- Piperidine compound and preparation method and medical application thereof
-
The invention discloses a piperidine compound shown as a formula (I) and a preparation method and medical application thereof, and particularly relates to a piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof and a preparation method and application of the piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof. The compound provided by the invention can inhibit the activity of USP7 enzyme, has very good selectivity and druggability, and can be used for preparing medicines for preventing or treating tumor diseases or virus infectious diseases.
- -
-
Paragraph 0598-0600; 0602; 0603
(2021/04/07)
-
- Biphenyl compound as well as preparation method and medical application thereof
-
The invention discloses a biphenyl compound as well as a preparation method and medical application thereof, the structure of the biphenyl compound is shown as a formula (I) or a formula (II), and thebiphenyl compound or pharmaceutically acceptable salt, tautomer, meso-isomer, raceme, stereoisomer, metabolite, metabolite precursor, prodrug or solvate thereof is a PD-L1 inhibitor. The compound hasa remarkable inhibiting effect on the interaction of PD-1 and PD-L1 protein, so that the compound can be applied to the preparation of PD-L1 inhibitors and immunomodulator drugs for preventing or treating tumors, autoimmune diseases, organ transplant rejection, infectious diseases and inflammatory diseases.
- -
-
-
- Microwave Assisted Synthesis of Trifluoro Substituted 2-Aminobenzimidazole Derivatives via Iodoacetic Acid Mediated One-pot Condensation
-
Microwave-assisted efficient one-pot syntheses of trifluoro substituted 2-aminobenzimidazole derivative were synthesized using iodoacetic acid mediated cyclodesulfurization of thioureas. This method eliminates need to handle preformed substituted thioureas, requires lesser reaction time and temperature, is facile, and also gives higher yields of the target molecules.
- Sriram,Sapthagiri,Ilavarasan,Ravi
-
p. 2440 - 2446
(2017/07/25)
-
- Surprising characteristics of D-A-type functional dyes by introducing 4-alkoxythiazoles as the donor-unit
-
In this study, we report on the syntheses of novel donor-acceptor molecules. These new dyes comprised benzo[c][1,2,5]thiadiazole and pendants with one or two 4-alkoxythiazoles as donor parts, which were introduced without Pd-catalyzed cross coupling reactions. The optical and electrochemical properties were studied via absorption, emission spectroscopy and cyclovoltammetric measurements. We experimentally found surprising small band gaps from HOMO to LUMO of 2.4 eV and 2 eV, respectively, which were also investigated using DFT calculations.
- Gampe,N?ller,H?nsch,Schramm,Darsen,Habenicht,Ehrhardt,Wei?,G?rls,Beckert
-
p. 3232 - 3239
(2016/05/24)
-
- Synthesis and electronic and photophysical properties of [2.2]- and [3.3]paracyclophane-based donor-donor′-acceptor triads
-
Three types of the donor(D)-donor′(D′)-acceptor(A) triads 1-6 with different D-A combinations, carbazole (Cz, D)-[n.n]PCP(D′)-1,8-naphthalimide (NI, A) (1-3), 10H-phenothiazine (PTZ, D)-[n.n]PCP(D′)-NI(A) (4, 5), and 10-methyl-10H-phenothiazine (Me-PTZ, D)-[2.2]PCP-2,1,3-benzothiadiazole (BTD, A) 6, were synthesized for the elucidation of their photophysical properties. The absorption spectra and electrochemical properties indicated that the chromophores (D, D′, and A) do not interact with each other in the ground state. Cz-(CH2)3-[2.2]PCP-(CH2)3-NI 1 and Cz-(CH2)3-[3.3]PCP-(CH2)3-NI 2 show an exciplex emission between the PCP and NI moieties in cyclohexane and the intensity of the band is much higher in 2 than in 1, whereas Cz-(CH2)2-[2.2]PCP-(CH2)2-NI 3 does not show any exciplex emission in cyclohexane. These results indicated that the combination of [3.3]PCP and a trimethylene chain is preferable for the exciplex formation. PTZ-(CH2)3-[2.2]PCP-(CH2)3-NI 4 shows a broad band at 519 nm in cyclohexane, which is associated with the formation of the exterplex band among the NI, [2.2]PCP, and PTZ moieties, while PTZ-(CH2)3-[3.3]PCP-(CH2)3-NI 5 does not show the band. Me-PTZ-(CH2)2-[2.2]PCP-(CH2)2-BTD 6 shows a broad fluorescence band due to both the BTD and PTZ moieties in cyclohexane. In CH3CN, the fluorescence spectra of 1-6 suggest the presence of a photoinduced charge separation process. The study of the photoinduced charge separation process will be soon reported elsewhere.
- Miyazaki, Takaaki,Shibahara, Masahiko,Fujishige, Jun-Ichi,Watanabe, Motonori,Goto, Kenta,Shinmyozu, Teruo
-
p. 11440 - 11453
(2015/01/16)
-
- Cyclic bis-benzimidazole ligands and metal complexes thereof
-
Cyclic bis benzimidazole ligands of the following formula are formed by contacting a (2-aminophenyl)-benzimidazole-4-carboxaldehyde ethylene acetal or a (2-nitrophenyl)-benzimidazole-4-benzaldehyde with an acid optionally in the presence of a metal or a metal salt. wherein R1and R2may be the same or different and are selected from H, an alkyl having 1 to 10 carbon atoms, a benzyl group, a substituted 2-ethylphenyl group, a carbonyl group, a phenyl substituent, a tosyl group, and an alkylsulfonate group; R3and R4may be the same or different and are selected from H, methyl, and ethyl; and R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, and R18may be the same or different and are selected from H, alkyl having 1 to 10 carbon atoms, fluoride, chloride, bromide, iodide, nitro, amino, a carboxylate, an ester, and a phenyl group.
- -
-
-
- An original way for synthesis of new nitro-benzothiadiazole derivatives
-
The C-alkylation reaction of 4-chloromethyl-7-nitro-2,1,3-benzothiadiazole with 2-nitropropane anion which is shown to proceed by an SRN1 mechanism is an original way for the synthesis of new 2,1,3-benzothiadiazoles.
- Vanelle, Patrice,Liegeois, Celine Tremblais,Meuche, Jacobine,Maldonado, Jose,Crozet, Michel P.
-
p. 955 - 962
(2007/10/03)
-
- Synthesis of a new type of "bent" heterocyclic benzimidazolo-pyridazinones
-
The synthesis of some new heterocyclic benzimidazolo-pyridazinines starting from 2,1,3-benzothiadiazole-4-carboxaldehyde 2 is described.Biological evaluation of all new compounds proved them to be inhibitors of phosphodiesterase III with no marked positiv
- Jonas, R,Pruecher, H,Wurziger, H
-
p. 141 - 148
(2007/10/02)
-