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-12006324-B1 优先权日:2022-12-15 标题:Preparation method of trilaciclib and precursors of trilaciclib 发明人:KAMANI SATYANARAYANA; CHANG HSIN-YUN; LU TZU-CHIANG; MAI CHIN-CHENG 权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD 摘要:Disclosed herein is a specific method of preparation of Trilaciclib. The said method is to provide an efficacy of a protection free synthetic method of Trilaciclib with less steps and good yields.
专利号:WO-2024116069-A1 优先权日:2022-11-28 标题 :Novel trilaciclib intermediates, method of preparation and use thereof 发明人:KADU Rushikesh Vilasrao; RENGASAMY VADIVELANV; SINGH SATNAM; SHARMA SUBRAMANYA; DAUND VAIBHAV SURESH; KUSHWAHA SANDEEP; LAL KANHAIYA; YAZALI VENKATA SUBBARAO 权利人:ASSIA CHEM IND LTD 摘要:Aspects of the present disclosure provide novel intermediates that may be used for synthesis of Trilaciclib, pharmaceutically acceptable salts or derivatives thereof. Aspects of the present disclosure also relate to a method for preparation of Trilaciclib intermediates. Further aspects of the present disclosure relate to method for preparation of Trilaciclib, pharmaceutically acceptable salts and derivatives thereof. Still further aspects of the present disclosure are drawn towards use of the Trilaciclib intermediates for the production of Trilaciclib, pharmaceutically acceptable salts or derivatives thereof.
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: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.
专利号:US-12390420-B1 优先权日:2024-10-22 标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof 发明人:EGUCHI MASAKATSU 权利人:BRYET US INC 摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.
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