CO2017003321A2 - Inhibidores de gingipaina de lisina - Google Patents

Inhibidores de gingipaina de lisina

Info

Publication number
CO2017003321A2
CO2017003321A2 CONC2017/0003321A CO2017003321A CO2017003321A2 CO 2017003321 A2 CO2017003321 A2 CO 2017003321A2 CO 2017003321 A CO2017003321 A CO 2017003321A CO 2017003321 A2 CO2017003321 A2 CO 2017003321A2
Authority
CO
Colombia
Prior art keywords
lysine gingipain
lysine
gingipain inhibitors
gingivalis
inhibitors
Prior art date
Application number
CONC2017/0003321A
Other languages
English (en)
Inventor
Andrei Konradi
Stephen S Dominy
Lynch Casey Crawford
Craig Coburn
Joseph VACCA
Original Assignee
Cortexyme Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Cortexyme Inc filed Critical Cortexyme Inc
Publication of CO2017003321A2 publication Critical patent/CO2017003321A2/es

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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/164—Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
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    • A61K31/33—Heterocyclic compounds
    • 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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    • A61K31/41—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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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/62—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
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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
    • C07D213/24—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 with substituted hydrocarbon radicals attached to ring carbon atoms
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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
    • C07D213/24—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 with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
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  • Chemical & Material Sciences (AREA)
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Abstract

La presente invención se refiere generalmente a agentes terapéuticos dirigidos a la bacteria Porphyromonas gingivalis, incluyendo su proteasa gingipaína de lisina (Kgp), y su uso para el tratamiento de trastornos asociados con la infección por P. gingivalis, incluyendo trastornos cerebrales tales como la enfermedad de Alzheimer. En ciertas realizaciones, la invención proporciona compuestos de acuerdo con la Fórmula I, como se describe en la presente memoria, y sales farmacéuticamente aceptables de los mismos.
CONC2017/0003321A 2014-10-06 2017-04-05 Inhibidores de gingipaina de lisina CO2017003321A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462060483P 2014-10-06 2014-10-06
PCT/US2015/054050 WO2016057413A2 (en) 2014-10-06 2015-10-05 Inhibitors of lysine gingipain

Publications (1)

Publication Number Publication Date
CO2017003321A2 true CO2017003321A2 (es) 2017-07-28

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CONC2017/0003321A CO2017003321A2 (es) 2014-10-06 2017-04-05 Inhibidores de gingipaina de lisina

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US (5) US9758473B2 (es)
EP (1) EP3204352B1 (es)
JP (1) JP6642948B2 (es)
KR (1) KR20170068521A (es)
CN (2) CN107108468B (es)
AU (1) AU2015328385B2 (es)
BR (1) BR112017006920A8 (es)
CA (1) CA2963305A1 (es)
CL (1) CL2017000845A1 (es)
CO (1) CO2017003321A2 (es)
CY (1) CY1123532T1 (es)
DK (1) DK3204352T3 (es)
ES (1) ES2819218T3 (es)
HR (1) HRP20201473T1 (es)
HU (1) HUE050876T2 (es)
IL (2) IL251501B (es)
MX (1) MX2017004569A (es)
PE (1) PE20171335A1 (es)
PH (1) PH12017500637A1 (es)
PL (1) PL3204352T3 (es)
PT (1) PT3204352T (es)
RU (1) RU2728785C2 (es)
SG (1) SG11201702797RA (es)
WO (1) WO2016057413A2 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2728785C2 (ru) 2014-10-06 2020-07-31 Кортексим, Инк. Ингибиторы лизинспецифичного гингипаина
EP3374352A4 (en) 2015-11-09 2019-10-02 Cortexyme, Inc. GINGIPAINE ARGININE INHIBITORS
WO2017201322A1 (en) * 2016-05-19 2017-11-23 Cortexyme, Inc. Treatment of osteoarthritis with gingipain blocking agents
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
WO2020069397A1 (en) * 2018-09-27 2020-04-02 Cortexyme, Inc. Methods for detection of microbial nucleic acids in body fluids
CA3200407A1 (en) * 2020-11-03 2022-05-12 Keystone Bio, Inc. Antigen-binding molecules that bind to porphyromonas gingivalis

