JP5520831B2 - Pi3キナーゼの阻害薬 - Google Patents
Pi3キナーゼの阻害薬 Download PDFInfo
- Publication number
- JP5520831B2 JP5520831B2 JP2010539504A JP2010539504A JP5520831B2 JP 5520831 B2 JP5520831 B2 JP 5520831B2 JP 2010539504 A JP2010539504 A JP 2010539504A JP 2010539504 A JP2010539504 A JP 2010539504A JP 5520831 B2 JP5520831 B2 JP 5520831B2
- Authority
- JP
- Japan
- Prior art keywords
- pyridin
- imidazo
- acetamide
- pyridazin
- mmol
- 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.)
- Expired - Fee Related
Links
- 0 CC1*****1 Chemical compound CC1*****1 0.000 description 6
- DABNGBABBPZAIY-UHFFFAOYSA-N C=[S](c1cc(OC(F)F)ccc1)(Nc1cc(Br)cnc1Cl)(=O)=O Chemical compound C=[S](c1cc(OC(F)F)ccc1)(Nc1cc(Br)cnc1Cl)(=O)=O DABNGBABBPZAIY-UHFFFAOYSA-N 0.000 description 1
- IJNUKTNWXJMZIU-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CC=C1c1c(NC(C)=O)nc(cc2)[n]1nc2-c(cc1NS(c2cc(OC(F)F)ccc2)(=O)=O)cnc1Cl)=O Chemical compound CC(C)(C)OC(N(CC1)CC=C1c1c(NC(C)=O)nc(cc2)[n]1nc2-c(cc1NS(c2cc(OC(F)F)ccc2)(=O)=O)cnc1Cl)=O IJNUKTNWXJMZIU-UHFFFAOYSA-N 0.000 description 1
- KBFJYZWCROOHAH-UHFFFAOYSA-N CC(C)(C)c(cc1)ccc1S(Nc1cc(-c(cc2)n[n]3c2nc(NC(C)=O)c3)cnc1C#C)(=O)=O Chemical compound CC(C)(C)c(cc1)ccc1S(Nc1cc(-c(cc2)n[n]3c2nc(NC(C)=O)c3)cnc1C#C)(=O)=O KBFJYZWCROOHAH-UHFFFAOYSA-N 0.000 description 1
- BLJRCNSXJLQTSS-UHFFFAOYSA-N CC(C)(C)c(cc1)ccc1S(Nc1cc(-c(cc2)n[n]3c2nc(NC(C)=O)c3)cnc1C#N)(=O)=O Chemical compound CC(C)(C)c(cc1)ccc1S(Nc1cc(-c(cc2)n[n]3c2nc(NC(C)=O)c3)cnc1C#N)(=O)=O BLJRCNSXJLQTSS-UHFFFAOYSA-N 0.000 description 1
- MUWXXVHFJQHSBQ-UHFFFAOYSA-N CC(C)(c(cc1)ccc1S(Nc1cc(-c(cc2)n[n]3c2nc(NC(C)=O)c3)cnc1Cl)(=O)=O)O Chemical compound CC(C)(c(cc1)ccc1S(Nc1cc(-c(cc2)n[n]3c2nc(NC(C)=O)c3)cnc1Cl)(=O)=O)O MUWXXVHFJQHSBQ-UHFFFAOYSA-N 0.000 description 1
- RCOOXCLQIUIXJB-UHFFFAOYSA-N CC(Nc(nc(cc1)[n]2nc1-c(cc1NS(c3cc(OC(F)F)ccc3)(=O)=O)cnc1Cl)c2I)=O Chemical compound CC(Nc(nc(cc1)[n]2nc1-c(cc1NS(c3cc(OC(F)F)ccc3)(=O)=O)cnc1Cl)c2I)=O RCOOXCLQIUIXJB-UHFFFAOYSA-N 0.000 description 1
- GPMFRGLHEJIIDJ-UHFFFAOYSA-N CC(Nc(nc(cc1)[n]2nc1Cl)c2I)=O Chemical compound CC(Nc(nc(cc1)[n]2nc1Cl)c2I)=O GPMFRGLHEJIIDJ-UHFFFAOYSA-N 0.000 description 1
- HYAVDBLWDKUYEK-UHFFFAOYSA-N CC(Nc(nc1cc2)c[n]1nc2-c(cc1NS(c2ccc(C)cc2)(=O)=O)cnc1Cl)=O Chemical compound CC(Nc(nc1cc2)c[n]1nc2-c(cc1NS(c2ccc(C)cc2)(=O)=O)cnc1Cl)=O HYAVDBLWDKUYEK-UHFFFAOYSA-N 0.000 description 1
- GVQACZSEGZYBKO-UHFFFAOYSA-N CC(Nc(nc1cc2)c[n]1nc2-c(cc1OC)ccc1OC)=O Chemical compound CC(Nc(nc1cc2)c[n]1nc2-c(cc1OC)ccc1OC)=O GVQACZSEGZYBKO-UHFFFAOYSA-N 0.000 description 1
- WQJAPCZXLCHGEO-UHFFFAOYSA-N CC(Nc(nc1cc2)c[n]1nc2-c1cccc(NS(c2ccc(C)cc2)(=O)=O)c1)=O Chemical compound CC(Nc(nc1cc2)c[n]1nc2-c1cccc(NS(c2ccc(C)cc2)(=O)=O)c1)=O WQJAPCZXLCHGEO-UHFFFAOYSA-N 0.000 description 1
- MVJUDIWGLAFUEU-UHFFFAOYSA-N CC(Nc(nc1cc2)c[n]1nc2-c1ccnc(Sc(cccc2)c2F)c1)=O Chemical compound CC(Nc(nc1cc2)c[n]1nc2-c1ccnc(Sc(cccc2)c2F)c1)=O MVJUDIWGLAFUEU-UHFFFAOYSA-N 0.000 description 1
- FPJNXVCSICMXRJ-UHFFFAOYSA-N Nc(nc1cc2)c[n]1nc2-c(cc1NS(c(cc2)ccc2F)(=O)=O)cnc1Cl Chemical compound Nc(nc1cc2)c[n]1nc2-c(cc1NS(c(cc2)ccc2F)(=O)=O)cnc1Cl FPJNXVCSICMXRJ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US843007P | 2007-12-19 | 2007-12-19 | |
| US61/008,430 | 2007-12-19 | ||
| PCT/US2008/013940 WO2009085230A1 (en) | 2007-12-19 | 2008-12-18 | Inhibitors of pi3 kinase |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011507854A JP2011507854A (ja) | 2011-03-10 |
| JP2011507854A5 JP2011507854A5 (enExample) | 2014-04-17 |
| JP5520831B2 true JP5520831B2 (ja) | 2014-06-11 |
Family
ID=40364443
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010539504A Expired - Fee Related JP5520831B2 (ja) | 2007-12-19 | 2008-12-18 | Pi3キナーゼの阻害薬 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US7820665B2 (enExample) |
| EP (1) | EP2231661A1 (enExample) |
| JP (1) | JP5520831B2 (enExample) |
| AR (1) | AR069862A1 (enExample) |
| AU (1) | AU2008343813B2 (enExample) |
| CA (1) | CA2710194C (enExample) |
| CL (1) | CL2008003798A1 (enExample) |
| PE (1) | PE20091268A1 (enExample) |
| TW (1) | TW200940544A (enExample) |
| WO (1) | WO2009085230A1 (enExample) |
Families Citing this family (107)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US8431608B2 (en) | 2007-08-17 | 2013-04-30 | Icagen Inc. | Heterocycles as potassium channel modulators |
| CA2696631A1 (en) * | 2007-08-17 | 2009-02-26 | Icagen, Inc. | Heterocycles as potassium channel modulators |
| EP2234977A4 (en) | 2007-12-19 | 2011-04-13 | Boehringer Ingelheim Int | VIRAL POLYMERASE INHIBITORS |
| US20110105457A1 (en) * | 2008-04-18 | 2011-05-05 | Shionogi & Co., Ltd. | Heterocyclic compound having inhibitory activity on pi3k |
| WO2009133127A1 (en) * | 2008-04-30 | 2009-11-05 | Merck Serono S.A. | Fused bicyclic compounds and use thereof as pi3k inhibitors |
| JP5599783B2 (ja) * | 2008-05-30 | 2014-10-01 | アムジエン・インコーポレーテツド | Pi3キナーゼの阻害薬 |
| WO2010007099A1 (en) * | 2008-07-15 | 2010-01-21 | Cellzome Limited | 2-aminoimidazo[1,2-b]pyridazine derivatives as pi3k inhibitors |
| TWI378933B (en) | 2008-10-14 | 2012-12-11 | Daiichi Sankyo Co Ltd | Morpholinopurine derivatives |
| CA2755285C (en) | 2009-03-20 | 2014-02-11 | Yunxin Y. Bo | Inhibitors of pi3 kinase |
| CA2760778A1 (en) * | 2009-05-13 | 2010-11-18 | Amgen Inc. | Heteroaryl compounds as pikk inhibitors |
| ES2459468T3 (es) | 2009-05-15 | 2014-05-09 | Novartis Ag | Arilpiridinas como inhibidores de aldosterona sintasa |
| EP2448938B9 (en) | 2009-06-29 | 2015-06-10 | Incyte Corporation | Pyrimidinones as pi3k inhibitors |
| WO2011075643A1 (en) | 2009-12-18 | 2011-06-23 | Incyte Corporation | Substituted heteroaryl fused derivatives as pi3k inhibitors |
| CA2787714C (en) | 2010-01-22 | 2019-04-09 | Joaquin Pastor Fernandez | Inhibitors of pi3 kinase |
