Chalcogen Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/424)
  • Patent number: 11407710
    Abstract: Provided is a method for preparing an N-cyclopropylmethyl aniline compound, which comprises hydrogenating a compound represented by Formula II and cyclopropyl formaldehyde as raw materials in the presence of an acid and catalyst to generate an N-cyclopropylmethyl aniline compound represented by Formula I, wherein R is alkoxy, alkylamino or a substituted anilino group represented by Formula III.
    Type: Grant
    Filed: December 3, 2021
    Date of Patent: August 9, 2022
    Inventors: Chaoqun Huang, Jintao Zhu, Liang Lv, Liangming Luo, Rong Zhang, Jiyong Liu
  • Patent number: 11298347
    Abstract: Methods and uses for diagnosing and treating Tourette syndrome are encompassed, wherein diagnosis and treatment may be based upon an assessment of genetic alterations in metabotropic glutamate receptor (mGluR) network genes and wherein treatment is with nonspecific activators of mGluRs such as fasoracetam.
    Type: Grant
    Filed: March 4, 2020
    Date of Patent: April 12, 2022
    Assignee: THE CHILDREN'S HOSPITAL OF PHILADELPHIA
    Inventors: Hakon Hakonarson, Charlly Kao
  • Patent number: 11173153
    Abstract: Methods and uses for diagnosing and treating anxiety disorders are encompassed, wherein diagnosis and treatment may be based upon an assessment of genetic alterations in metabotropic glutamate receptor (mGluR) network genes and wherein treatment is with nonspecific activators of mGluRs such as fasoracetam.
    Type: Grant
    Filed: September 7, 2016
    Date of Patent: November 16, 2021
    Assignee: THE CHILDREN'S HOSPITAL OF PHILADELPHIA
    Inventors: Hakon Hakonarson, Charlly Kao
  • Patent number: 11123311
    Abstract: This invention provides methods for preventing, mitigating, ameliorating and/or controlling psychiatric disorders, including depression, major depression, bipolar disorder, schizophrenia and substance abuse (including addiction and dependence) by administration of an agent that increases epoxy-fatty acids (e.g., an inhibitor of soluble epoxide hydrolase), as sole active agent or in combination with another agent (e.g., an antidepressant, an antipsychotic, an anxiolytic). When co-administered in combination with another agent, one or both agent may be administered at a subtherapeutic dose.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: September 21, 2021
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Bruce D. Hammock, Christophe Morisseau, Jun Yang, Kenji Hashimoto
  • Patent number: 11021513
    Abstract: The present invention is directed to compounds, compositions and methods for preventing, treating or curing Norovirus infection in human subjects or other animal hosts.
    Type: Grant
    Filed: May 15, 2017
    Date of Patent: June 1, 2021
    Assignee: EMORY UNIVERSITY
    Inventors: Raymond F. Schinazi, Franck Amblard, Ladislau Kovari, Peng Liu, Shaoman Zhou, Benjamin D. Kuiper, Bradley J. Keusch
  • Patent number: 10875830
    Abstract: Lactams for use in the treatment of respiratory tract infections, including chronic lung infections in patients having cystic fibrosis.
    Type: Grant
    Filed: July 13, 2017
    Date of Patent: December 29, 2020
    Assignee: Conopeo, Inc.
    Inventors: Neil James Parry, Paolo Pantalone, Paul Williams
  • Patent number: 10806717
    Abstract: This invention relates to methods and compositions for treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of inhibitors of synaptic vesicle glycoprotein 2A (SV2A), alone or in combination with valproate, in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: October 20, 2020
    Assignee: The Johns Hopkins University
    Inventors: Michela Gallagher, Rebecca Haberman, Ming Teng Koh, Arnold Bakker
  • Patent number: 10781170
    Abstract: A process for the preparation of Brivaracetam, an anti-convulsion drug, is provided comprising Hofmann rearrangement of (S)-3-(2-(chloroamino)-2-oxoethyl) hexanoic acid, followed by cyclization resulting in (R)-4-propyl-pyrrolidin-2-one which on condensation with bromo butyric acid or ester followed by reaction with ammonia results in Brivaracetam.
    Type: Grant
    Filed: October 23, 2019
    Date of Patent: September 22, 2020
    Assignee: Divi's Laboratories Ltd.
