Chalcogen Bonded Directly To Ring Carbon Of 1,4-oxazine Ring Patents (Class 514/230.8)
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Publication number: 20080267888Abstract: The present invention relates to novel heterocyclic derivatives of the general formula (I), their pharmaceutically acceptable salts and compositions, their analogs, their tautomeric forms, and their stereoisomers. The present invention more particularly provides novel compounds of the general formula (I).Type: ApplicationFiled: May 25, 2006Publication date: October 30, 2008Inventors: Surendrakumar Satyanarayan Pandey, Gaddam Om Reddy, Gajendra Singh, Chitra Santhanagopalan, Sanjay Venkatachalapathi Kadnur, Debendranath Dey, Abhijeet Nag
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Patent number: 7427618Abstract: Novel compounds of the formula (I), in which R1, R2, R3, X and Y have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.Type: GrantFiled: January 30, 2004Date of Patent: September 23, 2008Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Werner Mederski, Christos Tsaklakidis, Dieter Dorsch, Bertram Cezanne, Johannes Gleitz, Christoph van Amsterdam
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Publication number: 20080214535Abstract: A coprecipitate comprising amorphous aprepitant and a pharmaceutically acceptable carrier is prepared by rapidly removing solvent from a solution containing aprepitant and the carrier.Type: ApplicationFiled: July 31, 2006Publication date: September 4, 2008Applicants: DR. REDDY'S LABORATORIES LTD., DR. REDDY'S LABORATORIES, INC.Inventors: Vijayavitthal Thippannachar Mathad, Pravinchandra Vankawala Jayantilal, Chandrasekhar Ravi Ram Elati, Subrahmanyeswara Rao Chlamala, Naveen Kumar Kolla, Srinivas Gangula, Srirami Reddy Kikkuru, Srinivasan Neti, Raveendra Reddy Chinta
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Publication number: 20080207589Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:Type: ApplicationFiled: January 3, 2008Publication date: August 28, 2008Inventors: Rustum Boyce, Eric Martin, Weibo Wang, Hong Yang, Paul A. Barsanti
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Patent number: 7417144Abstract: The invention is concerned with novel heteroaryl fused cyclic amines of formula (I) wherein A, X1 to X3, Y1 to Y3, Z, R1, R2, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit coagulation factor Xa and can be used as medicaments.Type: GrantFiled: July 7, 2006Date of Patent: August 26, 2008Assignee: Hoffman-La Roche Inc.Inventors: Markus Boehringer, Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Narendra Panday, Fabienne Ricklin
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Patent number: 7351707Abstract: The present invention relates to optionally substituted 1-oxa-4,9-diaza-spiro[5.5]undecan-3-one compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: GrantFiled: May 3, 2006Date of Patent: April 1, 2008Assignee: Acadia Pharmaceuticals, Inc.Inventor: Nathalie Schlienger
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Patent number: 7314883Abstract: The present invention relates to methods of treating neurogenic vasodilation, neurogenic inflammaton, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors using pharmaceutical compositions comprising compounds of Formula (I)Type: GrantFiled: January 5, 2007Date of Patent: January 1, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Ling Chen, Prasad V. Chaturvedula, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, George N. Karageorge, Guanglin Luo, John E. Macor, Graham S. Poindexter, George O. Tora
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Patent number: 7265109Abstract: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein the substituents have the significance given in the specification, and the compounds are neuropeptide Y(NPY) antagonists which are useful in the treatment of obesity.Type: GrantFiled: August 10, 2004Date of Patent: September 4, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger, Sven Taylor
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Patent number: 7220862Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: December 5, 2003Date of Patent: May 22, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Ling Chen, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, George N. Karageorge, Guanglin Luo, John E. Macor, Graham Poindexter, George Tora
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Patent number: 7214701Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: June 25, 2004Date of Patent: May 8, 2007Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 7205408Abstract: Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.Type: GrantFiled: January 22, 2002Date of Patent: April 17, 2007Assignee: SmithKline Beecham, p.l.c.Inventors: David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, William Miller, Neil David Pearson
