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 (enExample) | 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 (enExample) |
| EP (1) | EP2477987B1 (enExample) |
| JP (1) | JP5763077B2 (enExample) |
| AU (1) | AU2010292102B2 (enExample) |
| CA (1) | CA2772253C (enExample) |
| ES (1) | ES2661850T3 (enExample) |
| NO (1) | NO2477987T3 (enExample) |
| NZ (1) | NZ598384A (enExample) |
| PL (1) | PL2477987T3 (enExample) |
| PT (1) | PT2477987T (enExample) |
| SI (1) | SI2477987T1 (enExample) |
| WO (1) | WO2011031965A1 (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA026557B1 (ru) | 2008-12-09 | 2017-04-28 | Джилид Сайэнс, Инк. | Промежуточные соединения для получения модуляторов толл-подобных рецепторов |
| EP2992878A1 (en) * | 2010-02-03 | 2016-03-09 | 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 |
| WO2013025733A1 (en) | 2011-08-15 | 2013-02-21 | 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 |
| EA030808B1 (ru) | 2013-04-17 | 2018-09-28 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | ПРИМЕНЕНИЕ 1-ЭТИЛ-7-(2-МЕТИЛ-6-(1Н-1,2,4-ТРИАЗОЛ-3-ИЛ)ПИРИДИН-3-ИЛ)-3,4-ДИГИДРОПИРАЗИНО[2,3-b]ПИРАЗИН-2(1Н)-ОНА В ЛЕЧЕНИИ МУЛЬТИФОРМНОЙ ГЛИОБЛАСТОМЫ |
| WO2014172432A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| HK1221150A1 (zh) | 2013-04-17 | 2017-05-26 | 西格诺药品有限公司 | 用二氢吡嗪并-吡嗪类对癌症的治疗 |
| SG11201508527VA (en) | 2013-04-17 | 2015-11-27 | Signal Pharm Llc | Pharmaceutical formulations, processes, solid forms and methods of use relating to 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 |
| CA2909579A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer |
| MX364101B (es) | 2013-04-17 | 2019-04-12 | Signal Pharm Llc | Terapia de combinación que comprende un compuesto de dihidropirazino-pirazina y un antagonista de receptor de andrógenos para tratar cáncer de próstata. |
| HK1221174A1 (zh) | 2013-04-17 | 2017-05-26 | 西格诺药品有限公司 | 用於治疗癌症的包括tor激酶抑制剂和5-取代喹唑啉酮化合物的组合疗法 |
| CA3143529A1 (en) | 2013-05-29 | 2014-12-04 | Signal Pharmaceuticals, Llc | Pharmaceutical compositions 0f 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 |
| WO2015160880A1 (en) | 2014-04-16 | 2015-10-22 | 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, COMPOSITIONS AND METHODS OF USE THEREOF |
| 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 |
| CN107074860B (zh) * | 2014-09-16 | 2022-07-15 | 吉利德科学公司 | 制备toll样受体调节剂的方法 |
| AU2015318061B2 (en) | 2014-09-16 | 2018-05-17 | Gilead Sciences, Inc. | Solid forms of a toll-like receptor modulator |
| CN118286245A (zh) | 2014-12-26 | 2024-07-05 | 埃莫里大学 | N4-羟基胞苷和衍生物及与其相关的抗病毒用途 |
| US11117898B2 (en) | 2016-11-28 | 2021-09-14 | Jiangsu Hengrui Medicine Co., Ltd. | Pyrazolo-heteroaryl derivative, preparation method and medical use thereof |
| WO2018137614A1 (zh) * | 2017-01-24 | 2018-08-02 | 江苏恒瑞医药股份有限公司 | 杂芳基并噻二嗪-2,2-二氧化物类衍生物、其制备方法及其在医药上的应用 |
| 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 |
| MY198676A (en) | 2017-06-22 | 2023-09-15 | Celgene Corp | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| RS66222B1 (sr) | 2017-12-07 | 2024-12-31 | Univ Emory | N4-hidroksicitidin i derivati i antivirusne upotrebe povezane sa njim |
| SI3752501T1 (sl) | 2018-02-13 | 2023-08-31 | Gilead Sciences, Inc. | Inhibitorji pd-1/pd-l1 |
| CA3093130C (en) | 2018-04-19 | 2023-10-17 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| TWI704916B (zh) | 2018-05-25 | 2020-09-21 | 大陸商江蘇恒瑞醫藥股份有限公司 | 一種吡唑并雜芳基類衍生物鹽酸鹽的晶型及製備方法 |
| US12128047B2 (en) | 2018-05-25 | 2024-10-29 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | TLR7 agonist and pharmaceutical combination thereof for treating lung cancer |
| SI3820572T1 (sl) | 2018-07-13 | 2023-12-29 | Gilead Sciences, Inc. | Inhibitorji pd-1/pd-l1 |
| JP7158577B2 (ja) | 2018-10-24 | 2022-10-21 | ギリアード サイエンシーズ， インコーポレイテッド | Ｐｄ－１／ｐｄ－ｌ１阻害剤 |
| 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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-
2010
- 2010-09-10 CA CA2772253A patent/CA2772253C/en active Active
- 2010-09-10 NO NO10760831A patent/NO2477987T3/no unknown
- 2010-09-10 ES ES10760831.7T patent/ES2661850T3/es active Active
- 2010-09-10 AU AU2010292102A patent/AU2010292102B2/en active Active
- 2010-09-10 US US12/879,697 patent/US8476270B2/en active Active
- 2010-09-10 WO PCT/US2010/048424 patent/WO2011031965A1/en not_active Ceased
- 2010-09-10 PT PT107608317T patent/PT2477987T/pt 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 SI SI201031640T patent/SI2477987T1/en unknown
- 2010-09-10 EP EP10760831.7A patent/EP2477987B1/en active Active
- 2010-09-10 JP JP2012528926A patent/JP5763077B2/ja active Active