CAS: 1143532-39-1; (S)-4-Amino-N-(1-(4-Chlorophenyl)-3-Hydroxypropyl)-1-(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)Piperidine-4-Carboxamide

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CAS号1143534-59-1 (S)-4-amino-N-(... | CAS号3680-69-1 6-氯-7-氮杂嘌呤 | CAS号1143534-12-6 (S)-tert-butyl ... | CAS号131690-60-3 (S)-3-氨基-3-(4-溴... | CAS号252720-31-3 4-(B°C-氨基)哌啶-4-甲酸

(S)-3-氨基-3-(4-氯苯基)丙酸置于硼烷四氢呋喃络合物,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺体系中,用 四氢呋喃,乙二醇二甲醚 用作溶剂,化学反应 22.25H,反应生成(S)-4-氨基-N-(1-(4-氯苯基)-3-羟基丙基)-1-(7H-吡咯并[2,3-D]嘧啶-4-基)哌啶-4-羧酰胺
参考文献:Discovery Of 4-Amino-N-[(1S)-1-(4-Chlorophenyl)-3-Hydroxypropyl]-1-(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)Piperidine-4-Carboxamide (Azd5363),An Orally Bioavailable,Potent Inhibitor Of Akt Kinases
标题:Discovery Of 4-Amino-N-[(1S)-1-(4-Chlorophenyl)-3-Hydroxypropyl]-1-(7H-Pyrrolo[2,3-D]Pyrimidin-4-yl)Piperidine-4-Carboxamide (Azd5363),An Orally Bioavailable,Potent Inhibitor Of Akt Kinases
摘要:Wide-Ranging Exploration Of Analogues Of An Atp-Competitive Pyrrolopyrimidine Inhibitor Of Akt Led To The Discovery Of Clinical Candidate Azd5363,Which Showed Increased Potency,Reduced Herg Affinity,And Higher Selectivity Against The Closely Related Agc Kinase Rock. This Compound Demonstrated Good Preclinical Drug Metabolism And Pharmacokinetics (Dmpk) Properties And,After Oral Dosing,Showed Pharmacodynamic Knockdown Of Phosphorylation Of Akt And Downstream Biomarkers In Vivo,And Inhibition Of Tumor Growth In A Breast Cancer Xenograft Model.
Doi:10.1021/jm301762V

专利信息

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

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.

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

专利号:US-2022411407-A1
优先权日:2019-11-15
标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof
发明人：WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN
权利人:UNIV NORTH CAROLINA CHAPEL HILL
摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.

专利号:CN-119059929-A
优先权日:2023-06-01
标 题:Synthesis method of fluoroalkyl amine compound