At Least Three Rings In The Polycyclo Ring System Patents (Class 514/250)
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Patent number: 11066406Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK.Type: GrantFiled: January 29, 2020Date of Patent: July 20, 2021Assignee: Janssen Pharmaceutica NVInventors: Philippe Fernandes, Paul J. Krawczuk, Mark S. Tichenor
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Patent number: 11059826Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).Type: GrantFiled: April 23, 2019Date of Patent: July 13, 2021Assignee: VERTEX PHARMACEUTICALS INCORPORATEDInventors: David J. Lauffer, Guy Bemis, Michael Boyd, David Deininger, Hongbo Deng, Warren Dorsch, Wenxin Gu, Russell R. Hoover, Mac Arthur Johnson, Jr., Mark Willem Ledeboer, Brian Ledford, Francois Maltais, Marina Penney, Darin Takemoto, Nathan D. Waal, Tiansheng Wang, Pan Li
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Patent number: 11052083Abstract: The disclosure provides new transmucosal and subcutaneous pharmaceutical compositions comprising 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or 1-(4-fluoro-phenyl)-4-((6bR,10aS)-2,2-d2-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or comprising -(4-fluoro-phenyl)-4-((6bR,10aS)-1,1,2,2-d4-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, in free base, co-crystal or salt form, together with methods of making and using them.Type: GrantFiled: June 12, 2020Date of Patent: July 6, 2021Assignee: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Wei Yao, Robert Davis
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Patent number: 11041856Abstract: The invention provides immunochromatographic test strips and methods and systems or kits for detecting and quantifying S-Adenosylmethionine (SAM), S-Adenosylhomocysteine (SAH) and Homocysteine (HCy) in a sample, comprising: (a) making fluorophore conjugated antibodies; (b) immobilizing SAM, SAH and HCy on a solid support; (c) providing a sample, combining said sample with a conjugate selected from the group consisting of lanthanide chelate conjugates and quantum dot conjugates (QD) with anti-SAM, anti-SAH or anti-HCy, wherein said combining is performed under conditions that allow formation of a competitive complex comprising said conjugate, said SAM, SAH or HCy on the solid support and SAM, SAH or HCy in a sample when present; and (d) detecting the presence of the complex, if present, by monitoring a spectral emission mediated by the fluorescent conjugates in the complex, wherein the emission indicates the presence and quantity of SAM, SAH or HCy in the sample.Type: GrantFiled: September 3, 2018Date of Patent: June 22, 2021Assignee: HUNAN SKYWORLD BIOTECHNOLOGIES COInventors: Xiujuan Hao, Chaoyi Deng
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Patent number: 11020491Abstract: The present invention provides a biocompatible conjugate for treating a disease or an injury. The conjugate contains a polymer covalently linked to one or more moieties each containing a polymerizable functional group. The conjugate forms a cross-linked polymer network after being exposed to an elevated level of free radicals associated with the disease or injury.Type: GrantFiled: June 14, 2018Date of Patent: June 1, 2021Assignee: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Christopher Lowe, David I. Shreiber, Emily DiMartini, Adam Gormley
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Patent number: 10995095Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and atopic dermatitis), kits, methods of synthesis, and products-by-process.Type: GrantFiled: December 19, 2019Date of Patent: May 4, 2021Assignee: AbbVie Inc.Inventors: Aileen L. Pangan, Henrique D. Teixeira, Mohamed-Eslam F. Mohamed, Ahmed A. Othman, Ben Klünder
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Patent number: 10981923Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.Type: GrantFiled: June 18, 2020Date of Patent: April 20, 2021Assignee: AbbVie Inc.Inventors: Ayman Allian, Thomas B. Borchardt, Jayanthy Jayanth, Patrick J. Marroum, Peter T. Mayer, Mathew M. Mulhern, Fredrik Lars Nordstrom, Ahmad Y. Sheikh
