Patents Issued in March 21, 2024
  • IMIDAZOLO INDAZOLE COMPOUNDS AS JAK INHIBITORS
    Publication number: 20240092758
    Abstract: Provided herein are compounds of formula (I): and pharmaceutically-acceptable salts thereof, where A, W, X, Y and Z are defined in the specification. The compounds of formula (I) and pharmaceutically-acceptable salts thereof are Janus kinase (JAK) inhibitors. Also provided herein are pharmaceutical compositions comprising such compounds; and methods of using such compounds to treat, e.g., inflammatory and fibrotic diseases, including respiratory diseases.
    Type: Application
    Filed: June 24, 2022
    Publication date: March 21, 2024
    Inventors: Robert Murray MCKINNELL, Tom M. LAM, Cameron SMITH, Philip GERKEN, Paul ALLEGRETTI, Gabrielle Elaine DOLGONOS, Christina OWENS
  • Non-Covalent Inhibitors of the Main Protease of SARS-CoV-2 and Methods of Use
    Publication number: 20240092759
    Abstract: Provided herein are compounds of formula (I) or (I-A), which act as non-covalent inhibitors of SARS-CoV2 main protease (Mpro). The compounds of formula (I) or (I-A) are useful in treating COVID-19 infections, as well as reducing or ameliorating symptoms associated with COVID-19 infection.
    Type: Application
    Filed: January 7, 2022
    Publication date: March 21, 2024
    Inventor: William L. Jorgensen
  • QUINOLINE cGAS ANTAGONIST COMPOUNDS
    Publication number: 20240092760
    Abstract: The present disclosure provides compounds that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
    Type: Application
    Filed: June 13, 2023
    Publication date: March 21, 2024
    Inventors: Jian QIU, Qi WEI, Matt TSCHANTZ, Heping SHI, Youtong WU, Huiling TAN, Lijun SUN, Chuo CHEN, Zhijian CHEN
  • QUINAZOLINE COMPOUNDS AND METHODS OF USE
    Publication number: 20240092761
    Abstract: Substituted quinazoline compounds, conjugates, and pharmaceutical compositions for use in the treatment of cancer are disclosed herein. The disclosed compounds are useful, among other things, in the inhibition of CDK. In certain aspects, the disclosure generally relates to substituted quinolinone amide compounds or salts of Formula (I), (IA), (IAA), (IAAA), (IB), (IBB), (IC), (ICC), (II), or (IIA) and pharmaceutical compositions thereof.
    Type: Application
    Filed: July 18, 2023
    Publication date: March 21, 2024
    Inventors: William VERNIER, Quynh Nhu NGUYEN, Nomaan REZAYEE, Laurent GOMEZ, Chao Zhang, Thomas Francis MILLER, III, Frederick Roy MANBY
  • OPTICALLY ACTIVE PYRROLIDINE COMPOUND AND METHOD FOR PRODUCING SAME
    Publication number: 20240092762
    Abstract: The present invention provides: a methyl 1-{2-[(3S,4R) -1-[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4 -methoxyphenyl)pyrrolidine-3-carbonyl]-4 -(methoxymethyl)pyrrolidin-3-yl]-5 -(trifluoromethyl)phenyl}piperidine-4-carboxylate 1/2 ethane-1,2-disulfonic acid which is represented by formula (1) and is excellent in crystallinity; and a method for producing the same; and a production intermediate thereof; and a production method using this compound.
    Type: Application
    Filed: October 31, 2023
    Publication date: March 21, 2024
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Joji TSURUMOTO, Kenji MOROKUMA
  • ISOINDOLINONE AMINOPYRIMIDINE COMPOUNDS AS INHIBITORS OF NUAK KINASES, COMPOSITIONS AND USES THEREOF
    Publication number: 20240092763
    Abstract: The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting or blocking NUAK kinase, such as cancers and fibrosis.
