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Применить Всего найдено 14. Отображено 14.
06-06-2013 дата публикации

THIENYL [3, 2-D] PYRIMIDIN-4-ONE COMPOUNDS, PREPARATION METHOD, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF

Номер: WO2013078765A1
Принадлежит:

Disclosed are new thienyl [3, 2-d] pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPⅣ (dipeptide peptidase Ⅳ) inhibitors and can treat type II diabetes through well inhibiting DPPⅣ, indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.

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08-10-2015 дата публикации

2,2'-TANDEM DITHIAZOLE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF

Номер: WO2015149656A1
Принадлежит:

The present invention relates to a thiazole compound, a preparation method therefor, and a user thereof. More specifically, the present invention relates to a 2,2'-tandem dithiazole compound, a preparation method therefor, and the use thereof as a histone deacetylase inhibitor in preparing anti-tumor medications, and medications for treating autoimmune diseases, type II diabetes and complications thereof, or neurodegenerative diseases.

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17-05-2018 дата публикации

2-SUBSTITUTED AROMATIC RING-PYRIMIDINE DERIVATIVE, AND PREPARATION AND APPLICATION THEREOF

Номер: WO2018086547A1
Принадлежит:

Provided are a 2-substituted aromatic ring-pyrimidine derivative represented by general formula (I), and an optical isomer thereof, or a pharmaceutically acceptable salt or solvate thereof. N-substituted pyridine-2-aminopyrimidine obtained by structure-based virtual screening is used as a lead compound, and then a series of novel small-molecular Chk1 inhibitors are designed and synthesized. The compounds are then subjected to Chk1 kinase inhibitory activity assay at molecular level. The assay proves that the compound has strong anticancer performance, has Chk1 kinase inhibitory activity, has prospect as a Chk1 inhibitor, and can be applied to medicines for therapy of human or animal cell proliferation related solid tumors or leukaemia.

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08-10-2015 дата публикации

2,2'-TANDEM DITHIAZOLE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF

Номер: WO2015149656A8
Принадлежит:

The present invention relates to a thiazole compound, a preparation method therefor, and a user thereof. More specifically, the present invention relates to a 2,2'-tandem dithiazole compound, a preparation method therefor, and the use thereof as a histone deacetylase inhibitor in preparing anti-tumor medications, and medications for treating autoimmune diseases, type II diabetes and complications thereof, or neurodegenerative diseases.

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17-05-2018 дата публикации

2-POLYSUBSTITUTED AROMATIC RING-PYRIMIDINE DERIVATIVE AND PREPARATION AND MEDICAL USE

Номер: WO2018086546A1
Принадлежит:

Provided are a 2-polysubstituted aromatic ring-pyrimidine derivative and an optical isomer thereof or a pharmaceutically acceptable salt or solvate thereof. The compound and the optical isomer thereof or the pharmaceutically acceptable salt or solvate thereof can be used in the preparation of an anti-tumor drug. The present invention uses the N-substituted pyridine-2-aminopyrimidine obtained through the structure-based virtual screening as a lead compound, designs and synthesizes a series of brand new small molecular Chk1 inhibitors, and tests the compounds for the Chk1 kinase inhibitory activity on a molecular level. The experiments confirm that the compound is a promising Chk1 inhibitor having strong anti-cancer effects and that the Chk1 kinase inhibitory activity and is a new drug for treating cancers, and can be used to treat solid tumours or leukemia associated with cell proliferation in humans or animals. The 2-polysubstituted aromatic ring-pyrimidine derivative provided by the present ...

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21-09-2017 дата публикации

FLUORINATED CYCLOPROPYLAMINE COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION THEREOF, AND USERS THEREOF

Номер: WO2017157322A1
Принадлежит:

Provided are a compound represented by formula I, a raceme thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof, a preparation method therefor, a pharmaceutical composition comprising the compound, and uses thereof serving as an lysine specific demethylase 1 (LSD1) inhibitor. Provided are uses of the fluorinated cyclopropylamine compound represented by formula I in the treatment of cancers.

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18-08-2016 дата публикации

CRYSTAL FORM A OF COMPOUND AND PREPARATION METHOD THEREOF

Номер: WO2016127898A1
Принадлежит:

The present invention relates to the crystal form A of a compound. The present invention further discloses a preparation method and a pharmaceutical composition of the crystal form A of the compound. The crystal form A has a relative strong hypoglycemic activity in vivo, and is hoped to be a new pharmaceutically active ingredient for treating or preventing type II diabetes and/or the complications of type II diabetes.

