Patents Issued in May 26, 2016
  • Publication number: 20160143859
    Abstract: Disclosed is a system including (1) an injection device including injectable magnetizable nanoparticles and a component for injecting the same, and (2) a unit for applying a constraint physically and/or mechanically to a tumor associated to an neoangiogenic network where, after having been injected, the particles are retained. Also disclosed is a method for treating tumors, especially tumors associated with a neoangiogenic network, including the steps of: injecting a composition including magnetizable nanoparticles; optionally performing imaging using an imaging device to detect a concentration of nanoparticles retained in the neoangiogenic network; and applying a contact-free constraint onto a tumor in vivo, by a gradient of magnetic field and the application being directed to the tumor region.
    Type: Application
    Filed: July 11, 2014
    Publication date: May 26, 2016
    Inventor: Remy BROSSEL
  • Publication number: 20160143860
    Abstract: The invention relates to the film products and methods of their preparation that demonstrate a non-self-aggregating uniform heterogeneity. Desirably the films disintegrate in water and may be formed by a controlled drying process, or other process that maintains the required uniformity of the film.
    Type: Application
    Filed: November 18, 2015
    Publication date: May 26, 2016
    Inventors: Robert K. Yang, Richard C. Fuisz, Garry L. Myers, Joseph M. Fuisz
  • Publication number: 20160143861
    Abstract: The present invention refers to novel compositions comprising hydroxytyrosol, resveratrol, lycopene, flavanols, and/or flavonoids and their use in treating and/or preventing pro-inflammatory diseases or disorders and ROS-mediated diseases or disorders. This invention also generally relates to compositions and to methods of using the compositions to increase tissue oxygenation.
    Type: Application
    Filed: July 11, 2014
    Publication date: May 26, 2016
    Applicant: Specialty Nutrition Group, Inc.
    Inventor: Gregory T. Hom
  • Publication number: 20160143862
    Abstract: A method of using beta-ionone, E)-4-(2,6,6-trimethylcyclohex-1-en-1-yl)but-3-en-2-one, treats and prevents diseases otherwise induced by Propionibacterium acnes and thus effectively reduces inflammatory responses otherwise caused by Propionibacterium acnes.
    Type: Application
    Filed: February 27, 2015
    Publication date: May 26, 2016
    Inventors: PO-JUNG TSAI, WEN-CHENG HUANG, YA-HSIN SHIH
  • Publication number: 20160143863
    Abstract: The present invention relates to pharmaceutical composition of Cinacalcet or a pharmaceutically acceptable salt thereof comprising diluents, binders and lubricants, wherein said composition is substantially free of disintegrant. It further relates to process for preparing such compositions.
    Type: Application
    Filed: June 26, 2014
    Publication date: May 26, 2016
    Applicant: JUBILANT GENERICS LIMITED
    Inventors: GOUTAM MUHURI, RAVIKUMAR NITHIYANANDAM, GANESH VINAYAK GAT, SWATI MUKHERJEE, BHARAT BHUSHAN
  • Publication number: 20160143864
    Abstract: The present invention relates to timed extended-release pharmaceutical compositions comprising metoprolol and an extended-release polymer. The pharmaceutical compositions of the present invention exhibit an in-vivo lag time of at least 2 hours as and a Tmax of more than 8 hours. Further, said pharmaceutical compositions provide an in-vitro release of metoprolol over a period of at least 20 hours.
    Type: Application
    Filed: July 9, 2014
    Publication date: May 26, 2016
    Inventors: Sandeep Kumar VATS, Balaram MONDAL, Kalaiselvan RAMARAJU, Romi Barat SINGH, Ajay Kumar SINGLA
  • Publication number: 20160143865
    Abstract: The disclosure relates, in general, to treatment of fatty liver disorders comprising administering compositions comprising cysteamine products. The disclosure provides administration of enterically coated cysteamine compositions to treat fatty liver disorders, such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH).
