Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
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Patent number: 12233054Abstract: Disclosed are small molecules against cereblon to enhance effector T cell function. Methods of making these molecules and methods of using them to treat various disease states are also disclosed.Type: GrantFiled: August 21, 2023Date of Patent: February 25, 2025Assignee: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.Inventors: Pearlie Burnette, Nicholas J. Lawrence, Harshani Lawrence
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Patent number: 12158431Abstract: A colorimetric method for detecting copper in a liquid hydrocarbon, preferably, a liquid hydrocarbon fuel, in particular an aviation fuel. A test kit for use in administering the test method is also described.Type: GrantFiled: June 16, 2022Date of Patent: December 3, 2024Assignee: PRECISION COMBUSTION, Inc.Inventors: Robert W. Dean, Codruta Maria Zoican-Loebick
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Patent number: 12049467Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof, or an N-oxide thereof) of formula (I), which are positive allosteric modulators of one or more GABA-A receptors, e.g., which are peripherally restricted, positive allosteric modulators of one or more GABA-A receptors; e.g., which are positive allosteric modulators of one or more GABA-A receptors and which selectively target the peripheral nervous system and organs of the body, and which do not substantially pass through the blood-brain barrier. Said compounds are useful e.g., for the treatment of systemic diseases of the body, e.g., diseases in which modulation of one or more peripherally restricted GABA-A receptors is beneficial (e.g., diseases or disorders which are mediated by GABA-A neuronal activity. This disclosure also features pharmaceutical compositions containing the chemical entities described herein as well as methods of using same for the treatment of systemic diseases of the body.Type: GrantFiled: February 1, 2022Date of Patent: July 30, 2024Assignees: The Johns Hopkins University, Lieber Institute, Inc.Inventors: Yifang Huang, Pankaj Jay Pasricha, James C. Barrow, Ingrid Buchler, Michael Poslusney
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Patent number: 11998516Abstract: The present invention relates to methods for the treatment or prevention of depression, and related pharmaceutical compositions. Of particular interest are pharmaceutical compositions comprising cyclobenzaprine, alone, or in combination with an antidepressant drug.Type: GrantFiled: March 5, 2012Date of Patent: June 4, 2024Assignee: TONIX PHARMA HOLDINGS LIMITEDInventor: Seth Lederman
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Patent number: 11992495Abstract: Embodiments methods of reducing an inflammatory immune response (e.g., inhibiting a Th1 response) and/or promoting a regulatory immune response (e.g., enhancing Treg(s)) in a mammal are provided where the method methods involve administering to the mammal a GABAA receptor positive allosteric modulator (PAM) in an amount sufficient to reduce an inflammatory immune response and/or to promote a regulatory immune response said mammal. In certain embodiments the PAM is administered in conjunction with a GABA receptor activating ligand (e.g., GABA).Type: GrantFiled: June 20, 2018Date of Patent: May 28, 2024Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Daniel Kaufman, Jide Tian
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Patent number: 11975112Abstract: Compositions, devices, and methods for transdermal administration of olanzapine and uses thereof, e.g., to treat nausea and vomiting.Type: GrantFiled: January 13, 2021Date of Patent: May 7, 2024Assignee: Starton Therapeutics, Inc.Inventors: James Oliver, Fotios Plakogiannis, Tamanna Lather, Marina Borovinskaya, Nisarg Modi, Rod L. Hartwig
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Patent number: 11925649Abstract: Treatments for therapy of a diabetic symmetrical polyneuropathy a subject in need thereof. The treatments includes administration of compositions comprising: an effective amount of a muscarinic acetylcholine receptor antagonist exemplified by pirenzepine, telenzepine, atropine, or derivatives thereof or salts thereof or analogs thereof or derivatives thereof, and a pharmacologically acceptable carrier. The composition may be injectable or alternatively, may be applied topically or alternatively, may be delivered orally. A suitable topical composition may comprise a lotion, a cream, a gel, or a viscous fluid. The muscarinic acetylcholine receptor antagonist may be a muscarinic acetylcholine receptor antagonist salt or a muscarinic acetylcholine receptor antagonist derivative or a muscarinic acetylcholine receptor antagonist analog.Type: GrantFiled: October 15, 2018Date of Patent: March 12, 2024Assignees: University of Manitoba, University Health Network, The Regents of the university of CaliforniaInventors: Paul Fernyhough, Nigel A. Calcutt, Lakshmi Kotra
