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PE20120506A1 - Derivados de pirazolopiridina como inhibidores de quinasas - Google Patents

Derivados de pirazolopiridina como inhibidores de quinasas

Info

Publication number
PE20120506A1
PE20120506A1 PE2011001662A PE2011001662A PE20120506A1 PE 20120506 A1 PE20120506 A1 PE 20120506A1 PE 2011001662 A PE2011001662 A PE 2011001662A PE 2011001662 A PE2011001662 A PE 2011001662A PE 20120506 A1 PE20120506 A1 PE 20120506A1
Authority
PE
Peru
Prior art keywords
methyl
pyridin
amine
cycloalkyl
kinase inhibitors
Prior art date
Application number
PE2011001662A
Other languages
English (en)
Inventor
Edward Giles Mciver
Ela Smiljanic
Denise Jamilla Harding
Joanne Hough
Original Assignee
Medical Res Council Technology
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
Priority claimed from GB0904746A external-priority patent/GB0904746D0/en
Priority claimed from GB0912238A external-priority patent/GB0912238D0/en
Priority claimed from GBGB1001418.1A external-priority patent/GB201001418D0/en
Application filed by Medical Res Council Technology filed Critical Medical Res Council Technology
Publication of PE20120506A1 publication Critical patent/PE20120506A1/es

Links

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
    • C07D471/02—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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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 two hetero rings
    • C07D401/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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 Table
    • 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
    • C07F9/65611—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 containing the ring system (X = CH2, O, S, NH) optionally with an additional double bond and/or substituents, e.g. penicillins and analogs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

REFERIDA A UN DERIVADO DE PIRAZOLOPIRIDINA DE FORMULA (I), DONDE R1 ES HETEROCICLOALQUILO C4-C7, NHR3, OR3, OH, ENTRE OTROS; R2 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, CICLOALQUILO C3-C7, ENTRE OTROS; R3 ES HETEROCICLOALQUILO C4-C7, CICLOALQUILO C3-C7, ARILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (4-CLORO-BENCIL)-(3-METIL-1H-PIRAZOLO[4,3-c]PIRIDIN-4-IL)-AMINA, CICLOHEXIL-(3-METIL-1H-PIRAZOLO[4,3-c]PIRIDIN-4-IL)-AMINA, (3-METIL-1H-PIRAZOLO[4,3-c]PIRIDIN-4-IL)-(1-METIL-1H-PIRAZOL-3-IL)-AMINA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN PROCESO DE PREPARACION. DICHOS COMPUESTOS INHIBEN UNA O MAS QUINASAS, PARTICULARMENTE, LRRK2 Y SON UTILES EN EL TRATAMIENTO DE DEL CANCER, ENFERMEDADES NEURODEGENERATIVAS, ENTRE OTROS
PE2011001662A 2009-03-19 2010-03-19 Derivados de pirazolopiridina como inhibidores de quinasas PE20120506A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0904746A GB0904746D0 (en) 2009-03-19 2009-03-19 Compounds
US16202409P 2009-03-20 2009-03-20
GB0912238A GB0912238D0 (en) 2009-07-14 2009-07-14 Compounds
GBGB1001418.1A GB201001418D0 (en) 2010-01-28 2010-01-28 Compounds

Publications (1)

Publication Number Publication Date
PE20120506A1 true PE20120506A1 (es) 2012-05-14

Family

ID=42226628

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2011001662A PE20120506A1 (es) 2009-03-19 2010-03-19 Derivados de pirazolopiridina como inhibidores de quinasas

Country Status (13)