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Patent number: 10981888Abstract: Methods for preparing compounds of formula (I) Wherein R1 to R5 and A1 to A4 are as defined in the application.Type: GrantFiled: December 4, 2017Date of Patent: April 20, 2021Assignee: Bayer CropScience AktiengesellschaftInventors: Florian Erver, Frank Memmel, Alexander Arlt, Werner Hallenbach, Tobias Harschneck, Christoph Schotes, Robert Velten
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Patent number: 10981924Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.Type: GrantFiled: August 3, 2020Date of Patent: April 20, 2021Assignee: AbbVie Inc.Inventors: Jayanthy Jayanth, Ben Klünder, Mohamed-Eslam Mohamed, Ahmed A. Othman, Patrick J. Marroum, Peter T. Mayer
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Patent number: 10927129Abstract: The present invention is directed to N-[(2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide of the formula: or a pharmaceutically acceptable salt or stereoisomer thereof, and pharmaceutical compositions comprising the same. The present invention has HIV integrase inhibitory activity.Type: GrantFiled: May 1, 2019Date of Patent: February 23, 2021Assignees: SHINOGI & CO., LTD., VIIV HEALTHCARE COMPANYInventors: Brian A. Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Patent number: 10918735Abstract: The synthesis of various pyrazino[1?,2?:1,5]pyrrolo[2,3-B]-indole-1,4-dione analogs has been successfully implemented in the present application. From these efforts, compounds having the structure of Formula I-a or Formula I-b: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, are provided herein. These biologically active derivatives have been used to effectively treat various diseases including cancer.Type: GrantFiled: March 5, 2019Date of Patent: February 16, 2021Assignees: Massachusetts Institute of Technology, The Board of Trustees of the University of IllinoisInventors: Mohammad Movassaghi, Justin Kim, Paul Hergenrother, Karen Morrison, Nicolas Boyer
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Patent number: 10913747Abstract: Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.Type: GrantFiled: May 15, 2018Date of Patent: February 9, 2021Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.Inventors: Ottorino De Lucchi, Pierluigi Padovan, Elena Brasola
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Patent number: 10898449Abstract: The present invention relates to transdermal therapeutic systems (TTS) for the transdermal administration of asenapine comprising a self-adhesive layer structure containing a therapeutically effective amount of asenapine, such asenapine TTS for use in a method of treatment, processes of manufacture of such TTS as well as asenapine and transdermal therapeutic systems containing asenapine for use in a method of treatment and to a method of treating a human patient by transdermal administration of asenapine.Type: GrantFiled: February 11, 2020Date of Patent: January 26, 2021Assignee: LTS LOHMANN THERAPIE-SYSTEME AGInventors: Patrick Mohr, René Rietscher, René Eifler, Olga Bourquain
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Patent number: 10829499Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.Type: GrantFiled: June 20, 2019Date of Patent: November 10, 2020Assignee: MERCK SHARP & DOHME CORP.Inventors: Thomas H. Graham, Tao Yu, Yonglian Zhang, John A. McCauley
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Patent number: 10813919Abstract: Compositions including combinations of class I histone deacetylase (HDAC) inhibitors and programmed cell death protein 1 (PD-1) inhibitors for enhancing antitumor activity are disclosed. Further disclosed are methods of administering these compositions as immunotherapies for suppressing regulatory T cells in renal cell carcinoma.Type: GrantFiled: January 27, 2017Date of Patent: October 27, 2020Assignee: Indiana University Research and Technology CorporationInventor: Roberto Pili
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Patent number: 10787456Abstract: Disclosed is a composition and method for a therapeutic treatment that is able to combat certain conditions such as alcohol dependence, opioid abuse treatment, neurological disorders, neuropathic pain, and fibromyalgia. The novel gliotoxin analog compound acts by acting as an antagonist to one or more opioid receptors, which, when present leads to the inhibition of conditions, providing increased performance over known treatments. The disclosed compounds also shows the ability to cross the blood-brain-barrier in a highly efficient manner.Type: GrantFiled: October 30, 2018Date of Patent: September 29, 2020Assignee: TEXAS TECH UNIVERSITY SYSTEMInventors: Nadezhda German, Mohammad Anwar Hossain
