JP2011511003A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2011511003A5 JP2011511003A5 JP2010545233A JP2010545233A JP2011511003A5 JP 2011511003 A5 JP2011511003 A5 JP 2011511003A5 JP 2010545233 A JP2010545233 A JP 2010545233A JP 2010545233 A JP2010545233 A JP 2010545233A JP 2011511003 A5 JP2011511003 A5 JP 2011511003A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- amino
- dihydropyrido
- fluoro
- phenyl
- 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
- -1 amino, carbonylamino, aminocarbonyl Chemical group 0.000 claims 90
- 150000001875 compounds Chemical class 0.000 claims 31
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000005842 heteroatom Chemical group 0.000 claims 16
- 125000002344 aminooxy group Chemical group [H]N([H])O[*] 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- BDTRIDKONHOQQN-UHFFFAOYSA-N 4h-pyrimidin-5-one Chemical compound O=C1CN=CN=C1 BDTRIDKONHOQQN-UHFFFAOYSA-N 0.000 claims 6
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 150000001602 bicycloalkyls Chemical group 0.000 claims 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 3
- 150000002923 oximes Chemical class 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- DRQRNJQGXVDZBU-TZIWHRDSSA-N (2r)-2-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxy-4-hydroxy-n,n-dimethylbutanamide Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\O[C@H](CCO)C(=O)N(C)C)=N1 DRQRNJQGXVDZBU-TZIWHRDSSA-N 0.000 claims 1
- DRQRNJQGXVDZBU-CTNGQTDRSA-N (2s)-2-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxy-4-hydroxy-n,n-dimethylbutanamide Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\O[C@@H](CCO)C(=O)N(C)C)=N1 DRQRNJQGXVDZBU-CTNGQTDRSA-N 0.000 claims 1
- VWBPRIBQAARILO-MJGOQNOKSA-N (2s)-4-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxy-2-hydroxybutanamide Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCC[C@H](O)C(N)=O)=N1 VWBPRIBQAARILO-MJGOQNOKSA-N 0.000 claims 1
- NELKHPYWKAUWEN-MJGOQNOKSA-N (2s)-4-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxy-2-hydroxybutanoic acid Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCC[C@H](O)C(O)=O)=N1 NELKHPYWKAUWEN-MJGOQNOKSA-N 0.000 claims 1
- WZUYUECAUGEKFC-SQJMNOBHSA-N (4s)-4-[[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxymethyl]-3-benzyl-1,3-oxazolidin-2-one Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OC[C@H]2N(C(=O)OC2)CC=2C=CC=CC=2)=N1 WZUYUECAUGEKFC-SQJMNOBHSA-N 0.000 claims 1
- NOELJGWWOVBLOL-KBXCAEBGSA-N (5s)-5-[[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxymethyl]-1,3-oxazolidin-2-one Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OC[C@H]2OC(=O)NC2)=N1 NOELJGWWOVBLOL-KBXCAEBGSA-N 0.000 claims 1
- LVDVFHGRIJTUMH-OAQYLSRUSA-N (7r)-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-5-n-(2-morpholin-4-ylethoxy)-7,8-dihydropyrido[4,3-d]pyrimidine-2,5-diamine Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCCN2CCOCC2)=N1 LVDVFHGRIJTUMH-OAQYLSRUSA-N 0.000 claims 1
- VPUBOTVYSMAHIN-OTOKDRCRSA-N (7r)-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-5-n-(morpholin-2-ylmethoxy)-7,8-dihydropyrido[4,3-d]pyrimidine-2,5-diamine Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCC2OCCNC2)=N1 VPUBOTVYSMAHIN-OTOKDRCRSA-N 0.000 claims 1
