JP2010533160A5 - - Google Patents
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- JP2010533160A5 JP2010533160A5 JP2010515602A JP2010515602A JP2010533160A5 JP 2010533160 A5 JP2010533160 A5 JP 2010533160A5 JP 2010515602 A JP2010515602 A JP 2010515602A JP 2010515602 A JP2010515602 A JP 2010515602A JP 2010533160 A5 JP2010533160 A5 JP 2010533160A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- amino
- phenyl
- alkoxy
- methylmorpholin
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 66
- 125000003545 alkoxy group Chemical group 0.000 claims 24
- -1 nitro, hydroxy Chemical group 0.000 claims 23
- 150000003839 salts Chemical class 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 17
- 125000001475 halogen functional group Chemical group 0.000 claims 16
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 11
- 125000004093 cyano group Chemical group *C#N 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 6
- 125000004452 carbocyclyl group Chemical group 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 241001465754 Metazoa Species 0.000 claims 4
- 125000005236 alkanoylamino group Chemical group 0.000 claims 4
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 4
- 125000005153 alkyl sulfamoyl group Chemical group 0.000 claims 4
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- 125000001589 carboacyl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 230000009422 growth inhibiting effect Effects 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 2
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 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 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims 2
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims 1
- ONMGSCFILROWDA-AWEZNQCLSA-N 1-(2-hydroxyethyl)-3-[4-[4-(2-hydroxypropan-2-yl)-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]thiourea Chemical compound C[C@H]1COCCN1C1=CC(C(C)(C)O)=NC(C=2C=CC(NC(=S)NCCO)=CC=2)=N1 ONMGSCFILROWDA-AWEZNQCLSA-N 0.000 claims 1
- IKTUOUAOGSCKIL-HNNXBMFYSA-N 1-(2-hydroxyethyl)-3-[4-[4-[(3s)-3-methylmorpholin-4-yl]-6-(2-methylsulfonylpropan-2-yl)pyrimidin-2-yl]phenyl]thiourea Chemical compound C[C@H]1COCCN1C1=CC(C(C)(C)S(C)(=O)=O)=NC(C=2C=CC(NC(=S)NCCO)=CC=2)=N1 IKTUOUAOGSCKIL-HNNXBMFYSA-N 0.000 claims 1
- VNUWIQPKVVNUPA-KRWDZBQOSA-N 1-(2-hydroxyethyl)-3-[4-[4-[2-(3-hydroxypropylsulfonyl)propan-2-yl]-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]thiourea Chemical compound C[C@H]1COCCN1C1=CC(C(C)(C)S(=O)(=O)CCCO)=NC(C=2C=CC(NC(=S)NCCO)=CC=2)=N1 VNUWIQPKVVNUPA-KRWDZBQOSA-N 0.000 claims 1
- LKGWPTKBPOHHNP-INIZCTEOSA-N 1-(4-fluorophenyl)-3-[4-[4-[(3s)-3-methylmorpholin-4-yl]-6-(methylsulfonylmethyl)pyrimidin-2-yl]phenyl]thiourea Chemical compound C[C@H]1COCCN1C1=CC(CS(C)(=O)=O)=NC(C=2C=CC(NC(=S)NC=3C=CC(F)=CC=3)=CC=2)=N1 LKGWPTKBPOHHNP-INIZCTEOSA-N 0.000 claims 1
- MKMSWAKWCOVXBQ-KRWDZBQOSA-N 1-(4-methoxyphenyl)-3-[4-[4-[(3s)-3-methylmorpholin-4-yl]-6-(methylsulfonylmethyl)pyrimidin-2-yl]phenyl]thiourea Chemical compound C1=CC(OC)=CC=C1NC(=S)NC1=CC=C(C=2N=C(C=C(CS(C)(=O)=O)N=2)N2[C@H](COCC2)C)C=C1 MKMSWAKWCOVXBQ-KRWDZBQOSA-N 0.000 claims 1
