JP2013512264A5 - - Google Patents
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- Publication number
- JP2013512264A5 JP2013512264A5 JP2012541336A JP2012541336A JP2013512264A5 JP 2013512264 A5 JP2013512264 A5 JP 2013512264A5 JP 2012541336 A JP2012541336 A JP 2012541336A JP 2012541336 A JP2012541336 A JP 2012541336A JP 2013512264 A5 JP2013512264 A5 JP 2013512264A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- halo
- group
- hydroxy
- 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 22
- 150000003839 salts Chemical class 0.000 claims description 6
- 239000000203 mixture Substances 0.000 claims description 5
- 239000012453 solvate Substances 0.000 claims description 5
- 238000000034 method Methods 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- -1 hydroxyl- Chemical group 0.000 claims 37
- 125000005843 halogen group Chemical group 0.000 claims 21
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 13
- 125000001424 substituent group Chemical group 0.000 claims 13
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 4
- 150000001204 N-oxides Chemical class 0.000 claims 3
- 238000005859 coupling reaction Methods 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 150000001502 aryl halides Chemical class 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- WTVXIBRMWGUIMI-UHFFFAOYSA-N trifluoro($l^{1}-oxidanylsulfonyl)methane Chemical group [O]S(=O)(=O)C(F)(F)F WTVXIBRMWGUIMI-UHFFFAOYSA-N 0.000 claims 1
- 230000017205 mitotic cell cycle checkpoint Effects 0.000 description 4
- 206010028980 Neoplasm Diseases 0.000 description 3
- 0 *c1c(*)c(*)c(*)[n]2nc(N*)nc12 Chemical compound *c1c(*)c(*)c(*)[n]2nc(N*)nc12 0.000 description 2
- 208000005623 Carcinogenesis Diseases 0.000 description 1
- 201000009030 Carcinoma Diseases 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 206010039491 Sarcoma Diseases 0.000 description 1
- 208000036878 aneuploidy Diseases 0.000 description 1
- 231100001075 aneuploidy Toxicity 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 230000036952 cancer formation Effects 0.000 description 1
- 231100000504 carcinogenesis Toxicity 0.000 description 1
- 230000022131 cell cycle Effects 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 230000002759 chromosomal effect Effects 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000006882 induction of apoptosis Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- 230000036210 malignancy Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 230000009038 pharmacological inhibition Effects 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 150000008523 triazolopyridines Chemical class 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09075535.6 | 2009-11-30 | ||
| EP09075535A EP2343297A1 (en) | 2009-11-30 | 2009-11-30 | Triazolopyridines |
| PCT/EP2010/006994 WO2011063908A1 (en) | 2009-11-30 | 2010-11-17 | Triazolopyridines |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013512264A JP2013512264A (ja) | 2013-04-11 |
| JP2013512264A5 true JP2013512264A5 (enExample) | 2013-12-26 |
| JP5805653B2 JP5805653B2 (ja) | 2015-11-04 |
Family
ID=42028156
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012541336A Expired - Fee Related JP5805653B2 (ja) | 2009-11-30 | 2010-11-17 | トリアゾロピリジン |
