Nitrogen In Q Patents (Class 514/603)
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Publication number: 20140163110Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 10, 2013Publication date: June 12, 2014Applicant: GENENTECH, INC.Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
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Publication number: 20140163017Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 19, 2013Publication date: June 12, 2014Applicant: UNIVERSITY OF UTAHInventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
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Patent number: 8722669Abstract: A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.Type: GrantFiled: June 8, 2012Date of Patent: May 13, 2014Assignee: Case Western Reserve UniversityInventors: Krzysztof Palczewski, Akiko Maeda, Marcin Golczak
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COMPOUNDS AND METHODS FOR MODULATING MITOCHONDRIAL METABOLISM AND REACTIVE OXYGEN SPECIES PRODUCTION
Publication number: 20140128352Abstract: Compounds that modulate mitochondrial reactive oxygen species (ROS) production are provided. The compounds may modulate ROS production at defined sites without also altering energy production. Methods of using and identifying such compounds are also provided.Type: ApplicationFiled: September 20, 2013Publication date: May 8, 2014Applicant: Buck Institute for Research on AgingInventors: Martin D. Brand, Adam Orr -
Publication number: 20140121211Abstract: Disclosed herein are thiol mediated/activated prodrugs of SO2, particularly 2,4-dinitrophenylsulfonamide analogues, having Formula-I or pharmaceutically acceptable salts thereof exhibiting tunable release profiles of SO2 with significant therapeutic efficacy against bacterial infections. Further, the present invention provides pharmaceutical compositions comprising compound of Formula I or pharmaceutically acceptable salts thereof, along with pharmaceutically acceptable carriers/excipients.Type: ApplicationFiled: November 30, 2012Publication date: May 1, 2014Applicant: INDIAN INSTITUTE OF SCIENCE EDUCATION AND RESEARCH -PUNEInventors: Harinath CHAKRAPANI, Satish Ramesh Malwal
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Publication number: 20140107160Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: October 9, 2013Publication date: April 17, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Geraldine C.B. Harriman, Zhan Shi, B. Shaowu Chen
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Publication number: 20140094445Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: August 15, 2012Publication date: April 3, 2014Applicant: University of Utah Research FoundationInventors: Hariprasad Vakayalapati, Venkataswamy Soma, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
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Patent number: 8673910Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds. In one embodiment, a compound of the invention has the chemical structure shown in formula I: or a pharmaceutically acceptable salt or hydrate thereof. In another embodiment, a compound of the invention has the chemical structure shown in formula II: or a pharmaceutically acceptable salt or hydrate thereof.Type: GrantFiled: June 30, 2009Date of Patent: March 18, 2014Assignees: H. Lee Moffitt Cancer Center and Research Institute, University of South FloridaInventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
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Patent number: 8669261Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.Type: GrantFiled: April 30, 2013Date of Patent: March 11, 2014Assignee: Congenia SLRInventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
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Publication number: 20140066504Abstract: Novel analogs and prodrugs of the loop diuretic bumetanide are described. Pharmaceutical compositions containing bumetanide analogs and prodrugs are also described. These analogs and prodrugs are particularly useful for the treatment and/or prophylaxis of conditions that involve the NKCC cotransporter family (NKCC1 and NKCC2), or the KCC cotransporter family (KCC1, KCC2, KCC3, KCC4), or GABAa receptors. Such conditions include, but are not limited to anxiety disorders, epilepsy, migraine, non-epileptic seizures, sleep disorders, obesity, eating disorders, autism, depression, edema, glaucoma, stroke, ischemia, neuropathic pain, addictive disorders, schizophrenia, psychosis, and tinnitus.Type: ApplicationFiled: September 3, 2013Publication date: March 6, 2014Inventor: Daryl W. HOCHMAN
