Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 514/418)
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Patent number: 5780498Abstract: The present invention provides novel compounds represented by the general formula I: ##STR1## wherein R.sub.1 is a straight or branched lower alkyl, a cycloalkyl-lower alkyl, an aryl-lower alkyl, a cycloalkyl, an aryl an aryl-cycloalkyl, lower alkoxy, an aryloxy, or a heteroaryl;R.sub.2 is hydrogen, a straight or branched lower alkyl, a cycloalkyl, or a cycloalkyl-lower alkyl;R.sub.3 and R.sub.3 ' are each the same or different and each is hydrogen atom, a straight or branched lower alkyl, a cycloalkyl, an aryl-lower alkyl, an aryl, or a heteroaryl; orR.sub.3 and R.sub.3 ' together form a ring structure;R.sub.3 " is hydrogen, lower alkyl or an aryl; orR.sub.2 and R.sub.3 " together form a lower alkylene group --(CH.sub.2).sub.n -- wherein n is an integer of 1, 2 or 3; orR.sub.2 and R.sub.3 " together form a group represented by the formula: --(CH.sub.2).sub.p --Ar-- or --Ar--(CH.sub.2).sub.p --, respectively, wherein p is zero or an integer of 1 or 2, and Ar is an arylene or heteroarylene;C(.dbd.X) is C(.dbd.Type: GrantFiled: April 30, 1996Date of Patent: July 14, 1998Assignee: Ciba-Geigy Japan LimitedInventors: Hideyuki Saika, Toshiki Murata, Thomas Pitterna, Thomas Fruh, Lene D. Svensson, Yoshihiro Urade, Takaki Yamamura, Toshikazu Okada
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Patent number: 5776969Abstract: Disorders of sleep are treated with a combination of a serotonin reuptake inhibitor and a serotonin 1A receptor antagonist.Type: GrantFiled: February 27, 1997Date of Patent: July 7, 1998Assignee: Eli Lilly and CompanyInventor: Steven Parker James
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Patent number: 5776932Abstract: 1,3,5-trisubstituted indazole derivatives of the formula ##STR1## wherein R1 is H, (b) a C.sub.1-6 straight or branched, substituted or unsubstituted alkyl residue, (c) a C.sub.3-7 cycloalkyl residue, (d) an unsustituted or substituted phenyl, naphthyl, anthranyl, or fluorenyl residue, (e) a quinolin-2-ylmethoxy, or pyridin-2-ylmethoxy residue; X is O, or a --NH, --NH--(C.dbd.O)--NH--, --NH--(C.dbd.O)--O--, --NH--(C.dbd.O)--, or --NH--CH.sub.2 --(C.dbd.O)-- residue; Y is O, or S; R.sub.2 is H; Z is a SO, SO.sub.2, --(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --O--, --O--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--, --(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--NH--, --NH--(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CHOH--, --CHOH--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CH.dbd.CH--, or --CH.dbd.CH--(CH.sub.2).sub.Type: GrantFiled: March 20, 1997Date of Patent: July 7, 1998Assignee: Arzneimittelwerk Dresden G.m.b.H.Inventors: Rudolf Schindler, Ilona Fleischhauer, Istvan Szelenyi
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Patent number: 5766578Abstract: A method of neutralizing axillary malodor by contacting the malodor with a sulfhydryl reactant.Type: GrantFiled: June 7, 1995Date of Patent: June 16, 1998Assignee: The Gillette CompanyInventor: Iris J. Davis
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Patent number: 5767139Abstract: The present invention provides compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, together with pharmaceutically compositions containing, uses of, processes for the preparation of and intermediates used in the preparation of, such compounds.Type: GrantFiled: August 2, 1994Date of Patent: June 16, 1998Assignee: Pfizer, Inc.Inventors: Graham Nigel Maw, Julian Blagg, Colin William Greengrass, Paul William Finn
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Patent number: 5763465Abstract: There are disclosed compounds of formula I,Ar--CH.sub.2 CH.sub.2 --NH--CR.sup.1 R.sup.2 --X--Y Iin whichAr represents a group, ##STR1## X represents a C.sub.1-12 alkylene chain optionally interrupted or terminated by one or more groups selected from --S(O).sub.n --, --O--, --C(Z)--, CR.sup.6 R.sup.7, phenylmethyne, --NR.sup.8 --, --CONH--, --NHCO-- and --NHCONH--,Y represents an optionally substituted aryl or cycloalkyl group,Z represents O or S,R.sup.1, R.sup.2, R.sup.5 and R.sup.9 each independently represent hydrogen or alkyl C.sub.1-6,R.sup.3 and R.sup.4 represent hydrogen, or R.sup.3 and R.sup.4 together form a group --S--, --NR.sup.9 -- or --CH.sub.2 --,R.sup.6 and R.sup.7 independently represent hydrogen, alkyl C.sub.1-6, fluoro, cyano, or CF.sub.3, provided that at least one of R.sup.6 and R.sup.7 is other than hydrogen,R.sup.8 represents hydrogen or alkyl C.sub.1-6, or when X is interrupted or terminated by more than one --NR.sup.8 -- group may together with another R.sup.8 group form the chain --CH.Type: GrantFiled: October 31, 1996Date of Patent: June 9, 1998Assignee: Astra Pharmaceuticals LimitedInventors: Roger V. Bonnert, Roger C. Brown, David R. Cheshire, Francis Ince, John Dixon
