- COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
-
This disclosure pertains to compounds, the preparation thereof, and the use of these compounds in the treatment of prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in subjects in need thereof.
- -
-
Paragraph 0781-0787
(2021/06/26)
-
- Adventitious isolation of a pseudorotaxane complex of a trans-bis(Hydroxymethylbenzo)-27-crown-9 pyridyl cryptand and a viologen
-
The adventitious isolation and crystal structure of a pseudorotaxane complex of a trans-substituted dibenzo-27-crown-9-based pyridyl cryptand (6) and N,N’-dimethyl-4,4?-bipyridinium bis(hexafluorophosphate) (5) are reported.
- Pederson, Adam M.-P.,Gibson, Harry W.,Slebodnick, Carla
-
p. 452 - 455
(2020/07/07)
-
- NOVEL ISOINDOLINE DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
-
Disclosed are a novel isoindoline derivative, a pharmaceutical composition and use thereof. The compound of formula I, or the pharmaceutically acceptable salt, solvate, polymorph, co-crystal, stereoisomer, isotopic compound, metabolite or prodrug thereof disclosed in the invention can regulate the generation and/or activity of PDE4 and/or TNF-α so as to effectively treat cancer and inflammatory diseases.
- -
-
-
- Compound for treating or preventing hepatopathy (by machine translation)
-
The invention discloses a compound, an optical isomer or a pharmaceutically acceptable salt, an optical isomer or a pharmaceutically acceptable salt thereof for treating or preventing hepatopathy, and the compound, optical isomer or pharmaceutically acceptable salt thereof can be applied to the preparation of a medicine for treating or preventing liver diseases. (by machine translation)
- -
-
Paragraph 0135-0136; 0140
(2019/10/01)
-
- Type III-C rotaxane dendrimers: Synthesis, dual size modulation and: In vivo evaluation
-
Type III-C rotaxane dendrimers were synthesized by a divergent approach. Dual shuttling behavior and size modulation were observed from non-methylated/methylated rotaxane dendrimers under the same external stimuli. The biological distribution of dendrimers in C57BL/6J mice determined by MALDI-TOF-MS shows predominant accumulation in the spleen and liver. Drug encapsulations with chlorambucil and lithocholic acid were demonstrated.
- Kwan, Chak-Shing,Wang, Tao,Li, Min,Chan, Albert S. C.,Cai, Zongwei,Leung, Ken Cham-Fai
-
supporting information
p. 13426 - 13429
(2019/11/16)
-
- Discovery of N-hydroxy-3-alkoxybenzamides as direct acid sphingomyelinase inhibitors using a ligand-based pharmacophore model
-
Acid sphingomyelinase (ASM) has been shown to be involved in many physiological processes, emerging to be a promising drug target. In this study, we constructed a ligand-based pharmacophore model of ASM inhibitors and applied this model to optimize the lead compound α-mangostin, a known inhibitor of ASM. 23 compounds were designed and evaluated in vitro for ASM inhibition, of these, 10 compounds were found to be more potent than α-mangostin. This high hit ratio confirmed that the presented model is very effective and practical. The most potent hit, 1c, was found to selectively and competitively inhibit the enzyme and inhibit the generation of ceramide in a dose-dependent manner. Furthermore, 1c showed favorable anti-apoptosis and anti-inflammatory activity. Interactions with key residues and the Zn2+ cofactor of 1c were found by docking simulation. These results provide promising leads and important guidance for further development of efficient ASM inhibitors and drug candidates.
- Yang, Kan,Nong, Keyi,Gu, Qinlan,Dong, Jibin,Wang, Jinxin
-
p. 389 - 400
(2018/04/12)
-
- ANTIVIRAL COMPOUNDS
-
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus v
- -
-
Paragraph 0251; 0254
(2016/09/26)
-
- AMIDO THIADIAZOLE DERIVATIVES AS NADPH OXIDASE INHIBITORS
-
The present invention is related to amino thiazole derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
- -
-
Page/Page column 63
(2016/07/05)
-
- A novel benzoyl amide compounds
-
The invention relates to the field of medicinal chemistry, in particular to a novel benzamides compound or a salt acceptable in parmacy of the novel benzamides compound, a preparation method of the novel benzamides compound, a pharmaceutical composition containing the novel benzamides compound and an application of the pharmaceutical composition in preparation of antineoplastic drugs.
