JP2013512903A5 - - Google Patents
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- JP2013512903A5 JP2013512903A5 JP2012542060A JP2012542060A JP2013512903A5 JP 2013512903 A5 JP2013512903 A5 JP 2013512903A5 JP 2012542060 A JP2012542060 A JP 2012542060A JP 2012542060 A JP2012542060 A JP 2012542060A JP 2013512903 A5 JP2013512903 A5 JP 2013512903A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- compound according
- heterocyclyl
- alkyl
- optionally
- 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 description 112
- 125000000623 heterocyclic group Chemical group 0.000 claims description 62
- 229910052717 sulfur Inorganic materials 0.000 claims description 34
- 125000001072 heteroaryl group Chemical group 0.000 claims description 33
- 229910052760 oxygen Inorganic materials 0.000 claims description 30
- 125000005842 heteroatom Chemical group 0.000 claims description 27
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 26
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 24
- 125000003107 substituted aryl group Chemical group 0.000 claims description 24
- 229910052757 nitrogen Inorganic materials 0.000 claims description 22
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 20
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 20
- 239000008194 pharmaceutical composition Substances 0.000 claims description 20
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 18
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 16
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 14
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims description 12
- 210000004027 cell Anatomy 0.000 claims description 12
- 239000012453 solvate Substances 0.000 claims description 12
- 125000005884 carbocyclylalkyl group Chemical group 0.000 claims description 11
- 239000003814 drug Substances 0.000 claims description 11
- 206010028980 Neoplasm Diseases 0.000 claims description 10
- 125000004432 carbon atom Chemical group C* 0.000 claims description 10
- 125000005843 halogen group Chemical group 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 229940002612 prodrug Drugs 0.000 claims description 10
- 239000000651 prodrug Substances 0.000 claims description 10
- 125000003118 aryl group Chemical group 0.000 claims description 9
- 201000011510 cancer Diseases 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 230000000694 effects Effects 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 229940124597 therapeutic agent Drugs 0.000 claims description 8
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 7
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000003282 alkyl amino group Chemical group 0.000 claims description 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 4
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims description 4
- 102000052052 Casein Kinase II Human genes 0.000 claims description 4
- 108010010919 Casein Kinase II Proteins 0.000 claims description 4
- 108091000080 Phosphotransferase Proteins 0.000 claims description 4
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 4
- 125000003342 alkenyl group Chemical group 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 4
- 239000002246 antineoplastic agent Substances 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 201000005787 hematologic cancer Diseases 0.000 claims description 4
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 210000004185 liver Anatomy 0.000 claims description 4
- 125000003884 phenylalkyl group Chemical group 0.000 claims description 4
- 102000020233 phosphotransferase Human genes 0.000 claims description 4
- 201000000849 skin cancer Diseases 0.000 claims description 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 4
- 230000033115 angiogenesis Effects 0.000 claims description 3
- 230000004663 cell proliferation Effects 0.000 claims description 3
- 229940079593 drug Drugs 0.000 claims description 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 2
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims description 2
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims description 2
- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 210000004369 blood Anatomy 0.000 claims description 2
- 239000008280 blood Substances 0.000 claims description 2
- 210000004556 brain Anatomy 0.000 claims description 2
- 210000000481 breast Anatomy 0.000 claims description 2
- 210000001072 colon Anatomy 0.000 claims description 2
- 125000004122 cyclic group Chemical group 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 210000003128 head Anatomy 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 201000010235 heart cancer Diseases 0.000 claims description 2
- 208000024348 heart neoplasm Diseases 0.000 claims description 2
- 208000026278 immune system disease Diseases 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 210000003734 kidney Anatomy 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 210000001165 lymph node Anatomy 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 208000026037 malignant tumor of neck Diseases 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 210000003739 neck Anatomy 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 210000000496 pancreas Anatomy 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 230000001717 pathogenic effect Effects 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 210000002307 prostate Anatomy 0.000 claims description 2
- 210000003491 skin Anatomy 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 208000019553 vascular disease Diseases 0.000 claims description 2
- 125000002704 decyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 0 CCCCN=C(*C)C(CCCC*C(*)=C(C)C(C)=C)=C(C)I*C(C)CC*C=C(C)N(*)[*+]C Chemical compound CCCCN=C(*C)C(CCCC*C(*)=C(C)C(C)=C)=C(C)I*C(C)CC*C=C(C)N(*)[*+]C 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 230000009707 neogenesis Effects 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26680109P | 2009-12-04 | 2009-12-04 | |
| US61/266,801 | 2009-12-04 | ||
| US35416510P | 2010-06-11 | 2010-06-11 | |
| US61/354,165 | 2010-06-11 | ||
| PCT/US2010/056712 WO2011068667A1 (en) | 2009-12-04 | 2010-11-15 | Pyrazolopyrimidines and related heterocycles as ck2 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013512903A JP2013512903A (ja) | 2013-04-18 |
| JP2013512903A5 true JP2013512903A5 (enExample) | 2013-12-19 |
| JP5802676B2 JP5802676B2 (ja) | 2015-10-28 |
Family
ID=44115232
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012542060A Active JP5802676B2 (ja) | 2009-12-04 | 2010-11-15 | Ｃｋ２阻害剤としてのピラゾロピリミジンおよび関連複素環化合物 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US8575177B2 (enExample) |
| EP (1) | EP2509602B9 (enExample) |
| JP (1) | JP5802676B2 (enExample) |
| KR (1) | KR101851130B1 (enExample) |
| CN (1) | CN102762208A (enExample) |
| AU (1) | AU2010326268B2 (enExample) |
| BR (1) | BR112012013508A2 (enExample) |
| CA (1) | CA2782684C (enExample) |
| ES (1) | ES2629170T3 (enExample) |
| IL (1) | IL220086B (enExample) |
| PL (1) | PL2509602T3 (enExample) |
| RU (1) | RU2607453C2 (enExample) |
| SG (1) | SG181507A1 (enExample) |
| WO (1) | WO2011068667A1 (enExample) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2801031A1 (en) * | 2010-06-01 | 2011-12-08 | Bayer Intellectual Property Gmbh | Substituted imidazopyrazines |
| NZ736048A (en) | 2010-06-03 | 2019-09-27 | Pharmacyclics Llc | The use of inhibitors of bruton’s tyrosine kinase (btk) |
| WO2012170827A2 (en) * | 2011-06-08 | 2012-12-13 | Cylene Pharmaceuticals, Inc. | Pyrazolopyrimidines and related heterocycles as ck2 inhibitors |
| EP2723746A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| CN104271786B (zh) * | 2012-04-27 | 2016-07-06 | 新日铁住金株式会社 | 无缝钢管及其制造方法 |
| MX367055B (es) | 2012-06-26 | 2019-08-02 | Del Mar Pharmaceuticals | El uso de una composición que comprende dianhidrogalactitol, diacetildianhidrogalactitol, y dibromodulcitol, y análogos o derivados de cada uno para el tratamiento de malignidades resistentes a inhibidores de tirosina cinasa. |
| TW201414737A (zh) * | 2012-07-13 | 2014-04-16 | 必治妥美雅史谷比公司 | 作爲激酶抑制劑之咪唑并三□甲腈 |
| KR20180088926A (ko) | 2012-07-24 | 2018-08-07 | 파마싸이클릭스 엘엘씨 | 브루톤 티로신 키나제(btk)의 억제제에 대한 내성과 관련된 돌연변이 |
| LT3486245T (lt) | 2012-12-07 | 2021-08-25 | Vertex Pharmaceuticals Incorporated | 2-amino-n-(piperidin-1-il-piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamidas, kaip atr kinazės inhibitorius |
| US9278950B2 (en) | 2013-01-14 | 2016-03-08 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| AU2014207691B2 (en) | 2013-01-15 | 2018-08-30 | Incyte Holdings Corporation | Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors |
| EP2970288A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体 |
| WO2014143241A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| CN105492011A (zh) | 2013-04-08 | 2016-04-13 | 丹尼斯·M·布朗 | 不理想给药化学化合物的治疗增效 |
| CN103360399B (zh) * | 2013-08-02 | 2016-03-02 | 北京大学 | 6-芳基取代-咪唑-[1,2-b]哒嗪类衍生物，其制备方法及用途 |
