JP6522646B2 - ＲＯＳ１阻害剤としての置換４，５，６，７−テトラヒドロ−ピラゾロ［１，５−α］ピラジン誘導体および５，６，７，８−テトラヒドロ−４Ｈ−ピラゾロ［１，５−α］［１，４］ジアゼピン誘導体 - Google Patents
ＲＯＳ１阻害剤としての置換４，５，６，７−テトラヒドロ−ピラゾロ［１，５−α］ピラジン誘導体および５，６，７，８−テトラヒドロ−４Ｈ−ピラゾロ［１，５−α］［１，４］ジアゼピン誘導体 Download PDFInfo
- Publication number
- JP6522646B2 JP6522646B2 JP2016559326A JP2016559326A JP6522646B2 JP 6522646 B2 JP6522646 B2 JP 6522646B2 JP 2016559326 A JP2016559326 A JP 2016559326A JP 2016559326 A JP2016559326 A JP 2016559326A JP 6522646 B2 JP6522646 B2 JP 6522646B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- alkyloxy
- hydrogen
- cyano
- 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.)
- Active
Links
- VBQCKGIJFMLQDP-UHFFFAOYSA-N CC(C)c1ccc(COc(cc2)ccc2-c2c(CN(CC(NC)=O)CC3)[n]3nc2-c2ccncc2)cc1 Chemical compound CC(C)c1ccc(COc(cc2)ccc2-c2c(CN(CC(NC)=O)CC3)[n]3nc2-c2ccncc2)cc1 VBQCKGIJFMLQDP-UHFFFAOYSA-N 0.000 description 1
- KEOTWCXKWJTSDU-UHFFFAOYSA-N CC(C)c1ccc(COc(cc2)ccc2-c2c(CNCC3)[n]3nc2-c2ccncc2)cc1 Chemical compound CC(C)c1ccc(COc(cc2)ccc2-c2c(CNCC3)[n]3nc2-c2ccncc2)cc1 KEOTWCXKWJTSDU-UHFFFAOYSA-N 0.000 description 1
- QOKKFJSFDDLQLE-UHFFFAOYSA-N CCOC(CN(CC[n]1nc2C3C=CN=CC3)Cc1c2-c(cc1)ccc1OCc1ccc(C(C)C)cc1)=O Chemical compound CCOC(CN(CC[n]1nc2C3C=CN=CC3)Cc1c2-c(cc1)ccc1OCc1ccc(C(C)C)cc1)=O QOKKFJSFDDLQLE-UHFFFAOYSA-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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- 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
- C07D487/10—Spiro-condensed systems
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/20—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14161950.2 | 2014-03-27 | ||
| EP14161950 | 2014-03-27 | ||
| PCT/EP2015/056498 WO2015144799A1 (en) | 2014-03-27 | 2015-03-26 | SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRAZINE DERIVATIVES AND 5,6,7,8-TETRAHYDRO-4H-PYRAZOLO[1,5-a][1,4]DIAZEPINE DERIVATIVES AS ROS1 INHIBITORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017508779A JP2017508779A (ja) | 2017-03-30 |
| JP2017508779A5 JP2017508779A5 (https=) | 2019-02-28 |
| JP6522646B2 true JP6522646B2 (ja) | 2019-05-29 |
Family
ID=50389872
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016559326A Active JP6522646B2 (ja) | 2014-03-27 | 2015-03-26 | ＲＯＳ１阻害剤としての置換４，５，６，７−テトラヒドロ−ピラゾロ［１，５−α］ピラジン誘導体および５，６，７，８−テトラヒドロ−４Ｈ−ピラゾロ［１，５−α］［１，４］ジアゼピン誘導体 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US10280170B2 (https=) |
| EP (1) | EP3129376B1 (https=) |
| JP (1) | JP6522646B2 (https=) |
| KR (1) | KR102455519B1 (https=) |
| CN (1) | CN106164076B (https=) |
| AU (1) | AU2015238296B2 (https=) |
| BR (1) | BR112016022105B1 (https=) |
| CA (1) | CA2940918C (https=) |
| EA (1) | EA032255B1 (https=) |
| ES (1) | ES2715676T3 (https=) |
| IL (1) | IL247947B (https=) |
| MX (1) | MX367914B (https=) |
| WO (1) | WO2015144799A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102630720B1 (ko) | 2015-08-28 | 2024-01-29 | 세키스이 메디칼 가부시키가이샤 | 벤질 화합물 |
| 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 |
| WO2019233456A1 (zh) * | 2018-06-08 | 2019-12-12 | 贝达药业股份有限公司 | Erk抑制剂及其应用 |