Country Status (36)
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| UY33452A (es) * | 2010-06-16 | 2012-01-31 | Bayer Schering Pharma Ag | Triazolopiridinas sustituidas |
| TWI541243B (zh) | 2010-09-10 | 2016-07-11 | 拜耳知識產權公司 | 經取代咪唑并嗒 |
| CN103429591A (zh) | 2010-12-17 | 2013-12-04 | 拜耳知识产权有限责任公司 | 在治疗过度增殖性病症中用作mps-1和tkk抑制剂的6-取代的咪唑并吡嗪 |
| CA2821829A1 (en) | 2010-12-17 | 2012-06-21 | Bayer Intellectual Property Gmbh | Imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| ES2544609T3 (es) | 2010-12-17 | 2015-09-02 | Bayer Intellectual Property Gmbh | Imidazopirazinas 2-sustituidas para uso como inhibidores de Mps-1 y TTK en el tratamiento de trastornos hiper-proliferativos |
| CA2821819A1 (en) | 2010-12-17 | 2012-06-21 | Marcus Koppitz | 6-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders |
| EP2651944B1 (en) | 2010-12-17 | 2015-09-23 | Bayer Intellectual Property GmbH | Substituted 6-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 |
| JP6001049B2 (ja) | 2011-03-31 | 2016-10-05 | 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 | Ｍｐｓ−１キナーゼ阻害剤としての置換ベンズイミダゾール類 |
| CA2832310A1 (en) | 2011-04-06 | 2012-10-11 | Bayer Intellectual Property Gmbh | Substituted imidazopyridines and intermediates thereof |
| US20140120087A1 (en) * | 2011-04-21 | 2014-05-01 | Bayer Intellectual Property Gmbh | Triazolopyridines |
| WO2012160029A1 (en) | 2011-05-23 | 2012-11-29 | Bayer Intellectual Property Gmbh | Substituted triazolopyridines |
| UA112096C2 (uk) * | 2011-12-12 | 2016-07-25 | Байєр Інтеллектуал Проперті Гмбх | Заміщені триазолопіридини та їх застосування як інгібіторів ttk |
| 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 |
| BR112015000308A2 (pt) | 2012-07-10 | 2017-06-27 | Bayer Pharma AG | método para preparo de triazolopiridinas substituídas |
| 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 |
| ES2634014T3 (es) | 2013-01-30 | 2017-09-26 | Bayer Pharma Aktiengesellschaft | Isotiazoles sustituidos con amino |
| AR096469A1 (es) * | 2013-06-06 | 2015-12-30 | Bayer Pharma AG | Composiciones farmacéuticas que comprenden compuestos del tipo triazolpiridinas |
| CA2914516A1 (en) * | 2013-06-07 | 2014-12-11 | Bayer Pharma Aktiengesellschaft | Substituted triazolopyridines |
| PE20160156A1 (es) | 2013-06-11 | 2016-04-20 | Bayer Pharma AG | Derivados de prodroga de triazolpiridinas sustituidas |
| EP3007692A1 (en) | 2013-06-11 | 2016-04-20 | Bayer Pharma Aktiengesellschaft | Combinations for the treatment of cancer comprising a mps-1 kinase inhibitor and a mitotic inhibitor |
| EP2980088A1 (en) | 2014-07-28 | 2016-02-03 | Bayer Pharma Aktiengesellschaft | Amino-substituted isothiazoles |
| DK3129374T3 (en) | 2014-04-07 | 2019-04-08 | Netherlands Translational Res Center B V | (5,6-dihydro) pyrimido [4,5-e] INDOLIZINER |
| EP2977375A1 (en) | 2014-07-25 | 2016-01-27 | Bayer Pharma Aktiengesellschaft | Amino-substituted isoxazoles |
| EP2977377A1 (en) | 2014-07-25 | 2016-01-27 | Bayer Pharma Aktiengesellschaft | Amino-substituted isoxazoles |
| EP2977376A1 (en) | 2014-07-25 | 2016-01-27 | Bayer Pharma Aktiengesellschaft | Amino-substituted isoxazoles |
| EP3283642B1 (en) | 2015-04-17 | 2023-10-11 | Netherlands Translational Research Center Holding B.V. | Prognostic biomarkers for ttk inhibitor chemotherapy |
