Nitrogen Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/229)
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Patent number: 5733756Abstract: Novel lactams and processes for the preparation of chiral compounds having utility as intermediates in the synthesis of compounds with Central Nervous System stimulant activity.Type: GrantFiled: January 5, 1996Date of Patent: March 31, 1998Assignee: Celgene CorporationInventors: Andrew L. Zeitlin, David I. Stirling
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Patent number: 5708006Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: June 7, 1995Date of Patent: January 13, 1998Assignee: Boehringer Ingelheim KGInventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 5686483Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.Type: GrantFiled: June 1, 1995Date of Patent: November 11, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
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Patent number: 5686446Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.Type: GrantFiled: June 1, 1995Date of Patent: November 11, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
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Patent number: 5686447Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.Type: GrantFiled: June 1, 1995Date of Patent: November 11, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
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Patent number: 5684021Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.Type: GrantFiled: June 1, 1995Date of Patent: November 4, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
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Patent number: 5665756Abstract: Novel aminoalkyloximes of the formula ##STR1## wherein: a. X is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, or a group of the formula ##STR2## wherein Y is hydrogen or loweralkyl, and p is 1 or 2; b. A is a group of the formula ##STR3## c. R.sup.1 and R.sup.2 are independently hydrogen or lowerakyl; and d. m is 2 to 6 and n is 0, or 2 to 6, inclusive, serotonin reuptake inhibitors, useful for treating depression and obsessive compulsive disorders are described. Also described are precursors of and processes for the preparation of such aminoakyloximes.Type: GrantFiled: August 3, 1994Date of Patent: September 9, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gregory M. Shutske, Brian S. Freed, John D. Tomer, IV, R. Richard L. Hamer
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Patent number: 5661162Abstract: The present invention is directed to compounds of the formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.6, R.sup.7, R.sup.8, m, n and X are defined herein, and pharmaceutically acceptable salts thereof, which are useful as tachykinin antagonists.Type: GrantFiled: June 6, 1995Date of Patent: August 26, 1997Assignee: Merck Sharp & Dohme LimitedInventors: Angus Murray MacLeod, Graeme Irvine Stevenson
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Patent number: 5646144Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalized carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Ciba-Geigy CorporationInventors: Walter Schilling, Silvio Ofner, Siem J. Veenstra
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Patent number: 5622971Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.Type: GrantFiled: June 1, 1995Date of Patent: April 22, 1997Assignee: Abbott LaboratoriesInventors: Martin Winn, Steven A. Boyd, Charles W. Hutchins, Hwan-Soo Jae, Andrew S. Tasker, Thomas W. von Geldern, Jeffrey A. Kester, Bryan K. Sorensen
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Patent number: 5618825Abstract: Combinatorial libraries are disclosed which are represented by Formula I:(T'--L).sub.q -- S--C(O)--L'--II' Iwherein:S is a solid support; T'--L-- is an identifier residue; and --L'--II' is a ligand/linker residue. Compounds which contain aryl sulfonamides, N-acyl derivatives, and N-substituted pyrrolidines and piperidines of the formula :Y--A--CO--R.sup.1are inhibitors of serine proteases and carbonic anhydrase isozymes. They are useful in the treatment of hyper-coagulation disease and ocular diseases such as glaucoma.Type: GrantFiled: June 7, 1995Date of Patent: April 8, 1997Assignee: Pharmacopeia, Inc.Inventors: John J. Baldwin, Michael H. J. Ohlmeyer, Ian Henderson
