Patents Examined by Catherine Scalzo
  • Patent number: 5112976
    Abstract: 3-Alkyl- or fluoroalkyl-3-(4-pyridyl)piperidine-2,6-diones, useful in the treatment of breast cancer, of formula ##STR1## wherein R represents an alkyl group having 2 to 10 carbon atoms or a fluoroalkyl group having 2 to 5 carbon atoms and A is hydrogen or an alkyl group having 1 to 4 carbon atoms, are prepared by reacting a 4-pyridylacetate with an alkyl or fluoroalkyl iodide, chloride or bromide, in the presence of a sterically bulky base and reacting the product with acrylamide in the presence of a sodium or potassium branched chain alkoxide. Preferably potassium t-butoxide is used in both stages and they are carried out sequentially at room temperature in an alcoholic or polar, aprotic solvent in a single reaction vessel.
    Type: Grant
    Filed: May 15, 1991
    Date of Patent: May 12, 1992
    Assignee: National Research Development Corporation
    Inventors: Derek W. Clissold, John Mann, Christopher P. Thickitt
  • Patent number: 5112972
    Abstract: The invention relates to new chroman derivatives of the formula I ##STR1## in which R.sup.1 is A,R.sup.2 and R.sup.8 are each H or A,R.sup.1 and R.sup.2 together are also alkylene with 3-6 C atoms,R.sup.3 is OH, OA or OAc,R.sup.4 is H,R.sup.3 and R.sup.4 together are also a bond,R.sup.5 is Ar or C.sub.n H.sub.2n -R.sup.9,R.sup.9 is alkenyl or alkynyl with 2-4 C atoms in each case, OH, OA, CHO, CO-A, CS-A, COOH, COOA, COO-alkyl-Ar, CS-OA, NO.sub.2, NH.sub.2, NHA, NA.sub.2, CN, F, Cl, Br, I, CF.sub.3, SA, SO-A, SO.sub.2 -A or Ar,Ar is a phenyl group which is unsubstituted or substituted once or twice by R.sup.10, R.sup.6, R.sup.7 and R.sup.10 are each H, A, HO, AO, CHO, ACO, CF.sub.3 CO, ACS, HOOC, AOOC, AO-CS, ACOO, A-CS-O, hydroxy-alkyl, mercapto-alkyl, NO.sub.2, NH.sub.2, NHA, NA.sub.2, CN, F, Cl, Br, I, CF.sub.3, AS, ASO, ASO.sub.2, AO-SO, AO-SO.sub.2, AcNH, AO-CO-NH, H.sub.2 NSO, HANSO, A.sub.2 NSO, H.sub.2 NSO.sub.2, HANSO.sub.2, A.sub.2 NSO.sub.2, H.sub.2 NCO, HANCO, A.sub.2 NCO, H.sub.2 NCS, HANCS, A.
    Type: Grant
    Filed: May 31, 1990
    Date of Patent: May 12, 1992
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rolf Gericke, Manfred Baumgarth, Ingeborg Lues, Rolf Bergmann, De Peyer
  • Patent number: 5112829
    Abstract: Novel 9-amino-1,2,3,4-tetrahydroacridines and related compounds of the formula ##STR1## wherein R.sup.1 is H, loweralkyl, or benzyl; R.sup.3 is H, loweralkyl, a group of the formula CH.sub.2 CHR.sup.2 Hal wherein R.sup.2 is hydrogen, loweralkyl, or phenyl and Hal is chloro, bromo, or iodo, or a group of the formula CHR.sup.2 CO.sub.2 R.sup.5 wherein R.sup.2 is as above and R.sup.5 is H or loweralkyl; Z is O or S; X is H, halogen, loweralkoxy, loweralkyl, or trifluoromethyl; n is 1, 2, or 3; the group ZR.sup.3 is bound to either the A- or B-position of the heteroaromatic nucleus; the pharmaceutically acceptable salts thereof; and the optical isomers thereof, useful as intermediates for the preparation of memory dysfunction relieving hexahydro-1H-quino[4,3,2-ef][1,4]benzoxazepines are related compounds and for relieving memory dysfunction are disclosed.
    Type: Grant
    Filed: August 6, 1990
    Date of Patent: May 12, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
  • Patent number: 5098462
    Abstract: Substituted semicarbazones, thiosemicarbazones and isothiosemicarbazones and salts thereof, intermediates therefor, synthesis thereof, and the use of said compounds for the control of weeds.