- -
-
Paragraph 0477-0479
(2016/11/21)
-
- One-step radiosynthesis of18F-IRS: A novel radiotracer targeting mutant EGFR in NSCLC for PET/CT imaging
-
EGFR (epidermal growth factor receptor) targeted therapy has shown great success in clinical comparing with chemotherapy in EGFR mutation NSCLCs. Such as, gefitinib, first generation EGFR TKI, has obviously prolonged the FPS (progression free survival) of the subgroup of patients, but to those who did not get a certain mutation in EGFR kinase domain, the outcome is poor. In view of this situation, scientists have synthesized many radiotracers for selecting the right people by PET/CT imaging to NSCLC TKI therapy. In this study, we developed a novel PET radiotracer18F-IRS in one-step with a radio yield 20% (non-corrected), radiochemistry > 98.5%, specific activity > 105G Bq/μmol, the pharmacokinetics and capacity of the tracer binding to mutant EGFR were evaluated both in vitro and in vivo.
- Xiao, Zunyu,Song, Yan,Wang, Kai,Sun, Xilin,Shen, Baozhong
-
supporting information
p. 5985 - 5988
(2016/12/09)
-
- FLUORINATED LYSYL OXIDASE-LIKE 2 INHIBITORS AND USES THEREOF
-
Described herein are compounds that are LOXL2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.
- -
-
Paragraph 00415
(2016/09/26)
-
- Regioselective alkylation of catechols via Mitsunobu reactions
-
A mild and efficient Mitsunobu protocol for the regioselective alkylation of catechols such as 3,4-dihydroxybenzaldehyde and methyl 3,4-dihydroxybenzoate is described. The para-alkylation products could be easily prepared via the Mitsunobu reaction with high selectivity in moderate to good yields. Georg Thieme Verlag Stuttgart - New York.
- Wang, Xiaolong,Ju, Tingting,Li, Xiaodong,Cao, Xiaoping
-
experimental part
p. 2947 - 2949
(2011/02/22)
-
- Syntheses of cis- and trans-dibenzo-30-crown-10 derivatives via regioselective routes and their complexations with paraquat and diquat
-
(Chemical Equation Presented) cis-Dibenzo-30-crown-10 (cis-DB30C10) diester and trans-dibenzo-30-crown-10 (trans-DB30C10) diester were synthesized regioselectively with reasonable yields. These two isomers were further reduced to cis-dibenzo-30-crown-10 d
- He, Chunlin,Shi, Zuming,Zhou, Qizhong,Li, Shijun,Li, Ning,Huang, Feihe
-
p. 5872 - 5880
(2008/12/21)
-
- Regioselective routes to disubstituted dibenzo crown ethers and their complexations
-
Two isomers of bis(carbomethoxybenzo)-24-crown-8 (cis-BCMB24C8, 1, and trans-BCMB24C8, 2) were synthesized regiospecifically with acceptable to excellent yields. Cyclization in the presence of a template reagent, KPF 6, led to an essentially quantitative yield of the potassium complex of the crown ether 1; the isolated cyclization yield of pure 1 was a remarkable 89%! The methods not only avoid the very difficult separation of the isomers, but also greatly shorten the synthesis time by eliminating syringe pump usage during cyclization. The complexations of the isomeric BCMB24C8 with dibenzylammonium hexafluorophosphate (10) were studied by NMR; association constants (Ka) for 1 and 2 with the dibenzylammonium cation are 190 and 312 M-1, respectively. The X-ray crystal structures of crown ether 2 and the complexes 1·KPF6, 2·KPF6 and pseudorotaxane 2·10 were determined. The Royal Society of Chemistry 2005.
- Gibson, Harry W.,Wang, Hong,Bonrad, Klaus,Jones, Jason W.,Slebodnick, Carla,Zackharov, Lev N.,Rheingold, Arnold L.,Habenicht, Bradley,Lobue, Peter,Ratliff, Amy E.
-
p. 2114 - 2121
(2007/10/03)
-