Chalcogen Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/248)
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Patent number: 5922707Abstract: This invention provides novel oxazolidinone derivatives represented by chemical Formula (I), or pharmaceutically acceptable salts thereof: ##STR1## wherein X is NR.sub.1, CR.sub.2 R.sub.3, O, S, SO, or SO.sub.2 ; and Z is NR.sub.4, S, SO, SO.sub.2 or O. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.Type: GrantFiled: May 2, 1997Date of Patent: July 13, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Richard C. Thomas, Gary J. Cleek, Douglas K. Hutchinson, Hiroyoshi Yamada
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Patent number: 5908863Abstract: Compounds of formula I: ##STR1## wherein R.sub.a, R.sub.b, .PHI., B and R are as defined in the disclosure, have antagonistic activity on osteoclast hyper-reactivity.Type: GrantFiled: February 26, 1997Date of Patent: June 1, 1999Assignee: Dompe' S.p.A.Inventors: Marcello Allegretti, Marco Mantovanini, Gianfranco Caselli, Simonetta Fiorentino, Gaetano Clavenna, Carmelo A. Gandolfi
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Patent number: 5863903Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.Type: GrantFiled: March 14, 1995Date of Patent: January 26, 1999Assignee: Novo Nordisk A/SInventors: Karsten Lundgren, Ole Kirk
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Patent number: 5856492Abstract: An efficient method for the quantitative preparation and isolation of a compound of formula I ##STR1## or its enantiomer, a chiral mediator used in enantioselective synthesis.Type: GrantFiled: January 5, 1998Date of Patent: January 5, 1999Assignee: Merck & Co., Inc.Inventors: Cheng Yi Chen, Feng Xu, Richard D. Tillyer, Dalian Zhao
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Patent number: 5837016Abstract: A fuel additive which comprises an amide compound of the formula ##STR1## wherein R.sup.1 is hydrogen or a C.sub.1 -C.sub.30 hydrocarbon group, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each are selected from the group consisting of hydrogen, a C.sub.1 -C.sub.10 hydrocarbon group and a group of formula (II), provided that at least one of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 group of formula (II) R.sup.6 is a C.sub.2 -C.sub.6 alkylene group, R.sup.7 is a C.sub.1 -C.sub.6 alkylene group, a is an integer of 1-100, b is an integer of 0-100, the sum of a and b being equal to 1-200, c is an integer of 1-3, d is an integer of 0-2, the sum of c and d being equal to 3, and X is selected from the group consisting of hydrogen, a C.sub.1 -C.sub.30 hydrocarbon group, a group of formula (III), and a group of formula (IV), wherein formulas (II), (III) and (IV) are defined in the disclosure.Type: GrantFiled: April 10, 1997Date of Patent: November 17, 1998Assignee: Nippon Oil Co., Ltd.Inventors: Noboru Ishida, Takashi Nakano, Masaki Nagao, Takashi Kaneko
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Patent number: 5837867Abstract: The present invention is directed to the use of cyclic amide alkoxylate compounds as additives in fuel compositions having a major amount of a mixture of hydrocarbons in the gasoline boiling range and a minor amount of one or more cyclic amide alkoxylate compounds of the formula: ##STR1## wherein x is from 2 to 20 and y is from 1 to 50. R.sub.1 and R.sub.2 are independently hydrogen or hydrocarbyl of 1 to 100 carbon atoms. R.sub.3 is hydrocarbyl of 1 to 100 carbon atoms and R.sub.4 is independently hydrocarbyl of 2 to 100 carbon atoms. R.sub.5 is hydrogen, hydrocarbyl of 1 to 100 carbon atoms or acyl of 1 to 20 carbon atoms.The invention is also directed to the use of these cyclic amide alkoxylate compounds for decreasing intake valve deposits, controlling octane requirement increases and reducing octane requirement. The invention is further directed to novel cyclic amide alkoxylate compounds.Type: GrantFiled: August 6, 1996Date of Patent: November 17, 1998Assignee: Shell Oil CompanyInventors: Jiang-Jen Lin, Charles Lee Edwards, Pen-Chung Wang, Garo Garbis Vaporciyan