    Type: Application
    Filed: January 7, 2022
    Publication date: March 21, 2024
    Inventors: Rima Al-Awar, Liliana Attisano, Methvin Isaac, Yong Liu, David Smil, David Uehling, Jeff Wrana
  • KINASE INHIBITORS
    Publication number: 20240092764
    Abstract: A TNIK and/or MAP4K4 kinase inhibitor can include: Formula A, derivative, prodrug, salt, stereoisomer, tautomer polymorph, or solvate thereof, or having chirality at any chiral center, wherein: ring 1 is an aromatic ring with or without hetero atoms; ring 2 is a hetero aromatic ring; ring 3 includes at least one hetero aromatic ring and optionally at least one cycloaliphatic ring fused with the at least one hetero aromatic ring; ring 4 is an aromatic ring with or without hetero atoms; Y is a bond or a linker; Y1 is a linker; each n is independently 0, 1, or 2; each o is independently 0, 1, 2, 3, 4, or 5; each R1, R6, R11, and R12 is independently a substituent; and RA is a ring structure, straight aliphatics, or branched aliphatics, which can be substituted or unsubstituted, any with or without hetero atoms.
    Type: Application
    Filed: August 30, 2023
    Publication date: March 21, 2024
    Inventors: Aleksandr Aliper, Vladimir Aladinskiy, Aleksandrs Zavoronkovs
  • METHODS OF INHIBITING KINASES
    Publication number: 20240092765
    Abstract: A method of inhibiting TNIK and/or MAP4K4 kinase can include: contacting the kinase with a compound of Formula A, wherein: ring 1 is an aromatic ring with or without hetero atoms; ring 2 is a hetero aromatic ring; ring 3 includes at least one hetero aromatic ring and optionally at least one cycloaliphatic ring fused with the at least one hetero aromatic ring; ring 4 is an aromatic ring with or without hetero atoms; Y is a bond or a linker; Y1 is a linker; each n is independently 0, 1, or 2; each o is independently 0. 1, 2, 3, 4, or 5; each R1, R6, R11, and R12 is independently a substituent; and RA is a ring structure, straight aliphatics, or branched aliphatics, which can be substituted or unsubstituted, any with or without hetero atoms.
    Type: Application
    Filed: July 6, 2023
    Publication date: March 21, 2024
    Inventors: Aleksandr Aliper, Vladimir Aladinskiy, Aleksandrs Zavoronkovs
  • MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
    Publication number: 20240092766
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: February 10, 2023
    Publication date: March 21, 2024
    Inventors: Sara S. HADIDA RUAH, Peter D.J. GROOTENHUIS, Fredrick VAN GOOR, Jinglan ZHOU, Brian BEAR, Mark T. MILLER, Jason McCARTNEY, Mehdi Michel Jamel NUMA, Xiaoqing YANG
  • Renewable Highly Biobased Polybenzoxazine Thermosets for Composite Applications
    Publication number: 20240092767
    Abstract: Benzoxazine compounds, methods of making them, polymers made therefrom and methods of polymerizing the benzoxazines. These renewable benzoxazine monomers and polymers that utilize the variety of building blocks found in renewable plant biomass, demonstrate excellent processability and large temperature windows for processing of resin systems.
    Type: Application
    Filed: March 24, 2023
    Publication date: March 21, 2024
    Applicants: DREXEL UNIVERSITY, The Government of the United States of America, as represented by The Secretary of the Army
    Inventors: Giuseppe R. Palmese, Santosh K. Yadav, John J. LaScala
  • CRYSTAL FORM OF ANTI-INFLUENZA VIRUS COMPOUND, PREPARATION METHOD FOR CRYSTAL FORM, AND USE OF CRYSTAL FORM
    Publication number: 20240092768
    Abstract: Disclosed are a crystal form of a compound (1S,2S)-2-fluoro-N-(2-(2-(4-((R)-(5-methyl-2H-tetrazol-2-yl)(phenyl)methyl)piperidine-1-formyl)pyridin-4-yl)benzo[d]oxazol-5-yl)cyclopropyl-1-carboxamide having a structure of formula (A), a preparation method for the crystal form, and a use of the crystal form in the preparation of a drug for treating and/or preventing influenza.
    Type: Application
    Filed: January 20, 2022
    Publication date: March 21, 2024
    Applicant: XIZANG HAISCO PHARMACEUTICAL CO., LTD.
