Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
  • Patent number: 9931325
    Abstract: The present invention provides new methods and kits for treating IBS; treating IBS in females; treating IBS in older subjects; and treating IBS in non-white subjects.
    Type: Grant
    Filed: January 4, 2017
    Date of Patent: April 3, 2018
    Assignee: Salix Pharmaceuticals, Ltd.
    Inventors: William Forbes, Enoch Bortey
  • Patent number: 9890166
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: May 26, 2014
    Date of Patent: February 13, 2018
    Assignee: NOVARTIS AG
    Inventors: Jutta Blank, Guido Bold, Simona Cotesta, Vito Guagnano, Heinrich Rueeger, Andrea Vaupel
  • Patent number: 9809558
    Abstract: Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent.
    Type: Grant
    Filed: October 1, 2014
    Date of Patent: November 7, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Peter Kumpalume, Oliver Schon, Christine Patricia Donahue, Ghotas Evindar, David I. Israel, David Paolella, Letian Kuai, Ninad V. Prabhu
  • Patent number: 9765081
    Abstract: A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: September 19, 2017
    Assignee: NeOnc Technologies, Inc.
    Inventors: Thomas Chen, Daniel Levin, Satish Puppali
  • Patent number: 9765088
    Abstract: The present invention relates to an improved and industrially advantageous process for the preparation of Rifaximin with high purity and yield. Particularly, the present invention relates to improved processes for the preparation of Rifaximin from Rifamycin O and S. More particularly the present invention relates to a process for the preparation of Rifaximin through 3-halorifamycin S. The present invention further relates to a novel polymorph of Rifaximin and process for its preparation.
    Type: Grant
    Filed: April 19, 2015
    Date of Patent: September 19, 2017
    Assignee: GRANULES INDIA LIMITED
    Inventors: Prasada Raju Vetukuri Vnkv, Goverdhan Gilla, Ambaiah Boini, Krishna Prasad Chigurupati
  • Patent number: 9725425
    Abstract: Provided are small molecule inhibitors of ubiquitin specific protease 2, 8 and 12 (USP2 and USP8 and USP12) activity and methods for their use in treating cancers. The small molecule inhibitors of the invention are particularly useful in the treatment of non-small cell lung cancers that are resistant to tyrosine kinase inhibitors and in the treatment of prostate cancer that is resistant to AR inhibitor therapy.
    Type: Grant
    Filed: February 25, 2015
    Date of Patent: August 8, 2017
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Alan D. D'Andrea, Nathanael Gray, Sara Jean Buhrlage, Kalindi Parmar
  • Patent number: 9657026
    Abstract: A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: May 23, 2017
    Assignee: NeOnc Technologies Inc.
    Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
  • Patent number: 9624219
    Abstract: The present invention relates to a compound of Formula (I) having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasitic protozoal infections such as malaria, in particular infection by Plasmodium falciparum. (S)—N-(2-fluoropyridin-4-yl)-3-methyl-2-(5-methyl-2,4-dioxo-1,2-dihydropyrido[3,4-d]pyrimidin-3(4H)-yl)butanamide.
    Type: Grant
    Filed: April 19, 2016
    Date of Patent: April 18, 2017
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Jose-Miguel Coteron Lopez, Esther Pilar Fernandez Velando, Jorge Fernandez-Molina, Maria Luisa Leon-Diaz, David Matthew Wilson
  • Patent number: 9556188
    Abstract: The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
    Type: Grant
    Filed: November 25, 2015
    Date of Patent: January 31, 2017
    Assignee: BeiGene, Ltd.
    Inventors: Zhiwei Wang, Yunhang Guo
  • Patent number: 9504674
    Abstract: Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-dihydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.
