Patents Issued in October 25, 2016
  • Patent number: 9475776
    Abstract: 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: Grant
    Filed: April 1, 2015
    Date of Patent: October 25, 2016
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin
  • Patent number: 9475777
    Abstract: 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: Grant
    Filed: May 8, 2015
    Date of Patent: October 25, 2016
    Assignee: UNIVERSITY OF HOUSTON SYSTEM
    Inventors: Ognjen {hacek over (S)} Miljanić, Teng-Hao Chen, Ilya Popov, Watchareeya Kaveevivitchai, Olafs Daugulis
  • Patent number: 9475778
    Abstract: 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: Grant
    Filed: June 3, 2015
    Date of Patent: October 25, 2016
    Assignee: FUJIFILM Corporation
    Inventors: Tomoyuki Tanaka, Yu Koseki
  • Patent number: 9475779
    Abstract: Substituted bicyclic dihydropyrimidinones of formula 1 which are inhibitors of neutrophil elastase and useful as medicaments for the treatment of, inter alia, COPD.
    Type: Grant
    Filed: July 27, 2015
    Date of Patent: October 25, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thorsten Oost, Ralf Anderskewitz, Christian Gnamm, Holger Hoesch, Gerd Morschhaeuser, Stefan Peters, Uwe Joerg Ries
  • Patent number: 9475780
    Abstract: 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: Grant
    Filed: July 19, 2012
    Date of Patent: October 25, 2016
    Assignee: Allnex IP S.ar.L.
    Inventors: Ram Gupta, Irina Kobylanska, Urvee Treasurer, Lawrence Flood
  • Patent number: 9475781
    Abstract: 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: Grant
    Filed: July 31, 2015
    Date of Patent: October 25, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Matthew Duncton, Somasekhar Bhamidipati, Jiaxin Yu, Ihab Darwish, Rajinder Singh
  • Patent number: 9475782
    Abstract: 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: Grant
    Filed: November 21, 2012
    Date of Patent: October 25, 2016
    Assignee: ABBVIE DEUTSCHLAND GMBH & CO. KG
    Inventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling
  • Patent number: 9475783
    Abstract: 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: Grant
    Filed: March 21, 2013
    Date of Patent: October 25, 2016
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
  • Patent number: 9475784
    Abstract: 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 Z
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: October 25, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Jason M. Guernon
  • Patent number: 9475785
    Abstract: 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: Grant
    Filed: February 27, 2015
    Date of Patent: October 25, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Jeffrey A. Misiaszek, Guoqing Li
  • Patent number: 9475786
    Abstract: 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: Grant
    Filed: September 26, 2013
    Date of Patent: October 25, 2016
    Assignee: ROQUETTE FRERES
    Inventors: Mathias Ibert, Flora Chambon, Laurent Dambrine
  • Patent number: 9475787
    Abstract: 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: Grant
    Filed: September 2, 2013
    Date of Patent: October 25, 2016
    Assignee: Annikki GMBH
    Inventors: Marko Mihovilovic, Michael Schön, Johanna Hölbling
  • Patent number: 9475788
    Abstract: 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: Grant
    Filed: October 21, 2015
    Date of Patent: October 25, 2016
    Assignee: MediSynergics, LLC
    Inventors: Dennis Michael Godek, Harry Ralph Howard
  • Patent number: 9475789
    Abstract: 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: Grant
    Filed: April 2, 2014
    Date of Patent: October 25, 2016
    Assignee: WELLHEAD BIOLOGICAL TECHNOLOGY CORP.
    Inventor: Yu-Chieh Lee
  • Patent number: 9475790
    Abstract: 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: Grant
    Filed: November 5, 2014
    Date of Patent: October 25, 2016
    Assignee: XIAOGAN ESUN MATERIAL CO., LTD.
    Inventors: Yihu Yang, Jie Xu
  • Patent number: 9475791
    Abstract: 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: Grant
    Filed: October 24, 2013
    Date of Patent: October 25, 2016
    Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Gregory R. Thatcher, Debra Tonetti, Mary Ellen Molloy, Bradley Michalsen, Zihui Qin
  • Patent number: 9475792
    Abstract: 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: Grant
    Filed: December 22, 2009
    Date of Patent: October 25, 2016
    Assignee: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Christof Pflumm, Arne Buesing, Holger Heil, Philipp Stoessel
  • Patent number: 9475793
    Abstract: 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: Grant
    Filed: March 1, 2016
    Date of Patent: October 25, 2016
    Assignee: Pfizer Inc.
