Patents Examined by Bruck Kifle
  • Macrocyclic fluorine substituted indole derivatives
    Patent number: 11286263
    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: March 29, 2022
    Assignees: The Broad Institute, Inc., Bayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
    Inventors: Steven James Ferrara, Michael H. Serrano-Wu, Chris Lemke, David McKinney, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Laura Furst, Guo Wei, Patrick Ryan McCarren, Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Sack, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning
  • 5-fluorouracil derivatives, preparation methods and uses thereof
    Patent number: 11279678
    Abstract: Disclosed is a 5-fluorouracil derivative having the molecular structure shown in general formula VI, in which Ra and Rb groups are an alkoxy group or a fluorine-substituted alkoxy group having 1, 2, 3, or 4 carbon atoms, and are mono-, bis-, tri-, tetra- or penta-substituted on a phenyl group; a linking group L1 is an alkyl or alkenyl group having 1, 2, 3, or 4 carbon atoms, a linking group L2 is oxygen, or an alkyl or alkoxy group having 1, 2, 3, or 4 carbon atoms, or an amino acid, or an alkyl group having 1, 2, 3, or 4 carbon atoms containing an amino moiety, or a furyl group, and an X group is O or —NH—. Further disclosed is a method for preparing such a derivative and a use of the same in the treatment of cancer, tumor diseases, and diseases caused by abnormal neovascularization in a human or non-human mammal, and a medicament or a composition containing the 5-fluorouracil derivative.
    Type: Grant
    Filed: November 9, 2017
    Date of Patent: March 22, 2022
    Inventors: Fanhong Wu, Jinwen Huang, Jiujiu Zhou, Wan Pang, Lei Zhao, Zhonglin Ma, Zhikai Zhang, Xiaodong Yu, Jianyue Wu
  • Pentacyclic heterocycles
    Patent number: 11267821
    Abstract: The present invention provides compounds represented by formulas (I) to (XVII) or pharmaceutically acceptable salts thereof:
    Type: Grant
    Filed: March 3, 2020
    Date of Patent: March 8, 2022
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yoshiaki Ohashi, Yoshihiko Norimine, Tamaki Hoshikawa, Yu Yoshida, Yoshihisa Kobayashi, Nobuhiro Sato, Koji Hagiwara, Nobuaki Sato, Shinsuke Hirota, Takaaki Harada, Hikaru Yoshimura
  • Solid forms of (4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl) piperazine-1-yl)(1-hydroxycyclopropyl)methanone
    Patent number: 11267805
    Abstract: The present disclosure reports solid forms of (4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone:
    Type: Grant
    Filed: August 28, 2020
    Date of Patent: March 8, 2022
    Assignee: FORMA Therapeutics, Inc.
    Inventors: George P. Luke, Stephen Hubbs, Matthew W. Martin, Shawn E. R. Schiller, Robert Wenslow, Yawei Shi, Jun Huang
  • Pyrazole O-linked carbamoyl cyclohexyl acids as LPA antagonists
    Patent number: 11261174
    Abstract: The present invention provides compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
    Type: Grant
    Filed: December 18, 2018
    Date of Patent: March 1, 2022
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter Tai Wah Cheng, Jun Li, Yan Shi, Ying Wang, Hao Zhang, Lawrence J. Kennedy, Steven J. Walker, Ramesh Babu Reddigunta
  • Plinabulin compositions
    Patent number: 11254657
    Abstract: Disclosed herein are plinabulin polymorphs, compositions, their use and preparation as therapeutic agents. In particular, some embodiments relate to plinabulin monohydrate in a crystalline form.
    Type: Grant
    Filed: February 3, 2020
    Date of Patent: February 22, 2022
    Assignee: BeyondSpring Pharmaceuticals, Inc.
    Inventors: Lan Huang, Aniruddh Singh
  • Pyrimidine derivative having effect of inhibiting cancer cell growth and pharmaceutical composition containing same
    Patent number: 11248003
    Abstract: A novel pyrimidine derivative compound and a salt thereof are disclosed. The pyrimidine derivative compound effectively inhibits the growth of C797S mutant EGFR-expressed and MET-amplified cancer cells, which are the main resistance mechanisms of third generation EGFR anticancer agents, and thus may be effectively used in the treatment of lung cancer.
