JP2015536306A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2015536306A5 JP2015536306A5 JP2015536951A JP2015536951A JP2015536306A5 JP 2015536306 A5 JP2015536306 A5 JP 2015536306A5 JP 2015536951 A JP2015536951 A JP 2015536951A JP 2015536951 A JP2015536951 A JP 2015536951A JP 2015536306 A5 JP2015536306 A5 JP 2015536306A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- methyl
- phenyl
- carbonyl
- benzenesulfonamide
- 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 C 1-6 alkyl-OH Chemical group 0.000 claims description 67
- 150000001875 compounds Chemical class 0.000 claims description 45
- 125000000217 alkyl group Chemical group 0.000 claims description 42
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 40
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 29
- 230000035772 mutation Effects 0.000 claims description 20
- 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 description 20
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 19
- 125000000623 heterocyclic group Chemical group 0.000 claims description 18
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 18
- 125000003118 aryl group Chemical group 0.000 claims description 16
- 239000000203 mixture Substances 0.000 claims description 15
- 206010028980 Neoplasm Diseases 0.000 claims description 13
- 201000011510 cancer Diseases 0.000 claims description 13
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 101000599886 Homo sapiens Isocitrate dehydrogenase [NADP], mitochondrial Proteins 0.000 claims description 10
- 102100037845 Isocitrate dehydrogenase [NADP], mitochondrial Human genes 0.000 claims description 10
- 101001042041 Bos taurus Isocitrate dehydrogenase [NAD] subunit beta, mitochondrial Proteins 0.000 claims description 9
- 101000960234 Homo sapiens Isocitrate dehydrogenase [NADP] cytoplasmic Proteins 0.000 claims description 9
- 102100039905 Isocitrate dehydrogenase [NADP] cytoplasmic Human genes 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 9
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 8
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 8
- 125000005843 halogen group Chemical group 0.000 claims description 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 7
- OEYGXEYESNDHQS-UHFFFAOYSA-N 1-(2-methyl-5-piperidin-1-ylsulfonylphenyl)-3-(3,5,7-trimethyl-1-adamantyl)urea Chemical compound C1=C(NC(=O)NC23CC4(C)CC(C)(CC(C4)(C)C2)C3)C(C)=CC=C1S(=O)(=O)N1CCCCC1 OEYGXEYESNDHQS-UHFFFAOYSA-N 0.000 claims description 6
- CYCFHZPFMAXQRB-UHFFFAOYSA-N 1-(4-chlorophenyl)-3-[5-morpholin-4-ylsulfonyl-2-(2-oxopyrrolidin-1-yl)phenyl]urea Chemical compound C1=CC(Cl)=CC=C1NC(=O)NC1=CC(S(=O)(=O)N2CCOCC2)=CC=C1N1C(=O)CCC1 CYCFHZPFMAXQRB-UHFFFAOYSA-N 0.000 claims description 6
- JADAACJWFPKJSC-UHFFFAOYSA-N 1-[2-(diethylamino)-5-morpholin-4-ylsulfonylphenyl]-3-(3-methylphenyl)urea Chemical compound CCN(CC)C1=CC=C(S(=O)(=O)N2CCOCC2)C=C1NC(=O)NC1=CC=CC(C)=C1 JADAACJWFPKJSC-UHFFFAOYSA-N 0.000 claims description 6
- RSIFRBLCVZDPFI-UHFFFAOYSA-N 1-[3-(azepan-1-ylsulfonyl)-4-methylphenyl]-3-[2-(3-prop-1-en-2-ylphenyl)propan-2-yl]urea Chemical compound CC(=C)C1=CC=CC(C(C)(C)NC(=O)NC=2C=C(C(C)=CC=2)S(=O)(=O)N2CCCCCC2)=C1 RSIFRBLCVZDPFI-UHFFFAOYSA-N 0.000 claims description 6
- GUNQZZMJRXGITI-UHFFFAOYSA-N 1-[3-[(2-methoxyphenyl)sulfamoyl]-4-piperidin-1-ylphenyl]-3-[2-(3-prop-1-en-2-ylphenyl)propan-2-yl]urea Chemical compound COC1=CC=CC=C1NS(=O)(=O)C1=CC(NC(=O)NC(C)(C)C=2C=C(C=CC=2)C(C)=C)=CC=C1N1CCCCC1 GUNQZZMJRXGITI-UHFFFAOYSA-N 0.000 claims description 6
- AQEFBMVFUWQQGA-UHFFFAOYSA-N 1-[3-[(3-chlorophenyl)sulfamoyl]-4-methylphenyl]-3-[2-(3-prop-1-en-2-ylphenyl)propan-2-yl]urea Chemical compound CC(=C)C1=CC=CC(C(C)(C)NC(=O)NC=2C=C(C(C)=CC=2)S(=O)(=O)NC=2C=C(Cl)C=CC=2)=C1 AQEFBMVFUWQQGA-UHFFFAOYSA-N 0.000 claims description 6
