C-o- Group In R Patents (Class 514/622)
  • Patent number: 10259777
    Abstract: The present invention pertains to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and (E)-3-(3,4-dihydroxyphenyl)-N-(prop-2-yn-1-yl)acrylamide of Formula (I): The invention also pertains to a method for stimulating neurite outgrowth by administering to cells in the area where neurite outgrowth is desired a therapeutically effective amount of the compound of Formula (I). Further, the invention pertains to a method for attenuating neuron injury in a subject by contacting a neuron in a subject in need thereof with a therapeutically effective amount of the compound of Formula (I). Furthermore, a method of preparing the compound of Formula (I) are provided.
    Type: Grant
    Filed: May 13, 2016
    Date of Patent: April 16, 2019
    Assignee: The University of Hong Kong
    Inventor: Jianhui Rong
  • Patent number: 9427418
    Abstract: The present invention relates to methods for reducing testosterone levels by reduction of luteinizing hormone (LH) or independent of LH levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate cancer, and castration-resistant prostate cancer (CRPC) and palliative treatment of prostate cancer, advanced prostate cancer and castration-resistant prostate cancer (CRPC). The compounds of this invention suppress free or total testosterone levels to castrate levels which may be used to treat prostate cancer, advanced prostate cancer, and CRPC without causing bone loss, decreased bone mineral density, increased risk of bone fractures, increased body fat, hot flashes and/or gynecomastia.
    Type: Grant
    Filed: August 23, 2011
    Date of Patent: August 30, 2016
    Assignee: GTX, INC.
    Inventors: James T. Dalton, Mitchell S. Steiner, Ronald A. Morton
  • Patent number: 9181176
    Abstract: The present invention provides a new crystalline form of bimatoprost, designated as crystalline form II. This new crystalline form is the most stable form known to date of bimatoprost. Moreover, it has been found that bimatoprost crystalline form II is readily prepared from crystalline form I.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: November 10, 2015
    Assignee: Allergan, Inc.
    Inventors: Gyorgy F. Ambrus, Thomas K. Karami, Ke Wu
  • Patent number: 9133103
    Abstract: Compounds for use in the treatment or prophylaxis of an affective disorder, which compound is represented by formula I: in which: the dotted line represents a single or a double bond; and R5 and R5? are independently —H, —OH or —OR6, where R6 is a linear or branched C1-C4 alkyl; X is —CH2O—; Z is —CH2CH2O—, —CH(CH3)CH2O— or —CH2CH(CH3)O—; m is 1; and n is an integer of 1-5; or a pharmaceutically acceptable salt, prodrug, metabolite, or hydrate thereof.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: September 15, 2015
    Assignee: Novaremed, Ltd.
    Inventors: Eliahu Kaplan, Irit Gil-ad
  • Publication number: 20150148414
    Abstract: Prostacyclin compounds and compositions comprising the same are provided herein. Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C5-C18 alkyl, branched C5-C18 alkyl, linear C2-C18 alkenyl, branched C3-C18 alkenyl, aryl, aryl-C1-C18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide) are described. The linkage, in one embodiment, is via a carbamate, amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. Methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension are also provided.
    Type: Application
    Filed: October 24, 2014
    Publication date: May 28, 2015
    Inventors: Vladimir Malinin, Walter Perkins, Franziska Leifer, Donna Konicek, Zhili Li, Adam Plaunt
  • Publication number: 20150141517
    Abstract: Provided is a rapid release tablet excellent in binding capability and disintegrability and also excellent in storage stability and the like. More specifically, provided are a granulated composite comprising low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of from 5 to 16% by weight and D-mannitol, wherein the D-mannitol contains 0.9% by weight or less of D-sorbitol; a rapid release tablet comprising the granulated composite and a drug; and a method for producing a granulated composite comprising the steps of: mixing low-substituted hydroxypropyl cellulose having a degree of hydroxypropoxy substitution of from 5 to 16% by weight, first D-mannitol, and water to obtain an aqueous dispersion, and granulating while adding the aqueous dispersion to second D-mannitol, wherein the first D-mannitol and the second D-mannitol contain 0.9% by weight or less of D-sorbitol in total.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 21, 2015
    Inventors: Yasuyuki Hirama, Naosuke Maruyama
  • Publication number: 20150141506
    Abstract: Compounds particularly for use in an autoimmune inflammatory disease and especially the treatment of inflammatory bowel disease have the absolute stereochemistry and formula: In some cases R1 is leucine and R is selected from: OH, OCH3, OCH2CH3, OCH2CH2CH3, NH2, NHCH2CH2OH, NHCH3, N(CH3)2, NH(4-OH-3-benzoic acid).