    Type: Grant
    Filed: December 6, 2018
    Date of Patent: February 15, 2022
    Assignee: ONCOBIX CO., LTD.
    Inventors: Sung-Eun Kim, Sunho Lee, Rengasamy Rajesh, Dae Ho Kang, Hyung Chui Ryu, Jae-Sun Kim, Sangryul Lee, Kyong Cheol Kim, Jin Kyung Rho, Jae Cheol Lee
  • Degradation of cyclin-dependent kinase 8 (CDK8) by conjugation of CDK8 inhibitors with E3 ligase ligand and methods of use
    Patent number: 11247991
    Abstract: The present application provides bifunctional compounds of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 8 (CDK8). The present application also relates to methods for the targeted degradation of CDK8 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 which can be utilized in the treatment of disorders modulated by CDK8.
    Type: Grant
    Filed: October 29, 2020
    Date of Patent: February 15, 2022
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski
  • Thermally activated delayed fluorescent material based on 9,10-dihydro-9,9-dimethylacridine analogues for prolonging device longevity
    Patent number: 11245078
    Abstract: Thermally activated delayed fluorescent compounds and uses thereof are described. The thermally activated delayed fluorescent compounds are an analogues of 9,10-dihydro-9,9-dimethylacridine compounds.
    Type: Grant
    Filed: February 19, 2019
    Date of Patent: February 8, 2022
    Assignee: Arizona Board of Regents on behalf of Arizona State University
    Inventors: Jian Li, Diajun Feng
  • Ethynyl derivatives
    Patent number: 11242349
    Abstract: The present invention relates to compounds that may be used in the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression or diabetes type 2.
    Type: Grant
    Filed: May 1, 2020
    Date of Patent: February 8, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Barbara Biemans, Georg Jaeschke, Antonio Ricci, Daniel Rueher, Fionn O'Hara
  • Biocompatible modular tetrazine platform
    Patent number: 11242359
    Abstract: A modular tetrazine platform, can be used as diagnostic, theragnostic agent and/or medicinal product. An inverse electron demand Diels-Alder reaction can be used for synthesizing bifunctionalized tetrazines, which can be obtained from monofunctionalised tetrazines.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: February 8, 2022
    Assignees: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITÉ DE BOURGOGNE
    Inventors: Victor Goncalves, Franck Denat, Claire Bernhard, Coline Canovas
  • Crystal forms of demethyleneberberine hydrochloride and preparation method therefor
    Patent number: 11242340
    Abstract: Provided are four crystal forms, A, B, C and D, of demethyleneberberine hydrochloride, and a preparation method therefor, and further provided are X-ray powder diffraction characteristic absorption peaks, infrared absorption peaks and DSC spectra of the four crystal forms. The X-ray powder diffraction characteristic diffraction peaks of the crystal forms are at about 8.205°, 8.805°, 10.817°, 14.835°, 15.479°, 16.668°, 17.492°, 18.529°, 20.656°, 21.536°, 23.538°, 25.657°, 26.192°, and 28.808°. A preparation method for the four crystal forms of the demethyleneberberine hydrochloride is also involved. The preparation method has a simple process, a high yield and a low cost; and has a high product purity and a stable quality.
    Type: Grant
    Filed: July 12, 2018
    Date of Patent: February 8, 2022
    Assignee: CHINA PHARMACEUTICAL UNIVERSITY
    Inventors: Yubin Zhang, Yuanqiang Zhang, Miao Zhang, Qingxia Li
  • Tetrahydro-benzo[d]azepine derivatives as GPR120 modulators
    Patent number: 11220483
    Abstract: Novel tetrahydroisoquinoline and tetrahydrobenzazepine compounds of formula (I) capable of modulating the G-protein-coupled receptor GPR120, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as of diabetes, inflammation, obesity and metabolic diseases.