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Patent number: 5583000Abstract: Non-peptide, protease-binding compounds are described as useful in the detection, labelling, and inhibition of retroviral proteases. Aryl piperidinyl derivatives and other compounds related in structure have been found to be HIV-1 and HIV-2 protease-binding compounds.Type: GrantFiled: September 16, 1993Date of Patent: December 10, 1996Assignee: The Regents of the University of CaliforniaInventors: Paul R. Ortiz de Montellano, Irwin D. Kuntz, Charles S. Craik, Paul S. Furth, Juan C. Alvarez, Patricia S. Caldera, Dianne L. DeCamp, Lilia M. Bab e, James De Voss, Rafael Salto, Zhihua Sui
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Patent number: 5576334Abstract: The invention concerns chemical compounds of formula IR.sup.1 --CON(R.sup.2)--CON(R.sup.3)--X.sup.1 --Q--X.sup.2 --GIand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention concerns processes for the preparation of the chemical compounds of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.Type: GrantFiled: June 27, 1994Date of Patent: November 19, 1996Assignee: Zeneca LimitedInventors: George R. Brown, Richard E. Shute
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Patent number: 5565494Abstract: This invention provides certain benzenesulfonamide derivatives and methods for using them in the treatment of susceptible neoplasms in mammals. Also provided are certain novel pharmaceutical formulations employing these benzenesulfonamide derivatives in combination with a carrier, and processes for preparing the benzenesulfonamide derivatives.Type: GrantFiled: March 10, 1995Date of Patent: October 15, 1996Assignee: Eli Lilly and CompanyInventors: Gerald B. Grindey, Cora S. Grossman, J. Jeffry Howbert, Karen L. Lobb, James E. Ray, John E. Toth
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Patent number: 5552412Abstract: Compounds of this formula ##STR1## are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.Type: GrantFiled: January 9, 1995Date of Patent: September 3, 1996Assignee: Pfizer IncInventors: Kimberly O. Cameron, Paul A. Dasilva Jardine, Robert L. Rosati
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Patent number: 5532255Abstract: Compounds of the formula ##STR1## in which R.sup.1, X and Y have the meanings defined herein, and their salts, inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and tumors.Type: GrantFiled: April 29, 1994Date of Patent: July 2, 1996Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Peter Raddatz, Joachim Gante, Horst Juraczyk, Hanns Wurziger, Helmut Prucher, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 5525633Abstract: The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.Type: GrantFiled: June 15, 1994Date of Patent: June 11, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Donald P. Matthews, Alan J. Bitonti, William A. Van Sickle, Donald A. Kaplan
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Patent number: 5506227Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: April 13, 1992Date of Patent: April 9, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
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Patent number: 5491262Abstract: Bis{[1-(2-A-2-B)ethenyl]} [2-R.sup.2 -4-X-phenyl- or 1-(2-R.sup.2 -4-X-phenyl) ethenyl]methanes useful as color formers, particularly in transfer imaging, pressure sensitive and thermal-responsive carbonless duplicating systems, are prepared by the interaction of two molecular proportions of the corresponding 1-A-1-B-ethene with the appropriate 2-R.sup.2 -4-X-phenyl-(CH.dbd.CH).sub.n --CHO presence of an acidic catalyst.Type: GrantFiled: July 28, 1989Date of Patent: February 13, 1996Assignee: Hilton Davis Chemical Co.Inventor: William M. Hung
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Patent number: 5489599Type: GrantFiled: June 28, 1993Date of Patent: February 6, 1996Assignee: Shell Research LimitedInventors: Paul A. Carter, Steven J. Tapp, Nicholas J. Daniels
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Patent number: 5478934Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.Type: GrantFiled: November 23, 1994Date of Patent: December 26, 1995Inventors: Jun Yuan, Jan W. F. Wasley
