Patents Issued in October 25, 2016
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Patent number: 9475776Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.Type: GrantFiled: April 1, 2015Date of Patent: October 25, 2016Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin
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Patent number: 9475777Abstract: Porous partially fluorinated materials which bind aliphatic and aromatic hydrocarbons, fluorocarbons and freons with high weight adsorption capacities are provided. Such compounds may be used in separation of materials by exclusion such as selective separation of isomers of xylene.Type: GrantFiled: May 8, 2015Date of Patent: October 25, 2016Assignee: UNIVERSITY OF HOUSTON SYSTEMInventors: Ognjen {hacek over (S)} Miljanić, Teng-Hao Chen, Ilya Popov, Watchareeya Kaveevivitchai, Olafs Daugulis
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Patent number: 9475778Abstract: Sulfate of 5-hydroxy-1H-imidazole-4-carboxamide has such characteristics as suppressed blue coloring, high purity, low hygroscopic property, and superior storage stability, and thus is useful as an active pharmaceutical ingredient of drugs.Type: GrantFiled: June 3, 2015Date of Patent: October 25, 2016Assignee: FUJIFILM CorporationInventors: Tomoyuki Tanaka, Yu Koseki
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Patent number: 9475779Abstract: Substituted bicyclic dihydropyrimidinones of formula 1 which are inhibitors of neutrophil elastase and useful as medicaments for the treatment of, inter alia, COPD.Type: GrantFiled: July 27, 2015Date of Patent: October 25, 2016Assignee: Boehringer Ingelheim International GmbHInventors: Thorsten Oost, Ralf Anderskewitz, Christian Gnamm, Holger Hoesch, Gerd Morschhaeuser, Stefan Peters, Uwe Joerg Ries
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Patent number: 9475780Abstract: The invention relates to a process for the synthesis of cyclic alkylene ureas comprising reacting in the presence of a basic catalyst, a difunctional amine A having two primary amino groups, and an aliphatic organic carbonate component C selected from the group consisting of dialkyl carbonates CD and of alkylene carbonates CA, wherein the ratio of the amount of substance Ji(—NH2) of primary amino groups —NH2 in the difunctional amine A to the sum M(C) of the amount of substance n(CD) of carbonate groups of a dialkyl carbonate CD and the amount of substance n(CA) of carbonate groups in an alkylene carbonate CA, is at least more than 2, and to the product obtained by this process.Type: GrantFiled: July 19, 2012Date of Patent: October 25, 2016Assignee: Allnex IP S.ar.L.Inventors: Ram Gupta, Irina Kobylanska, Urvee Treasurer, Lawrence Flood
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Patent number: 9475781Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: July 31, 2015Date of Patent: October 25, 2016Assignee: Rigel Pharmaceuticals, Inc.Inventors: Matthew Duncton, Somasekhar Bhamidipati, Jiaxin Yu, Ihab Darwish, Rajinder Singh
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Patent number: 9475782Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.Type: GrantFiled: November 21, 2012Date of Patent: October 25, 2016Assignee: ABBVIE DEUTSCHLAND GMBH & CO. KGInventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling
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Patent number: 9475783Abstract: The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.Type: GrantFiled: March 21, 2013Date of Patent: October 25, 2016Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
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Patent number: 9475784Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein R1 and R2 are independently hydrogen, or —CH3; or R1 and R2 can join together in a ring by adding —(CH2)4—; R3 is hydrogen or C1-C3 alkyl; Y and Z are independently a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, —C?OC1-4alkyl, —SO2C1-4alkyl, and C2-C4 alkynyl; A is selected from the group of phenyl, benzyl, oxazolyl, thiazolyl, isoxazolyl, imidazolyl, pyrazolyl, pyridyl, pyrimidinyl, and pyrazinyl groups which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, hydroxyC1-6 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is —NHCO— or is a single bond; and L and ZType: GrantFiled: December 19, 2012Date of Patent: October 25, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Jason M. Guernon