    Type: Grant
    Filed: March 5, 2015
    Date of Patent: November 29, 2016
    Assignee: Emory University
    Inventor: Keqiang Ye
  • Patent number: 9388159
    Abstract: This invention provides for compounds of the Formula II: wherein A, B, Het, R1, R2 and R3 are as described herein. These compounds are androgen receptor modulators useful for the treatment of androgen receptor-associated conditions.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: July 12, 2016
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Michael E. Jung, Charles L. Sawyers, Samedy Ouk, Chris Tran, John Wongvipat
  • Patent number: 9284281
    Abstract: Disclosed are naphtho[2,3-f]quinoxaline compounds and pharmaceutical composition thereof. The compounds of the invention have been demonstrated as having analgesic effects and therefore may be applicable for use as a novel agent in relieving acute or chronic pain.
    Type: Grant
    Filed: September 16, 2014
    Date of Patent: March 15, 2016
    Assignee: NATIONAL CENTRAL UNIVERSITY
    Inventors: Wei-Hsin Sun, Shir-Ly Huang, Hsu-Shan Hunag
  • Patent number: 9050246
    Abstract: The present invention concerns an injectable composition comprising a filler or a botulinum toxin and an adrenergic receptor agonist, and its use for diminishing, decreasing or avoiding skin reactions due to injection, specially redness, ecchymosis, bruising, bleeding, erythema, oedema, necrosis, ulceration, swelling and/or inflammation.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: June 9, 2015
    Assignee: Galderma Research & Development
    Inventors: Isabelle Bertholon, Florence Brunel, Benjamin Herbage, Sylviane Villard
  • Publication number: 20150148391
    Abstract: The present invention relates to stabilized pharmaceutical formulations prepared from solutions comprising an antineoplastic compound having a cyclic or non-cyclic hydrazine, triazine, or tetrazine group, or a pharmaceutically acceptable salt thereof, and a stabilizer, wherein the stabilizer is an antioxidant and/or more susceptible to nucleophilic attack than the antineoplastic compound.
    Type: Application
    Filed: February 3, 2015
    Publication date: May 28, 2015
    Inventors: Mahmoud S. AlSwisi, Mahmoud A.A. Ghannam
  • Publication number: 20150148390
    Abstract: The present invention relates to glioblastoma inhibiting compounds, in particular gambogic acid amid and derivatives thereof for the treatment of glioblastoma. Moreover, methods for determining whether a treatment with the compounds of the invention is suitable for a patient are disclosed.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 28, 2015
    Applicant: Life & Brain GmbH
    Inventors: Björn Scheffler, Martin Glas, Matthias Simon, Sabine Gogolok, Daniel Trageser, Roman Reinartz, Anja Wieland
  • Publication number: 20150141418
    Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Applicant: PTC Therapeutics, Inc.
    Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
  • Publication number: 20150133366
    Abstract: C. difficile infection (CDI) is the most common cause of antibiotic-associated diarrhea. Unfortunately, antibiotic therapy remains as the standard treatment for this antibiotic-induced disease and relapses are common. Antibiotic treatment typically is given for 10 to 14 days for initial or second episode of CDI. For recurrent episodes, more prolonged courses are recommended. It is disclosed herein that lower dose or shorter course of the antimicrobial treatment is sufficient to treat the disease and prevent recurrent disease by enabling a good immunologic response to infection, and perhaps also by better preserving normal flora, thus protecting against relapses or reinfection.
    Type: Application
    Filed: November 12, 2014
    Publication date: May 14, 2015
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Richard L. Guerrant, Cirle Alcantara Warren, John Hudson Moore, II, Edward van Opstal
  • Patent number: 9029561
    Abstract: Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-dihydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: May 12, 2015
    Assignee: Emory University
    Inventor: Keqiang Ye
  • Publication number: 20150111907
    Abstract: The invention relates to methods of predicting the clinical outcome of brain cancer patients based on the LOH levels of the PTEN gene and on the expression levels or the polysomy/amplification levels of EGFR gene in a sample from said patients.
