Tetrazoles (including Hydrogenated) Patents (Class 514/381)
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Publication number: 20150087512Abstract: The subject invention is directed toward antimicrobial agents and methods of treating and preventing infection by pathogenic microorganisms and endophytic microorganisms in a plant through the use of SecA inhibitors.Type: ApplicationFiled: September 26, 2014Publication date: March 26, 2015Inventors: Nian WANG, Nagaraju AKULA
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Patent number: 8987315Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: December 29, 2010Date of Patent: March 24, 2015Assignee: Innocrin Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
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Publication number: 20150080412Abstract: The invention disclosed herein is directed to compounds of Formula (I) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula (I), or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a of a therapeutically effective amount of a selective PPAR? antagonist.Type: ApplicationFiled: March 7, 2013Publication date: March 19, 2015Applicant: INCEPTION 2, INC.Inventors: Nicholas Simon Stock, Austin Chih-Yu Chen, Yalda Mostofi Bravo, Jason Duarte Jacintho, Jill Melissa Baccei, Brian Andrew Stearns, Ryan Christopher Clark, Yen Pham Truong
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Patent number: 8980920Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.Type: GrantFiled: May 28, 2010Date of Patent: March 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Patent number: 8981110Abstract: The present invention provides novel process for preparation of olmesartan medoxomil (I) substantially free of olmesartan acid impurity (II) comprising, reacting trityl olmesartan medoxomil (III) with acid, filtering the precipitate of trityl alcohol, subjecting the filtrate to agitated thin film drying and recovering olmesartan medoxomil (I).Type: GrantFiled: July 31, 2012Date of Patent: March 17, 2015Assignee: Lupin LimitedInventors: Rajendra Vishwanath Firke, Ujjwal Komalsing Sisodiya, Chandrakant Shriram Bhangale, Radhakrishna Bhikaji Shivdavkar, Himanshu Madhav Godbole, Girij Pal Singh
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Patent number: 8980837Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: GrantFiled: January 23, 2012Date of Patent: March 17, 2015Assignee: Genentech, Inc.Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Patent number: 8975288Abstract: A compound or its pharmaceutically acceptable salt, as well as a pharmaceutical, composition containing that compound or salt dissolved or dispersed in a pharmaceutically acceptable carrier, and a method of using that compound or salt in an antibacterial treatment. A contemplated compound corresponds in structure to structural Formula I or a pharmaceutically acceptable salt of that compound, wherein V is O or NR9, Y is halogen, OR10, C1-C4 hydrocarbyl or NHR10, Z is NR2—X—R1 or CH2—R8, n is 1-6, X is H, S(O)2, C(O), C(O)NR7, C(NH)NR7 or C(O)O, and R1, R2, R7, R8, R9 and R10 are defined within.Type: GrantFiled: March 15, 2013Date of Patent: March 10, 2015Assignee: The Penn State Research FoundationInventors: Kenneth Charles Keiler, John Nandwa Alumasa
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Publication number: 20150065543Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: October 23, 2014Publication date: March 5, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20150065508Abstract: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.Type: ApplicationFiled: March 26, 2014Publication date: March 5, 2015Applicant: ABBVIE INC.Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Steven Fung, Peer B. Jacobson, Lynne E. Rueter, Marina I. Strakhova, Jiahong Wang, Jyoti R. Patel, Qi Shuai, James T. Link, Jeffrey J. Rohde, Jurgen Dinges, Bryan K. Sorensen, Martin Winn, Hong Yong, Vince S. Yeh
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Publication number: 20150065506Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: August 13, 2014Publication date: March 5, 2015Applicant: ROCHE PALO ALTO LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Patent number: 8969341Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: GrantFiled: November 28, 2012Date of Patent: March 3, 2015Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Publication number: 20150057322Abstract: A method for treatment of a cardiovascular or renal condition or disease with a specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi.Type: ApplicationFiled: June 23, 2014Publication date: February 26, 2015Applicant: NOVARTIS PHARMACEUTICALS CORPORATIONInventors: Li Feng, Sven Erik Godtfredsen, Paul Allen Sutton, Mahavir Prashad, Michael J. Girgis, Bin Hu, Yugang Liu, Thomas J. Blacklock, Piotr Henryk Karpinski