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Patent number: 11918590Abstract: Disclosed are stable extended release formulations and pharmaceutical compositions of Clozapine that exhibit improved stability under a variety of conditions, as well as processes for the preparation of such formulations and compositions.Type: GrantFiled: April 8, 2022Date of Patent: March 5, 2024Assignee: Intas Pharmaceuticals Ltd.Inventors: Rikin Patel, Kavan Pandya, Piyush Kansagra, Satyavan Dhavale, Ashish Sehgal
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Patent number: 11919905Abstract: Disclosed are a pyridyl imidazobenzodiazepine propionate (compound 1) and the synthesis and use thereof. Also provided are intermediates for the preparation. Compound 1 provided by the present invention has an obvious venous anesthesia activity equivalent to that of the positive control drug remimazolam p-toluenesulfonate or remimazolam besylate. In addition, compound 1 can be significantly reduced in mouse model experiments, and same can even overcome common limb jitters, head tilting, opisthotonus and other side effects caused by the remimazolam besylate or remimazolam p-toluenesulfonate as a drug during development in preclinical animal experiments, thereby allowing same to be used in the preparation of intravenous anesthetics. The structural general formula of compound 1 is as follows, wherein each group and substituent are as defined in the description.Type: GrantFiled: December 28, 2018Date of Patent: March 5, 2024Assignee: Hangzhou Adamerck Pharmlabs, Inc.Inventor: Youmao Qi
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Patent number: 11883385Abstract: Provided herein are methods of treating Tourette Syndrome in a subject in need thereof by administering to the subject compositions comprising a PDE10 inhibitor.Type: GrantFiled: December 2, 2022Date of Patent: January 30, 2024Assignee: Noema Pharma AGInventor: George Garibaldi
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Patent number: 11820776Abstract: The present disclosure relates to novel processes for the preparation of short acting benzodiazepines as well as to novel intermediates in this process. More particularly the disclosure relates to processes and intermediates for preparation of Methyl 3-[(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate, commonly known as Remimazolam. The present disclosure also relates to solid state forms of Remimazolam salts, processes for the preparation thereof, pharmaceutical formulations/compositions thereof, and methods of use thereof.Type: GrantFiled: May 24, 2021Date of Patent: November 21, 2023Assignee: ASSIA CHEMICAL INDUSTRIES LTD.Inventors: Dolitzky Ben-Zion, Mendelovici Marioara, Bodkhe Arjun Rajaram, Mane Ganesh Shivaji, Samala Rajamouli Srihari, Joshi Ashutosh Vijay, Parven Kumar Luthra, Amit Singh, Anantha Rajmohan Muthusamy
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Patent number: 11813359Abstract: 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: May 11, 2020Date of Patent: November 14, 2023Assignee: Teva Pharmaceuticals International GMBHInventors: Carine Claassen-Punt, Mark Alan Smith, Ling Chen, Ari Andrew Gershon
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Patent number: 11718620Abstract: The present invention relates to a method for treating a cancer mediated by abnormality of multi-kinases, comprising administrating 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. Also provided is a method for treating a cancer mediated by abnormality of multi-kinases, comprising administrating 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: December 31, 2020Date of Patent: August 8, 2023Assignee: TransThera Sciences (Nanjing), Inc.Inventor: Frank Wu
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Patent number: 11708368Abstract: The present invention provides a crystalline form of a benzodiazepine derivative hydrochloride of Formula I or its ethanolate, wherein R is methyl or ethyl. The present invention also provides a method of preparing the crystal form of the compound of Formula I and a pharmaceutical composition comprising the crystal form.Type: GrantFiled: February 13, 2019Date of Patent: July 25, 2023Assignee: JIANGSU NHWALUOKANG PHARMACEUTICAL RESEARCH AND DEVELOPMENT CO., LTD.Inventors: Qingeng Li, Chen Duan, Tao Wang, Jian Liao, Changwen Li, Chao Hao
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Patent number: 11623930Abstract: Disclosed are compounds according to Formula (I) or (II), and pharmaceutical compositions comprising them. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (I) or (II).Type: GrantFiled: March 5, 2019Date of Patent: April 11, 2023Assignee: Goldfinch Bio, Inc.Inventors: Matthew H. Daniels, Maolin Yu, Jean-Christophe P. Harmange, Thomas T. Tibbitts, Mark W. Ledeboer, Neil A. Castle, Goran Malojcic
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Patent number: 11608339Abstract: The present invention relates to compounds of Formula A and pharmaceutical compositions thereof that modulate the activity of the 5-HT2C receptor.Type: GrantFiled: October 19, 2020Date of Patent: March 21, 2023Assignee: Arena Pharmaceuticals, Inc.Inventors: Graeme Semple, Albert S. Ren, Thomas O. Schrader, Michelle Kasem, Xiuwen Zhu