| KR101686411B1 (ko) * | 2015-12-28 | 2016-12-14 | 한국원자력의학원 | 피리딘계 유도체를 포함하는 암 예방 또는 치료용 조성물 |
| CN107641118B (zh) * | 2016-07-22 | 2020-11-06 | 爱科诺生物医药股份有限公司 | 具有细胞坏死抑制活性的化合物及其组合物和应用 |
| EP3492500B1 (en) | 2017-12-01 | 2023-09-20 | Daikin Industries, Ltd. | Use of a crosslinked product of a fluorine-containing amorphous elastomer |
| EP3876939A4 (en) | 2018-11-07 | 2022-08-10 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| EP3876930A4 (en) | 2018-11-07 | 2022-07-20 | Dana-Farber Cancer Institute, Inc. | BENZIMIDAZOLE DERIVATIVES AND AZA-BENZIMIDAZOLE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF |
| WO2020097400A1 (en) | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Imidazopyridine derivatives and aza-imidazopyridine derivatives as janus kinase 2 inhibitors and uses thereof |
| BR112022022409A2 (pt) | 2020-05-06 | 2023-02-07 | Ajax Therapeutics Inc | 6-heteroarilóxi benzimidazóis e azabenzimidazóis como inibidores de jak2 |
| WO2022140527A1 (en) | 2020-12-23 | 2022-06-30 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| US20240123043A1 (en) * | 2021-02-22 | 2024-04-18 | Orgenesis Inc. | Pharmaceutical compositions comprising ranpirnase |
| WO2023086320A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of jak2 |
| CA3234638A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
Family Cites Families (22)
| 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 |
| US6514989B1 (en) | 2001-07-20 | 2003-02-04 | Hoffmann-La Roche Inc. | Aromatic and heteroaromatic substituted 1,2,4-triazolo pyridine derivatives |
| JP4499721B2 (ja) | 2003-06-30 | 2010-07-07 | ヒフ バイオ，インク． | 化合物、組成物および方法 |
| MX2007004179A (es) | 2004-10-07 | 2007-06-07 | Warner Lambert Co | Derivados de triazolpiridina como agentes antibacterianos. |
| WO2007065010A2 (en) | 2005-12-02 | 2007-06-07 | Hif Bio, Inc. | Anti-angiogenesis compounds |
| DE602007006010D1 (de) | 2006-05-31 | 2010-06-02 | Galapagos Nv | Triazolopyrazinverbindungen zur behandlung von degenerations- und entzündungskrankheiten |
| ES2549862T3 (es) | 2006-08-30 | 2015-11-02 | Cellzome Limited | Derivados de triazol como inhibidores de quinasa |
| EP2178868A1 (en) * | 2007-07-18 | 2010-04-28 | Novartis Ag | Bicyclic heteroaryl compounds and their use as kinase inhibitors |
| MX2010002115A (es) * | 2007-08-23 | 2010-06-01 | Aztrazeneca Ab | 2-anilinopurin-8-onas como inhibidores de ttk/mps1 para el tratamiento de trastornos .proliferativos. |
| MX2010002312A (es) * | 2007-08-31 | 2010-03-18 | Merck Serono Sa | Compuestos de triazolopiridina y su uso como inhibidores de cinasa reguladora de señal de apoptosis. |
| GB0719803D0 (en) | 2007-10-10 | 2007-11-21 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| EP2222674B8 (en) | 2007-11-27 | 2016-01-06 | Cellzome Limited | Amino triazoles as pi3k inhibitors |
| WO2010092015A1 (en) | 2009-02-10 | 2010-08-19 | Cellzome Limited | Urea triazololo [1, 5-a] pyridine derivatives as pi3k inhibitors |
| CN102317288A (zh) * | 2009-02-13 | 2012-01-11 | 佛维雅制药公司 | 作为激酶抑制剂的[1,2,4]三唑并[1,5-a]吡啶 |
| ES2547328T3 (es) | 2009-04-29 | 2015-10-05 | Bayer Intellectual Property Gmbh | Imidazoquinoxalinas sustituidas |
