JP2013504593A5 - - Google Patents
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- Publication number
- JP2013504593A5 JP2013504593A5 JP2012528926A JP2012528926A JP2013504593A5 JP 2013504593 A5 JP2013504593 A5 JP 2013504593A5 JP 2012528926 A JP2012528926 A JP 2012528926A JP 2012528926 A JP2012528926 A JP 2012528926A JP 2013504593 A5 JP2013504593 A5 JP 2013504593A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- heteroalkyl
- alkyl
- carbocyclyl
- heterocyclylalkyl
- 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
Links
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 127
- 125000000623 heterocyclic group Chemical group 0.000 claims description 103
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 86
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 80
- 125000005884 carbocyclylalkyl group Chemical group 0.000 claims description 78
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 76
- 125000001072 heteroaryl group Chemical group 0.000 claims description 76
- 125000000217 alkyl group Chemical group 0.000 claims description 75
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 70
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 60
- 125000001188 haloalkyl group Chemical group 0.000 claims description 52
- 125000003118 aryl group Chemical group 0.000 claims description 45
- 125000002947 alkylene group Chemical group 0.000 claims description 40
- 125000004447 heteroarylalkenyl group Chemical group 0.000 claims description 40
- 125000005312 heteroarylalkynyl group Chemical group 0.000 claims description 40
- 125000004449 heterocyclylalkenyl group Chemical group 0.000 claims description 40
- 125000005015 aryl alkynyl group Chemical group 0.000 claims description 39
- 150000001875 compounds Chemical class 0.000 claims description 36
- 125000004474 heteroalkylene group Chemical group 0.000 claims description 36
- 125000005018 aryl alkenyl group Chemical group 0.000 claims description 34
- 125000003107 substituted aryl group Chemical group 0.000 claims description 29
- 125000003342 alkenyl group Chemical group 0.000 claims description 27
- 229910052736 halogen Inorganic materials 0.000 claims description 24
- 150000002367 halogens Chemical class 0.000 claims description 24
- 125000000304 alkynyl group Chemical group 0.000 claims description 22
- 150000003839 salts Chemical class 0.000 claims description 22
- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 22
- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 22
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 20
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 16
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 12
- 229910052757 nitrogen Inorganic materials 0.000 claims description 12
- 229910052760 oxygen Inorganic materials 0.000 claims description 11
- 208000036142 Viral infection Diseases 0.000 claims description 9
- 125000005842 heteroatom Chemical group 0.000 claims description 9
- 230000009385 viral infection Effects 0.000 claims description 9
- 125000004450 alkenylene group Chemical group 0.000 claims description 8
- 125000004419 alkynylene group Chemical group 0.000 claims description 8
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims description 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 8
- 229910052717 sulfur Inorganic materials 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 7
- 108020000999 Viral RNA Proteins 0.000 claims description 6
- 230000003612 virological effect Effects 0.000 claims description 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 5
- 229910052799 carbon Inorganic materials 0.000 claims description 5
- 238000004519 manufacturing process Methods 0.000 claims description 5
- 206010004146 Basal cell carcinoma Diseases 0.000 claims description 4
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 4
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 4
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 4
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 4
- 206010039085 Rhinitis allergic Diseases 0.000 claims description 4
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 4
- 201000010105 allergic rhinitis Diseases 0.000 claims description 4
- 125000000732 arylene group Chemical group 0.000 claims description 4
