JP6214643B2 - ピリミジニルチロシンキナーゼ阻害剤 - Google Patents
ピリミジニルチロシンキナーゼ阻害剤 Download PDFInfo
- Publication number
- JP6214643B2 JP6214643B2 JP2015516256A JP2015516256A JP6214643B2 JP 6214643 B2 JP6214643 B2 JP 6214643B2 JP 2015516256 A JP2015516256 A JP 2015516256A JP 2015516256 A JP2015516256 A JP 2015516256A JP 6214643 B2 JP6214643 B2 JP 6214643B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- acceptable salt
- pharmaceutically acceptable
- amino
- optionally substituted
- 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.)
- Expired - Fee Related
Links
- 0 C*C([C@@](CCN(C1)c(ncnc2N)c2F)[C@]1N(CCC[C@]1Nc2cc(Cl)cc(*)c2)C1=O)=O Chemical compound C*C([C@@](CCN(C1)c(ncnc2N)c2F)[C@]1N(CCC[C@]1Nc2cc(Cl)cc(*)c2)C1=O)=O 0.000 description 6
- NNHLHUQUOSCOEN-YSTUSHMSSA-N CN(CC1)CCN1C([C@@H](CCN(C1)c2ncnc(N)c2F)[C@H]1N(CCCC1Nc2cc(Cl)cc(C(F)(F)F)c2)C1=O)=O Chemical compound CN(CC1)CCN1C([C@@H](CCN(C1)c2ncnc(N)c2F)[C@H]1N(CCCC1Nc2cc(Cl)cc(C(F)(F)F)c2)C1=O)=O NNHLHUQUOSCOEN-YSTUSHMSSA-N 0.000 description 1
- XIXPQPAHEZDFNG-WMEOFMBSSA-N CN(CC1)CCN1C([C@@H](CCNC1)[C@H]1N(CCCC1Nc2cc(Cl)cc(C(F)(F)F)c2)C1=O)=O Chemical compound CN(CC1)CCN1C([C@@H](CCNC1)[C@H]1N(CCCC1Nc2cc(Cl)cc(C(F)(F)F)c2)C1=O)=O XIXPQPAHEZDFNG-WMEOFMBSSA-N 0.000 description 1
- GUPKEOUZKHLRGS-HYPNFROTSA-N C[C@@H](c1ccccc1)/N=C(\CN(CC1)c(ncnc2N)c2F)/C1C(O)=O Chemical compound C[C@@H](c1ccccc1)/N=C(\CN(CC1)c(ncnc2N)c2F)/C1C(O)=O GUPKEOUZKHLRGS-HYPNFROTSA-N 0.000 description 1
- SUMCMXORPZCWHU-UHFFFAOYSA-N NC(C1F)=NC=NC1Cl Chemical compound NC(C1F)=NC=NC1Cl SUMCMXORPZCWHU-UHFFFAOYSA-N 0.000 description 1
- OVENUGPMQDFGLE-UHFFFAOYSA-N Nc1cc(Cl)cc(C(F)(F)F)c1 Chemical compound Nc1cc(Cl)cc(C(F)(F)F)c1 OVENUGPMQDFGLE-UHFFFAOYSA-N 0.000 description 1
- FEIFDRDCVMVUJA-UHFFFAOYSA-N Nc1ncnc(Cl)c1F Chemical compound Nc1ncnc(Cl)c1F FEIFDRDCVMVUJA-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
- A61K31/505—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Dermatology (AREA)
- Transplantation (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Gastroenterology & Hepatology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261657360P | 2012-06-08 | 2012-06-08 | |
| US61/657,360 | 2012-06-08 | ||
| PCT/US2013/044800 WO2013185084A1 (en) | 2012-06-08 | 2013-06-07 | Pyrimidinyl tyrosine kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017150480A Division JP2017193583A (ja) | 2012-06-08 | 2017-08-03 | ピリミジニルチロシンキナーゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015518903A JP2015518903A (ja) | 2015-07-06 |
| JP2015518903A5 JP2015518903A5 (enExample) | 2016-07-28 |
| JP6214643B2 true JP6214643B2 (ja) | 2017-10-18 |
Family
ID=49712704
Family Applications (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015516256A Expired - Fee Related JP6214643B2 (ja) | 2012-06-08 | 2013-06-07 | ピリミジニルチロシンキナーゼ阻害剤 |
| JP2017150480A Withdrawn JP2017193583A (ja) | 2012-06-08 | 2017-08-03 | ピリミジニルチロシンキナーゼ阻害剤 |
| JP2019017850A Withdrawn JP2019077728A (ja) | 2012-06-08 | 2019-02-04 | ピリミジニルチロシンキナーゼ阻害剤 |
| JP2021018128A Pending JP2021073299A (ja) | 2012-06-08 | 2021-02-08 | ピリミジニルチロシンキナーゼ阻害剤 |
| JP2021018127A Pending JP2021073298A (ja) | 2012-06-08 | 2021-02-08 | ピリミジニルチロシンキナーゼ阻害剤 |
| JP2023004462A Pending JP2023052415A (ja) | 2012-06-08 | 2023-01-16 | ピリミジニルチロシンキナーゼ阻害剤 |
Family Applications After (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017150480A Withdrawn JP2017193583A (ja) | 2012-06-08 | 2017-08-03 | ピリミジニルチロシンキナーゼ阻害剤 |
| JP2019017850A Withdrawn JP2019077728A (ja) | 2012-06-08 | 2019-02-04 | ピリミジニルチロシンキナーゼ阻害剤 |
| JP2021018128A Pending JP2021073299A (ja) | 2012-06-08 | 2021-02-08 | ピリミジニルチロシンキナーゼ阻害剤 |
| JP2021018127A Pending JP2021073298A (ja) | 2012-06-08 | 2021-02-08 | ピリミジニルチロシンキナーゼ阻害剤 |
| JP2023004462A Pending JP2023052415A (ja) | 2012-06-08 | 2023-01-16 | ピリミジニルチロシンキナーゼ阻害剤 |
Country Status (30)
| Country | Link |
|---|---|
| US (6) | US9394277B2 (enExample) |
| EP (3) | EP3385263B1 (enExample) |
| JP (6) | JP6214643B2 (enExample) |
| KR (4) | KR102468430B1 (enExample) |
