CAS: 2222112-77-6; N-(Trans-4-(3-Chloro-4-Cyanophenoxy)Cyclohexyl)-6-(4-((4-(2-(2,6-Dioxopiperidin-3-yl)-6-Fluoro-1,3-Dioxoisoindolin-5-yl)Piperazin-1-yl)Methyl)Piperidin-1-yl)Pyridazine-3-Carboxamide

专利信息

专利号:US-12043612-B2
优先权日:2020-05-09
标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
发明人：ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY
权利人:ARVINAS OPERATIONS INC
摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.

专利号:US-2024261416-A1
优先权日:2023-01-31
标题:Synthesis of novel cereblon e3 ligase ligands, compounds formed thereby, and pharmaceutical compositions containing them
发明人：TANG WEIPING; XIE HAIBO; WU YUNXIANG; LIAO JUNZHUO; LI CHUNRONG; TANDON IRA; TANG HUA
权利人:WISCONSIN ALUMNI RES FOUND
摘要:Provided herein are achiral cereblon (CRBN) ligands based on phenyl dihydrouracil that have optimal binding to CRBN without having chiral carbons. Also provided herein are the proteolysis targeting chimeras (PROTACs) comprising the CRBN ligands and a protein binder, pharmaceutical compositions containing the PROTACs, and methods of treating diseases using the PROTACs.

专利号:US-2024400552-A1
优先权日:2016-11-11
标题 :Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-11622968-B2
优先权日:2011-03-08
标 题:Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-2022118123-A1
优先权日:2019-02-22
标 题 :Combination of ar antagonists and targeted thorium conjugates
发明人：HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
权利人:BAYER AG; BAYER AS
摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.

专利号:WO-2023143427-A1
优先权日:2022-01-27
标题 :Crystal form of arv-110 and preparation method therefor and use thereof
发明人：SHENG XIAOXIA; SHENG XIAOHONG; CAO YAQING
权利人:HANGZHOU SOLIPHARMA CO LTD
摘要:The present application relates to the field of drug synthesis, in particular to a crystal form of ARV-110 and a preparation method therefor and a use thereof. The crystal form of the ARV-110 at least has one of the following improved characteristics: the stability is good, the hygroscopicity is low, the solubility is good, the melting point is high, stable storage can be achieved, crystal transformation of a drug in a development process and storage is avoided, the preparation method is simple and reliable, and great development values are achieved.