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical compound O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 claims 1
- HDFHEIOIKDQXSX-LMNIDFBRSA-N 2-[2-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxyacetyl]-1,3,4,7,8,8a-hexahydropyrrolo[1,2-a]pyrazin-6-one Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCC(=O)N2CC3N(C(CC3)=O)CC2)=N1 HDFHEIOIKDQXSX-LMNIDFBRSA-N 0.000 claims 1
- YJOHWPAQHRFQFA-GOSISDBHSA-N 2-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxy-1-(3,3-difluoroazetidin-1-yl)ethanone Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCC(=O)N2CC(F)(F)C2)=N1 YJOHWPAQHRFQFA-GOSISDBHSA-N 0.000 claims 1
- NQHCNSDEHKYAOC-OAQYLSRUSA-N 2-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxy-1-(4-hydroxypiperidin-1-yl)ethanone Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCC(=O)N2CCC(O)CC2)=N1 NQHCNSDEHKYAOC-OAQYLSRUSA-N 0.000 claims 1
- NXWODOMWROKIKJ-DUSLRRAJSA-N 2-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxy-4-hydroxybutanamide Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OC(CCO)C(N)=O)=N1 NXWODOMWROKIKJ-DUSLRRAJSA-N 0.000 claims 1
- VCEAAVLZGHPLBA-HXUWFJFHSA-N 2-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxy-n-(2-methoxyethyl)-n-methylacetamide Chemical compound C1([C@@H]2N\C(C3=C(C)N=C(N)N=C3C2)=N/OCC(=O)N(C)CCOC)=CC=C(F)C=C1C1=CC=CC(OC)=N1 VCEAAVLZGHPLBA-HXUWFJFHSA-N 0.000 claims 1
- VXBCMBJFQXGFJD-GOSISDBHSA-N 2-[[2-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxyacetyl]-methylamino]acetamide Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCC(=O)N(C)CC(N)=O)=N1 VXBCMBJFQXGFJD-GOSISDBHSA-N 0.000 claims 1
- ZPNUCOCBFHMOMV-GOSISDBHSA-N 3-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxypropan-1-ol Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCCCO)=N1 ZPNUCOCBFHMOMV-GOSISDBHSA-N 0.000 claims 1
- YJQOTPHRPJQSLQ-FQNRMIAFSA-N 4-[[(7r)-2-amino-7-[2-(5-amino-6-methoxypyrazin-2-yl)-4-fluorophenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxybutane-1,2-diol Chemical compound N1=C(N)C(OC)=NC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCCC(O)CO)=C1 YJQOTPHRPJQSLQ-FQNRMIAFSA-N 0.000 claims 1
- QGNOTWMPRVBVFZ-FBMWCMRBSA-N 4-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyrazin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxybutane-1,2-diol Chemical compound COC1=CN=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCCC(O)CO)=N1 QGNOTWMPRVBVFZ-FBMWCMRBSA-N 0.000 claims 1
- RTIMCVAWDIGQHH-LJQANCHMSA-N 4-[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxybutan-1-ol Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCCCCO)=N1 RTIMCVAWDIGQHH-LJQANCHMSA-N 0.000 claims 1
- AEOIOPGFKIUHME-TYJDENFWSA-N 4-[[(7s)-2-amino-7-[2-(5-amino-6-methoxypyrazin-2-yl)-4-fluorophenyl]-8,8-difluoro-4-methyl-7h-pyrido[4,3-d]pyrimidin-5-yl]amino]oxybutane-1,2-diol Chemical compound N1=C(N)C(OC)=NC(C=2C(=CC=C(F)C=2)[C@H]2C(C3=NC(N)=NC(C)=C3C(=N/OCCC(O)CO)/N2)(F)F)=C1 AEOIOPGFKIUHME-TYJDENFWSA-N 0.000 claims 1
