Chalcogen Attached Indirectly To The Morpholine Ring By Acyclic Nonionic Bonding Patents (Class 514/238.8)
  • Patent number: 9499526
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of neurologic diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of depression, Alzheimer's disease, multiple sclerosis, Batten disease, multiple sclerosis, Parkinson's disease (PD) and restless legs syndrome (RLS).
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: November 22, 2016
    Assignee: CELLIX BIO PRIVATE LIMITED
    Inventor: Mahesh Kandula
  • Patent number: 9416196
    Abstract: There is provided a composition for prophylaxis or treatment of vascular or valvular calcification including a dipeptidylpeptidase-4 (DPP-4) inhibitor. The DPP-4 according to one exemplary embodiment of the present disclosure is expressed at an increased level when blood vessels and valves are calcified, and the calcification decreases remarkably upon administration of the DPP-4 inhibitor. Therefore, the DPP-4 inhibitor can be useful in treatment or prophylaxis of blood vessels or valves.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: August 16, 2016
    Assignees: THE ASAN FOUNDATION, UNIVERSITY OF ULSAN FOUNDATION FOR INDUSTRY COOPERATION
    Inventors: Jae Kwan Song, Eun Ju Chang, Mi Jeong Kim, Bongkun Choi, Sahmin Lee
  • Patent number: 9029371
    Abstract: The present invention relates to bisaryl (thio)morpholine derivatives of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof, with the proviso that the derivative of formula (I) is not 2-[4-(4-chlorophenoxy)-2-chlorophenyl]-4 -morpholineethanol. The compounds of the invention have affinity to S1 Preceptors and may be used in the treatment, alleviation or prevention of S1 Preceptor mediated diseases and conditions.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: May 12, 2015
    Assignee: Abbvie B.V.
    Inventors: Wouter I. Iwema Bakker, Raymond Bronger
  • Patent number: 8987263
    Abstract: Basic esters of fatty alcohols of the general formula: R1-O—CO-A or pharmaceutically acceptable salts thereof, wherein R1 is C12-C24 alkyl or C10-C24 alkenyl, and A is a residue containing at least one acyclic or cyclic amino group and/or at least one heteroaromatic ring containing a tertiary or quaternary nitrogen atom, are anti-inflammatory and immunomodulatory agents, useful in the treatment of immunologically-mediated inflammation, as adjuvants for antigens involved in both cellular and humoral responses.
    Type: Grant
    Filed: October 9, 2003
    Date of Patent: March 24, 2015
    Inventors: Meir Shinitzky, Irun R. Cohen, Raanan Margalit, Yaacov Herzig, Jeffrey Sterling, Gyorgy Toth, Istvan Miskolczi, Ferenc Rantal, Tivadar Tamas
  • Publication number: 20150010479
    Abstract: The present invention relates to the use of compositions in the prevention and/or treatment of infections by a number of microbial species associated with the pathological colonisation of wounds and periodontal lesions. The compositions of the invention comprise a morpholino compound in combination with a cetylpyridinium salt, which have been found by the present inventors to exert either a potentiating or synergistic antimicrobial effect on a range of microbes associated with the above pathological activity. Accordingly, the present invention provides novel uses of such compositions in treating or preventing infections or conditions in wounds or periodontal lesions, caused by the microbial species, in addition to methods for treating or preventing such disorders.
    Type: Application
    Filed: March 20, 2013
    Publication date: January 8, 2015
    Inventor: Simon Youlton
  • Publication number: 20150005306
    Abstract: Provided is a pharmaceutical composition for preventing or treating a cognitive impairment-related disease, the pharmaceutical composition including N-(2-hydroxyethyl)piperazine-N?(3-propane sulfonic acid), a pharmaceutically acceptable salt thereof or a derivative thereof, and donepezil, a pharmaceutically acceptable salt thereof or a derivative thereof. The composition may be used in preventing or treating a cognitive impairment-related disease.
