CN102666512B - 对疾病治疗有用的mek抑制剂 - Google Patents
对疾病治疗有用的mek抑制剂 Download PDFInfo
- Publication number
- CN102666512B CN102666512B CN201080053278.5A CN201080053278A CN102666512B CN 102666512 B CN102666512 B CN 102666512B CN 201080053278 A CN201080053278 A CN 201080053278A CN 102666512 B CN102666512 B CN 102666512B
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- China
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- compound
- mmol
- compounds
- formula
- cancer
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- 0 Fc1cc(I)ccc1Nc(c1c(cc2F)OCC=CCC3(CC3)*N1)c2F Chemical compound Fc1cc(I)ccc1Nc(c1c(cc2F)OCC=CCC3(CC3)*N1)c2F 0.000 description 3
- HTZBZCBRKDRXJX-UHFFFAOYSA-N C=CCOc(cc(c(F)c1Nc(c(F)c2)ccc2Br)F)c1N Chemical compound C=CCOc(cc(c(F)c1Nc(c(F)c2)ccc2Br)F)c1N HTZBZCBRKDRXJX-UHFFFAOYSA-N 0.000 description 1
- OWBKBKRLGJMUHN-UHFFFAOYSA-N C=[Br]c(cc1F)ccc1Nc(c(NS(C1(CC1)CC1O)(=O)=O)c(cc2F)OCC1O)c2F Chemical compound C=[Br]c(cc1F)ccc1Nc(c(NS(C1(CC1)CC1O)(=O)=O)c(cc2F)OCC1O)c2F OWBKBKRLGJMUHN-UHFFFAOYSA-N 0.000 description 1
- VLKHLGCNHVRXPC-UHFFFAOYSA-N CC1(CC(C(COc(c(NC)c2Nc(c(F)c3)ccc3I)cc(F)c2F)O)O)CC1 Chemical compound CC1(CC(C(COc(c(NC)c2Nc(c(F)c3)ccc3I)cc(F)c2F)O)O)CC1 VLKHLGCNHVRXPC-UHFFFAOYSA-N 0.000 description 1
- IRQGAAJKPKQZGE-UHFFFAOYSA-N CC1(CC(C(COc(cc(c(F)c2Nc(c(Cl)c3)ccc3I)F)c2NC)O)O)CC1 Chemical compound CC1(CC(C(COc(cc(c(F)c2Nc(c(Cl)c3)ccc3I)F)c2NC)O)O)CC1 IRQGAAJKPKQZGE-UHFFFAOYSA-N 0.000 description 1
- WQTCCBJRAQSTKR-UHFFFAOYSA-N COc(c(F)c1Nc(c(F)c2)ccc2[Br]=C)cc(F)c1[N+]([O-])=O Chemical compound COc(c(F)c1Nc(c(F)c2)ccc2[Br]=C)cc(F)c1[N+]([O-])=O WQTCCBJRAQSTKR-UHFFFAOYSA-N 0.000 description 1
- RJZKEDQKZPRSHT-UHFFFAOYSA-N Cc(cc1F)ccc1Nc(c(F)c(cc1F)OC)c1N Chemical compound Cc(cc1F)ccc1Nc(c(F)c(cc1F)OC)c1N RJZKEDQKZPRSHT-UHFFFAOYSA-N 0.000 description 1
- POOBBXSKIXNTCS-UHFFFAOYSA-N Cc(cc1F)ccc1Nc(c([N+]([O-])=O)c(cc1OC)F)c1F Chemical compound Cc(cc1F)ccc1Nc(c([N+]([O-])=O)c(cc1OC)F)c1F POOBBXSKIXNTCS-UHFFFAOYSA-N 0.000 description 1
- FENWEVRRFMFDBS-UHFFFAOYSA-N OC(CC1(CC1)S(Nc(c(Nc(ccc(I)c1)c1F)c(c(F)c1)F)c1OC1)(=O)=O)C1O Chemical compound OC(CC1(CC1)S(Nc(c(Nc(ccc(I)c1)c1F)c(c(F)c1)F)c1OC1)(=O)=O)C1O FENWEVRRFMFDBS-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D291/00—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms
- C07D291/08—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25093609P | 2009-10-13 | 2009-10-13 | |
| US61/250,936 | 2009-10-13 | ||
| PCT/US2010/052514 WO2011047055A2 (en) | 2009-10-13 | 2010-10-13 | Novel mek inhibitors, useful in the treatment of diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102666512A CN102666512A (zh) | 2012-09-12 |
| CN102666512B true CN102666512B (zh) | 2014-11-26 |
Family
ID=43876849
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080053278.5A Active CN102666512B (zh) | 2009-10-13 | 2010-10-13 | 对疾病治疗有用的mek抑制剂 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9034861B2 (https=) |
