Patents Issued in April 9, 2015
  • Publication number: 20150099694
    Abstract: Devices, systems, and methods for strain-specific identification and assessment of susceptibility of microorganisms based on the response of sensors in a colorimetric sensor array to metabolic products of the microorganism.
    Type: Application
    Filed: April 26, 2013
    Publication date: April 9, 2015
    Applicant: Specific Technologies LLC
    Inventors: Sung Hyun Lim, Raymond Anthony Martino, Paul A. Rhodes
  • Publication number: 20150099695
    Abstract: Compositions and methods for treatment of obesity and/or Type II diabetes and related metabolic disorders are provided wherein the methods and treatments comprise an effective amount of an isolated and/or purified C1q/TNF-related Protein-9 (CTRP9) or a functional portion thereof, and a pharmaceutically acceptable carrier. Methods of screening for molecules which elevate levels of CTRP9 in vivo are also provided. The present inventors provide the first in vivo evidence linking CTRP9 to regulation of fat metabolism in liver and skeletal muscle via AMPK signaling pathway, and highlight its protective metabolic function in the context of HFD-mediated metabolic insults.
    Type: Application
    Filed: May 28, 2013
    Publication date: April 9, 2015
    Inventors: Guang William Wong, Jonathan M. Peterson
  • Publication number: 20150099696
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.
    Type: Application
    Filed: June 26, 2012
    Publication date: April 9, 2015
    Applicant: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
  • Publication number: 20150099697
    Abstract: Described herein is a treatment comprising the following step: (a) injecting a therapeutically effective amount of a pharmaceutical composition into the celiac artery of an individual, wherein the pharmaceutical composition reverses recent onset Type 1 Diabetes (T1D). Also described is a method for identifying an individual who will be responsive to this treatment. In addition there is described a device containing the pharmaceutical composition for injecting the pharmaceutical composition into the celiac artery.
    Type: Application
    Filed: April 4, 2014
    Publication date: April 9, 2015
    Inventor: Hans-Michael DOSCH
  • Publication number: 20150099698
    Abstract: Nanoparticles having a core and a corona of ligands covalently linked to the core, wherein differing species of peptides are bound to the nanoparticles and incorporated into various dosage forms.
    Type: Application
    Filed: October 8, 2013
    Publication date: April 9, 2015
    Inventors: Phillip Williams, Thomas Rademacher, Alexander Mark Schobel, Eric Dadey
  • Publication number: 20150099699
    Abstract: A conjugate consisting of an insulin-like growth factor-1 (IGF-I) variant and one or two poly(ethylene glycol) group(s), characterized in that said IGF-I variant has an amino acid alteration at up to three amino acid positions 27, 37, 65, 68 of the wild-type IGF-I amino acid sequence so that one or two of said amino acids is/are lysine and amino acid 27 is a polar amino acid but not lysine, is conjugated via the primary amino group(s) of said lysine(s) and said poly(ethylene glycol) group(s) have an overall molecular weight of from 20 to 100 kDa is disclosed. This conjugate is useful for the treatment of neurodegenerative disorders like Alzheimer's Disease.
    Type: Application
    Filed: September 10, 2014
    Publication date: April 9, 2015
    Inventors: Beat Amrein, Stefan Foser, Kurt Lang, Friedrich Metzger, Joerg Thomas Regula, Andreas Schaubmar, Friederike Hesse, Klaus-Peter Kuenkele, Martin Lanzendoerfer
  • Publication number: 20150099700
    Abstract: Diagnostic and therapeutic methods pertaining to diseases and disorders of the breast, uterus and ovary are encompassed herein. More particularly, diagnostic methods for early detection of progenitor cells of breast, uterine, and ovarian cancers are described herein. The identification of markers for these cancer predisposing progenitor cells, which co-express the progesterone receptor (PR) and p63, provides tools and methods of use thereof that facilitate early detection of increased frequency of PR/p63 double positive (PR/p63+) progenitor cells in asymptomatic patients and thus, early detection of increased cancer risk in such patients and assessment, diagnostic stratification, and evaluation of therapeutic intervention in symptomatic patients.
    Type: Application
    Filed: September 16, 2014
    Publication date: April 9, 2015
    Inventors: David L. Kleinberg, Mary Helen Barcellos-Hoff
  • Publication number: 20150099701
    Abstract: The present invention provides acidic fibroblast growth factor (aFGF) composition, comprising: (i) aFGF of SEQ ID NO: 1, (ii) aFGF of SEQ ID NO: 1 having an N-terminal phosphogluconoylation, (iii) aFGF of SEQ ID NO: 1 having an N-terminal gluconoylation, (iv) aFGF of SEQ ID NO: 2 and (v) aFGF of SEQ ID NO: 3, or a combination thereof. Also provided is a modified acidic fibroblast growth factor (aFGF) which has an N-terminal phosphogluconoylation or gluconoylation.
