Abstract: The present invention relates to chromen-4-one derivatives, and to associated multi-salts, solvates, and pharmaceutical compositions. The present invention also relates to the use of such compounds and compositions in the treatment and prevention of cancer.
Abstract: Described herein are novel methods of synthesizing 5-Bromo-2-(3-chloro-pyridin-2-yl)-2H-pyrazole-3-carboxylic acid from pyrazole or pyrazole derivatives.
Abstract: In one aspect, the disclosure relates to substituted N-(2-(2,6-dioxopiperidinyl-3-yl)-1,3-dioxoisoindolin-5-yl)arylsulfonamide analogs that useful as modulators of cereblon (CRBN) activity, methods of making same, pharmaceutical compositions comprising same, and methods of treating various clinical conditions and disorders using same, e.g., a disorder of uncontrolled cellular proliferation, such as a cancer, which may be associated with cereblon protein dysfunction and/or a GSPT1 dysfunction. In various further aspects, the disclosed compounds can selectively modulate the degradation of GSPT1 protein, i.e., the disclosed compounds can act as GSPT1 degraders. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
Type:
Application
Filed:
September 14, 2023
Publication date:
April 25, 2024
Inventors:
Marcus FISHER, Fatemeh KERAMATNIA, Kevin MCGOWAN, Jaeki MIN, Gisele A. NISHIGUCHI, Jeanine PRICE, Zoran RANKOVIC, Sourav Das, Charles G. MULLIGHAN, Yunchao CHANG
Abstract: The present disclosure relates to novel compounds that inhibit glucose-induced degradation-deficient (GID) E3 ligase, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and related diseases and conditions.
Type:
Application
Filed:
September 27, 2023
Publication date:
April 25, 2024
Applicant:
Accutar Biotechnology Inc.
Inventors:
Ji Liu, Yimin Qian, Pin Huang, Xiangyan Sun, Ke Liu, Jie Fan
Abstract: Described herein are MAT2A inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of a disease or disorder associated with MAT2A.
Abstract: Compounds of general formula (I): (I) wherein R1, R2, R3, R4, R5, Y and Z are as defined herein are useful for treating respiratory disease and other diseases and conditions modulated by TMEM16A.
Type:
Application
Filed:
June 9, 2023
Publication date:
April 25, 2024
Applicant:
TMEM16A Limited
Inventors:
Stephen COLLINGWOOD, Jonathan David Hargrave, Duncan Alexander Hay, Clive McCarthy, Thomas Beauregard Schofield, Edward Walker, Naomi Went
Abstract: The present invention relates to compound having the following Formula (I) a semiconducting layer comprising this compound, an organic electronic device comprising said organic semiconducting layer, as well as to a device comprising the organic electronic device.
Type:
Application
Filed:
October 8, 2020
Publication date:
April 25, 2024
Inventors:
Elena Galán García, Benjamin Schulze, Domagoj Pavicic, Lidia Marin
Abstract: Provided herein are novel heterocyclic compounds, for example, compounds having Formula I, I-P, II, II-P, III, or IV. Also provided herein are pharmaceutical compositions comprising the compounds and methods of using the same, for example, in inhibiting aldehyde dehydrogenases, retinoid pathway activation, and/or for treating various cancers, cancer metastasis, type 2 diabetes, pulmonary arterial hypertension (PAH) or neointimal hyperplasia (NIH) or as a male contraceptive.
Type:
Application
Filed:
October 17, 2023
Publication date:
April 25, 2024
Applicants:
KayoThera Inc., The Trustees of Princeton University
Inventors:
Mark ESPOSITO, John PROUDFOOT, Yibin KANG, John PIWINSKI
Abstract: The present invention relates to the following compounds wherein the integers are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of tuberculosis.
Type:
Application
Filed:
November 29, 2023
Publication date:
April 25, 2024
Inventors:
Jérôme Émile Georges Guillemont, Magali Madeleine Simone Motte, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri
Abstract: The invention relates to novel compounds having the general formula Ib wherein R1, R2, R1, R4, R5 and Z are as described herein, composition including the compounds and methods of using the compounds.
