JP2010536753A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2010536753A5 JP2010536753A5 JP2010521020A JP2010521020A JP2010536753A5 JP 2010536753 A5 JP2010536753 A5 JP 2010536753A5 JP 2010521020 A JP2010521020 A JP 2010521020A JP 2010521020 A JP2010521020 A JP 2010521020A JP 2010536753 A5 JP2010536753 A5 JP 2010536753A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- hydroxy
- compound
- independently
- 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 cyano, nitro, guanidino Chemical group 0.000 claims description 153
- 150000001875 compounds Chemical class 0.000 claims description 152
- 238000000034 method Methods 0.000 claims description 72
- 125000000623 heterocyclic group Chemical group 0.000 claims description 68
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 63
- 125000001072 heteroaryl group Chemical group 0.000 claims description 62
- 229910052757 nitrogen Inorganic materials 0.000 claims description 61
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 52
- 125000003107 substituted aryl group Chemical group 0.000 claims description 52
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 52
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 51
- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 47
- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 45
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 45
- 125000001188 haloalkyl group Chemical group 0.000 claims description 44
- 125000001475 halogen functional group Chemical group 0.000 claims description 40
- 125000000217 alkyl group Chemical group 0.000 claims description 38
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 34
- 229910052799 carbon Inorganic materials 0.000 claims description 32
- 125000004432 carbon atom Chemical group C* 0.000 claims description 29
- 125000001424 substituent group Chemical group 0.000 claims description 27
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 26
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 26
- 241000124008 Mammalia Species 0.000 claims description 24
- 229910052717 sulfur Inorganic materials 0.000 claims description 23
- 150000003839 salts Chemical class 0.000 claims description 21
- 239000012453 solvate Substances 0.000 claims description 21
- 206010028980 Neoplasm Diseases 0.000 claims description 17
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 15
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 15
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 15
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 13
- 125000003342 alkenyl group Chemical group 0.000 claims description 12
- 201000011510 cancer Diseases 0.000 claims description 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 11
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 125000004414 alkyl thio group Chemical group 0.000 claims description 9
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 9
- 229910019142 PO4 Inorganic materials 0.000 claims description 8
- 229910052760 oxygen Inorganic materials 0.000 claims description 8
- 239000010452 phosphate Substances 0.000 claims description 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 6
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 6
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 5
- 125000000131 cyclopropyloxy group Chemical group C1(CC1)O* 0.000 claims description 5
- WEVYNIUIFUYDGI-UHFFFAOYSA-N 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide Chemical compound NC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 WEVYNIUIFUYDGI-UHFFFAOYSA-N 0.000 claims description 3