    Inventors: Janice Ethel Sieser, Robert Alan Singer
  • Patent number: 9475794
    Abstract: 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: Grant
    Filed: November 12, 2015
    Date of Patent: October 25, 2016
    Assignee: ROTAM AGROCHEM INTERNATIONAL COMPANY LIMITED
    Inventors: James Timothy Bristow, Yifan Wu
  • Patent number: 9475795
    Abstract: 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: Grant
    Filed: May 29, 2013
    Date of Patent: October 25, 2016
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Colm Carroll, Anne Goldby, Martin Teall
  • Patent number: 9475796
    Abstract: 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: Grant
    Filed: October 3, 2012
    Date of Patent: October 25, 2016
    Assignee: Respivert Limited
    Inventors: Kazuhiro Ito, Catherine Elisabeth Charron, John King-Underwood, Stuart Thomas Onions, Alistair Ian Longshaw
  • Patent number: 9475797
    Abstract: 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: Grant
    Filed: June 25, 2013
    Date of Patent: October 25, 2016
    Assignee: Saniona A/S
    Inventors: Janus Schreiber Larsen, Magnus Gustafsson, Carsten Jessen
  • Patent number: 9475798
    Abstract: 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: Grant
    Filed: December 9, 2015
    Date of Patent: October 25, 2016
    Assignee: Genentech, Inc.
    Inventors: Steven P. Govek, Mehmet Kahraman, Nicholas D. Smith, Jeffrey H. Hager, Edna Chow Maneval
  • Patent number: 9475799
    Abstract: 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: Grant
    Filed: June 28, 2016
    Date of Patent: October 25, 2016
    Assignee: Emcure Pharmaceuticals Limited
    Inventors: Mukund Keshav Gurjar, Swapnil Panditrao Sonawane, Golakchandra Sudarshan Maikap, Gulabrao Dagadu Patil, Shivnath Bhaupatil Shinde, Pankaj Shalikrao, Samit Satish Mehta
  • Patent number: 9475800
    Abstract: 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: Grant
    Filed: March 9, 2015
    Date of Patent: October 25, 2016
    Assignee: VERNALIS (R&D) LTD.
    Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
  • Patent number: 9475801
    Abstract: 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: Grant
    Filed: July 8, 2015
    Date of Patent: October 25, 2016
    Assignee: ALLERGAN, INC.
    Inventors: Xialing Guo, Zhen Zhu
  • Patent number: 9475802
    Abstract: 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: Grant
    Filed: October 11, 2013
    Date of Patent: October 25, 2016
    Assignee: LABORATOIRE BIODIM
    Inventors: Richard Benarous, Francis Chevreuil, Benoit Ledoussal, Sophie Chasset, Frédéric Le Strat
  • Patent number: 9475803
    Abstract: 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: Grant
    Filed: February 19, 2014
    Date of Patent: October 25, 2016
    Assignee: Senomyx, Inc.
    Inventors: Sara Adamski-Werner, Vincent Darmohusodo, Catherine Tachdjian, Donald Karanewsky, Goran Petrovic, Rachel Kimmich, Joseph Fotsing
  • Patent number: 9475804
    Abstract: 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: Grant
    Filed: June 1, 2012
    Date of Patent: October 25, 2016
    Assignee: 3M Innovative Properties Company
    Inventor: Paul D. Wightman
  • Patent number: 9475805
    Abstract: 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: Grant
    Filed: May 26, 2015
    Date of Patent: October 25, 2016
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Arata Yanagisawa, Keiji Uehara, Masahiro Matsubara, Kimihisa Ueno, Michihiko Suzuki, Takeshi Kuboyama, Keisuke Yamamoto, Tomohiro Tamura
  • Patent number: 9475806
    Abstract: 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: Grant
    Filed: March 13, 2014
    Date of Patent: October 25, 2016
    Assignee: Novartis AG
    Inventors: 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
  • Patent number: 9475807
    Abstract: 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: Grant
    Filed: September 8, 2015
    Date of Patent: October 25, 2016
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 9475808
    Abstract: 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: Grant
    Filed: September 15, 2015
    Date of Patent: October 25, 2016
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Hervé Geneste, Michael Ochse, Karla Drescher, Berthold Behl, Loic Laplanche, Jürgen Dinges, Clarissa Jakob
  • Patent number: 9475809
    Abstract: 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: Grant
    Filed: July 21, 2014
    Date of Patent: October 25, 2016
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Susanne Röhrig, Alexander Hillisch, Julia Straβburger, Stefan Heitmeier, Martina Victoria Schmidt, Karl-Heinz Schlemmer, Anja Buchmüller, Christoph Gerdes, Henrik Teller, Martina Schäfer, Adrian Tersteegen
  • Patent number: 9475810
    Abstract: 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: Grant
    Filed: November 11, 2013
    Date of Patent: October 25, 2016
    Assignee: Solenne BV
    Inventors: David F. Kronholm, Alexander B. Sieval, Jan C. Hummelen
  • Patent number: 9475811
    Abstract: 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: Grant
    Filed: December 3, 2014
    Date of Patent: October 25, 2016
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas Troxler, Konstanze Hurth, Mathias Frederiksen
  • Patent number: 9475812
    Abstract: 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: Grant
    Filed: June 4, 2012
    Date of Patent: October 25, 2016
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Frank Wu, Yan Zhang
  • Patent number: 9475813
    Abstract: 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: Grant
    Filed: February 5, 2014
    Date of Patent: October 25, 2016
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Keiji Takahashi, Tsuneo Watanabe, Keishi Hayashi, Kazunori Kurihara, Takanori Nakamura, Akio Yamamoto, Takuya Nishimura, Toshihiko Kamiyama, Yuuki Hidaka
  • Patent number: 9475814
    Abstract: 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: Grant
    Filed: October 3, 2012
    Date of Patent: October 25, 2016
    Assignee: Euroscreen S.A.
