Nitrogen Containing Patents (Class 514/459)
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Publication number: 20040209824Abstract: Anticonvulsant derivatives useful for preventing the development of Type II diabetes mellitus and Syndrome X are disclosed.Type: ApplicationFiled: May 11, 2004Publication date: October 21, 2004Inventors: Carlos Plata-Salaman, Jeffrey Crooke
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Patent number: 6762178Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.Type: GrantFiled: June 14, 2001Date of Patent: July 13, 2004Assignee: Wyeth Holdings CorporationInventors: Jeremy I. Levin, James M. Chen
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Patent number: 6762183Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.Type: GrantFiled: October 7, 2002Date of Patent: July 13, 2004Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Christoph Erdelen, Thomas Bretschneider
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Patent number: 6740649Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NR1, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), aggrecanase or a combination thereof, pharmaceutical compositions containing the same, and methods of using the same.Type: GrantFiled: September 16, 2002Date of Patent: May 25, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Gregory R. Ott, Xiao-Tao Chen, Jingwu Duan, Zhonghui Lu
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Publication number: 20040097499Abstract: The present invention provides certain amide, carbamate and urea derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: ApplicationFiled: July 3, 2003Publication date: May 20, 2004Inventors: MacKlin Brian Arnold, David Michael Bender, Thomas John Bleisch, Winton Dennis Jones, Paul Leslie Ornstein, Hamid H. Zarrinmayeh, Dennis Michael Zimmerman
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Publication number: 20040087513Abstract: The invention relates to new drug combinations based on sodium channel blockers 1 and magnesium salts 2, processes for the preparation thereof as well as the use thereof for preparing pharmaceutical compositions for the treatment of ischaemic conditions.Type: ApplicationFiled: July 2, 2003Publication date: May 6, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Judith Duettmann, Thomas Weiser
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Patent number: 6730783Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: April 22, 2003Date of Patent: May 4, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
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Publication number: 20040082519Abstract: A method for treating snoring, sleep apnoea and other forms of sleep disordered breathing comprises administration to a patient of a therapeutically effective amount of topiramate over an appropriate period of time, such as a period substantially coniciding with the sleep period of a patient. A useful route of administration is per os. Also disclosed is the use of topiramate for the diagnosis of snoring, sleep apnoea and other forms of sleep disordered breathing.Type: ApplicationFiled: December 12, 2003Publication date: April 29, 2004Inventors: Jan Hedner, Kars Sjstrm, Kaj Stenlf, Ludger Grote
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Patent number: 6716881Abstract: The present invention provides carbanilides of formula (I), wherein A, Q, R, X, Z and m are as defined herein. A plurality of processes for preparing these compounds is provided, along with methods of using the compounds to control microorganisms in crops and in the protection of materials. The compounds of the present invention also find use in controlling animal pests.Type: GrantFiled: May 30, 2002Date of Patent: April 6, 2004Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Bernd-Wieland Krüger, Robert Markert, Ralf Tiemann, Dietmar Kuhnt, Stefan Dutzmann, Klaus Stenzel, Christoph Erdelen, Martin Kugler, Hans-Ulrich Buschhaus
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Publication number: 20040058853Abstract: The invention relates to a multimeric compound or a pharmaceutically acceptable salt or derivative thereof which comprises three or more neuraminidase-binding groups attached to a spacer or linking group, in which the neuraminidase-binding group is a compound which binds to the active site of influenza virus neuraminidase, but is not cleaved by the neuraminidase. The invention also relates to processes for the preparation of the multimeric compound defined above, pharmaceutical compositions containing them or methods for the treatment and/or prophylaxis of a viral infection involving them.Type: ApplicationFiled: October 14, 2003Publication date: March 25, 2004Inventors: Wen-Yang Wu, Michael Dennis Dowle, Betty Jin, Simon John Fawcett Macdonald, Andrew McMurtrie Mason, Darryl McConnell, Keith Watson
