Patents Examined by Erich A. Leeser
  • Further substituted triazolo quinoxaline derivatives
    Patent number: 10981918
    Abstract: The present invention relates to compounds according to general formula (I) which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
    Type: Grant
    Filed: July 19, 2019
    Date of Patent: April 20, 2021
    Assignee: GRÜNENTHAL GMBH
    Inventors: Florian Jakob, Jo Alen, Simon Lucas, Tobias Craan, Ingo Konetzki, Achim Kless, Stefan Schunk, Paul Ratcliffe, Sebastian Wachten, Simon Cruwys
  • Pyrimidine seven-membered-ring compounds, preparation method therefor, pharmaceutical composition thereof, and uses thereof
    Patent number: 10975092
    Abstract: The present invention relates to compounds (I) capable of inhibiting the Mst1/2 protein kinase activity, a preparation method therefor, a pharmaceutical composition comprising the compounds, and uses of the compounds and the pharmaceutical composition comprising the compounds in the preparation of drugs for prompting repair and regeneration of tissues and organs, prompting stem cell proliferation and somatic cell dedifferentiation, immunosuppression, and preventing or treating diseases related to nervous disorders and local ischemia.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: April 13, 2021
    Assignee: Anhui New Star Pharmaceutical Development Co., Ltd.
    Inventors: Xianming Deng, Dawang Zhou, Lanfen Chen, Zhixiang He, Fuqin Fan
  • Fused 1,4-diazepines as BET protein degraders
    Patent number: 10975093
    Abstract: The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3, R4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.
    Type: Grant
    Filed: September 13, 2017
    Date of Patent: April 13, 2021
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Yang Hu, Chong Qin, Fuming Xu, Jiantao Hu, Weiguo Xiang, Bing Zhou
  • 3-substituted propionic acids as ?V integrin inhibitors
    Patent number: 10968219
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to ?v-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of ay-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: April 6, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guohua Zhao, Pratik Devasthale, Xiang-Yang Ye, Kumaravel Selvakumar, Suresh Dhanusu, Palanikumar Balasubramanian, Leatte R. Guernon, Rita Civiello, Xiaojun Han, Michael Frederick Parker, Swanee E. Jacutin-Porte
  • 4-(P-quinonyl)-2-hydroxybutanamide derivatives for treatment of mitochondrial diseases
    Patent number: 10968166
    Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinoly)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: April 6, 2021
    Assignee: PTC THERAPEUTICS, INC.
    Inventors: Orion D. Jankowski, Kieron E. Wesson, Paul Mollard, William D. Shrader
  • Flame retardants
    Patent number: 10968204
    Abstract: The invention relates to flame retardants comprising atriazine compound according to Formula 1: (1) with R=phosphite substituted with alkyl, functionalized alkyl, aryl, functionalized aryl, except halogen-substituted alkyl or aryl; R?=alkylene, arylene, alkoxy or aryloxy, all unsubstituted or functionalized, except halogen-substituted; X1 and X2=hetero atoms and X1=X2 or X1 not=X2 and to specific triazine compounds as such.
    Type: Grant
    Filed: October 9, 2017
    Date of Patent: April 6, 2021
    Assignees: Bruag Fire Protection AG, EMPA Swiss Federal Laboratories for Materials Science and Technology
    Inventors: Khalifah Salmeia, Sabyasachi Gaan, Markus Brühwiler
  • JAK1 selective inhibitors
    Patent number: 10961228
    Abstract: Disclosed herein are compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1-R8 have any of the meanings defined herein. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I) and methods of using the same.
    Type: Grant
    Filed: January 16, 2018
    Date of Patent: March 30, 2021
    Assignee: ASTRAZENECA AB
    Inventors: Karl Magnus Nilsson, Annika Birgitta Margareta Astrand, Anna Ingrid Kristina Berggren, Johan R. Johansson, Matti Juhani Lepisto, Sameer Pralhad Kawatkar, Qibin Su, Jason Grant Kettle
  • Pyrazolopyrimidine derivatives as kinase inhibitor
    Patent number: 10961247
    Abstract: The present invention relates to a pyrazolopyrimidine derivative, or a pharmaceutically acceptable salt thereof. The compound according to the present invention can be usefully used for the prevention or treatment of diseases which are associated with kinase inhibitory actions.
    Type: Grant
    Filed: June 30, 2017
    Date of Patent: March 30, 2021
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: In Woo Kim, Mi Ryeong Han, Jakyung Yoo, Yun Ju Oh, Ji Duck Kim, Nam Youn Kim, Sun Ah Jun, Jun Hee Lee, Joon Seok Park
  • Hybrid cyclic libraries and screens thereof
    Patent number: 10954273
    Abstract: Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
    Type: Grant
    Filed: September 6, 2019
    Date of Patent: March 23, 2021
    Assignee: The Johns Hopkins University
    Inventors: Jun O. Liu, Jingxin Wang, Zufeng Guo, Wei Li, Shridhar Bhat, Manisha Das
  • Cryptophycin compounds and conjugates, their preparation and their therapeutic use
    Patent number: 10941139
    Abstract: The present invention relates to cryptophycin compounds of formula (I). The invention also relates to cryptophycin payloads, to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The invention also relates to the process for preparing these conjugates.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: March 9, 2021
    Assignee: SANOFI
    Inventors: Antony Bigot, Hervé Bouchard, Marie-Priscille Brun, François Clerc, Jidong Zhang
  • Condensed thiophene derivatives useful as NaPi-IIb inhibitors
    Patent number: 10934280
    Abstract: The invention provides compounds of the formula: (A), pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds, salts, or compositions to treat hyperphosphatemia, chronic kidney disease, and/or the cardiovascular disease associated with chronic kidney disease.
