Ring Nitrogen Shared By Two Of The Cyclos Patents (Class 514/233.2)
  • Patent number: 12013405
    Abstract: A reagent composition for releasing vitamin D compounds bound to vitamin D-binding protein and an in vitro method for the detection of a vitamin D compound in which the vitamin D compound is released from vitamin D-binding protein by the use of this reagent composition as well as the reagent mixture obtained in this manner. Also disclosed is the use of the reagent compositions to release vitamin D compounds as well as a kit for detecting a vitamin D compound.
    Type: Grant
    Filed: October 26, 2021
    Date of Patent: June 18, 2024
    Assignee: Roche Diagnostics Operations, Inc.
    Inventors: Sascha Antoni, Christian Vogl
  • Patent number: 11999758
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5 and are as defined in the description.
    Type: Grant
    Filed: October 2, 2019
    Date of Patent: June 4, 2024
    Assignee: INVENTIVA
    Inventors: Martine Barth, Sylvie Contal, Jean-Louis Junien, Christine Massardier, Christian Montalbetti, Anne Soude
  • Patent number: 11999729
    Abstract: Provided herein are compounds that interrupt the function of SALL4. Also described are pharmaceutical compositions and medical uses of these compounds.
    Type: Grant
    Filed: November 1, 2022
    Date of Patent: June 4, 2024
    Assignees: DANA-FARBER CANCER INSTITUTE, INC., THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
    Inventors: Jun Qi, Anthony Varca, Li Chai
  • Patent number: 11964974
    Abstract: Novel imidazo[1,2-c]pyrido[3,4-e]pyrimidine-3-carboxylic acid compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The imidazo[1,2-c]pyrido[3,4-e]pyrimidine-3-carboxylic acid compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.
    Type: Grant
    Filed: January 8, 2024
    Date of Patent: April 23, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Christophe Tratrat, Michelyne Haroun
  • Patent number: 11945827
    Abstract: The present disclosure provides macrocyclic compounds inspired by the immunophilin ligand family of natural products FK506 and rapamycin. The generation of a Rapafucin library of macrocyles that contain FK506 and rapamycin binding domains should have great potential as new leads for developing drugs to be used for treating diseases.
    Type: Grant
    Filed: May 27, 2021
    Date of Patent: April 2, 2024
    Assignee: The Johns Hopkins University
    Inventors: Jun Liu, Sam Hong, Brett R. Ullman, Joseph E. Semple, Kana Yamamoto, Puneet Kumar, Magesh Sadagopan, Jennifer C. Schmitt
  • Patent number: 11939344
    Abstract: The specification relates to spirocyclic compounds of Formula (I) and pharmaceutically acceptable salts thereof. The specification also relates to processes and intermediates used for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
    Type: Grant
    Filed: June 15, 2023
    Date of Patent: March 26, 2024
    Assignee: AstraZeneca AB
    Inventor: James Michael Smith
  • Patent number: 11905287
    Abstract: Disclosed are novel analogs of cytisine, a process for their preparation, pharmaceutical compositions containing them, and their use in the prevention of or treatment of CNS disorders including addictive disorders.
    Type: Grant
    Filed: March 3, 2023
    Date of Patent: February 20, 2024
    Assignee: THE UNIVERSITY OF BRISTOL
    Inventors: Timothy Charles Gallagher, Hugo Rego Campello
  • Patent number: 11857544
    Abstract: The present disclosure provides a composition for treating or preventing symptoms, disorders, or diseases of the corneal endothelium. The present invention specifically provides a composition which is for treating or preventing symptoms, disorders, or diseases of the corneal endothelium, and includes (T)EW-7197 (N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline), a derivative thereof, a pharmaceutically acceptable salt thereof, or a solvate of any of the foregoing.
    Type: Grant
    Filed: December 13, 2018
    Date of Patent: January 2, 2024
    Assignees: THE DOSHISHA, SENJU PHARMACEUTICAL CO., LTD.
    Inventors: Noriko Koizumi, Naoki Okumura, Mayumi Yamamoto
  • Patent number: 11739102
    Abstract: Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.