    Type: Application
    Filed: September 28, 2015
    Publication date: May 26, 2016
    Inventors: Ranjan Dohil, Jerry Schneider
  • Publication number: 20160143866
    Abstract: A combination therapy is disclosed for the treatment of a patient, such as a human, with a monoclonal antibody. The methods can include administering to a patient a monoclonal antibody, for example, a TNT-alpha inhibitor such as adalimumab, certolizumab pegol, golimumab, and infliximab; and administering to the patient colchicine. The present teachings also provide a therapeutic combination and a kit including the therapeutic combination.
    Type: Application
    Filed: November 20, 2015
    Publication date: May 26, 2016
    Inventor: Eli D. Ehrenpreis
  • Publication number: 20160143867
    Abstract: The invention relates to methods and pharmaceutical compositions for treating cancer. In particular, the present invention relates to a compound selected from the group consisting of gamma-hydroxybutyrate (GHB), GHB derivatives, and GHB structurally-related compounds thereof, or a pharmaceutically acceptable salt thereof for use in the treatment of cancer in a subject in need thereof.
    Type: Application
    Filed: June 20, 2014
    Publication date: May 26, 2016
    Inventors: MARIE-PIERRE JUNIER, HERVÉ CHNEWEISS, ELIAS EL-HABR, LUIZ-GUSTAVO FEIJO-DUBOIS, THIERRY VIROLLE, LAURENT TURCHI, MOHAMED FAREH
  • Publication number: 20160143868
    Abstract: Treprostinil can be administered using a metered dose inhaler. Such administration provides a greater degree of autonomy to patients. Also disclosed are kits that include a metered dose inhaler containing a pharmaceutical formulation containing treprostinil.
    Type: Application
    Filed: February 1, 2016
    Publication date: May 26, 2016
    Applicant: United Therapeutics Corporation
    Inventors: Horst OLSCHEWSKI, Robert ROSCIGNO, Lewis J. RUBIN, Thomas SCHMEHL, Werner SEEGER, Carl STERRITT, Robert VOSWINCKEL
  • Publication number: 20160143869
    Abstract: The present invention provides a stable, aqueous solution comprising bromfenac or a pharmacologically acceptable salt, polymorph, ester or hydrate thereof and/or pharmaceutically acceptable excipients wherein the invention is preferably devoid of an alkyl aryl polyether alcohol type polymer such as tyloxapol, a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate and BAC. Also the present invention is preferably devoid of antioxidants such as sulfite but not limited to sodium sulfite, potassium sulfite and the like. The present invention also provides for a method for treating ocular inflammation and pain, e.g., after cataract surgery, wherein the method comprises topical application of a formulation according to the present invention to the eye of a patient in need thereof.
    Type: Application
    Filed: June 17, 2014
    Publication date: May 26, 2016
    Applicant: SENTISS RESEARCH CENTER
    Inventors: Mandar V. SHAH, Prafulla CHAUDHARI, Deepak BAHRI
  • Publication number: 20160143870
    Abstract: There are disclosed compounds of Formula (I) that modulate or inhibit the enzymatic activity of indoleamine 2,3-di-oxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compounds of the invention.
    Type: Application
    Filed: July 10, 2014
    Publication date: May 26, 2016
    Inventors: Jay A Markwalder, James Aaron Balog, Audris Huang, Steven P Seitz
  • Publication number: 20160143871
    Abstract: Agents containing (A) cystine or a derivative thereof and (B) theanine, in combination, are useful for reducing side effects of cancer chemotherapy, can reduce various side effects of cancer chemotherapy, and can improve the treatment completion rate of cancer chemotherapy.
    Type: Application
    Filed: January 28, 2016
    Publication date: May 26, 2016
    Applicant: AJINOMOTO CO., INC.
