JP2011529066A5 - - Google Patents
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- JP2011529066A5 JP2011529066A5 JP2011520175A JP2011520175A JP2011529066A5 JP 2011529066 A5 JP2011529066 A5 JP 2011529066A5 JP 2011520175 A JP2011520175 A JP 2011520175A JP 2011520175 A JP2011520175 A JP 2011520175A JP 2011529066 A5 JP2011529066 A5 JP 2011529066A5
- Authority
- JP
- Japan
- Prior art keywords
- independently
- optionally
- substituted
- ring
- pharmaceutically acceptable
- 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.)
- Withdrawn
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- 150000001875 compounds Chemical class 0.000 claims description 87
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 65
- 229910052736 halogen Inorganic materials 0.000 claims description 64
- 125000001931 aliphatic group Chemical group 0.000 claims description 62
- 150000003839 salts Chemical class 0.000 claims description 61
- 150000002367 halogens Chemical class 0.000 claims description 60
- 125000005842 heteroatom Chemical group 0.000 claims description 52
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 46
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 46
- 229910052757 nitrogen Inorganic materials 0.000 claims description 46
- 229910052760 oxygen Inorganic materials 0.000 claims description 46
- 239000001301 oxygen Chemical group 0.000 claims description 46
- 229910052717 sulfur Chemical group 0.000 claims description 46
- 239000011593 sulfur Chemical group 0.000 claims description 46
- 229920006395 saturated elastomer Polymers 0.000 claims description 43
- -1 pyridopyrazazinyl Chemical group 0.000 claims description 32
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 27
- 125000004076 pyridyl group Chemical group 0.000 claims description 26
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 24
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 24
- 125000004193 piperazinyl group Chemical group 0.000 claims description 20
- 125000003386 piperidinyl group Chemical group 0.000 claims description 20
- 230000001404 mediated effect Effects 0.000 claims description 19
- 125000005959 diazepanyl group Chemical group 0.000 claims description 18
- 125000002950 monocyclic group Chemical group 0.000 claims description 17
- 239000000203 mixture Substances 0.000 claims description 16
- 125000000217 alkyl group Chemical group 0.000 claims description 13
- 208000023275 Autoimmune disease Diseases 0.000 claims description 12
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 11
- NFDXQGNDWIPXQL-UHFFFAOYSA-N 1-cyclooctyldiazocane Chemical group C1CCCCCCC1N1NCCCCCC1 NFDXQGNDWIPXQL-UHFFFAOYSA-N 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 125000002393 azetidinyl group Chemical group 0.000 claims description 8
- 125000002619 bicyclic group Chemical group 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 8
- 125000006574 non-aromatic ring group Chemical group 0.000 claims description 8
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 8
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 8
- 125000004429 atom Chemical group 0.000 claims description 6
- 125000003725 azepanyl group Chemical group 0.000 claims description 6
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 125000002632 imidazolidinyl group Chemical group 0.000 claims description 6
- 125000001041 indolyl group Chemical group 0.000 claims description 6
- 125000002757 morpholinyl group Chemical group 0.000 claims description 6
- 201000006417 multiple sclerosis Diseases 0.000 claims description 6
