Patents Examined by Niloofar Rahmani
  • Hemi (L)-tartrate forms of 3-({5-chloro-1-[3-(methylsulfonyl)propyl]-1-indol-2-yl}methyl)-1-(2,2,2-trifluoroethy)-1,3-dihydro-2-imidazo[4,5-C]pyridin-2-one and pharmaceutical compositions comprising the same
    Patent number: 12145933
    Abstract: The present invention relates to hemi (L)-tartrate forms of the RSV fusion inhibitor 3-({5-chloro-1-[3-(methylsulfonyl)propyl]-1H-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one (also known under its INN as rilematovir), and to processes for preparing said forms and the use of these forms in a pharmaceutical composition.
    Type: Grant
    Filed: June 10, 2021
    Date of Patent: November 19, 2024
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: Jan Jos L. Bevernage, Jasmine Bogaerts, Kristof Leonard Kimpe, Eszter Tieger
  • Pyrido[3,2-d]pyrimidine compounds uses thereof for treating a proliferative disease
    Patent number: 12139488
    Abstract: Compounds, compositions and their use in the treatment of a proliferative disease or condition such as a said proliferative disease or disorder is associated with a RAF gene mutation and/or a RAS gene mutation.
    Type: Grant
    Filed: April 5, 2024
    Date of Patent: November 12, 2024
    Assignee: Université de Montréal
    Inventors: Pierre Louis Beaulieu, Michael Dore
  • Complexes and ligands
    Patent number: 12134721
    Abstract: The present application provides ligands and fluorescent or luminescent complexes comprising these ligands.
    Type: Grant
    Filed: October 22, 2019
    Date of Patent: November 5, 2024
    Assignee: The General Hospital Corporation
    Inventors: Ralph Mazitschek, N. Connor Payne, Alena Kalyakina
  • N-oxide inhibitors of NLRP3 inflammasome
    Patent number: 12129251
    Abstract: The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging.
    Type: Grant
    Filed: September 6, 2023
    Date of Patent: October 29, 2024
    Assignee: BioAge Labs, Inc.
    Inventor: George Hartman
  • Forms of pyrido[1,2-a]pyrimidin-4-one derivatives, its formulation and its process of making
    Patent number: 12122789
    Abstract: The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one useful as pharmaceutically active compounds.
    Type: Grant
    Filed: April 16, 2021
    Date of Patent: October 22, 2024
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Meier, Urs Schwitter, Anne De Paepe, Juergen Thun, Frank Stowasser
  • Azaindole rock inhibitors
    Patent number: 12116366
    Abstract: This invention provides rho-associated protein kinase (ROCK) inhibiting compounds for therapeutic applications as described further herein.
    Type: Grant
    Filed: March 19, 2024
    Date of Patent: October 15, 2024
    Assignee: Avicenna Biosciences, Inc.
    Inventor: Thomas Maxwell Kaiser
  • Pyrrolo[2,3-d]pyrimidine tosylate salt, crystalline form thereof and manufacturing process and intermediates thereto
    Patent number: 12116368
    Abstract: The present invention discloses a novel p-toluenesulfonic acid salt and a crystalline polymorphic Form 1 of said salt of 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one, pharmaceutical composition containing the same, as well as preparations and uses thereof. The present invention also discloses a novel phosphoric acid salt of 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one, pharma-ceutical composition containing the same, as well as preparations and uses thereof.
    Type: Grant
    Filed: October 21, 2019
    Date of Patent: October 15, 2024
    Assignee: Pfizer Inc.
    Inventors: Brian Matthew Samas, Yong Tao, Douglas James Critcher, David Sydney Bernard Daniels, Kevin Paul Girard, Gregory Scott Goeken, Peter Robert Rose
  • Triazolopyridinyl compounds as kinase inhibitors
    Patent number: 12110290
    Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
    Type: Grant
    Filed: July 6, 2023
    Date of Patent: October 8, 2024
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guanglin Luo, Jie Chen, Carolyn Diane Dzierba, David B. Frennesson, Junqing Guo, Amy C. Hart, Xirui Hu, Michael E. Mertzman, Matthew Reiser Patton, Jianliang Shi, Steven H. Spergel, Brian Lee Venables, Yong-Jin Wu, Zili Xiao, Michael G. Yang
  • Glutarimide-containing pan-KRAS-mutant degrader compounds and uses thereof
    Patent number: 12110291
    Abstract: The present disclosure relates to novel pan-KRAS glutarimide-containing compounds with KRAS degradation activities, pharmaceutical compositions containing such compounds, and their use in prevention and treatment diseases and conditions.
