1,2 Diazine Attached Directly Or Indirectly To An Additional Hetero Ring By Nonionic Bonding Patents (Class 514/252.01)
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Patent number: 8759346Abstract: The present invention relates to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5, R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: (Ia) in free base or acid addition salt form, to processes for their production, to pharmaceutical compositions comprising them and their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and neurodegenerative disorders.Type: GrantFiled: March 26, 2010Date of Patent: June 24, 2014Assignee: Novartis AGInventors: Mathias Frederiksen, Dominik Feuerbach, Konstanze Hurth, Manuel Koller, Bernard Lucien Roy
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Publication number: 20140148462Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: November 25, 2013Publication date: May 29, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Elke LANGKOPF, Holger WAGNER
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Patent number: 8735394Abstract: The present invention provides combination therapy methods of treating proliferative diseases (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include, for example, radiation, surgery, administration of chemotherapeutic agents (such as an anti-VEGF antibody), or combinations thereof. Also provided are methods of administering to an individual a drug taxane in a nanoparticle composition based on a metronomic dosing regime.Type: GrantFiled: May 6, 2009Date of Patent: May 27, 2014Assignee: Abraxis BioScience, LLCInventors: Neil P. Desai, Patrick Soon-Shiong
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Patent number: 8716289Abstract: Compound corresponding to general formula (I): in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C1-8-alkylene group; R1 is a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; R3 is a hydrogen or fluorine atom, a C1-6-alkyl group or a tritluoromethyl group; R4 is a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or oType: GrantFiled: November 13, 2009Date of Patent: May 6, 2014Assignee: SanofiInventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Mourad Saady, Julien Vache, Corinne Veronique, Philippe Yaiche
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Patent number: 8703770Abstract: The present invention is directed to pyridazine carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.Type: GrantFiled: October 26, 2009Date of Patent: April 22, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Paul J. Coleman, Christopher D. Cox, Swati P. Mercer, Anthony J. Roecker, John D. Schreier
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Patent number: 8703803Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: September 21, 2012Date of Patent: April 22, 2014Inventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Patent number: 8686155Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: June 28, 2011Date of Patent: April 1, 2014Assignee: Amgen Inc.Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
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Patent number: 8685978Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.Type: GrantFiled: July 26, 2010Date of Patent: April 1, 2014Assignee: University of Tennessee Research FoundationInventors: Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, Vnr Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
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Patent number: 8642585Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: GrantFiled: March 14, 2013Date of Patent: February 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Sara Frattini, Dieter Hamprecht, Frank Himmelsbach, Elke Langkopf, Iain Lingard, Stefan Peters, Holger Wagner
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Publication number: 20140030223Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: September 25, 2013Publication date: January 30, 2014Applicant: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Martzman, Philip Anthony Morganelli, William J. Watkins, Hong Ye
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Patent number: 8637517Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.Type: GrantFiled: October 4, 2011Date of Patent: January 28, 2014Assignee: Novartis AGInventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
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Publication number: 20140024648Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof (I) wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.Type: ApplicationFiled: March 6, 2012Publication date: January 23, 2014Applicant: BIOTIE THERAPIES CORPORATIONInventors: Marjo Pihlavisto, David Smith, Auni Juhakoski, Ferenc Fulop, Laszlo Lazar, Istvan Szatmari, Ferenc Miklos, Zsolt Szakonyi, Lorand Kiss, Marta Palko
