JP2011529063A5 - - Google Patents
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- JP2011529063A5 JP2011529063A5 JP2011520170A JP2011520170A JP2011529063A5 JP 2011529063 A5 JP2011529063 A5 JP 2011529063A5 JP 2011520170 A JP2011520170 A JP 2011520170A JP 2011520170 A JP2011520170 A JP 2011520170A JP 2011529063 A5 JP2011529063 A5 JP 2011529063A5
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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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- 150000001875 compounds Chemical class 0.000 claims description 51
- -1 pyrrolopyridinyl Chemical group 0.000 claims description 48
- 150000003839 salts Chemical class 0.000 claims description 30
- 125000001931 aliphatic group Chemical group 0.000 claims description 27
- 229910052736 halogen Inorganic materials 0.000 claims description 20
- 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 16
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 14
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 14
- 208000023275 Autoimmune disease Diseases 0.000 claims description 12
- 125000002883 imidazolyl group Chemical group 0.000 claims description 12
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 12
- 125000000335 thiazolyl group Chemical group 0.000 claims description 12
- NFDXQGNDWIPXQL-UHFFFAOYSA-N 1-cyclooctyldiazocane Chemical group C1CCCCCCC1N1NCCCCCC1 NFDXQGNDWIPXQL-UHFFFAOYSA-N 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
- 125000002393 azetidinyl group Chemical group 0.000 claims description 10
- 125000005842 heteroatom Chemical group 0.000 claims description 10
- 125000001041 indolyl group 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
- 125000004193 piperazinyl group Chemical group 0.000 claims description 10
- 125000003386 piperidinyl group Chemical group 0.000 claims description 10
- 125000004076 pyridyl group Chemical group 0.000 claims description 10
- 125000000719 pyrrolidinyl group Chemical group 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
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 10
- 125000003725 azepanyl group Chemical group 0.000 claims description 9
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 9
- 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 8
- 125000005959 diazepanyl group Chemical group 0.000 claims description 8
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 8
- 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
- 125000005961 oxazepanyl group Chemical group 0.000 claims description 7
- 125000005942 tetrahydropyridyl group Chemical group 0.000 claims description 7
- 125000004925 dihydropyridyl group Chemical group N1(CC=CC=C1)* 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 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 6
- 125000002950 monocyclic group Chemical group 0.000 claims description 6
- 201000006417 multiple sclerosis Diseases 0.000 claims description 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 6
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 6
- 125000002632 imidazolidinyl 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
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 4
- 125000002971 oxazolyl group Chemical group 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
- 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
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-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
- FLUVVESHOANMOG-UHFFFAOYSA-N 1-cyclodecyldiazecane Chemical group C1CCCCCCCCC1N1NCCCCCCCC1 FLUVVESHOANMOG-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
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 239000012973 diazabicyclooctane Substances 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
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 description 12
- 0 *N1C(CI*=C)CN(CCS=C)CC1 Chemical compound *N1C(CI*=C)CN(CCS=C)CC1 0.000 description 4
