JP2007537295A5 - - Google Patents
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- JP2007537295A5 JP2007537295A5 JP2007513432A JP2007513432A JP2007537295A5 JP 2007537295 A5 JP2007537295 A5 JP 2007537295A5 JP 2007513432 A JP2007513432 A JP 2007513432A JP 2007513432 A JP2007513432 A JP 2007513432A JP 2007537295 A5 JP2007537295 A5 JP 2007537295A5
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- JP
- Japan
- Prior art keywords
- disorder
- compound
- aliphatic
- optionally substituted
- compound according
- 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.)
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Claims (11)
- 請求項1に記載の化合物であって、R1が、−ORまたは−C1〜3ハロアルキルで必要に応じて置換されるC1〜4脂肪族である、化合物。
- 請求項2に記載の化合物であって、R1が、−OH、−CHF2、−CH2F、または−CF3で必要に応じて置換されるC1〜4脂肪族である、化合物。
- 請求項3に記載の化合物であって、R1が、イソプロピル、2−ブチル、シクロプロピル、またはエチルであり、各部分が、−OH、または−CF3で必要に応じて置換される、化合物。
- 請求項1に記載の化合物であって、R2が、水素、C1〜3脂肪族、またはクロロである、化合物。
- 請求項1に記載の化合物であって、R3が、水素、メチル、またはクロロである、化合物。
- 請求項1に記載の化合物であって:
前記R1が、イソプロピルまたは2−ブチルであって、1つの−OHで必要に応じて置換され;
R2が、HまたはClであり;
mが、1であり;そして
R3が、Clまたはメチルである
化合物。 - 請求項1に記載の化合物、および薬学的に受容可能なキャリア、アジュバント、またはビヒクルを含む、組成物。
- 生物学的サンプル中のERK1プロテインキナーゼまたはERK2プロテインキナーゼ活性を阻害する方法であって、該方法が:
a)請求項9に記載の組成物;または
b)請求項1に記載の化合物
と該生物学的サンプルとを接触させる工程を包含する、方法。 - 増殖性障害、心臓障害、神経変性障害、自己免疫障害、臓器移植と関連付けられる状態、炎症性障害、免疫媒介性障害、または骨障害から選択される疾患、状態、または障害を処置するか、あるいはそれらから選択される疾患、状態、または障害の重篤度を軽減することを必要としている患者において、増殖性障害、心臓障害、神経変性障害、自己免疫障害、臓器移植と関連付けられる状態、炎症性障害、免疫媒介性障害、または骨障害から選択される疾患、状態、または障害を処置するか、あるいはそれらから選択される疾患、状態、または障害の重篤度を軽減するための組成物であって、請求項1に記載の化合物を含有する、組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US57130904P | 2004-05-14 | 2004-05-14 | |
US60/571,309 | 2004-05-14 | ||
PCT/US2005/016902 WO2005113541A1 (en) | 2004-05-14 | 2005-05-13 | Pyrrole compounds as inhibitors of erk protein kinase, synthesis thereof and intermediates thereto |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2007537295A JP2007537295A (ja) | 2007-12-20 |
JP2007537295A5 true JP2007537295A5 (ja) | 2008-06-26 |
JP5132305B2 JP5132305B2 (ja) | 2013-01-30 |
Family
ID=35106760
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2007513432A Active JP5132305B2 (ja) | 2004-05-14 | 2005-05-13 | Erkプロテインキナーゼのインヒビターとしてのピロール化合物、それらの合成、およびそれらの中間体 |
Country Status (26)
Country | Link |
---|---|
US (6) | US7354939B2 (ja) |
EP (5) | EP3305776B1 (ja) |
JP (1) | JP5132305B2 (ja) |
CN (1) | CN1976919A (ja) |
AR (2) | AR051735A1 (ja) |
AU (1) | AU2005245885B2 (ja) |
BR (1) | BRPI0511111A (ja) |
CA (1) | CA2566461C (ja) |
CY (1) | CY1122336T1 (ja) |
DK (1) | DK3305776T3 (ja) |
ES (4) | ES2751761T3 (ja) |
HK (2) | HK1203505A1 (ja) |
HU (1) | HUE047130T2 (ja) |
IL (1) | IL179207A0 (ja) |
LT (1) | LT3305776T (ja) |
MX (1) | MXPA06013209A (ja) |
NO (1) | NO20065727L (ja) |
NZ (1) | NZ551582A (ja) |
PL (1) | PL3305776T3 (ja) |
PT (1) | PT3305776T (ja) |
RU (1) | RU2376299C2 (ja) |
SI (1) | SI3305776T1 (ja) |
TW (1) | TW200607803A (ja) |
UA (1) | UA84930C2 (ja) |
WO (1) | WO2005113541A1 (ja) |
ZA (1) | ZA200609975B (ja) |