    Type: Application
    Filed: May 23, 2013
    Publication date: May 21, 2015
    Inventors: Neil Frankish, Helen Sheridan
  • Publication number: 20150139934
    Abstract: A method for screening a patient for angioinhibition resistance and treating said patient having a disease susceptible to treatment via an anti-angiogenic agent. The screening method includes an assay for identifying the presence of angioinhibition resistance in patients by collecting patient blood or serum and subjecting it to a Chick Chorioallantoic Membrane (CAM) angiogenesis assay configured for accepting a human tumor wherein the human tumor xenograft includes a vasculature system. The screening method and assay further includes steps that include using the CAM results for identifying the endogenous pro-angiogenic non-peptide hormone concentrations of the blood sample by calculating the vascular activity of the vasculature system of the human tumor xenograft in the presence of anti-angiogenic drugs and inducing in the patient, a state of subclinical hypothyroidism prior to commencing anti-angiogenic treatment.
    Type: Application
    Filed: November 18, 2014
    Publication date: May 21, 2015
    Inventors: SHAKER A. MOUSA, PAUL J. DAVIS
  • Publication number: 20150140053
    Abstract: A pesticidal composition in the form of an aqueous emulsion contains: (a) an agriculturally active ingredient in which a retention rate is 50% or more after irradiation with xenon light (290 nm cutoff) at an intensity of 0.68 W/m2 at 340 nm for 8 hours, and a retention rate is 40% or more and 60% or less after irradiation for 56 hours; (b) a hydrophobic organic solvent; (c) a water-soluble polymer dispersing agent; and (d) water; wherein liquid droplets in which the agriculturally active ingredient is suspended or dissolved in the hydrophobic organic solvent are emulsified in an aqueous continuous phase. A weight ratio of the agriculturally active ingredient to the hydrophobic organic solvent is from 5:95 to 70:30. With this pesticidal composition, it is possible to inhibit photodegradation of the agriculturally active ingredient.
    Type: Application
    Filed: June 20, 2013
    Publication date: May 21, 2015
    Inventors: Kazuyuki Yanagisawa, Motofumi Mizutani
  • Publication number: 20150132358
    Abstract: A method and apparatus for administering an active agent such as a medicine to a subject, uses an ocular implant such as a punctal plug, to which the active agent has been applied. The implant is installed at the eye of the subject for administering the active agent via tissues of the eye.
    Type: Application
    Filed: August 29, 2014
    Publication date: May 14, 2015
    Inventors: Steven A. Odrich, Liane C. Glazer
  • Publication number: 20150133405
    Abstract: The present invention relates to the use of selective aquaporin inhibitors, e.g., of aquaporin-4 or aquaporin-2, e.g., certain phenylbenzamide compounds, for the prophylaxis, treatment and control of aquaporin-mediated conditions, e.g., diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord, e.g., following trauma or ischemic stroke, as well as the edema associated with glioma, meningitis, acute mountain sickness, epileptic seizures, infections, metabolic disorders, hypoxia, water intoxication, hepatic failure, hepatic encephalopathy, diabetic ketoacidosis, abscess, eclampsia, Creutzfeldt-Jakob disease, and lupus cerebritis, as well as edema consequent to microgravity and/or radiation exposure, as well as edema consequent to invasive central nervous system procedures, e.g.