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Publication number: 20040058880Abstract: This invention relates to novel aminoglycoside compounds having antibacterial and anti-infective activity and to pharmaceutical compositions, methods of making and methods of treatment employing the same.Type: ApplicationFiled: June 26, 2003Publication date: March 25, 2004Inventors: Chang-Hsing Liang, Kenneth Marby, David Rabuka, Alex Romero, Paul W. M. Sgarbi, Steven J. Sucheck, Youe-Kong Shue, Sulan Yao
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Publication number: 20040048815Abstract: The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or quanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates.Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.Type: ApplicationFiled: August 18, 2003Publication date: March 11, 2004Inventors: Dieter Herr, Helmut Mack, Werner Seitz, Wilfried Hornberger
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Patent number: 6703425Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disordersType: GrantFiled: November 15, 2002Date of Patent: March 9, 2004Assignee: Eli Lilly and CompanyInventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6699840Abstract: The invention encompasses novel salts of topiramate, and pharmaceutically acceptable polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, or amorphous forms thereof, as well as pharmaceutical compositions and pharmaceutical unit dosage forms containing the same. In particular, the invention encompasses pharmaceutically acceptable salts of topiramate, including without limitation topiramate sodium, topiramate lithium, topiramate potassium, or polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, and amorphous forms thereof. The invention further encompasses novel co-crystals or complexes of topiramate, as well as pharmaceutical compositions comprising them. The invention also encompasses methods of treating or preventing a variety of diseases and conditions including, but not limited to, seizures, epileptic conditions, tremors, cerebral function disorders, obesity, neuropathic pain, affective disorders, tobacco cessation, migraines, and cluster headache.Type: GrantFiled: November 18, 2002Date of Patent: March 2, 2004Assignee: Transform Pharmaceuticals, Inc.Inventors: Örn Almarsson, Julius F. Remenar, Matthew L. Peterson
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Publication number: 20040038911Abstract: The present invention is directed to novel compounds of the formula (I) 1Type: ApplicationFiled: May 8, 2003Publication date: February 26, 2004Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff, Steven Mehrman, Kirk Sorgi, Frank Villani, Cheryl Kordik, Allen B. Reitz, Bruce Maryanoff
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Patent number: 6696442Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl-82-; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: June 25, 2002Date of Patent: February 24, 2004Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana, Victor I. Ilyin
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Publication number: 20040033988Abstract: Compounds of the formula: 1Type: ApplicationFiled: February 27, 2003Publication date: February 19, 2004Applicant: WyethInventors: Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
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Publication number: 20040033965Abstract: The present invention relates, in general, to obesity, and, in particular, to a method of treating obesity and minimizing metabolic risk factors associated therewith using, for example, zonisamide or other weight-loss promoting anticonvulsant either alone or in combination with bupropion or other compound that enhances the activity of norepinephrine and/or dopamine via uptake inhibition or other mechanism.Type: ApplicationFiled: May 19, 2003Publication date: February 19, 2004Inventors: Kishore M. Gadde, K. Ranga R. Krishnan
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Publication number: 20040029955Abstract: The present invention relates to a composition for use in prevention or treatment of a vascular-related disease, particularly used for angiogenesis inhibition, tumor growth inhibition or tumor metastasis inhibition, or immunostimulation, which comprises glutamic acid or derivatives thereof, preferably glutamic acid is anhydrous glutamic acid represented by Formula (1) or pyroglutamic acid, and a pharmaceutically acceptable carrier or an edible carrier, and a method of preventing or treating a vascular-related disease.Type: ApplicationFiled: May 15, 2003Publication date: February 12, 2004Inventors: Takashi Kouge, Akihiro Yamashita, Keno Ishihara
