Patents Examined by Catherine Scalzo
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Patent number: 5112976Abstract: 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: GrantFiled: May 15, 1991Date of Patent: May 12, 1992Assignee: National Research Development CorporationInventors: Derek W. Clissold, John Mann, Christopher P. Thickitt
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Patent number: 5112972Abstract: 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: GrantFiled: May 31, 1990Date of Patent: May 12, 1992Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rolf Gericke, Manfred Baumgarth, Ingeborg Lues, Rolf Bergmann, De Peyer
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Patent number: 5112829Abstract: 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: GrantFiled: August 6, 1990Date of Patent: May 12, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples, John D. Tomer, IV
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Patent number: 5098462Abstract: Substituted semicarbazones, thiosemicarbazones and isothiosemicarbazones and salts thereof, intermediates therefor, synthesis thereof, and the use of said compounds for the control of weeds.Type: GrantFiled: May 23, 1988Date of Patent: March 24, 1992Assignee: Sandoz Ltd.Inventors: Richard J. Anderson, Michael M. Leippe, Joe T. Bamberg
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Patent number: 5095032Abstract: 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: GrantFiled: July 19, 1990Date of Patent: March 10, 1992Assignee: Bayer AktiengesellschaftInventors: Heinz-Jurgen Bertram, Nikolaus Muller, Achim Harder
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Patent number: 5091409Abstract: 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: GrantFiled: May 17, 1990Date of Patent: February 25, 1992Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Kenneth L. Shepard, Theresa M. Williams
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Patent number: 5039697Abstract: 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: GrantFiled: May 9, 1990Date of Patent: August 13, 1991Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Charles Willbe, David Middlemiss
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Patent number: 5026724Abstract: 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: GrantFiled: July 5, 1989Date of Patent: June 25, 1991Assignee: Akzo N.V.Inventors: Robert T. Logan, James Redpath, George McGarry, Robert G. Roy
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Patent number: 5011831Abstract: 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: GrantFiled: November 7, 1988Date of Patent: April 30, 1991Assignee: Nippon Shinyaku Co. Ltd.Inventors: Masahiro Kise, Masahiko Kitano, Masakuni Ozaki, Kenji Kazuno, Masahito Matsuda, Ichiro Shirahase, Yoshifumi Tomii
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Patent number: 5010095Abstract: 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: GrantFiled: November 23, 1988Date of Patent: April 23, 1991Assignee: Cedona Pharmaceuticals B.V.Inventors: Geert J. Sterk, Henk Timmerman, Henk van der Goot
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Patent number: 5004565Abstract: 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: GrantFiled: July 27, 1988Date of Patent: April 2, 1991Assignee: The Board of Governors of Wayne State UniversityInventor: Arthur P. Schaap
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Patent number: 5002966Abstract: 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: GrantFiled: May 9, 1990Date of Patent: March 26, 1991Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Charles Willbe, David Middlemiss
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Patent number: 4999366Abstract: 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: GrantFiled: March 12, 1990Date of Patent: March 12, 1991Assignees: The North Carolina Central Univ., The Univ. of North Carolina at Chapel HillInventors: Robert A. Izydore, Iris H. Hall
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Patent number: 4994448Abstract: 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: GrantFiled: September 30, 1988Date of Patent: February 19, 1991Assignee: Egis GyogyszergyarInventors: Andras Messmer, Gyorgy Hajos, Zsuzsa Juhasz nee Riedl, Pal Benko, Laszlo Pallos, Lujza Petocz, Eniko Szirt nee Kiszelly, Gabor Gigler, Istvan Gyertyan, Maria Hegedus
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Patent number: 4987230Abstract: A new class of sensitizers for photopolymerizable compositions is disclosed derived from cyclic ketones and tricyclic aminoaldehydes.Type: GrantFiled: December 8, 1989Date of Patent: January 22, 1991Assignee: E. I. du Pont de Nemours and CompanyInventor: Bruce M. Monroe
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Patent number: 4985445Abstract: 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: GrantFiled: February 6, 1989Date of Patent: January 15, 1991Assignee: Meiji Seika Kaisha, Ltd.Inventors: Tsutomu Tsuruoka, Satoru Nakabayashi, Harumi Fukuyasu, Yuuko Ishii, Takashi Tsuruoka, Haruo Yamamoto, Shigeharu Inouye, Shinichi Kondo
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Patent number: 4983325Abstract: 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: GrantFiled: April 4, 1989Date of Patent: January 8, 1991Assignee: Hoechst Celanese Corp.Inventors: Eui W. Choe, Alan Buckley, Dagobert E. Stuetz, Anthony F. Garito
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Patent number: 4980472Abstract: (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: GrantFiled: November 15, 1989Date of Patent: December 25, 1990Assignee: American Cyanamid CompanyInventors: Andrew S. Tomcufcik, John P. Dusza
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Patent number: 4978762Abstract: 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: GrantFiled: February 26, 1990Date of Patent: December 18, 1990Assignee: E. R. Squibb & Sons, Inc.Inventor: David Kronenthal
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Patent number: 4976888Abstract: 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: GrantFiled: December 30, 1988Date of Patent: December 11, 1990Assignee: BASF AktiengesellschaftInventors: Arnold De Clercq, Wolfram Bergold, Hans-Juergen Degen, Jaroslav Melzer