Families Citing this family (36)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP4808154B2 (ja) * | 2003-03-13 | 2011-11-02 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼインヒビターとして有用な組成物 |
WO2005100342A1 (en) * | 2004-03-26 | 2005-10-27 | Vertex Pharmaceuticals, Incorporated | Pyridine inhibitors of erk2 and uses thereof |
ES2751761T3 (es) * | 2004-05-14 | 2020-04-01 | Vertex Pharma | Compuestos de pirrol como inhibidores de proteínas cinasas ERK y composiciones farmacéuticas que contienen esos compuestos |
US8546404B2 (en) | 2005-12-13 | 2013-10-01 | Merck Sharp & Dohme | Compounds that are ERK inhibitors |
EP1984331B1 (en) | 2006-02-16 | 2010-10-20 | Schering Corporation | Pyrrolidine derivatives as erk inhibitors |
WO2008153858A1 (en) * | 2007-06-05 | 2008-12-18 | Schering Corporation | Polycyclic indazole derivatives and their use as erk inhibitors for the treatment of cancer |
WO2009105500A1 (en) | 2008-02-21 | 2009-08-27 | Schering Corporation | Compounds that are erk inhibitors |
CN102146074B (zh) * | 2011-01-26 | 2013-02-06 | 江苏先声药物研究有限公司 | 吡咯衍生物的制备方法及应用 |
WO2012172093A1 (en) | 2011-06-17 | 2012-12-20 | Merz Pharma Gmbh & Co. Kgaa | Dihydroindolizine derivate as metabotropic glutamate receptor modulators |
DK3058371T3 (da) | 2013-10-14 | 2021-08-02 | Univ Indiana Res & Tech Corp | Anvendelse af acamprosat til at modulere erk-1-2-aktivering i dyremodeller til fxs og asd og individer diagnosticeret med fxs og asd |
WO2015060368A1 (ja) | 2013-10-23 | 2015-04-30 | 武田薬品工業株式会社 | 複素環化合物 |
EP3082423A4 (en) | 2013-12-20 | 2017-09-20 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of cdk and erk inhibitors |
WO2015095833A1 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Treatment of hematologic cancers |
EP3984537B1 (en) | 2013-12-20 | 2024-03-20 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of type 2 mek and erk inhibitors |
EP4062917A1 (en) | 2013-12-20 | 2022-09-28 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of pi3k/akt pathway and erk inhibitors |
WO2015095842A2 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Methods and compositions for treating non-erk mapk pathway inhibitor-resistant cancers |
WO2015095835A1 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Methods of modulating radioiodine uptake for the treatment of radioiodine-refractory cancers |
CA3168002A1 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Cancer treatment using combinations of erk and raf inhibitors |
WO2015095831A1 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of mtor and erk inhibitors |
WO2015095838A2 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of mek type i and erk inhibitors |
WO2015095807A1 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of egfr and erk inhibitors |
NZ772411A (en) * | 2015-01-30 | 2022-05-27 | Vertex Pharma | Crystalline forms of c21h22ci2n4o2 |
ES2830044T3 (es) * | 2015-01-30 | 2021-06-02 | Biomed Valley Discoveries Inc | Malonato de C21H22C12N4O2 cristalino |
WO2016187028A1 (en) * | 2015-05-15 | 2016-11-24 | Celgene Avilomics Research, Inc. | Heteroaryl compounds, synthesis thereof, and intermediates thereto |
