35179-98-7Relevant articles and documents
Halogenated imidazole compound as well as preparation method and application thereof
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Paragraph 0025-0031, (2020/01/25)
The invention discloses alogenated imidazole compounds as well as a preparation method and application thereof. The structure of the halogenated imidazole compounds is disclosed in the invention, wherein, C * in the formula is R-type chiral carbon, and R1 and R2 can be independently selected from H and C1-6 alkyl; R3 is a substituted or unsubstituted C1-18 saturated or unsaturated aliphatic hydrocarbon, the aliphatic hydrocarbon comprises linear, branched or cyclic aliphatic hydrocarbon groups; X is H or a halogen atom; Y is H or a halogen atom; and X and Y cannot be H at the same time. The compounds or pharmaceutically acceptable salts or solvates thereof almost have no corticoid inhibition effect, can generate a rapid reversible anesthetic effect, can be rapidly metabolized into inactivecarboxylic acid metabolites, and have good revival quality after drug withdrawal; the corticoid function of the body can be rapidly recovered after single administration or continuous administration,the occurrence rate of muscular tremor after administration is low, and the body is rapidly awakened after drug withdrawal. The compounds or the salt compounds thereof can be used for preparing central inhibitory drugs which have sedative-hypnotic and/or anesthetic effects on humans or animals.
Benzodiazepine compound as well as preparation method and medical action thereof (by machine translation)
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Paragraph 0199-0201; 0328; 0329; 0331; 0334; 0335; 0337, (2021/01/11)
The invention provides a benzodiazepine compound as well as a preparation method and a medicine effect thereof, and belongs to the field of chemical medicine. The benzodiazepine compound is a compound shown in formula I. Or a salt thereof, or a stereoisomer thereof, or a solvate thereof, or a eutectic thereof, or a composition thereof. The anesthetic effect of the compound of the invention is good, and the anesthetic effect of the compound is equivalent to that of Ramozolam, and even better than that of repirzolam, and particularly shows that the effective dosage is obviously reduced, and the duration and the recovery time are remarkably reduced. At the same time, in the rat tail vein anesthesia model, the compound of the present invention is remarkably improved in comparison with the quality of the Ramozolam wake-up. The compound has the advantages of high effectiveness, short duration, fast resuscitation and good tolerance, can be used for anesthesia induction, anesthesia maintenance and inter-day operation anesthesia, and has a good application prospect. (by machine translation)
Antiviral novel nucleoside reverse transcriptase inhibitors
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Paragraph 0245; 0246; 0248; 0249; 0250, (2019/02/25)
The invention relates to compounds of antiviral novel nucleoside reverse transcriptase inhibitors, pharmaceutical compositions containing the compounds, and preparation and use of the compounds, and particularly discloses fused pyrimidine compounds shown in formula (I) and the pharmaceutical compositions containing the compounds, pharmaceutically acceptable salts, stereoisomers, solvates, hydrates, crystal forms, prodrugs or isotope derivatives. The compounds can be used for treating and/or preventing viral infectious diseases, such as human immunodeficiency virus (HIV) and hepatitis B virus (HBV). The formula (I) is shown in the specification.
BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF
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Paragraph 0319-0321, (2018/02/28)
Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).
N-substituted imidazole carboxylate compound, preparation method and use thereof
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Paragraph 0021, (2018/03/26)
A N-substituted imidazole carboxylate compound shown as a formula (I), a preparation method and use thereof are disclosed. In the formula (I), C * is a R type chiral carbon atom, R 1 and R 2 are independently selected from the group consisting of H, methyl, ethyl, cyclopropyl, cyclobutyl or isopropyl or a C2-5 ene-group formed by R1 and R2; and R3 is substituted or unsubstituted C1-18 saturated orunsaturated aliphatic hydrocarbon or aromatic hydrocarbon, wherein the aliphatic hydrocarbon includes a linear, branched or cyclic aliphatic hydrocarbon group. The N-substituted imidazole carboxylatecompound or pharmaceutically acceptable salts thereof can be used to prepare central inhibitory drugs that exert sedative, hypnotic and/or anesthetic effects on humans or animals, can produce rapid and reversible anesthetic effects, and rapidly metabolises into inactive etomidate acid, and after drug withdrawal, recovery quality is good; body's corticosteroid function can be quickly recovered after single administration or continuous administration, the incidence of muscle tremor is low after the administration, and after the drug withdrawal, the recovery is quick.
Substituted aza indole compounds and salts thereof, composition and use thereof
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Paragraph 0584; 0586; 0587, (2018/11/03)
The invention provides a substituted azaindole compound having a structure as represented by a formula (I) and a pharmaceutically acceptable salt and a medicinal preparation thereof. The compound is used for adjusting activity of protein kinase and adjusting intercellular or intracellular signal response. The invention further relates to a pharmaceutical composition including the compound and a method of applying the pharmaceutical composition to treatment of highly proliferative diseases of mammals, especially of mankind.
NUCLEOTIDE ANALOGS
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Paragraph 0182-0184, (2018/11/22)
PROBLEM TO BE SOLVED: To provide, e.g., intermediates for phosphonomethoxy nucleotide analogs, in particular, intermediates suitable for use in efficient oral delivery of such analogs. SOLUTION: Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure -OC(R2)2OC(O)X(R)a, The compounds are useful as intermediates for the preparation of antiviral compounds or oligonucleotides, or are useful for administration directly to patients for antiviral therapy or prophylaxis (R2 is as described in the specifications ). COPYRIGHT: (C)2015,JPOandINPIT
SUBSTITUTED AZAINDOLE COMPOUNDS, SALTS, PHARMACEUTICAL COMPOSITIONS THEREOF AND METHODS OF USE
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Paragraph 0435-0436, (2014/03/24)
The present invention provides substituted azaindole prodrugs, methods of making said prodrugs, pharmaceutical compositions of said prodrugs and methods of using said prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as cancer.
SUBSTITUTED METHYLFORMYL REAGENTS AND METHOD OF USING SAME TO MODIFY PHYSICOCHEMICAL AND/OR PHARMACOKINETIC PROPERTIES OF COMPOUNDS
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Page/Page column 93; 98, (2012/10/18)
The present invention relates to the synthesis and application of novel chiral/ achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
Overcoming steric effects in the coupling reaction of alkyloxycarbonyloxymethyl (AOCOM) halides with phenols: an efficient synthesis of AOCOM phenolic prodrugs
Thomas, Joshua D.,Sloan, Kenneth B.
, p. 109 - 112 (2007/10/03)
Steric hindrance is a key factor in the coupling reaction of AOCOM halides with phenols. Sterically unhindered alkoxy groups favor the formation of acylated phenol. Under phase-transfer conditions, alkylated phenol is favored regardless of steric hindrance.