    Inventors: Yao LI, Guobiao ZHANG, Xiaobo ZHANG
  • (CYANO-DIMETHYL-METHYL)-ISOXAZOLES AND -[1,3,4]THIADIAZOLES
    Publication number: 20240092769
    Abstract: This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.
    Type: Application
    Filed: June 30, 2023
    Publication date: March 21, 2024
    Inventors: Doris Riether, Florian Paul Christian Binder, Henri Doods, Stephan George Mueller, Janet Rachel Nicholson, Achim Sauer
  • Heterocycle RMB39 Modulators
    Publication number: 20240092770
    Abstract: Provided herein are compounds that modulate RMB39 and methods of using the compounds in RMB39-associated disorders, such as cancer (e.g., renal cell carcinoma).
    Type: Application
    Filed: August 15, 2023
    Publication date: March 21, 2024
    Inventors: Ashraf Saeed, Chris Bailey, Carl Brooks, Kevin Fales, Janet Paulsen
  • CRYSTAL FORM OF LANIFIBRANOR, PREPARATION METHOD THEREFOR, AND USE THEREOF
    Publication number: 20240092771
    Abstract: Provided are novel crystalline forms of Lanifibranor (Referred to as “Compound I”) and preparation methods thereof, pharmaceutical compositions containing the crystalline forms, and uses of the crystalline forms for preparing pan-PPAR agonists drugs and drugs for treating NASH. Compared with prior arts, the provided crystalline forms of Compound I have one or more improved properties, which solve the problems of the prior art and is of great value to the optimization and development of the drugs.
    Type: Application
    Filed: November 24, 2023
    Publication date: March 21, 2024
    Applicant: CRYSTAL PHARMACEUTICAL (SUZHOU) CO., LTD.
    Inventors: Minhua CHEN, Hongyan ZHU
  • CRYSTALLINE FORM OF A PIPERAZINYL-THIAZOLE DERIVATIVE
    Publication number: 20240092772
    Abstract: The invention relates to a crystalline form of 1-{(R)-2-(2-Hydroxy-ethyl)-4-[2-trifluoromethyl-4-(2-trifluoromethyl-pyrimidin-5-yl)-thiazol-5-yl]-piperazin-1-yl}-2-(3-methyl-[1,2,4]triazol-1-yl)-ethanone, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline form, pharmaceutical compositions prepared from such crystalline forms, and their use as CXCR3 receptor modulators in the treatment of various diseases and disorders related to the CXCR3 receptor and its ligands.
    Type: Application
    Filed: January 26, 2022
    Publication date: March 21, 2024
    Inventor: Dominik FOSSHAG
  • DIHYDRO-CYCLOPENTA-ISOQUINOLINE SULFONAMIDES DERIVATIVES
    Publication number: 20240092773
    Abstract: The present invention relates to dihydro-cyclopenta-isoquinoline derivatives of formula (I): processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses, non-allergic mast cell responses or certain autoimmune responses), and in particular, disorders caused by the interaction of IgE with the Fc?RI receptor.
    Type: Application
    Filed: December 22, 2020
    Publication date: March 21, 2024
    Inventors: Timothy John NORMAN, Zhaoning ZHU, Selvaratnam SUGANTHAN, Konstantinos RAMPALAKO, James MADDEN, Jag Paul HEER, Richard Jeremy FRANKLIN, Rickki Lee CONNELLY, Thierry DEMAUDE, Gregory William HASLETT, Benedicte LALLEMAND, Nathaniel Julius Thomas MONCK, Julian Hugh ROWLEY, Giancarlo TRANI
  • HETEROAROMATIC COMPOUNDS AND USES THEREOF
    Publication number: 20240092774
    Abstract: Providing heteraromatic compounds and uses thereof. In particular, providing heteraromatic compounds of formula (I), pharmaceutical compositions comprising same, methods for preparing same and uses thereof, wherein the variables are as defined in the description.
