JP2015503571A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2015503571A5 JP2015503571A5 JP2014550627A JP2014550627A JP2015503571A5 JP 2015503571 A5 JP2015503571 A5 JP 2015503571A5 JP 2014550627 A JP2014550627 A JP 2014550627A JP 2014550627 A JP2014550627 A JP 2014550627A JP 2015503571 A5 JP2015503571 A5 JP 2015503571A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- alkyl
- ring
- phenyl
- optionally substituted
- 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
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 100
- 150000001875 compounds Chemical class 0.000 claims description 86
- -1 CF 3 Chemical group 0.000 claims description 75
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 56
- 230000035772 mutation Effects 0.000 claims description 51
- 101000599886 Homo sapiens Isocitrate dehydrogenase [NADP], mitochondrial Proteins 0.000 claims description 31
- 102100037845 Isocitrate dehydrogenase [NADP], mitochondrial Human genes 0.000 claims description 31
- 125000005843 halogen group Chemical group 0.000 claims description 30
- 125000002947 alkylene group Chemical group 0.000 claims description 28
- 125000001424 substituent group Chemical group 0.000 claims description 24
- 125000000217 alkyl group Chemical group 0.000 claims description 19
- 206010028980 Neoplasm Diseases 0.000 claims description 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 18
- 125000000623 heterocyclic group Chemical group 0.000 claims description 16
- 201000011510 cancer Diseases 0.000 claims description 15
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 239000001257 hydrogen Substances 0.000 claims description 14
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 12
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 12
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 12
- 239000000203 mixture Substances 0.000 claims description 11
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 10
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 10
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 10
- 125000004076 pyridyl group Chemical group 0.000 claims description 10
- 102200116484 rs121913502 Human genes 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- ICNPHUJONLGYDI-UHFFFAOYSA-N 4-butyl-2-n-(4-methylphenyl)-6-phenyl-1h-1,3,5-triazine-2,4-diamine Chemical compound N1C(C=2C=CC=CC=2)=NC(CCCC)(N)N=C1NC1=CC=C(C)C=C1 ICNPHUJONLGYDI-UHFFFAOYSA-N 0.000 claims description 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 8
- 125000001153 fluoro group Chemical group F* 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 125000002971 oxazolyl group Chemical group 0.000 claims description 8
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 8
- HWXBTNAVRSUOJR-UHFFFAOYSA-N 2-hydroxyglutaric acid Chemical compound OC(=O)C(O)CCC(O)=O HWXBTNAVRSUOJR-UHFFFAOYSA-N 0.000 claims description 7
- KPGXRSRHYNQIFN-UHFFFAOYSA-N 2-oxoglutaric acid Chemical compound OC(=O)CCC(=O)C(O)=O KPGXRSRHYNQIFN-UHFFFAOYSA-N 0.000 claims description 7
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 7
- 230000001419 dependent effect Effects 0.000 claims description 7
- 239000003814 drug Substances 0.000 claims description 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 6
- 102000004190 Enzymes Human genes 0.000 claims description 6
- 108090000790 Enzymes Proteins 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 6
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims description 6
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 6
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 6
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 6
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 5
- 229940124597 therapeutic agent Drugs 0.000 claims description 5
- CLBHAIBDFNDDJP-MEFGMAGPSA-N (e)-3-[4-[[4-[3-(diethylamino)propylamino]-6-phenyl-1,3,5-triazin-2-yl]amino]-2-methoxyphenyl]-2-phenylprop-2-enenitrile Chemical compound N=1C(C=2C=CC=CC=2)=NC(NCCCN(CC)CC)=NC=1NC(C=C1OC)=CC=C1\C=C(\C#N)C1=CC=CC=C1 CLBHAIBDFNDDJP-MEFGMAGPSA-N 0.000 claims description 4