- JMMZFYORIQSJKO-UHFFFAOYSA-N 1-[4-(diethylamino)-3-[(2-methoxyphenyl)sulfamoyl]phenyl]-3-[2-(3-prop-1-en-2-ylphenyl)propan-2-yl]urea Chemical compound C1=C(S(=O)(=O)NC=2C(=CC=CC=2)OC)C(N(CC)CC)=CC=C1NC(=O)NC(C)(C)C1=CC=CC(C(C)=C)=C1 JMMZFYORIQSJKO-UHFFFAOYSA-N 0.000 claims description 6
- XOFACLCJHFUIDE-UHFFFAOYSA-N 1-[4-chloro-3-[(4-ethoxyphenyl)sulfamoyl]phenyl]-3-[2-(3-prop-1-en-2-ylphenyl)propan-2-yl]urea Chemical compound C1=CC(OCC)=CC=C1NS(=O)(=O)C1=CC(NC(=O)NC(C)(C)C=2C=C(C=CC=2)C(C)=C)=CC=C1Cl XOFACLCJHFUIDE-UHFFFAOYSA-N 0.000 claims description 6
- VAZOYARPRLVOKK-UHFFFAOYSA-N 1-[5-(butylsulfamoyl)-2-methoxyphenyl]-3-[4-[6-(morpholin-4-ylmethyl)pyridin-3-yl]naphthalen-1-yl]urea Chemical compound CCCCNS(=O)(=O)C1=CC=C(OC)C(NC(=O)NC=2C3=CC=CC=C3C(C=3C=NC(CN4CCOCC4)=CC=3)=CC=2)=C1 VAZOYARPRLVOKK-UHFFFAOYSA-N 0.000 claims description 6
- HRKRDXGIYSURLR-UHFFFAOYSA-N 1-[5-[(2,5-dichlorophenyl)sulfamoyl]-2-(diethylamino)phenyl]-3-(4-nitrophenyl)urea Chemical compound CCN(CC)C1=CC=C(S(=O)(=O)NC=2C(=CC=C(Cl)C=2)Cl)C=C1NC(=O)NC1=CC=C([N+]([O-])=O)C=C1 HRKRDXGIYSURLR-UHFFFAOYSA-N 0.000 claims description 6
- JDUBSDSPWVKMFO-UHFFFAOYSA-N 1-[5-[3-[2,4-bis(2-methylbutan-2-yl)phenoxy]propylsulfamoyl]-2-chlorophenyl]-3-(3,5-dichloro-2-hydroxy-4-methylphenyl)urea Chemical compound CCC(C)(C)C1=CC(C(C)(C)CC)=CC=C1OCCCNS(=O)(=O)C1=CC=C(Cl)C(NC(=O)NC=2C(=C(Cl)C(C)=C(Cl)C=2)O)=C1 JDUBSDSPWVKMFO-UHFFFAOYSA-N 0.000 claims description 6
- DVNJUHFYDMTVCU-UHFFFAOYSA-N 1-[5-[[4-[bis(2-hydroxyethyl)amino]-2-methylphenyl]methylidene]-2-phenylimidazol-4-yl]-3-[5-(hexadecylsulfamoyl)-2-methoxyphenyl]urea Chemical compound CCCCCCCCCCCCCCCCNS(=O)(=O)C1=CC=C(OC)C(NC(=O)NC=2C(N=C(N=2)C=2C=CC=CC=2)=CC=2C(=CC(=CC=2)N(CCO)CCO)C)=C1 DVNJUHFYDMTVCU-UHFFFAOYSA-N 0.000 claims description 6
- GSPWDUPQFBOLPX-UHFFFAOYSA-N 1-[6-[4-[bis(2-cyanoethyl)amino]-2-methylphenyl]imino-3,4-dicyano-5-(trifluoromethyl)pyrrolo[1,2-b]pyrazol-2-yl]-3-[2-chloro-5-(hexadecylsulfamoyl)phenyl]urea Chemical compound CCCCCCCCCCCCCCCCNS(=O)(=O)c1ccc(Cl)c(NC(=O)Nc2nn3C(=Nc4ccc(cc4C)N(CCC#N)CCC#N)C(=C(C#N)c3c2C#N)C(F)(F)F)c1 GSPWDUPQFBOLPX-UHFFFAOYSA-N 0.000 claims description 6
- KRYZQVQMDSSVHM-UHFFFAOYSA-N 3-(4-chloro-3-pyrrolidin-1-ylsulfonylphenyl)-1-methyl-1-[(2-methyl-1,3-thiazol-5-yl)methyl]urea Chemical compound C=1C=C(Cl)C(S(=O)(=O)N2CCCC2)=CC=1NC(=O)N(C)CC1=CN=C(C)S1 KRYZQVQMDSSVHM-UHFFFAOYSA-N 0.000 claims description 6
- YLOIWATYZNZGIC-UHFFFAOYSA-N 3-(4-methoxy-3-piperidin-1-ylsulfonylphenyl)-1-methyl-1-[(2-methyl-1,3-thiazol-5-yl)methyl]urea Chemical compound C1=C(S(=O)(=O)N2CCCCC2)C(OC)=CC=C1NC(=O)N(C)CC1=CN=C(C)S1 YLOIWATYZNZGIC-UHFFFAOYSA-N 0.000 claims description 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 6
- SNRUBQQJIBEYMU-UHFFFAOYSA-N Dodecane Natural products CCCCCCCCCCCC SNRUBQQJIBEYMU-UHFFFAOYSA-N 0.000 claims description 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 6
- 125000003438 dodecyl 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])C([H])([H])C([H])([H])* 0.000 claims description 6
- LDZOUHCRTQBWTF-UHFFFAOYSA-O n-[4-[[5-[3-(4-butyl-3,5-dimethylpyridin-1-ium-1-yl)propylcarbamoylamino]-2-chlorophenyl]sulfonylamino]anilino]formamide Chemical compound C1=C(C)C(CCCC)=C(C)C=[N+]1CCCNC(=O)NC1=CC=C(Cl)C(S(=O)(=O)NC=2C=CC(NNC=O)=CC=2)=C1 LDZOUHCRTQBWTF-UHFFFAOYSA-O 0.000 claims description 6
- IJAIFRUQXADQJV-UHFFFAOYSA-N n-[4-[[5-[3-(4-butyl-3,5-dimethylpyridin-1-ium-1-yl)propylcarbamoylamino]-2-chlorophenyl]sulfonylamino]anilino]formamide;chloride Chemical compound [Cl-].C1=C(C)C(CCCC)=C(C)C=[N+]1CCCNC(=O)NC1=CC=C(Cl)C(S(=O)(=O)NC=2C=CC(NNC=O)=CC=2)=C1 IJAIFRUQXADQJV-UHFFFAOYSA-N 0.000 claims description 6
- RIHISJPMISXXNE-UHFFFAOYSA-N n-[5-chloro-3-[[4-chloro-3-(dodecylsulfamoyl)phenyl]carbamoylamino]-2-hydroxyphenyl]acetamide Chemical compound C1=C(Cl)C(S(=O)(=O)NCCCCCCCCCCCC)=CC(NC(=O)NC=2C(=C(NC(C)=O)C=C(Cl)C=2)O)=C1 RIHISJPMISXXNE-UHFFFAOYSA-N 0.000 claims description 6