    Inventors: Shigekazu KURIHARA, Takashi TSUCHIYA
  • Publication number: 20160143872
    Abstract: The invention relates to a lipid composition comprising fatty acids mainly in the form of triacylglycerols, in which composition at least 50% of the fatty acids are 14-methyl pentadecanoic acids, and at least 8% of the fatty acids are 12-methyl tetradecanoic acids, the percentages being expressed by weight with respect to the total fatty acids of the composition.
    Type: Application
    Filed: June 20, 2014
    Publication date: May 26, 2016
    Applicants: AVRIL, UNIVERSITE PARIS-SUD
    Inventors: FRANCE THEVENIEAU, SOPHIE SAMBOU, MARIE-JOËLLE VIROLLE, THIERRY DULERMO
  • Publication number: 20160143873
    Abstract: Substantially anhydrous topical gel compositions comprising ingenol-3-angelate as a suspension in non-aqueous carriers.
    Type: Application
    Filed: June 12, 2015
    Publication date: May 26, 2016
    Inventors: Per-Ola Arvidsson, Edit Farkas, Chinar S. Saeed, Mikkel Krogh-Madsen, Karsten Petersson
  • Publication number: 20160143874
    Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for exmaple. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
    Type: Application
    Filed: September 23, 2015
    Publication date: May 26, 2016
    Inventors: James Elliot Bradner, Ralph Mazitschek
  • Publication number: 20160143875
    Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent obesity.
    Type: Application
    Filed: February 2, 2016
    Publication date: May 26, 2016
    Inventor: Joseph S. Zakrzewski
  • Publication number: 20160143876
    Abstract: A maintenance therapy regimen is described for the treatment of acne related diseases. The novel therapy regimen follows a course of oral antibiotic therapy with a topical fixed-dose combination of a retinoid, such as adapalene, and an anti-bacterial agent, such as benzoyl peroxide.
    Type: Application
    Filed: August 31, 2015
    Publication date: May 26, 2016
    Inventors: Jean-Charles DHUIN, Nabil KERROUCHE, Stéphanie ARSONNAUD, Pascale SOTO
  • Publication number: 20160143877
    Abstract: The present invention relates to a composition for suppressing adipocyte differentiation, for reducing fat accumulation in adipocytes and/or for promoting adiponectin secretion from adipocytes, including sesaminol as an active component. The present invention also relates to a method for suppressing adipocyte differentiation, for reducing fat accumulation in adipocytes and/or for promoting adiponectin secretion of adipocytes, including administering a composition including sesaminol as an active component.
    Type: Application
    Filed: June 2, 2014
    Publication date: May 26, 2016
    Inventors: Akiko KOJIMA, Isao YUASA, Kunio KIYOMOTO, Ayano OMURA
  • Publication number: 20160143878
    Abstract: An antibacterial agent comprising a compound represented by the following general formula (I), which can exhibit potent antibacterial activity against bacteria that have acquired resistance to quinolones (in the formula, R1 and R4 represents hydrogen atom, hydroxyl group, or a lower alkoxy group; R2 and R3 represents hydrogen atom or hydroxyl group; R5 represents hydrogen atom, a lower cyclic alkyl group, or a lower alkoxy group; R1? and R5? represents hydrogen atom; R2? and R3? represents hydrogen atom, hydroxyl group, or a lower alkoxy group; and R4? represents hydrogen atom or hydroxyl group).
    Type: Application
    Filed: February 8, 2016
    Publication date: May 26, 2016
    Applicant: JUNTENDO EDUCATIONAL FOUNDATION
    Inventors: Keiichi HIRAMATSU, Yuh MORIMOTO, Tadashi BABA
  • Publication number: 20160143879
    Abstract: Provided are methods and compositions for treating and preventing ulcers, ulceratic conditions and/or the symptoms thereof, including gastric, intestinal, e.g., duodenal, and colonic ulcers in non-human animals, especially horses. The methods involve treating an afflicted animal a compositions comprising effective amounts of one or more acid reducing or inhibiting drugs, such as antacids and/or a proton-ion pump inhibitors, and a therapeutically effective amount of a proanthocyanidin polymer from Croton lechleri, or a Croton lechleri extract, in either enteric or non-enteric form. The ulcer treatment compositions are formulated as a paste, gel, or gel paste containing associated microparticles comprising antacid, proton-ion inhibitor, and C. lechleri proanthocyanidin polymer or C. lechleri extract, as well as other components, to particularly provide a colon targeted delivery system to treat and prevent ulcers in animals in need.