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Michael J. DONOVAN, Anna Colomer Valero, Nadina Erill Sagales, Isidre Ferrer Abinzanda, Susana Boluda Casas
  • Patent number: 9005670
    Abstract: The present invention provides methods for treating cancer comprising inhibiting the activity of p300/CBP histone acetyltransferase (HAT). Also provided are p300/CBP HAT inhibitors for treating a subject having cancer. In addition, the present invention includes biomarkers for p300/CBP HAT inhibition, which are used to i) monitor the effectiveness of cancer therapy, and ii) identify anti-cancer agents for use in combination therapy.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: April 14, 2015
    Assignee: The Johns Hopkins University
    Inventors: Rhoda Myra Alani, Philip A. Cole, Gai Yan, Erin M. Bowers
  • Patent number: 9006258
    Abstract: The present invention relates to a new use for compounds that inhibit phosphodiesterase 1 (PDE1), e.g., that inhibit PDE1-mediated suppression of the dopamine D1 receptor and/or progesterone signaling pathways, including, e.g., methods of treatment or prophylaxis for conditions which may be ameliorated by enhancing the progesterone signaling response, particularly female sexual dysfunction.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: April 14, 2015
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Allen A. Fienberg, Sharon Mates, Lawrence P. Wennogle
  • Patent number: 8993607
    Abstract: The invention provides compounds of formula I, II, and III as defined herein, as well as salts thereof. The compounds may have activity as anti-proliferative agents.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: March 31, 2015
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Joseph E. Rice
  • Patent number: 8980920
    Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Publication number: 20150064252
    Abstract: Disclosed are solid dispersions comprising a compound having the formula: wherein the compound is dispersed within a polymer matrix formed by a pharmaceutically acceptable polymer, and further wherein the compound is substantially amorphous. Also disclosed are pharmaceutical compositions comprising the compound and methods of use for the compound.
    Type: Application
    Filed: January 30, 2014
    Publication date: March 5, 2015
    Inventors: Eric Gorman, Erik Mogalian, Reza Oliyai, Dimitrios Stefanidis, Vahid Zia
  • Patent number: 8969372
    Abstract: Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents.
    Type: Grant
    Filed: November 15, 2004
    Date of Patent: March 3, 2015
    Assignee: Aptose Boisciences Inc.
    Inventors: Mario Huesca, Raed Al-Qawasmeh, Aiping H. Young, Yoon Lee
  • Publication number: 20150051257
    Abstract: Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted; or 9- or 10-membered bicyclic group, linked to —(O)x—(CH2)y— through one of its aromatic carbon atoms, consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5- or 6-membered non-aromatic heterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1-C3-alkyls; D represents a group selected from: phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted; thiophene unsubstituted or substituted; bicyclic group consisting of imidazolering fused with 5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2 heteroatoms independently selected from the group consisting of N, O and
    Type: Application
    Filed: March 20, 2013
    Publication date: February 19, 2015
    Applicant: ADAMED SP. ZO.O
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Tomasz Lysakowski, Maciej Pawlowski
  • Publication number: 20150038501
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Inventors: Leping LI, Min ZHONG
  • Patent number: 8946274
    Abstract: Methods of improving skin quality are disclosed. Generally, the methods include topically administering an IRM compound to a treatment area of skin for a period of time and in an amount effective for improving the quality of the skin. Suitable IRM compound compounds include agonists of one or more TLRs.
    Type: Grant
    Filed: September 10, 2012
    Date of Patent: February 3, 2015
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Richard L. Miller, James H. Lee, Mary L. Owens
  • Publication number: 20150030579
    Abstract: Hydroxytyrosol or olive juice containing hydroxytyrosol in combination with at least one of the compounds selected from the group consisting of: creatine, coenzyme Q10, resveratrol, caffeine, carnitine, B vitamins (B1, B2, B3, B5, B6, and/or B12) and ginseng (preferably: root) extract. can be used to maintain or increase mitochondrial biogenesis in cardiac muscle, skeletal muscles, and liver tissue.
    Type: Application
    Filed: August 1, 2014
    Publication date: January 29, 2015
    Applicant: DSM IP ASSETS B.V.
