Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
  • Patent number: 10526294
    Abstract: The present disclosure relates generally to derivatives of pyrrolobenzodiazepines and antibody-drug conjugates thereof and to methods of using these conjugates as therapeutics and/or diagnostics.
    Type: Grant
    Filed: June 22, 2017
    Date of Patent: January 7, 2020
    Assignee: Mersana Therapeutics, Inc.
    Inventors: Joshua D. Thomas, Mao Yin, Aleksandr V. Yurkovetskiy, Patrick R. Conlon, Ahmed Hilmy, Eugene W. Kelleher, Timothy B. Lowinger, Cheri A. Stevenson, Shuyi Tang
  • Patent number: 10512643
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: December 24, 2019
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10493045
    Abstract: A method for treating alcohol dependence or alcohol abuse in a subject comprising administering to the subject a composition comprising an effective amount of memantine, wherein the effective amount of memantine is 2-4.7 mg/day. Low dose of memantine having anti-inflammatory and neurotrophic effect is able to reduce alcohol use.
    Type: Grant
    Filed: December 8, 2017
    Date of Patent: December 3, 2019
    Inventor: Ru-Band Lu
  • Patent number: 10463638
    Abstract: Technologies are described for a formulation and production of a formulation. The methods may comprise depositing a non-steroidal anti-inflammatory drug (NSAID) compound into a chamber. The methods may comprise depositing a N-methyl-D-aspartate (NMDA) receptor antagonist into the chamber. The methods may comprise respectively depositing a muscle relaxant, a local anesthetic into the chamber, depositing an anticonvulsant into the chamber, depositing an antidepressant into the chamber, and depositing a calcium channel blocking agent into the chamber. The methods may comprise milling the NSAID compound, the NMDA receptor antagonist, the muscle relaxant, the local anesthetic, the anticonvulsant, the antidepressant, and the calcium channel blocking agent into a powder. The methods may comprise adding a solvent with the powder and mixing the solvent with the powder to form a solution. The methods may comprise adding a base cream to the solution and mixing the base cream and the solution to form the formulation.
    Type: Grant
    Filed: April 12, 2018
    Date of Patent: November 5, 2019
    Assignee: SYNERGISTIC THERAPEUTICS, LLC
    Inventors: Anthony H. Salce, Jr., William F. Greenwood, Shivsankar Misir
  • Patent number: 10450319
    Abstract: The present invention relates to a salt form of a benzodiazepine derivative, in particular crystalline solid state forms, to pharmaceutical compositions comprising the same and to its use in therapy.
    Type: Grant
    Filed: April 18, 2018
    Date of Patent: October 22, 2019
    Assignee: GlaxoSmithKline Intellectual Property (No.2) Limited
    Inventors: Gossett Augustus Campbell, Asa Elisabeth Gladwin
  • Patent number: 10442819
    Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: October 15, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Stephane L. Bogen, Matthew L. Childers, Francesc Xavier Fradera Llinas, J. Michael Ellis, Sara Esposite, Qingmei Hong, Chunhui Huang, Alexander J. Kim, John W. Lampe, Michelle R. Machacek, Daniel R. McMasters, Ryan D. Otte, Dann L. Parker, Jr., Michael Reutershan, Nunzio Sciammetta, Pengcheng P. Shao, David L. Sloman, Feroze Ujjainwalla, Catherine White, Zhicai Wu, Yang Yu, Kake Zhao, Craig Gibeau, Tesfaye Biftu, Purakkattle Biju, Lei Chen, Joshua Close, Peter H. Fuller, Xianhai Huang, Min K. Park, Valdimir Simov, David J. Witter, Hongjun Zhang
  • Patent number: 10421763
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
    Type: Grant
    Filed: August 14, 2017
    Date of Patent: September 24, 2019
    Assignee: Purdue Pharma L.P.
