Patents Issued in January 24, 2017
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Patent number: 9550746Abstract: The present invention relates to novel benzofuran-2-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: GrantFiled: January 5, 2015Date of Patent: January 24, 2017Assignee: ALLERGAN, INC.Inventors: Haiqing Yuan, Richard L. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 9550747Abstract: The present invention relates to a new crystalline form of dapagliflozin represented by formula (I). The crystalline form has a characteristic absorption peak at about 4.318 (20.45) in an X-ray powder diffraction pattern shown by angle 2 theta and interplanar spacing (value d). It can be prepared by dissolving dapagliflozin in good organic solvents, adding poor solvents, stirring to crystallization, filtering and drying. The new crystalline form of dapagliflozin of the present invention has the following superior features: good solubility, low hygroscopicity, high stability and good preparation reproducibility.Type: GrantFiled: January 19, 2015Date of Patent: January 24, 2017Assignee: Jiangsu Hansoh Pharmaceutical Group Co., Ltd.Inventors: Xifeng Zhu, Xiaobi Li, Tiancheng Zhang, Fuping Yuan
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Patent number: 9550748Abstract: A cyclic carbonate monomer including the reaction product of (a) a divinylarene dioxide, and (b) carbon dioxide; a process for making the cyclic carbonate monomer; and a polymer such as a poly(hydroxyurethane) composition made therefrom. The poly(hydroxyurethane) composition made from the above cyclic carbonate monomer forms a reactive intermediate that can be used for making, for example, a poly(hydroxyurethane) foam product.Type: GrantFiled: July 19, 2012Date of Patent: January 24, 2017Assignee: BLUE CUBE IP LLCInventors: Maurice J. Marks, Allen S. Bulick, Phillip S. Athey, Dwight D. Latham
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Patent number: 9550749Abstract: An object of the present invention is to provide a novel endoparasite control agent as a parasiticide, an antiprotozoal or the like. Provided is an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I): or a salt thereof as an active ingredient.Type: GrantFiled: August 29, 2013Date of Patent: January 24, 2017Assignees: The University of Tokyo, Nihon Nohyaku Co., Ltd.Inventors: Kiyoshi Kita, Akiyuki Suwa, Masatsugu Oda, Koji Tanaka
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Patent number: 9550750Abstract: This invention relates to indo line compounds of the structural formula I, or their pharmaceutically acceptable salts, wherein the variables are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.Type: GrantFiled: October 2, 2013Date of Patent: January 24, 2017Assignees: Merck Sharp & Dohme Corp., Elexopharm GMBHInventors: Amjad Ali, Michael Man-Chu Lo, Edward Metzger, Lina Yin, Rolf Hartmann, Qingzhong Hu, Ralf Heim, Christina Zimmer
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Patent number: 9550751Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: GrantFiled: August 3, 2015Date of Patent: January 24, 2017Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Ronald Ross, Jr., Kaitlyn Gray, Yu Zhang, Gary Roth
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Patent number: 9550752Abstract: The present invention relates to novel triazolinthione derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.Type: GrantFiled: April 9, 2014Date of Patent: January 24, 2017Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Sebastian Hoffmann, Alexander Sudau, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Helene Lachaise, Stephane Brunet, Jacky Vidal, Pierre Genix, Pierre-Yves Coqueron, Julie Geist, Jean-Pierre Vors, Philippe Kennel, Ricarda Miller
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Mono quaternary ammonium salts and methods for modulating neuronal nicotinic acetylcholine receptors
Patent number: 9550753Abstract: Provided are monoquaternary 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 gastrointestinal tract disorders.Type: GrantFiled: August 27, 2014Date of Patent: January 24, 2017Assignee: University of Kentucky Research FoundationInventors: Peter Crooks, Linda P. Dwoskin, Guangrong Zheng, Sangeetha Sumithran, Zhenfa Zhang -
Patent number: 9550754Abstract: The present invention relates to 4,5-dihydropyrazole derivatives of the formula (I) and physiologically tolerated salts thereof which are GlyT1 inhibitors. The invention further relates to pharmaceutical compositions comprising such 4,5-dihydropyrazole derivatives, and the use of such 4,5-dihydropyrazole derivatives for therapeutic purposes.Type: GrantFiled: September 9, 2015Date of Patent: January 24, 2017Assignees: ABBVIE DEUTSCHLAND GMBH & CO. KG, ABBVIE INC.Inventors: Wilhelm Amberg, Jason Brewer, Charles Hutchins, Udo Lange, Yanbin Lao, Huan-Qiu Li, Frauke Pohlki, Anil Vasudevan, Ying Wang, Hongyu Zhao