    Type: Grant
    Filed: March 26, 2018
    Date of Patent: January 11, 2022
    Assignee: CALDAN THERAPEUTICS LTD
    Inventors: Jane Brown, Stephen Connolly, Steffen V. F. Hansen, Gavin Milne, Bharat Shimpukade, Don Smyth, Gerard Thomas, Trond Ulven, Matjaz Brvar, Aaron Rigby
  • Imidazo[1,5-a]pyrazine derivatives as PI3Kdelta inhibitors
    Patent number: 11220506
    Abstract: Disclosed is a compound of Formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions comprising thereof. Also disclosed is a method of treating PI3K? related disorders or diseases by using the compound disclosed herein.
    Type: Grant
    Filed: September 7, 2018
    Date of Patent: January 11, 2022
    Assignee: BEIGENE, LTD.
    Inventors: Jing Li, Haibo Zhao, Zhiwei Wang
  • Process for the preparation of rucaparib and novel synthesis intermediates
    Patent number: 11220507
    Abstract: The present invention relates to a process for the preparation of rucaparib; the invention also refers to novel intermediates of synthesis as well as their use in the preparation of i.a. rucaparib.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: January 11, 2022
    Assignee: Advitech Advisory and Technologies SA
    Inventors: Brent Christopher Beck, Joe B. Perales, Jason D. Speake, Ilaria Ferrando
  • Industrial process of mono-alkylating piperidine nitrogen in piperidine derivative with deuterated-lower-alkyl
    Patent number: 11214545
    Abstract: The present invention relates to a method of mono-alkylating a piperidine nitrogen in a piperidine derivative with a deuterated lower-alkyl, which comprises protecting the piperidine nitrogen with an aralkyl protective group, lower-alkylating the piperidine nitrogen with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl protective group.
    Type: Grant
    Filed: September 6, 2018
    Date of Patent: January 4, 2022
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Yuya Nakai, Masashi Hayashi, Wataru Mitsuhashi
  • Compound, compositions, and methods
    Patent number: 11214565
    Abstract: Compounds having activity as LRRK2 inhibitors are disclosed. The compounds are of formula (I) including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds are also disclosed.
    Type: Grant
    Filed: November 18, 2016
    Date of Patent: January 4, 2022
    Assignee: DENALI THERAPEUTICS INC.
    Inventors: Anthony A. Estrada, Jianwen A. Feng, Joseph P. Lyssikatos, Zachary K. Sweeney, Javier de Vicente Fidalgo
  • Process for the purification of caprolactam from a solution of crude caprolactam without organic solvent extraction
    Patent number: 11208380
    Abstract: The present invention relates to a process for purifying caprolactam from solutions of crude caprolactam by a direct treatment with one or more alkaline compounds of polyvalent metals, preferably bivalent and trivalent, without resorting to organic solvent extraction as used in the usual purification process. A further subject of the present invention is a facility devoid of a unit for organic solvent extraction and designed to carry out the caprolactam purification process described herein.
    Type: Grant
    Filed: August 21, 2020
    Date of Patent: December 28, 2021
    Assignee: AquafilSLO d.o.o.
    Inventors: Anacleto Dal Moro, Michele Cecchetto, Denis Jahic, Vid Margon
  • Substituted xanthines and methods of use thereof
    Patent number: 11208409
    Abstract: Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
    Type: Grant
    Filed: April 29, 2019
    Date of Patent: December 28, 2021
    Assignee: Hydra Biosciences, LLC
    Inventors: Bertrand L. Chenard, Randall J. Gallaschun
  • Nitrogenous tricyclic compounds and uses thereof in medicine
    Patent number: 11208418
    Abstract: Nitrogenous tricyclic compounds and uses thereof in medicine, in particular, a novel nitrogenous tricyclic compound used as an FXR active regulator and a stereoisomer, a geometrical isomer, a tautomer, a N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and use of the compound in the manufacture of a drug for treating a disease and/or disorder regulated by FXR. A pharmaceutically acceptable composition containing the compound and a method of treating a disease and/or disorder mediated by FXR comprising administering the compound or pharmaceutical composition thereof.
    Type: Grant
    Filed: January 28, 2019
    Date of Patent: December 28, 2021
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Xinye Yang, Xiaojun Wang, Junwen Wu, Hong Chen, Shengtian Cao, Yingjun Zhang