Patents Examined by Catherine S. Kilby
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Patent number: 5541160Abstract: Compounds represented by the formula I (SEQ ID NO. 1) are disclosed: ##STR1## as well as pharmaceutically acceptable salts and hydrates thereof. R.sup.I represents C.sub.9 to C.sub.19 alkyl, C.sub.9 to C.sub.19 alkenyl, an aryl group which includes phenyl, biphenyl, naphthyl and terphenyl or a C.sub.1 to C.sub.12 alkyl, alkylamino, dialkylamino or alkoxyaryl group.R.sup.1, R.sup.2 and R.sup.4 independently represent H or --OH.R.sup.3 represents H, --OH, --O(CH.sub.2).sub.n NR.sup.V R.sup.VI, where R.sup.V and R.sup.VI independently represent H or C.sub.1-4 alkyl, or --O(CH.sub.2).sub.n NR.sup.V R.sup.VI R.sup.VII+ Y.sup.-, wherein R.sup.V and R.sup.VI are as defined above, R.sup.VII represents H or C.sub.1-4 alkyl, n is an integer of from 2-6 inclusive, and Y represents a counterion.R.sup.5 represents H, --CH.sub.3 or --OH;R.sup.6 represents H or --CH.sub.3 ;R.sup.7 represents H, --CH.sub.3, --CH.sub.2 C(.dbd.O)NH.sub.2, --(CH.sub.2).sub.2 NR.sup.V R.sup.VI or --(CH.sub.2).sub.2 NR.sup.V R.sup.VI R.sup.Type: GrantFiled: April 4, 1994Date of Patent: July 30, 1996Assignee: Merck & Co., Inc.Inventors: James M. Balkovec, Frances A. Bouffard, Regina M. Black
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Patent number: 5519029Abstract: This invention is directed to 2-aminoalkyl-5-aminoalkylamino substituted isoquino [8,7,6-cd]indazole-6-(2H)-ones and to 2-aminoalkyl-5-aminoalkylamino substituted-isoquino [5,6,7-cd] indazole-6(2H)-ones. These compounds have been shown to have antitumor activity.Type: GrantFiled: August 11, 1993Date of Patent: May 21, 1996Assignees: Boehringer Mannheim Italia, S.p.A., University of Vermont & State Agricultural CollegeInventors: A. Paul Krapcho, Ernesto Menta, Ambrogio Oliva, Silvano Spinelli
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Patent number: 5506360Abstract: There is provided a process for the manufacture of 2-alkoxymethylacrolein compounds via the reaction of an appropriate alcohol and acrolein in the presence of an acid and a trisubstituted amine to form an intermediate and the subsequent reaction of the intermediate with formaldehyde in the presence of an acid and a disubstituted amine. There is also provided a process for the manufacture of 3-alkoxymethylquinolines from 2-alkoxymethylacrolein.Type: GrantFiled: November 5, 1993Date of Patent: April 9, 1996Assignee: American CYanamid CompanyInventors: Henry L. Strong, David A. Cortes, Zareen Ahmed
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Patent number: 5506364Abstract: A process for the production of bis(fluoromethyl)ether by contacting formaldehyde with hydrogen fluoride in a reaction/distillation vessel. The reaction/distillation vessel is preferably a reaction/distillation column through which formaldehyde and hydrogen fluoride preferably flow in counter current.The bis(fluoromethyl)ether may be converted to difluoromethane, preferably by heating the bis(fluoromethyl)ether to elevated temperature in the presence of a metal, metal oxide, metal fluoride or metal oxyfluoride catalyst.Type: GrantFiled: May 5, 1994Date of Patent: April 9, 1996Assignee: Imperial Chemical Industries PLCInventors: John S. Martin, Thomas A. Ryan, Rachel A. Spooncer
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Patent number: 5491137Abstract: 14.alpha.,17.alpha.-(Propano-and 17.sup.2 -propeno)-estratrienes of general formula I ##STR1## in which R.sup.1 means a hydrogen atom, a methyl or an acyl group with 1-12 carbon atoms,R.sup.2 means a hydrogen atom or an acyl group with 1-12 carbon atoms and ##STR2## a C--C single or double bond. The new compounds of general formula I are estrogen effective just as ethinyl estradiol.Type: GrantFiled: October 29, 1993Date of Patent: February 13, 1996Assignee: Schering AktiengesellschaftInventors: James R. Bull, Walter Elger, Karl-Heinrich Fritzemeier, Rolf Krattenmacher
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Patent number: 5486626Abstract: Process for the preparation of 3.beta.-aminocholanic acid derivativesA process for the preparation of 3.beta.-aminocholanic acid derivatives of the formula II ##STR1## wherein R(1), R(2) and R(3) have the meanings given, starting from the corresponding 3.beta.-hydroxycholanic acid esters, is described.Type: GrantFiled: March 7, 1994Date of Patent: January 23, 1996Assignee: Hoechst AktiengesellschaftInventors: Alfons Enhsen, Heiner Glombik, Werner Kramer, Gunther Wess
