AR106756A1 - Compuestos y composiciones útiles para el tratamiento de trastornos relacionados con ntrk - Google Patents

Compuestos y composiciones útiles para el tratamiento de trastornos relacionados con ntrk

Info

Publication number
AR106756A1
AR106756A1 ARP160103546A ARP160103546A AR106756A1 AR 106756 A1 AR106756 A1 AR 106756A1 AR P160103546 A ARP160103546 A AR P160103546A AR P160103546 A ARP160103546 A AR P160103546A AR 106756 A1 AR106756 A1 AR 106756A1
Authority
AR
Argentina
Prior art keywords
alkyl
heteroalkyl
monocyclic
hydroxyalkyl
heterocyclyl
Prior art date
Application number
ARP160103546A
Other languages
English (en)
Inventor
L Kim Joseph
Bifulco Neil Jr
V Miduturu Chandrasekhar
Mark Wenglowsky Steven
Original Assignee
Blueprint Medicines Corp
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 Blueprint Medicines Corp filed Critical Blueprint Medicines Corp
Publication of AR106756A1 publication Critical patent/AR106756A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, caracterizado porque: el anillo A se selecciona entre arilo monocíclico o bicíclico, heteroarilo monocíclico o bicíclico, cicloalquilo y heterociclilo; cada RA se selecciona en forma independiente entre arilo monocíclico o bicíclico, heteroarilo monocíclico o bicíclico, cicloalquilo monocíclico o bicíclico, heterociclilo monocíclico o bicíclico, C₁₋₆ alquilo, C₁₋₆ alcoxilo, halo, C₁₋₆ haloalquilo, C₁₋₆ haloalcoxilo, C₁₋₆ hidroxialquilo, C₁₋₆ heteroalquilo, -N(R¹)(R¹), nitro, ciano, -C(O)R¹, -OC(O)R¹, -C(O)OR¹, -SR¹, -S(O)₂R¹, -S(O)₂-N(R²)(R²), -(C₁₋₆ alquilen)-S(O)₂-N(R²)(R²), -C(O)-N(R²)(R²), -N(R²)(R²)-C(O)R¹, -(C₁₋₆ alquilen)-N(R²)-C(O)R¹, -NR²S(O)₂R¹, -P(O)(R¹)(R¹), y -OR¹; donde cada uno de arilo, heteroarilo, cicloalquilo, heterociclilo, alquilo, alcoxilo, haloalquilo, hidroxialquilo, heteroalquilo está sustituido en forma independiente con 0 - 5 instancias de Rᵃ; cada RB se selecciona en forma independiente entre C₁₋₆ alquilo, C₁₋₆ alcoxilo, halo, C₁₋₆ haloalquilo, C₁₋₆ haloalcoxilo, C₁₋₆ hidroxialquilo, C₁₋₆ heteroalquilo, -N(R¹)(R¹), nitro, ciano, y -OR¹; cada R¹ se selecciona en forma independiente entre hidrógeno, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ haloalcoxilo, C₁₋₆ hidroxialquilo, C₁₋₆ heteroalquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, y heterociclilalquilo, donde cada uno de C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₁₋₆ heteroalquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, y heterociclilalquilo está sustituido en forma independiente con 0 - 5 instancias de Rᵇ; cada R² se selecciona en forma independiente entre hidrógeno, C₁₋₆ alquilo, C₁₋₆ heteroalquilo; o 2 R² junto con el nitrógeno al cual están unidos forman un anillo heterociclilo sustituido con 0 - 5 instancias de Rᵇ; cada Rᵃ y Rᵇ se selecciona en forma independiente entre halo, ciano, hidroxilo, C₁₋₆ alquilo, C₁₋₆ alcoxilo, C₁₋₆ haloalcoxilo, -N(R’’)(R’’), -C(O)-N(R’’)(R’’), -N(R’’)(R’’)-C(O)R’, y -(C₁₋₆ alquilen)-N(R’’)-C(O)R’; cada R’ y R’’ se selecciona en forma independiente entre hidrógeno y C₁₋₆ alquilo o C₁₋₆ hidroxialquilo; m es 0, 1, 2, 3, 4 ó 5; y n es 0, 1 ó 2; con la condición de que el compuesto no es (R)-5-(2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-carbonitrilo.
ARP160103546A 2015-11-19 2016-11-18 Compuestos y composiciones útiles para el tratamiento de trastornos relacionados con ntrk AR106756A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562257476P 2015-11-19 2015-11-19

Publications (1)

Publication Number Publication Date
AR106756A1 true AR106756A1 (es) 2018-02-14

Family

ID=57517997

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP160103546A AR106756A1 (es) 2015-11-19 2016-11-18 Compuestos y composiciones útiles para el tratamiento de trastornos relacionados con ntrk

Country Status (18)

