JP6325573B2 - Ｂｔｋキナーゼ抑制剤としての２，３−ジヒドロ−イソインドール−１−オン誘導体及びこれを含む薬学的組成物 - Google Patents
Ｂｔｋキナーゼ抑制剤としての２，３−ジヒドロ−イソインドール−１−オン誘導体及びこれを含む薬学的組成物 Download PDFInfo
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- JP6325573B2 JP6325573B2 JP2015550315A JP2015550315A JP6325573B2 JP 6325573 B2 JP6325573 B2 JP 6325573B2 JP 2015550315 A JP2015550315 A JP 2015550315A JP 2015550315 A JP2015550315 A JP 2015550315A JP 6325573 B2 JP6325573 B2 JP 6325573B2
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- Prior art keywords
- phenyl
- methyl
- fluoro
- imidazol
- urea
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- 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.)
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- 0 *c(cc1*)c(*)c(*)c1N Chemical compound *c(cc1*)c(*)c(*)c1N 0.000 description 1
- APUQSKGNRMHVQC-UHFFFAOYSA-N Cc1cnc(-c(ccc(-c(ccc(N)c2)c2F)c2CN3)c2C3=O)[nH]1 Chemical compound Cc1cnc(-c(ccc(-c(ccc(N)c2)c2F)c2CN3)c2C3=O)[nH]1 APUQSKGNRMHVQC-UHFFFAOYSA-N 0.000 description 1
- NXLNNXIXOYSCMB-UHFFFAOYSA-N [O-][N+](c(cc1)ccc1OC(Cl)=O)=O Chemical compound [O-][N+](c(cc1)ccc1OC(Cl)=O)=O NXLNNXIXOYSCMB-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/4035—Isoindoles, e.g. phthalimide
-
- 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
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261746980P | 2012-12-28 | 2012-12-28 | |
| US61/746,980 | 2012-12-28 | ||
| PCT/KR2013/012204 WO2014104757A1 (ko) | 2012-12-28 | 2013-12-26 | Btk 키나아제 억제제로서의 2,3-디하이드로-이소인돌-1-온 유도체 및 이를 함유하는 약학적 조성물 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018076877A Division JP6596537B2 (ja) | 2012-12-28 | 2018-04-12 | Ｂｔｋキナーゼ抑制剤としての２，３−ジヒドロ−イソインドール−１−オン誘導体及びこれを含む薬学的組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016504351A JP2016504351A (ja) | 2016-02-12 |
| JP2016504351A5 JP2016504351A5 (OSRAM) | 2017-02-16 |
| JP6325573B2 true JP6325573B2 (ja) | 2018-05-16 |
Family
ID=51021712
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015550315A Active JP6325573B2 (ja) | 2012-12-28 | 2013-12-26 | Ｂｔｋキナーゼ抑制剤としての２，３−ジヒドロ−イソインドール−１−オン誘導体及びこれを含む薬学的組成物 |
| JP2018076877A Active JP6596537B2 (ja) | 2012-12-28 | 2018-04-12 | Ｂｔｋキナーゼ抑制剤としての２，３−ジヒドロ−イソインドール−１−オン誘導体及びこれを含む薬学的組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018076877A Active JP6596537B2 (ja) | 2012-12-28 | 2018-04-12 | Ｂｔｋキナーゼ抑制剤としての２，３−ジヒドロ−イソインドール−１−オン誘導体及びこれを含む薬学的組成物 |
Country Status (15)
| Country | Link |
|---|---|
| US (4) | US9758508B2 (OSRAM) |
| EP (2) | EP2940014B1 (OSRAM) |
| JP (2) | JP6325573B2 (OSRAM) |
| KR (1) | KR102009163B1 (OSRAM) |
| CN (1) | CN104995184B (OSRAM) |
| AU (3) | AU2013371146C1 (OSRAM) |
| BR (1) | BR112015015477B1 (OSRAM) |
| CA (1) | CA2896711C (OSRAM) |
| DK (1) | DK2940014T3 (OSRAM) |
| ES (2) | ES2696700T3 (OSRAM) |
| MX (2) | MX2021011563A (OSRAM) |
| PL (1) | PL2940014T3 (OSRAM) |
| PT (1) | PT2940014T (OSRAM) |
