[go: up one dir, main page]

PE20190811A1 - Derivados de pirazolopirimidinas como inhibidor de quinasa - Google Patents

Derivados de pirazolopirimidinas como inhibidor de quinasa

Info

Publication number
PE20190811A1
PE20190811A1 PE2018003174A PE2018003174A PE20190811A1 PE 20190811 A1 PE20190811 A1 PE 20190811A1 PE 2018003174 A PE2018003174 A PE 2018003174A PE 2018003174 A PE2018003174 A PE 2018003174A PE 20190811 A1 PE20190811 A1 PE 20190811A1
Authority
PE
Peru
Prior art keywords
pyrazolopyrimidines
derivatives
kinase inhibitor
compound
halogen
Prior art date
Application number
PE2018003174A
Other languages
English (en)
Inventor
In Woo Kim
Mi Ryeong Han
Jakyung Yoo
Yun Ju Oh
Ji Duck Kim
Nam Youn Kim
Sun Ah Jun
Jun Hee Lee
Joon Seok Park
Original Assignee
Dae Woong Pharma
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 Dae Woong Pharma filed Critical Dae Woong Pharma
Publication of PE20190811A1 publication Critical patent/PE20190811A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Referido a un compuesto derivado de pirazolopirimidina de formula I, en donde R1 es arilo C6-C10; o heteroarilo C2-10 que contiene de uno a tres de N, O o S; R2 es H, alquilo C1-4 o halogeno; R3 es alquilo C1-4 no sustituido o sustituido con ciano o halogeno, entre otros; X1 es CR4 o N; X2 es CR5 o N; X3 es NR6, O o S; X4 es CH o N; X5 es un enlace, o NH. Un compuesto seleccionado es (R)-1-(3-(2-(4-(4-metilpiperazin-1-il)fenilamino)-7H-pirrolo[2,3-d]pirimidin-4-ilamino)piperidin-1-il)prop-2-en-1-ona. Dicho compuesto tiene actividad inhibidora de quinasas. Tambien se refiere a un procedimiento para la preparacion del mismo y a una composicion farmaceutica para el tratamiento de enfermedad inflamatoria, autoinmunitaria, proliferativa, entre otros.
PE2018003174A 2016-06-30 2017-06-30 Derivados de pirazolopirimidinas como inhibidor de quinasa PE20190811A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR20160083050 2016-06-30
PCT/KR2017/006980 WO2018004306A1 (en) 2016-06-30 2017-06-30 Pyrazolopyrimidine derivatives as kinase inhibitor

Publications (1)

Publication Number Publication Date
PE20190811A1 true PE20190811A1 (es) 2019-06-13

Family

ID=60785389

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2018003174A PE20190811A1 (es) 2016-06-30 2017-06-30 Derivados de pirazolopirimidinas como inhibidor de quinasa

Country Status (23)