    Type: Grant
    Filed: May 12, 2021
    Date of Patent: August 29, 2023
    Assignee: INCYTE CORPORATION
    Inventors: Gia Hoang, Xiaozhao Wang, Wenqing Yao
  • Patent number: 11739100
    Abstract: The invention relates to the novel products of formula (I): with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2—Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO2Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is and the isomer of configuration R,R these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
    Type: Grant
    Filed: February 21, 2019
    Date of Patent: August 29, 2023
    Assignee: SANOFI
    Inventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo
  • Patent number: 11629150
    Abstract: This invention is in the area of synthesizing pyrimidine-based compounds useful in the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
    Type: Grant
    Filed: December 14, 2020
    Date of Patent: April 18, 2023
    Assignee: G1 Therapeutics, Inc.
    Inventors: Alexander Smith, Hannah S. White, Francis Xavier Tavares, Sergiy Krasutsky, Jian-Xie Chen, Roberta L. Dorrow, Hua Zhong
  • Patent number: 11471456
    Abstract: Provided is a composition comprising a polyglycolized glyceride and a compound having the following structure (I): or a pharmaceutically acceptable salt thereof. Also provided are crystalline forms of the compound of structure (I), or a pharmaceutically acceptable salt thereof. Methods of making the same, and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated diseases, disorders or conditions are also disclosed.
    Type: Grant
    Filed: February 12, 2020
    Date of Patent: October 18, 2022
    Assignee: Sumitomo Pharma Oncology, Inc.
    Inventors: Steven L. Warner, Adam Siddiqui-Jain, Paul Flynn
  • Patent number: 11459329
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting ALK2 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with ALK2 activity such as cancer.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: October 4, 2022
    Assignee: Incyte Corporation
    Inventors: Jun Pan, Jeremy Roach, Song Mei, Chunhong He, Liangxing Wu, Wenqing Yao
  • Patent number: 11427590
    Abstract: Small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) and their use for treating neurodegenerative diseases, such as, neurodegenerative diseases associated with high levels of ceramide, including, but not limited to Alzheimer's disease (AD), HIV-associated neurocognitive disorder (HAND), multiple sclerosis (MS), and amyotrophic lateral sclerosis (ALS), and, in other aspects, for treating cancer, are provided.
    Type: Grant
    Filed: January 5, 2018
    Date of Patent: August 30, 2022
    Assignees: The Johns Hopkins University, Institute of Organic Chemistry & Biochemistry
    Inventors: Barbara Slusher, Camilo Rojas, Ajit G. Thomas, Radim Nencka, Michal Sala, Hubert Hrebabecky, Norman Haughey
  • Patent number: 11427592
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting ALK2 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with ALK2 activity such as cancer.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: August 30, 2022
    Assignee: Incyte Corporation
    Inventors: Jun Pan, Jeremy Roach, Song Mei, Chunhong He, Liangxing Wu, Wenqing Yao
  • Patent number: 11401278
    Abstract: The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: November 15, 2018
    Date of Patent: August 2, 2022
    Assignees: The Broad Institute, Inc., Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Laura Furst, Michael H. Serrano-Wu, Chris Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven J. Ferrara, Guo Wei, Patrick R. McCarren, Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Rauh, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning, Katrin Nowak-Reppel
  • Patent number: 11351156
    Abstract: PI3K signalling is the most increased pathway in human cancers. The four isoforms of PI3K are thought to be activated by different redundant mechanisms leading to a common downstream signalling. The inventors questioned this concept, by mapping differential isoform-specific downstream signalling in response to their constant selective inhibition in pancreatic cancer, a disease currently without therapy. They identified common and specific signals activated by each PI3K isoform. These data make the rational for the development of highly selective PI3K isoform drugs used in combination, instead of compounds inhibiting all PI3Ks. In particular, the inventors showed that combined p110a and 110? inhibition is the most efficient strategy for pancreatic cancer patients.
    Type: Grant
    Filed: October 12, 2018
    Date of Patent: June 7, 2022
    Assignees: INSERM, Université Paul Sabatier Toulouse III, CNRS, Klinikum Rechts der Isar der Technischen Universität München
    Inventors: Julie Guillermet-Guibert, Maximillian Reichert, Célia Cintas
  • Patent number: 11339343
    Abstract: A method for preparing a refinery fuel composition having a target octane number, comprises: (i) blending fuel components in proportions which are designed to give a refinery fuel composition with an octane number which is greater than the target octane number by a margin of less than 1; and (ii) testing the octane number of the refinery fuel composition and, if the octane number falls below the target octane number, blending the refinery fuel composition with a non-metallic octane-boosting additive. A further method comprises: (a) passing a first refinery fuel composition comprising a non-metallic octane-boosting additive to a fuel handing system, and discharging the first refinery fuel composition from the fuel handing system; and (b) passing a second refinery fuel composition to the fuel handing system.
