Nitrogen Double Bonded Directly At 2-position Of The Diazole Ring, Or Tautomeric Equivalent Patents (Class 514/388)
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Publication number: 20100280087Abstract: This invention relates to novel 2-amino benzimidazole derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: July 8, 2010Publication date: November 4, 2010Inventors: Ulrik Svane Sørensen, Lene Teuber, Dan Peters, Dorte Strøbæk, Tina Holm Johansen, Karin Sandager Nielsen, Palle Christophersen
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Patent number: 7763643Abstract: The present invention comprises compounds and compositions comprising substituted thiophene derivatives with the following backbone structure: The compounds of this type are of useful in the treatment of various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.Type: GrantFiled: January 30, 2009Date of Patent: July 27, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Hans-Jochen Lang, Uwe Heinelt, Armin Hofmeister, Klaus Wirth, Michael Gekle, Markus Bleich
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Patent number: 7741493Abstract: The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.Type: GrantFiled: November 29, 2007Date of Patent: June 22, 2010Assignee: Aventis Pharmaceuticals Inc.Inventors: Patrick Shum, Alexandre Gross, Liang Ma, Daniel G. McGarry, Gregory H. Merriman, David Rampe, Garth Ringheim, Jeffrey Stephen Sabol, Francis A. Volz
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Publication number: 20100150840Abstract: Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.Type: ApplicationFiled: June 4, 2009Publication date: June 17, 2010Inventor: Masashi Yanagisawa
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Patent number: 7714009Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): wherein, ring A is a 5-membered ring represented by the formula (A?): wherein X is a carbon and X1 is an oxygen, a sulfur or —NR5—, or formula (A?): wherein X is a nitrogen and R6 is an optionally substituted hydrocarbyl, R1 is an amino substituted by two optionally substituted hydrocarbyl groups, R2 is an phenyl, Y1 is CR3a or a nitrogen, Y2 is CR3b or a nitrogen and Y3 is CR3c or a nitrogen, provided that one or less of Y1, Y2, and Y3 is nitrogen, W is a bond, —(CH2)n-, and Z is a bond, —NR4—, etc.; or a salt thereof or a prodrug thereof.Type: GrantFiled: October 27, 2004Date of Patent: May 11, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Albert Charles Gyorkos, Christopher Peter Corrette, Suk Young Cho, Timothy Mark Turner, Scott Alan Pratt, Kazuyoshi Aso, Masakuni Kori, Michiyo Gyoten
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Patent number: 7601745Abstract: The present invention relates to compounds of the general formula (III) or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof, wherein R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4?OR5?, NH2, amine, alkylamine, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; R4 is H, halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hyodroxyalkylamino, alkylamino, heteroaryl, or aryl; R5 is halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hydroxyalkylamino, alkylamino, heteroaryl, or aryl.Type: GrantFiled: March 15, 2006Date of Patent: October 13, 2009Assignee: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Patent number: 7541477Abstract: This invention relates to a benzimidazole derivative of the general formula [I] [wherein B1, B2, and B3 represent hydrogen atom or lower alkyl; R1 and R2 are same or different and represent lower alkyl, etc.; R3 and R4 represent hydrogen atom, etc.; W represents a 3 to 8-membered aromatic or alphatic heterocycle, etc.; and Ar represents a substituted or unsubstituted aromatic heterocycle, etc.] This compound functions as an antagonist to melanin-concentrating hormone receptor and is useful as a drug for central diseases, circulatory diseases and metabolic diseases.Type: GrantFiled: July 29, 2003Date of Patent: June 2, 2009Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Minoru Moriya, Akio Kanatani, Hisashi Iwaasa, Akane Ishihara, Takehiro Fukami
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Patent number: 7528259Abstract: Taught herein are new derivatives of 4,5,6,7-tetrabromobenzimidazole of Formula 1 wherein R1 is a hydrogen or an aliphatic group, and R2 is an aliphatic group, optionally substituted with a hydrogen or a substituent such as a hydroxyl group or substituted amino group, and a method of their preparation.Type: GrantFiled: March 29, 2005Date of Patent: May 5, 2009Assignee: Selvita SP. Z O. O.Inventors: Zygmunt Kazimierczuk, Lorenzo A. Pinna, Flavio Meggio, Mariola Andrzejewska
