专利号:US-2021220331-A1 优先权日:2016-05-03 标题:Inhibitors of ires-mediated protein synthesis 发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA 权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS 摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
专利号:US-10975069-B2 优先权日:2014-04-01 标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof 发明人:HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN 权利人:UNIV WASHINGTON 摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
专利号:US-9573873-B2 优先权日:2014-06-03 标题:Catalytic method for dibenzocycloheptane synthesis and allocolchicinoid synthesis 发明人:GREEN JAMES; MEHDI MARIAM; DJURDJEVIC SINISA 权利人:UNIV OF WINDSOR 摘要:In a non-limiting embodiment, there is provided a compound of formula (I), which may permit for a method or use in treating or preventing a cancer, such as pancreatic cancer or leukemia. In one embodiment, there is also provide a method of preparing a compound of formula (Ia), the method including conducting a cyclization reaction of a compound of formula (III) to obtain a compound of formula (IV), wherein conducting the cyclization reaction comprises conducting a Michael reaction in the presence of a Lewis acid.
专利号:US-4150236-A 优先权日:1976-05-26 标 题 :Steroidal intermediates from the condensation product of dimethyl-3-ketoglutarate and glyoxal 发明人:WEISS ULRICH; RICE KENNER C 权利人:US HEALTH EDUCATION & WELFARE 摘要:Tricyclic aromatic compounds of the formula ##STR1## including those wherein: (A) R 1 is H, R 2 is carbomethoxy, and R 3 is methyl; n (b) R 1 is acetyl, R 2 is carbomethoxy, and R 3 is methyl; n (c) R 1 and R 3 are methyl and R 2 is carbomethoxy; n (d) R 1 , R 2 , and R 3 are hydrogen; and n (e) R 1 and R 3 are methyl and R 2 is hydrogen n Are intermediates for the total synthesis of steroids.
专利号:US-4041055-A 优先权日:1975-11-17 标题:Process for the preparation of 17α-hydroxyprogesterones and corticoids from androstenes 发明人:SHEPHARD KENNETH PAUL; VAN RHEENEN VERLAN H 权利人:UPJOHN CO 摘要:This invention discloses a general process for the production of corticoids from androstenes. This invention provides an economically viable alternative synthesis of 17α-hydroxyprogesterones and the corticoids.
专利号:US-2010247433-A1 优先权日:2005-10-14 标题:Use of non-canonical amino acids as metabolic markers for rapidly-dividing cells 发明人:TIRRELL DAVID; DIETERICH DANIELA C; LINK AARON J; SCHUMAN ERIN 权利人:CALIFORNIA INST OF TECHN 摘要:The invention provides methods, reagents and systems to preferentially mark fast-proliferating cells/tissues (such as cancer), by incorporating non-natural amino acids into proteins, preferably in vivo, using the endogenous protein synthesis machinery of an organism. The incorporated non-natural amino acids contain reactive groups for further chemical reagents, which may serve as a “handleâ€? to for a number of uses, such as imaging of cancer cells, targeting drugs to preferentially kill cancer cells, and proteomic analysis in the context of large scale or high throughput screening for candidate drug leads that affects the proliferation of a target cell, etc.
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