KR20130048293A - 단백질 키나제 억제제로서의 헤테로아릴 화합물 및 조성물 - Google Patents
단백질 키나제 억제제로서의 헤테로아릴 화합물 및 조성물 Download PDFInfo
- Publication number
- KR20130048293A KR20130048293A KR1020137001935A KR20137001935A KR20130048293A KR 20130048293 A KR20130048293 A KR 20130048293A KR 1020137001935 A KR1020137001935 A KR 1020137001935A KR 20137001935 A KR20137001935 A KR 20137001935A KR 20130048293 A KR20130048293 A KR 20130048293A
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- chloro
- mmol
- pyrimidin
- phenyl
- 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.)
- Abandoned
Links
- WBEURMWKHBNAMD-UHFFFAOYSA-N CC(C)(C)c1nc(-c2cc(Cl)cc(NS(C)(=O)=O)c2Cl)c(-c2nc(SC)ncc2)[s]1 Chemical compound CC(C)(C)c1nc(-c2cc(Cl)cc(NS(C)(=O)=O)c2Cl)c(-c2nc(SC)ncc2)[s]1 WBEURMWKHBNAMD-UHFFFAOYSA-N 0.000 description 1
- PFRJYJSPWLELPX-UHFFFAOYSA-N CCCS(Nc(cccc1-c2c(-c3nc(S(C)(=O)=O)ncc3)[o]c(C3CC3)n2)c1F)(=O)=O Chemical compound CCCS(Nc(cccc1-c2c(-c3nc(S(C)(=O)=O)ncc3)[o]c(C3CC3)n2)c1F)(=O)=O PFRJYJSPWLELPX-UHFFFAOYSA-N 0.000 description 1
- MUHRJMGGJPOWRC-UHFFFAOYSA-N CCCS(Nc1cccc(-c2c(-c3nc(NC)ncc3)[o]c(C3CC3)n2)c1F)(=O)=O Chemical compound CCCS(Nc1cccc(-c2c(-c3nc(NC)ncc3)[o]c(C3CC3)n2)c1F)(=O)=O MUHRJMGGJPOWRC-UHFFFAOYSA-N 0.000 description 1
- LSISENKINCBKER-LBPRGKRZSA-N C[C@@H](CNc1nccc(-c2c(-c3cc(F)cc(NS(C)(=O)=O)c3C)nc(C3CC3)[s]2)n1)NC(OC)=O Chemical compound C[C@@H](CNc1nccc(-c2c(-c3cc(F)cc(NS(C)(=O)=O)c3C)nc(C3CC3)[s]2)n1)NC(OC)=O LSISENKINCBKER-LBPRGKRZSA-N 0.000 description 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
- A61K31/435—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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (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 (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35860310P | 2010-06-25 | 2010-06-25 | |
| US61/358,603 | 2010-06-25 | ||
| US36853410P | 2010-07-28 | 2010-07-28 | |
| US61/368,534 | 2010-07-28 | ||
| PCT/EP2011/060561 WO2011161216A1 (en) | 2010-06-25 | 2011-06-23 | Heteroaryl compounds and compositions as protein kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147024689A Division KR20140117684A (ko) | 2010-06-25 | 2011-06-23 | 단백질 키나제 억제제로서의 헤테로아릴 화합물 및 조성물 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20130048293A true KR20130048293A (ko) | 2013-05-09 |
Family
ID=44280749
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020137001935A Abandoned KR20130048293A (ko) | 2010-06-25 | 2011-06-23 | 단백질 키나제 억제제로서의 헤테로아릴 화합물 및 조성물 |
| KR1020147024689A Withdrawn KR20140117684A (ko) | 2010-06-25 | 2011-06-23 | 단백질 키나제 억제제로서의 헤테로아릴 화합물 및 조성물 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147024689A Withdrawn KR20140117684A (ko) | 2010-06-25 | 2011-06-23 | 단백질 키나제 억제제로서의 헤테로아릴 화합물 및 조성물 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20130096149A1 (enExample) |
| EP (1) | EP2585454A1 (enExample) |
| JP (1) | JP2013529619A (enExample) |
| KR (2) | KR20130048293A (enExample) |
| CN (1) | CN103080107A (enExample) |
| AU (1) | AU2011268906A1 (enExample) |
| BR (1) | BR112012032884A2 (enExample) |
| CA (1) | CA2803055A1 (enExample) |
| EA (1) | EA201201676A1 (enExample) |
| MX (1) | MX2012015100A (enExample) |
| WO (1) | WO2011161216A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103403002B (zh) * | 2011-02-24 | 2016-06-22 | 内尔维阿诺医学科学有限公司 | 作为激酶抑制剂的噻唑基苯基-苯磺酰氨基衍生物 |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| WO2014172639A1 (en) * | 2013-04-19 | 2014-10-23 | Ruga Corporation | Raf kinase inhibitors |
