1,4-diazine As One Of The Cyclos Patents (Class 514/249)
  • Patent number: 8906911
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: December 9, 2014
    Assignee: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Guo Ping Wei, Lijuan Jane Wang
  • Publication number: 20140356430
    Abstract: Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologues and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition.
    Type: Application
    Filed: May 28, 2014
    Publication date: December 4, 2014
    Applicant: Signal Pharmaceuticals, LLC
    Inventors: Marie Georges BEAUCHAMPS, Antonio Christian FERRETTI, Juan Antonio GAMBOA, Kevin KLOPFER, William Edward KONNECKE, Matthew Michael KREILEIN, Anil MENON, Amanda Nicole MIKLOS, John Fitzgerald TRAVERSE
  • Publication number: 20140357640
    Abstract: The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula (I), (R2)n wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 18, 2012
    Publication date: December 4, 2014
    Applicant: SANOFI
    Inventors: Marc Nazare, Nis Halland, Friedemann chmidt, Tilo Weiss, Uwe Dietz, Armin Hofmeister
  • Publication number: 20140357611
    Abstract: A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventors: Krzysztof Palczewski, Akiko Maeda, Marcin Golczak
  • Publication number: 20140357641
    Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients.
    Type: Application
    Filed: January 11, 2013
    Publication date: December 4, 2014
    Applicant: NOVARTIS AG
    Inventors: Gurdip Bhalay, Steven Carl Chatlton, Mark Patrick Healy, Catherine Leblanc, Stephen Carl McKeown
  • Publication number: 20140357632
    Abstract: Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: August 13, 2012
    Publication date: December 4, 2014
    Inventors: Rajan Anand, Vincent J. Colandrea, Maud Reiter, Petr Vachal, Aaron Zwicker, Jonathan E. Wilson, Fengqi Zhang, Kake Zhao
  • Publication number: 20140356360
    Abstract: The present invention relates to piperazinyl derivatives of formula (I) and the use thereof as a drug, particularly for the treatment of cancer, the pharmaceutical compositions containing said derivatives, and the method for synthesising same.
    Type: Application
    Filed: December 28, 2012
    Publication date: December 4, 2014
    Inventor: Marc-Henry PITTY
  • Publication number: 20140357639
    Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.
    Type: Application
    Filed: June 19, 2014
    Publication date: December 4, 2014
    Inventors: Jan Kehler, Jacob Nielsen, Mauro Marigo, John Paul Kilburn, Morten Langgârd
  • Patent number: 8901117
    Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: December 2, 2014
    Assignee: The Regents of The University of Michigan
    Inventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
  • Patent number: 8901125
    Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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: Grant
    Filed: June 19, 2013
    Date of Patent: December 2, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
  • Patent number: 8900565
    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: Grant
    Filed: November 21, 2012
    Date of Patent: December 2, 2014
    Assignee: Pharmacyclics, Inc.
    Inventors: Joseph J. Buggy, Sriram Balasubramanian, Erik Verner, Vincent W. F. Tai, Chang-Sun Lee
  • Publication number: 20140350024
    Abstract: The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a substituted bicyclic heteroaromatic ring compound of formula I: wherein two of X1 to X8 are N and the remaining of X1 to X8 are CH; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 11, 2013
    Publication date: November 27, 2014
    Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Malvika Kaul
  • Publication number: 20140350023
    Abstract: The present invention claims amorphous solid state forms of sitagliptin salts, processes for their preparation, and pharmaceutical compositions thereof. As salt forming anions are claimed: The maleate, fumarate, besylate, mesylate and succinate.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 27, 2014
    Inventors: Suresh Babu Jayachandra, Jigar Bhaskarbhai Shah, Chiguru Sailu, Sandeep Thakaji Kanawade
  • Publication number: 20140349986
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 27, 2014
    Applicant: SANOFI
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Publication number: 20140350022
    Abstract: The present invention relates to a beneficial treatment of tumours in patients suffering from NSCLC, and to a clinical marker useful as as predictive variable of the responsiveness of tumours in patients suffering from NSCLC. The present invention further relates to a method for selecting patients likely to respond to a given therapy, wherein said method optionally comprises the use of a specific clinical marker. The present invention further relates to a method for delaying disease progression and/or prolonging patient survival of NSCLC patients, wherein said method comprises the use of a specific clinical marker.