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Patent number: 9475785Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (“A?”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's disease, are also disclosed.Type: GrantFiled: February 27, 2015Date of Patent: October 25, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Jeffrey A. Misiaszek, Guoqing Li
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Patent number: 9475786Abstract: A method for selective hydrogenation of furan-2,5-dialdehyde (DFF) into 2,5-di(hydroxymethyl)furan (DHMF) and into 2,5-di(hydroxymethyl)tetrahydrofuran (DHMTHF). In relation to the prior art, which uses C6 sugars or 5-hydroxymethyl furaldehyde (5-HMF) as raw materials, the method can be performed at low temperatures (lower than 120° C., preferably 80° C.), while consuming low amounts of catalyst relative to the initial reagent (in particular less than 5%, preferably less than 2% relative to the weight of the reagent). The heterogeneous catalyst used can also be recycled from one reaction to another. Finally, the choice of experimental conditions enables the selective formation of DHMF or DHMTHF.Type: GrantFiled: September 26, 2013Date of Patent: October 25, 2016Assignee: ROQUETTE FRERESInventors: Mathias Ibert, Flora Chambon, Laurent Dambrine
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Patent number: 9475787Abstract: A process for the production of furan derivatives from carbohydrates in the presence of an acidic catalyst, characterized in that N-methylpyrrolidone is used as a solvent and that the acidic catalyst is homogeneous.Type: GrantFiled: September 2, 2013Date of Patent: October 25, 2016Assignee: Annikki GMBHInventors: Marko Mihovilovic, Michael Schön, Johanna Hölbling
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Patent number: 9475788Abstract: The invention is directed to a compound of formula I, a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing a compound of formula I, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria.Type: GrantFiled: October 21, 2015Date of Patent: October 25, 2016Assignee: MediSynergics, LLCInventors: Dennis Michael Godek, Harry Ralph Howard
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Patent number: 9475789Abstract: The preset invention relates to a method for treating inflammation comprising administering a subject in need thereof with a therapeutically effective amount of polyenylpyrrole derivatives of formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 2, 2014Date of Patent: October 25, 2016Assignee: WELLHEAD BIOLOGICAL TECHNOLOGY CORP.Inventor: Yu-Chieh Lee
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Patent number: 9475790Abstract: A method for preparing lactide from recovered polylactic acid, the method including the following steps: A. pretreating the recovered polylactic acid; B. extruding the treated polylactic acid from a twin screw extruder to yield a polylactic acid melt, and introducing the polylactic acid melt to a pre-depolymerization kettle; C. carrying out a chain scission reaction to break molecular chains in the polylactic acid melt and to decrease the number-average molecular weight of the polylactic acid melt to below 5000; D. conducting depolymerization reaction to yield a crude lactide; and E. purifying the crude lactide and crystallizing the purified lactide.Type: GrantFiled: November 5, 2014Date of Patent: October 25, 2016Assignee: XIAOGAN ESUN MATERIAL CO., LTD.Inventors: Yihu Yang, Jie Xu
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Patent number: 9475791Abstract: Disclosed herein are methods for treatment of estrogen-related medical disorders. The methods of treatment may comprise administering to a subject in need of such treatment a composition comprising a therapeutically effective amount of at least one compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 24, 2013Date of Patent: October 25, 2016Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Gregory R. Thatcher, Debra Tonetti, Mary Ellen Molloy, Bradley Michalsen, Zihui Qin
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Patent number: 9475792Abstract: The present invention describes indenofluorene derivatives of the general formula I, II, III or IV having emitting and hole-transporting properties, in particular for use in the emission and/or charge-transport layer of electroluminescent devices. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising same.Type: GrantFiled: December 22, 2009Date of Patent: October 25, 2016Assignee: Merck Patent GmbHInventors: Amir Hossain Parham, Christof Pflumm, Arne Buesing, Holger Heil, Philipp Stoessel