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Patent number: 11548899Abstract: The present disclosure provides fused 1,4-oxazepines and related analogs represented by Formula (I) and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, R5, A, and Y are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer.Type: GrantFiled: February 15, 2017Date of Patent: January 10, 2023Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Bing Zhou, Yang Hu, Chao-Yie Yang, Chong Qin
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Patent number: 11478483Abstract: Disclosed herein are compositions and methods for the treatment of pulmonary hypertension, including pulmonary arterial hypertension. The methods include administering to a patient in need thereof an effective amount of Quetiapine or derivative thereof. The compositions include an effective amount of Quetiapine or derivative thereof, in some instances combined with one or more additional agents for the treatment of pulmonary hypertension.Type: GrantFiled: September 6, 2018Date of Patent: October 25, 2022Assignee: Cipla LimitedInventors: Geena Malhotra, Kalpana Joshi, Jeevan Ghosalkar
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Patent number: 11447495Abstract: Substituted benzo[f]imidazo[1,5-?][1,4]diazepines of formula (I?) target alpha-4 and alpha-5 GABAA receptors for use in the treatment of airway hyperresponsiveness and inflammation in asthma. Compounds selectively partition to the peripheral compartment and have reduced CNS effects.Type: GrantFiled: August 16, 2017Date of Patent: September 20, 2022Assignees: UWM Research Foundation, Inc., The Trustees of Columbia University in the City of New YorkInventors: Alexander E. Arnold, Douglas C. Stafford, James M. Cook, Charles W. Emala, Gloria Forkuo, Rajwana Jahan, Revathi Kodali, Guanguan Li, Michael Rajesh Stephen
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Patent number: 11446262Abstract: The present inventive concept defines as “Neuroquiescence” a method for treating neurovascular dysregulation underlying neurodevelopmental and neurodegenerative dysfunctions by improving immunovascular robustness for fueling glial cells while pausing neuronal bioelectrical activity for remyelination and astrocyte resetting cellular homeostasis.Type: GrantFiled: July 21, 2020Date of Patent: September 20, 2022Inventors: Debora Zucco Sassi Yonezawa Siviglia, Gary Aaron Howard
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Patent number: 11439636Abstract: 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: August 18, 2021Date of Patent: September 13, 2022Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 11426401Abstract: 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: August 5, 2021Date of Patent: August 30, 2022Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 11391740Abstract: This document provides methods and materials involved in identifying and/or treating mammals having a treatment-resistant prostate cancer (e.g., an enzalutamide-resistant, castration-resistant prostate cancer). For example, methods and materials for identifying a mammal (e.g., a human) having treatment-resistant prostate cancer (e.g., an enzalutamide-resistant, castration-resistant prostate cancer) as having an elevated level of one or more polypeptides (e.g., one or more of a CXXC5, a CXXC4, a TET2, an ID1, an ID3, and/or a PFN2 polypeptide) in treatment-resistant prostate tissue are provided. Methods and materials for administering one or more targeted therapies with or without one or more chemotherapeutic agents to a mammal having treatment-resistant prostate cancer identified as having an elevated level of one or more polypeptides (e.g., one or more of a CXXC5, a CXXC4, a TET2, an ID1, an ID3, and/or a PFN2 polypeptide) in treatment-resistant prostate tissue also are provided.Type: GrantFiled: May 19, 2020Date of Patent: July 19, 2022Assignee: Mayo Foundation for Medical Education and ResearchInventor: Haojie Huang
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Patent number: 11369583Abstract: Provided are a long-acting prodrug of Rasagiline, which has application in the treatment of Central Nervous System diseases such as Parkinson's disease, preparation method and use thereof. The long-acting prodrug of Rasagiline has a structure of formula (I), wherein T is absent, or T is selected from each of R1 and R2 is independently selected from H, D, and alkyl; W is absent, or W is selected from (CH2)n, wherein n is an integer selected from 1 to 15; X is absent, or X is selected from (CH2)m, wherein m is an integer selected from 1 to 10; Y is absent, or Y is selected from —C(?O)NH—, —NHC(?O)—; R3 is selected from substituted or unsubstituted C1-C30 alkyl, substituted or unsubstituted C2-C30 alkenyl, substituted or unsubstituted C2-C30 alkynyl, substituted or unsubstituted C3-C30 cycloalkyl, cholane aliphatic group, —R3a—C(?O)O—R3b, —R3a—OC(?O)—R3b, —R3a—C(?O)NH—R3b, —R3a—NHC(?O)—R3b, —R3a—S(?O)1-2O—R3b and —R3a—OS(?O)1-2—R3b.Type: GrantFiled: August 27, 2018Date of Patent: June 28, 2022Assignee: GUANGZHOU HENOVCOM BIOSCIENCE CO. LTDInventors: Jiancun Zhang, Deyao Li, Yiqian Zhou, Yiwu Wu
