The Chalcogen Is Bonded Directly To Two Carbon Atoms Patents (Class 514/239.2)
  • Patent number: 10561624
    Abstract: The present invention relates to the use of compositions comprising trans-clomiphene for treating men with hypogonadism. The invention is also directed to methods for treating males with hypogonadism.
    Type: Grant
    Filed: August 17, 2016
    Date of Patent: February 18, 2020
    Assignee: REPROS THERAPEUTICS INC.
    Inventor: Joseph S. Podolski
  • Patent number: 10385004
    Abstract: The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.
    Type: Grant
    Filed: February 11, 2016
    Date of Patent: August 20, 2019
    Assignee: Novartis AG
    Inventors: Benjamin Martin, Francesca Mandrelli, Francesco Venturoni
  • Patent number: 10343979
    Abstract: Methods for making prodrugs of trepreostinil and treprostinil derivatives are provided. Specifically, methods are provided herein for producing 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). The linkage, in one embodiment, is via an amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. The compounds provided herein can be used to treat pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension.
    Type: Grant
    Filed: November 18, 2015
    Date of Patent: July 9, 2019
    Assignee: Insmed Incorporated
    Inventors: Vladimir Malinin, Walter Perkins, Franziska Leifer, Donna M. Konicek, Zhili Li, Adam Plaunt
  • Patent number: 10160733
    Abstract: Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: December 25, 2018
    Assignee: Supernus Pharmaceuticals, Inc.
    Inventors: Likan Liang, Padmanabh P. Bhatt, David Dain, Jean-Philippe Taquet, Aleksandr Pechenov, Alexei Tchesnokov, Reynold Mariaux
  • Patent number: 10118055
    Abstract: Topical anti-pruritic compositions and methods of using the same to treat pruritus. These anti-pruritic compositions are capable of temporarily or permanently reducing, inhibiting, treating, ameliorating, and/or preventing pruritic skin conditions, as well as other related skin conditions. In a particular aspect, the present formulations provide a quicker and more effective treatment of pruritus than do certain present pruritus-treating compositions.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: November 6, 2018
    Assignee: STIEFEL LABORATORIES, INC.
    Inventors: Kathleen L. Clark, Joanne M. Fraser
  • Patent number: 10106491
    Abstract: Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: October 23, 2018
    Assignee: BioTheryX, Inc.
    Inventors: Kyle W. H. Chan, Frank Mercurio, David I. Stirling
  • Patent number: 9693953
    Abstract: The present invention provides novel pharmaceutical compositions containing triphenylethylene derivative compounds, and methods of using the composition for treatment of symptoms associated with atrophic vaginitis. The pharmaceutical compositions are prepared for the vaginal administration of triphenylethylene derivative compounds in single or combination therapies. Preferably, the triphenylethylene derivative is tamoxifen.
    Type: Grant
    Filed: June 4, 2007
    Date of Patent: July 4, 2017
    Inventors: Janet A. Chollet, Fred H. Mermelstein, Bernadette Klamerus
  • Patent number: 9604998
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure, kidney disease, edema, and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: March 28, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Reynalda Keh DeJesus, Fa-Xiang Ding, Shuzhi Dong, Jessica L. Frie, Xin Gu, Jinlong Jiang, Aurash Shahripour, Barbara Pio, Haifeng Tang, Shawn Walsh
  • Patent number: 9561201
    Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogs thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: February 7, 2017
    Assignee: Fibrotech Therapeutics PTY LTD
    Inventors: Spencer John Williams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Patent number: 9333207
    Abstract: A pharmaceutical composition for parenteral administration containing the active ingredient 1-adamantylethyloxy-3-morpholino-2-propanol, or pharmaceutically acceptable salts thereof, in a concentration range of from 3 to 100 mg/ml for the treatment of cerebrovascular disease.
    Type: Grant
    Filed: September 17, 2013
    Date of Patent: May 10, 2016
    Inventor: Gleb Vladimirovich Zagorii
  • Patent number: 9174975
    Abstract: The present invention provides a novel method for treatment of schizophrenia which can improve wide-ranging symptoms of schizophrenia, especially positive symptoms and negative symptoms without being accompanied by extrapyramidal symptoms, which comprises orally administering as an active compound (1R,2S,3R,4S)—N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboxyimide or a pharmaceutically acceptable salt thereof (e.g., hydrochloride) at a daily dose of 5 mg to 120 mg once a day to a patient with schizophrenia, and a therapeutic agent to be used in the method.