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Patent number: 5760248Abstract: A description is given of tachykinin receptor antagonists having general formula (I) ##STR1## their preparation and use in pharmaceutical formulations.Type: GrantFiled: May 31, 1996Date of Patent: June 2, 1998Assignee: A.Menarini Industrie Farmaceutiche Riunite S.r.l.Inventors: Alessandro Sisto, Christopher Fincham, Edoardo Potier, Stefano Manzini, Federico Arcamone, Paolo Lombardi
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Patent number: 5731326Abstract: Methods for inhibiting intimal hyperplasia in the vasculature of mammals, including primates, are disclosed. The methods comprise administering to the mammal a non-peptide PDGF antagonist such as 4-(2-(N-(2-carboxamidoindole)aminoethyl)-benzenesulfonamides or sulfonylureas. The methods are useful in reducing intimal hyperplasia due to, for example, vascular injuries resulting from angioplasty, endarterectomy, reduction atherectomy or anastomosis of a vascular graft. The non-peptide PDGF antagonists may optionally be administered coordinately with heparin, whereby the coordinately administered of non-peptide PDGF antagonist and heparin are combinatorially effective in inhibiting intimal hyperplasia.Type: GrantFiled: May 29, 1996Date of Patent: March 24, 1998Assignee: ZymoGenetics, Inc.Inventors: Charles E. Hart, Mark W. Orme, Kristen M. Moynihan
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Patent number: 5728723Abstract: The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.Type: GrantFiled: June 7, 1995Date of Patent: March 17, 1998Assignee: SanofiInventors: Alain Di Malta, Loic Foulon, Georges Garcia, Dino Nisato, Richard Roux, Claudine Serradeil-Legal, Gerard Valette, Jean Wagnon
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Patent number: 5728712Abstract: 3,4-Disubstituted-phenylsulphonamides have therapeutic utility via TNF or phosphodiesterase inhibition.Type: GrantFiled: May 20, 1996Date of Patent: March 17, 1998Assignee: Chiroscience LimitedInventors: John Gary Montana, Hazel Joan Dyke, Robert James Maxey, Christopher Lowe
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Patent number: 5721245Abstract: A compound of the formula ##STR1## wherein R is hydrogen or hydroxy, R.sup.1 and R.sup.2 taken together are a group of the formula --(CH.sub.2).sub.m -- and R.sup.7 is hydrogen or R.sup.1 and R.sup.7 taken together are a group of the formula --(CH.sub.2).sub.n -- and R.sup.2 is hydrogen; R.sup.3 is an aryl or aromatic heterocyclic group; R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halogen, alkyl, hydroxy, alkoxy, haloalkyl, nitro, amino, acylamino, alkylthio, alkylsulfinyl or alkylsulfonyl; R.sup.8 is a group of the formula --(CH.sub.2).sub.p --R.sup.9 or --(CH.sub.2).sub.q --R.sup.10 ; R.sup.9 is hydrogen, alkylcarbonyl, aminoalkylcarbonyl, cyano, amidino, alkoxycarbonyl, aryloxycarbonyl, alkylsulfonyl, aminocarbonyl or aminothiocarbonyl; R.sup.Type: GrantFiled: January 17, 1995Date of Patent: February 24, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Peter David Davis, Christopher Huw Hill, Geoffrey Lawton
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Patent number: 5714509Abstract: A sialidase inhibitor of the shown formula I: ##STR1## where dashed lines d.sub.1 and d.sub.2, X.sub.1, R.sub.1, R.sub.2, R.sub.6, R.sub.3, R.sub.4 and R.sub.5 are as described in the specification; or an analog, pharmaceutically acceptable salt, or derivative of the inhibitor, with the proviso that the inhibitor is not HNBA GBA or Neu5Ac2en. The inhibitor in a composition with a pharmaceutically acceptable carrier. Methods of making a pharmaceutical composition of an acceptable carrier and the inhibitor. Methods of inhibiting sialidase and methods of treating and preventing bacterial or trypanosomal infection using the inhibitor.Type: GrantFiled: May 3, 1995Date of Patent: February 3, 1998Assignee: The University of AlabamaInventors: Ming Luo, Clinton L. White