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Publication number: 20140065246Abstract: Tumor cells exhibit consistent abnormalities in calcium regulation. The present disclosure teaches methods by which such differences are exploited to induce Apoptosis selectively in tumor/cancer cells while sparing normal cells. These methods are based upon employing drugs that, acting in synergistic combinations, trigger selective killing of malignant cells. Since the invention is based upon fundamental cell cycle requirements, to the extent that calcium handling abnormalities are a general characteristic of the malignant state, the methods presented here are widely applicable regardless of tissue of origin and degree of cellular de-differentiation.Type: ApplicationFiled: November 6, 2013Publication date: March 6, 2014Inventor: Charles E. Zeilig
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Publication number: 20140051716Abstract: There is provided a compound which is a histone deacetylase (HDAC) inhibitor, or a pharmaceutically acceptable ester, amide, solvate or salt thereof, for use in: (I) treating or preventing a pathological condition associated with excess fibrin deposition and/or thrombus formation; and/or (II) potentiating the degradation of fibrin deposits and preventing such deposits associated with pathological conditions or which may lead to such conditions, wherein the HDAC inhibitor, and the dose thereof, is as described in the description. There is also provided valproic acid, or a pharmaceutically acceptable salt thereof, for use in improving or normalizing endogenous fibrinolysis impaired by local or systemic inflammation.Type: ApplicationFiled: March 9, 2012Publication date: February 20, 2014Applicant: Cereno Scientific ABInventors: Pia Larsson, Niklas Bergh, Sverker Jern
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Patent number: 8653002Abstract: The present invention relates to aqueous suspension concentrate formulation for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its crystalline anhydrate; at least one non-ionic surfactant selected from polyoxyethylene-polyoxy-C3-C4-alkylene block copolymers; at least one anionic surfactant comprising at least one arylsulfonate group; and water; wherein the pH value of the formulation is in the range of 3 to 7.Type: GrantFiled: August 26, 2010Date of Patent: February 18, 2014Assignee: BASF SEInventors: Michael Krapp, Wolfgang Gregori, Klaus Kolb, Bernd Sievernich, Heidi Emilia Saxell, Joerg Steuerwald, Steven Bowe, Rex Liebl, Terrance M. Cannan
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Patent number: 8653141Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: April 19, 2012Date of Patent: February 18, 2014Assignee: AbbVie Inc.Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
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Patent number: 8647615Abstract: A method for attracting honey bee parasitic mites to an object or area, involving treating the object or area with a composition containing a honey bee parasitic mites attracting effective amount of at least one compound selected from butyric acid, isobutyric acid, or mixtures thereof, and optionally a carrier or carrier material.Type: GrantFiled: August 29, 2011Date of Patent: February 11, 2014Assignee: The United States of America, as represented by the Secretary of AgricultureInventors: Peter EA Teal, Adrian J. Duehl, Mark J. Carroll
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Publication number: 20140031395Abstract: The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.Type: ApplicationFiled: February 2, 2012Publication date: January 30, 2014Applicant: Bionomics LimitedInventors: Andrew Harvey, Audrey Fluck, Bruno Giethlen, Dharam Paul, Laurent Schaeffer
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Publication number: 20140031429Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: May 23, 2013Publication date: January 30, 2014Inventors: Keizo Koya, Weiwen Ying, Teresa Kowalczyk-Prezewloka, Lijun Sun
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Publication number: 20140024608Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: March 14, 2013Publication date: January 23, 2014Applicant: METHYLGENE INC.Inventors: Robert Deziel, Alain Ajamian
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Patent number: 8633228Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(?G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.Type: GrantFiled: June 29, 2009Date of Patent: January 21, 2014Assignee: Mitsui Chemicals Agro, Inc.Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
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Publication number: 20130331313Abstract: Provided are methods and compositions for the prevention and/or treatment of viral conditions, virally-induced conditions and inflammatory conditions. The methods can comprise administering to a subject a viral inducing agent with an antiviral agent, and optionally an additional agent. The viral inducing agent can be a HDAC inhibitor administered orally.Type: ApplicationFiled: June 7, 2013Publication date: December 12, 2013Inventors: Ronald J. Berenson, Douglas V. Faller
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Publication number: 20130303491Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: July 22, 2013Publication date: November 14, 2013Applicant: Siga Technologies Inc.Inventors: Chelsea M. Byrd, Robert Jordan, Dongcheng Dai, Tove Bolken, Dennis E. Hruby
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Publication number: 20130287841Abstract: The invention relates to medicine, and specifically to synthetic biologically active derivatives of carbopentoxysulfanilic acid. The novel substance comprises a (2,6-dichlorophenyl)amide salt of carbopentoxysulfanilic acid of general formula: where X is Na, K, NH4; the drug may be contained in tablets, including sublingual tablets, or in capsules, or in suppositories, or in drops, or in mixtures, or in ointments, creams or other forms for application to the skin and mucosae, or in an oral-buccal film, or in a spray, or in a liquid for parenteral administration, or in chewing gum. A preparation having pronounced activity against herpes viruses is thus produced.Type: ApplicationFiled: January 28, 2011Publication date: October 31, 2013Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets, Viktor Iosifovich Krutikov
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Publication number: 20130261132Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.Type: ApplicationFiled: November 21, 2011Publication date: October 3, 2013Applicant: LEO PHARMA A/SInventors: Per Vedso, Lars Kristian Albert BlÆher
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Publication number: 20130252984Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 12, 2013Publication date: September 26, 2013Applicant: ALLERGAN, INC.Inventors: Haiqing YUAN, Richard L. BEARD, Xiaoxia LIU, John E. DONELLO, Veena VISWANATH, Michael E. GARST
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Publication number: 20130251673Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.Type: ApplicationFiled: December 21, 2012Publication date: September 26, 2013Applicant: Novira Therapeutics, INC.Inventors: George D. HARTMAN, Osvaldo A. FLORES
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Patent number: 8541410Abstract: The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.Type: GrantFiled: January 6, 2012Date of Patent: September 24, 2013Assignee: Sanofi-aventis Deutschland GmbHInventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel
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Publication number: 20130243837Abstract: Methods, compounds, and topical formulations for reduction of skin sagging, creasing and/or wrinkling are disclosed. The methods comprise topically applying a composition comprising an ?2 adrenergic receptor agonist. Amelioration of skin sagging, creasing and/or wrinkling begins within minutes after topical application of a disclosed composition. A single application can significantly reduce skin sagging, creasing and/or wrinkling for at least about 8 hours.Type: ApplicationFiled: April 15, 2013Publication date: September 19, 2013Applicant: Galderma Laboratories Inc.Inventors: Jack DeJovin, Isabelle Jean DeJovin
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Publication number: 20130244995Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.Type: ApplicationFiled: November 21, 2011Publication date: September 19, 2013Applicant: LEO PHARMA A/SInventors: Per Vedsø, Lars Kristian Albert Blæhr
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Publication number: 20130237542Abstract: The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.Type: ApplicationFiled: October 17, 2011Publication date: September 12, 2013Applicants: DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION, KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGYInventors: Kyeong Lee, Mi Sun Won, Hwan Mook Kim, Song Kyu Park, Kiho Lee, Ki Hoon Lee, Chang Woo Lee, Jung Joon Lee, Kyung Sook Chung, Bo Kyung Kim, Yinglan Jin, Seung-hee Lee
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Publication number: 20130236480Abstract: The present invention relates to TG2 inhibitors for use in the prevention or treatment of rapidly progressive glomerulonephritis and to pharmaceutical compositions thereof.Type: ApplicationFiled: June 1, 2011Publication date: September 12, 2013Inventors: Pierre-Louis Tharaux, Cécile Fligny
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Patent number: 8529953Abstract: The present invention provides a method for producing spherical fine particles containing tamsulosin hydrochloride, the method includes the steps of: (1) mixing and stirring tamsulosin hydrochloride (a), microcrystalline cellulose (b), and water until a mixture of the component (a) and the component (b) is uniformly impregnated with the water; (2) granulating the mixture obtained in step (1) using an stirring granulator whose peripheral speed is set to be 5.5 to 9.0 m/s; and (3) drying the granules obtained in step (2). The present invention also provides spherical fine particles obtained according to the method, coated fine particles obtained by applying a coating to the spherical fine particles, and an orally disintegrating tablet containing the coated fine particles.Type: GrantFiled: June 29, 2009Date of Patent: September 10, 2013Assignee: Sawai Pharmaceutical Co., Ltd.Inventors: Toshihiro Yanagi, Yoshitaka Iwakura, Hisaya Sangawa, Yasufumi Okamura
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Publication number: 20130231323Abstract: Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.Type: ApplicationFiled: September 6, 2011Publication date: September 5, 2013Applicant: DUKE UNIVERSITYInventors: Pei Zhou, Eric J. Toone
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Publication number: 20130216609Abstract: Disclosed herein are compositions and methods for the treatment of otic diseases or conditions with antimicrobial agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).Type: ApplicationFiled: March 21, 2013Publication date: August 22, 2013Applicants: The Regents of the University of California, Otonomy, Inc.Inventors: Otonomy, Inc., The Regents of the University of California
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Publication number: 20130203709Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.Type: ApplicationFiled: August 9, 2011Publication date: August 8, 2013Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDAInventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
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Publication number: 20130203733Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.Type: ApplicationFiled: December 20, 2012Publication date: August 8, 2013Applicants: Massachusetts Institute of Technology, The General Hospital CorporationInventors: The General Hospital Corporation, Massachusetts Institute of Technology
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Publication number: 20130196956Abstract: A method for reducing the frequency of urination is disclosed. The method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising one or more analgesic agents and one or more ?-blockers. In one embodiment, the one or more analgesic agents are formulated for extended-release.Type: ApplicationFiled: March 14, 2013Publication date: August 1, 2013Applicant: WELLESLEY PHARMACEUTICALS, LLCInventor: Wellesley Pharmaceuticals, LLC
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Publication number: 20130190321Abstract: Methods and kits for aiding in detection, assessment and treatment of a proliferative disorder of the prostate gland in a subject are provided according to aspects of the present invention which include assaying a first biological sample comprising prostate gland cells obtained from the subject for expression of one or more biomarkers selected from the group consisting of: alcohol dehydrogenase 1B, alcohol dehydrogenase 1C, alcohol dehydrogenase 4 and hepatocyte nuclear factor 1B; and determining, based on the expression of the one or more biomarkers in the sample that the subject has, or is at risk of having, a proliferative disorder of the prostate gland.Type: ApplicationFiled: January 23, 2013Publication date: July 25, 2013Applicant: WEST CHESTER UNIVERSITY OF PENNSYLVANIAInventor: West Chester University of Pennsylvania
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Publication number: 20130190356Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 18, 2012Publication date: July 25, 2013Applicant: GENENTECH, INC.Inventor: Genetech, Inc.
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Publication number: 20130178533Abstract: The present invention relates to a composition for diagnosing, treating, and preventing liver disease, more particularly a composition for diagnosing liver disease comprising a material for measuring the grade of TM4SF5 (transmembrane 4 L six family member 5 or four-transmembrane L6 superfamily member 5) protein, a kit for diagnosing liver disease comprising the said composition, a method for providing information necessary for diagnosing liver disease composed of the following steps; measuring the level of TM4SF5 protein and the expressions and phosphorylations of TM4SF5 expression related signaling proteins; and comparing the measured levels with those of the normal control, a method for screening a material for treating liver disease, and a composition for treating or preventing liver disease comprising a material inhibiting TM4SF5 protein expression or the expressions and phosphorylations of TM4SF5 expression related signaling proteins.Type: ApplicationFiled: July 22, 2011Publication date: July 11, 2013Applicant: SNU R&DB FOUNDATIONInventors: Jung Weon Lee, Ki Hun Park, Min Kyung Kang
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Publication number: 20130171199Abstract: An oral controlled release pharmaceutical composition comprising a core and a polymer dispersion and its preparation method are disclosed. The core is selected from the group consisting of ‘the drug coated core’ and ‘the drug loaded core’. The drug coated core comprises an inert excipient based sphere and a coat of drug composition. The drug loaded core comprises at least a drug, a binder and at least one pharmaceutically acceptable excipient. The polymer dispersion used to coat the core comprises at least one controlled release polymer and at least one pharmaceutically acceptable excipient. The oral controlled release pharmaceutical composition further comprises an in-situ gelling system comprising at least one gelling polymer.Type: ApplicationFiled: December 20, 2010Publication date: July 4, 2013Applicant: Abbott Healthcare Private LimitedInventors: Sanjay Boldhane, Shripad Jathar, Maneesh Nerurkar
