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PE20160901A1 - Reguladores de nrf2 - Google Patents

Reguladores de nrf2

Info

Publication number
PE20160901A1
PE20160901A1 PE2016000789A PE2016000789A PE20160901A1 PE 20160901 A1 PE20160901 A1 PE 20160901A1 PE 2016000789 A PE2016000789 A PE 2016000789A PE 2016000789 A PE2016000789 A PE 2016000789A PE 20160901 A1 PE20160901 A1 PE 20160901A1
Authority
PE
Peru
Prior art keywords
methyl
phenyl
hydrogen
compounds
thiadiazepin
Prior art date
Application number
PE2016000789A
Other languages
English (en)
Inventor
Jeffrey Charles Boehm
Thomas Glanmor Davies
Roderick S Davis
Charlotte Mary Griffiths-Jones
Thomas Daniel Heightman
Hongxing Yan
Tindy Li
David Norton
Gordon Saxty
Hendrika Maria Gerarda Willems
Alison Jo-Anne Woolford
Jeffrey K Kerns
Original Assignee
Astex Therapeutics Ltd
Glaxosmithkline Ip Dev Ltd
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 Astex Therapeutics Ltd, Glaxosmithkline Ip Dev Ltd filed Critical Astex Therapeutics Ltd
Publication of PE20160901A1 publication Critical patent/PE20160901A1/es

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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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Abstract

La presente invencion se refiere a compuestos analogos de bis arilo de formula (I) donde A es –C(O)OR1 o tetrazolilo; R1 es hidrogeno, -CH2C(O)N(R7)2, entre otros; R2 es –(CH2)n-fenilo, benzotriazolilo, –(CH2)n-triazolilo, entre otros; n es 0-3; R3 es R4-SO2-N(R6)-; R4 es fenilo, tienilo, entre otros; R5 es hidrogeno, -F, entre otros; R8 es hidrogeno, -NH2, entre otros; R12 es hidrogeno. Son compuestos preferidos: acido 3-(7-metoxi-1-metil-1H-benzo[d][1,2,3]triazol-5-il)-3-(4-metil-3-((5-metil-1,1-dioxido-4,5-dihidrobenzo[f][1,2,5]tiadiazepin-2(3H)-il)metil)fenil)propanoico; acido 3-(1,4-dimetil-1H-benzo[d][1,2,3]triazol-5-il)-3-(4-metil-3-((5-metil-1,1-dioxido-4,5-dihidrobenzo[f][1,2,5]tiadiazepin-2(3H)-il)metil)fenil)propanoico; entre otros. Dichos compuestos son reguladores de Nrf2 (factor 2 relacionado con NF-E2), siendo utiles en el tratamiento de trastornos respiratorios y no respiratorios como enfermedad obstructiva cronica (COPD), asma, entre otros.
PE2016000789A 2013-12-18 2014-12-17 Reguladores de nrf2 PE20160901A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361917466P 2013-12-18 2013-12-18
US201461980091P 2014-04-16 2014-04-16

Publications (1)

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PE20160901A1 true PE20160901A1 (es) 2016-08-27

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US (2) US10144731B2 (es)
EP (1) EP3083614B1 (es)
JP (1) JP6630671B2 (es)
KR (1) KR102301867B1 (es)
CN (1) CN105829305B (es)
AU (2) AU2014369153B2 (es)
BR (1) BR112016014180A2 (es)
CA (1) CA2934216C (es)
CL (1) CL2016001516A1 (es)
CR (1) CR20160272A (es)
DO (1) DOP2016000145A (es)
EA (1) EA030431B1 (es)
ES (1) ES2784244T3 (es)
IL (1) IL245727B (es)
MX (1) MX370410B (es)
PE (1) PE20160901A1 (es)
PH (1) PH12016501151A1 (es)
SG (1) SG11201604611SA (es)
WO (1) WO2015092713A1 (es)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI3782996T3 (fi) * 2015-06-15 2024-06-26 Glaxosmithkline Ip Dev Ltd Nrf2-säätelijöitä
AU2016280236B2 (en) 2015-06-15 2019-02-07 Astex Therapeutics Limited Nrf2 regulators
AU2016280235A1 (en) * 2015-06-15 2017-12-14 Astex Therapeutics Limited Nrf2 regulators
US10351530B2 (en) * 2015-10-06 2019-07-16 Glaxosmithkline Intellectual Property Development Limited Arylcyclohexyl pyrazoles as NRF2 regulators
EP3359532A1 (en) * 2015-10-06 2018-08-15 GlaxoSmithKline Intellectual Property Development Limited Biaryl pyrazoles as nrf2 regulators
CN105566241B (zh) 2016-01-18 2018-05-25 中国药科大学 1-磺酰胺基-4-芳氧基类化合物、制备方法及其医药用途
CN114617868A (zh) * 2016-02-03 2022-06-14 参宿七制药股份有限公司 Nrf2活化性化合物及其用途
WO2018104766A1 (en) * 2016-12-06 2018-06-14 Glaxosmithkline Intellectual Property Development Limited 3-(2,3-dihydro-1h-inden-5-yl)propanoic acid derivatives and their use as nrf2 regulators
EP3551621A1 (en) * 2016-12-12 2019-10-16 GlaxoSmithKline Intellectual Property Development Limited N-aryl pyrazoles as nrf2 regulators
WO2018109641A1 (en) * 2016-12-12 2018-06-21 Glaxosmithkline Intellectual Property Development Limited 3-carboxylic acid pyrroles as nrf2 regulators
JP2020502123A (ja) * 2016-12-14 2020-01-23 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｎｒｆ２アクチベーターとしてのビスアリール複素環
US20220002272A1 (en) * 2016-12-14 2022-01-06 Glaxosmithkline Intellectual Property Development Limited Bisaryl lactams as nrf2 activators
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