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21-12-2017 дата публикации

TRANS-INDOLINE CYCLOPROPYLAMINE CHEMICAL COMPOUND, AND METHOD FOR PREPARATION, PHARMACEUTICAL COMPOSITION, AND USE THEREOF

Номер: WO2017215464A1
Принадлежит:

The present invention relates to the fields of medicinal chemistry and pharmacotherapy, and specifically relates to the chemical compound of formula (I), and its racemate, R-isomer, S-isomer, pharmaceutically acceptable salt, and mixtures thereof, as well as its method for preparation, a pharmaceutical composition containing said chemical compound, and use as a lysine-specific demethylase 1 (LSD1) inhibitor. The cyclopropylamine chemical compound to which the present invention relates may be used in the treatment of cancer.

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15-11-2012 дата публикации

THIAZOLE COMPOUND AND PREPARATION METHOD AND USE THEREOF

Номер: WO2012152208A1
Принадлежит:

The present invention disclosed a class of thiazole compounds of general formula (I) and the preparation method and use thereof. More particularly, The present invention disclosed a derivative of natural product largazole, the preparation method thereof and the use in the field of antitumor and multiple sclerosis treatment as a histone deacetylase inhibitor.

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08-03-2018 дата публикации

ARYL-2,2'-TANDEM BISTHIAZOLE COMPOUND AND PREPARATION METHOD AND USE THEREOF

Номер: WO2018041004A1
Принадлежит:

The present invention relates to an aryl-2,2'-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2'-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs.

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23-05-2023 дата публикации

Multifunctional compound capable of degrading BTK kinase, composition and application

Номер: CN116143757A
Принадлежит:

The invention discloses a Bruton's tyrosine kinase degradation agent. The Bruton's tyrosine kinase degradation agent has a structure as shown in a general formula I, or a stereoisomer thereof, or a stereoisomer mixture thereof, or a pharmaceutically acceptable salt and prodrug thereof; the invention also discloses application of the compound and a pharmaceutical composition containing the compound in preparation of drugs for treating diseases related to Bruton's tyrosine kinase, such as B cell or plasma cell proliferative diseases. The compound provided by the invention has strong cell proliferation inhibition activity, can effectively degrade Bruton's tyrosine kinase, and has good liver microparticle metabolism stability and better oral absorption property. The compound can be applied to drugs for treating diseases, obstacles or symptoms which benefit from inhibition or degradation of the activity of Bruton's tyrosine kinase alone or in combination with other drugs.

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14-04-2023 дата публикации

Heterocyclic compound as well as preparation method and application thereof

Номер: CN115960083A
Принадлежит:

The invention discloses a heterocyclic compound as well as a preparation method and application thereof, and particularly discloses a compound as shown in a formula I, pharmaceutically acceptable salt thereof, enantiomer thereof, diastereoisomer thereof, isotope derivative thereof, prodrug thereof, solvate thereof or hydrate thereof, which can be used for preventing and/or treating BCL-2 mediated related diseases. Especially hematologic tumors.

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06-06-2023 дата публикации

Anti-apoptotic protein BCL-2 inhibitor, pharmaceutical composition and application thereof

Номер: CN116217566A
Принадлежит:

The invention discloses a Bcl-2 protein apoptosis inducer, and further discloses application of a compound and a pharmaceutical composition containing the compound in preparation of drugs for treating anti-apoptosis protein BCL-2 related diseases such as infectious diseases, immune diseases, inflammatory diseases and cell proliferation abnormality diseases. The compound disclosed by the invention has strong BCL2/BAK blocking activity, and can be applied to treatment of infectious diseases, immune diseases, inflammatory diseases or cell proliferation abnormality and other diseases which benefit from inhibition of anti-apoptotic protein BCL-2.

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12-05-2023 дата публикации

Aromatic heterocyclic compound and application thereof

Номер: CN116102533A
Принадлежит:

The invention discloses an aromatic heterocyclic compound and application thereof. The invention provides an aromatic heterocyclic compound as shown in a formula I. The aromatic heterocyclic compound has better LSD1 enzyme inhibition activity, can be used as an LSD1 inhibitor and is used for treating tumors and the like.

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