CN103702991A - 用作jak抑制剂的吡啶-2(1h)-酮衍生物 - Google Patents

用作jak抑制剂的吡啶-2(1h)-酮衍生物 Download PDF

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Publication number
CN103702991A
CN103702991A CN201280036953.2A CN201280036953A CN103702991A CN 103702991 A CN103702991 A CN 103702991A CN 201280036953 A CN201280036953 A CN 201280036953A CN 103702991 A CN103702991 A CN 103702991A
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group
branched
cycloalkyl
alkyl
hydrogen atom
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P·R·伊斯特伍德
J·巴赫塔纳
L·M·帕格斯圣塔卡纳
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Almirall SA
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Almirall SA
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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CN201280036953.2A 2011-08-01 2012-07-23 用作jak抑制剂的吡啶-2(1h)-酮衍生物 Pending CN103702991A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP11382263A EP2554544A1 (en) 2011-08-01 2011-08-01 Pyridin-2(1h)-one derivatives as jak inhibitors
EP11382263.9 2011-08-01
US201161556948P 2011-11-08 2011-11-08
US61/556,948 2011-11-08
PCT/EP2012/064426 WO2013017461A1 (en) 2011-08-01 2012-07-23 Pyridin-2(1h)-one derivatives as jak inhibitors

Publications (1)

Publication Number Publication Date
CN103702991A true CN103702991A (zh) 2014-04-02

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CN201280036953.2A Pending CN103702991A (zh) 2011-08-01 2012-07-23 用作jak抑制剂的吡啶-2(1h)-酮衍生物

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Country Link
US (1) US9034311B2 (https=)
EP (2) EP2554544A1 (https=)
JP (1) JP2014521673A (https=)
KR (1) KR20140044865A (https=)
CN (1) CN103702991A (https=)
AR (1) AR087355A1 (https=)
AU (1) AU2012292276A1 (https=)
BR (1) BR112014002245A2 (https=)
CA (1) CA2839805A1 (https=)
CL (1) CL2014000203A1 (https=)
CO (1) CO6852079A2 (https=)
CR (1) CR20140031A (https=)
EA (1) EA201400182A1 (https=)
GT (1) GT201400017A (https=)
MX (1) MX2014000635A (https=)
PE (1) PE20141409A1 (https=)
PH (1) PH12014500103A1 (https=)
UY (1) UY34212A (https=)
WO (1) WO2013017461A1 (https=)
ZA (1) ZA201309187B (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107735091A (zh) * 2015-06-22 2018-02-23 爱维斯健有限公司 包含伊马替尼作为活性成分的用于预防和治疗干眼病的药物组合物

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
CR20170077A (es) 2014-08-04 2017-06-26 Nuevolution As Derivados de heterociclilo opcionalmente condensados de pirimidina útiles para el tratamiento de enfermedades inflamatorias, metabólicas, oncológicas y autoinmunitarias
WO2016060963A1 (en) * 2014-10-14 2016-04-21 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
MX388576B (es) 2016-06-07 2025-03-20 Jacobio Pharmaceuticals Co Ltd Derivados heterociclicos novedosos utiles como inhibidores de shp2.
JP2020502126A (ja) * 2016-12-14 2020-01-23 プロジェニティ, インコーポレイテッド 消化管疾病のjak阻害薬による治療
EA202190196A1 (ru) 2017-03-23 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
JP7117029B2 (ja) * 2017-09-21 2022-08-12 北京賽特明強医薬科技有限公司 2-置換ピラゾールアミノ-4-置換アミノ-5-ピリミジンホルムアミド系化合物、組成物およびその使用
EP3707138B1 (en) 2017-11-06 2022-07-13 Bristol-Myers Squibb Company Isofuranone compounds useful as hpk1 inhibitors
CN110372664A (zh) * 2018-04-13 2019-10-25 华东理工大学 选择性jak2抑制剂及其应用
WO2020051424A1 (en) 2018-09-07 2020-03-12 Pic Therapeutics Eif4e inhibitors and uses thereof
US20210393623A1 (en) 2018-09-26 2021-12-23 Jacobio Pharmaceuticals Co., Ltd. Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
MX2022007265A (es) 2019-12-20 2022-09-09 Nuevolution As Compuestos activos frente a receptores nucleares.
UY38994A (es) 2019-12-20 2021-07-30 Nuevolution As Compuestos activos frente a receptores nucleares
TW202146393A (zh) 2020-03-03 2021-12-16 美商皮克醫療公司 Eif4e抑制劑及其用途
AU2021245397A1 (en) 2020-03-31 2022-10-20 Nuevolution A/S Compounds active towards nuclear receptors
WO2021198956A1 (en) 2020-03-31 2021-10-07 Nuevolution A/S Compounds active towards nuclear receptors
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
US12157732B2 (en) 2021-08-25 2024-12-03 PIC Therapeutics, Inc. eIF4E inhibitors and uses thereof
CA3229560A1 (en) 2021-08-25 2023-03-02 Christopher L. Vandeusen Eif4e inhibitors and uses thereof
KR102503968B1 (ko) 2022-09-22 2023-02-28 이진석 실꼬리 절단장치 및 그를 구비하는 양말 편직기