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Patent number: 10758530Abstract: Described herein are carboxamide derivatives that are useful as inhibitors of p90 ribosomal S6 kinase (RSK), pharmaceutical compositions comprising the derivatives, and methods of using the derivatives in treating diseases or conditions associated with RSK activity. Such carboxamide derivatives form bicyclic and tricyclic ring systems and the disease or condition associated with RSK activity in a mammal is cancer.Type: GrantFiled: February 17, 2017Date of Patent: September 1, 2020Assignee: PHOENIX MOLECULAR DESIGNSInventors: Sandra E. Dunn, Aarthi Jayanthan, Jaipal Reddy Nagireddy, Subhash Annedi, John H. Van Drie, Timothy S. Daynard, My-my Huynh
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Patent number: 10758532Abstract: Disclosed herein are pharmaceutical compositions, devices, their combinations, and their uses thereof for example in treating or preventing headaches.Type: GrantFiled: December 11, 2019Date of Patent: September 1, 2020Assignee: Satsuma Pharmaceuticals, Inc.Inventors: John Kollins, Fumiyoshi Iwashima, Detlef Albrecht, Robert David Schultz
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Patent number: 10752624Abstract: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.Type: GrantFiled: May 18, 2018Date of Patent: August 25, 2020Assignee: ORIGENIS GMBHInventors: Michael Almstetter, Michael Thormann, Andreas Treml, Roland Koestler, Nasser Yehia
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Patent number: 10736893Abstract: In some embodiments, the invention relates to a BTK inhibitor or a pharmaceutically acceptable salt, cocrystal, ester, prodrug, solvate, hydrate or derivative thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, in some embodiments, the present invention relates to imidazopyrazine compounds, pharmaceutical compositions thereof, and the use of the compounds and pharmaceutical compositions in the treatment of a hyperproliferative disorder, an inflammatory disorder, an immune disorder, or an autoimmune disorder.Type: GrantFiled: November 4, 2016Date of Patent: August 11, 2020Assignee: Acerta Pharma B.V.Inventors: Tjeerd Barf, Edwin de Zwart, Saskia Verkaik, Niels Hoogenboom, Dennis Demont
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Patent number: 10736972Abstract: Described herein is a method of induced cell death via ferroptosis by nanoparticle ingestion. Moreover, the present disclosure describes the administration of high concentrations of ultrasmall nanoparticles at multiple times over the course of treatment in combination with a nutrient-depleted environment, thereby modulating cellular metabolic pathways to induce cell death by the mechanism ferroptosis. Ferroptosis involves iron, reactive oxygen species, and a synchronous mode of cell death execution.Type: GrantFiled: May 26, 2016Date of Patent: August 11, 2020Assignees: Memorial Sloan Kettering Cancer Center, Cornell UniversityInventors: Michelle S. Bradbury, Ulrich Wiesner, Michael Overholtzer, Howard Scher, Kai Ma
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Patent number: 10730883Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.Type: GrantFiled: February 11, 2020Date of Patent: August 4, 2020Assignee: AbbVie Inc.Inventors: Ayman Allian, Jayanthy Jayanth, Ben Klünder, Mohamed-Eslam F. Mohamed, Ahmed A. Othman, Patrick J. Marroum, Peter T. Mayer
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Patent number: 10716786Abstract: The disclosure provides new transmucosal and subcutaneous pharmaceutical compositions comprising 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or 1-(4-fluoro-phenyl)-4-((6bR,10aS)-2,2-d2-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one or comprising -(4-fluoro-phenyl)-4-((6bR,10aS)-1,1,2,2-d4-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, in free base, co-crystal or salt form, together with methods of making and using them.Type: GrantFiled: March 23, 2018Date of Patent: July 21, 2020Assignee: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Wei Yao, Robert Davis
