专利号:US-9873688-B2 优先权日:2013-11-08 标 题:Process for the synthesis of an indoleamine 2,3-dioxygenase inhibitor 发明人:TAO MING; FRIETZE WILLIAM; MELONI DAVID J; WENG LINGKAI; ZHOU JIACHENG; PAN YONGCHUN 权利人:INCYTE CORP; INCYTE HOLDINGS CORP 摘要:The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.
专利号:US-2022243244-A1 优先权日:2019-10-10 标 题 :Compositions and methods for in vivo synthesis of unnatural polypeptides 发明人:ROMESBERG FLOYD E; FISCHER EMIL C; HASHIMOTO KOJI; FELDMAN AARON W; DIEN VIVIAN T; ZHANG YORKE 权利人:SCRIPPS RESEARCH INST 摘要:Disclosed herein are compositions, methods, and kits for a cell incorporating unnatural amino acids into an unnatural polypeptide. Also disclosed herein are compositions, methods, and kits for increasing activity and yield of the unnatural polypeptide synthesized by the cell.
专利号:US-2023037284-A9 优先权日:2018-11-30 标题:Combination therapy of peptidomimetic macrocycles 发明人:GUERLAVAIS VINCENT; ANNIS DAVID ALLEN 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:US-2025084410-A1 优先权日:2015-01-12 标 题:Incorporation of unnatural nucleotides and methods thereof 发明人:PTACIN JEROD; MALYSHEV DENIS A; CAFFARO CAROLINA E 权利人:SYNTHORX INC 摘要:Disclosed herein are methods, compositions and kits for the synthesis of proteins which comprises unnatural amino acids that utilize a mutant tRNA.
专利号:US-5856107-A 优先权日:1997-02-04 标 题 :Combinatorial libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene derivatives, methods of making the libraries and compounds therein 发明人:OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TREGA BIOSCIENCES INC 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of libraries of imidazol-pyrido-indole and imidazol-pyrido-benzothiophene compounds. The present invention further provides methods of preparing the libraries and the individual compounds made by the combinatorial synthesis.
专利号:US-11918657-B2 优先权日:2017-11-10 标 题 :Dendrimer delivery system and methods of use thereof 发明人:RANGARAMANUJAM KANNAN; SHARMA RISHI; SHARMA ANJALI; KANNAN SUJATHA; ZHANG ZHI; KAMBHAMPATI SIVA PRAMODH 权利人:UNIV JOHNS HOPKINS 摘要:Low-generation dendrimers containing a high density of surface hydroxyl groups, and methods of synthesis thereof are provided. In particular, oligo ethylene glycol (OEG)-like dendrimers with a high surface functional groups at relatively low generations (e.g. Ëœ120 hydroxyls in the third generation, with a size of just 1-2 nm) is described. Dendrimer formulations including one or more prophylactic, therapeutic, and/or diagnostic agents, and methods of use thereof are also described. The formulations are suitable for topical, enteral, and/or parenteral delivery for treating one or more diseases, conditions, and injuries in the eye, the brain and nervous system (CNS), particularly those associated with pathological activation of microglia and astrocytes.
1: Zhang L, Huang Y, Cui X, Tan X, Zhu Y, Zhou W, Wang C, Yuan G, Cao Q, Su G, Kijlstra A, Yang P. Increased Expression of Indoleamine 2,3-Dioxygenase (IDO) in Vogt-Koyanagi-Harada (VKH) Disease May Lead to a Shift of T Cell Responses Toward a Treg Population. Inflammation. 2020 Oct;43(5):1780-1788. doi: 10.1007/s10753-020-01252-7. 7(1):246. doi: 10.1186/s40425-019-0725-7. 3: Huang GL, Tao A, Miyazaki T, Khan T, Hong T, Nakagawa Y, Cabral H. PEG- Poly(1-Methyl-l-Tryptophan)-Based Polymeric Micelles as Enzymatically Activated Inhibitors of Indoleamine 2,3-Dioxygenase. Nanomaterials (Basel). 2019 May 9;9(5):719. doi: 10.3390/nano9050719. 4: Gao W, He Y, Li F, Chai C, Zhang J, Guo J, Chen C, Wang J, Zhu H, Hu Z, Zhang Y. Antibacterial activity against drug-resistant microbial pathogens of cytochalasan alkaloids from the arthropod-associated fungus Chaetomium globosum TW1-1. Bioorg Chem. 2019 Mar;83:98-104. doi: 10.1016/j.bioorg.2018.10.020. Epub 2018 Oct 10. 40(2):576-582. doi: 10.3892/ijmm.2017.3043. Epub 2017 Jun 26.
合成参考文献
参考文献:10.1074/jbc.m111.229518 摘要:Karunakaran S, Ramachandran S, Coothankandaswamy V, Elangovan S, Babu E, Periyasamy-Thandavan S, Gurav A, Gnanaprakasam JP, Singh N, Schoenlein PV, Prasad PD, Thangaraju M, Ganapathy V. SLC6A14 (ATB0,+) Protein, a Highly Concentrative and Broad Specific Amino Acid Transporter, Is a Novel and Effective Drug Target for Treatment of Estrogen Receptor-positive Breast Cancer. Journal of Biological Chemistry. 2011 Sep;286(36):31830–8. doi: 10.1074/jbc.m111.229518. 参考文献:10.1002/eji.200535602 摘要:Wingender G, Garbi N, Schumak B, Jüngerkes F, Endl E, von Bubnoff D, Steitz J, Striegler J, Moldenhauer G, Tüting T, Heit A, Huster KM, Takikawa O, Akira S, Busch DH, Wagner H, Hämmerling GJ, Knolle PA, Limmer A. Systemic application of CpG-rich DNA suppresses adaptive T cell immunity via induction of IDO. Eur J Immunol. 2006 Jan;36(1):12–20. doi: 10.1002/eji.200535602.