Country Link
US (1) US10961247B2 (es)
EP (3) EP3478687B1 (es)
JP (2) JP2019519579A (es)
KR (1) KR102329162B1 (es)
CN (2) CN109311896B (es)
AU (1) AU2017287762C1 (es)
BR (1) BR112018074621B1 (es)
CA (1) CA3025636C (es)
CL (1) CL2018003511A1 (es)
CO (1) CO2018013293A2 (es)
DO (1) DOP2018000275A (es)
EC (1) ECSP18093777A (es)
ES (1) ES2977557T3 (es)
IL (1) IL263306B (es)
MX (2) MX393499B (es)
MY (1) MY191110A (es)
PE (1) PE20190811A1 (es)
PH (1) PH12018502507B1 (es)
RU (1) RU2714206C1 (es)
SA (2) SA518400547B1 (es)
SG (1) SG11201811470PA (es)
WO (1) WO2018004306A1 (es)
ZA (1) ZA201808431B (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112020002265A2 (pt) 2017-08-01 2020-07-28 Theravance Biopharma R&D Ip, Llc compostos pirazólicos e triazólicos bicíclicos como inibidores de jak quiinase
KR102577241B1 (ko) * 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-플루오로피페리딘 유도체
MA51431B1 (fr) * 2017-12-28 2022-08-31 Daewoong Pharmaceutical Co Ltd Dérivés d'oxy-fluoropipéridine utilisés en tant qu'inhibiteur de kinase
KR102577242B1 (ko) 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-메틸피페리딘 유도체
CN108586341B (zh) * 2018-05-25 2020-05-08 天津商业大学 酰胺类化合物和其药用盐及其制备方法和药物用途
BR112021002479A2 (pt) * 2018-08-10 2021-07-27 Aclaris Therapeutics, Inc. composto, composição farmacêutica, método para inibir a atividade de itk ou jak3 em uma população de células, método para tratar um distúrbio mediado por itk ou jak3 em um indivíduo necessitando do mesmo e uso de um composto
WO2020154350A1 (en) 2019-01-23 2020-07-30 Theravance Biopharma R&D Ip, Llc Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors
EP3851438A4 (en) * 2019-03-18 2021-11-10 Shanghai Haiyan Pharmaceutical Technology Co., Ltd BTK INHIBITOR, PHARMACEUTICALLY ACCEPTABLE SALT, POLYMORPHIC AND APPLICATION OF THE SAME
CN110317176A (zh) * 2019-07-04 2019-10-11 沈阳药科大学 2-氨基嘧啶类化合物及其用途
CN114901659A (zh) 2019-11-26 2022-08-12 施万生物制药研发Ip有限责任公司 作为jak抑制剂的稠合嘧啶吡啶酮化合物
WO2021147952A1 (zh) * 2020-01-21 2021-07-29 江苏先声药业有限公司 嘧啶并吡咯类化合物
CN115244055B (zh) * 2020-01-21 2024-09-03 江苏先声药业有限公司 嘧啶并五元环类衍生物及其应用
CN113214265B (zh) * 2020-01-21 2023-07-07 江苏先声药业有限公司 嘧啶并五元环类化合物
CN111620878A (zh) * 2020-06-10 2020-09-04 中国药科大学 吡咯并嘧啶类衍生物作为蛋白激酶抑制剂及其应用
TW202202498A (zh) * 2020-07-01 2022-01-16 大陸商四川海思科製藥有限公司 一種並環雜環衍生物及其在醫藥上的應用
WO2022062601A1 (zh) * 2020-09-22 2022-03-31 江苏先声药业有限公司 嘧啶并吡咯类化合物
CN114315838B (zh) * 2020-09-30 2024-09-03 江苏先声药业有限公司 嘧啶并吡咯类化合物
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
CN114907357A (zh) * 2021-02-07 2022-08-16 江苏先声药业有限公司 嘧啶并吡咯类化合物
JP2025525347A (ja) * 2022-06-16 2025-08-05 アンフィスタ セラピューティクス リミテッド 標的タンパク質分解のための新規の二官能性分子
CN115368366A (zh) * 2022-08-02 2022-11-22 江苏省中医药研究院 嘧啶并吡唑类化合物及其应用
US20250078283A1 (en) * 2022-11-28 2025-03-06 Rakuten Group, Inc. Image processing system, image processing method, and program
WO2024228580A1 (ko) * 2023-05-04 2024-11-07 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물
WO2025121899A1 (ko) * 2023-12-05 2025-06-12 주식회사 대웅제약 1-((3s,4r)-3-((2-((1-에틸-1h-피라졸-4-일)아미노)-7h-피롤로[2,3-d]피리미딘-4-일)옥시)-4-플루오로피페리딘-1-일)프로프-2-엔-1-온의 제조 방법, 및 이의 중간체 화합물