    Inventors: Ann FOWLER, Angelika FRIEDEL, Darko KNUTTI, Karin KURATLI, Daniel RAEDERSTORFF, Ying WANG-SCHMIDT, Karin WERTZ
  • Publication number: 20150005288
    Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: January 22, 2013
    Publication date: January 1, 2015
    Applicants: Bayer Pharma Aktiengesellschaft, Bayer Intellectual Property GmbH
    Inventors: Frank Süssmeier, Mario Lobell, Sylvia Grünewald, Michael Härter, Bernd Buchmann, Joachim Telser, Hannah Jörissen, Melanie Heroult, Antje Kahnert, Klemens Lustig, Niels Lindner
  • Publication number: 20140371235
    Abstract: A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: (a) a phenyl-substituted imidazole, or a pharmaceutically acceptable salt or ester thereof; or (b) a compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; R21 is an alkanediyl or a substituted alkanediyl; a is 0 or 1; c is 0 or 1; X is C or S; R22 is a moiety that includes at least one divalent amino radical; and R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing
    Type: Application
    Filed: October 10, 2012
    Publication date: December 18, 2014
    Applicant: University of Pittsburgh - Of the Commonweath System of Higher Education
    Inventors: Zhou Wang, Joel Byron Nelson, Minh Mindy Bao Nguyen, John S. Lazo, Paul A. Johnston, Peter Wipf
  • Publication number: 20140364471
    Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene for sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
    Type: Application
    Filed: August 8, 2014
    Publication date: December 11, 2014
    Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
  • Publication number: 20140364472
    Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
    Type: Application
    Filed: August 8, 2014
    Publication date: December 11, 2014
    Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
  • Publication number: 20140364470
    Abstract: The invention relates to a phosphate salt or a nitrate salt of 4-(R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl-3-fluoro-benzonitrile, especially in crystalline form, and specific forms of these salts, as well as related invention embodiments. The salts and salt forms allow for the prophylactic and/or therapeutic treatment of aldosterone synthase and/or aromatase mediated diseases or disorders.
    Type: Application
    Filed: January 15, 2013
    Publication date: December 11, 2014
    Applicant: Novartis AG
    Inventors: Paul Alan Sutton, Eric Loeser
  • Publication number: 20140357621
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Applicant: Novartis AG
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • Patent number: 8895599
    Abstract: The present invention provides pharmaceutical compositions containing benzene compound(s) represented by General Formula (1) below and, particularly, LPL-activating compositions for use in hyperlipidemia therapeutic and preventive agents, anti-obesity agents, and the like: wherein R1, R2, R3 and R4 are as defined in the specification.
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: November 25, 2014
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Irina Neagu, Michael Ohlmeyer, Vidyadhar M. Paradkar, Kurt W. Saionz, Koushi Iwata, Takashi Okamura, Tadao Shibutani
  • Patent number: 8895597
    Abstract: The additive effect of combined intracranial carmustine (“BCNU”) with intracranial temozolomide (“TMZ”), and particularly in combination with radiation (“XRT”), in the treatment of two rat intracranial glioma models, the 9L gliosarcoma and the F98 glioma, demonstrates that local delivery of both drugs, especially in combination with radiation, is far more effective than delivery of either drug alone or one systemically and one locally, either with or without radiation. The triple therapy showed a significant improvement in survival when compared to controls (p=0.0004), local BCNU (p=0.0043), oral TMZ (p=0.0026), local TMZ (p=0.0105), and the combinations of either BCNU and XRT (p=0.0378) or oral TMZ and local BCNU (p=0.0154).