    Type: Grant
    Filed: August 20, 2003
    Date of Patent: November 3, 2015
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD
    Inventors: Mitsutaka Nakamura, Masaaki Ogasa, Shunsuke Sami
  • Publication number: 20150148347
    Abstract: A compound of formula I, wherein the groups R1, R2, R3, X, m, and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Application
    Filed: November 25, 2014
    Publication date: May 28, 2015
    Inventors: Iain LINGARD, Dieter HAMPRECHT
  • Publication number: 20150148318
    Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 28, 2015
    Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
  • Publication number: 20150093365
    Abstract: Provided herein are compositions containing photoactivatable caged tamoxifen and tamoxifen derivative molecules. Also provided are kits containing one of these compositions and a light source. Also provided are methods of optically inducing nuclear translocation of a fusion protein containing a mammalian estrogen receptor ligand binding domain in a eukaryotic cell and methods of optically inducing recombination in a eukaryotic cell that include contacting a eukaryotic cell with at least one of these compositions. Also provided are methods of treating breast cancer in a subject that include administering a photoactivatable caged tamoxifen or tamoxifen derivative molecule to a subject having breast cancer.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 2, 2015
    Inventors: Xin Lu, Sarit S. Agasti, Ronald A. DePinho, Ralph Weissleder
  • Publication number: 20150080369
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 19, 2015
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • 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
  • 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
  • Patent number: 8952006
    Abstract: Morpholinoalkyl fumarates, pharmaceutical compositions comprising the morpholinoalkyl fumarates, and methods of using morpholinoalkyl fumarates and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: February 10, 2015
    Assignee: XenoPort, Inc.
    Inventors: Kenneth C. Cundy, Suresh K. Manthati, David J. Wustrow
  • Publication number: 20150018340
    Abstract: The present invention relates to compounds having a pipecolate diketoamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pipecolate diketoamide compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
    Type: Application
    Filed: December 24, 2012
    Publication date: January 15, 2015
    Inventors: Ranganath Gopalakrishnan, Felix Hausch
  • Publication number: 20140371177
    Abstract: A method of treating cancer, inflammatory disease, and autoimmune disease by administering to a subject in need thereof an effective amount of one or more 1,5-dipenylpenta-1,4-dien-3-one compounds. The compounds feature either or both of the phenyl rings being substituted with hydroxyl, diethyl(2-alkoxyethyl)amine, 1-(2-alkoxyethyl)piperidine, sulfonate, phosphinate, or phosphate.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
  • 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: 20140348959
    Abstract: Compositions and methods for treatment of conditions such as ear pain are disclosed.
    Type: Application
    Filed: August 12, 2014
    Publication date: November 27, 2014
    Inventors: Mark A. Mitchnick, Garry Gwozdz
  • Publication number: 20140350018
    Abstract: Methods of reducing undesirable side effects during therapeutic treatment using monomethyl fumarate and prodrugs of monomethyl fumarate are disclosed.
    Type: Application
    Filed: August 22, 2013
    Publication date: November 27, 2014
    Applicant: XenoPort, Inc.
    Inventors: Kenneth C. Cundy, Sami Karaborni, Peter A. Virsik
  • Publication number: 20140350019
    Abstract: The present invention relates to aniline derivatives of formula (I), to their preparation and to their therapeutic application, for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C1-C6)alkyl or a CN; R1b represents H, an halogen or a (C1-C6)alkyl; R1c represents H or a (C1-C6)alkyl; R2 represents H, an halogen, an OH, an O—(C1-C6)alkyl or (C1-C6)alkyl; R3 represents H, an halogen, a (C1-C6)alkyl, an OH, an O—(C1-C6)alkyl, a CONH2 or CN; R4 represents H, an halogen or a (C1-C6)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C1-C6)alkyl, or one of its enantiomers.
    Type: Application
    Filed: September 7, 2012
    Publication date: November 27, 2014
    Applicant: FOVEA PHARMACEUTICALS
    Inventors: John Feutrill, Caroline Leriche, David Middlemiss
  • Publication number: 20140348914
    Abstract: Improved oral dosage forms of methyl hydrogen fumarate and prodrugs thereof are disclosed. Methods of treating diseases such as multiple sclerosis and psoriasis using such dosage forms are also disclosed.
