KR20170090476A - 야누스 키나제 저해제로서의 4,6-치환된-피라졸로[1,5-a]피라진 - Google Patents
야누스 키나제 저해제로서의 4,6-치환된-피라졸로[1,5-a]피라진 Download PDFInfo
- Publication number
- KR20170090476A KR20170090476A KR1020177018122A KR20177018122A KR20170090476A KR 20170090476 A KR20170090476 A KR 20170090476A KR 1020177018122 A KR1020177018122 A KR 1020177018122A KR 20177018122 A KR20177018122 A KR 20177018122A KR 20170090476 A KR20170090476 A KR 20170090476A
- Authority
- KR
- South Korea
- Prior art keywords
- alkyl
- formula
- hetcyc
- mmol
- pyrazol
- 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.)
- Withdrawn
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- 0 *C(*)(*)[n]1ncc(-c2nc(-c3c[n]nc3)c[n]3nccc23)c1 Chemical compound *C(*)(*)[n]1ncc(-c2nc(-c3c[n]nc3)c[n]3nccc23)c1 0.000 description 5
- MOTGHCGCHYLZMI-LBPRGKRZSA-N CC(C)C[C@H](C)[n]1ncc(B2OC(C)(C)C(C)(C)O2)c1 Chemical compound CC(C)C[C@H](C)[n]1ncc(B2OC(C)(C)C(C)(C)O2)c1 MOTGHCGCHYLZMI-LBPRGKRZSA-N 0.000 description 1
- IHZCYGIKKXIIOQ-NNJIEVJOSA-N CCC(C(C)(F)F)[n]1ncc(-c2nc(-c3c[n](C[C@H](CO)O)nc3)c[n]3nccc23)c1 Chemical compound CCC(C(C)(F)F)[n]1ncc(-c2nc(-c3c[n](C[C@H](CO)O)nc3)c[n]3nccc23)c1 IHZCYGIKKXIIOQ-NNJIEVJOSA-N 0.000 description 1
- RRUMNCYHIPZCJS-UHFFFAOYSA-N CCC(CC)[n]1ncc(-c2nc(-c3c[n](C(C)CO)nc3)c[n]3nccc23)c1 Chemical compound CCC(CC)[n]1ncc(-c2nc(-c3c[n](C(C)CO)nc3)c[n]3nccc23)c1 RRUMNCYHIPZCJS-UHFFFAOYSA-N 0.000 description 1
- GQMPILIYOVYDCB-UHFFFAOYSA-N CCC(CC)[n]1ncc(-c2nc(-c3c[n](C(C4)CC4(C)O)nc3)c[n]3nccc23)c1 Chemical compound CCC(CC)[n]1ncc(-c2nc(-c3c[n](C(C4)CC4(C)O)nc3)c[n]3nccc23)c1 GQMPILIYOVYDCB-UHFFFAOYSA-N 0.000 description 1
- NZWKRMFCKXOQMF-UHFFFAOYSA-N CCC(CC)[n]1ncc(-c2nc(-c3c[n](C(C4)CC4C(NCCO)=O)nc3)c[n]3nccc23)c1 Chemical compound CCC(CC)[n]1ncc(-c2nc(-c3c[n](C(C4)CC4C(NCCO)=O)nc3)c[n]3nccc23)c1 NZWKRMFCKXOQMF-UHFFFAOYSA-N 0.000 description 1
- HJUVFZGONSIZFY-UHFFFAOYSA-N CCC(CC)[n]1ncc(-c2nc(-c3c[n](C(C4)CC4O)nc3)c[n]3nccc23)c1 Chemical compound CCC(CC)[n]1ncc(-c2nc(-c3c[n](C(C4)CC4O)nc3)c[n]3nccc23)c1 HJUVFZGONSIZFY-UHFFFAOYSA-N 0.000 description 1
- VYIVPIOHJVLMDT-HNNXBMFYSA-N CCC(CC)[n]1ncc(-c2nc(-c3c[n](C(C4)CN4C([C@H](C)O)=O)nc3)c[n]3nccc23)c1 Chemical compound CCC(CC)[n]1ncc(-c2nc(-c3c[n](C(C4)CN4C([C@H](C)O)=O)nc3)c[n]3nccc23)c1 VYIVPIOHJVLMDT-HNNXBMFYSA-N 0.000 description 1
- MXGPPMXKCJUMCI-UHFFFAOYSA-N CCC(CC)[n]1ncc(-c2nc(-c3c[n](CC(NC(C)C)=O)nc3)c[n]3nccc23)c1 Chemical compound CCC(CC)[n]1ncc(-c2nc(-c3c[n](CC(NC(C)C)=O)nc3)c[n]3nccc23)c1 MXGPPMXKCJUMCI-UHFFFAOYSA-N 0.000 description 1
- QMHIQYFDHQKWPO-LJQANCHMSA-N CCC(CC)[n]1ncc(-c2nc(-c3c[n](C[C@@H](CN(C)C)O)nc3)c[n]3nccc23)c1 Chemical compound CCC(CC)[n]1ncc(-c2nc(-c3c[n](C[C@@H](CN(C)C)O)nc3)c[n]3nccc23)c1 QMHIQYFDHQKWPO-LJQANCHMSA-N 0.000 description 1
- HQYCIYSQINFXHM-LNKXUWQBSA-N CCC([C@H](C1)C1(F)F)[n]1ncc(-c2nc(-c3c[n](C[C@H](CO)O)nc3)c[n]3nccc23)c1 Chemical compound CCC([C@H](C1)C1(F)F)[n]1ncc(-c2nc(-c3c[n](C[C@H](CO)O)nc3)c[n]3nccc23)c1 HQYCIYSQINFXHM-LNKXUWQBSA-N 0.000 description 1
