CO2019002950A2 - Inhibidores cetónicos de gingipain de lisina. - Google Patents
Inhibidores cetónicos de gingipain de lisina.Info
- Publication number
- CO2019002950A2 CO2019002950A2 CONC2019/0002950A CO2019002950A CO2019002950A2 CO 2019002950 A2 CO2019002950 A2 CO 2019002950A2 CO 2019002950 A CO2019002950 A CO 2019002950A CO 2019002950 A2 CO2019002950 A2 CO 2019002950A2
- Authority
- CO
- Colombia
- Prior art keywords
- gingipain
- lysine gingipain
- lysine
- methods
- well
- Prior art date
Links
- 108091020100 Gingipain Cysteine Endopeptidases Proteins 0.000 title abstract 4
- 239000003112 inhibitor Substances 0.000 title 1
- 150000002576 ketones Chemical class 0.000 title 1
- 241000605862 Porphyromonas gingivalis Species 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 208000014644 Brain disease Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 239000000523 sample Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
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- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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Abstract
La presente invención proporciona compuestos de acuerdo con la Fórmula I como se describe en la presente, y su uso para inhibir la proteasa de gingipaina de lisina (Kgp) de la bacteria Porphyromonas gingivalis. Asimismo, se describen compuestos de sondas con actividad de las gingipainas, así como se describen métodos para ensayar la actividad de las gingipainas, así como métodos para el tratamiento de trastornos asociados a infección por P. gingivalis, que incluyen trastornos cerebrales tales como enfermedad de Alzheimer.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US201662395938P | 2016-09-16 | 2016-09-16 | |
US201762459456P | 2017-02-15 | 2017-02-15 | |
PCT/US2017/051912 WO2018053353A1 (en) | 2016-09-16 | 2017-09-15 | Ketone inhibitors of lysine gingipain |
Publications (1)
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CO2019002950A2 true CO2019002950A2 (es) | 2019-05-31 |
Family
ID=61618978
Family Applications (1)
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CONC2019/0002950A CO2019002950A2 (es) | 2016-09-16 | 2019-03-27 | Inhibidores cetónicos de gingipain de lisina. |
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EP (1) | EP3512846B1 (es) |
JP (1) | JP7113815B2 (es) |
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CN (1) | CN109983012B (es) |
AU (2) | AU2017326466B2 (es) |
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TW (1) | TWI787202B (es) |
WO (1) | WO2018053353A1 (es) |
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Publication number | Priority date | Publication date | Assignee | Title |
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BR112019004864A8 (pt) | 2016-09-16 | 2023-03-07 | Cortexyme Inc | Inibidores cetona de lisina gingipain |
CN110944637A (zh) | 2017-05-10 | 2020-03-31 | 库特克希米公司 | 氨基吡啶化合物及其制备方法和使用方法 |
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