Patents Examined by Ann M. Kessinger
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Patent number: 6130215Abstract: The invention refers to novel piperazinylalkylthiopyrimidine derivatives of formula (I) being suitable for the treatment of diseases due to pathological alterations of the central nervous system, pharmaceutical compositions containing the above derivatives, and a process for the preparation of the novel compounds.Type: GrantFiled: June 23, 1998Date of Patent: October 10, 2000Assignee: Egis Gyoyszergyar RTInventors: Ivan Jakoczi, Daniel Bozsing, Ildiko Ratz nee Simonek, Istvan Gacsalyi, Gabor Szenasi, Eva Schmidt, Aniko Miklos nee Kovacs, Andras Bilkei-Gorzo, Gabor Blasko, Istvan Gyertyan, Gabor Nemeth, Gyula Simig, Karoly Tihanyi, Andras Egyed
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Patent number: 6093727Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human a, adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: October 20, 1998Date of Patent: July 25, 2000Assignee: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Yoon T. Jeon, Charles Gluchowski
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Patent number: 6093716Abstract: Compounds of general formula (1): ##STR1## are described wherein Het is an optionally substituted heteroaromatic group; R.sup.1 is a hydrogen atom or a straight or branched chain alkyl group; R.sup.2 is a hydrogen or halogen atom or a group --X.sup.1 --R.sup.2a where X.sup.1 is a direct bond or a linker atom or group, and R.sup.2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R.sup.3 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein kinase inhibitors, particularly the kinases p56.sup.lck, ZAP-70 and protein kinase C and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.Type: GrantFiled: September 15, 1997Date of Patent: July 25, 2000Assignee: Celltech Therapeutics, LimitedInventors: Peter David Davis, David Festus Charles Moffat, Mark James Batchelor
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Patent number: 6071913Abstract: Disclosed are novel 1,2,4-triazin-5-one biphenyl derivatives having structural formula (I) useful as non-peptide antagonists of angiotensin II receptor: ##STR1## where R.sub.1 represents alkyl, cycloalkyl, or substituted or unsubstituted aryl;R.sub.2 represents alkyl, substituted or unsubstituted aryl, or arylalkyl;A and D independently represent C--R.sub.3, N, NH or C.dbd.O, wherein when A and D independently denote C--R.sub.3 or N, b and c are independently a double bond, and when A and D independently denote NH or C.dbd.O, b and c are independently a single bond; provided that b and c are not both double bonds; andR.sub.3 is hydrogen, dialkylphosphonate or halogen;and pharmaceutically acceptable salts thereof.Also disclosed is the use of the compounds of formula (I) as non-peptide antagonists of angiotensin II receptor, in the treatment of cardiovascular diseases, in particular hypertension and congestive heart failure.Type: GrantFiled: December 9, 1997Date of Patent: June 6, 2000Assignee: Development Center for BiotechnologyInventors: Paw-Hwa Yang, Pei-Ling Lee, Shan-Yen Chou, Chia-Lin Wang, Hsiao-Hwa Lu
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Patent number: 6063787Abstract: The present invention relates to the use of (-)-(2S,4S)-1-(2-hydroxymethyl-1,3-dioxolan-4-yl) cytosine to treat psoriasis, genital warts and other hyperproliferative keratinocyte diseases such as hyperkeratosis, ichthyosis, keratoderma or lichen planus.Type: GrantFiled: January 26, 1998Date of Patent: May 16, 2000Assignees: The University of Georgia Research Foundation Center, Yale UniversityInventors: Chung K. Chu, Yung-Chi Cheng
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Patent number: 6060469Abstract: The present invention relates to compounds of formula (I), ##STR1## wherein R.sup.1 represents halogen, hydroxy, C.sub.1-6 alkyl group optionally substituted by one or three fluorine atoms, C.sub.1-6 alkoxy group optionally substituted by one to three fluorine atoms, or C.sub.1-6 alkylthio optionally substituted by one to three fluorine atoms; R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or when R.sup.2 is adjacent to R.sup.1, they may be joined together such that there is formed a 5- or 6-membered saturated or unsaturated ring containing one or two oxygen atoms; R.sup.3 represents an optionally substituted 5- or 6-membered aromatic heterocyclic group containing 1, 2, 3 or 4 heteroatoms, selected from nitrogen, oxygen and sulphur; m is 0-3 and n is 0-3, with the proviso that the sum total of m+n is 2 or 3; p is zero or 1; q is 1 or 2; and when m is 1 and n is 1 or 2, the broken line represents an optional double bond; R.sup.4, R.sup.5, R.sup.6, R.sup.9 and R.sup.Type: GrantFiled: May 18, 1998Date of Patent: May 9, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Raymond Baker, Timothy Harrison, Christopher John Swain, Brian John Williams
