AR064002A1 - SUBSTITUTED KINAZOLINS - Google Patents

SUBSTITUTED KINAZOLINS

Info

Publication number
AR064002A1
AR064002A1 ARP070105272A ARP070105272A AR064002A1 AR 064002 A1 AR064002 A1 AR 064002A1 AR P070105272 A ARP070105272 A AR P070105272A AR P070105272 A ARP070105272 A AR P070105272A AR 064002 A1 AR064002 A1 AR 064002A1
Authority
AR
Argentina
Prior art keywords
group
hydrogen
bromine
iodine
alkyl
Prior art date
Application number
ARP070105272A
Other languages
Spanish (es)
Inventor
Bernard Golding
Richard Franklin
Original Assignee
Shire Llc
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 Shire Llc filed Critical Shire Llc
Publication of AR064002A1 publication Critical patent/AR064002A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Los compuestos de la presente actuan por inhibicion de la megacariocitopoiesis y en consecuencia la formacion de plaquetas sanguíneas. Reivindicacion 1: Un compuesto de la formula (1) o una de sus sales o solvatos farmacéuticamente aceptables, caracterizado porque R1, R2, R3 y R4 independientemente representan hidrogeno o un grupo bloqueador con funcion de prevencion de la reaccion metabolica en la posicion de sustitucion 3; o en donde R1 y R2, y/o R3 y R4 junto con el carbono al que están adosados forman un grupo bloqueador que funciona para prevenir en forma directa o indirecta las reacciones metabolicas en la posicion 3, en donde el resto de los grupos R1 a R4 son hidrogeno; R5 se selecciona del grupo que comprende: fluor cloro, bromo y yodo; R6 se selecciona del grupo que comprende: fluor cloro, bromo y yodo; R7 y R8 son seleccionados independientemente del grupo que comprende: H; halo; ciano; alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, y haloalcoxi C1-6; y R9 es H, alquilo C1-6, o un ion metálico de Grupo I; siempre que R1, R2, R3 y R4 no sean todos hidrogeno, o que cuando uno de R1 y R2 es metilo y R3 y R4 son hidrogeno, entonces el otro de R1 y R2 no es hidrogeno.The compounds of the present act by inhibition of megakaryocytopoiesis and consequently the formation of blood platelets. Claim 1: A compound of the formula (1) or a pharmaceutically acceptable salt or solvate thereof, characterized in that R1, R2, R3 and R4 independently represent hydrogen or a blocking group with function of preventing the metabolic reaction in the substitution position 3; or where R1 and R2, and / or R3 and R4 together with the carbon to which they are attached form a blocking group that works to prevent directly or indirectly the metabolic reactions in position 3, where the rest of the R1 groups to R4 are hydrogen; R5 is selected from the group comprising: chlorine fluorine, bromine and iodine; R6 is selected from the group comprising: chlorine fluorine, bromine and iodine; R7 and R8 are independently selected from the group comprising: H; halo; cyano; C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, and C1-6 haloalkoxy; and R9 is H, C1-6 alkyl, or a Group I metal ion; provided that R1, R2, R3 and R4 are not all hydrogen, or when one of R1 and R2 is methyl and R3 and R4 are hydrogen, then the other of R1 and R2 is not hydrogen.

ARP070105272A 2006-11-28 2007-11-28 SUBSTITUTED KINAZOLINS AR064002A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0623750.7A GB0623750D0 (en) 2006-11-28 2006-11-28 Substituted quinazolines

Publications (1)

Publication Number Publication Date
AR064002A1 true AR064002A1 (en) 2009-03-04

Family

ID=37671460

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070105272A AR064002A1 (en) 2006-11-28 2007-11-28 SUBSTITUTED KINAZOLINS

Country Status (14)

Country Link
EP (1) EP2099802A2 (en)
JP (1) JP2010511030A (en)
KR (1) KR20090094268A (en)
CN (1) CN101558071B (en)
AR (1) AR064002A1 (en)
AU (1) AU2007327047B2 (en)
BR (1) BRPI0719570A2 (en)
CA (1) CA2670123A1 (en)
EA (1) EA018259B1 (en)
GB (1) GB0623750D0 (en)
IL (1) IL198809A0 (en)
MX (1) MX2009005579A (en)
TW (1) TW200838537A (en)
WO (1) WO2008065444A2 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8304420B2 (en) 2006-11-28 2012-11-06 Shire Llc Substituted quinazolines for reducing platelet count
GB0808944D0 (en) * 2008-05-16 2008-06-25 Shire Llc Substituted quinazolines
GB2462022B (en) * 2008-06-16 2011-05-25 Biovascular Inc Controlled release compositions of agents that reduce circulating levels of platelets and methods thereof
GB0822970D0 (en) * 2008-12-17 2009-01-21 Shire Llc Process for the preparation of anagrelide and analogues
GB201004495D0 (en) 2010-03-18 2010-05-05 Shire Llc Subtituted quinazolines
GB201017783D0 (en) 2010-10-21 2010-12-01 Shire Llc Process for the preparation of anagrelide and analogues thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL7807507A (en) * 1977-07-25 1979-01-29 Hoffmann La Roche TRICYCLICAL CONNECTIONS.
CA1131631A (en) * 1979-06-20 1982-09-14 Madhukar S. Chodnekar Quinazoline derivatives and pharmaceutical preparations
ZA803535B (en) * 1979-06-20 1981-06-24 Hoffmann La Roche Novel quinazoline derivatives and pharmaceutical preparations
US20040209907A1 (en) * 2003-01-23 2004-10-21 Richard Franklin Formulation and methods for the treatment of thrombocythemia
US20060030574A1 (en) * 2004-08-04 2006-02-09 Shire Holdings Ag Quinazoline derivatives useful for the treatment of peripheral arterial disease and as phosphodiesterase inhibitors
US7700608B2 (en) * 2004-08-04 2010-04-20 Shire Holdings Ag Quinazoline derivatives and their use in the treatment of thrombocythemia

Also Published As

Publication number Publication date
KR20090094268A (en) 2009-09-04
AU2007327047A1 (en) 2008-06-05
EA200900740A1 (en) 2010-02-26
WO2008065444A2 (en) 2008-06-05
GB0623750D0 (en) 2007-01-10
JP2010511030A (en) 2010-04-08
CN101558071A (en) 2009-10-14
IL198809A0 (en) 2010-02-17
EA018259B1 (en) 2013-06-28
WO2008065444B1 (en) 2008-10-09
BRPI0719570A2 (en) 2013-12-10
TW200838537A (en) 2008-10-01
WO2008065444A3 (en) 2008-07-31
CN101558071B (en) 2013-04-24
MX2009005579A (en) 2009-08-12
CA2670123A1 (en) 2008-06-05
EP2099802A2 (en) 2009-09-16
AU2007327047B2 (en) 2012-08-30

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