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 claims description 4
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 4
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims description 4
- BKLDIEBDLYULCF-UHFFFAOYSA-N 3-[4-(5-aminopentylamino)-6-(3-fluoroanilino)-1,3,5-triazin-2-yl]phenol Chemical compound N=1C(C=2C=C(O)C=CC=2)=NC(NCCCCCN)=NC=1NC1=CC=CC(F)=C1 BKLDIEBDLYULCF-UHFFFAOYSA-N 0.000 claims description 4
- MUVWXGCFCZGJAL-MRXNPFEDSA-N 3-[[4-(3-chlorophenyl)-6-[[(3r)-pyrrolidin-3-yl]amino]-1,3,5-triazin-2-yl]amino]-4-methylbenzamide Chemical compound CC1=CC=C(C(N)=O)C=C1NC1=NC(N[C@H]2CNCC2)=NC(C=2C=C(Cl)C=CC=2)=N1 MUVWXGCFCZGJAL-MRXNPFEDSA-N 0.000 claims description 4
- QTSZJXMCNWRULJ-UHFFFAOYSA-N 4,6-bis(3-fluorophenyl)-2-piperidin-3-ylimino-1,3-dihydro-1,3,5-triazin-4-amine Chemical compound FC=1C=C(C=CC=1)C1(NC(=NC(=N1)NC1CNCCC1)C1=CC(=CC=C1)F)N QTSZJXMCNWRULJ-UHFFFAOYSA-N 0.000 claims description 4
- VPVZLIPBRXHMGH-UHFFFAOYSA-N 4-(furan-2-ylmethyl)-6-phenyl-2-N-[3-(trifluoromethyl)phenyl]-1H-1,3,5-triazine-2,4-diamine Chemical compound O1C(=CC=C1)CC1(NC(=NC(=N1)NC1=CC(=CC=C1)C(F)(F)F)C1=CC=CC=C1)N VPVZLIPBRXHMGH-UHFFFAOYSA-N 0.000 claims description 4
- RXQOFEFFFQEPEF-UHFFFAOYSA-N 4-[[4-(furan-2-ylmethylamino)-6-pyridin-4-yl-1,3,5-triazin-2-yl]amino]phenol Chemical compound C1=CC(O)=CC=C1NC1=NC(NCC=2OC=CC=2)=NC(C=2C=CN=CC=2)=N1 RXQOFEFFFQEPEF-UHFFFAOYSA-N 0.000 claims description 4
- OSRCRCDGQNLBNM-UHFFFAOYSA-N 4-cyclohexyl-2-N,6-diphenyl-1H-1,3,5-triazine-2,4-diamine Chemical compound C1(CCCCC1)C1(NC(=NC(=N1)NC1=CC=CC=C1)C1=CC=CC=C1)N OSRCRCDGQNLBNM-UHFFFAOYSA-N 0.000 claims description 4
- TXYRXGLQBFUCPR-UHFFFAOYSA-N 6-(3-methoxyphenyl)-4-n-methyl-2-n-(3-nitrophenyl)-1,3,5-triazine-2,4-diamine Chemical compound N=1C(C=2C=C(OC)C=CC=2)=NC(NC)=NC=1NC1=CC=CC([N+]([O-])=O)=C1 TXYRXGLQBFUCPR-UHFFFAOYSA-N 0.000 claims description 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 4
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical class CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims description 4
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Chemical class CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims description 4
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims description 4
- 206010039491 Sarcoma Diseases 0.000 claims description 4
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 4
- 125000000304 alkynyl group Chemical group 0.000 claims description 4
- BVCRERJDOOBZOH-UHFFFAOYSA-N bicyclo[2.2.1]heptanyl Chemical group C1C[C+]2CC[C-]1C2 BVCRERJDOOBZOH-UHFFFAOYSA-N 0.000 claims description 4
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 235000018417 cysteine Nutrition 0.000 claims description 4
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims description 4
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 4
- VYFOAVADNIHPTR-UHFFFAOYSA-N isatoic anhydride Chemical compound NC1=CC=CC=C1CO VYFOAVADNIHPTR-UHFFFAOYSA-N 0.000 claims description 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 4
- 150000004702 methyl esters Chemical class 0.000 claims description 4
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims description 4
- VJKPSOVHUPAUDR-UHFFFAOYSA-N n-(4-anilino-6-pyridin-2-yl-1,3,5-triazin-2-yl)-2-chloro-4-methylsulfonylbenzamide Chemical compound ClC1=CC(S(=O)(=O)C)=CC=C1C(=O)NC1=NC(NC=2C=CC=CC=2)=NC(C=2N=CC=CC=2)=N1 VJKPSOVHUPAUDR-UHFFFAOYSA-N 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims description 4
- 125000003566 oxetanyl group Chemical group 0.000 claims description 4
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims description 4
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims description 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 4
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 4
- 125000004496 thiazol-5-yl group Chemical group S1C=NC=C1* 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 3