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Patent number: 10399972
    Abstract: The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
    Type: Grant
    Filed: October 25, 2016
    Date of Patent: September 3, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David J. Witter, Tesfaye Biftu, Purakkattle Biju, Stephane L. Bogen, Qingmei Hong, Chunhui Huang, Xianhai Huang, Bing Li, Min K. Park, David L. Sloman
  • Patent number: 10369143
    Abstract: Provided herein is a method of treating a central nervous system disorder in a patient in need thereof, wherein the central nervous system disorder is selected from schizophrenia, Alzheimer's disease, Huntington's disease, Parkinson's disease, and Lewy Body dementia. The method comprises orally administering an initial dose of between 75 mg and 300 mg xanomeline and an initial dose of between 20 mg and 200 mg trospium chloride to the patient during a 24-hour period. Provided that the patient tolerates said administration, an increased dose of trospium chloride and an increased dose of xanomeline are orally administering to the patient, wherein the increased dose of trospium chloride is greater than the initial dose of the trospium chloride, and wherein the increased dose of xanomeline is greater than the initial dose of the xanomeline.
    Type: Grant
    Filed: February 7, 2019
    Date of Patent: August 6, 2019
    Assignee: PureTech Health LLC
    Inventors: Eric Elenko, Philip E. Murray, III, Andrew C. Miller
  • Patent number: 10328076
    Abstract: The present invention relates to a stable pharmaceutical formulation of solid dosage forms for oral administration comprising a therapeutically effective amount of a triazole antifungal agent or pharmaceutical acceptable salt thereof, in particular Voriconazole and an effective amount of a solubility enhancing agent. It also relates to a process for the preparation thereof.
    Type: Grant
    Filed: June 9, 2015
    Date of Patent: June 25, 2019
    Assignee: PHARMATHEN S.A.
    Inventor: Evangelos Karavas
  • Patent number: 10278975
    Abstract: Compounds having the formula I wherein R1, X1, X2, X3 and X4 as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
    Type: Grant
    Filed: September 14, 2017
    Date of Patent: May 7, 2019
    Assignee: GENENTECH, INC.
    Inventors: Aleksandr Kolesnikov, Steven Do
  • Patent number: 10265311
    Abstract: Methods for the treatment of CNS disorders using combinations of muscarinic activators and inhibitors, and medicaments comprising muscarinic activators and inhibitors.
    Type: Grant
    Filed: December 14, 2016
    Date of Patent: April 23, 2019
    Assignee: PureTech Health LLC
    Inventors: Eric Elenko, Andrew C. Miller, Philip E. Murray, III
  • Patent number: 10259815
    Abstract: Described herein are ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as ?3 or ?2 or ?2/?3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.
    Type: Grant
    Filed: March 18, 2016
    Date of Patent: April 16, 2019
    Assignee: UWM Research Foundation, Inc.
    Inventors: James Cook, Michael Ming-Jin Poe, Kashi Reddy Methuku, Guanguan Li
  • Patent number: 10251879
    Abstract: Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.
    Type: Grant
    Filed: March 22, 2018
    Date of Patent: April 9, 2019
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 10238620
    Abstract: Methods of preventing early awakenings, and improving sleep efficiency in hours 7 and 8 of a period of sleep, by administration of low doses of doxepin (e.g., 1-6 mg).
    Type: Grant
    Filed: January 8, 2018
    Date of Patent: March 26, 2019
    Assignees: Pernix Sleep, Inc., ProCom One, Inc.
    Inventors: Roberta L. Rogowski, Susan E. Dubé, Philip Jochelson, Neil B. Kavey
  • Patent number: 10238651
    Abstract: The present invention relates to pharmaceutical compositions comprising a compound of Formula (I) that are useful for the intramuscular delivery of antipsychotic drugs using rapid injection rates.
    Type: Grant
    Filed: August 29, 2018
    Date of Patent: March 26, 2019
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Magali B. Hickey, Jennifer Vandiver
  • Patent number: 10239888
    Abstract: The present application provides bifunctional compounds of Formula I or II: or an enantiomer, diastereomer, or stereoisomer, or a pharmaceutically acceptable salt thereof, which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds of Formula (I) or (II) that link a mutant cereblon-binding moiety to a ligand that is capable of binding to a targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof. The present application also relates to polynucleotides or polypeptides of a mutant cereblon and methods of use thereof.