| CN (3) | CN113549055A (enExample) |
| AR (1) | AR091273A1 (enExample) |
| AU (5) | AU2013271407B2 (enExample) |
| BR (2) | BR112014030655B1 (enExample) |
| CA (2) | CA2875799C (enExample) |
| CY (1) | CY1120638T1 (enExample) |
| DK (1) | DK2858499T3 (enExample) |
| EA (2) | EA201790418A1 (enExample) |
| ES (2) | ES2684268T3 (enExample) |
| HR (1) | HRP20181294T1 (enExample) |
| HU (1) | HUE039897T2 (enExample) |
| IL (2) | IL235938B (enExample) |
| IN (1) | IN2014DN10576A (enExample) |
| LT (1) | LT2858499T (enExample) |
| MX (2) | MX385593B (enExample) |
| NZ (1) | NZ702715A (enExample) |
| PH (2) | PH12018501463B1 (enExample) |
| PL (1) | PL2858499T3 (enExample) |
| PT (1) | PT2858499T (enExample) |
| RS (1) | RS57978B1 (enExample) |
| SG (2) | SG11201408173WA (enExample) |
| SI (1) | SI2858499T1 (enExample) |
| SM (1) | SMT201800442T1 (enExample) |
| TW (3) | TWI719209B (enExample) |
| WO (1) | WO2013185084A1 (enExample) |
| ZA (1) | ZA201409255B (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE043522T2 (hu) * | 2009-09-04 | 2019-08-28 | Biogen Ma Inc | Bruton tirozinkináz inhibitorok |
| EP2632898A4 (en) | 2010-10-29 | 2014-04-02 | Biogen Idec Inc | HETEROCYCLIC TYROSINE KINASE HEMMER |
| EP2858500A4 (en) | 2012-06-08 | 2016-04-06 | Biogen Ma Inc | BRUTON TYROSINE KINASE HEMMER |
| AR091273A1 (es) * | 2012-06-08 | 2015-01-21 | Biogen Idec Inc | Inhibidores de pirimidinil tirosina quinasa |
| KR102413253B1 (ko) * | 2013-12-11 | 2022-06-27 | 바이오젠 엠에이 인코포레이티드 | 종양, 신경 및 면역에서 인간 질환을 치료하는데 유용한 바이아릴 화합물 |
| WO2015151006A1 (en) | 2014-03-29 | 2015-10-08 | Lupin Limited | Substituted purine compounds as btk inhibitors |
| WO2015170266A1 (en) | 2014-05-07 | 2015-11-12 | Lupin Limited | Substituted pyrimidine compounds as btk inhibitors |
| PE20190710A1 (es) | 2014-10-24 | 2019-05-17 | Bristol Myers Squibb Co | Compuestos de indol carboxamida utiles como inhibidores de cinasas |
| EP3487852A1 (en) * | 2016-07-21 | 2019-05-29 | Biogen MA Inc. | Succinate forms and compositions of bruton's tyrosine kinase inhibitors |
| WO2019208805A1 (ja) | 2018-04-27 | 2019-10-31 | 小野薬品工業株式会社 | Ｂｔｋ阻害活性を有する化合物を有効成分として含む自己免疫疾患の予防および／または治療剤 |
| CA3224985A1 (en) | 2018-07-31 | 2020-02-06 | Loxo Oncology, Inc. | Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide |
| 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 |
| EP4313023A1 (en) | 2021-04-02 | 2024-02-07 | Biogen MA Inc. | Combination treatment methods of multiple sclerosis |
| WO2023081715A1 (en) | 2021-11-03 | 2023-05-11 | Viracta Therapeutics, Inc. | Combination of car t-cell therapy with btk inhibitors and methods of use thereof |
| WO2023081709A1 (en) | 2021-11-03 | 2023-05-11 | Viracta Therapeutics, Inc. | Vecabrutinib for the treatment of graft-versus-host disease |
| US20250074911A1 (en) | 2021-12-14 | 2025-03-06 | Crossfire Oncology Holding B.V. | Macrocyclic btk inhibitors |
| 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 |
| WO2024246287A1 (en) | 2023-06-02 | 2024-12-05 | Crossfire Oncology Holding B.V. | Medical use of a macrocyclic reversible btk inhibitor |
| WO2024256568A1 (en) | 2023-06-13 | 2024-12-19 | Crossfire Oncology Holding B.V. | Salt and crystal forms of a macrocyclic btk inhibitor |
| WO2024256574A1 (en) | 2023-06-13 | 2024-12-19 | Crossfire Oncology Holding B.V. | Process for preparing macrocyclic btk inhibitors |
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| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| DE69212850T2 (de) | 1991-01-15 | 1997-03-06 | Alcon Lab Inc | Verwendung von Karrageenan in topischen ophthalmologischen Zusammensetzungen |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
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| PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
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| ATE437872T1 (de) | 2003-10-14 | 2009-08-15 | Univ Arizona | Proteinkinaseinhibitoren |
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