JOP20190257A1 - مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats - Google Patents

مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats

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Publication number
JOP20190257A1
JOP20190257A1 JOP/2019/0257A JOP20190257A JOP20190257A1 JO P20190257 A1 JOP20190257 A1 JO P20190257A1 JO P20190257 A JOP20190257 A JO P20190257A JO P20190257 A1 JOP20190257 A1 JO P20190257A1
Authority
JO
Jordan
Prior art keywords
bicyclic heteroaryl
fused bicyclic
heteroaryl compounds
present
lats
Prior art date
Application number
JOP/2019/0257A
Other languages
English (en)
Inventor
Dirk Behnke
Jun Liu
Juergen Klaus Maibaum
Tingting Mo
Arnaud Lacoste
Timothy Hoffman
Yefen Zou
Yahu Liu
Xueshi Hao
Frada Berenshteyn
Jan Tchorz
Yun Feng Xie
Shanshan Yan
Jianfeng Pan
Cameron Lee
Qihui Jin
Xin Qu
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 JOP20190257A1 publication Critical patent/JOP20190257A1/ar

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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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    • A61K31/4353—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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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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    • A61K35/12—Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/30—Nerves; Brain; Eyes; Corneal cells; Cerebrospinal fluid; Neuronal stem cells; Neuronal precursor cells; Glial cells; Oligodendrocytes; Schwann cells; Astroglia; Astrocytes; Choroid plexus; Spinal cord tissue
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • C07D401/02—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
    • 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

يتعلق الاختراع الحالي بمركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 بالصيغة A2 أو A1 واستخدامها كمثبطات LATS، أو ملح، أيزومر فراغي أو تركيبة صيدلانية منها؛ حيث تكون المتغيرات كما تم تعريفها في هذه الوثيقة. يتعلق الاختراع الحالي أيضاً بطريقة لتثبيط LATS في مجموعة خلايا باستخدام مركب بالصيغة A1، أو ملح، أيزومر فراغي أو تركيبة صيدلانية منها. يقدم الاختراع الحالي أيضاً طريقة لتصنيع مركبات الاختراع، واستخداماتها العلاجية. يقدم الاختراع أيضاً طرق لتحضيرها، واستخدامها الطبي، واستخدامها في معالجة وإدارة الأمراض أو الاضطرابات. الشكل 1 و صور A1, A2
JOP/2019/0257A 2017-04-28 2017-06-16 مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats JOP20190257A1 (ar)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762491573P 2017-04-28 2017-04-28
US201762491526P 2017-04-28 2017-04-28
US201762491484P 2017-04-28 2017-04-28
US201762491475P 2017-04-28 2017-04-28
US201862650232P 2018-03-29 2018-03-29

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JOP20190257A1 true JOP20190257A1 (ar) 2019-10-28

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US (2) US11458138B2 (ar)
EP (1) EP3615537B1 (ar)
JP (2) JP7247102B2 (ar)
KR (1) KR20190142776A (ar)
CN (3) CN114621222A (ar)
AU (2) AU2018260495B2 (ar)
BR (1) BR112019022512A2 (ar)
CA (1) CA3056906A1 (ar)
CL (1) CL2019003049A1 (ar)
CO (1) CO2019011873A2 (ar)
CR (1) CR20190483A (ar)
CU (2) CU20190086A7 (ar)
DO (1) DOP2019000273A (ar)
EC (1) ECSP19076732A (ar)
IL (2) IL269293B (ar)
JO (1) JOP20190257A1 (ar)
MA (1) MA49285A (ar)
MX (1) MX2019012756A (ar)
PE (1) PE20200292A1 (ar)
PH (1) PH12019502436A1 (ar)
SG (1) SG11201908615RA (ar)
TW (1) TW201843140A (ar)
UY (1) UY37703A (ar)
WO (1) WO2018198077A2 (ar)

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JP2022188056A (ja) 2022-12-20
IL269293B (en) 2022-06-01
WO2018198077A3 (en) 2019-02-14
PE20200292A1 (es) 2020-02-05
CU20190086A7 (es) 2020-11-30
IL292857A (en) 2022-07-01
US11458138B2 (en) 2022-10-04
RU2019138304A (ru) 2021-05-28
JP2020517698A (ja) 2020-06-18
CN110573511B (zh) 2023-04-25
MA49285A (fr) 2020-03-04
ECSP19076732A (es) 2019-10-31
KR20190142776A (ko) 2019-12-27
IL269293A (en) 2019-11-28
EP3615537B1 (en) 2024-03-06
WO2018198077A2 (en) 2018-11-01
CO2019011873A2 (es) 2020-01-17
AU2018260495A1 (en) 2019-10-17
US20230190751A1 (en) 2023-06-22
US20180344738A1 (en) 2018-12-06
AU2018260495B2 (en) 2021-09-16
MX2019012756A (es) 2019-12-16
CN114621222A (zh) 2022-06-14
CL2019003049A1 (es) 2020-02-07
CU20200080A7 (es) 2021-05-12
CN110573511A (zh) 2019-12-13
CN114703144A (zh) 2022-07-05
TW201843140A (zh) 2018-12-16
PH12019502436A1 (en) 2020-07-20
SG11201908615RA (en) 2019-11-28
AU2021286281A1 (en) 2022-01-06
RU2019138304A3 (ar) 2021-07-13
BR112019022512A2 (pt) 2020-06-16
EP3615537A2 (en) 2020-03-04
DOP2019000273A (es) 2019-12-15
UY37703A (es) 2018-11-30
CA3056906A1 (en) 2018-11-01
CR20190483A (es) 2019-11-20
JP7247102B2 (ja) 2023-03-28

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