| UY36294A (es) | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
| AU2017329090B9 (en) | 2016-09-19 | 2019-09-05 | Novartis Ag | Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor |
| US20190263796A1 (en) | 2016-09-23 | 2019-08-29 | Cellipse | Lim kinase inhibitors, pharmaceutical composition and method of use in limk-mediated diseases |
| CA3057969A1 (en) | 2017-05-02 | 2018-11-08 | Novartis Ag | Combination therapy |
| WO2020124397A1 (en) * | 2018-12-19 | 2020-06-25 | Inventisbio Shanghai Ltd. | C-terminal src kinase inhibitors |
| EP3969449B1 (en) | 2019-05-13 | 2025-02-12 | Novartis AG | New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer |
| EP4069692A1 (en) * | 2019-12-05 | 2022-10-12 | Institut National de la Santé et de la Recherche Médicale (INSERM) | N-(3-(5-(pyrimidin-4-yl)thiazol-4-yl)phenyl)sulfonamide compounds and their uses as braf inhibitors |
| CN111320548B (zh) * | 2020-04-24 | 2022-10-18 | 浦拉司科技（上海）有限责任公司 | 抗癌药物中间体2-氟-3-氨基苯甲酸甲酯的合成方法 |
| CN116724021A (zh) * | 2021-01-20 | 2023-09-08 | 巴斯夫欧洲公司 | 多氟化芳基和杂芳基羧酰胺的合成 |
| CN119053595A (zh) | 2022-03-28 | 2024-11-29 | 尼坎治疗公司 | 作为细胞周期蛋白依赖性激酶2抑制剂的磺酰氨基衍生物 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6391636B1 (en) | 1994-05-31 | 2002-05-21 | Isis Pharmaceuticals, Inc. | Antisense oligonucleotide modulation of raf gene expression |
| US6358932B1 (en) | 1994-05-31 | 2002-03-19 | Isis Pharmaceticals, Inc. | Antisense oligonucleotide inhibition of raf gene expression |
| US6037136A (en) | 1994-10-24 | 2000-03-14 | Cold Spring Harbor Laboratory | Interactions between RaF proto-oncogenes and CDC25 phosphatases, and uses related thereto |
| US5717100A (en) | 1995-10-06 | 1998-02-10 | Merck & Co., Inc. | Substituted imidazoles having anti-cancer and cytokine inhibitory activity |
| JP2000511419A (ja) | 1996-05-23 | 2000-09-05 | アプライド・リサーチ・システムズ・エイアールエス・ホールディング・ナムローゼ・フェンノートシャップ | Ｒａｆ―１または１４―３―３タンパク質のＩＬ―２受容体β鎖への結合を阻害する化合物およびそれを含有する医薬組成物 |
| AR012634A1 (es) | 1997-05-02 | 2000-11-08 | Sugen Inc | Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion |
| US6187799B1 (en) | 1997-05-23 | 2001-02-13 | Onyx Pharmaceuticals | Inhibition of raf kinase activity using aryl ureas |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| US6022884A (en) | 1997-11-07 | 2000-02-08 | Amgen Inc. | Substituted pyridine compounds and methods of use |
| US6204467B1 (en) | 1998-03-24 | 2001-03-20 | Ford Global Technologies, Inc. | Method and apparatus for resistive welding |
| ME00275B (me) | 1999-01-13 | 2011-02-10 | Bayer Corp | ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE |
| US6756410B2 (en) | 2000-08-30 | 2004-06-29 | Kamal D. Mehta | Induction of LDL receptor expression by extracellular-signal regulated kinase, ERK-1/2 |
| JP2003063993A (ja) * | 2001-06-11 | 2003-03-05 | Takeda Chem Ind Ltd | 医薬組成物 |
| KR100984595B1 (ko) | 2002-03-13 | 2010-09-30 | 어레이 바이오파마 인크. | Ｍｅｋ 억제제로서의 ｎ3 알킬화 벤즈이미다졸 유도체 |
| EP1799699A1 (en) | 2004-10-13 | 2007-06-27 | Wyeth | Analogs of 17-hydroxywortmannin as pi3k inhibitors |
| CA2599320A1 (en) | 2005-02-25 | 2006-08-31 | Kudos Pharmaceuticals Limited | Hydrazinomethyl, hydr zonomethyl and 5-membered heterocylic compounds which act as mtor inhibitors and their use as anti cancer agents |
