JP2018519343A5 - - Google Patents
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- JP2018519343A5 JP2018519343A5 JP2018500297A JP2018500297A JP2018519343A5 JP 2018519343 A5 JP2018519343 A5 JP 2018519343A5 JP 2018500297 A JP2018500297 A JP 2018500297A JP 2018500297 A JP2018500297 A JP 2018500297A JP 2018519343 A5 JP2018519343 A5 JP 2018519343A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- nhs
- nhc
- cycloalkyl
- independently
- Prior art date
- Legal status (The legal status 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 status listed.)
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- 125000000217 alkyl group Chemical group 0.000 claims 144
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 56
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 53
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 43
- 150000003839 salts Chemical class 0.000 claims 41
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 40
- 125000003118 aryl group Chemical group 0.000 claims 40
- 229910052805 deuterium Inorganic materials 0.000 claims 40
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 38
- 150000001875 compounds Chemical class 0.000 claims 38
- 229910052736 halogen Inorganic materials 0.000 claims 30
- 150000002367 halogens Chemical class 0.000 claims 30
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 25
- 125000002950 monocyclic group Chemical group 0.000 claims 21
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 15
- 229910052717 sulfur Inorganic materials 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 7
- 125000001246 bromo group Chemical group Br* 0.000 claims 7
- 125000001309 chloro group Chemical group Cl* 0.000 claims 7
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- -1 C 1 -C 6 alkyl Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 102000001253 Protein Kinase Human genes 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 2
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 claims 1
- 101000686031 Homo sapiens Proto-oncogene tyrosine-protein kinase ROS Proteins 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 1
- 102100023347 Proto-oncogene tyrosine-protein kinase ROS Human genes 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562188043P | 2015-07-02 | 2015-07-02 | |
| US62/188,043 | 2015-07-02 | ||
| US201662353728P | 2016-06-23 | 2016-06-23 | |
| US62/353,728 | 2016-06-23 | ||
| PCT/US2016/040329 WO2017004342A1 (en) | 2015-07-02 | 2016-06-30 | Chiral diaryl macrocycles as modulators of protein kinases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018519343A JP2018519343A (ja) | 2018-07-19 |
| JP2018519343A5 true JP2018519343A5 (enExample) | 2019-07-25 |
| JP6871903B2 JP6871903B2 (ja) | 2021-05-19 |
Family
ID=57609146
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018500297A Active JP6871903B2 (ja) | 2015-07-02 | 2016-06-30 | プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10316044B2 (enExample) |
| EP (1) | EP3317285B1 (enExample) |
| JP (1) | JP6871903B2 (enExample) |
| KR (1) | KR102599788B1 (enExample) |
| CN (1) | CN107735399B (enExample) |
| AU (2) | AU2016287568B2 (enExample) |
| CA (1) | CA2989327A1 (enExample) |
| ES (1) | ES2864839T3 (enExample) |
| IL (1) | IL256377A (enExample) |
| MX (1) | MX2017017097A (enExample) |
| RU (1) | RU2732405C2 (enExample) |
| TW (1) | TW201716415A (enExample) |
| WO (1) | WO2017004342A1 (enExample) |
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
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| DK2350075T3 (da) | 2008-09-22 | 2014-05-26 | Array Biopharma Inc | Substituerede imidazo[1,2b]pyridazinforbindelser som trk-kinase-inhibitorer |
| PT3106463T (pt) | 2008-10-22 | 2018-05-18 | Array Biopharma Inc | Compostos de pirazolo[1,5-]pirimidina substituídos como inibidores de cinase trk |
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| RU2735545C2 (ru) | 2010-05-20 | 2020-11-03 | Эррэй Биофарма Инк. | Макроциклические соединения в качестве ингибиторов киназы trk |
| HRP20191283T1 (hr) | 2014-01-24 | 2019-10-18 | Turning Point Therapeutics, Inc. | Diaril makrocikli kao modulatori protein kinaze |
| EP3218380B1 (en) | 2014-11-16 | 2021-03-17 | Array Biopharma, Inc. | Preparation of a crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| EP4397665A3 (en) * | 2015-07-06 | 2024-08-21 | Turning Point Therapeutics, Inc. | Diaryl macrocycle polymorph |
| DK3325488T3 (da) * | 2015-07-21 | 2020-09-14 | Turning Point Therapeutics Inc | Chiral diaryl-makrocyklus og anvendelse deraf til behandling af cancer |
| TN2019000271A1 (en) | 2015-10-26 | 2021-01-07 | Univ Colorado Regents | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| IL304018A (en) | 2016-04-04 | 2023-08-01 | Loxo Oncology Inc | Liquid formulations of (S)-N-(5-((R)-2-(5,2-difluorophenyl)-pyrrolidine-1-yl)-pyrazolo[5,1-A]pyrimidin-3-yl)-3 -hydroxypyrrolidine-1-carboxamide |
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| FI3674307T3 (fi) * | 2017-08-23 | 2023-09-11 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | Aminopyratsolin ja pyrimidiinin sisältävä makrosykli ja sen farmaseuttinen koostumus ja käyttö |
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| CA3081790C (en) * | 2017-11-10 | 2023-03-07 | Angex Pharmaceutical, Inc. | Macrocyclic compounds as trk kinase inhibitors and uses thereof |
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-
2016
- 2016-06-30 AU AU2016287568A patent/AU2016287568B2/en not_active Ceased
- 2016-06-30 WO PCT/US2016/040329 patent/WO2017004342A1/en not_active Ceased
- 2016-06-30 RU RU2018103907A patent/RU2732405C2/ru active
- 2016-06-30 JP JP2018500297A patent/JP6871903B2/ja active Active
- 2016-06-30 EP EP16818768.0A patent/EP3317285B1/en active Active
- 2016-06-30 ES ES16818768T patent/ES2864839T3/es active Active
- 2016-06-30 KR KR1020187002777A patent/KR102599788B1/ko active Active
- 2016-06-30 US US15/740,462 patent/US10316044B2/en active Active
- 2016-06-30 CN CN201680038613.1A patent/CN107735399B/zh active Active
- 2016-06-30 CA CA2989327A patent/CA2989327A1/en active Pending
- 2016-06-30 MX MX2017017097A patent/MX2017017097A/es unknown
- 2016-07-01 TW TW105121035A patent/TW201716415A/zh unknown
-
2017
- 2017-12-18 IL IL256377A patent/IL256377A/en unknown
-
2019
- 2019-05-29 US US16/425,407 patent/US11008337B2/en active Active
-
2020
- 2020-08-11 AU AU2020217336A patent/AU2020217336A1/en not_active Abandoned
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