    Type: Grant
    Filed: August 13, 2018
    Date of Patent: May 24, 2022
    Assignee: BP Oil International Limited
    Inventors: Sorin Vasile Filip, Amardeep Kaur Mudhar, Nicolaas Richard Van Wezel
  • Patent number: 11278530
    Abstract: The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt (s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of compound formula (I).
    Type: Grant
    Filed: October 26, 2018
    Date of Patent: March 22, 2022
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Anil Karbhari Shinde, Shankar Reddy Gagginapally, Durga Malleshwari Kancharla, Santosh Kumar Pandey, Renny Abraham, Venkateswarlu Jasti
  • Patent number: 11229638
    Abstract: Compounds having the following Formula I and/or Formula II and methods of their use and preparation are disclosed:
    Type: Grant
    Filed: August 20, 2018
    Date of Patent: January 25, 2022
    Assignee: Gilead Sciences, Inc.
    Inventors: Mark J. Bartlett, Britton Kenneth Corkey, Jennifer Leigh Cosman, Kristyna M. Elbel, Elfatih Elzein, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Eric Q. Parkhill, Thao Perry
  • Patent number: 11185549
    Abstract: The present invention relates to: • combinations of: * a component A: which is a PI3K kinase inhibitor, such as copanlisib, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, in particular a physiologically acceptable salt, or a mixture of same, for example; * a component B: which is an androgen receptor antagonist, such as darolutamide or enzalutamide for example; and, optionally, * one or more pharmaceutical agents C; in which optionally either or both of said components A and B are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially; • use of such combinations: * in the treatment or prophylaxis of a cancer, particularly prostate cancer, or * for the preparation of a medicament for the treatment or prophylaxis of a cancer, particularly prostate cancer; • methods of treatment or prophylaxis of a cancer, particularly prostate cancer, in a subject, comprising administering to said subject
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: November 30, 2021
    Assignees: BAYER CONSUMER CARE AG, BAYER PHARMA AKTIENGESELLSCHAFT
    Inventor: Bernard Haendler
  • Patent number: 11180509
    Abstract: Disclosed in the present invention are a thiazolidone spiro pyrimidine trione compound, a preparation method therefor and uses thereof, the compound having a structure represented by formula (I). In the formula, the definitions of the substituents are described in the specification and the claims. The thiazolidone spiro pyrimidine trione compound in the present invention has high in vivo and in vitro antibacterial activity, has better metabolic properties, and is obviously superior to existing compounds of the same kind.
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: November 23, 2021
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Yushe Yang, Yinyong Zhang, Chenghui Shi, Qian Chen
  • Patent number: 11155547
    Abstract: The present invention provides heterocyclic compounds of formula (I) that modulate biological metals and to pharmaceutical compositions containing such compounds. The invention particularly relates to compounds that modulate iron and to compounds for the treatment of diseases, particularly neurological diseases such as Parkinson's disease (PD), Alzheimer's disease (AD), Alzheimer-type dementia, Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), frontotemporal dementia (FTD) and multiple system atrophy (MSA).
    Type: Grant
    Filed: April 23, 2021
    Date of Patent: October 26, 2021
    Assignee: Alterity Therapeutics Limited
    Inventors: Silas Bond, Penelope Jane Huggins, Jack Gordon Parsons
  • Patent number: 11072619
    Abstract: A compound or its acid addition salt of the general formula (I), wherein R1 represents phenyl substituted with one or two substituents selected from the group consisting of halogen and C1-C3 alkoxyl, or 6-membered heteroaryl with 1 or 2 nitrogen atoms, which is unsubstituted or substituted with a substituent selected from the group consisting of —NH2, halogen, alkyl C1-C4, alkoxyl C1-C3, and 6-membered heterocyclyl comprising 1 or 2 heteroatoms selected from the group consisting of N and O. The compound has the activity of kinase JAK1/JAK3 inhibitor and can find use in the treatment of chronic inflammatory and autoimmunological diseases.
    Type: Grant
    Filed: May 10, 2018
    Date of Patent: July 27, 2021
    Assignee: Celon Pharma S.A.