- 208000032612 Glial tumor Diseases 0.000 claims description 3
- 206010018338 Glioma Diseases 0.000 claims description 3
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 3
- 208000005017 glioblastoma Diseases 0.000 claims description 3
- 201000001441 melanoma Diseases 0.000 claims description 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 125000003107 substituted aryl group Chemical group 0.000 claims description 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 3
- 230000002792 vascular Effects 0.000 claims description 3
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims description 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims description 2
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims description 2
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims description 2
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims description 2
- 125000004208 3-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C([H])C(*)=C1[H] 0.000 claims description 2
- 125000004917 3-methyl-2-butyl group Chemical group CC(C(C)*)C 0.000 claims description 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 2
- 125000002393 azetidinyl group Chemical group 0.000 claims description 2
- 125000001246 bromo group Chemical group Br* 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000004284 isoxazol-3-yl group Chemical group [H]C1=C([H])C(*)=NO1 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 125000006299 oxetan-3-yl group Chemical group [H]C1([H])OC([H])([H])C1([H])* 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims description 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 2
- 208000005243 Chondrosarcoma Diseases 0.000 claims 2
- JWZZKOKVBUJMES-UHFFFAOYSA-N (+-)-Isoprenaline Chemical compound CC(C)NCC(O)C1=CC=C(O)C(O)=C1 JWZZKOKVBUJMES-UHFFFAOYSA-N 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000003145 oxazol-4-yl group Chemical group O1C=NC(=C1)* 0.000 claims 1
- 150000002993 phenylalanine derivatives Chemical class 0.000 claims 1
- 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 1
- 238000000034 method Methods 0.000 description 10
- 125000001072 heteroaryl group Chemical group 0.000 description 6
- XJLXINKUBYWONI-DQQFMEOOSA-N [[(2r,3r,4r,5r)-5-(6-aminopurin-9-yl)-3-hydroxy-4-phosphonooxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [(2s,3r,4s,5s)-5-(3-carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphate Chemical compound NC(=O)C1=CC=C[N+]([C@@H]2[C@H]([C@@H](O)[C@H](COP([O-])(=O)OP(O)(=O)OC[C@@H]3[C@H]([C@@H](OP(O)(O)=O)[C@@H](O3)N3C4=NC=NC(N)=C4N=C3)O)O2)O)=C1 XJLXINKUBYWONI-DQQFMEOOSA-N 0.000 description 5
- 229930027945 nicotinamide-adenine dinucleotide Natural products 0.000 description 5
- 108700028369 Alleles Proteins 0.000 description 4
- 230000000694 effects Effects 0.000 description 3
- 150000002994 phenylalanines Chemical class 0.000 description 3
- KZKRRZFCAYOXQE-UHFFFAOYSA-N 1$l^{2}-azinane Chemical group C1CC[N]CC1 KZKRRZFCAYOXQE-UHFFFAOYSA-N 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 2
- 235000001014 amino acid Nutrition 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 150000004677 hydrates Chemical class 0.000 description 2
- 0 *C(*)(*)Nc1nc(N/C2=C/C=C/C=C/C=C2)nc(C2=CC=CC=CC=CC2)n1 Chemical compound *C(*)(*)Nc1nc(N/C2=C/C=C/C=C/C=C2)nc(C2=CC=CC=CC=CC2)n1 0.000 description 1
- JNYLMODTPLSLIF-UHFFFAOYSA-N 6-(trifluoromethyl)pyridine-3-carboxylic acid Chemical group OC(=O)C1=CC=C(C(F)(F)F)N=C1 JNYLMODTPLSLIF-UHFFFAOYSA-N 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 230000036952 cancer formation Effects 0.000 description 1
- 150000001721 carbon Chemical group 0.000 description 1
- 210000000845 cartilage Anatomy 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 125000004498 isoxazol-4-yl group Chemical group O1N=CC(=C1)* 0.000 description 1
- 230000000869 mutational effect Effects 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 238000012163 sequencing technique Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261584214P | 2012-01-06 | 2012-01-06 | |