Type:
Application
Filed:
November 30, 2023
Publication date:
April 25, 2024
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Lea Aurelie BOUCHE, Wolfgang GUBA, Georg JAESCHKE, Stefanie Katharina MESCH, Angélique PATINY-ADAM, Christian SCHNIDER, Sandra STEINER, Andreas Michael TOSSTORFF
Abstract: A solid form of 1-(4-{[6-Amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone, or pharmaceutically acceptable salts thereof, is useful as a BTK inhibitor.
Type:
Application
Filed:
December 7, 2023
Publication date:
April 25, 2024
Applicant:
Merck Patent GmbH
Inventors:
Michael LANGE, Clemens Kuetin, Tobias Schiueter, Werner Mederski, David Maillard, Edoardo Burini
Abstract: The present invention relates to the technical field of biomedicine, in particular to a sulfoximide substituted indazole compound, an isomer thereof, or a pharmaceutically acceptable salt thereof.
Abstract: Provided are compounds useful for treating of cancer and methods for treating of cancer, comprising administering to a subject in need thereof a compound described therein.
Type:
Application
Filed:
May 8, 2023
Publication date:
April 25, 2024
Inventors:
Samuel V. Agresta, Chong-Hui Gu, David Schenkein, Hua Yang, Liting Guo, Zhen Tang, Jianming Wang, Yanfeng Zhang, Yan Zhou
Abstract: The present invention is directed to compound of formula (I) and, a pharmaceutically acceptable salt or a stereoisomer thereof that useful as MALT-1 inhibitors for the treatment of diseases or disorders dependent on MALT-1. The present invention also relates to a method of preparation of the said compounds and pharmaceutical compositions comprising the said compounds.
Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which is associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH).
Type:
Application
Filed:
October 25, 2023
Publication date:
April 25, 2024
Inventors:
Guoqiang Wang, Ruichao Shen, Brett Granger, Jing He, Xuechao Xing, Yong He, Jiang Long, Jun Ma, Bin Wang, Yat Sun Or
Abstract: The invention relates to benzimidazoles of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.
Type:
Application
Filed:
December 13, 2021
Publication date:
April 25, 2024
Applicant:
Pfizer Inc.
Inventors:
Scott William Bagley, Agustin Casimiro Garcia, Jennifer Elizabeth Davoren, Rajiah Aldrin Denny, Brian Stephen Gerstenberger, Frank Eldridge Lovering, Mihir Dineshkumar Parikh, Joseph Walter Strohbach, John Isidro Trujillo
Abstract: The invention relates to cocrystals comprising a substituted 2-oxo-1-pyrrolidinyl triazole of formula (I) and a carboxylic acid of formula (II).
Type:
Application
Filed:
November 1, 2021
Publication date:
April 25, 2024
Inventors:
Andrew BAXTER, Suzanne BUTTAR, Dyanne CRUIKSHANK, Adam PATTERSON
Abstract: A liner in a label-liner combination is provided with a die cut portion made in the liner. The die cut portion is aligned with at least one edge in a label and a front side of the liner is attached to a backside of the label. The die cut portion of the liner is adapted to be removed from the liner when the label is removed from the label-liner combination. Dimensions, and orientation, and a location of the die cut portion in the liner are adapted to allow the label to be removed from the label-liner combination and applied to a surface by digits of a hand without touching an adhesive coating on the backside of the label and adapted to maintain proper printer waste liner spool operations when the liner is wound after application of the label.
Type:
Application
Filed:
January 28, 2022
Publication date:
April 25, 2024
Inventors:
Robert B. Abramovitch, Edmund Ellsworth, John Williams
Abstract: There are provided a compound of Formula (1) and a labeled biological substance having the compound. A ring Z1 and a ring Z2 represent a 6-membered ring formed of a ring-constituting atom selected from a carbon atom and a nitrogen atom. R1 to R4, R11 to R13, L1, and L2 represents specific groups, and n, ?1, and ?2 represent specific numbers. At least one of R11, R12, or R13 contains a carboxy group or a substituent capable of being bonded to a biological substance. the compound represented by Formula (1) has at least one structure represented by —(CH2—CH2—O)m—R21, where R21 represents a specific group, and m represents a specific number. The compound represented by Formula (1) is a neutral compound.
Abstract: The present invention relates to a benzo seven-membered ring bifunctional compound and an application thereof, and in particular to a compound represented by formula (IV) and a pharmaceutically acceptable salt thereof. The compound can be used for preparing a drug for treating diseases related to an estrogen receptor protein degradation targeting chimera.
Type:
Application
Filed:
January 29, 2022
Publication date:
April 25, 2024
Applicants:
CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., MEDSHINE DISCOVERY INC.
Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
Type:
Application
Filed:
November 20, 2023
Publication date:
April 25, 2024
Applicant:
Pfizer Inc.
Inventors:
Gary Erik Aspnes, Scott W. Bagley, Edward L. Conn, John M. Curto, David J. Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Chris Limberakis, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
Abstract: Compounds and methods of using the same for treating conditions alleviated by SKI complex inhibition, viral replication inhibition, or interferon signaling inducement are provided.
Type:
Application
Filed:
December 3, 2021
Publication date:
April 25, 2024
Inventors:
Matthew Frieman, Alexander D. Mackerell, JR., Stuart WESTON
Abstract: The present invention relates to compounds with the ability to stimulate/induce ubiquitination of a target protein/target proteins. The compounds of the present invention may stimulate/induce ubiquitination of a target protein/target proteins; i.e. via degradation of a target protein/target proteins by the cullin-RING ubiquitin ligase (CRL). Such target protein/target proteins may be proteins involved in diseases, like cancer, metabolic disorder, infectious disease and/or neurological disorder. The invention also relates to the compounds and composition for use as medicaments as well as pharmaceutical compositions comprising these compounds. Particularly, the compounds of the present invention may degrade proteins associated with cancer, metabolic disorder, infectious disease and/or neurological disorder.
Type:
Application
Filed:
October 15, 2021
Publication date:
April 25, 2024
Inventors:
Georg WINTER, Cristina MAYOR RUIZ, Stefan KUBICEK, Alastair David Graham DONALD, Grasilda ZENKEVICIUTE
Abstract: The present invention provides compounds and pharmaceutical compositions comprising thereof. Further, methods for treating or preventing development of a RNF4 related disorder in a subject in need thereof are also provided.
Type:
Application
Filed:
September 21, 2023
Publication date:
April 25, 2024
Inventors:
Amir ORYAN (ORIAN), Ashraf BRIK, Yamen ABU AHMAD, Satish GANDHESIRI
Abstract: Disclosed are TRPM8 modulators as defined by formula (I) for achieving a cooling effect on skin and mucousa.
Type:
Application
Filed:
October 15, 2020
Publication date:
April 25, 2024
Inventors:
Nicolas COCITO ARMANINO, Agnes BOMBRUN, An CHAI, Julie CHARPENTIER, Chun CHEN, Roger EMTER, Marion MATHYS, Andreas NATSCH, Chao WANG, Lijun ZHOU
Abstract: The present invention belongs to the medical field, and relates to novel ?-lactamase inhibitors, for the treatment of bacterial infections in combination with ?-lactam antibiotics, including infection caused by drug resistant organisms and especially multi-drug resistant organisms. The present invention includes compounds according to formula (I): or pharmaceutically acceptable salts thereof, wherein M and R are as defined herein.
Abstract: An aromatic heterocyclic compound, a pharmaceutical composition and use thereof. Specifically disclosed are a compound as shown in formula I, a stereoisomer thereof, a diastereomer thereof, or a pharmaceutically acceptable salt of any one of the foregoing, or a crystal form or solvate of any one of the foregoing. The aromatic heterocyclic compound has a novel structure, good CDK7 inhibitory activity, and good selectivity.
Abstract: Described herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof and solvates of any of the foregoing capable of inhibiting protein kinase A and/or its mutants, pharmaceutical compositions comprising at least one of the compounds, pharmaceutically acceptable salts thereof, and solvates of any of the foregoing, processes for making the compounds, pharmaceutically acceptable salts thereof, and solvates of any of the foregoing, and methods of using the same.
