214910-41-5Relevant articles and documents
Substituted phenoxy-2-azabicyclo[3.2.1]octane compound as well as preparation method and application thereof
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Paragraph 0055; 0058-0059, (2020/06/02)
The invention belongs to the technical field of medicines, and particularly relates to a substituted phenoxy-2-azabicyclo[3.2.1]octane compound as well as a preparation method and application thereof.The general structural formula I of the substituted phenoxy-2-azabicyclo[3.2.1]octane compound is specifically shown in the specification, wherein R is methyl, methoxy, cyano, fluorine, chlorine, bromine or nitro groups. Pharmacological research shows that the compound shows a good effect in an in-vitro antitumor activity test, and can be used for preparing antitumor drugs. The preparation methodof the substituted phenoxy-2-azabicyclo [3.2.1]octane compound provided by the invention is simple and feasible, relatively high in yield and easy for large-scale production.
ALKYNE COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Paragraph 0581, (2017/03/14)
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is alkyne substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein can reduce the excessive activation of complement.
COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS
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Paragraph 0528, (2017/03/14)
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula (I), or a pharmaceutically acceptable salt or composition thereof The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.
AMIDE COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Paragraph 0633, (2017/03/14)
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an amide substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein are capable of reducing the excessive activation of complement.
ETHER COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Paragraph 0661, (2017/03/14)
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an ether substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.
PHOSPHONATE COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Paragraph 0567, (2017/03/14)
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula (I), or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is a phosphonate substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Paragraph 0720, (2017/03/14)
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors of Factor D described herein reduce the excessive activation of complement.
Substituted piperidine amide derivative, preparation method thereof, and application of derivative to pharmacy
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Paragraph 0334; 0347; 0348; 0349; 0350, (2017/08/30)
The invention relates to a substituted piperidine amide derivative as shown in a general formula (I) or a stereisomer and pharmaceutically acceptable salt thereof, a preparation method of the derivative, medicinal combination as well as application of the derivative to the aspects of local anaesthesia or analgesia. The definition of each group of the general formula (I) is consistent with that of the description. (The general formula (I) is as shown in the description).
SUBSTITUTED OXETANES AND THEIR USE AS INHIBITORS OF CATHEPSIN C
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Page/Page column 45; 46, (2016/03/04)
This invention relates to a compound of formula I and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
Method for reducing content of diastereoisomer impurity in Ledipasvir intermediate
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Paragraph 0049; 0050; 0051; 0052, (2016/10/10)
The invention discloses a method for reducing content of a diastereoisomer impurity (Ia) in a Ledipasvir intermediate (1R,3S,4S)-N-t-butyloxycarboryl-2-azabicyalo[2.2.1]heptane-3-carboxylic acid (I). The method comprises the steps of firstly taking a crude product of a compound shown as a formula (I) and containing the diastereoisomer impurity (Ia), dissolving in an organic solvent, adding alkaline organic amine to react with the crude product, separating out a solid, and filtering to obtain an amine salt of the compound shown as the formula (I); acidizing the obtained amine salt in an aqueous phase solution; extracting an obtained aqueous phase, separating out a solid, and separating to obtain the high-purity Ledipasvir intermediate (I). The product obtained by the method has a de value up to more than 99.5 percent, and the yield of more than 80 percent; reaction conditions in the method are mild, raw materials are easy to get, and the method is suitable for industrial application.