    Type: Grant
    Filed: August 8, 2017
    Date of Patent: March 2, 2021
    Assignee: Eli Lilly and Company
    Inventors: David Andrew Coates, Kevin Robert Fales, Jeffrey Allen Peterson, Jeffrey Michael Schkeryantz, Quanrong ' Shen, Matthew John Valli, John Rowley Wetterau, II, Dariusz Stanislaw Wodka, Yanping Xu
  • Inhibitors of Bruton's tyrosine kinase and method of their use
    Patent number: 10934310
    Abstract: The present disclosure is directed to compounds of Formula (I) and methods of their use and preparation, as well as compositions comprising compounds of Formula (I).
    Type: Grant
    Filed: May 15, 2019
    Date of Patent: March 2, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Nidhi Arora, Genesis M. Bacani, Joseph Kent Barbay, Scott D. Bembenek, Min Cai, Wei Chen, Charlotte Pooley Deckhut, James P. Edwards, Brahmananda Ghosh, Kevin D. Kreutter, Gang Li, Mark S. Tichenor, Jennifer D. Venable, Jianmei Wei, John J. M. Wiener, Yao Wu, Kun Xiao, Feihuang Zhang, Yaoping Zhu
  • Combination, application thereof and treatment method
    Patent number: 10933059
    Abstract: Provided are a combination, an application thereof and a treatment method. The combination comprises one or more of a benzoheterocyclic compound of formula (I), a pharmaceutically acceptable salt, a solvate, a crystalline form, a cocrystal, a stereoisomer, an isotope compound, a metabolite and a prodrug thereof, and an androgen receptor pathway modulator and/or a hormone drug. The combination and treatment method may effectively inhibit the growth of prostate cancer cells.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: March 2, 2021
    Assignee: KANGPU BIOPHARMACEUTICALS. LTD.
    Inventors: Chuansheng Ge, Baisong Liao, Wen-Cherng Lee
  • Atropisomerism for enhanced kinase inhibitor selectivity
    Patent number: 10934300
    Abstract: The invention provides a series of conformationally stable and selective kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly interconverting parent compounds. The compounds herein are atropisomers having increased kinase selectivity, and are for use in treating conditions that benefit from selective kinase inhibition.
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: March 2, 2021
    Assignee: San Diego State University (SDSU) Foundation
    Inventors: Jeffrey L. Gustafson, Sean T. Toenjes, Sean M. Maddox
  • Benzyl amine-containing heterocyclic compounds and compositions useful against mycobacterial infection
    Patent number: 10919888
    Abstract: Described herein are compounds and compositions, and methods of making and their use as effective agents against mycobacterial infections.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: February 16, 2021
    Assignee: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Marvin J. Miller, Garrett C. Moraski
  • Substituted 4-benzyl and 4-benzoyl piperidine derivatives
    Patent number: 10919875
    Abstract: Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds. Also described herein are methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.
    Type: Grant
    Filed: June 17, 2016
    Date of Patent: February 16, 2021
    Assignee: 89BIO LTD
    Inventors: Nadine C. Becknell, Reddeppa Reddy Dandu, Bruce D. Dorsey, Dimitar B. Gotchev, Robert L. Hudkins, Linda Weinberg, Craig A. Zificsak
  • Methods of treating myeloproliferative disorders
    Patent number: 10918646
    Abstract: The present disclosure relates to the use of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, and pharmaceutically acceptable salts thereof, for treating myelofibrosis.
    Type: Grant
    Filed: October 7, 2020
    Date of Patent: February 16, 2021
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Adrian Senderowicz, Michael Cooper
  • [1,2,4]triazolo[1,5-A]pyridinyl substituted indole compounds
    Patent number: 10912766
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: October 15, 2019
    Date of Patent: February 9, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, Dharmpal S. Dodd, Tasir Shamsul Haque, Louis J. Lombardo, John E. Macor, Christopher P. Mussari, Laxman Pasunoori, Sreekantha Ratna Kumar, Trevor C. Sherwood, Shoshana L. Posy, Ramesh Kumar Sistla, Subramanya Hegde, Anupama Kandhi Ramachandra Reddy
  • Substituted aminothiazoles
    Patent number: 10913734
    Abstract: Described herein are substituted aminothiazoles, compositions comprising same; and methods of making and using same.
    Type: Grant
    Filed: July 11, 2017
    Date of Patent: February 9, 2021
    Inventors: Yanming Du, Huagang Lu, John Rogowsky, William A. Kinney, Andrea Cuconati
  • Multi-tyrosine kinase inhibitors derivatives and methods of use
    Patent number: 10899712
    Abstract: The present invention is directed to multi-tyrosine kinase inhibitor compounds. The present invention is further directed to compositions comprising those compounds. Finally, the present invention is directed to methods of treating eye conditions including, but not limited to, diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, dry macular degeneration with drusen and wet macular degeneration, using compounds and compositions of the invention.
    Type: Grant
    Filed: July 22, 2019
    Date of Patent: January 26, 2021
    Assignee: Ontogenesis, LLC
    Inventor: Gerald Horn