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Patent number: 10702521Abstract: The present invention relates to methods for treating Neisseria Gonorrhoeae infection which comprises administering to a subject in need thereof novel 1,2-dihydro-2a,5,8a-triazaacenaphthylene-3,8-dione compounds: or pharmaceutically acceptable salts thereof and/or corresponding pharmaceutical compositions.Type: GrantFiled: August 20, 2015Date of Patent: July 7, 2020Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventor: Katherine Louisa Widdowson
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Patent number: 10696682Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.Type: GrantFiled: December 19, 2018Date of Patent: June 30, 2020Assignee: G1 Therapeutics, Inc.Inventors: Francis X. Tavares, Jay Copeland Strum
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Patent number: 10695345Abstract: The present disclosure relates to pharmaceutical capsules comprising lumateperone, in free, or pharmaceutically acceptable salt form, optionally in combination with one or more additional therapeutic agents, processes for manufacture thereof and methods of use in the treatment or prophylaxis of disease.Type: GrantFiled: August 30, 2019Date of Patent: June 30, 2020Assignee: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Robert Davis
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Patent number: 10689387Abstract: A crystalline form of (1R,2R)-2-[4-(3-Methyl-1H-pyrazol-5-yl)benzoyl]-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-3-yl)cyclohexanecarboxamide, pharmaceutical compositions containing it and its use in the prevention or treatment of cardiovascular diseases.Type: GrantFiled: October 27, 2017Date of Patent: June 23, 2020Assignee: AstraZeneca ABInventor: Anna Matilda Angelica Pettersen
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Patent number: 10689399Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: GrantFiled: June 25, 2018Date of Patent: June 23, 2020Assignee: Gilead Sciences, Inc.Inventors: Elizabeth M. Bacon, Zhenhong R. Cai, Xiaowu Chen, Jeromy J. Cottell, Manoj C. Desai, Mingzhe Ji, Haolun Jin, Scott E. Lazerwith, Michael R. Mish, Philip Anthony Morganelli, Hyung-Jung Pyun, James G. Taylor, Teresa Alejandra Trejo Martin
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Patent number: 10682354Abstract: The invention provides methods for the prophylaxis or treatment of one or more disorders associated with dementia comprising administering to a patient in need thereof, a therapeutically effective amount of (i) a 5-HT2A or 5-HT2A/D2 receptor ligand and (ii) a PDE1 inhibitor, and pharmaceutical compositions comprising (i) a 5-HT2A or 5-HT2A/D2 receptor ligand and (ii) a PDE1 inhibitor.Type: GrantFiled: March 28, 2017Date of Patent: June 16, 2020Assignee: INTRA-CELLULAR THERAPIES, INC.Inventor: Lawrence P. Wennogle
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Patent number: 10661099Abstract: A method for the treatment of a person suffering from neurodegenerative disease such as Alzheimer's, Parkinson's, or Huntington's disease by treating the patient's brain, over the span of one year or less with a plurality of doses of ionizing radiation, each dose being more than 2.5 mJ/kg but less than 150 mJ/kg with the total dose being more than 10 mJ/kg but less than 400 mJ/kg.Type: GrantFiled: June 14, 2016Date of Patent: May 26, 2020Inventor: Eugene R. Moore
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Patent number: 10597400Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.Type: GrantFiled: July 1, 2019Date of Patent: March 24, 2020Assignee: AbbVie Inc.Inventors: Ahmed A. Othman, Mohamed-Eslam F. Mohamed, Ben Klünder, Aileen L. Pangan
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Patent number: 10576078Abstract: The present invention relates to method of treating chronic myeloid leukemia (CML) or drug resistant CML comprising, administering to human being or any other mammal or animal in need thereof, a therapeutically effective amount of Clofazimine (CFZ) or its pharmaceutically acceptable derivative, analogue, salt or composition; or a combination of a therapeutically effective amount of Clofazimine (CFZ) or its pharmaceutically acceptable derivative, analogue, salt or composition with a tyrosine kinase inhibitor (TKI). The invention also provides the kit for treatment of CML or drug resistant CML.Type: GrantFiled: August 30, 2018Date of Patent: March 3, 2020Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Sabyasachi Sanyal, Harish Kumar, Naibedya Chattopadhyay, Ravishankar Ramachandran, Arun Kumarv Trivedi, Sonal Shree, Anagha Ashok Gurjar, Sourav Chattopadhyay, Sapana Kushwaha, Abhishek Kumar Singh, Shikha Dubey, Kiran Lata, Riyazuddin Mohammed, Jiaur Rahaman Gayen, Anil Kumar Tripathi
