- Immune checkpoint small-molecule inhibitor as well as preparation method and application thereof
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The invention provides a PD-1/PD-L1 interaction inhibitor as well as a preparation method, pharmaceutical composition and application thereof. Specifically, the invention provides a compound with a structure as shown in a formula (I), and definition of each functional group is described in the specification. The compound and a composition containing the compound can be used for treating and/or preventing diseases related to PD-1/PD-L1 signaling pathways, such as cancers, infectious diseases and autoimmune diseases.
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Paragraph 0242-0244
(2020/12/08)
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- [...] compound or its salt and its preparation and use
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The invention relates to novel prazole compounds, salts thereof, and a preparation method and applications of the prazole compound. The novel prazole compounds all have a structural formula represented by the formula (I); wherein the R1 and R2 individually represent a C1-C6 alkyl group, and the X represents a hydrogen atom, an alkali metal atom like lithium, sodium or potassium, or an alkali earth metal atom like magnesium or calcium. The novel prazole compounds have better safety, and moreover the curative effect of the novel prazole compounds is prominently better than that of various conventional prazole compounds.
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- Identification and synthesis of potential impurities of rabeprazole sodium
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Rabeprazole sodium (1, Achiphex) is a gastric proton pump inhibitor. It causes dose-dependent inhibition of acid secretion and is useful as an anti-ulcer agent. In the process for the preparation of 1, two potential unknown impurities were identified in HPLC at levels ranging from 0.05-0.8%. Based on mass spectral data vide LC-MS, the two impurities were characterized as 2-{[(4-chloro-3-methyl-2-pyridinyl) methyl] sulfinyl}-1H-bezimidazole (2, chloro analogue of rabeprazole) and 2-[{(4-methoxy-3-methyl-2-pyridinyl)methyl} sulfinyl]-1H-benzimidazole (3, methoxy analogue of rabeprazole). The structures were unambiguously established by independently synthesizing them and co-injecting in HPLC. To our knowledge, the compounds 2 and 3 have not been reported as process impurities elsewhere.
- Pingili, R. Reddy,Jambula, M. Reddy,Ganta, M. Reddy,Ghanta, M. Reddy,Sajja,Sundaram,Boluggdu, V. Bhaskar
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p. 814 - 818
(2007/10/03)
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- 4-Oxoquinolizine antimicrobial having 2-pyridone skeleton as partial structure
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A compound represented by the following Formula (I) or a pharmaceutically acceptable salt thereof: 1wherein R1 represents a hydrogen atom or a carboxyl-protecting group, R2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a hydroxyl group, R3 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a nitro group, a cyano group, a hydroxyl group or an amino group; R4 represents a hydrogen atom, an amino-protecting group, an alkyl group or a cycloalkyl group, and R5 represents a hydrogen atom, a halogen atom, an alkyl group, an alkenyl group, a cycloalkyl group, an aryl group, an alkoxy group, an alkylthio group, a hydroxyl group, an imino group or an amino group.
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- Potential antitumor agents. 14. 4 Substituted 2 formylpyridine thiosemicarbazones
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A series of 4 substituted 2 formylpyridine thiosemicarbazones has been synthesized which contain a tertiary N at the 4 position. These materials were obtained by reacting 4 nitro 2 picoline N oxide, either directly or after conversion to the corresponding 4 chloro derivative, with a variety of secondary amines. Rearrangement of the 4 substituted 2 picoline N oxides with Ac2O yielded respective methyl acetates, which upon acid hydrolysis, MnO2 oxidation, and reaction with thiosemicarbazide resulted in the desired compounds. An alternate procedure which consisted of reacting 4 chloro 2 formylpyridine ethylene acetal with various amines, followed by hydrolysis and reaction with thiosemicarbazide, was also employed. Introduction of an alkyl group at the 3 position of the pyridine ring of 4 morpholino 2 formylpyridine thiosemicarbazone was achieved by utilizing 2,3 dimethyl 4 nitropyridine N oxide; this material was converted to the corresponding 4 chloro derivative which was then subjected to nucleophilic substitution. 4 Morpholino 2 formylpyridine thiosemicarbazone was the most active antineoplastic agent of this series in mice bearing Sarcoma 180 ascites cells and was significantly superior to 5 hydroxy 2 formylpyridine thiosemicarbazone in this test system.
- Agrawal,Booth,DeNuzzo andSartorelli
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p. 1209 - 1214
(2007/10/04)
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