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 6
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 4
- HWXBTNAVRSUOJR-UHFFFAOYSA-N 2-hydroxyglutaric acid Chemical compound OC(=O)C(O)CCC(O)=O HWXBTNAVRSUOJR-UHFFFAOYSA-N 0.000 claims description 4
- CTJVLIALFREFQS-UHFFFAOYSA-N 3-(4-ethoxy-3-pyrrolidin-1-ylsulfonylphenyl)-1-methyl-1-(4-methylcyclohexyl)urea Chemical compound C1=C(S(=O)(=O)N2CCCC2)C(OCC)=CC=C1NC(=O)N(C)C1CCC(C)CC1 CTJVLIALFREFQS-UHFFFAOYSA-N 0.000 claims description 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 4
- 208000005243 Chondrosarcoma Diseases 0.000 claims description 4
- 108090000790 Enzymes Proteins 0.000 claims description 4
- 102000004190 Enzymes Human genes 0.000 claims description 4
- 208000032612 Glial tumor Diseases 0.000 claims description 4
- 206010018338 Glioma Diseases 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 4
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 4
- 230000001419 dependent effect Effects 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 208000005017 glioblastoma Diseases 0.000 claims description 4
- 239000001257 hydrogen Substances 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 102200116484 rs121913502 Human genes 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 2
- 206010004593 Bile duct cancer Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 206010039491 Sarcoma Diseases 0.000 claims description 2
- 125000004104 aryloxy group Chemical group 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 125000003725 azepanyl group Chemical group 0.000 claims description 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 2
- 102200069708 rs121913499 Human genes 0.000 claims description 2
- 102200069690 rs121913500 Human genes 0.000 claims description 2
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims description 2
- 125000005309 thioalkoxy group Chemical group 0.000 claims description 2
- 125000004001 thioalkyl group Chemical group 0.000 claims description 2
- 230000002792 vascular Effects 0.000 claims description 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 description 12
- KNPYUBYMGCLBEJ-UHFFFAOYSA-N 1-[5-(azepan-1-ylsulfonyl)-2-chlorophenyl]-3-(4-nitrophenyl)urea Chemical compound C1=CC([N+](=O)[O-])=CC=C1NC(=O)NC1=CC(S(=O)(=O)N2CCCCCC2)=CC=C1Cl KNPYUBYMGCLBEJ-UHFFFAOYSA-N 0.000 description 3
- KPGXRSRHYNQIFN-UHFFFAOYSA-N 2-oxoglutaric acid Chemical compound OC(=O)CCC(=O)C(O)=O KPGXRSRHYNQIFN-UHFFFAOYSA-N 0.000 description 1
- 208000029742 colonic neoplasm Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261714179P | 2012-10-15 | 2012-10-15 | |
| US61/714,179 | 2012-10-15 | ||
| PCT/US2013/064601 WO2014062511A1 (en) | 2012-10-15 | 2013-10-11 | Therapeutic compounds and compositions |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018130743A Division JP2018199677A (ja) | 2012-10-15 | 2018-07-10 | 治療化合物および組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015536306A JP2015536306A (ja) | 2015-12-21 |
| JP2015536306A5 true JP2015536306A5 (cg-RX-API-DMAC7.html) | 2016-11-24 |
| JP6385352B2 JP6385352B2 (ja) | 2018-09-05 |
Family
ID=50488660
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015536951A Expired - Fee Related JP6385352B2 (ja) | 2012-10-15 | 2013-10-11 | 治療化合物および組成物 |
| JP2018130743A Withdrawn JP2018199677A (ja) | 2012-10-15 | 2018-07-10 | 治療化合物および組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018130743A Withdrawn JP2018199677A (ja) | 2012-10-15 | 2018-07-10 | 治療化合物および組成物 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US10202339B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2906212A4 (cg-RX-API-DMAC7.html) |
| JP (2) | JP6385352B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN104822373B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2013331626B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2888360A1 (cg-RX-API-DMAC7.html) |
