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 |
|---|---|---|---|---|
| WO2010077613A1 (en) | 2008-12-09 | 2010-07-08 | Gilead Sciences, Inc. | Modulators of toll-like receptors |
| PH12012501581A1 (en) * | 2010-02-03 | 2012-10-22 | Signal Pharm 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 |
| AU2012296662A1 (en) | 2011-08-15 | 2014-03-27 | 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 |
| CN105339008A (zh) | 2013-04-17 | 2016-02-17 | 西格诺药品有限公司 | 用于治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯酰胺的组合疗法 |
| EP2986321A1 (en) | 2013-04-17 | 2016-02-24 | 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 |
| MX393164B (es) | 2013-04-17 | 2025-03-21 | Signal Pharm Llc | Formulaciones farmacéuticas, proceso, formas sólidas y métodos de uso relacionados con 1-etil-7-(2-metil-6-(1h-1,2,4-triazol-3-ii)piridin-3-ii)-3,4-dihidropirazino[2,3-b]pirazin-2(1h)-ona. |
| MX368286B (es) | 2013-04-17 | 2019-09-27 | Signal Pharm Llc | Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer. |
| BR112015026257B1 (pt) | 2013-04-17 | 2022-12-20 | Signal Pharmaceuticals, Llc | Uso de um composto dihidropirazino-pirazina e enzalutamida, composição farmacêutica que os compreende, e kit |
| JP6382945B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ，エルエルシー | ジヒドロピラジノ−ピラジンによる癌治療 |
| NZ629486A (en) | 2013-05-29 | 2017-11-24 | Signal Pharm 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 |
| EP3131551A4 (en) | 2014-04-16 | 2017-09-20 | 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 |
| EP4140485A1 (en) | 2014-07-11 | 2023-03-01 | Gilead Sciences, Inc. | Modulators of toll-like receptors for the treatment of hiv |
| JP6373490B2 (ja) * | 2014-09-16 | 2018-08-15 | ギリアード サイエンシーズ， インコーポレイテッド | Ｔｏｌｌ様受容体モジュレーターを調製する方法 |
| EA201790369A1 (ru) | 2014-09-16 | 2017-10-31 | Джилид Сайэнс, Инк. | Твердые формы модулятора толл-подобного рецептора |
| SG10202105371YA (en) | 2014-12-26 | 2021-07-29 | Univ Emory | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| ES2886973T3 (es) | 2016-11-28 | 2021-12-21 | Jiangsu Hengrui Medicine Co | Derivado pirazolo-heteroarilo, método de preparación y uso médico del mismo |
| 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 |
| TW201900647A (zh) | 2017-05-18 | 2019-01-01 | 大陸商江蘇恒瑞醫藥股份有限公司 | 雜芳基并吡唑類衍生物、其製備方法及其在醫藥上的應用 |
| IL271491B2 (en) | 2017-06-22 | 2023-09-01 | Celgene Corp | Treatment of carcinoma of the liver characterized by hepatitis b virus infection |
| FI3706762T3 (fi) | 2017-12-07 | 2024-12-13 | Univ Emory | N4-hydroksisytidiini ja johdannaisia sekä niihin liittyviä virusten vastaisia käyttötapoja |
| WO2019160882A1 (en) | 2018-02-13 | 2019-08-22 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| WO2019204609A1 (en) | 2018-04-19 | 2019-10-24 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| JP2021526520A (ja) | 2018-05-25 | 2021-10-07 | 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司Ｊｉａｎｇｓｕ Ｈｅｎｇｒｕｉ Ｍｅｄｉｃｉｎｅ Ｃｏ．， Ｌｔｄ． | ピラゾロヘテロアリール誘導体の塩酸塩の結晶形および調製方法 |
| WO2019223788A1 (zh) * | 2018-05-25 | 2019-11-28 | 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 |
| BR112020026746A2 (pt) | 2018-07-13 | 2021-03-30 | Gilead Sciences, Inc. | Composto, composição farmacêutica, métodos para inibir pd-1, pd-l1 e/ou a interação de pd-1/pd-l1 e para tratar câncer, e, kit para tratar ou prevenir câncer ou uma doença ou condição. |
| CN112955435B (zh) | 2018-10-24 | 2024-09-06 | 吉利德科学公司 | Pd-1/pd-l1抑制剂 |
| 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 EP EP10760831.7A patent/EP2477987B1/en active Active
- 2010-09-10 NO NO10760831A patent/NO2477987T3/no unknown
- 2010-09-10 SI SI201031640T patent/SI2477987T1/en unknown
- 2010-09-10 US US12/879,697 patent/US8476270B2/en active Active
- 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 ES ES10760831.7T patent/ES2661850T3/es active Active
- 2010-09-10 WO PCT/US2010/048424 patent/WO2011031965A1/en not_active Ceased
- 2010-09-10 CA CA2772253A patent/CA2772253C/en active Active
- 2010-09-10 JP JP2012528926A patent/JP5763077B2/ja active Active
- 2010-09-10 AU AU2010292102A patent/AU2010292102B2/en active Active
- 2010-09-10 PT PT107608317T patent/PT2477987T/pt unknown