Patents Issued in April 18, 2024
  • Publication number: 20240124435
    Abstract: The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
    Type: Application
    Filed: September 27, 2023
    Publication date: April 18, 2024
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Matthew Lucas, Bertrand Le Bourdonnec, Iwona Wrona, Bhaumik Pandya, Parcharee Tivitmahaisoon, Kerem Ozboya, Benjamin Vincent, Daniel Tardiff, Jeff Piotrowski, Eric Solis, Robert Scannevin, Chee-Yeun Chung, Rebecca Aron, Kenneth Rhodes
  • Publication number: 20240124436
    Abstract: A fluorine-containing pyrimidine compound represented by formula (1), (2) or (3) is provided: wherein in formulae (1) to (3), R represents a hydrocarbon group having 1 to 12 carbon atoms, X and Y each independently represent a hydrogen atom, a halogen atom, a hydrocarbon group having 1 to 10 carbon atoms, —CnF2n+1, a nitro group, a boronic acid group, —OA1, —SOmA1, —NA1A2, —COOA1 or —CONA1A2, Z represents CW or N, W represents a hydrogen atom, a halogen atom, a hydrocarbon group having 1 to 10 carbon atoms, —CnF2n+1, a nitro group, a boronic acid group, —OA1, —SOmA1, —NA1A2, —COOA1 or —CONA1A2, n is an integer of 1 to 10 and m is an integer of 0 to 3, and A1 and A2 each independently represent a hydrogen atom or a hydrocarbon group having 1 to 10 carbon atoms.
    Type: Application
    Filed: October 29, 2020
    Publication date: April 18, 2024
    Inventors: Junya SEINO, Rie AOTSU, Keisuke KOKIN
  • Publication number: 20240124437
    Abstract: The present disclosure relates to an injectable lurasidone suspension and a preparation method thereof, and in particular to an irregular form of a lurasidone solid and a pharmaceutical composition thereof. The present disclosure also relates to a preparation method for the solid and the pharmaceutical composition thereof, and an application thereof in the treatment of mental diseases. According to the present disclosure, the lurasidone solid prepared has controllable particle size and has Dv5O particle size of 6 ?m to 110 ?m. The good particle size stability can also he maintained in the pharmaceutical composition. The lurasidone suspension preparation obtained by the method is fast-acting, has a long sustained release period, and can effectively reduce the risk caused by poor patient compliance.
    Type: Application
    Filed: March 21, 2022
    Publication date: April 18, 2024
    Inventors: Ming LI, Xiangyong LIANG, Zhengxing SU, Dan LI, Duo KE, Cong YI, Wei WEI, Guifu DENG, Ya PENG, Dong ZHAO, Jingyi WANG
  • Publication number: 20240124438
    Abstract: Provided are a phenanthroline-based compound, a method of preparing the same, and a perovskite solar cell including the same. The phenanthroline-based compound may be formed as a uniform layer even by a solution process due to its low average surface roughness (root mean square, RMS) and excellent processability. When a layer having the phenanthroline-based compound is provided as a polymer functional layer of the perovskite solar cell, the ionic defects on the surface between the perovskite and a metal oxide, may be passivated and charge transfer may be facilitated so that the energy efficiency and photostability of the solar cell are improved.
    Type: Application
    Filed: August 29, 2023
    Publication date: April 18, 2024
    Inventors: Kwang Hee LEE, Hee Joo KIM, Yong Ryun KIM, Ju Hyeon KIM
  • Publication number: 20240124439
    Abstract: The invention relates to imidazopyridines of Formula (I) and pharmaceutically acceptable salts thereof, wherein R0 to R5 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 18, 2024
    Applicant: Pfizer Inc.
    Inventors: Scott William Bagley, Agustin Casimiro-Garcia, Jennifer Elizabeth Davoren, Rajiah Aldrin Denny, Brian Stephen Gerstenberger, Katherine Lin Lee, Frank Eldridge Lovering, Mihir Dineshkumar Parikh, Joseph Walter Strohbach, John Isidro Trujillo
  • Publication number: 20240124440
    Abstract: Described herein are compounds that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity.