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Publication number: 20040024024Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.Type: ApplicationFiled: November 12, 2002Publication date: February 5, 2004Inventors: John N. Freskos, Y vette M. Fobian, Alok K. Awasthi, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Nizal S. Chandrakumar, Gary A. DeCrescenzo, Bipin N. Desai, Marcia I. Heron, Susan L. Hockerman, Sara M. Jull, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Patrick B. Mullins, Monica B. Norton, Joseph G. Rico, John J. Talley, Mahima Trivedi, Clara I. Villamil, Lijuan Jane Wang
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Publication number: 20040019083Abstract: The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: 1Type: ApplicationFiled: June 25, 2003Publication date: January 29, 2004Applicant: Sloan-Kettering Institute for Cancer ResearchInventors: William G. Bornmann, Francis Sirotnak, Howard Scher, Ephraim Vidal, Christopher Borelle, David Scheinberg
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Patent number: 6680340Abstract: This invention provides a drug combination comprised of a thyroid hormone receptor beta agonist with a fibrate in therapeutically effective amounts, which is useful for reducing cholesterol synthesis, lowering plasma cholesterol levels and lowering plasma triglyceride levels.Type: GrantFiled: February 13, 2003Date of Patent: January 20, 2004Assignee: Merck & Co., Inc.Inventors: Kang Cheng, Samuel D. Wright, Tsuei-Ju Wu
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Patent number: 6680054Abstract: The invention provides novel macromolecules, methods for their preparation, pharmaceutical formulations thereof and their use as anti-influenza agents. The invention also provides a novel diagnostic method which can be used for detection of all types of influenza A and B virus. The macromolecular compound of the invention has attached to it one or more molecules (neuraminidase binders) which bind to the active site of influenza virus neuraminidase but which are not cleaved by the neuraminidase.Type: GrantFiled: July 16, 1999Date of Patent: January 20, 2004Assignee: Biota Scientific Management PTY Ltd.Inventors: Phillip A. Reece, Keith Geoffrey Watson, Wen-Yang Wu, Betty Jin, Guy Y. Krippner
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Patent number: 6677355Abstract: Compounds of the formula; are useful for inhibiting matrix metalloproteinase enzymes in animals, and as such, prevent and treat diseases resulting from the breakdown of connective tissues. Also disclosed are methods for the preparation of such compounds, pharmaceutical compositions including the same, and methods of treating diseases in which matrix metalloproteinases are involved including multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurysm, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, osteoporosis, rheumatoid or osteoarthritis, renal disease, left ventricular dilation, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: February 13, 2002Date of Patent: January 13, 2004Assignee: Warner-Lambert CompanyInventors: Christopher Alan Conrad, Patrick Michael O'Brien, Daniel Fred Ortwine, Joseph Armand Picard, Drago Robert Sliskovic
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Patent number: 6673965Abstract: A compound of formula (I) wherein: R isopropyl; n is 0; R1 is naphthylmethyl; R2 is t-butyl; and R3 is methyl; is useful in the treatment of disorders mediated by s-CD23.Type: GrantFiled: July 16, 2002Date of Patent: January 6, 2004Assignee: SmithKline Beecham P.L.C.Inventors: John Gerard Ward, Andrew Faller
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Publication number: 20030236200Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.Type: ApplicationFiled: March 20, 2003Publication date: December 25, 2003Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat
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Patent number: 6664259Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: September 6, 2002Date of Patent: December 16, 2003Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Qi Jin
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Publication number: 20030229122Abstract: The present invention makes available methods and reagents for facilitating LTP, e.g., to increase memory function such as long-term memory and recall ability.Type: ApplicationFiled: February 25, 2003Publication date: December 11, 2003Applicant: Sention, Inc.Inventors: Kjesten A. Wiig, Mel H. Epstein
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Publication number: 20030225133Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: ApplicationFiled: March 28, 2003Publication date: December 4, 2003Inventor: Aloke A Dutta