    Type: Application
    Filed: August 22, 2013
    Publication date: November 27, 2014
    Applicant: XenoPort, Inc.
    Inventors: Sami Karaborni, Sarina Grace Harris Ma, Chen Mao, Ching Wah Chong, Peter Robert Prinz Freed, Mesut Ciper, Stefanie Krenzlin, David J. Wustrow, Peter A. Virsik
  • Publication number: 20140348915
    Abstract: Improved oral dosage forms of methyl hydrogen fumarate and prodrugs thereof are disclosed. Methods of treating diseases such as multiple sclerosis and psoriasis using such dosage forms are also disclosed.
    Type: Application
    Filed: August 22, 2013
    Publication date: November 27, 2014
    Applicant: XenoPort, Inc.
    Inventors: Sami Karaborni, Laura Elizabeth Bauer, Chen Mao, Ching Wah Chong, David J. Wustrow, Peter A. Virsik
  • Patent number: 8877753
    Abstract: The invention relates to the use of a group of sigma receptor ligands of formula (I) for the potentiation of the analgesic effect of opioids and opiates and at the same time for decreasing the dependency induced by them.
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: November 4, 2014
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Helmut Heinrich Buschmann, Jose Miguel Vela Hernandez, Daniel Zamanillo-Castanedo
  • Publication number: 20140323487
    Abstract: Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: David John Cowan, Andrew Lamont Larkin, Cunyu Zhang, David Lee Musso, Gary Martin Green, Rodolfo Cadilla, Paul Kenneth Spearing, Michael Joseph Bishop, Jason Daniel Speake
  • Publication number: 20140315905
    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: July 2, 2014
    Publication date: October 23, 2014
    Inventor: Soren Ebdrup
  • Publication number: 20140301954
    Abstract: The present invention provides methods of administering an active agent to a specifically identified area of mucous membrane of a human being, as well as a body dissolving film formed therefore.
    Type: Application
    Filed: June 18, 2014
    Publication date: October 9, 2014
    Inventor: Andrew L. Skigen
  • Publication number: 20140286876
    Abstract: The present invention, as described above and as further defined by the claims, provides methods of administering an active agent via adhesion of a film to a mucous membrane in the oral cavity of a mammal, as well as and ODF formed therefore. An active agent may be ingested as the ODF dissolves resulting in systemic treatment of the mammal. In additional embodiments, an ODF may provide topical administration of an active agent.
    Type: Application
    Filed: March 28, 2014
    Publication date: September 25, 2014
    Inventor: Andrew L. Skigen
  • Publication number: 20140275048
    Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Alkermes Pharma Ireland Limited
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Publication number: 20140271921
    Abstract: A topical composition comprises at least 5 wt % metronidazole or a pharmacologically acceptable derivative thereof in a non-aqueous vehicle. The composition may be used in the treatment of conditions of the colon, rectum, anorectum and perianal region, in particular inflammatory bowel disease and perianal Crohn's disease. The composition also relieves pain and inflammation and promotes healing of the colon, rectum, anorectum and perianal region following surgical operations. One advantage of the composition is that topical administration of metronidazole results in a primarily local effect and thus side effects observed from systemic administration are avoided.
    Type: Application
    Filed: May 28, 2014
    Publication date: September 18, 2014
    Applicant: SLA PHARMA AG
    Inventor: DAVID NIGEL ARMSTRONG
  • Publication number: 20140256688
    Abstract: A topical anorectal composition includes trimethylsiloxysilicate; at least one surfactant selected from the group consisting of sodium lauryl sulfate, alkyl- and alkoxy-dimethicone copolyol, polysorbate and a combination thereof; a non-polar volatile siloxane solvent; at least 15% (w/w) water; and a pharmaceutical agent selected from the group consisting of pramoxine, phenylephrine, hydrocortisone, salicylic acid, nitroglycerine, sildenafil, or their salts and combinations thereof, wherein the composition is sufficiently designed to dry within 60 seconds after application to the anorectal mucosa to form a dried composition, and wherein the dried composition forms: a flexible film, wherein the flexible film closely follows irregularities of the body surface as well as movement of the body surface, and (ii) a durable film, wherein the durable film does not crack or flake off and remains intact for more than 12 hours giving release of the pharmaceutical agent for an extended period of time.