    Type: Application
    Filed: December 16, 2021
    Publication date: April 18, 2024
    Inventors: Anjali PANDEY, Gregory DIETSCH, Bhaskar CHAUDHURI, Swapan Kumar SAMANTA, Seetharaman MANOJVEER, Mahesh THAKKAR, Athisayamani Jeyaraj DURAISWAMY, Sukesh KALVA
  • Publication number: 20240124441
    Abstract: The specification relates to a crystalline Latrepirdine dihydrochloride, Form DMB-I, method of its preparation, pharmaceutical composition containing it and its uses.
    Type: Application
    Filed: January 31, 2022
    Publication date: April 18, 2024
    Inventors: Boris GORINE, Marina YUROVSKAYA
  • Publication number: 20240124442
    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: February 3, 2022
    Publication date: April 18, 2024
    Applicant: AMGEN INC.
    Inventors: Albert AMEGADZIE, Diane Jennifer BEYLKIN, Shon BOOKER, Matthew Paul BOURBEAU, John R. BUTLER, Kevin Lloyd GREENMAN, Todd J. KOHN, Kexue LI, Qingyian LIU, Ana Elena MINATTI, Primali Vasundera NAVARATNE, Liping H. PETTUS, Rene RAHIMOFF, Hui-Ling WANG, Nicholas Anthony WEIRES
  • Publication number: 20240124443
    Abstract: The present invention relates to a compound of formula (I) capable of inhibiting plasmin activity and having blood coagulation and hemostasis activity, and a pharmaceutically acceptable salt, hydrate, isomer, prodrug and mixture thereof, wherein R1 to R3 are as defined in the description.
    Type: Application
    Filed: January 28, 2022
    Publication date: April 18, 2024
    Inventors: Anle YANG, Sen JI, Zhi WANG, Hao WANG, Dewei ZHANG, Xiao WANG, Huan SHEN, Jie XIANG, Jialing XIAN, Yan WANG, Xiao HU, Xiaodong ZHANG, Jun TANG
  • Publication number: 20240124444
    Abstract: Provided herein are compounds of Formula (I) and pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R1, R2, R3, R4 and R5 are as defined herein (referred to herein as “Heterocyclic Compounds”), compositions comprising an effective amount of a Heterocyclic Compound, as well as methods of preventing and/or treating cryptosporidiosis and/or inhibiting a parasite or parasitic activity.
    Type: Application
    Filed: December 27, 2021
    Publication date: April 18, 2024
    Applicant: Celgene Corporation
    Inventors: Dale E. Robinson, Natalie Hawryluk, Stacie Canan
  • Publication number: 20240124445
    Abstract: The present invention relates to a benzene ring compound and a use thereof. In particular, provided is a compound as shown in formula I, or an optical isomer thereof or a racemate thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 17, 2021
    Publication date: April 18, 2024
    Applicant: NANJING SHIJIANG MEDICINE TECHNOLOGY CO., LTD
    Inventors: Yufeng SHI, Wenjiang MA
  • Publication number: 20240124446
    Abstract: The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
    Type: Application
    Filed: April 28, 2023
    Publication date: April 18, 2024
    Inventors: Lara C. CZABANIUK, Timothy HOPPER, Jonathan B. HOUZE, Gwenaella RESCOURIO, Vincent SANTORA, Haoxuan WANG, Ryan D. WHITE, Alice R. WONG, Yongwei WU
  • Publication number: 20240124447
    Abstract: The present invention is directed to inhibitors of the interaction of menin with MLL and MLL fusion proteins, pharmaceutical compositions containing the same, and their use in the treatment of cancer and other diseases mediated by the menin-MLL interaction.
    Type: Application
    Filed: May 18, 2023
    Publication date: April 18, 2024
    Applicant: Vitae Pharmaceuticals, LLC
    Inventors: Salvacion CACATIAN, David A. CLAREMON, Chengguo DONG, Yi FAN, Lanqi JIA, Stephen D. LOTESTA, Suresh B. SINGH, Shankar VENKATRAMAN, Jing YUAN, Yajun ZHENG, Linghang ZHUANG
  • Publication number: 20240124448
    Abstract: The invention provides a novel class of therapeutic agents that are safe and effective TYK2 inhibitors and pharmaceutical compositions of these compounds and methods of preparation and use thereof against various TYK2-mediated diseases and disorders.
    Type: Application
    Filed: September 25, 2023
    Publication date: April 18, 2024
    Inventors: Zhaokui Wan, Michael Lawrence Vazquez, Gurmit Grewal, Xiaodong Li, Lin Su, Jingyu Wu
  • Publication number: 20240124449
    Abstract: Provided are compounds, compositions and methods for inhibiting fascin activity or treating a condition or disorder mediated by fascin activity in a subject in need thereof.
    Type: Application
    Filed: December 21, 2023
    Publication date: April 18, 2024
    Applicants: NOVITA PHARMACEUTICALS, INC., CORNELL UNIVERSITY
    Inventors: Xin-Yun Huang, Christy Young Shue
  • Publication number: 20240124450
    Abstract: A compound of formula I having the structure: or a pharmaceutically acceptable salt thereof, wherein A1 and A2 are independently O or S; X is selected from CH2, CD2, NR3, O, and S, where R3 is selected from hydrogen, C1-C4 linear or branched chain alkyl, halo(C1-C4)linear or branched chain alkyl, and hydroxyl(C1-C4)linear or branched chain alkyl; Y and Z are selected from C and N, where when Y is C, then Z is N, and when Y is N, then Z is C; R1 and R2 are independently selected from hydrogen, deuterium, C1-C4 linear or branched chain alkyl, etc.; or a C1-C2 alkyl substituted with a C3-C5 cycloalkyl ring; or taken together to form a C3-C6 cycloalkyl ring; or where X is CH2 or CD2, then R1 and R2 are independently selected from hydrogen, deuterium, halogen, hydroxyl, C1-C4 linear or branched chain alkyl, etc.; R4 is selected from hydrogen, deuterium, cyano, halogen, (C1-C3) alkoxy, etc.; R5 is selected from hydrogen, deuterium, halogen, C1-C3 alkoxy, amino, (C1-C4 linear or branched chain alkyl)amino, etc.
    Type: Application
    Filed: September 13, 2023
    Publication date: April 18, 2024
    Applicant: Pfizer Inc.
    Inventors: Andrea Nicole Bootsma, David Christopher Ebner, Daniel Wei-Shung Kung, Matthew Alexander Perry, Daniel Copley Schmitt, Joseph Walter Strohbach, Atli Thorarensen
  • Publication number: 20240124451
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of NLRP3 and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by NLPR3. The compounds of the present invention may be useful in the treatment, prevention or management of diseases, disorders and conditions mediated by NLRP3 such as, but not limited to, gout, pseudogout, CAPS, NASH fibrosis, heart failure, idiopathic pericarditis, atopic dermatitis, inflammatory bowel disease, Alzheimer's Disease, Parkinson's Disease and traumatic brain injury.
    Type: Application
    Filed: September 21, 2023
    Publication date: April 18, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Donna A.A.W. Hayes, Prabha Karnachi, Madeleine Eileen Kieffer, Kyle S. McClymont, Rohan Rajiv Merchant, Essam Metwally, Anilkumar G. Nair, Ning Qi, Jillian Rose Sanzone, Nunzio Sciammetta, Emma H. Southgate, Zheng Tan, Brandon M. Taoka
  • Publication number: 20240124452
    Abstract: The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
    Type: Application
    Filed: November 16, 2023
    Publication date: April 18, 2024
    Inventors: Andrew BELFIELD, Clifford David Jones, Jean-François Margathe, Chiara Colletto
  • Publication number: 20240124453
    Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Application
    Filed: November 17, 2023
    Publication date: April 18, 2024
    Applicant: Array BioPharma Inc.
    Inventors: James Francis BLAKE, Mark Laurence BOYS, Mark Joseph CHICARELLI, Adam Wade COOK, Mohamed S. A. ELSAYED, Jay Bradford FELL, John P. FISCHER, Ronald Jay HINKLIN, Yutong JIANG, Oren Teague MCNULTY, Macedonio J. MEJIA, Martha E. RODRIGUEZ, Christina Elizabeth WONG
  • Publication number: 20240124454
    Abstract: The compound as shown in formula (I) or a pharmaceutically acceptable salt or pharmaceutical composition thereof, and a preparation method therefor, and the use thereof as an MAT2A inhibitor. Ring A, ring Q, X, Y, X1, X2, L and R1 in formula (I) are as defined in the description.
