3-amino-5-phenyl-pyrazole derivative tubulin inhibitor as well as preparation and medical application thereof
The invention provides a 3-amino-5-phenyl-pyrazole derivative tubulin inhibitor and preparation and medical application thereof, the structure of the 3-amino-5-phenyl-pyrazole derivative is shown as a formula (I), in the formula (I), R1 is independently selected from 3, 4, 5-trimethoxy phenyl, 3, 4-dimethoxy phenyl or dioxolane [1, 3-d] phenyl, R2 is independently selected from 3, 4, 5-trimethoxy phenyl, 3, 4-dimethoxy phenyl or dioxolane [1, 3-d] phenyl, and R3 is independently selected from 3, 4, 5-trimethoxy phenyl, 3, 4-dimethoxy phenyl or dioxolane [1, 3-d] phenyl; r2 and R3 are independently selected from methyl, methoxyl, fluorine, chlorine or bromine. The compound not only has strong anti-tumor activity, but also has an anti-angiogenesis effect, can effectively inhibit proliferation of tumor cells, and can be used for preparing a tumor proliferation inhibitor. Moreover, the tubulin inhibitor has very strong capability of inhibiting aggregation of tubulin, and a novel tubulin inhibitor is provided for inhibiting proliferation of tumor cells..
| Medienart: |
|
|---|
Patent| Erscheinungsjahr: |
2023 |
|---|---|
| Erschienen: |
2023 |
| Enthalten in: |
Europäisches Patentamt - (2023) vom: 04. Aug. Zur Gesamtaufnahme - year:2023 |
|---|
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
LI CAOLONG [VerfasserIn] |
|---|
| Links: |
Volltext [kostenfrei] |
|---|
| Anmerkungen: |
Source: www.epo.org (no modifications made), First posted: 2023-08-04, Last update posted on www.tib.eu: 2023-12-05, Last updated: 2023-12-08 |
|---|
| Patentnummer: |
CN116535356 |
|---|
| Förderinstitution / Projekttitel: |
|
|---|
| PPN (Katalog-ID): |
EPA018559581 |
|---|
| LEADER | 01000caa a22002652 4500 | ||
|---|---|---|---|
| 001 | EPA018559581 | ||
| 003 | DE-627 | ||
| 005 | 20231208115547.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231117s2023 xx |||||o 00| ||eng c | ||
| 035 | |a (DE-627)EPA018559581 | ||
| 035 | |a (EPA)CN116535356 | ||
| 035 | |a (EPA)87454865 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 0 | |a LI CAOLONG |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a 3-amino-5-phenyl-pyrazole derivative tubulin inhibitor as well as preparation and medical application thereof |
| 264 | 1 | |c 2023 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a Computermedien |b c |2 rdamedia | ||
| 338 | |a Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Source: www.epo.org (no modifications made), First posted: 2023-08-04, Last update posted on www.tib.eu: 2023-12-05, Last updated: 2023-12-08 | ||
| 520 | |a The invention provides a 3-amino-5-phenyl-pyrazole derivative tubulin inhibitor and preparation and medical application thereof, the structure of the 3-amino-5-phenyl-pyrazole derivative is shown as a formula (I), in the formula (I), R1 is independently selected from 3, 4, 5-trimethoxy phenyl, 3, 4-dimethoxy phenyl or dioxolane [1, 3-d] phenyl, R2 is independently selected from 3, 4, 5-trimethoxy phenyl, 3, 4-dimethoxy phenyl or dioxolane [1, 3-d] phenyl, and R3 is independently selected from 3, 4, 5-trimethoxy phenyl, 3, 4-dimethoxy phenyl or dioxolane [1, 3-d] phenyl; r2 and R3 are independently selected from methyl, methoxyl, fluorine, chlorine or bromine. The compound not only has strong anti-tumor activity, but also has an anti-angiogenesis effect, can effectively inhibit proliferation of tumor cells, and can be used for preparing a tumor proliferation inhibitor. Moreover, the tubulin inhibitor has very strong capability of inhibiting aggregation of tubulin, and a novel tubulin inhibitor is provided for inhibiting proliferation of tumor cells. | ||
| 650 | 4 | |a C07D: Heterocyclic compounds (macromolecular compounds c08) | |
| 650 | 4 | |a A61K: Preparations for medical, dental, or toilet purposes (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms a61j0003000000;chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles a61l; soap compositions c11d) | |
| 650 | 4 | |a A61P: Specific therapeutic activity of chemical compounds or medicinal preparations | |
| 650 | 4 | |a che | |
| 650 | 4 | |a 615 | |
| 700 | 0 | |a LI MENGHUA |4 aut | |
| 700 | 0 | |a GE YANAN |4 aut | |
| 700 | 0 | |a YU XINYU |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Europäisches Patentamt |g (2023) vom: 04. Aug. |
| 773 | 1 | 8 | |g year:2023 |g day:04 |g month:08 |
| 856 | 4 | 0 | |u https://worldwide.espacenet.com/patent/search/family/87454865/publication/CN116535356A1?q=CN116535356 |z kostenfrei |3 Volltext |
| 912 | |a GBV_EPA | ||
| 936 | u | w | |j 2023 |b 04 |c 08 |
| 951 | |a AR | ||
| 952 | |j 2023 |b 04 |c 08 | ||