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Patent number: 9475793Abstract: The present invention relates in part to chemical compounds, and methods for producing these compounds. The compounds may also be incorporated into compositions to enhance quit rates or reduce relapse in smoking cessation and further in treating nicotine-related dependence.Type: GrantFiled: March 1, 2016Date of Patent: October 25, 2016Assignee: Pfizer Inc.Inventors: Janice Ethel Sieser, Robert Alan Singer
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Patent number: 9475794Abstract: A process for the preparation of a Form I crystalline polymorph of imidacloprid, including: (i) dissolving imidacloprid in an appropriate amount of aqueous solvent or mixture of solvents to obtain an aqueous solution; (ii) cooling the aqueous solution slowly, thereby forming crystals of polymorph Form I of imidacloprid; (iii) isolating the crystals. A process for the preparation of a Form II crystalline polymorph of imidacloprid, comprising: dissolving imidacloprid in an appropriate amount of non-aqueous solvent or mixture of non-aqueous solvents to obtain a non-aqueous solution; (ii) cooling the solution rapidly, thereby forming crystals of polymorph Form II of imidacloprid; (iii) isolating the crystals.Type: GrantFiled: November 12, 2015Date of Patent: October 25, 2016Assignee: ROTAM AGROCHEM INTERNATIONAL COMPANY LIMITEDInventors: James Timothy Bristow, Yifan Wu
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Patent number: 9475795Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: (I) in which m, n, W, X, Y, Z, R1, R2, R3 and R4 are as defined in the specification, for use in the treatment or prevention of a diseases o conition mediated by a prokineticin, such as psychiatric and neurological conditions.Type: GrantFiled: May 29, 2013Date of Patent: October 25, 2016Assignee: Takeda Pharmaceutical Company LimitedInventors: Colm Carroll, Anne Goldby, Martin Teall
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Patent number: 9475796Abstract: There are provided compounds of formula (I) which are inhibitors of the family of p38 mitogen-activated protein kinase enzymes, and to their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.Type: GrantFiled: October 3, 2012Date of Patent: October 25, 2016Assignee: Respivert LimitedInventors: Kazuhiro Ito, Catherine Elisabeth Charron, John King-Underwood, Stuart Thomas Onions, Alistair Ian Longshaw
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Patent number: 9475797Abstract: This invention relates to a novel phenyl triazole derivative, pharmaceutical compositions containing this compound, and methods of treatment therewith. The compound of the invention is in particular considered useful for the treatment of central nervous system diseases and disorders which are responsive to modulation of GABAA receptors containing the ?5 subunit.Type: GrantFiled: June 25, 2013Date of Patent: October 25, 2016Assignee: Saniona A/SInventors: Janus Schreiber Larsen, Magnus Gustafsson, Carsten Jessen
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Patent number: 9475798Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: GrantFiled: December 9, 2015Date of Patent: October 25, 2016Assignee: Genentech, Inc.Inventors: Steven P. Govek, Mehmet Kahraman, Nicholas D. Smith, Jeffrey H. Hager, Edna Chow Maneval
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Patent number: 9475799Abstract: The present invention relates to a novel synthetic route for the preparation of raltegravir and pharmaceutically acceptable salts, starting from 2-amino-2-methylpropanenitrile and oxadiazole carbonyl chloride, through the formation of a pyrimidinone intermediate of formula (V).Type: GrantFiled: June 28, 2016Date of Patent: October 25, 2016Assignee: Emcure Pharmaceuticals LimitedInventors: Mukund Keshav Gurjar, Swapnil Panditrao Sonawane, Golakchandra Sudarshan Maikap, Gulabrao Dagadu Patil, Shivnath Bhaupatil Shinde, Pankaj Shalikrao, Samit Satish Mehta
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Patent number: 9475800Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.Type: GrantFiled: March 9, 2015Date of Patent: October 25, 2016Assignee: VERNALIS (R&D) LTD.Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
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Patent number: 9475801Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.Type: GrantFiled: July 8, 2015Date of Patent: October 25, 2016Assignee: ALLERGAN, INC.Inventors: Xialing Guo, Zhen Zhu