    Type: Application
    Filed: November 3, 2015
    Publication date: May 26, 2016
    Inventor: Serge Martinod
  • Publication number: 20160143880
    Abstract: The invention relates to a novel use of the antimuscarinic agent glycopyrrolate, for example the salt glycopyrronium bromide. In particular, the invention relates to glycopyrrolate for use as a heart rate lowering agent and more particularly, but not exclusively, for use in patients suffering from respiratory conditions such as chronic obstructive pulmonary disease.
    Type: Application
    Filed: January 31, 2016
    Publication date: May 26, 2016
    Inventors: Susan SNAPE, Robert TANSLEY
  • Publication number: 20160143881
    Abstract: The present invention relates to a method of preventing and/or treating chronic traumatic encephalopathy.
    Type: Application
    Filed: July 2, 2014
    Publication date: May 26, 2016
    Applicant: EUSTRALIS PHARMACETICALS LIMITED (TRADING AS PRESSURA NEURO)
    Inventor: Robert Vink
  • Publication number: 20160143882
    Abstract: The invention relates to methods for treating pruritus with NK-1 receptor antagonists such as serlopitant. The invention further relates to pharmaceutical compositions comprising NK-1 receptor antagonists such as serlopitant. In addition, the invention encompasses treatment of a pruritus-associated condition with serlopitant and an additional antipruritic agent, and the use of serlopitant as a sleep aid, optionally in combination with an additional sleep-aiding agent.
    Type: Application
    Filed: June 24, 2014
    Publication date: May 26, 2016
    Inventors: Xiaoming ZHANG, Edward F. SCHNIPPER, Andrew J. PERLMAN, James W. LARRICK
  • Publication number: 20160143883
    Abstract: Invented is a method of treating thrombocytopenia in a human in need thereof which comprises the administration of a therapeutically effective amount of a 3?-{N?-[1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1,5-dihydropyrazol-4-ylidene]hydrazino}-2?-hydroxybiphenyl-3-carboxylic acid to such human.
    Type: Application
    Filed: December 21, 2015
    Publication date: May 26, 2016
    Applicant: NOVARTIS AG
    Inventors: Shivakumar G. Kapsi, Francis Xavier Muller, Mary Beth Wire
  • Publication number: 20160143884
    Abstract: Provided are methods of treating or inhibiting Human Immunodeficiency Virus (HIV) infection, or treating or inhibiting Acquired Human Immunodeficiency Syndrome (AIDS) in a subject in need thereof, comprising administering an Hsp90 inhibitor in a therapeutically effective amount.
    Type: Application
    Filed: November 25, 2015
    Publication date: May 26, 2016
    Inventors: Everardus O.M. Orlemans, Barton F. Haynes, Guido Ferrari, Timothy Haystead, Jesse John Kwiek
  • Publication number: 20160143885
    Abstract: Invented is a method of treating steroid responsive dermatoses in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a compound selected from the group consisting of: N-{(1S)-2-Amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide or a pharmaceutically acceptable salt thereof, and the compound N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide or a pharmaceutically acceptable salt thereof, to such mammal.
    Type: Application
    Filed: February 2, 2016
    Publication date: May 26, 2016
    Inventors: Pankaj Agarwal, Vinod KUMAR, Qing XIE
  • Publication number: 20160143886
    Abstract: A method and composition for the treatment of ischemic neuronal reperfusion injury are provided. The composition can include a compound which is a combination of dantrolene and a residue of FMOC-valine. This composition can be used to provide a faster and higher CNS penetration than heretofore experienced with dantrolene. In another form, dantrolene may be formulated as a pro-drug, a pro-pro-drug and the like.