- 125000005961 oxazepanyl group Chemical group 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 6
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 6
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 6
- LLSRLLPHUVVLQJ-UHFFFAOYSA-N 1-cycloheptyldiazepane Chemical group C1CCCCCC1N1NCCCCC1 LLSRLLPHUVVLQJ-UHFFFAOYSA-N 0.000 claims description 4
- 102000001253 Protein Kinase Human genes 0.000 claims description 4
- 102000003923 Protein Kinase C Human genes 0.000 claims description 4
- 208000000389 T-cell leukemia Diseases 0.000 claims description 4
- 208000028530 T-cell lymphoblastic leukemia/lymphoma Diseases 0.000 claims description 4
- 206010042971 T-cell lymphoma Diseases 0.000 claims description 4
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims description 4
- 206010003246 arthritis Diseases 0.000 claims description 4
- 125000004925 dihydropyridyl group Chemical group N1(CC=CC=C1)* 0.000 claims description 4
- 125000001188 haloalkyl group Chemical group 0.000 claims description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 4
- 125000005956 isoquinolyl group Chemical group 0.000 claims description 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 4
- 125000002971 oxazolyl group Chemical group 0.000 claims description 4
- 108060006633 protein kinase Proteins 0.000 claims description 4
- 125000006085 pyrrolopyridyl group Chemical group 0.000 claims description 4
- 125000005942 tetrahydropyridyl group Chemical group 0.000 claims description 4
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 125000005412 pyrazyl group Chemical group 0.000 claims description 3
- FLUVVESHOANMOG-UHFFFAOYSA-N 1-cyclodecyldiazecane Chemical group C1CCCCCCCCC1N1NCCCCCCCC1 FLUVVESHOANMOG-UHFFFAOYSA-N 0.000 claims description 2
- JWGMXWNVAYWSNI-UHFFFAOYSA-N 1-cyclohexyldiazinane Chemical group C1CCCCC1N1NCCCC1 JWGMXWNVAYWSNI-UHFFFAOYSA-N 0.000 claims description 2
- PPNCOQHHSGMKGI-UHFFFAOYSA-N 1-cyclononyldiazonane Chemical group C1CCCCCCCC1N1NCCCCCCC1 PPNCOQHHSGMKGI-UHFFFAOYSA-N 0.000 claims description 2
- WJWNYPADNFOIPT-UHFFFAOYSA-N 5-cycloheptyl-1,4-diazepane Chemical group C1CCCCCC1C1NCCNCC1 WJWNYPADNFOIPT-UHFFFAOYSA-N 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 206010052779 Transplant rejections Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- ARUKYTASOALXFG-UHFFFAOYSA-N cycloheptylcycloheptane Chemical group C1CCCCCC1C1CCCCCC1 ARUKYTASOALXFG-UHFFFAOYSA-N 0.000 claims description 2
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 125000005047 dihydroimidazolyl group Chemical group N1(CNC=C1)* 0.000 claims description 2
- 125000005051 dihydropyrazinyl group Chemical group N1(CC=NC=C1)* 0.000 claims description 2
- 125000005052 dihydropyrazolyl group Chemical group N1(NCC=C1)* 0.000 claims description 2
- 125000005053 dihydropyrimidinyl group Chemical group N1(CN=CC=C1)* 0.000 claims description 2
- 125000005054 dihydropyrrolyl group Chemical group [H]C1=C([H])C([H])([H])C([H])([H])N1* 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000003463 hyperproliferative effect Effects 0.000 claims description 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims description 2
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims description 2
- 125000004628 isothiazolidinyl group Chemical group S1N(CCC1)* 0.000 claims description 2
- 125000003965 isoxazolidinyl group Chemical group 0.000 claims description 2
- 208000018937 joint inflammation Diseases 0.000 claims description 2
- 206010025135 lupus erythematosus Diseases 0.000 claims description 2