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Patent number: 10544124Abstract: The present invention relates to compounds of the general formula (I) in which Q, V, T, W, X, Y and A have the meanings given in the description—and to their use for controlling animal pests.Type: GrantFiled: February 6, 2017Date of Patent: January 28, 2020Assignee: Bayer CropScience AktiengesellschaftInventors: Johannes-Rudolf Jansen, Markus Heil, Reiner Fischer, David Wilcke, Matthieu Willot, Kerstin Ilg, Sascha Eilmus, Peter Lösel, Wolfram Andersch
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Patent number: 10526331Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: GrantFiled: February 26, 2019Date of Patent: January 7, 2020Assignee: Janssen Sciences Ireland Unlimited CompanyInventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
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Patent number: 10517876Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.Type: GrantFiled: January 5, 2017Date of Patent: December 31, 2019Assignee: CTI BIOPHARMA CORP.Inventors: Stephanie Blanchard, Cheng Hsia Angeline Lee, Harish Kumar Mysore Nagaraj, Anders Poulsen, Eric T. Sun, Yee Ling Evelyn Tan, Anthony Deodaunia William
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Patent number: 10513524Abstract: The present invention relates to PDE9 inhibitors and their use for treatment of benign prostate hyperplasia and sickle cell disease.Type: GrantFiled: July 6, 2016Date of Patent: December 24, 2019Assignee: H. LUNDBECK A/SInventors: Niels Svenstrup, Kate Wen, Yazhou Wang
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Patent number: 10501463Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: GrantFiled: November 16, 2018Date of Patent: December 10, 2019Assignee: Janssen Sciences Ireland Unlimited CompanyInventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
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Patent number: 10500202Abstract: Disclosed herein are pharmaceutical compositions comprising Tadalafil, or a salt, or derivatives thereof and pharmaceutical excipients, processes for the preparation thereof, and pharmaceutical compositions containing them. The pharmaceutical compositions have improved physicochemical properties that provide faster onset of action for the treatment of erectile dysfunction.Type: GrantFiled: November 30, 2017Date of Patent: December 10, 2019Assignee: Druggability Technologies IP Holdco LimitedInventors: Betti Szabóné Ordasi, Tamás Jordán, Richárd Balázs Kárpáti, Andrea Ujhelyi, Tamás Solymosi, Hristos Glavinas, Genovéva Filipcsei
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Patent number: 10493075Abstract: The present invention relates to a method of preparing 4-Amino-(6R,S)-5,6,7,8-tetrahydro-L-biopterin dihydrochloride dihydrate.Type: GrantFiled: June 8, 2018Date of Patent: December 3, 2019Assignee: VASOPHARM GMBHInventors: Peter Scheurer, Frank Tegtmeier, Reinhard Schinzel
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Patent number: 10479801Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.Type: GrantFiled: November 30, 2017Date of Patent: November 19, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Thomas H. Graham, Tao Yu, Yonglian Zhang, John A. McCauley
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Patent number: 10456395Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein L, R1, R5, W, X, Y1, Y2, and Z are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: GrantFiled: May 17, 2018Date of Patent: October 29, 2019Assignee: Gilead Sciences, Inc.Inventors: Hyung-Jung Pyun, Manoj C. Desai, Haolun Jin, Mingzhe Ji, Teresa Alejandra Trejo Martin
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Patent number: 10414777Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: GrantFiled: October 27, 2017Date of Patent: September 17, 2019Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