| WO2015027124A1 (en) | 2013-08-23 | 2015-02-26 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
| CN103570728B (zh) * | 2013-11-12 | 2015-12-30 | 山东大学 | 一种取代吡唑并[1,5-a]嘧啶类衍生物及其制备方法与应用 |
| CA2932757C (en) | 2013-12-06 | 2023-10-31 | Vertex Pharmaceuticals Incorporated | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
| EP3080131B1 (en) * | 2013-12-10 | 2018-10-10 | Bristol-Myers Squibb Company | Imidazopyridazine compounds useful as modulators of il-12, il-23 and/or ifn alpha responses |
| TWI534148B (zh) * | 2014-02-13 | 2016-05-21 | 生華生物科技股份有限公司 | 吡唑並嘧啶前藥及其使用方法 |
| GB201403093D0 (en) | 2014-02-21 | 2014-04-09 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| ES2738695T3 (es) * | 2014-05-28 | 2020-01-24 | Novartis Ag | Nuevos Derivados de Pirazolo Pirimidina y su uso como inhibidores de MALT1 |
| AU2015271030B2 (en) | 2014-06-05 | 2019-05-16 | Vertex Pharmaceuticals Incorporated | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo [1,5-a] pyrimidin-3-carboxamide compound useful as ATR kinase inhibitor, the preparation of said compound and different solid forms thereof |
| LT3157566T (lt) | 2014-06-17 | 2019-08-12 | Vertex Pharmaceuticals Incorporated | Vėžio gydymo būdas, panaudojant chk1 ir atr inhibitorių derinį |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| CN105457029A (zh) * | 2014-09-29 | 2016-04-06 | 中国科学院上海巴斯德研究所 | 抑制酪蛋白激酶2活性在促进i型干扰素表达的应用 |
| WO2016094688A1 (en) * | 2014-12-10 | 2016-06-16 | Massachusetts Institute Of Technology | Fused 1,3-azole derivatives useful for the treatment of proliferative diseases |
| CR20170339A (es) * | 2015-01-23 | 2018-01-22 | Glaxosmithkline Ip Dev Ltd | Derivados de pirazol[3,4-d] pirimidina y su uso para el tratamiento de leshmaniasis |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
| AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| WO2017059357A1 (en) | 2015-09-30 | 2017-04-06 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of dna damaging agents and atr inhibitors |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| CN109071456A (zh) | 2016-02-16 | 2018-12-21 | 麻省理工学院 | 作为myc调节剂的max结合剂及其用途 |
| EP3474855B1 (en) * | 2016-06-24 | 2022-01-26 | Polaris Pharmaceuticals, Inc. | Ck2 inhibitors, compositions and methods thereof |
| CN110831600B (zh) | 2017-04-21 | 2023-10-17 | 医肯纳肿瘤学公司 | 吲哚ahr抑制剂和其用途 |
| CN107188901A (zh) * | 2017-05-27 | 2017-09-22 | 无锡捷化医药科技有限公司 | 一种(3‑(3‑(二甲氨基)丙氧基)苯基)硼酸的制备方法 |
| KR102688084B1 (ko) | 2017-07-28 | 2024-07-24 | 주식회사유한양행 | 아미노피리미딘 유도체의 개선된 제조방법 |
| DK3658557T3 (da) | 2017-07-28 | 2024-07-29 | Takeda Pharmaceuticals Co | Tyk2-inhibitorer og anvendelser deraf |
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| US11071727B2 (en) | 2018-01-26 | 2021-07-27 | Northwestern University | Therapeutic targeting of proteolytic cleavage of the mixed lineage leukemia gene product (MLL1) by taspase1 using kinase inhibitors |
| CR20210202A (es) | 2018-10-30 | 2022-02-08 | Kronos Bio Inc | Compuestos, composiciones y métodos para modular la actividad cdk9 |
| CN112574214B (zh) * | 2019-07-30 | 2021-09-28 | 杭州阿诺生物医药科技有限公司 | 腺苷受体拮抗剂的制备方法 |
| FI4065582T3 (fi) | 2019-11-26 | 2025-05-25 | Ikena Oncology Inc | Polymorfisia karbatsolijohdannaisia ja niiden käyttötapoja |
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| WO2022149167A1 (en) * | 2021-01-09 | 2022-07-14 | Bugworks Research India Pvt Ltd | Diaminopyrazolo[1,5-a]pyrimidine-6-carbonitrile compounds as adenosine 2a receptor and adenosine 2b receptor antagonist |
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-
2010
- 2010-11-15 BR BR112012013508A patent/BR112012013508A2/pt not_active IP Right Cessation
- 2010-11-15 EP EP10834934.1A patent/EP2509602B9/en active Active
- 2010-11-15 PL PL10834934T patent/PL2509602T3/pl unknown
- 2010-11-15 WO PCT/US2010/056712 patent/WO2011068667A1/en not_active Ceased
- 2010-11-15 AU AU2010326268A patent/AU2010326268B2/en active Active
- 2010-11-15 CN CN2010800630542A patent/CN102762208A/zh active Pending
- 2010-11-15 CA CA2782684A patent/CA2782684C/en active Active
- 2010-11-15 ES ES10834934.1T patent/ES2629170T3/es active Active
- 2010-11-15 JP JP2012542060A patent/JP5802676B2/ja active Active
- 2010-11-15 SG SG2012041034A patent/SG181507A1/en unknown
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- 2010-11-15 KR KR1020127017450A patent/KR101851130B1/ko active Active
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