Plural Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 546/197)
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Patent number: 5856493Abstract: The present invention relates to paroxetine hydrochloride anhydrate substantially free of bound propan-2-ol, several forms of the above, processes for preparing the above, new intermediates useful in preparing the above and methods of treating and/or preventing certain diseases by administering the compounds of the invention to a patient in need thereof.Type: GrantFiled: February 29, 1996Date of Patent: January 5, 1999Assignee: SmithKline Beecham CorporationInventors: Neal Ward, Victor Witold Jacewicz
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Patent number: 5852042Abstract: The invention relates to novel substituted N-(4-pyridyl)carboxamides of the formula ##STR1## in which Q is substituted 4-pyridyl, A is hydrogen, alkyl, acyl or aralkyl and Y-Z is an optionally modified hydrocarbon radical or Y is a bond or a bivalent radical and Z is aryl, O-aryl, cycloalkyl, cycloalkenyl or heterocyclyl, all of which are optionally substituted, to processes for their preparation, to intermediates during their preparation, and to their use as pesticides, in particular as insecticides, acaricides and nematicides, and also as fungicides.Type: GrantFiled: September 26, 1995Date of Patent: December 22, 1998Assignee: Hoechst Schering AgrEvo GmbHInventors: Harald Jakobi, Werner Knauf, Ulrich Sanft, Manfred Kern, Dieter Bernd Reuschling, Adolf Heinz Linkies, Werner Bonin
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Patent number: 5852008Abstract: Compounds having the following structural formula, ##STR1## are useful for enhancing synaptic response mediated by AMPA receptors are disclosed, the invention compounds can also be used for the treatment of non-impaired subject for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptor and for improving memory encoding.Type: GrantFiled: June 5, 1995Date of Patent: December 22, 1998Assignee: The Regents of the University of CaliforniaInventors: Gary S. Lynch, Gary A. Rogers
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Patent number: 5847167Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: June 30, 1997Date of Patent: December 8, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
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Patent number: 5847168Abstract: A photochromic article that includes a host material and a photochromic amount of a naphthopyran compound, the naphthopyran compound represented by the formula: ##STR1## wherein R.sub.1 ', R.sub.2 ', R.sub.3 ', R.sub.4 ', R.sub.5 ', R.sub.6 ', R.sub.7 ', R.sub.8 ', R.sub.9 ', R.sub.10 ', R.sub.1 ", R.sub.2 ", R.sub.3 ", R.sub.4 ", R.sub.5 ", R.sub.6 ", R.sub.7 ", R.sub.8 ", R.sub.9 ", and R.sub.10 " are each selected from the following group: a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.Type: GrantFiled: December 1, 1997Date of Patent: December 8, 1998Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
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Patent number: 5798350Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 represents C.sub.1-4 alkyl;Y is selected from CH and N;n is 0, 1 or 2;q is 1 or 2;R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S;D is cyclohexane or benzene; andE is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl;and acid addition salts, solvates and hydrates thereof.Type: GrantFiled: May 3, 1996Date of Patent: August 25, 1998Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
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Patent number: 5786372Abstract: Compounds of formula (I), or pharmaceutically acceptable salts thereof are provided: ##STR1## in which X.sub.1 --(CH.sub.2).sub.x --X.sub.2 forms a 5-7 membered ring wherein:X.sub.1 is O or S;X.sub.2 is O, S or NR wherein R is hydrogen;x is 1, 2 or 3;R.sub.1 is hydrogen, amino, halo, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkoxy;R.sub.2 is hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, nitro, amino or C.sub.1-6 alkylthio;R.sub.3 is hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino;R.sub.4 and R.sub.5 are independently hydrogen or C.sub.1-6 alkyl;Y is NH;Z is of sub-formula (a): ##STR2## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon; andn.sup.1 is 0, 1, 2, 3 or 4;q is 0, 1, 2 or 3;R.sub.a is (CH.sub.2).sub.n.sup.2 --R.sub.7 wherein n.sup.2 is 2 or 3 and R.sub.7 is selected from cyano, hydroxyl, C.sub.1-6 alkoxy, phenoxy, C(O)C.sub.1-6 alkyl, COC.sub.6 H.sub.5, --CONR.sub.8 R.sub.9, NR.sub.8 COR.sub.9, SO.sub.2 NR.sub.8 R.sub.9 or NR.sub.8 SO.sub.2 R.sub.9 whereinR.sub.8 and R.sub.Type: GrantFiled: December 20, 1996Date of Patent: July 28, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