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Patent number: 11324732Abstract: The disclosure is directed to methods of treating dyskinesia in cerebral palsy in human patients using deutetrabenazine and its active metabolites.Type: GrantFiled: December 13, 2019Date of Patent: May 10, 2022Assignee: Auspex Pharmaceuticals, Inc.Inventors: Juha-Matti Savola, Mark Forrest Gordon, Frank Schneider
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Patent number: 11273158Abstract: The present invention relates to methods of treating schizophrenia using a combination of aripiprazole, aripiprazole lauroxil, and a nanoparticle dispersion of aripiprazole lauroxil.Type: GrantFiled: March 4, 2019Date of Patent: March 15, 2022Assignee: Alkermes Pharma Ireland LimitedInventors: Lisa L. von Moltke, Peter J. Weiden, Marjie L. Hard
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Patent number: 11267822Abstract: The present disclosure provides compounds represented by Formula (I): Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Y, ?, Ar, W, L, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I)I for use to treat a condition or disorder responsive to inhibition and/or degradation of BET bromodomains such as cancer.Type: GrantFiled: September 12, 2018Date of Patent: March 8, 2022Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Weiguo Xiang, Fuming Xu, Longchuan Bai, Ester Fernandez-Salas, Donna McEachern
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Patent number: 11241441Abstract: Formulations of lixivaptan, and methods of using the same, are provided for the treatment of polycystic disease.Type: GrantFiled: June 8, 2018Date of Patent: February 8, 2022Assignee: PALLADIO BIOSCIENCES, INC.Inventor: Lorenzo Pellegrini
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Patent number: 11173132Abstract: Methods, compositions, and devices for transdermally administering an active agent such as memantine are provided.Type: GrantFiled: December 20, 2018Date of Patent: November 16, 2021Assignee: Corium, Inc.Inventors: Eun Soo Lee, Parminder Singh, Appala Sagi, Amit K. Jain
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Patent number: 11155555Abstract: The invention relates to new quinoxaline, quinoline and quinazolinone derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: September 22, 2016Date of Patent: October 26, 2021Assignee: Janssen Pharmaceutica NVInventors: Patrick Rene Angibaud, Diego Fernando Domenico Broggini, Helene France Solange Colombel, Filip Albert C Cuyckens, Steven Anna Hostyn, Russell Mark Jones, Olivier Alexis Georges Querolle, Wim Vermeulen
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Patent number: 11141388Abstract: 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 24, 2020Date of Patent: October 12, 2021Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 11090300Abstract: 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 18, 2020Date of Patent: August 17, 2021Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 11066419Abstract: The present invention relates to 1H-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.Type: GrantFiled: December 21, 2017Date of Patent: July 20, 2021Assignee: Frequency Therapeutics, Inc.Inventors: Christopher Loose, Bradley Tait, Rajesh Manchanda, Will Mclean
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Patent number: 11046709Abstract: The present disclosure provides fused 1,4-diazepines represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, E, R1, R2, R3, R4, R5, and Ar are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds having Formula (I) to treat diseases, conditions, or disorders responsive to inhibition of BET bromodomain proteins such as cancer.Type: GrantFiled: February 2, 2018Date of Patent: June 29, 2021Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Jiantao Hu, Fuming Xu
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Patent number: 11034697Abstract: The present disclosure relates to novel processes for the preparation of short acting benzodiazepines as well as to novel intermediates in this process. More particularly the disclosure relates to processes and intermediates for preparation of Methyl 3-[(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate, commonly known as Remimazolam. The present disclosure also relates to solid state forms of Remimazolam salts, processes for the preparation thereof, pharmaceutical formulations/compositions thereof, and methods of use thereof.Type: GrantFiled: February 8, 2018Date of Patent: June 15, 2021Assignee: WATSON LABORATORIES INC.Inventors: Dolitzky Ben-Zion, Mendelovici Marioara, Bodkhe Arjun Rajaram, Mane Ganesh Shivaji, Samala Rajamouli Srihari, Joshi Ashutosh Vijay, Parven Kumar Luthra, Amit Singh, Anantha Rajmohan Muthusamy
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Patent number: 11007189Abstract: 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 23, 2020Date of Patent: May 18, 2021Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 10988459Abstract: The invention provides novel compounds having the general formula I: wherein R1, X, Z1, L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.Type: GrantFiled: July 1, 2016Date of Patent: April 27, 2021Assignee: Genentech, Inc.Inventors: Snahel Patel, Gregory Hamilton, Craig Stivala, Huifen Chen, Guiling Zhao
