ECSP12011752A - Compuestos de benzoxepina inhibidores de la pi3k y métodos de uso - Google Patents

Compuestos de benzoxepina inhibidores de la pi3k y métodos de uso

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Publication number
ECSP12011752A
ECSP12011752A ECSP12011752A ECSP12011752A EC SP12011752 A ECSP12011752 A EC SP12011752A EC SP12011752 A ECSP12011752 A EC SP12011752A EC SP12011752 A ECSP12011752 A EC SP12011752A
Authority
EC
Ecuador
Prior art keywords
methods
pi3k
formula
benzoxepine
compounds
Prior art date
Application number
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English (en)
Inventor
Adrian FOLKES
Richard Goldsmith
Tim Heffron
Steven Staben
Chudi Ndubaku
Nicole Blaquiere
Steven Do
Danette Dudley
Robert Heald
Aleksandr Kolesnikov
Alan G Olivero
Stephen Price
Binqing Wei
Original Assignee
Hoffmann La Roche
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.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43125543&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ECSP12011752(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of ECSP12011752A publication Critical patent/ECSP12011752A/es

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    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
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Abstract

Los compuestos de benzoxepina de la fórmula I, incluidos sus estereoisómeros, isómeros geométricos, tautómeros, solvatos, metabolitos y sales farmacéuticamente aceptables, en los que: Z1 es CR1 o N; Z2 es CR2 o N; Z3 es CR3 o N; Z4 es CR4 o N; y en los que (i) X1 es N y X2 es S, (ii) X1 es S y X2 es N, (iii) X1 es CR7 y X2 es S, (iv) X1 es S y X2 es CR7; (v) X1 es NR8 y X2 es N, (vi) X1 es N y X2 es NR8, (vii) X1 es CR7 y X2 es O, (viii) X1 es O y X2 es CR7, (ix) X1 es CR7 y X2 es C(R7)2, (x) X1 es C(R7)2 y X2 es CR7; (xi) X1 es N y X2 es O, o (xii) X1 es O y X2 es N, son útiles para inhibir las lípido-quinasas, incluidas la p110 alfa y otras isoformas de la PI3K, y para tratar trastornos tales como el cáncer mediado por las lípido-quinasas. Se describen métodos de uso de los compuestos de la fórmula I para el diagnóstico, la prevención o el tratamiento de dichos trastornos "in vitro", "in situ" e "in vivo" en células de mamíferos, o de estados patológicos asociados.
ECSP12011752 2009-09-28 2012-09-28 Compuestos de benzoxepina inhibidores de la pi3k y métodos de uso ECSP12011752A (es)

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AU (1) AU2010299820A1 (es)
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EC (1) ECSP12011752A (es)
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