JP2016145262A5 - - Google Patents
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- JP2016145262A5 JP2016145262A5 JP2016101964A JP2016101964A JP2016145262A5 JP 2016145262 A5 JP2016145262 A5 JP 2016145262A5 JP 2016101964 A JP2016101964 A JP 2016101964A JP 2016101964 A JP2016101964 A JP 2016101964A JP 2016145262 A5 JP2016145262 A5 JP 2016145262A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- ethyl
- amino
- compound
- propyl
- 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
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- -1 alkyl amides Chemical class 0.000 claims 36
- 150000001875 compounds Chemical class 0.000 claims 34
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000000304 alkynyl group Chemical group 0.000 claims 15
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 125000003342 alkenyl group Chemical group 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 11
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 10
- 125000004103 aminoalkyl group Chemical group 0.000 claims 9
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 9
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000004122 cyclic group Chemical group 0.000 claims 7
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 125000003282 alkyl amino group Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000004663 dialkyl amino group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000004442 acylamino group Chemical group 0.000 claims 4
- 125000003302 alkenyloxy group Chemical group 0.000 claims 4
- 125000004104 aryloxy group Chemical group 0.000 claims 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 150000008282 halocarbons Chemical class 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000005422 alkyl sulfonamido group Chemical group 0.000 claims 3
- 125000003368 amide group Chemical group 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 3
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 3
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000006321 2-propynyl amino group Chemical group [H]C#CC([H])([H])N([H])* 0.000 claims 2
- 125000003682 3-furyl group Chemical group O1C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 2
- 101100016370 Danio rerio hsp90a.1 gene Proteins 0.000 claims 2
- 101100285708 Dictyostelium discoideum hspD gene Proteins 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 claims 2
- 101100071627 Schizosaccharomyces pombe (strain 972 / ATCC 24843) swo1 gene Proteins 0.000 claims 2
- 150000001408 amides Chemical class 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 238000009472 formulation Methods 0.000 claims 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- PJTYPDPBEAVGGJ-UHFFFAOYSA-N 1-[4-[2-[6-amino-8-[[6-(dimethylamino)-2,3-dihydro-1-benzofuran-5-yl]sulfanyl]purin-9-yl]ethyl]piperidin-1-yl]ethanone Chemical compound CN(C)C1=CC=2OCCC=2C=C1SC1=NC2=C(N)N=CN=C2N1CCC1CCN(C(C)=O)CC1 PJTYPDPBEAVGGJ-UHFFFAOYSA-N 0.000 claims 1
- MCLGGGDNODCJCQ-UHFFFAOYSA-N 2-chloro-8-[[5-(dimethylamino)-2,3-dihydro-1-benzofuran-6-yl]methyl]-9-[2-(2,2-dimethylpropylamino)ethyl]purin-6-amine Chemical compound ClC1=NC(=C2N=C(N(C2=N1)CCNCC(C)(C)C)CC1=CC2=C(CCO2)C=C1N(C)C)N MCLGGGDNODCJCQ-UHFFFAOYSA-N 0.000 claims 1
- BCQCHTGXLYCEAP-UHFFFAOYSA-N 2-fluoro-8-[(5-iodo-2,3-dihydro-1-benzofuran-6-yl)methyl]-9-[2-(2-methylpropylamino)ethyl]purin-6-amine Chemical compound N1=C(F)N=C2N(CCNCC(C)C)C(CC=3C(=CC=4CCOC=4C=3)I)=NC2=C1N BCQCHTGXLYCEAP-UHFFFAOYSA-N 0.000 claims 1