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1341029C (en) * 1985-02-04 2000-06-20 Michael Kolb Peptidase inhibitors
US5055451A (en) 1986-12-22 1991-10-08 Syntex Inc. Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors
JPH01163162A (ja) * 1987-12-18 1989-06-27 Showa Denko Kk アミノ酸誘導体および酵素阻害剤
US5451410A (en) * 1993-04-22 1995-09-19 Emisphere Technologies, Inc. Modified amino acids for encapsulating active agents
GB9019558D0 (en) 1990-09-07 1990-10-24 Szelke Michael Enzyme inhibitors
AU2299592A (en) 1991-07-02 1993-02-11 Children's Medical Center Corporation Treatment of periodontal disease with protease inhibitors
SE9102462D0 (sv) 1991-08-28 1991-08-28 Astra Ab New isosteric peptides
US5374623A (en) 1992-08-20 1994-12-20 Prototek, Inc. Cysteine protease inhibitors effective for in vivo use
EE9700113A (et) 1994-12-22 1997-12-15 Biochem Pharma Inc. Madala molekulmassiga bitsüklilised trombiini inhibiitorid
CA2215720A1 (en) 1995-03-24 1996-10-03 Molecumetics, Ltd. .beta.-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins
WO1996030396A1 (en) 1995-03-24 1996-10-03 Molecumetics Ltd. β-SHEET MIMETICS AND USE THEREOF AS PROTEASE INHIBITORS
GB9510264D0 (en) 1995-05-22 1995-07-19 Iaf Biochem Int Low molecular weight bicyclic-urea type thrombin inhibitors
US5523308A (en) 1995-06-07 1996-06-04 Costanzo; Michael J. Peptidyl heterocycles useful in the treatment of thrombin related disorders
US5827860A (en) 1995-06-07 1998-10-27 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
US5827866A (en) 1995-06-07 1998-10-27 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
IL119466A (en) * 1995-11-03 2001-08-26 Akzo Nobel Nv Thrombin inhibitors, their preparation and pharmaceutical compositions containing them
KR20000029838A (ko) 1996-08-05 2000-05-25 몰레큐메틱스 리미티드 프로테아제및키나제억제제로서그리고전사인자억제제로서의베타-시트유사체의용도
AU4172397A (en) 1996-09-06 1998-03-26 Biochem Pharma Inc. Lactam inhibitors of thrombin
AU1176299A (en) 1997-11-26 1999-06-15 Yoshitomi Pharmaceutical Industries, Ltd. Tryptase inhibitors comprising heterocyclic amide compounds
DE69810513T2 (de) 1998-02-12 2004-03-18 Molecumetics, Ltd., Bellevue Mimetika von beta-faltblatt und verfahren zur verwendung davon
US6323219B1 (en) 1998-04-02 2001-11-27 Ortho-Mcneil Pharmaceutical, Inc. Methods for treating immunomediated inflammatory disorders
US7053056B2 (en) * 1998-07-02 2006-05-30 Idun Pharmaceuticals, Inc. C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
AU2847200A (en) * 1999-01-27 2000-08-18 G.D. Searle & Co. Novel hydroxyamidino carboxylate derivatives useful as nitric oxide synthase inhibitors
TR200102766T2 (tr) * 1999-01-27 2001-12-21 Ortho-Mcneil Pharmaceutical, Inc. Triptaz inhibitörü olarak kullanılan peptidil heterosiklik ketonlar
US6506733B1 (en) 1999-03-15 2003-01-14 Axys Pharmaceuticals, Inc. Compounds and compositions as protease inhibitors
US6790989B2 (en) * 2000-01-13 2004-09-14 Idun Pharmaceuticals, Inc. Inhibitors of the ICE/ced-3 family of cysteine proteases
US7205384B2 (en) 2003-08-05 2007-04-17 Ortho-Mcneil Pharmaceutical Inc. Process for preparing peptidyl heterocyclic ketone derivatives
US8263563B2 (en) 2004-07-23 2012-09-11 Robert E. Smith Furin inhibitors
US7951823B2 (en) 2006-05-23 2011-05-31 Irm Llc Compounds and compositions as channel activating protease inhibitors
EP2262783A2 (en) * 2008-02-21 2010-12-22 Sanofi-Aventis Covalently binding imaging probes
NZ704666A (en) * 2012-08-23 2018-05-25 Alios Biopharma Inc Compounds for the treatment of paramoxyvirus viral infections
EP4218829A3 (en) 2013-03-15 2023-08-16 The Board of Trustees of the Leland Stanford Junior University Activity-based probe compounds, compositions, and methods of use
RU2728785C2 (ru) * 2014-10-06 2020-07-31 Кортексим, Инк. Ингибиторы лизинспецифичного гингипаина

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