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Patent number: 10966999Abstract: Provided herein are the 3?3? cyclic phosphonate dinucleotides of general formula J, their pharmaceutically acceptable salts, a pharmaceutical composition containing them and combinations of said substances and other medicaments or pharmaceuticals. The disclosure also relates to the use of said compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. In addition, these substances can be used as adjuvants in vaccines.Type: GrantFiled: December 19, 2018Date of Patent: April 6, 2021Assignee: INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.Inventors: Gabriel Birkus, Ondrej Pav, Tomas Jandusik, Ivan Rosenberg, Radim Nencka
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Patent number: 10966974Abstract: 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 18, 2020Date of Patent: April 6, 2021Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 10945973Abstract: 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: August 3, 2020Date of Patent: March 16, 2021Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 10925967Abstract: The present application provides bifunctional compounds of Formula (X): or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.Type: GrantFiled: November 22, 2017Date of Patent: February 23, 2021Assignee: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Dennis Dobrovolsky, Hai-Tsang Huang
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Patent number: 10913752Abstract: The present invention provides bivalent inhibitors of BET bromodomains, such as compounds of Formulae (I), (II), (III), (IV), (V), and (VI). Some bromdomain-containing proteins (e.g., BRD4) have a tandem bromodomain primary structure comprising more than one bromodomain binding site (e.g., BRD4 comprises BD1 and BD2). Bivalent inhibitors of BET bromodomains provided herein can target bromodomains through advantageous multivalent interactions, and can therefore can be to treat diseases or conditions associated with bromodomain-containing proteins. The present also provides pharmaceutical compositions and kits comprising the inventive compounds, as well as methods of using the inventive compounds.Type: GrantFiled: November 23, 2016Date of Patent: February 9, 2021Assignee: Dana-Farber Cancer Institute, Inc.Inventors: James E. Bradner, Jun Qi, Minoru Tanaka, Justin M. Roberts
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Patent number: 10894046Abstract: 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 17, 2020Date of Patent: January 19, 2021Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 10894047Abstract: 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 20, 2020Date of Patent: January 19, 2021Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 10874663Abstract: 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 17, 2020Date of Patent: December 29, 2020Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 10874665Abstract: 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 19, 2020Date of Patent: December 29, 2020Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 10874664Abstract: 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 19, 2020Date of Patent: December 29, 2020Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 10864209Abstract: 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 20, 2020Date of Patent: December 15, 2020Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 10836764Abstract: The present invention relates to compounds of Formula A and pharmaceutical compositions thereof that modulate the activity of the 5-HT2C receptor.Type: GrantFiled: August 18, 2017Date of Patent: November 17, 2020Assignee: Arena Pharmaceuticals, Inc.Inventors: Graeme Semple, Albert S. Ren, Thomas O. Schrader, Michelle Kasem, Xiuwen Zhu
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Patent number: 10807973Abstract: New compounds and a method of treating a retinal disease that leads to photoreceptor loss or outer-retina degeneration, including administering compound of the formula (I) or a pharmaceutically acceptable salt, a racemic mixture, a corresponding enantiomer or, if applicable, a corresponding diastereomer thereof, wherein: A is a 5-oxazolyl residue or a pyridine-4-yl residue, R1 is selected from the group consisting of fluoro, chloro and methoxy; B is selected from the group consisting of a residue of formula (II), (III) and (IV) wherein, “*” denotes the point of attachment to the remainder of the molecule, and R2, R2?, R2?, R3, R3?, R3?, R4, R4?, R4?, R5, R5? and R5? are independently selected from the group consisting of hydrogen, a linear or branched alkyl having 1 to 4 carbon atoms, trifluoromethyl, 2,2,2-trifluoroethyl, methylsulfanyl, ethylsulfanyl, methylsulfonyl, ethylsulfonyl, difluoromethoxy, trifluoromethoxy, fluoro, bromo, chloro, methoxy, ethoxy, propoxy, butoxy, hydroxy and amino.Type: GrantFiled: December 28, 2018Date of Patent: October 20, 2020Assignee: ENDOGENA THERAPEUTICS, INC.Inventors: Matthias Steger, Alex Mueller, Bernhard Fasching, Daphna Mokady