.1 are the same or different and are as defined above for R.sup.1 and X is as defined above with a compound of formula (III) ##STR3## wherein R.sup.2 to R.sup.7 are as defined above, in the presence of an inert organic solvent.
    Type: Grant
    Filed: June 4, 1997
    Date of Patent: July 6, 1999
    Assignee: Eastman Kodak Company
    Inventor: Michael W. Crawley
  • Patent number: 5892098
    Abstract: This invention relates to derivatives of 3,3-(disubstituted)cyclohexan-1-one monomers and related compounds which are useful for treating allergic and inflammatory diseases.
    Type: Grant
    Filed: April 15, 1997
    Date of Patent: April 6, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski, M. Dominic Ryan, Paul E. Bender
  • Patent number: 5872282
    Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.
    Type: Grant
    Filed: March 13, 1998
    Date of Patent: February 16, 1999
    Assignee: Virginia Commonwealth University
    Inventors: Donald J. Abraham, Gajanan Joshi, Ramnarayan Randad
  • Patent number: 5872281
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, phenyl-lower alkyl, lower alkanoyl or benzoyl, and each phenyl in the phenyl-lower alkyl and the benzoyl is unsubstituted or substituted by halogen, lower alkyl or alkoxy; R.sup.2 represents a carboxyl or a carboxyl which is converted into an ester, an amide or a hydroxamic acid; R.sup.3 represent a lower alkyl; R.sup.4 represents a lower alkyl; A.sup.1 represents a lower alkylene which is unsubstituted or substituted by a phenyl and the phenyl is unsubstituted or substituted by halogen, lower alkyl or a lower alkoxy; A.sup.2 represents a lower alkylene; A.sup.3 represents a lower alkylene; and Z represents a sulfur or an oxygen. The compounds have inhibitory effects on LTA.sub.4 hydrolase and are useful for treating rheumatic diseases, psoriasis, inflammatory intestinal diseases, gout and cystic fibrosis.
    Type: Grant
    Filed: September 5, 1997
    Date of Patent: February 16, 1999
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Yoichi Kawashima, Masato Horiuchi
  • Patent number: 5871713
    Abstract: Biological or synthetic macromolecular polyamine compound. optionally of the dendrimer type, characterized in that it carries at least three radio-opaque iodine-containing derivatives.
    Type: Grant
    Filed: August 16, 1996
    Date of Patent: February 16, 1999
    Assignee: Guerbet S.A.
    Inventors: Dominique Meyer, Soizic Le Greneur
  • Patent number: 5866100
    Abstract: The invention relates to non-ionic triiodo aromatic compounds and compositions comprising triiodo aromatic polymers useful for X-ray imaging of gastro-intestinal tract. Disclosed compounds are acrylic acid esters of triiodobenzenes with a different degree of reticulation and their polymers/homopolymers. A method of making the polymers, method of making X-ray contrast agents using the polymers and use of the contrast agents is also disclosed.
    Type: Grant
    Filed: December 19, 1996
    Date of Patent: February 2, 1999
    Assignee: Bracco Research S.A.
    Inventors: Herve Tournier, Philippe Bussat
  • Patent number: 5847196
    Abstract: Oxalic acid diarylamides are described as useful monomers and comonomers in the polymerization of polycarbonates. The resin products resist degradation by ultra-violet light radiation. They can also be incorporated as comonomer or monomer in the polyester, polyester, polyether, polyethersulfone resins. They can also be used as UV stabilizers in the aforemetioned systems.
    Type: Grant
    Filed: October 6, 1997
    Date of Patent: December 8, 1998
    Assignee: General Electric Company
    Inventor: Parfait Jean Marie Likibi
  • Patent number: 5834468
    Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.
    Type: Grant
    Filed: July 2, 1996
    Date of Patent: November 10, 1998
    Assignee: Zeneca Limited
    Inventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
  • Patent number: 5824705
    Abstract: Carbamates of the formula I ##STR1## where the substituents have the following meanings: Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: October 20, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Mueller, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5811572
    Abstract: Process for the preparation of N-carboxymethyleneanthranilic acid esters of the formula (3) ##STR1## by reacting a compound of the formula (1) ##STR2## in which R' is hydrogen or a straight-chain or branched alkyl radical having 1 to 4 carbon atoms and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different and independently of one another are hydrogen, halogen, NO.sub.2, a straight-chain or branched alkyl, alkoxy or halogenated alkyl radical having in each case 1 to 6 carbon atoms, with a glyoxylic acid ester of the formula (2)OHC--COOR (2)in which R is a straight-chain or branched alkyl radical having 1 to 20 carbon atoms, phenyl radical or benzyl radical, which are unsubstituted or mono- or polysubstituted by halogen or an alkyl or alkoxy group having in each case 1 to 4 carbon atoms, in the presence of a solvent at 0.degree. to 200.degree. C.