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims description 3
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims description 3
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims description 3
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims description 3
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 3
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims description 3
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- SAFUWGYHSHRERQ-UHFFFAOYSA-N [2-[4-(2,3-dihydro-1H-inden-5-yl)-5-oxo-1H-1,2,4-triazol-3-yl]-5-hydroxy-4-propan-2-ylphenyl] dihydrogen phosphate Chemical compound C1=C(O)C(C(C)C)=CC(C=2N(C(O)=NN=2)C=2C=C3CCCC3=CC=2)=C1OP(O)(O)=O SAFUWGYHSHRERQ-UHFFFAOYSA-N 0.000 claims description 2
- HSPYRDASOJURBP-UHFFFAOYSA-N [4-(2,3-dihydro-1H-inden-5-yl)-5-(2,4-dihydroxy-5-propan-2-ylphenyl)-1,2,4-triazol-3-yl] dihydrogen phosphate Chemical compound C1=C(O)C(C(C)C)=CC(C=2N(C(OP(O)(O)=O)=NN=2)C=2C=C3CCCC3=CC=2)=C1O HSPYRDASOJURBP-UHFFFAOYSA-N 0.000 claims description 2
- BALPIGOECICYSD-UHFFFAOYSA-N [4-[4-(1,3-dimethylindol-5-yl)-5-oxo-1H-1,2,4-triazol-3-yl]-2-ethyl-5-hydroxyphenyl] dihydrogen phosphate Chemical compound C1=C(OP(O)(O)=O)C(CC)=CC(C=2N(C(O)=NN=2)C=2C=C3C(C)=CN(C)C3=CC=2)=C1O BALPIGOECICYSD-UHFFFAOYSA-N 0.000 claims description 2
- CKKHGJCUBHEFQY-UHFFFAOYSA-N [4-[4-(2,3-dihydro-1,4-benzodioxin-6-ylmethyl)-5-oxo-1H-1,2,4-triazol-3-yl]-5-hydroxy-2-propan-2-ylphenyl] dihydrogen phosphate Chemical compound C1=C(OP(O)(O)=O)C(C(C)C)=CC(C=2N(C(O)=NN=2)CC=2C=C3OCCOC3=CC=2)=C1O CKKHGJCUBHEFQY-UHFFFAOYSA-N 0.000 claims description 2
- BYPDYJHVTIARDI-UHFFFAOYSA-N [4-[4-(2,3-dihydro-1H-inden-5-yl)-5-oxo-1H-1,2,4-triazol-3-yl]-5-hydroxy-2-propan-2-ylphenyl] dihydrogen phosphate Chemical compound C1=C(OP(O)(O)=O)C(C(C)C)=CC(C=2N(C(O)=NN=2)C=2C=C3CCCC3=CC=2)=C1O BYPDYJHVTIARDI-UHFFFAOYSA-N 0.000 claims description 2
- WLUZVUCJKRMBER-UHFFFAOYSA-N [4-[4-(4-bromo-2-methylphenyl)-5-oxo-1H-1,2,4-triazol-3-yl]-3-hydroxyphenyl] dihydrogen phosphate Chemical compound CC1=CC(Br)=CC=C1N1C(C=2C(=CC(OP(O)(O)=O)=CC=2)O)=NN=C1O WLUZVUCJKRMBER-UHFFFAOYSA-N 0.000 claims description 2
- YBUMENZYNGJBRV-UHFFFAOYSA-N [5-hydroxy-2-propan-2-yl-4-(4-spiro[1,3-dihydroindene-2,2'-1,3-dioxolane]-5-yl-5-sulfanylidene-1H-1,2,4-triazol-3-yl)phenyl] dihydrogen phosphate Chemical compound C1=C(OP(O)(O)=O)C(C(C)C)=CC(C=2N(C(S)=NN=2)C=2C=C3CC4(CC3=CC=2)OCCO4)=C1O YBUMENZYNGJBRV-UHFFFAOYSA-N 0.000 claims description 2
- JNWFIPVDEINBAI-UHFFFAOYSA-N [5-hydroxy-4-[4-(1-methylindol-5-yl)-5-oxo-1H-1,2,4-triazol-3-yl]-2-propan-2-ylphenyl] dihydrogen phosphate Chemical compound C1=C(OP(O)(O)=O)C(C(C)C)=CC(C=2N(C(=O)NN=2)C=2C=C3C=CN(C)C3=CC=2)=C1O JNWFIPVDEINBAI-UHFFFAOYSA-N 0.000 claims description 2
- KDGFMVVMKCWWMT-UHFFFAOYSA-N [5-hydroxy-4-[4-(6-morpholin-4-ylpyridin-3-yl)-5-oxo-1H-1,2,4-triazol-3-yl]-2-propan-2-ylphenyl] dihydrogen phosphate Chemical compound C1=C(OP(O)(O)=O)C(C(C)C)=CC(C=2N(C(O)=NN=2)C=2C=NC(=CC=2)N2CCOCC2)=C1O KDGFMVVMKCWWMT-UHFFFAOYSA-N 0.000 claims description 2