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Patent number: 8618107Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: May 6, 2011Date of Patent: December 31, 2013Assignees: Gilead Connecticut, Inc., Genentech, Inc.Inventors: Antonio J. M. Barbosa, Peter A. Blomgren, Kevin S. Currie, Ravi Krishnamoorthy, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Daniel Ortwine, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Wendy Young, Honglu Zhang, Zhongdong Zhao, Pavel E. Zhichkin
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Patent number: 8618296Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: GrantFiled: June 10, 2013Date of Patent: December 31, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20130323203Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: August 2, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman Belmont, Philip Anthony Morganelli, William J. Watkins
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Patent number: 8598174Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: GrantFiled: November 12, 2009Date of Patent: December 3, 2013Assignees: Genetech, Inc., Gilead Connecticut, Inc.Inventors: Antonio J. M. Barbosa, Jr., Peter A. Blomgren, Kevin S. Currie, Seung Lee, Jeffrey E. Kropf, Scott A. Mitchell, Daniel Ortwine, William M. Rennells, Aaron C. Schmitt, Jianjun Xu, Wendy B. Young, Zhongdong Zhao, Pavel E. Zhichkin
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Patent number: 8592591Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.Type: GrantFiled: August 14, 2008Date of Patent: November 26, 2013Assignee: Bayer Intellectual Property GmbHInventors: Swen Hölder, Armin Zülch, Thomas Bär, Thomas Maier, Astrid Zimmermann, Thomas Beckers, Volker Gekeler, Hemant Joshi, Yogesh Munot, Umesh Bhise, Sunil Chavan, Sachin Shivatare, Sarvesh Patel, Vikas Gore
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Publication number: 20130310379Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.Type: ApplicationFiled: November 21, 2011Publication date: November 21, 2013Applicant: CONSTELLATION PHARMACEUTICALSInventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Naveschuk
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Patent number: 8575166Abstract: This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N—N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: GrantFiled: February 4, 2010Date of Patent: November 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Jason L. Davis, Michael John Mayer, Hubert B. Josien
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Patent number: 8569302Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: GrantFiled: July 19, 2010Date of Patent: October 29, 2013Assignee: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Mertzman, Philip A. Morganelli, William J. Watkins, Hong Ye
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Patent number: 8551963Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: GrantFiled: November 5, 2009Date of Patent: October 8, 2013Assignee: Ambit Biosciences CorporationInventors: Julius L. Apuy, Darren E. Insko, Joyce J. James
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Patent number: 8551997Abstract: Provided herein are methods of treating a pathophysiological state or symptoms thereof resulting from aldose reductase-mediated signaling in a cytotoxic pathway in a subject using an inhibitor of aldose reductase. Particularly, specific inhibitors may be a small-interfering RNA (siRNA) or may be inhibitors of glutathione-aldehyde binding to aldose reductase which are designed via at least computer modeling of the ternary AR:NADPH:DCEG structure. Also, methods of treating a cancer or suppressing metastasis thereof using the siRNAs and aldose reductase inhibitors are provided.Type: GrantFiled: June 29, 2007Date of Patent: October 8, 2013Assignee: The Board of Regents of the University of Texas SystemInventors: Satish K. Srivastava, Kota V. Ramana
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Publication number: 20130252937Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: March 14, 2013Publication date: September 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
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Patent number: 8541414Abstract: A pyridazinone compound represented by the formula (I) has excellent effect on weed control and is useful as an active ingredient of herbicides.Type: GrantFiled: March 13, 2007Date of Patent: September 24, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Toshiyuki Kiji, Takafumi Fusaka
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Publication number: 20130225596Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: August 9, 2011Publication date: August 29, 2013Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Kentaro Asahi, Tohru Horiguchi
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Patent number: 8476273Abstract: The present invention provides materials and methods for modulating an immune response. The materials and methods may be used to treat diseases associated with an aberrant immune response. In some embodiments, materials and methods of the invention may be used to treat autoimmune diseases, for example, rheumatoid arthritis.Type: GrantFiled: August 18, 2008Date of Patent: July 2, 2013Assignee: University of Maryland, BaltimoreInventors: Jun Hayashi, Alexander Mackerell, Younus Mia, Guanjun Xia
