JP2013507453A5 - - Google Patents
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- Publication number
- JP2013507453A5 JP2013507453A5 JP2012534327A JP2012534327A JP2013507453A5 JP 2013507453 A5 JP2013507453 A5 JP 2013507453A5 JP 2012534327 A JP2012534327 A JP 2012534327A JP 2012534327 A JP2012534327 A JP 2012534327A JP 2013507453 A5 JP2013507453 A5 JP 2013507453A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- tautomer
- solvate
- 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.)
- Granted
Links
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 10
- 239000012453 solvate Substances 0.000 claims 9
- 241000124008 Mammalia Species 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 241000282412 Homo Species 0.000 claims 2
- JGLMVXWAHNTPRF-CMDGGOBGSA-N CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O Chemical compound CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O JGLMVXWAHNTPRF-CMDGGOBGSA-N 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 230000003463 hyperproliferative effect Effects 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 239000003471 mutagenic agent Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 238000003419 tautomerization reaction Methods 0.000 claims 1
- 102000043136 MAP kinase family Human genes 0.000 description 4
- 108091054455 MAP kinase family Proteins 0.000 description 4
- 229940124647 MEK inhibitor Drugs 0.000 description 4
- 239000003112 inhibitor Substances 0.000 description 3
- 108090000623 proteins and genes Proteins 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 102100031480 Dual specificity mitogen-activated protein kinase kinase 1 Human genes 0.000 description 2
- 101710146526 Dual specificity mitogen-activated protein kinase kinase 1 Proteins 0.000 description 2
- 102100023266 Dual specificity mitogen-activated protein kinase kinase 2 Human genes 0.000 description 2
- 101710146529 Dual specificity mitogen-activated protein kinase kinase 2 Proteins 0.000 description 2
- 102000001253 Protein Kinase Human genes 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 230000007170 pathology Effects 0.000 description 2
- 108060006633 protein kinase Proteins 0.000 description 2
- 102100024193 Mitogen-activated protein kinase 1 Human genes 0.000 description 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 230000003915 cell function Effects 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 230000014509 gene expression Effects 0.000 description 1
- 239000003102 growth factor Substances 0.000 description 1
- 239000003226 mitogen Substances 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 125000000341 threoninyl group Chemical group [H]OC([H])(C([H])([H])[H])C([H])(N([H])[H])C(*)=O 0.000 description 1
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2013507453A JP2013507453A (ja) | 2013-03-04 |
| JP2013507453A5 true JP2013507453A5 (https=) | 2013-11-28 |
| JP5892612B2 JP5892612B2 (ja) | 2016-03-23 |
Family
ID=43876849
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012534327A Active JP5892612B2 (ja) | 2009-10-13 | 2010-10-13 | 疾患の処置に有用な新規のｍｅｋ阻害剤 |
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 |
Family Cites Families (35)
| 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 |
| CA2473545A1 (en) | 2002-01-23 | 2003-07-31 | Warner-Lambert Company Llc | N-(4-substituted phenyl)-anthranilic acid hydroxamate esters |
| TWI361066B (en) | 2004-07-26 | 2012-04-01 | Chugai Pharmaceutical Co Ltd | 5-substituted-2-phenylamino benzamides as mek inhibitors |
| 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 |
| SI1912636T1 (sl) | 2005-07-21 | 2014-08-29 | Ardea Biosciences, Inc. | N-(arilamino)-sulfonamidni inhibitorji 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
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