- 专利标题: USE OF SIMPLE ACYCLIC POLYAMINES FOR THE TREATMENT OF DISEASES CAUSED BY PARASITES OF THE GENUS LEISHMANIA
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申请号: US18004932申请日: 2021-07-09
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公开(公告)号: US20230346769A1公开(公告)日: 2023-11-02
- 发明人: Enrique Gargía-España Monsonís , María Paz Clares García , Estefanía Delgado Pinar , Clotilde Marín Sánchez , Manuel Sánchez Moreno , Rubén Martín Escolano , Álvaro Martín Montes
- 申请人: Universidad De Granada , Universitat De València
- 申请人地址: ES Granada
- 专利权人: Universidad De Granada,Universitat De València
- 当前专利权人: Universidad De Granada,Universitat De València
- 当前专利权人地址: ES Granada; ES Valencia
- 优先权: ES 02030713 2020.07.10
- 国际申请: PCT/ES2021/070503 2021.07.09
- 进入国家日期: 2023-01-10
- 主分类号: A61K31/4406
- IPC分类号: A61K31/4406 ; A61K31/4409 ; A61P33/02 ; A61K31/47 ; A61K31/4402 ; A61K45/06
摘要:
Use of simple acyclic polyamines for the treatment of parasites of the family Trypanosomatidae
The present invention provides the use of certain single acyclic polyamines of Formula (I), attached to heterocycles, for the treatment of leishmaniasis and trypanosomiasis. All the compounds studied show antiparasitic activity against Leishmania species, comparable or superior to that of the active ingredient of the drug commonly used to treat this disease, but with a macrophage toxicity similar to or, in most cases, lower than that of the commercial reference compound, and with higher selectivity indices against strains representative of the three clinical forms of the disease: cutaneous, mucocutaneous and visceral. The compounds show ability to inhibit parasite superoxide dismutase, generally at concentrations lower than those required to inhibit human superoxide dismutase. All this supports its usefulness for treating leishmaniasis and also trypanosomiasis.
The present invention provides the use of certain single acyclic polyamines of Formula (I), attached to heterocycles, for the treatment of leishmaniasis and trypanosomiasis. All the compounds studied show antiparasitic activity against Leishmania species, comparable or superior to that of the active ingredient of the drug commonly used to treat this disease, but with a macrophage toxicity similar to or, in most cases, lower than that of the commercial reference compound, and with higher selectivity indices against strains representative of the three clinical forms of the disease: cutaneous, mucocutaneous and visceral. The compounds show ability to inhibit parasite superoxide dismutase, generally at concentrations lower than those required to inhibit human superoxide dismutase. All this supports its usefulness for treating leishmaniasis and also trypanosomiasis.
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