26918-14-9Relevant academic research and scientific papers
NEW SUBSTITUTED AZAINDOLINE DERIVATIVES AS NIK INHIBITORS
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Page/Page column 160; 161, (2019/01/21)
The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK - also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
METHOD FOR SYNTHESIS OF 9-CIS-BETA-CAROTENE AND FORMULATIONS THEREOF
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Paragraph 0052, (2017/12/29)
The present invention relates to a method for total chemical synthesis of 9-cis-β-carotene (9CBC), and further provides stable formulations thereof.
Iron-catalyzed aerobic C-H functionalization of pyrrolones
Liu, Li-Wei,Wang, Zhen-Zhen,Zhang, Hui-Hui,Wang, Wan-Shu,Zhang, Ji-Zong,Tang, Yu
supporting information, p. 9531 - 9534 (2015/06/08)
The aerobic oxidation of pyrrolones catalyzed by Fe(OTf)3 to form reactive N-acyliminium ion intermediates that undergo nucleophilic additions with alcohols to give the corresponding products in moderate to good yields is described.
Conformationally Defined Rexinoids and Their Efficacy in the Prevention of Mammary Cancers
Atigadda, Venkatram R.,Xia, Gang,Deshpande, Anil,Wu, Lizhi,Kedishvili, Natalia,Smith, Craig D.,Krontiras, Helen,Bland, Kirby I.,Grubbs, Clinton J.,Brouillette, Wayne J.,Muccio, Donald D.
supporting information, p. 7763 - 7774 (2015/10/20)
(2E,4E,6Z,8Z)-8-(3′,4′-Dihydro-1′(2H)-naphthalen-1′-ylidene)-3,7-dimethyl-2,3,6-octatrienoinic acid (UAB30) is currently undergoing clinical evaluation as a novel cancer prevention agent. In efforts to develop even more highly potent rexinoids that prevent breast cancer without toxicity, we further explore here the structure-activity relationship of two separate classes of rexinoids. UAB30 belongs to the class II rexinoids and possesses a 9Z-tetraenoic acid chain bonded to a tetralone ring, whereas the class I rexinoids contain the same 9Z-tetraenoic acid chain bonded to a disubstituted cyclohexenyl ring. Among the 12 class I and class II rexinoids evaluated, the class I rexinoid 11 is most effective in preventing breast cancers in an in vivo rat model alone or in combination with tamoxifen. Rexinoid 11 also reduces the size of established tumors and exhibits a therapeutic effect. However, 11 induces hypertriglyceridemia at its effective dose. On the other hand rexinoid 10 does not increase triglyceride levels while being effective in the in vivo chemoprevention assay. X-ray studies of four rexinoids bound to the ligand binding domain of the retinoid X receptor reveal key structural aspects that enhance potency as well as those that enhance the synthesis of lipids.
METHOD FOR PRODUCING 4-HALOSENECIOIC ACID DERIVATIVE
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Paragraph 0083; 0084, (2016/11/24)
In addition the present invention refers to high yield and a low cost method for preparing derivatives hour Osan which it counts 4-halo in provides. General formula (1) : (in formula, the protector for a difference from an R) the reel alcohol which will know derivatives represented by, characterized by reacting a halogenating agent, general formula (2) : (in formula, R the equal to the meanings exhibits, for a difference from an represent halogen X) represented by derivatives of 4-halo hour Osan which it counts is manufacturing method.
Synthesis and herbicidal activity of diphenyl ether derivatives containing unsaturated carboxylates
Yu, Haibo,Yang, Huibin,Cui, Dongliang,Lv, Liang,Li, Bin
scheme or table, p. 11718 - 11726 (2012/04/04)
A series of novel diphenyl ether derivatives containing unsaturated carboxylates were designed and synthesized. Their structures were identified by 1H nuclear magnetic resonance and elemental analyses. The bioassays indicated that the compounds 5b and 5c exhibited good herbicidal activities against velvetleaf at a concentration of 30-40 g/hm2. The relationship between structure and herbicidal activity was also discussed. Among unsaturated carboxylates group, butenoate is the most promising one. Amonst them, 4-ethoxy-4-oxobutenyl 5-(2-chloro-4-(trifluoromethyl)phenoxy)-2- nitrobenzoate 5b was identified as the most promising candidate due to its high protoporphyrinogen IX oxidase inhibition effect (pI50 = 6.64) and good herbicidal activity against broadleaf weeds with selectivity to soybean and low toxicity to mammals.
Conjugate boration of β,β-disubstituted unsaturated esters: Asymmetric synthesis of functionalized chiral tertiary organoboronic esters
Feng, Xinhui,Yun, Jaesook
supporting information; scheme or table, p. 13609 - 13612 (2011/02/28)
Challenging tertiary organoboronic esters containing a β-ester group were prepared enantioselectively via the asymmetric conjugate boration of β,β-disubstituted α,β-unsaturated esters with a copper-phosphine catalyst (see scheme). The functionalized organoboron derivatives can be utilized as a carbon nucleophile to form all-carbon quaternary centers. Copyright
SYNTHESIS OF RADIOACTIVE ZEATIN RIBOSIDE AND RELATED COMPOUNDS BY ALKYLATION OF PURINE MOIETIES
Young, H.,Letham, D. S.,Hocart, C. H.,Eichholzer, J. V.
, p. 385 - 386 (2007/10/02)
A method for the synthesis of (E)-4-(tetrahydropyran-2-yloxy)-3-methylbut-2-enyl bromide is described and its use in the synthesis of 3H>zeatin riboside, zeatin and a xanthine derivative by alkylation is reported.
SYNTHESIS OF (E)-β-FLUOROMETHYLENEGLUTAMIC ACID
McDonald, Ian A.,Palfreyman, Michael G.,Jung, Michel,Bey, Philippe
, p. 4091 - 4092 (2007/10/02)
A potential dual-enzyme activated inhibitor of γ-aminobutyric acid transaminase, (E)-β-fluoromethyleneglutamic acid, was prepared from ethyl 3,3-dimethylacrylate in 11 steps.
SYNTHETIC INVESTIGATIONS INTO THE CHEMISTRY OF POLYENE COMPOUNDS XLVII. TOTAL SYNTHESIS OF (+/-)-(2E,4E,6E,6Z,8E)-3,7-DIMETHYL-9-(2,6-DIMETHYL-3-OXO-6-ETHOXYCARBONYL-1-CYCLOHEXENYL)-2,4,6,8-NONATETRAENOIC ACID. THE WITTIG REACTION AT HIGH PRESURES
Zhidkova, T. A.,Stashina, G. A.,Bekker, A. R.,Vakulova, L. A.,Zhulin, V. M.,Samokhvalov, G. I.
, p. 2328 - 2333 (2007/10/02)
The synthesis of the C20 retinoids (+/-)-2E,4E,6E,6Z,8E-3,7-dimethyl-9-(2,6-dimethyl-3-oxo-6-ethoxycarbonyl-1-cyclohexenyl)-2,4,6,8-nonatetraenoic acid the previously undescribed ethyl (+/-)-2E,4Z,6E-2-isopropenyl-5-methyl-7-(2,6-dimethyl-3-oxo-6-ethoxycarbonyl-1-cyclohexenyl)-2,4,6-heptatrienoate was realized by the C10 + C10 to C20 scheme with the use of the Wittig reaction at high presure.