| US61/584,214 | 2012-01-06 | ||
| PCT/CN2013/000009 WO2013102431A1 (en) | 2012-01-06 | 2013-01-05 | Therapeutically active compounds and their methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017019547A Division JP6409081B2 (ja) | 2012-01-06 | 2017-02-06 | 治療活性化合物およびその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015503571A JP2015503571A (ja) | 2015-02-02 |
| JP2015503571A5 true JP2015503571A5 (cg-RX-API-DMAC7.html) | 2018-02-01 |
| JP6411895B2 JP6411895B2 (ja) | 2018-10-24 |
Family
ID=48744984
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014550627A Active JP6411895B2 (ja) | 2012-01-06 | 2013-01-05 | 治療活性化合物およびその使用方法 |
| JP2017019547A Active JP6409081B2 (ja) | 2012-01-06 | 2017-02-06 | 治療活性化合物およびその使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017019547A Active JP6409081B2 (ja) | 2012-01-06 | 2017-02-06 | 治療活性化合物およびその使用方法 |
Country Status (39)
Families Citing this family (101)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| PT2448582T (pt) | 2009-06-29 | 2017-07-10 | Agios Pharmaceuticals Inc | Compostos e composições terapêuticas |
| EP2525790B1 (en) | 2009-10-21 | 2020-05-27 | Agios Pharmaceuticals, Inc. | Methods and compositions for cell-proliferation-related disorders |
| ES2594402T3 (es) | 2009-10-21 | 2016-12-20 | Agios Pharmaceuticals, Inc. | Métodos y composiciones para trastornos relacionados con la proliferación celular |
| SG194697A1 (en) | 2011-05-03 | 2013-12-30 | Agios Pharmaceuticals Inc | Pyruvate kinase activators for use in therapy |
| 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 |
| CN102827073A (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 |
| EA028085B1 (ru) | 2012-01-06 | 2017-10-31 | Эбайд Терапьютикс, Инк. | Карбаматные соединения и их применение |
| SI2800743T1 (en) | 2012-01-06 | 2018-08-31 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and methods for their use |
| US9474779B2 (en) | 2012-01-19 | 2016-10-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compositions and their methods of use |
| NZ706999A (en) | 2012-10-15 | 2018-12-21 | Agios Pharmaceuticals Inc | Inhibitors of mutant isocitrate dehydrogenase and therapeutical uses thereof |
| CN111087353B (zh) * | 2013-07-11 | 2023-10-24 | 法国施维雅药厂 | 治疗活性化合物及其使用方法 |
| 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 |
| US9579324B2 (en) | 2013-07-11 | 2017-02-28 | Agios Pharmaceuticals, Inc | Therapeutically active compounds and their methods of use |
| NZ715738A (en) * | 2013-07-11 | 2021-06-25 | Agios Pharmaceuticals Inc | N,6-bis(aryl or heteroaryl)-1,3,5-triazine-2,4-diamine 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 |
| EA030428B1 (ru) * | 2013-08-02 | 2018-08-31 | Аджиос Фармасьютикалз, Инк. | Терапевтически активные соединения и способы их применения |
| WO2015018060A1 (en) * | 2013-08-09 | 2015-02-12 | Agios Pharmaceuticals, Inc. | Crystalline forms of therapeutically active compounds and use thereof |
| KR102316886B1 (ko) * | 2013-08-02 | 2021-10-19 | 아지오스 파마슈티컬스 아이엔씨. | 치료학적 활성 화합물 및 이의 사용방법 |
| TWI651310B (zh) * | 2014-02-20 | 2019-02-21 | 日商日本煙草產業股份有限公司 | 三化合物及其醫藥用途 |
| UA122962C2 (uk) * | 2014-03-14 | 2021-01-27 | Аджіос Фармасьютикалз, Інк. | Спосіб лікування поширених солідних пухлин, які характеризуються наявністю мутантного алеля idh1 |
| 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 |
| CN106132946A (zh) * | 2014-03-28 | 2016-11-16 | 巴斯夫欧洲公司 | 作为除草剂的二氨基三嗪衍生物 |
| WO2015155129A1 (en) * | 2014-04-07 | 2015-10-15 | Basf Se | Diaminotriazine compound |
| EP2930174A1 (en) * | 2014-04-07 | 2015-10-14 | Basf Se | Diaminotriazine derivatives as herbicides |
| MX373789B (es) * | 2014-09-19 | 2020-03-23 | Forma Therapeutics Inc | Derivados de piridinil quinolinona como inhibidores de isocitrato deshidrogenasa mutante (mt-idh). |
| LT3194376T (lt) * | 2014-09-19 | 2019-02-25 | Forma Therapeutics, Inc. | Piridin-2(1h)-ono chinolinono dariniai, kaip mutantinės izocitratdehidrogenazės inhibitoriai |
