Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/312)
-
Publication number: 20140309180Abstract: The present invention relates to diuretic pharmaceutical compositions and methods and in particular to certain derivatives of the formula I wherein R1, R2, R3, R5, R6 and R7 are independently X3R where R is selected from the group consisting of H, halo; optionally substituted saccharide, aliphatic, cycloalkyl, heterocycloalkyl, aryl and heteroaryl; —P(O)(ORa)(ORb) and —NRaRb, where Ra and Rb are independently H, optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; X1, X2 and X3 are independently —C(O)O—, —OC(O)—, —C(O)NH—, —NHC(O)—, —OC(O)NH—, —NHC(O)O—, —OS(O)y—, —S(O)y—, —O—, —NHC(O)—, —NHC(O)O—, —S(O)2NH—, a bond or absent; where y is an integer from 0 to 3; and R4 and R8 are independently H, (?O); hydroxy; or optionally substituted saccharide, aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or —P(O)(ORa)(ORb) or —NRaRb, where Ra and Rb are independently H, or optionally substituted aliphatic, cycloalkyl or heterocycloalkyl, aryl or heteroaryl; or a prodrugType: ApplicationFiled: April 10, 2014Publication date: October 16, 2014Applicant: NATURON PHARMACEUTICALS, INC.Inventors: Neal S. Bricker, Stewart Shankel, Christopher D. Cain, Mark A. Mitchnick, Michael Schmertzler
-
Publication number: 20140308333Abstract: A coating material including a bio-absorbable cross-linked material and a cellular uptake inhibitor. The bio-absorbable cross-linked material includes two or more fatty acids cross-linked into a substantially random configuration by ester bonds. The coating material may be adhered to a medical device. A medical device system including a medical device and a coating is also included.Type: ApplicationFiled: April 14, 2014Publication date: October 16, 2014Applicant: ATRIUM MEDICAL CORPORATIONInventors: Roger Labrecque, Geoffrey Moodie, Joseph F. Ferraro, Lisa Rogers, Paul Martakos, Theodore Karwoski, Steve A. Herweck
-
Patent number: 8859544Abstract: The invention relates to compounds corresponding to formula (I): in which R3 and R4 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: in which the wavy lines represent the phenyl nucleus to which R3 and R4 are attached. Preparation process and therapeutic use.Type: GrantFiled: July 4, 2011Date of Patent: October 14, 2014Assignee: SanofiInventors: Chantal Alcouffe, Corentin Herbert, Gilbert Lassalle
-
Patent number: 8859462Abstract: Disclosed is a pest control composition comprising at least one pyripyropene derivative of formula (I) or agriculturally and horticulturally acceptable salt thereof and at least one other pest control agent as active ingredients. The combined use of the two ingredients can provide a better insecticidal effect.Type: GrantFiled: March 10, 2008Date of Patent: October 14, 2014Assignee: Meiji Seika Pharma Co., Ltd.Inventors: Ryo Horikoshi, Kazuhiko Oyama, Mitsuyuki Yabuzaki
-
Publication number: 20140303150Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.Type: ApplicationFiled: December 22, 2011Publication date: October 9, 2014Applicant: LEO Laboratories LimitedInventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
-
Publication number: 20140302147Abstract: Embodiments of the present invention provide a dry powder composition comprising porous carrier particles associated with one, two, three or more micronized drugs or APIs wherein an ordered mixture between the micronized drug or drugs and the carrier particle results, such that the micronized drug or drugs adhere strongly to the carrier particles forming a stable ordered mixture of respirable agglomerates. Embodiments of the present invention further comprise a spray-drying process to create the respirable agglomerates. Embodiments of the present invention further relate to the use of the dry powder formulation comprising respirable agglomerates for the treatment of a patient having a disease or condition which is treatable thereby.Type: ApplicationFiled: March 10, 2014Publication date: October 9, 2014Applicant: NOVARTIS AGInventors: Michael HARTMAN, Thomas E TARARA, Patrick TEUNG, Jeffry G WEERS
-
Publication number: 20140303204Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: ApplicationFiled: June 6, 2014Publication date: October 9, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T.D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
-
Publication number: 20140303127Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.Type: ApplicationFiled: November 9, 2012Publication date: October 9, 2014Inventors: Jose Aiguade Bosch, Silvia Gual Roig, Maria Prat Quinones, Carlos Puig Duran
-
Publication number: 20140303205Abstract: This invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is COOH or CH2OH.Type: ApplicationFiled: June 20, 2014Publication date: October 9, 2014Inventors: Xiaoqing Yang, Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Martyn Curtis Botfield, Gregor Zlokarnik
