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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- CN
- China
- Prior art keywords
- compound
- mmol
- compounds
- formula
- cancer
- Prior art date
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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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (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 (enExample) |
| EP (1) | EP2488507B1 (enExample) |
| JP (1) | JP5892612B2 (enExample) |
| KR (1) | KR20120094165A (enExample) |
| CN (1) | CN102666512B (enExample) |
| AU (1) | AU2010306830C1 (enExample) |
| BR (1) | BR112012008599A2 (enExample) |
| CA (1) | CA2814617C (enExample) |
| ES (1) | ES2534358T3 (enExample) |
| WO (1) | WO2011047055A2 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20190008859A1 (en) | 2015-08-21 | 2019-01-10 | Acerta Pharma B.V. | Therapeutic Combinations of a MEK Inhibitor and a BTK Inhibitor |
| AU2018319344B2 (en) | 2017-08-23 | 2024-04-04 | Cell Receptor AG | Combination of a MAPK/ERK pathway inhibitor and a glycosaminoglycan for the treatment of cancer |
| KR20210142154A (ko) | 2019-03-21 | 2021-11-24 | 옹쎄오 | 암 치료를 위한 키나제 억제제와 조합된 dbait 분자 |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム(インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル) | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CN117083265A (zh) * | 2020-12-16 | 2023-11-17 | 璧辰医药技术股份有限公司 | 激酶抑制剂及其用途 |
| JP2024521788A (ja) | 2021-05-27 | 2024-06-04 | ミラティ セラピューティクス, インコーポレイテッド | 併用療法 |
| 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 |
| WO2025147497A1 (en) | 2024-01-05 | 2025-07-10 | Pasithea Therapeutics Corp. | Solid forms comprising (5r,6s)-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, and compositions comprising and methods of using the same |
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 |
| DK0821671T3 (da) | 1995-04-20 | 2001-04-23 | Pfizer | Arylsulfonylhydroxamsyrederivater som MMP- og TNF-inhibitorer |
| DE69624081T2 (de) | 1995-12-20 | 2003-06-12 | Agouron Pharmaceuticals, Inc. | 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 |
| YU1899A (sh) | 1996-07-18 | 2000-03-21 | Pfizer Inc. | Inhibitori matričnih metaloproteaza na bazi fosfinata |
| EA199900139A1 (ru) | 1996-08-23 | 1999-08-26 | Пфайзер, Инк. | Производные арилсульфониламиногидроксамовой кислоты |
| AU5131998A (en) | 1997-01-06 | 1998-08-03 | Pfizer Inc. | Cyclic sulfone derivatives |
| US6303636B1 (en) | 1997-02-03 | 2001-10-16 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| AU5493598A (en) | 1997-02-07 | 1998-08-26 | Pfizer Inc. | N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases |
| CN1247531A (zh) | 1997-02-11 | 2000-03-15 | 辉瑞大药厂 | 芳基磺酰基异羟肟酸衍生物 |
| PL338633A1 (en) | 1997-08-08 | 2000-11-06 | Pfizer Prod Inc | Derivatives of aryloxyarylsuphonylamino hydroxamic acid |
| 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 |
| ATE260255T1 (de) | 1998-11-05 | 2004-03-15 | Pfizer Prod Inc | 5-oxo-pyrrolidine-2-carbonsäure- hydroxamidderivate |
| 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 |
| ES2481402T3 (es) * | 2005-07-21 | 2014-07-30 | Ardea Biosciences, Inc. | Inhibidores de N-(arilamino)sulfonamida de 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 |
| AU2007237901B2 (en) | 2006-04-18 | 2012-07-05 | Ardea Biosciences, Inc. | Pyridone sulfonamides and pyridone sulfamides as MEK inhibitors |
| MX2009007661A (es) | 2007-01-19 | 2009-12-14 | Ardea Biosciences Inc | Inhibidores de mek. |
| AU2008282338B2 (en) | 2007-07-30 | 2015-02-12 | Ardea Biosciences, Inc. | Derivatives of N-(arylamino) sulfonamides including polymorphs as inhibitors of MEK as well as compositions, methods of use and methods for preparing the same |
| EP2175885B1 (en) | 2007-07-30 | 2016-10-12 | Ardea Biosciences, Inc. | Combinations of mek inhibitors and raf kinase inhibitors and uses thereof |
| ES2380010T3 (es) | 2007-10-16 | 2012-05-07 | Pharmathen S.A. | Composición farmacéutica mejorada que contiene un anticonvulsivante derivado de la pirrolidona y método para su preparación |
| 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 |
| SG189784A1 (en) * | 2008-04-14 | 2013-05-31 | Ardea Biosciences Inc | Compositions and methods for preparing and using same |
| 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 US US13/501,442 patent/US9034861B2/en active Active
- 2010-10-13 JP JP2012534327A patent/JP5892612B2/ja active Active
- 2010-10-13 CA CA2814617A patent/CA2814617C/en active Active
- 2010-10-13 WO PCT/US2010/052514 patent/WO2011047055A2/en not_active Ceased
- 2010-10-13 BR BR112012008599A patent/BR112012008599A2/pt not_active IP Right Cessation
- 2010-10-13 KR KR1020127012271A patent/KR20120094165A/ko not_active Ceased
- 2010-10-13 ES ES10824026.8T patent/ES2534358T3/es active Active
- 2010-10-13 CN CN201080053278.5A patent/CN102666512B/zh active Active
- 2010-10-13 AU AU2010306830A patent/AU2010306830C1/en active Active
- 2010-10-13 EP EP10824026.8A patent/EP2488507B1/en active Active
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 |
|---|---|
| JP5892612B2 (ja) | 2016-03-23 |
| US20120208859A1 (en) | 2012-08-16 |
| AU2010306830B2 (en) | 2014-11-06 |
| CA2814617C (en) | 2017-12-19 |
| CA2814617A1 (en) | 2011-04-21 |
| CN102666512A (zh) | 2012-09-12 |
| EP2488507B1 (en) | 2014-12-17 |
| WO2011047055A8 (en) | 2012-05-24 |
| BR112012008599A2 (pt) | 2019-09-24 |
| AU2010306830A1 (en) | 2012-05-31 |
| EP2488507A2 (en) | 2012-08-22 |
| EP2488507A4 (en) | 2013-05-01 |
| KR20120094165A (ko) | 2012-08-23 |
| US9034861B2 (en) | 2015-05-19 |
| AU2010306830C1 (en) | 2015-05-28 |
| JP2013507453A (ja) | 2013-03-04 |
| WO2011047055A2 (en) | 2011-04-21 |
| ES2534358T3 (es) | 2015-04-21 |
| WO2011047055A3 (en) | 2011-08-18 |
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| Date | Code | Title | Description |
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| C06 | Publication | ||
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| REG | Reference to a national code |
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| C14 | Grant of patent or utility model | ||
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| C56 | Change in the name or address of the patentee |
Owner name: ALLOMEK THERAPEUTICS LLC Free format text: FORMER NAME: ALLOSTEM THERAPEUTICS LLC |
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| CP01 | Change in the name or title of a patent holder |
Address after: American Connecticut Patentee after: Errol Mike medical Inc. Address before: American Connecticut Patentee before: Allostem Therapeutics LLC |