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Patent number: 5684033Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.Type: GrantFiled: June 5, 1995Date of Patent: November 4, 1997Assignee: Eli Lilly and CompanyInventors: Sung Y. Cho, Thomas A. Crowell, Bruce D. Gitter, Philip A. Hipskind, J. Jeffry Howbert, Joseph H. Krushinski, Jr., Karen L. Lobb, Brian S. Muehl, James A. Nixon
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Patent number: 5684034Abstract: A class of novel 1-indole-3-acetamides represented by the formula; ##STR1## is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids.Type: GrantFiled: May 5, 1995Date of Patent: November 4, 1997Assignee: Eli Lilly and CompanyInventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
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Patent number: 5679700Abstract: Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. These inhibitors may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.Type: GrantFiled: November 9, 1995Date of Patent: October 21, 1997Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Philippe L. Durette, Joung L. Goulet, William K. Hagmann, Soumya P. Sahoo
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Patent number: 5679828Abstract: Some betulinic acid and dihydrobetulinic acid acyl derivatives according to the present invention have been found to have potent anti-HIV activity. Introducing a C.sub.2 -C.sub.20 substituted or unsubstituted acyl group at the C.sub.3 -hydroxy group of betulinic acid and dihydrobetulinic acid produces the corresponding 3-O-acyl derivatives. The compounds of the present invention have the following formulae: ##STR1## where R may be a mono- or dicarboxylacyl group, substituted or unsubstituted, of from about 2 to about 20 carbon atoms, and R' may be hydrogen or a C.sub.2 -C.sub.10 substituted and unsubstituted alkyl or aryl group.Type: GrantFiled: June 5, 1995Date of Patent: October 21, 1997Assignees: Biotech Research Labs, Inc., University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yoshiki Kashiwada, Fumio Hashimoto, Louis Mark Cosentino, Mark Manak
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Patent number: 5674888Abstract: The invention concerns the recognition that certain non-steroidal anti-inflammatory agents can overcome or ameliorate limitations on trabecular meshwork cell division produced by environmental stresses (e.g., oxidative or phagocytic injury, or glucocorticoid exposure), and thus can be used to prevent or treat loss of trabecular cells found in certain forms of glaucoma and in normal aging. The use of such non-steroidal anti-inflammatory agents can ameliorate the severity, or prevent glaucoma.Type: GrantFiled: June 7, 1995Date of Patent: October 7, 1997Assignee: University of CaliforniaInventors: Jon R. Polansky, Ernest Bloom, Donald J. Fauss
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Patent number: 5672596Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which 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 increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient therefore are also disclosed.Type: GrantFiled: April 18, 1995Date of Patent: September 30, 1997Assignee: Merck & Co., Inc.Inventors: Matthew Wyvratt, Robert DeVita, Richard Bochis, William Schoen
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Patent number: 5670507Abstract: There is disclosed a method for reversing the multiple drug resistant (MDR) phenotype in tumors insensitive to hydrophobic chemotherapeutic drugs due to over expression of mdr-1, comprising administering an effective amount of a long chain amino alcohol compound. There is further disclosed a method for preventing the development of MDR during cancer chemotherapy treatments, comprising administering during cancer chemotherapy treatments an effective amount of a long chain amino alcohol compound.Type: GrantFiled: January 27, 1995Date of Patent: September 23, 1997Assignee: Cell Therapeutics, Inc.Inventors: Glenn C. Rice, Jack W. Singer