| CA2961807A1 (en) | 2014-09-19 | 2016-03-24 | Forma Therapeutics, Inc. | Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| JP6648116B2 (ja) | 2014-09-19 | 2020-02-14 | フォーマ セラピューティクス，インコーポレイテッド | 変異イソクエン酸デヒドロゲナーゼ阻害剤としてのキノリノンピリミジン組成物 |
| WO2016053850A1 (en) | 2014-09-29 | 2016-04-07 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| WO2016126798A1 (en) | 2015-02-04 | 2016-08-11 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| CN107660199B (zh) | 2015-03-18 | 2021-11-23 | H.隆德贝克有限公司 | 哌嗪氨基甲酸酯及其制备和使用方法 |
| US10407419B2 (en) | 2015-04-21 | 2019-09-10 | Forma Therapeutics, Inc. | Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors |
| EA038574B1 (ru) * | 2015-04-21 | 2021-09-16 | Форма Терапьютикс, Инк. | Хинолиноновые производные пиридин-2(1h)-она и фармацевтические композиции на их основе |
| WO2016171755A1 (en) | 2015-04-21 | 2016-10-27 | Forma Therapeutics, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| WO2016177347A1 (en) * | 2015-05-07 | 2016-11-10 | Teligene Ltd | Heterocyclic compounds as idh2 inhibitors |
| WO2016183097A1 (en) | 2015-05-11 | 2016-11-17 | Abide Therapeutics, Inc. | Methods of treating inflammation or neuropathic pain |
| SI3307271T1 (sl) | 2015-06-11 | 2023-11-30 | Agios Pharmaceuticals, Inc. | Postopki za uporabo aktivatorjev piruvat kinaze |
| KR102303011B1 (ko) | 2015-07-30 | 2021-09-16 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | 1,3,5-트라이아진 유도체 및 이의 사용 방법 |
| CN108349933A (zh) * | 2015-08-05 | 2018-07-31 | 安吉奥斯医药品有限公司 | 制备6-(芳基或杂芳基)-1,3,5-三嗪-2,4-二醇和6-(芳基或杂芳基)-1,3,5-三嗪-2,4-二胺的方法 |
| 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 |
| AU2016340098B2 (en) | 2015-10-15 | 2022-06-02 | Celgene Corporation | Combination therapy for treating malignancies |
| HUE057263T2 (hu) | 2015-10-15 | 2022-04-28 | Servier Lab | Kombinációs terápia rosszindulató betegségek kezelésére |
| WO2017066599A1 (en) | 2015-10-15 | 2017-04-20 | Agios Pharmaceuticals, Inc. | Combination therapy for treating malignancies |
| JP6588647B2 (ja) * | 2015-10-21 | 2019-10-09 | ノイフォルム・ファーマシューティカルズ・インコーポレイテッドＮｅｕｆｏｒｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | 血液悪性腫瘍を治療するための重水素化合物及びその組成物並びに方法 |
| ES2905915T3 (es) * | 2015-12-04 | 2022-04-12 | Servier Lab | Procedimientos de tratamiento de neoplasias malignas |
| CN105503754B (zh) * | 2015-12-11 | 2017-11-17 | 浙江大学 | 2‑氨基‑4‑苄基‑6‑吗啉‑1,3,5‑三嗪及其制备和应用 |
| CN105399695B (zh) * | 2015-12-11 | 2019-04-19 | 浙江大学 | 三嗪类化合物及其制备方法和用途 |
| CN105384702B (zh) * | 2015-12-11 | 2018-04-10 | 浙江大学 | 三取代均三嗪类化合物及其制备方法 |
| US10463753B2 (en) | 2016-02-19 | 2019-11-05 | Lundbeck La Jolla Research Center, Inc. | Radiolabeled monoacylglycerol lipase occupancy probe |
| 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 |
| JP6930991B2 (ja) | 2016-02-26 | 2021-09-01 | セルジーン コーポレイション | 血液学的悪性腫瘍及び固形腫瘍の治療のためのｉｄｈ２阻害剤 |
| CN105820133B (zh) * | 2016-03-25 | 2018-06-05 | 浙江工业大学 | 多取代均三嗪类化合物及其制备方法和应用 |
| CN105753801B (zh) * | 2016-03-25 | 2018-06-01 | 浙江工业大学 | 一种均三嗪类化合物的制备方法 |
| WO2018014852A1 (zh) * | 2016-07-21 | 2018-01-25 | 南京圣和药业股份有限公司 | 作为异柠檬酸脱氢酶抑制剂的化合物及其应用 |
| EP3493809B1 (en) | 2016-08-03 | 2023-08-23 | Celgene Corporation | Enasidenib for treatment of myelodysplastic syndrome |
| SG11201901873PA (en) | 2016-09-07 | 2019-03-28 | Celgene Corp | Tablet compositions |
| US10899737B2 (en) | 2016-09-19 | 2021-01-26 | Lundbeck La Jolla Research Center, Inc. | Piperazine carbamates and methods of making and using same |
| JOP20190105A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| JOP20190106A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| JP7111725B2 (ja) | 2017-01-22 | 2022-08-02 | 正大天晴▲藥▼▲業▼集▲団▼股▲フン▼有限公司 | １，３，５－トリアジン誘導体の塩およびその結晶、その製造方法、医薬組成物、ならびにそれらの使用 |
| US11229653B2 (en) | 2017-05-05 | 2022-01-25 | Celgene Corporation | Methods of treatment of myeloproliferative neoplasm |
| EP3644999B1 (en) | 2017-06-30 | 2022-12-14 | Celgene Corporation | Compositions and methods of use of 2-(4-chlorophenyl)-n-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl) methyl) -2,2-difluoroacetamide |
