CR20190483A - Compuestos de heteroarilo bicíclicos 6-6 fusionados y su uso como inhibidores de lats - Google Patents

Compuestos de heteroarilo bicíclicos 6-6 fusionados y su uso como inhibidores de lats

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Publication number
CR20190483A
CR20190483A CR20190483A CR20190483A CR20190483A CR 20190483 A CR20190483 A CR 20190483A CR 20190483 A CR20190483 A CR 20190483A CR 20190483 A CR20190483 A CR 20190483A CR 20190483 A CR20190483 A CR 20190483A
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CR
Costa Rica
Prior art keywords
present
invention further
lats
compounds
bicyclic heteroaryl
Prior art date
Application number
CR20190483A
Other languages
English (en)
Inventor
Timothy Hoffmann
Jun Liu
Tingting Mo
Jiangfeng Pan
Yefen Zou
Dirk Behnke
Xueshi Hao
Juergen Klaus Maibaum
Frada Berenshteyn
Arnaud Lacoste
Cameron Lee
Yahu Liu
Yun Feng Xie
Shanshan Yan
Qihui Jin
Jan Tchorz
Xin Qu
Original Assignee
Novartis Ag
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Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CR20190483A publication Critical patent/CR20190483A/es

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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • C12N5/0602—Vertebrate cells
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    • C12N5/0621—Eye cells, e.g. cornea, iris pigmented cells
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/4375—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 containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/47—Quinolines; Isoquinolines
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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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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D471/02—Heterocyclic 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
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Abstract

La presente invención se refiere a compuestos de heteroarilo bicíclicos 6¿6 fusionados de la Fórmula A2 o A1 y su uso como inhibidores de LATS, o una sal, un estereoisómero o una composición farmacéutica de dichos compuestos; donde las variables son como se definen en el presente documento (A1 & A2). La presente invención se refiere además a un método de inhibición de LATS en una población de células, usando un compuesto de Fórmula A1, o una sal, un estereoisómero o una composición farmacéutica de dicho compuesto. La presente invención proporciona además un método para fabricar compuestos de la invención y sus usos terapéuticos. La invención proporciona adicionalmente métodos para su preparación, para su uso médico, su uso en el tratamiento y el abordaje de enfermedades o trastornos.The present invention is related to 6-6 Fused Bicyclic Heteroaryl Compounds of the Formula A2 or A1 and their Use as LATS Inhibitors, or a salt, stereoisomer or pharmaceutical composition thereof; wherein the variables are as defined herein (A1 & A2). The present invention further relates to a method of LATS inhibition in a cell population using a compound of Formula A1, or a salt, stereoisomer or pharmaceutical composition thereof. The present invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, their use in the treatment and management of diseases or disorders.
CR20190483A 2017-04-28 2018-04-26 Compuestos de heteroarilo bicíclicos 6-6 fusionados y su uso como inhibidores de lats CR20190483A (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201762491526P 2017-04-28 2017-04-28
US201762491484P 2017-04-28 2017-04-28
US201762491573P 2017-04-28 2017-04-28
US201762491475P 2017-04-28 2017-04-28
US201862650232P 2018-03-29 2018-03-29
PCT/IB2018/052919 WO2018198077A2 (en) 2017-04-28 2018-04-26 6-6 fused bicyclic heteroaryl compounds and their use as lats inhibitors

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CR20190483A true CR20190483A (es) 2019-11-20

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US (2) US11458138B2 (es)
EP (1) EP3615537B1 (es)
JP (2) JP7247102B2 (es)
KR (1) KR20190142776A (es)
CN (3) CN114703144A (es)
AU (2) AU2018260495B2 (es)
BR (1) BR112019022512A2 (es)
CA (1) CA3056906A1 (es)
CL (1) CL2019003049A1 (es)
CO (1) CO2019011873A2 (es)
CR (1) CR20190483A (es)
CU (2) CU20200080A7 (es)
DO (1) DOP2019000273A (es)
EC (1) ECSP19076732A (es)
IL (2) IL269293B (es)
JO (1) JOP20190257A1 (es)
MA (1) MA49285A (es)
MX (1) MX2019012756A (es)
PE (1) PE20200292A1 (es)
PH (1) PH12019502436A1 (es)
SG (1) SG11201908615RA (es)
TW (1) TW201843140A (es)
UY (1) UY37703A (es)
WO (1) WO2018198077A2 (es)

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UY38427A (es) * 2018-10-26 2020-05-29 Novartis Ag Métodos y composiciones para terapia con células oculares

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