Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
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Publication number: 20120065200Abstract: Compounds are disclosed for the treatment, management and prevention of diseases and disorders affecting the bone. Particular compounds are potent inhibitors of Notum Pectinacetylesterase, and are of the formula: wherein E, G, Y, Z, R1, R2, and R3 are defined herein.Type: ApplicationFiled: September 13, 2011Publication date: March 15, 2012Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Wei HE, Victoria LOMBARDO, Praveen PABBA, James TARVER, JR.
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Publication number: 20120065217Abstract: Phycotoxins are purified from a mixture of phycotoxins produced in a continuous process. Cyanobacteria are produced in a continuous culture, then lyzed, the cells pelleted and extracted, and the extract purified using an organic solvent-aqueous mixture and repeated passage through a diatomaceous earth column. The column is washed with acetic acid, then the neosaxitoxin extracted with an alcohol-water mixture. The eluate is passed through activated charcoal columns, which are washed with distilled water to remove the retained pigments and impurities, the further purified by HPLC. In one embodiment, the process produces only neosaxitoxin and saxitoxin. In another embodiment, the process produces only GTX2/3.Type: ApplicationFiled: September 23, 2011Publication date: March 15, 2012Applicant: PROTEUS S.A.Inventor: Marcelo Santiago Lagos González
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Patent number: 8129398Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: March 18, 2009Date of Patent: March 6, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Francis Beaulieu, Carl Ouellet, B. Narasimhulu Naidu, Manoj Patel, Yasutsugu Ueda, Timothy P. Connolly, Jonathan R. Weiss, Michael A. Walker, Nicholas A. Meanwell, Kevin M. Peese, Margaret E. Sorenson, Chen Li
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Publication number: 20120046282Abstract: The present invention provides Wall Teichoic Acid biosynthesis inhibitors such as compound 1835F03 (targocil) and related synthetic analogs. The invention also provides pharmaceutical compositions thereof and methods for treating bacterial infection and the suppression of growth of bacterial cells by administering a Wall Teichoic Acid biosynthesis inhibitor. The invention is particularly useful for the treatment of Methicillin-resistant Staphylococcus aureus (MRSA). The invention further provides procedures for the syntheses of Wall Teichoic Acid biosynthesis inhibitors. The invention also provides methods for the identification of antibacterial therapeutic agents.Type: ApplicationFiled: June 5, 2009Publication date: February 23, 2012Applicant: President and Fellows of Harvard CollegeInventors: Suzanne Walker Kahne, Jonathan G. Swoboda, Timothy C. Meredith, Kyungae Lee, Jennifer Campbell
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Patent number: 8119647Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: GrantFiled: April 9, 2009Date of Patent: February 21, 2012Assignee: Glenmark Pharmaceuticals S.A.Inventors: Prasada Rao V. S. Lingam, Sachin Sundarlal Chaudhari, Abraham Thomas, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20120040966Abstract: The compounds provided herein are suitable for inhibiting a virus in a patient and for treating a patient suffering from a viral infection such as an influenza virus. Also provided is a method for screening of compounds for use in treating and preventing viral infections. The assay screens compounds for activity against an influenza virus by measuring the cytopathogenic effect (CPE) of the compound on influenza infected-cells using percent cell viability as the end point.Type: ApplicationFiled: December 28, 2009Publication date: February 16, 2012Applicant: Southern Research Institute Office of Commercialization and Intellectual PropInventors: Joseph A. Maddry, Bill Severson, Colleen B. Jonsson, James W. Noah, Diana L. Noah, Xi Chen
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Publication number: 20120039913Abstract: The invention relates to Histamine H4 receptor antagonists or inhibitors of Histamine H4 receptor gene expression for the treatment and/or the prevention of vestibular disorders.Type: ApplicationFiled: December 23, 2009Publication date: February 16, 2012Applicant: INSERM (institut National de la Sante de la Recher Medicale)Inventors: Gilles Desmadryl, Christian Chabbert