Country Link
US (2) US10370379B2 (es)
EP (1) EP3377497A1 (es)
JP (1) JP2019500328A (es)
KR (1) KR20180081790A (es)
CN (1) CN108431008A (es)
AR (1) AR106756A1 (es)
AU (1) AU2016355196A1 (es)
BR (1) BR112018010024A8 (es)
CA (1) CA3005741A1 (es)
HK (1) HK1259453A1 (es)
IL (1) IL259164A (es)
MX (1) MX2018006195A (es)
PH (1) PH12018501065A1 (es)
RU (1) RU2018122089A (es)
SG (2) SG10201912607SA (es)
TW (1) TWI733713B (es)
WO (1) WO2017087778A1 (es)
ZA (1) ZA201803530B (es)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2872491T3 (da) 2012-07-11 2021-08-09 Blueprint Medicines Corp Inhibitorer af fibroblastvækstfaktorreceptoren
US9499522B2 (en) 2013-03-15 2016-11-22 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
DK3057969T3 (en) 2013-10-17 2018-09-24 Blueprint Medicines Corp COMPOSITIONS USED FOR TREATMENT OF DISEASES RELATED TO ENZYMETE KIT
EP3060560A1 (en) 2013-10-25 2016-08-31 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
AU2016297754A1 (en) 2015-07-24 2018-02-15 Blueprint Medicines Corporation Compounds useful for treating disorders related to KIT and PDGFR
CA2995997A1 (en) 2015-08-26 2017-03-02 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
LT3371171T (lt) 2015-11-02 2024-01-10 Blueprint Medicines Corporation Ret inhibitoriai
SG10201912607SA (en) 2015-11-19 2020-02-27 Blueprint Medicines Corp Compounds and compositions useful for treating disorders related to ntrk
US10183928B2 (en) 2016-03-17 2019-01-22 Blueprint Medicines Corporation Inhibitors of RET
HUE063042T2 (hu) 2016-04-15 2023-12-28 Blueprint Medicines Corp Az aktivin receptorszerû kináz inhibitorai
WO2018017983A1 (en) 2016-07-22 2018-01-25 Blueprint Medicines Corporation Compounds useful for treating disorders related to ret
US10035789B2 (en) 2016-07-27 2018-07-31 Blueprint Medicines Corporation Compounds useful for treating disorders related to RET
US11040979B2 (en) 2017-03-31 2021-06-22 Blueprint Medicines Corporation Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR
WO2019079649A1 (en) 2017-10-18 2019-04-25 Blueprint Medicines Corporation SUBSTITUTED PYRROLOPYRIDINES AS INHIBITORS OF ACTIVIN RECEPTOR-RELATED KINASE
KR20200139749A (ko) 2018-04-03 2020-12-14 블루프린트 메디신즈 코포레이션 Ret 변경을 갖는 암을 치료하는 데 사용하는 데 사용하기 위한 ret 억제제
KR20210068597A (ko) 2018-10-30 2021-06-09 크로노스 바이오, 인코포레이티드 Cdk9 활성을 조절하기 위한 화합물, 조성물 및 방법
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
CN112979654B (zh) * 2019-12-16 2024-03-19 赛诺哈勃药业（成都）有限公司 杂芳基稠环化合物、其制备方法及应用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5251911A (en) 1992-12-09 1993-10-12 Blake Carlton E Safety construction for passenger vehicle
ATE291022T1 (de) 1996-10-02 2005-04-15 Novartis Pharma Gmbh Pyrimiderivate und verfahren zu ihrer herstellung
PL224879B1 (pl) * 2002-09-04 2017-02-28 Pharmacopeia Drug Discovery Inc Pirazolo [1,5-a] pirymidynowy związek, jego zastosowanie do wytwarzania leku oraz zawierająca go farmaceutyczna kompozycja
US7329662B2 (en) * 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
ATE433979T1 (de) 2004-04-02 2009-07-15 Osi Pharm Inc Mit einem 6,6-bicyclischen ring substituierte heterobicyclische proteinkinaseinhibitoren
CA2563699C (en) 2004-04-23 2014-03-25 Exelixis, Inc. Kinase modulators and method of use
WO2009032694A1 (en) 2007-08-28 2009-03-12 Dana Farber Cancer Institute Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis
PT2725028T (pt) 2008-10-22 2016-08-31 Array Biopharma Inc Compostos de pirazolo[1,5-]pirimidina substituídos como intermediários na síntese de inibidores de cinase trk
AR077468A1 (es) * 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
CA2761074A1 (en) 2010-05-05 2011-11-10 Vertex Pharmaceuticals Incorporated 4 substituted pyrazolopyrimidines useful as pkc-theta inhibitors
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors
CN102241678B (zh) * 2011-04-26 2014-10-29 辽宁利锋科技开发有限公司 含有脂环结构化合物的抗肿瘤作用与应用
DK2872491T3 (da) 2012-07-11 2021-08-09 Blueprint Medicines Corp Inhibitorer af fibroblastvækstfaktorreceptoren