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Patent number: 5462947Abstract: A compound of Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein n is 1 or 2; R.sup.1 and R.sup.2 are independently H (provided only one is H at the same time), --OH, CN, CH.sub.2 CN, 2-- or 4--CF.sub.3, CH.sub.2 CF.sub.3, CH.sub.2 CHF.sub.2, CH.dbd.CF.sub.2, (CH.sub.2).sub.2 CF.sub.3, ethenyl, 2-propenyl, OSO.sub.2 CH.sub.3, OSO.sub.2 CF.sub.3, SSO.sub.2 CF.sub.3, COR, COOR, CON(R).sub.2, SO.sub.x CH.sub.3 (where, x is 0-2), SO.sub.x CF.sub.3, O(CH.sub.2).sub.x CF.sub.3, SO.sub.2 N(R).sub.2, CH.dbd.NOR, COCOOR, COCOON(R).sub.2, C.sub.1-8 alkyls, C.sub.3-8 cycloalkyls, CH.sub.2 OR, CH.sub.2 (R).sub.2, NRSO.sub.2 CF.sub.3, NO.sub.2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R.sup.3 is hydrogen, CF.sub.3, CH.sub.2 CF.sub.3, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.9 cycloalkyl-methyl, C.sub. 2 -C.sub.8 alkenyl, C.sub.2 -C.sub.Type: GrantFiled: October 12, 1993Date of Patent: October 31, 1995Assignee: The Upjohn CompanyInventors: Kjell A. I. Svensson, Hakan V. Wikstrom, Per A. E. Carlsson, Anna M. P. Boije, R. Nicholas Waters, Clas A. Sonesson, Nils P. Stjernlof, Bengt R. Andersson, Lars O. Hansson
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Patent number: 5413997Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5386058Abstract: A method for producing polymethine dyes comprising the steps of:(a) reacting a 1,1-diaryl-2-metallo-ethene with an .omega., .omega.,-diaryl-polyalkene-aldehyde in an anhydrous solvent under an inert atmosphere; and(b) neutralizing the reaction mixture from step (a) with an acid, thereby producing a polymethine dye.Type: GrantFiled: October 29, 1993Date of Patent: January 31, 1995Assignee: Minnesota Mining and Manufacturing CompanyInventor: Roger A. Mader
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Patent number: 5382687Abstract: An enamine derivative containing a fluoroalkyl group, a fluoroaryl group or a fluoroaralkyl group is effective as a charge transport material in an electrophotographic member excellent in sensitivity, residual potential, durability and the like electrophotographic properties.Type: GrantFiled: August 2, 1993Date of Patent: January 17, 1995Assignee: Hitachi Chemical Company Ltd.Inventors: Yoshii Morishita, Shigeru Hayashida, Yasushi Sugimoto, Hiroko Ishikawa, Hiroshi Kobayashi, Takaaki Sonoda
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Patent number: 5374724Abstract: A process for the preparation of a substituted acetic acid of the Formula (2): ##STR1## wherein --X--Z is an optionally substituted aromatic or heteroaromatic optionally substituted amino radical; by reacting a compound of the Formula (7):Z--Y--H Formula 7with glyoxylic acid. The compounds of Formula (2) are useful as intermediates in the preparation of polycyclic dyes.Type: GrantFiled: November 2, 1992Date of Patent: December 20, 1994Assignee: Zeneca, LimitedInventors: Nigel Hall, Nigel Hughes, Prakash Patel
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Patent number: 5350852Abstract: The invention relates to a process for making compounds of formula: ##STR1##Type: GrantFiled: August 13, 1993Date of Patent: September 27, 1994Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5350754Abstract: The invention concerns a heterocyclic cycloalkane of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents orAr is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl;and R.sup.2 and R.sup.3 together form a (3-6C)alkylene group which, together with the carbon atom to which R.sup.2 and R.sup.3 are attached, defines a ring having 4 to 7 ring atoms, and which ring may bear one or two substituents; or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: March 1, 1993Date of Patent: September 27, 1994Assignees: Zeneca Limited, ICI PharmaInventors: Graham C. Crawley, Jean-Marc M. M. Girodeau
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Patent number: 5349063Abstract: A novel group of radiolabelled diamines are provided, effective for pancreatic imaging and represented by the formula ##STR1## wherein n is 1 to 10; R.sub.1 and R.sub.2 are the same or different and are hydrogen, hydroxyl or lower alkyl having 1 to 6 carbon atoms; R.sub.3 is lower alkyl having 1 to 6 carbon atoms; and N' is a nitrogen atom forming part of a 4- to 8-membered heterocyclic ring containing one or two hetero atoms, one of which is said nitrogen, said heterocyclic ring being unsubstituted or substituted with one or more lower alkyl groups and pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: January 4, 1993Date of Patent: September 20, 1994Assignee: Alberta Cancer BoardInventors: Alummoottil V. Joshua, John R. Scott
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Patent number: 5346907Abstract: Analogs of CCK-tetrapeptides, which analogs have the formula ##STR1## wherein A, B, D, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are specifically defined, having activity as CCK antagonists, useful in the treatment or prevention of disorders of the gastrointestinal, central nervous, appetite regulating or pain regulating systems.Type: GrantFiled: February 16, 1993Date of Patent: September 13, 1994Assignee: Abbott LaboratoriesInventors: James F. Kerwin, Jr., Mark W. Holladay, Michael J. Bennett
