JP2011529065A5 - - Google Patents
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- JP2011529065A5 JP2011529065A5 JP2011520173A JP2011520173A JP2011529065A5 JP 2011529065 A5 JP2011529065 A5 JP 2011529065A5 JP 2011520173 A JP2011520173 A JP 2011520173A JP 2011520173 A JP2011520173 A JP 2011520173A JP 2011529065 A5 JP2011529065 A5 JP 2011529065A5
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- JP
- Japan
- Prior art keywords
- independently
- optionally
- substituted
- ring
- acceptable salt
- 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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- -1 pyrrolopyridinyl Chemical group 0.000 claims description 51
- 150000001875 compounds Chemical class 0.000 claims description 48
- 150000003839 salts Chemical class 0.000 claims description 30
- 229910052736 halogen Inorganic materials 0.000 claims description 20
- 125000001931 aliphatic group Chemical group 0.000 claims description 19
- 150000002367 halogens Chemical class 0.000 claims description 19
- 230000001404 mediated effect Effects 0.000 claims description 19
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 16
- 239000000203 mixture Substances 0.000 claims description 15
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 13
- 208000023275 Autoimmune disease Diseases 0.000 claims description 12
- 125000002883 imidazolyl group Chemical group 0.000 claims description 11
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 11
- 125000000335 thiazolyl group Chemical group 0.000 claims description 11
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 10
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 10
- 125000005842 heteroatom Chemical group 0.000 claims description 10
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 229910052760 oxygen Inorganic materials 0.000 claims description 10
- 239000001301 oxygen Substances 0.000 claims description 10
- 229920006395 saturated elastomer Polymers 0.000 claims description 10
- 229910052717 sulfur Inorganic materials 0.000 claims description 10
- 239000011593 sulfur Substances 0.000 claims description 10
- NFDXQGNDWIPXQL-UHFFFAOYSA-N 1-cyclooctyldiazocane Chemical group C1CCCCCCC1N1NCCCCCC1 NFDXQGNDWIPXQL-UHFFFAOYSA-N 0.000 claims description 9
- 125000002393 azetidinyl group Chemical group 0.000 claims description 9
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 9
- 125000001041 indolyl group Chemical group 0.000 claims description 9
- 125000004193 piperazinyl group Chemical group 0.000 claims description 9
- 125000003386 piperidinyl group Chemical group 0.000 claims description 9
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 9
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 9
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 125000003725 azepanyl group Chemical group 0.000 claims description 7
- 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 7
- 125000005959 diazepanyl group Chemical group 0.000 claims description 7
- 125000002632 imidazolidinyl group Chemical group 0.000 claims description 7
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims description 7
- 125000002757 morpholinyl group Chemical group 0.000 claims description 7
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 7
- 125000005961 oxazepanyl group Chemical group 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 6
- 201000006417 multiple sclerosis Diseases 0.000 claims description 6
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 6
- 125000002971 oxazolyl group Chemical group 0.000 claims description 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 5
- 125000005942 tetrahydropyridyl group Chemical group 0.000 claims description 5
- 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
- 125000005334 azaindolyl group Chemical group N1N=C(C2=CC=CC=C12)* 0.000 claims description 4
- 125000004925 dihydropyridyl group Chemical group N1(CC=CC=C1)* 0.000 claims description 4
- 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 description 4
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 4
- 125000002950 monocyclic group Chemical group 0.000 claims description 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 4
- 108060006633 protein kinase Proteins 0.000 claims description 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 4