| HK (1) | HK1213798A1 (cg-RX-API-DMAC7.html) |
| MX (1) | MX365747B (cg-RX-API-DMAC7.html) |
| NZ (1) | NZ706999A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2014062511A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2448582T (pt) | 2009-06-29 | 2017-07-10 | Agios Pharmaceuticals Inc | Compostos e composições terapêuticas |
| CN102827170A (zh) | 2011-06-17 | 2012-12-19 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
| US9474779B2 (en) | 2012-01-19 | 2016-10-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compositions and their methods of use |
| US9579324B2 (en) | 2013-07-11 | 2017-02-28 | Agios Pharmaceuticals, Inc | Therapeutically active compounds and their methods of use |
| WO2015003355A2 (en) | 2013-07-11 | 2015-01-15 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| US10376510B2 (en) | 2013-07-11 | 2019-08-13 | Agios Pharmaceuticals, Inc. | 2,4- or 4,6-diaminopyrimidine compounds as IDH2 mutants inhibitors for the treatment of cancer |
| WO2015003360A2 (en) | 2013-07-11 | 2015-01-15 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| US20150031627A1 (en) | 2013-07-25 | 2015-01-29 | Agios Pharmaceuticals, Inc | Therapeutically active compounds and their methods of use |
| CN112159391A (zh) | 2014-03-14 | 2021-01-01 | 阿吉奥斯制药公司 | 治疗活性化合物的药物组合物 |
| US20150273088A1 (en) * | 2014-03-28 | 2015-10-01 | Washington University | Zaprinast analogues as glutaminase inhibitors and methods to predict response thereto |
| EP3303286B1 (en) * | 2015-06-01 | 2023-10-04 | Cedars-Sinai Medical Center | Compounds that bind to rela of nf-kb for use in treating cancer |
| TW201704203A (zh) * | 2015-07-30 | 2017-02-01 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | 靶向idh2突變的抗腫瘤化合物及其使用方法 |
| EP3362065B1 (en) | 2015-10-15 | 2024-04-03 | Les Laboratoires Servier | Combination therapy comprising ivosidenib, cytarabine and daunorubicin or idarubicin for treating acute myelogenous leukemia |
| HUE057263T2 (hu) | 2015-10-15 | 2022-04-28 | Servier Lab | Kombinációs terápia rosszindulató betegségek kezelésére |
| EP3412663B1 (en) * | 2016-02-04 | 2022-09-07 | Shionogi & Co., Ltd. | Nitrogen-containing heterocycle and carbocycle derivatives having trka inhibitory activity |
| WO2017140758A1 (en) | 2016-02-19 | 2017-08-24 | Debiopharm International S.A. | Derivatives of 2-amino-4-(2-oxazolidinon-3-yl)-pyrimidine fused with a five-membered heteroaromatic ring in 5,6-position which are useful for the treatment of various cancers |
| EP3444237B1 (en) * | 2016-03-22 | 2020-10-28 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Iridinesulfonamide compound and use method thereof |
| CN107556366B (zh) * | 2016-06-30 | 2025-02-07 | 上海海和药物研究开发股份有限公司 | 具有突变型异柠檬酸脱氢酶抑制活性的化合物、其制备方法及用途 |
| CN107973748A (zh) * | 2017-12-22 | 2018-05-01 | 潘劲松 | 含磺酸酯基或磺酰胺基的吡啶酮类偶氮分散染料及其合成方法 |
| WO2019200100A1 (en) * | 2018-04-12 | 2019-10-17 | Andrew Cook | Pladienolide derivatives as spliceosome targeting agents for treating cancer |
| US10980788B2 (en) | 2018-06-08 | 2021-04-20 | Agios Pharmaceuticals, Inc. | Therapy for treating malignancies |
| IT201900001009A1 (it) | 2019-01-23 | 2020-07-23 | Torino Politecnico | Vettore nanoporoso biomimetico comprendente un inibitore diretto verso la forma nativa della proteina IDH2 |
| WO2021150756A1 (en) * | 2020-01-21 | 2021-07-29 | Emory University | Inhibitors of glutathione s-transferases (gsts) and nad(p)h:quinone oxidoreductase 1 (nqo1), pharmaceutical compositions, and uses in managing cancer |
| CN112375069B (zh) * | 2020-11-20 | 2022-09-13 | 湖北民族大学 | 一种4-脲基嘧啶类化合物及其用途 |
Family Cites Families (117)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2390529A (en) | 1942-02-03 | 1945-12-11 | Ernst A H Friedheim | Hydrazino-1,3,5-triazino derivatives of substituted phenylarsenic compounds |