    Type: Application
    Filed: October 7, 2014
    Publication date: April 9, 2015
    Inventor: Ya-Hui Lee
  • Publication number: 20150099702
    Abstract: This invention is directed to the compositions and methods for inducing female gonad maturation in crustacean species such as shrimp, lobster or crab. In one embodiment, the composition for inducing gonad maturation comprises a dsRNA corresponding to the GIH DNA, recombinant protein of a gonad stimulatory hormone (GSH) and farnesoic acid (FA). In another embodiment, the composition for inducing gonad maturation comprises a dsRNA corresponding to the GIH DNA, recombinant MeMIH-B protein and farnesoic acid (FA).
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventor: Siu Ming CHAN
  • Publication number: 20150099703
    Abstract: The present invention refers to the use of certain sulfated glycosaminoglycans for treatment or prevention of postpartum haemorrhage. The sulfated glycosaminoglycans have a reduced anticoagulant activity and are administered in combination with at least one uterotonic agent capable of promoting myometrial contractions of the uterus and thereby compress the vessels and cease the bleeding.
    Type: Application
    Filed: May 7, 2013
    Publication date: April 9, 2015
    Inventors: Gunvor Ekman-Ordeberg, Anders Malmström
  • Publication number: 20150099704
    Abstract: In an embodiment, the present disclosure pertains to a composition for inhibiting calcium oxalate monohydrate crystal growth comprising at least one isolated polypeptide comprising a plurality of amino acids that bind the surface of the calcium oxalate monohydrate crystal; and a plurality of amino acids spacers, wherein the amino acid spacers are arranged in varying sequences between the plurality of amino acids that bind the surface of the calcium oxalate monohydrate crystal. In some embodiments, the present disclosure related to a method of controlling calcium oxalate monohydrate crystal growth in a subject in need thereof comprising administering to the subject therapeutically effective amount of the calcium oxalate monohydrate inhibiting polypeptide. In some embodiments, the present disclosure relates to a method of identifying calcium oxalate monohydrate inhibiting peptides.
    Type: Application
    Filed: July 9, 2014
    Publication date: April 9, 2015
    Applicants: University of Houston, Rensselaer Polytechnic Institute
    Inventors: Jeffrey D. Rimer, Pankaj Karande
  • Publication number: 20150099705
    Abstract: The present invention relates to Protoxin-II variants, polynucleotides encoding them, and methods of making and using the foregoing.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Mack FLINSPACH, Alan Wickenden, Ross Fellows, Robert Neff, Yi Liu, Rebecca Hagan, Qinghao Xu
  • Publication number: 20150099706
    Abstract: Methods and compositions used in treating ischemic stroke using a recombinant DR?-MOG-35-55 construct are disclosed. The disclosed methods involve administering a pharmaceutical composition comprising DR?-MOG-35-55 and a pharmaceutically acceptable carrier to a subject that has had or is at risk of developing ischemic stroke.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Halina Offner-Vandenbark, Nabil Alkayed, Arthur A. Vandenbark
  • Publication number: 20150099707
    Abstract: The invention provides a Pseudomonas exotoxin A (PE) comprising an amino acid sequence having a substitution of one or more B-cell and/or T-cell epitopes. The invention further provides related chimeric molecules, as well as related nucleic acids, recombinant expression vectors, host cells, populations of cells, and pharmaceutical compositions. Methods of treating or preventing cancer in a mammal, methods of inhibiting the growth of a target cell, methods of producing the PE, and methods of producing the chimeric molecule are further provided by the invention.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Ira H. Pastan, Ronit Mazor, Masanori Onda, Byungkook Lee, Gerhard Niederfellner, Sabine Imhof-Jung, Ulrich Brinkmann, Werner Scheuer, Guy Georges
  • Publication number: 20150099708
    Abstract: The invention provides novel Wnt polypeptides that have improved production characteristics, solubility, systemic delivery, and tissue uptake, and polynucleotides encoding the Wnt polypeptides of the invention. The Wnt polypeptides of the invention can be used therapeutically, such as, for example, in methods of preventing or treating muscle loss and/or promoting muscle hypertrophy and growth.