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008118823A2 (en) * 2007-03-26 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2010085684A1 (en) * 2009-01-23 2010-07-29 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2010090290A1 (ja) * 2009-02-06 2010-08-12 日本新薬株式会社 アミノピラジン誘導体及び医薬

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS54128591A (en) 1978-03-25 1979-10-05 Kyowa Hakko Kogyo Co Ltd Cephalosporin analog
IT7920688U1 (it) 1979-02-05 1980-08-05 Chiesi Paolo Inalatore per sostanze medicamentose pulverulente, con combinata funzione di dosatore
DE3274065D1 (de) 1981-07-08 1986-12-11 Draco Ab Powder inhalator
US4570630A (en) 1983-08-03 1986-02-18 Miles Laboratories, Inc. Medicament inhalation device
FI69963C (fi) 1984-10-04 1986-09-12 Orion Yhtymae Oy Doseringsanordning
DE3927170A1 (de) 1989-08-17 1991-02-21 Boehringer Ingelheim Kg Inhalator
IT1237118B (it) 1989-10-27 1993-05-18 Miat Spa Inalatore multidose per farmaci in polvere.
US5201308A (en) 1990-02-14 1993-04-13 Newhouse Michael T Powder inhaler
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
SG45171A1 (en) 1990-03-21 1998-01-16 Boehringer Ingelheim Int Atomising devices and methods
GB9015522D0 (en) 1990-07-13 1990-08-29 Braithwaite Philip W Inhaler
WO1992003175A1 (en) 1990-08-11 1992-03-05 Fisons Plc Inhalation device
DE4027391A1 (de) 1990-08-30 1992-03-12 Boehringer Ingelheim Kg Treibgasfreies inhalationsgeraet
DE69132850T2 (de) 1990-09-26 2002-05-29 Pharmachemie B.V., Haarlem Wirbelkammer-Pulverinhalator
GB9026025D0 (en) 1990-11-29 1991-01-16 Boehringer Ingelheim Kg Inhalation device
AU650953B2 (en) 1991-03-21 1994-07-07 Novartis Ag Inhaler
DE4239402A1 (de) 1992-11-24 1994-05-26 Bayer Ag Pulverinhalator
DK0674533T3 (da) 1992-12-18 1999-09-27 Schering Corp Inhalator for medikamenter i pulverform
TR199701169T1 (xx) 1995-04-14 1998-03-21 Glaxo Wellcome Inc. Salmeterol i�in �l��lm�� doz inhaleri.
ATE209518T1 (de) 1995-06-21 2001-12-15 Asta Medica Ag Arzneipulverkartusche mit integrierter dosiereinrichtung, sowie pulverinhalator
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
DE19536902A1 (de) 1995-10-04 1997-04-10 Boehringer Ingelheim Int Vorrichtung zur Hochdruckerzeugung in einem Fluid in Miniaturausführung
WO2000035296A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Improved release of medicament active agents from a chewing gum coating
GB9919778D0 (en) 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
PE20020506A1 (es) 2000-08-22 2002-07-09 Glaxo Group Ltd Derivados de pirazol fusionados como inhibidores de la proteina cinasa
US7074801B1 (en) 2001-04-26 2006-07-11 Eisai Co., Ltd. Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof
DE10129703A1 (de) 2001-06-22 2003-01-02 Sofotec Gmbh & Co Kg Zerstäubungssystem für eine Pulvermischung und Verfahren für Trockenpulverinhalatoren
WO2003000682A1 (en) 2001-06-25 2003-01-03 Merck & Co., Inc. (pyrimidyl)(phenyl)substituted fused heteroaryl p38 inhibiting and pkg kinase inhibiting compounds
ATE381332T1 (de) 2002-05-02 2008-01-15 Merck & Co Inc Tyrosinkinase-hemmer
ES2195785B1 (es) 2002-05-16 2005-03-16 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
GB0216383D0 (en) 2002-07-13 2002-08-21 Astrazeneca Ab Compounds
ES2211344B1 (es) 2002-12-26 2005-10-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2232306B1 (es) 2003-11-10 2006-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2364340T3 (es) 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
ES2251866B1 (es) 2004-06-18 2007-06-16 Laboratorios Almirall S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2251867B1 (es) 2004-06-21 2007-06-16 Laboratorios Almirall S.A. Nuevos derivados de piridazin-3(2h)-ona.
ES2353018T3 (es) 2004-07-16 2011-02-24 Almirall, S.A. Inhalador para la administración de productos farmacéuticos en polvo, y un cartucho de polvo para uso con este inhalador.
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
ES2325035T3 (es) 2004-12-21 2009-08-24 Smithkline Beecham Corporation Inhibidores de quinasa erbb de 2-pirimidinil pirazolopiridina.
US20080287437A1 (en) 2005-05-16 2008-11-20 Astrazeneca Ab Pyrazolylaminopyrimidine Derivatives Useful as Tyrosine Kinase Inhibitors
ES2265276B1 (es) 2005-05-20 2008-02-01 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
JP2009513615A (ja) * 2005-10-28 2009-04-02 アストラゼネカ アクチボラグ 癌の治療においてチロシンキナーゼ阻害剤として使用するための4−(3−アミノピラゾール)ピリミジン誘導体
ES2296516B1 (es) 2006-04-27 2009-04-01 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
RU2008152776A (ru) 2006-06-06 2010-07-20 Эвиджен Инк. (Us) СОЕДИНЕНИЯ ЗАМЕЩЕННОГО ПИРАЗОЛО[1,5-a]ПИРИДИНА И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
US7919490B2 (en) 2006-10-04 2011-04-05 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
WO2008045393A2 (en) 2006-10-11 2008-04-17 Amgen Inc. Imidazo- and triazolo-pyridine compounds and methods of use therof
ES2302447B1 (es) 2006-10-20 2009-06-12 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
ES2555803T3 (es) * 2006-10-23 2016-01-08 Cephalon, Inc. Fusión de derivados bicíclicos 2,4-diaminopirimidina como utilizar inhibidores ALK y c-Met
ES2319596B1 (es) 2006-12-22 2010-02-08 Laboratorios Almirall S.A. Nuevos derivados de los acidos amino-nicotinico y amino-isonicotinico.
US8513276B2 (en) 2006-12-22 2013-08-20 Astex Therapeutics Limited Imidazo[1,2-a]pyridine compounds for use in treating cancer
US7977336B2 (en) 2006-12-28 2011-07-12 Banyu Pharmaceutical Co. Ltd Aminopyrimidine derivatives as PLK1 inhibitors
ES2306595B1 (es) 2007-02-09 2009-09-11 Laboratorios Almirall S.A. Sal de napadisilato de 5-(2-((6-(2,2-difluoro-2-feniletoxi)hexil)amino)-1-hidroxietil)-8-hidroxiquinolin-2(1h)-ona como agonista del receptor adrenergico beta2.
WO2008132502A1 (en) * 2007-04-25 2008-11-06 Astrazeneca Ab Pyrazolyl-amino-substituted pyrimidines and their use for the treatment of cancer
