CN102596937B - 作为蛋白激酶抑制剂的化合物和组合物 - Google Patents
作为蛋白激酶抑制剂的化合物和组合物 Download PDFInfo
- Publication number
- CN102596937B CN102596937B CN201080038235.XA CN201080038235A CN102596937B CN 102596937 B CN102596937 B CN 102596937B CN 201080038235 A CN201080038235 A CN 201080038235A CN 102596937 B CN102596937 B CN 102596937B
- Authority
- CN
- China
- Prior art keywords
- amino
- pyrimidine
- imidazoles
- phenyl
- cyclopropyl
- 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.)
- Active
Links
- 0 *C[C@@](*C(OC(*)(*)**)=*)N Chemical compound *C[C@@](*C(OC(*)(*)**)=*)N 0.000 description 10
- WFFDTMNHOINATE-UHFFFAOYSA-N CC1(C)OB(c(cc(cc2N)Cl)c2F)OC1(C)C Chemical compound CC1(C)OB(c(cc(cc2N)Cl)c2F)OC1(C)C WFFDTMNHOINATE-UHFFFAOYSA-N 0.000 description 1
- NTVVSBYQCPBGLK-UHFFFAOYSA-N CCCS(Nc1cc(F)cc(-c2c(-c3nc(NC)ncc3)[nH]c(C3CC3)n2)c1Cl)(=O)=O Chemical compound CCCS(Nc1cc(F)cc(-c2c(-c3nc(NC)ncc3)[nH]c(C3CC3)n2)c1Cl)(=O)=O NTVVSBYQCPBGLK-UHFFFAOYSA-N 0.000 description 1
- KPPGQWZCAXPGKF-HNNXBMFYSA-N C[C@@H](CNc1nc(-c2c(-c3cc(NS(C4CC4)(=O)=O)c(C)c(OC)c3)nc(C(C)(C)C)[nH]2)ccn1)NC(OC)=O Chemical compound C[C@@H](CNc1nc(-c2c(-c3cc(NS(C4CC4)(=O)=O)c(C)c(OC)c3)nc(C(C)(C)C)[nH]2)ccn1)NC(OC)=O KPPGQWZCAXPGKF-HNNXBMFYSA-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
- A61K31/495—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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (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)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Immunology (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 |
|---|---|---|---|
| US23808309P | 2009-08-28 | 2009-08-28 | |
| US61/238,083 | 2009-08-28 | ||
| US31306110P | 2010-03-11 | 2010-03-11 | |
| US61/313,061 | 2010-03-11 | ||
| PCT/EP2010/062495 WO2011023773A1 (en) | 2009-08-28 | 2010-08-26 | Compounds and compositions as protein kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102596937A CN102596937A (zh) | 2012-07-18 |
| CN102596937B true CN102596937B (zh) | 2014-02-12 |
Family
ID=42829939
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080038235.XA Active CN102596937B (zh) | 2009-08-28 | 2010-08-26 | 作为蛋白激酶抑制剂的化合物和组合物 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US8242260B2 (OSRAM) |
| EP (1) | EP2470528B1 (OSRAM) |
| JP (1) | JP5726190B2 (OSRAM) |
| KR (1) | KR101714107B1 (OSRAM) |
| CN (1) | CN102596937B (OSRAM) |
| AR (1) | AR077977A1 (OSRAM) |
| AU (1) | AU2010288455B2 (OSRAM) |
| BR (1) | BR112012004448A2 (OSRAM) |
| CA (1) | CA2771673C (OSRAM) |
| EA (1) | EA020479B1 (OSRAM) |
| ES (1) | ES2527176T3 (OSRAM) |
| IN (1) | IN2012DN00869A (OSRAM) |
| JO (1) | JO3007B1 (OSRAM) |
| MX (1) | MX2012002542A (OSRAM) |
| PL (1) | PL2470528T3 (OSRAM) |
| PT (1) | PT2470528E (OSRAM) |
| TW (1) | TWI487701B (OSRAM) |
| UY (1) | UY32859A (OSRAM) |
| WO (1) | WO2011023773A1 (OSRAM) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3002B1 (ar) | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
| MX360932B (es) | 2010-02-25 | 2018-11-21 | Dana Farber Cancer Inst Inc | Mutaciones del protooncogen de serina/treonina-proteina cinasa b-raf (braf) que confieren resistencia a los inhibidores del protooncogen de serina/treonina-proteina cinasa b-raf. |
| WO2013059634A1 (en) | 2011-10-20 | 2013-04-25 | The Regents Of The University Of California | Use of cdk9 inhibitors to reduce cartilage degradation |
| CA2855243C (en) | 2011-11-11 | 2020-04-14 | Novartis Ag | Method of treating a proliferative disease |
| RS58048B1 (sr) | 2011-11-23 | 2019-02-28 | Array Biopharma Inc | Farmaceutske formulacije |
| US9408885B2 (en) | 2011-12-01 | 2016-08-09 | Vib Vzw | Combinations of therapeutic agents for treating melanoma |