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Patent number: 9475802Abstract: Inhibitors of viral replication of formula (I), their process of preparation and their therapeutical uses. The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.Type: GrantFiled: October 11, 2013Date of Patent: October 25, 2016Assignee: LABORATOIRE BIODIMInventors: Richard Benarous, Francis Chevreuil, Benoit Ledoussal, Sophie Chasset, Frédéric Le Strat
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Patent number: 9475803Abstract: The present invention includes compounds having structural formula (Ia): or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.Type: GrantFiled: February 19, 2014Date of Patent: October 25, 2016Assignee: Senomyx, Inc.Inventors: Sara Adamski-Werner, Vincent Darmohusodo, Catherine Tachdjian, Donald Karanewsky, Goran Petrovic, Rachel Kimmich, Joseph Fotsing
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Patent number: 9475804Abstract: Conjugates of an immune response modifier, a linker, and an antigen are disclosed. The linker is represented by formula (I): wherein A is CH or N, p is in a range from 1 to 50, R? is a bond or -alkylene-O—, R? is alkylene that is optionally interrupted or terminated with one or more amide or ether groups, and E is an amine- or thiol-reactive group. Pharmaceutical compositions containing the compound or the conjugate, methods of making a conjugate, and methods of use of the compounds or conjugates as immunomodulators for inducing cytokine biosynthesis in an animal and for vaccinating an animal are also disclosed. An antigen modified by the linker is also disclosed.Type: GrantFiled: June 1, 2012Date of Patent: October 25, 2016Assignee: 3M Innovative Properties CompanyInventor: Paul D. Wightman
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Patent number: 9475805Abstract: The invention provides a method of activating PPAR ? and a method of treating or preventing a disease associated with PPAR ? by administering a tricyclic compound having a PPAR ? agonist activity, which is represented by the formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:Type: GrantFiled: May 26, 2015Date of Patent: October 25, 2016Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Arata Yanagisawa, Keiji Uehara, Masahiro Matsubara, Kimihisa Ueno, Michihiko Suzuki, Takeshi Kuboyama, Keisuke Yamamoto, Tomohiro Tamura
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Patent number: 9475806Abstract: The present invention provides a compound of formula (I): wherein X is N or CH, Y is NH, O or S, methods for manufacturing these compounds, and their uses as Factor B inhibitors for the treatment of conditions and diseases associated with complement alternative pathway activation such as age-related macular degeneration, diabetic retinopathy and related ophthalmic diseases. The present invention further provides pharmaceutical compositions and combinations of pharmacologically active agents.Type: GrantFiled: March 13, 2014Date of Patent: October 25, 2016Assignee: Novartis AGInventors: Christopher Michael Adams, Charles Babu, Michael Paul Capparelli, Jian Ding, Takeru Ehara, Keith Jendza, Nan Ji, Rajeshri Ganesh Karki, Toshio Kawanami, Liang Xue, Nello Mainolfi, James J. Powers, Michael H. Serrano-Wu, Chun Zhang
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Patent number: 9475807Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: GrantFiled: September 8, 2015Date of Patent: October 25, 2016Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 9475808Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: GrantFiled: September 15, 2015Date of Patent: October 25, 2016Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.Inventors: Hervé Geneste, Michael Ochse, Karla Drescher, Berthold Behl, Loic Laplanche, Jürgen Dinges, Clarissa Jakob
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Patent number: 9475809Abstract: The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.Type: GrantFiled: July 21, 2014Date of Patent: October 25, 2016Assignee: Bayer Pharma AktiengesellschaftInventors: Susanne Röhrig, Alexander Hillisch, Julia Straβburger, Stefan Heitmeier, Martina Victoria Schmidt, Karl-Heinz Schlemmer, Anja Buchmüller, Christoph Gerdes, Henrik Teller, Martina Schäfer, Adrian Tersteegen
