Three Or More Hetero Atoms In The Tricyclo Ring System Patents (Class 514/293)
  • Patent number: 10208032
    Abstract: The present disclosure provides benzamide and nicotinamide compounds and pharmaceutical uses of the compounds. The compounds can be used to treat, for example, cancers such hematopoietic cancers (e.g., leukemia). The preferred compounds of the invention contain a phenylethynyl moiety as well as an amine-based heterocyclyl or heteroaryl moiety attached to the benzamide or nicotinamide compound.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: February 19, 2019
    Assignee: ONCOTARTIS INC.
    Inventors: Alexander Polinsky, Lioubov Korotchkina, Slavoljub Vujcic, Olga Chernova
  • Patent number: 10206930
    Abstract: The present invention is directed to methods of treating T-ALL that involve administering an inhibitor of jumonji D3 (JMJD3) demethylase. Another embodiment of the invention relates to methods inhibiting T-ALL cell proliferation and/or survival that involves administering an inhibitor of jumonji D3 (JMJD3) demethylase to a population of T-ALL cells.
    Type: Grant
    Filed: August 15, 2016
    Date of Patent: February 19, 2019
    Assignee: New York University
    Inventors: Iannis Aifantis, Panagiotis Ntziachristos
  • Patent number: 10201536
    Abstract: The present invention relates to methods and pharmaceutical compositions for the treatment of bacterial infections in patients suffering from cirrhosis. In particular, the present invention relates to a method of treating bacterial infection in a patient suffering from cirrhosis comprising administering to the patient a therapeutically effective amount of a TLR7 and/or TLR8 agonist.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: February 12, 2019
    Assignees: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), UNIVERISTE PARIS DIDEROT—PARIS 7, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
    Inventors: Axel Joseph Perianin, Loiec Rolas
  • Patent number: 10137122
    Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.
    Type: Grant
    Filed: July 14, 2015
    Date of Patent: November 27, 2018
    Assignees: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., The General Hospital Corporation
    Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop, Kimberly Stegmaier, Michel Weiwer, Versha Banerji
  • Patent number: 9908880
    Abstract: Imidazoquinolines of formula I that contain substituted amine or amide functionality at 1-position and that are effective as Toll like Receptor 7 activators are disclosed. These compounds are useful as anticancer agents.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: March 6, 2018
    Assignee: 4SC AG
    Inventors: Volker Gekeler, Thomas Maier, Astrid Zimmermann, Hans-Peter Hofmann, Sanjeev A. Kulkarni, Anil P. Jagtap, Ganesh S. Chaure
  • Patent number: 9908895
    Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: March 6, 2018
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Wenyu Zhu, Song Mei, Joseph Glenn
  • Patent number: 9893299
    Abstract: The invention concerns heterocyclic compounds and electronic devices, in particular organic electroluminescent devices, containing these compounds.
    Type: Grant
    Filed: August 13, 2014
    Date of Patent: February 13, 2018
    Assignee: Merck Patent GmbH
    Inventors: Philipp Stoessel, Nils Koenen
  • Patent number: 9777017
    Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: October 3, 2017
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Yun-Long Li, Wenyu Zhu, Song Mei
  • Patent number: 9550776
    Abstract: 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: Grant
    Filed: April 3, 2014
    Date of Patent: January 24, 2017
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yoshihiko Norimine, Nobuaki Sato, Yuki Ishihara, Kunitoshi Takeda
  • Patent number: 9499564
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: May 14, 2015
    Date of Patent: November 22, 2016
    Assignee: G1 Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay C. Strum
  • Patent number: 9265769
    Abstract: The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: February 23, 2016
    Inventors: Roberto Pellicciari, Flavio Moroni
  • Patent number: 9216980
    Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.
    Type: Grant
    Filed: April 17, 2014
    Date of Patent: December 22, 2015
    Assignee: Genentech, Inc.
