JP2011512361A5 - - Google Patents
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- Publication number
- JP2011512361A5 JP2011512361A5 JP2010546945A JP2010546945A JP2011512361A5 JP 2011512361 A5 JP2011512361 A5 JP 2011512361A5 JP 2010546945 A JP2010546945 A JP 2010546945A JP 2010546945 A JP2010546945 A JP 2010546945A JP 2011512361 A5 JP2011512361 A5 JP 2011512361A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- group
- heterocyclyl
- alkyl
- compound
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 17
- -1 3,4-dihydro- 2H-benzo [b] [1,4] thiazinyl Chemical group 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000001188 haloalkyl group Chemical group 0.000 claims 10
- 125000005843 halogen group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 8
- 125000000262 haloalkenyl group Chemical group 0.000 claims 7
- 125000003107 substituted aryl group Chemical group 0.000 claims 7
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000002947 alkylene group Chemical group 0.000 claims 6
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000005356 cycloalkylalkenyl group Chemical group 0.000 claims 5
- 125000005357 cycloalkylalkynyl group Chemical class 0.000 claims 5
- 125000000232 haloalkynyl group Chemical group 0.000 claims 5
- 125000004447 heteroarylalkenyl group Chemical group 0.000 claims 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 5
- 125000005312 heteroarylalkynyl group Chemical group 0.000 claims 5
- 125000004449 heterocyclylalkenyl group Chemical group 0.000 claims 5
- 125000002785 azepinyl group Chemical group 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000004419 alkynylene group Chemical group 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000005605 benzo group Chemical group 0.000 claims 2
- 125000005876 benzo[b][1,4]oxazinyl group Chemical group 0.000 claims 2
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 1
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2926508P | 2008-02-15 | 2008-02-15 | |
| US61/029,265 | 2008-02-15 | ||
| US3867208P | 2008-03-21 | 2008-03-21 | |
| US61/038,672 | 2008-03-21 | ||
| US11204608P | 2008-11-06 | 2008-11-06 | |
| US61/112,046 | 2008-11-06 | ||
| PCT/US2009/034159 WO2009103032A1 (en) | 2008-02-15 | 2009-02-13 | Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014224663A Division JP2015061846A (ja) | 2008-02-15 | 2014-11-04 | ピリミジン−２−アミン化合物およびｊａｋキナーゼの阻害剤としてのその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011512361A JP2011512361A (ja) | 2011-04-21 |
| JP2011512361A5 true JP2011512361A5 (enExample) | 2012-03-29 |
| JP5711537B2 JP5711537B2 (ja) | 2015-05-07 |
Family
ID=40591956
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010546945A Expired - Fee Related JP5711537B2 (ja) | 2008-02-15 | 2009-02-13 | ピリミジン−２−アミン化合物およびｊａｋキナーゼの阻害剤としてのその使用 |
| JP2014224663A Pending JP2015061846A (ja) | 2008-02-15 | 2014-11-04 | ピリミジン−２−アミン化合物およびｊａｋキナーゼの阻害剤としてのその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014224663A Pending JP2015061846A (ja) | 2008-02-15 | 2014-11-04 | ピリミジン−２−アミン化合物およびｊａｋキナーゼの阻害剤としてのその使用 |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US8309566B2 (enExample) |
| EP (1) | EP2265607B1 (enExample) |
| JP (2) | JP5711537B2 (enExample) |
| KR (1) | KR101700454B1 (enExample) |
