JP2011528039A5 - - Google Patents
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- JP2011528039A5 JP2011528039A5 JP2011518843A JP2011518843A JP2011528039A5 JP 2011528039 A5 JP2011528039 A5 JP 2011528039A5 JP 2011518843 A JP2011518843 A JP 2011518843A JP 2011518843 A JP2011518843 A JP 2011518843A JP 2011528039 A5 JP2011528039 A5 JP 2011528039A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- amino
- isopropyl
- methylimidazol
- ylamino
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- -1 cyano, hydroxy, hydroxy Chemical group 0.000 claims description 220
- 125000000217 alkyl group Chemical group 0.000 claims description 110
- 150000001875 compounds Chemical class 0.000 claims description 43
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 36
- 229910052757 nitrogen Inorganic materials 0.000 claims description 36
- 125000000623 heterocyclic group Chemical group 0.000 claims description 28
- 125000003118 aryl group Chemical group 0.000 claims description 24
- ZYHQGITXIJDDKC-UHFFFAOYSA-N 2-[2-(2-aminophenyl)ethyl]aniline Chemical group NC1=CC=CC=C1CCC1=CC=CC=C1N ZYHQGITXIJDDKC-UHFFFAOYSA-N 0.000 claims description 22
- 125000001188 haloalkyl group Chemical group 0.000 claims description 22
- 125000005843 halogen group Chemical group 0.000 claims description 22
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims description 20
- 125000000304 alkynyl group Chemical group 0.000 claims description 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 20
- 125000003545 alkoxy group Chemical group 0.000 claims description 18
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 18
- 125000001072 heteroaryl group Chemical group 0.000 claims description 16
- 150000003839 salts Chemical class 0.000 claims description 16
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 14
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims description 12
- 125000005236 alkanoylamino group Chemical group 0.000 claims description 12
- 125000001589 carboacyl group Chemical group 0.000 claims description 12
- 201000010099 disease Diseases 0.000 claims description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 12
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims description 10
- 125000003342 alkenyl group Chemical group 0.000 claims description 10
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 10
- 125000004423 acyloxy group Chemical group 0.000 claims description 8
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 8
- 125000005110 aryl thio group Chemical group 0.000 claims description 8
- ICCBZGUDUOMNOF-UHFFFAOYSA-N azidoamine Chemical compound NN=[N+]=[N-] ICCBZGUDUOMNOF-UHFFFAOYSA-N 0.000 claims description 8
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 8
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 8
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 7
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims description 6
- 206010016654 Fibrosis Diseases 0.000 claims description 6
- 125000004104 aryloxy group Chemical group 0.000 claims description 6
- 230000004761 fibrosis Effects 0.000 claims description 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 6
- 239000000203 mixture Substances 0.000 claims description 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims description 4
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 4
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims description 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 125000003106 haloaryl group Chemical group 0.000 claims description 4
- 125000004468 heterocyclylthio group Chemical group 0.000 claims description 4
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims description 4
