Additional Nitrogen Containing Hetero Ring Attached Directly Or Indirectly To The Seven-membered Hetero Ring By Nonionic Bonding Patents (Class 514/211.15)
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Publication number: 20090203666Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: ApplicationFiled: May 4, 2007Publication date: August 13, 2009Applicant: IRM LLCInventors: Wenqi Gao, Jiqing Jiang, Yongqin Wan, Dai Cheng, Dong Han, Xu Wu, Shifeng Pan
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Publication number: 20090197866Abstract: The disclosure relates to compounds of formula (I): wherein R1, R2, R3, R4, and R5 are as defined in the disclosure, to the compositions containing them and to the use thereof as medicaments, in particular as anticancer agents. The disclosure also relates to the process for preparing the compounds of formula (I) and to reaction intermediates.Type: ApplicationFiled: December 18, 2008Publication date: August 6, 2009Applicant: AVENTIS PHARMA S.A.Inventors: Marie-Pierre CHERRIER, Eric PARMANTIER, Herve MINOUX, Francois CLERC, Odile ANGOUILLANT-BONIFACE, Maurice BROLLO, Laurent SCHIO
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Publication number: 20090185975Abstract: The invention provides a probe compound useful for early diagnosis of conformation disease, a composition and a kit comprising it for diagnosis for conformation disease, and a medical composition for treatment and/or prevention of conformation disease.Type: ApplicationFiled: December 25, 2006Publication date: July 23, 2009Applicant: TOHOKU UNIVERSITYInventors: Yukitsuka Kudo, Hiroyuki Arai, Nobuyuki Okamura, Masahiro Maruyama, Syozo Furumoto, Katsumi Doh-Ura
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Publication number: 20090186870Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: October 9, 2008Publication date: July 23, 2009Applicant: AstraZeneca ABInventors: Jack McQueen ALLEN, Roger John Butlin, Clive Green, William McCoull, Graeme Richard Robb, James Matthew Wood
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Publication number: 20090156571Abstract: The present invention discloses novel compounds of Formula I: possessing 11 ?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 ?-HSD type 1 activity.Type: ApplicationFiled: April 19, 2007Publication date: June 18, 2009Inventors: Thomas Daniel Aicher, Zhaogen Chen, Ronald Jay Hinklin, Gary Alan Hite, Alexei Pavlovych Krasutsky, Renhua Li, Jefferson Ray McCowan, Ashraf Saeed, Nancy June Snyder, James Lee Toth, Owen Brendan Wallace, Leonard Larry Winneroski, Jr., Yanping Xu, Jeremy Schulenburg York
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Publication number: 20090143358Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.Type: ApplicationFiled: March 20, 2008Publication date: June 4, 2009Applicants: ICAgen, Inc., Pfizer LimitedInventors: Brian Edward Marron, Paul Christopher Fritch, Christopher John Markworth, Andrew Thomas Maynard, Nigel Alan Swain
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Publication number: 20090143357Abstract: Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division, also are disclosed.Type: ApplicationFiled: March 29, 2006Publication date: June 4, 2009Applicant: ICOS CORPORATIONInventors: Frank Diaz, Francine S. Farouz, Ryan Coatsworth Holcomb, Edward A. Kesicki, Hua Chee Ooi, Alexander Rudolph, Frank Stappenbeck, Eugene D. Thorsett, John Joseph Gaudino, Kimba Lee Fischer, Adam Wade Cook
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Publication number: 20090137553Abstract: The present invention relates to a new class of oxazolidinone derivatives, to their use as antibacterial agents, to pharmaceutical compositions containing these compounds and to methods for their preparation.Type: ApplicationFiled: November 17, 2005Publication date: May 28, 2009Applicants: Pharmacia and Upjohn Company LLCInventors: Charles Francis Donovan, Vara Prasad Venkata Nagendra Josyula, Manjinder Singh Lall, Adam Robert Renslo
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Publication number: 20090124596Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.Type: ApplicationFiled: January 10, 2008Publication date: May 14, 2009Inventors: Roger Victor Bonnert, Frank Burkamp, Rhona Jane Cox, Simon De Sousa, Mark Dickinson, Simon Fraser Hunt, Premji Meghani, Austen Pimm, Hitesh Jayantilal Sanganee
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Publication number: 20090105217Abstract: Novel oxadiazole derivatives of formula (I) having pharmacological activity, processes for their preparation, compositions containing them and their use in the treatment of neurological, psychiatric disorders and gastrointestinal disorders through modulation of the nicotinic ?7 receptor.Type: ApplicationFiled: May 29, 2007Publication date: April 23, 2009Inventors: Frank Teen Coppo, Emma S.L. Maskell, Sally Redshaw, John Skidmore, Robert William Ward, David Matthew Wilson