- TVMXDCGIABBOFY-UHFFFAOYSA-N octane Chemical compound CCCCCCCC TVMXDCGIABBOFY-UHFFFAOYSA-N 0.000 claims description 2
- 125000000160 oxazolidinyl group Chemical group 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims description 2
- 125000004590 pyridopyridyl group Chemical group N1=C(C=CC2=C1C=CC=N2)* 0.000 claims description 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000005493 quinolyl group Chemical group 0.000 claims description 2
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 2
- 125000001984 thiazolidinyl group Chemical group 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 description 12
- 0 C*(C)C1CCNCC1 Chemical compound C*(C)C1CCNCC1 0.000 description 2
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- KXIXHISTUVHOCY-UHFFFAOYSA-N CC(C)N1CCCCC1 Chemical compound CC(C)N1CCCCC1 KXIXHISTUVHOCY-UHFFFAOYSA-N 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8291908P | 2008-07-23 | 2008-07-23 | |
| US61/082,919 | 2008-07-23 | ||
| US11603208P | 2008-11-19 | 2008-11-19 | |
| US61/116,032 | 2008-11-19 | ||
| US14010008P | 2008-12-23 | 2008-12-23 | |
| US61/140,100 | 2008-12-23 | ||
| US16315209P | 2009-03-25 | 2009-03-25 | |
| US61/163,152 | 2009-03-25 | ||
| PCT/US2009/051437 WO2010011772A2 (en) | 2008-07-23 | 2009-07-22 | Tri-cyclic pyrazolopyridine kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014163360A Division JP5931976B2 (ja) | 2008-07-23 | 2014-08-11 | 三環式ピラゾロピリジンキナーゼ阻害剤 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011529066A JP2011529066A (ja) | 2011-12-01 |
| JP2011529066A5 true JP2011529066A5 (https=) | 2012-08-16 |
Family
ID=41137604
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011520175A Withdrawn JP2011529066A (ja) | 2008-07-23 | 2009-07-22 | 三環式ピラゾロピリジンキナーゼ阻害剤 |
| JP2014163360A Active JP5931976B2 (ja) | 2008-07-23 | 2014-08-11 | 三環式ピラゾロピリジンキナーゼ阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014163360A Active JP5931976B2 (ja) | 2008-07-23 | 2014-08-11 | 三環式ピラゾロピリジンキナーゼ阻害剤 |
Country Status (12)
| Country | Link |
|---|---|
| EP (1) | EP2318408B1 (https=) |
| JP (2) | JP2011529066A (https=) |
| KR (1) | KR20110033299A (https=) |
| CN (1) | CN102159574A (https=) |
| AR (1) | AR074171A1 (https=) |
| AU (1) | AU2009274027A1 (https=) |
| BR (1) | BRPI0916295A2 (https=) |
| CA (1) | CA2731432A1 (https=) |
| IL (1) | IL210822A0 (https=) |
| MX (1) | MX2011000843A (https=) |
| TW (1) | TW201018680A (https=) |
| WO (1) | WO2010011772A2 (https=) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3140759B2 (ja) | 1990-04-02 | 2001-03-05 | キンセキ株式会社 | 弾性表面波素子の製造方法 |
| JP3362860B2 (ja) | 1991-01-09 | 2003-01-07 | 大日本印刷株式会社 | 表面弾性波素子の製造方法 |
| JP2013518112A (ja) * | 2010-01-27 | 2013-05-20 | 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 | ピラゾロピリジンキナーゼ阻害剤 |
| MX2012008643A (es) * | 2010-01-27 | 2013-02-26 | Vertex Pharma | Inhibidores de cinasas de pirazolopiridinas. |
| EP2528917B1 (en) * | 2010-01-27 | 2016-10-19 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridines useful for the treatment of autoimmune, inflammatory or (hyper)proliferative diseases |
| WO2011094288A1 (en) | 2010-01-27 | 2011-08-04 | Vertex Pharmaceuticals Incorporated | Pyrazolopyrazine kinase inhibitors |
| WO2011130515A1 (en) * | 2010-04-14 | 2011-10-20 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Arylthiazolyl piperidines and related compounds as modulators of survival motor neuron (smn) protein production |
| AU2011343642A1 (en) | 2010-12-16 | 2013-05-02 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| MX2013006840A (es) | 2010-12-16 | 2014-01-31 | Vertex Pharma | Inhibidores de la replicacion de los virus de la influenza. |