- 102000003964 Histone deacetylase Human genes 0.000 claims description 3
- 108090000353 Histone deacetylase Proteins 0.000 claims description 3
- 230000002159 abnormal effect Effects 0.000 claims description 3
- 230000024245 cell differentiation Effects 0.000 claims description 3
- 230000004663 cell proliferation Effects 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 claims description 2
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims description 2
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims description 2
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- LIFLMLCUISLUOZ-UHFFFAOYSA-N 4-[ethyl-[4-(2-methyl-3-propan-2-ylimidazol-4-yl)pyrimidin-2-yl]amino]-n-hydroxybenzamide Chemical compound N=1C=CC(C=2N(C(C)=NC=2)C(C)C)=NC=1N(CC)C1=CC=C(C(=O)NO)C=C1 LIFLMLCUISLUOZ-UHFFFAOYSA-N 0.000 claims description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- WYWHKKSPHMUBEB-UHFFFAOYSA-N 6-Mercaptoguanine Natural products N1C(N)=NC(=S)C2=C1N=CN2 WYWHKKSPHMUBEB-UHFFFAOYSA-N 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 102000015790 Asparaginase Human genes 0.000 claims description 2
- 108010024976 Asparaginase Proteins 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 108010006654 Bleomycin Proteins 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- HSMKDMQMUYSZHJ-UHFFFAOYSA-N C(C1=CC=CC=C1)(=O)NNC1=NC=NC(=N1)C1=CN=C(N1C(C)C)C Chemical compound C(C1=CC=CC=C1)(=O)NNC1=NC=NC(=N1)C1=CN=C(N1C(C)C)C HSMKDMQMUYSZHJ-UHFFFAOYSA-N 0.000 claims description 2
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims description 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 2
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 2
- 208000024934 IgG4-related mediastinitis Diseases 0.000 claims description 2
- 208000014919 IgG4-related retroperitoneal fibrosis Diseases 0.000 claims description 2
- 208000026350 Inborn Genetic disease Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 208000002805 Mediastinal fibrosis Diseases 0.000 claims description 2
- 229930192392 Mitomycin Natural products 0.000 claims description 2
- 206010028594 Myocardial fibrosis Diseases 0.000 claims description 2
- NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 claims description 2
- NUROKKSTJCHODO-UHFFFAOYSA-N NC1=C(C=C(C=C1)C=1SC=CC1)N(C1=CC=CS1)C1=NC=C(C(=N1)C1=CN=C(N1C(C)C)C)F Chemical compound NC1=C(C=C(C=C1)C=1SC=CC1)N(C1=CC=CS1)C1=NC=C(C(=N1)C1=CN=C(N1C(C)C)C)F NUROKKSTJCHODO-UHFFFAOYSA-N 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000012902 Nervous system disease Diseases 0.000 claims description 2
- 208000025966 Neurological disease Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 2
- 229930012538 Paclitaxel Natural products 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010036805 Progressive massive fibrosis Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 206010038979 Retroperitoneal fibrosis Diseases 0.000 claims description 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims description 2
- JKOQGQFVAUAYPM-UHFFFAOYSA-N amifostine Chemical compound NCCCNCCSP(O)(O)=O JKOQGQFVAUAYPM-UHFFFAOYSA-N 0.000 claims description 2
- 229960001097 amifostine Drugs 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 229960003272 asparaginase Drugs 0.000 claims description 2
- DCXYFEDJOCDNAF-UHFFFAOYSA-M asparaginate Chemical compound [O-]C(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-M 0.000 claims description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
- 229960001561 bleomycin Drugs 0.000 claims description 2
- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 claims description 2
- 125000001246 bromo group Chemical group Br* 0.000 claims description 2
