AR076688A1 - Derivados de isoquinolin-1(2h)-ona - Google Patents

Derivados de isoquinolin-1(2h)-ona

Info

Publication number
AR076688A1
AR076688A1 ARP100101720A ARP100101720A AR076688A1 AR 076688 A1 AR076688 A1 AR 076688A1 AR P100101720 A ARP100101720 A AR P100101720A AR P100101720 A ARP100101720 A AR P100101720A AR 076688 A1 AR076688 A1 AR 076688A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocyclyl
heteroaryl
optionally substituted
cycloalkyl
Prior art date
Application number
ARP100101720A
Other languages
English (en)
Original Assignee
Nerviano Medical Sciences Srl
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42372343&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR076688(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Nerviano Medical Sciences Srl filed Critical Nerviano Medical Sciences Srl
Publication of AR076688A1 publication Critical patent/AR076688A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T436/00—Chemistry: analytical and immunological testing
    • Y10T436/14—Heterocyclic carbon compound [i.e., O, S, N, Se, Te, as only ring hetero atom]
    • Y10T436/145555—Hetero-N

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se proporcionan derivados de isoquinolin-1(2H)-ona sustituidos que inhiben selectivamente la actividad de poli (ADP-ribosa) polimerasa PARP-1 con respecto a poli (ADP-ribosa) polimerasa PARP-2. Por lo tanto, los compuestos de la presente son utiles para tratar enfermedades tales como cáncer, enfermedades cardiovasculares, lesiones del sistema nervioso central y diferentes formas de inflamacion. La presente también proporciona métodos para preparar estos compuestos, composiciones farmacéuticas que comprenden estos compuestos, y métodos para tratar enfermedades utilizando composiciones farmacéuticas que comprenden estos compuestos. Un método de sondeo para la identificacion de compuestos capaces de unirse a varias proteínas PARP, y también las sondas usadas en ese método, son otros objetivos de la solicitud. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1): donde L es un grupo opcionalmente sustituido C2-6 alquilo lineal o ramificado, C3-7 cicloalquilo o, incluyendo el átomo de nitrogeno al cual está unido, un heterociclilo o heterociclil C1-6 alquilo opcionalmente sustituido; R y R1 son independientemente un átomo de hidrogeno, un grupo opcionalmente sustituido C1-6 alquilo lineal o ramificado, C3-7 cicloalquilo, heterociclilo, arilo, heteroarilo o COR5 o, tomados juntos con el átomo de nitrogeno al cual están unidos, forman un grupo heterociclilo o heteroarilo opcionalmente sustituido; R2 y R3 son independientemente un átomo de hidrogeno o de halogeno; un grupo ciano, nitro, NHCOR5, COR5, NR6R7, NR6COR5, OR8, SR8, SOR11, SO2R11, NHSOR11, NHSO2R11, R9R10N-C1-6 alquilo, R9O-C1-6 alquilo, o un grupo opcionalmente sustituido C1-6 alquilo lineal o ramificado, C2-6 alquenilo, C2-6 alquinilo, C3-7 cicloalquilo, heterociclilo, arilo o heteroarilo; R4 es un grupo opcionalmente sustituido C1-6 alquilo lineal o ramificado. C3-7 cicloalquilo, C2-6 alquenilo, C2-6 alquinilo, arilo, aril C1-6 alquilo, aril C3-7 cicloalquilo, aril C2-6 alquenilo, aril C2-6 alquinilo, heterociclilo, heterociclil C1-6 alquilo, heterociclil C3-7 cicloalquilo, heterociclil C2-6 alquenilo, heterociclil C2-6 alquinilo, heteroarilo, heteroaril C1-6 alquilo, heteroaril C3-7 cicloalquilo, heteroaril C2-6 alquenilo, heteroaril C2-6 alquinilo; R5 es un átomo de hidrogeno o NR6R8, OR8, SR8, R9R10N-C1-6 alquilo, R9O- C1-6 alquilo, o un grupo opcionalmente sustituido C1-6 alquilo lineal o ramificado, C2-6 alquenilo, C2-6 alquinilo, C3-7 cicloalquilo, heterociclilo, arilo o heteroarilo; R6 y R7 son independientemente un átomo de hidrogeno, un grupo opcionalmente sustituido C1-6 alquilo lineal o ramificado, C2-6 alquenilo, C2-6 alquinilo, C3-7 cicloalquilo, R9R10N-C2-6 alquilo, R9O-C2-6 alquilo, heterociclilo, arilo o heteroarilo, o R6 y R7, tomados juntos con el átomo de nitrogeno al cual están unidos, pueden formar un grupo heterociclilo opcionalmente sustituido; R8 es hidrogeno o un grupo COR6, SOR11, SO2R11, R9R10N-C2-6 alquilo o R9O-C2-6 alquilo, o un grupo opcionalmente sustituido C1-6 alquilo lineal o ramificado, C2-6 alquenilo, C2-6 alquinilo, C3-7-, cicloalquilo, heterociclilo, arilo o heteroarilo, donde R6 es como se definio más arriba; R9 y R10 son independientemente hidrogeno, COR5, o un grupo opcionalmente sustituido C1-6 alquilo lineal o ramificado, C2-6 alquenilo, C2-6 alquinilo, C3-7 cicloalquilo, heterociclilo, arilo o heteroarilo, o R9 y R10, tomados juntos con el átomo de nitrogeno al cual están unidos, pueden formar un grupo heterociclilo opcionalmente sustituido, donde R5 es como se definio más arriba; R11 es un átomo de hidrogeno, NR6R7, OR8, R9R10N-C1-6 alquilo, R9O-C1-6 alquilo, o un grupo opcionalmente sustituido C1-6 alquilo lineal o ramificado, C2-6 alquenilo, C2-6 alquinilo, C3-7 cicloalquilo, heterociclilo, arilo o heteroarilo, donde R6, R7, R8, R9 y R10 son como se definio más arriba; o una sal farmacéuticamente aceptable del mismo.
ARP100101720A 2009-05-21 2010-05-18 Derivados de isoquinolin-1(2h)-ona AR076688A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09160869 2009-05-21