| US20150232452A1 (en) * | 2012-09-19 | 2015-08-20 | Ruga Corporation | Novel raf kinase inhibitors |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| CA2912568A1 (en) * | 2013-05-30 | 2014-12-04 | Plexxikon Inc. | Compounds for kinase modulation, and indications therefor |
| EP3013815B1 (en) | 2013-06-25 | 2017-05-03 | Bristol-Myers Squibb Company | Carbazole carboxamide compounds useful as kinase inhibitors |
| AR096721A1 (es) | 2013-06-25 | 2016-01-27 | Bristol Myers Squibb Co | Compuestos de tetrahidrocarbazol y carbazol carboxamida sustituidos |
| JP2017506618A (ja) * | 2013-08-28 | 2017-03-09 | メディベイション テクノロジーズ, インコーポレイテッド | 複素環式化合物および使用方法 |
| GB2517988A (en) * | 2013-09-09 | 2015-03-11 | Redx Pharma Ltd | Compounds |
| UY36294A (es) | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
| HK1243021A1 (zh) | 2014-10-14 | 2018-07-06 | The Regents Of The University Of California | 使用cdk9和brd4抑制剂来抑制炎症 |
| CN104402920B (zh) * | 2014-11-27 | 2018-04-03 | 河南科技学院 | 一种合成2‑卤代‑3‑频那醇硼酸酯‑5‑氯苯胺的方法 |
| ES2974991T3 (es) | 2016-09-19 | 2024-07-02 | Novartis Ag | Combinaciones terapéuticas que comprenden un inhibidor de RAF y un inhibidor de ERK |
| WO2018146253A1 (en) | 2017-02-10 | 2018-08-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway |
| AU2018262891B2 (en) | 2017-05-02 | 2021-04-01 | Novartis Ag | Combination therapy |
| WO2019133810A1 (en) | 2017-12-28 | 2019-07-04 | Tract Pharmaceuticals, Inc. | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
| WO2020124397A1 (en) * | 2018-12-19 | 2020-06-25 | Inventisbio Shanghai Ltd. | C-terminal src kinase inhibitors |
| AU2020276695A1 (en) | 2019-05-13 | 2021-12-23 | 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 |
| WO2022036176A1 (en) * | 2020-08-13 | 2022-02-17 | Albert Einstein College Of Medicine | N-cyclyl-sulfonamides useful for inhibiting raf |
| KR20240167846A (ko) | 2022-03-28 | 2024-11-28 | 니캉 테라퓨틱스 인코포레이티드 | 사이클린 의존적 키나제 2 억제제로서의 설폰아미도 유도체 |
| WO2023240024A1 (en) | 2022-06-08 | 2023-12-14 | Nikang Therapeutics, Inc. | Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors |
| WO2025072462A1 (en) | 2023-09-27 | 2025-04-03 | Nikang Therapeutics, Inc. | Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2659739A (en) | 1950-04-14 | 1953-11-17 | Eastman Kodak Co | 1-hydroxy-4-beta-cyanopropylamino-anthraquinone and process for preparing same |
| US6358932B1 (en) | 1994-05-31 | 2002-03-19 | Isis Pharmaceticals, Inc. | Antisense oligonucleotide inhibition of raf gene expression |
| US6391636B1 (en) | 1994-05-31 | 2002-05-21 | Isis Pharmaceuticals, Inc. | Antisense oligonucleotide modulation 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 |
| GB2306108A (en) * | 1995-10-13 | 1997-04-30 | Merck & Co Inc | Treatment of Raf-mediated cancers with imidazole derivatives |
| CA2256109A1 (en) | 1996-05-23 | 1997-11-27 | Applied Research Systems Ars Holding N.V. | Compounds that inhibit the binding of raf-1 or 14-3-3 proteins to the beta chain of il-2 receptor, and pharmaceutical compositions containing same |
| 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 |
| AU2001285349A1 (en) | 2000-08-30 | 2002-03-13 | The Board Of Trustees Of The University Of Arkansas | Induction of ldl receptor expression by extracellular-signal regulated kinase, erk-1/2 |
| DOP2003000613A (es) | 2002-03-13 | 2003-09-30 | Array Biopharma Inc | Derivados de bencimidazol n3 alquilado como inhibidores de mek (n3 alkylated benzimidazole derivatives as mek inhibitors) |
| US6644516B1 (en) | 2002-11-06 | 2003-11-11 | Continental Afa Dispensing Company | Foaming liquid dispenser |
| 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 |
| AU2006217742A1 (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 |
| 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 |