| CA3126334A1 (en) * | 2019-01-11 | 2020-07-16 | Shionogi & Co., Ltd. | Dihydropyrazolopyrazinone derivative having mgat2 inhibitory activity |
| JP7068743B2 (ja) * | 2019-01-11 | 2022-05-17 | 塩野義製薬株式会社 | Ｍｇａｔ２阻害活性を有する縮合環誘導体を含有する医薬組成物 |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN114315866B (zh) * | 2020-09-30 | 2023-10-31 | 烟台药物研究所 | 一种盐酸左旋咪唑的合成方法 |
| TW202229282A (zh) * | 2020-09-30 | 2022-08-01 | 美商史考皮恩治療有限公司 | 治療癌症之方法 |
| WO2022127756A1 (en) * | 2020-12-15 | 2022-06-23 | Gritscience Biopharmaceuticals Co., Ltd. | Compounds as casein kinase inhibitors |
| CN114957259A (zh) * | 2021-02-25 | 2022-08-30 | 南京明德新药研发有限公司 | 氰基取代的芳香双环类化合物及其应用 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5356897A (en) | 1991-09-09 | 1994-10-18 | Fujisawa Pharmaceutical Co., Ltd. | 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines |
| EP1505068A4 (en) | 2002-04-23 | 2008-03-19 | Shionogi & Co | PYRAZOLO (1,5-a) PYRIMIDINE DERIVATIVE AND INHIBITOR OF NAD (P) H OXIDASE CONTAINING SAID DERIVATIVE |
| KR101050700B1 (ko) | 2002-08-26 | 2011-07-20 | 다케다 야쿠힌 고교 가부시키가이샤 | 칼슘 수용체 조절 화합물 및 이의 용도 |
| CN1747949A (zh) * | 2002-12-20 | 2006-03-15 | 法马西亚公司 | 无环吡唑化合物 |
| JP2005343889A (ja) * | 2004-05-06 | 2005-12-15 | Taisho Pharmaceut Co Ltd | イミダゾピリジン誘導体 |
| US8288375B2 (en) * | 2007-12-12 | 2012-10-16 | E.I. Du Pont De Nemours And Company | Fungicidal bicyclic pyrazoles |
| CN101952293A (zh) | 2007-12-21 | 2011-01-19 | 惠氏有限责任公司 | 吡唑并[1,5-a]嘧啶化合物 |
| US20100029657A1 (en) * | 2008-02-29 | 2010-02-04 | Wyeth | Bridged, Bicyclic Heterocyclic or Spiro Bicyclic Heterocyclic Derivatives of Pyrazolo[1, 5-A]Pyrimidines, Methods for Preparation and Uses Thereof |
| US8592432B2 (en) | 2008-04-07 | 2013-11-26 | Bei Chen | Compounds and compositions as protein kinase inhibitors |
| KR20110002080A (ko) * | 2008-04-07 | 2011-01-06 | 아이알엠 엘엘씨 | 키나제 억제제로서의 화합물 및 조성물 |
| WO2009140128A2 (en) * | 2008-05-13 | 2009-11-19 | Irm Llc | Compounds and compositions as kinase inhibitors |
| CN102459264A (zh) * | 2009-05-27 | 2012-05-16 | 雅培制药有限公司 | 激酶活性的嘧啶抑制剂 |
| AU2010254151B2 (en) | 2009-05-28 | 2013-11-28 | Cook Medical Technologies Llc | Tacking device and methods of deployment |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| AU2012291744A1 (en) * | 2011-08-02 | 2014-02-20 | Pfizer Inc. | Crizotinib for use in the treatment of cancer |
| TWI585088B (zh) * | 2012-06-04 | 2017-06-01 | 第一三共股份有限公司 | 作爲激酶抑制劑之咪唑并［１，２－ｂ］嗒衍生物 |
-
2015
- 2015-03-26 EP EP15713436.2A patent/EP3129376B1/en active Active
- 2015-03-26 CN CN201580016470.XA patent/CN106164076B/zh active Active
- 2015-03-26 JP JP2016559326A patent/JP6522646B2/ja active Active
- 2015-03-26 AU AU2015238296A patent/AU2015238296B2/en active Active
- 2015-03-26 US US15/129,582 patent/US10280170B2/en active Active
- 2015-03-26 ES ES15713436T patent/ES2715676T3/es active Active
- 2015-03-26 WO PCT/EP2015/056498 patent/WO2015144799A1/en not_active Ceased
- 2015-03-26 EA EA201691930A patent/EA032255B1/ru not_active IP Right Cessation
- 2015-03-26 BR BR112016022105-2A patent/BR112016022105B1/pt active IP Right Grant