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Patent number: 9550755Abstract: The present invention provides a compound of formula I: 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: June 27, 2013Date of Patent: January 24, 2017Assignee: NOVARTIS AGInventors: Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
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Patent number: 9550756Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0): wherein R1 represents a substituent, R2 represents a hydrogen atom, or a substituent, R3 represents a hydrogen atom, or a substituent, Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: GrantFiled: October 17, 2014Date of Patent: January 24, 2017Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
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Patent number: 9550757Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).Type: GrantFiled: June 28, 2013Date of Patent: January 24, 2017Assignee: Karyopharm Therapeutics Inc.Inventors: Sharon Shacham, Michael Kauffman, Vincent P. Sandanayaka, Sharon Shechter
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Patent number: 9550758Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.Type: GrantFiled: September 10, 2014Date of Patent: January 24, 2017Assignee: NOVARTIS AGInventors: Sangamesh Badiger, Murali Chebrolu, Konstanze Hurth, Sebastien Jacquier, Rainer Martin Lueoend, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
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Patent number: 9550759Abstract: New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.Type: GrantFiled: November 14, 2014Date of Patent: January 24, 2017Assignee: BIAL—PORTELA & CA, S.A.Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto Dos Santos Ferreira, Patricio Manuel Vieira Araujo Soares Da Silva
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Patent number: 9550760Abstract: The present invention relates generally to the use of compounds to treat a variety of disorders, diseases and pathologic conditions and more specifically to the use of substituted indol-5-ol derivatives to modulate protein kinases and for treating protein kinase-mediated diseases.Type: GrantFiled: March 17, 2014Date of Patent: January 24, 2017Assignee: NantBioScience, Inc.Inventor: Chunlin Tao
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Patent number: 9550761Abstract: 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: GrantFiled: August 21, 2013Date of Patent: January 24, 2017Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Patent number: 9550762Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, and each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.Type: GrantFiled: August 5, 2015Date of Patent: January 24, 2017Assignee: Amgen, Inc.Inventors: Jennifer R. Allen, Albert Amegadzie, Matthew P. Bourbeau, James A. Brown, Jian J. Chen, Yuan Cheng, Michael J. Frohn, Angel Guzman-Perez, Paul E. Harrington, Longbin Liu, Qingyian Liu, Jonathan D. Low, Vu Van Ma, James Manning, Ana Elena Minatti, Thomas T. Nguyen, Nobuko Nishimura, Mark H. Norman, Liping H. Pettus, Alexander J. Pickrell, Wenyuan Qian, Shannon Rumfelt, Robert M. Rzasa, Aaron C. Siegmund, Markian M. Stec, Ryan D. White, Qiufen Xue
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Patent number: 9550763Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect, e.g. a compound of Formula (I): wherein R2 is a hydrogen atom or the like; ring A is five- to seven-cycloalkane or the like; C is a carbon atom; Q1 and Q2 are carbon atoms or the like; R9a and R9b are carbon atoms or the like; R6 is cycloalkyl or the like; R7 is a group represented by the formula: wherein ring D is benzene or the like; carbon atom a and b are carbon atoms; ring B is an aromatic carbocyclic ring or the like; s and s? are 0 or the like; R9 and R9? are halogen or the like, or the like, or its pharmaceutically acceptable salt.Type: GrantFiled: February 8, 2013Date of Patent: January 24, 2017Assignee: SHIONOGI & CO., LTD.Inventors: Hiroyuki Kai, Satoru Tanaka, Yoshiharu Hiramatsu, Azusa Nozu, Ken'ichioh Nakamura
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Patent number: 9550764Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof for use in the treatment of cancer:Type: GrantFiled: August 22, 2013Date of Patent: January 24, 2017Assignee: The Institute of Cancer Research: Royal Cancer HospitalInventors: Keith Jones, Matthew David Cheeseman, Spyridon Linardopoulos, Amir Faisal, Olivier Remi Barbeau, Andrew Kalusa
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Patent number: 9550765Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: GrantFiled: July 28, 2015Date of Patent: January 24, 2017Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Chu-Biao Xue, Yun-Long Li, Hao Feng, Ke Zhang, Wenqing Yao