    Type: Grant
    Filed: July 25, 2018
    Date of Patent: March 26, 2019
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: James Bradner, Mette Ishoey, Dennis Buckley, Joshiawa Paulk, Marc Andrew Cohen, Rhamy Zeid
  • Patent number: 10239834
    Abstract: The present disclosure describes a method to treat conditions, including bacterial infections and cancer, using a photosensitive compound that, upon exposure to white light, can be activated. The photosensitive compound can also interact synergistically with antibiotics used concomitantly to kill drug-resistant bacteria. The photosensitive compounds can also be used to inhibit the proliferation of cancer cells.
    Type: Grant
    Filed: October 31, 2017
    Date of Patent: March 26, 2019
    Assignee: NEW MEXICO TECH UNIVERSITY RESEARCH PARK CORPORATION
    Inventors: Snezna Rogelj, Liliya Frolova, Alexander Kornienko, Leslie D. Edwards, Cody Champion, Kailee Zingler, Danielle Nicole Turner
  • Patent number: 10208042
    Abstract: The present invention relates to a compound as represented by formula (I) or a pharmaceutically acceptable salt and stereoisomer thereof, wherein R1, R2, X, Y, P, W, and Ar are as defined in the description. The compound of formula (I) of the present invention can be used in the preparation of a drug for treating cancers mediated by abnormality of multi-kinases. Also provided is a crystal form I of a compound 4-(5-(2-chlorophenyl)-3-methyl-2,10-dihydropyrazolo[4,3-b]pyrido[4,3-e] [1,4]diazepin-8-yl)morpholine, wherein in an X-ray powder diffraction pattern of crystal form I, there are characteristic peaks at 7.4±0.2°, 17.9±0.2°, 18.9±0.2°, 19.4±0.2°, 21.5±0.2°, and 23.7±0.2°.
    Type: Grant
    Filed: October 10, 2018
    Date of Patent: February 19, 2019
    Assignee: Nanjing TransThera Biosciences Co. Ltd.
    Inventor: Frank Wu
  • Patent number: 10188657
    Abstract: Provided are articles of manufacture, compositions and methods for prophylaxis and/or therapy for disorders involving dizziness and/or vertigo. The articles of manufacture and compositions contain lamotrigen and/or bupropion. The compositions include pharmaceutical compositions which are intended to alleviate dizziness and/or vertigo. In certain aspects the disclosure includes articles of manufacture and kits which include printed material which provides an indication that the articles or compositions are intended to be used for prophylaxis and/or therapy of Meniere's Disease or a symptom thereof.
    Type: Grant
    Filed: November 9, 2017
    Date of Patent: January 29, 2019
    Inventor: Lixin Zhang
  • Patent number: 10143695
    Abstract: The present disclosure relates generally to derivatives of pyrrolobenzodiazepines and antibody-drug conjugates thereof and to methods of using these conjugates as therapeutics and/or diagnostics.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: December 4, 2018
    Assignee: Mersana Therapeutics, Inc.
    Inventors: Mao Yin, Joshua D. Thomas, Aleksandr V. Yurkovetskiy, Patrick R. Conlon, Bingfan Du, Eugene W. Kelleher, Timothy B. Lowinger, Shuyi Tang
  • Patent number: 10143676
    Abstract: The invention relates to use of the trans-(E) isomer or isomeric mixtures containing specified ratios of the trans-(E) and cis-(Z) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disorders.
    Type: Grant
    Filed: November 21, 2016
    Date of Patent: December 4, 2018
    Assignees: Pernix Sleep, Inc., ProCom One, Inc.