    Type: Application
    Filed: March 10, 2014
    Publication date: September 11, 2014
    Inventors: Evgenia Lozinsky, Eran Eilat
  • Publication number: 20140255521
    Abstract: A topical composition includes at least one film forming ingredient; at least one surfactant; at least one non-polar volatile siloxane solvent; at least 15% (w/w) water; and a therapeutically effective concentration of at least one pharmaceutical agent, wherein the composition is sufficiently designed to dry within 60 seconds after application to a body surface to form a dried composition, and wherein the dried composition forms: a flexible film, wherein the flexible film closely follows irregularities of the body surface as well as movement of the body surface, and (ii) a durable film, wherein the durable film does not crack or flake off and remains intact for more than 12 hours giving release of the pharmaceutical agent for an extended period of time.
    Type: Application
    Filed: March 10, 2014
    Publication date: September 11, 2014
    Applicant: PeriTech Pharma Ltd.
    Inventors: Evgenia Lozinsky, Eran Eilat
  • Publication number: 20140255522
    Abstract: A topical anorectal or genital composition includes at least one film forming ingredient; at least one surfactant; at least one non-polar volatile siloxane solvent; at least 15% (w/w) water, and a therapeutically effective concentration of at least one pharmaceutical agent, wherein the composition is sufficiently designed to dry within 60 seconds after application to the anorectal or genital surface to form a dried composition, and wherein the dried composition forms: a flexible film, wherein the flexible film closely follows irregularities of the body surface as well as movement of the body surface, and (ii) a durable film, wherein the durable film does not crack or flake off and remains intact for more than 12 hours giving release of the pharmaceutical agent for an extended period of time.
    Type: Application
    Filed: March 10, 2014
    Publication date: September 11, 2014
    Applicant: PeriTech Pharma Ltd.
    Inventors: Evgenia Lozinsky, Eran Eilat
  • Publication number: 20140256730
    Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
    Type: Application
    Filed: January 13, 2014
    Publication date: September 11, 2014
    Applicant: Corsair Pharma, Inc.
    Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
  • Publication number: 20140234271
    Abstract: We have discovered that p63 inhibition results in increased cellular proliferation. We have also performed a screen for agents capable of increasing cellular proliferation, (e.g., of stem cells such as skin-derived precursors (SKPs)). The invention therefore invention provides compositions, methods, and kits for increasing proliferation of cells, using compounds that decrease p63 expression or activity or using the compounds described herein. The invention also features methods of using these compounds for increasing hair growth, improving skin health, or promoting skin repair in a subject.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 21, 2014
    Applicant: THE HOSPITAL FOR SICK CHILDREN
    Inventors: Freda D. MILLER, David KAPLAN, Kristen SMITH, Maryline PARIS, Sibel NASKA
  • Publication number: 20140234428
    Abstract: The invention, a transdermal delivery method, relates to penetration-enhancing pharmaceutical compositions comprising a novel, stable mixture of cetylated esters, cetyl or stearyl alcohols, polar solvents and surfactants, which, under appropriate conditions, combine into amphiphilic nanoparticles within a stabilized liquid dispersion for use in delivery of medicinal agents through the skin. The term cetosomes is used to describe these particles in order to differentiate them from other nanoparticles, such as niosomes, cerasomes, polymeric micelles, dendrimers, liposomes, lipoids, solid lipid nanoparticles and other particles. The self-assembling cetosomes, with both ionic and nonionic points of attraction, incorporate and concentrate a variety of different bioactive agents of interest and demonstrate stable properties with similarities to colloidal molecular structures. The compositions enhance topical transdermal fluxes of bioactives without permanently disrupting natural skin barrier function.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 21, 2014
    Applicant: Cymbiotics, Inc.
    Inventors: Raj R. Barathur, Jack Bain Bookout
  • Publication number: 20140228357
    Abstract: The present invention relates to novel compounds as HIF-1? inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1?, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1?-mediated VEGFA expression.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 14, 2014
    Inventors: Kyeong Lee, Mi-Sun Won, Hwan-Mook Kim, Song-Kyu Park, Ki-Ho Lee, Chang-Woo Lee, Bo-Kyung Kim, Hyun-Seung Ban, Kyung-Sook Chung, Naik Ravi
  • Publication number: 20140221330
    Abstract: An objective of the present invention is to provide a novel NDM (New Delhi metallo-?-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of ?-lactam antibiotics that have been inactivated as a result of decomposition by NDM.