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Patent number: 8461156Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: August 27, 2012Date of Patent: June 11, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Patent number: 8455477Abstract: The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.Type: GrantFiled: July 27, 2009Date of Patent: June 4, 2013Assignees: Merck Sharp & Dohme Corp., MSD K.K.Inventors: Jason Katz, James Jewell, Joon Jung, Solomon Kattar, Yongquan Hou, Rachel MacCoss, Satoru Ito
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Publication number: 20130131075Abstract: The present invention relates to the compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and X are defined as described hereinafter, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the medicaments containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: January 15, 2013Publication date: May 23, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Norbert HAUEL, Angelo CECI, Henri DOODS, Ingo KONETZKI, Juergen MACK, Henning PRIEPKE, Annette SCHULER-METZ, Rainer WALTER, Dieter WIEDENMAYER
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Publication number: 20130131062Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.Type: ApplicationFiled: December 21, 2007Publication date: May 23, 2013Inventors: Hakim Djaballah, Harold E. Varmus, David Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
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Patent number: 8420651Abstract: The subject of the present invention is compounds corresponding to the formula (I) in which: X represents a divalent (C2-C5)alkylene radical which is unsubstituted or substituted one or more times by an Alk group; R1 represents a phenyl, a naphthyl, a pyridyl, a 1-benzothienyl or a 1,3-benzodioxolyl; R2 represents a hydrogen atom, a halogen atom, an Alk group, an OAlk group or else a group chosen from —S-Alk, —SO-Alk, —SO2-Alk, —CO—N(R4)-Alk, —N(R4)SO2-Alk, —N(R4)CO-Alk, —N(R4)SO2—N(Alk)2; R3 represents a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R4 represents a hydrogen atom or a (C1-C4)alkyl; Alk represents an unsubstituted or substituted (C1-C4)alkyl. Preparation process and therapeutic application.Type: GrantFiled: April 6, 2010Date of Patent: April 16, 2013Assignee: SanofiInventors: Elodie Barbagallo, Carole Legeay, Murielle Rinaldi-Carmona, Pascale Roux, Claude Vernhet
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Patent number: 8410104Abstract: The present invention is concerned with isoxazole-pyridazines of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: April 28, 2010Date of Patent: April 2, 2013Assignees: Hoffmann-La Roche Inc., Roche Palo Alto LLCInventors: Matthew C. Lucas, Andrew Thomas
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Patent number: 8399468Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.Type: GrantFiled: March 2, 2010Date of Patent: March 19, 2013Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Chen Zhao, Minghua Sun, Lawrence A. Black, Guo Zhu Zheng, Robert J. Gregg, Geoff G. Z. Zhang, Ahmad Y. Sheikh, Xiaochun Lou, Rodger F. Henry, David M. Barnes, Lawrence Kolaczkowski, Anthony R. Haight, Sou-Jen Chang, Steven J. Wittenberger, Michael G. Fickes
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Publication number: 20130052281Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 22, 2012Publication date: February 28, 2013Applicant: Takeda Pharmaceutical Company LimitedInventors: William FARNABY, Charlotte FIELDHOUSE, Catrina KERR, Natasha KINSELLA, David LIVERMORE, Kevin MERCHANT, David MILLER, Katherine HAZEL
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Patent number: 8383625Abstract: Compounds of formula (I) in salt or zwitterionic form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: December 22, 2005Date of Patent: February 26, 2013Assignee: Novartis AGInventors: Neil J Press, Collingwood P Stephen
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Patent number: 8372836Abstract: Pharmaceutical compositions comprising a poorly water soluble ionizable drug, a cationic species and a dispersion polymer are disclosed, together with a process for forming the compositions. The neutral form of the drug has (i) a solubility of less than 1 mg/ml, in aqueous solution at a pH between 6 and 7, (ii) a solubility of less than 20 mg/mL in a volatile organic solvent, and (iii) an acidic pKa value of greater than 5. At least 90 wt % of the drug in the solid dispersion being in a non-crystalline form. The drug, the cationic species, and the dispersion polymer constitute at least 80 wt % of the solid dispersion.Type: GrantFiled: October 8, 2007Date of Patent: February 12, 2013Assignee: Bend Research, Inc.Inventors: Rodney James Ketner, Douglas Alan Lorenz, David Keith Lyon