    Inventors: Murali Krishna Prasad Divi, Mysore Aswatha Narayana Rao, Shaik Nowshuddin
  • Patent number: 10570090
    Abstract: Compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a —COOH, a —OH or a —OPO(OH)2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a —OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a —COOH, —OH or —OPO(OH)2 group, then R5 represents a hydrogen atom; when R5 represents a —OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group; and the preparation and the therapeutic uses of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: February 25, 2020
    Assignee: SANOFI
    Inventors: Monsif Bouaboula, Maurice Brollo, Victor Certal, Youssef El-Ahmad, Bruno Filoche-Romme, Frank Halley, Gary McCort, Laurent Schio, Michel Tabart, Corinne Terrier, Fabienne Thompson
  • Patent number: 10538484
    Abstract: A maleamic acid monomer, and a preparation method and a use of the maleamic acid monomer. The structural formula of the monomer is as follows: formula (1), wherein, R is selected from The maleamic acid monomer provided in the present invention may be used as a comonomer to prepare temperature-tolerant and calcium salt-tolerant polymers.
    Type: Grant
    Filed: September 12, 2018
    Date of Patent: January 21, 2020
    Assignees: China Petroleum & Chemical Corporation, SINOPEC Research Institute of Petroleum Engineering
    Inventors: Xiaohua Yang, Yongxue Lin, Jian He, Lin Wang, Haibo Wang, Fan Yang, Zhoujun Li, Xiaoqiang Dong
  • Patent number: 10537550
    Abstract: The present invention describes the combination of topically inhaled medicinal formulations comprising an anticholinergic component and a glucocorticosteroid component and its use in the symptomatic and prophylactic treatment of diseases of the respiratory tract, especially with an obstructive component or underlying inflammation like asthma and chronic obstructive pulmonary disease (COPD). It further comprises the presentation of this combination in a locally applied (inhaled) formulation and application in an inhalation device for instance in the NOVOLIZER®.
    Type: Grant
    Filed: August 11, 2008
    Date of Patent: January 21, 2020
    Assignee: MEDA PHARMA GMBH & CO. KG
    Inventors: Joachim Goede, Joachim Maus, Peter Jürgen Cnota, Istvan Szelenyi
  • Patent number: 9789044
    Abstract: This invention relates to a group of compounds for repelling blood-feeding ectoparasitic arthropods, and a method of deterring their landing and feeding on animals including humans, by applying in one or more formulations compounds that incorporate one or more sulfide and one or more hydroxyl groups to the skin, clothing or environment of animals, including humans. A method of repelling and deterring landing and feeding by blood-feeding arthropods on an animal by applying in effective amount one or more compounds that incorporate alkyl sulfide and alcohol moieties, or alkyl sulfide and amide moieties, or alkyl sulfide and amide moieties to the skin, clothing or environment of an animal.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: October 17, 2017
    Assignee: SCOTTS CANADA LTD
    Inventors: Regine M. Gries, Grigori Khaskin, Gerhard G. Gries
  • Patent number: 9688627
    Abstract: Disclosed herein are compounds of formula (I) wherein L1, L2, L3, L4, R1, R4, R5, R6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: June 27, 2017
    Assignee: CAYMAN CHEMICAL COMPANY, INC.
    Inventors: Stephen Douglas Barrett, Joseph Michael Colombo, Bradlee David Germain, Gregory William Endres, Andriy Komilov, James Bernard Kramer, Adam Uzieblo, Fred Lawrence Ciske, Kirk M. Maxey, James Paul O'Malley, Thomas Allen Owen
  • Patent number: 9669009
    Abstract: A high dose rapidly dispersing three-dimensionally printed dosage form comprising a high dose of levetiracetam in a porous matrix that disperses in water within a period of less than about 15 seconds is disclosed. Also disclosed are methods of preparing the dosage form and of treating a condition, disease or disorder that is therapeutically responsive to levetiracetam.