- NDJSGZXZPFMUSO-UHFFFAOYSA-N 2-fluoro-8-[(5-iodo-2,3-dihydro-1-benzofuran-6-yl)methyl]-9-[3-(propan-2-ylamino)propyl]purin-6-amine Chemical compound N1=C(F)N=C2N(CCCNC(C)C)C(CC=3C(=CC=4CCOC=4C=3)I)=NC2=C1N NDJSGZXZPFMUSO-UHFFFAOYSA-N 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- QTCOVPRGVVTMJX-UHFFFAOYSA-N 8-[(5-iodo-2,3-dihydro-1-benzofuran-6-yl)sulfanyl]-9-[2-(2-methylpropylamino)ethyl]purin-6-amine Chemical compound N1=CN=C2N(CCNCC(C)C)C(SC=3C(=CC=4CCOC=4C=3)I)=NC2=C1N QTCOVPRGVVTMJX-UHFFFAOYSA-N 0.000 claims 1
- MZWFMXHWZJGGMO-UHFFFAOYSA-N 8-[(5-iodo-2,3-dihydro-1-benzofuran-6-yl)sulfanyl]-9-[3-(propan-2-ylamino)propyl]purin-6-amine Chemical compound N1=CN=C2N(CCCNC(C)C)C(SC=3C(=CC=4CCOC=4C=3)I)=NC2=C1N MZWFMXHWZJGGMO-UHFFFAOYSA-N 0.000 claims 1
- CIIBAZYPJXIWNJ-UHFFFAOYSA-N 8-[(6-iodo-2,3-dihydro-1-benzofuran-5-yl)sulfanyl]-9-[3-(propan-2-ylamino)propyl]purin-6-amine Chemical compound N1=CN=C2N(CCCNC(C)C)C(SC=3C(=CC=4OCCC=4C=3)I)=NC2=C1N CIIBAZYPJXIWNJ-UHFFFAOYSA-N 0.000 claims 1
- VWVGMLARXOSBEN-UHFFFAOYSA-N 8-[[5-(dimethylamino)-2,3-dihydro-1-benzofuran-6-yl]methyl]-9-[2-(2,2-dimethylpropylamino)ethyl]-2-fluoropurin-6-amine Chemical compound CN(C=1C(=CC2=C(CCO2)C1)CC=1N(C2=NC(=NC(=C2N1)N)F)CCNCC(C)(C)C)C VWVGMLARXOSBEN-UHFFFAOYSA-N 0.000 claims 1
- CWVKSRPTMKYPHI-UHFFFAOYSA-N 8-[[6-(dimethylamino)-2,3-dihydro-1-benzofuran-5-yl]methyl]-2-fluoro-9-[2-(2-methylpropylamino)ethyl]purin-6-amine Chemical compound N1=C(F)N=C2N(CCNCC(C)C)C(CC=3C(=CC=4OCCC=4C=3)N(C)C)=NC2=C1N CWVKSRPTMKYPHI-UHFFFAOYSA-N 0.000 claims 1
- QBKWGGUJUXOAJI-UHFFFAOYSA-N 8-[[6-(dimethylamino)-2,3-dihydro-1-benzofuran-5-yl]sulfanyl]-9-[2-(1-methylsulfonylpiperidin-3-yl)ethyl]purin-6-amine Chemical compound CN(C)C1=CC=2OCCC=2C=C1SC1=NC2=C(N)N=CN=C2N1CCC1CCCN(S(C)(=O)=O)C1 QBKWGGUJUXOAJI-UHFFFAOYSA-N 0.000 claims 1
- GFJYUYJJNJYDCC-UHFFFAOYSA-N 8-[[6-(dimethylamino)-2,3-dihydro-1-benzofuran-5-yl]sulfanyl]-9-[2-(2,2-dimethylpropylamino)ethyl]purin-6-amine Chemical compound N1=CN=C2N(CCNCC(C)(C)C)C(SC3=CC=4CCOC=4C=C3N(C)C)=NC2=C1N GFJYUYJJNJYDCC-UHFFFAOYSA-N 0.000 claims 1
- DIBMXFJVQGNKAJ-UHFFFAOYSA-N 9-[2-(2,2-dimethylpropylamino)ethyl]-2-fluoro-8-[(5-iodo-2,3-dihydro-1-benzofuran-6-yl)methyl]purin-6-amine Chemical compound N1=C(F)N=C2N(CCNCC(C)(C)C)C(CC=3C(=CC=4CCOC=4C=3)I)=NC2=C1N DIBMXFJVQGNKAJ-UHFFFAOYSA-N 0.000 claims 1
- YVMQDVQLTUCVFQ-UHFFFAOYSA-N 9-[2-(2,2-dimethylpropylamino)ethyl]-8-[(5-iodo-2,3-dihydro-1-benzofuran-6-yl)sulfanyl]purin-6-amine Chemical compound N1=CN=C2N(CCNCC(C)(C)C)C(SC=3C(=CC=4CCOC=4C=3)I)=NC2=C1N YVMQDVQLTUCVFQ-UHFFFAOYSA-N 0.000 claims 1
- OPXYFGXVVSJYCU-UHFFFAOYSA-N 9-[3-(tert-butylamino)propyl]-8-[[5-(dimethylamino)-2,3-dihydro-1-benzofuran-6-yl]sulfanyl]purin-6-amine Chemical compound N1=CN=C2N(CCCNC(C)(C)C)C(SC3=CC=4OCCC=4C=C3N(C)C)=NC2=C1N OPXYFGXVVSJYCU-UHFFFAOYSA-N 0.000 claims 1
- CHFJGWUKTLJFQG-UHFFFAOYSA-N 9-[3-(tert-butylamino)propyl]-8-[[6-(dimethylamino)-2,3-dihydro-1-benzofuran-5-yl]sulfanyl]purin-6-amine Chemical compound N1=CN=C2N(CCCNC(C)(C)C)C(SC3=CC=4CCOC=4C=C3N(C)C)=NC2=C1N CHFJGWUKTLJFQG-UHFFFAOYSA-N 0.000 claims 1
- 241001024304 Mino Species 0.000 claims 1
- 125000006323 alkenyl amino group Chemical group 0.000 claims 1