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Patent number: 8367672Abstract: The invention relates to novel chemical compounds and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.Type: GrantFiled: November 2, 2005Date of Patent: February 5, 2013Assignees: Universite de Strasbourg, Northwestern University, Centre National de la Recherche Scientifique (CNRS)Inventors: D. Martin Watterson, Linda J. Van Eldik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Velentza, Wenhui Hu, Magdalena Zasadzki
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Publication number: 20130023538Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: September 26, 2012Publication date: January 24, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Patent number: 8357679Abstract: The present invention relates to hexafluoroisopropanol derivatives having the general formula I to pharmaceutical compositions comprising the same and to the use of these hexafluoroisopropanol derivatives in the treatment of atherosclerosis.Type: GrantFiled: May 13, 2009Date of Patent: January 22, 2013Assignee: MSD Oss B.V.Inventors: Andrew John Cooke, Andrew Stanley Edwards, Fiona Elizabeth Andrews, David Jonathan Bennett, Olaf Nimz, Emma Louise Carswell
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Patent number: 8354410Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: March 9, 2011Date of Patent: January 15, 2013Assignee: Bristol-Meyers Squibb CompanyInventors: Kap-Sun Yeung, Katharine A. Grant-Young, John F. Kadow
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Publication number: 20130012381Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts and N-oxides thereof, wherein the substituents have the meanings as defined in the description, a method for controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites and to an agricultural composition containing at least one compound according to the present invention.Type: ApplicationFiled: March 21, 2011Publication date: January 10, 2013Applicant: BASF SEInventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Douglas D. Anspaugh, Deborah L. Culbertson
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Patent number: 8349839Abstract: Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.Type: GrantFiled: April 8, 2010Date of Patent: January 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Claudio Sturino, Patrick Deroy, Martin Duplessis, Paul J. Edwards, Anne-Marie Faucher, Teddy Halmos, Clint James, Jean-Eric Lacoste, Eric Malenfant, Joannie Minville, Louis Morency, Sebastien Morin, Martin Tremblay, Christiane Yoakim
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Patent number: 8343957Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: November 29, 2010Date of Patent: January 1, 2013Assignee: Dart Neuroscience (Cayman) Ltd.Inventors: Alan P. Kaplan, Varsha Gupta
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Publication number: 20120328661Abstract: The present invention relates to novel 2-oxo-2H-chromene-3-carboxamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: October 20, 2010Publication date: December 27, 2012Applicant: ALLERGAN, INC.Inventors: Todd M. Heidelbaugh, John R. Cappiello, Phong X. Nguyen, Dario G. Gomez
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Publication number: 20120322798Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: August 27, 2012Publication date: December 20, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Patent number: 8334316Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: GrantFiled: February 9, 2009Date of Patent: December 18, 2012Assignee: ACEA Biosciences, Inc.Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
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Patent number: 8324209Abstract: Pesticide compositions and their use in controlling pests are provided.Type: GrantFiled: August 25, 2009Date of Patent: December 4, 2012Assignee: Dow AgroSciences, LLCInventors: Benjamin M. Nugent, Zoltan L. Benko, James M. Renga, Michael R. Loso, Timothy P. Martin
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Patent number: 8324211Abstract: This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: wherein, variables Q, R, X, Y1, Y2, Y3, Y4, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.Type: GrantFiled: July 15, 2009Date of Patent: December 4, 2012Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth
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Publication number: 20120301458Abstract: The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereofType: ApplicationFiled: July 27, 2010Publication date: November 29, 2012Applicant: Auspex Pharmaceuticals, Inc.Inventors: Tadimeti Rao, Chengzhi Zhang
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Patent number: 8299253Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: December 22, 2006Date of Patent: October 30, 2012Assignee: University of Kentucky Research FoundationInventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha P Sumithran