    Type: Grant
    Filed: May 23, 1988
    Date of Patent: March 24, 1992
    Assignee: Sandoz Ltd.
    Inventors: Richard J. Anderson, Michael M. Leippe, Joe T. Bamberg
  • Patent number: 5095032
    Abstract: Parasiticidal new substituted thienopyranones of the formula ##STR1## in which X represents O or S,R.sup.1 and R.sup.2 independently of one another represent hydrogen, halogen, CN, NO.sub.2, alkyl, aralkyl, aryl, alkylcarbonyl or alkoxycarbonyl, or, together with the adjacent C atoms, form a carbocyclic ring which is optionally interrupted by heteroatoms,R.sup.3 represents optionally substituted alkyl or phenyl,R.sup.4 represents hydrogen or alkyl,R.sup.3 and R.sup.4, together with the adjacent nitrogen atom, represent a heterocyclic 5- or 6-membered ring.Some of the intermediates for making them are also new.
    Type: Grant
    Filed: July 19, 1990
    Date of Patent: March 10, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz-Jurgen Bertram, Nikolaus Muller, Achim Harder
  • Patent number: 5091409
    Abstract: 4-Alkylamino-6-(C.sub.3-5 -hydrocarbyl)thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxides wherein the 4-alkylamino group is an ethylamino or propylamino are powerful carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.
    Type: Grant
    Filed: May 17, 1990
    Date of Patent: February 25, 1992
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Kenneth L. Shepard, Theresa M. Williams
  • Patent number: 5039697
    Abstract: The invention relates to compounds of general formula (I) and physiologically acceptable salts and solvates thereof, methods for their preparation and pharmaceutical formulations thereof. ##STR1## wherein Ar represents a substituted phenyl or nitrogen-containing heterocyclic ring;X and Y represent alkylene, alkenylene or alkynylene chains;R.sup.1, R.sup.2 and R.sup.18 each represent hydrogen or alkyl groups; andQ represents an optionally substituted furan or thiophene ring.The compounds of the invention have a stimulant action at .beta..sub.2 -adrenoreceptors and are useful in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
    Type: Grant
    Filed: May 9, 1990
    Date of Patent: August 13, 1991
    Assignee: Glaxo Group Limited
    Inventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Charles Willbe, David Middlemiss
  • Patent number: 5026724
    Abstract: A method is provided for treating patients suffering from or susceptible to bronchoconstriction, particularly for patients suffering from an asthmatic attach which comprises the use of benzothiophene, benzofuran, dihydronaphthalene or indene derivatives represented by formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently H, (1-4C) alkyl, (1-4C) halogen substituted alkyl, OH, (1-4C) alkoxy, (1-4C) halogen substituted alkoxy, NO.sub.2, CN, halogen, an unsubstituted or (1-4C) alkyl substituted amino group, or wherein two adjacent groups R.sup.1, R.sup.2, R.sup.3 or R.sup.4 together form methylenedioxy;X is S, O or (CH.sub.2).sub.m in which m is 1 or 2;R.sup.5 is H or (1-4C) alkyl;R.sup.6 is H, NH.sub.2 or (1-4C) alkyl;R.sup.7 is H, (1-4C) alkyl or OR.sup.8 in whichR.sup.8 is H, (1-4C) alkyl or (1-8C) acyl;and its pharmaceutically acceptable salts for the preparation of a medicament with bronchodilator activity.
    Type: Grant
    Filed: July 5, 1989
    Date of Patent: June 25, 1991
    Assignee: Akzo N.V.
    Inventors: Robert T. Logan, James Redpath, George McGarry, Robert G. Roy
  • Patent number: 5011831
    Abstract: Quinolinecarboxylic acid derivatives of the formula (I) ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 is hydrogen, straight or branch chain lower alkyl or phenyl unsubstituted or substituted by one or more halo moieties; R.sup.2 is hydrogen or straight or branch chain lower alkyl; and ##STR2## is a 5- or 6-membered ring wherein the nitrogen atom is the only heteroatom or where there is a second heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, said 5- or 6-membered ring being unsubstituted or substituted by lower alkyl, amino or mono- or di-lower alkyl amino are useful for treating bacterial infections in humans and animals.
    Type: Grant
    Filed: November 7, 1988
    Date of Patent: April 30, 1991
    Assignee: Nippon Shinyaku Co. Ltd.