    Inventors: Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis J. Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum MacLeod, Karen Williams
  • Patent number: 9216999
    Abstract: Novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities are provided. A tricyclic heterocyclic compound represented by the formula (Ia): wherein the rings Aa and Ba, Xa, Ya, R1a, R2a, R3a, L1a L2a, L3a and na are as defined in the description.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: December 22, 2015
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Keishi Hayashi, Tsuneo Watanabe, Koji Toyama, Junji Kamon, Masataka Minami, Miyuki Uni, Mariko Nasu
  • Patent number: 9127015
    Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: September 8, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
  • Patent number: 9072876
    Abstract: The present invention is directed to airless storage and dispensing systems that include a pump or dispensing package pre-filled with a topical semi-solid imiquimod pharmaceutical formulation (“pump systems”) and methods for storing and dispensing from the pump systems a plurality of precisely measured and uniform unit doses of a topical semi-solid imiquimod pharmaceutical formulation, and more particularly to pump systems, pre-filled with a topical imiquimod pharmaceutical cream and methods for delivering multiple precisely measured unit doses of a topical imiquimod pharmaceutical cream, and methods for using a controlled delivery pump system to store and dispense a plurality of consistent and precisely measured unit doses of a topical imiquimod pharmaceutical cream for use in topically treating a dermal and mucosal-associated condition, such as, external genital warts and/or perianal warts (EGWs), actinic keratosis or actinic keratoses (AK or AKs) and superficial basal cell carcinoma (sBCC).
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: July 7, 2015
    Assignee: MEDICIS PHARMACEUTICAL CORPORATION
    Inventors: Michael T. Nordsiek, Kodumudi S. Balaji
  • Publication number: 20150148341
    Abstract: The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Hazel Hunt, Iain Walters, Benoit Gourdet
  • Publication number: 20150141410
    Abstract: Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 21, 2015
    Applicants: UNIVERSITA' DEGLI STUDI DI MILANO, FONDAZIONE ITALIANA SCLEROSI MULTIPLA - FISH ONLUS
    Inventors: Maria Pia Abbracchio, Mario Alberto Battaglia, Ivano Eberini, Marta Fumagalli, Chiara Parravicini, Cristina Sensi, Paola Zaratin
  • Patent number: 9034336
    Abstract: The invention provides compounds of formula I: wherein R1-R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: May 19, 2015
    Assignee: Regents of the University of Minnesota
    Inventors: David M. Ferguson, John Ohlfest, Courtney Aldrich
  • Publication number: 20150133436
    Abstract: The use of compounds in the treatment of autoimmune and inflammatory diseases or conditions, pharmaceutical compositions containing such compounds and to methods for identifying compounds for use in the treatment of such diseases or conditions.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 14, 2015
    Inventors: Chun-Wa CHUNG, Edwige NICODEME
  • Publication number: 20150133443
    Abstract: The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Roberto Pellicciari, Flavio Moroni
  • Publication number: 20150133434
    Abstract: The present disclosure provides compositions and methods for reactivating latent immunodeficiency vims. The methods generally involve contacting an HIV-infected cell in which HIV is latent with an agent that binds a bromodomain (BRD) in the cell. Latently infected cells contain replication-competent integrated HIV-1 genomes that are blocked at the transcriptional level, resulting in the absence of viral protein expression. The present disclosure provides methods for reducing the reservoir of latent immunodeficiency virus in an individual.
    Type: Application
    Filed: March 13, 2013
    Publication date: May 14, 2015
    Inventors: Melanie Ott, Eric M. Verdin, Ming-Ming Zhou
  • Patent number: 9029388
    Abstract: The present invention provides a compound having a superior PDE10A inhibitory action and use thereof. The compound is a compound represented by the following formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: May 12, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Haruhi Kamisaki, Shinkichi Suzuki, Kasei Miura
  • Publication number: 20150126501
    Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
  • Patent number: 9023863
    Abstract: The present invention provides a foamable composition comprising water and an organic solvent, wherein the organic solvent comprises a fatty acid. The composition may further comprise a pharmaceutically active agent. The composition of the invention is also useful for the treatment of a dermatological disorder in a mammal by the topical administration of the composition.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: May 5, 2015
    Assignee: Stiefel Research Australia Pty Ltd
    Inventors: Albert Zorko Abram, Iulian Goldstein
  • Publication number: 20150110784
    Abstract: The present invention provides therapeutic combinations that include an immune response modifier (IRM) component and an anti-inflammatory component. The inventions further provide methods of treating a condition by administering to one having the condition a therapeutic combination that includes an IRM component and an anti-inflammatory component.