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Patent number: 5480885Abstract: A method of treating psychosis including administering an antipsychotically effective amount of an ergolinyl derivative of 2-propinylamine of the formula I ##STR1## wherein, R.sub.1, R.sub.2, and R.sub.3 independently represent a hydrogen atom or a straight-chain or branched-chain C.sub.1 -C.sub.6 alkyl group, X represents a hydrogen or a halogen atom, Z represents a carbonyl or methylene group, and C.sub.9 - - - -C.sub.10 represents a single or a double, diastereomeric forms, racemates and acid addition salts thereof.Type: GrantFiled: December 2, 1993Date of Patent: January 2, 1996Assignee: Lek, Tovarna Farmacevtskih in KemicnihInventors: Rudolf Rucman, Breda Bole-Vunduk, Magdalena Ocvirk, Bogomila Lavric, Igor Krisch
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Patent number: 5480880Abstract: The invention provides compounds of the general formula I ##STR1## wherein R.sub.1 is a hydrogen atom, a negative charge or an ester residue; R is:a) --(CH.sub.2).sub.n --A--CO.sub.2 H, --(CH.sub.2)n--A--SO.sub.3 H or --(CH.sub.2).sub.n --A--PO.sub.3 H.sub.2, wherein n is either zero, one or two and A is a group --CH.dbd.CH-- (either E or Z), --OCH.sub.2 --, --SCH.sub.2 -- or --CHOH--;b) --(CH.sub.2).sub.n --PO.sub.3 H.sub.2, --(CH.sub.2).sub.n SO.sub.2 NHCN, --(CH.sub.2).sub.n NHSO.sub.3 H, --(CH.sub.2).sub.n CONHSO.sub.2 CH.sub.3 or --(CH.sub.2).sub.n CONHSO.sub.2 CF.sub.3, wherein n is as defined above;c) --(CH.sub.2 S).sub.m --W--(CH.sub.2).sub.n Z, wherein W is an arylene group or a heterocyclediyl group, m is 0 or 1, n is as above defined, and Z represents CO.sub.2 H, PO.sub.3 H.sub.2, SO.sub.2 NHCN, NHSO.sub.3 H, CONHSO.sub.2 CH.sub.3 or CONHSO.sub.2 CF.sub.3 ;d) ##STR2## wherein Y is O or NH and X is NH, N--OH or N--O--(CH.sub.2).sub.n+1 COOH wherein n is as defined above; ore) --(CH.sub.2 S).sub.Type: GrantFiled: April 9, 1993Date of Patent: January 2, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Giuseppina Visentin, Franco Zarini, Daniela Jabes, Ettore Perrone, Costantino della Bruna, Marco Alpegiani
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Patent number: 5473075Abstract: A diastereomer salt of optically active quinolinemevalonic acid of the formula ((-)I.Type: GrantFiled: September 20, 1993Date of Patent: December 5, 1995Assignee: Nissan Chemical Industries Ltd.Inventors: Yoshio Ohara, Mikio Suzuki, Yoshinobu Yanagawa, Hiroshi Iwasaki, Nobuhide Miyachi
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Patent number: 5470844Abstract: The present invention is directed to a class of 3-phosphono-pyrrolidine derivatives as described by Formula I and their use as NMDA antagonists.Type: GrantFiled: November 30, 1993Date of Patent: November 28, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Jeffrey P. Whitten
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Patent number: 5468717Abstract: Oxime ether derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or alkyl, Het is quinolyl, unsubstituted or substituted, and X is oxygen or sulfur, their plant-tolerated acid addition salts, metal complexes and N-oxides, and fungicides containing these compounds.Type: GrantFiled: May 4, 1994Date of Patent: November 21, 1995Assignee: BASF AktiengesellschaftInventors: Bernd Wenderoth, Siegbert Brand, Franz Schuetz, Thomas Kuekenhoehner, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5468767Abstract: Certain 3-amino-cycloalkanyl and cycloalkenyl derivatives of 5-cyano-substituted indoles of Formula I are useful antidepressant agents. ##STR1## The substituent R.sup.1 is hydrogen or C.sub.1-4 alkyl and R.sup.2 is C.sub.1-4 alkyl or --(CH.sub.2).sub.p --Ar with Ar being a phenyl, pyridinyl, pyrimidinyl or 1,4-benzodioxan-2-yl moiety. The symbol m is zero or 1, n is 1 to 3 and p is zero or 1 to 4.Type: GrantFiled: January 6, 1994Date of Patent: November 21, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Joseph A. Cipollina, Ronald J. Mattson, Charles P. Sloan