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Publication number: 20090099208Abstract: This invention relates to novel guanidine derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: March 22, 2007Publication date: April 16, 2009Inventors: Ulrik Svane Sorensen, Birgitte L. Eriksen, Lene Teuber, Dan Peters, Dorte Strobaek, Tina Holm Johansen, Palle Christophersen
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Patent number: 7488746Abstract: Substituted thiophenes, processes for their preparation, their use as medicament or diagnostic agent. The substituted thiophene derivatives have the following backbone structure: Medicaments comprising compounds of this type are of use for preventing or treating various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.Type: GrantFiled: September 28, 2007Date of Patent: February 10, 2009Assignee: sanofi-aventis Deutschland GmbHInventors: Hans-Jochen Lang, Uwe Heinelt, Armin Hofmeister, Klaus Wirth, Michael Gekle, Markus Bleich
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Publication number: 20090022729Abstract: The present invention provides methods and pharmaceutical compositions for treating or preventing cardiac dysfunctions (e.g., cardiac hypertrophy, cardiac remodeling, or heart failure) in subjects who have or are likely to develop cardiomyopathies. Some of the methods are directed to therapeutic or prophylactic treatment of cardiac dysfunctions in subjects having undergone myocardial injuries such as cardiac ischemia/reperfusion or myocardial infarction. Typically, these methods comprising administering to the subjects a therapeutic composition comprising a compound which can specifically inhibit PAR1 mediated signaling or down-regulate the cellular level of PAR1.Type: ApplicationFiled: April 11, 2008Publication date: January 22, 2009Inventors: Nigel Mackman, Rafal Pawlinski, Burns C. Blaxall
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Patent number: 7468440Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.Type: GrantFiled: May 14, 2007Date of Patent: December 23, 2008Assignee: Bristol-Myers Squibb CompanyInventor: Percy Carter
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Publication number: 20080275098Abstract: The present invention comprises novel substituted 2-aminoimidazoles of formula I, processes for their preparation, pharmaceutical compositions thereof, and methods for their use in the treatment of disorders of the central nervous system, cardiovascular disorders, stroke and pulmonary disorders, urinary disorders such as acute or chronic renal failure, disorders of biliary function, respiratory disorders such as snoring or sleep apnea. wherein the substitutents R1-R8 are further defined herein.Type: ApplicationFiled: July 14, 2008Publication date: November 6, 2008Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Uwe HEINELT, Hans-Jochen LANG, Armin HOFMEISTER, Klaus WIRTH, Hans-Willi JANSEN
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Publication number: 20080249153Abstract: This invention relates to the preparation of veterinary anthelmintic formulations including triclabendazole in solution, particularly for the treatment of parasitic infections such as fasciolisis, and particularly for administration to an animal in the form of a pour-on. The solutions may include triclabendazole dissolved in a solvent system including at least one solvent selected from 2-pyrrolidone and liquid polyethylene glycol. Additional solvents may also be included. The present invention is advantageous as triclabendazole can be included in solution up to a concentration of about 60% w/v allowing for an effective dose to be delivered to the animal in a volume of 25 ml or less.Type: ApplicationFiled: March 14, 2008Publication date: October 9, 2008Inventor: Majid Hameed Abdul Razzak
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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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Patent number: 7423015Abstract: The present invention is directed to the use of benzimidazole derivatives for the treatment of tumors and in combination with tumor suppressor gene therapy. In a particular embodiment, treatment of p53-positive tumors with benzimidazole derivatives induces p53 expression and increases its half-life, resulting in apoptotic death of the tumor cells. Similarly, in conjunction with p53 gene therapy, benzimidazole derivatives induce p53 expression and accumulation in tumor cells regardless of their p53 status. The combination treatment subsequently elicits apoptosis of the tumor cells.Type: GrantFiled: January 9, 2002Date of Patent: September 9, 2008Assignees: Board of Regents, The University of Texas System, Introgen Therapeutics, Inc.Inventors: Tapas Mukhopadhyay, Sunil Chada, Abner Mhashilkar, Jack A. Roth