    Type: Grant
    Filed: November 30, 2023
    Date of Patent: October 8, 2024
    Assignee: Tiger Biotherapeutics Inc.
    Inventors: Robert Luo, Ji Liu, Pin Huang, Jie Su, Yan Feng, Ke Liu, Jie Fan, Wei He, Yimin Qian
  • Processes for preparing a diazabicyclooctane compound
    Patent number: 12103928
    Abstract: A process for preparing a diazabicyclooctane compound represented by the following formula (I): wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
    Type: Grant
    Filed: May 18, 2023
    Date of Patent: October 1, 2024
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Takeshi Furuuchi, Yoshiaki Sakamaki
  • Synthesis of chromanol derivatives
    Patent number: 12103918
    Abstract: The present invention relates to a process for the production of chromanol derivatives, more specifically to a process for preparing a compound of the general formula (I) wherein R1, R2 and R3 independently of each other are selected from hydrogen and methyl, R4 is selected from hydrogen and C1-C6-alkanoyl, and X is selected from C1-C20-alkyl and C2-C20-alkenyl.
    Type: Grant
    Filed: August 16, 2019
    Date of Patent: October 1, 2024
    Assignee: BASF SE
    Inventors: Melanie Weingarten, Wolfgang Siegel, Michael Puhl
  • Method for manufacturing cyclopropane compound
    Patent number: 12098137
    Abstract: The present invention provides an industrially advantageous production method of (1R,2S)-2-{[((2,4-dimethylpyrimidin-5-yl)oxy}methyl]-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide. (1R,2S)-2-{[((2,4-Dimethylpyrimidin-5-yl)oxy}methyl]-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide (compound [A]) is produced by an industrially advantageous method by a route via a novel compound. wherein each symbol is as described in the description.
    Type: Grant
    Filed: September 5, 2019
    Date of Patent: September 24, 2024
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Kazuhiro Yamauchi, Junichi Tomokawa
  • Methods and compositions for treating polycystic ovary syndrome
    Patent number: 12098152
    Abstract: Polycystic ovary syndrome (PCOS) is characterized by elevated levels of androgens, cysts in the ovaries, and irregular periods. Women with PCOS present with additional symptoms, including hirsutism, alopecia, acne, infertility, weight gain, fatigue, depression and mood changes. The present disclosure provides new compounds, salts, compositions and uses thereof in the treatment of PCOS due to elevated adrenal androgens. Further, the present disclosure provides methods for treating PCOS due to elevated adrenal androgens.
    Type: Grant
    Filed: February 9, 2023
    Date of Patent: September 24, 2024
    Assignee: SPRUCE BIOSCIENCES, INC.
    Inventors: Christopher Barnes, David Karpf, Mustafa Noor
  • Inhibitors of NEK7 kinase
    Patent number: 12091413
    Abstract: Compounds having activity as inhibitors of NEK7 are provided. The compounds have Structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein, A, X, Y, R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of the NLRP3 inflammasome are also provided.
    Type: Grant
    Filed: May 23, 2023
    Date of Patent: September 17, 2024
    Assignee: Halia Therapeutics, Inc.
    Inventors: David James Bearss, John Sai Keong Kauwe, III, Alexis Henri Abel Mollard
  • Process of preparing a PD-1/PD-L1 inhibitor
    Patent number: 12084443
    Abstract: The present invention relates to processes of preparing PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3?-(3-(((R)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-ylamino)-2,2?-dimethylbiphenyl-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid, or salts thereof, related synthetic intermediates, and salts of the intermediates, where the PD-1/PD-L1 inhibitor is useful in the treatment of various diseases including infectious diseases and cancer.