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Publication number: 20150057238Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.Type: ApplicationFiled: March 13, 2013Publication date: February 26, 2015Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, William Leonard Mitchell, Peter Johnson, Naomi Went
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Patent number: 8962580Abstract: The invention features compounds of formula I or II: In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.Type: GrantFiled: September 23, 2009Date of Patent: February 24, 2015Assignee: Alnylam Pharmaceuticals, Inc.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Takeshi Yamada, David Butler, Narayanannair K. Jayaprakash, Muthusamy Jayaraman, Shigeo Matsuda, Rajendra K. Pandey, Chang Geng Peng
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Patent number: 8962667Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.Type: GrantFiled: July 24, 2014Date of Patent: February 24, 2015Assignee: Microdose Therapeutix, Inc.Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laquerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
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Publication number: 20150051256Abstract: The present invention provides a medicament that suppresses (or mitigates) various neurological symptoms caused by a peripheral nerve disorder induced by an anti-cancer agent.Type: ApplicationFiled: October 28, 2014Publication date: February 19, 2015Applicant: Takeda Pharmaceutical Company LimitedInventor: Naomi Kitamoto
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Publication number: 20150051171Abstract: The present invention provides a compound having an excellent efficacy for controlling pests. A tetrazolinone compound of a formula (1): [wherein R1 represents an C6-C16 aryl group, an C1-C12 alkyl group, or a C3-C12 cycloalkyl group, etc., which each optionally be substituted; R2, R3, R4 and R5 represent independently of each other a hydrogen atom, a halogen atom or an C1-C3 alkyl group, etc.; R6 represents an C1-C6 alkyl group, a C3-C6 cycloalkyl group, a halogen atom, a C1-C6 haloalkyl group, an C2-C6 alkenyl group, an C1-C6 alkoxy group, or a C1-C6 haloalkoxy group, etc.; R7, R8 and R9 represent independently of each other a hydrogen atom, a halogen atom, or an C1-C4 alkyl group, etc.; X represents an oxygen atom or a sulfur atom; and R10 represents an C1-C6 alkyl group, etc.] shows an excellent controlling efficacy on pests.Type: ApplicationFiled: April 26, 2013Publication date: February 19, 2015Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yuya Yoshimoto, Sadayuki Arimori, Yuichi Matsuzaki
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Patent number: 8957096Abstract: What is described are oxime ether-substituted benzoylamides of the general formula (I) as herbicides. In this formula (I), R, Y and Y are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical.Type: GrantFiled: October 29, 2012Date of Patent: February 17, 2015Assignee: Bayer Intellectual Property GmbHInventors: Andreas Van Almsick, Hartmut Ahrens, Hansjörg Dietrich, Isolde Häuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Rosinger
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Patent number: 8952169Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.Type: GrantFiled: May 21, 2013Date of Patent: February 10, 2015Assignees: Xenon Pharmaceuticals Inc., Genentech, Inc.Inventors: Jean-Christophe Andrez, Sultan Chowdhury, Shannon Marie Decker, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Jun Li, Daniel F. Ortwine, Brian Safina, Tao Sheng, Shaoyi Sun, Daniel P. Sutherlin, Michael Scott Wilson, Alla Yurevna Zenova
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Patent number: 8940735Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: June 20, 2012Date of Patent: January 27, 2015Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Robert J. Schotzinger, Gary D. Gustafson
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Patent number: 8940774Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine 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: November 26, 2013Date of Patent: January 27, 2015Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Publication number: 20150025119Abstract: A method of releasing an antihypertensive agent on a plant fiber bundle is proposed. Firstly, the antihypertensive agent is fixed onto the plant fiber bundle. Then, the antihypertensive agent is fixed onto the plant fiber bundle and released in a buffer solution system. Next, fluorescence analysis of released antihypertensive agent is performed to evaluate the release efficiency of the antihypertensive agent.Type: ApplicationFiled: August 19, 2013Publication date: January 22, 2015Applicant: National Tsing Hua UniversityInventors: Chen-Meng Kuan, Chao-Min Cheng, Robert S. Langer