| EP2558463A1 (en) | 2010-04-14 | 2013-02-20 | Incyte Corporation | Fused derivatives as i3 inhibitors |
| US20130131057A1 (en) | 2010-05-13 | 2013-05-23 | Centro Nacional De Investigaciones Oncologicas (Cnio | New bicyclic compounds as pi3-k and mtor inhibitors |
| JO2998B1 (ar) | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
| US8440662B2 (en) | 2010-10-31 | 2013-05-14 | Endo Pharmaceuticals, Inc. | Substituted quinazoline and pyrido-pyrimidine derivatives |
| JP5961187B2 (ja) | 2010-12-20 | 2016-08-02 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Pi3k阻害剤としてのn−(1−(置換フェニル)エチル)−9h−プリン−6−アミン |
| CN103501610A (zh) * | 2011-03-09 | 2014-01-08 | 西建阿维拉米斯研究公司 | Pi3激酶抑制剂和其用途 |
| US9108984B2 (en) | 2011-03-14 | 2015-08-18 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors |
| US9126948B2 (en) | 2011-03-25 | 2015-09-08 | Incyte Holdings Corporation | Pyrimidine-4,6-diamine derivatives as PI3K inhibitors |
| WO2012174312A2 (en) * | 2011-06-15 | 2012-12-20 | Glaxosmithkline Llc | Benzimidazole derivatives as antiviral agents |
| MX389479B (es) | 2011-09-02 | 2025-03-20 | Incyte Holdings Corp | Heterociclilaminas como inhibidores de fosfoinositida 3-cinasas (pi3k) |
| MX352672B (es) | 2011-09-27 | 2017-12-04 | Amgen Inc | Compuestos heterocíclicos como inhibidores de mdm2 para el tratamiento del cáncer. |
| US10292390B2 (en) | 2011-11-04 | 2019-05-21 | Wisconsin Alumni Research Foundation | Inhibition and dispersion of bacterial biofilms with 2-aminobenzimidazole derivatives |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| TWI574962B (zh) * | 2012-11-14 | 2017-03-21 | 加拓科學公司 | 作爲pi3激酶調節劑的芳雜環化合物及其使用方法和用途 |
| EP2935272B1 (en) | 2012-12-21 | 2017-02-22 | Bristol-Myers Squibb Company | Pyrazole substituted imidazopyrazines as casein kinase 1 d/e inhibitors |
| JP6267231B2 (ja) | 2012-12-21 | 2018-01-24 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | カゼインキナーゼ1δ/ε阻害剤としての新規な置換イミダゾール |
| CN103965199B (zh) * | 2013-02-02 | 2017-07-07 | 广东东阳光药业有限公司 | 一种芳杂环化合物、包含它的药物组合物及其用途 |
| US20160002185A1 (en) | 2013-02-19 | 2016-01-07 | Amgen Inc. | Cis-morpholinone and other compounds as mdm2 inhibitors for the treatment of cancer |
| KR102148681B1 (ko) * | 2013-02-21 | 2020-08-27 | 칼리토르 사이언시즈, 엘엘씨 | Pi3 키나제 모듈레이터로서의 헤테로방향족 화합물 |
| WO2014151863A1 (en) | 2013-03-14 | 2014-09-25 | Amgen Inc. | Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer |
| WO2014145852A2 (en) | 2013-03-15 | 2014-09-18 | Knopp Biosciences Llc | Imidazo(4,5-b) pyridin-2-yl amides as kv7 channel activators |
| MA53572A1 (fr) | 2013-06-10 | 2021-10-29 | Amgen Inc | Procédés de production et formes cristallines d'un inhibiteur mdm2 |
| MY192088A (en) | 2013-11-11 | 2022-07-26 | Amgen Inc | Combinantion therapy including an mdm2 inhibitor and one or more additional pharmaceutically active agents for the treatment of cancers |
| GB201321734D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic Agents |