    Inventors: Masahiro Kise, Masahiko Kitano, Masakuni Ozaki, Kenji Kazuno, Masahito Matsuda, Ichiro Shirahase, Yoshifumi Tomii
  • Patent number: 5010095
    Abstract: N-(2-substituted alkyl)-N'[(imidazole-4-yl)alkylguanidines are provided by the reaction of a primary amine with benzoylisothiocyante to a benzoylthiourea derivative, followed by hydrolysis of this derivative to form the corresponding thiourea, converting this thiourea with methyliodide into an isothiourea and producing the desired compound by reaction of the isothiourea with aminopropylimidazole or aminoethylimidazole. The compound can be converted into an acid addition salt or the free compound obtained from such salt. The compounds are useful as the active ingredient in pharmaceutical compositions for the treatment of congestion, heart failure and some allergic conditions.
    Type: Grant
    Filed: November 23, 1988
    Date of Patent: April 23, 1991
    Assignee: Cedona Pharmaceuticals B.V.
    Inventors: Geert J. Sterk, Henk Timmerman, Henk van der Goot
  • Patent number: 5004565
    Abstract: A method and compositions including a 1,2-dioxetane and a fluorescent compound is described. In particular, enzymatic triggering of a triggerable 1,2-dioxetane admixed with a surfactant and the fluorescent compound attached to a hydrocarbon to provide a co-surfactant in a micelle or other structure providing close association of these molecules is described. The method and compositions are useful in immunoassays and in DNA probes used for various purposes.
    Type: Grant
    Filed: July 27, 1988
    Date of Patent: April 2, 1991
    Assignee: The Board of Governors of Wayne State University
    Inventor: Arthur P. Schaap
  • Patent number: 5002966
    Abstract: The invention relates to compounds of general formula (I) and physiologically acceptable salts and solvates thereof, methods for their preparation and pharmaceutical formulations thereof. ##STR1## wherein Ar represents a substituted phenyl or nitrogen-containing heterocyclic ring;X and Y represent alkylene, alkenylene or alkynylene chains;R.sup.1, R.sup.2 and R.sup.18 each represent hydrogen or alkyl groups; andQ represents an optionally substituted furan or thiophene ring.The compounds of the invention have a stimulant action at .beta..sub.2 -adrenoreceptors and are useful in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
    Type: Grant
    Filed: May 9, 1990
    Date of Patent: March 26, 1991
    Assignee: Glaxo Group Limited
    Inventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Charles Willbe, David Middlemiss
  • Patent number: 4999366
    Abstract: A method of controlling hyperlipidemia in mammals which comprises adminstering to a mammal an amount effective to control hyperlipidemia of a compound having hypolipidemic activity and the structural formula: ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different provided both are not hydrogen when R.sup.3 is an alkenyl or cycloalkenyl group, are selected from the group consisting of hydrogen; alkyl of 1 to 18 carbons; substituted alkyl of 1 to 18 carbons; cycloalkyl of 4 to 10 ring carbon atoms; substituted cycloalky of 4 to 10 ring carbon stoms; alkoxy of 1 to 8 carbon atoms; amido; carbamoyl; acyloxy; alkoxycarbonyl; halogen, aryl and substituted aryl, or together R.sup.1 and R.sup.2 from a C.sub.3 to C.sub.7 alkylene group; andR.sup.3 is hydrogen; lower alkyl; substituted lower alkyl; cycloalkyl; substituted cyloalkyl; aryl; substituted aryl; a group --COR.sup.4 were R.sup.
    Type: Grant
    Filed: March 12, 1990
    Date of Patent: March 12, 1991
    Assignees: The North Carolina Central Univ., The Univ. of North Carolina at Chapel Hill
    Inventors: Robert A. Izydore, Iris H. Hall
  • Patent number: 4994448
    Abstract: The new compounds of the general Formula I ##STR1## (wherein R.sub.1 stands for C.sub.1-4 alkyl or aralkyl; andR.sub.2 represents hydroxy; orR.sub.1 and R.sub.2 together form a valency bond;R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl, amino, alkylthio or a group of the Formula --NR.sub.7 R.sub.8 in which R.sub.7 and R.sub.8 may be the same or different and stand for hydrogen, C.sub.1-4 alkyl, phenyl-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl or di-(C.sub.1-4 alkyl)-amino-C.sub.1-4 alkyl or together with the nitrogen atom they are attached to form a 6-membered heterocyclic ring which may optionally contain a further nitrogen, oxygen or sulfur atom; orR.sub.2 and R.sub.3 together form an oxo (.dbd.O) or thixo (.dbd.S) group;R.sub.4 represents hydrogen, C.sub.1-4 alkyl or phenyl which may optionally bear one or two halogen or nitro substituent(s);Z is a group of the Formula (a) or (b) ##STR2## A.sup.