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Patent number: 5780486Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: May 27, 1997Date of Patent: July 14, 1998Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
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Patent number: 5767118Abstract: The present invention is directed to certain novel compounds identified as 4-heterocycle substituted piperidines of the general structural formula: ##STR1## wherein R.sup.1, R.sup.4, R.sup.5, A, R.sup.3 and the dashed line are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: October 26, 1994Date of Patent: June 16, 1998Assignee: Merck & Co., Inc.Inventors: Ravi Nargund, Arthur A. Patchett, Lihu Yang
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Patent number: 5767116Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or --O--; B is methylene or --O--; and g is 0, 1, 2, 3 or 4;R.sub.1, R.sub.2, R.sub.3, R.sub.4, U, Q and T are defined in claim 1.The compounds have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: June 5, 1996Date of Patent: June 16, 1998Assignee: Knoll AtkiengesellschaftInventors: Frank Kerrigan, David John Heal, Keith Frank Martin
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Patent number: 5756533Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: June 7, 1995Date of Patent: May 26, 1998Assignee: G.D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 5753662Abstract: A compound selected from those of formula: ##STR1## wherein: A--B, n, D and E are as defined in the specification, their racemic mixtures, and their optical isomers, and also the physiologically tolerable salts thereof with appropriate acids.The products of the invention may be used therapeutically.Type: GrantFiled: May 30, 1996Date of Patent: May 19, 1998Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Aimee Dessinges, Bertrand Goument, Mark Millan, Adrian Newman-Tancredi, Alain Gobert
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Patent number: 5753678Abstract: The present invention relates to novel N-substituted amino alcohols, amino acids and acid derivatives thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: September 18, 1996Date of Patent: May 19, 1998Assignee: Novo Nordisk A/SInventors: Rolf Hohlweg, Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Uffe Bang Olsen, Peter Madsen, Zdenek Polivka, Otylie Konigova, Frantisek Miksik, Martina Kovandova, Alexandra Silhankova, Karel Sindelar
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Patent number: 5739134Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.Type: GrantFiled: April 13, 1995Date of Patent: April 14, 1998Assignee: Janssen Pharmacetuica N.V.Inventors: Georges H.P. Van Daele, deceased, Frans M.A. Van den Keybus, Marie L. Hendrickx, heiress, Kurt G.C.E. Van Daele, heir, Peter J.V. Van Daele, heir, Glenn K.L. Van Daele, heir
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Patent number: 5731309Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: October 24, 1995Date of Patent: March 24, 1998Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Scott C. Miller
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Patent number: 5726186Abstract: The present invention provides compounds of formula I: ##STR1## wherein X is --O-- or --S--,Y is --O--, --S--, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, or --NR.sup.5 --;R.sup.1, R.sup.2, and R.sup.3 are each independently --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), --OSO.sub.2 CF.sub.3, Cl, or F;n is 1 or 2;W is CH.sub.2 or C.dbd.O;R.sup.4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;R.sup.5 is C.sub.1 -C.sub.3 alkyl, --COC.sub.6 H.sub.5, --CO(C.sub.1 -C.sub.6 alkyl), --C(O)OC.sub.6 H.sub.5, --C(O)O(C.sub.1 -C.sub.6 alkyl), --SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --SO.sub.2 C.sub.6 H.sub.5, or --SO.sub.2 CF.sub.3 ;or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: August 13, 1996Date of Patent: March 10, 1998Assignee: Eli Lilly and CompanyInventor: Timothy Alan Grese
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Patent number: 5723072Abstract: Described are novel photochromic heterocyclic fused indenonaphthopyran compounds having a substituted or unsubstituted heterocyclic ring fused to the g, h, i, n, o or p side of the indenonaphthopyran. These compounds may be represented by either of the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds.Type: GrantFiled: March 18, 1997Date of Patent: March 3, 1998Assignee: PPG Industries, Inc.Inventor: Anil Kumar
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Patent number: 5721253Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.Type: GrantFiled: September 23, 1996Date of Patent: February 24, 1998Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Melissa S. Egbertson, Wasyl Halczenko, Ben Askew