    Type: Grant
    Filed: August 31, 2023
    Date of Patent: September 10, 2024
    Assignee: Incyte Corporation
    Inventors: Jiacheng Zhou, Zhongjiang Jia, Qiyan Lin, Pingli Liu, Yongchun Pan, Timothy Martin, Bo Shen, Naijing Su, Yongzhong Wu
  • Preparation method for deuterated macrocyclic compound
    Patent number: 12077528
    Abstract: Provided are a compound as represented by formula (D) and a preparation method therefor, where X2 is a halogen, Pg is selected from H and an amino protecting group, such as Cbz, Boc, Fmoc, Alloc, Teoc, methoxycarbonyl or ethoxycarbonyl. Also provided are a synthesized intermediate compound of the formula (D) compound and a preparation method for the intermediate compound.
    Type: Grant
    Filed: November 27, 2019
    Date of Patent: September 3, 2024
    Assignee: Shenzhen TargetRx, Inc.
    Inventors: Yihan Wang, Huanyin Li
  • Bicyclic pyridine derivative
    Patent number: 12077546
    Abstract: The present disclosure provides bicyclic pyridine derivatives. A compound represented by formula I: or a pharmaceutically acceptable salt thereof, wherein X is a oxygen atom, sulfur atom, NR, or CR?R?, n is 0 or 1, R1, R2a, R2b, R2c, R2d, R, R? and R? are each independently a hydrogen atom, a halogen atom, optionally substituted C1-6 alkyl, or an optionally substituted C6-10 aryl, or two of R2a, R2b, R2c, R2d, R, R?, and R?, together with a carbon atom or a nitrogen atom to which they are attached, form a 3- to 6-membered saturated carbocyclic ring or saturated heterocyclic ring, and R3a, R3b, R3c and R5a and R5b, are as defined in the description.
    Type: Grant
    Filed: November 10, 2023
    Date of Patent: September 3, 2024
    Assignee: Sumitomo Pharma Co., Ltd.
    Inventors: Satoshi Adachi, Hidefumi Yoshinaga, Hajime Shibata, Yusuke Shioda, Riko Nagahama
  • Prolyl hydroxylase domain-containing protein (PHD) inhibitors and uses thereof
    Patent number: 12071443
    Abstract: Described herein are PHD inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of inflammatory bowel disease.
    Type: Grant
    Filed: June 22, 2023
    Date of Patent: August 27, 2024
    Assignee: INSILICO MEDICINE IP LIMITED
    Inventors: Xiao Ding, Liena Qin, Feng Ren, Jianyu Xu
  • Pyrido[3,2-d]pyrimidine compounds uses thereof for treating a proliferative disease
    Patent number: 12060353
    Abstract: Compounds, compositions and their use in the treatment of a proliferative disease or condition such as a said proliferative disease or disorder is associated with a RAF gene mutation and/or a RAS gene mutation.
    Type: Grant
    Filed: November 2, 2023
    Date of Patent: August 13, 2024
    Assignee: Université de Montréal
    Inventors: Pierre Louis Beaulieu, Eric Beaulieu, Sasmita Tripathy, Emeline Benoit, Joanne Tan, Hugo Lavoie, Yannick Rose, Michael Dore, Doris Schuetz, Mukund Ghavre, Jacques Banville
  • Compositions and methods for inhibiting phenyl triazole MLL1-WDR5 protein-protein interaction
    Patent number: 12054478
    Abstract: The present disclosure relates to the field of medicinal chemistry, in particular to a phenyl triazole MLL1-WDR5 protein-protein interaction inhibitor (I) and a preparation method thereof, and pharmacodynamics experiments prove that the compound of the present disclosure has relatively strong MLL1-WDR5 protein-protein interaction inhibition activity.
    Type: Grant
    Filed: September 14, 2022
    Date of Patent: August 6, 2024
    Assignee: HUYABIO International, LLC
    Inventors: Qidong You, Xiaoke Guo, Dongdong Li, Weilin Chen, Zhihui Wang