- IHZCYGIKKXIIOQ-QAPCUYQASA-N CC[C@@H](C(C)(F)F)[n]1ncc(-c2nc(-c3c[n](C[C@H](CO)O)nc3)c[n]3nccc23)c1 Chemical compound CC[C@@H](C(C)(F)F)[n]1ncc(-c2nc(-c3c[n](C[C@H](CO)O)nc3)c[n]3nccc23)c1 IHZCYGIKKXIIOQ-QAPCUYQASA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
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- Obesity (AREA)
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- Oncology (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Transplantation (AREA)
- Biochemistry (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462088068P | 2014-12-05 | 2014-12-05 | |
| US62/088,068 | 2014-12-05 | ||
| PCT/US2015/064062 WO2016090285A1 (en) | 2014-12-05 | 2015-12-04 | 4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20170090476A true KR20170090476A (ko) | 2017-08-07 |
Family
ID=55069089
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020177018122A Withdrawn KR20170090476A (ko) | 2014-12-05 | 2015-12-04 | 야누스 키나제 저해제로서의 4,6-치환된-피라졸로[1,5-a]피라진 |
Country Status (29)
| Country | Link |
|---|---|
| US (3) | US10189845B2 (enExample) |
| EP (2) | EP3878451A1 (enExample) |
| JP (2) | JP6641373B2 (enExample) |
| KR (1) | KR20170090476A (enExample) |
| CN (1) | CN107278203B (enExample) |
| AU (1) | AU2015357585B2 (enExample) |
| BR (1) | BR112017011798A2 (enExample) |
| CA (1) | CA2969709A1 (enExample) |
| CL (1) | CL2017001422A1 (enExample) |
| CO (1) | CO2017006674A2 (enExample) |
| CR (1) | CR20170309A (enExample) |
| DK (1) | DK3227297T3 (enExample) |
| ES (1) | ES2865483T3 (enExample) |
| HR (1) | HRP20210501T1 (enExample) |
| HU (1) | HUE054371T2 (enExample) |
| IL (1) | IL252656A0 (enExample) |
| MX (1) | MX386316B (enExample) |
| MY (1) | MY191016A (enExample) |
| PH (1) | PH12017501032A1 (enExample) |
| PL (1) | PL3227297T3 (enExample) |
| PT (1) | PT3227297T (enExample) |
| RS (1) | RS61693B1 (enExample) |
| RU (2) | RU2742938C2 (enExample) |
| SG (1) | SG11201704542SA (enExample) |
| SI (1) | SI3227297T1 (enExample) |
| TW (1) | TWI725004B (enExample) |
| UA (1) | UA120065C2 (enExample) |
| WO (1) | WO2016090285A1 (enExample) |
| ZA (1) | ZA201704494B (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20170090476A (ko) | 2014-12-05 | 2017-08-07 | 어레이 바이오파마 인크. | 야누스 키나제 저해제로서의 4,6-치환된-피라졸로[1,5-a]피라진 |
| MX383747B (es) | 2016-02-24 | 2025-03-14 | Pfizer | Derivados de pirazolo[1,5-a]pirazin-4-ilo como inhibidores de quinasas janus (jak) |
| US11028080B2 (en) | 2016-03-11 | 2021-06-08 | Denali Therapeutics Inc. | Substituted pyrimidines as LRKK2 inhibitors |
| PT3472153T (pt) | 2016-06-16 | 2021-12-31 | Denali Therapeutics Inc | Pirimidin-2-ilamino-1h-pirazóis como inibidores de lrrk2 para uso no tratamento de distúrbios neurodegenerativos |
| GB201617758D0 (en) * | 2016-10-20 | 2016-12-07 | Almac Discovery Limited | Pharmaceutical compounds |
