Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
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Patent number: 10688047Abstract: Physically and chemically stable oral liquid formulations of Givinostat (Diethyl-[6-(4-hydroxycarbamoyl-phenylcarbamoyloxymethyl)-naphthalen-2-yl-methyl]-ammonium chloride) are disclosed, together with methods for the preparation thereof. Such oral formulations are in the form of aqueous suspensions and contain Givinostat and/or pharmaceutically acceptable salts and/or derivatives thereof, at least a wetting agent and/or at least a density-imparting agent. Such formulations are suitable for oral administration for systemic therapeutic action.Type: GrantFiled: October 28, 2016Date of Patent: June 23, 2020Assignee: ITALFARMACO SPAInventors: Giuseppe Colombo, Roberta Artico, Paolo Mascagni, Maria Valmen Monzani, Silvia Puccianti
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Patent number: 10676484Abstract: The invention provides compositions, methods, and kits for the treatment of acute myeloid leukemia in a subject.Type: GrantFiled: October 17, 2017Date of Patent: June 9, 2020Assignees: Dana-Farber Cancer Institute, Inc., Cold Spring Harbor InstituteInventors: James Elliott Bradner, Johannes Zuber, Junwei Shi, Christopher R. Vakoc, Scott W. Lowe, Constantine S. Mitsiades
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Patent number: 10675258Abstract: Provided herein are pharmaceutical compositions and formulations comprising mixed salts of gamma-hydroxybutyrate (GHB). Also provided herein are methods of making the pharmaceutical compositions and formulations, and methods of their use for the treatment of sleep disorders such as apnea, sleep time disturbances, narcolepsy, cataplexy, sleep paralysis, hypnagogic hallucination, sleep arousal, insomnia, and nocturnal myoclonus.Type: GrantFiled: December 21, 2018Date of Patent: June 9, 2020Assignee: Jazz Pharmaceuticals Ireland LimitedInventors: Clark P. Allphin, Michael DesJardin
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Patent number: 10668030Abstract: The present invention relates to methods of treatment of a disease or pathology of the central nervous system, an eating disorder, or substance use disorder, drug dependence/abuse and withdrawal therefrom comprising administering at least one N-phenylalkyl amphetamine derivative and pharmaceutical compositions comprising at least one N-phenylalkyl amphetamine derivative to an individual in need thereof.Type: GrantFiled: April 21, 2017Date of Patent: June 2, 2020Assignee: University of Kentucky Research FoundationInventors: Linda P. Dwoskin, Peter Anthony Crooks, Guangrong Zheng, Justin R. Nickell, Zheng Cao, Na-Ra Lee
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Patent number: 10646443Abstract: The disclosure is directed to methods of treating schizophrenia or bipolar disorder by subcutaneously administering a sustained-release dosage form of olanzapine, or a pharmaceutically acceptable salt thereof. Methods of subcutaneously administering olanzapine, or a pharmaceutically acceptable salt thereof, are also described.Type: GrantFiled: March 20, 2018Date of Patent: May 12, 2020Assignee: Teva Pharmaceuticals International GmbHInventors: Carine Claassen-Punt, Mark Alan Smith, Ling Chen, Ari Andrew Gershon
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Patent number: 10640507Abstract: The invention relates to pyrrolobenzodiazepines compounds (PBDs) and to pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular, to treat bacterial infections.Type: GrantFiled: December 9, 2016Date of Patent: May 5, 2020Assignees: King's College London, Secretary of State for Health and Social CareInventors: Khondaker Mirazur Rahman, John Mark Sutton, Pietro Picconi
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Patent number: 10526294Abstract: 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: GrantFiled: June 22, 2017Date of Patent: January 7, 2020Assignee: 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
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Patent number: 10512643Abstract: 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: GrantFiled: November 22, 2017Date of Patent: December 24, 2019Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 10493045Abstract: 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: GrantFiled: December 8, 2017Date of Patent: December 3, 2019Inventor: Ru-Band Lu
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Patent number: 10463638Abstract: 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: GrantFiled: April 12, 2018Date of Patent: November 5, 2019Assignee: SYNERGISTIC THERAPEUTICS, LLCInventors: Anthony H. Salce, Jr., William F. Greenwood, Shivsankar Misir
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Patent number: 10450319Abstract: 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: GrantFiled: April 18, 2018Date of Patent: October 22, 2019Assignee: GlaxoSmithKline Intellectual Property (No.2) LimitedInventors: Gossett Augustus Campbell, Asa Elisabeth Gladwin
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Patent number: 10442819Abstract: 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: GrantFiled: December 1, 2015Date of Patent: October 15, 2019Assignee: 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
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Patent number: 10421763Abstract: 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: GrantFiled: August 14, 2017Date of Patent: September 24, 2019Assignee: Purdue Pharma L.P.Inventors: Jay Jie-Qiang Wu, Ling Wang
