MX367913B - Derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirimidina y 2,3-dihidro-1h-imidazo[1,2-b]pirazol sustituidos como inhibidores de ros1. - Google Patents

Derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirimidina y 2,3-dihidro-1h-imidazo[1,2-b]pirazol sustituidos como inhibidores de ros1.

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Publication number
MX367913B
MX367913B MX2016012669A MX2016012669A MX367913B MX 367913 B MX367913 B MX 367913B MX 2016012669 A MX2016012669 A MX 2016012669A MX 2016012669 A MX2016012669 A MX 2016012669A MX 367913 B MX367913 B MX 367913B
Authority
MX
Mexico
Prior art keywords
derivatives
pyrazolo
imidazo
tetrahydro
dihydro
Prior art date
Application number
MX2016012669A
Other languages
English (en)
Other versions
MX2016012669A (es
Inventor
Laurence Anne Mevellec
Ludovic JEANTY Matthieu
François Alain Jean JOUSSEAUME Thierry
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of MX2016012669A publication Critical patent/MX2016012669A/es
Publication of MX367913B publication Critical patent/MX367913B/es

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    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invención se refiere a derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirimidina sustituidos y derivados de 2,3-dihidro-1H-imidazo[1,2-b]pirazol de fórmula (I) (ver Fórmula) y también a compuestos de fórmula (I') (ver Fórmula) en donde las variables tienen el significado definido en las reivindicaciones; los compuestos de acuerdo con la presente invención son útiles como inhibidores ROS1; la invención también se refiere a procesos para preparar tales compuestos novedosos, a composiciones farmacéuticas que comprenden dichos compuestos como principio activo, así como al uso de dichos compuestos como un medicamento.
MX2016012669A 2014-03-27 2015-03-26 Derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirimidina y 2,3-dihidro-1h-imidazo[1,2-b]pirazol sustituidos como inhibidores de ros1. MX367913B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14161959 2014-03-27
PCT/EP2015/056501 WO2015144801A1 (en) 2014-03-27 2015-03-26 SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AND 2,3-DIHYDRO-1H-IMIDAZO[1,2-b]PYRAZOLE DERIVATIVES AS ROS1 INHIBITORS

Publications (2)

Publication Number Publication Date
MX2016012669A MX2016012669A (es) 2016-12-14
MX367913B true MX367913B (es) 2019-09-11

Family

ID=50389875

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016012669A MX367913B (es) 2014-03-27 2015-03-26 Derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirimidina y 2,3-dihidro-1h-imidazo[1,2-b]pirazol sustituidos como inhibidores de ros1.

Country Status (13)

Country Link
US (1) US10342795B2 (es)
EP (1) EP3126366B1 (es)
JP (1) JP6527167B2 (es)
KR (1) KR102455518B1 (es)
CN (1) CN106132967B (es)
AU (1) AU2015238298B2 (es)
BR (1) BR112016021507B1 (es)
CA (1) CA2941206C (es)
EA (1) EA031639B1 (es)
ES (1) ES2686747T3 (es)
IL (1) IL247948B (es)
MX (1) MX367913B (es)
WO (1) WO2015144801A1 (es)

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CN107737125A (zh) * 2016-11-26 2018-02-27 王玉美 一种治疗药物流产后子宫出血的药物
CN106866536A (zh) * 2017-04-12 2017-06-20 中国农业大学 一种制备4‑卤代‑5‑氨基吡唑的方法
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
CN111087398A (zh) * 2019-12-24 2020-05-01 上海万巷制药有限公司 一种制备拉罗替尼中间体的清洁工艺
JP2023511302A (ja) 2020-01-13 2023-03-17 アプタバイオ セラピューティクス インコーポレイテッド 新規なピラゾール誘導体
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN113416140B (zh) * 2021-06-03 2023-01-13 万华化学集团股份有限公司 一种制备2-甲基戊二胺的方法

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US5356897A (en) * 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
GB9204464D0 (en) * 1992-03-02 1992-04-15 Fujisawa Pharmaceutical Co New heterocyclic derivatives
WO2003091256A1 (fr) 2002-04-23 2003-11-06 Shionogi & Co., Ltd. Derive de pyrazolo[1,5-a]pyrimidine et inhibiteur de la nad(p)h oxydase contenant ledit derive
KR101050700B1 (ko) 2002-08-26 2011-07-20 다케다 야쿠힌 고교 가부시키가이샤 칼슘 수용체 조절 화합물 및 이의 용도
UA80295C2 (en) * 2002-09-06 2007-09-10 Biogen Inc Pyrazolopyridines and using the same
AU2003301226A1 (en) 2002-12-20 2004-07-22 Pharmacia Corp Acyclic pyrazole compounds for the inhibition of mitogen activated protein kinase-activated protein kinase-2
WO2009086129A1 (en) 2007-12-21 2009-07-09 Wyeth Pyrazolo [1,5-a] pyrimidine compounds
US20100029657A1 (en) * 2008-02-29 2010-02-04 Wyeth Bridged, Bicyclic Heterocyclic or Spiro Bicyclic Heterocyclic Derivatives of Pyrazolo[1, 5-A]Pyrimidines, Methods for Preparation and Uses Thereof
MX2010012457A (es) 2008-05-13 2010-12-07 Irm Llc Heterociclos que contienen nitrogeno fusionado y composiciones de los mismos como inhibidores de cinasa.
ES2520991T3 (es) * 2009-05-27 2014-11-12 Abbvie Inc. Inhibidores de pirimidina de la actividad cinasa
WO2011153553A2 (en) * 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
JO3407B1 (ar) * 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
TWI585088B (zh) * 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并［１，２－ｂ］嗒衍生物

Also Published As

Publication number Publication date
EA031639B1 (ru) 2019-01-31
EP3126366B1 (en) 2018-06-06
EP3126366A1 (en) 2017-02-08
KR20160137566A (ko) 2016-11-30
US10342795B2 (en) 2019-07-09
AU2015238298B2 (en) 2019-04-18
CN106132967A (zh) 2016-11-16
MX2016012669A (es) 2016-12-14
CN106132967B (zh) 2019-05-28
EA201691934A1 (ru) 2017-01-30
AU2015238298A1 (en) 2016-09-15
IL247948B (en) 2019-03-31
ES2686747T3 (es) 2018-10-19
BR112016021507B1 (pt) 2022-10-18
JP6527167B2 (ja) 2019-06-05
WO2015144801A1 (en) 2015-10-01
JP2017508777A (ja) 2017-03-30
KR102455518B1 (ko) 2022-10-14
CA2941206C (en) 2022-09-20
CA2941206A1 (en) 2015-10-01
BR112016021507A2 (es) 2017-08-15
US20170173014A1 (en) 2017-06-22

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