    Inventors: Michal Mroczkiewicz, Bartosz Stypik, Anna Bujak, Krzysztof Szymczak, Pawel Gunerka, Krzysztof Dubiel, Maciej Wieczorek, Jerzy Pieczykolan
  • Patent number: 11058678
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: July 13, 2021
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Joseph Panarese, Samuel Bartlett, Katherine Chong, Yat Sun Or
  • Patent number: 10966970
    Abstract: A fused tricyclic compound and use thereof as a medicament, in particular as a medicament for the treatment and/or prevention of hepatitis B. Specifically, a compound having Formula (I) or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein each variate is as defined in specification. The compound also includes a Formula (I) or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof as a medicament, especially as a medicament for the treatment and/or prevention of hepatitis B.
    Type: Grant
    Filed: June 2, 2018
    Date of Patent: April 6, 2021
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Xinchang Liu, Qingyun Ren, Jianzhou Huang, Zhimin Xiong, Jinfeng Xiong, You Li, Yang Liu, Zhifu Zou, Guanghua Yan, Siegfried Goldmann, Yingjun Zhang
  • Patent number: 10954229
    Abstract: The present invention relates to novel compounds of formula (I), process for preparation of the same and composition comprising these compounds.
    Type: Grant
    Filed: June 23, 2020
    Date of Patent: March 23, 2021
    Assignee: MANKIND PHARMA LTD.
    Inventors: Rakesh Ishwar Patil, Jeevan Verma, Puneet Kumar, Amol Pandurang Gunjal, Himanshu Rai, Santosh Kumar Rai, Anil Kumar
  • Patent number: 10941136
    Abstract: The present invention provides a quinazoline derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same and a use thereof. The quinazoline derivative or its pharmaceutically acceptable salt has a selective inhibitory activity against the phosphatidylinositol 3-kinase delta subunit, and therefore can be usefully applied for preventing or treating cancer, along with avoiding side effects such as lymphopenia-associated inflammatory responses.
    Type: Grant
    Filed: April 26, 2017
    Date of Patent: March 9, 2021
    Assignee: YUHAN CORPORATION
    Inventors: Young-Hwan Kim, Tae-Dong Han, Dong-Hoon Kim, Eun-Hye Jung, Su-Bin Choi, Eui-Chul Lee, Won-Ee Chong, Jin-Hwi Park, Jun-Chul Park, Ho-Woong Kang, Ji-Yeong Gal, Chan-Sun Park, Jong-Gyun Kim, Su-Youn Nam
  • Patent number: 10941151
    Abstract: The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.
    Type: Grant
    Filed: May 21, 2020
    Date of Patent: March 9, 2021
    Assignee: Ogeda SA
    Inventors: Hamid R. Hoveyda, Guillaume Dutheuil, Graeme Lovat Fraser, Marie-Odile Roy, Mohamed El Bousmaqui, Frederic Batt
  • Patent number: 10849901
    Abstract: Disclosed herein are compounds and methods for inhibiting Arf6. Pharmaceutical compositions and methods for treating a subject with an inhibitor of Arf6 are also disclosed herein.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: December 1, 2020
    Assignees: Navigen, Inc., The University of Utah Research Foundation
    Inventors: Kirill Ostanin, Mark Shenderovich, Ashok Bajji, Christopher L. Cioffi, Neil Moss, Hariprasad Vankayalapati, Dean Li
  • Patent number: 10821103
    Abstract: The present invention includes substituted pyridinone-containing tricyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infection in a patient. In certain embodiments, the compounds and compositions of the invention inhibit and/or reduce HBsAg secretion.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: November 3, 2020
    Assignee: Arbutus Biopharma Corporation
    Inventors: Laurèn Danielle Bailey, Yingzhi Bi, Shuai Chen, Bruce D. Dorsey, Dimitar B. Gotchev, Richard James Holland, Ramesh Kakarla, Duyan Nguyen, Mark Christopher Wood
  • Patent number: 10822352
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: November 3, 2020
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang
  • Patent number: 10765687
    Abstract: A compound having an antiviral activity for inhibiting release of an enveloped virus from a cell is disclosed, including methods of inhibiting release of an enveloped virus from a cell. The antiviral activity of the compound includes inhibiting formation of an associative complex or disrupting formation of an associative complex. The associative complex comprises an L-domain motif of the enveloped virus and at least one cellular polypeptide, or fragment thereof, capable of binding the L-domain motif of the enveloped virus.