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: November 25, 2014
    Inventors: Violette Renard Recinos, Betty Tyler, Sarah Brem Sunshine, Henry Brem
  • Publication number: 20140343045
    Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
    Type: Application
    Filed: May 23, 2014
    Publication date: November 20, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
  • Patent number: 8883826
    Abstract: The present invention relates to novel compounds of formula I wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: November 11, 2014
    Assignee: Addex Pharma SA
    Inventors: Anne-Sophie Bessis, Christelle Bolea, Beatrice Bonnet, Mark Epping-Jordan, Nicolas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
  • Patent number: 8865911
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: October 21, 2014
    Assignee: Astrazeneca AB
    Inventors: Gabor Csjernyik, Sofia Karlstrom, Annika Kers, Karin Kolmodin, Martin Nylof, Liselotte Ohberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Soderman, Britt-Marie Swahn, Stefan Von Berg
  • Publication number: 20140308243
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—Z—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: April 16, 2014
    Publication date: October 16, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yao-Ling Qiu, Hui Cao, Xiaowen Peng, Zhigang Chen, Yat Sun Or
  • Publication number: 20140309197
    Abstract: The present invention relates to stabilized pharmaceutical formulations prepared from solutions comprising an antineoplastic compound having a cyclic or non-cyclic hydrazine, triazine, or tetrazine group, or a pharmaceutically acceptable salt thereof, and a stabilizer, wherein the stabilizer is an antioxidant and/or more susceptible to nucleophilic attack than the antineoplastic compound.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 16, 2014
    Inventors: Mahmoud S. AlSwisi, Mahmoud A.A. Ghannam
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8853212
    Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: October 7, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
  • Publication number: 20140288059
    Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.
    Type: Application
    Filed: April 25, 2014
    Publication date: September 25, 2014
    Applicant: THE PENN STATE RESEARCH FOUNDATION
    Inventors: Gong Chen, Yanming Wang, Pingxin Li, Jing Hu, Shu Wang, Yuji Wang
  • Publication number: 20140286931
    Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventor: Chengzhi Zhang
  • Publication number: 20140288115
    Abstract: It is discovered that noscapine is effective in treating temozolomide (TMZ)-resistant brain cancer. Provided are compositions and methods of treating brain cancer patients, in particular those that are TMZ-resistant. The patients are treated by administration of a therapeutically effective amount of noscapine or an analog thereof. In certain aspects, TMZ is also administered to the patients. Examples of brain cancers include glioma such as glioblastoma multiforme.
    Type: Application
    Filed: June 6, 2014
    Publication date: September 25, 2014
    Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Thomas C. Chen, Florence M. Hofman, Stan G. Louie, Axel H. Schonthal, Nicos A. Petasis
  • Publication number: 20140275195
    Abstract: The present invention relates to stabilized pharmaceutical formulations prepared from solutions comprising an antineoplastic compound having a cyclic or non-cyclic hydrazine, triazine, or tetrazine group, or a pharmaceutically acceptable salt thereof, and a stabilizer, wherein the stabilizer is an antioxidant and/or more susceptible to nucleophilic attack than the antineoplastic compound.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 18, 2014
    Inventors: Mahmoud S. AlSwisi, Mahmoud A.A. Ghannam
  • Publication number: 20140256693
    Abstract: The present invention mainly aims to provide a drug for the prophylaxis or treatment of androgen-independent prostate cancer, which is highly useful as a pharmaceutical agent. The present invention provides a drug for the prophylaxis or treatment of androgen-independent prostate cancer, containing a steroid C17,20 lyase inhibitor, particularly, a compound represented by the formula (I): wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof or a prodrug thereof.
    Type: Application
    Filed: February 5, 2014
    Publication date: September 11, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masuo Yamaoka, Takahito Hara
  • Patent number: 8828429
    Abstract: The present invention relates to a controlled release capsule preparation for oral administration, which contains (i) a granule containing a physiologically active substance which is a compound represented by the formula: wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof, and a hydrophilic polymer, and coated with an enteric coating agent and the like, and (ii) a fluidizer. According to the present invention, a controlled release composition for oral administration of an imidazole derivative, which has steroid C17,20-lyase inhibiting activity and which has remarkably improved sustainability of the blood concentration, is provided.
    Type: Grant
    Filed: March 3, 2006
    Date of Patent: September 9, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Hajime Ishida, Yukihiro Nomura