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Publication number: 20150025114Abstract: In one aspect, the invention relates to substituted 1H-benzo[d][1,2,3]triazol-1-ol analgoues, derivatives thereof, and related compound; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders, e.g. various tumors and cancers, associated with ?-catenin/Tcf protein-protein interaction dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: February 10, 2013Publication date: January 22, 2015Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATIONInventors: Haitao Ji, Binxun Yu, Min Zhang, Wenxing Guo
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Patent number: 8933102Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I).Type: GrantFiled: October 24, 2011Date of Patent: January 13, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Gregori J. Morriello, Lehua Chang, Scott D. Edmondson
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Publication number: 20150011598Abstract: Provided is a pharmaceutical composition comprising candesartan or ester thereof and chlorthalidone, and use thereof, wherein the weight ratio of candesartan or ester thereof to chlorthalidone is 5.3:1 to 1:6.25. The pharmaceutical composition has a synergistic antihypertensive effect, and can enhance the antihypertensive effect and extend duration of antihypertension.Type: ApplicationFiled: December 21, 2012Publication date: January 8, 2015Inventors: Lida Tang, Zhuanyou Zhao, Weiting Wang, Wengong Xi, Chunhua Hao, Xiangwei Xu, Bing Yu
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Publication number: 20150011553Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Inventors: Ulrich GÖRGENS, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
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Publication number: 20150011597Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.Type: ApplicationFiled: March 27, 2014Publication date: January 8, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLC.Inventors: Sharath Hegde, Daniel Marquess
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Patent number: 8927586Abstract: The present invention relates to novel TP receptor antagonists, which optionally cross the blood-brain barrier of a mammal. The invention also provides methods for treating a disorder related to activation of TP receptor utilizing the compounds of the invention.Type: GrantFiled: February 28, 2013Date of Patent: January 6, 2015Assignee: The Trustees of the University of PennsylvaniaInventors: John Q. Trojanowski, Virginia M. Y. Lee, Kurt R. Brunden, Amos B. Smith, Donna M. Huym, Carlo Ballatore, Anne-Marie Hogan, Francesco Piscitelli, Sugiyama Shimpei, Xiaozhao Wang
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Publication number: 20150005345Abstract: The present invention features benzhydrol-pyrazole derivatives and related compounds having kinase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions, such as cancers, inflammatory disorders, or autoimmune disorders.Type: ApplicationFiled: January 9, 2013Publication date: January 1, 2015Inventors: Anthony D. Keefe, Richard W. Wagner, Matthew Clark, Ying Zhang, Diana Gikunju, John Cuozzo, Heather Thomson
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Publication number: 20140378459Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.Type: ApplicationFiled: September 14, 2012Publication date: December 25, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Jiro Fujiyasu, Kazuhiko Ohne, Susumu Yamaki, Tomoyoshi Imaizumi, Takeshi Hondo, Keisuke Matsuura, Tomohki Satou, Satoshi Sasamura
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Publication number: 20140378516Abstract: Embodiments of the present disclosure, in one aspect, relate to a beta-lactamase inhibitor, pharmaceutical compositions including a beta-lactamase inhibitor, methods of treatment of a condition (e.g., infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.Type: ApplicationFiled: January 4, 2013Publication date: December 25, 2014Inventors: Yu Chen, Derek Nichols, Adam R. Renslo, Priyadarshini Jaishankar, Erica M.W. Lauterwasser
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Publication number: 20140378430Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.Type: ApplicationFiled: January 4, 2013Publication date: December 25, 2014Applicant: SPINIFEX PHARMACEUTICALS PTY LTDInventors: Thomas David McCarthy, Alan Naylor
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Publication number: 20140378453Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.Type: ApplicationFiled: June 27, 2014Publication date: December 25, 2014Inventors: Aleksandr KOLESNIKOV, Roopa RAI, William Dvorak SHRADER, Steven M. TORKELSON, Kieron E. WESSON, Wendy B. YOUNG