    Type: Application
    Filed: September 14, 2012
    Publication date: April 9, 2015
    Inventors: Tom Tong Lee, Michael J. Fitch, Kevin Lai, Peter Flynn, Monica Bennett
  • Publication number: 20150099709
    Abstract: The present invention relates to a use of a compound having ghrelin receptor agonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for treatment of diseases including achlorhydria in which abnormal gastric acid secretion is involved. In addition, the present invention relates to the method of treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agents. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound of the present invention or a pharmaceutically acceptable salt thereof for the treatment of said diseases.
    Type: Application
    Filed: May 27, 2013
    Publication date: April 9, 2015
    Inventors: Nobuyuki Takahashi, Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi
  • Publication number: 20150099710
    Abstract: Objects are to provide an additive for a feed which can improve growth performance and meat quality of livestock, and can improve palatability of the feed, a feed and a method for preparing the feed, and the objects can be solved by an additive for a feed which comprises at least one or two or more of a polyphenol derived from EFB, ?-tocopherol derived from EFB and xyloses derived from EFB, a feed which comprises an additive for a feed being added to a formulating material for a feed in the range of 0.05 to 20% by weight with a dry basis, and a method for preparing the feed.
    Type: Application
    Filed: December 21, 2012
    Publication date: April 9, 2015
    Inventors: Shunichiro Nishioka, Eri Ishikawa, Toshimi Tsukada, Masamori Kato, Masaaki Toyomizu, Motoi Kikusato, Tomomi Kamizono
  • Publication number: 20150099711
    Abstract: A method for modifying a quality of a fruit includes cutting a live stem attached to a live fruit at a cut distance from the fruit, producing a cut end of the stem, contacting only the cut end of the stem with a solution comprising at least one mobile and quality-modifying food ingredient while protecting the fruit from contact with the solution, and keeping the cut end of the stem in contact with the solution for an incubation time sufficient to allow absorption and transport of the food ingredient into the fruit, the food ingredient conferring a modified quality upon the fruit. A system for practicing the method and an edible raw plant product produced by the method are also disclosed.
    Type: Application
    Filed: April 7, 2014
    Publication date: April 9, 2015
    Applicant: Nightshade, LLC
    Inventors: Caius D. Rommens, Heather M. Holloway, Roy D. Holloway
  • Publication number: 20150099712
    Abstract: A method for treating cancer by using an agent which is capable of inhibiting the functionality of the MCM complex, a heterohexameric ring formed from six subunits, in the process of DNA replication and a method of screening for such agents by detecting the locations and functions of the MCM subunits, such as hMcm2 and hMcm6, in cells treated with candidate compounds.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 9, 2015
    Inventors: Chun Liang, Zhihong Jiang, Ziyi Wang, Zhiling Yu, Jingrong Wang, Liping Bai
  • Publication number: 20150099713
    Abstract: Disclosed is a method of manipulating the rate of gastrointestinal transit in a mammalian subject. Also disclosed is the use, in the manufactiurc of a medicament for the treatment of constipation, of a selective inhibitor of methanogensis, a methanogen-displacing probiotic agent, or a prebiotic agent that inhibits the growth of methanogenic bacteria or promotes the growth of competing non-methanogenic intestinal flora. Alternatively, in accordance with the invention, is disclosed the use in the manufacture of a medicament for the treatment of diarrhea, of methane or a methane precursor, a methanogenic or other methane-enhancing probiotic agent, or a methanogenesis-enhancing prebiotic agent.
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: Mark Pimentel, Henry C. Lin
  • Publication number: 20150099714
    Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
  • Publication number: 20150099715
    Abstract: This invention provides a buffered solution comprising acadesine, as well as compositions, formulations and kits containing said solution. The solution, compositions, formulation, and kits can be used to prevent morbidity/mortality in a patient or to treat an ischaemic condition, a condition regulated by adenosine, or a condition associated with reduced blood flow to a tissue in a patient.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Valentyn Antochshuk, Mohammed Shameem, Amadeep Singh Bhupender BHALLA
  • Publication number: 20150099716
    Abstract: A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure is described. The method of this invention can be used for patients in need of antiplatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding.
    Type: Application
    Filed: May 5, 2014
    Publication date: April 9, 2015
    Applicant: The Medicines Company
    Inventors: Lisa Ruderman Chen, Simona Skerjanec, Dawn Bell, Jayne Prats, Meredith Todd
  • Publication number: 20150099717
    Abstract: A method of treating a vaginal or vulvar vestibule mucosa disorder involves administering a composition comprising a hyaluronic acid or a salt thereof to the vagina, vulvar or vulvar vestibule of an individual that has the disorder to treat the disorder. The method may be used to treat vaginal atrophy or vulvar vestibulitis syndrome, among other vulvovaginal mucosa disorders.