    Type: Grant
    Filed: February 7, 1997
    Date of Patent: September 22, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Theodor Papenfuhs, Andreas Dierdorf, Stefan Krause, Doris Neumann-Grimm
  • Patent number: 5801197
    Abstract: This invention relates to the method of using specially formulated neurotrophic pipecolic acid derivative compounds having an affinity for FKBP-type immunophilins as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity to stimulate or promote neuronal growth or regeneration.
    Type: Grant
    Filed: May 13, 1996
    Date of Patent: September 1, 1998
    Assignee: GPI Nil Holdings, Inc.
    Inventors: Joseph P. Steiner, Gregory S. Hamilton
  • Patent number: 5756813
    Abstract: Y is O or S;R.sup.1 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy;R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkenyloxy, C.sub.2 -C.sub.4 alkynyl, C.sub.2 -C.sub.4 alkynyloxy, mono-, di- or tri-halomethyl, trifluoromethoxy, C.sub.2 -C.sub.4 alkylthio, C.sub.3 -C.sub.4 branched alkylthio, nitro, or cyano;R.sup.3 is hydrogen, halogen, methyl, mono-, di- or tri-halomethyl;R.sup.4 isa) C.sub.3 -C.sub.8 cycloalkyl substituted by one or more C.sub.1 -C.sub.4 alkyl, preferably one or two methyl;orb) ##STR2## wherein R.sup.6 and R.sup.7 are independently, hydrogen or linear or branched, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, or C.sub.2 -C.sub.4 alkynyl, and R.sup.8 is C.sub.3 -C.sub.8 cycloalkyl substituted by one or more C.sub.1 -C.sub.4 alkyl; andR.sup.5 is an acyclic or cyclic side chain as defined herein.These compounds are useful for inhibiting the growth or replication of retroviruses such as HIV.
    Type: Grant
    Filed: March 22, 1996
    Date of Patent: May 26, 1998
    Assignee: Uniroyal Chemical Ltd/Uniroyal Chemical Ltee
    Inventors: Dong Dao-Cong, William Ashley Harrison
  • Patent number: 5750549
    Abstract: The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, Q, W, X, Y, Z and n are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
    Type: Grant
    Filed: October 15, 1996
    Date of Patent: May 12, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Ping Chen, Philippe L. Durette, Paul Finke, Jeffrey Hale, Edward Holson, Ihor Kopka, Malcolm MacCoss, Laura Meurer, Sander G. Mills, Albert Robichaud
  • Patent number: 5741924
    Abstract: Novel polymeric compositions and their intermediates are provided, providing for broad range protection from ultraviolet radiation. Acryl polymers comprising at least two different ultraviolet absorbing moieties having different light absorbing ranges are employed in conjunction with another hydrophilic monomer to provide sunscreen formulations for invisibility, and enhanced protection, without deleterious effects in the dermis.
    Type: Grant
    Filed: June 14, 1995
    Date of Patent: April 21, 1998
    Assignee: Biophysica Inc.
    Inventors: Milos Sovak, Ronald Calvin Terry, James Gordon Douglass, III, Farid Bakir
  • Patent number: 5731440
    Abstract: An industrially advantageous process for producing 5,7-dichloro-4-hydroxyquinoline (DCHQ) useful as an intermediate for agrohorticultural bactericides. The process comprises (i) hydrolyzing 3-cyano- or 3-ethoxycarbonyl-5,7-dichloro-4-hydroxyquinoline into 5,7-dichloro-3-carboxy-4-hydroxyquinoline (DCQA) in the presence of hydrochloric, sulfuric or phosphoric acid and (ii) decarboxylating the formed DCQA into DCHQ in the presence of sulfuric or phosphoric acid. In particular, this process comprises continuously conducting the hydrolysis of 5,7-dichloro-3-ethoxycarbonyl-4-hydroxyquinoline and the decarboxylation of the hydrolyzate in the presence of sulfuric acid having a specified concentration. The invention also relates to a process for producing DCQA by hydrolyzing 3-cyano- or 3-ethoxycarbonyl-5,7-dichloro-4-hydroxyquinoline in the presence of hydrochloric, sulfuric or phosphoric acid and a process for producing DCHQ by decarboxylating DCQA in the presence of sulfuric or phosphoric acid.
    Type: Grant
    Filed: September 3, 1996
    Date of Patent: March 24, 1998
    Assignees: Ishihara Sangyo Kaisha Ltd., Chemipro Kasei Kaisha, Ltd.
    Inventors: Hiroshi Yoshizawa, Motohiko Hamaguchi, Tomizo Fujino
  • Patent number: 5731454
    Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: March 24, 1998
    Assignee: Virginia Commonwealth University
    Inventors: Donald J. Abraham, Gajanan Joshi, Ramnarayan Randad, Jayashree Panikker
  • Patent number: 5726205
    Abstract: This document describes O-acyl-4-phenyl-cycloalkanols of general formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between them denote 5- to 7-membered saturated, monocyclic, heterocyclic rings which may optionally also be interrupted by an oxygen or sulphur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl or alkynyl having up to 17 carbon atoms, and also processes for preparing them, pharmaceutical compositions containing these compounds and the use of these pharmaceutical compositions which intervene in cholesterol biosynthesis.