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Mark A. Tomai, Gary W. Gullikson, David M. Hammerbeck, Elaine A. Egging, Michael J. Reiter, Christopher D. Gram, John P. Vasilakos
  • Patent number: 9012470
    Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I in the manufacture of a medicament for the treatment of GABAA receptor associated disorders. The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: April 21, 2015
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Varsha Gupta, Joel Renick, Graeme Freestone, Alan P. Kaplan
  • Publication number: 20150105415
    Abstract: The present invention relates to the compound represented by formula (I): (wherein, all the symbols have the same meaning as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuyuki OHMOTO, Masashi KATO, Yoshifumi KAGAMIISHI, Junichiro MANAKO
  • Publication number: 20150105417
    Abstract: The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.
    Type: Application
    Filed: December 19, 2014
    Publication date: April 16, 2015
    Inventors: Carlos Garcia-Echeverria, Sauveur-Michel Maira, Darrin Stuart, Susan Wee, Christine Fritsch, Tobi Nagel
  • Patent number: 9006246
    Abstract: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (I): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: April 14, 2015
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Akira Ohata, Shingo Nakatani, Tetsuya Sugiyama, Takashi Morimoto
  • Patent number: 9006264
    Abstract: 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: Grant
    Filed: September 9, 2013
    Date of Patent: April 14, 2015
    Assignee: 3M Innovative Properties Company
    Inventors: Doris Stoermer, Joseph F. Dellaria, Jr., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk
  • Patent number: 9000153
    Abstract: The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).
    Type: Grant
    Filed: July 26, 2011
    Date of Patent: April 7, 2015
    Assignee: Merck Patent GmbH
    Inventors: Thomas Fuchss, Werner Mederski, Frank Zenke
  • Patent number: 8993765
    Abstract: The present invention relates to tetrahydro-azacarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: March 31, 2015
    Assignee: Albany Molecular Research, Inc.
    Inventors: Matthew D. Surman, Peter R. Guzzo, Emily Freeman
  • Publication number: 20150087630
    Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.
    Type: Application
    Filed: April 17, 2014
    Publication date: March 26, 2015
    Applicant: Genentech, Inc.
    Inventors: Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum MacLeod, Karen Williams
  • Publication number: 20150087627
    Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject.
    Type: Application
    Filed: April 15, 2014
    Publication date: March 26, 2015
    Applicant: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
  • Publication number: 20150087636
    Abstract: The use of BETi as a potential treatment for FSHD is provided. Specifically, the use of BETi, and particularly selective BETi for BRD4, are shown to inhibit DUX4 expression which is expected to result in a decrease in the severity of symptoms of FSHD. Further, the treatments are shown to work when pulsed as opposed to continuous. This allows for a BETi to be supplied to a human in a pulse, and then allows the human to not need any additional treatment for a window at least as long as the one of the treatment pulse.