WO2008135786A1 (en) * 2007-05-04 2008-11-13 Astrazeneca Ab Amino-thiazolyl- pyrimidine derivatives and their use for the treatment of cancer
UY31272A1 (es) 2007-08-10 2009-01-30 Almirall Lab Nuevos derivados de ácido azabifenilaminobenzoico
WO2009021990A1 (en) 2007-08-14 2009-02-19 Bayer Schering Pharma Aktiengesellschaft Fused imidazoles for cancer treatment
ES2400604T3 (es) 2007-08-17 2013-04-11 Icagen, Inc. Heterociclos como moduladores del canal de potasio
WO2009027736A2 (en) * 2007-08-27 2009-03-05 Astrazeneca Ab 2,4 diaminopyrimid'lnes for the treatment of myeloproliferative disorders and cancer
AR068877A1 (es) 2007-10-17 2009-12-09 Novartis Ag Derivados heterociclicos de imidazol
EP2211620B1 (en) 2007-10-25 2013-12-25 Merck Sharp & Dohme Corp. 3-PYRAZIN SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AS JANUS KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES
ES2320961B1 (es) 2007-11-28 2010-03-17 Laboratorios Almirall, S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor adrenergico beta2.
CN101932583A (zh) 2007-12-19 2010-12-29 沃泰克斯药物股份有限公司 用作JAK2抑制剂的吡唑并[1,5-a]嘧啶类
EP2231660A1 (en) 2007-12-21 2010-09-29 Wyeth LLC Imidazo [1,2-a] pyridine compounds
JP5368485B2 (ja) 2008-02-25 2013-12-18 エフ.ホフマン−ラ ロシュ アーゲー ピロロピラジンキナーゼインヒビター
AU2009238590A1 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
PE20100087A1 (es) * 2008-06-25 2010-02-08 Irm Llc Compuestos y composiciones como inhibidores de cinasa
JP5576370B2 (ja) 2008-08-06 2014-08-20 ファイザー・インク Chk−1阻害剤としての6置換2−ヘテロシクリルアミノピラジン化合物
UY32055A (es) * 2008-08-19 2010-03-26 Astrazeneca Ab Derivados sustituidos de la 5-Halo-N2-[sustituido](1-metil-1H-imidazol-4-il)pirimidin-2,-diamina y sus sales farmacéuticamente aceptables, procesos de preparación, composiciones y aplicaciones.
EP2196465A1 (en) 2008-12-15 2010-06-16 Almirall, S.A. (3-oxo)pyridazin-4-ylurea derivatives as PDE4 inhibitors
UY32297A (es) 2008-12-22 2010-05-31 Almirall Sa Sal mesilato de 5-(2-{[6-(2,2-difluoro-2-fenilitoxi) hexil]amino}-1-hidroxietil)-8-hidroxiquinolin-2( 1h)-ona como agonista del receptor b(beta)2 acrenérgico
AR074870A1 (es) 2008-12-24 2011-02-16 Palau Pharma Sa Derivados de pirazolo (1,5-a ) piridina
ES2629006T3 (es) 2009-10-29 2017-08-07 Vectura Limited Derivados que contienen N-heteroarilo como inhibidores de la quinasa jak3
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
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
EP2527344A1 (en) 2011-05-25 2012-11-28 Almirall, S.A. Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008118823A2 (en) * 2007-03-26 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2010085684A1 (en) * 2009-01-23 2010-07-29 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2010090290A1 (ja) * 2009-02-06 2010-08-12 日本新薬株式会社 アミノピラジン誘導体及び医薬

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107735091A (zh) * 2015-06-22 2018-02-23 爱维斯健有限公司 包含伊马替尼作为活性成分的用于预防和治疗干眼病的药物组合物

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