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Patent number: 5332743Abstract: Compounds of the general formula I: ##STR1## are disclosed as potent antipsychotic agents. Novel methods of use and intermediates used to make the compounds of formula I are also disclosed.Type: GrantFiled: June 12, 1992Date of Patent: July 26, 1994Assignee: McNeilab, Inc.Inventors: Ellen W. Baxter, Allen B. Reitz
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Patent number: 5317024Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.Type: GrantFiled: August 3, 1993Date of Patent: May 31, 1994Assignee: DuPont Merck Pharmaceutical Co.Inventors: Gary A. Cain, Thomas E. Christos, Sang W. Tam
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Patent number: 5310902Abstract: Novel alkylenediamine derivatives effectively employable glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5 R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.Type: GrantFiled: August 7, 1991Date of Patent: May 10, 1994Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mitsuo Masaki, Masaru Satoh, Naoya Moritoh, Koichi Hashimoto, Toshiro Kamishiro, Haruhiko Shinozaki
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Patent number: 5296485Abstract: Substituted N-phenylpiperidines I ##STR1## (R.sup.1 =H, NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -alkyl, CF.sub.3, OCF.sub.3, OH, CH.sub.2 OH, COOH, CHO, NH--CHO, NH.sub.2, CO--NH.sub.2, 5-tetrazinyl, R.sup.4 --O--, R.sup.4 --O--CH.sub.2 --, R.sup.4 O--CO--, R.sup.4 --CO--, R.sup.4 --NH--CO, R.sup.4 --CO--NH--, R.sup.4 --SO.sub.2 --NH--;R.sup.2 =H, NO.sub.2, halogen, C.sub.1 -C.sub.4 -alkyl or R.sup.4 --O--; ##STR2## R.sup.4 =C.sub.1 -C.sub.4 -alkyl or phenyl which can carry one of the R.sup.2 radicals;R.sup.5, R.sup.6 =H or one of the R.sup.4 radicals; R.sup.7 =one of the R.sup.1 radicals;n=0 or 1; m=1 or 2; with the proviso that R.sup.3 is ##STR3## only when n is 1, and the optical isomers in the case of optical isomerism, and the physiologically tolerated acid addition salts, are suitable as drugs.Type: GrantFiled: March 11, 1992Date of Patent: March 22, 1994Assignee: BASF AktiengesellschaftInventors: Wilfried Lubisch, Sabine Schult, Berthold Behl, Michael Kirchengast
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Patent number: 5290796Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein R.sup.1 is lower-alkyl, or phenyl-lower-alkyl;R.sup.2, R.sup.3 and R.sup.4 are the same or different lower-alkyl;n is zero or one;R.sup.5 is hydrogen, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, lower-alkoxy, phenyl, phenyl-lower-alkyl, phenyl-lower-alkyl in which the phenyl ring is substituted in the 2, 3, or 4-position by one to two, the same or different, halogen substituents, or R.sup.5 is a 5-membered aromatic monocyclic heterocycle selected from the group consisting of thienyl, furanyl and isoxazolyl;R.sup.6 is hydrogen or lower-alkyl; or when n is zero, R.sup.5 and R.sup.6 together are --(CH.sub.2).sub.m -- wherein m is an integer from four to six; with the proviso that when R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are methyl, n is zero and R.sup.6 is hydrogen or methyl, R.sup.5 cannot be hydrogen; further provided that when n is zero, R.sup.Type: GrantFiled: November 20, 1992Date of Patent: March 1, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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Patent number: 5290940Abstract: 2,6-Diarylpiperidin-1-yl substituted 2-butene stabilizers of the formula I or IIT--CH.sub.2 --CH.dbd.CH--CH.sub.2 --T (I)T--CH.sub.2 --CH.dbd.CH--CH.sub.2 --N(E.sub.1)(E.sub.2) (II)where T is a 2,6-diarylpiperidin-1-yl moiety and E.sub.1 and E.sub.2 are independently alkyl, cycloalkyl, aralkyl or aryl, are effective in stabilizing organic materials against the deleterious effects of oxygen, heat and actinic radiation.Type: GrantFiled: December 14, 1992Date of Patent: March 1, 1994Assignee: Ciba-Geigy CorporationInventors: Glen T. Cunkle, Joseph E. Babiarz