- PESPGTPZJKWRDS-UHFFFAOYSA-N [5-hydroxy-4-[4-[(4-methoxyphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]-2-propan-2-ylphenyl] dihydrogen phosphate Chemical compound C1=CC(OC)=CC=C1CN1C(C=2C(=CC(OP(O)(O)=O)=C(C(C)C)C=2)O)=NN=C1O PESPGTPZJKWRDS-UHFFFAOYSA-N 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- AWHPLFDGSGMBIN-UHFFFAOYSA-L disodium [5-hydroxy-4-[4-(1-methylindol-5-yl)-5-oxo-1H-1,2,4-triazol-3-yl]-2-propan-2-ylphenyl] phosphate Chemical compound [Na+].[Na+].CC(C)c1cc(-c2nnc(O)n2-c2ccc3n(C)ccc3c2)c(O)cc1OP([O-])([O-])=O AWHPLFDGSGMBIN-UHFFFAOYSA-L 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 125000000081 (C5-C8) cycloalkenyl group Chemical group 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 description 14
- 239000000651 prodrug Substances 0.000 description 14
- 239000000243 solution Substances 0.000 description 7
- 125000000304 alkynyl group Chemical group 0.000 description 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 description 5
- RGICCULPCWNRAB-UHFFFAOYSA-N 2-[2-(2-hexoxyethoxy)ethoxy]ethanol Chemical compound CCCCCCOCCOCCOCCO RGICCULPCWNRAB-UHFFFAOYSA-N 0.000 description 5
- 210000004027 cell Anatomy 0.000 description 5
- 230000002401 inhibitory effect Effects 0.000 description 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 description 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 4
- 125000005334 azaindolyl group Chemical group N1N=C(C2=CC=CC=C12)* 0.000 description 4
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 4
- 125000005605 benzo group Chemical group 0.000 description 4
- 125000004618 benzofuryl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 description 4
- 125000005874 benzothiadiazolyl group Chemical group 0.000 description 4
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 description 4
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 description 4
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 4
- 230000015556 catabolic process Effects 0.000 description 4
- 238000006731 degradation reaction Methods 0.000 description 4
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 description 4
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 description 4
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 description 4
- 125000001041 indolyl group Chemical group 0.000 description 4
- 230000001939 inductive effect Effects 0.000 description 4
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 description 4
- 230000003204 osmotic effect Effects 0.000 description 4
- 125000004076 pyridyl group Chemical group 0.000 description 4
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 4
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 4
- 125000005888 tetrahydroindolyl group Chemical group 0.000 description 4
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 description 3
- 101001016865 Homo sapiens Heat shock protein HSP 90-alpha Proteins 0.000 description 3
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 description 3
- 239000002246 antineoplastic agent Substances 0.000 description 3
- 229940127089 cytotoxic agent Drugs 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 125000001544 thienyl group Chemical group 0.000 description 3
- 0 *c1nnc(-c2ccc(*)cc2*)[n]1* Chemical compound *c1nnc(-c2ccc(*)cc2*)[n]1* 0.000 description 2
- 208000028564 B-cell non-Hodgkin lymphoma Diseases 0.000 description 2
- 206010025323 Lymphomas Diseases 0.000 description 2
- 206010061309 Neoplasm progression Diseases 0.000 description 2
- 208000009052 Precursor T-Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 2
- 125000002947 alkylene group Chemical group 0.000 description 2
- 230000017531 blood circulation Effects 0.000 description 2