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Patent number: 6060487Abstract: A compound of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X--Y, A, Z and Z' are as defined in the description, in the form of the cis or trans isomers each in racemic or optically active form, and acid addition salts thereof, and medicinal products containing the same are useful in the treatment of diseases of the central nervous system or of manifestations of pain.Type: GrantFiled: March 22, 1999Date of Patent: May 9, 2000Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Mark Millan, Adrian Newman-Tancredi, Anne Dekeyne
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Patent number: 6057440Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.Type: GrantFiled: November 14, 1997Date of Patent: May 2, 2000Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
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Patent number: 6057269Abstract: Benzylhydroxylamines I ##STR1## (X=--N(R.sup.7)--O--; Y=O, S; R.sup.1 =halogen, CN, NO.sub.2, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3 =H, NH.sub.2, CH.sub.3 ;R.sup.4 =H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl;R.sup.5 =H, halogen, C.sub.1 -C.sub.6 -alkyl;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl;R.sup.7 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.2 -C.sub.8 -alkenyloxycarbonyl, C.sub.2 -C.sub.6 -alkynyloxycarbonyl, C.sub.1 -C.sub.6 -alkylthiocarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.Type: GrantFiled: January 5, 1998Date of Patent: May 2, 2000Assignee: BASF AktiengesellschaftInventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz, Olaf Menke, Markus Menges
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Patent number: 6048865Abstract: A series of adenosine-5'-uronamide derivatives bearing N.sup.6 -arylurea, alkarylurea, heteroarylurea, arylcarbonyl, alkarylcarbonyl or heteroarylcarbonyl groups which have affinity and, in some cases, selectivity for the adenosine A.sub.1 or A.sub.3 receptors are disclosed. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A.sub.1 or A.sub.3 receptors, or can be used in a diagnostic application to determine the relative binding of other compounds to the A.sub.1 or A.sub.3 receptors.Type: GrantFiled: July 29, 1998Date of Patent: April 11, 2000Assignee: Medco Research, Inc.Inventor: Pier Giovanni Baraldi
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Patent number: 6048866Abstract: Compounds of formula (1) are described: ##STR1## and the salts, solvates, hydrates and N-oxides thereof, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in claim 1. The compounds are selective inhibitors of protein kinases, especially src-family protein kinases and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.Type: GrantFiled: March 13, 1998Date of Patent: April 11, 2000Assignee: Celltech Therapeutics, LimitedInventors: Martin Clive Hutchings, Peter David Davis, David Festus Charles Moffat
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Patent number: 6046204Abstract: The invention provides certain novel 5-substituted pyrrolo[3,4-d]pyrimidine-2,4-diones, processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and methods of treatment involving their use.Type: GrantFiled: February 24, 1998Date of Patent: April 4, 2000Assignee: Astra Pharmaceuticals LimitedInventors: Martin E Cooper, David R Cheshire, David K Donald, Mark Furber, Matthew W.D Perry, Richard P Harrison, Nicholas P Tomkinsson
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Patent number: 6046329Abstract: Compounds of formula I, in which the substituents and symbols have the meanings indicated in the description, R5-HT.sub.1A -agonists and .alpha..sub.1 -adrenoceptor blockers. Compositions containing these compounds as active ingredients are useful for treating those diseases which can be treated by 5-HT.sub.1A agonists or by .alpha..sub.1 -adrenoreceptor blockers.Type: GrantFiled: June 6, 1997Date of Patent: April 4, 2000Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventors: Wolfgang Prusse, Wolf-Rudiger Ulrich