| JP2008531538A (ja) | 2005-02-25 | 2008-08-14 | クドス ファーマシューティカルズ リミテッド | ２，４−ジアミノ−ピリドピリミジン誘導体とｍＴＯＲ阻害剤としてのその使用 |
| JP5161102B2 (ja) | 2005-11-22 | 2013-03-13 | クドス ファーマシューティカルズ リミテッド | ｍＴＯＲ阻害剤としてのピリドピリミジン、ピラゾピリミジンおよびピリミドピリミジン誘導体 |
| EP1979325A1 (en) | 2006-01-11 | 2008-10-15 | AstraZeneca AB | Morpholino pyrimidine derivatives and their use in therapy |
| CA2659851C (en) | 2006-08-23 | 2014-02-25 | Kudos Pharmaceuticals Limited | 2-methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors |
| WO2009012283A1 (en) * | 2007-07-17 | 2009-01-22 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2009076140A1 (en) * | 2007-12-13 | 2009-06-18 | Smithkline Beecham Corporation | Thiazole and oxazole kinase inhibitors |
| UA103319C2 (en) * | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| PT2324008E (pt) * | 2008-07-24 | 2012-06-25 | Nerviano Medical Sciences Srl | 3,4-diarilpirazoles como inibidores da proteína quinase |
| EP2498608A4 (en) * | 2009-11-10 | 2013-04-24 | Glaxosmithkline Llc | BENZOLSULFONAMIDE THIAZOL AND OXAZOLE COMPOUNDS |
-
2011
- 2011-06-23 JP JP2013515902A patent/JP2013529619A/ja active Pending
- 2011-06-23 CN CN201180040746XA patent/CN103080107A/zh active Pending
- 2011-06-23 MX MX2012015100A patent/MX2012015100A/es not_active Application Discontinuation
- 2011-06-23 BR BR112012032884A patent/BR112012032884A2/pt not_active IP Right Cessation
- 2011-06-23 AU AU2011268906A patent/AU2011268906A1/en not_active Abandoned
- 2011-06-23 CA CA2803055A patent/CA2803055A1/en not_active Abandoned
- 2011-06-23 EA EA201201676A patent/EA201201676A1/ru unknown
- 2011-06-23 US US13/805,793 patent/US20130096149A1/en not_active Abandoned
- 2011-06-23 KR KR1020137001935A patent/KR20130048293A/ko not_active Abandoned
- 2011-06-23 WO PCT/EP2011/060561 patent/WO2011161216A1/en not_active Ceased
- 2011-06-23 KR KR1020147024689A patent/KR20140117684A/ko not_active Withdrawn
- 2011-06-23 EP EP11728247.5A patent/EP2585454A1/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| CN103080107A (zh) | 2013-05-01 |
| JP2013529619A (ja) | 2013-07-22 |
| EP2585454A1 (en) | 2013-05-01 |
| MX2012015100A (es) | 2013-05-01 |
| EA201201676A1 (ru) | 2013-06-28 |
| BR112012032884A2 (pt) | 2016-11-08 |
| WO2011161216A1 (en) | 2011-12-29 |
| CA2803055A1 (en) | 2011-12-29 |
| US20130096149A1 (en) | 2013-04-18 |
| KR20140117684A (ko) | 2014-10-07 |
| AU2011268906A1 (en) | 2013-01-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A201 | Request for examination | ||
| PA0105 | International application |
Patent event date: 20130124 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20130124 Comment text: Request for Examination of Application |
|
| PG1501 | Laying open of application | ||
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 20140602 Patent event code: PE09021S01D |
|
| A107 | Divisional application of patent | ||
| PA0104 | Divisional application for international application |
Comment text: Divisional Application for International Patent Patent event code: PA01041R01D Patent event date: 20140902 |
|
| E701 | Decision to grant or registration of patent right | ||
| PE0701 | Decision of registration |
Patent event code: PE07011S01D Comment text: Decision to Grant Registration Patent event date: 20150102 |
|
| NORF | Unpaid initial registration fee | ||
| PC1904 | Unpaid initial registration fee |