| BRPI0706395A2 (pt) | 2006-01-11 | 2011-03-22 | Astrazeneca Ab | composto, uso do mesmo, métodos para produzir um efeito anti-proliferativo em um animal de sangue quente e para tratar doença, composição farmacêutica, e, processo para preparar um composto |
| DK2057156T3 (en) | 2006-08-23 | 2017-05-08 | Kudos Pharm Ltd | 2-METHYLMORPHOLINPYRIDO, PYRAZO AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS |
| TW200922582A (en) | 2007-08-20 | 2009-06-01 | Organon Nv | N-benzyl, N'-arylcarbonylpiperazine derivatives |
| BRPI0908906A2 (pt) * | 2008-03-21 | 2019-09-24 | Novartis Ag | compostos heterocíclicos e usos dos mesmos |
| UA103319C2 (en) | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| CN102105459B (zh) * | 2008-07-24 | 2014-09-10 | 内尔维阿诺医学科学有限公司 | 作为蛋白激酶抑制剂的3,4-二芳基吡唑类 |
-
2010
- 2010-08-24 US US12/862,418 patent/US8242260B2/en not_active Expired - Fee Related
- 2010-08-26 MX MX2012002542A patent/MX2012002542A/es active IP Right Grant
- 2010-08-26 ES ES10745280.7T patent/ES2527176T3/es active Active
- 2010-08-26 IN IN869DEN2012 patent/IN2012DN00869A/en unknown
- 2010-08-26 PL PL10745280T patent/PL2470528T3/pl unknown
- 2010-08-26 PT PT107452807T patent/PT2470528E/pt unknown
- 2010-08-26 BR BR112012004448A patent/BR112012004448A2/pt not_active Application Discontinuation
- 2010-08-26 WO PCT/EP2010/062495 patent/WO2011023773A1/en active Application Filing
- 2010-08-26 EP EP10745280.7A patent/EP2470528B1/en active Active
- 2010-08-26 JP JP2012526067A patent/JP5726190B2/ja active Active
- 2010-08-26 CA CA2771673A patent/CA2771673C/en not_active Expired - Fee Related
- 2010-08-26 EA EA201200323A patent/EA020479B1/ru not_active IP Right Cessation
- 2010-08-26 AR ARP100103125A patent/AR077977A1/es unknown
- 2010-08-26 KR KR1020127007838A patent/KR101714107B1/ko not_active Expired - Fee Related
- 2010-08-26 CN CN201080038235.XA patent/CN102596937B/zh active Active
- 2010-08-26 AU AU2010288455A patent/AU2010288455B2/en not_active Ceased
- 2010-08-26 JO JOP/2010/0298A patent/JO3007B1/ar active
- 2010-08-27 TW TW099128938A patent/TWI487701B/zh not_active IP Right Cessation
- 2010-08-27 UY UY0001032859A patent/UY32859A/es not_active Application Discontinuation
-
2012
- 2012-05-16 US US13/473,230 patent/US8563553B2/en active Active
-
2013
- 2013-09-10 US US14/022,540 patent/US8859548B2/en active Active
Non-Patent Citations (2)
| Title |
|---|
| Dual binding site inhibitors of B-RAF kinase;Ronald L. Wolin, et al;《Bioorg. Med. Chem. Lett.》;20080404;第18卷;2825–2829 * |
| Ronald L. Wolin, et al.Dual binding site inhibitors of B-RAF kinase.《Bioorg. Med. Chem. Lett.》.2008,第18卷2825–2829. |
Also Published As
| Publication number | Publication date |
|---|---|
| US8859548B2 (en) | 2014-10-14 |
| KR20120092577A (ko) | 2012-08-21 |
| BR112012004448A2 (pt) | 2017-05-30 |
| JP5726190B2 (ja) | 2015-05-27 |
| US20110052578A1 (en) | 2011-03-03 |
| AU2010288455A1 (en) | 2012-02-23 |
| AU2010288455B2 (en) | 2013-01-31 |
| WO2011023773A1 (en) | 2011-03-03 |
| US20140011825A1 (en) | 2014-01-09 |
| PT2470528E (pt) | 2014-12-29 |
| AR077977A1 (es) | 2011-10-05 |
| US8242260B2 (en) | 2012-08-14 |
| MX2012002542A (es) | 2012-04-02 |
| CA2771673A1 (en) | 2011-03-03 |
| KR101714107B1 (ko) | 2017-03-08 |
| UY32859A (es) | 2011-03-31 |
| TWI487701B (zh) | 2015-06-11 |
| PL2470528T3 (pl) | 2015-03-31 |
| JO3007B1 (ar) | 2016-09-05 |
| CA2771673C (en) | 2016-07-12 |
| ES2527176T3 (es) | 2015-01-21 |
| EP2470528A1 (en) | 2012-07-04 |
| IN2012DN00869A (OSRAM) | 2015-07-10 |
| CN102596937A (zh) | 2012-07-18 |
| US8563553B2 (en) | 2013-10-22 |
| EA020479B1 (ru) | 2014-11-28 |
| TW201111365A (en) | 2011-04-01 |
| EA201200323A1 (ru) | 2012-09-28 |
| EP2470528B1 (en) | 2014-10-01 |
| US20120225899A1 (en) | 2012-09-06 |
| JP2013503139A (ja) | 2013-01-31 |
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