JP2011529073A5 - - Google Patents
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- Publication number
- JP2011529073A5 JP2011529073A5 JP2011520196A JP2011520196A JP2011529073A5 JP 2011529073 A5 JP2011529073 A5 JP 2011529073A5 JP 2011520196 A JP2011520196 A JP 2011520196A JP 2011520196 A JP2011520196 A JP 2011520196A JP 2011529073 A5 JP2011529073 A5 JP 2011529073A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- heterocyclyl
- heteroaryl
- alkenyl
- 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.)
- Withdrawn
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- 125000000217 alkyl group Chemical group 0.000 claims 45
- 125000000623 heterocyclic group Chemical group 0.000 claims 33
- 229910052739 hydrogen Inorganic materials 0.000 claims 25
- 239000001257 hydrogen Substances 0.000 claims 25
- 125000001072 heteroaryl group Chemical group 0.000 claims 24
- 125000004452 carbocyclyl group Chemical group 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- -1 amino, substituted amino, amide Chemical class 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 12
- 125000003545 alkoxy group Chemical group 0.000 claims 11
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 11
- 125000000547 substituted alkyl group Chemical group 0.000 claims 11
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical class *C#N 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- RGICCULPCWNRAB-UHFFFAOYSA-N 2-[2-(2-hexoxyethoxy)ethoxy]ethanol Chemical compound CCCCCCOCCOCCOCCO RGICCULPCWNRAB-UHFFFAOYSA-N 0.000 claims 4
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 150000001408 amides Chemical class 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 3
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- NMPVEAUIHMEAQP-UHFFFAOYSA-N 2-Bromoacetaldehyde Chemical compound BrCC=O NMPVEAUIHMEAQP-UHFFFAOYSA-N 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- FUSFWUFSEJXMRQ-UHFFFAOYSA-N 2-bromo-1,1-dimethoxyethane Chemical compound COC(CBr)OC FUSFWUFSEJXMRQ-UHFFFAOYSA-N 0.000 claims 1
- CRZJPEIBPQWDGJ-UHFFFAOYSA-N 2-chloro-1,1-dimethoxyethane Chemical compound COC(CCl)OC CRZJPEIBPQWDGJ-UHFFFAOYSA-N 0.000 claims 1
- QSKPIOLLBIHNAC-UHFFFAOYSA-N 2-chloro-acetaldehyde Chemical compound ClCC=O QSKPIOLLBIHNAC-UHFFFAOYSA-N 0.000 claims 1
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 208000037979 autoimmune inflammatory disease Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 239000003153 chemical reaction reagent Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 0 C*1*CCC1 Chemical compound C*1*CCC1 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8327108P | 2008-07-24 | 2008-07-24 | |
| US61/083,271 | 2008-07-24 | ||
| PCT/US2009/051536 WO2010011837A1 (en) | 2008-07-24 | 2009-07-23 | Fused heterocyclic compounds useful as kinase modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011529073A JP2011529073A (ja) | 2011-12-01 |
| JP2011529073A5 true JP2011529073A5 (enExample) | 2012-07-26 |
Family
ID=41119904
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011520196A Withdrawn JP2011529073A (ja) | 2008-07-24 | 2009-07-23 | キナーゼ調節因子として有用な縮合ヘテロ環化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8476430B2 (enExample) |
| EP (1) | EP2323665B1 (enExample) |
| JP (1) | JP2011529073A (enExample) |
| CN (1) | CN102164604A (enExample) |
| WO (1) | WO2010011837A1 (enExample) |
Families Citing this family (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101981033B (zh) | 2008-02-06 | 2015-02-04 | 百时美施贵宝公司 | 用作激酶抑制剂的取代的咪唑并哒嗪化合物 |
| ES2651296T3 (es) | 2009-10-30 | 2018-01-25 | Janssen Pharmaceutica, N.V. | Derivados de imidazo[1,2-b]piridacina y su uso como inhibidores de PDE10 |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| JP6115962B2 (ja) | 2011-06-27 | 2017-04-19 | ヤンセン ファーマシューティカ エヌ．ベー． | １−アリール−４−メチル−［１，２，４］トリアゾロ［４，３−ａ］キノキサリン誘導体 |
| JP5808869B2 (ja) * | 2011-11-03 | 2015-11-10 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 二環式ピペラジン化合物 |