| RU (2) | RU2671847C2 (OSRAM) |
| WO (1) | WO2014104757A1 (OSRAM) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2018109069A (ja) * | 2012-12-28 | 2018-07-12 | クリスタルジェノミクス・インコーポレイテッドＣｒｙｓｔａｌｇｅｎｏｍｉｃｓ， Ｉｎｃ． | Ｂｔｋキナーゼ抑制剤としての２，３−ジヒドロ−イソインドール−１−オン誘導体及びこれを含む薬学的組成物 |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2918588B1 (en) | 2010-05-20 | 2017-05-03 | Array Biopharma, Inc. | Macrocyclic compounds as TRK kinase inhibitors |
| DK3322706T3 (da) | 2015-07-16 | 2021-02-01 | Array Biopharma Inc | Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| MA46995A (fr) | 2016-12-03 | 2019-10-09 | Acerta Pharma Bv | Méthodes et compositions pour l'utilisation de lymphocytes t thérapeutiques en association avec des inhibiteurs de kinase |
| CA3049136C (en) | 2017-01-18 | 2022-06-14 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| CN110621665A (zh) * | 2017-02-21 | 2019-12-27 | 艾普托斯生物科学公司 | 用于治疗患有恶性血液病的患者的方法 |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| CA3087578C (en) | 2018-01-18 | 2023-08-08 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| CA3087354C (en) | 2018-01-18 | 2023-01-03 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| EP3886840A4 (en) * | 2018-11-30 | 2022-08-24 | Aptose Biosciences Inc. | Combination therapy with 2,3-dihydro-isoindole-1-one compounds and methods for treating patients with various mutations |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| CN116829143A (zh) * | 2021-01-05 | 2023-09-29 | 住友制药肿瘤公司 | 非受体型酪氨酸激酶1（tnk1）抑制剂的形式和制剂 |
| WO2022187856A1 (en) * | 2021-03-05 | 2022-09-09 | Nimbus Saturn, Inc. | Hpk1 antagonists and uses thereof |
| US12071442B2 (en) | 2021-03-29 | 2024-08-27 | Nimbus Saturn, Inc. | Substituted pyrrolo[3,4-c]pyridines as HPK1 antagonists |
| WO2024245578A1 (en) | 2023-06-02 | 2024-12-05 | Netherlands Translational Research Center Holding B.V. | Therapeutic combinations of an irreversible btk inhibitor and a macrocyclic reversible btk inhibitor |
| WO2024245577A1 (en) | 2023-06-02 | 2024-12-05 | Netherlands Translational Research Center Holding B.V. | Therapeutic combinations of an irreversible btk inhibitor and a reversible btk inhibitor |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL157873A0 (en) * | 2001-04-12 | 2004-03-28 | Hoffmann La Roche | DIHYDRO-BENZO [b] [1,4] DIAZEPIN-2-ONE DERIVATIVES AS MGLUR2 ANTAGONISTS II |
| JP2006526648A (ja) * | 2003-06-02 | 2006-11-24 | アボット・ラボラトリーズ | キナーゼ阻害剤としてのイソインドリン−１−オン化合物 |
| PE20061119A1 (es) * | 2005-01-19 | 2006-11-27 | Aventis Pharma Sa | PIRAZOLO PIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE CINASAS FAK, KDR Y Tie |
| US7745641B2 (en) | 2005-04-19 | 2010-06-29 | Kyowa Hakko Kirin Co., Ltd. | Nitrogen-containing heterocyclic compound |
| US20070161648A1 (en) | 2005-10-14 | 2007-07-12 | Hughes Terry V | Substituted dihydro-isoindolones useful in treating kinase disorders |