- 229940127093 camptothecin Drugs 0.000 claims description 2
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 150000003857 carboxamides Chemical class 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 2
- 229960004316 cisplatin Drugs 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 239000002875 cyclin dependent kinase inhibitor Substances 0.000 claims description 2
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 claims description 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 2
- 229960004397 cyclophosphamide Drugs 0.000 claims description 2
- 229960000684 cytarabine Drugs 0.000 claims description 2
- 229960003901 dacarbazine Drugs 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 125000006264 diethylaminomethyl group Chemical group [H]C([H])([H])C([H])([H])N(C([H])([H])*)C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 208000016097 disease of metabolism Diseases 0.000 claims description 2
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims description 2
- 229960004679 doxorubicin Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 2
- 125000005448 ethoxyethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 229960002949 fluorouracil Drugs 0.000 claims description 2
- MKXKFYHWDHIYRV-UHFFFAOYSA-N flutamide Chemical compound CC(C)C(=O)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 MKXKFYHWDHIYRV-UHFFFAOYSA-N 0.000 claims description 2
- 229960002074 flutamide Drugs 0.000 claims description 2
- 208000016361 genetic disease Diseases 0.000 claims description 2
- 230000002068 genetic effect Effects 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 2
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims description 2
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 125000004282 imidazolidin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])N([H])C1([H])* 0.000 claims description 2
- 125000004283 imidazolin-2-yl group Chemical group [H]N1C(*)=NC([H])([H])C1([H])[H] 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- GOTYRUGSSMKFNF-UHFFFAOYSA-N lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 claims description 2
- 229960004942 lenalidomide Drugs 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 claims description 2
- 229960001428 mercaptopurine Drugs 0.000 claims description 2
- 208000030159 metabolic disease Diseases 0.000 claims description 2
- 229960000485 methotrexate Drugs 0.000 claims description 2
- HRDXJKGNWSUIBT-UHFFFAOYSA-N methoxybenzene Chemical group [CH2]OC1=CC=CC=C1 HRDXJKGNWSUIBT-UHFFFAOYSA-N 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 2
- 229960004857 mitomycin Drugs 0.000 claims description 2
- 125000004312 morpholin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])OC([H])(*)C1([H])[H] 0.000 claims description 2
- 125000004572 morpholin-3-yl group Chemical group N1C(COCC1)* 0.000 claims description 2
- 125000002912 morpholin-4-ylsulfonyl group Chemical group O1C([H])([H])C([H])([H])N(S(=O)(=O)[*])C([H])([H])C1([H])[H] 0.000 claims description 2
- 206010028537 myelofibrosis Diseases 0.000 claims description 2
- DILRJUIACXKSQE-UHFFFAOYSA-N n',n'-dimethylethane-1,2-diamine Chemical compound CN(C)CCN DILRJUIACXKSQE-UHFFFAOYSA-N 0.000 claims description 2
- BESOEZXXILQXLZ-UHFFFAOYSA-N n-(2-aminophenyl)-4-[[4-(2-methyl-3-propan-2-ylimidazol-4-yl)-1,3,5-triazin-2-yl]amino]benzamide Chemical compound CC(C)N1C(C)=NC=C1C1=NC=NC(NC=2C=CC(=CC=2)C(=O)NC=2C(=CC=CC=2)N)=N1 BESOEZXXILQXLZ-UHFFFAOYSA-N 0.000 claims description 2
- 125000004043 oxo group Chemical group O=* 0.000 claims description 2
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- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 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 2