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Patent number: 5808160Abstract: Hydroxyalkyl-substituted aminoalkynes of the general formula I ##STR1## where at least one of the substituents R.sup.1, R.sup.4 or R.sup.5 is hydroxyalkyl are prepared in a reaction with heterogeneous catalysis.Type: GrantFiled: April 25, 1997Date of Patent: September 15, 1998Assignee: BASF AktiengesellschaftInventors: Thomas Ruhl, Thomas Preiss, Jochem Henkelmann
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Patent number: 5792778Abstract: The present invention addresses 2-substituted aryl pyrroles, as well as compositions containing such compounds and methods of treatment. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production or activity of one or more cytokines occurs. Interleukin-1 (IL-1), Interleukin-6 (IL-6), Interleukin-8 (IL-8) and Tumor Necrosis Factor (TNF) are cytokines which are involved.Type: GrantFiled: August 8, 1996Date of Patent: August 11, 1998Assignee: Merck & Co., Inc.Inventors: Stephen E. de Laszlo, Nigel J. Liverton, Gerald S. Ponticello, Harold G. Selnick, Nathan B. Mantlo
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Patent number: 5686464Abstract: A 3,3-diphenylpropylamine of the formula I, or its physiologically acceptable acid salt thereof: ##STR1## wherein R.sup.1 represents hydrogen or methyl, R.sup.2 and R.sup.3 independently represent hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula II ##STR2## wherein R.sup.4 and R.sup.5 independently represent a hydroxy substituted or unsubstituted non-aromatic hydrocarbyl group which can join together to form a ring and which together contain at least three carbon atoms, wherein at least one of R.sup.4 and R.sup.5 is hydroxy substituted, is useful in treating acetylcholine-mediated disorders such as urinary incontinence.Type: GrantFiled: July 22, 1996Date of Patent: November 11, 1997Assignee: Pharmacia ABInventors: Rolf Arne Johansson, Pinchas Moses, Lisbeth Nilvebrant, Bengt .ANG.ke Sparf
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Patent number: 5656656Abstract: Tartronic acid acetalic ethers and esters of the general formula: ##STR1## are provided and are useful in treatment of bone dysmetabolism. As examples, Ra and Rb may be hydrogen, B is a C.sub.2 -C.sub.12 acyl group, R is phenyl and n is 0-12.Type: GrantFiled: May 23, 1995Date of Patent: August 12, 1997Assignee: Dompe Farmaceutici S.p.A.Inventors: Carmelo A. Gandolfi, Lorella Cotini, Marco Mantovanini, Gianfranco Caselli, Gaetano Clavenna, Claudio Omini
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Patent number: 5631376Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: May 31, 1995Date of Patent: May 20, 1997Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
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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: 5614548Abstract: Quaternary amine-containing ether lipid analogs of the formulaR.sub.1 --X--R.sub.2 --N.sup.+ (R.sub.3) (R.sub.4) (R.sub.5) Z.sup.-are disclosed. R.sub.1 represents a hydrophobic group and R.sub.2 represents the backbone of the molecule, with the quaternary amine being linked directly to the backbone. Pharmaceutical compositions including these compounds and methods of combating tumors with these compounds are disclosed. Also disclosed is a method of combating viral infections with both these compounds and ET-18-OMe and its analogs.Type: GrantFiled: September 8, 1994Date of Patent: March 25, 1997Assignee: Wake Forest UniversityInventors: Claude Piantadosi, Khalid S. Ishaq, Canio J. Marasco, Jr., Larry W. Daniel, Louis S. Kucera, Edward J. Modest, Barry P. Goz
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Patent number: 5596125Abstract: The present invention relates to a process for the preparation of quaternary diesters of the formula: ##STR1## wherein X.sup.- represents a halogen atom, R.sub.1 and R.sub.2 are the same or different and are selected from an alkyl group having 1 to 3 carbon atoms or a hydroxyethyl group, or may be linked together to form an alkylene group having 4 to 6 carbon atoms which may be interrupted by an N atom or O atom, and R.sub.3 and R.sub.4 are the same or different and are selected from an alkyl group or alkenyl group having 8 to 22 carbon atoms, or may be linked together to form an alk(en)ylene group having 8 to 22 carbon atoms. In the processa) a secondary amine of the formula R.sub.1 --NH--R.sub.2 is gradually added to and converted with one or more liquid compounds of the formula ##STR2## a molar ratio in the range of 1.0:1.0 and 1.0:1.Type: GrantFiled: August 25, 1995Date of Patent: January 21, 1997Assignee: Akzo Nobel nvInventors: Burkhard Weuste, Hans J. Weissen, Andrea G. Fischer