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
PL373246A1 (en) 2002-04-12 2005-08-22 Pfizer Inc. Use of ep4 receptor ligands in the treatment of il-6 involved diseases
US8163767B2 (en) 2005-07-14 2012-04-24 Astellas Pharma Inc. Heterocyclic Janus Kinase 3 inhibitors
SI2426129T1 (sl) 2005-12-13 2017-02-28 Incyte Holdings Corporation Heteroarilno substituirani pirolo(2,3-b)piridini in pirolo(2,3-b)pirimidini kot zaviralci janusove kinaze
PL2529622T3 (pl) 2006-09-22 2018-07-31 Pharmacyclics Llc Inhibitory kinazy tyrozynowej brutona
SG183036A1 (en) 2007-07-17 2012-08-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
WO2009026107A1 (en) * 2007-08-17 2009-02-26 Portola Pharmaceuticals, Inc. Protein kinase inhibitors
US8183245B2 (en) 2007-10-25 2012-05-22 Merck Sharp & Dohme Corp. Pyrazine substituted pyrrolopyridines as inhibitors of JAK and PDK1
CN102066338A (zh) * 2008-04-22 2011-05-18 波托拉医药品公司 蛋白激酶抑制剂
PE20091846A1 (es) * 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
CN102159214A (zh) 2008-07-16 2011-08-17 药品循环公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
EP2440559B1 (en) * 2009-05-05 2018-01-10 Dana-Farber Cancer Institute, Inc. Egfr inhibitors and methods of treating disorders
US8785639B2 (en) 2009-12-01 2014-07-22 Abbvie Inc. Substituted dihydropyrazolo[3,4-D]pyrrolo[2,3-B]pyridines and methods of use thereof
MX342164B (es) * 2010-06-23 2016-09-19 Hanmi Science Co Ltd Derivados de pirimidina fusionados novedosos para la inhibicion de la actividad de tirosina cinasa.
ES2640911T3 (es) 2011-09-22 2017-11-07 Merck Sharp & Dohme Corp. Cicloalquilnitrilpirazolcarboxamidas como inhibidores de la quinasa Janus
WO2013169401A1 (en) * 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
HK1217695A1 (zh) * 2013-03-05 2017-01-20 F. Hoffmann-La Roche Ag 布鲁顿氏酪氨酸激酶抑制剂
MX368491B (es) 2013-07-11 2019-10-04 Acea Biosciences Inc Derivados de pirimidina como inhibidores de cinasa.
KR101879422B1 (ko) * 2013-09-18 2018-07-17 베이징 한미 파마슈티컬 컴퍼니 리미티드 Btk 및/또는 jak3 키나제의 활성을 억제하는 화합물
PT3077395T (pt) * 2013-12-05 2018-01-03 Pfizer Pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinilo e pirrolo[2,3-d]piridinilo acrilamidas
CN105777756B (zh) * 2014-07-02 2019-03-01 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
CN105315285B (zh) * 2014-07-25 2017-12-08 上海海雁医药科技有限公司 2,4‑二取代7H‑吡咯并[2,3‑d]嘧啶衍生物、其制法与医药上的用途
KR101710127B1 (ko) 2014-08-29 2017-02-27 한화제약주식회사 야누스인산화효소 억제제로서의 치환된 N-(피롤리딘-3-일)-7H-피롤로[2,3-d]피리미딘-4-아민
CN105732637B (zh) 2014-12-30 2020-04-21 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
CA2976109A1 (en) 2015-02-13 2016-08-18 Dana-Farber Cancer Institute, Inc. Substituted pyrrolopyrimidine, pyrazolopyrimidine and purine derivatives and use thereof as lrrk2 inhibitors