    Inventors: Susan E. Dubé, Neil B. Kavey
  • Patent number: 10124009
    Abstract: The present invention relate to bromodomain inhibitor compounds, pharmaceutical compositions comprising the bromodomain inhibitor compounds and methods of treating a disorder responsive to fee modulation of a BET family polypeptide using the compounds and pharmaceutical compositions described.
    Type: Grant
    Filed: October 27, 2015
    Date of Patent: November 13, 2018
    Assignee: Tensha Therapeutics, Inc.
    Inventors: Steven B. Landau, Michael Kagey
  • Patent number: 10098892
    Abstract: The present invention is directed to a pharmaceutical composition comprising the compound suvorexant, or a pharmaceutically acceptable salt thereof, a concentration-enhancing polymer, and optionally a pharmaceutically acceptable surfactant. The concentration-enhancing polymer is a polymer that forms an amorphous dispersion with suvorexant, that is insoluble or almost completely insoluble in water by (a) dissolving the suvorexant or (b) interacting with the suvorexant in such a way that the suvorexant does not form crystals or crystalline domains in the polymer. A concentration-enhancing polymer is water soluble or readily disperse in water, so that when the polymer is placed in water or an aqueous environment (e.g. fluids in the gastrointestinal (GI) tract or simulated GI fluids), the solubility and/or bioavailability of suvorexant is increased over the solubility or bioavailability in the absence of the polymer.
    Type: Grant
    Filed: May 29, 2013
    Date of Patent: October 16, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul A. Harmon, Narayan Variankaval
  • Patent number: 10085980
    Abstract: The present invention relates to pharmaceutical compositions comprising a compound of Formula (I) that are useful for the intramuscular delivery of antipsychotic drugs using rapid injection rates.
    Type: Grant
    Filed: November 11, 2016
    Date of Patent: October 2, 2018
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Magali B. Hickey, Jennifer Vandiver
  • Patent number: 10071129
    Abstract: Disclosed herein are methods and compositions useful for inhibiting interaction between a bromodomain protein and an immunoglobulin (Ig) regulatory element. The methods and compositions are particularly useful for downregulating expression of an oncogene translocated with an Ig locus, as well as for treating a cancer (e.g., hematological malignancy) characterized by increased expression of an oncogene which is translocated with an Ig locus. Also disclosed herein are methods and assays for identifying agents that interfere with binding of bromodomain proteins to Ig regulatory elements, as well as methods and assays for identifying inhibitors of bromodomain.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: September 11, 2018
    Assignee: WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Richard A. Young, Peter B. Rahl, James Bradner
  • Patent number: 10071163
    Abstract: The invention provides a conjugate comprising (i) a nucleic acid which is complementary to a target nucleic acid sequence and which expression prevents or reduces expression of the target nucleic acid and (ii) a selectivity agent which is capable of binding with high affinity to a neurotransmitter transporter. The conjugates of the present invention are useful for the delivery of the nucleic acid to a cell of interests and thus, for the treatment of diseases which require a down-regulation of the protein encoded by the target nucleic acid as well as for the delivery of imaging agents to the cells for diagnostic purposes.
    Type: Grant
    Filed: November 23, 2015
    Date of Patent: September 11, 2018
    Assignee: nLife Therapeutics, S.L.
    Inventors: Andrés Pablo Montefeltro, Gabriel Alvarado Urbina, Analia Bortolozzi Biassoni, Francesc Artigas Pérez, Miquel Vila Bover, Maria del Carmen Carmona Orozco
  • Patent number: 10064859
    Abstract: Processes for providing depot injections of recrystallized aripiprazole lauroxil in which particles of the aripiprazole lauroxil have a surface area of about 0.50 to about 3.3 m2/g; and crystals of aripiprazole lauroxil produced by such processes.