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Patent number: 5270471Abstract: A branched chain polyalkylene polyamine ("PAPA") having plural amine groups, including a secondary amine group intermediate terminal primary amine groups one of which is hindered, and having at least two carbon atoms between each group, is selectively reductively alkylated with a ketone. The reaction provides a convenient method for selectively reductively alkylating a PAPA having a hindered primary amine group, the method comprising contacting the PAPA with hydrogen and the ketone in the presence of a catalytically effective amount of a Group VIII metal on a catalyst support, at a pressure in the range from about 500-1000 psi and a temperature in the range from about 50.degree. C. to about 200.degree. C. for a period of time sufficient to preferentially alkylate the unhindered amine primary terminal amine group. The alkylation proceeds essentially without alkylating either the sterically hindered terminal primary amine group or the intermediate unhindered secondary amine group.Type: GrantFiled: October 27, 1992Date of Patent: December 14, 1993Assignee: The B. F. Goodrich CompanyInventors: John T. Lai, Pyong-Nae Son
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Patent number: 5252586Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.Type: GrantFiled: September 28, 1990Date of Patent: October 12, 1993Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Thomas E. Christos, Sang W. Tam
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Patent number: 5245030Abstract: An IR-ray absorptive compound represented by the formula (1) or (2): ##STR1## and an optical recording medium having a substrate and an organic dye thin film, comprising the formulae (1) and/or (2).Type: GrantFiled: January 31, 1992Date of Patent: September 14, 1993Assignee: Canon Kabushiki KaishaInventors: Tetsuro Fukui, Yoshihiro Oguchi, Hiroyuki Sugata, Kyo Miura
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Patent number: 5236921Abstract: The invention relates to compounds of formula: ##STR1## in which Y represents--either a group Cy--N in whichCy represents a phenyl, optionally substituted; a C.sub.3 -C.sub.7 cycloalkyl group; a pyrimidinyl group or a pyridyl group;or a group ##STR2## in which Ar represents a phenyl, optionally substituted, a pyridyl group; a thienyl group;x is zero or one;X represents a hydroxyl, a C.sub.1 -C.sub.4 alkoxy; a hydroxyalkyl; a C.sub.1 -C.sub.4 acyloxy; a phenacyloxy; a carboxyl; a C.sub.1 -C.sub.4 carbalkoxy; a cyano; an aminoalkylene; a group --N--(X.sub.1).sub.2 in which the groups X.sub.1 independently represent hydrogen, a C.sub.1 -C.sub.4 alkyl; a group ##STR3## in which Alk represents a C.sub.1 -C.sub.6 alkyl; a group ##STR4## in which the Alk.sub.1 is a C.sub.1 -C.sub.3 alkylene and Alk'.sub.1 is a C.sub.1 -C.sub.3 alkyl; a C.sub.1 -C.sub.4 acyl; a group --S--X.sub.2 in which X.sub.2 represents hydrogen or a C.sub.1 -C.sub.Type: GrantFiled: September 5, 1991Date of Patent: August 17, 1993Assignee: SanofiInventors: Xavier Emonds-Ai, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5233048Abstract: Color formers of the general formula ##STR1## in which --independently of one another-- R.sup.1 and R.sup.2 are hydrogen, halogen, alkyl, aralkyl etc.,Y.sup.1 and Y.sup.2 are alkyl, aryl, cycloalkyl or aralkyl,X.sup.1 is alkyl, alkenyl, cycloalkyl, aralkyl etc.,X.sup.2 is H, alkyl, alkenyl, cycloalkyl etc.X.sup.1 with X.sup.2 with the inclusion of the nitrogen atom carrying them can form a saturated or unsaturated 5- or 6-membered heterocyclic ring, andfurther isocyclic or heterocyclic rings can be fused with the rings A, B and C, upon incorporation in recording materials based on acid developers, show a particularly advantageous migration behaviour. Deep blue, green-blue, green, violet or red shades which have excellent sublimation and light fastness are obtained.Type: GrantFiled: September 8, 1992Date of Patent: August 3, 1993Assignee: Bayer AktiengesellschaftInventors: Udo Eckstein, Roderich Raue
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Patent number: 5227490Abstract: Novel fibrinogen receptor antagonists of the formula ##STR1## are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.Type: GrantFiled: February 21, 1992Date of Patent: July 13, 1993Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Wasyl Halczenko
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Patent number: 5189046Abstract: PKC modulating compounds of the formula ##STR1## Also disclosed are pharmaceutical compositions including these compounds which inhibit PKC activity, methods of using these compounds to inhibit PKC activity in mammals, and intermediates useful in preparing the PKC modulating compounds.Type: GrantFiled: June 4, 1991Date of Patent: February 23, 1993Assignee: Nova Pharmaceutical CorporationInventors: Ronald M. Burch, Raymond J. Patch, Barry G. Shearer, John J. Perumattam