-
Patent number: 8853242Abstract: [Object] An excellent agent for preventing or treating dementia, schizophrenia, and the like, based on serotonin 5-HT5A receptor modulating action, is provided. [Means for Solution] It was confirmed that acylguanidine derivatives (the following formula I; any one of Z1, Z2, Z3, Z4 and Z5 is nitrogen atom, and the others are carbon atoms) which have the characteristic structure in which the guanidine is bonded to one ring of the quinoline or isoquinoline via a carbonyl group, and a cyclic group is bonded to the other ring, exhibit potent 5-HT5A receptor modulating actions and excellent pharmacological actions based on the 5-HT5A receptor modulating action, and thus can be excellent agents for preventing or treating dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder. Thus, the present invention has been completed.Type: GrantFiled: August 5, 2010Date of Patent: October 7, 2014Assignee: Astellas Pharma Inc.Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Takuya Washio, Wataru Hamaguchi
-
Publication number: 20140286876Abstract: The present invention, as described above and as further defined by the claims, provides methods of administering an active agent via adhesion of a film to a mucous membrane in the oral cavity of a mammal, as well as and ODF formed therefore. An active agent may be ingested as the ODF dissolves resulting in systemic treatment of the mammal. In additional embodiments, an ODF may provide topical administration of an active agent.Type: ApplicationFiled: March 28, 2014Publication date: September 25, 2014Inventor: Andrew L. Skigen
-
Publication number: 20140287028Abstract: The use of chemotherapeutic agents for the preparation of a medicament for the topical and/or local treatment of diseases caused by bacteria and/or for prophylaxis in humans or animals.Type: ApplicationFiled: June 3, 2014Publication date: September 25, 2014Applicant: BAYER INNOVATION GMBHInventors: Hans-Herrmann SCHULZ, Gunther SCHLIMBACH
-
Publication number: 20140288020Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.Type: ApplicationFiled: April 16, 2014Publication date: September 25, 2014Applicant: Gilead Pharmasset LLCInventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
-
Patent number: 8841321Abstract: Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula; R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 1, 2 or 3; R4 and R5 are hydrogen, alkyl or benzyl; or R4 and R5 together and including the N to which they are attached may form a ring; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkythioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R6 radicaType: GrantFiled: June 26, 2006Date of Patent: September 23, 2014Assignee: Janssen Pharmaceutica NVInventors: Koenraad Jozef Lodewijk Marcel Andries, Anil Koul, Jérôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Ismet Dorange, Leo Jacobus Jozef Backx, Lieven Meerpoel
-
Patent number: 8841301Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.Type: GrantFiled: September 24, 2012Date of Patent: September 23, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Dalton King, John E. Macor, Richard E. Olson, Christiana I. Iwuagwu, George N. Karageorge
-
Publication number: 20140275163Abstract: The disclosure provides crystalline Sovaprevir forms. The crystalline forms of Sovaprevir comprise a Form A polymorph, a Form B polymorph, a Form C polymorph, a Form D polymorph, and a Form E polymorph. The Form A, B, C, D, and E polymorphs exhibit X-ray powder diffraction patterns having peak locations in accordance with FIGS. 1, 4, 7, 10, and 13, respectively.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Achillion Pharmaceuticals, Inc.Inventor: Avinash Phadke
-
Publication number: 20140271878Abstract: The subject invention provides a mixture of crystalline laquinimod sodium particles, wherein (i) 90% or more of the total amount by volume of the laquinimod sodium particles have a size of 40 microns or less or (ii) 50% or more of the total amount by volume of the laquinimod sodium particles have a size of 15 microns or less, and wherein: a) the mixture has a bulk density of 0.2 g/mL to 0.4 g/mL; b) the mixture has a tapped density of 0.40 g/mL to 0.7 g/mL; c) an amount of heavy metal in the mixture is no more than 0.002% of heavy metal relative to the amount by weight of laquinimod sodium; d) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline (MCQ) in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; e) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroqunoline-3-carboxylic acid (MCQCA) in the mixture is no more than 0.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.Inventors: Anton Frenkel, Avital Laxer
-