- 210000004204 blood vessel Anatomy 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 210000000987 immune system Anatomy 0.000 description 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 2
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 description 2
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 2
- DTXOCJGLLMAFBX-UHFFFAOYSA-N oxo-[[1-[2-[[4-(oxoazaniumylmethylidene)pyridin-1-yl]methoxy]ethoxymethyl]pyridin-4-ylidene]methyl]azanium;dichloride Chemical compound [Cl-].[Cl-].C1=CC(=C[NH+]=O)C=CN1COCCOCN1C=CC(=C[NH+]=O)C=C1 DTXOCJGLLMAFBX-UHFFFAOYSA-N 0.000 description 2
- 230000037361 pathway Effects 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 230000005751 tumor progression Effects 0.000 description 2
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 description 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 208000011691 Burkitt lymphomas Diseases 0.000 description 1
- 206010017533 Fungal infection Diseases 0.000 description 1
- 102000003676 Glucocorticoid Receptors Human genes 0.000 description 1
- 108090000079 Glucocorticoid Receptors Proteins 0.000 description 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 description 1
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 description 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 description 1
- 208000031888 Mycoses Diseases 0.000 description 1
- 206010029113 Neovascularisation Diseases 0.000 description 1
- 206010029461 Nodal marginal zone B-cell lymphomas Diseases 0.000 description 1
- 208000030852 Parasitic disease Diseases 0.000 description 1
- 208000027190 Peripheral T-cell lymphomas Diseases 0.000 description 1
- 208000033014 Plasma cell tumor Diseases 0.000 description 1
- 208000007452 Plasmacytoma Diseases 0.000 description 1
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 208000031672 T-Cell Peripheral Lymphoma Diseases 0.000 description 1
- 206010042971 T-cell lymphoma Diseases 0.000 description 1
- 208000020982 T-lymphoblastic lymphoma Diseases 0.000 description 1
- 108091023040 Transcription factor Proteins 0.000 description 1
- 102000040945 Transcription factor Human genes 0.000 description 1
- 102000007537 Type II DNA Topoisomerases Human genes 0.000 description 1
- 108010046308 Type II DNA Topoisomerases Proteins 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 208000016025 Waldenstroem macroglobulinemia Diseases 0.000 description 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 description 1
- 125000003282 alkyl amino group Chemical group 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 description 1
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 description 1
- 125000000522 cyclooctenyl group Chemical group C1(=CCCCCCC1)* 0.000 description 1
- 125000004663 dialkyl amino group Chemical group 0.000 description 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 1
- 201000003444 follicular lymphoma Diseases 0.000 description 1
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 description 1
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 description 1
- 230000001401 hemangioblastic effect Effects 0.000 description 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 1
- 208000026278 immune system disease Diseases 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 230000000527 lymphocytic effect Effects 0.000 description 1
- 208000020968 mature T-cell and NK-cell non-Hodgkin lymphoma Diseases 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 230000014399 negative regulation of angiogenesis Effects 0.000 description 1