- ZWSDBPUELLQSJZ-WQHGFJKVSA-N 4-[[(7s)-2-amino-7-[2-(5-amino-6-methoxypyrazin-2-yl)-4-fluorophenyl]-8-fluoro-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxybutane-1,2-diol Chemical compound N1=C(N)C(OC)=NC(C=2C(=CC=C(F)C=2)[C@H]2C(C3=NC(N)=NC(C)=C3C(=N/OCCC(O)CO)/N2)F)=C1 ZWSDBPUELLQSJZ-WQHGFJKVSA-N 0.000 claims 1
- UUMCAVHRUOVLEN-QPDBELLOSA-N 4-[[(7s)-2-amino-8-fluoro-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxybutane-1,2-diol Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@H]2C(C3=NC(N)=NC(C)=C3C(=N/OCCC(O)CO)/N2)F)=N1 UUMCAVHRUOVLEN-QPDBELLOSA-N 0.000 claims 1
- MGITXHIKJISZGA-IHTASXDUSA-N 5-[[[(7r)-2-amino-7-[2-(5-amino-6-methoxypyrazin-2-yl)-4-fluorophenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxymethyl]-3,4-dihydroxyoxolan-2-one Chemical compound N1=C(N)C(OC)=NC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCC2C(C(O)C(=O)O2)O)=C1 MGITXHIKJISZGA-IHTASXDUSA-N 0.000 claims 1
- IUJOVWRTZOKKAK-JLGDOQARSA-N 5-[[[(7r)-2-amino-7-[4-fluoro-2-(6-methoxypyrazin-2-yl)phenyl]-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5-yl]amino]oxymethyl]-3,4-dihydroxyoxolan-2-one Chemical compound COC1=CN=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(/C3=C(C)N=C(N)N=C3C2)=N\OCC2C(C(O)C(=O)O2)O)=N1 IUJOVWRTZOKKAK-JLGDOQARSA-N 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- XLXNSEBFJITLOU-UHFFFAOYSA-N OCC(CCON=C1C=NC=NC1)O Chemical compound OCC(CCON=C1C=NC=NC1)O XLXNSEBFJITLOU-UHFFFAOYSA-N 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000002723 alicyclic group Chemical group 0.000 claims 1
- 125000001931 aliphatic group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000001118 alkylidene group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- VGPBPWRBXBKGRE-UHFFFAOYSA-N n-(oxomethylidene)hydroxylamine Chemical compound ON=C=O VGPBPWRBXBKGRE-UHFFFAOYSA-N 0.000 claims 1
- 125000005188 oxoalkyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229940124531 pharmaceutical excipient Drugs 0.000 claims 1
- AKCMCFPQVUTWFW-UHFFFAOYSA-N pyrrolidin-3-yl acetate Chemical compound CC(=O)OC1CCNC1 AKCMCFPQVUTWFW-UHFFFAOYSA-N 0.000 claims 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2572508P | 2008-02-01 | 2008-02-01 | |
| US61/025,725 | 2008-02-01 | ||
| US10159508P | 2008-09-30 | 2008-09-30 | |
| US61/101,595 | 2008-09-30 | ||
| PCT/US2009/032728 WO2009097578A1 (en) | 2008-02-01 | 2009-01-30 | Oxim derivatives as hsp90 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011511003A JP2011511003A (ja) | 2011-04-07 |
| JP2011511003A5 true JP2011511003A5 (OSRAM) | 2012-03-15 |
| JP5524084B2 JP5524084B2 (ja) | 2014-06-18 |
Family
ID=40436400
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010545233A Expired - Fee Related JP5524084B2 (ja) | 2008-02-01 | 2009-01-30 | Hsp90阻害剤としてのオキシム誘導体 |
Country Status (26)
| Country | Link |
|---|---|
| US (4) | US20110053873A1 (OSRAM) |
| EP (1) | EP2252595B1 (OSRAM) |
| JP (1) | JP5524084B2 (OSRAM) |
| KR (1) | KR20100116206A (OSRAM) |
| CN (1) | CN101983191B (OSRAM) |
| AR (1) | AR071452A1 (OSRAM) |
| AU (1) | AU2009208947B2 (OSRAM) |
| BR (1) | BRPI0906598A2 (OSRAM) |
| CA (1) | CA2713658C (OSRAM) |
| CL (1) | CL2009000228A1 (OSRAM) |
| CR (1) | CR11659A (OSRAM) |
| DO (1) | DOP2010000236A (OSRAM) |
| EA (1) | EA019156B1 (OSRAM) |
| EC (1) | ECSP10010434A (OSRAM) |