| CN (1) | CN102007124B (enExample) |
| AU (1) | AU2009214440B2 (enExample) |
| CA (1) | CA2715658C (enExample) |
| CY (1) | CY1118969T1 (enExample) |
| DK (1) | DK2265607T3 (enExample) |
| ES (1) | ES2617622T3 (enExample) |
| HR (1) | HRP20170317T1 (enExample) |
| HU (1) | HUE030912T2 (enExample) |
| IL (1) | IL207609A (enExample) |
| LT (1) | LT2265607T (enExample) |
| MX (1) | MX2010008926A (enExample) |
| NZ (1) | NZ587589A (enExample) |
| PL (1) | PL2265607T3 (enExample) |
| PT (1) | PT2265607T (enExample) |
| SI (1) | SI2265607T1 (enExample) |
| WO (1) | WO2009103032A1 (enExample) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
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| EP2074115B1 (en) * | 2006-12-29 | 2018-03-07 | Rigel Pharmaceuticals, Inc. | N3-heteroaryl substituted triazoles and n5-heteroaryl substituted triazoles useful as axl inhibitors |
| US8012965B2 (en) | 2006-12-29 | 2011-09-06 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| AU2007342007A1 (en) | 2006-12-29 | 2008-07-10 | Rigel Pharmaceuticals, Inc. | Substituted triazoles useful as Axl inhibitors |
| WO2008083353A1 (en) | 2006-12-29 | 2008-07-10 | Rigel Pharmaceuticals, Inc. | Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| EP2078010B1 (en) | 2006-12-29 | 2014-01-29 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| WO2009032861A1 (en) | 2007-09-04 | 2009-03-12 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
| ES2424259T3 (es) * | 2007-10-26 | 2013-09-30 | Rigel Pharmaceuticals, Inc. | Triazoles sustituidos con arilo policíclico y heteroarilo policíclico, útiles como agentes inhibidores del Axl |
| LT2265607T (lt) | 2008-02-15 | 2017-03-27 | Rigel Pharmaceuticals, Inc. | Pirimidin-2-amino junginiai ir jų panaudojimas kaip jak kinazių slopiklių |
| JP5592884B2 (ja) | 2008-07-09 | 2014-09-17 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ａｘｌ阻害剤として有用な多環式ヘテロアリール置換トリアゾール |
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| CA2749843C (en) | 2009-01-16 | 2017-09-05 | Rigel Pharmaceuticals, Inc. | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
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| PH12013500880A1 (en) | 2010-11-10 | 2013-07-01 | Hoffmann La Roche | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
| CN103619172A (zh) | 2011-05-10 | 2014-03-05 | 默沙东公司 | 作为syk抑制剂的氨基嘧啶 |
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| US9206127B2 (en) | 2012-03-16 | 2015-12-08 | Purdue Pharm, L.P. | Substituted pyridines as sodium channel blockers |
| WO2013173506A2 (en) | 2012-05-16 | 2013-11-21 | Rigel Pharmaceuticals, Inc. | Method of treating muscular degradation |
| US8809359B2 (en) * | 2012-06-29 | 2014-08-19 | Ym Biosciences Australia Pty Ltd | Phenyl amino pyrimidine bicyclic compounds and uses thereof |
| CN103709172B (zh) * | 2012-09-28 | 2018-02-13 | 江苏先声药业有限公司 | 取代呋喃并哌啶衍生物及其应用 |
| US9714252B2 (en) | 2012-12-20 | 2017-07-25 | Purdue Pharma L.P. | Cyclic sulfonamides as sodium channel blockers |
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| ES2618072T3 (es) * | 2013-08-07 | 2017-06-20 | Cadila Healthcare Limited | N-Cianometilamidas como inhibidores de la quinasa Janus |
| CN111493682A (zh) * | 2013-08-26 | 2020-08-07 | 皇家飞利浦有限公司 | 用于准备食物的具有带滑动机构的抽屉的装置 |