    Type: Grant
    Filed: August 24, 2015
    Date of Patent: September 4, 2018
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Wilfredo Morales, Jr., Tarek A. Zeidan, Renato A. Chiarella, Steven G. Wright, Jason M. Perry
  • Patent number: 10052319
    Abstract: The present invention relates to a medicament comprising lurasidone or a pharmaceutically acceptable acid addition salt thereof for treating pervasive developmental disorders and a method of the treatment thereof.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: August 21, 2018
    Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventor: Tsuyoshi Tsujimura
  • Patent number: 10047096
    Abstract: The present application relates to novel (3-hydroxyphenyl)amino-substituted pyrido[2,3-b][1,5]benzodiazepin-5-one derivatives, to processes for preparation thereof, to the use thereof alone or in combination for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially of angiogenic disorders and hyperproliferative disorders in which neovascularization plays a role, for example ophthalmological disorders and cancers and tumours. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Grant
    Filed: November 23, 2015
    Date of Patent: August 14, 2018
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Andreas Schall, Jürgen Klar, Mario Lobell, Hartmut Schirok, Joachim Telser, Steffen Müller, Dirk Brohm, Hans Briem, Hannah Jörißen, Joerg Keldenich, Michael Böttger, Georges Von Degenfeld, Thomas Schlange, Ulf Bömer, Niels Lindner, Hanna Eilken, Dmitrij Hristodorov, Pierre Wasnaire, Kersten Matthias Gericke, Lars Bärfacker
  • Patent number: 10039769
    Abstract: This invention relates to novel substituted triazolobenzodiazepines of the Formula I: wherein each of the variables are defined herein and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering I-BET762.
    Type: Grant
    Filed: May 31, 2017
    Date of Patent: August 7, 2018
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Scott L. Harbeson
  • Patent number: 10039760
    Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: December 21, 2016
    Date of Patent: August 7, 2018
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K. R. Rao, Greg Thomas
  • Patent number: 10035805
    Abstract: The present invention relates to new tricyclic triazolic compounds having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
    Type: Grant
    Filed: July 2, 2015
    Date of Patent: July 31, 2018
    Assignee: ESTEVE PHARMACEUTECALS, S.A.
    Inventors: Félix Cuevas-Cordobés, Miguel Angel Pericás-Brondo
  • Patent number: 10004699
    Abstract: Effective methods and compositions to deter abuse of pharmaceutical products (e.g., orally administered pharmaceutical products) including but not limited to immediate release, sustained or extended release and delayed release formulations for drugs subject to abuse.
    Type: Grant
    Filed: June 9, 2015
    Date of Patent: June 26, 2018
    Assignee: Acura Pharmaceuticals, Inc.
    Inventor: Ronald L. Leech, Jr.
  • Patent number: 10004807
    Abstract: The present invention relates to an injectable, pharmaceutical composition comprising a C1-6 alkyl ester of a C10-20 fatty acid. In an embodiment, the fatty acid is ethyl oleate, isopropyl oleate, ethyl myristate, or isopropyl myristate. These compositions are useful for the delivery of anti-psychotic drugs.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 26, 2018
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Jason M. Perry, Magali B. Hickey, Julius F. Remenar, Jennifer Vandiver
  • Patent number: 9993570
    Abstract: Disclosed are PARP-1 inhibitors, which can be 18F-labeled for use as tracers in positron emission tomographic (PET) imaging. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.04,13]trideca-2,4(13),5,7-tetraen-9-one (12) had the highest inhibition potency for PARP-1 (IC50=6.3 nM). Synthesis of [18F]-12 is disclosed under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET imaging using [18F]-12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [18F]-12 in a tumor. Binding, can be blocked by olaparib. The compounds have utility for tumor imaging.
    Type: Grant
    Filed: July 5, 2016
    Date of Patent: June 12, 2018
    Assignee: WASHINGTON UNIVERSITY
    Inventors: Robert Mach, Wenhua Chu, Dong Zhou, Loren Michel, Delphine Chen
  • Patent number: 9975901
    Abstract: The present invention relates to a salt form of a benzodiazepine derivative, in particular crystalline solid state forms, to pharmaceutical compositions comprising the same and to its use in therapy.