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- 125000006225 propoxyethyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 2
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- 125000004290 pyrazolidin-3-yl group Chemical group [H]N1N([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
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- 125000001424 substituent group Chemical group 0.000 claims description 2
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- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 2
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- MNRILEROXIRVNJ-UHFFFAOYSA-N tioguanine Chemical compound N1C(N)=NC(=S)C2=NC=N[C]21 MNRILEROXIRVNJ-UHFFFAOYSA-N 0.000 claims description 2
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- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims description 2
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Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2170882A1 (en) * | 2007-06-26 | 2010-04-07 | Gilead Colorado, Inc. | Imidazopyridinyl thiazolyl histone deacetylase inhibitors |
| AU2009271003A1 (en) | 2008-07-14 | 2010-01-21 | Gilead Sciences, Inc. | Imidazolylpyrimidine compounds as HDAC and/or CDK inhibitors |
| NZ602832A (en) | 2008-07-14 | 2014-04-30 | Gilead Sciences Inc | Fused heterocyclic hdac inhibitor compounds |
| CA2728228A1 (en) | 2008-07-14 | 2010-01-21 | Gilead Sciences, Inc. | Oxindolyl inhibitor compounds |
| AU2009276699A1 (en) * | 2008-07-28 | 2010-02-04 | Gilead Sciences, Inc. | Cycloalkylidene and heterocycloalkylidene histone deacetylase inhibitor compounds |
| JP2012501344A (ja) | 2008-08-29 | 2012-01-19 | トレヴェンティス コーポレイション | アミロイド症を治療する組成物及び方法 |
| AU2009289649B2 (en) | 2008-09-03 | 2016-05-05 | Biomarin Pharmaceutical Inc. | Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors |
| WO2010075542A1 (en) | 2008-12-23 | 2010-07-01 | Curis, Inc. | Cdk inhibitors |
| KR20120031170A (ko) | 2009-06-08 | 2012-03-30 | 길리애드 사이언시즈, 인코포레이티드 | 알카노일아미노 벤즈아미드 아닐린 ｈｄａｃ 저해제 화합물 |
| ES2463826T3 (es) * | 2009-06-08 | 2014-05-29 | Gilead Sciences, Inc. | Compuestos inhibidores de HDAC de cicloalquilcarbamato benzamida anilina |
| JP6250403B2 (ja) | 2011-02-28 | 2017-12-20 | バイオマリン ファーマシューティカル インク | ヒストン脱アセチル化酵素阻害剤 |
| US8957066B2 (en) | 2011-02-28 | 2015-02-17 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| US10059723B2 (en) | 2011-02-28 | 2018-08-28 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| EP2701699B1 (en) | 2011-04-28 | 2019-10-16 | The Broad Institute, Inc. | Inhibitors of histone deacetylase |
| WO2013006408A1 (en) * | 2011-07-01 | 2013-01-10 | Tempero Pharmaceuticals, Inc. | Compounds and methods |
| JP6337255B2 (ja) * | 2012-07-27 | 2018-06-06 | ザ ブロード インスティテュート, インコーポレーテッドThe Broad Institute, Inc. | ヒストンデアセチラーゼの阻害剤 |
| US9914717B2 (en) | 2012-12-20 | 2018-03-13 | The Broad Institute, Inc. | Cycloalkenyl hydroxamic acid derivatives and their use as histone deacetylase inhibitors |
| PT2970139T (pt) | 2013-03-15 | 2018-08-01 | Biomarin Pharm Inc | Inibidores de hdac |
| TWI720269B (zh) * | 2016-11-22 | 2021-03-01 | 財團法人生物技術開發中心 | 用於調節刺蝟途徑之雜芳基胺化合物及其製法及用途 |
| MX2021011775A (es) | 2017-04-26 | 2023-01-10 | Basilea Pharm Int Ag | Procesos para la preparacion de furazanobencimidazoles y formas cristalinas de estos. |
| CN108929312A (zh) * | 2017-05-22 | 2018-12-04 | 南开大学 | 具有cdk或hdac抑制活性的新型苯并杂环联嘧啶抑制剂 |
| JP2021510733A (ja) | 2018-01-12 | 2021-04-30 | ケーディーエーシー セラピューティクス，インコーポレーテッドＫｄａｃ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | がんの処置のための選択的ヒストンデアセチラーゼ３（ｈｄａｃ３）インヒビターと免疫治療剤との組み合わせ |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| CN109761842B (zh) * | 2019-02-01 | 2021-11-30 | 浙江工业大学 | α-F-β-NHAc-羰基化合物的合成方法 |