| CN104860941B (zh) * | 2014-02-25 | 2017-03-22 | 上海海雁医药科技有限公司 | 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物 |
| US10730866B2 (en) | 2014-04-07 | 2020-08-04 | Purdue Pharma L.P. | Indole derivatives and use thereof |
| BR112017019286B1 (pt) * | 2015-03-11 | 2023-02-14 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Derivados de 2h-pirazol substituídos ou um sal farmacêuticamente aceitável dos mesmos |
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| CN106810536A (zh) * | 2015-11-30 | 2017-06-09 | 甘李药业股份有限公司 | 一种蛋白激酶抑制剂及其制备方法和医药用途 |
| GB201702947D0 (en) | 2017-02-23 | 2017-04-12 | Domainex Ltd | Novel compounds |
| US12171764B2 (en) | 2018-06-20 | 2024-12-24 | Biora Therapeutics, Inc. | Treatment of a disease of the gastrointestinal tract with a JAK or other kinase inhibitor |
| CN114364675A (zh) | 2019-05-05 | 2022-04-15 | 上海齐鲁锐格医药研发有限公司 | Cdk抑制剂 |
| US20220372135A1 (en) | 2019-09-27 | 2022-11-24 | Disc Medicine, Inc. | Methods for treating myelofibrosis and related conditions |
| IL297437A (en) | 2020-05-13 | 2022-12-01 | Disc Medicine Inc | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| CN113880813B (zh) * | 2020-07-01 | 2024-05-28 | 杭州百诚医药科技股份有限公司 | 一种2-氨基嘧啶类杂环化合物及应用 |
| CN116113628A (zh) * | 2020-08-31 | 2023-05-12 | 甘李药业股份有限公司 | 一种含cdk4/6抑制剂的药物组合物 |
| JP2024502175A (ja) * | 2021-01-07 | 2024-01-17 | オンタリオ・インスティテュート・フォー・キャンサー・リサーチ（オーアイシーアール） | Ｎｕａｋキナーゼの阻害剤としてのイソインドリノンアミノピリミジン化合物、その組成物及び使用 |
| CN115073425B (zh) * | 2021-03-16 | 2023-11-14 | 中国科学院上海药物研究所 | 一类作为tbk1抑制剂的化合物、包含其的药物组合物及其用途 |
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-
2009
- 2009-02-13 LT LTEP09710734.6T patent/LT2265607T/lt unknown
- 2009-02-13 HU HUE09710734A patent/HUE030912T2/en unknown
- 2009-02-13 CN CN200980113512.6A patent/CN102007124B/zh not_active Expired - Fee Related
- 2009-02-13 WO PCT/US2009/034159 patent/WO2009103032A1/en not_active Ceased
- 2009-02-13 JP JP2010546945A patent/JP5711537B2/ja not_active Expired - Fee Related
- 2009-02-13 DK DK09710734.6T patent/DK2265607T3/en active
- 2009-02-13 KR KR1020107020561A patent/KR101700454B1/ko not_active Expired - Fee Related
- 2009-02-13 NZ NZ587589A patent/NZ587589A/xx not_active IP Right Cessation
- 2009-02-13 CA CA2715658A patent/CA2715658C/en active Active
- 2009-02-13 EP EP09710734.6A patent/EP2265607B1/en active Active
- 2009-02-13 AU AU2009214440A patent/AU2009214440B2/en not_active Ceased
- 2009-02-13 HR HRP20170317TT patent/HRP20170317T1/hr unknown
- 2009-02-13 US US12/371,550 patent/US8309566B2/en not_active Expired - Fee Related
- 2009-02-13 PT PT97107346T patent/PT2265607T/pt unknown
- 2009-02-13 ES ES09710734.6T patent/ES2617622T3/es active Active
- 2009-02-13 SI SI200931620A patent/SI2265607T1/sl unknown
- 2009-02-13 MX MX2010008926A patent/MX2010008926A/es active IP Right Grant
- 2009-02-13 PL PL09710734T patent/PL2265607T3/pl unknown
-
2010
- 2010-08-12 IL IL207609A patent/IL207609A/en active IP Right Grant
-
2012
- 2012-09-14 US US13/619,843 patent/US8735418B2/en active Active
-
2014
- 2014-04-02 US US14/243,579 patent/US9624229B2/en not_active Expired - Fee Related
- 2014-11-04 JP JP2014224663A patent/JP2015061846A/ja active Pending
-
2017
- 2017-03-13 CY CY20171100312T patent/CY1118969T1/el unknown
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