CN103080107A - 作为蛋白激酶抑制剂的杂芳基化合物和组合物 - Google Patents
作为蛋白激酶抑制剂的杂芳基化合物和组合物 Download PDFInfo
- Publication number
- CN103080107A CN103080107A CN201180040746XA CN201180040746A CN103080107A CN 103080107 A CN103080107 A CN 103080107A CN 201180040746X A CN201180040746X A CN 201180040746XA CN 201180040746 A CN201180040746 A CN 201180040746A CN 103080107 A CN103080107 A CN 103080107A
- Authority
- CN
- China
- Prior art keywords
- compound
- chloro
- pyrimidin
- phenyl
- mmol
- 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.)
- Pending
Links
- 0 C*C1=C(*)*(C2(CC3)C3CC2)C(*)=N1 Chemical compound C*C1=C(*)*(C2(CC3)C3CC2)C(*)=N1 0.000 description 5
- OADYQCGCQYXDHB-MCPKUPPWSA-N CC(C)(C)/C(/C)=N/C(/c1cc(Cl)cc(N)c1F)=C(/c1nc(SC)ncc1)\S Chemical compound CC(C)(C)/C(/C)=N/C(/c1cc(Cl)cc(N)c1F)=C(/c1nc(SC)ncc1)\S OADYQCGCQYXDHB-MCPKUPPWSA-N 0.000 description 1
- NDJDJAPJBPWWIV-UHFFFAOYSA-N CC(C)(C)c1nc(-c2cccc(NS(C)(=O)=O)c2F)c(-c2nc(Cl)ncc2)[s]1 Chemical compound CC(C)(C)c1nc(-c2cccc(NS(C)(=O)=O)c2F)c(-c2nc(Cl)ncc2)[s]1 NDJDJAPJBPWWIV-UHFFFAOYSA-N 0.000 description 1
- XUMYCALTFDDJTH-UHFFFAOYSA-N CCCS(Nc(cc(cc1-c2c(-c3nc(S(C)(=O)=O)ncc3)[o]c(C3CC3)n2)Cl)c1Cl)(=O)=O Chemical compound CCCS(Nc(cc(cc1-c2c(-c3nc(S(C)(=O)=O)ncc3)[o]c(C3CC3)n2)Cl)c1Cl)(=O)=O XUMYCALTFDDJTH-UHFFFAOYSA-N 0.000 description 1
- NSEBCIXPQANVCQ-UHFFFAOYSA-N CCCS(Nc(cccc1-c2c(-c3nc(C)ncc3)[s]c(C(C)(C)C)n2)c1F)(=O)=O Chemical compound CCCS(Nc(cccc1-c2c(-c3nc(C)ncc3)[s]c(C(C)(C)C)n2)c1F)(=O)=O NSEBCIXPQANVCQ-UHFFFAOYSA-N 0.000 description 1
- CKFJWHQKCHCNPN-UHFFFAOYSA-N CCCS(Nc(cccc1-c2c(-c3nc(C)ncc3)[s]c(C3CC3)n2)c1Cl)(=O)=O Chemical compound CCCS(Nc(cccc1-c2c(-c3nc(C)ncc3)[s]c(C3CC3)n2)c1Cl)(=O)=O CKFJWHQKCHCNPN-UHFFFAOYSA-N 0.000 description 1
- SFSXQTUBCMWHRJ-UHFFFAOYSA-N Cc1cc(C(C(c2ccnc(SC)n2)Br)=O)c(C)c(NS(C)(=O)=O)c1 Chemical compound Cc1cc(C(C(c2ccnc(SC)n2)Br)=O)c(C)c(NS(C)(=O)=O)c1 SFSXQTUBCMWHRJ-UHFFFAOYSA-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)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103080107A true CN103080107A (zh) | 2013-05-01 |
Family
ID=44280749
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180040746XA Pending CN103080107A (zh) | 2010-06-25 | 2011-06-23 | 作为蛋白激酶抑制剂的杂芳基化合物和组合物 |
Country Status (11)
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111320548A (zh) * | 2020-04-24 | 2020-06-23 | 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 |
| CN114746419A (zh) * | 2019-12-05 | 2022-07-12 | 国家医疗保健研究所 | N-(3-(5-(嘧啶-4-基)噻唑-4-基)苯基)磺酰胺化合物及其用作braf抑制剂的用途 |
| 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 |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9199979B2 (en) * | 2011-02-24 | 2015-12-01 | Nerviano Medical Sciences S.R.L. | Thiazolylphenyl-benzenesulfonamido derivatives as kinase inhibitors |
| 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 |
| CN109715163B (zh) | 2016-09-19 | 2022-11-22 | 诺华股份有限公司 | 包含raf抑制剂和erk抑制剂的治疗组合 |
| EP3515909A1 (en) | 2016-09-23 | 2019-07-31 | Cellipse | Lim kinase inhibitors, pharmaceutical composition and method of use in limk-mediated diseases |
| WO2018203219A1 (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 |
| EP4563150A3 (en) | 2019-05-13 | 2025-07-23 | 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 |
| KR20240167846A (ko) | 2022-03-28 | 2024-11-28 | 니캉 테라퓨틱스 인코포레이티드 | 사이클린 의존적 키나제 2 억제제로서의 설폰아미도 유도체 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009012283A1 (en) * | 2007-07-17 | 2009-01-22 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| US20090298815A1 (en) * | 2008-05-06 | 2009-12-03 | Jerry Leroy Adams | Benzene Sulfonamide Thiazole and Oxazole Compounds |
| WO2010010154A1 (en) * | 2008-07-24 | 2010-01-28 | Nerviano Medical Sciences S.R.L. | 3,4-diarylpyrazoles as protein kinase inhibitors |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| IL127210A0 (en) | 1996-05-23 | 1999-09-22 | Applied Research Systems | Compounds inhibiting the binding of raf-1 or 13-3-3 proteins to the beta-chain of il-2 pharmaceutical compositions containing them and their use |
