Patents Examined by Noble E Jarrell
  • Patent number: 10807945
    Abstract: The present invention provides a 1,4-disubstituted imidazole derivative of formula (1?) wherein ring Q1 is optionally-substituted C6-10 aryl group, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is optionally-substituted C1-4 alkylene group; W2 is —NR3aC(O)— wherein R3a is hydrogen atom or C1-6alkyl group, etc.; ring Q2 is 5- to 10-membered heteroaryl group, etc.; W3 is optionally-substituted C1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R4 is independently halogen atom, optionally-substituted C1-6 alkyl group, etc.; R5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.
    Type: Grant
    Filed: June 21, 2016
    Date of Patent: October 20, 2020
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Hitoshi Ban, Manabu Kusagi, Shingo Tojo, Futoshi Hasegawa, Miki Hashizume
  • Patent number: 10806737
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of FLT3 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein FLT3, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of the target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: October 20, 2020
    Assignees: Arvinas Operations, Inc., Yale University
    Inventors: Andrew P. Crew, Keith R. Hornberger, Craig M. Crews, George Burslem
  • Patent number: 10807962
    Abstract: The present invention concerns a process for the preparation of firocoxib, i.e. 3-(cyclopropylmethoxy)-5,5-dimethyl-4-(4-methylsulfonylphenyl)-furan-2-one, comprising steps (a)-(g), wherein the process provides for step (d) of the reaction of a new intermediate, i.e. 2-methyl-1-[4-(methylsulfanyl)phenyl]-1-oxopropan-2-yl (acetyloxy)acetate (compound VII) in the same organic solvent of step (a) in the presence of a catalyst and a phase transfer catalyst solution in the same organic solvent with hydrogen peroxide.
    Type: Grant
    Filed: April 14, 2017
    Date of Patent: October 20, 2020
    Assignee: COSMA S.P.A.
    Inventors: Paolo Celestini, Sergio Baretti, Enrica Pizzatti
  • Patent number: 10800730
    Abstract: The invention provides a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.
    Type: Grant
    Filed: September 20, 2018
    Date of Patent: October 13, 2020
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Robert W. Huigens, III, Karen C. Morrison, Robert W. Hicklin, II, Timothy A. Flood, Jr.
  • Patent number: 10800788
    Abstract: The present invention relates to a novel 4-(aryl)-N-(3-alkoxyfuro[2,3-b]pyrazin-2-yl)-piperazine-1-carboxamide derivative compound useful in the prevention or treatment of cancer; a preparation method thereof; and a pharmaceutical composition comprising the same. The novel 4-(aryl)-N-(3-alkoxyfuro[2,3-b]pyrazin-2-yl)-piperazine-1-carboxamide derivative compound of the present invention can effectively inhibit the growth of proliferating cells, and thus can be useful in the prevention or treatment of cancer.
    Type: Grant
    Filed: June 9, 2017
    Date of Patent: October 13, 2020
    Assignee: LSK NRDO CO., LTD.
    Inventors: Young-Dae Gong, Soo-Youl Kim, Eun Sil Lee, Tae-Sung Koo, Nam-Sook Kang, Na Yeon Kim
  • Patent number: 10799603
    Abstract: The present invention generally relates to assays of enzymes responsible for phosphoregulation including kinases (such as protein kinases, which mediate protein and peptide phosphorylation) and phosphatases (such as protein phosphatases, which mediate protein and peptide dephosphorylation). Certain aspects of the invention use lanthanide ions such as europium ions that exhibit chelation-enhanced luminescence. Phosphorylation of a peptide by a kinase may cause a complex to form between the lanthanide ion, the phosphate group, and a reporter group such as a hydroxyquinoline, which results in luminescence when in the complexed state. Thus, in certain embodiments, determination of luminescence may be indicative of kinase activity. Certain embodiments also include the use of substrates for detection of phosphatase activity, where dephosphorylation results in a loss of signal assay.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: October 13, 2020
    Assignees: Massachusetts Institute of Technology, Centre National de la Recherche Scientifique, ENSCM, UNIVERSITE DE MONTPELLIER
    Inventors: Barbara Imperiali, Juan Antonio González Vera
  • Patent number: 10800747
    Abstract: The present invention relates to macrocyclic compounds which are capable of selective binding to a target saccharide (e.g. glucose), making them particularly well suited for use in saccharide sensing applications. The present invention also relates to processes for the preparation of said compounds, to compositions and devices comprising them, and to their use in the detection of a target saccharide.
    Type: Grant
    Filed: March 15, 2018
    Date of Patent: October 13, 2020
    Assignee: ZIYLO LTD
    Inventors: Anthony Davis, Robert Tromans, Miriam Ruth Wilson, Michael Glen Orchard, Andrew Michael Chapman, Michael Roger Tomsett, Johnathan Vincent Matlock
  • Patent number: 10800745
    Abstract: The present disclosure relates to novel synthetic method of making 1, 4-diazo N-heterocycles via intermolecular amphoteric diamination of allenes, and to the compounds made by the novel synthetic method.
    Type: Grant
    Filed: July 13, 2018
    Date of Patent: October 13, 2020
    Assignee: Purdue Research Foundation
    Inventors: Mingji Dai, Zhishi Ye
  • Patent number: 10792372
    Abstract: The invention relates to novel cell-binding agent-maytansinoid conjugate having a self-immolative peptide linker and more specifically to conjugates of formula (I). The invention also provides novel maytansinoid compounds of formula (II), (III), (IV) or (V). The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: October 6, 2020
    Assignee: IMMUNOGEN, INC.