- 2015-03-26 MX MX2016012668A patent/MX367914B/es active IP Right Grant
- 2015-03-26 CA CA2940918A patent/CA2940918C/en active Active
- 2015-03-26 KR KR1020167028572A patent/KR102455519B1/ko active Active
-
2016
- 2016-09-21 IL IL247947A patent/IL247947B/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| AU2015238296A1 (en) | 2016-09-08 |
| EA032255B1 (ru) | 2019-04-30 |
| CN106164076B (zh) | 2019-03-26 |
| BR112016022105B1 (pt) | 2023-01-31 |
| EP3129376A1 (en) | 2017-02-15 |
| IL247947B (en) | 2019-03-31 |
| EA201691930A1 (ru) | 2017-02-28 |
| CA2940918C (en) | 2023-10-24 |
| BR112016022105A2 (https=) | 2017-08-15 |
| CA2940918A1 (en) | 2015-10-01 |
| ES2715676T3 (es) | 2019-06-05 |
| CN106164076A (zh) | 2016-11-23 |
| AU2015238296B2 (en) | 2018-10-18 |
| MX367914B (es) | 2019-09-11 |
| EP3129376B1 (en) | 2018-12-26 |
| KR20160137576A (ko) | 2016-11-30 |
| MX2016012668A (es) | 2016-12-14 |
| US20170174690A1 (en) | 2017-06-22 |
| WO2015144799A1 (en) | 2015-10-01 |
| US10280170B2 (en) | 2019-05-07 |
| KR102455519B1 (ko) | 2022-10-14 |
| JP2017508779A (ja) | 2017-03-30 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6522646B2 (ja) | ＲＯＳ１阻害剤としての置換４，５，６，７−テトラヒドロ−ピラゾロ［１，５−α］ピラジン誘導体および５，６，７，８−テトラヒドロ−４Ｈ−ピラゾロ［１，５−α］［１，４］ジアゼピン誘導体 | |
| JP2017508779A5 (https=) | ||
| KR102390276B1 (ko) | 마크로사이클릭 피리미딘 유도체 | |
| CN112778276A (zh) | 作为shp2抑制剂的化合物及其应用 | |
| JP6527167B2 (ja) | ＲＯＳ１阻害剤としての置換４，５，６，７−テトラヒドロ−ピラゾロ［１，５−ａ］ピリミジン誘導体および２，３−ジヒドロ−１Ｈ−イミダゾ［１，２−ｂ］ピラゾール誘導体 | |
| KR102784966B1 (ko) | Nik 억제제로서 신규 치환된 시아노인돌린 유도체 | |
| MX2013005897A (es) | Derivados de benzopirazina sustituidos como inhibidores de cinasa del receptor del factor de crecimiento de fibroblasto (fgfr) para el tratamiento de enfermedades cancerigenas. | |
| KR20160140739A (ko) | 마크로사이클릭 피리미딘 유도체 | |
| EP4055013B1 (en) | Wdr5 inhibitors and modulators | |
| JP2017508777A5 (https=) | ||
| EP4692088A1 (en) | Compound acting as wrn helicase inhibitor | |
| TW202110848A (zh) | 取代的稠合雙環類衍生物、其製備方法及其在醫藥上的應用 | |
| KR20220042127A (ko) | 피라졸로피리미딘 화합물, 그의 제조 방법 및 그의 응용 | |
| TW202102511A (zh) | 噻吩并雜環類衍生物、其製備方法及其在醫藥上的應用 | |
| JP6568588B2 (ja) | ＰＩ３Ｋβ阻害剤としてのイミダゾピリダジン誘導体 | |
| JP2022515309A (ja) | 置換アリール化合物、その製造方法及び用途 | |
| JP6586463B2 (ja) | ＰＩ３Ｋβ阻害剤としての複素環連結イミダゾピリダジン誘導体 | |
| TWI894448B (zh) | Ctla-4小分子降解劑及其應用 | |
| KR20250103668A (ko) | 축합 이환 화합물 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20171214 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20180807 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20180809 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20181106 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20181220 |
|
| A524 | Written submission of copy of amendment under article 19 pct |
Free format text: JAPANESE INTERMEDIATE CODE: A524 Effective date: 20190115 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20190409 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20190424 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6522646 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |