CAS: 875320-29-9; N-Hydroxy-2-[4-[[(1-Methylindol-3-yl)Methylamino]Methyl]Piperidin-1-Yl]Pyrimidine-5-Carboxamide

专利信息

专利号:US-11286271-B2
优先权日:2018-07-31
标 题 :Iridium (III) complexes containing N-heterocyclic carbene ligand, synthesis, and their use thereof in cancer treatment
发明人：CHE CHI MING; LAM TSZ LUNG; TONG KA CHUNG
权利人:UNIV HONG KONG
摘要:Provided herein are Ir(III) complexes comprising N-heterocyclic carbene ligand, method of synthesis of the Ir(III) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Ir(III) complexes under both dark and light conditions. Also provided is a method of detecting the Ir(III) complex in a biological system. Also provided is a method of making the Ir(III) complex. The Ir(III) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

专利号:US-11649285-B2
优先权日:2016-08-03
标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
发明人：KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
权利人:BIO TECHNE CORP
摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

专利号:US-10370455-B2
优先权日:2014-12-05
标题 :Identification of VSIG8 as the putative VISTA receptor (V-R) and use thereof to produce VISTA/VSIG8 agonists and antagonists
发明人：MOLLOY MICHAEL; GUO YALIN; ROTHSTEIN JAY; ROSENZWEIG MICHAEL
权利人:IMMUNEXT INC
摘要:The receptor for VISTA is identified (VSIG8) as well as the use of this receptor in the identification or synthesis of agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG8 and/or VISTA and/or the VSIG8/VISTA binding interaction. These antagonists may be used to suppress VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

专利号:US-2018371021-A1
优先权日:2017-05-11
标 题 :Peptidomimetic macrocycles and uses thereof
发明人：AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

专利号:US-2025064840-A1
优先权日:2021-12-16
标 题 :Drug delivery systems based on endoperoxides useful in diagnosis and therapy, and methods thereof
发明人：SILVA MAGALHAES DIOGO; MOREIRA RUI; LOPES FRANCISCA; RODRIGUES CECILIA; MARQUES VANDA
权利人:FACULDADE DE FARMACIA DA UNIV DE LISBOA
摘要:The present invention relates to novel drug delivery systems based on endoperoxide moieties such as 1,2,4,5-tetraoxanes, namely compounds of formula I, appropriately modified to release active pharmaceutical ingredients (API) in the presence of higher levels of Fe (II), in a subject, whereinIron metabolism dysregulation occurs in diseases such as malaria and cancer. Therefore, the present invention also relates to biomarkers comprising said compounds of formula I.Another aspect, the present invention relates to a process of synthesis of compounds of formula I and respective intermediaries.Further, the present invention also relates to a process for labelling, detection, and identification of tumours in a tissue sample.The present invention is thus applicable to the medical and pharmacological areas, in related to particular the ones cancer detection and treatment, and malaria treatment.

专利号:US-2024066133-A1
优先权日:2020-03-06
标 题 :Therapeutic agents and conjugates thereof
发明人：SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO
权利人:BEIJING XUANYI PHARMASCIENCES CO LTD
摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.