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Patent number: 10399972Abstract: 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: GrantFiled: October 25, 2016Date of Patent: September 3, 2019Assignee: 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
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Patent number: 10369143Abstract: 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: GrantFiled: February 7, 2019Date of Patent: August 6, 2019Assignee: PureTech Health LLCInventors: Eric Elenko, Philip E. Murray, III, Andrew C. Miller
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Pharmaceutical composition comprising a triazole antifungal agent and method for preparation thereof
Patent number: 10328076Abstract: 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: GrantFiled: June 9, 2015Date of Patent: June 25, 2019Assignee: PHARMATHEN S.A.Inventor: Evangelos Karavas -
Patent number: 10278975Abstract: 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: GrantFiled: September 14, 2017Date of Patent: May 7, 2019Assignee: GENENTECH, INC.Inventors: Aleksandr Kolesnikov, Steven Do
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Patent number: 10265311Abstract: Methods for the treatment of CNS disorders using combinations of muscarinic activators and inhibitors, and medicaments comprising muscarinic activators and inhibitors.Type: GrantFiled: December 14, 2016Date of Patent: April 23, 2019Assignee: PureTech Health LLCInventors: Eric Elenko, Andrew C. Miller, Philip E. Murray, III
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Patent number: 10259815Abstract: 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: GrantFiled: March 18, 2016Date of Patent: April 16, 2019Assignee: UWM Research Foundation, Inc.Inventors: James Cook, Michael Ming-Jin Poe, Kashi Reddy Methuku, Guanguan Li
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Patent number: 10251879Abstract: 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: GrantFiled: March 22, 2018Date of Patent: April 9, 2019Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 10238651Abstract: 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: GrantFiled: August 29, 2018Date of Patent: March 26, 2019Assignee: ALKERMES PHARMA IRELAND LIMITEDInventors: Magali B. Hickey, Jennifer Vandiver
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Patent number: 10239834Abstract: 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: GrantFiled: October 31, 2017Date of Patent: March 26, 2019Assignee: NEW MEXICO TECH UNIVERSITY RESEARCH PARK CORPORATIONInventors: Snezna Rogelj, Liliya Frolova, Alexander Kornienko, Leslie D. Edwards, Cody Champion, Kailee Zingler, Danielle Nicole Turner
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Patent number: 10238620Abstract: 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: GrantFiled: January 8, 2018Date of Patent: March 26, 2019Assignees: Pernix Sleep, Inc., ProCom One, Inc.Inventors: Roberta L. Rogowski, Susan E. Dubé, Philip Jochelson, Neil B. Kavey
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Patent number: 10239888Abstract: 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: GrantFiled: July 25, 2018Date of Patent: March 26, 2019Assignee: Dana-Farber Cancer Institute, Inc.Inventors: James Bradner, Mette Ishoey, Dennis Buckley, Joshiawa Paulk, Marc Andrew Cohen, Rhamy Zeid
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Patent number: 10208042Abstract: 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: GrantFiled: October 10, 2018Date of Patent: February 19, 2019Assignee: Nanjing TransThera Biosciences Co. Ltd.Inventor: Frank Wu
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Patent number: 10188657Abstract: 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: GrantFiled: November 9, 2017Date of Patent: January 29, 2019Inventor: Lixin Zhang
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Patent number: 10143676Abstract: 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: GrantFiled: November 21, 2016Date of Patent: December 4, 2018Assignees: Pernix Sleep, Inc., ProCom One, Inc.Inventors: Susan E. Dubé, Neil B. Kavey
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Patent number: 10143695Abstract: 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: GrantFiled: May 17, 2017Date of Patent: December 4, 2018Assignee: 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
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Patent number: 10124009Abstract: 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: GrantFiled: October 27, 2015Date of Patent: November 13, 2018Assignee: Tensha Therapeutics, Inc.Inventors: Steven B. Landau, Michael Kagey
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Patent number: 10098892Abstract: 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: GrantFiled: May 29, 2013Date of Patent: October 16, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Paul A. Harmon, Narayan Variankaval
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Patent number: 10085980Abstract: 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: GrantFiled: November 11, 2016Date of Patent: October 2, 2018Assignee: ALKERMES PHARMA IRELAND LIMITEDInventors: Magali B. Hickey, Jennifer Vandiver