    Inventors: Hamid R. Hoveyda, Guillaume Dutheuil, Graeme L. Fraser, Marie-Odile Roy, Mohamed El Bousmaqui, Frederic Batt
  • Patent number: 9475815
    Abstract: 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: Grant
    Filed: February 20, 2013
    Date of Patent: October 25, 2016
    Assignee: BAYER INTELLETUAL PROPERTY GMBH
    Inventors: Mario Lobell, Walter Hübsch, Hartmut Schirok, Mélanie Héroult, Dirk Brohm, Marie-Pierre Collin, Sylvia Grünewald, Klemens Lustig, Ulf Bömer, Verena Voehringer, Niels Lindner
  • Patent number: 9475816
    Abstract: 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: Grant
    Filed: September 6, 2013
    Date of Patent: October 25, 2016
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Zacharia Cheruvallath, Mallareddy Komandla, John David Lawson, Christopher McBride, Mingnam Tang
  • Patent number: 9475817
    Abstract: 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: Grant
    Filed: December 20, 2013
    Date of Patent: October 25, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Upender Velaparthi, Chetan Padmakar Darne, Dharmpal S. Dodd, Peiying Liu, Christopher P. Mussari, Mark D. Wittman, Selvakumar Kumaravel, Dibakar Mullick
  • Patent number: 9475818
    Abstract: 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: Grant
    Filed: August 21, 2015
    Date of Patent: October 25, 2016
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Swaroop Kumar V. S. Vakkalanka, Meyyappan Muthuppalaniappan, Dhanapalan Nagarathnam
  • Patent number: 9475819
    Abstract: 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: Grant
    Filed: May 21, 2015
    Date of Patent: October 25, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Heather R. Coate, Curt A. Dvorak, Terry P. Lebold, Cathy Preville, Brock T. Shireman
  • Patent number: 9475820
    Abstract: 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: Grant
    Filed: July 5, 2013
    Date of Patent: October 25, 2016
    Assignee: UCB Biopharma SPRL
    Inventors: 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
  • Patent number: 9475821
    Abstract: 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: Grant
    Filed: July 23, 2013
    Date of Patent: October 25, 2016
    Assignee: Laurus Labs Private Limited
    Inventors: Kameswar R. Chivukula, Venkata R. Murthy, Venkata S. Indukuri, Seeta R. Gorantla
  • Patent number: 9475822
    Abstract: 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: Grant
    Filed: July 29, 2015
    Date of Patent: October 25, 2016
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jun Terauchi, Hiroshi Nara, Hideyuki Oki, Kenjiro Sato
  • Patent number: 9475823
    Abstract: 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: Grant
    Filed: February 6, 2015
    Date of Patent: October 25, 2016
    Inventors: Tomas Hudlicky, Mary Ann Endoma-Arias, Brennan Augusta Murphy, Ivan Snajdr, Ales Machara
  • Patent number: 9475824
    Abstract: 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: Grant
    Filed: July 19, 2013
    Date of Patent: October 25, 2016
    Assignee: Cleave Biosciences, Inc.
    Inventors: Han-Jie Zhou, Francesco Parlati, David Wustrow
  • Patent number: 9475825
    Abstract: 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: Grant
    Filed: September 8, 2015
    Date of Patent: October 25, 2016
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood