79205-04-2Relevant academic research and scientific papers
BROMODOMAIN INHIBITORS FOR ANDROGEN RECEPTOR-DRIVEN CANCERS
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, (2022/03/31)
Methods for treating certain androgen receptor-positive forms of cancer using inhibitors of the CREB binding protein bromodomain are disclosed. In some methods, the AR-positive forms of cancer may be breast cancer, including triple negative forms, hormone receptor positive forms, and HER2-positive forms. In other methods, the AR-positive forms of cancer may be prostate cancer, including metastatic castration resistant prostate cancer. In some embodiments, methods of treating prostate cancer comprise the step of administering to a patient in need thereof the compound (1R,3R)-3-[(7S)-2-[(R)-(5-fluoro-2-methoxyphenyl)(hydroxy)methyl]-6-(methoxycarbonyl)-7-methyl-3H,6H,7H,8H,9H-imidazo[4,5-f]quinolin-3-yl]cyclohexane-1-carboxylic acid, or a pharmaceutically acceptable salt thereof.
TREATING CANCER WITH A BROMODOMAIN AND EXTRA-TERMINAL (BET) FAMILY INHIBITOR
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, (2021/01/23)
Methods of treating patients diagnosed with cancer with a BET inhibitor compound are provided, including intermittent dosing schedules for administering the compound as a single agent or as part of a combination therapy. For example, AML/MDS and NHL cancer patients can be treated with a BET inhibitor compound using intermittent dosing schedules provided herein.
Rapid Construction of Structurally Diverse Quinolizidines, Indolizidines, and Their Analogues via Ruthenium-Catalyzed Asymmetric Cascade Hydrogenation/Reductive Amination
Chen, Ya,He, Yan-Mei,Zhang, Shanshan,Miao, Tingting,Fan, Qing-Hua
, p. 3809 - 3813 (2019/01/14)
A rapid construction of enantioenriched benzo-fused quinolizidines, indolizidines, and their analogues by ruthenium-catalyzed asymmetric cascade hydrogenation/reductive amination of quinolinyl- and quinoxalinyl-containing ketones has been developed. This
TETRAHYDRO-IMIDAZO QUINOLINE COMPOSITIONS AS CBP/P300 INHIBITORS
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, (2019/04/11)
The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.
TETRAHYDROQUINOLINE COMPOSITIONS AS BET BROMODOMAIN INHIBITORS
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Paragraph 0205, (2015/06/03)
The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein W, X, Y, Z, R1, R2, R5, and R8 are as described herein.
HCV NS5A replication complex inhibitors. Part 4.1 optimization for genotype 1a replicon inhibitory activity
St. Laurent, Denis R.,Serrano-Wu, Michael H.,Belema, Makonen,Ding, Min,Fang, Hua,Gao, Min,Goodrich, Jason T.,Krause, Rudolph G.,Lemm, Julie A.,Liu, Mengping,Lopez, Omar D.,Nguyen, Van N.,Nower, Peter T.,O'Boyle, Donald R.,Pearce, Bradley C.,Romine, Jeffrey L.,Valera, Lourdes,Sun, Jin-Hua,Wang, Ying-Kai,Yang, Fukang,Yang, Xuejie,Meanwell, Nicholas A.,Snyder, Lawrence B.
, p. 1976 - 1994 (2014/04/03)
A series of symmetrical E-stilbene prolinamides that originated from the library-synthesized lead 3 was studied with respect to HCV genotype 1a (G-1a) and genotype 1b (G-1b) replicon inhibition and selectivity against BVDV and cytotoxicity. SAR emerging f
Identification and development of an efficient route to SB-649915
Armitage, Mark,Bret, Guillaume,Choudary, Bernie M.,Kingswood, Mike,Loft, Mike,Moore, Steve,Smith, Steve,Urquhart, Michael W. J.
, p. 1626 - 1634 (2013/02/22)
The discovery and development of an efficient manufacturing route to the SSRI-5-HT1A receptor antagonist 6-[(1-{2-[(2-methyl-5-quinolinyl)oxy]ethyl}-4- piperidinyl)methyl]-2H-1,4-benzoxazin-3(4H)-one (SB-649915) 1 is described. The existing route to 1 involved coupling quinoline 6 with piperidine 5 and was considered lengthy as a consequence of the nine synthetic steps required to prepare 5. Two new routes to the key piperidine intermediate 5 are identified which deliver this compound in five and two steps respectively, from readily available materials using novel lithiation and Friedel-Crafts methodology respectively. The latter of these two routes was successfully demonstrated at 5 L scale to deliver 700 g of 5. Development to the methanesulfonate 34, an alternative to quinoline 6, is also described as is the final alkylation of piperidine 5 with this methanesulfonate 34 to deliver SB-649915 1.
Au-doped TiO2 nanoparticles for selective photocatalytic synthesis of quinaldines from anilines in ethanol
Selvam,Swaminathan
scheme or table, p. 4911 - 4914 (2010/10/02)
A convenient eco-friendly photocatalytic synthesis of quinaldines has been developed by a simple one-pot reaction of anilines in ethanol solution with Au-loaded TiO2 under UV irradiation. Upon irradiation in the presence of Au-TiO2, aniline and oxidation products derived from ethanol undergo condensation-cyclization to afford quinaldines.
Electrophilic aromatic addition reaction: Electrophilic attack at an aromatic H substituent position
Han, Young Choi,Srisook, Ekaruth,Kun, Sam Jang,Dae, Yoon Chi
, p. 1222 - 1226 (2007/10/03)
(Chemical Equation Presented) We report and propose a mechanism for an unusual electrophilic aromatic addition reaction (AdEAr). During our preparation of 5,7-dibromo-8-methoxyquinaldine as a key intermediate in the synthesis of 7-bromoquinaldine-5,8-dione, direct bromination in either acidic or neutral conditions led only to the formation of 5-bromo-8-methoxyquinaldine. Under basic methanolic conditions, however, we unexpectedly obtained the 5,7-dibromo-8,8-dimethoxy-7,8-dihydroquinaldine adduct 2a. This result not only allows for the functionalization of aromatic compounds via the addition adducts, but also introduces the possibility of an alternate mechanism for electrophilic substitution reactions.