| BE754242A (fr) | 1970-07-15 | 1971-02-01 | Geigy Ag J R | Diamino-s-triazines et dinitro-s-triazines |
| US3867383A (en) | 1971-03-29 | 1975-02-18 | Ciba Geigy Corp | Monoanthranilatoanilino-s-triazines |
| CH606334A5 (cg-RX-API-DMAC7.html) | 1974-06-21 | 1978-10-31 | Ciba Geigy Ag | |
| DE2928485A1 (de) | 1979-07-14 | 1981-01-29 | Bayer Ag | Verwendung von harnstoffderivaten als arzneimittel bei der behandlung von fettstoffwechselstoerungen |
| JPS58186682A (ja) | 1982-04-27 | 1983-10-31 | 日本化薬株式会社 | セルロ−ス又はセルロ−ス含有繊維材料の染色法 |
| DE3512630A1 (de) | 1985-04-06 | 1986-10-23 | Hoechst Ag, 6230 Frankfurt | Verfahren zum faerben oder bedrucken von cellulosefasern oder cellulosemischfasern |
| JP2588711B2 (ja) * | 1987-04-06 | 1997-03-12 | 富士写真フイルム株式会社 | ハロゲン化銀写真感光材料 |
| US5041443A (en) | 1989-02-21 | 1991-08-20 | Dainippon Pharmaceutical Co., Ltd. | Medicament for treating cerebral insufficiency diseases, novel 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives, and process for the production thereof |
| ES2058630T3 (es) | 1989-03-03 | 1994-11-01 | Dainippon Pharmaceutical Co | Derivados de 2-(1-piperazinil)-4-fenilcicloalcanopiridinas, procedimientos de preparacion y composiciones farmaceuticas que los contienen. |
| JPH0499768A (ja) | 1990-08-17 | 1992-03-31 | Dainippon Pharmaceut Co Ltd | 4―(4―フェニルピリジン―2―イル)ピペラジン―1―オキシド誘導体 |
| WO1993017009A1 (fr) | 1992-02-28 | 1993-09-02 | Zenyaku Kogyo Kabushiki Kaisha | DERIVE DE s-TRIAZINE ET REMEDE CONTRE DES MALADIES DEPENDENTES DE L'×STROGENE LE CONTENANT COMME INGREDIENT ACTIF |
| IL115420A0 (en) | 1994-09-26 | 1995-12-31 | Zeneca Ltd | Aminoheterocyclic derivatives |
| WO1998021191A1 (en) | 1995-05-16 | 1998-05-22 | Nissan Chemical Industries, Ltd. | Cyanoethylmelamine derivatives and process for producing the same |
| FR2735127B1 (fr) | 1995-06-09 | 1997-08-22 | Pf Medicament | Nouvelles piperazines heteroaromatiques utiles comme medicaments. |
| GB9602166D0 (en) | 1996-02-02 | 1996-04-03 | Zeneca Ltd | Aminoheterocyclic derivatives |
| WO1997028128A1 (en) | 1996-02-02 | 1997-08-07 | Zeneca Limited | Heterocyclic compounds useful as pharmaceutical agents |
| US5807876A (en) | 1996-04-23 | 1998-09-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of IMPDH enzyme |
| JPH09291034A (ja) | 1996-02-27 | 1997-11-11 | Yoshitomi Pharmaceut Ind Ltd | 縮合ピリジン化合物およびその医薬としての用途 |
| US6262113B1 (en) | 1996-03-20 | 2001-07-17 | Smithkline Beecham Corporation | IL-8 receptor antagonists |
| AU722662B2 (en) | 1996-05-20 | 2000-08-10 | Darwin Discovery Limited | Quinoline sulfonamides as TNF inhibitors and as PDE-IV inhibitors |
| US5984882A (en) | 1996-08-19 | 1999-11-16 | Angiosonics Inc. | Methods for prevention and treatment of cancer and other proliferative diseases with ultrasonic energy |
| US6399358B1 (en) | 1997-03-31 | 2002-06-04 | Thomas Jefferson University | Human gene encoding human chondroitin 6-sulfotransferase |
| JPH11158073A (ja) | 1997-09-26 | 1999-06-15 | Takeda Chem Ind Ltd | アデノシンa3拮抗剤 |
| US7517880B2 (en) | 1997-12-22 | 2009-04-14 | Bayer Pharmaceuticals Corporation | Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas |
| DE69830513T2 (de) * | 1997-12-22 | 2006-03-16 | Bayer Pharmaceuticals Corp., West Haven | HEMMUNG DER p38 KINASE UNTER VERWENDUNG VON SYMMETRISCHEN UND ASYMMETRISCHEN DIPHENYLHARNSTOFFEN |
| UY25842A1 (es) * | 1998-12-16 | 2001-04-30 | Smithkline Beecham Corp | Antagonistas de receptores de il-8 |
| CA2366607A1 (en) * | 1999-03-08 | 2000-09-14 | Bayer Aktiengesellschaft | Thiazolyl urea derivatives and their utilization as antiviral agents |
| US6274620B1 (en) | 1999-06-07 | 2001-08-14 | Biochem Pharma Inc. | Thiophene integrin inhibitors |
| ES2252058T3 (es) | 1999-08-27 | 2006-05-16 | Sugen, Inc. | Mimicos de fosfato y metodos de tratamiento empleando inhibidores de fosfatasa. |