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Publication number: 20120041007Abstract: The present invention relates to novel crystalline form(s) of water-soluble salts and of free base of a cdk inhibitor. Such crystal salts are for example fumarate, L-malate, maleate, succinate, adipate, malonate, glycolate, phosphate, mesylate, L-lactate, hydrochloride, di-hydrochloride, tri-hydrochloride. Hydrates and polymorphs of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application.Type: ApplicationFiled: April 23, 2010Publication date: February 16, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Massimo Zampieri, Annalisa Airoldi, Maria Gioia Fornaretto, Maria Gabriella Brasca
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Publication number: 20120034296Abstract: Compositions containing site 1 sodium channel blockers for use as local anesthetics with rapid nerve block, improved potency and efficacy, and no local toxicity have been developed. Liposomes were employed for increased loading of the site 1 sodium channel blocker, producing prolonged duration of block without systemic toxicity. In one embodiment, the compositions contain a site 1 sodium channel blocker alone. In another embodiment, the compositions contain a site 1 sodium channel blocker in combination with a corticosteroid. As demonstrated by the examples, encapsulating site 1 sodium channel blockers in liposomes results in rapid and prolonged nerve block without systemic toxicity, which is enhanced by the addition of a corticosteroid. Fluid liposomes showed more rapid release of STX than did solid ones, and dexamethasone accelerated STX release.Type: ApplicationFiled: April 6, 2010Publication date: February 9, 2012Inventors: Hila Epstein-Barash, Daniel S. Kohane
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Publication number: 20120035172Abstract: The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.Type: ApplicationFiled: October 17, 2011Publication date: February 9, 2012Applicant: INCYTE CORPORATIONInventors: Changsheng Zheng, Chu-Biao Xue, Ganfeng Cao, Michael Xia, Anlai Wang, Hai Fen Ye, Brian Metcalf
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Publication number: 20120022045Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X1, X2, ?3, Y, Z, R1, R2 and R3 are defined herein. The N compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: January 25, 2010Publication date: January 26, 2012Inventors: Shankar Venkatraman, John S. Wai, Wayne Thompson, Boyoung Kim, Richard C.A. Isaacs, H. Marie Loughran, Dai-Shi Su, John Lim, Mark W. Embrey, Peter D. Williams
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Patent number: 8093254Abstract: Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4, R14, V, W, X, Y, Z, p, and ring A are as described in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: December 10, 2007Date of Patent: January 10, 2012Assignee: Schering CorporationInventors: Zhaoning Zhu, Andrew Stamford, Mihirbaran Mandal, Xiaoxiang Liu
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Publication number: 20120004250Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z are as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors, such as, for example, inflammation.Type: ApplicationFiled: September 19, 2011Publication date: January 5, 2012Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa, Patrick Allison
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Publication number: 20120004240Abstract: The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: March 3, 2010Publication date: January 5, 2012Inventors: Weiming Fan, Thomas F.N. Haxell, Matthew G. Jenks, Nobuhiko Kawanishi, Shuliang Lee, Hao Liu, Michael J. Malaska, Joseph A. Moore, III, Yoshio Ogino, Yu Onozaki, Bharathi Pandi, Michael R. Peel, Toshihiro Sakamoto, Tony Siu
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Publication number: 20120004233Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: January 26, 2010Publication date: January 5, 2012Applicant: AMIRA PHARMACEUTICALS, INCInventors: Brian Andrew Stearns, Ryan Clark
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Publication number: 20120004203Abstract: The present invention relates to novel heterocyclically fused diaryldihydropyrimidine derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: December 29, 2009Publication date: January 5, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
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Publication number: 20110312940Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, A, X, m and k 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 medicament having the above-mentioned properties.Type: ApplicationFiled: October 15, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Lars Van Der Veen, Darryl McConnell, Tobias Wunberg
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Publication number: 20110312956Abstract: This invention provides novel arylindenopyrimidines of the Formula (I), and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing adenosine A1 and/or A2a receptors. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.Type: ApplicationFiled: June 16, 2010Publication date: December 22, 2011Inventors: Paul JACKSON, Brian SHOOK
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Publication number: 20110312978Abstract: Compounds that inhibit phosphodiesterase 1 (PDE1) are useful to treat glaucoma or elevated intraocular pressure. The PDE1 inhibitors may be administered as monotherapy or in combination with additional intraocular-pressure lowering agents. In addition, the invention provides ophthalmic compositions comprising PDE 1 inhibitors and optionally one or more additional intraocular pressure-lowering agents. Topical and systemic therapy may be used.Type: ApplicationFiled: February 24, 2010Publication date: December 22, 2011Inventors: Robert Davis, Allen Fienberg
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Publication number: 20110301168Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: November 5, 2009Publication date: December 8, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong
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Publication number: 20110294662Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.Type: ApplicationFiled: April 14, 2011Publication date: December 1, 2011Applicant: Bayer CropScience AGInventors: Thomas SEITZ, Jürgen Benting, Ulrike Wachendorff-Neumann
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Publication number: 20110288108Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: ApplicationFiled: June 2, 2011Publication date: November 24, 2011Inventor: Aleem Gangjee
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Patent number: 8063056Abstract: Cyclopenta[g]quinazolines of the formula (I):— wherein: A is a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl, or R0 and R1 together with the intermediate N form a five- or six-membered heterocyclic ring; p is an integer in the range 1 to 4; R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and R3 is a group of one of the following formulae: -A1-Ar2-A2-Y1-A5-CON(R)CH(Y4)Y5-A8-X—Ar4 and pharmaceutically acceptable salts or esters thereof are of therapeutic value particularly in the treatment of cancer.Type: GrantFiled: March 3, 2010Date of Patent: November 22, 2011Assignee: BTG International LimitedInventors: Vasilios Bavetsias, Ann L Jackman
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Patent number: 8058285Abstract: The invention relates to compounds of general formula (I); 1a, 1 b, 1 c and 1 d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNF?-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes.Type: GrantFiled: January 22, 2007Date of Patent: November 15, 2011Assignee: The Medicines Company (Leipzig) GmbHInventors: Claudia Reichelt, Alexander Ludwig, Alexander Schulze, Mohammed Daghish, Siegfried Leistner, Andreas Krödel, Jochen Heinicke
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Publication number: 20110275581Abstract: A method of treating cancer in a subject comprising the step of administering to the subject in need thereof an effective amount of a combination of a compound that binds a nuclear export signal (NES inhibitor) on topoisomerase II? and a topoisomerase inhibitor. Twenty small molecule inhibitors (SMI) that bind to the two nuclear export sequences (NES) topo II? have been identified from the NCI database using computer-generated molecular modeling. These SMI will improve the effectiveness of topo II directed therapeutics, particularly in the treatment of diseases such as multiple myeloma (MM). In vitro apoptosis assays indicate that these drugs may be effective as single agents or in combination with currently used cancer drugs that target topo II.Type: ApplicationFiled: June 13, 2011Publication date: November 10, 2011Applicants: University of Florida Research Foundation, Inc., H. Lee Moffitt Cancer Center and Research Institute, Inc.Inventors: Daniel M. Sullivan, Joel G. Turner, Thomas C. Rowe, David A. Ostrov
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Publication number: 20110263581Abstract: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules.Type: ApplicationFiled: February 25, 2011Publication date: October 27, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Peter C. CHUA, Fabrice Pierre, Jeffrey P. Whitten
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Publication number: 20110262442Abstract: The present invention provides combination therapies for treating a disease, disorder, or condition, and methods thereof.Type: ApplicationFiled: November 8, 2010Publication date: October 27, 2011Applicant: Adenios, Inc.Inventors: Charles P. Hamilton, Nathan Dean Jorgensen
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Publication number: 20110257137Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: ApplicationFiled: March 10, 2011Publication date: October 20, 2011Applicant: KALYPSYS, INC.Inventors: Allen Borchardt, Robert Davis, Clay Beauregard, Daniel Becker, Daniel Gamache, Stewart A. Noble, Mark Hellberg, Peter Klimko, Zhihai Qiu, Joseph Payne, John Yanni