    Type: Grant
    Filed: January 17, 1997
    Date of Patent: March 10, 1998
    Assignee: Karl Thomae GmbH
    Inventors: Eberhard Woitun, Roland Maier, Peter Muller, Rudolf Hurnaus, Michael Mark, Bernard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
  • Patent number: 5723681
    Abstract: The present invention relates to novel 3,3-(disubstituted)cyclohexan-1-ol dimers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).
    Type: Grant
    Filed: June 23, 1997
    Date of Patent: March 3, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Joseph M. Karpinski
  • Patent number: 5708026
    Abstract: This invention concerns compounds of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted line represents an optional bond,one of R.sup.1 and R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.16 aralkyl, --(CHR.sup.6).sub.n CHR.sup.7 CN, --(CHR.sup.6).sub.n CHR.sup.7 CONH.sub.2, --(CHR.sup.6).sub.n CHR.sup.7 COOR.sup.8, --(CHR.sup.6).sub.n CHR.sup.7 CH.sub.2 OH wherein n is 0 or 1, R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.1 -C.sub.6 alkyl- or C.sub.7 -C.sub.16 aralkyl-, and R.sup.7 also represents hydroxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.2 -C.sub.7)alkanoyloxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6 alkoxy)carbonyl- and R.sup.8 is hydrogen or C.sub.1 -C.sub.6 alkyl;the other of R.sup.1 and R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.7 -C.sub.16 aralkyl; R.sup.3 is C.sub.6 -C.sub.10 aryl or heteroaryl group optionally substituted by one or more substituents the same or differnet,R.sup.2 and R.sup.
    Type: Grant
    Filed: July 15, 1996
    Date of Patent: January 13, 1998
    Assignee: John Wyeth & Brother
    Inventors: Roger Crossley, Albert Opalko
  • Patent number: 5703130
    Abstract: New retinoid compounds, as chalcone retinoids and compositions thereof, are provided which exhibit therapeutic and/or biological activity on cancer or precancer cells, as well as to methods of use of same.
    Type: Grant
    Filed: June 7, 1996
    Date of Patent: December 30, 1997
    Assignee: Institute of Materia Medica, an Institute of the Chinese Academy of Medical Sciences
    Inventors: Rui Han, Zong-Ru Guo
  • Patent number: 5698732
    Abstract: Oxalic acid diarylamides are described as useful monomers and comonomers in the polymerization of polycarbonates. The resin products resist degradation by ultra-violet light radiation. They can also be incorporated as comonomer or monomer in the polyester, polyester, polyether, polyethersulfone resins. They can also be used as UV stabilizers in the aforemetioned systems.
    Type: Grant
    Filed: January 13, 1997
    Date of Patent: December 16, 1997
    Assignee: General Electric Company
    Inventor: Parfait Jean Marie Likibi
  • Patent number: 5672750
    Abstract: The present invention is directed to a process for preparing an aromatic amide. More specifically, the process involves reacting carbon monoxide, an amine and an aromatic chloride in the presence of an iodide or bromide salt, a catalyst, and a base.
    Type: Grant
    Filed: May 31, 1996
    Date of Patent: September 30, 1997
    Assignee: Eastman Chemical Company
    Inventor: Robert James Perry
  • Patent number: 5672708
    Abstract: N-arylaminoacrylic acid derivatives are obtained in good yields and in high purities when benzoylacetic acid derivatives are reacted with N-arylimino ethers. The products thus prepared are used, in particular, for the preparation of 4-quinolone-3-carboxylic acid derivatives, which have an outstanding bactericidal action.
    Type: Grant
    Filed: August 31, 1995
    Date of Patent: September 30, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Rauchschwalbe, Bernhard Beitzke, Wolfgang Eymann, Helmut Fiege
  • Patent number: 5661166
    Abstract: A Saishin N derivative represented by the following general formula: ##STR1## wherein X represents a carbonyl group or a >CH--ORx group, or X bonds to a carbon atom in Y or Z to represent a >C(ORx)--O-- group; Y and Z may be the same or different and each represents a carbonyl group or a >CH--ORy group, or each bonds to an oxygen atom in X to represent a >CH-- group; the broken line represents an optional bond; and Rx and Ry may be the same or different and each represents a hydrogen atom or an alkyl, alkenyl, aralkenyl, aralkyl, heterocyclic-alkyl or acyl group, is provided which is therapeutically usable as an antiulcer agent.
    Type: Grant
    Filed: March 13, 1995
    Date of Patent: August 26, 1997
    Assignee: Tokyo Tanabe Co. Ltd.
    Inventors: Susumu Yokura, Kiyokazu Murakami, Nobuo Takoi, Hiroyuki Iizuka, Eiji Ohtubo