    Type: Grant
    Filed: March 22, 2019
    Date of Patent: September 8, 2020
    Assignees: Northwestern University, THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK
    Inventors: Jonathan Leis, Carol Carter
  • Patent number: 10759794
    Abstract: The present application relates to novel 2-phenyl-3-(piperazinomethyl)imidazo[1,2-a]pyridine derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of respiratory disorders including, sleep-related respiratory disorders such as obstructive sleep apnoeas and central sleep apnoeas and snoring.
    Type: Grant
    Filed: December 7, 2016
    Date of Patent: September 1, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Martina Delbeck, Michael Hahn, Thomas Müller, Heinrich Meier, Klemens Lustig, Johanna Mosig, Luisella Toschi, Udo Albus, Doris Gehring, Björn Rosenstein
  • Patent number: 10752622
    Abstract: The present invention relates to novel compounds of formula (I), process for preparation of the same and composition comprising these compounds.
    Type: Grant
    Filed: December 24, 2018
    Date of Patent: August 25, 2020
    Assignee: MANKIND PHARMA LTD.
    Inventors: Rakesh Ishwar Patil, Jeevan Verma, Puneet Kumar, Amol Pandurang Gunjal, Himanshu Rai, Santosh Kumar Rai, Anil Kumar
  • Patent number: 10738056
    Abstract: The present invention relates to pyrazolopyrimidinone compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating autoimmune, inflammatory, and neurodegenerative diseases by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: September 14, 2018
    Date of Patent: August 11, 2020
    Assignee: Aduro BioTech Inc.
    Inventors: Chudi Obioma Ndubaku, George Edwin Katibah, Tucker Curran Roberts, Leonard Sung, Stephane Ciblat, Franck Raeppel, Vu Linh Ly, Yeeman K. Ramtohul, Taras Rybak, Mariam Zaky, Laura Gillard, Hossein Ismaili
  • Patent number: 10653695
    Abstract: Disclosed are oral pharmaceutical compositions of neflamapimod that exhibit suitable exposure for administration in humans and/or that maintain a desirable dissolution profile under standard storage conditions.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: May 19, 2020
    Assignee: EIP Pharma, LLC
    Inventors: John Jahangir Alam, Jeffrey Douglas Wilson
  • Patent number: 10568879
    Abstract: A compound according to Formula I: wherein R1, LA, CyA, RA, R2, R3, and R4 are as described herein. The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions, pain, neuroinflammatory conditions, neurodegenerative conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, cardiovascular diseases, leukemia, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
    Type: Grant
    Filed: April 19, 2016
    Date of Patent: February 25, 2020
    Assignee: GALAPAGOS NV
    Inventors: Christel Jeanne Marie Menet, Julien Georges Pierre-Olivier Doyon, Pieter Isabelle Roger Claes, Brigitte Allart, Maxim Maria Paul De Wachter, Giovanni Alessandro Tricarico
  • Patent number: 10556869
    Abstract: The present invention relates to a process for providing the compound of formula I, comprising the step of reacting a compound of formula VII with a base in the presence of an alkaline- or alkaline earth metal salt (MX), wherein LG is a leaving group. The presence of an alkaline- or alkaline earth metal salt was surprisingly found to render said reaction highly reliable in terms of the yield and purity of the compound of formula I obtained. In a further aspect, the present invention relates to the compound of formula I, having less than an amount of 1.50% or less than an amount of 1.25% or less than an amount of 1.00% or less than an amount of 0.75% or less than an amount of 0.50% or less than an amount of 0.25% or less than an amount of 0.10% of the compound of formula VIII.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: February 11, 2020
    Assignee: Novartis AG
    Inventors: Andreas Bertogg, Hanspeter Schilling
  • Patent number: 10457683
    Abstract: The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells.
    Type: Grant
    Filed: April 12, 2018
    Date of Patent: October 29, 2019
    Assignee: Magenta Therapeutics Inc.