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Publication number: 20140378510Abstract: Provided herein are small molecule activators of calcium-activated chloride channels. These small molecules may be used for treatment of diseases and disorders that are treatable by activating calcium-activated chloride channels, such as cystic fibrosis, disorders related to salivary gland dysfunction (for example, Sjogren's syndrome and dysfunction following radiation injury), dry eye syndrome, and intestinal hypomotility.Type: ApplicationFiled: August 3, 2012Publication date: December 25, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Alan S. Verkman, Wan Namkung
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Patent number: 8916561Abstract: Disclosed herein are substituted quinoxaline of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.Type: GrantFiled: March 2, 2012Date of Patent: December 23, 2014Assignee: BioEnergenix, LLCInventors: John M. McCall, Donna L. Romero
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Publication number: 20140371240Abstract: The invention relates to compounds of the general formulae (I) and (II) in which the radicals A1, A2, A3, A4, M1, M2, M3, Q, R1, T, W1 and W2 have the meaning given in the description and to the use of the compounds for controlling animal pests. The invention furthermore relates to processes and intermediates for preparing the compounds of formula (I).Type: ApplicationFiled: December 17, 2012Publication date: December 18, 2014Inventors: Michael Maue, Tobias Kapferer, Friedrich August Muehlthau, Olga Malsam
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Publication number: 20140371282Abstract: The present invention provides a controlled release oral pharmaceutical composition having a therapeutically effective amount of one or more pharmacologically active agent having low bioavailability; one or more solubilizers; one or more biocompatible swelling agents; and a swelling enhancer. The swelling agent, in combination with swelling enhancer, swells in the presence of water in gastric fluid such that the size of the dosage form is sufficiently increased to provide retention of the dosage form in the stomach of a patient, which gradually erodes within the gastrointestinal tract over a prolonged time period.Type: ApplicationFiled: September 2, 2014Publication date: December 18, 2014Inventors: Pratibha S. Pilgaonkar, Anilkumar S. Gandhi
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Publication number: 20140371213Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: May 19, 2014Publication date: December 18, 2014Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Publication number: 20140364458Abstract: A composition comprising a compound of formula (I): in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, and at least one biological control agent selected from bacteria, fungi or yeasts, protozoas, viruses, entomopathogenic nematodes, and botanical extracts, or products produced by microorganisms including proteins or secondary metabolites, and optionally an inoculant, for reducing overall damage of plants and plant parts as well as losses in harvested fruits or vegetables caused by insects, nematodes and phytopathogens.Type: ApplicationFiled: December 17, 2012Publication date: December 11, 2014Inventors: Rüdiger Fischer, Heiki Hungenberg
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Patent number: 8907105Abstract: The present invention relates to compositions of matter that are ionic liquids, the compositions comprising substituted 1,2,3-triazolium cations combined with any anion. Compositions of the invention should be useful in the separation of gases and, perhaps, as catalysts for many reactions.Type: GrantFiled: September 1, 2011Date of Patent: December 9, 2014Assignee: U.S. Department of EnergyInventors: David Luebke, Hunaid Nulwala, Chau Tang
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Patent number: 8901313Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: GrantFiled: March 15, 2012Date of Patent: December 2, 2014Assignee: Genentech, Inc.Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
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Publication number: 20140350010Abstract: The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: November 28, 2012Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Publication number: 20140343017Abstract: Provided is a highly safe and effective compound represented by the following general formula (1) or a salt thereof which acts on tubulin and has an anticancer effect, wherein Ar represents an aryl group or a heteroaryl group; Z1, Z2, Z3, and Z4 each independently represent CH, a nitrogen atom, an oxygen atom, or a sulfur atom; R1 represents a hydrogen atom, a halogen atom, an alkyl group, or the like; R2 and R3 are the same or different and each represent a hydrogen atom, a halogen atom, a carboxyl group, or the like; n units of R4 are the same or different and each represent a hydrogen atom, an alkyl group, or the like; and n represents a number of 0 to 4.Type: ApplicationFiled: January 24, 2013Publication date: November 20, 2014Applicant: Kabushiki Kaisha Yakult HonshaInventors: Takashi Ikeda, Masahiro Ono, Satoshi Ueno, Ryuta Yamazaki, Takashi Yaegashi, Takeshi Matsuzaki