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Patent number: 5663192Abstract: This invention provides methods for treating or preventing a condition associated with an excess of neuropeptide Y which methods comprise administration of one or more substituted benzofurans, benzothiophenes or indoles.Type: GrantFiled: October 20, 1994Date of Patent: September 2, 1997Assignee: Eli Lilly and CompanyInventors: Robert F. Bruns, Jr., Donald R. Gehlert, J. Jeffry Howbert, William H. W. Lunn
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5658904Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: June 6, 1995Date of Patent: August 19, 1997Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5641783Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: September 8, 1994Date of Patent: June 24, 1997Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5635527Abstract: A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.Type: GrantFiled: February 6, 1996Date of Patent: June 3, 1997Assignee: The Green Cross CorporationInventors: Shinichiro Ono, Tomohiro Yoshida, Atsuyuki Ashimori, Keigo Kosaka, Takehiro Okada, Kazuhiro Maeda, Masahiro Eda, Fumio Mori, Yoshihisa Inoue, Hajime Ebisu, Teruaki Imada, Ruriko Ikegawa, Feng Wang, Norifumi Nakamura
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Patent number: 5631280Abstract: The present invention comprises peptidomimetic compounds which comprise a suitably aniline and aminoalkylbenzene moieties. The instant compounds inhibit the farnesyl-protein transferase enzyme and the farnesylation of certain proteins. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: May 24, 1995Date of Patent: May 20, 1997Assignee: Merck & Co., Inc.Inventors: Terrence M. Ciccarone, Christopher J. Dinsmore, Gerald E. Stokker, John S. Wai, Theresa M. Williams
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Patent number: 5612368Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which Ar, X, R.sub.1 and R.sub.2 are as defined in the description and a medicinal product containing the same in order to treat a disorder of the melatoninergic system.Type: GrantFiled: October 25, 1995Date of Patent: March 18, 1997Assignee: Adir et CompagnieInventors: Jean Andrieux, Michel Langlois, Pierre Renard, Philippe Delagrange
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Patent number: 5610174Abstract: The present invention provides a method of treating urinary incontinence in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the following structure: ##STR1## wherein each of the substiutents for the compound is as defined in the specification.Type: GrantFiled: June 2, 1995Date of Patent: March 11, 1997Assignee: Synaptic Pharmaceutical CorporationInventors: Douglas A. Craig, Carlos C. Forray, Charles Gluchowski, Theresa A. Branchek
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Patent number: 5607959Abstract: Compounds of formula (I) where R.sup.1 is thienyl, phenyl or furyl, X and Y are halogen or hydrogen and Q is alkoxy or amino are useful as analgesic and antiinflamatory agents.Type: GrantFiled: July 21, 1995Date of Patent: March 4, 1997Assignee: Pfizer Inc.Inventor: Ralph P. Robinson
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Patent number: 5602169Abstract: There is provided novel substituted 3-phenyl oxindole derivatives of the formula ##STR1## whereinR is hydrogen, hydroxy or fluoro;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are independently hydrogen, C.sub.1-4 alkyl, halogen, trifluoromethyl, phenyl, p-methylphenyl or p-trifluoromethylphenyl; or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 are joined together to form a benzo fused ring;R.sup.5 is hydrogen or C.sub.1-4 alkyl; andR.sup.6 is chlorine or trifluoromethyl; or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof, which are openers of the large-conductance calcium-activated potassium channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.Type: GrantFiled: April 19, 1996Date of Patent: February 11, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Piyasena Hewawasam, Nicholas A. Meanwell, Valentin K. Gribkoff
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Patent number: 5599832Abstract: There are provided methods for the control of insects and the protection of crops from the damage caused thereby which comprise the use of compositions comprising an indole compound of formula I ##STR1##Type: GrantFiled: December 13, 1995Date of Patent: February 4, 1997Assignee: American Cyanamid CompanyInventor: David M. Gange