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Patent number: 5563250Abstract: The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of a target cell an agent free of its targeting molecule carrier.Type: GrantFiled: May 13, 1994Date of Patent: October 8, 1996Assignee: NeoRx CorporationInventors: Mark D. Hylarides, Ananthachari Srinivasan, Jeffrey N. Fitzner, Vivekananda M. Vrudhula
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Patent number: 5543422Abstract: Heterocyclic amines of the formulaAr-X-A-NR.sup.1 R.sup.2wherein Ar is a bicyclic or tricyclic aromatic group which is unsubstituted or which bears one or more substituents selected from halo, nitro and cyano groups and alkyl and alkoxy groups each of up to 4 carbon atoms;wherein X is a direct link or is --O--, --S--, --SO-- or --SO.sub.2 -- or has the formula --C(R.sup.3).dbd.CH-- wherein R.sup.3 is hydrogen or alkyl of up to 4 carbon atoms;wherein A is straight or branched alkylene or alkenylene of 3 to 8 carbon atoms which may be interrupted by --O--, --S-- or --NH--;and wherein NR.sup.1 R.sup.2 is a cyclic amino group;or a pharmaceutically acceptable acid addition salt thereof, are of value for therapeutic use, particularly in the treatment of myocardial ischaemia and hypertension and in the treatment of fungal infections.Type: GrantFiled: March 23, 1995Date of Patent: August 6, 1996Assignee: British Technology Group LimitedInventors: Ian G. C. Coutts, Pamela J. Cummins
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Patent number: 5525732Abstract: Di-, tri- and poly-perfluoroalkyl-substituted alcohols and acids and derivatives thereof are described which are prepared from perfluoroalkyl iodides and di-, tri- or polyallyl alcohols or acids. These compounds contain two or more perfluoroalkyl-iodoalkyl or perfluoroalkyl-alkenyl groups and one or two alcohol or acid groups or derivatized alcohol or acid functions. They can be reacted with isocyanates, epoxy compounds, anhydrides, acids or acid derivatives to prepare a great variety of oil- and water-repellent compositions which are useful for oil- and water-repellent treatment of textiles, glass, paper, leather and other substrates.Type: GrantFiled: May 31, 1995Date of Patent: June 11, 1996Assignee: Ciba-Geigy CorporationInventors: Marlon Haniff, Robert Falk, Ted Deisenroth, Karl F. Mueller
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Patent number: 5512679Abstract: 2-aryl-ethane-sulphonic acids of the formulaAr.sup.1 --CH.sub.2 --CH.sub.2 --SO.sub.3 H (I),in whichAr.sup.1 denotes a carbocyclic or heterocyclic aromatic radical which can be bound to an anellated benzene nucleus,can be obtained by reaction of the underlying vinyl aromatic compound with sulphurous acid, if the reaction is carried out in the presence of an amine of the formulaN(R.sup.1,R.sup.2,R.sup.3 (III),in whichR.sup.1, R.sup.2 and R.sup.3 have the meaning mentioned in the description.Type: GrantFiled: September 8, 1994Date of Patent: April 30, 1996Assignee: Bayer AktiengesellschaftInventors: Jurgen-Dietrich Meier, Christian Munster, Volker Kass, Horst Siffrin
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Patent number: 5510386Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A-B have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: March 11, 1994Date of Patent: April 23, 1996Assignee: Zeneca LimitedInventors: James R. Empfield, Daniel R. Mayhugh, Keith Russell