AU2015396809B2 (en) * | 2015-06-03 | 2019-07-11 | Js Innopharm (Shanghai) Ltd. | Heterocyclic compounds for treating psoriasis |
CN107849046B (zh) * | 2015-06-03 | 2020-06-12 | 常州捷凯医药科技有限公司 | 作为erk抑制剂的杂环化合物 |
AU2016341520C1 (en) | 2015-10-21 | 2021-07-22 | Otsuka Pharmaceutical Co., Ltd. | Benzolactam compounds as protein kinase inhibitors |
EP3170822A1 (en) | 2015-11-18 | 2017-05-24 | AGV Discovery | Azaindole derivatives and their use as erk kinase inhibitors |
BR112019005305A2 (pt) * | 2016-10-05 | 2019-07-02 | Zeno Royalties & Milestones Llc | compostos espirocíclicos |
GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
EP3694518A1 (en) * | 2017-10-12 | 2020-08-19 | Novartis AG | Combinations of mdm2 inhibitors with inhibitors of erk for treating cancers |
WO2019180141A1 (en) | 2018-03-23 | 2019-09-26 | Bayer Aktiengesellschaft | Combinations of rogaratinib |
WO2021020841A1 (en) * | 2019-07-29 | 2021-02-04 | Standigm Inc. | Composition for preventing or treating metabolic liver disease |
EP4212531A1 (en) | 2022-01-14 | 2023-07-19 | AGV Discovery | Azaindole derivatives and their use as erk kinase inhibitors |
WO2023169480A1 (zh) * | 2022-03-08 | 2023-09-14 | 甘李药业股份有限公司 | 氘代化合物,及其制备方法和应用 |
TW202400572A (zh) * | 2022-03-24 | 2024-01-01 | 美商生物醫學谷探索公司 | Erk的吡咯抑制劑之氘化類似物、其合成及其中間物 |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
US5716981A (en) | 1993-07-19 | 1998-02-10 | Angiogenesis Technologies, Inc. | Anti-angiogenic compositions and methods of use |
US5565413A (en) * | 1994-12-06 | 1996-10-15 | Zeneca Limited | Substituted pyridyl phenyl ketone herbicides |
US5472966A (en) * | 1995-03-29 | 1995-12-05 | Bristol-Myers Squibb Company | Antidepressant heteroarylaminoalkyl derivatives of naphthyl-monazines |
US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
WO2000078747A1 (fr) | 1999-06-22 | 2000-12-28 | Takeda Chemical Industries, Ltd. | Derives acylhydrazine, procede d'elaboration et utilisation |
MY130778A (en) | 2001-02-09 | 2007-07-31 | Vertex Pharma | Heterocyclic inhibitiors of erk2 and uses thereof |
AU2003237121A1 (en) * | 2002-04-26 | 2003-11-10 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
JP4570955B2 (ja) * | 2002-07-09 | 2010-10-27 | バーテクス ファーマスーティカルズ インコーポレイテッド | プロテインキナーゼ阻害活性を持つイミダゾール類 |
HUE029020T2 (en) * | 2002-07-18 | 2017-02-28 | Janssen Pharmaceutica Nv | Substituted triazine kinase inhibitors |
GB0217780D0 (en) * | 2002-07-31 | 2002-09-11 | Glaxo Group Ltd | Compounds |
US7304071B2 (en) * | 2002-08-14 | 2007-12-04 | Vertex Pharmaceuticals Incorporated | Protein kinase inhibitors and uses thereof |
JP4808154B2 (ja) * | 2003-03-13 | 2011-11-02 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼインヒビターとして有用な組成物 |
ES2751761T3 (es) * | 2004-05-14 | 2020-04-01 | Vertex Pharma | Compuestos de pirrol como inhibidores de proteínas cinasas ERK y composiciones farmacéuticas que contienen esos compuestos |
-
2005
- 2005-05-13 ES ES17184079T patent/ES2751761T3/es active Active
- 2005-05-13 EP EP17184079.6A patent/EP3305776B1/en active Active