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Patent number: 5716993Abstract: The present invention provides an anthranilic acid derivative having a cGMP-PDE inhibitory activity.An anthranilic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, a nitro group, a hydroxyalkyl group, a cyano group or the like; R.sup.5 and R.sup.6 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group or the like;W represents a group of the formula: --N.dbd. or --CH.dbd.; R.sup.7 and R.sup.Type: GrantFiled: September 14, 1995Date of Patent: February 10, 1998Assignee: Eisai Co., Ltd.Inventors: Fumihiro Ozaki, Keiji Ishibashi, Hironori Ikuta, Hiroki Ishihara, Shigeru Souda
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Patent number: 5705509Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X.sub.1 --(CH.sub.2).sub.x --X.sub.2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X.sub.1 is O or S; X.sub.2 is O, S, NR.sub.5 or NR.sub.6 CO wherein R.sub.5 is hydrogen or C.sub.1-6 alkyl; or one of X.sub.1 and X.sub.2 is O, S or CH.sub.2 and the other is CH.sub.2 ; x is 1, 2 or 3; R.sub.1 and R.sub.2 together are Q--CH.sub.2 --CH.sub.2, Q--CH.dbd.CH, or Q--CH.dbd.N where Q is linked either to the R.sub.1 or the R.sub.2 substitution position and Q is O, S or NR.sub.t wherein R.sub.t is hydrogen or C.sub.1-6 alkyl; R.sub.3 is hydrogen halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino; R.sub.4.sup.1 and R.sub.4.sup.2 are independently hydrogen or C.sub.1-6 alkyl; Y is O or NH; Z is of sub-formula (a), (b) or (c) and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: July 28, 1995Date of Patent: January 6, 1998Assignee: SmithKline Beecham plcInventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5702645Abstract: Described herein are photochromic compounds or a structural isomer of the photochromic compound, the photochromic compounds represented by the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.4, R.sub.5, R.sub.6, R.sub.8, A, B, C, and D are each selected from the group consisting essentially of hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted radical, and a nitrogen-substituted ring radical.Type: GrantFiled: October 30, 1995Date of Patent: December 30, 1997Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
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Patent number: 5698141Abstract: Described are novel photochromic heterocyclic fused indenonaphthopyran compounds having a substituted or unsubstituted heterocyclic ring fused to the g, h, i, n, o or p side of the indenonaphthopyran. These compounds may be represented by either of the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds.Type: GrantFiled: January 16, 1997Date of Patent: December 16, 1997Assignee: PPG Industries, Inc.Inventor: Anil Kumar
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Patent number: 5698364Abstract: Dye-donor element for thermal dye transfer comprising at least one magenta dye having extremely low side absorption in the blue and red regions of the spectrum, said dye corresponding to the general formula (I) : ##STR1## wherein R.sup.1 is H, (cyclo)alkyl, or aryl; X represents the atoms completing a heterocycle; Z is an electron-withdrawing group; Y is an electron-withdrawing group or --N(R.sup.2)R.sup.3 ; R.sup.2 and R.sup.3 together represent the atoms completing a heterocycle; or R.sup.2 and R.sup.3 together represent .dbd.C(R.sup.4)R.sup.5, or each of R.sup.2 and R.sup.3 represents (same or different) (cyclo) alkyl, aryl, or an electron-withdrawing group; each of R.sup.4 and R.sup.5 (same or different) represents H, (cyclo)alkyl, aryl, a heterocycle, SO.sub.2 R.sup.6, COR.sup.6, CSR.sup.6, POR.sup.6 R.sup.7, OR.sup.8, NR.sup.8 R.sup.9, SR.sup.8, or R.sup.4 and R.sup.5 together represent the atoms completing an aliphatic ring or a heterocycle, each of R.sup.6 and R.sup.Type: GrantFiled: June 6, 1995Date of Patent: December 16, 1997Assignee: Agfa-Gevaert, N.V.Inventors: Wilhelmus Janssens, Luc Vanmaele
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Patent number: 5696137Abstract: Azaheterocyclylmethyl-chromans of the formula: ##STR1## in which E represents an azaheterocyclyl group selected from the group consisting of: ##STR2## wherein R.sup.6 represents hydrogen, hydroxyl, halogen or phenyl; andn represents an integer 0-8;and the other substituents are as defined herein;or an optically isomeric form thereof or a salt thereof;are useful to treat anxiety, depression and psychoses.Type: GrantFiled: June 2, 1995Date of Patent: December 9, 1997Assignee: Bayer AktiengesellschaftInventors: Hans-Georg Heine, Rudolf Schohe-Loop, Thomas Glaser, Jean Marie Viktor De Vry, Wolfgang Dompert, Henning Sommermeyer