| ES (1) | ES2475206T3 (OSRAM) |
| GE (1) | GEP20125718B (OSRAM) |
| IL (1) | IL207227A0 (OSRAM) |
| MA (1) | MA32104B1 (OSRAM) |
| MX (1) | MX2010008269A (OSRAM) |
| MY (1) | MY150596A (OSRAM) |
| NZ (1) | NZ587207A (OSRAM) |
| PE (1) | PE20091371A1 (OSRAM) |
| SG (1) | SG187502A1 (OSRAM) |
| TW (1) | TW200946531A (OSRAM) |
| WO (1) | WO2009097578A1 (OSRAM) |
| ZA (1) | ZA201005435B (OSRAM) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101052122B1 (ko) | 2005-10-25 | 2011-07-26 | 시오노기세야쿠 가부시키가이샤 | 아미노디히드로티아진 유도체 |
| AR061185A1 (es) | 2006-05-26 | 2008-08-13 | Chugai Pharmaceutical Co Ltd | Compuestos heterociclicos como inhibidores de hsp90. composiciones farmaceuticas. |
| ATE553107T1 (de) | 2007-03-01 | 2012-04-15 | Chugai Pharmaceutical Co Ltd | Makrocyclische verbindung |
| EP2147914B1 (en) | 2007-04-24 | 2014-06-04 | Shionogi&Co., Ltd. | Aminodihydrothiazine derivatives substituted with cyclic groups |
| EP2151435A4 (en) | 2007-04-24 | 2011-09-14 | Shionogi & Co | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ALZHEIMER'S DISEASE |
| GB2449293A (en) * | 2007-05-17 | 2008-11-19 | Evotec | Compounds having Hsp90 inhibitory activity |
| MY150596A (en) * | 2008-02-01 | 2014-01-30 | Takeda Pharmaceutical | Hsp90 inhibitors |
| MX2010013256A (es) | 2008-06-13 | 2010-12-21 | Shionogi & Co | Derivado heterociclico que contiene azufre que tiene actividad inhibitoria de beta-secretasa. |
| JPWO2010047372A1 (ja) | 2008-10-22 | 2012-03-22 | 塩野義製薬株式会社 | Bace1阻害活性を有する2−アミノピリミジン−4−オンおよび2−アミノピリジン誘導体 |
| JPWO2011071135A1 (ja) | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | オキサジン誘導体 |
| CA2816285A1 (en) | 2010-10-29 | 2012-05-03 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| EP2634188A4 (en) | 2010-10-29 | 2014-05-07 | Shionogi & Co | FUSIONED AMINODIHYDROPYRIMIDINE DERIVATIVE |
| TW201247635A (en) | 2011-04-26 | 2012-12-01 | Shionogi & Co | Oxazine derivatives and a pharmaceutical composition for inhibiting BAC1 containing them |
| ITTO20111013A1 (it) | 2011-11-03 | 2013-05-04 | Dac Srl | Composti farmaceutici |
| US20130210785A1 (en) | 2012-02-15 | 2013-08-15 | Emory University | Progesterone analogs and uses related thereto |
| JP2016501827A (ja) | 2012-10-24 | 2016-01-21 | 塩野義製薬株式会社 | Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
| US20150320723A1 (en) * | 2013-01-07 | 2015-11-12 | St. Jude Children's Research Hospital | Use of Small Molecule Unfolder Protein Response Modulators to Treat Tumors With Active Sonic Hedgehog (SSH) Signaling Due To Smoothened (SMO) Mutation |
| CA2905509A1 (en) | 2013-03-15 | 2014-09-18 | Memorial Sloan-Kettering Cancer Center | Hsp90-targeted cardiac imaging and therapy |
| ES2886839T3 (es) | 2013-08-12 | 2021-12-21 | Univ Emory | Análogos de fosfato de progesterona y usos relacionados con los mismos |
| CA2961499A1 (en) | 2014-09-17 | 2016-03-24 | Memorial Sloan Kettering Cancer Center | Hsp90-targeted inflammation and infection imaging and therapy |
| US9868738B2 (en) | 2014-09-19 | 2018-01-16 | Merck Sharp & Dohme Corp. | Diazine-fused amidines as BACE inhibitors, compositions, and their use |