    Type: Application
    Filed: September 19, 2014
    Publication date: March 26, 2015
    Inventor: Francis M. Sverdrup
  • Patent number: 8987274
    Abstract: The present invention provides a compound of Formula (1): as described herein or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: March 24, 2015
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Latha G. Nair, Stephane L. Bogen, Ronald J. Doll, Yao Ma, Yuan Tian
  • Publication number: 20150080389
    Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: September 16, 2014
    Publication date: March 19, 2015
    Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
  • Publication number: 20150080366
    Abstract: Compounds of Formula (I) wherein n, A, R1, R2, R3 and R5 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
    Type: Application
    Filed: April 3, 2013
    Publication date: March 19, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Lee Fader, Pierre Louis Beaulieu, Murray Bailey, Francois Bilodeau, Rebekah J. Carson, André Giroux, Cédrickx Godbout, Oliver Hucke, Marc-André Joly, Mélissa Leblanc, Olivier Lepage, Benoit Moreau, Julie Naud, Martin Poirier, Elisia Villemure
  • Publication number: 20150072978
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
    Type: Application
    Filed: November 17, 2014
    Publication date: March 12, 2015
    Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew J. Souers
  • Publication number: 20150072975
    Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.
    Type: Application
    Filed: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Berangere Gaucher, JR., Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin XU
  • Publication number: 20150065471
    Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
  • Publication number: 20150065431
    Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 5, 2015
    Inventors: Wei Xu, Seok Jong Hong, Robert D. Galiano, Thomas A. Mustoe
  • Publication number: 20150065447
    Abstract: This application relates to methods of increasing survival or progression-free survival in a patient with a solid tumor, wherein the patient has an elevated serum concentration of C-reactive protein (CRP), by administering a JAK inhibitor or an inhibitor of IL-6 signaling to the patient, as well as methods of predicting survival benefit in these patients from such therapy.
    Type: Application
    Filed: August 19, 2014
    Publication date: March 5, 2015
    Applicant: Incyte Corporation
    Inventor: Victor Sandor
  • Publication number: 20150065468
    Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Inventors: Mark W. HOLLADAY, Gang LIU, Martin W. ROWBOTTON
  • Patent number: 8962620
    Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: November 4, 2013
    Date of Patent: February 24, 2015
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
  • Patent number: 8962649
    Abstract: A multidose package containing an imiquimod formulation suitable for treating topical conditions includes: a) a dispensing aperture for dispensing the formulation from the package; b) a reservoir containing sufficient formulation to provide two or more doses; c) a metered dosage element for measuring a predetermined dose of the formulation, the element including an inlet from the reservoir and an outlet to the dispensing aperture; and d) an actuating element operating the dosage element so the predetermined dose is delivered to the dispensing aperture; wherein the dose is dispensed without microbial or other contamination or degradation of the formulation in reservoir. A corresponding course of treatment for various maladies includes providing a multidose package containing an imiquimod formulation suitable for the treatment. A corresponding method of treatment of diseases with multiple doses of an imiquimod formulation includes multiple doses provided by a multidose package.
    Type: Grant
    Filed: April 1, 2010
    Date of Patent: February 24, 2015
    Assignee: iNova Pharmaceuticals (Australia) Pty Limited
    Inventors: Mark J. Hutchings, Christiaan M. Van Niekerk
  • Publication number: 20150051209
    Abstract: The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 19, 2015
    Applicant: NOVARTIS AG
    Inventors: Mark Gary BOCK, Henrik MOEBITZ, Sunil Kumar PANIGRAHI, Ramulu PODDUTOORI, Susanta SAMAJDAR
  • Publication number: 20150045374
    Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
    Type: Application
    Filed: January 3, 2013
    Publication date: February 12, 2015
    Inventors: Kerim Babaoglu, Kyla L. Bjornson, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu
  • Patent number: 8946279
    Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.
    Type: Grant
    Filed: August 18, 2011
    Date of Patent: February 3, 2015
    Assignee: KBP Biosciences Co., Ltd.
    Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
  • Publication number: 20150030587
    Abstract: Methods of treating a head and neck cancer are disclosed.
    Type: Application
    Filed: February 11, 2014
    Publication date: January 29, 2015
    Applicant: FOUNDATION MEDICINE, INC.
    Inventors: Chris Hendrik Boshoff, Timothy Robert Fenton, Matthias Alexander Lechner, Philip James Stephens, Matthew J. Hawryluk, Garrett Michael Frampton, Roman Yelensky