130309-46-5Relevant articles and documents
Rigid aromatic linking moiety in cationic lipids for enhanced gene transfection efficiency
Wang, Bing,Zhao, Rui-Mo,Zhang, Ji,Liu, Yan-Hong,Huang, Zheng,Yu, Qing-Ying,Yu, Xiao-Qi
, p. 585 - 595 (2017)
Although numerous cationic lipids have been developed as non-viral gene vectors, the structure-activity relationship (SAR) of these materials remains unclear and needs further investigation. In this work, a series of lysine-derived cationic lipids contain
Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains
Jecs, Edgars,Miller, Eric J.,Wilson, Robert J.,Nguyen, Huy H.,Tahirovic, Yesim A.,Katzman, Brook M.,Truax, Valarie M.,Kim, Michelle B.,Kuo, Katie M.,Wang, Tao,Sum, Chi S.,Cvijic, Mary E.,Schroeder, Gretchen M.,Wilson, Lawrence J.,Liotta, Dennis C.
, p. 89 - 93 (2018)
A structure-activity relationship study of potent TIQ15-derived CXCR4 antagonists is reported. In this investigation, the TIQ15 side-chain was constrained to improve its drug properties. The cyclohexylamino congener 15a was found to be a potent CXCR4 inhi
Discovery of Hydroxyamidine Derivatives as Highly Potent, Selective Indoleamine-2,3-dioxygenase 1 Inhibitors
Jin, Fangfang,Hu, Qiyue,Fei, Hongbo,Lv, Hejun,Wang, Shenglan,Gui, Bin,Zhang, Junzhen,Tu, Wangyang,Zhang, Yun,Zhang, Lei,Wan, Hong,Zhang, Limin,Hu, Bin,Yang, Fanglong,Bai, Chang,He, Feng,Zhang, Lianshan,Tao, Weikang
supporting information, p. 195 - 201 (2021/02/06)
In this study, a series of novel hydroxyamidine derivatives were identified as potent and selective IDO1 inhibitors by structure-based drug design. Among them, compounds 13-15 and 18 exhibited favorable enzymatic and cellular activities. Compound 18 showed improved bioavailability in mouse, rat, and dog (F% = 44%, 58.8%, 102.1%, respectively). With reasonable in vivo pharmacokinetic properties, compound 18 was further evaluated in a transgenic MC38 xenograft mouse model. The combination of compound 18 with PD-1 monoclonal antibody showed a synergistic antitumor effect. These data indicated that compound 18 as a potential cancer immunotherapy agent should warrant further investigation.
Preparation method of trans 4 - (tert-butyloxycarbonylamino) cyclohexanecarboxylic acid and intermediate thereof
-
Paragraph 0043; 0046-0047; 0050, (2021/09/21)
The invention provides a preparation method of trans 4 - (tert-butyloxycarbonylamino) cyclohexanecarboxylic acid and an intermediate thereof. The preparation method is characterized by comprising the following steps of 4 - oxocyclohexane carboxylic ester and chiral ligand reagent tert-butyl sulfinamide as a raw material, reducing amination to obtain trans -4 -tert-butyl sulfinyl sulfenamide cyclohexane carboxylic acid ester by virtue of chiral ligand reagent tert-butyl sulfinamide and 4 - 95% -oxocyclohexane carboxylic ester, and is stable in basic conditions and easy to leave under an acidic condition. Reaction conditions are mild, operation is simple and convenient, yield is high, and industrial production is easy.
BIFUNCTIONAL DEGRADERS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASES AND THERAPEUTIC USE THEREOF
-
, (2021/08/27)
The present disclosure provides bifunctional compounds as IRAK4 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by IRAK4.
Compound serving as protein kinase inhibitor and application of compound
-
, (2021/04/07)
The invention discloses a compound used as a protein kinase inhibitor and application of the compound, the compound has an obvious inhibition effect on protein kinase activity, can be used as a BTK inhibitor for preparing medicines for treating BTK-mediated diseases such as malignant tumors, autoimmune diseases and the like, and has wide application prospect.
Generation of highly potent DYRK1A-dependent inducers of human β-Cell replication via Multi-Dimensional compound optimization
Allegretti, Paul A.,Horton, Timothy M.,Abdolazimi, Yassan,Moeller, Hannah P.,Yeh, Benjamin,Caffet, Matthew,Michel, Guillermina,Smith, Mark,Annes, Justin P.
supporting information, (2019/12/09)
Small molecule stimulation of β-cell regeneration has emerged as a promising therapeutic strategy for diabetes. Although chemical inhibition of dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) is sufficient to enhance β-cell replicat
Preparation method of trans-4-N-Bocaminocyclohexylamine carboxylic acid
-
Paragraph 0042-0047; 0048; 0052-0054, (2019/07/04)
The invention discloses a preparation method of trans-4-N-Bocaminocyclohexylamine carboxylic acid, and belongs to the technical field of organic synthesis. 4-oxocyclohexane carboxylic acid triphenyl methanol ester is taken as the raw material, and the pro
POLYCYCLIC AMINES AS OPIOID RECEPTOR MODULATORS
-
Paragraph 0129; 0272, (2018/10/11)
The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.
PROCESS FOR THE PREPARATION OF TRANS-4-AMINO-1-CYCLOHEXANECARBOXILIC ACID AND ITS DERIVATIVES
-
Page/Page column 11, (2017/09/02)
The present invention relates to a one-pot process for the preparation of trans-4-amino-l-cyclohexanecarboxylic acid derivatives where the trans ratio is more than 75% by reaction of a 4-aminobenzoic acid derivative using an appropriate catayst and an appropriate solvent or solvent mixture under basic conditions. The process uses low hydrogen pressure and is therefore suitable for industrial application.