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: May 22, 2018
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Gossett Augustus Campbell, Asa Elisabeth Gladwin
  • Patent number: 9975899
    Abstract: The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines substituted with heterocyclic derivatives of Formula (I) wherein R1, R2, R3, R4 and Het have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: May 22, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Lieven Meerpoel, Louis Jules Roger Marie Maes, Kelly de Wit, Koen Jan Ludovicus Augustyns
  • Patent number: 9968620
    Abstract: A method of treating lymphoma in a mammal comprises the step of: administering to a patient a pharmaceutical acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1) wherein R1 is alkyl having a carbon number of 1-4, R2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; —NR5—(CH2)m—R6 wherein R5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R6 is phenyl or pyridyl optionally substituted by a halogen atom; or —NR7—CO—(CH2)q—R8 wherein R is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R8 is phenyl or pyridyl optionally substituted by a halogen atom, and R4 is —(CH2)a—CO—NH—R9 wherein a is an integer of 1-4, and R9 is alkyl having a carbon number of 1-4; hydroxya
    Type: Grant
    Filed: August 19, 2015
    Date of Patent: May 15, 2018
    Assignee: ONCOETHIX GMBH
    Inventor: Francesco Bertoni
  • Patent number: 9969700
    Abstract: The present invention relates to a diazepine derivative represented by the following general formula (I) (in the formula, R1 and R2 represent hydrogen atom and the like, or R1 and R2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, R3 and R4 represent hydrogen atom and the like, R5 represents hydrogen atom and the like, R6 and R7 represent hydrogen atom and the like, X represents C, CH or N, Y represents N, NH or C(?O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(?O), Z represents oxygen atom or sulfur atom, A represents benzene ring and the like, B represents NHC(?O) and the like, D represents an atomic bond and the like, E represents an atomic bond and the like, G represents benzene which may be substituted and the like, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a P2X4 receptor antagonist.
    Type: Grant
    Filed: June 8, 2016
    Date of Patent: May 15, 2018
    Assignee: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Masatoshi Ushioda, Kunio Kobayashi, Daisuke Saito, Shogo Sakuma, Toshiyasu Imai, Kazuhide Inoue
  • Patent number: 9956228
    Abstract: A method of treating acute myeloid leukemia, acute lymphoblastic leukemia, high risk myelodysplastic syndrome, and/or HR-MDS/AML in a mammal by administering a solid dispersion comprising an amorphous thienotriazolodiazepine compound of the Formula (1) wherein R1 is alkyl having a carbon number of 1-4, R2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; —NR5-(CH2)m R6 wherein R5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R6 is phenyl or pyridyl optionally substituted by a halogen atom.
    Type: Grant
    Filed: May 1, 2015
    Date of Patent: May 1, 2018
    Assignee: OncoEthix GMBH
    Inventors: Kay Noel, Maria E. Riveiro
  • Patent number: 9938528
    Abstract: The present invention provides methods and pharmaceutical compositions for treating human immunodeficiency virus type 1 (HIV-1) infections. In particular, the present invention relates to a method for treating HIV-1 infection in a subject in need thereof comprising administering the subject with a therapeutically effective amount of an inhibitor of SGT1 activity or expression.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: April 10, 2018
    Assignees: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), UNIVERSITE PARIS-SUD, INSTITUT GUSTAVE ROUSSY, UNIVERSITE PARIS DECARTES, UNIVERSITE PIERRE ET MARIE CURIE, INSTITUT PASTEUR, INSTITUTO NAZIONALE PER LE MALATTIE INFETTIE IRCCS LAZZARO SPALLANZANI, ASSISTANCE PUBLIQUE HOPITAUX DE PARIS (APHP)
    Inventors: Guido Kroemer, Jean-Luc Perfettini, Marie-Lise Gougeon, Awatef Allouch, Mauro Piacentini
  • Patent number: 9926332
    Abstract: Compounds of formula (I) having a selective dual action on the central GABAergic system, and a process for their preparation and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 20, 2015
    Date of Patent: March 27, 2018
    Assignee: Egis Gyogyszergyar Zrt.