| JOP20170083B1 (ar) | 2016-04-07 | 2022-03-14 | Glaxosmithkline Ip Dev Ltd | أميدات هتيروسيكلية مفيدة كمعدلات بروتين |
| CA3061185A1 (en) * | 2017-04-24 | 2018-11-01 | Samus Therapeutics, Inc. | Hsp90 inhibitor oral formulations and related methods |
| CA3065005A1 (en) | 2017-05-26 | 2018-11-29 | Cancer Research Technology Limited | Benzimidazolone derived inhibitors of bcl6 |
| JP2020534285A (ja) | 2017-09-15 | 2020-11-26 | アンパサンド バイオファーマシューティカルズ インコーポレイテッドAmpersand Biopharmaceuticals Inc. | 投与および処置の方法 |
| JP2020534283A (ja) * | 2017-09-15 | 2020-11-26 | アンパサンド バイオファーマシューティカルズ インコーポレイテッドAmpersand Biopharmaceuticals Inc. | システインプロテアーゼのタンパク質阻害剤を介した自然転移の阻害 |
| KR102830237B1 (ko) | 2018-04-13 | 2025-07-07 | 캔써 리서치 테크놀로지 리미티드 | Bcl6 저해제 |
| CN112568222B (zh) * | 2020-04-13 | 2023-04-21 | 辽宁先达农业科学有限公司 | 除草组合物及其应用和除草剂 |
| CN111671749A (zh) * | 2020-06-12 | 2020-09-18 | 重庆医科大学 | 双香豆素在制备HBx蛋白稳定性抑制剂中的用途 |
| CN112661668B (zh) * | 2020-12-31 | 2023-07-28 | 辽宁先达农业科学有限公司 | 一种n-取代酰胺类化合物及其制备方法 |
| CN114259564B (zh) * | 2021-11-30 | 2023-03-14 | 清华大学 | Hsp90抑制剂阻碍stat3线粒体转运和治疗哮喘的新应用 |
| CN115073458A (zh) * | 2022-07-04 | 2022-09-20 | 山东致泰医药技术有限公司 | 一种阿维巴坦钠的制备方法 |
| CN115381816A (zh) * | 2022-08-04 | 2022-11-25 | 武汉市金银潭医院(武汉市传染病医院) | Ver50589在制备抗肠道病毒71型药物中的应用 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| CN117907491B (zh) * | 2024-03-12 | 2024-06-04 | 中国人民解放军军事科学院军事医学研究院 | 基于双衍生化技术的脱碱基位点lc-ms/ms分析方法 |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
Family Cites Families (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1197466B (de) | 1962-03-22 | 1965-07-29 | Thomae Gmbh Dr K | Verfahren zur Herstellung von neuen 5, 6, 7, 8-Tetrahydropyrido-[4, 3-d]pyrimidinen |
| CA762455A (en) | 1962-03-22 | 1967-07-04 | Dr. Karl Thomae Gesellschaft Mit Beschrankter Haftung | Pyrido-pyrimidines |
| GB8912336D0 (en) | 1989-05-30 | 1989-07-12 | Smithkline Beckman Intercredit | Compounds |
| US5679683A (en) * | 1994-01-25 | 1997-10-21 | Warner-Lambert Company | Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family |
| JP2000038350A (ja) | 1998-05-18 | 2000-02-08 | Yoshitomi Pharmaceut Ind Ltd | 糖尿病治療薬 |
| EE200000706A (et) | 1998-05-26 | 2002-06-17 | Warner-Lambert Company | Bitsüklilised pürimidiinid ja bitsüklilised 3,4-dihüdropürimidiinid kui rakkude proliferatsiooni inhibiitorid |
| US6184226B1 (en) | 1998-08-28 | 2001-02-06 | Scios Inc. | Quinazoline derivatives as inhibitors of P-38 α |
| WO2001070229A1 (en) | 2000-03-23 | 2001-09-27 | Merck & Co., Inc. | Thrombin inhibitors |
| US20030229113A1 (en) | 2000-03-24 | 2003-12-11 | Koji Hashimoto | Keratinocyte growth inhibitors and hydroxamic acid derivatives |
| ATE526019T1 (de) | 2000-07-28 | 2011-10-15 | Sloan Kettering Inst Cancer | Verfahren zur behandlung von zellproliferationen störungen und virusinfektionen |
| AU2001280105A1 (en) | 2000-08-22 | 2002-03-04 | Kyowa Hakko Kogyo Co. Ltd. | Methof of regulating apoptosis and apoptosis-regulatory polypeptide |
| EP1335920B1 (en) | 2000-11-02 | 2013-04-03 | Sloan-Kettering Institute For Cancer Research | Compositions containing purine derivatives for binding to hsp90 |
| WO2002069900A2 (en) | 2001-03-01 | 2002-09-12 | Conforma Therapeutics Corp. | Methods for treating genetically-defined proliferative disorders with hsp90 inhibitors |
| KR20020089883A (ko) | 2001-05-25 | 2002-11-30 | 주식회사 지인텍 | 마사지 장치 |
| HUP0700040A2 (en) | 2001-06-28 | 2007-05-29 | Essential Therapeutics | Fused pyrimidines as d-alanyl-d-alanine ligase inhibitors, and process for producing them |
| JP2005139066A (ja) * | 2001-12-14 | 2005-06-02 | Hsp Research Institute Inc | 2、3−ジヒドロ−1h−キノリン−4−オンオキシム誘導体および熱ショック蛋白質発現誘導阻害剤 |
| JPWO2003068776A1 (ja) | 2002-02-15 | 2005-06-02 | 協和醗酵工業株式会社 | [1,2,4]トリアゾロ[1,5−c]ピリミジン誘導体 |
| US7323479B2 (en) | 2002-05-17 | 2008-01-29 | Celgene Corporation | Methods for treatment and management of brain cancer using 1-oxo-2-(2,6-dioxopiperidin-3-yl)-4-methylisoindoline |
| WO2003097615A1 (en) | 2002-05-17 | 2003-11-27 | Scios, Inc. | TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-β INHIBITORS |
| WO2004037978A2 (en) | 2002-10-22 | 2004-05-06 | The Government Of The United States Of America, Represented By The Secretary, Dept. Of Health And Human Services | Methods of reducing the activity of and reducing the concentration of a mutant kit protein |
| EP1457499A1 (en) | 2003-03-12 | 2004-09-15 | Tufts University School Of Medicine | Inhibitors of extracellular Hsp90 |
| US20050020534A1 (en) * | 2003-05-30 | 2005-01-27 | Kosan Biosciences, Inc. | Method for treating diseases using HSP90-inhibiting agents in combination with antimetabolites |
| JPWO2005018674A1 (ja) | 2003-08-22 | 2006-10-19 | 協和醗酵工業株式会社 | イムノグロブリン遺伝子の転座を伴う疾患の治療薬 |
| US20070185007A1 (en) | 2003-09-19 | 2007-08-09 | Haolun Jin | Aza-quinolinol phosphonate integrase inhibitor compounds |
| MXPA06008257A (es) | 2004-01-23 | 2006-08-31 | Amgen Inc | Ligandos del receptor vanilloide y su uso en tratamientos. |
| EP1724268A4 (en) | 2004-02-20 | 2010-04-21 | Kirin Pharma Kk | COMPOUNDS WITH TGF-BETA-HEMMENDER EFFECT AND PHARMACEUTICAL COMPOSITION CONTAINING THEM |
| DE102004041163A1 (de) | 2004-08-25 | 2006-03-02 | Morphochem Aktiengesellschaft für kombinatorische Chemie | Neue Verbindungen mit antibakterieller Aktivität |
| EP1814392A4 (en) | 2004-11-02 | 2008-06-11 | Conforma Therapeutics Corp | METHODS AND COMPOSITIONS FOR TREATING CHRONIC LYMPHOCYTIC LEUKEMIA |
| WO2006050333A2 (en) | 2004-11-02 | 2006-05-11 | The Regents Of The University Of California | Methods and compositions for modulating apoptosis |
| US20080193932A1 (en) | 2004-11-05 | 2008-08-14 | University Of Rochester | Methods Of Inhibiting the Activity of Hsp90 and/or Aryl Hydrocarbon Receptor |
| US20080132510A1 (en) | 2005-01-21 | 2008-06-05 | Bingsong Han | Imidazolylmethyl and Pyrazolylmethyl Heteroaryl Derivatives |
| US8211875B2 (en) | 2005-02-02 | 2012-07-03 | Nexgenix Pharmaceuticals Inc | Local treatment of neurofibromas |
| BRPI0608934A2 (pt) | 2005-04-06 | 2010-02-17 | Irm Llc | compostos e composições contendo diarilamina, e seu uso como moduladores de receptores nucleares de hormÈnios esteróides |
| JP2008536867A (ja) * | 2005-04-14 | 2008-09-11 | ノバルティス ヴァクシンズ アンド ダイアグノスティクス, インコーポレイテッド | 増殖疾患を処置する際に有用なhsp90インヒビターとしての2−アミノ−キナゾリン−5−オン |
| MX2007013595A (es) | 2005-05-04 | 2008-01-24 | Renovis Inc | Compuestos heterociclicos fusionados y composiciones y usos de estos. |