| 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 |
| US7351834B1 (en) | 1999-01-13 | 2008-04-01 | Bayer Pharmaceuticals Corporation | ω-Carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| 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 |
| SG2013013339A (en) | 2002-03-13 | 2014-12-30 | Array Biopharma Inc | N3 alkylated benzimidazole derivatives as mek inhibitors |
| TW200626610A (en) | 2004-10-13 | 2006-08-01 | Wyeth Corp | Analogs of 17-hydroxywortmannin as PI3K inhibitors |
| MX2007010401A (es) | 2005-02-25 | 2008-02-19 | Kudos Pharm Ltd | Derivados de 2,4-diamino-piridopirimidina y su uso como inhbidores de mtor. |
| EP1877388A2 (en) | 2005-02-25 | 2008-01-16 | Kudos Pharmaceuticals Ltd | Hydrazinomethyl, hydrazonomethyl and 5-membered heterocylic compounds which act as mtor inhibitors and their use as anti cancer agents |
| KR101464384B1 (ko) | 2005-11-22 | 2014-11-21 | 쿠도스 파마슈티칼스 리미티드 | mTOR 억제제로서 피리도피리미딘, 피라조피리미딘 및피리미도피리미딘 유도체 |
| KR20080083188A (ko) | 2006-01-11 | 2008-09-16 | 아스트라제네카 아베 | 모르폴리노 피리미딘 유도체 및 요법에서의 그 유도체의용도 |
| JP5227321B2 (ja) | 2006-08-23 | 2013-07-03 | 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2−メチルモルホリンピリド−、ピラゾ−及びピリミド−ピリミジン誘導体 |
| JP2011506454A (ja) * | 2007-12-13 | 2011-03-03 | グラクソスミスクライン エルエルシー | チアゾールおよびオキサゾールキナーゼ阻害薬 |
| EP2498608A4 (en) * | 2009-11-10 | 2013-04-24 | Glaxosmithkline Llc | BENZOLSULFONAMIDE THIAZOL AND OXAZOLE COMPOUNDS |
-
2011
- 2011-06-23 BR BR112012032884A patent/BR112012032884A2/pt not_active IP Right Cessation
- 2011-06-23 CN CN201180040746XA patent/CN103080107A/zh active Pending
- 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 KR KR1020147024689A patent/KR20140117684A/ko not_active Withdrawn
- 2011-06-23 MX MX2012015100A patent/MX2012015100A/es not_active Application Discontinuation
- 2011-06-23 WO PCT/EP2011/060561 patent/WO2011161216A1/en not_active Ceased
- 2011-06-23 CA CA2803055A patent/CA2803055A1/en not_active Abandoned
- 2011-06-23 EA EA201201676A patent/EA201201676A1/ru unknown
- 2011-06-23 EP EP11728247.5A patent/EP2585454A1/en not_active Withdrawn
- 2011-06-23 AU AU2011268906A patent/AU2011268906A1/en not_active Abandoned
- 2011-06-23 JP JP2013515902A patent/JP2013529619A/ja active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009012283A1 (en) * | 2007-07-17 | 2009-01-22 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| US20090298815A1 (en) * | 2008-05-06 | 2009-12-03 | Jerry Leroy Adams | Benzene Sulfonamide Thiazole and Oxazole Compounds |
| WO2010010154A1 (en) * | 2008-07-24 | 2010-01-28 | Nerviano Medical Sciences S.R.L. | 3,4-diarylpyrazoles as protein kinase inhibitors |
Non-Patent Citations (1)
| Title |
|---|
| JAMES TSAI,等: "Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity", 《PNAS》, vol. 105, no. 8, 26 February 2008 (2008-02-26), XP008155384, DOI: doi:10.1073/pnas.0711741105 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114746419A (zh) * | 2019-12-05 | 2022-07-12 | 国家医疗保健研究所 | N-(3-(5-(嘧啶-4-基)噻唑-4-基)苯基)磺酰胺化合物及其用作braf抑制剂的用途 |
| CN114746419B (zh) * | 2019-12-05 | 2023-10-24 | 国家医疗保健研究所 | N-(3-(5-(嘧啶-4-基)噻唑-4-基)苯基)磺酰胺化合物及其用作braf抑制剂的用途 |
| CN111320548A (zh) * | 2020-04-24 | 2020-06-23 | 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 |
| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20130048293A (ko) | 2013-05-09 |
| MX2012015100A (es) | 2013-05-01 |
| BR112012032884A2 (pt) | 2016-11-08 |
| EP2585454A1 (en) | 2013-05-01 |
| WO2011161216A1 (en) | 2011-12-29 |
| JP2013529619A (ja) | 2013-07-22 |
| CA2803055A1 (en) | 2011-12-29 |
| EA201201676A1 (ru) | 2013-06-28 |
| AU2011268906A1 (en) | 2013-01-31 |
| US20130096149A1 (en) | 2013-04-18 |
| KR20140117684A (ko) | 2014-10-07 |
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| C53 | Correction of patent of invention or patent application | ||
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Address after: Basel Applicant after: Novartis Ag Address before: Basel Applicant before: Novartis AG |
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