    Type: Application
    Filed: July 26, 2012
    Publication date: August 7, 2014
    Inventors: Akihiro Morinaka, Kazunori Maebashi, Takashi Ida, Muneo Hikida, Mototsugu Yamada, Takao Abe
  • Publication number: 20140221361
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-19 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I and II: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Inventors: Jacob Swidorski, Brian Lee Venables, Zheng Liu, Ny Sin, Nicholas A. Meanwell, Alicia Regueiro-Ren
  • Publication number: 20140206670
    Abstract: The instant invention relates to a combination, particularly a synergistic combination, of an alpha-2-delta ligand and a dual serotonin-noradrenaline re-uptake inhibitor (DSNRI) or one or both of a selective serotonin re-uptake inhibitor (SSRI) and a selective noradrenaline re-uptake inhibitor (SNRI), and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Applicant: Pfizer Inc.
    Inventors: David James Dooley, Mark John Field, Richard Griffith Williams
  • Publication number: 20140194427
    Abstract: Provided is a compound of formula (I): or a pharmaceutically acceptable salt thereof. Also provided is a method of treating, prophylaxis, or amelioration of a disease, comprising administering to a subject in need of treatment for the disease an effective amount of a compound of formula (I) described herein. In one embodiment, the method is a neurodegenerative disease, such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, Huntington's disease, or Alzheimer's disease.
    Type: Application
    Filed: March 7, 2014
    Publication date: July 10, 2014
    Applicant: Biogen IDEC MA Inc.
    Inventor: Jianhua CHAO
  • Patent number: 8765812
    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 not Tranilast.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: July 1, 2014
    Assignee: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Willams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Publication number: 20140178503
    Abstract: The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: February 26, 2014
    Publication date: June 26, 2014
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventors: Ronald C. Newbold, Chengzhi Zhang
  • Publication number: 20140170196
    Abstract: The present invention provides disposable cloths that are designed to reduce itching discomfort when wiped across the vulvar tissue. These disposable cloths are wetted with a composition that includes at least one anesthetic, protectant, buffer, and surfactant. The composition is substantially clear and preferably does not bring about a cooling or stinging sensation when applied to the vulvar tissue. Furthermore, the composition has a pH adapted to vulvar use.
    Type: Application
    Filed: December 19, 2012
    Publication date: June 19, 2014
    Inventors: Bobby Corry, Russ Hovda, Michael L. Caswell
  • Publication number: 20140120185
    Abstract: The present invention provides a medicament having a wider treatment spectrum, causing a fewer side effects and superior in tolerability and safety, as compared to known typical antipsychotic agents and atypical antipsychotic agents. The present invention related to a medicament containing (I) a compound which is 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, and (II) at least one drug selected from the group consisting of a mood stabilizer, a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a serotonin and norepinephrine reuptake inhibitor, a noradrenergic and specific serotonergic antidepressant, an antianxiety drug, a tricyclic antidepressant, a tetracyclic antidepressant, an antipsychotic drug and an anti-ADHD drug, in combination.
    Type: Application
    Filed: April 4, 2012
    Publication date: May 1, 2014
    Inventors: Tsuyoshi Hirose, Kenji Maeda, Tetsuro Kikuchi, Masafumi Toda
  • Publication number: 20140065211
    Abstract: Improved oral dosage forms of methyl hydrogen fumarate and prodrugs thereof are disclosed. Methods of treating diseases such as multiple sclerosis and psoriasis using such dosage forms are also disclosed.
    Type: Application
    Filed: August 22, 2013
    Publication date: March 6, 2014
    Applicant: XenoPort, Inc.
    Inventors: Sami Karaborni, Sarina Grace Harris Ma, Chen Mao, Ching Wah Chong, Peter Robert Prinz Freed, Mesut Ciper, Stefanie Krenzlin, David J. Wustrow, Peter A. Virsik
  • Publication number: 20140057918
    Abstract: Methods of therapeutic treatment using monomethyl fumarate and prodrugs of monomethyl fumarate are disclosed.
    Type: Application
    Filed: August 22, 2013
    Publication date: February 27, 2014
    Applicant: XenoPort, Inc.
    Inventors: David J. Wustrow, Peter A. Virsik, Mark A. Gallop, Kenneth C. Cundy, Dmitri V. Lissin, Revati Shreeniwas