| WO2006124904A2 (en) | 2005-05-16 | 2006-11-23 | Geron Corporation | Cancer treatment by combined inhibition of telomerase and hsp90 activities |
| CA2610828A1 (en) | 2005-06-14 | 2006-12-28 | Schering Corporation | Heterocyclic aspartyl protease inhibitors, preparation and use thereof |
| EP1937258A2 (en) | 2005-09-23 | 2008-07-02 | Conforma Therapeutics Corporation | Anti-tumor methods using multi drug resistance independent synthetic hsp90 inhibitors |
| JO2783B1 (en) * | 2005-09-30 | 2014-03-15 | نوفارتيس ايه جي | Compounds 2-Amino-7, 8-dihydro-6H-Bayredo (3,4-D) Pyrimidine-5-Ones |
| WO2007082131A1 (en) | 2006-01-09 | 2007-07-19 | Bristol-Myers Squibb Company | Process for the preparation of hydroxy substituted heterocycles |
| US7851468B2 (en) | 2006-05-15 | 2010-12-14 | Cephalon, Inc. | Substituted pyrazolo[3,4-d]pyrimidines |
| US7812027B2 (en) | 2006-05-16 | 2010-10-12 | Merck Sharp & Dohme Corp. | Substitued [1,2,4]triazolo[1,5-a]pyrazines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes |
| WO2007139951A2 (en) | 2006-05-25 | 2007-12-06 | Synta Pharmaceuticals Corp. | Method for treating proliferative disorders associated with protooncogene products |
| WO2007143630A2 (en) | 2006-06-02 | 2007-12-13 | Nexgenix Pharmaceuticals | Treatment of neurofibromatosis with hsp90 inhibitors |
| CA2656825C (en) | 2006-06-22 | 2013-12-10 | Prana Biotechnology Limited | Method of treatment and agents useful for same |
| US20080160520A1 (en) | 2006-06-22 | 2008-07-03 | Angelika Amon | Methods and Composition for Diagnosing and Treating Cancer |
| WO2008021981A2 (en) | 2006-08-09 | 2008-02-21 | Nexgenix Pharmaceuticals, Llc. | Local treatment of epidermal and dermal hyperproliferative lesions |
| WO2008045529A1 (en) | 2006-10-12 | 2008-04-17 | Serenex, Inc. | Purine and pyrimidine derivatives for treatment of cancer and inflammatory diseases |
| ES2423029T3 (es) | 2006-11-15 | 2013-09-17 | Genentech, Inc. | Compuestos de arilsulfonamida |
| US20100111943A1 (en) | 2007-03-22 | 2010-05-06 | Medical College Of Georgia Research Institute, Inc | Compositions and methods for inhibiting cancer metastasis |
| GB2449293A (en) * | 2007-05-17 | 2008-11-19 | Evotec | Compounds having Hsp90 inhibitory activity |
| US7928111B2 (en) | 2007-06-08 | 2011-04-19 | Senomyx, Inc. | Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors |
| MY150596A (en) * | 2008-02-01 | 2014-01-30 | Takeda Pharmaceutical | Hsp90 inhibitors |
-
2009
- 2009-01-30 MY MYPI20103648 patent/MY150596A/en unknown
- 2009-01-30 NZ NZ587207A patent/NZ587207A/en not_active IP Right Cessation
- 2009-01-30 GE GEAP200911937A patent/GEP20125718B/en unknown
- 2009-01-30 BR BRPI0906598-9A patent/BRPI0906598A2/pt not_active IP Right Cessation
- 2009-01-30 MX MX2010008269A patent/MX2010008269A/es active IP Right Grant
- 2009-01-30 ES ES09706850.6T patent/ES2475206T3/es active Active
- 2009-01-30 US US12/865,713 patent/US20110053873A1/en not_active Abandoned
- 2009-01-30 CN CN2009801117170A patent/CN101983191B/zh not_active Expired - Fee Related
- 2009-01-30 AU AU2009208947A patent/AU2009208947B2/en not_active Expired - Fee Related