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Patent number: 9475810Abstract: The present invention relates to compositions and methods of using free radical scavengers with reduced 1O2 generation. In certain embodiments, these compositions and methods of use relate to fullerene-derived ketolactams and fullerene-derived ketolactam derivatives, fullerene derivatives, and/or fullerenes. In yet other embodiments, the invention relates to cosmetic or dermatological compositions comprising said free radical scavengers with reduced 1O2 generation.Type: GrantFiled: November 11, 2013Date of Patent: October 25, 2016Assignee: Solenne BVInventors: David F. Kronholm, Alexander B. Sieval, Jan C. Hummelen
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Patent number: 9475811Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.Type: GrantFiled: December 3, 2014Date of Patent: October 25, 2016Assignee: Novartis AGInventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas Troxler, Konstanze Hurth, Mathias Frederiksen
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Patent number: 9475812Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.Type: GrantFiled: June 4, 2012Date of Patent: October 25, 2016Assignee: Xuanzhu Pharma Co., Ltd.Inventors: Frank Wu, Yan Zhang
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Patent number: 9475813Abstract: To provide a novel tricyclic pyrrolopyridine compound having a JAK inhibitory activity and useful for prevention, treatment and/or improvement of particularly autoimmune diseases, inflammatory diseases and allergic diseases. A novel tricyclic pyrrolopyridine compound represented by the formula (I), a tautomer or pharmaceutically acceptable salt of the compound or a solvate thereof: wherein the respective substituents are defined in detail in the specification, and R1 is a C1-6 alkyl group or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or the like, the ring A is C3-11 cycloalkane or the like, L1 is a C1-6 alkylene group or the like, and R4 is NRaRb or the like.Type: GrantFiled: February 5, 2014Date of Patent: October 25, 2016Assignee: Nissan Chemical Industries, Ltd.Inventors: Keiji Takahashi, Tsuneo Watanabe, Keishi Hayashi, Kazunori Kurihara, Takanori Nakamura, Akio Yamamoto, Takuya Nishimura, Toshihiko Kamiyama, Yuuki Hidaka
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Patent number: 9475814Abstract: The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.Type: GrantFiled: October 3, 2012Date of Patent: October 25, 2016Assignee: Euroscreen S.A.Inventors: Hamid R. Hoveyda, Guillaume Dutheuil, Graeme L. Fraser, Marie-Odile Roy, Mohamed El Bousmaqui, Frederic Batt
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Patent number: 9475815Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.Type: GrantFiled: February 20, 2013Date of Patent: October 25, 2016Assignee: BAYER INTELLETUAL PROPERTY GMBHInventors: Mario Lobell, Walter Hübsch, Hartmut Schirok, Mélanie Héroult, Dirk Brohm, Marie-Pierre Collin, Sylvia Grünewald, Klemens Lustig, Ulf Bömer, Verena Voehringer, Niels Lindner
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Patent number: 9475816Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein L, R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.Type: GrantFiled: September 6, 2013Date of Patent: October 25, 2016Assignee: Takeda Pharmaceutical Company LimitedInventors: Zacharia Cheruvallath, Mallareddy Komandla, John David Lawson, Christopher McBride, Mingnam Tang
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Patent number: 9475817Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.Type: GrantFiled: December 20, 2013Date of Patent: October 25, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Upender Velaparthi, Chetan Padmakar Darne, Dharmpal S. Dodd, Peiying Liu, Christopher P. Mussari, Mark D. Wittman, Selvakumar Kumaravel, Dibakar Mullick
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Patent number: 9475818Abstract: The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them.Type: GrantFiled: August 21, 2015Date of Patent: October 25, 2016Assignee: RHIZEN PHARMACEUTICALS SAInventors: Swaroop Kumar V. S. Vakkalanka, Meyyappan Muthuppalaniappan, Dhanapalan Nagarathnam
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Patent number: 9475819Abstract: The present invention is directed to compounds of Formula I: wherein ring A is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; R1 is H, alkyl, alkoxy, hydroxyalkylene, OH, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; R2 is H, alkyl, alkoxy, hydroxyalkylene, or halo; Z is NH, N-alkyl, or O; R5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I.Type: GrantFiled: May 21, 2015Date of Patent: October 25, 2016Assignee: Janssen Pharmaceutica NVInventors: Heather R. Coate, Curt A. Dvorak, Terry P. Lebold, Cathy Preville, Brock T. Shireman
