Amidosiarczanowe pochodne 4-(1-fenylo-1H-[1,2,3]triazol-4-ylo)-fenolu, pochodne 4-(1-fenylo-1H-[1,2,3]triazol-4-ylo)-fenolu, ich zastosowanie medyczne i sposób otrzymywania amidosiarczanowych pochodnych 4-(1-fenylo-1H-[1,2,3]triazol-4-ylo)-fenolu - Invention - Bridge of Knowledge

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Amidosiarczanowe pochodne 4-(1-fenylo-1H-[1,2,3]triazol-4-ylo)-fenolu, pochodne 4-(1-fenylo-1H-[1,2,3]triazol-4-ylo)-fenolu, ich zastosowanie medyczne i sposób otrzymywania amidosiarczanowych pochodnych 4-(1-fenylo-1H-[1,2,3]triazol-4-ylo)-fenolu

Invention

Details

Creators
Property
Politechnika Gdańska
Supervisor unit

Legal protection

Status
Pending
Patent granting institution
WIPO
Application number
PCT/PL2018/000080 20-08-2018
Verified by:
Gdańsk University of Technology

Legal protection 239999

Status
Protected
Patent granting institution
Urząd Patentowy Rzeczpospolitej Polskiej
Application number
P.425970 18-06-2018
Patent number
239999
Verified by:
Gdańsk University of Technology

Legal protection 7160387

Status
Protected
Patent granting institution
Japoński Urząd Patentowy
Application number
2020-570953 20-08-2018
Patent number
7160387
Verified by:
Gdańsk University of Technology

Oferty komercjalizacji

Oferta

New molecular entity (NME) that proved to be a very promising drug candidate in the treatment of hormone-dependent diseases, particularly cancers such as breast, ovary, prostate, endometrium, testes.

During the course of the research many beneficial biological properties were confirmed, including:

high overall anti-cancer activity in vivo: +50% inhibition of tumor growth was observed for the most promising compound, highly inhibitory activity against the molecular target in vivo (apparently full blockage in the cancer cells and liver), essential reduction of estradiol levels in the blood, high solubility and permeability in vitro and in vivo, safety: observably no side effects during the experiments on mice even for doses as high as 50 mg / kg / day.

Application and audience

Recently, steroid sulfatase (STS) inhibitors have become promising drug candidates in the treatment of a wide spectrum of tumors. Cancer diseases are a critical medical problem - according to the International Agency for Research on Cancer and European Commission estimates in 2018, globally there were more than 18 million new cases (3 million in the European Union [EU]) and 9.5 million cancer-related deaths (1.4 million in the EU), which indicates that tumors are among the leading causes of death worldwide.

Innovative aspects and main features

The hormone biosynthesis pathway is a well-established target for the development of hormone-dependent cancer drugs. Anticancer therapies currently used often turn out to be unsatisfactory and result in the development of resistance, leading to relapses in tumor progression (e.g. in case of therapies based on aromatase inhibitors). In light of recent research STS is becoming a new interesting molecular target in the development of novel and effective hormone-dependent cancer treatment methods. In contrast to aromatase, the STS activity is present in most cancer cases (e.g. STS expression is detected in 90% of breast tumors). Furthermore, it has been noticed that STS mRNA levels in malignant tissues were higher than in normal breast tissues in 87% of tested patients.

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