MX368072B - Derivados de [1,2,4]-triazolo-[1,5-a]-pirimidina como inhibidores del proteasoma de protozoarios para el tratamiento de enfermedades parasitarias tales como leishmaniasis. - Google Patents
Derivados de [1,2,4]-triazolo-[1,5-a]-pirimidina como inhibidores del proteasoma de protozoarios para el tratamiento de enfermedades parasitarias tales como leishmaniasis.Info
- Publication number
- MX368072B MX368072B MX2016008079A MX2016008079A MX368072B MX 368072 B MX368072 B MX 368072B MX 2016008079 A MX2016008079 A MX 2016008079A MX 2016008079 A MX2016008079 A MX 2016008079A MX 368072 B MX368072 B MX 368072B
- Authority
- MX
- Mexico
- Prior art keywords
- leishmaniasis
- protozoan
- triazolo
- treatment
- pyrimidine derivatives
- Prior art date
Links
- 208000004554 Leishmaniasis Diseases 0.000 title abstract 2
- 208000030852 Parasitic disease Diseases 0.000 title 1
- 229940079156 Proteasome inhibitor Drugs 0.000 title 1
- SRNKZYRMFBGSGE-UHFFFAOYSA-N [1,2,4]triazolo[1,5-a]pyrimidine Chemical class N1=CC=CN2N=CN=C21 SRNKZYRMFBGSGE-UHFFFAOYSA-N 0.000 title 1
- 239000003207 proteasome inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 206010001935 American trypanosomiasis Diseases 0.000 abstract 1
- 208000024699 Chagas disease Diseases 0.000 abstract 1
- 241000223109 Trypanosoma cruzi Species 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000029080 human African trypanosomiasis Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 244000045947 parasite Species 0.000 abstract 1
- 230000007170 pathology Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/695—Silicon compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/027—Organoboranes and organoborohydrides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
- C07F7/0814—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring said ring is substituted at a C ring atom by Si
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invención proporciona los compuestos de la fórmula A: (ver Fórmula) o una sal farmacéuticamente aceptable, tautómero, o estereoisómero del mismo, en donde las variables son como se definen en la presente. La presente invención proporciona además composiciones farmacéuticas que comprenden estos compuestos, y los métodos para utilizar tales compuestos con el fin de tratar, prevenir, inhibir, mitigar o erradicar la patología y/o sintomatología de una enfermedad causada por un parásito, tal como leishmaniasis, tripanosomiasis africana humana y la enfermedad de Chagas.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361918089P | 2013-12-19 | 2013-12-19 | |
| PCT/US2014/071077 WO2015095477A1 (en) | 2013-12-19 | 2014-12-18 | [1,2,4]triazolo[1,5-a]pyrimidine derivatives as protozoan proteasome inhibitors for the treatment of parasitic diseases such as leishmaniasis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2016008079A MX2016008079A (es) | 2016-09-16 |
| MX368072B true MX368072B (es) | 2019-09-18 |
Family
ID=52302387
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2016008079A MX368072B (es) | 2013-12-19 | 2014-12-18 | Derivados de [1,2,4]-triazolo-[1,5-a]-pirimidina como inhibidores del proteasoma de protozoarios para el tratamiento de enfermedades parasitarias tales como leishmaniasis. |
Country Status (41)
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR104749A1 (es) * | 2015-05-29 | 2017-08-09 | Glaxosmithkline Ip Dev Ltd | Imidazo[1,2-b][1,2,4]triazina sustituida, composición farmacéutica y combinación que lo comprenden, y su uso para la fabricación de un medicamento |
| ES2856899T3 (es) * | 2015-08-07 | 2021-09-28 | Glaxosmithkline Ip Dev Ltd | Compuestos |
| WO2017127627A1 (en) | 2016-01-21 | 2017-07-27 | The University Of North Carolina At Chapel Hill | Compounds for treatment of trypanosomes and neurological pathogens and uses thereof |
| WO2018176134A1 (en) | 2017-03-27 | 2018-10-04 | HYDRO-QUéBEC | Salts for use in electrolyte compositions or as electrode additives |
| JOP20190278A1 (ar) * | 2017-05-31 | 2019-11-28 | Novartis Ag | مركبات 5، 6-ثنائية الحلقة مندمجة وتركيبات لعلاج الأمراض الطفيلية |
| EA039324B1 (ru) * | 2017-11-06 | 2022-01-13 | Новартис Аг | 5,6–конденсированные бициклические соединения и композиции для лечения паразитарных заболеваний |
| TW202028208A (zh) * | 2018-10-09 | 2020-08-01 | 瑞士商諾華公司 | N-(4-氟-3-(6-(3-甲基吡啶-2-基)-[1,2,4]三唑并[1,5-a]嘧啶-2-基)苯基)-2,4-二甲基㗁唑-5-甲醯胺固體形式 |
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| TW201406736A (zh) | 2012-06-28 | 2014-02-16 | Fujifilm Corp | 新穎的醯胺衍生物或其鹽 |
| CN103570625A (zh) | 2012-07-19 | 2014-02-12 | 南京英派药业有限公司 | N-(3-杂芳基芳基)-4-芳基芳基甲酰胺和类似物作为Hedgehog通路抑制剂及其应用 |
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| US9296754B2 (en) | 2013-03-15 | 2016-03-29 | Novartis Ag | Compounds and compositions for the treatment of parasitic diseases |
| WO2014151729A1 (en) | 2013-03-15 | 2014-09-25 | Irm Llc | Compounds and compositions for the treatment of parasitic diseases |
| UY35400A (es) * | 2013-03-15 | 2014-10-31 | Novartis Ag | Compuestos y composiciones para el tratamiento de enfermedades parasitarias |
| US9233961B2 (en) | 2013-03-15 | 2016-01-12 | Novartis Ag | Compounds and compositions for the treatment of parasitic diseases |
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