Country Link
US (2) US20100317646A1 (es)
EP (1) EP2408772B1 (es)
JP (1) JP5732036B2 (es)
KR (1) KR101700229B1 (es)
CN (1) CN102428084B (es)
AU (1) AU2010224693B2 (es)
CA (1) CA2754605C (es)
CL (1) CL2011002267A1 (es)
IL (1) IL215147A0 (es)
MX (1) MX2011009807A (es)
PE (1) PE20120506A1 (es)
RU (1) RU2011142182A (es)
WO (1) WO2010106333A1 (es)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2057125T3 (da) * 2006-08-16 2011-05-16 Hoffmann La Roche Ikke-nucleosid revers transkriptase-inhibitorer
GB201008134D0 (en) * 2010-05-14 2010-06-30 Medical Res Council Technology Compounds
GB201015949D0 (en) 2010-09-22 2010-11-03 Medical Res Council Technology Compounds
US9233977B2 (en) * 2010-10-29 2016-01-12 Merck Sharp & Dohme Corp. Leucine-rich repeat kinase enzyme activity
EP2680695A4 (en) * 2011-02-28 2014-09-10 Merck Sharp & Dohme COMPOUNDS FOR INHIBITING THE REPEATING ACTIVITY OF A LEUKINARY KINASEENZYME
WO2012135631A1 (en) 2011-03-30 2012-10-04 Arrien Pharmaeuticals Llc Substituted 5-(pyrazin-2-yl)-1h-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors
AU2012244549B2 (en) * 2011-04-21 2017-04-20 Origenis Gmbh Heterocyclic compounds as kinase inhibitors
AU2012258977A1 (en) * 2011-05-23 2014-01-16 Imago Pharmaceuticals, Inc. Inhibitors of LRRK2 kinase activity
CN102558174B (zh) * 2011-08-23 2014-03-19 天津市斯芬克司药物研发有限公司 一种全新吡唑并[4,3-c]吡啶化合物的发明及其合成方法
AU2012314035B2 (en) * 2011-09-30 2016-12-15 Oncodesign S.A. Macrocyclic LRRK2 kinase inhibitors
GB201204985D0 (en) 2012-03-21 2012-05-02 Genentech Inc Compounds
WO2013182612A1 (en) 2012-06-07 2013-12-12 Bayer Pharma Aktiengesellschaft Glucose transport inhibitors
EP3255049A1 (en) * 2012-06-29 2017-12-13 Pfizer Inc Novel 4-(substituted-amino)-7h-pyrrolo[2,3-d]pyrimidines as lrrk2 inhibitors
WO2014026330A1 (en) * 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. 3-AMINOCYCLOALKYL COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
WO2014060113A1 (en) 2012-10-19 2014-04-24 Origenis Gmbh Novel kinase inhibitors
CA2887887C (en) 2012-10-31 2020-08-25 Raqualia Pharma Inc. Pyrazolopyridine derivatives as ttx-s blockers
MX2015005506A (es) * 2012-11-08 2015-08-05 Pfizer Compuestos heteroaromaticos como ligandos d1 de dopamina.
US9045477B2 (en) * 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
WO2014150981A1 (en) * 2013-03-15 2014-09-25 Elan Pharmaceuticals, Llc Inhibitors of lrrk2 kinase activity
TW201533043A (zh) * 2013-04-18 2015-09-01 Lundbeck & Co As H 作爲ｌｒｒｋ２抑制劑的芳基吡咯并吡啶衍生化合物
AR096654A1 (es) 2013-06-20 2016-01-27 Ab Science Derivados de benzimidazol como inhibidores selectivos de proteína quinasa
WO2015026683A1 (en) * 2013-08-22 2015-02-26 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
ES2663622T3 (es) 2013-12-17 2018-04-16 Pfizer Inc. Novedosas 1H-pirrolo[2,3-b]piridinas 3,4-disustituidas y 7H-pirrolo[2,3-c]piridacinas 4,5-disustituidas como inhibidores de LRRK2
EP3134405B1 (en) 2014-04-25 2019-08-28 Pfizer Inc Heteroaromatic compounds and their use as dopamine d1 ligands
MX2016014878A (es) * 2014-05-14 2017-03-08 Pfizer Pirazolopiridinas y pirazolopirimidinas.
EP3190889B1 (en) 2014-09-03 2021-11-17 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
MX377305B (es) 2015-09-14 2025-03-07 Pfizer DERIVADOS DE IMIDAZO[4,5-c]QUINOLINA E IMIDAZO[4,5-c][1,5]NAFTIRIDINA NOVEDOSOS COMO INHIBIDORES DE LRRK2.
EP3472171B1 (en) 2016-06-15 2025-04-23 Suzhou Yabao Pharmaceutical R&D Co., Ltd. Substituted tricyclic herteocyclic compounds and use thereof
CN110678182B (zh) 2017-02-24 2022-08-23 大邱庆北尖端医疗产业振兴财团 含有能够穿透血脑屏障的化合物作为预防或治疗脑癌的有效成分的药物组合物
WO2019134985A1 (en) 2018-01-08 2019-07-11 F. Hoffmann-La Roche Ag Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors
KR101990738B1 (ko) * 2018-07-24 2019-06-19 재단법인 대구경북첨단의료산업진흥재단 혈액 뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 뇌암의 예방 또는 치료용 약학적 조성물
CN114760994A (zh) * 2019-12-04 2022-07-15 艾库斯生物科学有限公司 HIF-2α的抑制剂
PE20230838A1 (es) 2020-06-22 2023-05-19 Hoffmann La Roche Derivados de sulfona
IL299664A (en) 2020-09-03 2023-03-01 Hoffmann La Roche Heterocyclic compounds
TWI846353B (zh) * 2022-02-25 2024-06-21 大陸商蘇州亞寶藥物研發有限公司 取代的稠環化合物及其藥物組合物、製備方法和用途