| CN109265444B (zh) * | 2017-07-17 | 2022-03-11 | 南京圣和药业股份有限公司 | 取代的三嗪类idh抑制剂的光学异构体及其应用 |
| CN109467538A (zh) | 2017-09-07 | 2019-03-15 | 和记黄埔医药（上海）有限公司 | 环烯烃取代的杂芳环类化合物及其用途 |
| CN110051673B (zh) * | 2018-01-19 | 2022-03-11 | 南京圣和药业股份有限公司 | 一种包含三嗪类idh抑制剂的药物组合物及其用途 |
| CN110054615B (zh) * | 2018-01-19 | 2021-06-15 | 南京圣和药业股份有限公司 | 三嗪类idh抑制剂甲磺酸盐的晶型 |
| CN110054616B (zh) * | 2018-01-19 | 2021-11-23 | 南京圣和药业股份有限公司 | 三嗪类idh抑制剂的制备方法 |
| CN110054617A (zh) * | 2018-01-19 | 2019-07-26 | 南京圣和药业股份有限公司 | 三嗪类化合物、其制备方法及用途 |
| SG11202011228TA (en) | 2018-05-15 | 2020-12-30 | Lundbeck La Jolla Research Center Inc | Magl inhibitors |
| US11013733B2 (en) | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1) |
| WO2019222553A1 (en) | 2018-05-16 | 2019-11-21 | Forma Therapeutics, Inc. | Inhibiting mutant idh-1 |
| WO2019222551A1 (en) | 2018-05-16 | 2019-11-21 | Forma Therapeutics, Inc. | Solid forms of ((s)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile |
| US11311527B2 (en) | 2018-05-16 | 2022-04-26 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1) |
| US11013734B2 (en) | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation |
| US10980788B2 (en) | 2018-06-08 | 2021-04-20 | Agios Pharmaceuticals, Inc. | Therapy for treating malignancies |
| KR102328682B1 (ko) * | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| WO2020092894A1 (en) | 2018-11-02 | 2020-05-07 | Celgene Corporation | Solid forms of 2-methyl-1-[(4-[6-(trifluoromethyl) pyridin-2-yl]-6-{[2-(trifluoromethyl)pyridin-4-yl]amino}-1,3,5-triazin-2-yl) amino]propan-2-ol |
| US20220017489A1 (en) | 2018-11-02 | 2022-01-20 | Celgene Corporation | Solid dispersions for treatment of cancer |
| WO2020092906A1 (en) | 2018-11-02 | 2020-05-07 | Celgene Corporation | Co-crystals of 2-methyl-1 -[(4-[6-(trifluoromethyl)pyridin-2-yl]-6-{[2-(trifluoromethyl) pyridin-4-yl]amino}-1,3,5-triazin-2-yl)amino]propan-2-ol, compositions and methods of use thereof |
| CN111662271B (zh) * | 2019-03-08 | 2023-11-14 | 中国药科大学 | 具有idh突变体抑制活性的化合物及其制备方法与应用 |
| CN111662275B (zh) * | 2019-03-08 | 2023-08-22 | 中国药科大学 | 苯磺酰胺类idh突变体抑制剂、其制备方法和用途 |
| WO2020239759A1 (en) | 2019-05-27 | 2020-12-03 | Sandoz Ag | Amorphous enasidenib in a stabilized form |
| CN114502537A (zh) * | 2019-09-29 | 2022-05-13 | 贝达药业股份有限公司 | 突变型idh2抑制剂及其应用 |
| KR102333854B1 (ko) | 2019-10-24 | 2021-12-06 | 한국과학기술연구원 | 단백질 키나아제 저해 활성을 갖는 신규한 피리디닐트리아진 유도체 및 이를 포함하는 암의 예방, 개선 또는 치료용 약학 조성물 |
| WO2021097160A1 (en) | 2019-11-14 | 2021-05-20 | Celgene Corporation | Pediatric formulations for treatment of cancer |
| CA3175210A1 (en) | 2020-04-21 | 2021-10-28 | Cheryl A. Grice | Synthesis of a monoacylglycerol lipase inhibitor |
| CN111592524B (zh) * | 2020-05-20 | 2023-11-17 | 温州市天聚万迅信息科技有限公司 | 恩西德尼的制备方法 |
| WO2022074587A1 (en) * | 2020-10-06 | 2022-04-14 | Kures, Inc. | Mu-opioid receptor agonists and uses therefor |
| WO2022173961A1 (en) * | 2021-02-12 | 2022-08-18 | Servier Pharmaceuticals Llc | Therapeutically active compounds and their methods of use |
| US11865079B2 (en) | 2021-02-12 | 2024-01-09 | Servier Pharmaceuticals Llc | Therapeutically active compounds and their methods of use |
| CN113461660B (zh) * | 2021-06-11 | 2022-08-02 | 浙江大学 | 2,4,6-三取代-1,3,5-均三嗪类化合物及制备和应用 |
| US20250051301A1 (en) * | 2022-03-15 | 2025-02-13 | Betta Pharmaceuticals Co., Ltd | Mutant idh1 and idh2 inhibitor and application thereof |
| KR20250005157A (ko) | 2022-03-24 | 2025-01-09 | 에이2에이 파마수티칼스, 잉크. | 암 치료를 위한 조성물 및 방법 |
| CN114773320A (zh) * | 2022-05-29 | 2022-07-22 | 重庆医科大学 | 1,3,5-三嗪化合物及其制备方法和用途 |
| CN115536637B (zh) * | 2022-10-24 | 2025-03-18 | 陕西中医药大学 | 一种均三嗪类衍生物及其合成方法与用途 |
| CN115819363B (zh) * | 2022-12-16 | 2025-04-01 | 浙江工业大学 | 酮酰胺类化合物及其制备方法和应用 |
| TW202530204A (zh) * | 2023-09-27 | 2025-08-01 | 美商Ａ２Ａ製藥公司 | 用於治療與轉化酸性捲曲螺旋蛋白相關的癌症的方法 |
| CN118745158A (zh) * | 2024-06-06 | 2024-10-08 | 四川省医学科学院·四川省人民医院 | 三嗪环衍生物、其制备方法及其应用和pdgfr激酶抑制剂 |
Family Cites Families (93)
