WO2016195194A3 - Novel tlr2 antagonists - Google Patents

Novel tlr2 antagonists 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
French (fr)
Korean (ko)
Other versions
WO2016195194A2 (en
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/en
Application filed by 아주대학교산학협력단 filed Critical 아주대학교산학협력단
Priority to EP15894366.2A priority Critical patent/EP3305767B1/en
Priority to US15/578,086 priority patent/US10308655B2/en
Publication of WO2016195194A2 publication Critical patent/WO2016195194A2/en
Publication of WO2016195194A3 publication Critical patent/WO2016195194A3/en

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

The present invention relates to TLR2 antagonists, which are small novel molecules, and, particularly, to: 19 novel TLR2 antagonists; a pharmaceutical composition, containing the antagonists, for preventing or treating inflammatory diseases; and a TLR4 modulator, containing the antagonists. The novel TLR2 antagonists according to the present invention can be effectively used as a preparation for oral administration by having low molecular weight and high oral bioavailability, and can be useful in pharmaceutical compositions for preventing or treating inflammatory diseases since the secretion of IL-8 is effectively inhibited and in vivo cytotoxicity is not induced. In addition, the novel TLR2 antagonists according to the present invention can be used as a TLR4 modulator.
PCT/KR2015/014202 2015-05-29 2015-12-23 Novel tlr2 antagonists WO2016195194A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP15894366.2A EP3305767B1 (en) 2015-05-29 2015-12-23 Novel tlr2 antagonists for treating inflammatory diseases
US15/578,086 US10308655B2 (en) 2015-05-29 2015-12-23 Method of treating Crohn's disease comprising a TLR2 antagonist

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
KR20150076217 2015-05-29
KR10-2015-0076217 2015-05-29
KR10-2015-0175045 2015-12-09
KR1020150175045A KR101745524B1 (en) 2015-05-29 2015-12-09 Novel TLR2 antagonists

Publications (2)

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

Family

ID=57440661

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2015/014202 WO2016195194A2 (en) 2015-05-29 2015-12-23 Novel tlr2 antagonists

Country Status (1)

Country Link
WO (1) WO2016195194A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11807622B2 (en) 2019-01-30 2023-11-07 Insilico Medicine Ip Limited TLR 9 inhibitors
US10689360B1 (en) 2019-01-30 2020-06-23 Insilico Medicine Ip Limited TLR 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 (en) * 2007-08-03 2009-02-12 Opsona Therapeutics Limited Composition and method for treatment of reperfusion injury and tissue damage
KR20110071108A (en) * 2008-10-06 2011-06-28 이데라 파마슈티칼즈, 인코포레이티드 Use of inhibitors of toll-like receptors in the prevention and treatment of hypercholesterolemia and hyperlipidemia and diseases related thereto
KR20110081336A (en) * 2008-11-04 2011-07-13 이데라 파마슈티칼즈, 인코포레이티드 Modulation of toll-like receptor 2 expression by antisense oligonucleotides

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 (en) * 2007-08-03 2009-02-12 Opsona Therapeutics Limited Composition and method for treatment of reperfusion injury and tissue damage
KR20110071108A (en) * 2008-10-06 2011-06-28 이데라 파마슈티칼즈, 인코포레이티드 Use of inhibitors of toll-like receptors in the prevention and treatment of hypercholesterolemia and hyperlipidemia and diseases related thereto
KR20110081336A (en) * 2008-11-04 2011-07-13 이데라 파마슈티칼즈, 인코포레이티드 Modulation of toll-like receptor 2 expression by antisense oligonucleotides

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 (en) 2016-12-08

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