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Patent number: 7192957Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: March 20, 2007Assignee: Schering CorporationInventors: Srikanth Venkatraman, F. George Njoroge, Melissa L. Blackman, Wanli Wu, Latha G. Nair, Ashok Arasappan, Stephane L. Bogen, Kevin X. Chen, Mousumi Sannigrahi, Frank Bennett, Viyyoor M. Girijavallabhan
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Patent number: 7173057Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: February 6, 2007Assignee: Schering CorporationInventors: Kevin X. Chen, F. George Njoroge, Mousumi Sannigrahi, Latha G. Nair, Weiying Yang, Bancha Vibulbhan, Srikanth Venkatraman, Ashok Arasappan, Stephane L. Bogen, Frank Bennett, Viyyoor M. Girijavallabhan
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Patent number: 7125865Abstract: The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.Type: GrantFiled: July 21, 2003Date of Patent: October 24, 2006Assignee: Merck & Co., Inc.Inventors: A. Brian Jones, Alan D. Adams, Ahren I. Green, Shaei Y. Huang, Bruno Tse, Clare E. Gutteridge, Yuan Cheng
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Patent number: 7056929Abstract: A method for treating a living body afflicted with a cancer selected from lung and ovarian carcinoma, comprising the step of administering to the living animal body an amount of a compound selected from those of formula (I): wherein: X and Y represent group selected from hydrogen, halogen, mercapto, cyano, nitro, alkyl, trihaloalkyl, trihaloalkylcarbonylamino, —ORa, —NRaRb, —NRa—C(O)-T1, —O—C(O)-T1, —O-T2-NRaRb, —O-T2-ORa, —NRa-T2-NRaRb, —NRa-T2-ORa and —NRa-T2-CO2Ra wherein Ra, Rb, T1, T2 are as defined in the description, or X and Y together form a methylenedioxy or ethylenedioxy, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, —ORa, —NRaRb, —NRa—C(O)-T1, —O—C(O)-T1, —O-T2-NRaRb, —O-T2-ORa, —NRa-T2-NRaRb, —NRa-T2-ORa and —NRa-T2-CO2Ra wherein Ra, Rb, T1 and T2 are as defined hereinbefore, R3 and R4 represent hydrogen or alkyl, W represents a group of formula —CH(R5)—CH(R6)—, —CH?C(R7)—, —C(R7)?CH— or —C(O)—CH(R8)— wherein R5, R6, R7 and R8 are as defined in the descriptType: GrantFiled: July 26, 2003Date of Patent: June 6, 2006Assignee: Les Laboratoires ServierInventors: Michel Koch, Francois Tillequin, Sylvie Michel, Elisabeth Seguin, Abdelhakim El Omri, John Hickman, Alain Pierre, Bruno Pfeiffer, Pierre Renard
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Patent number: 7034017Abstract: This invention relates to compounds of formula (I) wherein R1 represents optionally substituted phenyl, R2 represents optionally substituted and the remaining “R” groups are as defined in the specification and claims, as well as a method for making such materials, pharmaceutical compositions containing such materials, and methods of using such materials in medical treatment.Type: GrantFiled: January 28, 2002Date of Patent: April 25, 2006Assignee: Bayer AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Josef Pernerstorfer, Elisabeth Perzborn, Jens Pohlmann, Susanne Röhrig, Karl-Heinz Schlemmer
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 6936726Abstract: The present invention refers to new products generated by the conjugation of flavanols with molecules that contain the thiol group. New molecules are obtained from polyphenolic plant extracts rich in oligomeric and polymeric procyanidines and prodelfinidins. In this way, new products are generated with antioxidant properties for application as protective agents for the organism against disorders such as cancer, cardiovascular diseases and premature aging. The invention also refers to obtaining these new agents from waste material generated by the agroalimentary industry. Since these waste materials are highly complex mixtures a simple and effective method is described to isolate and purify these, based on the physico-chemical characteristics of the new molecules.Type: GrantFiled: December 14, 2001Date of Patent: August 30, 2005Assignee: Consejo Superior de Investigaciones CientificasInventor: José Luis Torres Simón
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Patent number: 6903094Abstract: The present invention relates to a compound of the formula [1?] ? wherein R2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5 is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5 may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1?] as an active ingredient. The compound [1?] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1?] as a nociceptin antagonist or analgesic.Type: GrantFiled: May 10, 2002Date of Patent: June 7, 2005Assignee: Japan Tabacco, Inc.Inventors: Hisashi Shinkai, Takao Ito, Hideki Yamada
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Patent number: 6881735Abstract: The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.Type: GrantFiled: November 28, 2001Date of Patent: April 19, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel
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Patent number: 6864276Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: May 7, 2001Date of Patent: March 8, 2005Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 6841551Abstract: A treatment for brain, spinal and nerve injury comprising use of a substance P receptor antagonist optionally in combination with a magnesium compound. There is also provided a formulation for use in this treatment comprising a substance P receptor antagonist and a magnesium compound.Type: GrantFiled: January 18, 2001Date of Patent: January 11, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Alan John Nimmo, Robert Vink
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P2X7 receptor antagonists for use in the treatment of inflammatory, immune or cardiovascular disease
Patent number: 6812226Abstract: The invention provides piperidine compounds of general formula (I) in which A, B, X, Y, Z, R, R1 and R2 are as defined in the specification, their use as medicaments, compositions containing them and processes for their for their preparation.Type: GrantFiled: June 13, 2002Date of Patent: November 2, 2004Assignee: AstraZeneca ABInventors: Andrew Baxter, Nicholas Kindon, Garry Pairaudeau, Bryan Roberts, Stephen Thom -
Patent number: 6743790Abstract: The present invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5, R6, A, X, m and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, for example as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: June 6, 2001Date of Patent: June 1, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Otmar Klingler, Manfred Schudok, Hans-Peter Nestler, Hans Matter, Herman Schreuder
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Patent number: 6727244Abstract: This invention is concerned with mammalian metabolites of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)-phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist that is useful in the prevention and treatment of certain disorders, including emesis and psychiatric disorders such as depression and anxiety.Type: GrantFiled: April 24, 2003Date of Patent: April 27, 2004Assignee: Merck & Co., Inc.Inventors: Su-er Wu Huskey, Shuet-Hing Lee Chiu
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Patent number: 6660734Abstract: The invention relates to novel oxazinones designed to bind to the penicillin receptor, methods of synthesizing the compounds, and the use of the compounds as antibacterial agents. The compounds have the general formula (I) Preferably the compounds have a carboxyethyl or a substituted carboxymethyl substituent at the 2-position and a hydroxyl group at the 5-position and have a molecular shape suitable for binding to and reacting with the active site of a pencillin-recognizing enzyme. The compounds are synthesized by condensing a carboxyl-protected N-hydroxy amino acid with a 3-hydroxyprotected-4-bromobutanoic acid to form a a doubly protected N-hydroxy N-acylamino acid, which is cyclized with an organic base to yield a: doubly protected 1,2-oxazin-3-one. The protecting groups are then removed to provide an antibacterial agent.Type: GrantFiled: January 22, 2002Date of Patent: December 9, 2003Assignee: Simon Fraser UniversityInventors: Saul Wolfe, Christiana Akuche, Stephen Ro
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Patent number: 6656936Abstract: Acylcarnitine analogues having alkyl side chains of 10 to 30 carbon atoms display excellent spermicidal and anti-HIV activity, a well as being potent inhibitors of the growth of Candida albicans.Type: GrantFiled: July 5, 2002Date of Patent: December 2, 2003Assignee: Virginia Tech Intellectual Properties, Inc.Inventors: Prashant S. Savle, Richard D. Gandour, Gustavo F. Doncel
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Patent number: 6645960Abstract: A compound of general formula (I) and physiologically acceptable salts wherein R represents phthalidyl, (2-oxo-5-methyl-1,3-diox-olen-4-yl)methyl or the group CHR4 OCO(O)pR5 wherein R4 is hydrogen or C1-4 alcyl, p is zero or I, R5 is C1-6 alkly, C5-8 cycloalyl (optionally substituted by C1-3 alkyl or carboxyl), C1-4 alkyl substituted by C1-3 alkoxy or carboxy), C1-4 alkyl substituted by one or more groups selected from amino, (C1-4 alkylamino di(C1-4 alkyl)amino or carboxyl, phenyl (optionally substituted by carboxyl or aminoalkyl, C1-4 alkylaminoalkyl or di(C1-4 alkyl)aminoalcyl, or R5 is a 5-8 membered heterocyclic group containing 1 or 2 heteroatoms selected from oxygen or nitrogen, processes for their preparation, pharmaceutical compositions containing them and their use in medicine.Type: GrantFiled: September 24, 2002Date of Patent: November 11, 2003Assignee: Glaxo Wellcome S.A.Inventors: Jose Maria Fiandor, Sophie Huss