| 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 | |
| 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 |
| 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. |
| EP0466647B1 (de) * | 1990-07-12 | 1995-11-29 | Ciba-Geigy Ag | Verfahren zur photochemischen und thermischen Stabilisierung von Polyamid-Fasermaterialien |
| 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 |
| 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 |
| 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 |
| UY25842A1 (es) | 1998-12-16 | 2001-04-30 | Smithkline Beecham Corp | Antagonistas de receptores de il-8 |
| 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. |
| AU2001267910A1 (en) | 2000-07-03 | 2002-01-14 | Kansai Paint Co. Ltd. | Gas-barrier film |
| CA2415606A1 (en) | 2000-07-20 | 2002-01-31 | Neurogen Corporation | Capsaicin receptor ligands |
| 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 |
| US7291616B2 (en) * | 2001-10-31 | 2007-11-06 | Cell Therapeutics, Inc. | Aryl triazines as LPAAT-β inhibitors and uses thereof |
| US6878196B2 (en) | 2002-01-15 | 2005-04-12 | Fuji Photo Film Co., Ltd. | Ink, ink jet recording method and azo compound |
| 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 |
| WO2004074438A2 (en) | 2003-02-14 | 2004-09-02 | Smithkline Beecham Corporation | Ccr8 antagonists |
| WO2004073619A2 (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 |
| 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 |
| CA2581623A1 (en) | 2004-09-23 | 2006-03-30 | Reddy Us Therapeutics, Inc. | Novel pyridine compounds, process for their preparation and compositions containing them |
| 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 |
| 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 |
| 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 |
| WO2009027736A2 (en) * | 2007-08-27 | 2009-03-05 | Astrazeneca Ab | 2,4 diaminopyrimid'lnes for the treatment of myeloproliferative disorders and cancer |
| 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 |
| 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 |
| WO2010028179A1 (en) | 2008-09-03 | 2010-03-11 | Dr. Reddy's Laboratories Ltd. | Heterocyclic compounds as gata modulators |
| DK2546365T3 (en) | 2008-09-03 | 2017-01-16 | Univ Johns Hopkins | Genetic changes of isocitrate dehydrogenase and other genes in malignant glioma |
| 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 |
| 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 |
| 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 |
| US8261872B2 (en) * | 2009-06-08 | 2012-09-11 | Clark Equipment Company | Work machine having modular ignition switch keypad with latching output |
| 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 |
| WO2011005209A1 (en) | 2009-07-10 | 2011-01-13 | Milux Holding S.A. | Knee joint device and method |
| 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 |
| EP2525790B1 (en) | 2009-10-21 | 2020-05-27 | Agios Pharmaceuticals, Inc. | Methods and compositions for cell-proliferation-related disorders |
| 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 |
| EP2553116A4 (en) | 2010-04-01 | 2013-10-23 | Agios Pharmaceuticals Inc | METHOD FOR IDENTIFYING A CANDIDATE COMPOUND |
| MX342951B (es) | 2010-07-16 | 2016-10-18 | Agios Pharmaceuticals Inc * | Composiciones terapeuticamente activas y su metodo de uso. |
| 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 |
| CN102827073A (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 |
| 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 |
| EA028085B1 (ru) | 2012-01-06 | 2017-10-31 | Эбайд Терапьютикс, Инк. | Карбаматные соединения и их применение |
| US9474779B2 (en) | 2012-01-19 | 2016-10-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compositions and their methods of use |
| CA2860858A1 (en) | 2012-01-19 | 2013-07-25 | Agios Pharmaceuticals, Inc. | Therapeutically active compounds and their methods of use |
| 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 |