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Patent number: 5597814Abstract: The present invention relates to a method for regulating wrinkles and/or atrophy in mammalian skin comprising treating the skin with a safe and effective amount of salicylic acid and/or additional active component.Type: GrantFiled: June 5, 1995Date of Patent: January 28, 1997Assignee: Richardson-Vicks Inc.Inventor: Roy L. Blank
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Patent number: 5593990Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Importantly, these compounds can be administered orally.Type: GrantFiled: January 13, 1995Date of Patent: January 14, 1997Assignee: The Children's Medical Center CorporationInventor: Robert D'Amato
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Patent number: 5591768Abstract: A method for treating circadian rhythm phase disorders is described. The invention provides methods to specifically advance or delay the phase of certain circadian rhythms in humans. The disclosed methods relate to the administration of melatonin at times determined with relation to the time of dim light endogenous melatonin onset. Embodiments capable of alleviating the effects of jet lag, winter depression and shift-work sleep disturbance are provided.Type: GrantFiled: August 24, 1993Date of Patent: January 7, 1997Assignee: State of Oregan, Acting by and Through the Oregon State Board of Higher Education on Behalf of the Oregon Health Sciences UniversityInventors: Alfred J. Lewy, Robert L. Sack
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Patent number: 5583130Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which 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 increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such bezno-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: September 25, 1992Date of Patent: December 10, 1996Assignee: Merck & Co., Inc.Inventors: Richard J. Bochis, Michael H. Fisher, Robert J. Devita, William R. Schoen, Matthew J. Wyvratt
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Patent number: 5578633Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.Type: GrantFiled: June 2, 1995Date of Patent: November 26, 1996Assignee: SanofiInventors: Jean Wagnon, Paul de Cointet, Dino Nisato, Claude Plouzane, Claudine Serradeil-Legal, Bernard Tonnerre
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Patent number: 5576330Abstract: The new use of a compound of formula (I) ##STR1## wherein Y is a bicyclic ring selected from naphthalene, tetralin, quinoline, isoquinoline and indole;n is zero or an integer of 1 to 3;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro, or NHR, wherein R is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR, wherein R is as defined above;R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen; or a pharmaceutically acceptable salt thereof;and wherein when Y is naphthalene then n is zero or an integer of 1 to 3, whereas when Y is tetralin, quinoline, isoquinoline or indole then n is zero, 1 or 2; and wherein when the bicyclic ring Y is naphthalene, quinoline, isoquinoline or indole, then each of the substituents OR.sub.1, R.sub.Type: GrantFiled: December 12, 1994Date of Patent: November 19, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Maria G. Brasca, Fabrizio Orzi, Angelo Crugnola, Dario Ballinari, Mariangela Mariani
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Patent number: 5565484Abstract: The invention relates to use of at least one indole derivative of general formula: ##STR1## or of one of the pharmaceutically acceptable salts thereof, in which: Am is selected from radical (a) and (b) defined as follows: ##STR2## R is a C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl radical R.sub.1 represents hydrogen or a C.sub.1 -C.sub.4 alkyl radicalR.sub.2 and R.sub.3, which may be identical or different, represent hydrogen, the methyl or ethyl radical or a halogenR.sub.4, R.sub.5 and R.sub.6, which may be identical or different, represent hydrogen, a C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy radical or a halogenR.sub.7 represents hydrogen or a halogenR.sub.8 represents hydrogen or a C.sub.1 -C.sub.4 alkyl radicalR.sub.9 represents hydrogen or, when R.sub.8 and R.sub.9 are taken together, form the methylene radicalm represents 1 or 2n represents 2, 3 or 4for preventing or treating diseases involving a proliferation of smooth muscle cells.Type: GrantFiled: July 29, 1994Date of Patent: October 15, 1996Assignee: SanofiInventors: Jean-Marc Herbert, Pierre Chatelain