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Patent number: 5688952Abstract: The present invention is concerned with vasoconstricive ?(benzodioxan, benzofuran or benzopyran)alkylamino!alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.Type: GrantFiled: April 15, 1996Date of Patent: November 18, 1997Assignee: Janssen Pharmaceutica, N.V.Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Walter Jacobus Joseph Janssens
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Patent number: 5686484Abstract: Compounds of formula (I): ##STR1## and of formula (I).sub.w : ##STR2## in which: A represents group having one of the following formulae: ##STR3## wherein R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen atoms, halogen atoms, alkyl groups having from 1 to 4 carbon atoms, and alkoxy groups having from 1 to 4 carbon atoms;R.sup.1, R.sub.w.sup.1 and R.sub.w.sup.2 are, for example, hydrogen, halogen, cyano, nitro, optically substituted alkyl, alkoxy or alkoxyalkoxy;X or X.sub.w is hydroxy, alkanoyloxy, substituted alkanoyloxy or hydroxyimino; R.sup.3.sub.w and R.sup.4.sub.w are each hydrogen, alkyl or alkoxy; R.sup.5 and R.sup.5.sub.w are methyl, ethyl, isopropyl or sec-butyl; and salts thereof have valuable anthelmintic, acaricidal and insecticidal activities.Type: GrantFiled: March 1, 1995Date of Patent: November 11, 1997Assignees: Sankyo Co., Ltd., Ciba-Geigy CorporationInventors: Yasuhiro Morisawa, Akio Saito, Satoru Naito, Toshimitsu Toyama, Susumu Kaneko, Louis-Pierre Molleyres, Jean-Claude Gehret
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Patent number: 5684020Abstract: A compound selected from those of formula: ##STR1## wherein: A-B, n, D and E are as defined in the specification,their racemic mixtures, and their optical isomers,and also the physiologically tolerable salts thereof with appropriate acids.The products of the invention may be used therapeutically.Type: GrantFiled: January 30, 1997Date of Patent: November 4, 1997Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Aimee Dessinges, Bertrand Goument, Mark Millan, Adrian Newman-Tancredi, Alain Gobert
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Patent number: 5674894Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.Type: GrantFiled: May 15, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
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Patent number: 5672612Abstract: A free-flowing, amorphous paroxetine hydrochloride-ethanol composition suitable as a therapeutic agent for premature ejaculation can be prepared by dissolving paroxetine free base in a hydrochloric acid-ethanol solution followed by drying. In a preferred embodiment, the amount of ethanol present in the amorphous product is in the range of 1 to 4 weight percent based on paroxetine hydrochloride. The amorphous product is stable and substantially non-hygroscopic.Type: GrantFiled: September 9, 1996Date of Patent: September 30, 1997Assignee: Pentech Pharmaceuticals, Inc.Inventors: Bruce Ronsen, Ragab El-Rashidy
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Patent number: 5668148Abstract: Compounds that specifically bind to the human alpha1a adrenergic receptor, including compounds effective to reduce symptoms of benign prostatic hypertrophy include compounds of formula: ##STR1## wherein: Ar1 and Ar2 can be independantly aromatic, heteroaromatic, or condensed heteroaromatic unsubstituted or substituted with amino, alkoxy, sulfonamido, alkyl, heteroalkyl, halo;m is 0 or 1;n is 0, 1, or 2;het is an aromatic or nonaromatic heterocyclic ring, substituted with alkyl, halo, or alkoxy substituents; andX is a branched or straight chain aliphatic or halogen substituent.Type: GrantFiled: April 20, 1995Date of Patent: September 16, 1997Assignee: Merck & Co., Inc.Inventors: Linda S. Payne, Steven D. Young, Mary Jo L. Zaborowski
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Patent number: 5665736Abstract: The invention relates to new N-benzoylmethyl-piperidines of the general formula (I): ##STR1## wherein X is a halogen atom, as well as their pharmaceutically acceptable addition salts. The compounds are potentially useful to treat depressions.Type: GrantFiled: February 20, 1996Date of Patent: September 9, 1997Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Santiago Gubert, Aurelio Sacristan, Jose A. Ortiz
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Patent number: 5646149Abstract: Compounds having both calcium antagonist and antioxidant activity are disclosed. The compounds are useful in preventing or alleviating damage to tissues at the cellular level. Methods of treatment which employ these properties of the compounds and corresponding pharmaceutical compositions are also disclosed.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, George Barnes, Robert J. Collier, Jr.