- 208000010626 plasma cell neoplasm Diseases 0.000 description 1
- 229940081860 plasma-lyte 148 Drugs 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
- 230000009257 reactivity Effects 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 125000005415 substituted alkoxy group Chemical group 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US96444707P | 2007-08-13 | 2007-08-13 | |
| US60/964,447 | 2007-08-13 | ||
| PCT/US2008/009667 WO2009023211A1 (en) | 2007-08-13 | 2008-08-13 | Triazole compounds that modulate hsp90 activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010536753A JP2010536753A (ja) | 2010-12-02 |
| JP2010536753A5 true JP2010536753A5 (enExample) | 2011-09-22 |
| JP5596543B2 JP5596543B2 (ja) | 2014-09-24 |
Family
ID=39884398
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010521020A Expired - Fee Related JP5596543B2 (ja) | 2007-08-13 | 2008-08-13 | Ｈｓｐ９０活性を調節するトリアゾール化合物 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US8742133B2 (enExample) |
| EP (1) | EP2193135A1 (enExample) |
| JP (1) | JP5596543B2 (enExample) |
| KR (1) | KR20100057030A (enExample) |
| CN (1) | CN101801983B (enExample) |
| AU (1) | AU2008287367B2 (enExample) |
| BR (1) | BRPI0815116A2 (enExample) |
| CA (1) | CA2695995C (enExample) |
| IL (1) | IL203663A (enExample) |
| MX (1) | MX2010001565A (enExample) |
| NZ (1) | NZ583205A (enExample) |
| TW (1) | TWI438199B (enExample) |
| WO (1) | WO2009023211A1 (enExample) |
| ZA (1) | ZA201001064B (enExample) |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS52642B (sr) | 2004-11-18 | 2013-06-28 | Synta Pharmaceuticals Corp. | Jedinjenja triazola koja modulišu aktivnost hsp90 |
| EP1934185A1 (en) | 2005-08-12 | 2008-06-25 | Synta Pharmaceuticals Corporation | Pyrazole compounds that modulate hsp90 activity |
| US20070250391A1 (en) * | 2006-04-05 | 2007-10-25 | Prade Hendrik D | Merchandising system and method for food and non-food items for a meal kit |
| AU2007267859B2 (en) | 2006-05-25 | 2012-04-12 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate Hsp90 activity |
| EP2032545A2 (en) * | 2006-05-25 | 2009-03-11 | Synta Pharmaceuticals Corporation | Compounds that modulate hsp90 activity and methods for identifying same |
| US8034834B2 (en) | 2006-05-25 | 2011-10-11 | Synta Pharmaceuticals Corp. | Method for treating proliferative disorders with HSP90 inhibitors |
| EP2034996A2 (en) | 2006-05-25 | 2009-03-18 | Synta Pharmaceuticals Corporation | Triazole compounds that modulate hsp90 activity |
| CA2653336C (en) | 2006-05-25 | 2014-10-28 | Synta Pharmaceuticals Corp. | Method for treating non-hodgkin's lymphoma |
| NZ579403A (en) | 2007-02-08 | 2012-03-30 | Synta Pharmaceuticals Corp | Triazole compounds that are useful in the treatment of proliferative disorders, such as cancer |
| KR20100057030A (ko) * | 2007-08-13 | 2010-05-28 | 신타 파마슈티칼스 코프. | Ｈｓｐ90의 활성을 조절하는 트라이아졸 화합물 |
| US9156836B2 (en) * | 2008-05-16 | 2015-10-13 | Synta Pharmaceuticals Corp. | Tricyclic triazole compounds that modulate HSP90 activity |
| US8450500B2 (en) | 2008-06-04 | 2013-05-28 | Synta Pharmaceuticals Corp. | Pyrrole compounds that modulate HSP90 activity |
| WO2009158026A1 (en) | 2008-06-27 | 2009-12-30 | Synta Pharmaceuticals Corp. | Hydrazonamide compounds that modulate hsp90 activity |
| WO2010017479A1 (en) * | 2008-08-08 | 2010-02-11 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate hsp90 activity |
| WO2010017545A2 (en) | 2008-08-08 | 2010-02-11 | Synta Pharamceuticals Corp. | Triazole compounds that modulate hsp90 activity |
