JP2013545775A5 - - Google Patents
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- Publication number
- JP2013545775A5 JP2013545775A5 JP2013543703A JP2013543703A JP2013545775A5 JP 2013545775 A5 JP2013545775 A5 JP 2013545775A5 JP 2013543703 A JP2013543703 A JP 2013543703A JP 2013543703 A JP2013543703 A JP 2013543703A JP 2013545775 A5 JP2013545775 A5 JP 2013545775A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- halo
- group
- general formula
- 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
- 150000001875 compounds Chemical class 0.000 claims description 34
- 229910052799 carbon Inorganic materials 0.000 claims description 11
- 125000000524 functional group Chemical group 0.000 claims description 3
- 125000005843 halogen group Chemical group 0.000 claims 41
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 18
- 125000003118 aryl group Chemical group 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- 239000000203 mixture Substances 0.000 claims 9
- 150000001204 N-oxides Chemical class 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 230000001413 cellular effect Effects 0.000 claims 3
- 230000006806 disease prevention Effects 0.000 claims 3
- 230000028709 inflammatory response Effects 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 230000024932 T cell mediated immunity Effects 0.000 claims 2
- 150000001721 carbon Chemical group 0.000 claims 2
- 230000004663 cell proliferation Effects 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000002699 Digestive System Neoplasms Diseases 0.000 claims 1
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 claims 1
- 208000009849 Female Genital Neoplasms Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 206010059282 Metastases to central nervous system Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 206010029098 Neoplasm skin Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000011523 endocrine gland cancer Diseases 0.000 claims 1
- 208000037824 growth disorder Diseases 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 230000028993 immune response Effects 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000037841 lung tumor Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 208000037819 metastatic cancer Diseases 0.000 claims 1
- 208000011575 metastatic malignant neoplasm Diseases 0.000 claims 1
- KFHPWRRPBPUHBE-UHFFFAOYSA-N n-cyclopropyl-4-[8-[(2-hydroxy-2-methylpropyl)amino]-6-methylsulfanylimidazo[1,2-a]pyrazin-3-yl]-2-methylbenzamide Chemical compound C=1N=C2C(NCC(C)(C)O)=NC(SC)=CN2C=1C(C=C1C)=CC=C1C(=O)NC1CC1 KFHPWRRPBPUHBE-UHFFFAOYSA-N 0.000 claims 1
- GXVOCHPQFWSHPE-UHFFFAOYSA-N n-cyclopropyl-4-[8-[(2-hydroxy-2-methylpropyl)amino]-6-propylsulfanylimidazo[1,2-a]pyrazin-3-yl]-2-methylbenzamide Chemical compound C=1N=C2C(NCC(C)(C)O)=NC(SCCC)=CN2C=1C(C=C1C)=CC=C1C(=O)NC1CC1 GXVOCHPQFWSHPE-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 208000023958 prostate neoplasm Diseases 0.000 claims 1
- 201000004477 skin sarcoma Diseases 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 0 Cc(nc1S(C)(=O)=O)c(*)[n]2c1nc(*)c2* Chemical compound Cc(nc1S(C)(=O)=O)c(*)[n]2c1nc(*)c2* 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000008878 coupling Effects 0.000 description 1
- 238000010168 coupling process Methods 0.000 description 1
- 238000005859 coupling reaction Methods 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10195699 | 2010-12-17 | ||
| EP10195699.3 | 2010-12-17 | ||
| PCT/EP2011/072582 WO2012080228A1 (en) | 2010-12-17 | 2011-12-13 | 6-thio-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013545775A JP2013545775A (ja) | 2013-12-26 |
| JP2013545775A5 true JP2013545775A5 (enExample) | 2014-12-11 |
| JP5964853B2 JP5964853B2 (ja) | 2016-08-03 |
Family
ID=45349507