- NOPFSYBMFRVQFJ-KRWDZBQOSA-N 1-[2-(dimethylamino)ethyl]-3-[4-[4-[(3s)-3-methylmorpholin-4-yl]-6-(2-methylsulfonylpropan-2-yl)pyrimidin-2-yl]phenyl]thiourea Chemical compound C[C@H]1COCCN1C1=CC(C(C)(C)S(C)(=O)=O)=NC(C=2C=CC(NC(=S)NCCN(C)C)=CC=2)=N1 NOPFSYBMFRVQFJ-KRWDZBQOSA-N 0.000 claims 1
- MOOWHRZFBWMOQV-ZDUSSCGKSA-N 1-[4-[4-(2-hydroxypropan-2-yl)-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]-3-methylthiourea Chemical compound C1=CC(NC(=S)NC)=CC=C1C1=NC(N2[C@H](COCC2)C)=CC(C(C)(C)O)=N1 MOOWHRZFBWMOQV-ZDUSSCGKSA-N 0.000 claims 1
- TYSOCOFJTDKJAJ-KRWDZBQOSA-N 1-[4-[4-[(3s)-3-methylmorpholin-4-yl]-6-(methylsulfonylmethyl)pyrimidin-2-yl]phenyl]-3-phenylthiourea Chemical compound C[C@H]1COCCN1C1=CC(CS(C)(=O)=O)=NC(C=2C=CC(NC(=S)NC=3C=CC=CC=3)=CC=2)=N1 TYSOCOFJTDKJAJ-KRWDZBQOSA-N 0.000 claims 1
- RCWJOZAZRYSSTL-INIZCTEOSA-N 1-[4-[4-[2-(3-hydroxypropylsulfonyl)propan-2-yl]-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]-3-methylthiourea Chemical compound C1=CC(NC(=S)NC)=CC=C1C1=NC(N2[C@H](COCC2)C)=CC(C(C)(C)S(=O)(=O)CCCO)=N1 RCWJOZAZRYSSTL-INIZCTEOSA-N 0.000 claims 1
- REUGYWKSPAKXGW-IBGZPJMESA-N 1-[4-[4-[2-(benzenesulfonyl)propan-2-yl]-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]-3-(2-hydroxyethyl)thiourea Chemical compound C[C@H]1COCCN1C1=CC(C(C)(C)S(=O)(=O)C=2C=CC=CC=2)=NC(C=2C=CC(NC(=S)NCCO)=CC=2)=N1 REUGYWKSPAKXGW-IBGZPJMESA-N 0.000 claims 1
- IGGDGODNOYOSNH-IBGZPJMESA-N 1-[4-[4-[2-(benzenesulfonyl)propan-2-yl]-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]-3-cyclopropylthiourea Chemical compound C[C@H]1COCCN1C1=CC(C(C)(C)S(=O)(=O)C=2C=CC=CC=2)=NC(C=2C=CC(NC(=S)NC3CC3)=CC=2)=N1 IGGDGODNOYOSNH-IBGZPJMESA-N 0.000 claims 1
- CYTXIRTUVUNJSO-IBGZPJMESA-N 1-[4-[4-[2-(benzenesulfonyl)propan-2-yl]-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]-3-ethylthiourea Chemical compound C1=CC(NC(=S)NCC)=CC=C1C1=NC(N2[C@H](COCC2)C)=CC(C(C)(C)S(=O)(=O)C=2C=CC=CC=2)=N1 CYTXIRTUVUNJSO-IBGZPJMESA-N 0.000 claims 1
- RGGDCCFIVJIXBD-SFHVURJKSA-N 1-[4-[4-[2-(benzenesulfonyl)propan-2-yl]-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]-3-methylthiourea Chemical compound C1=CC(NC(=S)NC)=CC=C1C1=NC(N2[C@H](COCC2)C)=CC(C(C)(C)S(=O)(=O)C=2C=CC=CC=2)=N1 RGGDCCFIVJIXBD-SFHVURJKSA-N 0.000 claims 1
- WICIPQUDAGHUEP-AWEZNQCLSA-N 1-cyclopropyl-3-[4-[4-(2-hydroxypropan-2-yl)-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]thiourea Chemical compound C[C@H]1COCCN1C1=CC(C(C)(C)O)=NC(C=2C=CC(NC(=S)NC3CC3)=CC=2)=N1 WICIPQUDAGHUEP-AWEZNQCLSA-N 0.000 claims 1
- SEHCYWVKUYGYLL-HNNXBMFYSA-N 1-cyclopropyl-3-[4-[4-[(3s)-3-methylmorpholin-4-yl]-6-(2-methylsulfonylpropan-2-yl)pyrimidin-2-yl]phenyl]thiourea Chemical compound C[C@H]1COCCN1C1=CC(C(C)(C)S(C)(=O)=O)=NC(C=2C=CC(NC(=S)NC3CC3)=CC=2)=N1 SEHCYWVKUYGYLL-HNNXBMFYSA-N 0.000 claims 1
- OCIFAFLXUOYULU-AWEZNQCLSA-N 1-cyclopropyl-3-[4-[4-[(3s)-3-methylmorpholin-4-yl]-6-(methylsulfonylmethyl)pyrimidin-2-yl]phenyl]thiourea Chemical compound C[C@H]1COCCN1C1=CC(CS(C)(=O)=O)=NC(C=2C=CC(NC(=S)NC3CC3)=CC=2)=N1 OCIFAFLXUOYULU-AWEZNQCLSA-N 0.000 claims 1