    Type: Application
    Filed: June 27, 2014
    Publication date: January 1, 2015
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Dong Jin KIM, Young Soo Kim, Hye Yun Kim, Hyun Jin Kim
  • Patent number: 8906908
    Abstract: The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: December 9, 2014
    Assignees: Research Triangle Institute, Dignity Health, Virginia Commonwealth University
    Inventors: F. Ivy Carroll, Bruce E. Blough, Hernan A. Navarro, S. Wayne Mascarella, Ana Zamfira Muresan, M. Imad Damaj, Ronald J. Lukas
  • Patent number: 8895077
    Abstract: The present invention relates to methods for preventing or treating infectious diseases caused by extracellular microorganisms, such as bacteria and fungi, by systemically administering to a patient a compound containing gallium. The extracellular microorganisms targeted by the present methods include methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecalis (VRE), E. coli O157:H7, fluoroquinolone-resistant Salmonella typhi, and the like. Furthermore, in the present methods, gallium compounds can be co-administered with one or more conventional antimicrobial agents to treat infectious diseases with reduced risks of creating multi-drug resistant pathogens. The methods of the present invention is also applicable to those microorganisms, such as ulcer-causing Helicobacter pylori, complete eradication of which so far has been difficult to achieve.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: November 25, 2014
    Assignee: Mount Sinai School of Medicine
    Inventors: Daniel P. Perl, Sharon Moalem
  • Patent number: 8877747
    Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: November 4, 2014
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
  • Publication number: 20140271955
    Abstract: Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicants: The Scripps Research Institute, The California Institute for Biomedical Research
    Inventors: Peter G. SCHULTZ, Arnab K. CHATTERJEE, Shoutian ZHU, Joshua PAYETTE, Hongchul YOON, Baiyuan YANG
  • Publication number: 20140243334
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
  • Publication number: 20140194416
    Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Patent number: 8772336
    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: Grant
    Filed: October 11, 2012
    Date of Patent: July 8, 2014
    Assignees: Merck Frosst Canada Ltd., Axys Pharmaceuticals, Inc.
    Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra I. Baskaran
  • Publication number: 20140163017
    Abstract: 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: Application
    Filed: June 19, 2013
    Publication date: June 12, 2014
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Publication number: 20140142107
    Abstract: Antimicrobial agents, compositions that include the agent(s) and use(s) thereof are provided. Also disclosed are screening assays for identifying antimicrobial agents.
    Type: Application
    Filed: September 4, 2013
    Publication date: May 22, 2014
    Applicant: University of Massachusetts
    Inventors: Paul Kaufman, Jessica Lopes Da Rosa-Spiegler, Reeta Prusty Rao, Ahmed Fazly
  • Patent number: 8691977
    Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 8, 2014
    Assignee: Neupharma, Inc.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Publication number: 20140093490
    Abstract: The present invention investigate the two modes of glutamate release and the releasing rate of glutamate, and thus can provide a useful technique for neuron protection and acceleration of neurotransmission by controlling the glutamate release in astroctye. Thus, the present invention provides an inhibitor of the fast-mode release and/or the slow-mode release of astrocytic glutamate, a screening method of the inhibitor and a pharmaceutical composition or method of ameliorating, preventing and/or treating the disease associated with the over-release of glutamate via the Ca2+-activated anion channel, with the inhibition of fast-mode glutamate release.
    Type: Application
    Filed: July 23, 2013
    Publication date: April 3, 2014
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Changjoon Justin LEE, Soo Jin OH, Eun Mi HWANG, Dong Ho WOO
  • Publication number: 20140094445
    Abstract: 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: Application
    Filed: August 15, 2012
    Publication date: April 3, 2014
    Applicant: University of Utah Research Foundation
    Inventors: Hariprasad Vakayalapati, Venkataswamy Soma, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Publication number: 20140080833
    Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.
    Type: Application
    Filed: November 11, 2013
    Publication date: March 20, 2014
    Applicant: MannKind Corporation
    Inventors: Gary A. Flynn, Sandra A. Lee, Mary Faris, David W. Brandt, Subrata Chakravarty
  • Patent number: 8604031
    Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: December 10, 2013
    Assignee: MannKind Corporation
    Inventors: Gary A. Flynn, Sandra Aeyoung Lee, Mary Faris, David William Brandt, Subrata Chakravarty
  • Publication number: 20130323286
    Abstract: This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.
    Type: Application
    Filed: November 7, 2012
    Publication date: December 5, 2013
    Applicant: PROGENICS PHARMACEUTICALS, INC.
    Inventor: Progenics Pharmaceuticals, Inc.
  • Publication number: 20130310384
    Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.
    Type: Application
    Filed: October 4, 2011
    Publication date: November 21, 2013
    Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
    Inventors: Corinne E. Augelli-Szafran, Dai Lu, Hanxun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe
  • Patent number: 8546392
    Abstract: The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: October 1, 2013
    Assignee: Universitaet des Saarlandes
    Inventors: Rolf Hartmann, Martin Frotscher, Sandrine Oberwinkler, Erika Ziegler, Josef Messinger, Heinrich-Hubert Thole
  • Publication number: 20130237542
    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: Application
    Filed: October 17, 2011
    Publication date: September 12, 2013
    Applicants: DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION, KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    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: 20130231341
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: January 11, 2013
    Publication date: September 5, 2013
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventor: Soren Ebdrup
  • Publication number: 20130196998
    Abstract: The present invention relates to spiro-cyclic amine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)a
    Type: Application
    Filed: July 8, 2011
    Publication date: August 1, 2013
    Applicant: AbbVie B.V.
    Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Maria J.P. van Dongen, Nicolas J.-L.D. Leflemme
  • Patent number: 8399456
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: March 19, 2013
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Raaum
  • Publication number: 20130065889
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: October 26, 2012
    Publication date: March 14, 2013
    Applicant: AXIKIN PHARMACEUTICALS, INC.
    Inventor: Axikin Pharmaceuticals, Inc.
  • Publication number: 20130035312
    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 11, 2012
    Publication date: February 7, 2013
    Applicants: Axys Pharmaceuticals, Inc., Merck, Sharp & Dohme, Corp.
    Inventors: Merck, Sharp & Dohme, Corp., Axys Pharmaceuticals, Inc.
  • Patent number: 8288444
    Abstract: A device for iontophoretically delivering a charged curcuminoid across the skin of an Alzheimer's Disease patient.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: October 16, 2012
    Assignee: Codman & Shurtleff, Inc.
    Inventors: Sean Lilienfeld, Thomas M DiMauro
  • Publication number: 20120225848
    Abstract: Methods for treating an individual to improve cognitive function are provided. In the subject methods, an effective amount of a GABAB antagonist, or a blocker of Kir3.2 potassium channels, is administered to the individual, resulting in an improvement in cognitive function of the host. The subject methods find use in a variety of different applications.
    Type: Application
    Filed: September 17, 2010
    Publication date: September 6, 2012
    Inventors: Alexander M. Kleschevnikov, William C. Mobley
  • Publication number: 20120225108
    Abstract: Morpholino compounds of Formula (I) wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxy group except in the alpha-position, or pharmaceutically acceptable salts thereof, have been found to be surprisingly effective at promoting the healing of a wound.
    Type: Application
    Filed: May 21, 2012
    Publication date: September 6, 2012
    Applicant: SINCLAIR PHARMACEUTICALS LIMITED
    Inventor: OLOF TORGNY SJODIN
  • Publication number: 20120220552
    Abstract: The present disclosure relates to (thio)morpholine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, —SO2-(1-4C)alkyl, —CO-(1-4C)alkyl, —CO—O-(1-4C)alkyl, —NH—CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from —
    Type: Application
    Filed: August 27, 2010
    Publication date: August 30, 2012
    Inventors: Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena
  • Patent number: 8252788
    Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed, wherein a dashed line represents the presence or absence of a bond; and, wherein Y, A, R, D, and n are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: May 13, 2009
    Date of Patent: August 28, 2012
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20120178732
    Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: December 6, 2011
    Publication date: July 12, 2012
    Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
  • Publication number: 20120101039
    Abstract: A compound 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, methods of treating diseases with said compounds, and the use of said compounds in the manufacture of medicaments.
    Type: Application
    Filed: May 26, 2010
    Publication date: April 26, 2012
    Applicant: LEO PHARMA A/S
    Inventors: Jef Fenscholdt, Thomas Høyer, Xifu Liang, Sophie Elisabeth Havez
  • Publication number: 20120094977
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Application
    Filed: May 25, 2011
    Publication date: April 19, 2012
    Applicant: Dendreon Corporation
    Inventors: Sateesh K. Natarajan, Ofir Moreno, Thomas J. Graddis, David F. Duncan, Reiner Laus, Feng Chen
  • Publication number: 20120052019
    Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.
    Type: Application
    Filed: August 22, 2011
    Publication date: March 1, 2012
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Publication number: 20120052026
    Abstract: Antiplaque oral compositions are provided that contain an orally acceptable carrier and an antibacterial effective amount of the compound of formula (I). In various embodiments, the compositions contain from about 0.001% to about 10% by weight of the compound of formula (I).
    Type: Application
    Filed: November 9, 2011
    Publication date: March 1, 2012
    Applicant: COLGATE-PALMOLIVE COMPANY
    Inventors: Ravi Subramanyam, Prem Sreenivasan
  • Publication number: 20120035175
    Abstract: The present invention relates to a salt selected from the group comprising the N-methyl-D-glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2-hydroxyethyl)morpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.
    Type: Application
    Filed: July 1, 2011
    Publication date: February 9, 2012
    Applicant: 4SC AG
    Inventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT
  • Publication number: 20120035176
    Abstract: Analogs of 3-O-acetyl-11-keto-beta-boswellic acid and their method of preparation are presented. The analogs may be used as anti-inflammatory and anti-cancer agents. The compounds inhibit 5-lipoxygenase enzyme and various cell lines related to inflammation as well as to cancer showing a significantly better efficacy when compared to the normal boswellic acids. The analogs are capable of controlling and treating various inflammatory diseases and cancers.
    Type: Application
    Filed: September 30, 2011
    Publication date: February 9, 2012
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti, Krishanu Sengupta
  • Publication number: 20120022070
    Abstract: Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.
    Type: Application
    Filed: October 6, 2009
    Publication date: January 26, 2012
    Applicant: EMORY UNIVERSITY
    Inventors: Jaeki Min, Pahk Thepchatri, Yuhong Du, Dennis C. Liotta, Haian Fu
  • Publication number: 20120015947
    Abstract: A compound of formula (I): in which— X represents O or CH2; R3 and R4 each independently represent hydrogen or C1-6 alkyl; p represent 0 or 1; and R represents a five- or six-membered saturated or unsaturated ring selected from: or R represents a five- or six-membered oxo-substituted unsaturated ring selected from: wherein R1 and R2 together represent an oxo group, or R1 and R2 each represent hydrogen, methoxy or ethoxy, or R1 and R2 together with the interjacent carbon atom represent a 1,3-dioxolane or 1,3-dioxane ring, attached via the 2 position and optionally bearing one or more methyl or ethyl groups; or a salt thereof, is suitable for the treatment of anxiety and depression.
    Type: Application
    Filed: August 5, 2011
    Publication date: January 19, 2012
    Applicant: BTG International Limited
    Inventors: Phillip Parsons, Silvia Trasciatti, Sergio Rosini, Michael Annis
  • Publication number: 20120015942
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: July 18, 2011
    Publication date: January 19, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
  • Publication number: 20110281850
    Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.
    Type: Application
    Filed: July 7, 2011
    Publication date: November 17, 2011
    Applicant: MANNKIND CORPORATION
    Inventors: Gary A. Flynn, Sandra Aeyoung Lee, Mary Faris, David William Brandt, Subrata Chakravarty
  • Patent number: 8044048
    Abstract: Derivatives of sulindac are provided along with pharmaceutical compositions containing them and use for precancerous conditions and treating cancer. Derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.
    Type: Grant
    Filed: January 4, 2007
    Date of Patent: October 25, 2011
    Assignee: Southern Research Institute
    Inventors: Gary Piazza, Robert Reynolds
  • Patent number: 8026231
    Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.
    Type: Grant
    Filed: March 28, 2006
    Date of Patent: September 27, 2011
    Assignee: CNRS
    Inventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore
  • Publication number: 20110195929
    Abstract: Described are various compounds and methods for the treatment of flaviviral infections. In particular, alkaloids and imino sugars in arabinose and/or lyxose stereochemical configuration with antiflaviviral activity are described.
    Type: Application
    Filed: August 4, 2009
    Publication date: August 11, 2011
    Applicant: SUMMIT CORPORATION PLC
    Inventors: Olivier De Moor, Graeme Horne, Penny Jane Middleton, Frank Schroer, Stephen Paul Wren, Maria Ines Passos Eleuterio, Renate Van Well, Colin Richard Dorgan, Francis Xavier Wilson, Robert Nash, Richard Storer, Graham Michael Wynne, Alan Geoffrey Roach, Akane Kawamura, Jonathon Mark Tinsley
  • Patent number: 7985776
    Abstract: A method of delivering a curcuminoid to a patient, which includes iontophoretically delivering a charged curcuminoid across the skin of an Alzheimer's Disease patient.
    Type: Grant
    Filed: June 27, 2008
    Date of Patent: July 26, 2011
    Assignee: Codman & Shurtleff, Inc.
    Inventors: Sean Lilienfeld, Thomas M. Di Mauro
  • Publication number: 20110152267
    Abstract: A method of treating a hyperproliferative disorder in a subject in need of such treatment, comprising administering to said subject, in combination, a treatment effective amount of: (a) a ceramide-increasing retinoid such as fenretinide or a pharmaceutically acceptable salt thereof; and (b) at least one (and in certain embodiments at least two) compounds selected from the groups consisting of (i) a non-18 carbon chain length L-threo-sphinganine(s) or pharmaceuticeutically acceptable salt thereof, (ii) glucosylceramide or glucosyl(dihydro)ceramide synthesis inhibitor(s), and (iii) sphingomyelin or dihydrosphingomyelin synthase inhibitor(s). Preferred L-threo-sphinganines are of carbon chain length 17 carbons, 19 carbons and 20 carbons. A preferred glucosylceramide or glucosyl(dihydro)ceramide synthesis inhibitor is D-threo-1-phenyl-2-palmitoylamino-3-morpholino-1-propanol. A preferred sphingomyelin or dihydrosphingomyelin synthesis inhibitor is D-threo-1-phenyl-2-palmitoylamino-3-morpholino-1-propanol.
    Type: Application
    Filed: November 12, 2010
    Publication date: June 23, 2011
    Inventors: Barry James Maurer, Charles Patrick Reynolds