| CA2645583A1 (en) * | 2006-03-20 | 2007-09-27 | F. Hoffman-La Roche Ag | Methods of inhibiting btk and syk protein kinases |
| JPWO2008047831A1 (ja) * | 2006-10-17 | 2010-02-25 | 協和発酵キリン株式会社 | Ｊａｋ阻害剤 |
| CA2701275C (en) * | 2007-10-23 | 2016-06-21 | F. Hoffmann-La Roche Ag | Kinase inhibitors |
| WO2012014017A1 (en) | 2010-07-30 | 2012-02-02 | Poly Medicure Limited | Catheter introducer |
| WO2012047017A2 (ko) * | 2010-10-05 | 2012-04-12 | 크리스탈지노믹스(주) | 2,3-디히드로-이소인돌-1-온 유도체 및 이를 포함하는 조성물 |
| RU2671847C2 (ru) | 2012-12-28 | 2018-11-07 | Кристалдженомикс, Инк. | Производные 2,3-дигидро-изоиндол-1-она и способы их применения в качестве ингибиторов тирозинкиназы брутона |
| US10463658B2 (en) | 2013-10-25 | 2019-11-05 | Videra Pharmaceuticals, Llc | Method of inhibiting FLT3 kinase |
-
2013
- 2013-12-26 RU RU2015124381A patent/RU2671847C2/ru active
- 2013-12-26 EP EP13867650.7A patent/EP2940014B1/en active Active
- 2013-12-26 ES ES13867650T patent/ES2696700T3/es active Active
- 2013-12-26 CN CN201380068623.6A patent/CN104995184B/zh active Active
- 2013-12-26 MX MX2021011563A patent/MX2021011563A/es unknown
- 2013-12-26 PL PL13867650T patent/PL2940014T3/pl unknown
- 2013-12-26 DK DK13867650.7T patent/DK2940014T3/en active
- 2013-12-26 WO PCT/KR2013/012204 patent/WO2014104757A1/ko not_active Ceased
- 2013-12-26 PT PT13867650T patent/PT2940014T/pt unknown
- 2013-12-26 BR BR112015015477-8A patent/BR112015015477B1/pt active IP Right Grant
- 2013-12-26 KR KR1020157018342A patent/KR102009163B1/ko active Active
- 2013-12-26 ES ES18190153T patent/ES2929906T3/es active Active
- 2013-12-26 CA CA2896711A patent/CA2896711C/en active Active
- 2013-12-26 RU RU2018138028A patent/RU2018138028A/ru unknown
- 2013-12-26 JP JP2015550315A patent/JP6325573B2/ja active Active
- 2013-12-26 EP EP18190153.9A patent/EP3428161B1/en active Active
- 2013-12-26 AU AU2013371146A patent/AU2013371146C1/en active Active
- 2013-12-26 MX MX2015008396A patent/MX386542B/es unknown
- 2013-12-26 US US14/655,954 patent/US9758508B2/en active Active
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2017
- 2017-08-30 US US15/691,432 patent/US10604508B2/en active Active
-
2018
- 2018-04-12 JP JP2018076877A patent/JP6596537B2/ja active Active
- 2018-08-10 AU AU2018214134A patent/AU2018214134B2/en active Active
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2020
- 2020-02-14 US US16/791,753 patent/US11230539B2/en active Active
- 2020-02-27 AU AU2020201431A patent/AU2020201431B2/en active Active
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2022
- 2022-07-22 US US17/871,458 patent/US20220380346A1/en not_active Abandoned
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2018109069A (ja) * | 2012-12-28 | 2018-07-12 | クリスタルジェノミクス・インコーポレイテッドＣｒｙｓｔａｌｇｅｎｏｍｉｃｓ， Ｉｎｃ． | Ｂｔｋキナーゼ抑制剤としての２，３−ジヒドロ−イソインドール−１−オン誘導体及びこれを含む薬学的組成物 |
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