Type:
Application
Filed:
February 1, 2022
Publication date:
April 25, 2024
Applicant:
Blueprint Medicines Corporation
Inventors:
Neil Bifulco, Joseph L. Kim, Stefanie Sandra Schalm, Kevin J. Wilson, Michael Ross Palmer
Abstract: An indoline compound. Specifically disclosed is an application of a compound represented by formula (I) and pharmaceutically acceptable salts thereof in the preparation of drugs for treating related diseases.
Type:
Application
Filed:
February 8, 2022
Publication date:
April 25, 2024
Inventors:
Jianyu LU, Charles Z. DING, Huijun HE, Lihong HU, Yuanyuan HUANG, Jian LI, Shuhui CHEN
Abstract: The present disclosure provides a class of Pyridopyrimidine compounds having a structure shown in Formula (I) or their pharmaceutically acceptable salts, or stereoisomers or prodrug molecules and applications thereof. The compounds in the present disclosure can efficiently and selectively degrade AKT3 protein in cells without affecting AKT1/2, thereby significantly inhibiting tumor cell proliferation mediated by high expression of AKT3 protein. It can be used to prepare therapeutic drugs for cancer and other diseases related to abnormal expression of AKT3 protein.
Type:
Application
Filed:
September 6, 2023
Publication date:
April 25, 2024
Applicants:
JINAN UNIVERSITY, SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES
Abstract: Described herein, inter alia, are imidazopyridine derivatives (I), pharmaceutically acceptable salts and tautomers thereof, compounds, combinations and medicaments containing said compounds and processes for their preparation. In embodiments, the imidazopyridine derivatives can be used as regulators of a stimulator of interferon genes (STING) and a related signal path thereof, and can effectively treat and/or relieve multiple types of diseases, including but not limited to malignant tumors, inflammations, autoimmune diseases, infectious diseases and as vaccine adjuvants.
Abstract: Described herein are compounds having the following structure: or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof. Also disclosed are compositions containing the compounds, methods of inhibiting activity of DYRK1A in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.
Type:
Application
Filed:
November 28, 2023
Publication date:
April 25, 2024
Inventors:
Kunal KUMAR, Peng WANG, Roberto SANCHEZ, Adolfo OCAÑA, Andrew STEWART, Robert DEVITA
Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the Formula I including stereoisomers and pharmaceutically acceptable salts thereof, wherein R2a, R2b, R3, R3a, R4, R6, R7, R8, A, Z, X1 and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Application
Filed:
November 29, 2023
Publication date:
April 25, 2024
Applicant:
CHEMOCENTRYX, INC.
Inventors:
Pingchen FAN, Christopher W. LANGE, Rebecca M. LUI, Darren J. McMURTRIE, Ryan J. SCAMP, Ju YANG, Yibin ZENG, Penglie ZHANG
Abstract: An ionic compound, an absorbent and an absorption device are provided. The ionic compound has a structure represented by Formula (I): ABn, ??Formula (I) wherein A is B is R1, R2, R3, R4, R5, and R6 are independently H, C1-6 alkyl group; and n is 1 or 2.
Type:
Application
Filed:
June 9, 2023
Publication date:
April 25, 2024
Applicant:
Industrial Technology Research Institute
Abstract: The present invention provides in one aspect azabicyclo and diazepine derivatives useful as modulators of muscarinic receptors. In another aspect, the present invention provides pharmaceutical compositions for treating ocular diseases, the compositions comprising at least one muscarinic receptor modulator.
Abstract: Provided herein are crystalline forms of 5-(3,4-difluorobenzyl)-8-((1r,4r)-4-methylcyclohexyl)-6,9-dioxo-2,5,8-triazaspiro[3.5]nonane-2-carbaldehyde, compositions thereof, methods of preparation thereof, and methods of their uses.
Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
Type:
Application
Filed:
March 28, 2023
Publication date:
April 25, 2024
Inventors:
Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
Abstract: The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.