| US9579324B2 (en) | 2013-07-11 | 2017-02-28 | 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
- 2013-01-05 SI SI201331050T patent/SI2800743T1/en unknown
- 2013-01-05 EP EP13733752.3A patent/EP2800743B1/en active Active
- 2013-01-05 HR HRP20180844TT patent/HRP20180844T1/hr unknown
- 2013-01-05 CN CN201380009314.1A patent/CN104114543B/zh active Active
- 2013-01-05 BR BR112014016805-9A patent/BR112014016805B1/pt active IP Right Grant
- 2013-01-05 WO PCT/CN2013/000009 patent/WO2013102431A1/en not_active Ceased
- 2013-01-05 TR TR2018/09228T patent/TR201809228T4/tr unknown
- 2013-01-05 ES ES13733752.3T patent/ES2675760T3/es active Active
- 2013-01-05 MX MX2014008350A patent/MX358940B/es active IP Right Grant
- 2013-01-05 CA CA2860623A patent/CA2860623A1/en not_active Abandoned
- 2013-01-05 LT LTEP13733752.3T patent/LT2800743T/lt unknown
- 2013-01-05 EA EA201491330A patent/EA030187B1/ru not_active IP Right Cessation
- 2013-01-05 ES ES21194846T patent/ES3043635T3/es active Active
- 2013-01-05 NZ NZ722582A patent/NZ722582A/en unknown
- 2013-01-05 EP EP18164959.1A patent/EP3406608B8/en active Active
- 2013-01-05 SG SG10201602862RA patent/SG10201602862RA/en unknown
- 2013-01-05 JP JP2014550627A patent/JP6411895B2/ja active Active
- 2013-01-05 KR KR1020147021897A patent/KR101893112B1/ko active Active
- 2013-01-05 AU AU2013207289A patent/AU2013207289B2/en active Active
- 2013-01-05 EP EP25191184.8A patent/EP4647076A2/en active Pending
- 2013-01-05 CN CN202210633951.7A patent/CN115521264A/zh active Pending
- 2013-01-05 ES ES18164959T patent/ES2901430T3/es active Active
- 2013-01-05 PL PL13733752T patent/PL2800743T3/pl unknown
- 2013-01-05 CN CN201810599955.1A patent/CN108912066B/zh active Active
- 2013-01-05 HU HUE13733752A patent/HUE038403T2/hu unknown
- 2013-01-05 EP EP21194846.8A patent/EP3984997B1/en active Active
- 2013-01-05 MY MYPI2014002013A patent/MY185206A/en unknown
- 2013-01-05 UA UAA201408870A patent/UA117451C2/uk unknown
- 2013-01-05 NZ NZ627096A patent/NZ627096A/en unknown
- 2013-01-05 PT PT137337523T patent/PT2800743T/pt unknown
- 2013-01-05 SM SM20180334T patent/SMT201800334T1/it unknown
- 2013-01-05 CN CN202210260669.9A patent/CN114933585A/zh active Pending
- 2013-01-05 DK DK13733752.3T patent/DK2800743T3/en active
- 2013-01-05 SG SG11201403878QA patent/SG11201403878QA/en unknown
- 2013-01-05 PE PE2014001077A patent/PE20142098A1/es active IP Right Grant
- 2013-01-05 CN CN201710083141.8A patent/CN107417667B/zh active Active
- 2013-01-05 RS RS20180756A patent/RS57401B1/sr unknown
- 2013-01-05 CN CN202210634094.2A patent/CN115536635A/zh active Pending
- 2013-01-07 US US13/735,467 patent/US9732062B2/en active Active
- 2013-01-07 TW TW102100378A patent/TWI653228B/zh active
- 2013-01-07 AR ARP130100062A patent/AR090411A1/es active IP Right Grant
- 2013-09-20 NO NO13838217A patent/NO2897546T3/no unknown
-
2014
- 2014-07-03 IL IL233503A patent/IL233503B/en active IP Right Grant
- 2014-07-04 CL CL2014001793A patent/CL2014001793A1/es unknown
- 2014-07-04 PH PH12014501561A patent/PH12014501561A1/en unknown
- 2014-07-04 NI NI201400073A patent/NI201400073A/es unknown
- 2014-07-15 ZA ZA2014/05163A patent/ZA201405163B/en unknown
- 2014-08-06 EC ECIEPI201412726A patent/ECSP14012726A/es unknown
- 2014-08-06 CO CO14171766A patent/CO7030962A2/es unknown
- 2014-08-08 CR CR20140377A patent/CR20140377A/es unknown
-
2016
- 2016-06-03 US US15/173,519 patent/US9512107B2/en active Active
- 2016-10-28 US US15/337,683 patent/US9656999B2/en active Active
-
2017
- 2017-02-06 JP JP2017019547A patent/JP6409081B2/ja active Active
- 2017-06-29 US US15/638,279 patent/US10294215B2/en active Active
- 2017-11-23 AU AU2017265096A patent/AU2017265096B9/en active Active
-
2018
- 2018-06-29 CY CY20181100683T patent/CY1120506T1/el unknown
-
2019
- 2019-04-18 US US16/388,801 patent/US20200079755A1/en not_active Abandoned
-
2020
- 2020-06-18 US US16/905,736 patent/US11505538B1/en active Active
-
2022
- 2022-09-09 US US17/941,854 patent/US20230250078A1/en active Pending