| FR2949467B1 (fr) | 2009-09-03 | 2011-11-25 | Sanofi Aventis | Nouveaux derives de 5,6,7,8-tetrahydroindolizine inhibiteurs d'hsp90, compositions les contenant et utilisation |
| NZ599445A (en) * | 2009-10-19 | 2014-04-30 | Synta Pharmaceuticals Corp | Combination cancer therapy with hsp90 inhibitory compounds |
| WO2011133520A1 (en) | 2010-04-19 | 2011-10-27 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of a hsp90 inhibitory compounds and a egfr inhibitor |
| EP2560641A2 (en) | 2010-04-19 | 2013-02-27 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of a hsp90 inhibitory compounds and a vegf inhibitor |
| WO2011146803A1 (en) | 2010-05-20 | 2011-11-24 | Synta Pharmaceuticals Corp. | Method of treating lung adenocarcinoma with hsp90 inhibitory compounds |
| US20130172333A1 (en) | 2010-05-20 | 2013-07-04 | Synta Pharmaceuticals Corp. | Formulation and dosing of hsp90 inhibitory compounds |
| US20130171105A1 (en) | 2010-05-24 | 2013-07-04 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of a hsp90 inhibitory compound and a topoisomerase ii inhibitor |
| KR20130099006A (ko) * | 2010-08-23 | 2013-09-05 | 다이이찌 산쿄 가부시키가이샤 | 3 고리성 피라졸로피리미딘 유도체의 프리체 결정 |
| US9089570B2 (en) * | 2010-09-03 | 2015-07-28 | Tactical Therapeutics Inc | Compositions for treating cancers having acquired resitance to prior chemotherapeutic and targeted drugs using carboxyamidotriazole orotate |
| AU2011302344B2 (en) | 2010-09-13 | 2015-01-15 | Synta Pharmaceuticals Corp. | HSP90 inhibitors for treating non-small cell lung cancers in wild-type EGFR and/or KRAS patients |
| WO2012078757A2 (en) | 2010-12-08 | 2012-06-14 | Synta Pharmaceuticals Corp. | Combination breast cancer therapy with hsp90 inhibitory compounds |
| US20130331357A1 (en) | 2011-01-11 | 2013-12-12 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitory compounds with proteasome inhibitors |
| WO2012116061A1 (en) | 2011-02-23 | 2012-08-30 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitory compounds with radiotherapy |
| AU2012243289A1 (en) | 2011-02-24 | 2013-08-29 | Synta Pharmaceuticals Corp. | Prostate cancer therapy with Hsp90 inhibitory compounds |
| WO2012116247A1 (en) | 2011-02-25 | 2012-08-30 | Synta Pharmaceuticals Corp. | Hsp90 inhibitory compounds in treating jak/stat signaling-mediated cancers |
| EP2714039A1 (en) * | 2011-05-23 | 2014-04-09 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitory compounds with mek inhibitors |
| WO2012162372A1 (en) | 2011-05-24 | 2012-11-29 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitory compounds with mtor/p13k inhibitors |
| WO2012162584A1 (en) * | 2011-05-26 | 2012-11-29 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitory compounds with chk inhibitors |
| WO2013006864A2 (en) | 2011-07-07 | 2013-01-10 | Synta Pharmaceuticals Corp. | Treating cancer with hsp90 inhibitory compounds |
| WO2013067165A1 (en) | 2011-11-02 | 2013-05-10 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitors with platinum-containing agents |
| JP2014532712A (ja) * | 2011-11-02 | 2014-12-08 | シンタ ファーマシューティカルズ コーポレーション | トポイソメラーゼｉ阻害剤とｈｓｐ９０阻害剤の組合せを使用する癌療法 |
| WO2013074594A1 (en) | 2011-11-14 | 2013-05-23 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitors with braf inhibitors |
| JP2015515477A (ja) * | 2012-04-04 | 2015-05-28 | シンタ ファーマシューティカルズ コーポレーション | Ｈｓｐ９０活性を調節する新規トリアゾール化合物 |
| JP2015516439A (ja) | 2012-05-10 | 2015-06-11 | シンタ ファーマシューティカルズ コーポレーション | Ｈｓｐ９０阻害化合物で癌を治療すること |