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Patent number: 5498617Abstract: Guanidinealkyl-1,1-bisphosphonic acid derivatives, process for their preparation and their useCompounds of the tautomeric formula Ia, Ib or Ic, ##STR1## where R is a radical of the formula ##STR2## are effective compounds for the treatment and prophylaxis of degenerative bone disorders. They are used as pharmaceuticals.Type: GrantFiled: November 23, 1994Date of Patent: March 12, 1996Assignee: Hoechst AktiengesellschaftInventors: Christoph Naumann, Hans-Jochen Lang, Jurgen Sandow, Anne-Marie Moura
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Patent number: 5436343Abstract: Compounds of formula (I): ##STR1## in which: R.sub.1 and R.sub.2, which may be identical or different, represent a linear or branched (C.sub.1 C.sub.6) alkyl radical, a substituted or unsubstituted phenyl radical, a pyridyl radical or a thienyl radical, or, with the carbon atom to which they are attached, a substituted or unsubstituted (C.sub.4 -C.sub.7) cycloalkyl ring,R.sub.3 representsa substituted or unsubstituted phenylsulfonyl radical,a linear or branched (C.sub.1 -C.sub.6) alkyl radical,an alkylaminocarbonyl radical,or a linear or branched (C.sub.1 -C.sub.6) acyl radical,R.sub.4 represents any one of the radicals:--CH.dbd.CH--(CH.sub.2).sub.p --CO.sub.2 H or --CH.sub.2 --CH.sub.2 --(CH.sub.2)p--CO.sub.2 Hin which p is equal to 0, 1, 2 or 3, n and m, which may be identical or different, represent 0, 1 or 2,their isomers, enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid or base.Type: GrantFiled: May 14, 1993Date of Patent: July 25, 1995Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Michel Laubie, Tony Verbeuren
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Patent number: 5423998Abstract: Amino-derivative (poly)peroxycarboxylic acids which have the formula: ##STR1## wherein the symbols have the following meanings: R, R.sub.1, and R.sub.2, which may be equal to or different from one another, represent hydrogen atoms, alkyl groups or groups selected from R, R.sub.1 and R.sub.2, which taken together with the nitrogen atom to which they are linked, give rise to an aliphatic heterocyclic group, all of them being optionally substituted;A represents a (cyclo)alkylene group, an arylene group which may also be condensed with cycloaliphatic groups, a cycloalkylene-alkylene or an alkylene-cycloalkylene group, an arylene-alkylene or an alkylene-arylene group, which may be condensed with cyclo-aliphatic groups, wherein said alkylene group may also be interrupted by --CONR.sub.3 groups, wherein R.sub.3 represents a hydrogen atom or an alkyl or aryl group;X.sup.- represents HSO.sub.4.sup.- or CH.sub.3 SO.sub.3.sup.- ; a process for their preparation; and their use as bleaching agents.Type: GrantFiled: April 13, 1993Date of Patent: June 13, 1995Assignee: Ausimont S.r.l.Inventors: Carlo Venturello, Claudio Cavallotti
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Patent number: 5380856Abstract: The invention concerns a process for preparation of a polymorphic form of terphenadine having a high melting point and enhanced purity, according to which water and a raw terphenadine solution are mixed in dimethylformamide and the pure terphenadine thus precipitated is collected.The invention also concerns the product obtained.Type: GrantFiled: September 13, 1993Date of Patent: January 10, 1995Assignee: IsochemInventors: Didier G. Wirth, Marcel Deglave, Marc-Henri Mouton
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Patent number: 5354862Abstract: Antimicrobial compounds of the formula ##STR1## wherein R is selected from (A)(C.sub.1 to C.sub.20) straight or branched alkyl, optionally substituted with hydroxy, halogen, alkoxy, phenoxy, or --C(.dbd.O)R' wherein R' is selected from C.sub.1 -C.sub.20)alkyl, (C.sub.1 -C.sub.20)alkoxy, phenoxy, or NHR" wherein R" is (C.sub.1 -C.sub.6)alkyl or phenyl; (B) benzyl; (C) phenethyl; (D) cyanoethyl; (E) 2-cyanoethyl; (F) propargyl; and (G) allyl;X=halogen (chlorine, bromine, or iodine), phosphate, acetate, benzoate, citrate, tartrate, alkyl- or aryl-sulfonate, alkylsulfate; and ##STR2## represents a 3-to 7-membered ring that contains at least one nitrogen atom optionally substituted with one or more substituents selected from (C.sub.1 -C.sub.3)alkyl, halo, and carboxyl, said ring optionally containing one or two hetreoatoms in addition to said one nitrogen atom, selected from sulfur, oxygen, and a second nitrogen;Processes for inhibiting microbial growth, and compositions suitable therefore are also disclosed.Type: GrantFiled: August 31, 1993Date of Patent: October 11, 1994Assignee: Rohm and Haas CompanyInventor: Adam C. Hsu
