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

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/502Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic 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
    • C07D407/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (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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GB0610680D0 (en) 2006-05-31 2006-07-12 Istituto Di Ricerche D Biolog Therapeutic compounds
EA016079B1 (en) 2007-01-10 2012-01-30 Институто Ди Ричерке Ди Биолоджиа Молеколаре П. Анджелетти Спа Amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors
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AR070221A1 (en) * 2008-01-23 2010-03-25 Astrazeneca Ab DERIVATIVES OF FTALAZINONA POLYMERASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND USES OF THE SAME TO PREVENT AND / OR TREAT CANCERIGENE TUMORS, ISCHEMICAL INJURIES AND OTHER ASSOCIATED DISEASES.
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Also Published As

Publication number Publication date
MX2007002318A (en) 2007-04-17
KR20070057859A (en) 2007-06-07
EP1791827A1 (en) 2007-06-06
WO2006021801A1 (en) 2006-03-02
NZ553979A (en) 2009-05-31
CA2577191A1 (en) 2006-03-02
NO20071579L (en) 2007-05-29
JP2008510783A (en) 2008-04-10
AU2005276229A1 (en) 2006-03-02
IL181408A0 (en) 2007-07-04

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Legal Events

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B25A Requested transfer of rights approved

Owner name: KUDOS PHARMACEUTICALS LIMITED (GB) , MAYBRIDGE LIM

Free format text: TRANSFERIDO PARTE DOS DIREITOS DE: KUDOS PHARMACEUTICALS LIMITED

B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 7A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: NAO APRESENTADA A GUIA DE CUMPRIMENTO DE EXIGENCIA. REFERENTE A 7A ANUIDADE.