Type:
Application
Filed:
August 21, 2023
Publication date:
April 25, 2024
Applicant:
Praxis Precision Medicines, Inc.
Inventors:
Andrew Mark Griffin, Brian Edward Marron, Gabriel Martinez Botella
Abstract: The present disclosure relates to novel compounds that degrade Bruton's tyrosine kinase (BTK), pharmaceutical compositions containing such compounds, and their use in prevention and treatment of conditions modulated by BTK.
Type:
Application
Filed:
February 2, 2022
Publication date:
April 25, 2024
Applicant:
ACCUTAR BIOTECHNOLOGY INC.
Inventors:
Yimin Qian, Wei HE, Robert LUO, Jie SU, Hui ZHANG, Ke LIU, Jie FAN
Abstract: Provided are a salt form and a crystal form of a pyrazole substituted imidazo[1,2-a]quinoxaline derivative, and a preparation method therefor. Specifically disclosed are a salt form and a crystal form of a compound of formula (I), and a preparation method therefor and the use thereof in the preparation of drugs related to dual inhibitors of spleen tyrosine kinase (Syk) and vascular endothelial growth factor 2 (VEGFR2).
Abstract: The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, bonds a, b, c and d, X1, X2, X3, X4, R2, and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.
Type:
Application
Filed:
May 4, 2023
Publication date:
April 25, 2024
Applicant:
Cancer Research Technology Limited
Inventors:
Allan Jordan, Rebecca Newton, George Hynd, Jonathan Mark Sutton, Bohdan Waszkowycz
Abstract: Disclosed herein are arylpyridinone compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structures of Formulas (I)-(IV): wherein the R groups, m, n, and X are as defined in the detailed description. Methods of inhibition of ITK activity in a human or animal subject are also provided.
Type:
Application
Filed:
October 24, 2023
Publication date:
April 25, 2024
Inventors:
Eric Jon JACOBSEN, David Randolph ANDERSON, James Robert BLINN, Susan Landis HOCKERMAN, Richard HEIER, Paramita MUKHERJEE
Abstract: Presently provided are inhibitors of TD02 and IDO1 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
Abstract: Methods for preparing the Bruton's Tyrosine Kinase (“BTK”) inhibitor compound 2-{3?-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4?]bipyridinyl-2?-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided.
Type:
Application
Filed:
November 3, 2023
Publication date:
April 25, 2024
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Stephan BACHMANN, Lukas CHYTIL, Serena Maria FANTASIA, Alec FETTES, Ursula HOFFMANN, Christian Oliver KAPPE, Rene LEBL, Kurt PUENTENER, Paolo TOSATTI, Jason Douglas WILLIAMS
Abstract: Disclosed are quinoline and quinazoline compounds which modulate the activity of the gated ion channels. Compounds that modulate these gated ion channels are useful in the treatment of diseases and disorders related to pain, inflammation, the neurological system, the gastrointestinal system and genitourinary system. Preferred compounds include quinoline or quinazoline derivatives substituted at the 4-position via N(H), C(O) or O moieties.
Type:
Application
Filed:
November 13, 2023
Publication date:
April 25, 2024
Inventors:
Nadiya Sydorenko, Md Rauful Alam, Michael A. Arnold, Suresh Babu, Anuradha Bhattacharyya, Guangming Chen, Aleksey I. Gerasyuto, Gary Mitchell Karp, Andrew J. Kassick, Anthony R. Mazzotti, Young-Choon Moon, Jana Narasimhan, Jigar Patel, Anthony Turpoff, Matthew G. Woll, Wuming Yan, Nanjing Zhang
Abstract: Crystalline Forms of Compound (I): pharmaceutically acceptable salts thereof and solvates of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating disorders and conditions associated with oncogenic KIT and PDGFRA alterations using the same, and methods for making Compound (I) and crystalline forms thereof are also disclosed.
Type:
Application
Filed:
December 18, 2023
Publication date:
April 25, 2024
Inventors:
Joshua D. Waetzig, Brenton Mar, Gordon Wilkie