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Patent number: 5354901Abstract: Perfluoro(cycloaliphatic methyleneoxyalkylene) compositions are provided. These compositions comprise perfluoro(cycloaliphatic methyleneoxyalkylene) carbonyl fluoride compounds having (a) a perfluorocycloaliphatic moiety which can have up to two perfluoroalkyl substituents and a perfluoroalkylene substituent, and (b) a perfluoromethyleneoxyalkylene carbonyl fluoride radical, the methylene group of the radical being bonded to a ring carbon atom or the perfluoroalkylene substituent of the moiety and the alkylene group of the perfluoromethyleneoxyalkylene carbonyl fluoride being a perfluoro(methyl)methylene group, a perfluoroisopropyleneoxy(methyl)methylene group, or a poly(perfluoroisopropyleneoxy)perfluoro(methyl)methylene group having up to about 10 perfluoroisopropyleneoxy units.Type: GrantFiled: February 1, 1993Date of Patent: October 11, 1994Assignee: Minnesota Mining and Manufacturing CompanyInventors: Richard M. Flynn, Patricia M. Savu
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Patent number: 5350758Abstract: The present invention relates to piperidyl sulfonamides and sulfoxamides which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.Type: GrantFiled: December 18, 1992Date of Patent: September 27, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Marion W. Wannamaker, William A. VanSickle, William R. Moore
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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: 5348964Abstract: The present invention relates to certain novel piperidyl ethers and thioethers which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.Type: GrantFiled: July 15, 1993Date of Patent: September 20, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Charlotte L. Barney, James R. McCarthy, Marion W. Wannamaker
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Patent number: 5326873Abstract: A method of forming 4-amino-2-buten-1-ol using 3,4-epoxy-1-butene is disclosed. A nitrogen nucleophile (e.g., an amine) is reacted with 3,4-epoxy-1-butene in the presence of a polymer-bound complex of palladium having up to four phosphine ligands.Type: GrantFiled: June 5, 1992Date of Patent: July 5, 1994Assignee: Eastman Kodak CompanyInventors: Stephen A. Godleski, Yann Hung
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Patent number: 5326911Abstract: Ortho-amides of the formula ##STR1## can be prepared by reacting salts of the formula ##STR2## with alcoholates of the formulaM.sup.1 OR.sup.1 (III)where the radicals R.sup.1 to R.sup.4, M.sup.1 and X.sup..crclbar. have the meaning given in the description. The alcoholates are employed in highly active form with an effective content of 98-100% M.sup.1 OR.sup.1.Type: GrantFiled: July 20, 1992Date of Patent: July 5, 1994Assignee: Bayer AktiengesellschaftInventors: Heinz-Ulrich Blank, Helmut Kraus, Gerhard Marzolph, Nikolaus Muller
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Patent number: 5294616Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 15, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
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Patent number: 5290789Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein: R.sup.1 is hydrogen, lower-alkyl or phenyl-lower-alkyl;R.sup.2 and R.sup.4 are the same or different lower-alkyl;R.sup.3 is hydrogen or lower-alkyl;m is two or three;n is an integer from zero to three; andR.sup.5 is hydrogen, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, allyl, or propargyl;or a pharmaceutically acceptable acid-addition salt thereof.Type: GrantFiled: November 20, 1992Date of Patent: March 1, 1994Assignee: Sterling Wintrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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Patent number: 