    Type: Application
    Filed: May 2, 2014
    Publication date: November 27, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Birgit GASCHLER-MARKEFSKI, Ralf KAISER
  • Patent number: 8895557
    Abstract: Ecteinascidin formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: November 25, 2014
    Assignee: Pharma Mar, S.A., Sociedad Unipersonal
    Inventors: Jacob Hendrik Beijnen, Bastiaan Nuijen, Pilar Calvo Salve, Maria Tobio Barreira
  • Patent number: 8895558
    Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: November 25, 2014
    Assignee: Green Cross Corporation
    Inventors: Jinhwa Lee, Suk Youn Kang, Eun-Jung Park, Kwang-Seop Song, Min Ju Kim, Hee Jeong Seo, Suk Ho Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
  • Patent number: 8895559
    Abstract: A variety of specific compounds within the scope of formula I which are useful as PI3K inhibitors and can be employed for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours, and pharmaceutical compositions and kits containing said specific compounds.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Markus Klein, Ulrich Emde, Hans-Peter Buchstaller, Christina Esdar, Oliver Poeschke
  • Patent number: 8895750
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups ring A and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: November 25, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Todd Bosanac, Michael J. Burke, Darren Disalvo, Wang Mao, John Westbrook
  • Patent number: 8895740
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: November 25, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Juan-Miguel Jimenez, Luca Settimo, Damien Fraysse, Guy Brenchley, Christopher John Davis, Andrew W. Miller
  • Patent number: 8895560
    Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: November 25, 2014
    Assignee: Adolor Corporation
    Inventors: Roland E. Dolle, Bertrand Le Bourdonnec, Allan James Goodman
  • Publication number: 20140343066
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 20, 2014
    Inventors: Irini Akritopoulou-Zanze, Brian D. Wakefield, Helmut Mack, Sean C. Turner, Alan F. Gasiecki, Vijaya J. Gracias, Kathy A. Sarris, Douglas M. Kalvin, Melissa J. Michmerhuizen, Qi Shuai, Jyoti R. Patel, Margaretha H.M. Bakker, Nicole Teusch, Eric F. Johnson, Peter J. Kovar, Stevan W. Djuric, Andrew J. Long, Anil Vasudevan, Dawn M. George, Lu Wang, Biqin Li, Nigel S. Moore, Adrian D. Hobson, Keith W. Woods, Julie M. Miyashiro, Steven L. Swann, Jr., Thomas D. Penning
  • Publication number: 20140343069
    Abstract: One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Applicant: Sunovion Inc.
    Inventors: Karim LALJI, Timothy BARBERICH, Judy CARON, Thomas WESSEL
  • Publication number: 20140343068
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described. Specifically quinoxaline derivatives of Formula I and their use in modulating the activity of Braf and/or mutant Braf kinase to regulate and modulate abnormal or inappropriate cell proliferation, differentiation, or metabolism are disclosed. Also disclosed are methods of treating cancer associated with Braf and/or mutant Braf kinase activity in a subject, comprising administering the compounds of Formula I.
    Type: Application
    Filed: September 28, 2012
    Publication date: November 20, 2014
    Inventors: Xiangping Qian, Yong Zhu
  • Publication number: 20140341968
    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: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Inventors: Michael R. Robinson, Wendy M. Blanda, Patrick M. Hughes, Guadalupe Ruiz, Werhner C. Orilla, Scott M. Whitcup, Lon T. Spada, Devin F. Welty, Joan-En Lin
  • Publication number: 20140343067
    Abstract: The present invention relates to a method of reducing cutaneous facial flushing caused by systemic use of phosphodiesterase type 5 (PDE5) inhibitors by topical facial dermatological application of an effective dose of a composition comprising at least one alpha adrenergic receptor agonist.
    Type: Application
    Filed: October 12, 2012
    Publication date: November 20, 2014
    Inventors: Warren J. Scherer, Arthur Clapp, Philippe Andres
  • Publication number: 20140343480
    Abstract: Various agents and additives for cross-linking treatments are identified in disclosed studies. The characteristics of the various agents and additives may be advantageously employed in formulations applied in cross-linking treatments of the eye. In some embodiments, riboflavin is combined with Iron(II) to enhance the cross-linking activity generated by the riboflavin. In other embodiments, cross-linking treatments employ an Iron(II) solution in combination with a hydrogen peroxide pre-soak. In yet other embodiments, 2,3-butanedione is employed to increase the efficacy of corneal cross-linking with a photosensitizer, such as riboflavin. In further embodiments, folic acid is employed in combination with a photosensitizer, such as riboflavin, to enhance cross-linking activity. In yet further embodiments, 2,3-butanedione, folic acid, a quinoxaline, a quinoline, dibucaine, Methotrexate, menadione, or a derivative thereof is applied as a cross-linking agent.