EP2890815B1 (en) 2012-08-31 2019-03-20 The Regents of the University of Colorado Methods for diagnosis and treatment of cancer
AU2013326867B2 (en) * 2012-10-05 2018-03-08 Rigel Pharmaceuticals, Inc. GDF-8 inhibitors
CA2890207A1 (en) * 2012-11-05 2014-05-08 Foundation Medicine, Inc. Novel ntrk1 fusion molecules and uses thereof
TWI629266B (zh) 2012-12-28 2018-07-11 藍印藥品公司 纖維母細胞生長因子受體之抑制劑
CN105377845B (zh) 2013-02-01 2017-11-24 拜耳制药股份公司 取代的吡唑并嘧啶基氨基‑吲唑类
CN103965199B (zh) 2013-02-02 2017-07-07 广东东阳光药业有限公司 一种芳杂环化合物、包含它的药物组合物及其用途
WO2014130375A1 (en) * 2013-02-21 2014-08-28 Calitor Sciences, Llc Heteroaromatic compounds as pi3 kinase modulators
US10035801B2 (en) * 2013-03-13 2018-07-31 Genentech, Inc. Pyrazolo compounds and uses thereof
US9499522B2 (en) 2013-03-15 2016-11-22 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
GB2515785A (en) 2013-07-03 2015-01-07 Redx Pharma Ltd Compounds
US9334263B2 (en) 2013-10-17 2016-05-10 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
DK3057969T3 (en) 2013-10-17 2018-09-24 Blueprint Medicines Corp COMPOSITIONS USED FOR TREATMENT OF DISEASES RELATED TO ENZYMETE KIT
EP3060560A1 (en) 2013-10-25 2016-08-31 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
WO2015108328A1 (ko) * 2014-01-14 2015-07-23 주식회사 엘지생명과학 대장암 마커로서의 신규 ntrk1 융합유전자 및 이의 용도
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
US10233170B2 (en) * 2014-04-08 2019-03-19 Rigel Pharmaceuticals, Inc. 2,3-disubstituted pyridine compounds as TGF-beta inhibitors and methods of use
WO2016022569A1 (en) 2014-08-04 2016-02-11 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
US9701681B2 (en) 2014-12-15 2017-07-11 Cmg Pharmaceutical Co., Ltd. Fused ring heteroaryl compounds and their use as Trk inhibitors
US10202365B2 (en) 2015-02-06 2019-02-12 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors
US9981944B2 (en) * 2015-02-20 2018-05-29 Rigel Pharmaceuticals, Inc GDF-8 inhibitors
AU2016297754A1 (en) 2015-07-24 2018-02-15 Blueprint Medicines Corporation Compounds useful for treating disorders related to KIT and PDGFR
CA2995997A1 (en) 2015-08-26 2017-03-02 Blueprint Medicines Corporation Compounds and compositions useful for treating disorders related to ntrk
LT3371171T (lt) 2015-11-02 2024-01-10 Blueprint Medicines Corporation Ret inhibitoriai
SG10201912607SA (en) 2015-11-19 2020-02-27 Blueprint Medicines Corp Compounds and compositions useful for treating disorders related to ntrk
US10183928B2 (en) 2016-03-17 2019-01-22 Blueprint Medicines Corporation Inhibitors of RET
HUE063042T2 (hu) 2016-04-15 2023-12-28 Blueprint Medicines Corp Az aktivin receptorszerû kináz inhibitorai
WO2018017983A1 (en) 2016-07-22 2018-01-25 Blueprint Medicines Corporation Compounds useful for treating disorders related to ret
US10035789B2 (en) 2016-07-27 2018-07-31 Blueprint Medicines Corporation Compounds useful for treating disorders related to RET
US20190192522A1 (en) 2016-09-08 2019-06-27 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor 4 in combination with cyclin-dependent kinase inhibitors
CN107844168B (zh) 2017-11-23 2020-12-01 英业达科技有限公司 主板组件及其卡扣装置

Also Published As

Publication number Publication date
KR20180081790A (ko) 2018-07-17
BR112018010024A8 (pt) 2019-02-26
JP2019500328A (ja) 2019-01-10
ZA201803530B (en) 2021-08-25
CA3005741A1 (en) 2017-05-26
HK1259453A1 (zh) 2019-11-29
EP3377497A1 (en) 2018-09-26
WO2017087778A1 (en) 2017-05-26
AU2016355196A1 (en) 2018-06-21
US11059827B2 (en) 2021-07-13
RU2018122089A3 (es) 2019-12-30
RU2018122089A (ru) 2019-12-25
SG10201912607SA (en) 2020-02-27
PH12018501065A1 (en) 2019-01-28
US20170145018A1 (en) 2017-05-25
TWI733713B (zh) 2021-07-21
MX2018006195A (es) 2018-09-05
US20190382410A1 (en) 2019-12-19
IL259164A (en) 2018-06-28
BR112018010024A2 (pt) 2018-11-21
US10370379B2 (en) 2019-08-06
SG11201803920TA (en) 2018-06-28
TW201720826A (zh) 2017-06-16
CN108431008A (zh) 2018-08-21

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