| US11384083B2 (en) | 2019-02-15 | 2022-07-12 | Incyte Corporation | Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors |
| TW202100520A (zh) | 2019-03-05 | 2021-01-01 | 美商英塞特公司 | 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物 |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| CN116348458A (zh) | 2019-08-14 | 2023-06-27 | 因赛特公司 | 作为cdk2抑制剂的咪唑基嘧啶基胺化合物 |
| CN119930611A (zh) | 2019-10-11 | 2025-05-06 | 因赛特公司 | 作为cdk2抑制剂的双环胺 |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| CN114105958B (zh) * | 2021-12-03 | 2022-11-22 | 郑州大学第一附属医院 | 一组含羟肟酸的2-苯氨基嘧啶类衍生物及其应用 |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| MX2024007904A (es) | 2021-12-22 | 2024-09-18 | Augustine Therapeutics | Compuestos y uso de estos como inhibidores de hdac6. |
| WO2024261328A1 (en) * | 2023-06-21 | 2024-12-26 | Augustine Therapeutics | Amide-amine compounds and use thereof as hdac6 inhibitors |
| WO2024261327A1 (en) * | 2023-06-21 | 2024-12-26 | Augustine Therapeutics | 2-(heteroaryl-thio)-1-(heteroaryl)ethanone compounds and use thereof as hdac6 inhibitors |
Family Cites Families (103)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE264833T1 (de) | 1996-01-16 | 2004-05-15 | Bristol Myers Squibb Co | Konformationseingeschränkte aromatische inhibitoren des microsomalen triglyceridtransferproteins und verfahren |
| US20040006011A1 (en) | 1996-07-12 | 2004-01-08 | Gour Barbara J. | Peptidomimetic modulators of cell adhesion |
| US6174905B1 (en) | 1996-09-30 | 2001-01-16 | Mitsui Chemicals, Inc. | Cell differentiation inducer |
| US5760246A (en) | 1996-12-17 | 1998-06-02 | Biller; Scott A. | Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method |
| US6307049B1 (en) | 1998-09-30 | 2001-10-23 | The Procter & Gamble Co. | Heterocyclic 2-substituted ketoamides |
| GB9919778D0 (en) | 1999-08-21 | 1999-10-27 | Zeneca Ltd | Chemical compounds |
| DE60040676D1 (de) | 1999-09-17 | 2008-12-11 | Millennium Pharm Inc | BENZAMIDE UND ÄHNLICHE INHIBITOREN VON FAKTOR Xa |
| AU2001231154A1 (en) | 2000-01-24 | 2001-07-31 | Adherex Technologies Inc. | Peptidomimetic modulators of cell adhesion |
| AU2001234689A1 (en) | 2000-02-01 | 2001-08-14 | Cor Therapeutics, Inc. | Bivalent phenylene inhibitors of factor xa |
| US6403588B1 (en) | 2000-04-27 | 2002-06-11 | Yamanouchi Pharmaceutical Co., Ltd. | Imidazopyridine derivatives |
| AU2001252609A1 (en) | 2000-04-27 | 2001-11-12 | Imperial Cancer Research Technology Ltd. | Imidazopyridine derivatives |
| AU2001273040A1 (en) | 2000-06-27 | 2002-01-08 | Du Pont Pharmaceuticals Company | Factor xa inhibitors |
| GB0021726D0 (en) * | 2000-09-05 | 2000-10-18 | Astrazeneca Ab | Chemical compounds |
| AU2002214626A1 (en) | 2000-09-29 | 2002-04-08 | Cor Therapeutics, Inc. | Quaternary amines and related inhibitors of factor xa |
| AU2001295992A1 (en) | 2000-10-24 | 2002-05-06 | Sankyo Company Limited | Imidazopyridine derivatives |
| US7429599B2 (en) | 2000-12-06 | 2008-09-30 | Signal Pharmaceuticals, Llc | Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK |
| US7129242B2 (en) | 2000-12-06 | 2006-10-31 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto |
| GB0103926D0 (en) | 2001-02-17 | 2001-04-04 | Astrazeneca Ab | Chemical compounds |
| BR0207096A (pt) | 2001-02-20 | 2004-01-20 | Astrazeneca Ab | Uso de um composto, compostos, formulação farmacêutica, e, método de tratamento e/ou profilaxia de condições associadas com a inibição de glicogênio sintase quinase-3 |
| SE0100569D0 (sv) | 2001-02-20 | 2001-02-20 | Astrazeneca Ab | New compounds |
| EP1383799A4 (en) | 2001-04-10 | 2008-08-06 | Transtech Pharma Inc | PROBES, SYSTEMS AND METHODS FOR DISCOVERING MEDICAMENTS |