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Patent number: 9550766Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.Type: GrantFiled: November 6, 2015Date of Patent: January 24, 2017Assignee: Celgene CorporationInventors: George W. Muller, Alexander L. Ruchelman
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Patent number: 9550767Abstract: Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of manufacture and therapeutic uses thereof are described.Type: GrantFiled: January 20, 2016Date of Patent: January 24, 2017Assignee: Forum Pharmaceuticals, Inc.Inventors: Patricia Oliver-Shaffer, Gideon Shapiro, Richard Chesworth, Muneki Kishida, Takayuki Ishige
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Patent number: 9550768Abstract: Compounds, compositions and methods useful for treatment of Flt3-mediated diseases or conditions are provided herewith. Also provided herewith are methods for modulating the receptor protein tyrosine like kinase 3(Flt3).Type: GrantFiled: March 11, 2013Date of Patent: January 24, 2017Assignee: Plexxikon Inc.Inventors: Chao Zhang, Gideon Bollag, Gaston Habets, Jiazhong Zhang, Prabha N. Ibrahim, Guoxian Wu
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Patent number: 9550769Abstract: The invention provides a series of bioactive small molecules that target expanded r(CGG) repeats, termed r(CGG)exp, that causes Fragile X-associated Tremor Ataxia Syndrome (FXTAS). The compound was identified by using information on the chemotypes and RNA motifs that interact. Specifically, 9-hydroxy-5,11-dimethyl-2-(2-(piperidin-1-yl)ethyl)-6H-pyrido[4,3-b]carbazol-2-ium, binds the 5?CGG/3?GGC motifs in r(CGG)exp and disrupts a toxic r(CGG)exp-protein complex. Specifically, dimeric compounds incorporating two 9-hydroxyellipticine analog structures can even more potently bind the 5?CGG/3?GGC motifs in r(CGG)exp and disrupts a toxic r(CGG)exp-protein complex. Structure-activity relationships (SAR) studies determined that the alkylated pyridyl and phenolic side chains are important chemotypes that drive molecular recognition of r(CGG) repeats, such as r(CGG)exp.Type: GrantFiled: August 30, 2013Date of Patent: January 24, 2017Assignee: The Scripps Research InstituteInventors: Matthew D. Disney, Biao Liu, Jessica L. Childs-Disney, Wang-Yong Yang
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Patent number: 9550770Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions containing the same, and methods of use thereof are described. Specifically quinazoline derivatives of Formula Ia: and their uses in modulating kinase activities are disclosed.Type: GrantFiled: August 22, 2014Date of Patent: January 24, 2017Assignee: NeuPharma, Inc.Inventors: Xiangping Qian, Yong-Liang Zhu
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Patent number: 9550771Abstract: Compounds of the formula I or II: or pharmaceutically acceptable salts thereof, wherein R1 is a group of formula (a), (b), (c); (d) or (e): and m, n, X, Y, R1, R2, R3, R4, Rb and Rc are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: GrantFiled: September 10, 2014Date of Patent: January 24, 2017Assignee: Genentech, Inc.Inventors: Benjamin Fauber, Alberto Gobbi
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Patent number: 9550772Abstract: The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders.Type: GrantFiled: December 30, 2013Date of Patent: January 24, 2017Assignee: ORIBASE PHARMAInventors: Gwénaël Cheve, Bénédicte Dayde-Cazals, Bénédicte Fauvel, Cédric Bories, Abdelaziz Yasri
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Patent number: 9550773Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: GrantFiled: April 13, 2015Date of Patent: January 24, 2017Assignee: 3M Innovative Properties CompanyInventors: Doris Stoermer, Joseph F. Dellaria, Jr., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk, Matthew R. Radmer
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Patent number: 9550774Abstract: The present invention provides compounds of the formula (I) or a pharmaceutically acceptable salt thereof. Compounds of the invention are autotaxin inhibitors useful in the treatment of pain associated with osteoarthritis.Type: GrantFiled: April 4, 2014Date of Patent: January 24, 2017Assignee: Eli Lilly and CompanyInventors: Thomas John Bleisch, Robert Anthony Doti, Lance Allen Pfeifer, Bryan Hurst Norman
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Patent number: 9550775Abstract: The invention provides compounds having the general formula: [insert formula (I)] (I) and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.Type: GrantFiled: March 14, 2014Date of Patent: January 24, 2017Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.Inventors: Paul Robert Bichler, Sultan Chowdhury, Shannon Marie Decker, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Brian Safina, Tao Sheng, Shaoyi Sun, Michael Scott Wilson, Alla Yurevna Zenova