| JPWO2013133367A1 (ja) * | 2012-03-09 | 2015-07-30 | カルナバイオサイエンス株式会社 | 新規トリアジン誘導体 |
| US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
| JP6426603B2 (ja) | 2012-06-26 | 2018-11-21 | ヤンセン ファーマシューティカ エヌ．ベー． | 神経障害または代謝障害の治療に使用するための、１−アリール−４−メチル−［１，２，４］トリアゾロ［４，３−ａ］−キノキサリン化合物などのＰＤＥ２阻害剤とＰＤＥ１０阻害剤との組合せ |
| KR102171706B1 (ko) | 2012-07-09 | 2020-10-30 | 얀센 파마슈티카 엔.브이. | 포스포디에스테라아제 10 효소의 억제제 |
| 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 |
| CA2902686C (en) | 2013-04-25 | 2017-01-24 | Beigene, Ltd. | Fused heterocyclic compounds as protein kinase inhibitors |
| CN108715615B (zh) | 2013-09-13 | 2020-11-27 | 百济神州(广州)生物科技有限公司 | 抗pd1抗体及其作为治疗剂与诊断剂的用途 |
| CN104086551B (zh) * | 2014-06-06 | 2016-09-21 | 人福医药集团股份公司 | 化合物及其制备方法和用途 |
| CN110156892B (zh) | 2014-07-03 | 2023-05-16 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
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| CA2984496A1 (en) * | 2015-05-12 | 2016-11-17 | Kalyra Pharmaceuticals, Inc. | Bicyclic compounds |
| WO2017070089A1 (en) | 2015-10-19 | 2017-04-27 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| RS63762B1 (sr) | 2015-11-19 | 2022-12-30 | Incyte Corp | Heterociklična jedinjenja kao imunomodulatori |
| EP3390361B1 (en) | 2015-12-17 | 2022-03-16 | Incyte Corporation | N-phenyl-pyridine-2-carboxamide derivatives and their use as pd-1/pd-l1 protein/protein interaction modulators |
| TWI767896B (zh) | 2015-12-22 | 2022-06-21 | 美商英塞特公司 | 作為免疫調節劑之雜環化合物 |
| AR108396A1 (es) | 2016-05-06 | 2018-08-15 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| ES2905980T3 (es) | 2016-05-26 | 2022-04-12 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| CN109890819B (zh) | 2016-06-20 | 2022-11-22 | 因赛特公司 | 作为免疫调节剂的杂环化合物 |
| JP6993056B2 (ja) | 2016-07-05 | 2022-02-15 | ベイジーン リミテッド | 癌治療のためのｐｄ－１アンタゴニスト及びｒａｆ阻害剤の組合せ |
| EP3484866B1 (en) | 2016-07-14 | 2022-09-07 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| CN116478166A (zh) | 2016-08-16 | 2023-07-25 | 百济神州(苏州)生物科技有限公司 | 一种化合物的晶型、其制备和用途 |
| DK3500299T3 (da) | 2016-08-19 | 2024-01-29 | Beigene Switzerland Gmbh | Kombination af zanubrutinib med et anti-CD20- eller et anti-PD-1-antistof til anvendelse i behandling af cancer |
| WO2018044783A1 (en) | 2016-08-29 | 2018-03-08 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| MX390121B (es) | 2016-09-19 | 2025-03-20 | Mei Pharma Inc | Combinaciones de un inhibidor de btk y un inhibidor de pi3k para tratar neoplasias malignas hematológicas. |
| SMT202200415T1 (it) | 2016-12-22 | 2022-11-18 | Incyte Corp | Derivati di tetraidro imidazo[4,5-c]piridina come induttori di internalizzazione di pd-l1 |
| GEAP202215134A (en) | 2016-12-22 | 2022-05-10 | Incyte Corp | Heterocyclic compounds as immunomodulators |
| EP3558963B1 (en) | 2016-12-22 | 2022-03-23 | Incyte Corporation | Bicyclic heteroaromatic compounds as immunomodulators |
| WO2018119221A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Pyridine derivatives as immunomodulators |
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| US11555038B2 (en) | 2017-01-25 | 2023-01-17 | Beigene, Ltd. | Crystalline forms of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
| CN110799543A (zh) | 2017-06-26 | 2020-02-14 | 百济神州有限公司 | 肝细胞癌的免疫治疗 |
| US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
| CN111801334B (zh) | 2017-11-29 | 2023-06-09 | 百济神州瑞士有限责任公司 | 使用包含btk抑制剂的组合治疗惰性或侵袭性b-细胞淋巴瘤 |
| WO2019152719A1 (en) | 2018-01-31 | 2019-08-08 | Deciphera Pharmaceuticals, Llc | Combination therapy for the treatment of mastocytosis |
| EP3746059A1 (en) | 2018-01-31 | 2020-12-09 | Deciphera Pharmaceuticals, LLC | Combination therapy for the treatment of gastrointestinal stromal tumors |
| AU2019232437A1 (en) | 2018-03-07 | 2020-10-08 | Bayer Aktiengesellschaft | Identification and use of ERK5 inhibitors |
| PL4212529T3 (pl) | 2018-03-30 | 2025-07-07 | Incyte Corporation | Związki heterocykliczne jako immunomodulatory |
| JOP20200288A1 (ar) | 2018-05-11 | 2020-11-11 | Incyte Corp | مشتقات تترا هيدرو – إيميدازو[4، 5-c]بيريدين كمعدِّلات مناعية pd-l1 |
| US12509456B2 (en) | 2019-03-11 | 2025-12-30 | Deciphera Pharmaceuticals, Llc | Solid state forms of ripretinib |
| CN111825675B (zh) * | 2019-04-15 | 2023-08-01 | 武汉朗来科技发展有限公司 | Rock抑制剂及其制备方法和用途 |
| EP3972963A1 (en) | 2019-05-21 | 2022-03-30 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| EP3981399A4 (en) | 2019-06-10 | 2023-05-31 | BeiGene Switzerland GmbH | ORAL SOLID TABLET WITH A TYROSINE KINAS INHIBITOR AND METHOD OF MANUFACTURE THEREOF |
| TW202115059A (zh) | 2019-08-09 | 2021-04-16 | 美商英塞特公司 | Ｐｄ—１／ｐｄ—ｌ１抑制劑之鹽 |
| CA3150433A1 (en) | 2019-08-12 | 2021-02-18 | Deciphera Pharmaceuticals, Llc | Ripretinib for treating gastrointestinal stromal tumors |
| TWI878335B (zh) | 2019-08-12 | 2025-04-01 | 美商迪賽孚爾製藥有限公司 | 治療胃腸道基質瘤方法 |
| AR120109A1 (es) | 2019-09-30 | 2022-02-02 | Incyte Corp | Compuestos de pirido[3,2-d]pirimidina como inmunomoduladores |
| CR20220237A (es) | 2019-11-11 | 2022-08-05 | Incyte Corp | Sales y formas cristalinas de un inhibidor de pd-1/pd-l1 |
| DK4084779T3 (da) | 2019-12-30 | 2024-12-16 | Deciphera Pharmaceuticals Llc | Sammensætninger af 1-(4-brom-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro- 1,6-naphthyridin-3-yl)-2-fluorphenyl)-3-phenylurea |
| CN119970649A (zh) | 2019-12-30 | 2025-05-13 | 德西费拉制药有限责任公司 | 非晶型激酶抑制剂制剂及其使用方法 |
| IL302590A (en) | 2020-11-06 | 2023-07-01 | Incyte Corp | Process for preparing PD-1/PD-L1 inhibitor and salts and crystalline forms thereof |
| WO2022099018A1 (en) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Process of preparing a pd-1/pd-l1 inhibitor |
| TW202233615A (zh) | 2020-11-06 | 2022-09-01 | 美商英塞特公司 | Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式 |
| CN118715225A (zh) * | 2022-01-20 | 2024-09-27 | 原真股份有限公司 | Cdk9抑制剂 |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
| US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
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| US4327027A (en) * | 1979-06-15 | 1982-04-27 | Vertac Chemical Corporation | Chemical detoxification of toxic chlorinated aromatic compounds |
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| TWI312347B (en) | 2001-02-08 | 2009-07-21 | Eisai R&D Man Co Ltd | Bicyclic nitrogen-containing condensed ring compounds |
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| ES2289377T3 (es) | 2003-03-18 | 2008-02-01 | The Jordanian Pharmaceutical Manufacturing Co. Ltd. | Nuevas pirazolopirimidonas y su uso como inhibidores de pde. |
| US20060183746A1 (en) | 2003-06-04 | 2006-08-17 | Currie Kevin S | Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds |
| WO2005014599A1 (en) | 2003-06-04 | 2005-02-17 | Cellular Genomics, Inc. | Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds |
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| US20070078136A1 (en) * | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
| US7547782B2 (en) | 2005-09-30 | 2009-06-16 | Bristol-Myers Squibb Company | Met kinase inhibitors |
| US20100160292A1 (en) | 2006-09-11 | 2010-06-24 | Cgi Pharmaceuticals, Inc | Kinase Inhibitors, and Methods of Using and Identifying Kinase Inhibitors |
| WO2008037607A1 (de) | 2006-09-25 | 2008-04-03 | Basf Se | Carbonylgruppen-enthaltende heterocyclische verbindungen und deren verwendung zur bekämpfung von phytopathogenen pilzen |
| US7492329B2 (en) | 2006-10-12 | 2009-02-17 | Hewlett-Packard Development Company, L.P. | Composite material with chirped resonant cells |
| CN101730699A (zh) * | 2007-03-21 | 2010-06-09 | 百时美施贵宝公司 | 可用于治疗增殖性、变应性、自身免疫性和炎症性疾病的稠合杂环化合物 |
-
2009
- 2009-07-23 JP JP2011520196A patent/JP2011529073A/ja not_active Withdrawn
- 2009-07-23 WO PCT/US2009/051536 patent/WO2010011837A1/en not_active Ceased
- 2009-07-23 EP EP09790767.9A patent/EP2323665B1/en not_active Not-in-force
- 2009-07-23 CN CN2009801373694A patent/CN102164604A/zh active Pending
- 2009-07-23 US US13/055,601 patent/US8476430B2/en active Active
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