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Patent number: 5646175Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: June 1, 1995Date of Patent: July 8, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
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Patent number: 5645767Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the f side of the naphtho portion of the naphthopyran, and certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12, or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds, are also described.Type: GrantFiled: October 13, 1995Date of Patent: July 8, 1997Assignee: Transitions Optical, Inc.Inventor: Barry Van Gemert
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Patent number: 5639763Abstract: Compounds of the following structure, the corresponding N-oxides and agriculturally acceptable salts, are disclosed as effective insecticides: ##STR1## in which U is selected from --(CH.sub.2).sub.n -- and ethylidene; Q is selected from hydrogen, hydroxy, sulfhydryl, and fluorine; R is ##STR2## in which V is selected from hydrogen, halogen, alkyl, haloalkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsilyloxy, dialkylamino, cyano, nitro, hydroxy, and phenyl; Y and Z are independently selected from hydrogen and alkoxy; W and X taken together is --OCH.sub.2 CH.sub.2 O--, --CH.sub.2 C(CH.sub.3).sub.2 O--, --OC(CH.sub.3).sub.2 O--, or --N.dbd.C(C.sub.2 H.sub.5)O--; R.sup.1 and R.sup.2 are independently selected from phenyl substituted with halogen, alkyl, haloalkyl, haloalkoxy, alkoxyalkyl, hydroxy, arylthio, alkoxy, dialkylamino, dialkylaminosulfonyl, hydroxyalkylaminocarbonyl, alkylsulfonyloxy, and haloalkylsulfonyloxy; and n is 1, 2, or 3.Type: GrantFiled: February 16, 1995Date of Patent: June 17, 1997Assignee: FMC CorporationInventors: Ian R. Silverman, Daniel H. Cohen, John W. Lyga, Steven W. Szczepanski, Syed F. Ali
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Patent number: 5624981Abstract: Polyalkylpiperidine-containing acetic acid and 3-aminoacrylic acid derivatives I ##STR1## where R.sup.1 is hydrogen, C.sub.1 - to C.sub.6 -alkyl, formyl, C.sub.2 - to C.sub.6 -alkanoyl, C.sub.1 - to C.sub.12 -alkoxy, C.sub.5 - to C.sub.6 -cycloalkoxy, cyanomethyl, hydroxymethyl, 2-hydroxyethyl or a radical of the formula --CR.sup.3 =CH--CO--OR.sup.4, whereR.sup.3 is hydrogen, C.sub.1 -to C.sub.6 -alkyl or a radical of the formula --CO--OR.sup.4 andR.sup.4 is C.sub.1 - to C.sub.20 -alkyl, C.sub.5 - to C.sub.8 -cycloalkyl, C.sub.7 - to C.sub.18 -aralkyl, phenyl, tolyl or a radical of the formula --(CH.sub.2 CH.sub.2 O).sub.n H or --[CH(CH.sub.3)CH.sub.2 O].sub.n H, where n is a number from 1 to 30,X is O, NH or NR.sup.6, whereR.sup.6 is C.sub.1 - to C.sub.12 -alkyl, andY is hydrogen or a group of the formula =CH--NHR.sup.7 or =CH--NR.sup.6 R.sup.7, whereR.sup.7 is phenyl which can be substituted by one to three C.sub.1 - to C.sub.12 -alkyl, C.sub.1 - to C.sub.Type: GrantFiled: October 7, 1994Date of Patent: April 29, 1997Assignee: BASF AktiengesellschaftInventors: Martin Holderbaum, Alexander Aumueller, Hubert Trauth
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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: 5620992Abstract: A compound of formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, X.sub.1, X.sub.2, x, Y and Z are as defined in the specification are useful in the treatment or prophylaxis of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: March 10, 1995Date of Patent: April 15, 1997Assignee: SmithKline Beecham plcInventors: Francis D. King, Laramie M. Gaster, Keith R. Mulholland
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Patent number: 5616711Abstract: A method of producing an aminobutene derivative of formula (I) by allowing a butenol derivative of formula (II) to react with an amide derivative of formula (III) is disclosed. The aminobutene derivative of formula (I) can be deprotected to produce an aminobutene derivative of formula (I-1) or an aminobutene derivative of formula (I-2): ##STR1## The aminobutene derivative of formula (I-A) can also be deprotected to produce the aminobutene derivative of formula (I-B). Any or all of the above aminobutene derivatives are useful as intermediates for producing anti-ulcer drugs, and anti-ulcer drugs having an inhibitory effect on gastric acid secretion based on the antagonism against histamine H.sub.2 receptor.Type: GrantFiled: August 6, 1993Date of Patent: April 1, 1997Assignee: Fujirebio Inc.Inventors: Hiroshi Ikawa, Hajime Matsumoto, Masakatsu Matsumoto, Yasuo Sekine, Masato Nishimura, Akihiko Hosoda