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Patent number: 9550776Abstract: A compound represented by formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 represents a group represented by the formula: a group represented by the formula: or a group represented by the formula: and R2 represents a 3-methyltetrahydro-2H-pyran-4-yl group or 4-methoxycyclohexyl group.Type: GrantFiled: April 3, 2014Date of Patent: January 24, 2017Assignee: Eisai R&D Management Co., Ltd.Inventors: Yoshihiko Norimine, Nobuaki Sato, Yuki Ishihara, Kunitoshi Takeda
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Patent number: 9550777Abstract: The present invention provides for compounds of Formula (I) and various embodiments thereof, and compositions comprising compounds of Formula (I) and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6 and R7 have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula (I) as DLK inhibitors and for treating neurodegeneration diseases and disorders.Type: GrantFiled: July 16, 2015Date of Patent: January 24, 2017Assignee: Genentech, Inc.Inventors: Anthony Estrada, Wen Liu, Snahel Patel, Michael Siu
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Patent number: 9550778Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate 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: GrantFiled: October 2, 2015Date of Patent: January 24, 2017Assignee: Vanderbilt UniversityInventors: Kyle A. Emmitte, Craig W. Lindsley, P. Jeffrey Conn, Andrew S. Felts, Katrina A. Smith
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Patent number: 9550779Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.Type: GrantFiled: December 30, 2015Date of Patent: January 24, 2017Assignee: NOVIRA THERAPEUTICS, INC.Inventors: George D. Hartman, Scott Kuduk
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Patent number: 9550780Abstract: The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (VMAT2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.Type: GrantFiled: March 16, 2016Date of Patent: January 24, 2017Assignee: Auspex Pharmaceuticals, Inc.Inventors: Andreas Sommer, Chengzhi Zhang, John Carter, John Arthur, Margaret Bradbury, Thomas Gant, Manouchehr Shahbaz
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Patent number: 9550781Abstract: The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition.Type: GrantFiled: November 14, 2012Date of Patent: January 24, 2017Assignees: Centaurus Biopharma Co., Ltd., Chia Tai Tianqing Pharmaceutical Group Co., Ltd.Inventors: Dengming Xiao, Jijun Li, Yan Zhu, Yuandong Hu, Huting Wang, Zhe Wang, Zanping Wang, Yongheng Wei, Yinghui Sun, Qiong Wu, Hui Zhang, Yong Peng, Fansheng Kong, Ying Sun, Hong Luo, Yongxin Han
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Patent number: 9550782Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.Type: GrantFiled: March 7, 2013Date of Patent: January 24, 2017Assignee: MEDIVATION TECHNOLOGIES, INC.Inventors: Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain, Michael John Green
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Patent number: 9550783Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.Type: GrantFiled: May 19, 2014Date of Patent: January 24, 2017Assignee: MELINTA THERAPEUTICS, INC.Inventors: Jiacheng Zhou, Ashoke Bhattacharjee, Shili Chen, Yi Chen, Jay J. Farmer, Joel A. Goldberg, Roger Hanselmann, Rongliang Lou, Alia Orbin, Adegboyega K. Oyelere, Joseph M. Salvino, Dane M. Springer, Jennifer Tran, Deping Wang, Yusheng Wu
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Patent number: 9550784Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine and imidazo[1,2-a]-pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which may be useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.Type: GrantFiled: July 8, 2013Date of Patent: January 24, 2017Assignee: Beerse Pharmaceutica NVInventors: Laurent Christian L. Leclercq, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Michiel Luc Maria Van Gool
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Patent number: 9550785Abstract: The present invention relates to Compounds of formula (I) and salts thereof: wherein R1 is n-C3-6alkyl; R2 is hydrogen or methyl; R3 is hydrogen or C1-6alkyl, and m is an integer having a value of 0 to 3; are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: GrantFiled: November 18, 2013Date of Patent: January 24, 2017Assignee: GlaxoSmithKline LLCInventors: Diane Mary Coe, Stephen Allan Smith