    Type: Grant
    Filed: April 11, 2016
    Date of Patent: June 6, 2017
    Assignee: Aprecia Pharmaceuticals Company
    Inventors: Jules Jacob, Norman Coyle, Thomas G. West, Donald C. Monkhouse, Henry L. Surprenant, Nemichand B. Jain
  • Patent number: 9611284
    Abstract: The invention provides in part, conjugate compounds. The invention also provides synthesis methods for making the compounds, and uses of the compounds.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: April 4, 2017
    Assignee: Simon Fraser University
    Inventors: Robert N. Young, Stephen Arns, Anne Moreau, Mohammed Monzur Morshed, Romelo Gibe
  • Patent number: 9604932
    Abstract: Compounds are of the class of 1-pyrrolidinyloxy,1-piperidinyloxy, and 1-azepanyloxy derivatives of formula (I): The compounds are useful in prevention, treatment or management of diseases, disorders or conditions associated with oxidative stress or endothelial dysfunction. The compounds include 2,2,5,5,-tetramethyl-3-(nitrooxymethyl)pyrrolidin-1-yl acetate.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: March 28, 2017
    Assignee: Radikal Therapeutics Inc.
    Inventors: Andrew Lurie Salzman, Prakash Jagtap, Garry John Southan
  • Patent number: 9446011
    Abstract: The present invention is directed to a pharmaceutical composition comprising a Compound (a) of a class of peptide Compounds and at least one further Compound (b) for the prevention, alleviation or/and treatment of epileptic seizures.
    Type: Grant
    Filed: March 31, 2015
    Date of Patent: September 20, 2016
    Assignee: UCB PHARMA GMBH
    Inventor: Thomas Stöhr
  • Patent number: 9402826
    Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.
    Type: Grant
    Filed: September 29, 2014
    Date of Patent: August 2, 2016
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Richard Ambron, Ying-Ju Sung, Jeremy Greenwood, Leah Frye, Shi-Xian Deng, Yuli Xie, Donald W. Landry
  • Patent number: 9376441
    Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
    Type: Grant
    Filed: July 31, 2014
    Date of Patent: June 28, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel, Jennifer R. Lo, Seung H. Lee, Zhongdong Zhao, Jeffrey Kropf, Jianjun Xu, Peter Blomgren, Scott A. Mitchell, JinMing Xiong, Jayaraman Chandrasekhar
  • Patent number: 9210928
    Abstract: A method of stimulating germination in plant seeds and/or releasing plant tissue or plant organs from dormancy, comprising applying to a seed, plant, plant organ or plant tissue a compound of formula (I): where: R1 is alkyl or H; R2, R3, R4 and R5 are independently selectable from H, halide, —NO2, —SO2R?, —OH, —Oalkyl where R? is alkyl or aminoalkyl; and/or R1 and R5 are joined as —O(CH2)m—, where m is 1, 2, 3 or 4; R6 is a substituted or non-substituted alkyl, and/or substituted or non-substituted aryl; and n is an integer of 1 to 4.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: December 15, 2015
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Andrew Thompson, Timothy Bugg
  • Patent number: 9084778
    Abstract: A composition in the form of an oil in water emulsion, preferably without emulsifier, is described. The composition can include, in a physiologically acceptable environment, at least one new retinoid. Also described, is the method of preparing the composition and its use in cosmetics and dermatology.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: July 21, 2015
    Assignee: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Agnes Duprat, Claire Mallard
  • Publication number: 20150147403
    Abstract: Compositions including at least 3?-tert-butyl-4?-(2-hydroxy-ethoxy)-4?-pyrrolidin-1-yl-[1,1?;3,1?]-terphenyl-4-carboxylic acid are described. The compositions can be oil-in-water emulsions made up of oily liquid globules each provided with a lamellar liquid crystal coating dispersed in an aqueous phase; a retinoid is either in the oily liquid globules or in the aqueous phase; each oily liquid globule is individually coated with a unilamellar or oligolamellar layer, obtained from at least one lipophilic surfactant, at least one hydrophilic surfactant and at least one separate anionic surfactant, and the coated oily liquid globules have a mean diameter lower than 800 nm.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 28, 2015
    Inventor: Amel Djedour
  • Publication number: 20150141481
    Abstract: Inhalation solutions for administration of beta 2-agonists or combinations of muscarinic antagonists and beta 2-agonists for the treatment of breathing disorders, such as COPD, are provided. The inhalation solutions are administered by nebulization, particularly with a high efficiency nebulizer.
    Type: Application
    Filed: June 17, 2014
    Publication date: May 21, 2015
    Inventors: William GERHART, Ahmet TUTUNCU
  • Publication number: 20150126493
    Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20150126576
    Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.