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- IMSODMZESSGVBE-UHFFFAOYSA-N 2-Oxazoline Chemical compound C1CN=CO1 IMSODMZESSGVBE-UHFFFAOYSA-N 0.000 description 1
- ZHHCLIRTNOSAPB-UHFFFAOYSA-N CCC(C)N1CCNCC1 Chemical compound CCC(C)N1CCNCC1 ZHHCLIRTNOSAPB-UHFFFAOYSA-N 0.000 description 1
- WGCYRFWNGRMRJA-UHFFFAOYSA-N CCN1CCNCC1 Chemical compound CCN1CCNCC1 WGCYRFWNGRMRJA-UHFFFAOYSA-N 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 125000004122 cyclic group Chemical group 0.000 description 1
- ARUKYTASOALXFG-UHFFFAOYSA-N cycloheptylcycloheptane Chemical group C1CCCCCC1C1CCCCCC1 ARUKYTASOALXFG-UHFFFAOYSA-N 0.000 description 1
- 125000002704 decyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 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 (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8294108P | 2008-07-23 | 2008-07-23 | |
| US61/082,941 | 2008-07-23 | ||
| PCT/US2009/051423 WO2010011762A1 (en) | 2008-07-23 | 2009-07-22 | Pyrazolopyridine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011529063A JP2011529063A (ja) | 2011-12-01 |
| JP2011529063A5 true JP2011529063A5 (OSRAM) | 2012-07-19 |
| JP5542287B2 JP5542287B2 (ja) | 2014-07-09 |
Family
ID=41203687
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011520170A Expired - Fee Related JP5542287B2 (ja) | 2008-07-23 | 2009-07-22 | ピラゾロピリジンキナーゼ阻害剤 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20120165368A1 (OSRAM) |
| EP (1) | EP2321318A1 (OSRAM) |
| JP (1) | JP5542287B2 (OSRAM) |
| CN (1) | CN102131808A (OSRAM) |
| AU (1) | AU2009274017A1 (OSRAM) |
| CA (1) | CA2731496A1 (OSRAM) |
| MX (1) | MX2011000834A (OSRAM) |
| WO (1) | WO2010011762A1 (OSRAM) |
Families Citing this family (17)
| 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. |
| 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 |
| UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| 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 |
| 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 |
| CN108794480A (zh) * | 2017-04-28 | 2018-11-13 | 天津药物研究院有限公司 | 吡咯并嘧啶类化合物、其制备方法和用途 |
| JP7536767B2 (ja) | 2018-12-31 | 2024-08-20 | バイオメア フュージョン，インコーポレイテッド | メニン－ｍｌｌ相互作用の不可逆的阻害剤 |
| US11174263B2 (en) | 2018-12-31 | 2021-11-16 | Biomea Fusion, Inc. | Inhibitors of menin-MLL interaction |
| CA3228627A1 (en) | 2021-08-11 | 2023-02-16 | Thomas Butler | Covalent inhibitors of menin-mll interaction for diabetes mellitus |
| KR20240087693A (ko) | 2021-08-20 | 2024-06-19 | 바이오메아 퓨전, 인크. | 암 치료를 위한 비가역적 메닌-mll 억제제인 n-[4-[4-(4-모르폴리닐)-7h-피롤로[2,3-d]피리미딘-6-일]페닐]-4-[[3(r)-[(1-옥소-2-프로펜-1-일)아미노]-1-피페리디닐]메틸]-2-피리딘카르복스아미드의 결정질 형태 |
| TW202430528A (zh) | 2023-01-18 | 2024-08-01 | 美商拜歐米富士恩股份有限公司 | Ｎ－［４－［４－（４－嗎啉基）－７ｈ－吡咯並［２，３－ｄ］嘧啶－６－基］苯基］－４－［［３（ｒ）－［（１－氧代－２－丙烯－１－基）氨基］－１－哌啶基］甲基］－２－吡啶甲醯胺的結晶形式作為ｍｅｎｉｎ－ｍｌｌ相互作用的共價抑制劑 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA05001688A (es) * | 2002-08-12 | 2005-04-19 | Sugen Inc | 3-pirrolil-piridopirazoles y 3-pirrolil-indazoles como inhibidores de cinasa novedosos. |
| WO2005103050A2 (en) * | 2004-04-02 | 2005-11-03 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of rock and other protein kinases |
| ZA200704888B (en) * | 2004-11-22 | 2009-02-25 | Vertex Pharma | Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases |
-
2009
- 2009-07-22 CA CA2731496A patent/CA2731496A1/en not_active Abandoned
- 2009-07-22 CN CN2009801327342A patent/CN102131808A/zh active Pending
- 2009-07-22 EP EP09790732A patent/EP2321318A1/en not_active Withdrawn
- 2009-07-22 WO PCT/US2009/051423 patent/WO2010011762A1/en not_active Ceased
- 2009-07-22 AU AU2009274017A patent/AU2009274017A1/en not_active Abandoned
- 2009-07-22 MX MX2011000834A patent/MX2011000834A/es not_active Application Discontinuation
- 2009-07-22 JP JP2011520170A patent/JP5542287B2/ja not_active Expired - Fee Related
-
2011
- 2011-12-01 US US13/308,605 patent/US20120165368A1/en not_active Abandoned
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