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Patent number: 6642248Abstract: A compound selected from those of formula (I): wherein: X and Y represent group selected from hydrogen, halogen, mercapto, cyano, nitro, alkyl, trihaloalkyl, trihaloalkylcarbonylamino, —ORa, —NRaRb, —NRa—C(O)—T1, —O—C(O)—T1, —O—T2-NRaRb, —O—T2-ORa, —NRa—T2-NRaRb, —NRa—T2-ORa and —NRa—T2-CO2Ra wherein Ra, Rb, T1, T2 are as defined in the description, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, —ORa, —NRaRb, —NRa—C(O)—T1, —O—C(O)—T1, —O—T2-NRaRb, —O—T2-ORa, —NRa—T2-NRaRb, —NRa—T2-ORa and —NRa—T2-CO2Ra wherein Ra, Rb, T1 and T2 are as defined hereinbefore, R3 and R4 represent hydrogen or alkyl, W represents a group of formula —CH(R5)—CH(R6)—, —CH═C(R7)—, —C(R7)═CH— or —C(O)—CH(R8)Type: GrantFiled: July 25, 2002Date of Patent: November 4, 2003Assignee: Les Laboratories ServierInventors: Michel Koch, François Tillequin, Sylvie Michel, Elisabeth Seguin, Abdelhakim El Omri, John Hickman, Alain Pierre, Bruno Pfeiffer, Pierre Renard
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Patent number: 6630466Abstract: The present invention relates to new medicament compositions based on anticholinergic compounds, which have a long-lasting effect, and salmeterol, processes for their production and their use in the therapy of respiratory ailments.Type: GrantFiled: February 14, 2002Date of Patent: October 7, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Karl-Heinz Bozung, Michel Pairet, Richard Reichl, Alexander Walland
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Patent number: 6593323Abstract: A benzimidazole compound or a salt thereof which has an inhibitory action of forming of macrophages and is useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of arteriosclerosis, which is represented by the formula (I): wherein, R1 represents a functional group on the benzene ring selected from the group consisting of hydrogen atom, a halogen atom, a lower alkyl group and a lower alkoxy group; R2 represents hydrogen atom, an alkyl group or an acyl group; R3 represents a functional group on the ring containing the nitrogen atom and Z; Z represents a divalent group which forms a 5- or 6-membered ring; L represents a C4-C8 alkylene group or an ethyleneoxy linking group represented by (CH2CH2O)nCH2CH2 wherein n represents 1 or 2; and X represents O or S.Type: GrantFiled: June 3, 2002Date of Patent: July 15, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Aoki, Kazuhiro Aikawa, Masayuki Kawakami
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Patent number: 6525046Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: GrantFiled: June 7, 2002Date of Patent: February 25, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Roger Dinallo, John Robinson Regan, Paul S. Riska, Alan David Swinamer, Zhulin Tan, Brian Andrew Walter
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Patent number: 6503919Abstract: A compound selected from those of formula (I): wherein: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted amino, R3 and R4 represent hydrogen, or alkyl, R5 and R6 represent —O—CO—U—V wherein U and V are as defined in the description, or Z as defined in the description, it being understood that at least one of the R5 and R6 groups represents —O—CO—U—V, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.Type: GrantFiled: June 15, 2000Date of Patent: January 7, 2003Assignee: Les Laboratoires ServerInventors: Michel Koch, François Tillequin, Sylvie Michel, Ghanem Atassi, Alain Pierre, Pierre Renard, Bruno Pfeiffer
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Patent number: 6455524Abstract: The present invention relates to new medicament compositions based on anticholinergic compounds, which have a long-lasting effect, and &bgr;-mimetics, which have a long-lasting effect, processes for their production and their use in the therapy of respiratory ailments.Type: GrantFiled: May 9, 2000Date of Patent: September 24, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Karl-Heinz Bozung, Michel Pairet, Richard Reichl, Alexander Walland
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Patent number: 6410528Abstract: Compounds of formula (I) and pharmaceutically acceptable salts and or metabolically labile derivatives thereof, wherein R1 represents C1-6 straight or branched chain alkyl, C1-6 straight or branched chain alkoxy, optionally substituted phenoxy, C3-6straight or branched chain alkenyloxy or C1-4 straight or branched alkoxy substituted by an optionally substituted phenyl group. C3-6 straight or branched chain alkenyl, optionally substituted phenyl, optionally substituted C3-7 cycloalkyl, C2-4 straight or branched chain alkyl substituted by (C1-4 alkoxy, C1-4 alkyl thio or halogen), C1-4 straight or branched chain alkyl substituted by (C1-4 alkoxycarbonyl, aryloxycarbonyl, cyano, optionally substituted C3-7 cycloalkyl, optionally substituted 5 or 6 membered heteroaryl, or 1 or 2 optionally substituted phenyl groups), a process for their preparation and their use in medicine.Type: GrantFiled: November 8, 2000Date of Patent: June 25, 2002Assignee: Glaxo Wellcome S.A.Inventors: Jose M. Bueno, Jesus Chicharro Gonzalo, Jose-Miguel Coteron, Juan Carlos Cuevas, Jose M. Fiandor, Araceli Mallo
