CAS: 827318-97-8; (R)-N-(5-(2-Methoxy-2-Phenylacetyl)-1,4,5,6-Tetrahydropyrrolo[3,4-C]Pyrazol-3-yl)-4-(4-Methylpiperazin-1-yl)Benzamide

上下游产品

5-((2R)-2-甲氧基-2-苯基乙酰基)-3-[[4-(4-甲基哌嗪-1-基)苯甲酰基]氨基]-5,6-二氢吡咯并[3,4-C]吡唑-1(4H)-羧酸乙酯 5-[(2R)-2-Methoxy-2-Phenylethanoyl]-3-{[4-(4-Methylpiperazin-1-yl)Benzoyl]Amino}-5,6-Dihydropyrrolo[3,4-C]Pyrazole-1(4H)-Carboxylate 827318-78-5
1-乙基氧基羰基-3-[4-(4-甲基-1-哌嗪)-苯甲酰基氨基]-5-Boc-4,6-二氢-吡咯并[3,4-C]吡唑 5-Tert-Butyl 1-Ethyl 3-{[4-(4-Methylpiperazin-1-yl)Benzoyl]Amino}-4,6-Dihydropyrrolo[3,4-C]Pyrazole-1,5-Dicarboxylate 761443-69-0
1-乙基氧基羰基-3-[4-(4-甲基-1-哌嗪)-苯甲酰基氨基]-5,6-二氢-吡咯并[3,4-C]吡唑 3-[4-(N-Methylpiperazin-1-yl)Benzamido]-1-Ethoxycarbonyl-4,6-Dihydropyrrolo[3,4-C]Pyrazole 761443-50-9
5-Boc-3-氨基-4,6-二氢吡咯并[3,4-C]吡唑-1-甲酸乙酯 3-Amino-4,6-Dihydro-Pyrrolo[3,4-C]Pyrazole-1,5-Dicarboxylic Acid 5-Tert-Butyl Ester 1-Ethyl Ester 398495-65-3

📜3-氨基-5-叔丁氧羰基-吡咯并[3,4-C]吡唑置于盐酸,草酰氯,三乙胺,N,N-二异丙基乙胺,N,N-二甲基甲酰胺体系中,用 四氢呋喃,1,4-二氧六环,甲醇,二氯甲烷 作为反应溶剂,化学反应 82.0H,反应生成 达鲁舍替
参考文献:(R)-N-[5-(2-甲氧基-2-苯基乙酰基)-1,4,5,6-四氢吡咯并[3,4-C]吡唑-3-基]-4-(4-甲 基哌嗪-1-基)苯甲酰胺的合成方法
标题:(R)-N-[5-(2-甲氧基-2-苯基乙酰基)-1,4,5,6-四氢吡咯并[3,4-C]吡唑-3-基]-4-(4-甲 基哌嗪-1-基)苯甲酰胺的合成方法
摘要:本发明属于医药技术领域,涉及pha739358(danusertib)即(R)‑n‑[5‑(2‑甲氧基‑2‑苯基乙酰基)‑1,4,5,6‑四氢吡咯并[3,4‑c]吡唑‑3‑基]‑4‑(4‑甲基哌嗪‑1‑基)苯甲酰胺的制备,共设计了四条反应路线,以简单易得的甘氨酸为原料,经加成,酯化,氨基保护,环合等反应制得(R)‑n‑[5‑(2‑甲氧基‑2‑苯基乙酰基)‑1,4,5,6‑四氢吡咯并[3,4‑c]吡唑‑3‑基]‑4‑(4‑甲基哌嗪‑1‑基)苯甲酰胺,路线1,2,4收率可达25%以上,路线3收率可达20%以上.本发明具有反应步骤短,后处理操作简便,耗时短,收率高,总成本低的优点.为抗肿瘤药物pha739358的制备提供了新方法.