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Patent number: 8889724Abstract: Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum-induced inflammation.Type: GrantFiled: March 4, 2013Date of Patent: November 18, 2014Assignee: Wellstat Therapeutics CorporationInventors: James Dennen O'Neil, Shalini Sharma, Ramachandran Arudchandran
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Publication number: 20140336194Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Applicant: NOVARTIS AGInventor: Shi Yin FOO
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Publication number: 20140329676Abstract: The present invention relates to the use of anthranilic acid diamide derivatives with heteroaromatic and heterocyclic substituents of formula (I) wherein R1, R2, R3, R4, R5, R6, n, A, Q have the meanings as given in the description—for controlling animal pests, such as insects and/or unwanted acarids and/or nematodes in transgenic crops and to methods particularly useful for controlling insects, and/or acarids and/or nematodes and/or increasing crop yield in those crops.Type: ApplicationFiled: December 17, 2012Publication date: November 6, 2014Inventors: Rüdiger Fischer, Heike Hungenberg, Bill Striegel, Steven Riniker
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Publication number: 20140329872Abstract: The invention relates to methods and pharmaceutical compositions for treating hypertension and/or preventing or treating heart failure in a mammal receiving anti-coagulant therapy using compound(s) which are therapeutically effective but do not impact the pharmacokinetic or the pharmacodynamic effect(s) of the anti-coagulant, such as warfarin.Type: ApplicationFiled: July 21, 2014Publication date: November 6, 2014Applicant: NOVARTIS AGInventors: Diego Jochen Albrecht, Priyamvada Chandra, Sven Erik Godtfredsen, Pierre Jordaan, Martin Lefkowitz
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Patent number: 8877938Abstract: A compound of an angiotensin receptor antagonist (ARB), a neutral endopeptidase inhibitor (NEPi) and one or more monovalent cations are useful for the treatment of hypertension and/or heart failure. ARB includes S—N-valeryl-N-{[2?-(1H-tetrazole-5-yl)-biphenyl-4-yl]-methyl}-valine in the anion form, NEPi includes (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid ethyl ester in the anion form and cation includes monovalent cations such as Na+. The compound includes trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3?-methyl-2?-(pentanoyl{2?-(tetrazol-5-ylate)biphenyl-4?-ylmethyl}amino)butyrate] hemipentahydrate.Type: GrantFiled: November 8, 2006Date of Patent: November 4, 2014Assignee: Novartis Pharmaceuticals CorporationInventors: Lili Feng, Sven Erik Godtfredsen, Bin Hu, Yugang Liu, Piotr Karpinski, Paul Allen Sutton, Mahavir Prashad, Michael J. Girgis, Thomas J. Blacklock
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Patent number: 8877786Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: December 2, 2013Date of Patent: November 4, 2014Assignee: Novartis AGInventors: Yuki Iwaki, Toshio Kawanami, Gary Michael Ksander, Muneto Moji
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Publication number: 20140323424Abstract: Described herein are assays, kits and methods for treating mood disorders by testing for one or more polymorphisms in a specific group of genes and for analyzing the results of polymorphism testing; the genes included may converge in one or more signaling pathways, and may be epigenetic. The genes are included based on the relationships of the proteins encoded by the genes in the context of particular signaling pathways and provide a diagnostically relevant nexus. Also described herein are methods of presenting the data collected by the screen, including methods of delivering interpretive comments and/or treatment guidance based on the results of the genetic screening either individually or based on the genetic composition of particular clusters of genes which may be related to each other. Importantly, drugs which modulate these genetic disturbances are described for targeted therapeutic use based upon companion diagnostic method.Type: ApplicationFiled: July 7, 2014Publication date: October 30, 2014Inventor: Jay L. LOMBARD