Publication number: 20140275057Abstract: The present invention relates to compounds and composition for inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.Type: ApplicationFiled: September 2, 2011Publication date: September 18, 2014Inventors: Kenneth W. Bair, Timm Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
-
Publication number: 20140256770Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.Type: ApplicationFiled: May 23, 2014Publication date: September 11, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: John DeMattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Yap Guerette, Brian R. Krueger, Peter D.J. Grootenhuis, Fredrick F. Van Goor, Martyn C. Botfield, Gregor Zlokarnik
-
Publication number: 20140255483Abstract: The present invention relates to pharmaceutical compositions containing a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition.Type: ApplicationFiled: May 23, 2014Publication date: September 11, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Eleni Dokou, Shahla Jamzad, John P. Caesar, JR., Majed Fawaz, Laura Das, Chong-Hui Gu, Patricia Nell Hurter, Meghna Jai Israni, Meghan M. Johnston, Dragutin Knezic, Andrew G. Kuzmission, HongRen Wang
-
Patent number: 8829002Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.Type: GrantFiled: December 13, 2011Date of Patent: September 9, 2014Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
-
Patent number: 8828976Abstract: A screening method for identifying compounds that alter the fidelity with which the initiation codon in mRNAs is recognized by the translational apparatus in eukaryotes is disclosed. This screening method was used to identify compounds having such activity. Methods of altering the fidelity of initiation codon selection are also disclosed. Methods of treating disorders characterized by single nucleotide mutations in initiation codons using compounds identified by the screening method, as well as methods of treating fungal and parasitic infections and hyperproliferative disorders using compounds identified by the screening method are also disclosed.Type: GrantFiled: March 18, 2011Date of Patent: September 9, 2014Assignee: The Johns Hopkins UniversityInventors: Jon R. Lorsch, Julie Ellen Takacs, Timothy Brian Neary
-
Publication number: 20140249074Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: May 16, 2014Publication date: September 4, 2014Applicant: GILEAD PHARMASSET LLCInventors: Elizabeth M. Bacon, Eda Canales, Aesop Cho, Jeromy J. Cottell, Manoj C. Desai, Michael Graupe, Hongyan Guo, Randall L. Halcomb, Darryl Kato, Choung U. Kim, Thorsten A. Kirschberg, Evan S. Krygowski, Scott E. Lazerwith, John O. Link, Hongtao Liu, Qi Liu, Richard L. Mackman, Michael L. Mitchell, Jay P. Parrish, Hyung-Jung Pyun, Joseph H. Saugier, Scott D. Schroeder, Jianyu Sun, James G. Taylor, James D. Trenkle, Winston C. Tse, Randall W. Vivian, William J. Watkins, Lianhong Xu
-
Publication number: 20140248357Abstract: A pharmaceutical composition adapted for pulmonary administration by inhalation is described, wherein the composition comprises a glitazone and one or more pharmaceutically acceptable carriers and/or excipients, wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer, and wherein the glitazone is pioglitazone or rosiglitazone or a pharmaceutically acceptable salt thereof, and wherein the glitazone is in the form of microparticles.Type: ApplicationFiled: April 7, 2014Publication date: September 4, 2014Applicant: PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITEDInventors: Harry Finch, Craig Fox, Mohammed Sajad, Monique Bondil Van Niel, Andrew Forrest
-
Patent number: 8822496Abstract: The present invention relates to therapeutic combinations comprising (a) Compound (1), or a pharmaceutically acceptable salt thereof, as herein described, (b) an interferon alfa and (c) ribavirin and particular regimens for administering this combination. Compound (1) is a selective and potent inhibitor of the HCV NS3 serine protease. The present invention also relates to methods of using such therapeutic combinations for treating HCV infection or alleviating one or more symptoms thereof in a patient.Type: GrantFiled: October 27, 2010Date of Patent: September 2, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Carla Haefner, Gerhard Steinmann, Jerry O. Stern, Chan-Loi Yong
-
Patent number: 8822691Abstract: To provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Carboxamides represented by the following Formula (I) and use thereof as pesticides and an animal parasite control agent: wherein each substituent is as defined in the specification.Type: GrantFiled: July 10, 2010Date of Patent: September 2, 2014Assignee: Bayer CropScience AGInventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
-