| EP (1) | EP2488507B1 (https=) |
| JP (1) | JP5892612B2 (https=) |
| KR (1) | KR20120094165A (https=) |
| CN (1) | CN102666512B (https=) |
| AU (1) | AU2010306830C1 (https=) |
| BR (1) | BR112012008599A2 (https=) |
| CA (1) | CA2814617C (https=) |
| ES (1) | ES2534358T3 (https=) |
| WO (1) | WO2011047055A2 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017033113A1 (en) | 2015-08-21 | 2017-03-02 | Acerta Pharma B.V. | Therapeutic combinations of a mek inhibitor and a btk inhibitor |
| US11559544B2 (en) | 2017-08-23 | 2023-01-24 | Cell Receptor AG | Combination of a MAPK/ERK pathway inhibitor and a glycosaminoglycan for the treatment of cancer |
| EA202192575A1 (ru) | 2019-03-21 | 2022-01-14 | Онксео | Соединения dbait в сочетании с ингибиторами киназ для лечения рака |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| AU2021401282A1 (en) * | 2020-12-16 | 2023-07-13 | Mosaica Medicines, Inc. | Kinase inhibitors and uses thereof |
| US12280055B2 (en) | 2021-05-27 | 2025-04-22 | Mirati Therapeutics, Inc. | Combination therapies |
| WO2025073765A1 (en) | 2023-10-03 | 2025-04-10 | Institut National de la Santé et de la Recherche Médicale | Methods of prognosis and treatment of patients suffering from melanoma |
| WO2025147503A1 (en) | 2024-01-05 | 2025-07-10 | Pasithea Therapeutics Corp. | 10,11-difluoro-12-((2-fluoro-4-iodophenyl)amino)-5,6-dihydroxy-4,5,6,7-tetrahydro-1h-spiro[benzo[b][1,5,4]oxathiazecine-3,1'-cyclopropane] 2,2-dioxide stereoisomers, and compositions comprising and methods of using the same |
| TW202542122A (zh) | 2024-01-05 | 2025-11-01 | 美商帕熙席亞醫療股份有限公司 | 包含(5r,6s)—10,11—二氟—12—((2—氟—4—碘苯基)—5,6—二羥基—4,5,6,7—四氫—111—螺[苯并[b][1,5,4]氧雜噻西啶—3,1'—環丙烷]2,2—二氧化物之固體形式以及包含其之組合物及使用其之方法 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003062191A1 (en) * | 2002-01-23 | 2003-07-31 | Warner-Lambert Company Llc | N-(4-substituted phenyl)-anthranilic acid hydroxamate esters |
| CN101124199A (zh) * | 2004-07-26 | 2008-02-13 | 中外制药株式会社 | 作为mek抑制物质的5-取代-2-苯基氨基-苯甲酰胺类 |
| CN101495118A (zh) * | 2005-07-21 | 2009-07-29 | 阿迪亚生命科学公司 | Mek的n-(芳基氨基)磺酰胺抑制剂 |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8827305D0 (en) | 1988-11-23 | 1988-12-29 | British Bio Technology | Compounds |
| US5455258A (en) | 1993-01-06 | 1995-10-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
| US5863949A (en) | 1995-03-08 | 1999-01-26 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| ES2153031T4 (es) | 1995-04-20 | 2001-05-16 | Pfizer | Derivados del acido arilsulfonil hidroxamico como inhibidores de mmp y tnf. |
| ATE225343T1 (de) | 1995-12-20 | 2002-10-15 | Hoffmann La Roche | Matrix-metalloprotease inhibitoren |
| EP0818442A3 (en) | 1996-07-12 | 1998-12-30 | Pfizer Inc. | Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor |
| KR20000067904A (ko) | 1996-07-18 | 2000-11-25 | 디. 제이. 우드, 스피겔 알렌 제이 | 매트릭스 메탈로프로테아제의 포스피네이트계 억제제 |
| KR20000068248A (ko) | 1996-08-23 | 2000-11-25 | 디. 제이. 우드, 스피겔 알렌 제이 | 아릴설포닐아미노 하이드록삼산 유도체 |
| JP3338064B2 (ja) | 1997-01-06 | 2002-10-28 | ファイザー・インク | 環状スルホン誘導体 |
| NZ336840A (en) | 1997-02-03 | 2001-01-26 | Pfizer Prod Inc | Arylsulfonylamino hydroxamic acid derivatives useful in the treatment of tumor necrosis factor and matrix metalloproteinase mediated diseases |
| JP2000507975A (ja) | 1997-02-07 | 2000-06-27 | ファイザー・インク | N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用 |
| EP0960098A1 (en) | 1997-02-11 | 1999-12-01 | Pfizer Inc. | Arylsulfonyl hydroxamic acid derivatives |
| CA2299355C (en) | 1997-08-08 | 2005-09-27 | Pfizer Products Inc. | Aryloxyarylsulfonylamino hydroxamic acid derivatives |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| GB9801690D0 (en) | 1998-01-27 | 1998-03-25 | Pfizer Ltd | Therapeutic agents |
| PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
| PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
| EP1004578B1 (en) | 1998-11-05 | 2004-02-25 | Pfizer Products Inc. | 5-oxo-pyrrolidine-2-carboxylic acid hydroxamide derivatives |
| GB9912961D0 (en) | 1999-06-03 | 1999-08-04 | Pfizer Ltd | Metalloprotease inhibitors |
| GB0131034D0 (en) * | 2001-12-28 | 2002-02-13 | Pharmacia & Upjohn Spa | Benzocyclodecane derivatives with antitumor activity |
| US7429667B2 (en) | 2005-01-20 | 2008-09-30 | Ardea Biosciences, Inc. | Phenylamino isothiazole carboxamidines as MEK inhibitors |
| CA2618218C (en) * | 2005-07-21 | 2015-06-30 | Ardea Biosciences, Inc. | N-(arylamino)-sulfonamide inhibitors of mek |
| US8101799B2 (en) | 2005-07-21 | 2012-01-24 | Ardea Biosciences | Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK |
| US7842836B2 (en) | 2006-04-11 | 2010-11-30 | Ardea Biosciences | N-aryl-N'alkyl sulfamides as MEK inhibitors |
| JP5269762B2 (ja) | 2006-04-18 | 2013-08-21 | アーディア・バイオサイエンシーズ・インコーポレイテッド | Mek阻害剤としてのピリドンスルホンアミドおよびピリドンスルファミド |
| KR20090111847A (ko) | 2007-01-19 | 2009-10-27 | 아디아 바이오사이언스즈 인크. | Mek 억제제 |
| EA032294B1 (ru) | 2007-07-30 | 2019-05-31 | Арди Байосайенсиз, Инк. | Способ получения полиморфной формы производного n-(ариламино)сульфонамида, фармацевтическая композиция, содержащая указанное производное, и способ лечения с помощью указанного производного |
| CA2924436A1 (en) | 2007-07-30 | 2009-02-05 | Ardea Biosciences, Inc. | Pharmaceutical combinations of n-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide as inhibitors of mek and methods of use |
| EP2197428B1 (en) | 2007-10-16 | 2012-01-25 | Pharmathen S.A. | Improved pharmaceutical composition containing a pyrrolidone anticonvulsant agent and method for the preparation thereof |
| US8044240B2 (en) | 2008-03-06 | 2011-10-25 | Ardea Biosciences Inc. | Polymorphic form of N-(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and uses thereof |