    Type: Application
    Filed: September 17, 2021
    Publication date: March 21, 2024
    Applicant: HUTCHISON MEDIPHARMA LIMITED
    Inventors: Wei-Guo SU, Weihan ZHANG, Haibin YANG
  • FLUORINATED TETRAHYDRONAPHTHYRIDINYL NONANOIC ACID DERIVATIVES AND USES THEREOF
    Publication number: 20240092775
    Abstract: The present invention relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing the fluorinated compounds of the invention, and methods of treating fibrosis, macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: May 31, 2023
    Publication date: March 21, 2024
    Inventors: Ben C. ASKEW, Takeru FURUYA
  • HETEROCYCLIC COMPOUND, ORGANIC LIGHT-EMITTING DEVICE COMPRISING SAME
    Publication number: 20240092776
    Abstract: Disclosed (or Provided) are a heterocyclic compound and an organic light emitting device including the same.
    Type: Application
    Filed: June 22, 2023
    Publication date: March 21, 2024
    Applicant: LT MATERIALS CO., LTD.
    Inventors: Hyung-Jin LEE, Won-Jang JEONG, Dong-Jun KIM, Dae-Hyuk CHOI
  • Quinolone Derivatives as Fibroblast Growth Factor Receptor Inhibitors
    Publication number: 20240092777
    Abstract: Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Application
    Filed: June 30, 2023
    Publication date: March 21, 2024
    Applicant: Principia Biopharma Inc.
    Inventors: Erik Verner, Kenneth Albert Brameld
  • TOPICAL PHARMACEUTICAL COMPOSITIONS AND METHODS
    Publication number: 20240092778
    Abstract: The present disclosure relates to a topical pharmaceutical composition containing N-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-3-(5-isopropoxy-1H-pyrazol-3-yl)-3H-imidazo[4,5-b]pyridin-5-amine (hereinafter also referred to as “Compound A”), or a pharmaceutically acceptable salt thereof; to the use of the topical pharmaceutical composition as a medicament; to processes for the preparation of said topical pharmaceutical composition; to certain new methods of treating an inflammatory skin disorder, particularly psoriasis, by administering a topical pharmaceutical composition containing Compound A or a pharmaceutically acceptable salt thereof; and to novel crystalline forms of a mesylate salt of Compound A.
    Type: Application
    Filed: December 28, 2021
    Publication date: March 21, 2024
    Inventors: Kollol PAL, Abhijit BHAT, Jay BIRNBAUM, Vijendra NALAMOTHU, Srikanth MANNE, Gayathri KRISHNAN, Jean-Philippe THERRIEN
  • USP1 INHIBITORS AND USES THEREOF
    Publication number: 20240092779
    Abstract: Provided herein are inhibitors of ubiquitin-specific-processing Protease 1 (USP1), their pharmaceutical compositions, and methods of use for treating diseases or disorders, such as cancers described herein.
    Type: Application
    Filed: June 29, 2023
    Publication date: March 21, 2024
    Inventors: Qibin SU, Huawei CHEN, Guosheng WU
  • ADDUCTS AND DIMER COMPOUNDS SYNTHESIZED USING GK METHOD
    Publication number: 20240092780
    Abstract: The present disclosure is concerned with ?-carboline adducts and dimer compounds comprising two ?-carboline moieties and methods of synthesizing the same. The methods described herein may also be used to synthesize a wide array of ?-carboline adducts and dimer compounds, depending upon the reactants used. Generally, the method comprises reacting a tryptamine and an acid chloride or diacid chloride in acetonitrile to yield harmaline compounds which can be easily converted to harmine or tetrahydroharmine if desired.
    Type: Application
    Filed: August 30, 2023
    Publication date: March 21, 2024
    Inventors: Krishna Mohan Donavalli, Rajni Verma, Gene H. Zaid
  • ARYL PIPERIDINES AS MONOACYLGLYCEROL LIPASE MODULATORS
    Publication number: 20240092781
    Abstract: Aryl piperidine compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions: wherein X, R2a, R2b, R3, R4, R5a and R5b are as defined herein.