- FYQQFHSCAQTNDC-KRWDZBQOSA-N 1-cyclopropyl-3-[4-[4-[2-(3-hydroxypropylsulfonyl)propan-2-yl]-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]thiourea Chemical compound C[C@H]1COCCN1C1=CC(C(C)(C)S(=O)(=O)CCCO)=NC(C=2C=CC(NC(=S)NC3CC3)=CC=2)=N1 FYQQFHSCAQTNDC-KRWDZBQOSA-N 0.000 claims 1
- GASFVWYGHNKDQU-AWEZNQCLSA-N 1-ethyl-3-[4-[4-(2-hydroxypropan-2-yl)-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]thiourea Chemical compound C1=CC(NC(=S)NCC)=CC=C1C1=NC(N2[C@H](COCC2)C)=CC(C(C)(C)O)=N1 GASFVWYGHNKDQU-AWEZNQCLSA-N 0.000 claims 1
- DUTPGWMWELBIPF-HNNXBMFYSA-N 1-ethyl-3-[4-[4-[(3s)-3-methylmorpholin-4-yl]-6-(2-methylsulfonylpropan-2-yl)pyrimidin-2-yl]phenyl]thiourea Chemical compound C1=CC(NC(=S)NCC)=CC=C1C1=NC(N2[C@H](COCC2)C)=CC(C(C)(C)S(C)(=O)=O)=N1 DUTPGWMWELBIPF-HNNXBMFYSA-N 0.000 claims 1
- UPODFXWDGFKDKN-AWEZNQCLSA-N 1-ethyl-3-[4-[4-[(3s)-3-methylmorpholin-4-yl]-6-(methylsulfonylmethyl)pyrimidin-2-yl]phenyl]thiourea Chemical compound C1=CC(NC(=S)NCC)=CC=C1C1=NC(CS(C)(=O)=O)=CC(N2[C@H](COCC2)C)=N1 UPODFXWDGFKDKN-AWEZNQCLSA-N 0.000 claims 1
- ALGLLMWKQYVQDC-KRWDZBQOSA-N 1-ethyl-3-[4-[4-[2-(3-hydroxypropylsulfonyl)propan-2-yl]-6-[(3s)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]thiourea Chemical compound C1=CC(NC(=S)NCC)=CC=C1C1=NC(N2[C@H](COCC2)C)=CC(C(C)(C)S(=O)(=O)CCCO)=N1 ALGLLMWKQYVQDC-KRWDZBQOSA-N 0.000 claims 1
- JDWWSSNJYPSCJU-AWEZNQCLSA-N 1-methyl-3-[4-[4-[(3s)-3-methylmorpholin-4-yl]-6-(2-methylsulfonylpropan-2-yl)pyrimidin-2-yl]phenyl]thiourea Chemical compound C1=CC(NC(=S)NC)=CC=C1C1=NC(N2[C@H](COCC2)C)=CC(C(C)(C)S(C)(=O)=O)=N1 JDWWSSNJYPSCJU-AWEZNQCLSA-N 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000005302 thiazolylmethyl group Chemical group [H]C1=C([H])N=C(S1)C([H])([H])* 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000005301 thienylmethyl group Chemical group [H]C1=C([H])C([H])=C(S1)C([H])([H])* 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94853907P | 2007-07-09 | 2007-07-09 | |
| US60/948,539 | 2007-07-09 | ||
| PCT/GB2008/050548 WO2009007750A1 (en) | 2007-07-09 | 2008-07-08 | Morpholino pyrimidine derivatives used in diseases linked to mtor kinase and/or pi3k |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010533160A JP2010533160A (ja) | 2010-10-21 |
| JP2010533160A5 true JP2010533160A5 (cg-RX-API-DMAC10.html) | 2012-08-16 |
| JP5508260B2 JP5508260B2 (ja) | 2014-05-28 |
Family
ID=39791229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010515602A Expired - Fee Related JP5508260B2 (ja) | 2007-07-09 | 2008-07-08 | ｍＴＯＲキナーゼおよび／またはＰ１３Ｋに関連する病気に用いられるモルホリノピリミジン誘導体 |
Country Status (21)
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20100031639A (ko) * | 2007-07-09 | 2010-03-23 | 아스트라제네카 아베 | 증식성 질환의 치료용 삼중 치환된 피리미딘 유도체 |
| MX315904B (es) | 2008-05-30 | 2013-11-29 | Amgen Inc | Inhibidores de fosfoinosituro-3 cinasa. |
| US8785457B2 (en) | 2009-03-13 | 2014-07-22 | Cellzome Limited | Pyrimidine derivatives as mTOR inhibitors |
| UY32582A (es) | 2009-04-28 | 2010-11-30 | Amgen Inc | Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero |
| EA021088B1 (ru) | 2009-07-02 | 2015-04-30 | Санофи | Производные (6-оксо-1,6-дигидропиримидин-2-ил)амида, их получение и их фармацевтическое применение в качестве ингибиторов фосфорилирования akt (pkb) |
| EP2448932B1 (fr) | 2009-07-02 | 2014-03-05 | Sanofi | Nouveaux derives de 6-morpholin-4-yl-pyrimidin-4-(3h)-one, leur preparation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb) |
| PH12012500809A1 (en) | 2009-10-30 | 2012-11-26 | Ariad Pharma Inc | Methods and compositions for treating cancer |
| JP6114554B2 (ja) | 2010-02-03 | 2017-04-12 | シグナル ファーマシューティカルズ，エルエルシー | Ｔｏｒキナーゼ阻害剤に対する感受性についての予測的なバイオマーカーとしてのｌｋｂ１変異の同定 |
| WO2011107585A1 (en) | 2010-03-04 | 2011-09-09 | Cellzome Limited | Morpholino substituted urea derivatives as mtor inhibitors |
| JO2998B1 (ar) | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
| HUE030393T2 (en) | 2010-12-28 | 2017-05-29 | Sanofi Sa | New pyrimidine derivatives, a process for their preparation, and their pharmaceutical use as inhibitors of AKT (PKB) phosphorylation |
| JP2014510122A (ja) | 2011-04-04 | 2014-04-24 | セルゾーム リミテッド | ｍＴＯＲ阻害剤としてのジヒドロピロロピリミジン誘導体 |
| CN117205331A (zh) | 2011-04-29 | 2023-12-12 | 西莱克塔生物科技公司 | 用于降低抗体应答的致耐受性合成纳米载体 |
| CA2843887A1 (en) | 2011-08-03 | 2013-02-07 | Signal Pharmaceuticals, Llc | Identification of gene expression profile as a predictive biomarker for lkb1 status |
| CA2849189A1 (en) | 2011-09-21 | 2013-03-28 | Cellzome Limited | Morpholino substituted urea or carbamate derivatives as mtor inhibitors |
| JP6093770B2 (ja) | 2011-09-27 | 2017-03-08 | アムジエン・インコーポレーテツド | 癌の治療のためのｍｄｍ２阻害剤としての複素環化合物 |
| CN103946222B (zh) | 2011-10-07 | 2016-12-28 | 塞尔佐姆有限公司 | 作为mtor抑制剂的吗啉代取代的双环嘧啶脲或氨基甲酸衍生物 |
| HUE030858T2 (en) | 2012-07-04 | 2017-06-28 | Hoffmann La Roche | Covalently linked antigen-antibody conjugates |
| FR2994572B1 (fr) * | 2012-08-17 | 2015-04-17 | Centre Nat Rech Scient | Pyrido[3,2-d]pyrimidines trisubstituees, leurs procedes de preparation et leurs utilisation en therapeutique |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| US20160002185A1 (en) * | 2013-02-19 | 2016-01-07 | Amgen Inc. | Cis-morpholinone and other compounds as mdm2 inhibitors for the treatment of cancer |
| US11407721B2 (en) | 2013-02-19 | 2022-08-09 | Amgen Inc. | CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer |
| MX374513B (es) | 2013-03-14 | 2025-03-06 | Amgen Inc | Compuestos de morfolinona de ácido heteroarilo como inhibidores mdm2 para el tratamiento de cáncer. |
| MX377267B (es) | 2013-04-17 | 2025-03-07 | Signal Pharm Llc | Tratamiento de cáncer con dihidropirazino-pirazinas. |
| TWI631949B (zh) | 2013-04-17 | 2018-08-11 | 標誌製藥公司 | 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法 |
| TW201521725A (zh) | 2013-04-17 | 2015-06-16 | Signal Pharm Llc | 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法 |
| JP6382946B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ，エルエルシー | ジヒドロピラジノ−ピラジンによる癌治療 |
| SG10201708111YA (en) | 2013-04-17 | 2017-11-29 | Signal Pharm Llc | Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer |
| WO2014172436A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer |
| CA2909629C (en) | 2013-04-17 | 2022-12-13 | Signal Pharmaceuticals, Llc | Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one |
| US10668053B2 (en) | 2013-05-03 | 2020-06-02 | Selecta Biosciences, Inc. | Tolerogenic synthetic nanocarriers to reduce or prevent anaphylaxis in response to a non-allergenic antigen |
| CA3143529A1 (en) | 2013-05-29 | 2014-12-04 | Signal Pharmaceuticals, Llc | Pharmaceutical compositions 0f 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use |
| JOP20200296A1 (ar) | 2013-06-10 | 2017-06-16 | Amgen Inc | عمليات صنع وأشكال بلورية من mdm2 مثبط |
| RU2693438C2 (ru) | 2014-01-03 | 2019-07-02 | Ф. Хоффманн-Ля Рош Аг | Биспецифичные антитела против гаптена/против рецептора гематоэнцефалического барьера, их комплексы и их применение в качестве челноков гематоэнцефалического барьера |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| EP3131551A4 (en) | 2014-04-16 | 2017-09-20 | Signal Pharmaceuticals, LLC | SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF |
| EP3164419B1 (en) | 2014-06-26 | 2024-07-24 | F. Hoffmann-La Roche AG | Anti-brdu antibodies and methods of use |
| CA2957046C (en) | 2014-08-04 | 2022-11-15 | Nuevolution A/S | Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases |
| KR102692773B1 (ko) | 2014-09-07 | 2024-08-08 | 셀렉타 바이오사이언시즈, 인크. | 유전자 편집 항-바이러스 전달 벡터 면역 반응을 약화시키기 위한 방법 및 조성물 |
| TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201815787A (zh) | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| HUE072005T2 (hu) | 2017-03-11 | 2025-10-28 | Cartesian Therapeutics Inc | Gyulladásgátlókkal és immunszupresszánst tartalmazó szintetikus nanohordozókkal történõ kombinált kezeléssel összefüggõ eljárások és készítmények |
| EP3630116B1 (en) | 2017-05-26 | 2024-05-01 | The Board Of Regents Of The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase |
| BR112019027402A2 (pt) | 2017-06-22 | 2020-07-07 | Celgene Corporation | tratamento de carcinoma hepatocelular caracterizado por infecção pelo vírus da hepatite b |
| IL271930B (en) | 2017-07-13 | 2022-07-01 | Univ Texas | Heterocyclic inhibitors of atr kinase |
| US10800774B2 (en) | 2017-08-17 | 2020-10-13 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of ATR kinase |
| CN112218631B (zh) | 2018-03-16 | 2023-12-22 | 德州大学系统董事会 | Atr激酶的杂环抑制剂 |
| US11685727B2 (en) | 2019-12-20 | 2023-06-27 | Nuevolution A/S | Compounds active towards nuclear receptors |
| WO2021124277A1 (en) | 2019-12-20 | 2021-06-24 | Nuevolution A/S | Compounds active towards nuclear receptors |
| EP4126874A1 (en) | 2020-03-31 | 2023-02-08 | Nuevolution A/S | Compounds active towards nuclear receptors |
| AU2021249530A1 (en) | 2020-03-31 | 2022-12-01 | Nuevolution A/S | Compounds active towards nuclear receptors |
| CN111646985A (zh) * | 2020-06-01 | 2020-09-11 | 江苏集萃分子工程研究院有限公司 | 一种含嘧啶杂环抗肿瘤药物分子azd6738的合成方法 |
| TW202337494A (zh) | 2021-11-16 | 2023-10-01 | 美商建南德克公司 | 用莫蘇妥珠單抗治療全身性紅斑狼瘡（ｓｌｅ）之方法及組成物 |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3922735A1 (de) | 1989-07-11 | 1991-01-24 | Hoechst Ag | Aminopyrimidin-derivate, verfahren zu ihrer herstellung, sie enthaltende mittel und ihre verwendung als fungizide |