| CN103664910B (zh) * | 2012-09-14 | 2017-07-04 | 南京大学 | 含1，4‑苯并二噁烷的1，2，4‑三氮唑类衍生物及其制法与其抗菌活性 |
| KR101941004B1 (ko) * | 2013-03-25 | 2019-01-23 | 주식회사 엘지화학 | 조절 t 세포로의 분화 유도 및 증식 촉진을 통한 면역 반응 억제용 약학 조성물 |
| JP6497767B2 (ja) | 2013-12-16 | 2019-04-10 | 日本化薬株式会社 | 癌治療におけるｈｓｐ９０阻害剤の抗腫瘍効果を予測する方法 |
| JP2018504446A (ja) | 2015-02-09 | 2018-02-15 | シンタ ファーマシューティカルズ コーポレーション | がんを処置するためのｈｓｐ９０阻害剤およびｐｄ−１阻害剤の組み合わせ治療 |
| CA2985542C (en) | 2015-05-20 | 2023-10-10 | Amgen Inc. | Triazole agonists of the apj receptor |
| WO2017192485A1 (en) | 2016-05-03 | 2017-11-09 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
| WO2018097944A1 (en) | 2016-11-16 | 2018-05-31 | Amgen Inc. | Triazole furan compounds as agonists of the apj receptor |
| US10689367B2 (en) | 2016-11-16 | 2020-06-23 | Amgen Inc. | Triazole pyridyl compounds as agonists of the APJ receptor |
| US11191762B2 (en) | 2016-11-16 | 2021-12-07 | Amgen Inc. | Alkyl substituted triazole compounds as agonists of the APJ Receptor |
| US11020395B2 (en) | 2016-11-16 | 2021-06-01 | Amgen Inc. | Cycloalkyl substituted triazole compounds as agonists of the APJ receptor |
| WO2018093579A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Triazole phenyl compounds as agonists of the apj receptor |
| EP3541805B1 (en) | 2016-11-16 | 2020-10-14 | Amgen Inc. | Heteroaryl-substituted triazoles as apj receptor agonists |
| US10767164B2 (en) | 2017-03-30 | 2020-09-08 | The Research Foundation For The State University Of New York | Microenvironments for self-assembly of islet organoids from stem cells differentiation |
| MA50509A (fr) | 2017-11-03 | 2021-06-02 | Amgen Inc | Agonistes de triazole fusionnés du récepteur apj |
| MA52487A (fr) | 2018-05-01 | 2021-03-10 | Amgen Inc | Pyrimidinones substituées en tant qu'agonistes du récepteur apj |
| EP4072587A4 (en) * | 2019-12-10 | 2023-11-15 | Washington University | Debaryomyces species as an indicator of non-healing ulcers in crohn's disease |
| US20240226067A9 (en) * | 2021-03-02 | 2024-07-11 | The Johns Hopkins University | Anti-fibrotic therapies |
| CN113121505B (zh) * | 2021-03-02 | 2023-03-07 | 中国人民解放军海军军医大学 | 一种具有抗真菌与抗肿瘤双重作用的三唑酮类化合物及应用 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU621245B2 (en) * | 1989-10-17 | 1992-03-05 | Boehringer Mannheim Gmbh | Hydrolase substrates, a process for the preparation thereof and agents containing them |
| AU2004248160B2 (en) * | 2003-06-12 | 2010-05-27 | Merck Sharp & Dohme Corp. | Prodrugs of mitotic kinesin inhibitors |
| RS52642B (sr) * | 2004-11-18 | 2013-06-28 | Synta Pharmaceuticals Corp. | Jedinjenja triazola koja modulišu aktivnost hsp90 |
| DE102005007304A1 (de) * | 2005-02-17 | 2006-08-24 | Merck Patent Gmbh | Triazolderivate |
| EP1857446B1 (en) * | 2005-03-09 | 2013-05-01 | Nippon Kayaku Kabushiki Kaisha | Derivatives of 3-(2,4-dihydroxyphenyl)-1,2,4-triazole useful in the treatment of cancer |
| US8399464B2 (en) * | 2005-03-09 | 2013-03-19 | Nippon Kayaku Kabushiki Kaisha | HSP90 inhibitor |
| JP5149177B2 (ja) * | 2005-07-25 | 2013-02-20 | シンタ ファーマシューティカルズ コーポレーション | 増殖性疾患の治療のための、チューブリンポリマー化の１，２，３−トリアゾール系抑制剤 |
| US20070219129A1 (en) * | 2005-08-17 | 2007-09-20 | Pritchard Kirkwood A Jr | hsp90 decoy peptides and uses thereof |
| JP5118039B2 (ja) * | 2005-08-18 | 2013-01-16 | シンタ ファーマシューティカルズ コーポレーション | Ｈｓｐ９０活性を調節するトリアゾール化合物 |
| CA2618724A1 (en) * | 2005-08-18 | 2007-02-22 | Synta Pharmaceuticals Corp. | Imidazole compounds that modulate hsp90 activity |