| HUP0400266A2 (hu) | 2001-06-21 | 2004-08-30 | Smithkline Beecham Corp. | Imidazo[1,2-a]piridin-származékok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk herpeszvírus-fertőzések megelőzésére vagy kezelésére |
| CA2450555A1 (en) | 2001-06-25 | 2003-01-03 | Merck & Co., Inc. | (pyrimidyl)(phenyl)substituted fused heteroaryl p38 inhibiting and pkg kinase inhibiting compounds |
| EP1270551A1 (en) | 2001-06-26 | 2003-01-02 | Aventis Pharma Deutschland GmbH | Urea derivatives with antiproteolytic activity |
| US7868204B2 (en) * | 2001-09-14 | 2011-01-11 | Methylgene Inc. | Inhibitors of histone deacetylase |
| WO2003031446A1 (en) | 2001-10-05 | 2003-04-17 | Smithkline Beecham Corporation | Imidazo-pyridine derivatives for use in the treatment of herpes viral infection |
| DE60225316T2 (de) | 2001-11-13 | 2009-02-26 | AXYS Pharmaceuticals, Inc., South San Francisco | Cyanoalkylamino-derivate als protease-hemmer |
| US6995144B2 (en) | 2002-03-14 | 2006-02-07 | Eisai Co., Ltd. | Nitrogen containing heterocyclic compounds and medicines containing the same |
| JP2003313126A (ja) | 2002-04-23 | 2003-11-06 | Sankyo Co Ltd | イミダゾピリジン誘導体を有効成分とする医薬 |
| JP2004002826A (ja) | 2002-04-24 | 2004-01-08 | Sankyo Co Ltd | 高分子イミダゾピリジン誘導体 |
| US20040034084A1 (en) | 2002-05-24 | 2004-02-19 | Celgene Corporation | Methods for using JNK inhibitors for treating or preventing disease-related wasting |
| GB0212049D0 (en) | 2002-05-24 | 2002-07-03 | Merck Sharp & Dohme | Therapeutic agents |
| CA2388358A1 (en) | 2002-05-31 | 2003-11-30 | Voiceage Corporation | A method and device for multi-rate lattice vector quantization |
| UA80296C2 (en) | 2002-09-06 | 2007-09-10 | Biogen Inc | Imidazolopyridines and methods of making and using the same |
| EP1551795A1 (en) | 2002-10-17 | 2005-07-13 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| US20040087642A1 (en) | 2002-10-24 | 2004-05-06 | Zeldis Jerome B. | Methods of using and compositions comprising a JNK inhibitor for the treatment, prevention, management and/or modification of pain |
| US20040092568A1 (en) | 2002-10-31 | 2004-05-13 | Zeldis Jerome B. | Methods for the treatment, prevention and management of macular degeneration |
| KR20050084027A (ko) | 2002-11-28 | 2005-08-26 | 쉐링 악티엔게젤샤프트 | Ｃｈｋ-, ｐｄｋ- 및 ａｋｔ-억제성 피리미딘, 그의제조방법 및 약제로서의 그의 용도 |
| US20050019366A1 (en) | 2002-12-31 | 2005-01-27 | Zeldis Jerome B. | Drug-coated stents and methods of use therefor |
| TW200424174A (en) | 2003-02-06 | 2004-11-16 | Hoffmann La Roche | New TP diamide |
| US7208491B2 (en) | 2003-02-07 | 2007-04-24 | Hoffmann-La Roche Inc. | N-monoacylated o-phenylenediamines |
| WO2004076452A1 (en) | 2003-02-26 | 2004-09-10 | Merck Sharp & Dohme Limited | 5,8-DIFLUOROIMIDAZO[1,2-a]PYRIDINES AS GABA-A α2/α3 LIGANDS FOR TREATING ANXIETY AND/OR DEPRESSION |
| US7320989B2 (en) | 2003-02-28 | 2008-01-22 | Encysive Pharmaceuticals, Inc. | Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists |
| EP1603900A4 (en) | 2003-03-06 | 2008-08-20 | Merck & Co Inc | IMIDAZOPYRIDIN COMPOUNDS WITH EFFECT AGAINST PROTOZOEN |
| PL1611088T3 (pl) | 2003-04-07 | 2009-11-30 | Pharmacyclics Inc | Hydroksamiany jako środki terapeutyczne |
| EA200501462A1 (ru) | 2003-04-15 | 2006-04-28 | Пфайзер Инк. | Альфа-замещенные карбоновые кислоты в качестве модуляторов ppar |
| US20050234066A1 (en) | 2004-04-15 | 2005-10-20 | Agouron Pharmaceuticals, Inc. | Alpha substituted carboxylic acids |
| US20050187266A1 (en) | 2003-04-15 | 2005-08-25 | Pfizer Inc | Alpha substituted carboxylic acids |
| EP1628666B1 (en) | 2003-05-14 | 2015-09-23 | NeuroGenetic Pharmaceuticals, Inc. | Compouds and uses thereof in modulating amyloid beta |
