IL247948B - 7,6,5,4-tetrahydro-pyrazolo[5,1-a]pyrimidine derivatives and 3,2-dihydro-h1-imidazo[2,1-b]pyrazole derivatives as ros1 inhibitors - Google Patents
7,6,5,4-tetrahydro-pyrazolo[5,1-a]pyrimidine derivatives and 3,2-dihydro-h1-imidazo[2,1-b]pyrazole derivatives as ros1 inhibitorsInfo
- Publication number
- IL247948B IL247948B IL247948A IL24794816A IL247948B IL 247948 B IL247948 B IL 247948B IL 247948 A IL247948 A IL 247948A IL 24794816 A IL24794816 A IL 24794816A IL 247948 B IL247948 B IL 247948B
- Authority
- IL
- Israel
- Prior art keywords
- derivatives
- pyrazolo
- imidazo
- tetrahydro
- dihydro
- Prior art date
Links
- HJFZVTDRWQVFDN-UHFFFAOYSA-N 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine Chemical class C1CCNC2=CC=NN21 HJFZVTDRWQVFDN-UHFFFAOYSA-N 0.000 title 1
- 101100091501 Mus musculus Ros1 gene Proteins 0.000 title 1
- KPMVHELZNRNSMN-UHFFFAOYSA-N chembl1985849 Chemical class N1=CC=C2NCCN21 KPMVHELZNRNSMN-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
Classifications
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-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
- C07D487/02—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14161959 | 2014-03-27 | ||
| PCT/EP2015/056501 WO2015144801A1 (en) | 2014-03-27 | 2015-03-26 | SUBSTITUTED 4,5,6,7-TETRAHYDRO-PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AND 2,3-DIHYDRO-1H-IMIDAZO[1,2-b]PYRAZOLE DERIVATIVES AS ROS1 INHIBITORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL247948B true IL247948B (en) | 2019-03-31 |
Family
ID=50389875
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL247948A IL247948B (en) | 2014-03-27 | 2016-09-21 | 7,6,5,4-tetrahydro-pyrazolo[5,1-a]pyrimidine derivatives and 3,2-dihydro-h1-imidazo[2,1-b]pyrazole derivatives as ros1 inhibitors |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US10342795B2 (https=) |
| EP (1) | EP3126366B1 (https=) |
| JP (1) | JP6527167B2 (https=) |
| KR (1) | KR102455518B1 (https=) |
| CN (1) | CN106132967B (https=) |
| AU (1) | AU2015238298B2 (https=) |
| BR (1) | BR112016021507B1 (https=) |
| CA (1) | CA2941206C (https=) |
| EA (1) | EA031639B1 (https=) |
| ES (1) | ES2686747T3 (https=) |
| IL (1) | IL247948B (https=) |
| MX (1) | MX367913B (https=) |
| WO (1) | WO2015144801A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106580982B (zh) * | 2016-11-26 | 2017-09-22 | 王玉美 | 一种治疗药物流产后子宫出血的药物 |
| CN106866536A (zh) * | 2017-04-12 | 2017-06-20 | 中国农业大学 | 一种制备4‑卤代‑5‑氨基吡唑的方法 |
| CN115109116A (zh) * | 2017-08-17 | 2022-09-27 | 凯瑞康宁生物工程（武汉）有限公司 | 活性氧清除剂衍生物的制备及用途 |
| 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 |
| CN111087398A (zh) * | 2019-12-24 | 2020-05-01 | 上海万巷制药有限公司 | 一种制备拉罗替尼中间体的清洁工艺 |
| JP2023511302A (ja) | 2020-01-13 | 2023-03-17 | アプタバイオ セラピューティクス インコーポレイテッド | 新規なピラゾール誘導体 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN113416140B (zh) * | 2021-06-03 | 2023-01-13 | 万华化学集团股份有限公司 | 一种制备2-甲基戊二胺的方法 |
| US20250145628A1 (en) * | 2022-02-15 | 2025-05-08 | Novo Nordisk A/S | Pyrazolopyrimidines, compositions comprising them and uses thereof |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9204464D0 (en) * | 1992-03-02 | 1992-04-15 | Fujisawa Pharmaceutical Co | New heterocyclic derivatives |
| 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 |
| UA80295C2 (en) * | 2002-09-06 | 2007-09-10 | Biogen Inc | Pyrazolopyridines and using the same |
| CN1747949A (zh) | 2002-12-20 | 2006-03-15 | 法马西亚公司 | 无环吡唑化合物 |
| 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 |
| 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 |
| WO2011153553A2 (en) * | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| JO3407B1 (ar) * | 2012-05-31 | 2019-10-20 | Eisai R&D Man Co Ltd | مركبات رباعي هيدرو بيرازولو بيريميدين |
| 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 CN CN201580016427.3A patent/CN106132967B/zh active Active
- 2015-03-26 CA CA2941206A patent/CA2941206C/en active Active
- 2015-03-26 AU AU2015238298A patent/AU2015238298B2/en active Active
- 2015-03-26 KR KR1020167027337A patent/KR102455518B1/ko active Active
- 2015-03-26 ES ES15712138.5T patent/ES2686747T3/es active Active
- 2015-03-26 JP JP2016559277A patent/JP6527167B2/ja active Active
- 2015-03-26 BR BR112016021507-9A patent/BR112016021507B1/pt active IP Right Grant
- 2015-03-26 US US15/129,618 patent/US10342795B2/en active Active
- 2015-03-26 WO PCT/EP2015/056501 patent/WO2015144801A1/en not_active Ceased
- 2015-03-26 EP EP15712138.5A patent/EP3126366B1/en active Active
- 2015-03-26 EA EA201691934A patent/EA031639B1/ru not_active IP Right Cessation
- 2015-03-26 MX MX2016012669A patent/MX367913B/es active IP Right Grant
-
2016
- 2016-09-21 IL IL247948A patent/IL247948B/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| CA2941206A1 (en) | 2015-10-01 |
| JP2017508777A (ja) | 2017-03-30 |
| EA031639B1 (ru) | 2019-01-31 |
| KR102455518B1 (ko) | 2022-10-14 |
| US20170173014A1 (en) | 2017-06-22 |
| WO2015144801A1 (en) | 2015-10-01 |
| CN106132967A (zh) | 2016-11-16 |
| BR112016021507B1 (pt) | 2022-10-18 |
| KR20160137566A (ko) | 2016-11-30 |
| EP3126366B1 (en) | 2018-06-06 |
| AU2015238298A1 (en) | 2016-09-15 |
| ES2686747T3 (es) | 2018-10-19 |
| CA2941206C (en) | 2022-09-20 |
| AU2015238298B2 (en) | 2019-04-18 |
| US10342795B2 (en) | 2019-07-09 |
| MX2016012669A (es) | 2016-12-14 |
| MX367913B (es) | 2019-09-11 |
| CN106132967B (zh) | 2019-05-28 |
| BR112016021507A2 (https=) | 2017-08-15 |
| EP3126366A1 (en) | 2017-02-08 |
| JP6527167B2 (ja) | 2019-06-05 |
| EA201691934A1 (ru) | 2017-01-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed | ||
| KB | Patent renewed |