    Type: Application
    Filed: May 8, 2013
    Publication date: May 14, 2015
    Inventors: Marc F. Pelletier, George William Farr, Paul Robert Mcguirk, Christopher H. Hall, Walter F. Boron
  • Publication number: 20150133559
    Abstract: Methods for treating and preventing ocular conditions by administering an compound to the vitreous chamber of a patient at risk of, or suffering from, the ocular condition.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventors: Scott M. Whitcup, David A. Weber
  • Publication number: 20150118279
    Abstract: Prostamide-containing intraocular implants that biodegrade in the eye and that are effective for reducing intraocular pressure in an eye for a sustained period. The implants generally contain a prostamide, such as bimatoprost, and at least three distinct biodegradable polymers selected from polylactide and poly(lactide-co-glycolide) polymers and are optimized for placement in and compatibility with the anterior chamber of the eye, particularly the anterior chamber angle. Methods for making and using the implants to reduce ocular hypertension and intraocular pressure in a patient are described.
    Type: Application
    Filed: October 31, 2014
    Publication date: April 30, 2015
    Inventors: Alazar N. Ghebremeskel, Michael R. Robinson
  • Publication number: 20150119466
    Abstract: The present invention is in relation to a composition including nanosphere and histone acetyltransferase (HAT) activator. The nanosphere is carbon nanosphere (CSP) which is intrinsically fluorescent and the HAT activator is N-(4-Chloro-3-trifluoromethyl-phenyl)-2-n-propoxy-benzamide. The N-(4-Chloro-3-trifluoromethyl-phenyl)-2-n-propoxy-benzamide is covalently conjugated with the carbon nanosphere. The present invention further relates to a process for obtaining a composition including carbon nanosphere and Histone acetyltransferase (HAT) activator [N-(4-Chloro-3-trifluoromethyl-phenyl)-2-n-propoxy-benzamide]. The composition is capable of crossing blood brain barrier and inducing histone acetylation in brain. Further, the composition is capable of increasing neurogenesis, as well as improving long-term memory formation.
    Type: Application
    Filed: April 27, 2013
    Publication date: April 30, 2015
    Inventors: Tapas Kumar Kundu, Anne-Laurence Boutillier, Snehajyoti Chatterjee, Muthusamy Eswaramoorthy, Pushpak Mizar, Chantal Mathis, Jean-Christophe Cassel, Romain Neidl, Mohankrishna Dalvoy Vasudevarao, Vedamurthy Bhusainahalli Maheshwarappa
  • Publication number: 20150105433
    Abstract: Provided herein are methods for preventing or treating a viral infection in a subject, wherein the viral infection is mediated by a virus comprising one or more viral RNA molecules translated by a ribosomal shunting mechanism or a non-IRES mediated mechanism. The methods comprise administering to a subject an agent that reduces ribosomal protein (Rps25) expression or function. Also provided are methods of inhibiting or promoting ribosomal shunting-mediated translation or non-IRES mediated translation. Also provided are methods of screening for an agent that inhibits or promotes ribosomal shunting-mediated translation or non-IRES mediated translation.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 16, 2015
    Inventor: Sunnie R. Thompson
  • Patent number: 9006291
    Abstract: Compositions for application and methods of application of a composition to modify hair. In one embodiment, a composition includes a compound (molecule) represented by: wherein A and B are individually selected from a hydrogen, a hydroxyl group and a halogen, with the proviso that when one of A and B is a hydroxyl group, the other of A and B is a hydrogen and when one of A and B is a halogen, the other of A and B is a halogen or a hydrogen; wherein Z is, for example, an aryl moiety; and wherein X1 and X2 are, for example, individually selected from a hydrogen and an alkyl moiety, wherein R1 and R2 are individually selected from an oxo, a hydroxyl or an ester group; wherein y is 0 or 1, x is 0 or 1 and x and y are not both 1, or a salt.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: April 14, 2015
    Assignee: Pharma Patent Holding Inc.