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Patent number: 5565483Abstract: There is provided novel substituted 3-phenyl oxindole derivatives of the formula ##STR1## wherein R is hydrogen, hydroxy or fluoro; R.sup.1, R.sup.2, R.sup.3and R.sup.4 each are independently hydrogen, C.sub.1-4 alkyl, halogen, trifluoromethyl, phenyl, p-methylphenyl or p-trifluoromethylphenyl; or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 are joined together to form a benzo fused ring;R.sup.5 is hydrogen or C.sub.1-4 alkyl; andR.sup.6 is chlorine or trifluoromethyl;or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof, which are openers of the large-conductance calcium-activated potassium channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.Type: GrantFiled: June 7, 1995Date of Patent: October 15, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Piyasena Hewawasam, Nicholas A. Meanwell, Valentin K. Gribkoff
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Patent number: 5565460Abstract: The present invention relates to a therapeutic agent for Parkinson's disease containing as an active ingredient a polycyclic compound or a pharmaceutically acceptable salt thereof, the compound being represented by the following Formula (I): ##STR1## and A represents N or CR.sup.5 (in which R.sup.5 represents hydrogen, or substituted or unsubstituted lower alkyl), or represented by the following Formula (II): ##STR2## wherein Y, R.sup.6 and R.sup.8 are as defined herein and B and the adjacent two carbon atoms are combined to form a substituted or unsubstituted, partially saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic group.Type: GrantFiled: March 3, 1995Date of Patent: October 15, 1996Assignee: Kyowa Hakko Koygo Co., Ltd.Inventors: Fumio Suzuki, Junichi Shimada, Nobuaki Koike, Shunji Ichikawa, Joji Nakamura, Tomoyuki Kanda, Shigeto Kitamura
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Patent number: 5556874Abstract: 2-Thioindoles (2-selenoindoles) and analogous 2-indolinethione (2-indolineselenone) and polysulfide (selenide) compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for inhibiting protein kinase dependent disease in a mammal or treating aberrant cell growth in a mammal, using said compositions, are disclosed.Type: GrantFiled: May 10, 1995Date of Patent: September 17, 1996Assignee: Warner Lambert CompanyInventors: Ellen M. Dobrusin, Howard D. H. Showalter, William A. Denny, Brian D. Palmer, Gordon W. Rewcastle, Moana Tercel, Andrew M. Thompson
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Patent number: 5554642Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description,its optical isomers and its addition salts thereof with a pharmaceuticaliy-accepable acid or base,and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.Type: GrantFiled: May 22, 1995Date of Patent: September 10, 1996Assignee: Adir et CompagnieInventors: Michel Langlois, Pierre Renard, G erard Adam
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Patent number: 5545656Abstract: This invention relates to the use of certain 3-substituted 2-oxindole-1-carboxamides and their pharmaceutically acceptable base salts for the treatment or prevention of Alzheimer's disease in mammals, including humans.Type: GrantFiled: April 5, 1995Date of Patent: August 13, 1996Assignee: Pfizer Inc.Inventors: Leland D. Loose, Joseph G. Lombardino, Ethan S. Weiner
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Patent number: 5538992Abstract: The power of fluoxetine, venlafaxine, milnacipran and duloxetine to increase the availability of serotonin, norepinephrine and dopamine, particularly serotonin, is augmented by administration in combination with a drug which is a serotonin 1A receptor antagonist.Type: GrantFiled: May 17, 1995Date of Patent: July 23, 1996Assignee: Eli Lilly and CompanyInventors: David T. Wong, Juan I. Oguiza