    Type: Application
    Filed: September 21, 2023
    Publication date: March 21, 2024
    Inventors: Michael K. Ameriks, Cynthia B. Berry, Krisztián Biró, Pablo Garcia-Reynaga, Andrew V. Samant, Warren S. Wade
  • TRICYCLIC PESTICIDAL COMPOUNDS
    Publication number: 20240092782
    Abstract: The invention relates to compounds of formula (I)X(I), wherein the variables are as mined in the specification. It also relates to the use of compounds of formula (I) as an agrochemical pesticide; to pesticidal mixtures comprising compounds of formula (I); and to agrochemical or veterinary compositions comprising compounds of formula (I). Other objects are seed comprising compounds of formula (I); and methods for controlling invertebrate pests, infestation, or infection by invertebrate pests by application of compounds of formula (I).
    Type: Application
    Filed: March 1, 2022
    Publication date: March 21, 2024
    Inventors: Birte Schroeder, Rizwan Shabbir Shaikh, Pulakesh Maity, Ashokkumar Adisechan
  • HETEROAROMATIC COMPOUNDS FOR ORGANIC ELECTROLUMINESCENT DEVICES
    Publication number: 20240092783
    Abstract: The present invention relates to heteroaromatic compounds suitable for use in electronic devices, and to electronic devices, in particular organic electroluminescent devices, containing said compounds.
    Type: Application
    Filed: March 15, 2022
    Publication date: March 21, 2024
    Inventors: Amir Hossain PARHAM, Christian EHRENREICH
  • CONDENSED HETEROCYCLIC COMPOUND
    Publication number: 20240092784
    Abstract: A condensed heterocyclic compound has a sepiapterin reductase inhibitory action and is particularly useful for treatment of a pain. The condensed heterocyclic compound represented by Formula (I) below (R1 represents a hydrocarbon group or the like; R2 and R3 represent a hydrogen atom or the like; R4, X, and Y represent defined substituents), a tautomer or a pharmaceutically acceptable salt of the compound, or a solvate of any of these.
    Type: Application
    Filed: April 13, 2021
    Publication date: March 21, 2024
    Applicants: NISSAN CHEMICAL CORPORATION, SHIONOGI & CO., LTD.
    Inventors: Masahiro KAMAURA, Yusuke INABA, Yusuke SHINTANI, Yuki KUWANO, Moemi NAKAO, Hiroshi NAGAI, Noriyuki KUROSE, Kenji TAKAYA, Mado NAKAJIMA
  • PROCESS FOR MAKING IBRUTINIB
    Publication number: 20240092785
    Abstract: The presented invention relates to a process for preparation of Ibrutinib, comprising: a. Reacting compound of Formula (2) with compound of Formula (3) in a presence of Lewis acid to provide compound of Formula (4); b. Contacting compound of Formula (4) with toluene; c. Isolate a solid form of compound of Formula (4); d. Transforming compound of Formula (4) into Ibrutinib.
    Type: Application
    Filed: January 20, 2022
    Publication date: March 21, 2024
    Inventors: Petr MITAS, Libor VYKLICKY, Jiri BARTL, Oldrich SMEKAL
  • CRYSTALLINE FORM OF (S)-7-(1-ACRYLOYLPIPERIDIN-4-YL)-2-(4-PHENOXYPHENYL)-4,5,6,7-TETRA-HYDROPYRAZOLO[1,5-a]PYRIMIDINE-3-CARBOXAMIDE, PREPARATION, AND USES THEREOF
    Publication number: 20240092786
    Abstract: The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetr a-hydropyrazolo[1,5-a]pyrimi dine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease.
    Type: Application
    Filed: November 3, 2023
    Publication date: March 21, 2024
    Inventors: Zhiwei WANG, Yunhang GUO, Gongyin SHI
  • PHARMACEUTICAL PROCESS AND INTERMEDIATES
    Publication number: 20240092787
    Abstract: There is provided a new and improved synthetic route for the synthesis of the compound 1-{2-[(1R)-1-aminoethyl]-4-chlorobenzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one (Formula (I)) that is readily scalable for commercial production. Also provided are important intermediate compounds that are formed in the new and improved synthetic route for the synthesis of the compound of formula (I).