    Inventor: Michael C. Brinkenhoff
  • Patent number: 9006139
    Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.
    Type: Grant
    Filed: August 19, 2014
    Date of Patent: April 14, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
  • Publication number: 20150099807
    Abstract: The present invention is directed to preservative-free solutions of bimatoprost for lowering intraocular pressure and treatment of glaucoma.
    Type: Application
    Filed: June 18, 2014
    Publication date: April 9, 2015
    Inventors: Sukhon Likitlersuang, Ajay Parashar, Chetan P. Pujara, William F. Kelly
  • Publication number: 20150099781
    Abstract: Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
    Type: Application
    Filed: December 16, 2014
    Publication date: April 9, 2015
    Inventors: Lizbeth K. Hedstrom, Gregory D. Cuny, Deviprasad R. Gollapalli, Sivapriya Kirubakaran, Sushil K. Maurya, Boris Striepen, Suresh K. Gorla, Corey R. Johnson, Mandapati Kavitha, Jihan Khan
  • Patent number: 8999938
    Abstract: The ophthalmic drug delivery vehicles provide comfort and compliance; drug solubility, residence time and permeability; and reduce side effects. In addition, the delivery vehicle can be slightly modified to provide an artificial tear formulation.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: April 7, 2015
    Assignee: GNT LLC
    Inventor: Gerald Horn
  • Publication number: 20150087712
    Abstract: The present invention relates to methods for reducing testosterone levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC), metastatic castration resistant prostate cancer (mCRPC), and methods of reducing high or increasing PSA levels and/or increasing SHBG levels in a subject suffering from prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC) and metastatic castration resistant prostate cancer (mCRPC). The compounds of this invention suppress free or total testosterone levels despite castrate levels secondary to ADT and reduce high or increasing PSA levels. This reduction in testosterone levels may be used to treat prostate cancer, advanced prostate cancer, CRPC and mCRPC without causing bone loss, decreased bone mineral density, increased risk of bone fractures, increased body fat, hot flashes and/or gynecomastia.
    Type: Application
    Filed: October 24, 2014
    Publication date: March 26, 2015
    Inventors: James T. Dalton, Mitchell S. Steiner, Christopher C. Coss, Robert H. Getzenberg
  • Publication number: 20150087713
    Abstract: A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein. A method which is useful in treating glaucoma or ocular hypertension related thereto is also disclosed herein.
    Type: Application
    Filed: December 5, 2014
    Publication date: March 26, 2015
    Inventors: Chin-Ming Chang, James N. Chang, Rhett M. Schiffman, R. Scott Jordan, Joan-En Chang-Lin
  • Patent number: 8987262
    Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: March 24, 2015
    Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de Bordeaux
    Inventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
  • Patent number: 8981149
    Abstract: The invention relates to compounds of formula (I), and the use thereof as a drug, particularly for the treatment of tumors associated with hyperactivation of the hedgehog protein signaling pathway, treatment of neurodegenerative diseases, treatment of diseases related to cerebral development (holoprosencephaly), for stem cell monitoring treatment of cerebrovascular accidents and cardiovascular accidents, treatment of diseases involving oligodendrocytes and diseases involving neurolemmocytes, for application thereof in vitro for modulating human or animal stem cell renewal, and for the treatment of diabetes. The invention also relates to pharmaceutical compositions having a compound of formula (I).
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: March 17, 2015
    Assignees: Centre National de la Recherche Scientifique, Universite de Strasbourg
    Inventors: Martial Ruat, Hélène Faure, Hermine Roudaut, Lucile Hoch, Angèle Schoenfelder, Maurizio Taddei, André Mann
  • Patent number: 8980885
    Abstract: A plant disease controlling composition comprising, as active ingredients, a compound represented by the formula (I), as well as at least one compound A selected from the group consisting of dimoxystrobin, trifloxystrobin, azoxystrobin, pyraclostrobin, a compound represented by the formula (II) and an agrochemically acceptable salt of the compound represented by the formula (II): wherein, R1, Q, X, Y, Z, M and n are as defined in the description.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: March 17, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Masato Soma, Masanao Takaishi
  • Publication number: 20150065508
    Abstract: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
    Type: Application
    Filed: March 26, 2014
    Publication date: March 5, 2015
    Applicant: ABBVIE INC.
