MX2012006822A - 1,7-diazacarbazoles y metodos de uso. - Google Patents

1,7-diazacarbazoles y metodos de uso.

Info

Publication number
MX2012006822A
MX2012006822A MX2012006822A MX2012006822A MX2012006822A MX 2012006822 A MX2012006822 A MX 2012006822A MX 2012006822 A MX2012006822 A MX 2012006822A MX 2012006822 A MX2012006822 A MX 2012006822A MX 2012006822 A MX2012006822 A MX 2012006822A
Authority
MX
Mexico
Prior art keywords
cancer
compounds
useful
treatment
methods
Prior art date
Application number
MX2012006822A
Other languages
English (en)
Other versions
MX349550B (es
Inventor
Hazel Joan Dyke
Karen Williams
Huifen Chen
Joy Drobnick
Charles Ellwood
Lewis J Gazzard
Simon Goodacre
Samuel Kintz
Calum Macleod
Joseph P Lyssikatos
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MX2012006822A publication Critical patent/MX2012006822A/es
Publication of MX349550B publication Critical patent/MX349550B/es

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Classifications

    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring 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

Abstract

La invención se refiere a compuestos 1,7-diazacarbazol de la Fórmula ((I), (I-a) y ((I-b) que son útiles como inhibidores de cinasa, más específicamente útiles como inhibidores de cinasa reguladora de ciclo celular 1 (chk1 = checkpoint kinase 1), de esta manera útiles como agentes terapéuticos de cáncer. La invención también se refiere a composiciones, más específicamente a composiciones farmacéuticas que comprenden estos compuestos y métodos de uso de los mismos para tratar diversas formas de cáncer y desórdenes hiperproliferativos, así como métodos para utilizar los compuestos para diagnóstico o tratamiento in vitro, in situ, e in vivo de células de mamífero, o condiciones patológicas asociadas.
MX2012006822A 2009-12-16 2010-12-15 1,7-diazacarbazoles y metodos de uso. MX349550B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US28441409P 2009-12-16 2009-12-16
US28770209P 2009-12-17 2009-12-17
PCT/EP2010/069771 WO2011073263A1 (en) 2009-12-16 2010-12-15 1, 7 - diazacarbazoles and their use in the treatment of cancer

Publications (2)

Publication Number Publication Date
MX2012006822A true MX2012006822A (es) 2012-08-17
MX349550B MX349550B (es) 2017-08-02

Family

ID=43535586

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012006822A MX349550B (es) 2009-12-16 2010-12-15 1,7-diazacarbazoles y metodos de uso.

Country Status (9)

Country Link
US (3) US20110183938A1 (es)
EP (1) EP2513110B1 (es)
JP (1) JP5814931B2 (es)
KR (1) KR101496273B1 (es)
CN (1) CN102791711A (es)
BR (1) BR112012014652A2 (es)
CA (1) CA2782213C (es)
MX (1) MX349550B (es)
WO (1) WO2011073263A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110183938A1 (en) 2009-12-16 2011-07-28 Genentech, Inc. 1,7-diazacarbazoles and methods of use
MA37975B2 (fr) 2012-09-11 2021-03-31 Genzyme Corp Inhibiteurs de synthase de glucosylcéramide
CN105764501A (zh) 2013-07-26 2016-07-13 现代化制药公司 改善比生群治疗效益的组合物
EP3055308B1 (en) 2013-10-08 2017-11-22 F.Hoffmann-La Roche Ag Diazacarbazole derivatives as tau-pet-ligands
CN103755628B (zh) * 2014-01-27 2015-07-29 河北科技大学 2-氨基-3-碘-5-溴吡啶的合成方法
WO2015115339A1 (ja) * 2014-01-30 2015-08-06 住友化学株式会社 ピリジン化合物の製造方法
CN104744353B (zh) * 2015-03-31 2017-11-24 山东友帮生化科技有限公司 2‑氨基‑3‑碘‑5‑氯吡啶的合成方法
BR112019004091B1 (pt) 2016-09-09 2023-02-14 F. Hoffmann-La Roche Ag Processo para a preparação de 2-(6-nitropiridin-3-il)-9h-dipirido[2,3-b;3', 4'-d]pirrol
EP3860996A4 (en) 2018-10-02 2022-08-31 Northwestern University BETA-CARBOLINES AS POSITIVE ALLOSTERIC MODULATORS OF HUMAN SEROTONIN RECEPTOR 2C (5-HT2C)
IL300090A (en) 2020-07-24 2023-03-01 Genzyme Corp Pharmaceutical preparations containing VENGLUSTAT

