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BRPI0514632A - substituted 4-heteroarylmethyl phthalazinone derivatives - Google Patents

substituted 4-heteroarylmethyl phthalazinone derivatives

Info

Publication number
BRPI0514632A
BRPI0514632A BRPI0514632-1A BRPI0514632A BRPI0514632A BR PI0514632 A BRPI0514632 A BR PI0514632A BR PI0514632 A BRPI0514632 A BR PI0514632A BR PI0514632 A BRPI0514632 A BR PI0514632A
Authority
BR
Brazil
Prior art keywords
optionally substituted
heteroarylmethyl
alkyl
group
substituted
Prior art date
Application number
BRPI0514632-1A
Other languages
Portuguese (pt)
Inventor
Muhammad Hasmim Javaid
Graeme Cameron Murray Smith
Niall Morrison Barr Martin
Sylvie Gomez
Vincent Ming Lai Junior Loh
Xiao-Ling Fan Cockcroft
Stefano Forte
Keith Allan Menear
Ian Timothy Williams Matthews
Original Assignee
Kudos Pharm Ltd
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 GBGB0419072.4A external-priority patent/GB0419072D0/en
Application filed by Kudos Pharm Ltd filed Critical Kudos Pharm Ltd
Publication of BRPI0514632A publication Critical patent/BRPI0514632A/en

Links

Classifications

    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • 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
    • C07D409/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

DERIVADOS DE FTALAZINONA 4-HETEROARILMETILA SUBSTITUìDOS Composto da fórmula (I): para uso no tratamento de câncer ou de outras doenças melhoradas pela inibição de PARP, em que: A e B em conjunto representam um anel aromático fundido opcionalmente substituído; X pode ser NR¬ x¬ ou CR¬ x¬R¬ y¬; se X = NR¬ x¬ então n é 1 ou 2 e se x = CR¬ x¬R¬ y¬ então n é 1; R¬ x¬ é selecionado do grupo que consiste em H, grupos alquila C~ 1-20~, arila C~ 5-20~, heterociclila C~ 3-20~, amido, tioamido, éster, acila, e sulfonila opcionalmente substituídos; R¬ y¬ é selecionado de H, hidróxi, amino; ou então R¬ x¬ e R¬ y¬~ podem formar em conjunto um grupo cicloalquila ou heterociclila espiro-C~ 3-7~; R¬ C1¬ e R¬ C2¬ são independentemente selecionados do grupo que consiste em hidrogênio e alquila C~ 1~-~ 4~, ou quando X for CR¬ x¬R¬ y¬, R¬ C1¬, R¬ C2¬, R¬ x¬ e R¬ y¬, juntamente com os átomos de carbono aos quais eles estão ligados, poderão formar um anel aromático fundido opcionalmente substituído; R¬ 1¬ é selecionado de H e halo; e Het é selecionado de: (i) fórmula (i) em que Y¬ 1¬ é selecionado de CH e N, Y¬ 2¬ é selecionado de CH e N, Y¬ 3¬ é selecionado de CH, CF e N, sendo que somente um ou dois de Y¬ 1¬, Y¬ 2¬ e Y¬ 3¬ podem ser N; e (ii), em que Q é O ou S.SUBSTITUTED 4-HETEROARYLMETHYL FTAAZINONE DERIVATIVES Compound of formula (I): for use in the treatment of cancer or other diseases enhanced by PARP inhibition, wherein: A and B together represent an optionally substituted fused aromatic ring; X may be NR¬ x¬ or CR¬ x¬R¬ y¬; if X = NR¬ x¬ then n is 1 or 2 and if x = CR¬ x¬R¬ y¬ then n is 1; R¬ x¬ is selected from the group consisting of optionally substituted H, C 1-20 alkyl alkyl, C 5-20 aryl, C 3-20 heterocyclyl, starch, thioamido, ester, acyl and sulfonyl groups ; R¬ y¬ is selected from H, hydroxy, amino; or R¬x¬ and R¬y¬ may together form a C 3-7 spiro-cycloalkyl or heterocyclyl group; R¬ C1¬ and R¬ C2¬ are independently selected from the group consisting of hydrogen and alkyl C ~ 1 ~ - ~ 4 ~, or when X is CR¬ x¬R¬ y¬, R¬ C1¬, R¬ C2 ¬, R¬ x¬ and R¬ y¬, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; R¬ 1¬ is selected from H and halo; and Het is selected from: (i) formula (i) wherein Y¬ 1¬ is selected from CH and N, Y¬ 2¬ is selected from CH and N, Y¬ 3¬ is selected from CH, CF and N, whereas only one or two of Y¬ 1¬, Y¬ 2¬ and Y¬ 3¬ can be N; and (ii) where Q is O or S.

BRPI0514632-1A 2004-08-26 2005-08-26 substituted 4-heteroarylmethyl phthalazinone derivatives BRPI0514632A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0419072.4A GB0419072D0 (en) 2004-08-26 2004-08-26 Phthalazinone derivatives
US60495604P 2004-08-27 2004-08-27
PCT/GB2005/003343 WO2006021801A1 (en) 2004-08-26 2005-08-26 4-heteroarylmethyl substituted phthalazinone derivatives

Publications (1)

Publication Number Publication Date
BRPI0514632A true BRPI0514632A (en) 2008-06-17

Family

ID=35219560

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0514632-1A BRPI0514632A (en) 2004-08-26 2005-08-26 substituted 4-heteroarylmethyl phthalazinone derivatives

Country Status (11)

Country Link
EP (1) EP1791827A1 (en)
JP (1) JP2008510783A (en)
KR (1) KR20070057859A (en)
AU (1) AU2005276229A1 (en)
BR (1) BRPI0514632A (en)
CA (1) CA2577191A1 (en)
IL (1) IL181408A0 (en)
MX (1) MX2007002318A (en)
NO (1) NO20071579L (en)
NZ (1) NZ553979A (en)
WO (1) WO2006021801A1 (en)

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CA2674436C (en) 2007-01-10 2012-07-17 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors
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Publication number Publication date
CA2577191A1 (en) 2006-03-02
JP2008510783A (en) 2008-04-10
NO20071579L (en) 2007-05-29
WO2006021801A1 (en) 2006-03-02
KR20070057859A (en) 2007-06-07
MX2007002318A (en) 2007-04-17
EP1791827A1 (en) 2007-06-06
NZ553979A (en) 2009-05-31
IL181408A0 (en) 2007-07-04
AU2005276229A1 (en) 2006-03-02

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