    Type: Application
    Filed: August 18, 2023
    Publication date: March 21, 2024
    Inventors: MARK Andrew GRAHAM, JONATHAN ROBERT CARNEY, THOMAS GEORGE BISHOP, KATIE COOPER
  • MASP-2 INHIBITORS AND METHODS OF USE
    Publication number: 20240092788
    Abstract: The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
    Type: Application
    Filed: September 6, 2023
    Publication date: March 21, 2024
    Applicant: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Sara Rebecca Goldstein, Santosh Kumar Keshipeddy, Do Yeon Kwon, Robert Huerta Lemus, Thomas L. Little, Markus Metz, Jeremiah H. Nguyen, Peter Kurt Nollert Von Specht, Loren Michael Price, Jennifer Tsoung, Sudheer Babu Vaddela
  • COMPOUNDS FOR ELECTRONIC DEVICES
    Publication number: 20240092789
    Abstract: The present application relates to a compound of the formula (I), to the use thereof in electronic devices, to processes for preparing the compound, and electronic devices comprising the compound.
    Type: Application
    Filed: September 16, 2020
    Publication date: March 21, 2024
    Inventors: Elvira MONTENEGRO, Teresa MUJICA-FERNAUD, Rachel TUFFIN, Frank VOGES, Amir Hossain PARHAM, Alexander Christian COMELY, Antoni MORAGAS SOLA
  • DIHYDROFUROPYRIDINE DERIVATIVES AS RHO- KINASE INHIBITORS
    Publication number: 20240092790
    Abstract: The invention relates to compounds of formula (I) inhibiting Rho Kinase that are dihydrofuropyridine derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
    Type: Application
    Filed: December 13, 2021
    Publication date: March 21, 2024
    Applicant: CHIESI FARMACEUTICI S.P.A.
    Inventors: Fabio RANCATI, Alessandro ACCETTA, Anna Maria CAPELLI, Daniele PALA, Christine EDWARDS, Adele Elisa PASQUA, Prashant Bhimrao KAPADNIS, Arnaud Jean Francois Auguste CHEGUILLAUME, David Edward CLARK
  • DIHYDROFUROPYRIDINE DERIVATIVES AS RHO-KINASE INHIBITORS
    Publication number: 20240092791
    Abstract: The invention relates to compounds of formula (I) inhibiting Rho Kinase that are dihydrofuropyridine derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
    Type: Application
    Filed: December 13, 2021
    Publication date: March 21, 2024
    Applicant: CHIESI FARMACEUTICI S.P.A.
    Inventors: Fabio RANCATI, Alessandro ACCETTA, Anna Maria CAPELLI, Daniele PALA, Christine EDWARDS, Adele Elisa PASQUA, Prashant Bhimrao KAPADNIS, Arnaud Jean Francois Auguste CHEGUILLAUME, David Edward CLARK
  • DIHYDROFUROPYRIDINE DERIVATIVES AS RHO- KINASE INHIBITORS
    Publication number: 20240092792
    Abstract: The invention relates to compounds of formula (I) inhibiting Rho Kinase that are dihydrofuropyridine derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
    Type: Application
    Filed: December 13, 2021
    Publication date: March 21, 2024
    Applicant: CHIESI FARMACEUTICI S.P.A.
    Inventors: Fabio RANCATI, Alessandro ACCETTA, Anna Maria CAPELLI, Daniele PALA, Christine EDWARDS, Adele Elisa PASQUA, Prashant Bhimrao KAPADNIS, Arnaud Jean Francois Auguste CHEGUILLAUME
  • CHROMENE-BASED COMPOUNDS, METHODS AND USES THEREOF
    Publication number: 20240092793
    Abstract: The present disclosure relates to a compound or a pharmaceutically acceptable salt, hydrate, solvate, N-oxide, stereoisomer, diastereoisomer, enantiomer, atropisomer, dimer, or polymorph for use in medicine comprising the following formula: wherein R1, R2 and R3 are independently selected from each other; R1 is selected from an aryl, or heterocyclic ring; R2 is selected from a H, alkyl, aryl, alcoxyl, halogen, hydroxyl, amine, carbonyl, or heterocyclic ring; R3 is selected from a H, or
    Type: Application
    Filed: June 29, 2020
    Publication date: March 21, 2024
    Applicant: University of Minho
    Inventors: Marta Sílvia Freitas Da Costa, Maria De Fátima Monginho Baltazar, Maria Fernanda De Jesus Rego Paiva Proença, Patrícia Maciel, Olívia Alexandra Elias Pontes
  • NOVEL PRMT5 INHIBITORS
    Publication number: 20240092794
    Abstract: Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders.