    Type: Application
    Filed: September 29, 2014
    Publication date: May 7, 2015
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Richard Ambron, Ying-Ju Sung, Jeremy Greenwood, Leah Frye, Shi-Xian Deng, Yuli Xie, Donald W. Landry
  • Publication number: 20150126518
    Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
  • Publication number: 20150125441
    Abstract: The present invention provides methods of treating and pharmaceutical compositions useful for treating a mood disorder or depressive symptoms associated with pain, inducing analgesia and treating pain in a subject by administering a pharmaceutically effective amount of an agent capable of one or more of increasing GluA1 level, expression, concentration, or biological activity, increasing calcium permeable AMPA (? amino-3-hydroxy-5-methylisoxazole-4-propionic acid) receptor (CPAR) level, expression, concentration, or biological activity or potentiating a CPAR current. The agent may be an AMPA potentiator or ampakine. The agent may increase AMPA receptor currents by slowing the deactivation of open channels and may be, for instance, 2-pyrrolidinone, 4-[2-(phenylsulfonylamino)ethylthio]-2,6-difluorophenoxyacetamide (PEPA) or LY451646. The agent may also be a protein, RNA or DNA product.
    Type: Application
    Filed: May 24, 2013
    Publication date: May 7, 2015
    Applicant: New York University
    Inventors: Jing Wang, Edward Ziff
  • Patent number: 9012494
    Abstract: The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo,
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: April 21, 2015
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Libuse Jaroskova, Joannes Theodorus Maria Linders, Christophe Francis Robert Nestor Buyck, Louis Jozef Elisabeth Van Der Veken, Vladimir Dimtchev Dimitrov, Theo Teofanov Nikiforov
  • Publication number: 20150099720
    Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.
    Type: Application
    Filed: October 20, 2014
    Publication date: April 9, 2015
    Inventors: Lin Zhi, Robert I. Higuchi, E. Adam Kallel, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Daniel A. Ruppar, Bijan Pedram, Thomas Lot Stevens Lau, Todd A. Miller
  • Publication number: 20150099788
    Abstract: The present invention provides methods of treating and preventing arrhythmia and other diseases or disorders, using ion channel modulating compounds, including vernakalant hydrochloride. The present invention further provides controlled release oral formulations and dosages of vernakalant hydrochloride, which are effective in preventing arrhythmia. Certain methods and formulations of the present invention are adapted for the treatment and prevention of arrhythmia and other disease or disorders in subjects identified as having altered drug metabolism due to polymorphism of the gene encoding cytochrome P450 2D6.
    Type: Application
    Filed: June 17, 2014
    Publication date: April 9, 2015
    Inventors: Jeffery J. Wheeler, Gregory N. Beatch
  • Publication number: 20150099765
    Abstract: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson
  • Publication number: 20150099740
    Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
  • Publication number: 20150094353
    Abstract: The present invention provides STAT3 inhibitors which preferentially suppress proliferation of cancer over non-cancer cells and inhibit migration and invasion of malignant cells. The inhibitors of the present invention selectively inhibit STAT3 binding to DNA without affecting the activation and dimerization of STAT3. Furthermore, the inhibitors of the present invention inhibit expression of STAT3 downstream target genes and STAT3 binding to chromatin in situ.
    Type: Application
    Filed: September 25, 2014
    Publication date: April 2, 2015
    Inventor: Jian-Ting Zhang
  • Publication number: 20150094352
    Abstract: This invention relates to treating age-related cognitive impairment. This invention in particular relates to the use of inhibitors of synaptic vesicle protein 2A (SV2A), such as levetiracetam, seletracetam, and brivaracetam, in improving cognitive function in subjects that exhibit age-related cognitive impairment or are at risk thereof, including, without limitation, subjects having or at risk for Mild Cognitive Impairment (MCI), Age-related Cognitive Decline (ARCD) or Age-Associated Memory Impairment (AAMI).