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Publication number: 20090105215Abstract: The compounds of the present invention are of formula I: wherein A, R3, R4 is as defined herein, are useful as ligands for nicotinic receptors.Type: ApplicationFiled: April 6, 2007Publication date: April 23, 2009Inventors: Brian Herbert, Wenge Xie, Truc Minh Nguyen, Allen T. Hopper, Ashok Tehim
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Publication number: 20090105216Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2, R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: April 23, 2007Publication date: April 23, 2009Inventors: Matthias Treu, Andreas Mantoulidis, Ulrike Tontsch-Grunt
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Publication number: 20090093455Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.Type: ApplicationFiled: October 3, 2008Publication date: April 9, 2009Inventors: Johnny Yasuo NAGASAWA, Fabrice PIERRE, Mustapha HADDACH, Michael SCHWAEBE, Levan DARJANIA, Jeffrey P. WHITTEN
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Publication number: 20090054352Abstract: Problem: To provide compounds which have an anticoagulation effect based on their ability to inhibit the activated blood coagulation factor X and are useful as coagulation inhibitors or agents for prevention or treatment for diseases caused by thrombi or emboli. Means for Solution: Benzene derivatives or their salts having a characteristic chemical structure with a phenol ring and a benzene ring bonding to each other via an amide bond, in which the phenol ring further bonds to a benzene ring or a heteroaryl ring via an amide bond. They have an excellent effect of inhibiting the activated blood coagulation factor X, and especially have an excellent oral activity.Type: ApplicationFiled: November 7, 2006Publication date: February 26, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Fukushi Hirayama, Jiro Fujiyasu, Daisuke Kaga, Kenji Negoro, Daisuke Sasuga, Norio Seki, Ken-ichi Suzuki
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Publication number: 20080287419Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.Type: ApplicationFiled: May 15, 2008Publication date: November 20, 2008Applicant: Abbott LaboratoriesInventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Publication number: 20080280881Abstract: The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle Q is R7, pyrrolidinyl substituted with R7, piperidinyl substituted with R7 or homopiperidinyl substituted with R7; one of R2a and R3a is selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b), N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or —C(=Z)Ar2; and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen, C1-6alkyl or halogen and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen,Type: ApplicationFiled: June 17, 2008Publication date: November 13, 2008Inventors: Jean-Francois Bonfanti, Koenraad Josef Lodewijk Andries, Jerome Michel Claude Fortin, Philippe Muller, Frederic Marc Maurice Doublet, Christophe Meyer, Rudy Edmond Willebrords, Tom Valerius Josepha Gevers, Philip Maria Martha Born Timmerman
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Publication number: 20080254040Abstract: The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.Type: ApplicationFiled: June 17, 2008Publication date: October 16, 2008Applicant: Boehringer Ingelheim International GmbHInventors: Martin Friedrich STEFANIC, Frank HILBERG, Gerd MUNZERT, Flavio SOLCA, Anke BAUM, Jacobus C.A. van MEEL
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Patent number: 7407950Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. Said compounds are ligands of the TRPV1 vanilloid receptor, and are therefore, useful for treating diseases associated with TRPV1 receptors, such as pain and inflammation.Type: GrantFiled: June 20, 2007Date of Patent: August 5, 2008Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
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Patent number: 7390799Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.Type: GrantFiled: May 12, 2006Date of Patent: June 24, 2008Assignee: Abbott LaboratoriesInventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Publication number: 20080146536Abstract: The invention relates to 2-aminoimidazopyridine derivatives useful in treating disorders that are mediated by A2a receptor function, including neurodegenerative diseases including Parkinson's disease and inflammation.Type: ApplicationFiled: August 16, 2006Publication date: June 19, 2008Applicant: Pharmacopeia, Inc.Inventors: Andrew G. Cole, Brian F. McGuinness, Marc-Raleigh Brescia, Yuefei Shao, Guizhen Dong, Ian Henderson