- 2005-05-13 US US11/128,870 patent/US7354939B2/en not_active Ceased
- 2005-05-13 CA CA2566461A patent/CA2566461C/en active Active
- 2005-05-13 AR ARP050101987A patent/AR051735A1/es not_active Application Discontinuation
- 2005-05-13 BR BRPI0511111-0A patent/BRPI0511111A/pt not_active IP Right Cessation
- 2005-05-13 EP EP19199330.2A patent/EP3608315B1/en active Active
- 2005-05-13 DK DK17184079T patent/DK3305776T3/da active
- 2005-05-13 SI SI200532267T patent/SI3305776T1/sl unknown
- 2005-05-13 RU RU2006144445/04A patent/RU2376299C2/ru active
- 2005-05-13 UA UAA200613208A patent/UA84930C2/ru unknown
- 2005-05-13 ES ES19199330T patent/ES2897422T3/es active Active
- 2005-05-13 CN CNA200580021418XA patent/CN1976919A/zh active Pending
- 2005-05-13 EP EP05748073.3A patent/EP1753738B1/en active Active
- 2005-05-13 ZA ZA200609975A patent/ZA200609975B/en unknown
- 2005-05-13 ES ES05748073.3T patent/ES2513965T3/es active Active
- 2005-05-13 NZ NZ551582A patent/NZ551582A/en unknown
- 2005-05-13 AU AU2005245885A patent/AU2005245885B2/en active Active
- 2005-05-13 WO PCT/US2005/016902 patent/WO2005113541A1/en active Application Filing
- 2005-05-13 EP EP14163944.3A patent/EP2799434B1/en active Active
- 2005-05-13 ES ES14163944.3T patent/ES2651439T3/es active Active
- 2005-05-13 MX MXPA06013209A patent/MXPA06013209A/es active IP Right Grant
- 2005-05-13 PL PL17184079T patent/PL3305776T3/pl unknown
- 2005-05-13 HU HUE17184079A patent/HUE047130T2/hu unknown
- 2005-05-13 LT LTEP17184079.6T patent/LT3305776T/lt unknown
- 2005-05-13 TW TW094115644A patent/TW200607803A/zh unknown
- 2005-05-13 EP EP21190432.1A patent/EP3943489A1/en active Pending
- 2005-05-13 JP JP2007513432A patent/JP5132305B2/ja active Active
- 2005-05-13 PT PT171840796T patent/PT3305776T/pt unknown
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2006
- 2006-11-13 IL IL179207A patent/IL179207A0/en unknown
- 2006-12-12 NO NO20065727A patent/NO20065727L/no not_active Application Discontinuation
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2013
- 2013-08-23 US US14/544,396 patent/USRE46097E1/en active Active
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2015
- 2015-05-04 HK HK15104226.1A patent/HK1203505A1/xx unknown
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2016
- 2016-06-28 US US15/195,021 patent/USRE47318E1/en active Active
- 2016-11-18 AR ARP160103545A patent/AR106755A2/es active IP Right Grant
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2018
- 2018-05-15 HK HK18106295.9A patent/HK1247910A1/zh unknown
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2019
- 2019-03-25 US US16/363,905 patent/USRE48266E1/en active Active
- 2019-12-03 CY CY20191101265T patent/CY1122336T1/el unknown
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2020
- 2020-10-15 US US17/071,566 patent/USRE49500E1/en active Active
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2023
- 2023-02-22 US US18/173,004 patent/US20230183276A1/en active Pending
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