5286733Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein: R.sup.1 is hydrogen, lower-alkyl, phenyl-lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl-lower-alkyl, or hydroxy-C.sub.3 -C.sub.7 -monocycliccycloalkyl-lower-alkyl;R.sup.2 is lower-alkyl;R.sup.3 is hydrogen or lower-alkyl;R.sup.4 is lower-alkyl;n is an integer from zero to three; andR.sup.5 is hydroxy, lower-alkoxy, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, phenyl, or a 5-membered heterocycle selected from furanyl, thienyl and isoxazolyl;with the proviso that when n is zero, R.sup.5 is other than hydroxy or a pharmaceutically acceptable acid-addition salt thereof.Type: GrantFiled: November 20, 1992Date of Patent: February 15, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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Patent number: 5286899Abstract: An efficient and commercially-viable method for the stereoselective transformation of a diol to an alcohol is disclosed. The present method is particularly well-suited for the preparation of the unnatural D-isomer of malic acid or its derivatives from the abundant naturally occurring L-tartaric acid or derivatives thereof.Type: GrantFiled: August 27, 1992Date of Patent: February 15, 1994Assignee: Sepracor, Inc.Inventor: Yun Gao
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Patent number: 5266572Abstract: There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.Type: GrantFiled: June 18, 1992Date of Patent: November 30, 1993Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Paul J. Gilligan, Sang W. Tam
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Patent number: 5258138Abstract: A process for stabilizing an ethylenically unsaturated monomer or oligomer from premature polymerization is disclosed whereby a stabilizing amount of an amine, preferably a substituted hindered amine, in combination with phenothiazine or other related heterocyclic moiety is added to said polymerizable monomer or oligomer. The ethylenically unsaturated monomer or oligomer encompass vinyl monomers or oligomers bearing at least one polymerizable moiety. The combination of substituted hindered amine plus phenothiazine inhibits premature polymerization in the liquid and/or vapor phase.Type: GrantFiled: October 2, 1992Date of Patent: November 2, 1993Assignee: Ciba-Geigy CorporationInventors: Leslie R. Gatechair, Raymond Seltzer, James L. Hyun
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Patent number: 5217979Abstract: The present invention relates to a group of compounds which are novel substituted alkyl piperidines and which act to inhibit the synthesis of cholesterol in mammals and in fungi.Type: GrantFiled: March 17, 1992Date of Patent: June 8, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: James R. McCarthy, Charlotte L. Barney, Marion W. Wannamaker
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Patent number: 5175299Abstract: A pyrazole derivative having the formula ##STR1## is disclosed; the groups A, B, Q, V, W, X, Y, and Z are defined in the description.Type: GrantFiled: November 1, 1991Date of Patent: December 29, 1992Assignee: Nissan Chemical Industries, Ltd.Inventors: Masatoshi Baba, Takuya Kakuta, Norio Tanaka, Eiichi Oya, Takashi Ikai, Tsutomu Nawamaki, Shigeomi Watanabe
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Patent number: 5166373Abstract: The present invention provides novel acyclic terpenes of the formula: ##STR1## which are useful as intermediates for the industrially advantageous production of sarcophytol A.Type: GrantFiled: December 30, 1991Date of Patent: November 24, 1992Assignee: Mitsubishi Kasei CorporationInventors: Hisao Takayanagi, Yasunori Kitano, Yasuhiro Morinaka
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Patent number: 5145893Abstract: 1-Hydrocarbyloxy substituted hindered amine compounds which also contain a reactive functional group such as hydroxy, amino, oxirane or carboxyl can be chemically attached to selected polymer substrates by condensation reactions to give polymers containing a chemically-bonded, non-migrating stabilizer having excellent stabilization efficacy for protecting said polymer substrate from the adverse effects of actinic light.Type: GrantFiled: February 14, 1990Date of Patent: September 8, 1992Assignee: Ciba-Geigy CorporationInventors: James P. Galbo, Ramanathan Ravichandran, Peter J. Schirmann, Andrew Mar