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Publication number: 20080166378Abstract: Methods of identifying death receptor sensitizing compounds and methods of using death receptor sensitizing compounds are provided.Type: ApplicationFiled: January 11, 2007Publication date: July 10, 2008Inventors: Aaron D. Schimmer, John C. Reed
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Patent number: 7371773Abstract: The invention provides a drug which inhibits BCRP. A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1): [wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (—NHCOCH3 group); a cyano group (—CN group); a formyl group (—CHO group), —COOR1 (R1 is hydrogen or C1-C4 alkyl), —O(CH2)nCOOR2 (n=1?7: R2 is hydrogen or C1-C4 alkyl), —OOCCH2CH2COOR3 (R3 is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., —OP(O) (OH)2) or a salt thereof, a sulfate group (i.e.Type: GrantFiled: February 3, 2004Date of Patent: May 13, 2008Assignee: Kabushiki Kaisha Yakult HonshaInventors: Ryuta Yamazaki, Yukiko Nishiyama, Tomio Furuta, Takeshi Matsuzaki, Hiroshi Hatano, Oh Yoshida, Masato Nagaoka, Ritsuo Aiyama, Shusuke Hashimoto, Yoshikazu Sugimoto
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Patent number: 7317033Abstract: Substituted thiophenes, processes for their preparation, their use as medicament or diagnostic agent. The substituted thiophene derivatives have the following backbone structure: Medicaments comprising compounds of this type are of use for preventing or treating various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.Type: GrantFiled: March 21, 2006Date of Patent: January 8, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Hans-Jochen Lang, Uwe Heinelt, Armin Hofmeister, Klaus Wirth, Michael Gekle, Markus Bleich
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Patent number: 7304084Abstract: 6-[(4,5-Dihydro-1H-imidazol-2-yl)amino-]-7-methyl-1H-benzimidazole-4-carbonitrile substantially free of 2,3,7-triamino-4,6-dimethyl-1,9-phenazinedicarbonitrile, and the anhydrous monoacetate salt thereof, are useful in the treatment of alpha-2 mediated disorders such as ocular hypertension.Type: GrantFiled: January 17, 2006Date of Patent: December 4, 2007Assignee: The Board of Regents of the University of NebraskaInventors: Jared Lynn Randall, Richard Alan Gibbs, Gregory Kent Bosch, Michael David Curtis, Li Sun, Nicholas Nikolaides
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Patent number: 7238813Abstract: Benzimidazole derivatives, which are useful as TIE-2 and/or VEGFR2 inhibitors are described herein. The described invention also includes methods of making such benzimidazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.Type: GrantFiled: November 28, 2001Date of Patent: July 3, 2007Assignee: Smithkline Beecham CorporationInventors: Mui Cheung, Philip Anthony Harris, Masaichi Hasegawa, Satoru Ida, Kazuya Kano, Naohiko Nishigaki, Hideyuki Sato, James Marvin Veal, Yoshiaki Washio, Rob I. West
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Patent number: 7235576Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: GrantFiled: January 11, 2002Date of Patent: June 26, 2007Assignee: Bayer Pharmaceuticals CorporationInventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
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Patent number: 7179829Abstract: The invention relates to novel compounds of the type of the imidazolidines of the formula I in which R1 to R7 are as defined in the claims. They are used for preparing a medicament for the treatment or prophylaxis of the central nervous system, of lipid metabolism, of infection by ectoparasites, of disorders of gall function and for improving the respiratory drive and are therefore used for treating respiratory distress. Additionally, the compounds increase the muscle tone of the upper respiratory tract, thus suppressing snoring.Type: GrantFiled: July 16, 2004Date of Patent: February 20, 2007Assignee: Sanofi-aventis Deutschland GmbHInventors: Uwe Heinelt, Hans-Jochen Lang, Armin Hofmeister, Klaus Wirth
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Patent number: 7179830Abstract: Substituted thienoimidazoles with a backbone structure of formula I or II: These substituted thienoimidazoles are useful in prevention or treatment of various disorders, including respiratory disorders.Type: GrantFiled: August 25, 2004Date of Patent: February 20, 2007Assignee: Sanofi-aventis Deutschland GmbHInventors: Hans-Jochen Lang, Uwe Heinelt, Klaus Wirth, Thomas Licher
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Patent number: 7153840Abstract: This invention is directed towards a ready-to-use aqueous composition of fludarabine phosphate. In one embodiment, the invention is directed to an aqueous fludarabine phosphate composition which comprises fludarabine phosphate, a base, and water. The concentration of fludarabine phosphate in the composition may be between about 0.5 mg/mL and about 50 mg/mL. The pH of the composition may be between about 5.5 and about 7.1.Type: GrantFiled: May 23, 2003Date of Patent: December 26, 2006Assignee: Sicor, Inc.Inventors: Dorla Mirejovsky, Peter Lindsay Macdonald
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Patent number: 7141594Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: November 19, 2003Date of Patent: November 28, 2006Assignee: G. D. Searle & Co.Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L. Brown, Joseph J. McDonald
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Patent number: 7138420Abstract: Disclosed are substituted benzimidazole compounds of formula (I): wherein R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.Type: GrantFiled: August 1, 2003Date of Patent: November 21, 2006Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Joerg Martin Bentzien, Brian Nicholas Cook, Charles Cywin, Roman Wolfgang Fleck, Ho Yin Lo, Peter Allen Nemoto, Steven S. Pullen, Gregory Paul Roth, Roger John Snow, Hidenori Takahashi, Ji Wang, Kevin J. Moriarty, Lei Qiao, Michael Winters
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Patent number: 7132438Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, immune response regulation and cell proliferation. The subject compounds are 2-amino-imidazole derivatives.Type: GrantFiled: October 9, 2002Date of Patent: November 7, 2006Assignee: Amgen Inc.Inventors: Alexander David Frenkel, Sarah Elizabeth Lively, Jay P. Powers, Andrew Smith, Daqing Sun, Craig Tomooka, Zhulun Wang
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Patent number: 7105550Abstract: This invention concerns the use of a compound of formula (I?) a N-oxide, pharmaceutically acceptable addition salt, quaternary amine and stereochemically isomeric form thereof, wherein Q is optionally substituted C3-6cycloalkyl, phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl; or Q is a radical of formula wherein X and Y each independently are O, NR3, CH2 or S, with R3 being hydrogen or C1-4alkyl; q is 1 to 4; Z is O or NR4 with R4 being hydrogen or C1-4alkyl; r is 1 to 3; L is optionally substituted phenyl or L is Het with Het being an optionally substituted five- or six-membered heterocyclic ring or an optionally substituted bicyclic heterocyclic ring; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through cytokines.Type: GrantFiled: February 20, 2001Date of Patent: September 12, 2006Inventors: Christopher Love, Jean Pierre Frans Van Wauwe, Marc De Brabander, Ludwig Cooymans, Nele Vandermaesen, Ludo Edmond Josephine Kennis
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Patent number: 7094911Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.Type: GrantFiled: October 31, 2002Date of Patent: August 22, 2006Assignee: Bayer AktiengesellschaftInventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Patent number: 7081469Abstract: Vascular damaging agents composed of substituted 5(6)-substituted benzimidazole-2-carbamates are provided. These agents are useful in the preparation of medicaments for the treatment of diseases involving neovascularisation, particularly for the treatment of solid tumors, macular degeneration, diabetic retinopathy, rheumatoid arthritis, psoriasis, and atherosclerosis. Embodiments include a 5(6)-substituted benzimidazole-2-carbamate of formula I wherein A represents a multi-substituted alkyl group or aromatic ring.Type: GrantFiled: July 3, 2003Date of Patent: July 25, 2006Assignee: Angiogene Pharmaceuticals Ltd.Inventor: Peter David Davis
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Patent number: 7049333Abstract: Substituted thiophenes, processes for their preparation, their use as medicament or diagnostic agent. The substituted thiophene derivatives have the following backbone structure: Medicaments comprising compounds of this type are of use for preventing or treating various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.Type: GrantFiled: May 30, 2003Date of Patent: May 23, 2006Assignee: Sanofi-aventis Deutschland GmbHInventors: Hans-Jochen Lang, Uwe Heinelt, Armin Hofmeister, Klaus Wirth, Michael Gekle, Markus Bleich
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Patent number: 7041668Abstract: The present invention discloses and claims benzimidazole compounds of formula (I): in which A is aryl or heteroaryl; R1 is selected from optionally substituted alkyl, alkoxy, aryl or heteroaryl, NH-lower alkyl or NH-cycloalkyl, or halogen, NH2; 1-imidazolyl or SO2Me; R2 is selected from optionally substituted —CO-alkyl, —CO-cycloalkyl, —CO-aralkyl, —CO-aryl, —CO-alkoxy, aryl or aralkyl, or —CO-amino, CO—NHR3 or CO—R3R4 wherein R3 and R4 are selecteded independently from hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, fluoroalkyl, alkynyl, heteroalkyl, alkylheteroalkyl, aryl, aralkyl or together form an alkylene chain optionally containing one to 4 heteroatoms; a pharmaceutically acceptable salt or a prodrug thereof; the use of compounds of formula (I) for the treatment of cancer, and pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents.Type: GrantFiled: March 25, 2004Date of Patent: May 9, 2006Assignee: Aventis Pharma S.A.Inventors: Francois Clerc, Francois Hamy, Isabelle Depaty, Odile Angouillant-Boniface, Stéphanie Deprets, Chantal Carrez, Manfred Roesner
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Patent number: 6984654Abstract: A pharmaceutical composition that inhibits the growth of tumors and cancers in mammals and can be used to treat viral infections that comprises a fungicide is disclosed. The particular fungicide used is a benzimidazole derivative having the formula: wherein R is selected from the group consisting of H, carboxyl (—CO2H), hydroxyl, amino or esters (—CO2R?) wherein R? is selected from the group consisting of alkoxy, haloalkyl, alkenyl, and cycloalkyl wherein the alkyl groups have from 1–8 carbons or CH3CH2(OCH2CH2)n— or CH3CH2CH2(OCH2CH2CH2)n— or (CH3)2CH—(OCH(CH3)CH2)n— wherein n is from 1–3, the pharmaceutically acceptable salts thereof, or mixtures thereof.Type: GrantFiled: January 13, 2003Date of Patent: January 10, 2006Assignee: UAF Technologies and Research, LLCInventor: James Berger Camden
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Patent number: 6974823Abstract: The present invention relates generally to novel hydantoin derivative compounds, pharmaceutical compositions containing such compounds, and methods for their use in preventing and/or treating neurological disorders, including physically damaged nerves and neurodegenerative diseases; for treating alopecia and promoting hair growth; for treating vision disorders and/or improving vision; for treating memory impairment and/or enhancing memory performance; and for treating sensorineural hearing loss by administering such compounds.Type: GrantFiled: December 21, 2000Date of Patent: December 13, 2005Assignee: GPI NIL Holdindgs, Inc.Inventor: Gregory S. Hamilton
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Patent number: 6930121Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: October 8, 2002Date of Patent: August 16, 2005Assignee: UAF Technologies and Research, LLCInventors: James Berger Camden, James C. Quada, Jr., Joseph K. Agyin
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Patent number: 6927211Abstract: Compositions and methods are provided for use in the treatment of cancer.Type: GrantFiled: December 4, 2003Date of Patent: August 9, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Giorgio Minotti, Luca Gianni
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Patent number: 6924271Abstract: The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.Type: GrantFiled: November 27, 2002Date of Patent: August 2, 2005Assignee: Anadys Pharmaceuticals, Inc.Inventors: Devron R. Averett, Stephen E. Webber, Joseph R. Lennox, Erik J. Rueden
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Patent number: 6916836Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: August 5, 2003Date of Patent: July 12, 2005Assignee: UAF Technologies and Research, LLCInventors: James Berger Camden, James C. Quada, Jr., Joseph K. Agyin
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Patent number: 6906091Abstract: Methods of treating and inhibiting cancer in animals by administering a therapeutically effective amount of a pharmaceutical composition having benzimidazole of the general formula: wherein X is hydrogen, halogen, alkyl of less than 7 carbon atoms or alkoxy of less than 7 carbon atoms; n is a positive integer of less than 4; Y is hydrogen, chlorine, oxychloro, nitro, methyl or ethyl; and R is hydrogen, or an alkyl group of from 1 to 8 carbon atoms and R2 is NHCOOR1 wherein R1 is aliphatic hydrocarbon of less than 7 carbon atoms, and preferably an alkyl group of less than 7 carbon atoms and pharmaceutically acceptable derivatives alone, or in combination, or in conduction with other therapeutic agents such as other cancer inhibiting compounds, and operative combinations thereof.Type: GrantFiled: July 18, 2002Date of Patent: June 14, 2005Assignee: UAF Technologies and Research, LLCInventor: James Berger Camden
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Patent number: 6864275Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: September 29, 2000Date of Patent: March 8, 2005Assignee: UAF Technologies and Research, LLCInventors: James Berger Camden, James Clarence Quada, Jr., Joseph K. Agyin