    Type: Application
    Filed: October 7, 2013
    Publication date: April 9, 2015
    Inventors: Denis Couchourel, Elena Fasola
  • Publication number: 20150099718
    Abstract: The invention provides the use in combination of a heparin containing composition that has anticoagulant activity when used alone, such as an unfractionated heparin or low molecular weight heparin, in combination with an inhibitor of the anticoagulation activity/effect or effect of heparin, for the inhibition of metastasis.
    Type: Application
    Filed: December 9, 2014
    Publication date: April 9, 2015
    Inventor: Eugene J. Oliva
  • Publication number: 20150099719
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Shawn Stachel, Daniel V. Paone, Jing Li, Kausik Nanda
  • Publication number: 20150099720
    Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.
    Type: Application
    Filed: October 20, 2014
    Publication date: April 9, 2015
    Inventors: Lin Zhi, Robert I. Higuchi, E. Adam Kallel, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Daniel A. Ruppar, Bijan Pedram, Thomas Lot Stevens Lau, Todd A. Miller
  • Publication number: 20150099721
    Abstract: A method for treating cancer with a mutation in ROS or RET, comprising identifying a subject with a cancer with a mutation in ROS or RET, and administering to the subject an effective amount of a compound according to formulae (I) OR (la) or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein.
    Type: Application
    Filed: May 10, 2013
    Publication date: April 9, 2015
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jaime Acquaviva, Suqin He, David Proia
  • Publication number: 20150099722
    Abstract: The invention relates to compounds which are useful as inhibitors of 6-oxopurine phosphoribosyltransferases such as hypoxanthine-guanine-(xanthine) phosphoribosyltransferase (HG(X)PRT).
    Type: Application
    Filed: May 7, 2013
    Publication date: April 9, 2015
    Inventors: John De Jersey, Luke William Guddat, Dana Hockova, Dianne Therese Keough
  • Publication number: 20150099723
    Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.
    Type: Application
    Filed: April 11, 2014
    Publication date: April 9, 2015
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. MILNE, Michael R. JIROUSEK, Jean E. Bemis, Jesse J. Smith
  • Publication number: 20150099724
    Abstract: The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.
    Type: Application
    Filed: August 14, 2014
    Publication date: April 9, 2015
    Inventors: Luigi Anzalone, Frank J. Villani, Christopher A. Teleha, Penina Feibush, Barry Fegely
  • Publication number: 20150099725
    Abstract: The present patent application relates to a method of treating allergic rhinitis in a subject (preferably a human) by administering a combination of mometasone or its salt and olopatadine or its salt.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Neelima KHAIRATKAR-JOSHI, Abhay KULKARNI, Dinesh Pradeep WALE, Vikram Mansingh BHOSALE, Piyush AGARWAL, Patrick KEOHANE, Sudeesh K. TANTRY, Chad OH
  • Publication number: 20150099726
    Abstract: This invention provides a dry powder inhaler comprising: a dry powder medicament comprising fluticasone propionate, salmeterol xinafoate and a lactose carrier; wherein, the delivered dose of salmeterol per actuation is less than 50 ?g; and wherein the dose provides a baseline-adjusted FEV1 in a patient of more than 150 mL within 30 minutes of receiving the dose. A method of treating a patient includes administering to a patient a dry powder medicament having fluticasone propionate, salmeterol xinafoate and a lactose carrier; wherein, the delivered dose of salmeterol per actuation is less than 50 ?g; and wherein the dose provides a baseline-adjusted FEV1 in a patient of more than 150 mL within 30 minutes of receiving the dose.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Applicant: Teva Branded Pharmaceutical Products R&D, Inc.
    Inventors: Mukul DALVI, Seah Kee TEE
  • Publication number: 20150099727
    Abstract: This application is directed to the use of aminosteroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.
    Type: Application
    Filed: April 19, 2013
    Publication date: April 9, 2015
    Applicant: Ohr Pharmaceutical Inc.
    Inventors: Michael McLane, Inez Ruiz-White, W. Lee Maloy, Henry R. Wolfe
  • Publication number: 20150099728
    Abstract: Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Publication number: 20150099729
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Fa-Xiang Ding, Shuzhi Dong, Jessica Frie, Xin Gu, Jinlong Jiang, Alexander Pasternak, Haifeng Tang, Zhicai Wu, Yang Yu, Takao Suzuki
  • Publication number: 20150099730
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.
