RU2018138028A - Производные 2,3-дигидро-изоиндол-1-она и способы их применения в качестве ингибиторов тирозинкиназы брутона - Google Patents
Производные 2,3-дигидро-изоиндол-1-она и способы их применения в качестве ингибиторов тирозинкиназы брутона Download PDFInfo
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- RU2018138028A RU2018138028A RU2018138028A RU2018138028A RU2018138028A RU 2018138028 A RU2018138028 A RU 2018138028A RU 2018138028 A RU2018138028 A RU 2018138028A RU 2018138028 A RU2018138028 A RU 2018138028A RU 2018138028 A RU2018138028 A RU 2018138028A
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- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- methyl
- dihydro
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims 8
- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 title 1
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 title 1
- PXZQEOJJUGGUIB-UHFFFAOYSA-N isoindolin-1-one Chemical class C1=CC=C2C(=O)NCC2=C1 PXZQEOJJUGGUIB-UHFFFAOYSA-N 0.000 title 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 title 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 9
- 206010061218 Inflammation Diseases 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 230000004054 inflammatory process Effects 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- MWHHJYUHCZWSLS-UHFFFAOYSA-N FC=1C=C(C=CC1C1=C2CNC(C2=C(C=C1)C=1NC(=CN1)C)=O)NC(=O)NC1=C(C=C(C=C1F)F)F Chemical compound FC=1C=C(C=CC1C1=C2CNC(C2=C(C=C1)C=1NC(=CN1)C)=O)NC(=O)NC1=C(C=C(C=C1F)F)F MWHHJYUHCZWSLS-UHFFFAOYSA-N 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 102000001253 Protein Kinase Human genes 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 108060006633 protein kinase Proteins 0.000 claims 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 206010012438 Dermatitis atopic Diseases 0.000 claims 2
- 241000402754 Erythranthe moschata Species 0.000 claims 2
- 108091008794 FGF receptors Proteins 0.000 claims 2
- 102100035108 High affinity nerve growth factor receptor Human genes 0.000 claims 2
- 101000663003 Homo sapiens Non-receptor tyrosine-protein kinase TNK1 Proteins 0.000 claims 2
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 claims 2
- 101000662997 Homo sapiens TRAF2 and NCK-interacting protein kinase Proteins 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 102100021435 Macrophage-stimulating protein receptor Human genes 0.000 claims 2
- 241000772415 Neovison vison Species 0.000 claims 2
- 102100037669 Non-receptor tyrosine-protein kinase TNK1 Human genes 0.000 claims 2
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 claims 2
- 102100028286 Proto-oncogene tyrosine-protein kinase receptor Ret Human genes 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 102000001332 SRC Human genes 0.000 claims 2
- 102100037671 TRAF2 and NCK-interacting protein kinase Human genes 0.000 claims 2
- 102100038183 Tyrosine-protein kinase SYK Human genes 0.000 claims 2
- 102100029654 Tyrosine-protein kinase Srms Human genes 0.000 claims 2
- 102100022007 Tyrosine-protein kinase receptor Tie-1 Human genes 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 230000007815 allergy Effects 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 108091054455 MAP kinase family Proteins 0.000 claims 1
- 102000043136 MAP kinase family Human genes 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 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)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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 (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261746980P | 2012-12-28 | 2012-12-28 | |
| US61/746,980 | 2012-12-28 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2015124381A Division RU2671847C2 (ru) | 2012-12-28 | 2013-12-26 | Производные 2,3-дигидро-изоиндол-1-она и способы их применения в качестве ингибиторов тирозинкиназы брутона |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2018138028A true RU2018138028A (ru) | 2019-03-21 |
Family
ID=51021712
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2015124381A RU2671847C2 (ru) | 2012-12-28 | 2013-12-26 | Производные 2,3-дигидро-изоиндол-1-она и способы их применения в качестве ингибиторов тирозинкиназы брутона |
| RU2018138028A RU2018138028A (ru) | 2012-12-28 | 2013-12-26 | Производные 2,3-дигидро-изоиндол-1-она и способы их применения в качестве ингибиторов тирозинкиназы брутона |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2015124381A RU2671847C2 (ru) | 2012-12-28 | 2013-12-26 | Производные 2,3-дигидро-изоиндол-1-она и способы их применения в качестве ингибиторов тирозинкиназы брутона |
Country Status (15)
| Country | Link |
|---|---|
| US (4) | US9758508B2 (enExample) |
| EP (2) | EP2940014B1 (enExample) |
| JP (2) | JP6325573B2 (enExample) |
| KR (1) | KR102009163B1 (enExample) |
| CN (1) | CN104995184B (enExample) |
| AU (3) | AU2013371146C1 (enExample) |
| BR (1) | BR112015015477B1 (enExample) |
| CA (1) | CA2896711C (enExample) |
| DK (1) | DK2940014T3 (enExample) |
| ES (2) | ES2696700T3 (enExample) |
| MX (2) | MX2021011563A (enExample) |
| PL (1) | PL2940014T3 (enExample) |
| PT (1) | PT2940014T (enExample) |
| RU (2) | RU2671847C2 (enExample) |
| WO (1) | WO2014104757A1 (enExample) |
Families Citing this family (26)
| 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 |
| 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 |
| 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
-
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
-
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
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