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Patent number: 6858607Abstract: The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I: or pharmaceutically acceptable salts or prodrugs thereof, wherein: wherein A, R1, R2, R5, X, Y, and Z, are defined herein and B is a fused thiazole, oxazole, 2-imino-imidazole, 2,1,3-thiadiazo-2-one, thiazol-2-one, oxazol-2-one, imidazol-2-thione, thiazol-2-thione, oxazol-2-thione, imidazoline, oxazoline, thiazoline, triazole, oxazine, oxazine-2,3-dione, or piperazine ring. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: May 16, 2002Date of Patent: February 22, 2005Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Lifen Xu, Richard Storer, Giorgio Attardo
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Patent number: 6849634Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: December 7, 2001Date of Patent: February 1, 2005Assignee: ICAgenInventors: Serge Beaudoin, Aimee D. Reed, Michael F. Gross
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Patent number: 6825219Abstract: Disclosed are substituted benzimidazole compounds of formula(I): wherein R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention are useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.Type: GrantFiled: November 5, 2002Date of Patent: November 30, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles Cywin, Jinbo Lee, Steven S. Pullen, Gregory Paul Roth, Christopher Ronald Sarko, Roger John Snow, Noel Stewart Wilson
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Publication number: 20040127507Abstract: Disclosed are novel compounds and a method of treating inflammatory diseases.Type: ApplicationFiled: December 9, 2003Publication date: July 1, 2004Applicants: Millennium Pharmaceuticals, Inc., Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Hiroki Sone, Osamu Kotera, Jay R. Luly, Gregory J. LaRosa
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Patent number: 6720349Abstract: Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: April 25, 2002Date of Patent: April 13, 2004Assignee: UAF Technologies and Research, LLCInventors: James C. Quada, Jr., Joseph K. Agyin, James Berger Camden
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Patent number: 6693125Abstract: The invention features a method for treating a patient having a cancer or other neoplasm, by administering to the patient (i) a benzimidazole or a metabolite or analog thereof; and (ii) pentamidine or a metabolite or analog thereof simultaneously or within 14 days of each other in amounts sufficient to inhibit the growth of the neoplasm.Type: GrantFiled: January 24, 2001Date of Patent: February 17, 2004Assignee: CombinatoRx IncorporatedInventors: Alexis Borisy, Curtis Keith, Michael A. Foley, Brent R. Stockwell
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Patent number: 6673822Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: April 12, 2002Date of Patent: January 6, 2004Assignee: G.D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6653335Abstract: This invention is a method of treating cancer, both carcinomas and sarcomas, and viral infections, in particular HIV through the administration of a pharmaceutical composition containing a benzimidazole derivative. The composition is also claimed. The benzimidazole derivative is selected from the group consisting of: wherein X is hydrogen, halogen, alkyl of less than 7 carbon atoms or alkoxy of less than 7 carbon atoms; n is a positive integer of less than 4; Y is hydrogen, chlorine, nitro, methyl, ethyl or oxychloro; R is hydrogen, alkylaminocarbonyl wherein the alkyl group has from 3 to 6 carbon atoms, or an alkyl group of from 1 to 8 carbon atoms and R2 is 4-thiazolyl, NHCOOR1 wherein R1 is aliphatic hydrocarbon of less than 7 carbon atoms, prodrugs, pharmaceutically acceptable salts and mixtures thereof and a pharmaceutically acceptable carrier.Type: GrantFiled: November 6, 2002Date of Patent: November 25, 2003Assignee: University of Arizona FoundationaInventor: James Berger Camden
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Patent number: 6645950Abstract: Vascular damaging agents composed of substituted 5(6)-substituted benzimidazole-2-carbamates are provided. These agents are useful in the preparation of medicaments for the treatment of diseases involving neovascularisation, particularly for the treatment of solid tumors, macular degeneration, diabetic retinopathy, rheumatoid arthritis, psoriasis, and atherosclerosis. Embodiments include a 5(6)-substituted benzimidazole-2-carbamate of formula I wherein A represents a multi-substituted alkyl group or aromatic ring.Type: GrantFiled: October 22, 2001Date of Patent: November 11, 2003Assignee: Angiogene Pharmaceuticals Ltd.Inventor: Peter David Davis