- 208000006673 asthma Diseases 0.000 claims description 4
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 4
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 4
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 4
- 125000005549 heteroarylene group Chemical group 0.000 claims description 4
- 206010022000 influenza Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 4
- -1 -OH Chemical group 0.000 claims description 3
- 229910052739 hydrogen Inorganic materials 0.000 claims description 3
- 239000001257 hydrogen Substances 0.000 claims description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 239000000654 additive Substances 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000001301 oxygen Substances 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 3
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- KWEDUNSJJZVRKR-UHFFFAOYSA-N carbononitridic azide Chemical compound [N-]=[N+]=NC#N KWEDUNSJJZVRKR-UHFFFAOYSA-N 0.000 description 6
- 238000000034 method Methods 0.000 description 3
- 230000001154 acute effect Effects 0.000 description 2
- 230000001684 chronic effect Effects 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 125000003627 8 membered carbocyclic group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24219409P | 2009-09-14 | 2009-09-14 | |
| US61/242,194 | 2009-09-14 | ||
| PCT/US2010/048424 WO2011031965A1 (en) | 2009-09-14 | 2010-09-10 | Modulators of toll-like receptors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013504593A JP2013504593A (ja) | 2013-02-07 |
| JP2013504593A5 true JP2013504593A5 (https=) | 2013-10-31 |
| JP5763077B2 JP5763077B2 (ja) | 2015-08-12 |
Family
ID=43332257
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012528926A Active JP5763077B2 (ja) | 2009-09-14 | 2010-09-10 | トール様受容体のモジュレーター |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8476270B2 (https=) |
| EP (1) | EP2477987B1 (https=) |
| JP (1) | JP5763077B2 (https=) |
| AU (1) | AU2010292102B2 (https=) |
| CA (1) | CA2772253C (https=) |
| ES (1) | ES2661850T3 (https=) |
| NO (1) | NO2477987T3 (https=) |
| NZ (1) | NZ598384A (https=) |
| PL (1) | PL2477987T3 (https=) |
| PT (1) | PT2477987T (https=) |
| SI (1) | SI2477987T1 (https=) |
| WO (1) | WO2011031965A1 (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2467108T3 (es) | 2008-12-09 | 2014-06-11 | Gilead Sciences, Inc. | Moduladores de receptores tipo toll |
| EP2531194B1 (en) * | 2010-02-03 | 2018-04-18 | Signal Pharmaceuticals, LLC | Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors |
| WO2012167423A1 (en) * | 2011-06-08 | 2012-12-13 | Hutchison Medipharma Limited | Substituted pyridopyrazines as novel syk inhibitors |
| HK1199259A1 (en) | 2011-08-15 | 2015-06-26 | Intermune, Inc. | Lysophosphatidic acid receptor antagonists |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| BR112015026292B1 (pt) | 2013-04-17 | 2022-04-12 | Signal Pharmaceuticals, Llc | Uso de 1-etil-7-(2-metil-6-(1h-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino [2,3-b]pirazin-2(1h)- ona e métodos in vitro |
| BR112015026297B1 (pt) | 2013-04-17 | 2022-08-23 | Signal Pharmaceuticals, Llc | Uso de um inibidor da quinase tor e quinazolinona 5-substituída, composição farmacêutica que os compreende, e kit |
| US9782427B2 (en) | 2013-04-17 | 2017-10-10 | Signal Pharmaceuticals, Llc | Methods for treating cancer using TOR kinase inhibitor combination therapy |
| TW201521725A (zh) | 2013-04-17 | 2015-06-16 | Signal Pharm Llc | 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法 |
| AU2014254052B2 (en) | 2013-04-17 | 2019-06-06 | Signal Pharmaceuticals, Llc | Treatment of cancer with dihydropyrazino-pyrazines |
| US9937169B2 (en) | 2013-04-17 | 2018-04-10 | Signal Pharmaceuticals, Llc | Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy |
| TW201527300A (zh) | 2013-04-17 | 2015-07-16 | Signal Pharm Llc | 關於１－乙基－７－（２－甲基－６－（１Ｈ－１，２，４－三唑－３－基）吡啶－３－基）－３，４－二氫吡并［２，３－ｂ］吡－２（１Ｈ）－酮之醫藥調配物、方法、固態型式及使用方法 |
| EP3003313A1 (en) | 2013-05-29 | 2016-04-13 | Signal Pharmaceuticals, LLC | Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use |
| US9512129B2 (en) | 2014-04-16 | 2016-12-06 | Signal Pharmaceuticals, Llc | Solid forms comprising 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and a coformer |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| PT3166607T (pt) | 2014-07-11 | 2022-12-07 | Gilead Sciences Inc | Moduladores de receptores de tipo toll para o tratamento do vih |
| BR112017005100A2 (pt) * | 2014-09-16 | 2017-12-05 | Gilead Sciences Inc | métodos de preparação de moduladores de receptores do tipo toll |
| CA2960436C (en) | 2014-09-16 | 2021-01-05 | Gilead Sciences, Inc. | Solid forms of a toll-like receptor modulator |
| DK3236972T3 (en) | 2014-12-26 | 2021-10-04 | Univ Emory | Antivirale N4-hydroxycytidin-derivativer |
| RU2748833C2 (ru) | 2016-11-28 | 2021-05-31 | Цзянсу Хэнжуй Медсин Ко., Лтд. | Производное пиразоло-гетероарила, способ его получения и медицинское применение |
| TW201827442A (zh) * | 2017-01-24 | 2018-08-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 雜芳基並噻二嗪－２，２－二氧化物類衍生物、其製備方法及其在醫藥上的應用 |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| EP3636646A4 (en) | 2017-05-18 | 2020-12-09 | Jiangsu Hengrui Medicine Co., Ltd. | HETEROARYL PYRAZOL DERIVATIVE AND MANUFACTURING METHOD FOR IT AND MEDICAL USES THEREOF |
| EP3641772B1 (en) | 2017-06-22 | 2023-08-02 | Celgene Corporation | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| JP6804790B1 (ja) | 2017-12-07 | 2020-12-23 | エモリー ユニバーシティー | Ｎ４−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
| TWI707849B (zh) | 2018-02-13 | 2020-10-21 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
| KR102591947B1 (ko) | 2018-04-19 | 2023-10-25 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| CN112105620B (zh) | 2018-05-25 | 2026-02-24 | 正大天晴药业集团股份有限公司 | 用于治疗肺癌的tlr7激动剂及其药物组合 |
| CN111819178B (zh) | 2018-05-25 | 2022-04-12 | 江苏恒瑞医药股份有限公司 | 一种吡唑并杂芳基类衍生物盐酸盐的晶型及制备方法 |
| EP3820572B1 (en) | 2018-07-13 | 2023-08-16 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| US11236085B2 (en) | 2018-10-24 | 2022-02-01 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
| KR102514860B1 (ko) * | 2020-12-01 | 2023-03-29 | 한국과학기술연구원 | 5-ht7 세로토닌 수용체 활성 저해용 바이페닐 피롤리딘 및 바이페닐 다이하이드로이미다졸 유도체 및 이를 유효성분으로 포함하는 약학 조성물 |
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| US263470A (en) * | 1882-08-29 | Grate for boiler-furnaces | ||
| US29885A (en) * | 1860-09-04 | Improvement in harrows | ||
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| HU212924B (en) | 1989-05-25 | 1996-12-30 | Chiron Corp | Adjuvant formulation comprising a submicron oil droplet emulsion |
| JP2886570B2 (ja) | 1989-09-29 | 1999-04-26 | エーザイ株式会社 | 縮合ヘテロ環を有する化合物 |
| TW274550B (https=) | 1992-09-26 | 1996-04-21 | Hoechst Ag | |
| US5620978A (en) | 1994-01-03 | 1997-04-15 | State Of Oregon, Acting By And Through The Oregon State Board Of Higher Education, Acting For And On Behalf Of The Oregon Health Sciences University And The University Of Oregon, Eugene Oregon | 8-aza, 6-aza and 6,8-diaza-1,4-dihydroquinoxaline-2,3-diones and the use thereof as antagonists for the glycine/NMDA receptor |
| US5681835A (en) | 1994-04-25 | 1997-10-28 | Glaxo Wellcome Inc. | Non-steroidal ligands for the estrogen receptor |
| ZA973884B (en) | 1996-05-23 | 1998-11-06 | Du Pont Merck Pharma | Tetrahydropteridines and pyridylpiperazines for treatment of neurological disorders |
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| WO2009022185A2 (en) | 2007-08-16 | 2009-02-19 | Astrazeneca Ab | 6, 6-fused heterocycles, their pharmaceutical compositions and methos of use |
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| ES2467108T3 (es) * | 2008-12-09 | 2014-06-11 | Gilead Sciences, Inc. | Moduladores de receptores tipo toll |
-
2010
- 2010-09-10 NO NO10760831A patent/NO2477987T3/no unknown
- 2010-09-10 PL PL10760831T patent/PL2477987T3/pl unknown
- 2010-09-10 NZ NZ598384A patent/NZ598384A/en not_active IP Right Cessation
- 2010-09-10 US US12/879,697 patent/US8476270B2/en active Active
- 2010-09-10 ES ES10760831.7T patent/ES2661850T3/es active Active
- 2010-09-10 WO PCT/US2010/048424 patent/WO2011031965A1/en not_active Ceased
- 2010-09-10 AU AU2010292102A patent/AU2010292102B2/en active Active
- 2010-09-10 CA CA2772253A patent/CA2772253C/en active Active
- 2010-09-10 EP EP10760831.7A patent/EP2477987B1/en active Active
- 2010-09-10 SI SI201031640T patent/SI2477987T1/en unknown
- 2010-09-10 PT PT107608317T patent/PT2477987T/pt unknown
- 2010-09-10 JP JP2012528926A patent/JP5763077B2/ja active Active
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