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Patent number: 5616583Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.Type: GrantFiled: April 13, 1995Date of Patent: April 1, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
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Patent number: 5607950Abstract: The invetion is a method of treating irritable bowel syndrome with a compound selected from the formula ##STR1## wherein R, R.sup.1, m, n p are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 10, 1994Date of Patent: March 4, 1997Assignee: Pfizer Inc.Inventors: David Alker, Peter E. Cross, Alexander R. Mackenzie
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Patent number: 5604182Abstract: Compounds of formula (I): ##STR1## and salts and esters thereof have valuable anthelmintic, acaricidal and insecticidal activities. Methods of preparing the compounds are also provided.Type: GrantFiled: July 11, 1994Date of Patent: February 18, 1997Assignee: Sankyo Company LimitedInventors: Yasuhiro Morisawa, Akio Saito, Toshimitsu Toyama, Susumu Kaneko
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Patent number: 5602129Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.Type: GrantFiled: April 13, 1995Date of Patent: February 11, 1997Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Frans M. A. Van den Keybus
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Patent number: 5595993Abstract: Piperidinyl-substituted cyclohexanes of Formula I have anti-ischemic properties: ##STR1## wherein R=R.sub.1 and is independently H or halogen; or R and R.sub.1 may be taken together to form an --O(CH.sub.2).sub.m O-- (m=1 or 2);X=a phenyl residue;R.sub.2 =R.sub.3 and is independently H or C.sub.1-4 alkyl; andR.sub.4 =phenyl or substituted phenyl wherein the phenyl group is mono-, or di-substituted with groups selected from: F, Cl, I and C.sub.1-4 alkoxy.Type: GrantFiled: September 14, 1994Date of Patent: January 21, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Ronald J. Mattson, John D. Catt
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Patent number: 5589489Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: December 12, 1994Date of Patent: December 31, 1996Assignee: Zeneca LimitedInventors: Ashokkumar B. Shenvi, Robert T. Jacobs, Scott C. Miller, Cyrus J. Ohnmacht, Jr., Chris A. Veale
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Patent number: 5580885Abstract: The use of a compound of formula (I) or pharmaceutically acceptable salt thereof, in which X.sub.1 --(CH.sub.2).sub.x --X.sub.2 forms a 5-7 membered ring wherein: X.sub.1 is O or S; X.sub.2 is O, S, NR or NRCO wherein R is hydrogen or C.sub.1-6 alkyl; x is 1, 2 or 3; Y is O or NH; Z is sub-formula (a), (b) or (c) in the manufacture of a medicament for use in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: July 28, 1994Date of Patent: December 3, 1996Assignee: SmithKline Beecham p.l.c.Inventors: Francis D. King, Laramie M. Gaster, Keith R. Mulholland, Shirley K. Rahman, Paul A. Wyman, Gareth J. Sanger, Kay A. Wardle, Gordon S. Baxter, Guy A. Kennett, Alberto J. Kauman
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Patent number: 5576313Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.Type: GrantFiled: August 29, 1994Date of Patent: November 19, 1996Assignee: Merck & Co., Inc.Inventors: Thorsten E. Fisher, John S. Wai, J. Christopher Culberson, Walfred S. Saari
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Patent number: 5574046Abstract: Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.Type: GrantFiled: March 9, 1994Date of Patent: November 12, 1996Assignee: Pfizer Inc.Inventors: Yuhpyng L. Chen, Arthur A. Nagel
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Patent number: 5571914Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.Type: GrantFiled: June 6, 1995Date of Patent: November 5, 1996Assignee: Taiho Pharmaceutical Co. Ltd.Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
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Patent number: 5569664Abstract: Compounds of the following structure, the corresponding N-oxides and agriculturally acceptable salts, are disclosed as effective insecticides: ##STR1## in which U is selected from ##STR2## Q is selected from hydrogen, hydroxy, sulfhydryl, and fluorine; R is selected from a heterocycle having 5 or 6 ring atoms, optionally fused to a benzene ring, and ##STR3## wherein V, W, X, Y, Z are as defined in the specification.Type: GrantFiled: May 19, 1995Date of Patent: October 29, 1996Assignee: FMC CorporationInventors: Ian R. Silverman, Daniel H. Cohen, John W. Lyga, Steven W. Szczepanski, Syed F. Ali