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Patent number: 5177087Abstract: There is provided a cyclic amine compound of the formula ##STR1## wherein B means a saturated or unsaturated 5- to 7-membered aza-heterocyclic group which may be substituted; A means a bond or an alkylene or alkenylene group which may be substituted by hydrocarbon residues, oxo, hydroxyimino, and/or hydroxy, means either a single bond or a double bond (provided that when A means a bond, means a single bond); R.sub.2 and R.sub.3 independently mean a hydrogen atom or a hydrocarbon residue which may be substituted (provided that both of R.sub.2 and R.sub.3 are not hydrogen atoms) or jointly form a cyclic amino group together with the adjacent nitrogen atom, n is 0, 1 or 2 and p is 1 or 2 or a physiologically acceptable salt thereof.The compounds are useful for therapy of cerebral edema, acute symptoms in cerebral apoplexy and protection of brain and nerve cell, or useful as anticholinesterase or as brain function-improving agent.Type: GrantFiled: January 4, 1990Date of Patent: January 5, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Hidefumi Yukimasa, Tetsuji Imamoto
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Patent number: 5158961Abstract: Novel piperidine compounds having the formula ##STR1## wherein the symbols have the same meaning as set forth in the specification, and salts thereof with a pharmaceutically acceptable acid, are disclosed.The novel compound are useful in the treatment of anoxia, migraine, ischemia and epilepsy.Type: GrantFiled: March 22, 1991Date of Patent: October 27, 1992Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Jorgen Drejer
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Patent number: 5059391Abstract: It has been found out that polyaralkylamines of the formula stated in the claims are useful as corrosion inhibitors for metallic materials; furthermore were found out new polyaralkylamines of the formula stated in the claims and a process for their preparation.Type: GrantFiled: September 1, 1988Date of Patent: October 22, 1991Assignee: Bayer AktiengesellschaftInventors: Artur Botta, Christian Wegner, Heinz-Joachim Rother
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 5041663Abstract: The invention relates to novel oxime ethers of the formula I ##STR1## wherein R.sub.1 is hydrogen, halogen, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, lower alkylthio, lower haloalkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower haloalkylsulfinyl, lower haloalkylsulfonyl or nitro, each of R.sub.2 and R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or lower haloalkoxy, and Q is an unsubstituted or substituted lower alkyl, lower alkenyl, lower alkynyl or cycloalkyl group, a lower alkanoyl radical, an aliphatic, cycloaliphatic, aromatic or heterocyclic acyl radical which may be substituted or unsubstituted, a carbonyl or thiocarbonyl radical, an aryl or aralkyl radical, an acylimidomethyl radical, a phthalimidomethyl radical or a heterocyclic radical.These compounds are able to act as antidotes or safeners for protecting cultivated plants from the phytotoxic action of aggressive herbicides.Type: GrantFiled: December 11, 1990Date of Patent: August 20, 1991Assignee: Ciba-Geigy CorporationInventors: Henry Martin, Urs Fricker
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Patent number: 5021480Abstract: Compounds which contain azo linkages as well as a hindered amine light stabilizer moiety of low basicity function as free radical polymerization initiators and provide a polymer containing a hindered amine stabilizer chemically bonded to said polymer. The low basicity of the instant compounds prevents interaction with acid catalysts used in some polymerization systems.Type: GrantFiled: February 14, 1990Date of Patent: June 4, 1991Assignee: Ciba-Geigy CorporationInventor: Ramanathan Ravichandran
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Patent number: 4970022Abstract: Mustard oils of the formula IR--(A.sup.1 --Z.sup.1).sub.n --A.sup.2 --Z.sup.2 --A.sup.3 --NCSin which A.sup.1, A.sup.2, A.sup.3, R, Z.sup.1, Z.sup.2 and n have the meaning specified in claim 1 can be used as components of liquid-crystalline phases.Type: GrantFiled: August 19, 1987Date of Patent: November 13, 1990Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Bernhard Scheuble, Rudolf Eidenschink, Joachim Krause, Eike Poetsch, Andreas Wachtler