| GB0311276D0 (en) * | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
| WO2005006945A2 (en) | 2003-07-03 | 2005-01-27 | The Salk Institute For Biological Studies | Methods for treating neural disorders and compounds useful therefor |
| CA2539117A1 (en) | 2003-09-24 | 2005-04-07 | Methylgene Inc. | Inhibitors of histone deacetylase |
| CA2744997A1 (en) | 2003-09-26 | 2005-04-07 | Exelixis, Inc. | C-met modulators and method of use |
| KR20060124610A (ko) | 2003-11-06 | 2006-12-05 | 셀진 코포레이션 | 석면-관련된 질환 또는 장애를 치료 및 관리하기 위하여ｊｎｋ 억제제를 사용하는 방법 및 이 물질을 포함하는조성물 |
| US7524851B2 (en) | 2003-12-05 | 2009-04-28 | Robert Bosch Gesellschaft Fur Medizinische Forschung (Rbmf) | Diagnostic methods for therapeutic compounds and methods for monitoring azathioprine therapy |
| US7429590B2 (en) | 2003-12-10 | 2008-09-30 | Merck & Co. Inc. | Antiprotozoal imidazopyridine compounds |
| US7671181B2 (en) | 2004-01-16 | 2010-03-02 | Merck Sharp & Dohme Corp. | Polynucleotides encoding coccidian parasite casein kinase I, a chemotherapeutic target for antiprotozoal agents |
| WO2005077368A2 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
| WO2005077373A2 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
| DE102004008141A1 (de) | 2004-02-19 | 2005-09-01 | Abbott Gmbh & Co. Kg | Guanidinverbindungen und ihre Verwendung als Bindungspartner für 5-HT5-Rezeptoren |
| US20070093492A1 (en) | 2004-03-09 | 2007-04-26 | Weir-Torn Jiaang | Pyrrolidine derivatives |
| EP1735319B1 (en) | 2004-03-26 | 2017-05-03 | MethylGene Inc. | Inhibitors of histone deacetylase |
| US7253204B2 (en) | 2004-03-26 | 2007-08-07 | Methylgene Inc. | Inhibitors of histone deacetylase |
| MXPA06012130A (es) | 2004-04-20 | 2007-01-31 | Transtech Pharma Inc | Derivados de tiazol y pirimidina substituidos como moduladores del receptor de melanocortina. |
| WO2005102318A1 (en) | 2004-04-20 | 2005-11-03 | Ab Science | Use of c-kit inhibitors for treating hiv related diseases |
| WO2005102325A1 (en) | 2004-04-20 | 2005-11-03 | Ab Science | Use of c-kit inhibitors for treating inflammatory muscle disorders including myositis and muscular dystrophy |
| WO2005102326A2 (en) | 2004-04-23 | 2005-11-03 | Ab Science | Use of c-kit inhibitors for treating renal diseases |
| EP1758654A1 (en) | 2004-04-23 | 2007-03-07 | AB Science | Use of c-kit inhibitors for treating plasmodium related diseases |
| CA2564574A1 (en) | 2004-04-23 | 2005-11-03 | Ab Science | Use of c-kit inhibitors for treating fibrosis |
| US20070249628A1 (en) | 2004-05-18 | 2007-10-25 | Alain Moussy | Use of Mast Cells Inhibitors for Treating Patients Exposed to Chemical or Biological Weapons |
| WO2005115385A1 (en) | 2004-05-24 | 2005-12-08 | Ab Science | Use of c-kit inhibitors for treating acne |
| WO2005115304A2 (en) | 2004-05-24 | 2005-12-08 | Ab Science | Use of c-kit inhibitors for treating fibrodysplasia |
| PL1781639T3 (pl) | 2004-07-28 | 2012-07-31 | Janssen Pharmaceutica Nv | Podstawione pochodne indolilo-alkiloaminowe jako nowe inhibitory deacetylazy histonowej |
| WO2006038001A1 (en) | 2004-10-06 | 2006-04-13 | Celltech R & D Limited | Aminopyrimidine derivatives as jnk inhibitors |
| AU2005295734A1 (en) | 2004-10-15 | 2006-04-27 | Biogen Idec Ma Inc. | Methods of treating vascular injuries |
| CA2588558A1 (en) | 2004-11-23 | 2006-06-01 | Celgene Corporation | Jnk inhibitors for treatment of cns injury |
| CA2588517A1 (en) | 2004-12-01 | 2006-06-08 | Devgen N.V. | 5-carboxamido substituted thiazole derivatives that interact with ion channels, in particular with ion channels from the kv family |
| US20090099160A1 (en) | 2004-12-17 | 2009-04-16 | David Andrews | 4-(4-(Imidazol-4-Yl) Pyrimidin-2-Ylamino) Benzamides as CDK Inhibitors |
