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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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    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
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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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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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Family Applications (1)

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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) CN111349053A (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) MX378266B (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 (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6642948B2 (ja) * 2014-10-06 2020-02-12 コーテクシーミー， インコーポレイテッド リシンジンジパインの阻害剤
WO2017083433A1 (en) 2015-11-09 2017-05-18 Cortexyme, Inc. Inhibitors of arginine gingipain
WO2017201322A1 (en) * 2016-05-19 2017-11-23 Cortexyme, Inc. Treatment of osteoarthritis with gingipain blocking agents
DK3512846T3 (da) * 2016-09-16 2024-11-11 Lighthouse Pharmaceuticals Inc Ketonhæmmere af lysin-gingipain
JP7079794B2 (ja) * 2017-05-10 2022-06-02 コーテクシーミー， インコーポレイテッド アミノピリジン化合物ならびにその調製および使用のための方法
US20210355527A1 (en) * 2018-09-27 2021-11-18 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
KR102779135B1 (ko) * 2023-06-19 2025-03-12 한국과학기술연구원 신규한 형광 화합물 및 이를 이용한 진지페인 검출용 조성물, 포르피로모나스 진지발리스 감염 진단용 조성물 또는 포르피로모나스 진지발리스에 대한 항균용 조성물

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU600226B2 (en) 1985-02-04 1990-08-09 Merrell Pharmaceuticals Inc. Novel 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
WO1993000926A1 (en) 1991-07-02 1993-01-21 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
AU4250596A (en) 1994-12-22 1996-07-10 Biochem Pharma Inc. Low molecular weight bicyclic thrombin inhibitors
WO1996030396A1 (en) 1995-03-24 1996-10-03 Molecumetics Ltd. β-SHEET MIMETICS AND USE THEREOF AS PROTEASE INHIBITORS
AU712581B2 (en) 1995-03-24 1999-11-11 Molecumetics, Ltd. Beta-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins
GB9510264D0 (en) 1995-05-22 1995-07-19 Iaf Biochem Int Low molecular weight bicyclic-urea type thrombin inhibitors
US5827866A (en) 1995-06-07 1998-10-27 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
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
IL119466A (en) * 1995-11-03 2001-08-26 Akzo Nobel Nv Thrombin inhibitors, their preparation and pharmaceutical compositions containing them
WO1998005333A1 (en) 1996-08-05 1998-02-12 Molecumetics Ltd. Use of beta-sheet mimetics as protease and kinase inhibitors and as inhibitors of transcription factors
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
ES2192764T3 (es) 1998-02-12 2003-10-16 Molecumetics Ltd Mimeticos de lamina beta y metodos relacionados con el uso de los mismos.
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
BR0007778A (pt) * 1999-01-27 2002-06-04 Ortho Mcneil Pharm Inc Peptidila cetonas heterocìclicas úteis como inibidores de triptase
CA2367348A1 (en) 1999-03-15 2000-09-21 Axys Pharmaceuticals, Inc. Novel 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
EP1799244A4 (en) 2004-07-23 2010-06-09 Smith Judith INHIBITORS OF FURINE
WO2007137080A2 (en) * 2006-05-23 2007-11-29 Irm Llc Compounds and compositions as channel activating protease inhibitors
WO2009103432A2 (en) * 2008-02-21 2009-08-27 Sanofi-Aventis Covalently binding imaging probes
US9724351B2 (en) * 2012-08-23 2017-08-08 Alios Biopharma, Inc. Compounds for the treatment of paramoxyvirus viral infections
ES2938225T3 (es) 2013-03-15 2023-04-05 Univ Leland Stanford Junior Compuestos de sondas basadas en la actividad, composiciones y métodos de uso
JP6642948B2 (ja) * 2014-10-06 2020-02-12 コーテクシーミー， インコーポレイテッド リシンジンジパインの阻害剤

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