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Patent number: 5532250Abstract: The power of fluoxetine, venlafaxine, milnacipran and duloxetine to increase the availability of serotonin, norepinephrine and dopamine, particularly serotonin, is augmented by administration in combination with a drug which is a serotonin 1A receptor antagonist.Type: GrantFiled: May 17, 1995Date of Patent: July 2, 1996Assignee: Eli Lilly and CompanyInventors: David T. Wong, Juan I. Oguiza
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Patent number: 5532264Abstract: The power of fluoxetine, venlafaxine, milnacipran and duloxetine to increase the availability of serotonin, norepinephrine and dopamine, particularly serotonin, is augmented by administration in combination with a drug which is a serotonin 1A receptor antagonist.Type: GrantFiled: May 17, 1995Date of Patent: July 2, 1996Assignee: Eli Lilly and CompanyInventors: David T. Wong, Juan I. Oguiza
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Patent number: 5510379Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.Type: GrantFiled: December 19, 1994Date of Patent: April 23, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5502072Abstract: The present invention relates to novel substituted oxindoles of the formula I as defined below and related compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds as inhibitors of phosphodiesterase ("PDE") type IV. The compounds of this invention are useful in the treatment of AIDS, asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways disease, psoriasis, allergic rhinitis, atopic, dermatitis, shock, other inflammatory diseases, and other conditions where the action of phosphodiesterase type IV is implicated.Type: GrantFiled: November 26, 1993Date of Patent: March 26, 1996Assignee: Pfizer Inc.Inventor: Hiroko Masamune
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Patent number: 5498625Abstract: Lactams of 1-amino-3-carboxylic acid cyclic compounds are produced in enantiomeric form, together with an enantiomer of the corresponding ring-opened amino-acid or ester, by reaction of the racemic lactam with a novel lactamase. The products are useful in the synthesis of chiral carbocyclic nucleotides. The enantiomer is preferrably 2-azabicyclo(2.2.1)hept-5-en-3-one. It is desirable to isolate the enantiomer comprising predominantly the (+) enantiomer and a residual amount of the (-) enantiomer, wherein the (+) enantiomer is present in an enantiomeric excess of at least about 88% over the (-) enantiomer or the enantiomer comprising predominantly the (-) enantiomer and a residual amount of the (+) enantiomer, wherein the (-) enantiomer is present in an enantiomeric excess of at least about 98% over the (+) enantiomer.Type: GrantFiled: November 8, 1994Date of Patent: March 12, 1996Assignee: Chiroscience LimitedInventors: Christopher T. Evans, Stanley M. Roberts
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Patent number: 5494928Abstract: The invention releates to indole derivatives of the formula ##STR1## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl or trifluoromethyl, R.sup.5 and R.sup.6 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl, trifluoromethyl, hydroxy or lower-alkoxy and R.sup.7 is hydrogen or lower-alkyl, andpharmaceutically acceptable acid addition salts thereof.The compounds of formula I bind to serotonin receptors and are therefore useful in the treatment and/or prevention of central nervous system disorders, such as depression.Type: GrantFiled: October 3, 1994Date of Patent: February 27, 1996Assignee: Hoffmann-La Roche Inc.Inventor: Michael Bos
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Patent number: 5488057Abstract: The present invention provides novel aryl- and heteroarylethenylene derivatives which are useful as tyrosine kinase activity inhibitors.Type: GrantFiled: August 23, 1994Date of Patent: January 30, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
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Patent number: RE35279Abstract: The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives.The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton.The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.Type: GrantFiled: February 17, 1994Date of Patent: June 18, 1996Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Ei Mochida, Kimihiro Murakami, Kazuo Kato, Katsuaki Kato, Jun Okuda, Ichitomo Miwa