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

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-9365532-B1
优先权日:2011-02-14
标题:Synthesis, composition and use of novel therapeutic and cosmetic Schiff base products formed by reaction of a carbonyl containing moeity with a transimination nucleophilic catalyst and the use of transimination nucleophilic catalysts to increase the rate at which carbonyl containing therapeutic and cosmetic actives form Schiff base products with biological amines
发明人：ISAACMAN STEVEN
权利人:ISAACMAN STEVEN; NANOMETICS LLC
摘要:The present invention relates to the synthesis, composition and use of novel moieties formed by reacting a transimination nucleophilic catalyst, molecular or polymeric, with carbonyl-containing therapeutic or cosmetic moieties. The resultant Schiff base product is highly reactive towards transimination with a biological amine. The catalyst and carbonyl-containing moiety can be molecular or polymeric, and the resultant chemical and physical properties of the Schiff base products can be engineered by appropriate selection of said catalyst. The present invention also relates to the synthesis, composition and use of novel moieties that are used as actives in sunless tanning preparations. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate at which a carbonyl-containing moiety reacts with a biological amine. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate and efficacy of commercial sunless tanning preparations. Improvements on stability and efficacy of said preparations are disclosed. While the invention has been described in terms of its preferred embodiments, those skilled in the art will recognize that the invention can be practiced with modification within the spirit and scope of the appended claims. Accordingly, the present invention should not be limited to the embodiments as described above, but should further include all modifications and equivalents thereof within the spirit and scope of the description provided herein.

专利号:US-2019031650-A1
优先权日:2016-01-29
标 题 :Dna alkylation and cross-linking agents as compounds and payloads for targeted therapies
发明人：HERZON SETH; HEALY ALAN; CRAWFORD JASON; VIZCAINO MARIA; NIKOLAYEVSKIY HERMAN
权利人:UNIV YALE
摘要:The present invention is directed to compounds related to precolibactin pharmaceutical compositions based upon these compounds and methods of synthesis which are employed to provide intermediates and final compounds, which are principally alkylating agents and anticancer compounds. The chemical synthetic approach disclosed facilitates the synthesis of numerous precolibactin analogs which can be used in the treatment of cancer.

专利号:US-2017107577-A1
优先权日:2014-03-11
标题:Determining Cancer Aggressiveness, Prognosis and Responsiveness to Treatment
发明人：AL-EJEH FARES
权利人:THE COUNCIL OF THE QUEENSLAND INST OF MEDICAL RES
摘要:The invention provides methods of determining the aggressiveness, prognosis and response to therapy for particular cancers, which include comparing the expression levels of one or a plurality of differentially expressed genes from one or more 5 functional metagenes, including a Carbohydrate/Lipid Metabolism metagene, a Cell Signalling metagene, a Cellular Development metagene, a Cellular Growth metagene, a Chromosome Segregation metagene, a DNA Replication/Recombination metagene, an Immune system metagene, a Metabolic Disease metagene, a Nucleic Acid Metabolism metagene, a Post-Translational Modification metagene, a Protein 10 Synthesis/Modification metagene and a Multiple Networks metagene. The method disclosed herein may be particularly suitable as a companion diagnostic for cancer therapies.

专利号:US-2022143183-A1
优先权日:2019-02-23
标题:Photoswitchable protacs and synthesis and uses thereof
发明人：TRAUNER DIRK; REYNDERS MARTIN; MATSUURA BRYAN; BEROUTI MARLEEN; PAGANO MICHELE
权利人:UNIV NEW YORK
摘要:Provided are compounds, which may be referred to as PHOTACs (photoswitchable proteolysis targeting chimeras), and compositions, kits, and methods of making and using PHOTACs. PHOTACs have one or more E3 ligase ligand(s), one or more photoswitchable group(s), optionally, one or more linker(s), and one or more ligand(s) for a target protein. PHOTACs may be suitable for use in methods to treat diseases, such as, for example, cancer. PHOTACs may also be suitable for use in methods to induce selective degradation of a target protein.