    Type: Application
    Filed: January 28, 2016
    Publication date: May 26, 2016
    Applicant: Howard University
    Inventors: Harpal S. Mangat, Pradeep K. Karla
  • Publication number: 20160143887
    Abstract: Long term storage stable bendamustine-containing compositions are disclosed. The compositions can include bendamustine or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable fluid which can include in some embodiments PEG, PG or mixtures thereof and an antioxidant or chloride ion source. The bendamustine-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 223 nm, after at least about 15 months of storage at a temperature of from about 5° C. to about 25° C.
    Type: Application
    Filed: February 2, 2016
    Publication date: May 26, 2016
    Inventors: Nagesh R. Palepu, Philip Christopher Buxton
  • Publication number: 20160143888
    Abstract: Long term storage stable bendamustine-containing compositions are disclosed. The compositions can include bendamustine or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable fluid which can include in some embodiments PEG, PG or mixtures thereof and an antioxidant or chloride ion source. The bendamustine-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 223 nm, after at least about 15 months of storage at a temperature of from about 5° C. to about 25° C.
    Type: Application
    Filed: February 2, 2016
    Publication date: May 26, 2016
    Inventors: Nagesh R. Palepu, Philip Christopher Buxton
  • Publication number: 20160143889
    Abstract: Sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate is described. In addition, pharmaceutical compositions and uses of such compositions for the treatment of a variety of diseases and conditions are described.
    Type: Application
    Filed: November 12, 2015
    Publication date: May 26, 2016
    Inventors: Jeffrey MINER, Barry D. QUART, Jean-Luc GIRARDET
  • Publication number: 20160143890
    Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetyl choline esterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT3 receptor antagonist, a dopamine antagonist, a H1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholine esterase inhibitor are also described.
    Type: Application
    Filed: January 29, 2016
    Publication date: May 26, 2016
    Applicant: Chase Pharmaceuticals Corporation
    Inventors: Thomas N. CHASE, Kathleen E. CLARENCE-SMITH
  • Publication number: 20160143891
    Abstract: Provided herein are specific doses of, and dosing regimens for, using a HIF prolyl hydroxylase inhibitor in treating or preventing anemia, such as anemia secondary to or associated with chronic kidney disease, anemia associated with or resulting from chemotherapy, or anemia associated with AIDS.
    Type: Application
    Filed: June 4, 2014
    Publication date: May 26, 2016
    Applicant: Akebia Therapeutics, Inc.
    Inventors: Robert Shalwitz, Charlotte Hartman, Akshay Buch, Isaiah Shalwitz, John Janusz, Joseph Gardner
  • Publication number: 20160143892
    Abstract: A pharmaceutical dosage system comprising (a) an effective amount of one or more of Doxylamine, an analog thereof, a derivative thereof, a prodrug thereof, a metabolite thereof and/or a salt thereof; (b) an effective amount of one or more of (i) Pyridoxine, (ii) an analog thereof, (iii) a derivative thereof, (iv) a prodrug thereof, (v) a metabolite thereof and (vi) a salt of any of (i)-(v); and (c) an effective amount of one or more compounds of formula (I) wherein R is H, PO3 or. The system exhibits an improved pharmacokinetic profile relative to the current Diclectin®/Diclegis® formulation and is useful for example for the alleviation of the symptoms of nausea and vomiting, for example in the case of nausea and vomiting of pregnancy (NVP).
    Type: Application
    Filed: March 13, 2014
    Publication date: May 26, 2016
    Inventors: Manon VRANDERICK, Jean-Luc ST-ONGE, Michele GALLO, Éric GERVAIS
  • Publication number: 20160143893
    Abstract: The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Application
    Filed: July 3, 2014
    Publication date: May 26, 2016
    Inventors: Dirk KOSEMUND, Ulrich LÜCKING, Arne SCHOLZ, Gerhard SIEMEISTER, Philip Alexander LIENAU
  • Publication number: 20160143894
    Abstract: A crystalline Form N-1 of apixaban substantially free from one or more of: 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid; 7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-1-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide; or methyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate, relative to apixaban by area percentage of HPLC and having a mean particle size equal to or greater than 100 ?m.
