AR075383A1 - Derivados de triazolo[4,3-b]piridazina - Google Patents

Derivados de triazolo[4,3-b]piridazina

Info

Publication number
AR075383A1
AR075383A1 ARP100100350A ARP100100350A AR075383A1 AR 075383 A1 AR075383 A1 AR 075383A1 AR P100100350 A ARP100100350 A AR P100100350A AR P100100350 A ARP100100350 A AR P100100350A AR 075383 A1 AR075383 A1 AR 075383A1
Authority
AR
Argentina
Prior art keywords
alkyl
cr3r4
heteroatoms
independently selected
identically
Prior art date
Application number
ARP100100350A
Other languages
English (en)
Inventor
Robert Hugh Bradbury
Alfred Arthur Rabow
Gregory Richard Carr
Korupoju Srinivasa Rao
Harikrishna Tumma
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR075383A1 publication Critical patent/AR075383A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • 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
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • 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

Abstract

Se refiere a procesos para la preparacion de dichos compuestos, composiciones farmacéuticas que los contienen y su uso en el tratamiento de afecciones asociadas con el receptor de androgenos, en particular el cáncer de prostata. Reivindicacion 1: Un compuesto caracterizado porque es de Formula 1, o una sal farmacéuticamente aceptable del mismo: en donde R1 representa haloalquilo C1-4; k representa 0, 1 o 2: n y p independientemente representan 1 o 2: Y representa N, C, CH o COH; la línea punteada representa un enlace simple cuando Y es N, CH o COH; la línea punteada representa un enlace doble cuando Y es C, L1 es un enlace directo y J es indolilo pirrolopiridinilo: L1 representa un enlace directo,-(CR3R4)t-, -(CR3R4)v-O-(CR3R4)v-, -N(R5)-(CH2)q-, -S-, -S(O)- o S(O)2-; R3 y R4, de forma idéntica o diferente en cada aparicion, representan hidrogeno o metilo; R5 representa hidrogeno o metilo: q, de forma idéntica o diferente en cada aparicion, representa 0, 1, 2, 3 o 4; t representa 1, 2 o 3; v, de forma idéntica o diferente en cada aparicion, representa 0, 1 o 2; j representa: arilo; cicloalquilo C3-6; un anillo heterocíclico de 4, 5, 6 o 7 miembros monocíclico que comprende 1, 2 o 3 heteroátomos que se seleccionan independientemente de O, N o S; Un anillo heteroarilo monocíclico de 5 o 6 miembros que comprende 1, 2, 3 o 4 heteroátomos que se seleccionan independientemente de O, N o S; o un sistema de anillos heteroarilo bicíclico de 9 o 10 miembros que comprende 1, 2, 3, 4 o 5 heteroátomos que se seleccionan independientemente de O, N o S; L2 representa un enlace directo. -(CR3R4)t-, -C(O)N(R5)-(CH2)q-, -C(O)N(R5)-(CH2)q- S(O)2-, -NR5C(O)-(CH2)q-, -C(O)-(CH2)q-, -O-(CR9R10)q-, -O-(CR3R4)q-NR5-(CH2)q-, -O-(CR3R4)q-C(O)NR5-(CH2)q-, -S-, -S(O)- o -S(O)2-; R9 y R10, de forma idéntica o diferente en cada aparicion, representan hidrogeno, metilo, etilo, isopropilo, ciclopropilo o metoximetilo: R2 representa: halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carboxi, alcoxi C1-6, ciano, oxo, fluoroalquilo C1-6, hidroxi, animo, N-alquil C1-4amino o N,N-di-alquil C1-4amino; arilo, en donde el anillo arilo está opcionalmente sustituido por 1, 2 o 3 sustituyentes que se seleccionan de R6; un anillo heterocíclico de 4, 5, 6 o 7 miembros monocíclico que comprende 1, 2 o 3 heteroátomos que se seleccionan independientemente de O, N o S y en donde el anillo heterocíclico está opcionalmente sustituido por 1, 2 o 3 sustituyentes que se seleccionan de R6; un anillo heteroarilo de 5 o 6 miembros monocíclico que comprende 1, 2, 3 o 4 heteroátomos que se seleccionan independientemente de O, N o S y en donde el anillo heteroarilo está opcionalmente sustituido por 1, 2 o 3 sustituyentes que se seleccionan de R6: o un sistema de anillos heteroarilo bicíclico de 9 o 10 miembros que comprenden 1, 2, 3, 4 o 5 heteroátomos que se seleccionan independientemente de O, N o S y en donde el anillo heterocíclico está opcionalmente sustituido por 1, 2 o 3 sustituyentes que se seleccionan de R6; R6 representa amino, halo, alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcanoilo C2-6, alcoxi C1-6 alquilo C1-6, carboxi, ciano, oxo, fluoroalquilo C1-6, hidroxi, hidroxialquilo C1-6, alquil C1-6 sulfanilo, alquil C1-6 sulfinilo, alquil C1-6 sulfonilo, oxetan-3-ilcarbonilo, N-alquil C1-4 amino N,N-di-alquil C1-4 amino o -C(O)NR7R8 en donde R7 y R8 independientemente representan hidrogeno o metilo; y r representa 0, 1, 2 o 3.
ARP100100350A 2009-02-10 2010-02-09 Derivados de triazolo[4,3-b]piridazina AR075383A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15122109P 2009-02-10 2009-02-10
US18776609P 2009-06-17 2009-06-17