| CA2415606A1 (en) | 2000-07-20 | 2002-01-31 | Neurogen Corporation | Capsaicin receptor ligands |
| US6525091B2 (en) | 2001-03-07 | 2003-02-25 | Telik, Inc. | Substituted diarylureas as stimulators for Fas-mediated apoptosis |
| JP2004534017A (ja) | 2001-04-27 | 2004-11-11 | 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 | Baceのインヒビター |
| JP2005500294A (ja) | 2001-06-19 | 2005-01-06 | ブリストル−マイヤーズ スクイブ カンパニー | ホスホジエステラーゼ7に対するピリミジン阻害剤 |
| WO2003016289A1 (en) | 2001-08-17 | 2003-02-27 | Ciba Specialty Chemicals Holding Inc. | Triazine derivatives and their use as sunscreens |
| JP4753336B2 (ja) | 2001-09-04 | 2011-08-24 | 日本化薬株式会社 | 新規アリル化合物及びその製法 |
| JP2003098643A (ja) * | 2001-09-26 | 2003-04-04 | Fuji Photo Film Co Ltd | ハロゲン化銀カラー写真感光材料 |
| DE10155684A1 (de) * | 2001-11-13 | 2003-05-22 | Bayer Ag | Thiazolharnstoffe |
| US6878196B2 (en) | 2002-01-15 | 2005-04-12 | Fuji Photo Film Co., Ltd. | Ink, ink jet recording method and azo compound |
| DE10210319A1 (de) * | 2002-03-08 | 2003-09-18 | Bayer Ag | Thiazolylcarbonyl-Derivate |
| PL215132B1 (pl) * | 2002-06-27 | 2013-10-31 | Novo Nordisk As | Pochodna arylokarbonylowa jako srodek terapeutyczny, jej zastosowanie i kompozycja farmaceutyczna ja zawierajaca |
| US20040067234A1 (en) | 2002-07-11 | 2004-04-08 | Paz Einat | Isocitrate dehydrogenase and uses thereof |
| EP2256108B1 (en) | 2002-07-18 | 2016-03-23 | Janssen Pharmaceutica NV | Substituted triazine kinase inhibitors |
| JP2004107220A (ja) | 2002-09-13 | 2004-04-08 | Mitsubishi Pharma Corp | TNF−α産生抑制剤 |
| CL2003002353A1 (es) | 2002-11-15 | 2005-02-04 | Vertex Pharma | Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic |
| EP1575580A4 (en) | 2002-12-02 | 2009-06-10 | Arqule Inc | METHOD FOR TREATING CARCINOMA |
| EP1590364B1 (en) * | 2002-12-16 | 2011-10-05 | Genmab A/S | Human monoclonal antibodies against interleukin 8 (il-8) |
| JP2006515883A (ja) | 2003-01-10 | 2006-06-08 | スレッシュオールド ファーマシューティカルズ, インコーポレイテッド | 2−デオキシグルコースによる癌の処置 |
| US7358262B2 (en) | 2003-01-29 | 2008-04-15 | Whitehead Institute For Biomedical Research | Identification of genotype-selective anti-tumor agents |
| WO2004073619A2 (en) | 2003-02-14 | 2004-09-02 | Smithkline Beecham Corporation | Ccr8 antagonists |
| WO2004074438A2 (en) | 2003-02-14 | 2004-09-02 | Smithkline Beecham Corporation | Ccr8 antagonists |
| EP1689722A2 (en) | 2003-10-10 | 2006-08-16 | Bayer Pharmaceuticals Corporation | 4-aminopyrimidine derivatives for treatment of hyperproliferative disorders |
| JP4099768B2 (ja) | 2003-11-10 | 2008-06-11 | 富士電機デバイステクノロジー株式会社 | 電子写真感光体および該電子写真感光体に起因する干渉縞有無の判定方法 |
| US20070196395A1 (en) | 2003-12-12 | 2007-08-23 | Mackerell Alexander | Immunomodulatory compounds that target and inhibit the py'binding site of tyrosene kinase p56 lck sh2 domain |
| US20050245508A1 (en) | 2003-12-24 | 2005-11-03 | Scios, Inc. | Treatment of malignant gliomas with TGF-beta inhibitors |
| KR20070011475A (ko) * | 2004-05-12 | 2007-01-24 | 쉐링 코포레이션 | Cxcr1 및 cxcr2 케모카인 길항제 |
| CA2581623A1 (en) | 2004-09-23 | 2006-03-30 | Reddy Us Therapeutics, Inc. | Novel pyridine compounds, process for their preparation and compositions containing them |
| WO2006038594A1 (ja) | 2004-10-04 | 2006-04-13 | Ono Pharmaceutical Co., Ltd. | N型カルシウムチャネル阻害薬 |
| US20100160324A1 (en) | 2004-12-30 | 2010-06-24 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
| KR20070107061A (ko) | 2005-01-25 | 2007-11-06 | 아스트라제네카 아베 | 화학적 화합물 |
| EP1899486A4 (en) | 2005-06-08 | 2009-07-22 | Millennium Pharm Inc | METHOD FOR IDENTIFYING, ASSESSING AND TREATING PATIENTS IN CANCER THERAPY |
| AU2006261954A1 (en) * | 2005-06-28 | 2007-01-04 | Merck & Co., Inc. | Non-nucleoside reverse transcriptase inhibitors |