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Patent number: 5466807Abstract: Novel perylene compounds based on perylene-3,4,9,10-tetracarboxylic acid monoanhydride monoimides which are substituted by alkylene- or arylenesulfonic acid groups on one or both imide nitrogen atoms, or on corresponding tetracarboxylic acid diimides, or on a halogenation product thereof, have properties which render them accessible, in addition to their use as dispersing agent for pigments of the same class of compound or other categories, also for direct use as pigments and fluorescent dyestuffs as well as polymer-soluble dyestuffs.Type: GrantFiled: March 9, 1992Date of Patent: November 14, 1995Assignee: Hoechst AktiengesellschaftInventors: Erwin Dietz, Manfred Urban
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Patent number: 5464842Abstract: Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds of the formulas I to XVI are disclosed (See specification for definitions of the substituents). Specifically, the compounds are 1-azabicyclo [3.2.1]oximes, 1-azabicyclo[3.3.1]oximes, 1-aza-4-oxobicyclo[3.3.1]oximes, 1-aza-4-oxobicyclo[3.2.Type: GrantFiled: March 3, 1994Date of Patent: November 7, 1995Assignee: Warner-Lambert CompanyInventors: David J. Lauffer, Haile Tecle
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Patent number: 5463139Abstract: A composition comprising bis(fluoromethyl)ether and less than an equimolar amount of water, a process for the production of the composition comprising contacting formaldehyde with hydrogen fluoride and separating at least some of the by-product water from bis(fluoromethyl)ether, and use of the composition for the production of difluoromethane.Type: GrantFiled: June 29, 1994Date of Patent: October 31, 1995Assignee: Imperial Chemical Industries PLCInventors: Jane L. Butcher, Thomas A. Ryan, Leslie Burgess
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Patent number: 5453439Abstract: The invention concerns hydroxylamine derivatives of the formula I ##STR1## wherein R.sup.4 is hydrogen, carbamoyl, (1-4C)alkyl, (2-5C)alkanoyl, N-(1-4C)alkylcarbamoyl, N,N-di-(1-4C)alkylcarbamoyl, benzoyl or phenylsulphonyl;R.sup.5 includes hydrogen, (1-4C)alkyl and (2-5C)alkanoyl;R.sup.6 is hydrogen, (1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl;R.sup.7 is hydrogen or (1-4C)alkyl;Ar.sup.1 is phenylene;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazolediyl, thiadiazolediyl or oxadiazolediyl;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is independently (1-3C)alkylene and X.sup.Type: GrantFiled: February 8, 1993Date of Patent: September 26, 1995Assignees: Zeneca Limited, Zeneca-Pharma S.A.Inventor: Patrick Ple
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Patent number: 5441952Abstract: Fibrinogen receptor antagonists of the ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets, for example ##STR2##Type: GrantFiled: April 5, 1993Date of Patent: August 15, 1995Assignee: Merck & Co., Inc.Inventors: David A. Claremon, Nigel Liverton
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Patent number: 5442068Abstract: Azabicyclo [2.2.2.]octan-3-imines of the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein are prepared by reacting a compound of the formula ##STR2## with a compound of the formula ##STR3## wherein A is MgCl, MgBr or Li.Type: GrantFiled: January 19, 1993Date of Patent: August 15, 1995Assignee: Pfizer Inc.Inventors: Dennis M. Godek, Charles W. Murtiashaw
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Patent number: 5438064Abstract: Derivatives of 4-anilinoquinoline having the formula: ##STR1## where X is O or H.sub.2 and Z is 1-substituted-4-piperidinylamino or diloweralkylaminoloweralkyl inhibit binding of tritiated bradykinin to guinea pig ileum and inhibit bradykinin-induced writhing in mice. Bradykinin is a nonapeptide formed in plasma as a result of inflammation or injury and produces pain when it binds with pain receptors. A drug which inhibits the binding of bradykinin therefore has analgetic properties.Type: GrantFiled: December 23, 1991Date of Patent: August 1, 1995Assignee: American Home Products CorporationInventors: Dominick Mobilio, Albert J. Molinari
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Patent number: 5436345Abstract: A method is provided for making a 4-hydroxy-tetraorganopiperidinyloxy, such as 4-OH TEMPO. These free radical spin-traps can be used as anaerobic inhibitors which have been found useful for polymerizing reactive acrylic monomers.Type: GrantFiled: September 12, 1994Date of Patent: July 25, 1995Assignee: General Electric CompanyInventors: Larry N. Lewis, James E. Pickett