    Type: Application
    Filed: December 30, 2021
    Publication date: April 18, 2024
    Inventors: Zhen Li, Feng Tang, Le Liu, Chunyan Zhao, Ping Chen, Renhong Tang, Jinsheng Ren
  • Publication number: 20240124455
    Abstract: The present invention is directed to tricyclic compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: January 21, 2022
    Publication date: April 18, 2024
    Inventors: Ying HAN, Dapeng LI, Huajun LONG, Tong WANG, Zhiyu YIN, Yu WANG
  • Publication number: 20240124456
    Abstract: An aza-ergoline derivative and a preparation method therefor and an application thereof. The derivative has a structure as shown in formula (I). The aza-ergoline derivative has good affinity, agonistic activity or selectivity to a dopamine D2 receptor.
    Type: Application
    Filed: January 29, 2022
    Publication date: April 18, 2024
    Inventors: Jianjun CHENG, Sheng WANG, Huan WANG, Luyu FAN, Zhangcheng CHEN, Jing YU, Jianzhong QI, Fen NIE
  • Publication number: 20240124457
    Abstract: Described herein are cyclic amide-containing pyridyl-xanthines of formula I and pharmaceutical compositions thereof that are useful as antagonists of A2B adenosine receptors.
    Type: Application
    Filed: October 16, 2023
    Publication date: April 18, 2024
    Inventor: Robert D. Thompson
  • Publication number: 20240124458
    Abstract: The present invention relates to crystalline and non-crystalline forms of avapritinib, to processes for their preparation, and to pharmaceutical compositions containing the crystalline or non-crystalline forms.
    Type: Application
    Filed: October 23, 2020
    Publication date: April 18, 2024
    Inventors: Thierry BONNAUD, Zoe PRENTICE
  • Publication number: 20240124459
    Abstract: This disclosure relates to compounds of formula (I) as defined in the Specification. This disclosure also relates to methods of synthesizing the compound of formula (I) and using the compounds of formula (I) for treating a disease (e.g., cancer).
    Type: Application
    Filed: June 28, 2021
    Publication date: April 18, 2024
    Inventors: Kenneth C. Anderson, Teru Hideshima, Sirano Dhe-Paganon, Hyuk-Soo Seo, Takashi Mizutani, Tinghu Zhang
  • Publication number: 20240124460
    Abstract: Provided are compounds of Formula (I) and pharmaceutically acceptable salts and compositions thereof, which are useful for treating cancers and related conditions.
    Type: Application
    Filed: October 12, 2021
    Publication date: April 18, 2024
    Inventors: Weiwen Ying, Kevin P. Foley, Wei Yin, Long Ye, Mingkai Wang, Chenghao Ying, Lingjie Zhang
  • Publication number: 20240124461
    Abstract: The present disclosure provides new procedures and intermediates for the preparation of Zanubrutinib.
    Type: Application
    Filed: December 10, 2021
    Publication date: April 18, 2024
    Inventors: Tihamér Paál, Zsuzsa Potarine Juhasz, Tomislav Biljan, Irena Nekola, Moris Mihovilovic
  • Publication number: 20240124462
    Abstract: New synthetic methods to provide access to previously unexplored functionality at the C8 position of substituted imidazo[5,1-d][1,2,3,5]tetrazines of Formula I. Through synthesis and evaluation of a suite of compounds with a range of aqueous stabilities (from 0.5 to 40 hours), a predictive model for imidazotetrazine hydrolytic stability based on the Hammett constant of the C8 substituent was derived. Promising compounds were identified that possess activity against a panel of GBM cell lines, appropriate hydrolytic and metabolic stability, and brain-to-serum ratios dramatically elevated relative to TMZ, leading to lower hematological toxicity profiles and superior activity to TMZ in a mouse model of GBM.
    Type: Application
    Filed: December 16, 2022
    Publication date: April 18, 2024
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Paul J. HERGENROTHER, Timothy M. FAN, Riley L. SVEC
  • Publication number: 20240124463
    Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
    Type: Application
    Filed: January 9, 2023
    Publication date: April 18, 2024
    Inventors: Yun-Long Li, Xiaozhao Wang, Joseph Barbosa, David M. Burns, Hao Feng, Joseph Glenn, Chunhong He, Taisheng Huang, Song Mei, Jincong Zhuo
  • Publication number: 20240124464
    Abstract: Provided in the present invention are a substituted fused bicyclic compound as a kinase inhibitor and the use thereof. The substituted fused bicyclic compound has a structure as represented by formula I below, wherein a ring A, R0, B1-B3, D1-D3, R7 and R8 are defined herein. The compound of formula I is an NUAK1/2 inhibitor. Therefore, the compound of the present invention can be used for treating and preventing NUAK1/2-mediated diseases, disorders and conditions, such as cancer, and used in the preparation of drugs for treating and preventing NUAK1/2-mediated diseases, disorders and conditions.
    Type: Application
    Filed: November 29, 2021
    Publication date: April 18, 2024
    Inventors: Sui Xiong CAI, Ye Edward TIAN, Xiaozhu WANG
  • Publication number: 20240124465
    Abstract: The present disclosure relates to chemical compounds that modulate JAK-2 signaling, which are useful in the treatment of disorders associated with JAK-2 signaling dysfunction such as, for example, disorders of cellular proliferation (e.g., cancer) and autoimmune and inflammatory disorders, pharmaceutical compositions containing such compounds, and their use in treatment. 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 invention.
    Type: Application
    Filed: December 17, 2021
    Publication date: April 18, 2024
    Inventors: Jaeki Min, Jamie Jarusiewicz, Marisa Actis, Yunchao Chang, Lisa Alcock, Charles Mulligan, Zoran Rankovic
  • Publication number: 20240124466
    Abstract: Provided are, inter alia, compounds having a structure of Formula (X), or a pharmaceutically acceptable salt thereof composition including the same and methods of use. Ring A, L1, L2, W, R2A, R2B, and R10 are as described herein.
    Type: Application
    Filed: December 10, 2021
    Publication date: April 18, 2024
    Inventors: Thomas D. BANNISTER, Corinne LASMEZAS, Minghai ZHOU, Nicole KENNEDY
  • Publication number: 20240124467
    Abstract: Disclosed herein are heterocyclic compounds that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific irreversible inhibitors of menin-MLL interaction. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the menin-MLL irreversible inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL interaction.
    Type: Application
    Filed: December 16, 2021
    Publication date: April 18, 2024
    Inventors: Thomas Butler, James T. PALMER, Thorsten KIRSCHBERG, Nan-Homg LIN, Hon HUI, Ravindra UPASANI, Solomon B. UNGASHE, David SPERANDIO
  • Publication number: 20240124468
    Abstract: Some embodiments of the disclosure include inventive compounds (e.g., compounds of Formula (I)) and compositions (e.g., pharmaceutical compositions) which inhibit IRAK and/or FLT3 and which can be used for treating, for example, certain diseases. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as hematopoietic cancers, myelodysplastic syndromes (MDS), acute myeloid leukemia (AML), etc.), Additional embodiments provide disease treatment using combinations of the inventive IRAK and/or FLT3 inhibiting compounds with other therapies, such as cancer therapies.
    Type: Application
    Filed: December 15, 2021
    Publication date: April 18, 2024
    Inventors: Scott Bryan HOYT, Craig Joseph THOMAS, Daniel T. STARCZYNOWSKI, Patrick Joseph SUTTER, Gregory James TAWA, Chris James FINOCCHIO, Jan Susan ROSENBAUM, Gabriel GRACIA MALDONADO
  • Publication number: 20240124469
    Abstract: A compound having a structure as shown in general formula (I), a deuterated compound, a stereoisomer, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising same, and use thereof. The compound has a good PIM kinase inhibitory effect, is a novel and ideal PIM inhibitor having high activity and low toxicity, and can be used for treating and/or preventing hematoma such as acute myeloid leukemia, bone marrow fibrosis and chronic lymphocytic leukemia, solid tumors such as gastric cancer and prostate cancer, and other diseases.
    Type: Application
    Filed: January 29, 2022
    Publication date: April 18, 2024
    Inventors: Xin YANG, Rong CUI, Jianming YIN, Mei ZHENG, Nanyu CHEN, Yubin LV
  • Publication number: 20240124470
    Abstract: A compound represented by general formula (I) or a stereoisomer, tautomer, deuterated substance, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, an intermediate thereof and a preparation method therefor, as well as an application in preparation of a drug for treating diabetes.
    Type: Application
    Filed: December 24, 2021
    Publication date: April 18, 2024
    Inventors: Chen ZHANG, Ming LEI, Mingliang ZHAO, Yan YU, Pingming TANG, Guanglin WENG, Tao MOU, Yao LI, Jia NI, Pangke YAN
  • Publication number: 20240124471
    Abstract: Disclosed are a salt (camsylate salt) of D(+)-10-camphorsulfonic acid and a triazolopyrazine derivative of formula (1), pharmaceutical compositions thereof, methods of making the salt, and therapeutic use thereof:
    Type: Application
    Filed: December 26, 2023
    Publication date: April 18, 2024
    Inventors: Jun Young CHOI, Kyung-eui PARK, Na Young KIM
  • Publication number: 20240124472
    Abstract: Disclosed are a salt (camsylate salt) of D(+)-10-camphorsulfonic acid and a triazolopyrazine derivative of formula (1), pharmaceutical compositions thereof, methods of making the salt, and therapeutic use thereof:
    Type: Application
    Filed: December 26, 2023
    Publication date: April 18, 2024
    Inventors: Jun Young CHOI, Kyung-eui PARK, Na Young KIM
  • Publication number: 20240124473
    Abstract: Disclosed are a salt (mesylate salt) of methanesulfonic acid and a triazolopyrazine derivative of formula (1), pharmaceutical compositions thereof, methods of making the salt, and therapeutic use thereof:
    Type: Application
    Filed: December 26, 2023
    Publication date: April 18, 2024
    Inventors: Jun Young CHOI, Kyung-eui PARK, Na Young KIM
  • Publication number: 20240124474
    Abstract: This invention relates to compounds of Formula (I): and enantiomers thereof, and to pharmaceutically acceptable salts of Formula (I) and said enantiomers, wherein L1, L2, R1, R2, R3 and n are as defined herein. The invention further relates to pharmaceutical compositions comprising such compounds and salts, and to methods and uses of such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject in need thereof.
    Type: Application
    Filed: November 1, 2023
    Publication date: April 18, 2024
    Applicant: Array BioPharma Inc.
    Inventors: Mark Laurence BOYS, Bryan Daniel ELLIS, John Joseph GAUDINO, Erik James HICKEN, Ellen Ruth LAIRD, Nicholas Charles LAZZARA, Bradley Jon NEWHOUSE, Spencer Phillip PAJK
  • Publication number: 20240124475
    Abstract: The present invention relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: September 28, 2023
    Publication date: April 18, 2024
    Inventors: Daniel W. Robbins, Arthur T. SANDS, Joel MCINTOSH, Jeffrey MIHALIC, Jeffrey WU, Daisuke KATO, Dahlia WEISS, Ge PENG
  • Publication number: 20240124476
    Abstract: Acyclic CB[n]-type compounds, methods of making such compounds, and uses of the compounds. For example, these compounds can be used as nanocontainers to solubilize pharmaceutical agents. Also provided are compositions and methods of using them for therapy or prophylaxis of a wide variety of conditions for which therapy or prophylaxis is desirable.