    Inventor: Arthur Glenn Romero
  • Patent number: 10399995
    Abstract: The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, useful as a BACE1 inhibitor.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: September 3, 2019
    Assignee: Eli Lilly and Company
    Inventors: Steven James Green, Erik James Hembre, II, Dustin James Mergott
  • Patent number: 10364245
    Abstract: Compounds of formula (I) defined herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Grant
    Filed: May 23, 2018
    Date of Patent: July 30, 2019
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Carmelida Capaldi, Elisabetta Armani, Christopher Hurley, Barbara Giuseppina Avitabile-Woo, Roberta Lanaro, Neil Stuart Jennings
  • Patent number: 10351572
    Abstract: The disclosure relates to aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as methods of expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides methods of synthesizing aryl hydrocarbon receptor antagonists, such as substituted imidazopyridines and imidazopyrazines, as well as kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells.
    Type: Grant
    Filed: February 8, 2019
    Date of Patent: July 16, 2019
    Assignee: Magenta Therapeutics Inc.
    Inventor: Arthur Glenn Romero
  • Patent number: 10342795
    Abstract: The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrimidine derivatives and 2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives of formula (I) and also compounds of formula (I?) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as ROS1 inhibitors. The invention further relates to processes for preparing novel compounds of the present invention, pharmaceutical compositions comprising compounds of the present invention as an active ingredient as well as the use of compounds of the present invention as a medicament.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: July 9, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Laurence Anne Mevellec, Matthieu Ludovic Jeanty, Thierry Francois Alain Jean Jousseaume
  • Patent number: 10335411
    Abstract: Disclosed are methods for the treatment of cancer in patients in need of such treatment. The methods comprise administering to such a patient an ubiquitin-activating enzyme (UAE) inhibitor such as ((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(3-(trifluoromethylthio) phenyl)pyrazolo[1,5-a]pyrimidin-7-ylamino)cyclopentyl)methyl sulfamate (Compound 1) or a pharmaceutically acceptable salt in combination with radiation. Also disclosed are medicaments for use in the treatment of cancer.
    Type: Grant
    Filed: October 23, 2015
    Date of Patent: July 2, 2019
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Neil Bence, Marc Hyer, Michael Milhollen, Vivek Samnotra, Sergio Luis Santillana Soto, Darshan Sappal
  • Patent number: 10328066
    Abstract: The present disclosure pertains to a pharmaceutical combination comprising (a) an alpha-isoform specific PI3K inhibitor, (b) a cyclin dependent kinase 4/6 (CDK4/6) inhibitor, and (c) an antimetabolite antineoplastic agent; combined preparations and pharmaceutical compositions thereof; the uses of such a combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.
    Type: Grant
    Filed: August 24, 2016
    Date of Patent: June 25, 2019
    Assignee: Novartis AG
    Inventors: Giordano Caponigro, Thomas Horn-Spirohn, Joseph Lehar
  • Patent number: 10258615
    Abstract: The present invention provides a method of treating or ameliorating a neurodegenerative disease in a mammal, the method comprising administering to the mammal a therapeutically effective amount of a neurodegenerative disease drug, wherein the drug is a substrate of an ABC transporter inhibitor, wherein the mammal is further administered a therapeutically effective amount of an ABC transporter inhibitor, whereby the neurodegenerative disease is treated in the mammal. In certain embodiments, the neurodegenerative disease comprises at least one selected from the group consisting of spinal cord injury, Alzheimer's disease, Parkinson's disease, Huntington's disease, prion disease, amyotrophic lateral sclerosis, a tauopathy, and chronic traumatic encephalopathy.
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: April 16, 2019
    Assignee: Thomas Jefferson University
    Inventors: Davide Trotti, Piera Pasinelli, Michael R. Jablonski
  • Patent number: 10253043
    Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO 2 Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: April 9, 2019
    Assignee: SANOFI
    Inventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo
  • Patent number: 10208030
    Abstract: The present invention relates to novel compounds of formula (I), process for preparation of the same and composition comprising these compounds.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: February 19, 2019
    Assignee: Mankind Pharma Ltd.
    Inventors: Rakesh Ishwar Patil, Jeevan Verma, Puneet Kumar, Amol Pandurang Gunjal, Himanshu Rai, Santosh Kumar Rai, Anil Kumar
  • Patent number: RE49594
    Abstract: This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.
    Type: Grant
    Filed: May 4, 2020
    Date of Patent: August 1, 2023
    Assignee: RESEARCH TRIANGLE INSTITUTE
    Inventors: Scott P. Runyon, Rangan Maitra, Sanju Narayanan, James Barnwell Thomas, Kenneth S. Rehder, Srinivas Olepu