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Publication number: 20080146539Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: December 19, 2007Publication date: June 19, 2008Applicant: Boehringer Ingelheim International GmbHInventors: Henning PRIEPKE, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
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Publication number: 20080146542Abstract: The present invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles of formula (I): wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and their use for the treatment of pathological conditions, in particular as anticancer agents.Type: ApplicationFiled: August 29, 2007Publication date: June 19, 2008Applicant: Aventis Pharma S.A.Inventors: Claude BARBERIS, Jean-Christophe CARRY, Gilles DOERFLINGER, Dominique BARBALAT-DAMOUR, Francois CLERC, Herve MINOUX
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Patent number: 7378413Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C6,10 aryl group which may be substituted.Type: GrantFiled: January 13, 2005Date of Patent: May 27, 2008Assignees: Sanofi Aventis, Mitsubishi Pharma CorporationInventors: Antonio Almario Carcia, Ryoichi Ando, Keiichi Arimoto, Fumiaki Uehara, Adrien Tak Li, Aya Shoda, Jonathan Reid Frost, Kazutoshi Watanabe
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Patent number: 7351700Abstract: The present invention relates to compounds of formula wherein X is —S— or —NH—; R3/R4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7 membered ring, which optionally contains in addition to the N-atom one additional heteroatom selected from the group consisting of O, S and N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, —NR2, —CONR2, —CO-lower alkyl or benzyl; or R3/R4 form together with the N-atom to which they are attached a heterocyclic ring system, containing two or three rings and which optionally contains one or two additional heteroatoms selected from the group consisting of N and O and which has no more than 20 carbon atoms; and R, R1, R2, and R5 are as defined herein and to pharmaceutically suitable acid addition salts thereof.Type: GrantFiled: February 23, 2005Date of Patent: April 1, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Pari Malherbe, Raffaello Masciadri, Eric Prinssen, Will Spooren, Andrew William Thomas
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Patent number: 7329652Abstract: The present invention relates to inhibitors of protein kinases, particularly to inhibitors of JAK2 and JAK3. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: September 19, 2005Date of Patent: February 12, 2008Assignee: Vertex Pharamaceuticals IncorporatedInventors: Francesco Salituro, Mark Ledeboer, Brian Ledford, Jian Wang, Albert Pierce, John Duffy, David Messersmith
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Publication number: 20070287694Abstract: The invention encompasses compounds as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: May 31, 2007Publication date: December 13, 2007Inventors: Kap-Sun Yeung, Katharine A. Grant-Young, Min Ding, Robert G. Gentles, John F. Kadow
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Publication number: 20070275947Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: May 24, 2007Publication date: November 29, 2007Inventor: Carl P. Bergstrom
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Publication number: 20070219183Abstract: The present invention relates to dihydropyrazolo[1,5-a]pyrimidine and dihydroimidazo[1,5-a]pyrimidine derivatives, compositions comprising an effective amount of a dihydropyrazolo[1,5-a]pyrimidine or a dihydroimidazo[1,5-a]pyrimidine derivative and methods for treating or preventing cancer, comprising administering to a subject in need thereof an effective amount of a dihydropyrazolo[1,5-a]pyrimidine or a dihydroimidazo[1,5-a]pyrimidine derivative.Type: ApplicationFiled: March 15, 2007Publication date: September 20, 2007Applicant: WyethInventors: Jeremy Ian Levin, Zhong Li, Dennis Powell
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Patent number: 7244722Abstract: Compounds of the general formula (I): wherein m, n, R1, R2, R3 and R4 are as described in the specification. Further included are pharmaceutical compositions comprising the compounds, processes for their preparation, as well as the use of the compounds for the preparation of a medicament for the treatment of 5-HT2A receptor-related disorders or medical conditions.Type: GrantFiled: July 17, 2003Date of Patent: July 17, 2007Assignee: Biovitrum ABInventors: Magnus Cernerud, Helena Lundström, Björn M Nilsson, Markus Thor