    Type: Application
    Filed: September 6, 2013
    Publication date: April 9, 2015
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Peter J. Connolly
  • Publication number: 20150099731
    Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 me
    Type: Application
    Filed: May 5, 2014
    Publication date: April 9, 2015
    Applicant: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Publication number: 20150099732
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.
    Type: Application
    Filed: March 7, 2013
    Publication date: April 9, 2015
    Inventors: Alan Ashworth, Christopher James Lord, Richard James Rowland Elliot, Dan Niculescu-Duvaz, Roderick Porter, Raymond John Boffey, Melanie Jayne Bayford, Stuart Firth-Clark, Ashley Nicholas Jarvis, Trevor Robert Perrior, Rebekah Elisabeth Key
  • Publication number: 20150099733
    Abstract: Compounds represented by the following formula (I); wherein each symbol is as defined in the specification, are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 9, 2015
    Applicant: AJINOMOTO CO., INC.
    Inventors: Takahiro KOSHIBA, Munetaka TOKUMASU, Taisuke ICHIMARU, Koji OHSUMI, Tadakiyo NAKAGAWA, Tatsuhiro YAMADA, Kayo MATSUMOTO, Tamotsu SUZUKI
  • Publication number: 20150099734
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Daniel HUNZIKER, Patrizio MATTEI, Harald MAUSER, Marco PRUNOTTO, Christoph ULLMER
  • Publication number: 20150099735
    Abstract: The invention is concerned with triazolopyridine compounds of formula (I) wherein R1, R2 and R3 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: December 16, 2014
    Publication date: April 9, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner
  • Publication number: 20150099736
    Abstract: Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(?O)OH, carboxy-(C1-C3)-alkyl, or —C(?O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(?O)—N(—R16)— or —N(—R17)—C(?O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substitu
    Type: Application
    Filed: November 10, 2014
    Publication date: April 9, 2015
    Inventors: Stephen Stokes, Nicolas Foloppe, Andrea Fiumana, Martin Drysdale, Simon Bedford, Paul Webb
  • Publication number: 20150099737
    Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R1, R2y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: NOVARTIS AG
    Inventors: Christopher Thomas BRAIN, Young Shin CHO, John William GIRALDES, Bharat LAGU, Julian Roy LEVELL, Michael Joseph LUZZIO, Lawrence Blas PEREZ, Yaping WANG, Fan YANG
  • Publication number: 20150099738
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Application
    Filed: June 30, 2014
    Publication date: April 9, 2015
    Inventors: Mark L. BEHNKE, Alfredo C. CASTRO, Lawrence K. CHAN, Catherine A. EVANS, Louis GRENIER, Michael J. GROGAN, Yves LEBLANC, Tao LIU, Stephane PELUSO, Daniel A. SNYDER, Thomas T. TIBBITTS
  • Publication number: 20150099739
    Abstract: Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.
    Type: Application
    Filed: July 29, 2014
    Publication date: April 9, 2015
    Inventors: Padmanabh P. Bhatt, Argaw Kidane, Kevin Edwards
  • Publication number: 20150099740
    Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
  • Publication number: 20150099741
    Abstract: Disclosed are methods and kits for diagnosing, prognosing, and treating patients having psychiatric disorders. The methods may include assessing whether a patient has a treatment resistant psychiatric disorder or assessing whether the patient is likely to develop a treatment resistant psychiatric disorder. The methods may include detecting genetic markers such as the single nucleotide polymorphism (SNP) in genes present in a genomic nucleic acid sample from the patient, and/or receiving, as a caregiver, the results of tests indicating whether the genetic markers are present in the genomic nucleic acid sample from the patient. The methods may include administering treatment to the patient, for example, based on the detected genetic markers, and administering treatment may include administering new antipsychotic drugs (APDs) that are trace amine-associated receptor 1 (TAAR1) agonists.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Applicant: Northwestern University
    Inventors: Jiang Li, Herbert Y. Meltzer
  • Publication number: 20150099742
    Abstract: The present invention relates to a substance for the treatment of the phantom phenomena of tinnitus and/or phantom pain, a method for the diagnosis and for the treatment of these phantom phenomena.
    Type: Application
    Filed: December 16, 2014
    Publication date: April 9, 2015
    Applicant: OTOLANUM AG
    Inventors: Marlies KNIPPER-BREER, Lukas Rüttiger
  • Publication number: 20150099743
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Hui LI, Seiji NUKUI, Stephanie Anne SCALES, Min TENG, Chunfeng YIN