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1268477B1 (en) * 2000-03-15 2010-04-21 Sanofi-Aventis Deutschland GmbH Substituted beta-carbolines with ikb-kinase inhibiting activity
JP5000828B2 (ja) * 2000-03-15 2012-08-15 サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング ＩｋＢキナーゼ阻害活性を有する置換ベーターカルボリン
GB0121941D0 (en) 2001-09-11 2001-10-31 Astrazeneca Ab Chemical compounds
WO2003039545A2 (en) 2001-11-07 2003-05-15 Millennium Pharmaceuticals, Inc. Carboline derivatives as inhibitors of ikb in the treatment of multiple myeloma and others cancers
MXPA05008688A (es) * 2003-02-17 2005-10-05 Pharmacia Italia Spa Derivados tetraciclicos de pirazol como inhibidores de la cinasa, procedimiento para su preparacion y composiciones farmaceuticas que los comprenden.
AR049300A1 (es) * 2004-06-15 2006-07-12 Schering Corp Compuestos triciclicos antagonistas de mglur1 como agentes terapeuticos
SE0401655D0 (sv) 2004-06-24 2004-06-24 Astrazeneca Ab New compounds
US8119655B2 (en) * 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP2081930A2 (en) 2006-10-09 2009-07-29 Takeda San Diego, Inc. Kinase inhibitors
KR20090068277A (ko) 2006-10-09 2009-06-25 다케다 야쿠힌 고교 가부시키가이샤 키나아제 억제제
DE102006062203A1 (de) * 2006-12-22 2008-06-26 Curacyte Discovery Gmbh Substituierte 5H-Pyrimido[5,4-b]indole als Induktoren der Apoptose bei B-CLL Zellen
MX2009009304A (es) 2007-03-01 2009-11-18 Novartis Ag Inhibidores de cinasa pim y metodos para su uso.
WO2009004329A1 (en) * 2007-07-02 2009-01-08 Cancer Research Technology Limited 9h-pyrimido[4,5-b]indoles, 9h-pyrido[4',3':4,5]pyrrolo[2,3-d]pyridines, and 9h-1,3,6,9-tetraaza-fluorenes as chk1 kinase function inhibitors
JP2009151598A (ja) * 2007-12-21 2009-07-09 Duaxes Corp 試験装置
WO2009129401A1 (en) 2008-04-16 2009-10-22 Takeda Pharmaceutical Company Limited Kinase inhibitors
US8501765B2 (en) * 2008-06-11 2013-08-06 Genentech, Inc. Diazacarbazoles and methods of use
AR072084A1 (es) * 2008-06-12 2010-08-04 Sanofi Aventis Derivados de azacarbolinas, su preparacion y su utilizacion terapeutica como inhibidores de las quinasas pim
WO2010015589A1 (en) 2008-08-05 2010-02-11 Nycomed Gmbh Benzyl-substituted tetracyclic heterocyclic compounds as pde5 inhibitors
EP2411389A2 (fr) * 2009-03-24 2012-02-01 Sanofi DERIVES D'AZACARBOLINES 9H-PYRROLO[2,3-b:5,4-c']DIPYRIDINE, LEUR PREPARATION ET LEUR UTILISATION THERAPEUTIQUE
US20110183938A1 (en) 2009-12-16 2011-07-28 Genentech, Inc. 1,7-diazacarbazoles and methods of use

Also Published As

Publication number Publication date
CN102791711A (zh) 2012-11-21
RU2012127877A (ru) 2014-01-27
WO2011073263A1 (en) 2011-06-23
CA2782213C (en) 2014-10-28
JP2013514315A (ja) 2013-04-25
EP2513110A1 (en) 2012-10-24
JP5814931B2 (ja) 2015-11-17
US9440976B2 (en) 2016-09-13
KR20120103705A (ko) 2012-09-19
BR112012014652A2 (pt) 2020-09-15
MX349550B (es) 2017-08-02
US20140171407A1 (en) 2014-06-19
US20110183938A1 (en) 2011-07-28
US20150328195A1 (en) 2015-11-19
CA2782213A1 (en) 2011-06-23
KR101496273B1 (ko) 2015-02-26
EP2513110B1 (en) 2018-12-05

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