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Patent number: 6046205Abstract: Compound of formula (I): ##STR1## wherein: n is 0 or 1,A represents a .sigma. bond or alkylene or alkenylene,X represents nitrogen or C--R.sub.2,R.sub.1 represents hydrogen or alkyl,G.sub.1 represents any one of the groups defined in the description.These compounds are useful for treating a living body afflicted with venous insufficiency, and/or migraine, and/or migraine associated with vascular diseases.Type: GrantFiled: April 26, 1999Date of Patent: April 4, 2000Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Olivier Muller, Christine Vayssettes-Courchay, Jean-Jacques Descombes, Tony Verbeuren
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Patent number: 6046201Abstract: N-(12-Nitroxydodecyl)-6-(4-ethyl or isopropyl-1-piperazinyl)pyridine-3-carboxamide or physiologically acceptable salts thereof. The said compounds have excellent inhibiting activity of cerebral edema, especially ischemic cerebral edema, and inhibiting activity of delayed neuronal death (an inhibiting activity of Ca-influx in neuronal cells). Cerebral edema is a pathologic condition accompanying cerebrovascular disorders, especially the acute stage cerebrovascular disorders and then the compounds are useful as an inhibiting agent for cerebral edema or a therapeutic agent for cerebrovascular disorders. Moreover, because the compounds do hardly show a behavior suppressing action, which is considered to be side effect in treating cerebrovascular disorders at the acute stage, they are an excellent therapeutic agent for, in particular, the acute stage cerebrovascular disorders.Type: GrantFiled: July 15, 1998Date of Patent: April 4, 2000Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Norio Oshida, Yoji Mimaki, Hiroaki Satoh, Shinji Yokoyama, Yukiko Muraki, Kazumi Nishimura, Tamiko Hamada, Einosuke Sakurai, Hiroshi Sakai, Toshiji Sugai, Tomomi Tonoike, Koichi Itoh
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Patent number: 6043375Abstract: A method of preparing a taxoid of formula III by esterifying protected baccatin III or deacetylbaccatin III using an oxazolidinecarboxylic acid, or an acid halide, or an acid anhydride thereof.Type: GrantFiled: April 2, 1998Date of Patent: March 28, 2000Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Dominique Bourzat, Alain Commercon
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Patent number: 6030973Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinediones of the general formula (I), their analogues, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.Type: GrantFiled: August 17, 1998Date of Patent: February 29, 2000Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor, Inc.Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Rajagopalan Ramanujam, Ranjan Chakrabarti
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Patent number: 6025354Abstract: Arylalkyl-thiadiazinone derivatives of the formula I ##STR1## and physiologically unobjectionable salts thereof in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Q have the meanings given in claim 1, exhibit phosphodiesterase IV inhibition and can be used for the therapy of asthmatic disorders.Type: GrantFiled: January 20, 1998Date of Patent: February 15, 2000Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Rochus Jonas, Michael Wolf, Michael Klockow
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Patent number: 6020330Abstract: The present invention is concerned with new hypolipidemic compounds, with processes and novel intermediates for their preparation, with pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis.Compounds of the formula (I): ##STR1## wherein R.sup.1 to R.sup.10 and X are a defined in the specification and are useful as hypolipidemic compounds.Type: GrantFiled: March 13, 1998Date of Patent: February 1, 2000Assignee: Hoechst AktiengesellschaftInventors: Alfons Enhsen, Eugen Falk, Heiner Glombik, Siegfried Stengelin
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Patent number: 6020336Abstract: Compound of formula (I): ##STR1## wherein: n is 0 or 1,A represents a .sigma. bond or alkylene or alkenylene,X represents nitrogen or C--R.sub.2,R.sub.1 represents hydrogen or alkyl, andG.sub.1 represents any one of the groups defined in the description and medicaments containing the same.Type: GrantFiled: September 2, 1998Date of Patent: February 1, 2000Inventors: Gilbert Lavielle, Olivier Muller, Christine Vayssettes-Courchay, Jean-Jacques Descombes, Tony Verbeuren