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) | EP2799434B1 (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) | ES2513965T3 (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 |
JP2007530595A (ja) * | 2004-03-26 | 2007-11-01 | 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 | Erk2のピリジンインヒビターおよびそれらの使用 |
EP2799434B1 (en) * | 2004-05-14 | 2017-08-02 | Vertex Pharmaceuticals Incorporated | Pyrrole compounds as inhibitors of ERK protein kinases and pharmaceutical compositions containing these compounds |
US8546404B2 (en) | 2005-12-13 | 2013-10-01 | Merck Sharp & Dohme | Compounds that are ERK inhibitors |
CA2642762A1 (en) * | 2006-02-16 | 2007-08-30 | Schering Corporation | Pyrrolidine derivatives as erk inhibitors |
EP2155722B1 (en) * | 2007-06-05 | 2013-08-14 | Merck Sharp & Dohme Corp. | Polycyclic indazole derivatives and their use as erk inhibitors for the treatment of cancer |
JP5276676B2 (ja) | 2008-02-21 | 2013-08-28 | メルク・シャープ・アンド・ドーム・コーポレーション | Erk阻害剤である化合物 |
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 |
PL3058371T3 (pl) | 2013-10-14 | 2021-11-08 | Indiana University Research And Technology Corporation | Zastosowanie akamprozatu do modulowania aktywacji erk 1-2 w modelach zwierzęcych dla fxs i asd oraz u osób z rozpoznaniem fxs i asd |
US20160264536A1 (en) | 2013-10-23 | 2016-09-15 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
WO2015095807A1 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of egfr and erk inhibitors |
WO2015095840A1 (en) | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of cdk and erk inhibitors |
WO2015095831A1 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Cancer treatments using combinations of mtor and erk inhibitors |
JP6678583B2 (ja) * | 2013-12-20 | 2020-04-22 | バイオメッド バレー ディスカバリーズ,インコーポレイティド | 2型mek阻害剤およびerk阻害剤の組み合わせを用いるがん処置 |
CA3168002A1 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Cancer treatment using combinations of erk and raf inhibitors |
WO2015095833A1 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Treatment of hematologic cancers |
WO2015095842A2 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Methods and compositions for treating non-erk mapk pathway inhibitor-resistant cancers |
ES2918375T3 (es) * | 2013-12-20 | 2022-07-15 | Biomed Valley Discoveries Inc | Tratamientos contra el cáncer usando combinaciones de inhibidores de la ruta de PI3K/Akt y ERK |
WO2015095835A1 (en) * | 2013-12-20 | 2015-06-25 | Biomed Valley Discoveries, Inc. | Methods of modulating radioiodine uptake for the treatment of radioiodine-refractory cancers |
JP2017502016A (ja) * | 2013-12-20 | 2017-01-19 | バイオメッド バレー ディスカバリーズ,インコーポレイティド | 1型mek阻害剤およびerk阻害剤の組み合わせを使用するがんの処置 |
US9670177B2 (en) | 2015-01-30 | 2017-06-06 | Biomed Valley Discoveries, Inc. | Crystalline C21H22Cl2N4O2 malonate |
CN116854662A (zh) * | 2015-01-30 | 2023-10-10 | 生物医学谷探索股份有限公司 | C21H22Cl2N4O2的晶型 |
WO2016187028A1 (en) * | 2015-05-15 | 2016-11-24 | Celgene Avilomics Research, Inc. | Heteroaryl compounds, synthesis thereof, and intermediates thereto |
WO2016192063A1 (en) * | 2015-06-03 | 2016-12-08 | Changzhou Jiekai Pharmatech Co. Ltd | Heterocyclic compounds as erk inhibitors |
CA2987963C (en) * | 2015-06-03 | 2023-01-24 | Js Innopharm (Shanghai) Ltd. | Heterocyclic compounds for treating psoriasis |
MX2018004643A (es) | 2015-10-21 | 2018-08-01 | Otsuka Pharma Co Ltd | Compuestos de benzolactama como inhibidores de la proteina cinasa. |
EP3170822A1 (en) | 2015-11-18 | 2017-05-24 | AGV Discovery | Azaindole derivatives and their use as erk kinase inhibitors |
WO2018067512A1 (en) | 2016-10-05 | 2018-04-12 | Kalyra Pharmaceuticals, Inc. | Spirocyclic compounds |
GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
WO2019073435A1 (en) * | 2017-10-12 | 2019-04-18 | Novartis Ag | COMBINATIONS OF MDM2 INHIBITORS WITH ERK INHIBITORS TO TREAT 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 |
WO2023183905A2 (en) * | 2022-03-24 | 2023-09-28 | Biomed Valley Discoveries, Inc. | Deuterated analogs of pyrrole inhibitors of erk, synthesis thereof and intermediates thereto |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
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US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
US5994341A (en) | 1993-07-19 | 1999-11-30 | Angiogenesis Technologies, Inc. | Anti-angiogenic Compositions and methods for the treatment of arthritis |
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 |
US6723722B1 (en) | 1999-06-22 | 2004-04-20 | Takeda Chemical Industries, Ltd. | Acylhydrazine derivatives, their production and use |
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 |
US7361665B2 (en) * | 2002-07-09 | 2008-04-22 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases |
DK2256108T3 (en) * | 2002-07-18 | 2016-04-11 | Janssen Pharmaceutica Nv | Substituted triazinkinaseinhibitorer |
GB0217780D0 (en) * | 2002-07-31 | 2002-09-11 | Glaxo Group Ltd | Compounds |
WO2004016597A2 (en) * | 2002-08-14 | 2004-02-26 | 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 |
EP2799434B1 (en) * | 2004-05-14 | 2017-08-02 | Vertex Pharmaceuticals Incorporated | Pyrrole compounds as inhibitors of ERK protein kinases and pharmaceutical compositions containing these compounds |
-
2005
- 2005-05-13 EP EP14163944.3A patent/EP2799434B1/en active Active
- 2005-05-13 NZ NZ551582A patent/NZ551582A/en unknown
- 2005-05-13 PT PT171840796T patent/PT3305776T/pt unknown
- 2005-05-13 CA CA2566461A patent/CA2566461C/en active Active
- 2005-05-13 PL PL17184079T patent/PL3305776T3/pl unknown
- 2005-05-13 ES ES05748073.3T patent/ES2513965T3/es active Active
- 2005-05-13 US US11/128,870 patent/US7354939B2/en not_active Ceased
- 2005-05-13 LT LTEP17184079.6T patent/LT3305776T/lt unknown
- 2005-05-13 HU HUE17184079A patent/HUE047130T2/hu unknown
- 2005-05-13 RU RU2006144445/04A patent/RU2376299C2/ru active
- 2005-05-13 TW TW094115644A patent/TW200607803A/zh unknown
- 2005-05-13 EP EP21190432.1A patent/EP3943489A1/en active Pending
- 2005-05-13 EP EP05748073.3A patent/EP1753738B1/en active Active
- 2005-05-13 ES ES14163944.3T patent/ES2651439T3/es active Active
- 2005-05-13 JP JP2007513432A patent/JP5132305B2/ja active Active
- 2005-05-13 AR ARP050101987A patent/AR051735A1/es not_active Application Discontinuation
- 2005-05-13 SI SI200532267T patent/SI3305776T1/sl unknown
- 2005-05-13 MX MXPA06013209A patent/MXPA06013209A/es active IP Right Grant
- 2005-05-13 CN CNA200580021418XA patent/CN1976919A/zh active Pending
- 2005-05-13 EP EP17184079.6A patent/EP3305776B1/en active Active
- 2005-05-13 ES ES19199330T patent/ES2897422T3/es active Active
- 2005-05-13 WO PCT/US2005/016902 patent/WO2005113541A1/en active Application Filing
- 2005-05-13 ES ES17184079T patent/ES2751761T3/es active Active
- 2005-05-13 ZA ZA200609975A patent/ZA200609975B/en unknown
- 2005-05-13 AU AU2005245885A patent/AU2005245885B2/en active Active
- 2005-05-13 EP EP19199330.2A patent/EP3608315B1/en active Active
- 2005-05-13 DK DK17184079T patent/DK3305776T3/da active
- 2005-05-13 BR BRPI0511111-0A patent/BRPI0511111A/pt not_active IP Right Cessation
- 2005-05-13 UA UAA200613208A patent/UA84930C2/ru unknown
-
2006
- 2006-11-13 IL IL179207A patent/IL179207A0/en unknown
- 2006-12-12 NO NO20065727A patent/NO20065727L/no not_active Application Discontinuation
-
2013
- 2013-08-23 US US14/544,396 patent/USRE46097E1/en active Active
-
2015
- 2015-05-04 HK HK15104226.1A patent/HK1203505A1/xx unknown
-
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
-
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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