    Type: Application
    Filed: November 6, 2023
    Publication date: March 21, 2024
    Applicant: AMGEN INC.
    Inventors: Shon BOOKER, Matthew Paul BOURBEAU, John R. BUTLER, Sanne Ormholt Schroder GLAD, Brian Alan LANMAN, Patricia LOPEZ, Francesco MANONI, Liping H. PETTUS, Ian SARVARY, Nuria A. TAMAYO, Mikkel VESTERGAARD, Nicholas Anthony WEIRES
  • PYRIDINE COMPOUNDS AS ALLOSTERIC SHP2 INHIBITORS
    Publication number: 20240092795
    Abstract: The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.
    Type: Application
    Filed: April 25, 2023
    Publication date: March 21, 2024
    Inventors: Adrian GILL, Naing AAY, Kevin MELLEM, Andreas BUCKL, Elena S. KOLTUN, Christopher SEMKO, Gert KISS
  • PRODUCT OF INTERNAL DEHYDRATION OF HIGH-PURITY SORBITOL
    Publication number: 20240092796
    Abstract: The present invention relates to a product of internal dehydration of sorbitol, characterized in that it has a total residual nitrogen atom content of between 0.01 ppm and 150 ppm, preferably of between 0.02 ppm and 20 ppm, more preferably of between 0.05 ppm and 10 ppm, and, more preferentially, of between 0.07 ppm and 5 ppm, this residual content being expressed as dry weight relative to the total dry weight of said product, and in that it has a total residual sulphur atom content of between 0.0001 ppm and 100 ppm, preferably between 0.0002 ppm and 50 ppm, more preferably between 0.0004 ppm and 30 ppm, and more preferentially, between 0.0008 ppm and 20 ppm, this total residual content being expressed in dry weight relative to the dry weight of said product; a method for purifying such a product and a polymer comprising a unit corresponding to said product.
    Type: Application
    Filed: November 19, 2021
    Publication date: March 21, 2024
    Inventors: Nicolas JACQUEL, René SAINT-LOUP, Théodore VANBESIEN
  • METHODS OF MAKING LOW ODOR CHOLINE SALTS OF AN ORGANIC COMPOUND
    Publication number: 20240092797
    Abstract: Methods of making low odor choline salts of an organic compound, for example, choline ellagate compound(s), and uses and formulations thereof.
    Type: Application
    Filed: November 28, 2023
    Publication date: March 21, 2024
    Inventors: Michael REYES, Robert CABRERA
  • PROCESS FOR THE PREPARATION OF ERIBULIN
    Publication number: 20240092798
    Abstract: The present invention relates to a process for the preparation of Eribulin.
    Type: Application
    Filed: December 2, 2021
    Publication date: March 21, 2024
    Applicant: FineTech Pharmaceutical Ltd.
    Inventors: Igor RUKHMAN, Igor ZALTSMAN, Lev YUDOVICH, Olga GROSSMAN, Irina FEDOTEV, Arie GUTMAN
  • MNK INHIBITORS
    Publication number: 20240092799
    Abstract: The present technology is directed to compounds, compositions, and methods related to modulation of MNK. In particular, the present compounds and compositions may be used to treat MNK-mediated disorders and conditions, including, e.g., various solid and hematological cancers.
    Type: Application
    Filed: August 20, 2021
    Publication date: March 21, 2024
    Inventors: Cheng MO, Xiaodong Xu
  • USP13 INHIBITORS AND METHODS OF USE THEREOF
    Publication number: 20240092800
    Abstract: Novel ubiquitin specific protease 13 (USP13) inhibitors are provided, along with methods for their use. The USP13 inhibitors described herein are useful in treating and/or preventing USP13-related diseases, such as neurodegenerative diseases and cancer. Also provided are methods for inhibiting USP13 in a cell using the compounds and compositions described herein.
