MX2016012668A - Derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirazina sustituidos y derivados de 5,6,7,8-tetrahidro-4h-pirazolo[1,5-a][1 ,4]diazepina como inhibidores de ros1. - Google Patents

Derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirazina sustituidos y derivados de 5,6,7,8-tetrahidro-4h-pirazolo[1,5-a][1 ,4]diazepina como inhibidores de ros1.

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Publication number
MX2016012668A
MX2016012668A MX2016012668A MX2016012668A MX2016012668A MX 2016012668 A MX2016012668 A MX 2016012668A MX 2016012668 A MX2016012668 A MX 2016012668A MX 2016012668 A MX2016012668 A MX 2016012668A MX 2016012668 A MX2016012668 A MX 2016012668A
Authority
MX
Mexico
Prior art keywords
pyrazolo
tetrahydro
derivatives
substituted
diazepine
Prior art date
Application number
MX2016012668A
Other languages
English (en)
Other versions
MX367914B (es
Inventor
Lieven Meerpoel
Sophie Descamps
Laurence Anne Mevellec
Elisabeth Thérèse Jeanne Pasquier
Jorge Eduardo Vialard
Wroblowski Berthold
Ludovic JEANTY Matthieu
François Alain Jean JOUSSEAUME Thierry
Jean Maurice MERCEY Guillaume
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 MX2016012668A publication Critical patent/MX2016012668A/es
Publication of MX367914B publication Critical patent/MX367914B/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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-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
    • A61K31/495—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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
    • C07D487/10—Spiro-condensed systems
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Abstract

La presente invención se refiere a derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirazina sustituidos y a derivados de 5,6,7,8-tetrahidro-4H-pirazolo[1,5-a][1,4]diazepina de fórmula (I) (ver Fórmula) donde las variables tienen el significado definido en las reivindicaciones; los compuestos de acuerdo con la presente invención son útiles como inhibidores de 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.
MX2016012668A 2014-03-27 2015-03-26 Derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirazina sustituidos y derivados de 5,6,7,8-tetrahidro-4h-pirazolo[1,5-a][1 ,4]diazepina como inhibidores de ros1. MX367914B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14161950 2014-03-27
PCT/EP2015/056498 WO2015144799A1 (en) 2014-03-27 2015-03-26 SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRAZINE DERIVATIVES AND 5,6,7,8-TETRAHYDRO-4H-PYRAZOLO[1,5-a][1,4]DIAZEPINE DERIVATIVES AS ROS1 INHIBITORS

Publications (2)

Publication Number Publication Date
MX2016012668A true MX2016012668A (es) 2016-12-14
MX367914B MX367914B (es) 2019-09-11

Family

ID=50389872

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016012668A MX367914B (es) 2014-03-27 2015-03-26 Derivados de 4,5,6,7-tetrahidro-pirazolo[1,5-a]pirazina sustituidos y derivados de 5,6,7,8-tetrahidro-4h-pirazolo[1,5-a][1 ,4]diazepina como inhibidores de ros1.

Country Status (13)

Country Link
US (1) US10280170B2 (es)
EP (1) EP3129376B1 (es)
JP (1) JP6522646B2 (es)
KR (1) KR102455519B1 (es)
CN (1) CN106164076B (es)
AU (1) AU2015238296B2 (es)
BR (1) BR112016022105B1 (es)
CA (1) CA2940918C (es)
EA (1) EA032255B1 (es)
ES (1) ES2715676T3 (es)
IL (1) IL247947B (es)
MX (1) MX367914B (es)
WO (1) WO2015144799A1 (es)

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JP6116782B1 (ja) * 2015-08-28 2017-04-19 積水メディカル株式会社 ベンジル化合物
TWI782056B (zh) 2017-07-14 2022-11-01 日商鹽野義製藥股份有限公司 具有ｍｇａｔ２抑制活性的縮合環衍生物
WO2019233456A1 (zh) * 2018-06-08 2019-12-12 贝达药业股份有限公司 Erk抑制剂及其应用
MX2021008050A (es) * 2019-01-11 2021-08-05 Shionogi & Co Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2).
JP7068743B2 (ja) * 2019-01-11 2022-05-17 塩野義製薬株式会社 Ｍｇａｔ２阻害活性を有する縮合環誘導体を含有する医薬組成物
WO2020188015A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
AU2020378630A1 (en) 2019-11-08 2022-05-26 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2022072634A1 (en) * 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Bicyclic compounds for use in the treatment cancer
CN114315866B (zh) * 2020-09-30 2023-10-31 烟台药物研究所 一种盐酸左旋咪唑的合成方法
CN116744926A (zh) * 2020-12-15 2023-09-12 北京原基华毅生物科技有限公司 作为酪蛋白激酶抑制剂的化合物
CN114957259A (zh) * 2021-02-25 2022-08-30 南京明德新药研发有限公司 氰基取代的芳香双环类化合物及其应用

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US5356897A (en) 1991-09-09 1994-10-18 Fujisawa Pharmaceutical Co., Ltd. 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines
AU2003227437A1 (en) 2002-04-23 2003-11-10 Shionogi And Co., Ltd. PYRAZOLO(1,5-a)PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
KR101050700B1 (ko) 2002-08-26 2011-07-20 다케다 야쿠힌 고교 가부시키가이샤 칼슘 수용체 조절 화합물 및 이의 용도
BR0317430A (pt) * 2002-12-20 2005-10-25 Pharmacia Corp Compostos inibidores de quinase-2 de proteìna ativada por quinase de proteìna ativada por mitógeno
JP2005343889A (ja) * 2004-05-06 2005-12-15 Taisho Pharmaceut Co Ltd イミダゾピリジン誘導体
JP2011506465A (ja) * 2007-12-12 2011-03-03 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー 殺菌性二環式ピラゾール
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EA018282B1 (ru) 2008-04-07 2013-06-28 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназы
EP2300469B1 (en) * 2008-05-13 2015-06-24 Novartis AG Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors
WO2010138576A1 (en) * 2009-05-27 2010-12-02 Abbott Laboratories Pyrimidine inhibitors of kinase activity
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Also Published As

Publication number Publication date
CN106164076B (zh) 2019-03-26
JP6522646B2 (ja) 2019-05-29
AU2015238296A1 (en) 2016-09-08
KR102455519B1 (ko) 2022-10-14
CA2940918C (en) 2023-10-24
CN106164076A (zh) 2016-11-23
WO2015144799A1 (en) 2015-10-01
EP3129376A1 (en) 2017-02-15
ES2715676T3 (es) 2019-06-05
IL247947B (en) 2019-03-31
US10280170B2 (en) 2019-05-07
EP3129376B1 (en) 2018-12-26
AU2015238296B2 (en) 2018-10-18
JP2017508779A (ja) 2017-03-30
BR112016022105B1 (pt) 2023-01-31
EA201691930A1 (ru) 2017-02-28
KR20160137576A (ko) 2016-11-30
BR112016022105A2 (es) 2017-08-15
CA2940918A1 (en) 2015-10-01
US20170174690A1 (en) 2017-06-22
MX367914B (es) 2019-09-11
EA032255B1 (ru) 2019-04-30

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