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Patent number: 5145954Abstract: Compounds of formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 and R.sup.2, which are the same or different, are optionally substituted alkyl; W, X, Y and Z, which are the same or different, are hydrogen, halogen, hydroxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted aryloxyalkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted alkynyl, optionally substituted amino, optionally substituted arylazo, optionally substituted heteroarylalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted acylamino, nitro, cyano, --OR.sup.3, --SR.sup.3, --CO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --COR.sup.7, --CR.sup.8 .dbd.NR.sup.9, --N.dbd.CR.sup.10 R.sup.11, --SOR.sup.12 or --SO.sub.2 R.sup.Type: GrantFiled: April 17, 1989Date of Patent: September 8, 1992Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Paul DeFraine, Christopher R. A. Godfrey, Thomas E. Wiggins, David J. Tapolczay
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Patent number: 5145865Abstract: Phenylcarboxylic acid derivatives having a hetero ring in the substituent of the formula: ##STR1## wherein R.sup.1 is halogen, alkyl, cycloalkyl, hydroxy, alkoxy, phenoxy which has a substituent selected from halogen and alkyl, carboxyl, alkylsulfonyloxy, phenylsulfonyloxy optionally substituted by halogen, alkylsulfonyloxyalkoxy, amino, alkanoylamino, benzoylamino, alkenyloxy, phenylalkoxyalkoxy, hydroxyalkoxy, phenylalkoxy having optionally 1 to 3 substituents selected from halogen, alkyl and alkoxy, halogenoalkyl, cycloalkyloxy optionally substituted by hydroxy, alkoxy substituted by cycloalkyl having optionally hydroxy substituent, imidazolylalkyl or imidazolylalkoxy; k is 0 or 1 to 3; or (R.sup.1).sub.k is alkylenedioxy; A is alkylene or alkylenoxy; l is 0 or 1; B is methylene or carbonyl; m is 0 or 1; D is alkylene; E is alkylene or alkenylene; n is 0 or 1; and R.sup.Type: GrantFiled: April 19, 1990Date of Patent: September 8, 1992Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Setsuro Fujii, deceased, by Shinichiro Fujii, administrator, by Kaoruko Takada, administrator, Hiroyuki Kawamura, Shinichi Watanabe
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Patent number: 5143921Abstract: Novel terpene amino alcohols having an antiallergic activity or an activity of improving cerebral function are provided. Also provided are medicinal uses of the alcohols.Type: GrantFiled: June 4, 1990Date of Patent: September 1, 1992Assignee: Kuraray Co., Ltd.Inventors: Koichi Kanehira, Katsushi Eziri, Manzo Shiono, Yoshiji Fujita, Johji Yamahara
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Patent number: 5141648Abstract: The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of a target cell an agent free of its targeting molecule carrier.Type: GrantFiled: March 29, 1991Date of Patent: August 25, 1992Assignee: NeoRx CorporationInventors: Mark D. Hylarides, Ananthachari Srinivasan, Jeffrey N. Fitzner, Vivekananda M. Vrudhula
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Patent number: 5137923Abstract: Lipophilic quaternary ammonium salicylate, characterized in that it corresponds to the formula: ##STR1## in which: (i) R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote an alkyl or alkylcycloalkyl radical, optionally substituted or interrupted;(ii) R.sub.3 and/or R.sub.4 denote(s) a group:R.sub.8 --OC.sub.2 H.sub.3 R.sub.7 ].sub.n [OCH.sub.2 CHOH--CH.sub.2 ].sub.pin which: 0.ltoreq.n.ltoreq.4 and p denotes 0 or 1; R.sub.8 denotes H or an alkyl, alkenyl, alkylcycloalkyl or alkylaryl radical;(iii) R.sub.4 denotes an alkylphenyl radical;(iv), (v) R.sub.1 and R.sub.2 can form a saturated or unsaturated aromatic or non-aromatic heterocycle;(vi) R.sub.1, R.sub.2 and R.sub.3 form polycyclic derivatives with the nitrogen atoms; R.sub.5 denotes a group corresponding to the formula: ##STR2## in which n is an integer varying between 0 and 10.Type: GrantFiled: June 21, 1990Date of Patent: August 11, 1992Assignee: L'OrealInventors: Michel Philippe, Henri Sebag, Michel Hocquaux, Bernard Jacquet, Jean P. Laugier