| WO2015108881A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| TN2016000270A1 (en) | 2014-01-14 | 2017-10-06 | Millennium Pharm Inc | Heteroaryls and uses thereof. |
| LT3105218T (lt) | 2014-02-13 | 2019-12-10 | Incyte Corp | Ciklopropilaminai kaip lsd1 inhibitoriai |
| EP3392244A1 (en) | 2014-02-13 | 2018-10-24 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| WO2015123424A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| WO2015134854A2 (en) * | 2014-03-06 | 2015-09-11 | Oyagen, Inc. | Small molecule vif dimerization antagonists as anti-hiv agents and for use as hiv/aids therapeutics |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
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| ES2749103T3 (es) | 2014-09-12 | 2020-03-19 | Knopp Biosciences Llc | Benzoimidazol-1,2-ilamidas como activadores del canal Kv7 |
| CN105503877A (zh) | 2014-09-24 | 2016-04-20 | 和记黄埔医药(上海)有限公司 | 咪唑并哒嗪类化合物及其用途 |
| CN104447756A (zh) * | 2014-11-10 | 2015-03-25 | 常州大学 | 一种五氟磺草胺中间体的制备方法 |
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| AU2016315881B2 (en) * | 2015-09-03 | 2019-09-19 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of DYRK1A and uses thereof |
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| UA127968C2 (uk) | 2017-05-22 | 2024-02-28 | Емджен Інк. | Інгібітори g12c kras і способи їх застосування |
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| CN111566103B (zh) * | 2017-10-30 | 2023-06-23 | 百时美施贵宝公司 | 作为激酶抑制剂的氨基咪唑并吡嗪 |
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| CN119118926A (zh) | 2018-03-19 | 2024-12-13 | 诺普生物科学有限责任公司 | Kv7通道激活剂组合物和使用方法 |
| EP3788037A1 (en) | 2018-05-01 | 2021-03-10 | Amgen Inc. | Substituted pyrimidinones as agonists of the apj receptor |
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| IL278889B2 (en) | 2018-06-01 | 2025-11-01 | Incyte Corp | Dosing regimen for the treatment of pi3k related disorders |
| AU2019284472B2 (en) | 2018-06-11 | 2024-05-30 | Amgen Inc. | KRAS G12C inhibitors for treating cancer |
| JP7369719B2 (ja) | 2018-06-12 | 2023-10-26 | アムジエン・インコーポレーテツド | KRas G12C阻害剤及びそれを使用する方法 |
| CN117304191A (zh) | 2018-07-05 | 2023-12-29 | 因赛特公司 | 作为a2a/a2b抑制剂的稠合吡嗪衍生物 |
| CA3110525A1 (en) | 2018-08-31 | 2020-03-05 | Amgen, Inc. | Processes for preparing a mdm2 inhibitor |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
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| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
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- 2008-12-19 AR ARP080105607A patent/AR069862A1/es not_active Application Discontinuation
- 2008-12-19 TW TW097149904A patent/TW200940544A/zh unknown
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| CA2710194C (en) | 2014-04-22 |
| CL2008003798A1 (es) | 2009-10-09 |
| AR069862A1 (es) | 2010-02-24 |
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