| AU2007267859B2 (en) * | 2006-05-25 | 2012-04-12 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate Hsp90 activity |
| WO2007139952A2 (en) * | 2006-05-25 | 2007-12-06 | Synta Pharmaceuticals Corp. | Method for the preparation of triazole compounds with hsp90 modulating activity |
| CA2653332A1 (en) * | 2006-05-25 | 2007-12-06 | Synta Pharmaceuticals Corp. | Triazole compounds that modulate hsp90 activity |
| EP2034996A2 (en) * | 2006-05-25 | 2009-03-18 | Synta Pharmaceuticals Corporation | Triazole compounds that modulate hsp90 activity |
| DE102007002715A1 (de) * | 2007-01-18 | 2008-07-24 | Merck Patent Gmbh | Triazolderivat |
| KR20100057030A (ko) * | 2007-08-13 | 2010-05-28 | 신타 파마슈티칼스 코프. | Ｈｓｐ90의 활성을 조절하는 트라이아졸 화합물 |
-
2008
- 2008-08-13 KR KR1020107005268A patent/KR20100057030A/ko not_active Ceased
- 2008-08-13 CN CN200880102662.2A patent/CN101801983B/zh not_active Expired - Fee Related
- 2008-08-13 TW TW097130768A patent/TWI438199B/zh not_active IP Right Cessation
- 2008-08-13 EP EP08795272A patent/EP2193135A1/en not_active Withdrawn
- 2008-08-13 AU AU2008287367A patent/AU2008287367B2/en not_active Ceased
- 2008-08-13 BR BRPI0815116-4A2A patent/BRPI0815116A2/pt not_active IP Right Cessation
- 2008-08-13 NZ NZ583205A patent/NZ583205A/en not_active IP Right Cessation
- 2008-08-13 CA CA2695995A patent/CA2695995C/en not_active Expired - Fee Related
- 2008-08-13 MX MX2010001565A patent/MX2010001565A/es active IP Right Grant
- 2008-08-13 WO PCT/US2008/009667 patent/WO2009023211A1/en not_active Ceased
- 2008-08-13 JP JP2010521020A patent/JP5596543B2/ja not_active Expired - Fee Related
- 2008-08-13 US US12/673,254 patent/US8742133B2/en active Active
-
2010
- 2010-02-02 IL IL203663A patent/IL203663A/en not_active IP Right Cessation
- 2010-02-12 ZA ZA201001064A patent/ZA201001064B/xx unknown
-
2014
- 2014-05-23 US US14/285,834 patent/US9120745B2/en active Active
-
2015
- 2015-08-27 US US14/837,875 patent/US20150366885A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2010536753A5 (enExample) | ||
| JP2010518085A5 (enExample) | ||
| JP2010522750A5 (enExample) | ||
| JP2009538321A5 (enExample) | ||
| JP2009538320A5 (enExample) | ||
| CA2682665A1 (en) | Triazinone and diazinone derivatives useful as hsp90 inhibitors | |
| AU2018221076B2 (en) | Substituted imidazo-quinolines as NLRP3 modulators | |
| JP2013508378A5 (enExample) | ||
| JP2009538322A5 (enExample) | ||
| AU2010334958B2 (en) | Novel antiviral compounds | |
| TWI443102B (zh) | 苯并哌喃及苯并氧呯ｐｉ３ｋ抑制劑化合物及其使用方法 | |
| WO2017214339A4 (en) | Anti-b7-h3 antibodies and antibody drug conjugates | |
| CN103764655B (zh) | 作为alk5和／或alk4抑制剂的经2‑吡啶基取代的咪唑 | |
| CA3124678A1 (en) | Aza-heterobicyclic inhibitors of mat2a and methods of use for treating cancer | |
| KR101990605B1 (ko) | 아미노피리미딘 키나아제 억제제 | |
| CA3034705A1 (en) | Inhibitors of cellular metabolic processes | |
| WO2017214458A4 (en) | Anti-cd98 antibodies and antibody drug conjugates | |
| EP3010503A2 (en) | Novel bicyclic bromodomain inhibitors | |
| TW202126650A (zh) | Sting(干擾素基因刺激因子)調節劑 | |
| KR20210005106A (ko) | Nlrp3 조정제 | |
| TW201842919A (zh) | 經修飾環二核苷酸化合物 | |
| HRP20130095T1 (hr) | Spojevi triazola koji moduliraju aktivnost hsp90 | |
| KR20160104729A (ko) | 암 또는 염증성 질환의 치료를 위한 치환 피롤로피리딘 및 피롤로피라진 | |
| JP2009505988A5 (enExample) | ||
| HUP0500163A2 (hu) | Pirazolo [5,1-b] kinazolin származékok és ezeket tartalmazó gyógyszerkészítmények mint az IMPDH enzim inhibitorai |