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Patent number: 7241745Abstract: The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.Type: GrantFiled: August 5, 2002Date of Patent: July 10, 2007Assignee: Astellas Pharma GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Löser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt
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Patent number: 7229983Abstract: The present invention relates to novel, low molecular weight broad spectrum compounds in particular to a class of 4-substituted or unsubstituted-7-hydro-1,4-thiazepine-7-[bicyclic or tricyclic heteroaryl] substituted-3,6-dicarboxylic acid or their derivatives which have ?-lactamase inhibitory and antibacterial properties. The compounds are therefore useful in the treatment of antibacterial infections in humans or animals, either alone or in combination with other antibiotics.Type: GrantFiled: April 28, 2004Date of Patent: June 12, 2007Assignee: Wyeth Holdings CorporationInventors: Tarek Suhayl Mansour, Aranapakam Mudumbai Venkatesan
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Patent number: 7223749Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb, Rc, Rd, Re and X are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases and benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.Type: GrantFiled: February 13, 2004Date of Patent: May 29, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Flavio Solca
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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: 7208487Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: December 12, 2003Date of Patent: April 24, 2007Assignee: Cytokinetics, IncorporatedInventors: Gustave Bergnes, Dashyant Dhanak, Steven David Knight, Pu Ping Lu, David J. Morgans, Jr., Kenneth Allen Newlander
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Patent number: 7199117Abstract: The invention features pharmaceutically-active imidazopyridines and derivatives that are substituted with phenyl, methods of making them, and methods of using them.Type: GrantFiled: October 7, 2004Date of Patent: April 3, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: J. Guy Breitenbucher, Nicholas I. Carruthers, Xiaobing Li, Laura C. McAtee, Chandravadan R. Shah, Ronald L. Wolin
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Patent number: 7119084Abstract: The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to a patient in need thereof of a therapeutically effective amount of a bicyclic heterocyclic groups of general formula wherein said substituents are as defined herein.Type: GrantFiled: March 17, 2005Date of Patent: October 10, 2006Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Birgit Jung, Flavio Solca
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Patent number: 7081454Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inhibiting tyrosine kinase enzymes.Type: GrantFiled: October 2, 2002Date of Patent: July 25, 2006Assignee: Bristol-Myers Squibb Co.Inventors: Mark D. Wittman, Neelakantan Balasubramanian, Upender Velaparthi, Kurt Zimmermann, Mark G. Saulnier, Peiying Liu, Xiaopeng Sang, David B. Frennesson, Karen M. Stoffan, James G. Tarrant, Anne Marinier, Stephan Roy
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Patent number: 7030150Abstract: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.Type: GrantFiled: May 9, 2002Date of Patent: April 18, 2006Assignee: Trimeris, Inc.Inventors: John William Lackey, Daniel S Kinder, Nicolai A Tvermoes
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Patent number: 7030110Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the 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. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: October 4, 2002Date of Patent: April 18, 2006Assignee: Ortho-McNeil Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Patent number: 6974870Abstract: Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the I?B kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.Type: GrantFiled: December 6, 2003Date of Patent: December 13, 2005Assignee: Boehringer Ingelheim Phamaceuticals, Inc.Inventors: Charles L. Cywin, Can Mao, Jonathan Emeigh, Roman Wolfgang Fleck, Ming-Hong Hao, Eugene Hickey, Weimin Liu, Daniel Richard Marshall, Tina Morwick, Peter Nemoto, Ronald John Sorcek, Sanxing Sun, Jiang-Ping Wu, Erick Young, Darren DiSalvo, John Ginn, Pier Cirillo
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Patent number: 6964956Abstract: Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the I?B kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.Type: GrantFiled: June 3, 2003Date of Patent: November 15, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Zhidong Chen, Roman Wolfgang Fleck, Ming-Hong Hao, Eugene Hickey, Weimin Liu, Daniel Richard Marshall, Peter Nemoto, Ronald John Sorcek, Sanxing Sun, Jiang-Ping Wu, Tina Morwick, Jonathan Emeigh