- 125000001425 triazolyl group Chemical group 0.000 claims description 4
- FLUVVESHOANMOG-UHFFFAOYSA-N 1-cyclodecyldiazecane Chemical group C1CCCCCCCCC1N1NCCCCCCCC1 FLUVVESHOANMOG-UHFFFAOYSA-N 0.000 claims description 3
- JWGMXWNVAYWSNI-UHFFFAOYSA-N 1-cyclohexyldiazinane Chemical group C1CCCCC1N1NCCCC1 JWGMXWNVAYWSNI-UHFFFAOYSA-N 0.000 claims description 3
- PPNCOQHHSGMKGI-UHFFFAOYSA-N 1-cyclononyldiazonane Chemical group C1CCCCCCCC1N1NCCCCCCC1 PPNCOQHHSGMKGI-UHFFFAOYSA-N 0.000 claims description 3
- 125000002619 bicyclic group Chemical group 0.000 claims description 3
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 3
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims description 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
- 125000005047 dihydroimidazolyl group Chemical group N1(CNC=C1)* 0.000 claims description 3
- 125000005051 dihydropyrazinyl group Chemical group N1(CC=NC=C1)* 0.000 claims description 3
- 125000005052 dihydropyrazolyl group Chemical group N1(NCC=C1)* 0.000 claims description 3
- 125000005053 dihydropyrimidinyl group Chemical group N1(CN=CC=C1)* 0.000 claims description 3
- 125000005054 dihydropyrrolyl group Chemical group [H]C1=C([H])C([H])([H])C([H])([H])N1* 0.000 claims description 3
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 3
- 125000004594 isoindolinyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 claims description 3
- 125000004628 isothiazolidinyl group Chemical group S1N(CCC1)* 0.000 claims description 3
- 125000003965 isoxazolidinyl group Chemical group 0.000 claims description 3
- 125000000160 oxazolidinyl group Chemical group 0.000 claims description 3
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims description 3
- 125000005493 quinolyl group Chemical group 0.000 claims description 3
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 3
- 125000001984 thiazolidinyl group Chemical group 0.000 claims description 3
- 125000004169 (C1-C6) alkyl group Chemical group 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
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- ARUKYTASOALXFG-UHFFFAOYSA-N cycloheptylcycloheptane Chemical group C1CCCCCC1C1CCCCCC1 ARUKYTASOALXFG-UHFFFAOYSA-N 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 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
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 208000018937 joint inflammation Diseases 0.000 claims description 2
- 206010025135 lupus erythematosus Diseases 0.000 claims description 2
- 125000006574 non-aromatic ring group Chemical group 0.000 claims description 2
- TVMXDCGIABBOFY-UHFFFAOYSA-N octane Chemical compound CCCCCCCC TVMXDCGIABBOFY-UHFFFAOYSA-N 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 125000005412 pyrazyl group Chemical group 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 239000012973 diazabicyclooctane Substances 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 description 13
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- PAMIQIKDUOTOBW-UHFFFAOYSA-N CN1CCCCC1 Chemical compound CN1CCCCC1 PAMIQIKDUOTOBW-UHFFFAOYSA-N 0.000 description 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 125000004122 cyclic group Chemical group 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
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8292408P | 2008-07-23 | 2008-07-23 | |
| US61/082,924 | 2008-07-23 | ||
| PCT/US2009/051430 WO2010011768A1 (en) | 2008-07-23 | 2009-07-22 | Tri-cyclic pyrazolopyridine kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014162132A Division JP2014208708A (ja) | 2008-07-23 | 2014-08-08 | 三環式ピラゾロピリジンキナーゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011529065A JP2011529065A (ja) | 2011-12-01 |
| JP2011529065A5 true JP2011529065A5 (OSRAM) | 2012-07-19 |
| JP5631310B2 JP5631310B2 (ja) | 2014-11-26 |
Family
ID=41137557
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011520173A Expired - Fee Related JP5631310B2 (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 |
| JP2014162132A Withdrawn JP2014208708A (ja) | 2008-07-23 | 2014-08-08 | 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 |
|---|---|---|---|
| JP2014162132A Withdrawn JP2014208708A (ja) | 2008-07-23 | 2014-08-08 | 三環式ピラゾロピリジンキナーゼ阻害剤 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8563576B2 (OSRAM) |
