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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Применить Всего найдено 7. Отображено 7.
04-05-2017 дата публикации

PHTHALAZINE KETONE DERIVATIVE, AND PREPARATION METHOD AND USE THEREOF

Номер: WO2017071636A1
Принадлежит:

Provided are a phthalazine ketone derivative, and a preparation method and a use thereof. Specifically, a compound as shown in formula I, a prodrug, a metabolite form, a pharmaceutically acceptable salt or ester, an isomer, a hydrate, a solvate or a crystal form thereof, and a preparation method and a use thereof are provided. The compound of the invention can significantly suppress proliferation of tumor cells, increase in vivo molecular stability, and reduce the likelihood of generating toxic metabolites. Alternatively, structural modification can be performed on a phthalazine ketone compound, thereby reducing the oxidative metabolism ability of the compound under the action of an in vivo cytochrome P450 enzyme system, and increasing bioavailability.

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22-06-2017 дата публикации

SHORT-ACTING BENZODIAZEPINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF

Номер: WO2017101808A1
Принадлежит:

The present invention relates to a benzodiazepine derivative having formula (I) and acting as a short-acting anesthetic, a pharmaceutical composition including the benzodiazepine derivative, a drug kit including the benzodiazepine derivative, a preparation method for the benzodiazepine derivative, an anesthesia method using the benzodiazepine derivative, and a use of the benzodiazepine derivative in the preparation of an anesthetic drug.

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05-04-2018 дата публикации

AZABICYCLE DERIVATIVES AND PREPARATION METHOD AND USE THEREOF

Номер: WO2018059314A1
Принадлежит:

Provided are azabicycle derivatives and a preparation method and use thereof. In particular, provided are an FXR agonist compound and a stereomer, a tautomerid, a polymorphic substance, a solvate (such as a hydrate), a pharmaceutically acceptable salt, an ester, a metabolite, an N-oxide thereof and a chemically protected form and a prodrug thereof. Also provided are a method for preparing the compound, a pharmaceutical composition comprising the compound and a medicine box and the use thereof in treating FXR-mediated diseases or conditions.

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21-04-2022 дата публикации

HETEROCYCLIC DERIVATIVE AND MEDICAL APPLICATION THEREOF

Номер: WO2022078305A1
Принадлежит:

A compound represented by general formula (I) or a stereoisomer, tautomer, deuterated substance, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, an intermediate thereof, and a preparation method therefor, as well as an application in the preparation of a drug for treating diseases related to JAK kinase activity or expression.

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26-07-2018 дата публикации

HETEROCYCLIC COMPOUND, PREPARATION METHOD AND USE THEREFOR

Номер: WO2018133730A1
Принадлежит:

Disclosed in the present invention are a farnesoid X receptor (FXR) agonist compound and a preparation method and use therefor. Specifically, provided in the present invention are a heterocyclic FXR agonist compound, as well as stereoisomers, a tautomer, a polymorph, a solvate (e.g., a hydrate), a pharmaceutically acceptable salt, an ester, a metabolite and an N-oxide thereof, and a chemically protected form and a prodrug of the foregoing. The present invention also provides a method for preparing the compound and a pharmaceutical composition and a kit which contain the compound, as well as a use therefor in the treatment of diseases or conditions which are mediated by FXR.

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22-06-2017 дата публикации

PHTHALAZINONE DERIVATIVE, AND PREPARATION METHOD AND USE THEREOF

Номер: WO2017101796A1
Принадлежит:

The present application relates to a phthalazinone derivative, and a preparation method and a use thereof. In particular, the present application relates to a compound of formula I, and a prodrug, a metabolite form, a pharmaceutically acceptable salt or an ester thereof, or isomers, hydrates, solvates or crystalline forms of the above-mentioned items, and a preparation method and use thereof. The compounds of the present application can significantly enhance the inhibitory effect on the proliferation of tumour cells; and can increase the stability of molecules in vivo and reduce the possibility of producing toxic metabolites; or can reduce the oxidative metabolic capability of compounds under the action of a P450 cytochrome enzyme system in vivo by reducing the structural modification of the phthalazinone compounds, and can improve the bioavailability.

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04-04-2023 дата публикации

Ring-fused heterocyclic derivative and application thereof in medicine

Номер: CN115916747A
Принадлежит:

The invention relates to a compound as shown in a general formula (I) or a stereoisomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or a co-crystal of the compound, an intermediate and a preparation method of the compound, and application of the compound in preparation of drugs for treating diseases related to JAK kinase activity or expression quantity.

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