    Type: Grant
    Filed: September 30, 1988
    Date of Patent: February 19, 1991
    Assignee: Egis Gyogyszergyar
    Inventors: Andras Messmer, Gyorgy Hajos, Zsuzsa Juhasz nee Riedl, Pal Benko, Laszlo Pallos, Lujza Petocz, Eniko Szirt nee Kiszelly, Gabor Gigler, Istvan Gyertyan, Maria Hegedus
  • Patent number: 4987230
    Abstract: A new class of sensitizers for photopolymerizable compositions is disclosed derived from cyclic ketones and tricyclic aminoaldehydes.
    Type: Grant
    Filed: December 8, 1989
    Date of Patent: January 22, 1991
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Bruce M. Monroe
  • Patent number: 4985445
    Abstract: Sugar lactams such as N-(3-phenylpropyl)-1-deoxynojirimycin, 1-deoxynojirimycin, D-glucaro-.delta.-lactam, 6-O-triphenylmethyl-D-gluco-.delta.-lactam, etc. and new derivatives thereof which markedly inhibit metastasis of cancer cells.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: January 15, 1991
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Tsutomu Tsuruoka, Satoru Nakabayashi, Harumi Fukuyasu, Yuuko Ishii, Takashi Tsuruoka, Haruo Yamamoto, Shigeharu Inouye, Shinichi Kondo
  • Patent number: 4983325
    Abstract: In one embodiment this invention provides a high performance nonlinear optical medium which comprises a transparent organic polymer film containing an array of charge asymmetric molecules such as 13,13-diamino-14,14-dicyanodiphenoquinodimethane: ##STR1##
    Type: Grant
    Filed: April 4, 1989
    Date of Patent: January 8, 1991
    Assignee: Hoechst Celanese Corp.
    Inventors: Eui W. Choe, Alan Buckley, Dagobert E. Stuetz, Anthony F. Garito
  • Patent number: 4980472
    Abstract: (3-Amino-1H-pyrazol-4-yl)(aryl)methanones which are new compounds having utility as intermediates for the preparation of aryl and heteroaryl-[7-(aryl and heteroaryl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones, which are therapeutic agents.
    Type: Grant
    Filed: November 15, 1989
    Date of Patent: December 25, 1990
    Assignee: American Cyanamid Company
    Inventors: Andrew S. Tomcufcik, John P. Dusza
  • Patent number: 4978762
    Abstract: A new process for preparing [1S-[1.alpha.,2.alpha.(Z),-3.alpha.,4.alpha.]]-7-[3-[[[ (1-oxoheptyl)amino]acetyl]amino]-methyl]-7-oxabicyclo[2,2,1]hept-2-yl]-5-h eptenoic acid. New intermediates are also described. [1S-(1.alpha.,2.alpha.(Z),3.alpha.,4.alpha.]]-7-[3-[[[[(1-oxoheptyl)-amino ]acetyl]amino]methyl]-7-oxabicyclo[2.2.1]hept-2-yl]-5-heptenoic acid is useful in the treatment of thrombotic disease.
    Type: Grant
    Filed: February 26, 1990
    Date of Patent: December 18, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: David Kronenthal
  • Patent number: 4976888
    Abstract: In antifoams based on oil-in-water emulsions, the oil phase of the emulsions contains(a) a C.sub.12 -C.sub.26 -alcohol, a distillation residue which is obtainable in the preparation of alcohols having a relatively large number of carbon atoms by the oxo process or by the Ziegler process and which may furthermore be oxyalkylated and/or(b) a fatty acid ester of a C.sub.12 -C.sub.22 -carboxylic acid with a monohydric to trihydric C.sub.1 -C.sub.18 -alcohol and, if required,(c) a hydrocarbon having a boiling point above 200.degree. C. or a fatty acid of 12 to 22 carbon atoms,accounts for from 5 to 50% by weight of the emulsion and has a mean particle size of less than 25 .mu.m, and from 5 to 50% by weight of components (a) and (b) of the oil phase are replaced by(d) one or more compounds which melt at above 70.degree. C. and are selected from the group consisting of the fatty alcohols of not less than 28 carbon atoms, the esters of a C.sub.1 -C.sub.
    Type: Grant
    Filed: December 30, 1988
    Date of Patent: December 11, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Arnold De Clercq, Wolfram Bergold, Hans-Juergen Degen, Jaroslav Melzer