| KR100774855B1 (ko) | 2000-04-27 | 2007-11-08 | 아스텔라스세이야쿠 가부시키가이샤 | 축합 헤테로아릴 유도체 |
| JP3810017B2 (ja) * | 2000-04-27 | 2006-08-16 | アステラス製薬株式会社 | 縮合ヘテロアリール誘導体 |
| WO2002038551A1 (en) | 2000-11-10 | 2002-05-16 | F. Hoffman-La Roche Ag | Pyrimidine derivatives and their use as neuropeptide y receptor ligands |
| EP2316831B1 (en) | 2002-11-21 | 2013-03-06 | Novartis AG | 2-(morpholin-4-yl)pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer |
| TW200510394A (en) | 2003-05-29 | 2005-03-16 | Synta Pharmaceuticals Corp | Heterocyclic compounds for preventing and treating disorders associated with excessive bone loss |
| GB0415365D0 (en) * | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0415364D0 (en) * | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0415367D0 (en) | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| US7772271B2 (en) | 2004-07-14 | 2010-08-10 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| WO2007084413A2 (en) | 2004-07-14 | 2007-07-26 | Ptc Therapeutics, Inc. | Methods for treating hepatitis c |
| EP1819341A4 (en) * | 2004-11-10 | 2011-06-29 | Synta Pharmaceuticals Corp | IL-12 MODULATORY CONNECTIONS |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| WO2006124662A1 (en) | 2005-05-13 | 2006-11-23 | Synta Pharmaceuticals Corp. | Il-12 modulatory compounds |
| CA2608726C (en) | 2005-05-20 | 2013-07-09 | Methylgene Inc. | Inhibitors of vegf receptor and hgf receptor signaling |
| DE102005024494A1 (de) | 2005-05-27 | 2006-11-30 | Bayer Healthcare Ag | Verwendung von Cyanopyrimidinen |
| EP1899329B1 (en) | 2005-07-01 | 2011-10-05 | Irm Llc | Pyrimidine-substituted benzimidazole derivatives as protein kinase inhibitors |
| US20100160255A1 (en) | 2005-07-29 | 2010-06-24 | Takeda Pharmaceutical Company Limited | Spiro-cyclic compound |
| BRPI0615781A2 (pt) | 2005-09-01 | 2009-06-16 | Array Biopharma Inc | compostos inibidores de raf e métodos de uso destes |
| JP2007091649A (ja) | 2005-09-29 | 2007-04-12 | Taisho Pharmaceut Co Ltd | ピリミジン誘導体及びその使用に関連する治療方法 |
| JP4531027B2 (ja) | 2005-09-29 | 2010-08-25 | 田辺三菱製薬株式会社 | 医薬組成物 |
| EP1931674B1 (en) | 2005-09-30 | 2012-12-12 | Vertex Pharmaceuticals Incorporated | Deazapurines useful as inhibitors of janus kinases |
| ES2535854T3 (es) | 2005-09-30 | 2015-05-18 | Miikana Therapeutics, Inc. | Compuestos de pirazol sustituidos |
| GB0520657D0 (en) | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
| GB2431156A (en) | 2005-10-11 | 2007-04-18 | Piramed Ltd | 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase |
| EP1945631B8 (en) | 2005-10-28 | 2013-01-02 | AstraZeneca AB | 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer |
| US20100016319A1 (en) | 2005-11-29 | 2010-01-21 | Toray Industries, Inc. A Corporation Of Japan | Arylmethylene urea derivative and use thereof |
| GB0525083D0 (en) * | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0525080D0 (en) | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| GB0525081D0 (en) | 2005-12-09 | 2006-01-18 | Astrazeneca Ab | Pyrimidine derivatives |