- 2009-01-30 CA CA2713658A patent/CA2713658C/en not_active Expired - Fee Related
- 2009-01-30 KR KR1020107019568A patent/KR20100116206A/ko not_active Abandoned
- 2009-01-30 EA EA201070912A patent/EA019156B1/ru not_active IP Right Cessation
- 2009-01-30 JP JP2010545233A patent/JP5524084B2/ja not_active Expired - Fee Related
- 2009-01-30 US US12/363,640 patent/US8071766B2/en not_active Expired - Fee Related
- 2009-01-30 EP EP09706850.6A patent/EP2252595B1/en active Active
- 2009-01-30 WO PCT/US2009/032728 patent/WO2009097578A1/en not_active Ceased
- 2009-01-30 SG SG2013004676A patent/SG187502A1/en unknown
- 2009-02-02 CL CL2009000228A patent/CL2009000228A1/es unknown
- 2009-02-02 AR ARP090100342A patent/AR071452A1/es not_active Application Discontinuation
- 2009-02-02 TW TW098103333A patent/TW200946531A/zh unknown
- 2009-02-02 PE PE2009000150A patent/PE20091371A1/es not_active Application Discontinuation
-
2010
- 2010-07-26 IL IL207227A patent/IL207227A0/en unknown
- 2010-07-29 ZA ZA2010/05435A patent/ZA201005435B/en unknown
- 2010-07-30 DO DO2010000236A patent/DOP2010000236A/es unknown
- 2010-08-26 MA MA33117A patent/MA32104B1/fr unknown
- 2010-08-30 CR CR11659A patent/CR11659A/es not_active Application Discontinuation
- 2010-08-30 EC EC2010010434A patent/ECSP10010434A/es unknown
-
2011
- 2011-10-11 US US13/271,134 patent/US8618290B2/en not_active Expired - Fee Related
-
2012
- 2012-03-01 US US13/410,045 patent/US20120172321A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2011511003A5 (OSRAM) | ||
| ES2608940T3 (es) | Derivado de bicicloanilina | |
| KR100883289B1 (ko) | 암 치료용5-아미노-2,4,7-트리옥소-3,4,7,8-테트라히드로-2h-피리도[2,3-d]피리미딘 유도체 및 관련 화합물 | |
| RU2619465C2 (ru) | Ингибиторы тирозинкиназы брутона | |
| EP2214669B1 (en) | Cytokine inhibitors | |
| CA2623982A1 (en) | Pyrazolo[1,5-a]pyrimidine compounds as cannabinoid receptor antagonists | |
| FI3932919T3 (fi) | Jak-inhibiittoriyhdiste ja sen käyttö | |
| WO2019043610A1 (en) | NEW SUBSTITUTED SULFONYLUREA DERIVATIVES | |
| JP2018515521A (ja) | ウイルス感染症の治療と予防のための新規置換アミノチアゾロピリミジンジオン | |
| KR20080002963A (ko) | Dna-pk 억제제 | |
| HRP20140437T1 (hr) | Bicikliäśki spojevi i njihove uporabe kao dualnih c-src/jak inhibitora | |
| SK5402003A3 (en) | Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors | |
| RU2011116230A (ru) | Пиразолопиридиновые производные как ингибиторы надфн-оксидазы | |
| JP2007521287A5 (OSRAM) | ||
| JP2008523145A5 (OSRAM) | ||
| HRP20200564T1 (hr) | 1h-pirolo[2,3-c]piridin-7(6h)-oni i pirazolo[3,4-c]piridin-7(6h)-oni kao inhibitori bet proteina | |
| JP2012511501A (ja) | ジヒドロピリミドピリミジン誘導体 | |
| DK3164393T3 (en) | Flavagline derivatives | |
| ES2268154T3 (es) | 6,7-dihidro-5h-pirazolo (1,2-a) pirazol-1-onas espirociclicas que controlan citoquinas inflamatorias. | |
| UA121493C2 (uk) | ІНГІБІТОРИ Kv1.3 ТА ЇХ ЗАСТОСУВАННЯ В МЕДИЦИНІ | |
| RU2014146509A (ru) | Ингибиторы кат ii | |
| CN102617578B (zh) | 一种咪唑衍生物及其医药用途 | |
| ES2356576T3 (es) | Pirazolopirimidinas, un proceso para su preparación y su uso como medicamento. | |
| RU2007130893A (ru) | Производные триазолопиримидина | |
| JP2008007493A (ja) | ピラゾロ[1,5−a]ピリミジン化合物 |