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013543703A Expired - Fee Related JP5964853B2 (ja) | 2010-12-17 | 2011-12-13 | 過増殖性障害の処置におけるｍｐｓ−１およびｔｋｋ阻害剤としての使用のための、６−チオ置換イミダゾピラジン類 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9212184B2 (enExample) |
| EP (1) | EP2651947B1 (enExample) |
| JP (1) | JP5964853B2 (enExample) |
| CN (1) | CN103403006B (enExample) |
| CA (1) | CA2821827A1 (enExample) |
| ES (1) | ES2530802T3 (enExample) |
| WO (1) | WO2012080228A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI541243B (zh) | 2010-09-10 | 2016-07-11 | 拜耳知識產權公司 | 經取代咪唑并嗒 |
| US20140135319A1 (en) * | 2010-12-17 | 2014-05-15 | Bayer Intellectual Property Gmbh | 6-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| WO2012080228A1 (en) * | 2010-12-17 | 2012-06-21 | Bayer Pharma Aktiengesellschaft | 6-thio-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| JP6166289B2 (ja) | 2012-03-14 | 2017-07-19 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 置換イミダゾピリダジン |
| WO2014020041A1 (en) | 2012-08-02 | 2014-02-06 | Bayer Pharma Aktiengesellschaft | Combinations for the treatment of cancer |
| WO2014020043A1 (en) | 2012-08-02 | 2014-02-06 | Bayer Pharma Aktiengesellschaft | Combinations for the treatment of cancer |
| EP3283642B1 (en) | 2015-04-17 | 2023-10-11 | Netherlands Translational Research Center Holding B.V. | Prognostic biomarkers for ttk inhibitor chemotherapy |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US5011472A (en) | 1988-09-06 | 1991-04-30 | Brown University Research Foundation | Implantable delivery system for biological factors |
| JP4799864B2 (ja) | 2002-09-23 | 2011-10-26 | シェーリング コーポレイション | サイクリン依存性キナーゼインヒビターとしてのイミダゾピラジン |
| US7186832B2 (en) | 2003-02-20 | 2007-03-06 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
| EP1945644A2 (en) | 2005-11-10 | 2008-07-23 | Schering Corporation | Imidazopyrazines as protein kinase inhibitors |
| JP2009539840A (ja) | 2006-06-06 | 2009-11-19 | シェーリング コーポレイション | プロテインキナーゼ阻害剤としてのイミダゾピラジン |
| PE20080931A1 (es) | 2006-11-08 | 2008-07-19 | Schering Corp | Imidazopirazinas como inhibidores de proteina quinasa |
| GB0716292D0 (en) | 2007-08-21 | 2007-09-26 | Biofocus Dpi Ltd | Imidazopyrazine compounds |
| EP2212326A1 (en) * | 2007-08-23 | 2010-08-04 | AstraZeneca AB | 2-anilinopurin-8-ones as inhibitors of ttk/mps1 for the treatment of proliferative disorders |
| JP6168773B2 (ja) * | 2009-04-29 | 2017-07-26 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 置換イミダゾキノキサリン |
| TW201107329A (en) | 2009-07-30 | 2011-03-01 | Oncotherapy Science Inc | Fused imidazole derivative having ttk inhibitory action |
| WO2011026579A1 (en) | 2009-09-04 | 2011-03-10 | Bayer Schering Pharma Aktiengesellschaft | Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors |
| EP2343295A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Triazolopyridine derivates |
| EP2343294A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Substituted triazolopyridines |
| EP2343297A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Triazolopyridines |
| CN103038235B (zh) * | 2010-06-01 | 2015-07-29 | 拜耳知识产权有限责任公司 | 取代的咪唑并吡嗪 |
| WO2012080228A1 (en) * | 2010-12-17 | 2012-06-21 | Bayer Pharma Aktiengesellschaft | 6-thio-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
-
2011
- 2011-12-13 WO PCT/EP2011/072582 patent/WO2012080228A1/en not_active Ceased
- 2011-12-13 ES ES11796994T patent/ES2530802T3/es active Active
- 2011-12-13 EP EP11796994.9A patent/EP2651947B1/en not_active Not-in-force
- 2011-12-13 US US13/995,055 patent/US9212184B2/en not_active Expired - Fee Related
- 2011-12-13 JP JP2013543703A patent/JP5964853B2/ja not_active Expired - Fee Related
- 2011-12-13 CN CN201180067336.4A patent/CN103403006B/zh not_active Expired - Fee Related
- 2011-12-13 CA CA2821827A patent/CA2821827A1/en not_active Abandoned
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