| US8071597B2 (en) | 2005-08-26 | 2011-12-06 | Merck Serono Sa | Pyrazine compounds and uses as PI3K inhibitors |
| US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
| TW200815426A (en) | 2006-06-28 | 2008-04-01 | Astrazeneca Ab | New pyridine analogues II 333 |
| HUP0600810A3 (en) | 2006-10-27 | 2008-09-29 | Richter Gedeon Nyrt | New sulfonamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them |
| EP2121662A1 (en) | 2006-12-04 | 2009-11-25 | Neurocrine Biosciences, Inc. | Substituted pyrimidines as adenosine receptor antagonists |
| CA2672893C (en) | 2006-12-15 | 2016-02-23 | Abraxis Bioscience, Inc. | Triazine derivatives and their therapeutical applications |
| CN101679321B (zh) | 2007-04-30 | 2012-10-03 | 普罗米蒂克生物科学公司 | 三嗪衍生物、含所述衍生物的组合物以及所述衍生物在制备用于治疗癌症和自身免疫性疾病药物中的应用 |
| AU2008262291A1 (en) | 2007-06-11 | 2008-12-18 | Miikana Therapeutics, Inc. | Substituted pyrazole compounds |
| NZ583450A (en) | 2007-07-20 | 2012-05-25 | Nerviano Medical Sciences Srl | Substituted indazole derivatives active as kinase inhibitors |
| TW200906818A (en) | 2007-07-31 | 2009-02-16 | Astrazeneca Ab | Chemical compounds |
| AR068764A1 (es) | 2007-10-10 | 2009-12-02 | Takeda Pharmaceutical | N-piperazin amidas y su uso en medicamentos para el tratamiento de enfermedades mediadas por la inhibicion de faah. |
| CA2709784A1 (en) * | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| JP5277685B2 (ja) | 2008-03-26 | 2013-08-28 | 富士ゼロックス株式会社 | 電子写真感光体、画像形成装置、プロセスカートリッジ及び画像形成方法 |
| GB0805477D0 (en) | 2008-03-26 | 2008-04-30 | Univ Nottingham | Pyrimidines triazines and their use as pharmaceutical agents |
| US20090281089A1 (en) | 2008-04-11 | 2009-11-12 | Genentech, Inc. | Pyridyl inhibitors of hedgehog signalling |
| PE20091843A1 (es) * | 2008-04-18 | 2010-01-07 | Glaxo Group Ltd | Inhibidores de catepsina c |
| CN101575408B (zh) | 2008-05-09 | 2013-10-30 | Mca技术有限公司 | 用作阻燃剂和光稳定剂的聚三嗪基化合物 |
| FR2932483A1 (fr) | 2008-06-13 | 2009-12-18 | Cytomics Systems | Composes utiles pour le traitement des cancers. |
| TW201028381A (en) | 2008-07-14 | 2010-08-01 | Shionogi & Co | Pyridine derivative having ttk inhibition activity |
| DK2546365T3 (en) | 2008-09-03 | 2017-01-16 | Univ Johns Hopkins | Genetic changes of isocitrate dehydrogenase and other genes in malignant glioma |
| WO2010028179A1 (en) | 2008-09-03 | 2010-03-11 | Dr. Reddy's Laboratories Ltd. | Heterocyclic compounds as gata modulators |
| JP2010079130A (ja) | 2008-09-29 | 2010-04-08 | Fuji Xerox Co Ltd | 電子写真感光体、プロセスカートリッジ、及び画像形成装置 |
| WO2010059239A2 (en) | 2008-11-21 | 2010-05-27 | Millennium Pharmaceuticals, Inc | Lactate salt of 4-(6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide and pharmaceutical compositions thereof for the treatment of cancer and other diseases or disorders |
| JP2010181540A (ja) | 2009-02-04 | 2010-08-19 | Fuji Xerox Co Ltd | 電子写真感光体、プロセスカートリッジ、及び画像形成装置 |
| ES2453474T3 (es) | 2009-02-06 | 2014-04-07 | Nippon Shinyaku Co., Ltd. | Derivados de aminopirazina y medicamento correspondiente |
| CN108524505A (zh) | 2009-03-13 | 2018-09-14 | 安吉奥斯医药品有限公司 | 用于细胞增殖相关病症的方法和组合物 |
| CA2760929C (en) | 2009-05-04 | 2018-01-02 | Agios Pharmaceuticals, Inc. | Pkm2 activators for use in the treatment of cancer |
| CN102573485B (zh) | 2009-06-08 | 2014-11-26 | 加利福尼亚资本权益有限责任公司 | 三嗪衍生物及其治疗应用 |
| JP2012529518A (ja) | 2009-06-09 | 2012-11-22 | アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー | ヘッジホッグシグナル伝達のピリジル−トリアジン阻害剤 |
| US20120202818A1 (en) | 2009-06-09 | 2012-08-09 | California Capital Equity, Llc | Ureidophenyl substituted triazine derivatives and their therapeutical applications |
| PT2448582T (pt) | 2009-06-29 | 2017-07-10 | Agios Pharmaceuticals Inc | Compostos e composições terapêuticas |
| WO2011005209A1 (en) | 2009-07-10 | 2011-01-13 | Milux Holding S.A. | Knee joint device and method |