    Type: Application
    Filed: January 14, 2022
    Publication date: March 21, 2024
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Charbel MOUSSA, Christian WOLF, Balaraman KALUVU
  • ALLOSTERIC AKT INHIBITORS FOR USE IN THE TREATMENT OF HEREDITARY HEMORRHAGIC TELANGIECTASIA
    Publication number: 20240092801
    Abstract: The present invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, for use in the treatment of Hereditary Hemorrhagic Telangiectasia (HHT).
    Type: Application
    Filed: September 29, 2021
    Publication date: March 21, 2024
    Inventors: Damien PICARD, Pierre SAINT-MEZARD
  • MU-OPIOID RECEPTOR AGONISTS AND USES THEREFOR
    Publication number: 20240092802
    Abstract: The present disclosure relates to a compound having the structure: Formula (I) or a pharmaceutically acceptable salt or ester thereof, for treating or preventing a neurological disorder, including Huntington's disease, Rett syndrome, and CDKL5 disorder.
    Type: Application
    Filed: October 6, 2021
    Publication date: March 21, 2024
    Inventor: Andrew Kruegel
  • BRIDGED COMPOUNDS AS KRAS G12D INHIBITOR AND DEGRADER AND THE USE THEREOF
    Publication number: 20240092803
    Abstract: The disclosure herein provides bridged compounds as well as their compositions and methods of use. The compounds disclosed herein inhibit KRAS G12D activity and are useful in the treatment of various diseases including cancer.
    Type: Application
    Filed: January 7, 2022
    Publication date: March 21, 2024
    Inventors: Qi JI, Chao YU, Ce WANG, Hanzi SUN
  • SCANDIUM PRECURSOR FOR SC2O3 OR SC2S3 ATOMIC LAYER DEPOSITION
    Publication number: 20240092804
    Abstract: Described are precursor compounds and methods for atomic layer deposition of films containing scandium(III) oxide or scandium(III) sulfide. Such films may be utilized as dielectric layers in semiconductor manufacturing processes, particular for depositing dielectric films and the use of such films in various electronic devices.
    Type: Application
    Filed: November 28, 2023
    Publication date: March 21, 2024
    Applicant: Intel Corporation
    Inventor: Patricio E. ROMERO
  • BORON-CONTAINING COMPOUND AND ELECTROLYTE SOLUTION ADDITIVE FOR SECONDARY BATTERY INCLUDING THE SAME
    Publication number: 20240092805
    Abstract: Provided are a novel boron-containing compound and an electrolyte solution additive for a secondary battery including the same. The electrolyte solution for a secondary battery provided in one embodiment includes the novel boron-containing compound, thereby suppressing the decomposition of an electrolyte solution to improve the capacity and the life characteristics of a battery.
    Type: Application
    Filed: November 6, 2023
    Publication date: March 21, 2024
    Inventors: Myoung Lae KIM, Chanwoo KIM, Yu Na SHIM, Jaechan RYU, Cholho LEE, Han Sol LEE
  • BORON-CONTAINING COMPOUND AND ELECTROLYTE ADDITIVE FOR SECONDARY BATTERY CONTAINING THE SAME
    Publication number: 20240092806
    Abstract: The present disclosure relates to a novel boron-containing compound and an electrolyte additive for a secondary battery containing the same. An electrolyte for a secondary battery provided in one embodiment contains the novel boron-containing compound, such that decomposition of the electrolyte may be suppressed, thereby improving a capacity and a lifespan of the battery.
    Type: Application
    Filed: November 8, 2023
    Publication date: March 21, 2024
    Inventors: Myoung Lae KIM, Chanwoo KIM, Yu Na SHIM, Jaechan RYU, Cholho LEE, Han Sol LEE
  • PROCESS FOR BORON-CONTAINING COMPOUNDS
    Publication number: 20240092807
    Abstract: Described herein are boron-containing compounds, compositions, and methods for their preparation.
    Type: Application
    Filed: August 5, 2021
    Publication date: March 21, 2024
    Inventor: Julian Rudolf KUTTNER