Publications (1)

Publication Number Publication Date
AR076688A1 true AR076688A1 (es) 2011-06-29

Family

ID=42372343

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101720A AR076688A1 (es) 2009-05-21 2010-05-18 Derivados de isoquinolin-1(2h)-ona

Country Status (16)

Country Link
US (2) US8592416B2 (es)
EP (1) EP2432765B1 (es)
JP (1) JP5731486B2 (es)
CN (1) CN102438986B (es)
AR (1) AR076688A1 (es)
AU (1) AU2010251112B2 (es)
BR (1) BRPI1011046B1 (es)
CA (1) CA2762226C (es)
CL (1) CL2011002925A1 (es)
DK (1) DK2432765T3 (es)
EA (1) EA023112B1 (es)
ES (1) ES2568936T3 (es)
HK (1) HK1166076A1 (es)
MX (1) MX2011012187A (es)
TW (1) TWI499418B (es)
WO (1) WO2010133647A1 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI499418B (zh) 2009-05-21 2015-09-11 Nerviano Medical Sciences Srl 異喹啉－１（２ｈ）－酮衍生物
FR2956816B1 (fr) * 2010-03-01 2012-05-18 Univ Joseph Fourier Utilisation de quinolones pour la preparation de medicaments, nouvelles quinolones et leur procede de synthese
ES2616464T3 (es) 2011-07-26 2017-06-13 Nerviano Medical Sciences S.R.L. Derivados de 3-Oxo-2,3-dihidro-1H-indazol-4-carboxamida como inhibidores de PARP-1
EA027800B1 (ru) * 2011-11-25 2017-09-29 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Производные 3-фенилизохинолин-1(2h)-она в качестве ингибиторов parp-1
ES2611504T3 (es) 2012-03-07 2017-05-09 Institute Of Cancer Research: Royal Cancer Hospital (The) Compuestos de isoquinolin-1-ona 3-aril-5-sustituida y sus usos terapéuticos
CA2881330C (en) 2012-08-08 2020-07-21 Merck Patent Gmbh (aza-)isoquinolinone derivatives
EP2900643B1 (en) 2012-09-26 2017-09-27 Merck Patent GmbH Quinazolinone derivatives as parp inhibitors
WO2014055311A1 (en) * 2012-10-01 2014-04-10 Merck Sharp & Dohme Corp. Substituted isoquinolines as crth2 receptor modulators
PT2912032T (pt) 2012-10-26 2020-09-03 Nerviano Medical Sciences Srl Derivados de 4-carboxamido-isoindolinona como inibidores seletivos de parp-1
AU2014320149A1 (en) * 2013-09-11 2016-04-07 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
CA2977685C (en) 2015-03-02 2024-02-20 Sinai Health System Homologous recombination factors
WO2017174879A1 (en) 2016-04-06 2017-10-12 University Of Oulu Compounds for use in the treatment of cancer
CN106083716B (zh) * 2016-06-07 2018-10-30 温州医科大学仁济学院 一种3-芳基异喹啉化合物的制备方法
US9891509B2 (en) * 2016-06-17 2018-02-13 Mimono LLC Projector holder
US10899733B2 (en) 2017-08-23 2021-01-26 Oregon Health & Science University Inhibitors of PARPs that catalyze mono-ADP-ribosylation
US12030867B2 (en) 2018-05-30 2024-07-09 University Of Notre Dame Du Lac Hsp90β selective inhibitors
CN113549044B (zh) * 2021-07-23 2024-01-23 中国药科大学 8-氮杂环取代色酮类衍生物及其制备方法与制药用途
WO2023242302A1 (en) 2022-06-15 2023-12-21 Astrazeneca Ab Combination therapy for treating cancer