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Patent number: 9475820Abstract: A series of imidazo[1,2-a]pyrazine derivatives, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.Type: GrantFiled: July 5, 2013Date of Patent: October 25, 2016Assignee: UCB Biopharma SPRLInventors: Jonathan Mark Bentley, Daniel Christopher Brookings, Julien Alistair Brown, Thomas Paul Cain, Laura Jane Gleave, Alexander Heifetz, Victoria Elizabeth Jackson, Craig Johnstone, Deborah Leigh, James Madden, John Robert Porter, Matthew Duncan Selby, Zhaoning Zhu
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Patent number: 9475821Abstract: Provided are a process for preparation of darunavir or solvates or a pharmaceutically acceptable salt thereof substantially free of bisfuranyl impurities and a process for preparation of amorphous darunavir using the darunavir propionate solvate.Type: GrantFiled: July 23, 2013Date of Patent: October 25, 2016Assignee: Laurus Labs Private LimitedInventors: Kameswar R. Chivukula, Venkata R. Murthy, Venkata S. Indukuri, Seeta R. Gorantla
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Patent number: 9475822Abstract: The present invention provides a novel amide derivative having a matrix metalloproteinase inhibitory activity, and useful as a pharmaceutical agent, which is a compound represented by the formula (I) wherein ring A is an optionally substituted, nitrogen containing heterocycle, ring B is an optionally substituted monocyclic homocycle or an optionally substituted monocyclic heterocycle, Z is N or NR1 (R1 is a hydrogen atom or an optionally substituted hydrocarbon group), is a single bond or a double bond, R2 is a hydrogen atom or an optionally substituted hydrocarbon group, X is an optionally substituted spacer having 1 to 6 atoms, ring C is (1) an optionally substituted homocycle or (2) an optionally substituted heterocycle other than a ring represented by (II) (X? is S, O, SO, or CH2), and at least one of ring B and ring C has substituent(s), provided that N-{(1S,2R)-1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]2 hydroxypropyl} 5,6 dimethyl 4 oxo 1,4 dihydrothieno[2,3-d]pyrimidine-2-carboxamide is excluded,Type: GrantFiled: July 29, 2015Date of Patent: October 25, 2016Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Terauchi, Hiroshi Nara, Hideyuki Oki, Kenjiro Sato
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Patent number: 9475823Abstract: The present application relates to methods for the preparation of morphine derivatives. In particular, the present application relates to methods for the preparation of hydromorphone from oripavine and oripavine from thebaine.Type: GrantFiled: February 6, 2015Date of Patent: October 25, 2016Inventors: Tomas Hudlicky, Mary Ann Endoma-Arias, Brennan Augusta Murphy, Ivan Snajdr, Ales Machara
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Patent number: 9475824Abstract: Disclosed are fused pyrimidine compounds having scaffolds composed of left and right rings, the left ring being a saturated carbocyclic or heterocyclic ring and the right ring being a pyrimidine ring. The left saturated ring is fused to the pyrimidine ring at the 5 and 6 carbons of the pyrimidine. The saturated ring may be 5 or 6 members in size and may be all carbon or may contain a single oxygen, sulfur or nitrogen atom as one of the non-fused members of the ring. The pyrimidine ring is substituted at the two position by a 5:6 bicyclic aromatic heterocycle such as indole, benzimidazole or benzopyrazole and at the four position by an aryl methyl amino group. The 5:6 bicyclic aromatic heterocycle is substituted at its 2 position by hydrogen or an aliphatic or functional aliphatic group and at the 4 position by a functional group as described herein. The aryl methyl amino group may be aminobenzyl or aminomethyl-substituted phenyl.Type: GrantFiled: July 19, 2013Date of Patent: October 25, 2016Assignee: Cleave Biosciences, Inc.Inventors: Han-Jie Zhou, Francesco Parlati, David Wustrow
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Patent number: 9475825Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: GrantFiled: September 8, 2015Date of Patent: October 25, 2016Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood