JP2020502092A5 - - Google Patents
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- Publication number
- JP2020502092A5 JP2020502092A5 JP2019530500A JP2019530500A JP2020502092A5 JP 2020502092 A5 JP2020502092 A5 JP 2020502092A5 JP 2019530500 A JP2019530500 A JP 2019530500A JP 2019530500 A JP2019530500 A JP 2019530500A JP 2020502092 A5 JP2020502092 A5 JP 2020502092A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- haloalkyl
- cycloalkyl
- heteroaryl
- 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 51
- 150000001875 compounds Chemical class 0.000 claims 34
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 14
- 125000003545 alkoxy group Chemical group 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 14
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 11
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- 208000027104 Chemotherapy-Related Cognitive Impairment Diseases 0.000 claims 8
- 125000004414 alkyl thio group Chemical group 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 125000001475 halogen functional group Chemical group 0.000 claims 7
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 6
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 6
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 5
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 5
- 125000004043 oxo group Chemical group O=* 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- 239000000126 substance Substances 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 3
- 125000004404 heteroalkyl group Chemical group 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 2
- 238000002512 chemotherapy Methods 0.000 claims 2
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000004995 haloalkylthio group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims 2
- 125000004963 sulfonylalkyl group Chemical group 0.000 claims 2
- 230000009529 traumatic brain injury Effects 0.000 claims 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 102000014461 Ataxins Human genes 0.000 claims 1
- 108010078286 Ataxins Proteins 0.000 claims 1
- 206010068597 Bulbospinal muscular atrophy congenital Diseases 0.000 claims 1
- 206010008025 Cerebellar ataxia Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000027747 Kennedy disease Diseases 0.000 claims 1
- 208000009829 Lewy Body Disease Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 1
- -1 R 6 groups Compound Chemical class 0.000 claims 1
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 claims 1
- 208000006269 X-Linked Bulbo-Spinal Atrophy Diseases 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 1
- 201000004562 autosomal dominant cerebellar ataxia Diseases 0.000 claims 1
- 210000003169 central nervous system Anatomy 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
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 125000005322 morpholin-1-yl group Chemical group 0.000 claims 1
- 210000002569 neuron Anatomy 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- GEGDLANPARTRKE-UHFFFAOYSA-N CN1C=COCC1 Chemical compound CN1C=COCC1 GEGDLANPARTRKE-UHFFFAOYSA-N 0.000 description 1
- RXYPXQSKLGGKOL-UHFFFAOYSA-N CN1CCN(C)CC1 Chemical compound CN1CCN(C)CC1 RXYPXQSKLGGKOL-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662431504P | 2016-12-08 | 2016-12-08 | |
| US62/431,504 | 2016-12-08 | ||
| PCT/US2017/065385 WO2018107072A1 (en) | 2016-12-08 | 2017-12-08 | Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (dlk) kinase for the treatment of disease |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020502092A JP2020502092A (ja) | 2020-01-23 |
| JP2020502092A5 true JP2020502092A5 (https=) | 2021-01-21 |
| JP7128816B2 JP7128816B2 (ja) | 2022-08-31 |
Family
ID=62492159
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019530500A Active JP7128816B2 (ja) | 2016-12-08 | 2017-12-08 | 疾患の治療のための二重ロイシンジッパー（ｄｌｋ）キナーゼのビシクロ［１．１．１］ペンタン阻害剤 |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US10093664B2 (https=) |
| EP (1) | EP3551610B1 (https=) |
| JP (1) | JP7128816B2 (https=) |
| KR (1) | KR20190087622A (https=) |
| CN (1) | CN110191878B (https=) |
| AU (1) | AU2017371084B2 (https=) |
| BR (1) | BR112019011801A2 (https=) |
| CA (1) | CA3045947A1 (https=) |
| CL (1) | CL2019001539A1 (https=) |
| CO (1) | CO2019006785A2 (https=) |
| EA (1) | EA201991375A1 (https=) |
| EC (1) | ECSP19048477A (https=) |
| ES (1) | ES2895257T3 (https=) |
| IL (1) | IL267121B (https=) |
| MX (1) | MX386838B (https=) |
| WO (1) | WO2018107072A1 (https=) |
| ZA (1) | ZA201904402B (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190087622A (ko) | 2016-12-08 | 2019-07-24 | 보드 오브 리전츠 더 유니버시티 오브 텍사스 시스템 | 질환 치료를 위한 이중 류신 지퍼 (dlk) 키나아제의 바이시클로[1.1.1]펜탄 억제제 |
| CN118239937A (zh) | 2017-08-09 | 2024-06-25 | 戴纳立制药公司 | 化合物、组合物及方法 |
| DK3676297T3 (da) | 2017-09-01 | 2023-08-14 | Denali Therapeutics Inc | Forbindelser, sammensætninger og fremgangsmåder |
| WO2019241244A1 (en) * | 2018-06-13 | 2019-12-19 | Board Of Regents, The University Of Texas System | Salts of bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (dlk) kinase for the treatment of disease |
| GB201811165D0 (en) * | 2018-07-06 | 2018-08-29 | Metrion Biosciences Ltd | Novel compounds |
| WO2020027723A1 (en) | 2018-08-01 | 2020-02-06 | Agency For Science, Technology And Research | Bicyclic compounds as kinase modulators, methods and uses thereof |
| CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| EP3897670A4 (en) | 2018-12-19 | 2022-09-07 | Disarm Therapeutics, Inc. | MRSA1 INHIBITORS IN COMBINATION WITH NEUROPROTECTIVE AGENTS |
| US12091392B2 (en) | 2019-02-13 | 2024-09-17 | Denali Therapeutics Inc. | Compounds, compositions and methods |
| MA54953A (fr) | 2019-02-13 | 2021-12-22 | Denali Therapeutics Inc | Composés, compositions et procédés |
| IL291665B2 (en) * | 2019-09-27 | 2025-07-01 | Univ Texas | Inhibitors of receptor interacting protein kinase i for the treatment of disease |
| US11560366B2 (en) | 2019-10-21 | 2023-01-24 | Board Of Regents, The University Of Texas System | Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease |
| CA3193736A1 (en) | 2020-09-02 | 2022-03-10 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Lzk-targeting degraders and methods of use |
| KR20240055041A (ko) | 2021-09-01 | 2024-04-26 | 더 유나이티드 스테이츠 오브 아메리카, 애즈 레프리젠티드 바이 더 세크러테리, 디파트먼트 오브 헬스 앤드 휴먼 서비시즈 | 혼합 계통 키나제 억제제 및 억제제의 사용 방법 |
| CN115974795A (zh) * | 2022-12-26 | 2023-04-18 | 杭州师范大学 | 一种含全氟烷基和n杂环二取代双环[1.1.1]戊烷及其合成方法 |
| WO2025021997A1 (en) | 2023-07-27 | 2025-01-30 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | New map4k1 inhibitors |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2523134A1 (en) | 2003-04-25 | 2004-11-11 | Chiron Corporation | Pyridyl substituted ketolide antibiotics |
| TW200944520A (en) | 2008-01-29 | 2009-11-01 | Glaxo Group Ltd | Spiro compounds as NPY Y5 receptor antagonists |
| JP6097998B2 (ja) | 2010-12-16 | 2017-03-22 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ロイコトリエン生成のビアリールアミドインヒビター |
| CN104271566B (zh) | 2012-05-22 | 2017-05-31 | 霍夫曼-拉罗奇有限公司 | 取代的联吡啶胺及其用途 |
| JP6199991B2 (ja) | 2013-01-18 | 2017-09-20 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ３置換ピラゾール及びｄｌｋ阻害剤としての使用 |
| CN104119340A (zh) | 2013-01-22 | 2014-10-29 | 韩冰 | 一类蛋白酶抑制剂及其制备方法和用途 |
| AR096151A1 (es) | 2013-05-01 | 2015-12-09 | Hoffmann La Roche | Compuestos de biheteroarilo y usos de los mismos |
| JP6523251B2 (ja) | 2013-05-01 | 2019-05-29 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｃ−結合ヘテロシクロアルキル置換ピリミジン類及びそれらの用途 |
| MX2016008110A (es) | 2013-12-20 | 2016-08-19 | Hoffmann La Roche | Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos. |
| CN113336653A (zh) * | 2014-03-07 | 2021-09-03 | 里科瑞尔姆Ip控股有限责任公司 | 螺桨烷衍生物及合成 |
| US9307840B2 (en) | 2014-07-01 | 2016-04-12 | Carlos Arturo Restrepo | Foldable and portable lounge chair having an integrated lockable storage compartment |
| EA037112B1 (ru) * | 2015-03-02 | 2021-02-08 | Ригель Фармасьютикалс, Инк. | Ингибиторы tgf- |
| MX379622B (es) * | 2015-04-03 | 2025-03-11 | Recurium Ip Holdings Llc | Compuestos espirociclicos |
| WO2018044808A1 (en) | 2016-08-29 | 2018-03-08 | Board Of Regents, University Of Texas System | Inhibitors of dual leucine ziper (dlk) kinase for the treatment of disease |
| KR20190087622A (ko) | 2016-12-08 | 2019-07-24 | 보드 오브 리전츠 더 유니버시티 오브 텍사스 시스템 | 질환 치료를 위한 이중 류신 지퍼 (dlk) 키나아제의 바이시클로[1.1.1]펜탄 억제제 |
| US11560366B2 (en) * | 2019-10-21 | 2023-01-24 | Board Of Regents, The University Of Texas System | Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease |
-
2017
- 2017-12-08 KR KR1020197019246A patent/KR20190087622A/ko not_active Abandoned
- 2017-12-08 EP EP17879488.9A patent/EP3551610B1/en active Active
- 2017-12-08 CA CA3045947A patent/CA3045947A1/en active Pending
- 2017-12-08 WO PCT/US2017/065385 patent/WO2018107072A1/en not_active Ceased
- 2017-12-08 AU AU2017371084A patent/AU2017371084B2/en not_active Ceased
- 2017-12-08 CN CN201780082917.2A patent/CN110191878B/zh not_active Expired - Fee Related
- 2017-12-08 EA EA201991375A patent/EA201991375A1/ru unknown
- 2017-12-08 ES ES17879488T patent/ES2895257T3/es active Active
- 2017-12-08 US US15/836,442 patent/US10093664B2/en active Active
- 2017-12-08 BR BR112019011801-2A patent/BR112019011801A2/pt not_active IP Right Cessation
- 2017-12-08 JP JP2019530500A patent/JP7128816B2/ja active Active
- 2017-12-08 MX MX2019006645A patent/MX386838B/es unknown
-
2018
- 2018-09-04 US US16/121,198 patent/US10428057B2/en active Active
-
2019
- 2019-06-05 CL CL2019001539A patent/CL2019001539A1/es unknown
- 2019-06-05 IL IL267121A patent/IL267121B/en unknown
- 2019-06-26 CO CONC2019/0006785A patent/CO2019006785A2/es unknown
- 2019-07-04 ZA ZA2019/04402A patent/ZA201904402B/en unknown
- 2019-07-08 EC ECSENADI201948477A patent/ECSP19048477A/es unknown
-
2022
- 2022-03-10 US US17/654,301 patent/US20220267311A1/en not_active Abandoned