- 125000004422 alkyl sulphonamide group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 230000001548 androgenic effect Effects 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 150000002460 imidazoles Chemical class 0.000 claims 1
- 125000006316 iso-butyl amino group Chemical group [H]N(*)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000001294 propane Substances 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24934909P | 2009-10-07 | 2009-10-07 | |
| US61/249,349 | 2009-10-07 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012533327A Division JP5941407B2 (ja) | 2009-10-07 | 2010-10-07 | Ｈｓｐ９０阻害剤 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018024710A Division JP6804483B2 (ja) | 2009-10-07 | 2018-02-15 | Ｈｓｐ９０阻害剤として有用なプリン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016145262A JP2016145262A (ja) | 2016-08-12 |
| JP2016145262A5 true JP2016145262A5 (https=) | 2016-09-23 |
| JP6326088B2 JP6326088B2 (ja) | 2018-05-16 |
Family
ID=43857159
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012533327A Expired - Fee Related JP5941407B2 (ja) | 2009-10-07 | 2010-10-07 | Ｈｓｐ９０阻害剤 |
| JP2016101964A Expired - Fee Related JP6326088B2 (ja) | 2009-10-07 | 2016-05-20 | Ｈｓｐ９０阻害剤として有用なプリン誘導体 |
| JP2018024710A Expired - Fee Related JP6804483B2 (ja) | 2009-10-07 | 2018-02-15 | Ｈｓｐ９０阻害剤として有用なプリン誘導体 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012533327A Expired - Fee Related JP5941407B2 (ja) | 2009-10-07 | 2010-10-07 | Ｈｓｐ９０阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018024710A Expired - Fee Related JP6804483B2 (ja) | 2009-10-07 | 2018-02-15 | Ｈｓｐ９０阻害剤として有用なプリン誘導体 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US9328114B2 (https=) |
| EP (2) | EP3091019B1 (https=) |
| JP (3) | JP5941407B2 (https=) |
| KR (2) | KR101906568B1 (https=) |
| CN (3) | CN106083855B (https=) |
| AU (1) | AU2010303343B2 (https=) |
| BR (1) | BR112012008019A2 (https=) |
| CA (1) | CA2776308C (https=) |
| DK (1) | DK2486039T3 (https=) |
| EA (1) | EA029272B1 (https=) |
| ES (2) | ES2733131T3 (https=) |
| LT (1) | LT2486039T (https=) |
| MX (1) | MX340714B (https=) |
| NZ (2) | NZ599138A (https=) |
| PT (1) | PT2486039T (https=) |
| WO (1) | WO2011044394A1 (https=) |
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| US9403828B2 (en) | 2005-02-01 | 2016-08-02 | Sloan-Kettering Institute For Cancer Research | Small-molecule Hsp90 inhibitors |
| US7834181B2 (en) | 2005-02-01 | 2010-11-16 | Slaon-Kettering Institute For Cancer Research | Small-molecule Hsp90 inhibitors |
| WO2008005937A2 (en) | 2006-06-30 | 2008-01-10 | Sloan-Kettering Institute For Cancer Research | Treatment of neurodegenerative diseases through inhibiton of hsp90 |
| JP5941407B2 (ja) | 2009-10-07 | 2016-06-29 | スローン − ケッタリング インスティチュート フォー キャンサー リサーチ | Ｈｓｐ９０阻害剤 |
| CN103596955B (zh) | 2011-04-05 | 2016-11-16 | 索隆-基特林癌症研究协会 | Hsp90抑制剂 |
| JP6266506B2 (ja) | 2011-04-05 | 2018-01-24 | スローン − ケッタリング インスティチュート フォー キャンサー リサーチ | Ｈｓｐ９０阻害物質 |
| EA201490230A1 (ru) * | 2011-07-08 | 2014-06-30 | Слоан-Кеттеринг Инститьют Фор Кэнсер Рисерч | Применение меченых ингибиторов hsp90 |
| EP2972394A4 (en) | 2013-03-15 | 2016-11-02 | Sloan Kettering Inst Cancer | HSP90-DESIGNING AND THERAPY |
| SG11201601542SA (en) | 2013-08-16 | 2016-04-28 | Sloan Kettering Inst Cancer | Selective grp94 inhibitors and uses thereof |
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| WO2015138039A1 (en) | 2013-12-23 | 2015-09-17 | Memorial Sloan-Kettering Cancer Center | Methods and reagents for radiolabeling |