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Patent number: 6403580Abstract: Quinazolines of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation thereof.Type: GrantFiled: August 23, 2001Date of Patent: June 11, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
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Patent number: 6380182Abstract: The invention relates to a method to inhibit bacteria from adhering to a submergible surface. The method contacts the submergible surface with an effective amount of at least one sulfamic acid or salt thereof to inhibit bacterial adhesion to the submergible surface. The invention also relates to a method for controlling biofouling of an aqueous system. This method adds an effective amount of at least one sulfamic acid or salt thereof to inhibit bacteria from adhering to a submerged surface within the aqueous system. This method effectively controls biofouling without substantially killing the fouling organisms. The sulfamic acid used in the method of the invention has the formula R1R2NS(O)2(OH). In this formula, R1 and R2 are independently a hydrogen, a C4-C20 alkyl group or a cyclohexyl group. However, R1 and R 2 are not both hydrogen.Type: GrantFiled: June 12, 2000Date of Patent: April 30, 2002Inventors: Thomas E. McNeel, Marilyn S. Whittemore, Stephen D. Bryant, Graciela H. Vunk
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Patent number: 6329369Abstract: Methods of treating glaucoma or elevated pressure and other diseases with reduced side effects by treating a mammal in need thereof an agonist of the alpha 2B or alpha 2B/2C adrenergic receptor(s). Also described are compounds having such selective agonist activity.Type: GrantFiled: October 5, 2000Date of Patent: December 11, 2001Assignee: Allergan Sales, Inc.Inventors: Ken Chow, Daniel W. Gil, James A. Burke, Dale A. Harcourt, Michael E. Garst, Larry A. Wheeler, Stephen A. Munk
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Patent number: 6300342Abstract: Antithrombotic phenylalkyl derivatives of the formula Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphonamido)-1,2,3,4-tetrahydro-quinoline, (b) 1-[3-(4-amidino-phenyl)propionyl]-6-butylsulphonamido-1,2,3,4-tetrahydro-quinoline, (c) 1-[3-(4-amidino-phenyl)propionyl]-5-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, (d) 1-[3-(4-amidino-phenyl)propionyl]-3-methyl-6-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, and, (e) 1-[3-(4-amidino-phenyl)propionyl]-6-(5-chloro-thien-2-ylsulphonamido)-1,2,3,4-tetrahydro-quinoline.Type: GrantFiled: December 9, 1999Date of Patent: October 9, 2001Assignee: Boehringer Ingelheim Pharm KGInventors: Armin Heckel, Rainer Soyka, Wolfgang Grell, Eric Haaksma, Klaus Binder, Rainer Zimmerman
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Patent number: 6288073Abstract: A compound selected from those of formula (I): in which: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted ammo, R3 and R4 represent hydrogen, or alkyl, A represents —CH═CH—, or —CH(R5)—CH(R6)— wherein R5 and R6 are as defined in the description, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.Type: GrantFiled: June 19, 2000Date of Patent: September 11, 2001Assignee: Adir et CompagnieInventors: Michel Koch, François Tillequin, Sylvie Michel, Ghanem Atassi, Alain Pierre, Bruno Pfeiffer, Pierre Renard
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Patent number: 6265402Abstract: A 2-phenylmorpholin-5-one derivative having the formula (I): wherein R1 represents a C1 to C8 alkyl group, a C3 to C7 cycloalkyl group or an indanyl group, R2 represents a C1 to C4 alkyl group, R3 represents a hydrogen atom, a C1 to C5 alkyl group, etc., R4 represents a hydrogen atom, a C1 to C6 alkyl group, etc., R5, R6 represent a hydrogen atom, a C1 to C5 alkyl group, etc., an optical isomer thereof or a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof and a pharmaceutical composition containing the same. The above compound has a strong type IV phosphodiesterase (PDE) inhibitory activity and has bronchodilater and antiinflammatory effects.Type: GrantFiled: February 25, 1999Date of Patent: July 24, 2001Assignee: Nikken Chemicals Co., Ltd.Inventors: Shinji Ina, Kenjirou Yamana, Kyoji Noda
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Patent number: 6180624Abstract: This invention relates to methods and compositions for treating pain and nociception in a patient by administering a combination of a morpholine or thiomorpholine tachykinin antagonist and an opioid analgesic.Type: GrantFiled: February 25, 1999Date of Patent: January 30, 2001Assignee: Merck Sharp & Dohme LimitedInventor: Raymond George Hill
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Patent number: 6177564Abstract: The present invention is concerned with a novel process for the preparation of N-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one of the formula: This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.Type: GrantFiled: September 9, 1999Date of Patent: January 23, 2001Assignee: Merck & Co., Inc.Inventors: Todd D. Nelson, Mahadevan Bhupathy