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Patent number: 10071129Abstract: 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: GrantFiled: August 30, 2012Date of Patent: September 11, 2018Assignee: WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH DANA-FARBER CANCER INSTITUTE, INC.Inventors: Richard A. Young, Peter B. Rahl, James Bradner
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Patent number: 10071163Abstract: 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: GrantFiled: November 23, 2015Date of Patent: September 11, 2018Assignee: 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
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Patent number: 10064859Abstract: 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: GrantFiled: August 24, 2015Date of Patent: September 4, 2018Assignee: ALKERMES PHARMA IRELAND LIMITEDInventors: Wilfredo Morales, Jr., Tarek A. Zeidan, Renato A. Chiarella, Steven G. Wright, Jason M. Perry
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Patent number: 10052319Abstract: 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: GrantFiled: March 14, 2013Date of Patent: August 21, 2018Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.Inventor: Tsuyoshi Tsujimura
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Patent number: 10047096Abstract: 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: GrantFiled: November 23, 2015Date of Patent: August 14, 2018Assignee: Bayer Pharma AktiengesellschaftInventors: 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
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Patent number: 10039769Abstract: 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: GrantFiled: May 31, 2017Date of Patent: August 7, 2018Assignee: Concert Pharmaceuticals, Inc.Inventor: Scott L. Harbeson
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Patent number: 10039760Abstract: 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: GrantFiled: December 21, 2016Date of Patent: August 7, 2018Assignee: Ampio Pharmaceuticals, Inc.Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K. R. Rao, Greg Thomas
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Patent number: 10035805Abstract: 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: GrantFiled: July 2, 2015Date of Patent: July 31, 2018Assignee: ESTEVE PHARMACEUTECALS, S.A.Inventors: Félix Cuevas-Cordobés, Miguel Angel Pericás-Brondo
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Patent number: 10004699Abstract: 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: GrantFiled: June 9, 2015Date of Patent: June 26, 2018Assignee: Acura Pharmaceuticals, Inc.Inventor: Ronald L. Leech, Jr.
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Patent number: 10004807Abstract: 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: GrantFiled: March 13, 2013Date of Patent: June 26, 2018Assignee: ALKERMES PHARMA IRELAND LIMITEDInventors: Jason M. Perry, Magali B. Hickey, Julius F. Remenar, Jennifer Vandiver
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Patent number: 9993570Abstract: 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: GrantFiled: July 5, 2016Date of Patent: June 12, 2018Assignee: WASHINGTON UNIVERSITYInventors: Robert Mach, Wenhua Chu, Dong Zhou, Loren Michel, Delphine Chen
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Patent number: 9975901Abstract: 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: GrantFiled: September 30, 2015Date of Patent: May 22, 2018Assignee: GlaxoSmithKline Intellectual Property (No. 2) LimitedInventors: Gossett Augustus Campbell, Asa Elisabeth Gladwin
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Patent number: 9975899Abstract: 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: GrantFiled: November 3, 2016Date of Patent: May 22, 2018Assignee: Janssen Pharmaceutica NVInventors: Lieven Meerpoel, Louis Jules Roger Marie Maes, Kelly de Wit, Koen Jan Ludovicus Augustyns
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Patent number: 9968620Abstract: 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; hydroxyaType: GrantFiled: August 19, 2015Date of Patent: May 15, 2018Assignee: ONCOETHIX GMBHInventor: Francesco Bertoni
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Patent number: 9969700Abstract: 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: GrantFiled: June 8, 2016Date of Patent: May 15, 2018Assignee: NIPPON CHEMIPHAR CO., LTD.Inventors: Masatoshi Ushioda, Kunio Kobayashi, Daisuke Saito, Shogo Sakuma, Toshiyasu Imai, Kazuhide Inoue
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Patent number: 9956228Abstract: 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: GrantFiled: May 1, 2015Date of Patent: May 1, 2018Assignee: OncoEthix GMBHInventors: Kay Noel, Maria E. Riveiro
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Patent number: 9938528Abstract: 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: GrantFiled: December 10, 2015Date of Patent: April 10, 2018Assignees: 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
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Patent number: 9926332Abstract: 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: GrantFiled: January 20, 2015Date of Patent: March 27, 2018Assignee: 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
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Patent number: 9926276Abstract: 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: GrantFiled: February 7, 2014Date of Patent: March 27, 2018Assignee: DRACONIS PHARMA, S.L.Inventors: Marina Virgili Bernado, Elena Carceller Gonzalez, Jordi Salas Solana