| MX387627B (es) * | 2014-09-17 | 2025-03-18 | Memorial Sloan Kettering Cancer Center | Formación de imágenes de inflamación e infección dirigida a hsp90 y terapia |
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| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025099111A1 (en) | 2023-11-10 | 2025-05-15 | Wella Germany Gmbh | New telescoping syntheses of 6-hydroxy-benzomorpholine (3,4-dihydro-2h-1,4-benzoxazin-6-ol) |
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| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
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| KR101313804B1 (ko) | 2007-03-20 | 2013-10-01 | 쿠리스 인코퍼레이션 | Ｈｓｐ９０ 억제제로서의 융합된 아미노 피리딘 |
| WO2009007399A1 (en) * | 2007-07-12 | 2009-01-15 | Crystax Pharmaceuticals, S.L. | New compounds as hsp90 inhibitors |
| WO2009042646A1 (en) | 2007-09-24 | 2009-04-02 | Curis, Inc. | Anti-proliferative agents |
| NZ586129A (en) | 2007-11-14 | 2012-06-29 | Myrexis Inc | Therapeutic compounds and their use in treating diseases and disorders |
| JP5941407B2 (ja) | 2009-10-07 | 2016-06-29 | スローン − ケッタリング インスティチュート フォー キャンサー リサーチ | Ｈｓｐ９０阻害剤 |
| CN103596955B (zh) | 2011-04-05 | 2016-11-16 | 索隆-基特林癌症研究协会 | Hsp90抑制剂 |
| JP6266506B2 (ja) | 2011-04-05 | 2018-01-24 | スローン − ケッタリング インスティチュート フォー キャンサー リサーチ | Ｈｓｐ９０阻害物質 |
| SG11201601542SA (en) | 2013-08-16 | 2016-04-28 | Sloan Kettering Inst Cancer | Selective grp94 inhibitors and uses thereof |
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2010
- 2010-10-07 JP JP2012533327A patent/JP5941407B2/ja not_active Expired - Fee Related
- 2010-10-07 EP EP16171952.1A patent/EP3091019B1/en not_active Not-in-force
- 2010-10-07 AU AU2010303343A patent/AU2010303343B2/en not_active Ceased
- 2010-10-07 NZ NZ599138A patent/NZ599138A/en not_active IP Right Cessation
- 2010-10-07 BR BR112012008019A patent/BR112012008019A2/pt not_active IP Right Cessation
- 2010-10-07 NZ NZ625593A patent/NZ625593A/en not_active IP Right Cessation
- 2010-10-07 CA CA2776308A patent/CA2776308C/en not_active Expired - Fee Related
- 2010-10-07 LT LTEP10822718.2T patent/LT2486039T/lt unknown
- 2010-10-07 US US13/500,809 patent/US9328114B2/en active Active
- 2010-10-07 CN CN201610269904.3A patent/CN106083855B/zh not_active Expired - Fee Related
- 2010-10-07 KR KR1020127011546A patent/KR101906568B1/ko not_active Expired - Fee Related
- 2010-10-07 WO PCT/US2010/051872 patent/WO2011044394A1/en not_active Ceased
- 2010-10-07 EA EA201270535A patent/EA029272B1/ru not_active IP Right Cessation
- 2010-10-07 CN CN201610270112.8A patent/CN105924443A/zh active Pending
- 2010-10-07 ES ES16171952T patent/ES2733131T3/es active Active
- 2010-10-07 PT PT108227182T patent/PT2486039T/pt unknown
- 2010-10-07 MX MX2012004089A patent/MX340714B/es active IP Right Grant
- 2010-10-07 EP EP10822718.2A patent/EP2486039B1/en active Active
- 2010-10-07 DK DK10822718.2T patent/DK2486039T3/en active
- 2010-10-07 CN CN201080055473.1A patent/CN102639534A/zh active Pending
- 2010-10-07 KR KR1020187028594A patent/KR102129420B1/ko not_active Expired - Fee Related
- 2010-10-07 ES ES10822718.2T patent/ES2589403T3/es active Active
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2016
- 2016-04-21 US US15/135,121 patent/US10172863B2/en active Active
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