JP2015503625A5 - - Google Patents
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- Publication number
- JP2015503625A5 JP2015503625A5 JP2014552357A JP2014552357A JP2015503625A5 JP 2015503625 A5 JP2015503625 A5 JP 2015503625A5 JP 2014552357 A JP2014552357 A JP 2014552357A JP 2014552357 A JP2014552357 A JP 2014552357A JP 2015503625 A5 JP2015503625 A5 JP 2015503625A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- alkynyl
- alkenyl
- substituted
- 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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- 229910052739 hydrogen Inorganic materials 0.000 claims description 102
- 125000000217 alkyl group Chemical group 0.000 claims description 101
- 239000001257 hydrogen Substances 0.000 claims description 98
- -1 C (O) NR 2 Chemical group 0.000 claims description 86
- 229910052736 halogen Inorganic materials 0.000 claims description 56
- 150000002367 halogens Chemical class 0.000 claims description 56
- 150000002431 hydrogen Chemical class 0.000 claims description 53
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 45
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 44
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 42
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 40
- 150000001875 compounds Chemical class 0.000 claims description 39
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 39
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 37
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 31
- 125000003118 aryl group Chemical group 0.000 claims description 30
- 150000003839 salts Chemical class 0.000 claims description 30
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims description 29
- 229910052717 sulfur Inorganic materials 0.000 claims description 29
- 125000000304 alkynyl group Chemical group 0.000 claims description 28
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims description 27
- 229910052760 oxygen Inorganic materials 0.000 claims description 27
- 125000000623 heterocyclic group Chemical group 0.000 claims description 26
- 125000003342 alkenyl group Chemical group 0.000 claims description 24
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims description 24
- 125000006598 aminocarbonylamino group Chemical group 0.000 claims description 24
- 125000004442 acylamino group Chemical group 0.000 claims description 20
- 125000004432 carbon atom Chemical group C* 0.000 claims description 13
- 125000001072 heteroaryl group Chemical group 0.000 claims description 13
- 125000005842 heteroatom Chemical group 0.000 claims description 13
- 229920006395 saturated elastomer Polymers 0.000 claims description 13
- 206010028980 Neoplasm Diseases 0.000 claims description 11
- 201000011510 cancer Diseases 0.000 claims description 11
- 125000002837 carbocyclic group Chemical group 0.000 claims description 11
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 10
- 125000006296 sulfonyl amino group Chemical group [H]N(*)S(*)(=O)=O 0.000 claims description 10
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 150000003573 thiols Chemical class 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 5
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 230000000069 prophylactic effect Effects 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 16
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 11
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 11
- 239000000203 mixture Substances 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 26
- 125000003545 alkoxy group Chemical group 0.000 description 24
- 125000003358 C2-C20 alkenyl group Chemical group 0.000 description 2
- 125000001188 haloalkyl group Chemical group 0.000 description 2
- 125000005843 halogen group Chemical group 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 0 *C(*)=CC(N(*)c1cccc(*c2c(c(*)c(*)[n]3*)c3nc(N(*)C(C=C)=CC=C(*)N3CCN(*)CC3)n2)c1)=O Chemical compound *C(*)=CC(N(*)c1cccc(*c2c(c(*)c(*)[n]3*)c3nc(N(*)C(C=C)=CC=C(*)N3CCN(*)CC3)n2)c1)=O 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 208000008839 Kidney Neoplasms Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 206010061535 Ovarian neoplasm Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 206010038389 Renal cancer Diseases 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- 201000007455 central nervous system cancer Diseases 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 208000029742 colonic neoplasm Diseases 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 201000010536 head and neck cancer Diseases 0.000 description 1
- 208000014829 head and neck neoplasm Diseases 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 201000010982 kidney cancer Diseases 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- 201000005202 lung cancer Diseases 0.000 description 1
- 208000020816 lung neoplasm Diseases 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 210000000496 pancreas Anatomy 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261586718P | 2012-01-13 | 2012-01-13 | |
| US61/586,718 | 2012-01-13 | ||
| PCT/US2013/021338 WO2013106792A1 (en) | 2012-01-13 | 2013-01-12 | Heterocyclic compounds and uses as anticancer agents. |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015503625A JP2015503625A (ja) | 2015-02-02 |