| NL2000323C2 (nl) | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine-derivaten. |
| EP1979325A1 (en) | 2006-01-11 | 2008-10-15 | AstraZeneca AB | Morpholino pyrimidine derivatives and their use in therapy |
| JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| CA2640398A1 (en) | 2006-01-30 | 2007-08-09 | Exelixis, Inc. | 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as jak-2 modulators and pharmaceutical compositions containing them |
| EP2008210A1 (en) | 2006-03-15 | 2008-12-31 | Csir | Modulation of phosphoryl transferase activity of glutamine synthetase |
| JP5243696B2 (ja) | 2006-03-17 | 2013-07-24 | 田辺三菱製薬株式会社 | ベンゼン誘導体 |
| JPWO2007114323A1 (ja) | 2006-04-04 | 2009-08-20 | 大正製薬株式会社 | アミノピロリジン化合物 |
| KR20080110912A (ko) | 2006-04-19 | 2008-12-19 | 노파르티스 아게 | 인다졸 화합물 및 ｃｄｃ７의 억제 방법 |
| WO2007126043A1 (ja) | 2006-04-27 | 2007-11-08 | Mitsubishi Tanabe Pharma Corporation | チアゾール環を含むカルボン酸誘導体の医薬用途 |
| GB0610909D0 (en) | 2006-06-05 | 2006-07-12 | Merck Sharp & Dohme | Therapeutic treatment |
| AU2007269540B2 (en) | 2006-07-05 | 2013-06-27 | Exelixis, Inc. | Methods of using IGF1R and Abl kinase modulators |
| KR101435231B1 (ko) * | 2006-08-24 | 2014-10-02 | 아스트라제네카 아베 | 증식성 질환의 치료에 유용한 모르폴리노 피리미딘 유도체 |
| EP2057129A1 (en) * | 2006-08-24 | 2009-05-13 | AstraZeneca AB | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| US20080234262A1 (en) * | 2007-03-21 | 2008-09-25 | Wyeth | Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors |
| EP2146981A1 (en) | 2007-04-12 | 2010-01-27 | F. Hoffmann-Roche AG | Pharmaceutical compounds |
| AU2008273892A1 (en) | 2007-07-09 | 2009-01-15 | Astrazeneca Ab | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
-
2008
- 2008-07-08 US US12/668,056 patent/US8138183B2/en not_active Expired - Fee Related
- 2008-07-08 KR KR1020107002942A patent/KR20100042280A/ko not_active Ceased
- 2008-07-08 BR BRPI0814688A patent/BRPI0814688A2/pt not_active IP Right Cessation
- 2008-07-08 WO PCT/GB2008/050548 patent/WO2009007750A1/en not_active Ceased
- 2008-07-08 EP EP08776183A patent/EP2176238B1/en active Active
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- 2008-07-08 EA EA201000091A patent/EA018708B1/ru not_active IP Right Cessation
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- 2008-07-08 AU AU2008273891A patent/AU2008273891B2/en not_active Ceased
- 2008-12-19 PE PE2008002157A patent/PE20100138A1/es not_active Application Discontinuation
- 2008-12-30 AR ARP080105784A patent/AR070079A1/es unknown
- 2008-12-30 CL CL2008003940A patent/CL2008003940A1/es unknown
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- 2009-12-23 ZA ZA2009/09224A patent/ZA200909224B/en unknown
-
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- 2010-01-08 DO DO2010000012A patent/DOP2010000012A/es unknown
- 2010-01-08 CR CR11200A patent/CR11200A/es not_active Application Discontinuation
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- 2010-02-09 CO CO10014081A patent/CO6251364A2/es not_active Application Discontinuation