Patent number: 8821936Abstract: This invention provides a solid pharmaceutical formulation having high physical strength and further having excellent drug release properties and digestibility of excipients when administered, which comprises (a) an active medical ingredient and (b) a pre-gelatinized starch in an amount of 10 to 90% by weight, said pre-gelatinized starch being prepared by pre-gelatinizing a cheap and stable usual starch during the procedure for formulation. This invention also provides a method for preparing the solid pharmaceutical formulation.Type: GrantFiled: May 19, 2005Date of Patent: September 2, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventor: Tadashi Mukai
-
Publication number: 20140243390Abstract: Novel RET fusion molecules and uses are disclosed.Type: ApplicationFiled: February 23, 2014Publication date: August 28, 2014Applicant: FOUNDATION MEDICINE, INC.Inventors: Sean R. Downing, Matthew J. Hawryluk, Doron Lipson, Alexander N. Parker, Philip James Stephens
-
Publication number: 20140243289Abstract: The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: May 2, 2014Publication date: August 28, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Peter D.J. Grootenhuis, Sara Hadida Ruah, Jinglan Zhou, Anna Hazlewood, Hayley Binch
-
Publication number: 20140242172Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: ApplicationFiled: May 8, 2014Publication date: August 28, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
-
Publication number: 20140243314Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 24, 2012Publication date: August 28, 2014Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
-
Publication number: 20140243339Abstract: This invention is in the field of pharmaceutical agents and specifically relates to compounds, compositions, uses and methods for treating cancer, by combining VEGF(R) inhibitors and inhibitors of HGF/SF:c-Met.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Applicant: Amgen Inc.Inventors: Teresa L. Burgess, Angela Coxon, Isabelle Dussault, Paula Kaplan-Lefko, Anthony J. Polverino, Darrin Beaupre
-
Publication number: 20140243348Abstract: Compositions and methods that are useful for the treatment of herpesvirus infection (including herpes simplex virii) are disclosed. Methods for identifying compounds useful for the treatment of herpesvirus infection are also disclosed.Type: ApplicationFiled: January 22, 2014Publication date: August 28, 2014Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: David M. Knipe, Kevin Bryant, David H. Dreyfus
-
Patent number: 8815902Abstract: The present invention is directed to tetrahydroquinoline amide compounds of formula (I) (Formula should be inserted here) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: June 10, 2011Date of Patent: August 26, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin F. Gilbert, Scott D. Kuduk
-
Patent number: 8815849Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: GrantFiled: July 26, 2011Date of Patent: August 26, 2014Assignee: Janssen R&D IrelandInventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
-
Publication number: 20140235646Abstract: The present invention relates to methods for reducing body weight in an animal in need thereof via administration of a therapeutically effective amount of a compound having a general tripartite structure A-B-C. In the tripartite structure A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. The methods may utilize particular compounds, for example, having a piperidinyl, a pyrrolinyl or pyridinyl A ring, a thiazole B ring, and a phenyl C ring which may be further substituted independently. Also provided are methods for increasing thermogenesis without reducing lean body mass during weight loss in an animal by administering of a therapeutically effective amount of the compounds described.Type: ApplicationFiled: May 5, 2014Publication date: August 21, 2014Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Al-Elheiga, Mizuki Watanabe
-
Publication number: 20140235631Abstract: The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and/or stem cells).Type: ApplicationFiled: July 26, 2013Publication date: August 21, 2014Inventors: Antonius Martinus Gustave Bunt, Olaf van Tellingen
-
Publication number: 20140235670Abstract: This invention provides a method for treating a human subject afflicted with a progressive form of multiple sclerosis, comprising periodically administering to the human subject an amount of laquinimod effective to treat the human subject. This invention also provides laquinimod for use in treating a human subject afflicted with a progressive form of multiple sclerosis. This invention further provides pharmaceutical compositions and packages comprising an effective amount of laquinimod for treating a progressive form of multiple sclerosis.Type: ApplicationFiled: February 13, 2014Publication date: August 21, 2014Applicant: Teva Pharmaceutical Industries, Ltd.Inventors: Nora Tarcic, Dan Bar-Zohar, Liat Hayardeny, Yossi Gilgun Sherki, Tali Gorfine, Volker Knappertz, Ella Sorani
-
