CAS: 58-46-8; Rel-(3R,11Br)-3-Isobutyl-9,10-Dimethoxy-1,3,4,6,7,11B-Hexahydro-2H-Pyrido[2,1-A]Isoquinolin-2-One

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CAS号3382-18-1 6,7-二甲氧基-3,4-二氢异喹啉 | CAS号1069-62-1 (2-乙酰基-4-甲基戊基)三甲基碘化铵 | CAS号1346909-10-1 6,7-dimethoxy-2... | CAS号1346909-38-3 N-methoxy-N,4-d... | CAS号1346909-40-7 5-methyl-3-(((t... | CAS号1346909-31-6 3-(hydroxymethy... | CAS号1346909-44-1 4-methyl-2-(3-(...

(3S,11Bs)-Tetrabenazine Di-P-Toluoyl-D-Tartaric Acid置于水,Potassium Hydroxide体系中,用84 G的收率获得产物丁苯那嗪
参考文献:一种苯并喹嗪类衍生物的制备方法
标题:一种苯并喹嗪类衍生物的制备方法
摘要:本发明涉及一种苯并喹嗪类衍生物的制备方法,属于药物化学技术领域,具体涉及一种丁苯那嗪的手性拆分方法.以丁苯那嗪消旋体为原料,通过与手性酸成盐,打浆,解离等步骤简便有效地制得高光学纯度的(3R,11Br)‑丁苯那嗪或(3S,11Bs)‑丁苯那嗪.该方法和现有工艺相比,优势在于各步反应条件温和,收率高,操作简便,工艺稳定,适于大规模工业化生产.

专利信息

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-2024239791-A1
优先权日:2021-04-26
标题 :Processes for the synthesis of valbenazine
发明人：TUCKER JOHN LLOYD
权利人:NEUROCRINE BIOSCIENCES INC
摘要:The present application relates to processes for preparing (S)-(2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl 2-amino-3-methylbutanoate di(4-methylbenzenesulfonate), which is an inhibitor of vesicular monoamine transporter 2 (VMAT2) useful in the treatment of hyperkinetic movement disorders such as tardive dyskinesia (TD).

专利号:US-2022363680-A1
优先权日:2019-09-13
标题 :Processes for the synthesis of valbenazine
发明人：TUCKER JOHN; KUCERA DAVID; HETTINGER DONALD; COCHRAN BRIAN M; BRANUM SHAWN; LE JACKIE; MCGEE KEVIN
权利人:NEUROCRINE BIOSCIENCES INC
摘要:The present application relates to processes for making (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b -hexahydro-1H-pyrido[2,1-a]isoquinolin-2-yl (S)-2-amino-3-methylbutanoate di(4-methylbenzenesulfonate), which is an inhibitor of vesicular monoamine transporter 2 (VMAT2) useful in the treatment of hyperkinetic movement disorders such as tardive dyskinesia (TD).

专利号:US-10391067-B2
优先权日:2015-08-18
标题:Prevention and treatment of neurodegenerative diseases through autophagy activity mediated by a synthetic ligand or arginylated BIP binding to the P62 ZZ domain
发明人：KWON YONG TAE; KIM BO YEON; CHA HYUNJOO; YOO YOUNG DONG; Yu ji-eun
权利人:SEOUL NAT UNIV R&DB FOUNDATION; KOREA RES INST BIOSCIENCE & BIOTECHNOLOGY; AUTOTAC BIO
摘要:The pharmacokinetics and key technologies of the present invention are summarized in FIG. 1. Particularly, malignant misfolded proteins such as mutant huntingtin and alpha-synuclein are coagulated and grow into oligomeric coagulum ({circle around (1)}, {circle around (2)}, fibrillar coagulum ({circle around (3)}) and eventually inclusion body ({circle around (4)}). Young neurons produce a large amount of Nt-Arg through N-terminal arginylation ({circle around (5)}) of vesicle chaperones such as BiP secreted into the cytoplasm, and then arginylated BiP (R-BiP) is secreted binds to the misfolded proteins ({circle around (6)}). As a ligand, the Nt-Arg of R-BiP binds to the p62 ZZ domain ({circle around (7)}), and the normally inactivated closed form of p62 is changed to an open form, leading to structural activation ({circle around (8)}). As a result, PB1 and LC3-binding domains are exposed. The PB1 domain induces oligomerization ({circle around (9)}), leading to the concentration as a p62 body ({circle around (10)}) that is a coagulum capable of being degraded by autophagy. Then, p62 binds to LC3, which is protruding from the autopagosomal membranes, leading to the completion of autophagy targeting ({circle around (11)}) and lysosomal proteolysis. Since autophagy proteolysis including steps ({circle around (5)})-({circle around (11)}) is strong in young neurons, cytotoxic protein coagulums ({circle around (1)}-{circle around (5)}) do not accumulate. However in aged neurons, autophagy proteolysis including steps {circle around (5)}-{circle around (11)} is weakened, and protein coagulums ({circle around (1)}-{circle around (5)}) accumulate and become cytotoxic. In this invention, p62 is intentionally activated ({circle around (12)}, {circle around (13)}) by using low mass ligands of the p62 ZZ domain to effectively remove huntingtin and alpha-synuclein protein coagulums. Particularly, in step {circle around (12)}, p62 ligated with a ligand accelerates the oligomerization of p62-R-BiP-misfolded protein ({circle around (9)}) and the formation of autophagy coagulum ({circle around (10)}). In step ({circle around (13)}), the ligand-p62 conjugate acts as an autophagy activator ({circle around (14)}) to induce the synthesis of LC3 and the conversion of LC3-I into LC3-II in order to accelerate the formation of autophagosomes ({circle around (15)}).

专利号:US-12201669-B2
优先权日:2021-03-11
标 题:Small molecule suppressors of APOE gene expression and cerebral vascular amyloid pathology
发明人：TSAI LI-HUEI; BLANCHARD JOEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using small molecule inhibitors. The invention also includes methods of treating disease associated with amyloid synthesis, such as Alzheimer's disease. The small molecule inhibitors disclosed herein are compounds which are non-immunosuppressant cyclosporin including the pharmaceutically acceptable salts thereof.

专利号:US-2015352230-A1
优先权日:2013-01-11
标 题:Synthesis and isolation of dendrimer based imaging systems
发明人：MULLEN DOUGLAS GURNETT; BAKER JR JAMES R; BANASZAK HOLL MARK M; HUANG BAOHUA; DOUGHERTY CASEY; BALL JACK
权利人:UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).