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Steven Fung, Peer B. Jacobson, Lynne E. Rueter, Marina I. Strakhova, Jiahong Wang, Jyoti R. Patel, Qi Shuai, James T. Link, Jeffrey J. Rohde, Jurgen Dinges, Bryan K. Sorensen, Martin Winn, Hong Yong, Vince S. Yeh
  • Patent number: 8969415
    Abstract: Biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 10 days and one year or longer.
    Type: Grant
    Filed: December 1, 2006
    Date of Patent: March 3, 2015
    Assignee: Allergan, Inc.
    Inventors: Michael R. Robinson, Wendy M. Blanda, Patrick M. Hughes, Guadalupe Ruiz, Werhner C. Orilla, Scott M. Whitcup, Devin F. Welty, Joan-En Lin, Lon T. Spada
  • Publication number: 20150045367
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Application
    Filed: December 19, 2012
    Publication date: February 12, 2015
    Inventors: Erik Verner, Wei Chen, Sriram Balasubramanian
  • Publication number: 20150045387
    Abstract: Bi- and tri-aromatic compounds of the formula (I) wherein R1 to RIO and X are as defined, are Nox2 inhibitors that are useful as medicaments for the treatment of a disease or condition selected from: cardiovascular diseases, respiratory diseases, inflammatory diseases, cancers, ageing and age related disorders, kidney diseases, neurodegenerative diseases, diabetes and conditions associated with diabetes. The compounds, their preparation and pharmaceutical compositions comprising them are disclosed.
    Type: Application
    Filed: September 17, 2012
    Publication date: February 12, 2015
    Inventors: Jian-Mei Li, Brendan Howlin, Daniel Nathan Meijles
  • Patent number: 8940795
    Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more benzamide fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease. group (A): a group consisting of flutolanil, mepronil, and zoxamide.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: January 27, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
  • Patent number: 8940936
    Abstract: 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: Grant
    Filed: October 17, 2011
    Date of Patent: January 27, 2015
    Assignees: Korea Research Institute of Bioscience and Biotechnology, Dongguk University Industry-Academic Cooperation Foundation
    Inventors: 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
  • Publication number: 20150025151
    Abstract: The present invention relates to compositions, such as bimatoprost, latanoprost and travoprost, and methods to reduce fat in the body of an individual, for example, by topical administration, injection, and/or implantation of such compositions.
    Type: Application
    Filed: October 2, 2014
    Publication date: January 22, 2015
    Applicant: Topokine Therapeutics, Inc.
    Inventors: Cynthia L. Grosskreutz, Louis R. Pasquale, Michael S. Singer, Murat V. Kalayoglu
  • Publication number: 20150023921
    Abstract: The present invention relates to novel compositions having anti-viral activity and in particular it relates to synergistic compositions active against Hepatitis C virus (HCV). The invention also relates to methods for retarding, reducing or otherwise inhibiting HCV growth and/or functional activity.