    Type: Application
    Filed: November 24, 2015
    Publication date: May 26, 2016
    Inventors: Brij KHERA, Kumar Kamlesh SINGH, Santosh Devidas DIWAKAR, Sunil Dnyaneshwar NARODE, Hiteshkumar Natwarlal SUTHAR
  • Publication number: 20160143895
    Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: June 19, 2014
    Publication date: May 26, 2016
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shuwen He, Zhong Lai, Xing Dai, Dong Xiao, Clare London, Nicolas Zorn, Ravi Nargund, Anandan Palani, Casey C. McComas, Peng Li, Xuanjia Peng, Richard Soll
  • Publication number: 20160143896
    Abstract: Chiral 1-(4-methylphenylmethyl)-5-oxo-{N-[(3-t-butoxycarbonyl-aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion. The present invention provides chiral (2S)-1-(4-methyl-phenylmethyl)-5-oxo-(3S)-{N-[(3-t-butoxycarbonyl aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide, and (2S)-1-(4-methylphenylmethyl)-5-oxo-(3R)-{N-[(3-t-butoxycarbonyl amino methyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamide of formula 6 and 7 respectively. The present invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors. The present invention provides a process for preparation of chiral carboxamides of formula 6 and 7 using the process which has advantage to avoid any racemization at the a-carboxylic center, during N-alkylation. The reagent LiHMDS is used at low temperatures to furnish methyl N-(p-methylphenylmethyl)1pyroglutamate in good chiral purity.
    Type: Application
    Filed: November 5, 2015
    Publication date: May 26, 2016
    Inventors: Dinesh Kumar DIKSHIT, Madhu DIKSHIT, Tanveer Irshad SIDDIQUI, Anil KUMAR, Rabi Sankar BHATTA, Girish Kumar JAIN, Manoj Kumar BARTHWAL, Ankita MISRA, Vivek KHANNA, Prem PRAKASH, Manish JAIN, Vishal SINGH, Varsha GUPTA, Anil Kumar DWIVEDI
  • Publication number: 20160143897
    Abstract: The invention provides two crystalline freebase forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester. The invention also provides pharmaceutical compositions comprising the crystalline freebase or prepared using the crystalline freebases; processes and intermediates for preparing the crystalline freebases; and methods of using the crystalline freebases to treat a pulmonary disorder.
    Type: Application
    Filed: December 1, 2015
    Publication date: May 26, 2016
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventor: Grahame Woollam
  • Publication number: 20160143898
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: October 28, 2015
    Publication date: May 26, 2016
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • Publication number: 20160143899
    Abstract: A method for treating abnormal ?-amyloid mediated diseases is disclosed, comprising administering a pharmaceutical composition to a subject in need, wherein the pharmaceutical composition comprises an indolylquinoline derivative represented by the following formula 1:
    Type: Application
    Filed: May 12, 2015
    Publication date: May 26, 2016
    Inventors: Guey-Jen LEE-CHEN, Hsiu-Mei HSIEH, Ching-Fa YAO
  • Publication number: 20160143900
    Abstract: The present invention relates to the use of camptothecin derivatives as anti-HIV agents that disrupt self-association of the viral infectivity factor (Vif) found in HIV and other retroviruses. The present invention also relates to methods of identifying agents that disrupt VIf self-association and methods of using these agents, including methods of treating or preventing HIV infection.
    Type: Application
    Filed: June 24, 2014
    Publication date: May 26, 2016
    Applicant: OyaGen, Inc.