    Inventor: Wayne C. Widdison
  • Patent number: 10774072
    Abstract: The present invention relates to a method for producing N-substituted sulfonamide compounds including a step of reacting a sulfonamide compound of general formula (1) with a halogenated organic compound of general formula (2) in the presence of cesium carbonate or potassium carbonate in an organic solvent to produce an N-substituted sulfonamide compound of general formula (3).
    Type: Grant
    Filed: August 30, 2019
    Date of Patent: September 15, 2020
    Assignee: UBE INDUSTRIES, LTD.
    Inventors: Yasuhito Yamamoto, Masayoshi Oue, Yukinori Wada
  • Patent number: 10759809
    Abstract: The present invention relates to a compound represented by formula I and a non-toxic pharmaceutically acceptable salt thereof. In formula (I), R1 is H, CH3 or deuterated methyl (CD3); R2 is CH3 or CH2CH3; R3, R4 and R5 are each independently H or deuterium (D); when R1 is H or CH3, at least one of R3, R4 and R5 is D.
    Type: Grant
    Filed: January 26, 2018
    Date of Patent: September 1, 2020
    Inventors: Bohua Zhong, Jianming Wang, Jiajun Yang
  • Patent number: 10752642
    Abstract: The present compositions and methods generally relate to the treatment of diseases, such as idiopathic pulmonary fibrosis (IPF) and neurodegenerative diseases related to tau aggregation.
    Type: Grant
    Filed: April 30, 2019
    Date of Patent: August 25, 2020
    Assignee: George Mason University
    Inventors: Mikell Paige, Yun Michael Shim, Young-Ok You
  • Patent number: 10751340
    Abstract: Disclosed herein are methods and materials for improving brain function and/or promoting neurogenesis m a patient suffering from impaired brain function. Specifically exemplified herein ls the co-administration of phenserine and NBI-18. A method of treating a neurodegenerative disease in a patient in need thereof, said method comprising co-administering to the patient phenserine, or pharmaceutically acceptable salt thereof, and NBI-18, or pharmaceutically acceptable salt thereof, in respective amounts and frequency such that they work together to improve brain function or induce neurogenesis in the patient.
    Type: Grant
    Filed: June 6, 2017
    Date of Patent: August 25, 2020
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventor: Kiminobu Sugaya
  • Patent number: 10745418
    Abstract: Provided herein are supramolecular assemblies, the supramolecular assemblies comprising a racemic mixture of rigid macrocycles capable of interacting through [C—H . . . O] hydrogen bonds. Also provided herein are methods for preparing supramolecular assemblies, the method comprising providing a mixture of rigid macrocycles capable of interacting through [C—H . . . O] hydrogen bonds, the mixture of rigid macrocycles comprising a first rigid macrocycle enantiomer and a second rigid macrocycle enantiomer, and providing a solvent.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: August 18, 2020
    Assignee: Northwestern University
    Inventors: James Fraser Stoddart, Zhichang Liu
  • Patent number: 10745416
    Abstract: The present disclosure relates to certain macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat disease, such as cancer.
    Type: Grant
    Filed: January 30, 2020
    Date of Patent: August 18, 2020
    Assignee: Turning Point Therapeutics, Inc.
    Inventors: Evan W. Rogers, Jingrong J. Cui, Dayong Zhai, Han Zhang, Jane Ung, Wei Deng, Jeffrey Whitten
  • Patent number: 10738086
    Abstract: Described herein are compositions and methods for use in targeted drug delivery using cell-surface receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in treating disease states caused by pathogenic cell populations.
    Type: Grant
    Filed: February 13, 2017
    Date of Patent: August 11, 2020
    Assignee: Endocyte Inc.
    Inventors: Christopher Paul Leamon, Iontcho Radoslavov Vlahov, Hari Krishna R. Santhapuram, Paul Joseph Kleindl, Kevin Yu Wang, Fei You
  • Patent number: 10730850
    Abstract: The invention relates to new heteroaryl derivatives of the formula wherein X is selected from the group consisting of: N and CH; X is selected from the group consisting of: N and CF; (with the proviso that at least one of X1 and X2 is N), and A is as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: March 3, 2016
    Date of Patent: August 4, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Andreas Blum, Stefan Peters
  • Patent number: 10732108
    Abstract: Water soluble fluorogenic sensors for detecting a hydrazine analyte are provided. Aspects of the fluorogenic sensors include at least one water soluble group and a hydrazine reactive group. Methods of evaluating a sample for the presence of a hydrazine analyte and methods of detecting hydrazine diffusion across a phospholipid membrane are provided. Kits for practicing the subject methods are also provided.
    Type: Grant
    Filed: July 26, 2018
    Date of Patent: August 4, 2020
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Noah Burns, Steven R. Shuken
  • Patent number: 10730838
    Abstract: Pharmaceutical and chemical intermediates and related chemistry providing a green preparation method for quinoline compounds. N-Substituted arylamine derivatives as raw material react with arylacetylene or arylethylene derivatives for 24 hours at 80° C.-160° C. in the presence of Brønsted acid catalyst and oxidant without solvent, to obtain quinoline compounds. Beneficial characteristics include convenient operation, mild reaction conditions, environmentally friendly property and possibility of realizing industrialization, and provides the quinoline compounds in high yields. The quinoline compounds synthesized by this method can be further functionalized into various compounds which have potential applications in development and research of natural products, functional materials and fine chemicals.
    Type: Grant
    Filed: June 7, 2018
    Date of Patent: August 4, 2020
    Inventors: Sheng Zhang, Ming Bao, Waqar Ahmed, Xiaoqiang Yu, Xiujuan Feng
  • Patent number: 10729688
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs 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: March 27, 2019
    Date of Patent: August 4, 2020
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Jorden Kass, Byung-Chul Suh, Hui Cao, Wei Li, Xiaowen Peng, Xuri Gao, Yat Sun Or