Publications (1)

Publication Number Publication Date
AR075383A1 true AR075383A1 (es) 2011-03-30

Family

ID=42115693

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100100350A AR075383A1 (es) 2009-02-10 2010-02-09 Derivados de triazolo[4,3-b]piridazina

Country Status (27)

Country Link
US (2) US8258140B2 (es)
EP (1) EP2396333B1 (es)
JP (1) JP5059977B2 (es)
KR (1) KR20110113755A (es)
CN (1) CN102388048B (es)
AR (1) AR075383A1 (es)
AU (1) AU2010212590B2 (es)
CA (1) CA2749926A1 (es)
CL (1) CL2011001920A1 (es)
CO (1) CO6410299A2 (es)
CR (1) CR20110427A (es)
CU (1) CU20110158A7 (es)
DO (1) DOP2011000258A (es)
EA (1) EA019647B1 (es)
EC (1) ECSP11011257A (es)
ES (1) ES2427917T3 (es)
HK (1) HK1164870A1 (es)
IL (1) IL214112A0 (es)
MX (1) MX2011008452A (es)
NI (1) NI201100156A (es)
PE (1) PE20120603A1 (es)
SG (1) SG172986A1 (es)
SV (1) SV2011003993A (es)
TW (1) TW201033215A (es)
UY (1) UY32426A (es)
WO (1) WO2010092371A1 (es)
ZA (1) ZA201106625B (es)

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WO2020243378A1 (en) * 2019-05-31 2020-12-03 United States Government As Represented By The Department Of Veterans Affairs Compositions and methods comprising endothelin a receptor antagonists and androgen therapies
TWI813106B (zh) * 2020-12-30 2023-08-21 財團法人工業技術研究院 雄性激素受體結合分子及其用途
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Also Published As

Publication number Publication date
JP5059977B2 (ja) 2012-10-31
TW201033215A (en) 2010-09-16
ECSP11011257A (es) 2011-09-30
US20100267699A1 (en) 2010-10-21
CN102388048A (zh) 2012-03-21
DOP2011000258A (es) 2011-09-30
SG172986A1 (en) 2011-08-29
EP2396333A1 (en) 2011-12-21
NI201100156A (es) 2012-03-19
IL214112A0 (en) 2011-08-31
JP2012517462A (ja) 2012-08-02
US20130203714A1 (en) 2013-08-08
MX2011008452A (es) 2011-12-16
HK1164870A1 (en) 2012-09-28
CN102388048B (zh) 2014-07-30
EA201101180A1 (ru) 2012-03-30
ZA201106625B (en) 2013-02-27
AU2010212590B2 (en) 2013-01-10
US8258140B2 (en) 2012-09-04
CO6410299A2 (es) 2012-03-30
SV2011003993A (es) 2012-01-06
WO2010092371A1 (en) 2010-08-19
CR20110427A (es) 2011-09-21
PE20120603A1 (es) 2012-06-14
AU2010212590A1 (en) 2011-08-04
KR20110113755A (ko) 2011-10-18
ES2427917T3 (es) 2013-11-04
CL2011001920A1 (es) 2011-10-21
EP2396333B1 (en) 2013-07-03
EA019647B1 (ru) 2014-05-30
CA2749926A1 (en) 2010-08-19
UY32426A (es) 2010-09-30
CU20110158A7 (es) 2012-02-15

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