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Publication number: 20130165460Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: February 20, 2013Publication date: June 27, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Patent number: 8470831Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.Type: GrantFiled: September 23, 2009Date of Patent: June 25, 2013Assignee: Cogenia SRLInventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
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Publication number: 20130158035Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.Type: ApplicationFiled: August 23, 2011Publication date: June 20, 2013Applicant: Brigham Young UniversityInventor: Marc Hansen
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Patent number: 8466201Abstract: Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs wherein: Ar1 and Ar2=aryl or heteroaryl; a=0 to 5; R1=alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano and, where a is >1, each R1 is the same or different; b=0 to 5; R2=alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano and where b is >1, each R2 is the same or different; V=(CR3aR3b)pSO2N(R3b)X and (CR3aR3b)pN(R3b)SO2(X); W=NR4a, O, S, S?O, SO2 and C(R4aR4b)2; X=hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, aryloxyalkyl, polyalkylene glycol residues, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl and alkyl groups substituted with ?1 NR8R9 groups wherein R8 and R9+nitrogen atom form a saturated or partially unsaturated heterocyclic groupType: GrantFiled: December 5, 2008Date of Patent: June 18, 2013Assignee: Ramot at Tel-Aviv University ltd.Inventors: Simon David Edwards, Meriel Ruth Kimberly, Kanesalingam Suthaharan, Nawaz Mohammed Khan, Geoff Lawton
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Publication number: 20130121919Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.Type: ApplicationFiled: June 11, 2012Publication date: May 16, 2013Applicant: The Trustees of Columbia University in the City of New YorkInventors: Yan FENG, Mauro Fa, Ottavio Arancio, Shi Xian Deng, Donald W. Landry, Yitshak Francis
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Publication number: 20130123203Abstract: Disclosed herein are methods and compositions for treating autism. Disclosed herein are methods and compositions for treating an autism spectrum disorder.Type: ApplicationFiled: October 31, 2012Publication date: May 16, 2013Inventors: Paul Talalay, Andrew W. Zimmerman, Kirby D. Smith
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Publication number: 20130116227Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.Type: ApplicationFiled: July 12, 2011Publication date: May 9, 2013Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
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Publication number: 20130096105Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: November 30, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Patent number: 8394846Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.Type: GrantFiled: January 30, 2012Date of Patent: March 12, 2013Assignee: Theravance, Inc.Inventors: Seok-Ki Choi, Paul R. Fatheree, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Vivek Sasikumar
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Publication number: 20130052264Abstract: A controlled-release pharmaceutical composition including first and second groups of microparticles, each of the microparticles including a core including tamsulosin or pharmaceutically acceptable salts thereof, a controlled-release polymer coating layer formed on the core, and an enteric polymer outer layer formed on the controlled-release polymer coating layer, wherein the average thickness of the controlled-release polymer coating layer is different in each of the first and second groups of microparticles, and an oral formulation including the same, are provided. This pharmaceutical composition can easily control the extent of release of an active ingredient depending on changes in pH in the intestinal tract and the release pattern of the active ingredient in the small intestine, thus preventing the active ingredient from being rapidly transferred into the blood to thereby minimize side-effects, and maintaining the effective blood concentration of the active ingredient for a predetermined period of time.Type: ApplicationFiled: April 27, 2011Publication date: February 28, 2013Applicant: SAMYANG BIOPHARMACEUTICALS CORPORATIONInventors: Ho-Jin Chung, Sang-Yeob Park, Chaul-Min Pai