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Patent number: 10413553Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.Type: GrantFiled: February 1, 2018Date of Patent: September 17, 2019Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Giles Albert Brown, Julie Elaine Cansfield, Benjamin Gerald Tehan
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Patent number: 10376509Abstract: Methods for inhibiting the activity of Clostridium difficile in a subject comprise administering to the subject in need thereof a pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and a clofazimine analog selected from B746 clofazimine analog or B826 clofazimine analog.Type: GrantFiled: August 22, 2018Date of Patent: August 13, 2019Assignee: KamTek, Inc.Inventors: Venkata M. Reddy, Wolf Prensky, Sharanjit VedBrat
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Patent number: 10254297Abstract: Components for enabling immunodetection of methoxetamine are described including immunogens, haptens, antibodies and kits.Type: GrantFiled: July 1, 2016Date of Patent: April 9, 2019Assignee: Randox Laboratories Ltd.Inventors: Ivan McConnell, Philip Lowry, Elouard Benchikh, Peter Fitzgerald
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Patent number: 10220099Abstract: The synthesis of various pyrazino[1?,2?:1,5]pyrrolo[2,3-b]-indole-1,4-dione analogs has been successfully implemented in the present application. From these efforts, compounds having the structure of Formula I-c: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein R1, R2, R4-R8, R3?, R6?, and n are as defined herein, are provided. These biologically active derivatives have been further used to prepare cell-specific drug conjugates effective in treating various diseases including cancer.Type: GrantFiled: May 10, 2016Date of Patent: March 5, 2019Assignees: Massachusetts Institute of Technology, The Board of Trustees of the University of IllinoisInventors: Mohammad Movassaghi, Justin Kim, Paul J. Hergenrother, Karen Morrison, Nicolas Boyer
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Patent number: 10184932Abstract: The present invention inter alia provides a method, and use thereof, of predicting CV events such as AMI, ACS, stroke, and CV death by determining the concentration of at least one ceramide of Formula I or one lysophospholipid of Formula II and/or III and at least one lysophospholipid of Formula IV, V, VI, VII and/or VIII in a biological sample and comparing those concentrations to a control. Finding an increased concentration of the at least one Formula I ceramide or Formula II and/or III lysophospholipid and a decreased concentration of the at least one Formula IV, V, VI, VII and/or VIII lysophospholipid indicates that the subject has an increased risk of developing one or more CV events. The present disclosure also provides a method, and use thereof, of diagnosing subjects suffering acute ischemia. Also provided are kits and compositions comprising the same for use in predicting and/or diagnosing CV events.Type: GrantFiled: December 7, 2016Date of Patent: January 22, 2019Assignee: Zora Biosciences OYInventors: Mika Hilvo, Reini Hurme, Reijo Laaksonen, Virve Vaeisaenen
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Patent number: 10172854Abstract: The invention described herein relates to methods for treating mitochondrial diseases. In particular, the invention relates to methods for treating mitochondrial diseases by administering therapeutically effective amounts of one or more tetracyclic pyrazinoindoles, and/or pharmaceutically acceptable salts thereof.Type: GrantFiled: August 22, 2017Date of Patent: January 8, 2019Assignee: BIOVISTA, INC.Inventors: Spyros Deftereos, Andreas Persidis
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Patent number: 10155759Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: GrantFiled: December 18, 2017Date of Patent: December 18, 2018Assignee: Janssen Sciences Ireland UCInventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
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Patent number: RE47221Abstract: The invention provides compounds of Formula (I) and Formula (II) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: GrantFiled: March 1, 2017Date of Patent: February 5, 2019Assignee: AbbVie Inc.Inventors: Neil Wishart, Kristine E. Frank, Michael Friedman, Dawn M. George, Kent D. Stewart, Grier A. Wallace