| EP (1) | EP2328896B1 (OSRAM) |
| JP (2) | JP5631310B2 (OSRAM) |
| CN (1) | CN102131809A (OSRAM) |
| AU (1) | AU2009274023A1 (OSRAM) |
| CA (1) | CA2731498A1 (OSRAM) |
| MX (1) | MX2011000837A (OSRAM) |
| WO (1) | WO2010011768A1 (OSRAM) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8569337B2 (en) | 2008-07-23 | 2013-10-29 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| JP2011530527A (ja) * | 2008-08-06 | 2011-12-22 | 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 | アミノピリジンキナーゼ阻害剤 |
| DK2442809T3 (en) | 2009-06-17 | 2016-12-19 | Vertex Pharma | Inhibitors of the replication of influenza virus |
| MX2012008642A (es) * | 2010-01-27 | 2012-11-23 | Vertex Pharma | Inhibidores de cinasas de pirazolopiridinas. |
| JP2013518114A (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 | ピラゾロピリミジンキナーゼ阻害剤 |
| CN102858769A (zh) * | 2010-01-27 | 2013-01-02 | 沃泰克斯药物股份有限公司 | 吡唑并吡啶激酶抑制剂 |
| AU2011343642A1 (en) | 2010-12-16 | 2013-05-02 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| 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 |
| KR20130128435A (ko) | 2010-12-16 | 2013-11-26 | 버텍스 파마슈티칼스 인코포레이티드 | 인플루엔자 바이러스 복제의 억제제 |
| UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| WO2013184985A1 (en) | 2012-06-08 | 2013-12-12 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| JP6998657B2 (ja) | 2013-09-18 | 2022-02-04 | エピアクシス セラピューティクス プロプライエタリー リミテッド | 幹細胞調節ｉｉ |
| EP3068776B1 (en) | 2013-11-13 | 2019-05-29 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| RS57541B1 (sr) | 2013-11-13 | 2018-10-31 | Vertex Pharma | Postupci za pripremu inhibitora replikacije virusa gripa |
| AU2015309686B2 (en) | 2014-08-25 | 2020-05-14 | Epiaxis Therapeutics Pty Ltd | Compositions for modulating cancer stem cells and uses therefor |
| AU2015311730A1 (en) | 2014-09-05 | 2017-04-20 | Allosteros Therapeutics, Inc | Camkii inhibitors and uses thereof |
| JP2018509389A (ja) * | 2015-01-30 | 2018-04-05 | リ・ガリ・ベスローテン・フエンノートシャップＬｉ Ｇａｌｌｉ Ｂ．Ｖ． | 膣用薬物送達デバイス |
| JP6704416B2 (ja) | 2015-05-13 | 2020-06-03 | 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | インフルエンザウイルスの複製の阻害剤を調製する方法 |
| MA42422A (fr) | 2015-05-13 | 2018-05-23 | Vertex Pharma | Inhibiteurs de la réplication des virus de la grippe |
| US10730868B2 (en) | 2016-07-14 | 2020-08-04 | Bristol-Myers Squibb Company | Bicyclic heteroaryl substituted compounds |
| JP6903732B2 (ja) | 2016-07-14 | 2021-07-14 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｐａｒ４阻害剤としての三環式ヘテロアリール置換のキノリンおよびアザキノリン化合物 |
| WO2018013774A1 (en) | 2016-07-14 | 2018-01-18 | Bristol-Myers Squibb Company | Bicyclic heteroaryl substituted compounds |
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| CA2545821C (en) | 2003-12-22 | 2010-09-21 | Basilea Pharmaceutica Ag | Aroylfuranes and aroylthiophenes |
| WO2005103050A2 (en) * | 2004-04-02 | 2005-11-03 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of rock and other protein kinases |
| EP1751119A1 (en) | 2004-05-19 | 2007-02-14 | AstraZeneca AB | Novel fused heterocycles and uses thereof |
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| ZA200704888B (en) * | 2004-11-22 | 2009-02-25 | Vertex Pharma | Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases |
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| RU2412943C2 (ru) | 2005-03-23 | 2011-02-27 | Ф. Хоффманн-Ля Рош Аг | ПРОИЗВОДНЫЕ АЦЕТИЛЕНИЛ-ПИРАЗОЛО-ПИРИМИДИНА В КАЧЕСТВЕ АНТАГОНИСТОВ mGluR2 |
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-
2009
- 2009-07-22 CN CN2009801327408A patent/CN102131809A/zh active Pending
- 2009-07-22 EP EP09790733.1A patent/EP2328896B1/en not_active Not-in-force
- 2009-07-22 CA CA2731498A patent/CA2731498A1/en not_active Abandoned
- 2009-07-22 MX MX2011000837A patent/MX2011000837A/es not_active Application Discontinuation
- 2009-07-22 JP JP2011520173A patent/JP5631310B2/ja not_active Expired - Fee Related
- 2009-07-22 WO PCT/US2009/051430 patent/WO2010011768A1/en not_active Ceased
- 2009-07-22 AU AU2009274023A patent/AU2009274023A1/en not_active Abandoned
-
2011
- 2011-12-01 US US13/308,612 patent/US8563576B2/en not_active Expired - Fee Related
-
2014
- 2014-08-08 JP JP2014162132A patent/JP2014208708A/ja not_active Withdrawn
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