| CN103492382A (zh) | 2010-12-16 | 2014-01-01 | 沃泰克斯药物股份有限公司 | 流感病毒复制的抑制剂 |
| UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| EP2567959B1 (en) * | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013037390A1 (en) * | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| US8846712B2 (en) | 2011-09-12 | 2014-09-30 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| EP2760862B1 (en) * | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| EP2771340B1 (en) * | 2011-10-25 | 2016-04-13 | Sanofi | 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| EP2847191B1 (en) | 2012-05-09 | 2016-06-15 | Sanofi | Substituted 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine derivatives as kinase inhibitors |
| EP2858984A1 (en) | 2012-06-08 | 2015-04-15 | Vertex Pharmaceuticals Inc. | Inhibitors of influenza viruses replication |
| WO2014181813A1 (ja) * | 2013-05-10 | 2014-11-13 | 武田薬品工業株式会社 | 複素環化合物 |
| ES2824576T3 (es) * | 2015-06-19 | 2021-05-12 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de SHP2 |
| JP6828271B2 (ja) | 2016-05-18 | 2021-02-10 | ソニー株式会社 | 通信装置、通信方法、プログラム、および、通信システム |
| US11066410B2 (en) * | 2017-03-24 | 2021-07-20 | 3100 Central Expressway Llc | Fused triazolo-pyrimidine compounds having useful pharmaceutical application |
| DK3668513T3 (da) * | 2017-08-15 | 2022-01-10 | Agios Pharmaceuticals Inc | Pyruvatkinase-aktiveringsmidler til anvendelse til behandling af blodsygdomme |
| CN111620866A (zh) * | 2019-02-27 | 2020-09-04 | 南京药石科技股份有限公司 | 一种顺式-7,7-二氟-六氢-1H 吡咯并[3,4-c]吡啶衍生物及其制备方法 |
| PE20250663A1 (es) * | 2022-02-08 | 2025-03-04 | Theras Inc | Compuestos con estructura en t formada por al menos cuatro ciclos para usar en el tratamiento del cancer y otras indicaciones |
| CN118834206A (zh) * | 2023-04-24 | 2024-10-25 | 北京宇繁科技有限责任公司 | 一种map4k4抑制剂及其制备方法和应用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10222550A1 (de) * | 2002-05-17 | 2003-11-27 | Bayer Ag | Substituierte Benzyl-pyrazolopyridine |
| EP1545515A1 (en) * | 2002-08-12 | 2005-06-29 | Sugen, Inc. | 3-pyrrolyl-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors |
| TWI372624B (en) * | 2004-03-30 | 2012-09-21 | Vertex Pharma | Azaindoles useful as inhibitors of jak and other protein kinases |
| KR20070002081A (ko) * | 2004-04-02 | 2007-01-04 | 버텍스 파마슈티칼스 인코포레이티드 | Ｒｏｃｋ 및 기타 단백질 키나아제의 억제제로서 유용한아자인돌 |
| DE602006014540D1 (en) * | 2005-05-16 | 2010-07-08 | Irm Llc | Pyrrolopyridinderivate als proteinkinaseinhibitoren |
-
2009
- 2009-07-22 CN CN2009801367212A patent/CN102159574A/zh active Pending
- 2009-07-22 KR KR1020117004087A patent/KR20110033299A/ko not_active Withdrawn
- 2009-07-22 AU AU2009274027A patent/AU2009274027A1/en not_active Abandoned
- 2009-07-22 WO PCT/US2009/051437 patent/WO2010011772A2/en not_active Ceased
- 2009-07-22 CA CA2731432A patent/CA2731432A1/en not_active Abandoned
- 2009-07-22 JP JP2011520175A patent/JP2011529066A/ja not_active Withdrawn
- 2009-07-22 BR BRPI0916295A patent/BRPI0916295A2/pt not_active IP Right Cessation
- 2009-07-22 MX MX2011000843A patent/MX2011000843A/es not_active Application Discontinuation
- 2009-07-22 EP EP09790736.4A patent/EP2318408B1/en active Active
- 2009-07-23 AR ARP090102815A patent/AR074171A1/es unknown
- 2009-07-23 TW TW098124909A patent/TW201018680A/zh unknown
-
2011
- 2011-01-23 IL IL210822A patent/IL210822A0/en unknown
-
2014
- 2014-08-11 JP JP2014163360A patent/JP5931976B2/ja active Active
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