WO2016195194A3 - Nouveaux antagonistes de tlr2 - Google Patents

Nouveaux antagonistes de tlr2 Download PDF

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Publication number
WO2016195194A3
WO2016195194A3 PCT/KR2015/014202 KR2015014202W WO2016195194A3 WO 2016195194 A3 WO2016195194 A3 WO 2016195194A3 KR 2015014202 W KR2015014202 W KR 2015014202W WO 2016195194 A3 WO2016195194 A3 WO 2016195194A3
Authority
WO
WIPO (PCT)
Prior art keywords
antagonists
novel
present
tlr2 antagonists
tlr2
Prior art date
Application number
PCT/KR2015/014202
Other languages
English (en)
Korean (ko)
Other versions
WO2016195194A2 (fr
Inventor
최상돈
듀라이프라산나벤카테시
아첵아스마
Original Assignee
아주대학교산학협력단
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
Priority claimed from KR1020150175045A external-priority patent/KR101745524B1/ko
Application filed by 아주대학교산학협력단 filed Critical 아주대학교산학협력단
Priority to US15/578,086 priority Critical patent/US10308655B2/en
Priority to EP15894366.2A priority patent/EP3305767B1/fr
Publication of WO2016195194A2 publication Critical patent/WO2016195194A2/fr
Publication of WO2016195194A3 publication Critical patent/WO2016195194A3/fr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings

Abstract

La présente invention concerne des antagonistes de TLR2, qui sont de nouvelles petites molécules et, en particulier : 19 nouveaux antagonistes de TLR2 ; une composition pharmaceutique, contenant les antagonistes, pour prévenir ou traiter des maladies inflammatoires ; et un modulateur de TLR4 contenant les antagonistes. Les nouveaux antagonistes de TLR2 selon la présente invention peuvent être efficacement utilisés en tant que préparation pour administration orale car ils ont un faible poids moléculaire et une biodisponibilité orale élevée, et ils peuvent être utiles dans des compositions pharmaceutiques pour prévenir ou traiter des maladies inflammatoires du fait que la sécrétion d'IL-8 est efficacement inhibée et qu'aucune cytotoxicité in vivo n'est induite. De plus, les nouveaux antagonistes de TLR2 selon la présente invention peuvent être utilisés en tant que modulateur de TLR4.
PCT/KR2015/014202 2015-05-29 2015-12-23 Nouveaux antagonistes de tlr2 WO2016195194A2 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
US15/578,086 US10308655B2 (en) 2015-05-29 2015-12-23 Method of treating Crohn's disease comprising a TLR2 antagonist
EP15894366.2A EP3305767B1 (fr) 2015-05-29 2015-12-23 Nouveaux antagonistes de tlr2 pour le traitement des maladies inflammatoires

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
KR10-2015-0076217 2015-05-29
KR20150076217 2015-05-29
KR10-2015-0175045 2015-12-09
KR1020150175045A KR101745524B1 (ko) 2015-05-29 2015-12-09 신규한 tlr2 길항제

Publications (2)

Publication Number Publication Date
WO2016195194A2 WO2016195194A2 (fr) 2016-12-08
WO2016195194A3 true WO2016195194A3 (fr) 2017-01-26

Family

ID=57440661

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2015/014202 WO2016195194A2 (fr) 2015-05-29 2015-12-23 Nouveaux antagonistes de tlr2

Country Status (1)

Country Link
WO (1) WO2016195194A2 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10689360B1 (en) 2019-01-30 2020-06-23 Insilico Medicine Ip Limited TLR inhibitors
US11807622B2 (en) 2019-01-30 2023-11-07 Insilico Medicine Ip Limited TLR 9 inhibitors
US11008303B2 (en) 2019-01-30 2021-05-18 Insilico Medicine Ip Limited TLR 9 inhibitors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070167409A1 (en) * 2003-10-24 2007-07-19 Eisai Co., Ltd. Compounds and Methods for Treating Toll-Like Receptor 2-Related Diseases and Conditions
WO2009019260A2 (fr) * 2007-08-03 2009-02-12 Opsona Therapeutics Limited Composition et procédé pour le traitement d'une lésion de reperfusion et d'un dommage tissulaire
KR20110071108A (ko) * 2008-10-06 2011-06-28 이데라 파마슈티칼즈, 인코포레이티드 고콜레스테롤혈증 및 고지혈증 및 이에 관련된 질병의 예방 및 치료에서 톨-유사 수용체의 저해제의 용도
KR20110081336A (ko) * 2008-11-04 2011-07-13 이데라 파마슈티칼즈, 인코포레이티드 안티센스 올리고누클레오티드에 의한 ｔｏｌｌ―유사 수용체 2 발현의 조절

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070167409A1 (en) * 2003-10-24 2007-07-19 Eisai Co., Ltd. Compounds and Methods for Treating Toll-Like Receptor 2-Related Diseases and Conditions
WO2009019260A2 (fr) * 2007-08-03 2009-02-12 Opsona Therapeutics Limited Composition et procédé pour le traitement d'une lésion de reperfusion et d'un dommage tissulaire
KR20110071108A (ko) * 2008-10-06 2011-06-28 이데라 파마슈티칼즈, 인코포레이티드 고콜레스테롤혈증 및 고지혈증 및 이에 관련된 질병의 예방 및 치료에서 톨-유사 수용체의 저해제의 용도
KR20110081336A (ko) * 2008-11-04 2011-07-13 이데라 파마슈티칼즈, 인코포레이티드 안티센스 올리고누클레오티드에 의한 ｔｏｌｌ―유사 수용체 2 발현의 조절

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE Chemical Abstract XP055467834, retrieved from STN Database accession no. 1147401-24-8 *

Also Published As

Publication number Publication date
WO2016195194A2 (fr) 2016-12-08

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