Also Published As

Publication number Publication date
SA521430937B1 (ar) 2022-12-25
US20200317673A1 (en) 2020-10-08
AU2017287762A1 (en) 2018-12-13
NZ748746A (en) 2020-08-28
CO2018013293A2 (es) 2018-12-14
IL263306B (en) 2021-05-31
SA518400547B1 (ar) 2022-09-20
EP3478687A4 (en) 2020-02-19
JP7084961B2 (ja) 2022-06-15
SG11201811470PA (en) 2019-01-30
CN109311896B (zh) 2021-08-24
CA3025636A1 (en) 2018-01-04
CA3025636C (en) 2022-10-18
EP3478687A1 (en) 2019-05-08
MX393499B (es) 2025-03-24
IL263306A (en) 2018-12-31
US10961247B2 (en) 2021-03-30
MY191110A (en) 2022-05-30
CN113135920A (zh) 2021-07-20
PH12018502507B1 (en) 2023-11-15
AU2017287762B2 (en) 2019-09-26
ZA201808431B (en) 2020-05-27
DOP2018000275A (es) 2018-10-31
KR20180003472A (ko) 2018-01-09
CN109311896A (zh) 2019-02-05
ECSP18093777A (es) 2018-12-31
MX2021009378A (es) 2022-06-29
BR112018074621B1 (pt) 2021-06-08
AU2017287762C1 (en) 2020-04-23
JP2020143162A (ja) 2020-09-10
BR112018074621A2 (pt) 2019-03-06
WO2018004306A1 (en) 2018-01-04
CL2018003511A1 (es) 2019-04-05
EP4656249A2 (en) 2025-12-03
RU2714206C1 (ru) 2020-02-13
KR102329162B1 (ko) 2021-11-22
MX2018016287A (es) 2019-05-20
JP2019519579A (ja) 2019-07-11
ES2977557T3 (es) 2024-08-26
EP3950691A1 (en) 2022-02-09
PH12018502507A1 (en) 2019-07-08
EP3478687B1 (en) 2024-03-20
MX388591B (es) 2025-03-20

Similar Documents

Publication Publication Date Title
PE20190811A1 (es) Derivados de pirazolopirimidinas como inhibidor de quinasa
CY1125460T1 (el) Ενωσεις ιμιδαζο [4,5-d]πυρρολο [2,3-β]πυριδινης ως αναστολεις κινασων janus
PE20221905A1 (es) Aminas biciclicas como inhibidoras de la cdk2
MX381849B (es) Compuestos a base de pirazol[1,5-a]pirimidina, composiciones que los comprenden, y métodos para su uso.
PE20190656A1 (es) Compuestos de tiazolo-piridina sustituida como inhibidores de malt1
AR112833A2 (es) Compuestos pirazolo[1,5-a]pirimidina sustituida como inhibidores de trk cinasa
PE20191499A1 (es) Imidazopirrolopiridina como inhibidores de la familia de quinasas jak
MX382352B (es) Compuestos de heteroarilo y usos de los mismos.
MX387394B (es) Compuestos heterociclicos como inhibidores de la cinasa ret.
EA201691404A1 (ru) Бициклические гетероциклические производные в качестве ингибиторов бромодомена
EA201691428A1 (ru) Бициклические гетероциклические производные в качестве ингибиторов irak4
EA201691484A1 (ru) Соли и твердая форма ингибитора btk
PE20190395A1 (es) Pirimidin-2-ilamino-1h-pirazoles como inhibidores de lrrk2 para el uso en el tratamiento de trastornos neurodegenerativos
CO2018011408A2 (es) Compuestos de pirimidina como inhibidores de la quinasa jak
EA201690848A1 (ru) Производные бициклического пиридила с конденсированными кольцами в качестве ингибиторов fgfr4
PE20161427A1 (es) Inhibidores heteroarilo de syk
WO2015058163A3 (en) Heteromaromatic compounds useful for the treatment of prolferative diseases
WO2015058126A8 (en) Heteroaromatic compounds useful for the treatment of prolferative diseases
EA201592199A1 (ru) Производные бипиразола в качестве ингибиторов jak
ECSP11011113A (es) Piridiloxi-indoles inhibidores del vegf-r2 y uso de los mismos para el tratamiento de enfermedades
PE20152033A1 (es) Heterociclos bicicliclos como inhibidores de fgfr
EA201070395A1 (ru) Ингибиторы polo-подобных киназ
PE20160934A1 (es) (aza) piridopirazolopirimidinonas e indazolopirimidinonas como inhibidores de fibrinolisis
EA201500298A1 (ru) Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы
BR112014009006B8 (pt) Compostos heterocíclicos e métodos de uso dos mesmos