Family Cites Families (11)

* Cited by examiner, † Cited by third party
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JPS59116269A (ja) * 1982-12-24 1984-07-05 Nisshin Flour Milling Co Ltd イソカルボスチリル誘導体
JPS60237070A (ja) * 1984-05-08 1985-11-25 Nisshin Flour Milling Co Ltd 光学活性イソカルボスチリル誘導体の製法
ES2075082T3 (es) 1989-03-28 1995-10-01 Nisshin Flour Milling Co Derivados de isoquinolina para el tratamiento del glaucoma o hipertension ocular.
JP3141051B2 (ja) 1992-10-09 2001-03-05 日清製粉株式会社 抗動脈硬化剤
SE9902268D0 (sv) * 1999-06-16 1999-06-16 Astra Ab Pharmaceutically active compounds
JP2004528376A (ja) * 2001-05-08 2004-09-16 クドス ファーマシューティカルズ リミテッド Ｐａｒｐ阻害薬としてのイソキノリノン誘導体
WO2004031171A1 (ja) * 2002-10-01 2004-04-15 Mitsubishi Pharma Corporation イソキノリン化合物及びその医薬用途
ATE540928T1 (de) * 2002-11-22 2012-01-15 Mitsubishi Tanabe Pharma Corp Isochinolinverbindungen und ihre medizinische verwendung
DE102004028973A1 (de) * 2004-06-16 2006-01-05 Sanofi-Aventis Deutschland Gmbh Substituierte Tetrahydro-2H-isochinolin-1-on-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Medikament
US8389544B2 (en) 2007-01-17 2013-03-05 The Hong Kong University Of Science And Technology Isoquinolone compounds as subtype-selective agonists for melatonin receptors MT1 and MT2
TWI499418B (zh) 2009-05-21 2015-09-11 Nerviano Medical Sciences Srl 異喹啉－１（２ｈ）－酮衍生物

Also Published As

Publication number Publication date
BRPI1011046B1 (pt) 2020-02-27
EP2432765A1 (en) 2012-03-28
US20120157454A1 (en) 2012-06-21
JP5731486B2 (ja) 2015-06-10
TW201043232A (en) 2010-12-16
EA023112B1 (ru) 2016-04-29
CN102438986B (zh) 2015-07-01
US8592416B2 (en) 2013-11-26
CN102438986A (zh) 2012-05-02
HK1166076A1 (en) 2012-10-19
US8993594B2 (en) 2015-03-31
AU2010251112B2 (en) 2015-11-12
CA2762226A1 (en) 2010-11-25
EA201171448A1 (ru) 2012-06-29
AU2010251112A2 (en) 2012-02-02
EP2432765B1 (en) 2016-03-02
BRPI1011046A2 (pt) 2016-03-15
DK2432765T3 (en) 2016-04-25
ES2568936T3 (es) 2016-05-05
MX2011012187A (es) 2012-01-27
AU2010251112A1 (en) 2012-01-19
TWI499418B (zh) 2015-09-11
CL2011002925A1 (es) 2012-04-13
JP2012527428A (ja) 2012-11-08
US20140045846A1 (en) 2014-02-13
WO2010133647A1 (en) 2010-11-25
CA2762226C (en) 2017-12-05

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