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Patent number: 5130489Abstract: An improved process is provided for producing m-aminophenols comprising reacting resorcinol and an amino compound in an inert organic solvent and in the presence of an aluminosilicate catalyst.Type: GrantFiled: March 26, 1990Date of Patent: July 14, 1992Assignee: Indspec Chemical CorporationInventor: Hans Dressler
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Patent number: 5117055Abstract: A perfluoroalkyl halogenide represented by the formula: ##STR1## wherein X stands for one element selected from the group consisting of iodine and bromine, R.sub.f for a perfluorohydrocarbon group, n for an integer in the range of 1 to 3, and m for an integer in the range of 1 to 3, provided that n and m satisfy the relationship, n.gtoreq.m, is produced by a method which consists essentially in subjecting a perfluorocarboxylic acid fluoride represented by the formula, ##STR2## wherein R.sub.f and n have the same meanings as defined above, to a thermal reaction with a lithium halogenide represented by XI, wherein X has the same meaning as defined above.Type: GrantFiled: February 22, 1990Date of Patent: May 26, 1992Assignees: Agency of Industrial Science and Technology, Ministry of International Trade & IndustryInventors: Takashi Abe, Eiji Hayashi, Haruhiko Fukaya
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Patent number: 5100902Abstract: Compounds of formula I ##STR1## in which m represents an integer from 0 to 5, n represents an integer from 1 to 2, p is equal to 0, 1 or 2,X, Y and Z, which may be identical or different, each represent a hydrogen atom, a halogen atom, a linear or branched alkyl radical, a trifluoromethyl radical, an alkoxy radical, an alkylthio radical or a hydroxyl radical, andR represents a 2-benzofuranyl or 2,3-dihydro-2-benzofuranyl radical (it being possible for each to be substituted on the benzene ring), a 2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b']difuran-2-yl radical, a 4-oxo-4H-chromen-2-yl radical (optionally substituted on the benzene ring), a benzocyclobutenyl radical of formula A or an indanyl radical of formula B: ##STR2## (in which: R.sub.1 and R.sub.Type: GrantFiled: October 26, 1990Date of Patent: March 31, 1992Assignee: Adir et CompagnieInventors: Jean L. Peglion, Francis Colpaert
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Patent number: 5096918Abstract: The invention concerns pharmaceutially useful heterocyclic nitromethane compounds of the formula I: ##STR1## in which ring Q is a heterocycle of 4 to 7 ring atoms, the fragment completing the ring Q having 2 to 5 atoms, one of which is carbon, oxygen, sulphur or a group of the formula --NRa--, and the remainder are carbon; Ra is hydrogen, (1-6C)alkyl, (2-6C)alkanoyl, trifluoroacetyl, phenyl, benzoyl, or phenyl(1-4C)alkyl, the latter three optionally substituted; and R.sup.1 R.sup.2 and R.sup.3 are independently hydrogen, hydroxy, (1-6C)alkyl, (1-6C)alkoxy, phenyl, phenoxy or phenyl(1-4C)alkyl, the last three optionally substituted, or two of R.sup.1, R.sup.2 and R.sup.3 situated on adjacent ring carbon atoms and together with said carbon atoms form a benzene ring fused to ring Q, the benzene ring itself optionally substituted, provided that when the fragment completion ring Q is of 3 atoms then at least one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen; and salts thereof.Type: GrantFiled: February 5, 1990Date of Patent: March 17, 1992Assignee: Imperial Chemical Industries PLCInventor: Keith B. Mallion
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Patent number: 5064838Abstract: The present invention relates to 1,4-disubstituted-piperidinyl compounds that have utility as analgesics and as muscle relaxants.Type: GrantFiled: December 7, 1988Date of Patent: November 12, 1991Assignee: Merrell Dow PharmaceuticalsInventors: Albert A. Carr, Francis P. Miller, Thaddeus R. Nieduzak, Stephen M. Sorensen