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Patent number: 8039478Abstract: The present invention relates to purinone derivatives which are agonists of the HM74a receptor. Further provided are compositions and methods of using the compounds herein, and their pharmaceutically acceptable salts for the treatment of disease.Type: GrantFiled: November 3, 2008Date of Patent: October 18, 2011Assignee: Incyte CorporationInventors: Changsheng Zheng, Chu-Biao Xue, Ganfeng Cao, Michael Xia, Anlai Wang, Hai Fen Ye, Brian Metcalf
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Patent number: 8030304Abstract: The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.Type: GrantFiled: September 17, 2007Date of Patent: October 4, 2011Assignee: Eli Lilly and CompanyInventors: Zhaogen Chen, Chafiq Hamdouchi Hamdouchi, Erik James Hembre, Philip Arthur Hipskind, Jason Kenneth Myers, Takako Takakuwa, James Lee Toth
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Patent number: 8030321Abstract: Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: July 2, 2009Date of Patent: October 4, 2011Assignee: Janssen Pharmaceutica, NVInventors: Frank Chavez, Michael P. Curtis, James P. Edwards, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Brad M. Savall
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Publication number: 20110237561Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.Type: ApplicationFiled: December 7, 2009Publication date: September 29, 2011Inventors: Peng Li, Jun Zhao, Hailin Zeng, Lawrence Wennogle
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Publication number: 20110237611Abstract: Chemical permeation enhancers (CPEs) improve access of local anesthetics to the nerve, thereby improving their performance. Surfactants, representing three CPE sub-groups: anionic, cationic, and nonionic surfactants, were co-injected with tetrodotoxin (TTX) or bupivacaine at the sciatic nerve of Sprague-Dawley rats. All enhancers produced marked concentration-dependent improvements in the frequency and duration of block with TTX but not bupivacaine. An in vitro toxicity assay showed a wide range of CPE myotoxicity, but in vivo histological assessment showed no signs of muscle or nerve damage at concentrations of CPEs that produced a half-maximal increase in the duration of block of TTX. There was no systematic relationship between the enhancers' charge or hydrophobicity and their enhancement of block duration or potency.Type: ApplicationFiled: May 19, 2009Publication date: September 29, 2011Inventors: Daniel S. Kohane, Itay Sagie, Emmanuel J. Simons
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Patent number: 8026246Abstract: The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.Type: GrantFiled: November 14, 2007Date of Patent: September 27, 2011Assignee: Millennium Pharmaceuticials, Inc.Inventors: Christopher F. Claiborne, Todd B. Sells, Stephen G. Stroud
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Publication number: 20110230502Abstract: The present invention provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.Type: ApplicationFiled: March 18, 2011Publication date: September 22, 2011Applicant: SENOMYX, INC.Inventors: Catherine TACHDJIAN, Xiao-Qing Tang, Sara Werner, Marketa Rinnova, Qing Chen, Guy Servant, Xiaodong Li, Feng Zhang, Haitian Liu, Albert Zlotnik, Mark Zoller, Boris Klebansky, Richard Fine, Xinshan Kang
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Patent number: 8022078Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: GrantFiled: May 19, 2009Date of Patent: September 20, 2011Assignee: University of Tennessee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa, Patrick Allison
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Publication number: 20110224155Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.Type: ApplicationFiled: June 3, 2008Publication date: September 15, 2011Applicant: SENOMYX INC.Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
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Publication number: 20110224220Abstract: Compounds of formula (I): wherein: Z, R1, R2, R3, n, and m are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.Type: ApplicationFiled: December 15, 2010Publication date: September 15, 2011Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Antonio Almario GARCIA, Alistair LOCHEAD, Mourad SAADY, Philippe YAICHE
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Publication number: 20110224198Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Scott D. Kuduk, Douglas C. Beshore, ChristinaNg Di Marco, Thomas J. Greshock
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Publication number: 20110224195Abstract: The present invention is directed to substituted six-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as obesity and diabetes, particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: August 18, 2008Publication date: September 15, 2011Inventors: Tesfaye Biftu, Danqing Feng, Ann E. Weber, Jason M. Cox, Xiaoxia Qian, Jinyou Xu
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Patent number: 8017614Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease.Type: GrantFiled: October 17, 2008Date of Patent: September 13, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Brian C. Shook, Paul F. Jackson
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Patent number: 8017619Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: February 26, 2010Date of Patent: September 13, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Jeremy Green, Huai Gao, Young-Choon Moon, Guy Brenchley, Ronald Knegtel, Francoise Pierard
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Patent number: 8012973Abstract: Adenosine A2A receptor antagonists are useful for the preparation of medicaments against atrial fibrillation in mammals, including humans. It has been found that the adenosine A2A receptor is present in human atrial cardiomyocytes and participates in the pathological mechanisms underlying atrial fibrillation. An advantage of using A2A antagonists over other agents known in the art is that the A2A antagonists specifically target patients with atrial fibrillation.Type: GrantFiled: October 10, 2006Date of Patent: September 6, 2011Assignee: Proyecto de Biomedicina Cima S.L.Inventors: Rafael Franco Fernández, Franciso Ciruela Alférez, Carmen Lluís Biset, Christa Müller, Joan Cinca Cuscullola, Leif Hove-Madsen
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Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
Patent number: 8012965Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: December 28, 2007Date of Patent: September 6, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20110212929Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.Type: ApplicationFiled: March 18, 2011Publication date: September 1, 2011Inventors: Laurence H. Hurley, Daruka Mahadevan, Haiyong Han, David J. Bearss, Hariprasad Vankayalapati, Sridevi Bashyam, Ruben M. Munoz, Steven L. Warner, Kimiko Della Croce, Daniel D. Von Hoff, Cory L. Grand, James Welsh
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Publication number: 20110207757Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: ApplicationFiled: May 2, 2011Publication date: August 25, 2011Applicant: Duquesne University of the Holy GhostInventor: Aleem Gangjee
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Patent number: 7998967Abstract: Methods are provided for using methotrexate (MTX) in which reduced host toxicity is observed. Aspects of the methods include administering to a subject an effective amount of MTX in conjunction with a MTX toxicity-reducing adjuvant, such as a 2,2?-anhydropyrimidine, a derivative thereof or a uridine phosphorylase inhibitor. Also provided are compositions that find use in practicing embodiments of the invention. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions.Type: GrantFiled: March 2, 2009Date of Patent: August 16, 2011Assignee: Tosk, IncorporatedInventors: William A. Garland, Brian D. Frenzel, Travis Karg
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Publication number: 20110190325Abstract: Embodiments of the present invention provide compounds (such as Formula (I) compounds, Formula (II) compounds, and various embodiments thereof). Compositions comprising those compounds are also provided. Methods for their preparation are included. Also, uses of the compounds are included, such as administering and treating diseases (e.g., cancer and infections).Type: ApplicationFiled: August 14, 2009Publication date: August 4, 2011Inventors: Gerald B. Hammond, Jose C. Aponte, Robert H. Gilman, Michel Henri Auguste Sauvain, Abraham Caisberg
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Publication number: 20110190324Abstract: The present invention relates to adenosine A3 receptor antagonists and their use for the prevention and treatment of atherosclerosis by administering to a mammal, in need thereof, a therapeutically effective amount of an adenosine A3 receptor antagonist, or a pharmaceutically acceptable salt thereof, alone or in combination with other anti-atherosclerotic agents.Type: ApplicationFiled: July 15, 2009Publication date: August 4, 2011Inventor: Edward Leung
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Publication number: 20110189255Abstract: Drug eluting stents (DES) useful for the treatment of restenosis are described. The stents comprise biocompatible polymers and adenosine receptor modulators.Type: ApplicationFiled: October 1, 2010Publication date: August 4, 2011Inventors: Michael STUREK, Kinam PARK