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Patent number: 9550786Abstract: The present invention is directed to 4-fluoropiperidine 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: January 13, 2014Date of Patent: January 24, 2017Assignee: MERCK SHARP & DOHME CORP.Inventors: Andrew Cooke, Scott D. Kuduk, Craig Stump, Peter Williams
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Patent number: 9550787Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: GrantFiled: January 7, 2016Date of Patent: January 24, 2017Assignee: ImmunoGen, Inc.Inventors: Wei Li, Nathan Elliott Fishkin, Robert Yongxin Zhao, Michael Louis Miller, Ravi V.J. Chari
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Patent number: 9550788Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.Type: GrantFiled: July 24, 2014Date of Patent: January 24, 2017Assignee: SANOFIInventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
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Patent number: 9550789Abstract: Provided herein are halogenated indole and benzofuran derivatives of isoquinuclidene and intermediates thereto, and processes, preferably enantioselective processes, for preparing such derivatives including processes for preparing (?) and (+) noribogaine, in substantially enantiomerically pure forms.Type: GrantFiled: June 16, 2015Date of Patent: January 24, 2017Assignee: DEMERX, INC.Inventors: Robert M. Moriarty, Mark Kinch
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Patent number: 9550790Abstract: The invention relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as PI-3 kinase.Type: GrantFiled: September 30, 2013Date of Patent: January 24, 2017Assignee: SignalRx Pharmaceuticals, Inc.Inventors: Guillermo A. Morales, Kevin Weber, Jessica Newblom, Joseph R. Garlich
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Patent number: 9550791Abstract: The present invention relates to polymers comprising a repeating unit of the formula (I), and their use as organic semiconductor in organic electronic devices, especially in organic photovoltaics and photodiodes, or in a device containing a diode and/or an organic field effect transistor. The polymers according to the invention can have excellent solubility in organic solvents and excellent film-forming properties. In addition, high efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the polymers according to the invention are used in organic field effect transistors, organic photovoltaics (solar cells) and photodiodes.Type: GrantFiled: December 2, 2013Date of Patent: January 24, 2017Assignee: BASF SEInventors: Matthias Welker, Mathieu G. R. Turbiez, Natalia Chebotareva, Hans Jürg Kirner
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Patent number: 9550792Abstract: The present invention relates to the field of medicinal chemistry, and in particular relates to 4-(five-membered heterocyclic pyrimidine/pyridine substituted) amino-1H-3-pyrazolecarboxamide derivatives, the preparation method thereof, pharmaceutical compositions containing these compounds and the medicinal use thereof, especially as protein kinase inhibitors for anti-tumor use.Type: GrantFiled: January 7, 2014Date of Patent: January 24, 2017Assignee: SHANGHAI FOSUN PHARMACEUTICAL DEVELOPMENT CO., LTD.Inventors: Tao Lu, Yue Wang, Yadong Chen, Yi Lu, Zhanwei Wang, Qiaomei Jin, Taotao Yang, Guowu Lin, Qinglong Guo, Li Zhao
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Patent number: 9550793Abstract: The present disclosure relates to a series of spirocyclic compounds of formula (I), their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates, hydrates, N-Oxides, Co crystals and formulations thereof. The disclosure also relates to process of preparation of these spirocyclic compounds. These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of acyl CoA diacyl glycerol acyltransferase 1 (DGAT1).Type: GrantFiled: October 1, 2013Date of Patent: January 24, 2017Assignee: Advinus Therapeutics LimitedInventors: Summon Koul, Debnath Bhuniya, Kasim Mookhtiar, Sandeep Bhosale, Suresh Kurhade, Keshav Naik, Ravikumar Velayutham, Videsh Salunkhe
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Patent number: 9550794Abstract: The present invention relates to compounds of formula (I) Wherein R1, R2, R3, R4, L and Z have the meaning given in claim 1, and their use in the prophylaxis and treatment of diseases.Type: GrantFiled: February 7, 2014Date of Patent: January 24, 2017Assignee: MERCK PATENT GmbHInventors: Catherine Jorand-Lebrun, Santosh Kulkarni, Serge Christmann-Franck
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Patent number: 9550795Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: December 4, 2014Date of Patent: January 24, 2017Assignee: Pfizer Inc.Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Christopher John Helal, Brian Thomas O'Neill