| JP5728683B2 (ja) | 2009-09-04 | 2015-06-03 | 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 | チロシンスレオニンキナーゼ阻害剤としての置換アミノキノキサリン |
| EP2343294A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Substituted triazolopyridines |
| EP2343295A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Triazolopyridine derivates |
| EP2343297A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Triazolopyridines |
| AU2011206635B2 (en) | 2010-01-15 | 2015-01-22 | Cellzome Limited | Novel substituted triazole derivatives as gamma secretase modulators |
| US20110190269A1 (en) | 2010-02-01 | 2011-08-04 | Karlheinz Baumann | Gamma secretase modulators |
-
2009
- 2009-11-30 EP EP09075535A patent/EP2343297A1/en not_active Withdrawn
-
2010
- 2010-11-17 RS RS20140646A patent/RS53670B1/sr unknown
- 2010-11-17 PE PE2012000742A patent/PE20121509A1/es not_active Application Discontinuation
- 2010-11-17 ES ES10787274.9T patent/ES2525069T3/es active Active
- 2010-11-17 JP JP2012541336A patent/JP5805653B2/ja not_active Expired - Fee Related
- 2010-11-17 CN CN201080061524.1A patent/CN102762557B/zh not_active Expired - Fee Related
- 2010-11-17 KR KR1020127016940A patent/KR20120115290A/ko not_active Ceased
- 2010-11-17 UA UAA201207609A patent/UA108486C2/uk unknown
- 2010-11-17 PL PL10787274T patent/PL2507235T3/pl unknown
- 2010-11-17 HR HRP20141093AT patent/HRP20141093T1/hr unknown
- 2010-11-17 MY MYPI2012002378A patent/MY160325A/en unknown
- 2010-11-17 SI SI201030810T patent/SI2507235T1/sl unknown
- 2010-11-17 MX MX2012006252A patent/MX2012006252A/es active IP Right Grant
- 2010-11-17 US US13/512,701 patent/US9676766B2/en not_active Expired - Fee Related
- 2010-11-17 PT PT107872749T patent/PT2507235E/pt unknown
- 2010-11-17 CU CU2012000084A patent/CU24100B1/es active IP Right Grant
- 2010-11-17 PH PH1/2012/501055A patent/PH12012501055A1/en unknown
- 2010-11-17 CA CA2781915A patent/CA2781915A1/en not_active Abandoned
- 2010-11-17 NZ NZ600229A patent/NZ600229A/en not_active IP Right Cessation
- 2010-11-17 BR BR112012012906A patent/BR112012012906A2/pt not_active IP Right Cessation
- 2010-11-17 EP EP10787274.9A patent/EP2507235B1/en active Active
- 2010-11-17 WO PCT/EP2010/006994 patent/WO2011063908A1/en not_active Ceased
- 2010-11-17 DK DK10787274.9T patent/DK2507235T3/en active
- 2010-11-17 EA EA201200794A patent/EA022353B1/ru not_active IP Right Cessation
- 2010-11-17 AU AU2010324155A patent/AU2010324155B2/en not_active Ceased
- 2010-11-30 AR ARP100104406A patent/AR079166A1/es unknown
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2012
- 2012-05-13 IL IL219750A patent/IL219750A/en not_active IP Right Cessation
- 2012-05-24 ZA ZA2012/03806A patent/ZA201203806B/en unknown
- 2012-05-25 TN TNP2012000265A patent/TN2012000265A1/en unknown
- 2012-05-28 MA MA34899A patent/MA33768B1/fr unknown
- 2012-05-30 EC ECSP12011935 patent/ECSP12011935A/es unknown
- 2012-05-30 DO DO2012000150A patent/DOP2012000150A/es unknown
- 2012-05-30 CL CL2012001391A patent/CL2012001391A1/es unknown
- 2012-05-30 CR CR20120295A patent/CR20120295A/es unknown
- 2012-05-30 HN HN2012001162A patent/HN2012001162A/es unknown
- 2012-05-30 GT GT201200165A patent/GT201200165A/es unknown
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2014
- 2014-11-21 CY CY20141100970T patent/CY1115866T1/el unknown