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Publication number: 20030225002Abstract: The present invention describes a method for the treatment and/or prevention of migraine and associated symptoms (nausea, vomiting, photophobia, phonophobia, etc.) comprising co-therapy with a therapeutically effective amount of one or more anti-migraine agents and one or more anticonvulsant derivatives.Type: ApplicationFiled: February 25, 2003Publication date: December 4, 2003Inventor: Ian R. Livingstone
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Patent number: 6653321Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: July 28, 2000Date of Patent: November 25, 2003Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
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Patent number: 6645998Abstract: The present invention provides an antiproliferative compound having the structural formula wherein X is oxygen, nitrogen or sulfur; R1 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carboxylic acid, carboxylate, carboxamide, ester, thioamide, thiolacid, thiolester, saccharide, alkoxy-linked saccharide, amine, sulfonate, sulfate, phosphate, alcohol, ethers and nitriles; R2 is hydrogen, methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide and amine; R3 is selected from the group consisting of hydrogen, methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide and amine; R4 is of methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide and amine; and R5 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carboxyl, amide and ester. Also provided is a method for inducing apoptosis in a cell comprising administering a composition comprising a compound.Type: GrantFiled: April 12, 2002Date of Patent: November 11, 2003Assignee: Research Development FoundationInventors: Bob G. Sanders, Kimberly Kline, Laurence Hurley, Robb Gardner, Marla Menchaca, Weiping Yu, Puthucode N. Ramanan, Shenquan Liu, Karen Israel
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Patent number: 6638947Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: December 6, 2001Date of Patent: October 28, 2003Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, John F. W. Keana
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Patent number: 6638931Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 28, 2000Date of Patent: October 28, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Patent number: 6635634Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: October 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 6627653Abstract: Anticonvulsant derivatives useful for treating depression as monotherapy or combination therapy are disclosed.Type: GrantFiled: July 27, 2001Date of Patent: September 30, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Carlos R. Plata-Salaman, Josue Bacaltchuk, Pedro A. S. Prado-Lima
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Patent number: 6624190Abstract: The invention concerns compounds of formula (I) wherein: A represents R1 or (O)R1 where R1 represents an alkyl group comprising 1 to 30 carbon atoms, linear or branched, saturated or unsaturated, capable of being partly or totally substituted by Hal where Hal represents —Cl,—Br, or —F, and of being interrupted by one or several units selected among —O—,—S—,—C(O)—,—NR3C(O)—, —Ph(R4)n— and —CH2—CH2—O)n′—, wherein R3 represents or —CH2)n″—CH where n″=0 to 17; R4 represents, —CH3,—CH2H5,—C3H7 and n=0 to 4 and n′=1, 2, or 3, or R1 represents a cyclanic radical with diterpene or triterpene root; and R2 represents a C1−C11 linear or branched alkyl group.Type: GrantFiled: May 17, 2001Date of Patent: September 23, 2003Assignee: Universite Pierre et Marie Curie (Paris VI)Inventors: Chadi Khoury, Michel Minier, Francois Le Goffic
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Patent number: 6620819Abstract: The anticonvulsant derivative topiramate useful in treating dementia and/or behavioral and psychotic disturbances in dementia is disclosed.Type: GrantFiled: May 13, 2002Date of Patent: September 16, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventor: David B. Marcotte
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Publication number: 20030171425Abstract: The present invention related to novel dihydropyrones possessing 3-position nitrogen atom, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.Type: ApplicationFiled: October 16, 2002Publication date: September 11, 2003Inventors: Frederick Earl Boyer, John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Elizabeth Ann Lunney, Alexander Pavlovsky, Vara Prasad Venkata Nagendra Josyula, Bradley Dean Tait
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Publication number: 20030171300Abstract: The present invention concerns the use of compounds of the Formula (I) for treating different types and symptoms of acute and chronic pain, especially non neuropathic inflammatory pain in mammals. The pain to be treated may be e.g. chronic inflammatory pain, rheumatoid arthritis pain and/or secondary inflammatory osteoarthritic pain. The compounds show an antinociceptive profile and differ from classical analgesics like opioids and non-steroidal anti-inflammatory drugs (NSAIDS) and are useful as specific analgesics.Type: ApplicationFiled: February 11, 2003Publication date: September 11, 2003Inventor: Norma Selve