Publication number: 20140235548Abstract: Compounds, pharmaceutical compositions, and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by JAMM proteins are disclosed. The compounds and compositions inhibit the enzymatic activity of a JAMM domain, including the JAMM domain of the CSN5 subunit of the COP9-signalsome (CSN), the JAMM domain of the Rpn11/Poh1/Psmd14 subunit of the 26S proteasome, the JAMM domain of AMSH, the JAMM domain of AMSH-LP, the JAMM domain of BRCC36, among other JAMM domains.Type: ApplicationFiled: May 10, 2012Publication date: August 21, 2014Applicant: Cleave Biosciences, Inc.Inventors: Han-Jie Zhou, Francesco Parlati, Matthieu Roufflet, Ethan D. Emberley, Raymond J. Deshaies, Seth Cohen
-
Publication number: 20140235634Abstract: Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.Type: ApplicationFiled: February 14, 2014Publication date: August 21, 2014Applicant: Kala Pharmaceuticals, Inc.Inventors: Winston Zapanta ONG, Pawel Wojciech NOWAK, Ben C. ASKEW, Jinsoo KIM
-
Patent number: 8809537Abstract: The subject invention provides pharmaceutical compositions containing laquinimod or a pharmaceutically acceptable salt thereof, an isolated compound of N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide or a salt thereof, compositions containing N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl)amino)-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide and methods of preparing the same.Type: GrantFiled: May 7, 2013Date of Patent: August 19, 2014Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Avital Laxer, Konstantin Ulanenko
-
Patent number: 8809329Abstract: The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample.Type: GrantFiled: July 31, 2008Date of Patent: August 19, 2014Assignees: Tokyo Metropolitan Institute of Medical Science, Renascience Co., Ltd.Inventors: Masanari Itokawa, Toshio Miyata, Makoto Arai
-
Patent number: 8809360Abstract: The present invention relates to use of a pyridine compound of the following formula [I]: wherein R is a substituted pyridyl group having the following formula: R0 is a C1-6 alkoxy-C1-6 alkyl group, R1 and R2 are the same or different and a C1-6 alkoxy group, X is a group of the formula: ?N— or a group of the formula: Ring A is a saturated or unsaturated 10-membered nitrogen-containing hetero-bicyclic group optionally having a substituent(s), the dotted line means the presence or absence of a double bond, or a pharmaceutically acceptable salt thereof for the preparation of a medicament for treatment of skin lesion.Type: GrantFiled: October 28, 2005Date of Patent: August 19, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Tamotsu Takagi, Atsuko Naotsuka
-
Publication number: 20140228330Abstract: This invention provides a pharmaceutical composition comprising a eutectic composition of two pharmacologically active ingredients for delivery to the lung by inhalation. This invention also provides a pharmaceutical composition comprising a eutectic composition of two pharmacologically active ingredients for the treatment of respiratory disease.Type: ApplicationFiled: August 8, 2012Publication date: August 14, 2014Inventors: Graham Ruecroft, Dipesh Parikh
-
Publication number: 20140228399Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: ApplicationFiled: November 7, 2013Publication date: August 14, 2014Inventors: Hayley Binch, Lev T.D. Fanning, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
-
Publication number: 20140228400Abstract: This invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is COOH or CH2OH.Type: ApplicationFiled: November 19, 2013Publication date: August 14, 2014Inventors: Xiaoqing Yang, Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Martyn Curtis Botfield, Gregor Zlokarnik
-
Publication number: 20140228371Abstract: The invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.Type: ApplicationFiled: January 29, 2014Publication date: August 14, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
-
Publication number: 20140228401Abstract: This invention is directed to the treatment of osteoporosis using N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.Type: ApplicationFiled: September 20, 2012Publication date: August 14, 2014Applicant: Exelixis, Inc.Inventors: Dana T. Aftab, Douglas Clary
-
Patent number: 8802700Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: June 8, 2012Date of Patent: August 12, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Urvi Sheth, Lev T. D. Fanning, Mehdi Numa, Hayley Binch, Dennis James Hurley, Jinglan Zhou, Sara S. Hadida Ruah, Anna R. Hazlewood, Alina Silina, Rajendran Vairagoundar, Fredrick F. Van Goor, Peter Diederik Jan Grootenhuis, Martyn C. Botfield
-
Patent number: RE45108Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.Type: GrantFiled: September 27, 2013Date of Patent: September 2, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Kenji Otsubo, Takahito Yamauchi, Yuji Ochi