    Type: Application
    Filed: May 19, 2014
    Publication date: November 20, 2014
    Applicant: AVEDRO, INC.
    Inventors: Pavel Kamaev, Marc D. Friedman, Evan Sherr, David Muller
  • Publication number: 20140343046
    Abstract: The present invention relates to the pharmaceutical use of selective GABA A ?5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.
    Type: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Inventors: Rodolfo Gasser, Maria-Clemencia Hernandez, Andrew Thomas
  • Patent number: 8889194
    Abstract: Disclosed is a compound and methods for use by an individual attempting to reduce or cease tobacco smoking or one exposed to environmental tobacco smoke. The compound includes a first component blocking nicotine receptor sites to reduce nicotine cravings or withdrawal symptoms, a second component increasing serotonin levels and acting synergistically with the first component to reduce nicotine cravings or withdrawal symptoms, assisting in maintaining body weight and reducing increased stress and anxiety, and a third component acting synergistically with the first and/or second component to reduce nicotine cravings or withdrawal symptoms, maintain body weight, and/or reduce increased stress and anxiety. The third component comprises a supplement that replenishes depleted body substance(s), repairs damaged body substance(s), and/or ameliorates the impaired function of body substance(s). Some combination of the first, second, and third component alters the perceived taste of tobacco smoke.
    Type: Grant
    Filed: September 29, 2010
    Date of Patent: November 18, 2014
    Inventor: Harlan Clayton Bieley
  • Patent number: 8889686
    Abstract: L malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are disclosed for decreasing the bitterness of eszopiclone dosage forms
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: November 18, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Patent number: 8889684
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R6, A, X, Y and m are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: November 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Heinz Stadtmueller
  • Patent number: 8889685
    Abstract: Maleate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The salts are useful for treating sleep disorders.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: November 18, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Patent number: 8889683
    Abstract: The present invention relates to novel quinoxaline compounds of Formula I: as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the quinoxaline compounds and the use of the quinoxaline compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: November 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Clifford Cheng, Gerald W. Shipps, Jr., Xiaohua Huang, Ying Huang, Ning Shao, Ashwin Rao, Anandan Palani, Peter Orth, Johannes H. Voigt, Robert J. Herr, Lana Michele Rossiter, Qi Zeng, Xianfeng Sun
  • Patent number: 8889664
    Abstract: The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: November 18, 2014
    Assignee: Exelixis, Inc.
    Inventors: William Bajjalieh, Lynne Canne Bannen, S. David Brown, Patrick Kearney, Morrison Mac, Charles K. Marlowe, John M. Nuss, Zerom Tesfai, Yong Wang, Wei Xu
  • Publication number: 20140336177
    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 act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Application
    Filed: December 11, 2012
    Publication date: November 13, 2014
    Inventors: Barbara Pio, Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Shawn Walsh
  • Publication number: 20140336196
    Abstract: The present invention relates to novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, and polymorphs, hydrates and solvates thereof, which are potent inhibitors of dipeptidyl peptidase-IV useful for the prevention and/or treatment of non-insulin dependent diabetes mellitus, also referred to as type 2 diabetes. The present invention also relates to the process for preparing the novel phosphoric acid salts of 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, as well as pharmaceutical compositions containing the novel phosphoric acid salts, and methods of use thereof for the treatment of diabetes, obesity, and high blood pressure.
    Type: Application
    Filed: May 22, 2012
    Publication date: November 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Jerry L. Atwood
  • Publication number: 20140336164
    Abstract: Biodegradable non-ophthalmic implants include one or more agents dispersed within a biodegradable polymer component. The implants release the agents from the biodegradable polymer component to a target site of a patient as the implant degrades. The agents provided in the implants can be therapeutic agents or diagnostic agents and are useful in medical treatments of non-ocular regions of a patient.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Inventors: Steven Pal, Mitchell Brin
  • Publication number: 20140336189
    Abstract: Compounds corresponding to the general formula (I) wherein R2 represents a group C1-10-alkyl, C3-10-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyl-C3-7-cycloalkyl, C3-7-cycloalkyl-C3-7-cycloalkyl, C1-6-alkylthio-C-1-10-alkyl, C1-6-alkoxy-C1-10-alkyl, hydroxy-C1-10-alkyl, hydroxy-C1-6-alkyl-C3-7-cycloalkyl-C1-6-alkyl, hydroxy-C3-10-cycloalkyl, C1-10-fluoroalkyl or C3-10-fluorocycloalkyl; an optionally substituted heterocyclic group; a group C1-10-alkyl substituted with an optionally substituted heterocyclic group; X6 represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-fluoroalkyl or cyano; and R7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt, and the therapeutic use thereof.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Inventors: Sylvain COTE-DES-COMBES, Jacques FROISSANT, Jean-Francois GIBERT, Frank MARGUET, Christophe PACAUD, Frederic PUECH, Antoine RAVET
  • Publication number: 20140336169
    Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: May 9, 2014
    Publication date: November 13, 2014
    Applicant: GILEAD CONNECTICUT, INC.
    Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J. M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
  • Publication number: 20140336141
    Abstract: The invention exploits the elucidation of a connection between the S-adenosylmethionine one-carbon cycle and MAO-B levels and describes drug efficacy testing methods and the use of compounds of the S-adenosylmethionine one-carbon cycle as MAO-B inhibitors in disease prevention and treatment.
    Type: Application
    Filed: December 21, 2012
    Publication date: November 13, 2014
    Inventors: Maria Zellner, Ellen Umlauf
  • Patent number: 8883744
    Abstract: The canonical Wnt signaling pathway is implicated in many disorders including neural tube defects, limb malformations, and heart defects, developmental disorders associated with alcohol exposure (fetal alcohol syndrome) or exposure to bipolar medications (i.e. lithium), wound healing, and Alzheimer's disease. Elevated plasma homocysteine (HCy), which results from folate (folic acid, FA) deficiency, the mood-stabilizing drug lithium (Li), and alcohol (ethanol) are linked to the induction of human congenital heart and neural tube defects. FA supplementation ameliorates the observed developmental errors in the Li-HCy, or alcohol-exposed mouse embryos and normalized heart function. Li, HCy or Wnt3A suppress Wnt-modulated Hex and Islet-1 expression. FA protects from the gene misexpression that is induced by all three factors. Administration of myo-inositol with FA synergistically enhances the protective effect.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: November 11, 2014
    Assignee: University of South Florida
    Inventor: Kersti K. Linask
  • Patent number: 8883784
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
    Type: Grant
    Filed: August 12, 2013
    Date of Patent: November 11, 2014
    Assignee: AbbVie Inc.
    Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
  • Publication number: 20140329798
    Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119.
    Type: Application
    Filed: November 9, 2012
    Publication date: November 6, 2014
    Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
  • Publication number: 20140329795
    Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
    Type: Application
    Filed: August 28, 2012
    Publication date: November 6, 2014
    Inventors: Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson, Celia Dominguez, Leticia M. Toledo-Sherman, Ignacio Munoz
  • Publication number: 20140329821
    Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: July 9, 2014
    Publication date: November 6, 2014
    Inventors: Xicheng Sun, Jian Qiu, Adam Stout
  • Publication number: 20140329794
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 6, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Publication number: 20140328860
    Abstract: This disclosure demonstrates that blockade of TGF? signaling after a hematopoietic stress (e.g., chemotherapy, transplantation, and infection) accelerates hematopoietic reconstitution and delays the return of cycling hematopoietic stem and progenitor cells (HSPCs) to quiescence. TGF? blockade in these settings promotes multilineage hematopoietic regeneration by prolonging HSPC cycling and by promoting HSC self-renewal, and is useful for treating hematologic deficiencies caused various hematopoietic stresses.
    Type: Application
    Filed: November 21, 2012
    Publication date: November 6, 2014
    Applicant: CORNELL UNIVERSITY
    Inventors: Joseph Scandura, Fabienne Brenet
  • Patent number: 8877743
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: November 4, 2014
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
  • Patent number: 8877755
    Abstract: The present invention generally relates to pharmaceutical compositions comprising a dopamine agonist and sedative agent. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine. In a preferred embodiment, the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine; and the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. The pharmaceutical compositions of the invention are useful in the treatment of restless-leg syndrome and periodic-limb-movement disorder, as well as various sleep disorders.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: November 4, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventor: Timothy J. Barberich
  • Patent number: 8877757
    Abstract: The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: November 4, 2014
    Assignee: Merck Serono SA
    Inventors: Pascale Gaillard, Anna Quattropani, Vincent Pomel, Thomas Rueckle, Jasna Klicic, Dennis Church