    Inventors: Harold C. SMITH, Ryan P. BENNETT
  • Publication number: 20160143901
    Abstract: This disclosure provides pharmaceutical compositions comprising dextromethorphan in combination with quinidine, and methods for treating agitation and/or aggression in subjects with dementia by administering such compositions.
    Type: Application
    Filed: September 14, 2015
    Publication date: May 26, 2016
    Inventors: Joao SIFFERT, James BERG
  • Publication number: 20160143902
    Abstract: Provided herein are compositions comprising a dextromethorphan analog according to Formula I or Formula II or a pharmaceutically acceptable salt thereof of either of the foregoing, and a co-agent, e.g., an antidepressant such as a serotonin norepinephrine reuptake inhibitor; a serotonin noradrenaline dopamine reuptake inhibitor; a norepinephrine dopamine reuptake inhibitor; a monoamine oxidase inhibitor; a selective serotonin reuptake inhibitor; and a tricyclic antidepressant or a pharmaceutically acceptable salt of any of the foregoing. The compositions are useful in the the treatment of pseudobulbar affect, neuropathic pain, neurodegenerative diseases, brain injuries, and the like.
    Type: Application
    Filed: November 30, 2015
    Publication date: May 26, 2016
    Inventor: Amanda Thomas
  • Publication number: 20160143903
    Abstract: Disclosed are methods of providing weight loss therapy, particularly for patients suffering from major depression.
    Type: Application
    Filed: January 29, 2016
    Publication date: May 26, 2016
    Inventors: Eduardo Dunayevich, Gary D. Tollefson
  • Publication number: 20160143904
    Abstract: The invention relates to (among other things) oligomer modified diaromatic substituted compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over non-oligomer modified diaromatic substituted compounds.
    Type: Application
    Filed: November 24, 2015
    Publication date: May 26, 2016
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
  • Publication number: 20160143905
    Abstract: Provided is a superior, novel heterocyclic compound with improved solubility in oil such as sesame oil and benzyl benzoate, which has a broader treatment spectrum, causes less side effects, and is superior in tolerability and safety, and use thereof. A heterocyclic compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: December 29, 2015
    Publication date: May 26, 2016
    Applicant: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Yamashita, Yohji Sakurai, Motoyuki Miyamoto, Yuichi Nakamura, Hideaki Kuroda, Takuya Minowa
  • Publication number: 20160143906
    Abstract: The present invention relates to a beneficial treatment of tumours in patients suffering from NSCLC, and to a clinical marker useful as predictive variable of the responsiveness of tumours in patients suffering from NSCLC. The present invention further relates to a method for selecting patients likely to respond to a given therapy, wherein said method optionally comprises the use of a specific clinical marker. The present invention further relates to a method for delaying disease progression and/or prolonging patient survival of NSCLC patients, wherein said method comprises the use of a specific clinical marker.
    Type: Application
    Filed: January 29, 2016
    Publication date: May 26, 2016
    Inventors: Birgit GASCHLER-MARKEFSKI, Rolf KAISER
  • Publication number: 20160143907
    Abstract: Methods for treating a subject infected with Clostridium difficile comprises administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of clofazimine and/or a clofazimine analogue. Pharmaceutical compositions comprising clofazimine and/or an analogue(s) thereof, and optionally one or more additional therapeutic agents, are provided for treating Clostridium difficile infection and diseases or symptoms associated therewith.
    Type: Application
    Filed: November 20, 2015
    Publication date: May 26, 2016
    Applicant: KamTek, Inc.
    Inventors: Venkata M. Reddy, Wolf Prensky, Sharanjit VedBrat
  • Publication number: 20160143908
    Abstract: This application discloses a composition comprising an amiloride and/or an amiloride analog which can be used for reducing nerve injury or nervous system injury in a subject. The formulation of such composition is also disclosed. The application further directs to methods for treating nerve injury or nervous system injury by administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising amiloride, an amiloride analog or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 19, 2015
    Publication date: May 26, 2016
    Inventors: Zhigang XIONG, Roger P. Simon