PE20180279A1 - Derivados de 2-(pirazolopiridin-3-il)pirimidina como inhibidores de jak - Google Patents

Derivados de 2-(pirazolopiridin-3-il)pirimidina como inhibidores de jak

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Publication number
PE20180279A1
PE20180279A1 PE2017002479A PE2017002479A PE20180279A1 PE 20180279 A1 PE20180279 A1 PE 20180279A1 PE 2017002479 A PE2017002479 A PE 2017002479A PE 2017002479 A PE2017002479 A PE 2017002479A PE 20180279 A1 PE20180279 A1 PE 20180279A1
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Peru
Prior art keywords
pyrazolopyridin
compounds
ylpyrimidin
pyrazolo
pyridin
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PE2017002479A
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English (en)
Inventor
Trias Cristina Esteve
Moll Joan Taltavull
Rodriguez Jacob Gonzalez
Juan Bernat Vidal
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Almirall Sa
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Publication date
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Publication of PE20180279A1 publication Critical patent/PE20180279A1/es

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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

Referido a derivados de 2-(pirazolopiridin-3-il)pirimidina, de formula I, en donde: X es O, NR3; R1 y R2 son H, halogeno, alquilo C1-C4, alcoxilo C1-C4, CN; G1 es CN, CORa, OR6, entre otros. Estos compuestos son inhibidores de cinasa Janus (JAK). Entre los compuestos preferidos tenemos los siguientes: (trans-4-{[5-fluoro-6-(4-hidroxipiperidin-1-il)-2-pirazolo[1,5-a]piridin-3-ilpirimidin-4-il]amino}ciclohexil)acetonitrilo; (trans-4-{[6(4-aminopiperidin-1-il)-5-fluoro-2-pirazolo[1,5-a]piridin-3-ilpirimidin-4-il]amino}ciclohexil)acetonitrilo, entre otros. Estos compuestos se pueden emplear en el tratamiento de diversas enfermedades o estados patologicos como trastornos neurologicos, enfermedad cardiovascular, dolor, rechazo de trasplante de medula osea y de organos, sindrome mielodisplasico, cancer, leucemia, linfoma, dermatitis atopica, eccema, vitiligo, entre otras.
PE2017002479A 2015-06-11 2016-06-10 Derivados de 2-(pirazolopiridin-3-il)pirimidina como inhibidores de jak PE20180279A1 (es)

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EP15382305 2015-06-11

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PE20180279A1 true PE20180279A1 (es) 2018-02-07

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US (1) US10759793B2 (es)
EP (1) EP3307272A1 (es)
JP (1) JP2018516954A (es)
KR (1) KR20180012854A (es)
CN (1) CN107667106A (es)
AR (1) AR104963A1 (es)
AU (1) AU2016275716C1 (es)
BR (1) BR112017025781A2 (es)
CA (1) CA2987328A1 (es)
CL (1) CL2017003107A1 (es)
CO (1) CO2017011996A2 (es)
CR (1) CR20170557A (es)
EA (1) EA035312B1 (es)
HK (1) HK1246667A1 (es)
IL (1) IL255668A (es)
MA (1) MA42592A (es)
MX (1) MX2017015029A (es)
PE (1) PE20180279A1 (es)
PH (1) PH12017502236A1 (es)
SG (1) SG10201911926UA (es)
TW (1) TW201705961A (es)
WO (1) WO2016198663A1 (es)

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US10870695B2 (en) 2015-08-24 2020-12-22 Glaxosmithkline Intellectual Property (No. 2) Limited Biopharmaceutical compositions comprising interleukin-5 antibody
AU2017216861A1 (en) * 2016-02-12 2018-10-04 Universität Zürich Dimethyl fumarate (DMF) for prevention or treatment of gout, acne, diabetes, vitiligo and/or pyoderma gangrenosum
ES2877140T3 (es) * 2016-11-08 2021-11-16 Cancer Research Tech Ltd Derivados de pirimidinona como inhibidores de Cdc7
WO2018136554A1 (en) * 2017-01-17 2018-07-26 Menlo Therapeutics Inc. Use of neurokinin-1 antagonists as antitussives
WO2018160138A1 (en) * 2017-03-02 2018-09-07 Aslan Pharmaceuticals Pte Ltd Dhodh inhibitor for treating haematological cancer
US11311548B2 (en) 2017-03-02 2022-04-26 Aslan Pharmaceuticals Pte. Ltd. Cancer therapy
US11957931B2 (en) * 2017-04-26 2024-04-16 Yale University Compositions and methods for treating vitiligo
CN108514637A (zh) * 2018-05-07 2018-09-11 山东省眼科研究所 Stat3抑制剂s31-201在治疗干眼症中的应用
CN109810991B (zh) * 2019-03-02 2021-11-12 昆明理工大学 二氢蝶酸合酶基因folP的用途
KR20230018485A (ko) * 2020-06-02 2023-02-07 네르 쎄라퓨틱스 리미티드 폐에 대한 기계적 손상에 의해 촉진된 폐 섬유증 상태의 치료에 사용하기 위한 뉴로키닌 (nk)-1 수용체 길항제
IL308216A (en) * 2021-05-03 2024-01-01 Incyte Corp Jak1 pathway inhibitors for the treatment of prurigo nodularis

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JPS54128591A (en) 1978-03-25 1979-10-05 Kyowa Hakko Kogyo Co Ltd Cephalosporin analog
EP2338888A1 (en) * 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
UY33213A (es) * 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
EP2397482A1 (en) 2010-06-15 2011-12-21 Almirall, S.A. Heteroaryl imidazolone derivatives as jak inhibitors
AR086042A1 (es) * 2011-04-28 2013-11-13 Galapagos Nv Compuesto util para el tratamiento de enfermedades degenerativas e inflamatorias y composicion farmaceutica
WO2013025628A1 (en) 2011-08-15 2013-02-21 Ligand Pharmaceuticals Incorporated Janus kinase inhibitor compounds and methods
EP2758389B1 (en) * 2011-09-22 2017-06-07 Merck Sharp & Dohme Corp. Pyrazole carboxamides as janus kinase inhibitors
WO2015086693A1 (en) * 2013-12-11 2015-06-18 Almirall, S.A. Pyrazolopyrimidin-2-yl derivatives as jak inhibitors

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AU2016275716C1 (en) 2020-10-15
AR104963A1 (es) 2017-08-30
AU2016275716B2 (en) 2020-01-23
AU2016275716A1 (en) 2017-12-07
US10759793B2 (en) 2020-09-01
MA42592A (fr) 2018-06-20
NZ737314A (en) 2021-02-26
HK1246667A1 (zh) 2018-09-14
EA035312B1 (ru) 2020-05-27
CL2017003107A1 (es) 2018-04-02
PH12017502236A1 (en) 2018-06-11
CO2017011996A2 (es) 2018-03-28
SG10201911926UA (en) 2020-01-30
JP2018516954A (ja) 2018-06-28
BR112017025781A2 (pt) 2018-08-14
US20180162856A1 (en) 2018-06-14
EA201792689A1 (ru) 2018-07-31
WO2016198663A1 (en) 2016-12-15
CR20170557A (es) 2018-02-06
CN107667106A (zh) 2018-02-06
IL255668A (en) 2018-01-31
CA2987328A1 (en) 2016-12-15
KR20180012854A (ko) 2018-02-06
TW201705961A (zh) 2017-02-16
EP3307272A1 (en) 2018-04-18
MX2017015029A (es) 2018-04-13

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