    Type: Application
    Filed: December 26, 2023
    Publication date: April 18, 2024
    Inventors: Lyle David Isaacs, Volker Briken, Gaya Hettiarachchi, Da Ma, Duc M. Nguyen
  • Publication number: 20240124477
    Abstract: A novel organic compound is provided. Alternatively, an organic compound that exhibits light emission with favorable chromaticity is provided. Alternatively, an organic compound that exhibits blue light emission with favorable chromaticity is provided. Alternatively, an organic compound with favorable emission efficiency is provided. Alternatively, an organic compound having a high carrier-transport property is provided. Alternatively, an organic compound with favorable reliability is provided. An organic compound including at least one amino group in which any one of a substituted or unsubstituted dibenzofuranyl group, a substituted or unsubstituted dibenzothiophenyl group, and a substituted or unsubstituted carbazolyl group is boneded to any one of a substituted or unsubstituted naphthobisbenzofuran skeleton, a substituted or unsubstituted naphthobisbenzothiophene skeleton, and a substituted or unsubstituted naphthobenzofuranobenzothiophene skeleton is provided.
    Type: Application
    Filed: October 23, 2023
    Publication date: April 18, 2024
    Applicant: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Kyoko Takeda, Harue Osaka, Satoshi Seo, Tsunenori Suzuki, Naoaki Hashimoto, Yusuke Takita
  • Publication number: 20240124478
    Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, CS, R2, and R3 are as described herein. The compounds or their pharmaceutically acceptable salts can inhibit the G12C mutant of Kirsten rat sarcoma (KRAS) protein and are expected to have utility as therapeutic agents, for example, for treating cancer. The disclosure also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The disclosure also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of cancer and for preparing pharmaceuticals for this purpose.
    Type: Application
    Filed: November 23, 2021
    Publication date: April 18, 2024
    Inventors: Yongxin Han, Elisabeth Hennessy, Andrew J. Hoover, Jesus Moreno, David L. Sloman, Uma Swaminathan, Yingchun Ye
  • Publication number: 20240124479
    Abstract: A pyrimidine carboxamide compound as shown in formula I, or a tautomer, mesomer, racemate, enantiomer and diastereomer thereof, or a mixture form thereof, or a pharmaceutically acceptable salt thereof, which can be used as a Vanin enzyme inhibitor, and can be used to prepare a medicament for treating various conditions, including Crohn's disease and ulcerative colitis.
    Type: Application
    Filed: December 17, 2021
    Publication date: April 18, 2024
    Inventors: Yuanshan Yao, Linbo Luan, Yongkai Chen, Chaodong Wang
  • Publication number: 20240124480
    Abstract: The present document is directed to methods for producing therapeutically active limonoids as well as new limonoid-type compounds.
    Type: Application
    Filed: September 19, 2023
    Publication date: April 18, 2024
    Inventors: Jacob Westman, Catarina Malmberg
  • Publication number: 20240124481
    Abstract: The present document is directed to methods for producing therapeutically active limonoids as well as new limonoid-type compounds.
    Type: Application
    Filed: October 27, 2023
    Publication date: April 18, 2024
    Inventors: Jacob Westman, Catarina Malmberg
  • Publication number: 20240124482
    Abstract: The present document is directed to methods for producing therapeutically active limonoids as well as new limonoid-type compounds.
    Type: Application
    Filed: October 27, 2023
    Publication date: April 18, 2024
    Inventors: Jacob Westman, Catarina Malmberg
  • Publication number: 20240124483
    Abstract: Provided herein are methods and corresponding compounds for treating fibrotic disease by administering to a subject a compound of Formula I or pharmaceutically acceptable salt thereof, which inhibits phosphorylation of Smad2/3, according to Phospho-Smad2/3 Inhibition Assay, including compounds that are active according to MAPK p38 Activation Assay; or a compound of Formula II or III. Also provided are methods and corresponding compounds for treating cancers, inflammatory diseases, rasopathies and autoimmune leukoproliferative disorders.
    Type: Application
    Filed: January 27, 2022
    Publication date: April 18, 2024
    Inventors: Yaron R. Hadari, Michael Schmertzler, Theresa M. Williams, Luca Carta, Rebecca Hutcheson
  • Publication number: 20240124484
    Abstract: Disclosed herein are compounds having Formula I, or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, and Spacer are described herein. Also disclosed are methods of making and using such compounds, as well as pharmaceutical compositions comprising the compounds, for the treatment of a disease such as cancer.
    Type: Application
    Filed: December 14, 2021
    Publication date: April 18, 2024
    Inventors: Graham Albert Edwin GARNETT, Michael G. Brant