    Type: Application
    Filed: April 3, 2014
    Publication date: January 22, 2015
    Applicant: BIOTRON LIMITED
    Inventors: Gary Dinneen EWART, Carolyn Anne LUSCOMBE, Michelle MILLER
  • Publication number: 20150017216
    Abstract: Biodegradable and nutritionally attractive composition comprising biocidal or antibiotic compounds and/or microbes having bio-adhesion and controlled buoyancy properties are selectively fed to an aquatic organism in open or closed water-bodies, and bioactive components are released upon contact with mucosal tissues such as gill, skin or along the digestive tract of the selected aquatic organism.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 15, 2015
    Inventors: Moti Harel, Brian Carpenter, Pete Schmalz
  • Publication number: 20150018371
    Abstract: Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 15, 2015
    Inventors: Roger D. Cone, Julien A. Sebag, Jacques Pantel, Savannah Y. Williams, David C. Weaver, Gary A. Sulikowski, Craig W. Lindsley, Padma S. Portonova, Chao Zhang
  • Publication number: 20150010484
    Abstract: A method for anti-skin aging, especially for anti-skin photo-aging in a subject is provided. The method comprising administering to the subject an effective amount of an active component selected from the group consisting of a caffeamide derivative of formula (I), a pharmaceutically acceptable salt of the caffeamide derivative, and a combination thereof: wherein A is H or an alkyl; B is —[CH2]m—; m is an integer ranging from 0 to 10; R1 is H, an optionally substituted phenyl, an optionally substituted pyridyl, —OH, or —OCH3; or, N, A, B, and R1 together form an optionally substituted pyrrolyl or piperidyl.
    Type: Application
    Filed: October 8, 2013
    Publication date: January 8, 2015
    Applicant: CHINA MEDICAL UNIVERSITY
    Inventors: Hsiu-Mei CHIANG, Yueh-Hsiung KUO, Kuo-Ching WEN
  • Publication number: 20150004243
    Abstract: Biocompatible microparticles include an ophthalmically active cyclic lipid component and a biodegradable polymer that is effective, when placed into the subconjunctival space, in facilitating release of the cyclic lipid component into the anterior and posterior segments of an eye for an extended period of time. The cyclic lipid component can be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the cyclic lipid component can be encapsulated by the polymeric component. The present microparticles include oil-in-water emulsified microparticles. The subconjunctivally administered microparticles can be used to treat or to reduce at least one symptom of an ocular condition, such as glaucoma or age related macular degeneration.
    Type: Application
    Filed: March 27, 2014
    Publication date: January 1, 2015
    Applicant: Allergan, Inc.
    Inventors: James Chang, Patrick Hughes, Chin-Ming Chang
  • Publication number: 20140378391
    Abstract: The ophthalmic drug delivery vehicles provide comfort and compliance; drug solubility, residence time and permeability; and reduce side effects. In addition, the delivery vehicle can be slightly modified to provide an artificial tear formulation.
    Type: Application
    Filed: June 21, 2013
    Publication date: December 25, 2014
    Inventor: Gerald Horn
  • Publication number: 20140378460
    Abstract: This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated with Abeta pathology. This invention also relates to methods for screening compounds for activity in inhibiting cognitive decline on the basis of their ability to bind to a sigma-2 receptor.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: COGNITION THERAPEUTICS, INC.
    Inventors: Susan M. Catalano, Gilbert Rishton, Nicholas J. Izzo
  • Publication number: 20140378401
    Abstract: The ophthalmic drug delivery vehicles provide comfort and compliance; drug solubility, residence time and permeability; and reduce side effects. In addition, the delivery vehicle can be slightly modified to provide an artificial tear formulation.
    Type: Application
    Filed: December 18, 2013
    Publication date: December 25, 2014
    Applicant: GNT, LLC
    Inventor: Gerald Horn
  • Publication number: 20140371320
    Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent the presence or absence of a double bond which can be in the cis or trans configuration and A, B, Z, X, R1 and R2 are as defined in the specification and a penetration enhancer. Such compositions are used in stimulating hair growth of human or non-human animals.
    Type: Application
    Filed: January 24, 2014
    Publication date: December 18, 2014
    Applicant: Allergan, Inc.
    Inventors: John T. Trogden, Adnan K. Salameh, Chetan P. Pujara
  • Publication number: 20140371232
    Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.
