PE20190473A1 - Inhibidores cetonicos de gingipain de lisina - Google Patents
Inhibidores cetonicos de gingipain de lisinaInfo
- Publication number
- PE20190473A1 PE20190473A1 PE2019000533A PE2019000533A PE20190473A1 PE 20190473 A1 PE20190473 A1 PE 20190473A1 PE 2019000533 A PE2019000533 A PE 2019000533A PE 2019000533 A PE2019000533 A PE 2019000533A PE 20190473 A1 PE20190473 A1 PE 20190473A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- kingon
- lisina
- ketonic
- inhibitors
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 241000605862 Porphyromonas gingivalis Species 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 102000005600 Cathepsins Human genes 0.000 abstract 1
- 108010084457 Cathepsins Proteins 0.000 abstract 1
- 108091020100 Gingipain Cysteine Endopeptidases Proteins 0.000 abstract 1
- 208000037273 Pathologic Processes Diseases 0.000 abstract 1
- 108091005804 Peptidases Proteins 0.000 abstract 1
- 102000035195 Peptidases Human genes 0.000 abstract 1
- 239000004365 Protease Substances 0.000 abstract 1
- 125000006242 amine protecting group Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 230000002458 infectious effect Effects 0.000 abstract 1
- 230000009054 pathological process Effects 0.000 abstract 1
- 230000003389 potentiating effect Effects 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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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- 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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- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
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- C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C235/10—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
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- C07C235/50—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
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- C07C245/08—Azo compounds, i.e. compounds having the free valencies of —N=N— groups attached to different atoms, e.g. diazohydroxides with nitrogen atoms of azo groups bound to carbon atoms of six-membered aromatic rings with the two nitrogen atoms of azo groups bound to carbon atoms of six-membered aromatic rings, e.g. azobenzene
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- C07C323/39—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
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- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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Abstract
Se refiere a un compuesto de formula (I), donde A se selecciona del grupo integrado por -CH2- y -O- ; R1a y R1B se seleccionan, cada uno de manera independiente, del grupo integrado por H, alquilo C1-C4 y un grupo protector de aminas; R2a y R2B pueden ser H, halogeno, haloalquilo C1-C4 y haloalcoxi C1-C4; R3 puede ser cicloalquilo C3-C8, alquilo C3-C8, heterociclilo de 3 a 12 miembros, entre otros; R4 puede ser H y alquilo C1-C4; R5 puede ser haloalquilo C1-C6, entre otros. Dicho compuesto presenta una actividad potente para inhibir la gingipaina de lisina (Kgp) de P. gingivalis que presentan selectividad incrementada por Kgp respecto de proteasas endogenas tales como las catepsinas, y es util en el tratamiento de la enfermedad de Alzheimer, asi como procesos patologicos e infecciosos asociados a P. gingivalis.
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US201662395938P | 2016-09-16 | 2016-09-16 | |
US201762459456P | 2017-02-15 | 2017-02-15 |
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PE2019000533A PE20190473A1 (es) | 2016-09-16 | 2017-09-15 | Inhibidores cetonicos de gingipain de lisina |
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US (3) | US10730826B2 (es) |
EP (1) | EP3512846A4 (es) |
JP (1) | JP7113815B2 (es) |
KR (1) | KR20190072530A (es) |
CN (1) | CN109983012B (es) |
AU (2) | AU2017326466B2 (es) |
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CA (1) | CA3036862A1 (es) |
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AU2017326466B2 (en) | 2016-09-16 | 2021-11-11 | Lighthouse Pharmaceuticals, Inc. | Ketone inhibitors of lysine gingipain |
EP3621613A4 (en) | 2017-05-10 | 2020-12-02 | Cortexyme, Inc. | AMINOPYRIDINE COMPOUNDS AND METHODS FOR THEIR PREPARATION AND USE |
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PH12019500570A1 (en) | 2019-08-05 |
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