    Type: Application
    Filed: April 25, 2014
    Publication date: April 2, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Michela Gallagher, Rebecca Haberman, Ming Teng Koh
  • Patent number: 8974831
    Abstract: Carrier particles in which at least 60% of the surface is coated with magnesium stearate are useful for preparing dry powder formulations for inhalation.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: March 10, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Rossella Musa, Daniela Cocconi, Alain Chamayou, Laurence Galet
  • Publication number: 20150065497
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: March 5, 2015
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
  • 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: 20150059746
    Abstract: A method is disclosed for making a pharmaceutical composition for pulmonary administration, the method comprising a step in which an inhalable pharmaceutically active material is acoustically blended in a resonant acoustic blender. The invention also relates to compositions for inhalation prepared by the method.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventor: Matthew Green
  • Publication number: 20150065561
    Abstract: The present invention is based, in part, on our studies of molecular pathways that include the deubiquitinase CYLD. Accordingly, the present invention features, inter alia, nucleic acid constructs that express CYLD or a biologically active variant thereof (e.g., a variant including the catalytic domain), nucleic acids that inhibit the expression of a negative regulator of CYLD (e.g., PDE4B or LNK2), nucleic acids that modulate the expression of downstream CYLD targets (e.g., Akt, by inhibiting or promoting the expression of the downstream target), compositions including one or more of these types of constructs (e.g., pharmaceutical compositions), kits including one or more of the compositions described herein and instructions for use, screening methods to identify therapeutic agents {e.g., anti-inflammatory agents) that upregulate CYLD, downregulate a negative regulatory of CYLD, or modulate (e.g., inhibit) a downstream CYLD target (e.g.
    Type: Application
    Filed: April 9, 2013
    Publication date: March 5, 2015
    Applicant: Georgia State University Research Foundation, Inc.
    Inventor: Jian-Dong Li
  • Patent number: 8969401
    Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: March 3, 2015
    Assignee: 4SC AG
    Inventors: Thomas Maier, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
  • Patent number: 8969402
    Abstract: A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: March 3, 2015
    Inventor: Steven A. Rich
  • Publication number: 20150057248
    Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.
    Type: Application
    Filed: September 1, 2014
    Publication date: February 26, 2015
    Applicant: The Board of Regents of The University of Texas System
    Inventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
  • Patent number: 8962676
    Abstract: The present invention is directed to the treatment of demyelination as an underlying cause of the disease of multiple sclerosis (MS) in a mammal, the method comprising promoting remyelination of myelination of axonal cells by administering to the mammal a 2-oxopyrrolidine compound having a general formula I: wherein R?R??H, and R??CH2CONH-(2,6CH3)C6H3 or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: February 24, 2015
    Assignee: University College Dublin, National University of Ireland, Dublin
    Inventors: Mark Pickering, Keith Murphy
  • Publication number: 20150051161
    Abstract: The present invention provides compositions and methods for detecting carboxymethyl-lysine (CML) and circulating receptor for advanced glycation end (RAGE) products, and methods for correlating CML and RAGE levels with age-related disease. In particular, serum CML and/or circulating receptor for advanced glycation end (RAGE) products can be used as a clinical biomarker in diagnostics to identify people who are at a higher risk of developing adverse ageing-related outcomes.
    Type: Application
    Filed: April 10, 2014
    Publication date: February 19, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Richard David Semba, Luigi Ferruci, Edward G. Lakatta
  • Publication number: 20150051233
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reducing the risk of fibrosis in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction of the risk of fibrosis. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: February 19, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Sandeep K. Agarwal, Mesias Pedroza
  • Publication number: 20150037425
    Abstract: The present invention relates to pharmaceutical powders for inhalation produced by a method consisting of a first step of mixing particles of a force-controlling agent selected from a salt of a fatty acid with particles of one or more pharmacologically active materials and a second step of sieving or blending the powder with a carrier material.
    Type: Application
    Filed: September 22, 2014
    Publication date: February 5, 2015
    Inventor: Rudi Mueller-Walz
  • Patent number: 8946446
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: February 3, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Publication number: 20150031670
    Abstract: Compounds of the formula (I), in which R1, R3, R5, R6, R7, R, X and Y have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: March 21, 2013
    Publication date: January 29, 2015
    Applicant: MERCK PATENT GmbH
    Inventors: Timo Heinrich, Frank Zenke, Mireille Krier, Manja Friese-Hamim, Jeyaprakashnarayanan Seenisamy
  • Patent number: 8940776
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: January 27, 2015
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
  • Patent number: 8920846
    Abstract: A microcapsule in which a liquid droplet is coated with a resin, wherein in the droplet, a pesticidally active solid ingredient is suspended in a compound of formula (I), wherein R represents a C1-C5 alkyl group, is useful as a formulation of a pesticidally active solid ingredient.
    Type: Grant
    Filed: September 2, 2010
    Date of Patent: December 30, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Naoki Tsuda, Mayuko Ozawa