| WO2006070943A1 (ja) | 2004-12-28 | 2006-07-06 | Takeda Pharmaceutical Company Limited | 縮合イミダゾール化合物およびその用途 |
| WO2006077401A1 (en) | 2005-01-19 | 2006-07-27 | Biolipox Ab | Pyrrolopyridines useful in the treatment of inflammation |
| GB0504753D0 (en) * | 2005-03-08 | 2005-04-13 | Astrazeneca Ab | Chemical compounds |
| US20060223807A1 (en) | 2005-03-29 | 2006-10-05 | University Of Massachusetts Medical School, A Massachusetts Corporation | Therapeutic methods for type I diabetes |
| JP2008537748A (ja) | 2005-04-06 | 2008-09-25 | エクセリクシス、インコーポレイテッド | ｃ−Ｍｅｔモジュレーター及び使用方法 |
| SG159561A1 (en) | 2005-05-09 | 2010-03-30 | Achillion Pharmaceuticals Inc | Thiazole compounds and methods of use |
| JP4528918B2 (ja) | 2005-06-21 | 2010-08-25 | 学校法人 関西大学 | カルボキサミド誘導体 |
| MA28394B1 (fr) | 2005-06-24 | 2007-01-02 | Genelabs Tech Inc | Derives d'heteroaryle pour traitement des virus |
| US7309787B2 (en) | 2005-07-13 | 2007-12-18 | Allergan, Inc. | Kinase inhibitors |
| EP1904065A2 (en) | 2005-07-14 | 2008-04-02 | AB Science | Use of dual c-kit/fgfr3 inhibitors for treating multiple myeloma |
| US20100069387A1 (en) | 2005-09-07 | 2010-03-18 | Palmer Stephen S | IKK Inhibitors for the Treatment of Endometriosis |
| WO2007037187A1 (ja) | 2005-09-27 | 2007-04-05 | Shionogi & Co., Ltd. | Ｐｇｄ２受容体アンタゴニスト活性を有するスルホンアミド誘導体 |
| WO2007036732A1 (en) | 2005-09-30 | 2007-04-05 | Astrazeneca Ab | Imidazo [1,2-a] pyridine having anti-cell-proliferation activity |
| AR058073A1 (es) * | 2005-10-03 | 2008-01-23 | Astrazeneca Ab | Derivados de imidazol 5-il-pirimidina, procesos de obtencion, composiciones farmaceuticas y usos |
| ITMI20060296A1 (it) | 2006-02-17 | 2007-08-18 | Alberto Lodolo | Dispositivo di intercettazione multifunzionale |
| EP1996233A2 (en) | 2006-02-27 | 2008-12-03 | Gilead Colorado, Inc. | Combinations comprising a histone deacetylase inhibiting agent and a nuclear hormone receptor ligand for treating cardiovascular conditions |
| CA2649861A1 (en) | 2006-04-26 | 2007-11-08 | Merck & Co., Inc. | Disubstituted aniline compounds |
| US20080221132A1 (en) * | 2006-09-11 | 2008-09-11 | Xiong Cai | Multi-Functional Small Molecules as Anti-Proliferative Agents |
| EP2170882A1 (en) | 2007-06-26 | 2010-04-07 | Gilead Colorado, Inc. | Imidazopyridinyl thiazolyl histone deacetylase inhibitors |
| CA2728228A1 (en) | 2008-07-14 | 2010-01-21 | Gilead Sciences, Inc. | Oxindolyl inhibitor compounds |
| AU2009271003A1 (en) | 2008-07-14 | 2010-01-21 | Gilead Sciences, Inc. | Imidazolylpyrimidine compounds as HDAC and/or CDK inhibitors |
| NZ602832A (en) | 2008-07-14 | 2014-04-30 | Gilead Sciences Inc | Fused heterocyclic hdac inhibitor compounds |
| AU2009276699A1 (en) | 2008-07-28 | 2010-02-04 | Gilead Sciences, Inc. | Cycloalkylidene and heterocycloalkylidene histone deacetylase inhibitor compounds |
| ES2463826T3 (es) | 2009-06-08 | 2014-05-29 | Gilead Sciences, Inc. | Compuestos inhibidores de HDAC de cicloalquilcarbamato benzamida anilina |
| KR20120031170A (ko) | 2009-06-08 | 2012-03-30 | 길리애드 사이언시즈, 인코포레이티드 | 알카노일아미노 벤즈아미드 아닐린 ｈｄａｃ 저해제 화합물 |
-
2009
- 2009-07-14 AU AU2009271003A patent/AU2009271003A1/en not_active Abandoned
- 2009-07-14 WO PCT/US2009/050558 patent/WO2010009139A2/en not_active Ceased
- 2009-07-14 JP JP2011518843A patent/JP5640005B2/ja not_active Expired - Fee Related
- 2009-07-14 CA CA2729909A patent/CA2729909A1/en not_active Abandoned
- 2009-07-14 NZ NZ590283A patent/NZ590283A/xx not_active IP Right Cessation
- 2009-07-14 US US12/502,870 patent/US8134000B2/en not_active Expired - Fee Related
-
2014
- 2014-01-07 JP JP2014000744A patent/JP2014058583A/ja active Pending
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