| JP2015503625A5 true JP2015503625A5 (OSRAM) | 2016-03-31 |
| JP6353788B2 JP6353788B2 (ja) | 2018-07-04 |
Family
ID=47604241
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014552357A Active JP6353788B2 (ja) | 2012-01-13 | 2013-01-12 | 抗がん剤としての複素環式化合物およびその使用 |
Country Status (8)
| Country | Link |
|---|---|
| US (3) | US10799504B2 (OSRAM) |
| EP (1) | EP2802568A1 (OSRAM) |
| JP (1) | JP6353788B2 (OSRAM) |
| CN (2) | CN104203924B (OSRAM) |
| AU (1) | AU2013207712B2 (OSRAM) |
| CA (1) | CA2861010A1 (OSRAM) |
| HK (1) | HK1203927A1 (OSRAM) |
| WO (1) | WO2013106792A1 (OSRAM) |
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| US9464089B2 (en) * | 2012-01-13 | 2016-10-11 | Acea Biosciences Inc. | Heterocyclic compounds and uses thereof |
| US9586965B2 (en) | 2012-01-13 | 2017-03-07 | Acea Biosciences Inc. | Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases |
| CN104203924B (zh) | 2012-01-13 | 2019-06-11 | 艾森生物科学公司 | 杂环化合物及其作为抗癌药的用途 |
| US9034885B2 (en) | 2012-01-13 | 2015-05-19 | Acea Biosciences Inc. | EGFR modulators and uses thereof |
| DK3019496T3 (da) * | 2013-07-11 | 2019-12-09 | Acea Therapeutics Inc | Pyrimidinderivater som kinaseinhibitorer |
| PH12019500143B1 (en) | 2013-08-23 | 2023-03-24 | Neupharma Inc | Certain chemical entities, compositions, and methods |
| CN104418858B (zh) * | 2013-08-30 | 2018-12-11 | 浙江医药股份有限公司新昌制药厂 | 2,6-二含氮取代的嘌呤衍生物及其制备方法和其药物组合物与应用 |
| UA115388C2 (uk) | 2013-11-21 | 2017-10-25 | Пфайзер Інк. | 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань |
| NO2718543T3 (OSRAM) * | 2014-02-04 | 2018-01-06 | ||
| NZ629796A (en) * | 2014-07-14 | 2015-12-24 | Signal Pharm Llc | Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use |
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| JP6769963B2 (ja) | 2014-08-29 | 2020-10-14 | ティエエッセ ファルマ ソチエタ レスポンサビリタ リミタータ | α−アミノ−β−カルボキシムコン酸セミアルデヒド脱炭酸酵素の阻害剤 |
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| AU2016220219B2 (en) * | 2015-02-17 | 2020-05-14 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| JP6861166B2 (ja) | 2015-03-27 | 2021-04-21 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | サイクリン依存性キナーゼの阻害剤 |
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| WO2018035061A1 (en) | 2016-08-15 | 2018-02-22 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| JP2020516682A (ja) | 2017-04-07 | 2020-06-11 | エイシア セラピューティクス， インコーポレイテッド | ピロロピリミジンキナーゼの薬学的な塩、物理的形態および組成物、ならびにその作製方法 |
| EP3675860B1 (en) * | 2017-08-28 | 2023-03-08 | Zhihong, Chen | Substituted pyrimidines, pharmaceutical compositions and therapeutic methods thereof |
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| EP3613738A1 (en) * | 2018-08-23 | 2020-02-26 | Lead Discovery Center GmbH | 4-substituted pyrrolo[2,3-b]pyridine as erbb modulators useful for treating cancer |
| EP3876939A4 (en) | 2018-11-07 | 2022-08-10 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| CA3124422A1 (en) | 2018-12-28 | 2020-07-02 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 and uses thereof |
| US11691963B2 (en) | 2020-05-06 | 2023-07-04 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors |
| TW202241889A (zh) | 2020-12-23 | 2022-11-01 | 美商雅捷可斯治療公司 | 作為ｊａｋ２抑制劑之６－雜芳基氧基苯并咪唑及氮雜苯并咪唑 |
| US12162881B2 (en) | 2021-11-09 | 2024-12-10 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of JAK2 |
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| WO2024092047A1 (en) * | 2022-10-26 | 2024-05-02 | Sorrento Therapeutics, Inc. | Administration of pyrrolopyrimidine-based kinase inhibitors for treatment of psoriasis |
| WO2025155780A1 (en) * | 2024-01-17 | 2025-07-24 | Ohio State Innovation Foundation | Ttk kinase inhibitors and methods of use |
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| US9034885B2 (en) | 2012-01-13 | 2015-05-19 | Acea Biosciences Inc. | EGFR modulators and uses thereof |
| IN2015DN00914A (OSRAM) | 2012-08-06 | 2015-06-12 | Acea Biosciences Inc | |
| DK3019496T3 (da) | 2013-07-11 | 2019-12-09 | Acea Therapeutics Inc | Pyrimidinderivater som kinaseinhibitorer |
| CN104306348B (zh) | 2014-09-30 | 2017-05-31 | 地奥集团成都药业股份有限公司 | 一种辛伐他汀片及其制备方法 |
| MX2018004332A (es) | 2015-10-09 | 2019-01-10 | Acea Therapeutics Inc | Sales farmaceuticas, formas fisicas y composiciones de inhibidores de pirrolopirimidina cinasa, y metodos para fabricar las mismas. |
| JP2020516682A (ja) | 2017-04-07 | 2020-06-11 | エイシア セラピューティクス， インコーポレイテッド | ピロロピリミジンキナーゼの薬学的な塩、物理的形態および組成物、ならびにその作製方法 |
-
2013
- 2013-01-12 CN CN201380013279.0A patent/CN104203924B/zh active Active
- 2013-01-12 JP JP2014552357A patent/JP6353788B2/ja active Active
- 2013-01-12 EP EP13701326.4A patent/EP2802568A1/en not_active Withdrawn
- 2013-01-12 HK HK15104284.0A patent/HK1203927A1/xx unknown
- 2013-01-12 CA CA2861010A patent/CA2861010A1/en not_active Abandoned
- 2013-01-12 US US13/740,182 patent/US10799504B2/en active Active
- 2013-01-12 AU AU2013207712A patent/AU2013207712B2/en not_active Ceased
- 2013-01-12 CN CN201910414017.4A patent/CN110194748A/zh active Pending
- 2013-01-12 WO PCT/US2013/021338 patent/WO2013106792A1/en not_active Ceased
-
2017
- 2017-02-17 US US15/435,722 patent/US10596174B2/en active Active
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2020
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