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 (enExample) | 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 (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 |
|---|---|---|---|---|
| WO2017033113A1 (en) | 2015-08-21 | 2017-03-02 | Acerta Pharma B.V. | Therapeutic combinations of a mek inhibitor and a btk inhibitor |
| WO2019038367A1 (en) | 2017-08-23 | 2019-02-28 | Cell Receptor AG | ASSOCIATION OF A MAPK / ERK INHIBITOR AND A GLYCOSAMINOGLYCAN FOR THE TREATMENT OF CANCER |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたＤｂａｉｔ分子 |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| MX2023006434A (es) * | 2020-12-16 | 2023-06-13 | Abm Therapeutics Corp | Inhibidores de quinasa y usos de los mismos. |
| 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 |
| 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 |
| 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 |
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 |
| MX9708026A (es) | 1995-04-20 | 1997-11-29 | Pfizer | Derivados del acido arislfulfonil hidroxamico, composiciones que los contienen y uso de los mismos. |
| ES2183905T3 (es) | 1995-12-20 | 2003-04-01 | Hoffmann La Roche | Inhibidores de metaloproteasa de matriz. |
| 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 |
| IL127567A0 (en) | 1996-07-18 | 1999-10-28 | Pfizer | Phosphinate based inhibitors of matrix metalloproteases |
| JP2000501423A (ja) | 1996-08-23 | 2000-02-08 | ファイザー インク． | アリールスルホニルアミノヒドロキサム酸誘導体 |
| PT950059E (pt) | 1997-01-06 | 2004-10-29 | Pfizer | Derivados de sulfona ciclicos |
| ES2202796T3 (es) | 1997-02-03 | 2004-04-01 | Pfizer Products Inc. | Derivados de acidos arilsulfonilaminohidroxamicos. |
| EP0966438A1 (en) | 1997-02-07 | 1999-12-29 | Pfizer Inc. | N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases |
| CA2280151C (en) | 1997-02-11 | 2005-12-13 | Pfizer Inc. | Arylsulfonyl hydroxamic acid derivatives |
| EA002490B1 (ru) | 1997-08-08 | 2002-06-27 | Пфайзер Продактс Инк. | Производные арилоксиарилсульфониламиногидроксамовой кислоты |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| GB9801690D0 (en) | 1998-01-27 | 1998-03-25 | Pfizer Ltd | Therapeutic agents |
| PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
| PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
| DE69915004T2 (de) | 1998-11-05 | 2004-09-09 | Pfizer Products Inc., Groton | 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 |
| JP2005515253A (ja) | 2002-01-23 | 2005-05-26 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | Ｎ−（４−置換フェニル）−アントラニル酸ヒドロキサメートエステル |
| MY144232A (en) | 2004-07-26 | 2011-08-15 | 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 |
| WO2009018238A1 (en) | 2007-07-30 | 2009-02-05 | Ardea Biosciences, Inc. | Combinations of mek inhibitors and raf kinase inhibitors and uses thereof |
| CN101495118B (zh) | 2005-07-21 | 2012-09-05 | 阿迪亚生命科学公司 | Mek的n-(芳基氨基)磺酰胺抑制剂 |
| 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 |
| WO2007121269A2 (en) | 2006-04-11 | 2007-10-25 | Ardea Biosciences, Inc. | N-aryl-n'alkyl sulfamides as mek inhibitors |
| MX2008013097A (es) | 2006-04-18 | 2008-10-27 | Ardea Biosciences Inc | Piridona sulfonamidas y piridona sulfamidas como inhibidores de metiletilcetona. |
| EA200900959A1 (ru) | 2007-01-19 | 2010-02-26 | Арди Байосайенсиз, Инк. | Ингибиторы мек |
| CN101808516B (zh) | 2007-07-30 | 2013-08-28 | 阿迪生物科学公司 | 作为mek抑制剂的包括多晶型物的n-(芳氨基)磺酰胺衍生物和组合物、其使用方法和制备方法 |
| 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 |
| BRPI0911297A2 (pt) * | 2008-04-14 | 2019-09-24 | Ardea Biosciences Inc | composição e métodos para preparo e uso das mesmas |
| 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 CA CA2814617A patent/CA2814617C/en active Active
- 2010-10-13 KR KR1020127012271A patent/KR20120094165A/ko not_active Ceased
- 2010-10-13 EP EP10824026.8A patent/EP2488507B1/en active Active
- 2010-10-13 JP JP2012534327A patent/JP5892612B2/ja active Active
- 2010-10-13 BR BR112012008599A patent/BR112012008599A2/pt not_active IP Right Cessation
- 2010-10-13 WO PCT/US2010/052514 patent/WO2011047055A2/en not_active Ceased
- 2010-10-13 AU AU2010306830A patent/AU2010306830C1/en active Active
- 2010-10-13 US US13/501,442 patent/US9034861B2/en active Active
- 2010-10-13 CN CN201080053278.5A patent/CN102666512B/zh active Active
- 2010-10-13 ES ES10824026.8T patent/ES2534358T3/es active Active
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