JP2016537366A5 - - Google Patents
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- Publication number
- JP2016537366A5 JP2016537366A5 JP2016531020A JP2016531020A JP2016537366A5 JP 2016537366 A5 JP2016537366 A5 JP 2016537366A5 JP 2016531020 A JP2016531020 A JP 2016531020A JP 2016531020 A JP2016531020 A JP 2016531020A JP 2016537366 A5 JP2016537366 A5 JP 2016537366A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- independently selected
- heterocyclyl
- alkynyl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 91
- 125000000623 heterocyclic group Chemical group 0.000 claims 58
- 229910052739 hydrogen Inorganic materials 0.000 claims 50
- 229910052799 carbon Inorganic materials 0.000 claims 46
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 38
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 32
- 229910052760 oxygen Inorganic materials 0.000 claims 31
- 125000003118 aryl group Chemical group 0.000 claims 16
- 125000005842 heteroatom Chemical group 0.000 claims 16
- 229910052757 nitrogen Inorganic materials 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 16
- 229910052717 sulfur Inorganic materials 0.000 claims 15
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 14
- 150000001721 carbon Chemical group 0.000 claims 10
- 125000004432 carbon atom Chemical group C* 0.000 claims 9
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- -1 substituted Chemical class 0.000 claims 3
- 108010047048 Casein Kinase Idelta Proteins 0.000 claims 2
- 241000239366 Euphausiacea Species 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000004514 1,2,4-thiadiazolyl group Chemical group 0.000 claims 1
- 208000017164 Chronobiology disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 0 CC1(C)C2=C(C(N)=O)C(*)=**2C(*)(*)C(*)(*)*1C(**)=O Chemical compound CC1(C)C2=C(C(N)=O)C(*)=**2C(*)(*)C(*)(*)*1C(**)=O 0.000 description 21
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361904116P | 2013-11-14 | 2013-11-14 | |
| US61/904,116 | 2013-11-14 | ||
| PCT/US2014/065599 WO2015073767A1 (en) | 2013-11-14 | 2014-11-14 | Substituted 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine derivatives as casein kinase 1 d/e inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016537366A JP2016537366A (ja) | 2016-12-01 |
| JP2016537366A5 true JP2016537366A5 (enExample) | 2017-12-21 |
| JP6494622B2 JP6494622B2 (ja) | 2019-04-03 |
Family
ID=51952052
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016531020A Active JP6494622B2 (ja) | 2013-11-14 | 2014-11-14 | カゼインキナーゼ１ｄ／ｅ阻害剤としての置換された４，５，６，７−テトラヒドロピラゾロ［１，５−ａ］ピラジン誘導体 |
| JP2016531646A Active JP6494624B2 (ja) | 2013-11-14 | 2014-11-14 | カゼインキナーゼ１ｄ／ｅ阻害剤としての置換された４，５，６，７−テトラヒドロピラゾロ［１，５−ａ］ピラジン誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016531646A Active JP6494624B2 (ja) | 2013-11-14 | 2014-11-14 | カゼインキナーゼ１ｄ／ｅ阻害剤としての置換された４，５，６，７−テトラヒドロピラゾロ［１，５−ａ］ピラジン誘導体 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US9598423B2 (enExample) |
| EP (2) | EP3068784B1 (enExample) |
| JP (2) | JP6494622B2 (enExample) |
| CN (2) | CN105916855B (enExample) |
| AR (1) | AR098414A1 (enExample) |
| ES (2) | ES2744636T3 (enExample) |
| TW (1) | TW201605859A (enExample) |
| UY (1) | UY35834A (enExample) |
| WO (2) | WO2015073767A1 (enExample) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY35834A (es) | 2013-11-14 | 2015-05-29 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Piperazinas de pirazolo sustituido como inhibidores de caseína quinasa 1 delta y epsilon |
| JP6513075B2 (ja) * | 2014-02-27 | 2019-05-15 | 国立大学法人 東京大学 | オートタキシン阻害活性を有する縮合ピラゾール誘導体 |
| MA41338B1 (fr) * | 2015-01-16 | 2019-07-31 | Hoffmann La Roche | Composés de pyrazine pour le traitement de maladies infectieuses |
| CN109069488B (zh) | 2016-03-07 | 2021-09-07 | 英安塔制药有限公司 | 乙型肝炎抗病毒剂 |
| EP3426674A4 (en) | 2016-03-09 | 2019-08-14 | Blade Therapeutics, Inc. | CYCLIC KETO AMID COMPOUNDS AS CALPAIN MODULATORS AND METHOD FOR THE PRODUCTION AND USE THEREOF |
| CN109153682B (zh) * | 2016-05-20 | 2021-05-25 | 豪夫迈·罗氏有限公司 | 用于治疗感染性疾病的具有氧、硫和氮连接基的新的吡嗪化合物 |
| AU2017292646A1 (en) | 2016-07-05 | 2019-02-07 | Blade Therapeutics, Inc. | Calpain modulators and therapeutic uses thereof |
| EP3484886B1 (en) * | 2016-07-14 | 2020-03-04 | Hoffmann-La Roche AG | 6,7-dihydro-4h-pyrazolo[1,5-a]pyrazine and 6,7-dihydro-4h-triazolo[1,5-a]pyrazine compounds for the treatment of infectious diseases |
| KR20190063473A (ko) | 2016-09-28 | 2019-06-07 | 블레이드 테라퓨틱스, 인크. | 칼페인 조정자 및 그 치료학적 용도 |
| TWI782056B (zh) * | 2017-07-14 | 2022-11-01 | 日商鹽野義製藥股份有限公司 | 具有ｍｇａｔ２抑制活性的縮合環衍生物 |
| CA3070004A1 (en) * | 2017-07-27 | 2019-01-31 | Jiangsu Hengrui Medicine Co., Ltd. | Piperazine heteroaryl derivative, preparation method therefor and use of same in medicine |
| TWI811236B (zh) | 2017-08-28 | 2023-08-11 | 美商因那塔製藥公司 | B型肝炎抗病毒試劑 |
| TWI846350B (zh) | 2017-09-15 | 2024-06-21 | 美商佛瑪治療公司 | 作為ＣＢＰ／ｐ３００抑制劑之四氫－咪唑並喹啉化合物 |
| SG11202003827YA (en) | 2017-11-01 | 2020-05-28 | Bristol Myers Squibb Co | Bridged bicyclic compounds as farnesoid x receptor modulators |
| WO2019143902A2 (en) | 2018-01-22 | 2019-07-25 | Enanta Pharmaceuticals, Inc. | Substituted heterocycles as antiviral agents |
| WO2019191166A1 (en) * | 2018-03-29 | 2019-10-03 | Enanta Pharmaceuticals, Inc. | Hepatitis b antiviral agents |
| JP7090958B2 (ja) * | 2018-06-01 | 2022-06-27 | アドレイ・ノーティ・バイオファーマ・カンパニー・リミテッド | 高活性ｃｓｆ１ｒ阻害薬化合物 |
| MX2023013508A (es) | 2018-06-29 | 2023-12-13 | Forma Therapeutics Inc | Inhibicion de la proteina de union a creb (cbp). |
| US10865211B2 (en) | 2018-09-21 | 2020-12-15 | Enanta Pharmaceuticals, Inc. | Functionalized heterocycles as antiviral agents |
| US11198693B2 (en) | 2018-11-21 | 2021-12-14 | Enanta Pharmaceuticals, Inc. | Functionalized heterocycles as antiviral agents |
| JP7608166B2 (ja) | 2019-01-11 | 2025-01-06 | 塩野義製薬株式会社 | Ｍｇａｔ２阻害活性を有するジヒドロピラゾロピラジノン誘導体 |
| CN111484497B (zh) * | 2019-01-25 | 2021-07-02 | 江苏恒瑞医药股份有限公司 | 咪唑并[1,5-a]吡嗪类衍生物的可药用盐、晶型及其制备方法 |
| BR112021014327A2 (pt) * | 2019-01-25 | 2021-09-28 | Jiangsu Hengrui Medicine Co., Ltd. | Forma cristalina de derivado de 1,2,3-triazolo[1,5-a]pirazinas, método de preparação da referida forma cristalina, composições farmacêuticas compreendendo a mesma e seu uso |
| CN111484498B (zh) * | 2019-01-25 | 2021-05-14 | 江苏恒瑞医药股份有限公司 | 咪唑并[1,5-a]吡嗪类化合物的晶型及其制备方法 |
| CA3128946A1 (en) | 2019-02-07 | 2020-08-13 | Bayer Aktiengesellschaft | 3-amino-2-[2-(acylamino)pyridin-4-yl]-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one as csnk1 inhibitors |
| TW202102494A (zh) | 2019-03-15 | 2021-01-16 | 美商弗瑪治療公司 | 抑制環amp-反應元件-結合蛋白(creb) |
| US11236111B2 (en) | 2019-06-03 | 2022-02-01 | Enanta Pharmaceuticals, Inc. | Hepatitis B antiviral agents |
| WO2020247561A1 (en) | 2019-06-04 | 2020-12-10 | Enanta Pharmaceuticals, Inc, | Hepatitis b antiviral agents |
| US11472808B2 (en) | 2019-06-04 | 2022-10-18 | Enanta Pharmaceuticals, Inc. | Substituted pyrrolo[1,2-c]pyrimidines as hepatitis B antiviral agents |
| US11738019B2 (en) | 2019-07-11 | 2023-08-29 | Enanta Pharmaceuticals, Inc. | Substituted heterocycles as antiviral agents |
| US11236108B2 (en) | 2019-09-17 | 2022-02-01 | Enanta Pharmaceuticals, Inc. | Functionalized heterocycles as antiviral agents |
| US11802125B2 (en) | 2020-03-16 | 2023-10-31 | Enanta Pharmaceuticals, Inc. | Functionalized heterocyclic compounds as antiviral agents |
| CN114057745A (zh) * | 2020-07-29 | 2022-02-18 | 江苏恒瑞医药股份有限公司 | 一种三氮唑并[1,5-a]吡嗪制备方法及其应用 |
| WO2022058920A1 (en) * | 2020-09-17 | 2022-03-24 | Janssen Pharmaceutica Nv | Casein kinase 1 delta modulators |
| US11795168B2 (en) | 2020-09-23 | 2023-10-24 | Forma Therapeutics, Inc. | Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP) |
| US11801243B2 (en) | 2020-09-23 | 2023-10-31 | Forma Therapeutics, Inc. | Bromodomain inhibitors for androgen receptor-driven cancers |
| TW202245772A (zh) * | 2021-02-04 | 2022-12-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種衣殼蛋白抑制劑的醫藥組成物及其製備方法 |
| EP4469457A1 (en) * | 2022-01-27 | 2024-12-04 | The Broad Institute Inc. | Substituted heterocyclic csnk1 inhibitors |
| CA3257905A1 (en) * | 2022-06-13 | 2025-04-24 | Shionogi & Co | CRYSTAL OF A DIHYDROPYRIDINONE DERIVATIVE OR A SOLVATE THEREOF |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2002337142B2 (en) * | 2001-09-19 | 2007-10-11 | Aventis Pharma S.A. | Indolizines as kinase protein inhibitors |
| JP4691506B2 (ja) * | 2003-12-11 | 2011-06-01 | アベンティス・ファーマスーティカルズ・インコーポレイテツド | カゼインキナーゼＩεの阻害剤としての置換１Ｈ−ピロロ［３，２−ｂ，３，２−ｃ，及び２，３−ｃ］ピリジン−２−カルボキシアミド及び関連類似物 |
| US20050222171A1 (en) * | 2004-01-22 | 2005-10-06 | Guido Bold | Organic compounds |
| US20070155738A1 (en) | 2005-05-20 | 2007-07-05 | Alantos Pharmaceuticals, Inc. | Heterobicyclic metalloprotease inhibitors |
| CN101417999A (zh) | 2007-10-25 | 2009-04-29 | 上海恒瑞医药有限公司 | 哌嗪类衍生物,其制备方法及其在医药上的应用 |
| EP2085398A1 (en) | 2008-02-01 | 2009-08-05 | Merz Pharma GmbH & Co. KGaA | Pyrazolopyrimidines, a process for their preparation and their use as medicine |
| ES2710701T3 (es) | 2008-09-24 | 2019-04-26 | Basf Se | Compuestos de pirazol para el control de plagas de invertebrados |
| CA2738429C (en) | 2008-09-26 | 2016-10-25 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
| WO2010059836A1 (en) | 2008-11-20 | 2010-05-27 | Decode Genetics Ehf | Substituted aza-bridged bicyclics for cardiovascular and cns disease |
| TW201035102A (en) | 2009-03-04 | 2010-10-01 | Gruenethal Gmbh | Sulfonylated tetrahydroazolopyrazines and their use as medicinal products |
| FR2960876B1 (fr) * | 2010-06-03 | 2012-07-27 | Sanofi Aventis | Derives de 3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1h)-dicarboxamide leur preparation et leur application en therapeutique. |
| CN102372716A (zh) | 2010-08-09 | 2012-03-14 | 江苏恒瑞医药股份有限公司 | 酞嗪酮类衍生物、其制备方法及其在医药上的应用 |
| CA2826464C (en) | 2011-03-02 | 2020-07-28 | Lead Discovery Center Gmbh | Pharmaceutically active disubstituted triazine derivatives |
| UY35834A (es) | 2013-11-14 | 2015-05-29 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Piperazinas de pirazolo sustituido como inhibidores de caseína quinasa 1 delta y epsilon |
-
2014
- 2014-11-13 UY UY0001035834A patent/UY35834A/es unknown
- 2014-11-13 AR ARP140104277A patent/AR098414A1/es unknown
- 2014-11-13 TW TW103139448A patent/TW201605859A/zh unknown
- 2014-11-14 CN CN201480073088.8A patent/CN105916855B/zh not_active Expired - Fee Related
- 2014-11-14 ES ES14806145T patent/ES2744636T3/es active Active
- 2014-11-14 CN CN201480073199.9A patent/CN105916856B/zh not_active Expired - Fee Related
- 2014-11-14 ES ES14802796T patent/ES2718218T3/es active Active
- 2014-11-14 US US15/034,217 patent/US9598423B2/en active Active
- 2014-11-14 WO PCT/US2014/065599 patent/WO2015073767A1/en not_active Ceased
- 2014-11-14 EP EP14802796.4A patent/EP3068784B1/en active Active
- 2014-11-14 US US14/541,343 patent/US9273058B2/en active Active
- 2014-11-14 EP EP14806145.0A patent/EP3068785B1/en not_active Not-in-force
- 2014-11-14 JP JP2016531020A patent/JP6494622B2/ja active Active
- 2014-11-14 JP JP2016531646A patent/JP6494624B2/ja active Active
- 2014-11-14 WO PCT/US2014/065594 patent/WO2015073763A1/en not_active Ceased
-
2016
- 2016-01-13 US US14/994,346 patent/US20160122358A1/en not_active Abandoned