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PE20200292A1 - Compuestos de heteroarilo biciclicos 6-6 fusionados y su uso como inhibidores de lats - Google Patents

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

Info

Publication number
PE20200292A1
PE20200292A1 PE2019002107A PE2019002107A PE20200292A1 PE 20200292 A1 PE20200292 A1 PE 20200292A1 PE 2019002107 A PE2019002107 A PE 2019002107A PE 2019002107 A PE2019002107 A PE 2019002107A PE 20200292 A1 PE20200292 A1 PE 20200292A1
Authority
PE
Peru
Prior art keywords
heteroaryl compounds
halogen
alkyl
fused bicycle
lats inhibitors
Prior art date
Application number
PE2019002107A
Other languages
English (en)
Inventor
Dirk Behnke
Frada Berenshteyn
Xueshi Hao
Timothy Hoffmann
Qihui Jin
Arnaud Lacoste
Cameron Lee
Jun Liu
Yefen Zou
Yahu Liu
Juergen Klaus Maibaum
Tingting Mo
Jiangfeng Pan
Xin Qu
Jan Tchorz
Yun Feng Xie
Shanshan Yan
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of PE20200292A1 publication Critical patent/PE20200292A1/es

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    • 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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    • 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
    • A—HUMAN NECESSITIES
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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
    • A—HUMAN NECESSITIES
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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 invencion se refiere a compuestos de heteroarilo biciclicos 6-6 fusionados de formula A1 y A2, donde X1 y X2 son CH o N; el anillo A es un heteroarilo monociclico de 5 o 6 miembros o un heteroarilo biciclico fusionado de 9 miembros; R1 es H o alquilo C1-C6; R2 es alquilo C1-C8, CN, halogeno, oxo, entre otros; R3 es H, halogeno o alquilo C1-C6; R5 es H, halogeno, entre otros. Tambien esta referida a una composicion farmaceutica y a un metodo de preparacion. Dichos compuestos son inhibidores de LATS (quinasa supresora tumoral grande)
PE2019002107A 2017-04-28 2018-04-26 Compuestos de heteroarilo biciclicos 6-6 fusionados y su uso como inhibidores de lats PE20200292A1 (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201762491475P 2017-04-28 2017-04-28
US201762491526P 2017-04-28 2017-04-28
US201762491484P 2017-04-28 2017-04-28
US201762491573P 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

Publications (1)

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PE20200292A1 true PE20200292A1 (es) 2020-02-05

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PE2019002107A PE20200292A1 (es) 2017-04-28 2018-04-26 Compuestos de heteroarilo biciclicos 6-6 fusionados y su uso como inhibidores de lats

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US (2) US11458138B2 (es)
EP (1) EP3615537B1 (es)
JP (2) JP7247102B2 (es)
KR (1) KR20190142776A (es)
CN (3) CN114621222B (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)
ES (1) ES2983611T3 (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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