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Patent number: 6960575Abstract: A compound having 3-oxo-3, 4-dihydro-2H-1, 4-thiazine 4-tetrahydropyrazine as a main skeleton. The compound is a chymase inhibitor and is represented by the following formula [I] and salts thereof: In the formula [I], X is S; R1 and R2 are H, alkyl, cycloalkyl or aryl; R3 and R4 are H, alkyl, cycloalkyl, aryl or an aromatic heterocycle; R5 is H, alkyl, cycloalkyl, aryl or -A3-A4-R7; R6 is H, alkyl, cycloalkyl, hydroxy, alkoxy, aryl, aryloxy or an aromatic heterocycle; R7 is H, alkyl, hydroxy, alkoxy, aryl, aryloxy, amino, alkylamino, arylamino, an aromatic heterocycle or a nonaromatic heterocycle; A1 is alkylene; A2 is carbonyl or sulfonyl; A3 is alkylene; A4 is carbonyl or oxalyl; and n is 0 or 1.Type: GrantFiled: November 13, 2003Date of Patent: November 1, 2005Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kazuo Nishimura, Masakazu Ban, Ken-ichi Fujimura, Naoyuki Kobayashi, Masanori Hori, Takahiro Honda, Eiko Matsumoto, Junzo Matsumoto
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Patent number: 6919359Abstract: The invention provides compounds of Formula I: Azabicyclo-N(R1)—C(?X)—W??Formula I These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which ?7 is known to be involved.Type: GrantFiled: November 6, 2002Date of Patent: July 19, 2005Assignee: Pfizer IncInventors: David W. Piotrowski, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, Alice L. Bodnar, Vincent E. Groppi, Jr., Daniel Patrick Walker, Brad A. Acker
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Patent number: 6906057Abstract: Methods for modulating the activity of the mammalian FXR receptor. The methods include methods of treating a hyper- or hypocholesterolemic mammal comprising contacting the mammal with synthetic compounds having FXR receptor activity.Type: GrantFiled: June 9, 2000Date of Patent: June 14, 2005Assignees: Allergan, Inc., City of Hope National Medical CenterInventors: Barry M. Forman, Richard L. Beard, Roshantha A. Chandraratna
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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: 6861419Abstract: The present invention is directed to substituted 1,4-thiazepine and analogs thereof, represented by the general Formula I: wherein the dashed lines, A1, A2, A3, X1 and R1 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of capases 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: April 18, 2001Date of Patent: March 1, 2005Assignee: Cytovia, Inc.Inventors: John A. Drewe, Sui Xiong Cai, Emma Jane Shelton, Joane Litvak, David Sperandio, Jeffrey R. Spencer, Martin Sendzik
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Patent number: 6844335Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C6,10 aryl group which may be substituted.Type: GrantFiled: March 22, 2001Date of Patent: January 18, 2005Assignees: Sanofi-Synthelabo, Mitsubishi Pharma CorporationInventors: Antonio Almario Garcia, Ryoichi Ando, Keiichi Arimoto, Fumiaki Uehara, Adrien Tak Li, Aya Shoda, Jonathan Reid Frost, Kazutoshi Watanabe
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Publication number: 20040214812Abstract: The present invention relates to novel, low molecular weight broad spectrum compounds in particular to a class of 4-substituted or unsubstituted-7-hydro-1,4-thiazepine-7-[bicyclic or tricyclic heteroaryl] substituted-3,6-dicarboxylic acid or their derivatives which have &bgr;-lactamase inhibitory and antibacterial properties. The compounds are therefore useful in the treatment of antibacterial infections in humans or animals, either alone or in combination with other antibiotics.Type: ApplicationFiled: April 28, 2004Publication date: October 28, 2004Applicant: Wyeth Holdings CorporationInventors: Tarek Suhayl Mansour, Aranapakam Mudumbai Venkatesan
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Patent number: RE39112Abstract: The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is —CH2CH2—, or —CH?CH— or —C?C—; R1 is: (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.; and R5 and R6 are the same as or different from each other and each represents hydrogen atom, a lower alkyl group, a cycloalkyl group, etc.) and the like; R2 is an amino group, etc.Type: GrantFiled: December 24, 1998Date of Patent: May 30, 2006Assignee: Eisai Co., Ltd.Inventors: Osamu Asano, Hitoshi Harada, Yorihisa Hoshino, Seiji Yoshikawa, Takashi Inoue, Tatsuo Horizoe, Nobuyuki Yasuda, Kaya Ohashi, Junsaku Nagaoka, Manabu Murakami, Seiichi Kobayashi