2867-62-1Relevant articles and documents
KRAS G12C INHIBITORS
-
Paragraph 0283-0284, (2020/03/23)
The present invention relates to compounds that, inhibit KRas G12C, In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
KRAS G12C INHIBITORS
-
Paragraph 0280, (2020/07/25)
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
KRAS G12C INHIBITORS
-
Paragraph 0414-0415, (2019/05/24)
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
Synthesis and biological evaluation of novel anti-hepatitis C virus (HCV) agents: 2-hydroxylphenethyl sulfanyl-oxopyrimidines
Wu, Daochun,Feng, Yue,Wang, Hua,Yang, Junfeng,Chen, Xian,Wang, Yueping,Cong Lai, Christopher,Zhang, Yufang,Li, Cong,Xia, Xueshan,He, Yanping
, p. 1388 - 1396 (2017/06/05)
A novel series of dihydro-hydroxyl-phene-thylsulfanyl-ω-cyclohexyl/phenyl-oxopyrimidine derivatives have been synthesized and their in vitro anti-hepatitis C virus activities have been evaluated using Huh 7.5.1 cells. Some of the compounds showed moderate
KRAS G12C INHIBITORS
-
Paragraph 0259, (2017/12/18)
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
Preparation of fluorine-containing methyl or aryl alkyl ketone method
-
Paragraph 0097, (2016/10/07)
The invention discloses a method for preparing fluorine-containing methyl or alkylaryl ketones, belonging to an organic synthesis field. The method comprises two steps of: ester condensation: ester condensation reaction of an R1COOR2 compound represented by a formula A with a R2COOR2 compound represented by a formula B, is performed to form an R1COCH(R3)COOR2 intermediate represented by a formula C; and ester interchange: R1COCH(R3)COOR2 represented by the formula C is carried out ester interchange reaction with R2COOH under 100-110 DEG C and with catalysis of dilute H2SO4 or a cationic resin, and then decarboxylating to obtain R1COR2 fluorine-containing methyl or alkylaryl ketones represented by a formula D. The R1 group may be CF3-, CF2-, CF- or Ar-; the R2 group may be CH3-, Et- and n-Pr; and the R3 group may be CH3-, Et- and H-. Ester interchange in the invention avoids formation of HOR2 which has a nearly same boiling point with the compound represented by the formula D and is azeotropic with the compound represented by the formula D, enables the compound represented by the formula D to be purified without series rectification operation, and is suitable for large scale production. Simultaneously, ester interchange in the invention greatly raises cost. An ion exchange resin completes ester interchange in a waterless condition, which avoids a de-watering step, and simplifies technologies.
New efficient and flexible synthetic route to Emivirine and its analogs
Li, Li,Ma, Liying,Wang, Xiaowei,Liu, Junyi
, p. 164 - 168 (2013/04/24)
A revised synthetic route to Emivirine (MKC-442) via properly substituted β-keto ester converted from Meldrum's Acid was developed. This method could be applied to the synthesis of a variety of MKC-442 analogues and open the way for their systematic biological evaluation.
A double Mannich approach to the synthesis of substituted piperidones - Application to the synthesis of substituted E-ring analogues of methyllycaconitine
Chan, Yinman,Balle, Jared,Kevin Sparrow,Boyd, Peter D.W.,Brimble, Margaret A.,Barker, David
experimental part, p. 7179 - 7191 (2010/10/01)
The double Mannich reaction of acyclic α,γ-substituted β-keto esters and bis(aminol) ethers gives substituted 3,5-substituted-4- piperidones with high levels of diastereoselectivity. These piperdiones can be easily transformed into substituted E-ring analogues of the delphinium alkaloid methyllycacotine.
Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors
Qin, Hua,Liu, Chang,Guo, Ying,Wang, Ruiping,Zhang, Jianfang,Ma, Liying,Zhang, Zhili,Wang, Xiaowei,Cui, Yuxin,Liu, Junyi
scheme or table, p. 3231 - 3237 (2010/07/05)
A series of novel S-DABO analogues (4a1-5a12) have been synthesized by an efficient method and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). The biological testing results clearly indicated that the substitution of halogen at the C5 position of pyrimidine ring could increase the anti-HIV-1 RT activity. The most active compounds showed activity in the low micromole range with IC50 values (IC50 0.18-3.03 μM) comparable to nevirapine (IC50 4.12 μM). The docking showed that a new halogen bond was formed between halogen and carbonyl of TYR188 in the HIV-I RT.
Synthesis and anti-HIV-1 activity of S-dihydro(alkyloxy)benzyloxypyrimidine derivatives
Rao, Zhi-Kun,Long, Jing,Li, Cong,Zhang, Sui-Shuan,He, Mei,Ou, Ling-Cheng,Zheng, Yong-Tang,He, Yan-Ping
scheme or table, p. 967 - 974 (2009/10/16)
Several 2-heteroaryl-, 2-heteroarylcarbonylmethyl-, 2-arylcarbonylmethyl, and 2-arylethyl derivatives of S-dihydro(alkyloxy)benzyloxypyrimidines have been synthesized and the anti-HIV activities of these compounds were tested in C8166 cell and against RT