    Inventors: Agnes Kenez, Ferenc Bertha, Jozsef Barkoczy, Ferenc Antoni, Istvan Gacsalyi, Balazs Mihalik, Gabor Gigler, Krisztina Moricz, Gabor Nemeth, Agnes Angyalne Pataki, Gabor Laszlo Kapus, Adrienn Palvolgyi, Istvan Ling, Janos Petho, Gyula Simig, Balazs Volk, Lax Gyorgyi Kovanyine, Andras Dancso
  • Patent number: 9926276
    Abstract: The present invention belongs to the field of EP4 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP4 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP4 receptor as well as to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: March 27, 2018
    Assignee: DRACONIS PHARMA, S.L.
    Inventors: Marina Virgili Bernado, Elena Carceller Gonzalez, Jordi Salas Solana
  • Patent number: 9907803
    Abstract: The present invention provides a method of using arylpiperazine derivatives for treating attention deficit hyperactivity disorder (ADHD). The method comprises a step of administering to a patient in need thereof an effective amount of a compound of Formula 1, which is an arylpiperazine derivative.
    Type: Grant
    Filed: October 4, 2016
    Date of Patent: March 6, 2018
    Assignee: REVIVA PHARMACEUTICALS, INC.
    Inventor: Laxminarayan Bhat
  • Patent number: 9889207
    Abstract: A compound which is either A: or B: and salts and solvates thereof, as well as their conjugates with a cell-binding agent.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: February 13, 2018
    Assignee: MEDIMMUNE LIMITED
    Inventor: Philip Wilson Howard
  • Patent number: 9867819
    Abstract: This disclosure relates to methods administering various compounds in conjunction with dextromethorphan to a human being. Dosage forms, drug delivery systems, and methods related to dextromethorphan or dextrorphan and bupropion, hydroxybupropion, erythrohydroxybupropion, threohydroxybupropion, or a metabolite or prodrug of any of these compounds are also disclosed.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: January 16, 2018
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Patent number: 9861607
    Abstract: Methods of preventing early awakenings, and improving sleep efficiency in hours 7 and 8 of a period of sleep, by administration of low doses of doxepin (e.g., 1-6 mg).
    Type: Grant
    Filed: November 7, 2016
    Date of Patent: January 9, 2018
    Assignees: Procom One, Inc., Pernix Sleep, Inc.
    Inventors: Roberta L. Rogowski, Susan E. Dubé, Philip Jochelson, Neil B. Kavey
  • Patent number: 9820992
    Abstract: A method of treating non-small cell lung cancer in a mammal by administering to a patient a pharmaceutically acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1) wherein R1 is alkyl having a carbon number of 1-4, R2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; —NR5—(CH2)m—R6 wherein R5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R6 is phenyl or pyridyl optionally substituted by a halogen atom; or —NR7—CO—(CH2)n—R8 wherein R7 is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R8 is phenyl or pyridyl optionally substituted by a halogen atom, and R4 is —(CH2)a—CO—NH—R9 wherein a is an integer of 1-4, and R9 is alkyl having a carbon number of 1-4; hydroxy
    Type: Grant
    Filed: November 26, 2014
    Date of Patent: November 21, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Maria E. Riveiro, Eric Raymond
  • Patent number: 9815827
    Abstract: The present invention provides a novel method for treatment of schizophrenia which can improve wide-ranging symptoms of schizophrenia, especially positive symptoms and negative symptoms without being accompanied by extrapyramidal symptoms, which comprises orally administering as an active compound (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboxyimide or a pharmaceutically acceptable salt thereof (e.g., hydrochloride) at a daily dose of 5 mg to 120 mg once a day to a patient with schizophrenia, and a therapeutic agent to be used in said method.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: November 14, 2017
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Mitsutaka Nakamura, Masaaki Ogasa, Shunsuke Sami