| SG10201609290PA (en) * | 2009-08-25 | 2016-12-29 | Abraxis Bioscience Llc | Combination therapy with nanoparticle compositions of taxane and hedgehog inhibitors |
| JP5473851B2 (ja) | 2009-09-30 | 2014-04-16 | 富士フイルム株式会社 | 高分子フィルム、位相差フィルム、偏光板及び液晶表示装置 |
| US8652534B2 (en) | 2009-10-14 | 2014-02-18 | Berry Pharmaceuticals, LLC | Compositions and methods for treatment of mammalian skin |
| ES2594402T3 (es) | 2009-10-21 | 2016-12-20 | Agios Pharmaceuticals, Inc. | Métodos y composiciones para trastornos relacionados con la proliferación celular |
| EP2509600B1 (en) | 2009-12-09 | 2017-08-02 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds for use in the treatment of cancer characterized as having an idh mutation |
| WO2011143160A2 (en) | 2010-05-10 | 2011-11-17 | The Johns Hopkins University | Metabolic inhibitor against tumors having an idh mutation |
| MX342951B (es) | 2010-07-16 | 2016-10-18 | Agios Pharmaceuticals Inc * | Composiciones terapeuticamente activas y su metodo de uso. |
| RU2016116533A (ru) * | 2010-09-03 | 2018-11-30 | ФОРМА ТиЭм, ЭлЭлСИ | Новые соединения и композиции для ингибирования nampt |
| NZ609490A (en) | 2010-10-21 | 2015-06-26 | Biomarin Pharm Inc | Crystalline (8s,9r)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1h-1,2,4-triazol-5-yl)-8,9-dihydro-2h-pyrido[4,3,2-de]phthalazin-3(7h)-one tosylate salt |
| SG10201601507YA (en) | 2010-11-29 | 2016-04-28 | Galleon Pharmaceuticals Inc | Novel compounds as respiratory stimulants for treatment of breathing control disorders or diseases |
| TWI555737B (zh) | 2011-05-24 | 2016-11-01 | 拜耳知識產權公司 | 含有硫醯亞胺基團之4-芳基-n-苯基-1,3,5-三氮雜苯-2-胺 |
| CN102827170A (zh) | 2011-06-17 | 2012-12-19 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
| AU2012280725B2 (en) | 2011-07-07 | 2017-02-02 | Merck Patent Gmbh | Substituted azaheterocycles for the treatment of cancer |
| CN102659765B (zh) | 2011-12-31 | 2014-09-10 | 沈阳药科大学 | 嘧啶及三嗪类化合物的制备方法和应用 |
| SI2800743T1 (en) | 2012-01-06 | 2018-08-31 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and methods for their use |
| CA2860858A1 (en) | 2012-01-19 | 2013-07-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| US9474779B2 (en) | 2012-01-19 | 2016-10-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compositions and their methods of use |
| EP2634259A1 (en) | 2012-03-01 | 2013-09-04 | Deutsches Krebsforschungszentrum | Means and methods for the determination of (D)-2-hydroxyglutarate (D2HG) |
| CN104169260A (zh) | 2012-03-09 | 2014-11-26 | 卡尔那生物科学株式会社 | 新三嗪衍生物 |
| WO2014015422A1 (en) | 2012-07-27 | 2014-01-30 | Ontario Institute For Cancer Research | Cellulose-based nanoparticles for drug delivery |
| US9579324B2 (en) | 2013-07-11 | 2017-02-28 | Agios Pharmaceuticals, Inc | Therapeutically active compounds and their methods of use |
| WO2015003360A2 (en) | 2013-07-11 | 2015-01-15 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| US20150031627A1 (en) | 2013-07-25 | 2015-01-29 | Agios Pharmaceuticals, Inc | Therapeutically active compounds and their methods of use |
-
2013
- 2013-10-11 NZ NZ706999A patent/NZ706999A/en not_active IP Right Cessation
- 2013-10-11 JP JP2015536951A patent/JP6385352B2/ja not_active Expired - Fee Related
- 2013-10-11 AU AU2013331626A patent/AU2013331626B2/en not_active Ceased
- 2013-10-11 EP EP13846787.3A patent/EP2906212A4/en not_active Withdrawn
- 2013-10-11 CA CA2888360A patent/CA2888360A1/en active Pending
- 2013-10-11 HK HK16101848.4A patent/HK1213798A1/zh unknown
- 2013-10-11 MX MX2015004762A patent/MX365747B/es active IP Right Grant
- 2013-10-11 CN CN201380062951.5A patent/CN104822373B/zh not_active Expired - Fee Related
- 2013-10-11 WO PCT/US2013/064601 patent/WO2014062511A1/en not_active Ceased
- 2013-10-11 US US14/435,674 patent/US10202339B2/en not_active Expired - Fee Related
-
2018
- 2018-07-10 JP JP2018130743A patent/JP2018199677A/ja not_active Withdrawn