| MX2010011314A (es) | 2008-04-14 | 2010-11-12 | Ardea Biosciences Inc | Composiciones y metodos de preparacion y uso de las mismas. |
| CN102134218A (zh) | 2009-06-15 | 2011-07-27 | 凯美隆(北京)药业技术有限公司 | 6-芳氨基吡啶酮磺酰胺和6-芳氨基吡嗪酮磺酰胺mek抑制剂 |
-
2010
- 2010-10-13 CN CN201080053278.5A patent/CN102666512B/zh active Active
- 2010-10-13 CA CA2814617A patent/CA2814617C/en active Active
- 2010-10-13 BR BR112012008599A patent/BR112012008599A2/pt not_active IP Right Cessation
- 2010-10-13 AU AU2010306830A patent/AU2010306830C1/en active Active
- 2010-10-13 JP JP2012534327A patent/JP5892612B2/ja active Active
- 2010-10-13 EP EP10824026.8A patent/EP2488507B1/en active Active
- 2010-10-13 ES ES10824026.8T patent/ES2534358T3/es active Active
- 2010-10-13 KR KR1020127012271A patent/KR20120094165A/ko not_active Ceased
- 2010-10-13 US US13/501,442 patent/US9034861B2/en active Active
- 2010-10-13 WO PCT/US2010/052514 patent/WO2011047055A2/en not_active Ceased
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003062191A1 (en) * | 2002-01-23 | 2003-07-31 | Warner-Lambert Company Llc | N-(4-substituted phenyl)-anthranilic acid hydroxamate esters |
| CN101124199A (zh) * | 2004-07-26 | 2008-02-13 | 中外制药株式会社 | 作为mek抑制物质的5-取代-2-苯基氨基-苯甲酰胺类 |
| CN101495118A (zh) * | 2005-07-21 | 2009-07-29 | 阿迪亚生命科学公司 | Mek的n-(芳基氨基)磺酰胺抑制剂 |
Non-Patent Citations (3)
| Title |
|---|
| Advances in Targeting the Ras/Raf/MEK/Erk Mitogen-Activated Protein Kinase Cascade with MEK Inhibitors for Cancer Therapy;Bret B.Friday,等;《Clinical Cancer Research》;20080115;第14卷(第2期);第342-346页 * |
| MEK Inhibition Enhances Paclitaxel-induced Tumor Apoptosis;Jeffrey P.,等;《The Journal of Biological Chemistry》;20001018;第275卷(第50期);第38953-38956页 * |
| 结直肠癌中MEK2/ERK信号传导通路的研究;张辉,等;《中国普通外科杂志》;20040430;第13卷(第4期);第257-260页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20120208859A1 (en) | 2012-08-16 |
| US9034861B2 (en) | 2015-05-19 |
| CN102666512A (zh) | 2012-09-12 |
| WO2011047055A3 (en) | 2011-08-18 |
| EP2488507B1 (en) | 2014-12-17 |
| EP2488507A4 (en) | 2013-05-01 |
| AU2010306830A1 (en) | 2012-05-31 |
| CA2814617A1 (en) | 2011-04-21 |
| KR20120094165A (ko) | 2012-08-23 |
| BR112012008599A2 (pt) | 2019-09-24 |
| WO2011047055A2 (en) | 2011-04-21 |
| WO2011047055A8 (en) | 2012-05-24 |
| JP2013507453A (ja) | 2013-03-04 |
| ES2534358T3 (es) | 2015-04-21 |
| AU2010306830B2 (en) | 2014-11-06 |
| EP2488507A2 (en) | 2012-08-22 |
| CA2814617C (en) | 2017-12-19 |
| AU2010306830C1 (en) | 2015-05-28 |
| JP5892612B2 (ja) | 2016-03-23 |
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Owner name: ALLOMEK THERAPEUTICS LLC Free format text: FORMER NAME: ALLOSTEM THERAPEUTICS LLC |
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Address after: American Connecticut Patentee after: Errol Mike medical Inc. Address before: American Connecticut Patentee before: Allostem Therapeutics LLC |