| JP6888101B2 (ja) * | 2017-01-18 | 2021-06-16 | アレイ バイオファーマ インコーポレイテッド | ＲＥＴキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピラジン化合物 |
| WO2018217946A1 (en) * | 2017-05-24 | 2018-11-29 | Denali Therapeutics Inc. | Compounds, compositions and methods |
| WO2019034973A1 (en) | 2017-08-14 | 2019-02-21 | Pfizer Inc. | PYRAZOLO [1,5-A] PYRAZIN-4-YL AND RELATED DERIVATIVES |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| EP3740486A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CN111630054B (zh) | 2018-01-18 | 2023-05-09 | 奥瑞生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物 |
| ES2922314T3 (es) | 2018-09-10 | 2022-09-13 | Array Biopharma Inc | Compuestos heterocíclicos condensados como inhibidores de cinasa RET |
| PL3954689T3 (pl) * | 2019-04-12 | 2024-08-05 | Primegene (Beijing) Co., Ltd. | Związki pochodne pirazolopirazyny, kompozycja farmaceutyczna i ich zastosowanie |
| JP7137696B2 (ja) | 2019-05-14 | 2022-09-14 | プロヴェンション・バイオ・インコーポレイテッド | １型糖尿病を予防するための方法および組成物 |
| CN113150012B (zh) * | 2020-01-22 | 2023-03-24 | 浙江海正药业股份有限公司 | 吡唑并[1,5-a]吡嗪类衍生物及其制备方法和用途 |
| BR112022020020A2 (pt) | 2020-04-04 | 2022-11-22 | Pfizer | Métodos de tratamento da doença do coronavírus 2019 |
| KR20230092863A (ko) | 2020-06-11 | 2023-06-26 | 프로벤션 바이오, 인코포레이티드 | 제1형 당뇨병을 예방하기 위한 방법 및 조성물 |
| MX2023013851A (es) | 2021-05-24 | 2023-12-08 | Provention Bio Inc | Metodos para el tratamiento de diabetes tipo 1. |
| AU2022387652B2 (en) * | 2021-11-12 | 2025-10-16 | Cms Research & Development Pte. Ltd. | Pyrazolo fused ring compound and use thereof |
| EP4711367A1 (en) * | 2023-05-12 | 2026-03-18 | CMS Research & Development Pte. Ltd. | Pyrazolopyrazine compound and method for preparing crystal form thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU5682799A (en) | 1998-08-21 | 2000-03-14 | Parker Hughes Institute | Quinazoline derivatives |
| DE102007032349A1 (de) | 2007-07-11 | 2009-01-15 | Bayer Healthcare Ag | Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung |
| EP2516434B1 (en) | 2009-12-23 | 2015-05-27 | Takeda Pharmaceutical Company Limited | Fused heteroaromatic pyrrolidinones as syk inhibitors |
| CA2787714C (en) * | 2010-01-22 | 2019-04-09 | Joaquin Pastor Fernandez | Inhibitors of pi3 kinase |
| UY33213A (es) * | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| US20110241987A1 (en) * | 2010-04-01 | 2011-10-06 | Smart Technologies Ulc | Interactive input system and information input method therefor |
| KR20130094710A (ko) * | 2010-04-14 | 2013-08-26 | 어레이 바이오파마 인크. | Ｊａｋ 키나아제의 억제제로서 5,7-치환된-이미다조［1,2-ｃ］피리미딘 |
| SG11201401342VA (en) * | 2011-10-12 | 2014-09-26 | Array Biopharma Inc | 5,7-substituted-imidazo[1,2-c]pyrimidines |
| HRP20160908T1 (hr) * | 2012-03-28 | 2016-09-23 | Merck Patent Gmbh | Biciklički derivati pirazinona |
| KR20170090476A (ko) | 2014-12-05 | 2017-08-07 | 어레이 바이오파마 인크. | 야누스 키나제 저해제로서의 4,6-치환된-피라졸로[1,5-a]피라진 |
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