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Patent number: 6613803Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: October 21, 1999Date of Patent: September 2, 2003Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana, Victor I. Ilyin, Eckard Weber
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Patent number: 6608104Abstract: A compound of the formula wherein R1-R13, X, Z and Q are as defined above, useful in the treatment of arthritis, cancer, and other diseases involving the dysregulated production/release of reprolysins such as Aggrecanase and other diseases characterized by matrix metalloproteinase activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID's), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.Type: GrantFiled: March 27, 2001Date of Patent: August 19, 2003Assignee: Pfizer IncInventor: Mark C. Noe
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Patent number: 6602879Abstract: The present invention relates to novel Pyrrole-Type compounds, compositions comprising Pyrrole-Type compounds, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a composition comprising a Pyrrole-Type compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for treating or preventing a viral infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the replication and/or infectivity of a virus.Type: GrantFiled: April 4, 2002Date of Patent: August 5, 2003Assignee: Gemin X Biotechnologies Inc.Inventors: Madiraju S. R. Murthy, Nancy A. E. Steenaart, Roy A. Johnson, Gordon C. Shore
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Publication number: 20030144322Abstract: The invention provides a compound of formula (I): 1Type: ApplicationFiled: October 23, 2002Publication date: July 31, 2003Inventors: Alan P. Kozikowski, Gian Luca Araldi
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Publication number: 20030144347Abstract: The present invention is directed to a method for treating autoimmune diseases comprising administering a therapeutically effective amount of a compound of the following formula (I) 1Type: ApplicationFiled: November 14, 2002Publication date: July 31, 2003Inventor: Ralph Ryback
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Patent number: 6596759Abstract: A medicament for preventive and/or therapeutic treatment of irritable bowel syndrome which comprises as an active ingredient a substance selected from the group consisting of an alkylenedioxybenzene derivative represented by the following general formula (I) and a pharmaceutically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein m represents an integer of from 2 to 5, and n represents an integer of from 1 to 3 (e.g., 5-[3-[(2S)-(1,4-benzodioxan-2-ylmethyl)amino]propoxy]-1,3-benzodioxol).Type: GrantFiled: December 20, 2001Date of Patent: July 22, 2003Assignee: Mitsubishi Chemical CorporationInventors: Michikazu Abe, Ken-Ichi Saito
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Publication number: 20030134859Abstract: A compound of the following formula or a pharmacologically acceptable salt thereof: 1Type: ApplicationFiled: October 23, 2002Publication date: July 17, 2003Applicant: SANKYO COMPANY, LIMITEDInventors: Yoshiya Amemiya, Kenji Wakabayashi, Sachiko Takaishi, Chie Fukuda
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Publication number: 20030119791Abstract: The present invention relates to pharmacologically active compounds which are capable of binding to nuclear hormone receptors and are useful for the stimulation of osteoblast proliferation and ultimately bone growth. This invention also relates to the use of such compounds for the treatment or prevention of diseases and/or disorders associated with nuclear hormone receptor families.Type: ApplicationFiled: March 27, 2002Publication date: June 26, 2003Inventors: Sean M. Kerwin, Laurence H. Hurley, Mark R. DeLuca, Bob M. Moore, Gregory R. Mundy
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Patent number: 6583179Abstract: The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.Type: GrantFiled: December 21, 2000Date of Patent: June 24, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Steven J. Coats, Louis J. Fitzpatrick, Dennis J. Hlasta, Carolina L. Lanter, Mark J. Macielag, Ke Pan, Ralph A. Rivero, Stephen S. Palmer
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Patent number: 6583172Abstract: Anticonvulsant derivatives useful in treating chronic neurodegenerative conditions are disclosed.Type: GrantFiled: March 30, 2000Date of Patent: June 24, 2003Inventor: Richard P. Shank