    Type: Application
    Filed: December 18, 2012
    Publication date: December 18, 2014
    Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
  • Publication number: 20140364494
    Abstract: Biocompatible implants comprising a cyclic lipid therapeutic agent are made using a low temperature melt extrusion process. The implants are suitable for intraocular use to treat an ocular condition.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Inventors: Lon T. Spada, James N. Chang, Michelle H. Luu
  • Publication number: 20140357678
    Abstract: A pharmaceutically acceptable salt, prodrug or derivative compound of the formula I, wherein R1 is selected from H, a (C1-C5) alkyl group and a COR4 group; R2 is selected from H, a (C1-C5) alkyl group and a COR5 group; R3 is selected from H, a (C1-C5) alkyl group, a (C1-C5)-O-alkyl group, a cycloalkyl of (C5-C6) carbon atoms, an aryl group, and an aryl (C1-C5) alkyl group wherein the aryl group can be an unsubstituted aryl or substituted with one or more R6 groups and an NHCOR5 group, or the R2 and R3 groups together with N may form a piperidine, morpholine or piperazine group; R4 is selected from H and a (C1-C5)alkyl group; R5 is selected from an aryl group unsubstituted or substituted with one or more R6, linear or branched(C1-C5) alkyl or pyridyne groups and a pyridine group; R6 is selected from (C1-C5)alkyl groups, halogen and nitro.
    Type: Application
    Filed: January 10, 2013
    Publication date: December 4, 2014
    Inventors: Gerardo Burton, Javier Duran, David Martinez, Elvira Zini, Veronica Mora Munoz, Lucila Bertoncello
  • Publication number: 20140357628
    Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.
    Type: Application
    Filed: June 27, 2014
    Publication date: December 4, 2014
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Publication number: 20140343108
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel amidated derivatives of oleanolic acid according to formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 20, 2014
    Inventors: Frank Rong, Rongzhen Xu, Fuwen Xie, Hongxi Lai
  • Publication number: 20140328894
    Abstract: An implant for insertion into a punctum of a patient comprises a body. The body has a distal end, a proximal end, and an axis therebetween. The distal end of the body is insertable distally through the punctum into the canalicular lumen. The body comprises a therapeutic agent included within an agent matrix drug core. Exposure of the agent matrix to the tear fluid effects an effective therapeutic agent release into the tear fluid over a sustained period. The body has a sheath disposed over the agent matrix to inhibit release of the agent away from the proximal end. The body also has an outer surface configured to engage luminal wall tissues so as to inhibit expulsion when disposed therein. In specific embodiments, the agent matrix comprises a non-bioabsorbable polymer, for example silicone in a non-homogenous mixture with the agent.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Inventors: Eugene de Juan, JR., Cary Reich, Stephen Boyd, Hanson S. Gifford, Mark Deem
  • Publication number: 20140329905
    Abstract: The present invention relates to a method of identifying a subject being susceptible to a co-treatment with an histone deacetylase 10 (HDAC10)-inhibitor, said subject being in need of and/or being treated with cancer therapy against a cancer, comprising the steps of a) determining the amount of an HDAC10 gene product and/or an autophagy-related gene 4D (ATG4D) product in a cancer sample from said subject, b) comparing the amount of said HDAC10 gene product as determined in step a) with a reference amount for said HDAC10 gene product and/or the amount of ATG4D product as determined in step a) with a reference amount for said ATG4D product, and c) identifying a subject being susceptible to co-treatment with an HDAC10-inhibitor.
    Type: Application
    Filed: December 21, 2012
    Publication date: November 6, 2014
    Inventors: Ina Oehme, Olaf Witt, Nathan Brady
  • Patent number: 8877754
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
  • Publication number: 20140323457
    Abstract: The present invention relates to beta-O/S/N fatty acids and derivatives thereof, in particular the compounds of formula (I) as described and defined herein, and their pharmaceutical use, including their use in the treatment or prevention of bacterial as well as protozoan infections, in particular the treatment or prevention of infections with Gram-positive and/or Gram-negative bacteria and infectious diseases caused by and/or related to Gram-positive and/or Gram-negative bacteria. The invention further relates to the use of these compounds for preventing or eliminating biofilms.
    Type: Application
    Filed: December 6, 2012
    Publication date: October 30, 2014
    Inventors: Thomas Böttcher, Vadim Korotkov, Katrin Lorenz-Baath, Oliver Baron, Stephan Sieber