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3835144A (en) * 1972-06-16 1974-09-10 Squibb & Sons Inc Amino derivatives of (4,3-c pyrazolopyridine cabroxylic acids and esters
NZ207394A (en) 1983-03-08 1987-03-06 Commw Serum Lab Commission Detecting or determining sequence of amino acids
US5478830A (en) * 1992-05-29 1995-12-26 The Du Pont Merck Pharmaceutical Company Fused-ring heterocycles for the treatment of atherosclerosis
US5300478A (en) * 1993-01-28 1994-04-05 Zeneca Limited Substituted fused pyrazolo compounds
CN1656079A (zh) * 2002-05-31 2005-08-17 卫材株式会社 吡唑化合物和含有该化合物的药物组合物
US7186716B2 (en) * 2002-08-12 2007-03-06 Sugen, Inc. 3-Pyrrol-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors
US7348338B2 (en) * 2003-07-17 2008-03-25 Plexxikon, Inc. PPAR active compounds
JP2007501229A (ja) * 2003-08-06 2007-01-25 スゲン，インコーポレイティド 強力なプロテインキナーゼ阻害剤としての幾何学的に束縛された３−シクロペンチリデン−１，３−ジヒドロインドール−２−オン類
WO2005121094A1 (en) * 2004-06-09 2005-12-22 Pfizer Limited Piperazine and piperidine derivatives as anti-hiv-agents
WO2006009245A1 (ja) * 2004-07-23 2006-01-26 Tanabe Seiyaku Co., Ltd. 含窒素縮合二環式化合物
PE20061119A1 (es) * 2005-01-19 2006-11-27 Aventis Pharma Sa PIRAZOLO PIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE CINASAS FAK, KDR Y Tie
CA2641219A1 (en) * 2006-01-31 2007-08-09 Elan Pharmaceuticals, Inc. Alpha-synuclein kinase
AU2007245129A1 (en) * 2006-03-29 2007-11-08 Foldrx Pharmaceuticals, Inc. Inhibition of alpha-synuclein toxicity
AP2739A (en) * 2008-09-26 2013-09-30 Boehringer Ingelheim Int Azaindazole compounds as CCRI receptor antagonists
GB201015949D0 (en) * 2010-09-22 2010-11-03 Medical Res Council Technology Compounds

Also Published As

Publication number Publication date
US20170320870A1 (en) 2017-11-09
IL215147A0 (en) 2011-12-29
WO2010106333A1 (en) 2010-09-23
AU2010224693B2 (en) 2016-07-28
CN102428084A (zh) 2012-04-25
JP2012520861A (ja) 2012-09-10
KR20110128925A (ko) 2011-11-30
JP5732036B2 (ja) 2015-06-10
CN102428084B (zh) 2016-05-18
AU2010224693A1 (en) 2011-09-15
US20100317646A1 (en) 2010-12-16
EP2408772B1 (en) 2015-07-01
CA2754605C (en) 2018-04-17
RU2011142182A (ru) 2013-04-27
EP2408772A1 (en) 2012-01-25
MX2011009807A (es) 2011-09-29
CL2011002267A1 (es) 2012-05-11
KR101700229B1 (ko) 2017-01-26
CA2754605A1 (en) 2010-09-23

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