JP2020517732A5 - - Google Patents
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- JP2020517732A5 JP2020517732A5 JP2019559089A JP2019559089A JP2020517732A5 JP 2020517732 A5 JP2020517732 A5 JP 2020517732A5 JP 2019559089 A JP2019559089 A JP 2019559089A JP 2019559089 A JP2019559089 A JP 2019559089A JP 2020517732 A5 JP2020517732 A5 JP 2020517732A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- optionally
- aryl
- alkynyl
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 34
- 125000003118 aryl group Chemical group 0.000 claims 32
- 229910052739 hydrogen Inorganic materials 0.000 claims 28
- 239000001257 hydrogen Substances 0.000 claims 25
- -1 F or Cl Chemical group 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 22
- 150000002367 halogens Chemical group 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 21
- 239000003826 tablet Substances 0.000 claims 20
- 229910052799 carbon Inorganic materials 0.000 claims 19
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 claims 18
- 125000000623 heterocyclic group Chemical group 0.000 claims 17
- 229910052760 oxygen Inorganic materials 0.000 claims 17
- 125000000753 cycloalkyl group Chemical group 0.000 claims 16
- 229910052717 sulfur Inorganic materials 0.000 claims 16
- 229910052757 nitrogen Inorganic materials 0.000 claims 15
- 125000003545 alkoxy group Chemical group 0.000 claims 13
- 150000002431 hydrogen Chemical group 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 11
- 125000000304 alkynyl group Chemical group 0.000 claims 11
- 125000004093 cyano group Chemical group *C#N 0.000 claims 11
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 11
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 239000002775 capsule Substances 0.000 claims 7
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 7
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 7
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical group O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 6
- 125000001931 aliphatic group Chemical group 0.000 claims 6
- 125000004663 dialkyl amino group Chemical group 0.000 claims 6
- 239000007884 disintegrant Substances 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 6
- 239000002253 acid Substances 0.000 claims 5
- 125000004442 acylamino group Chemical group 0.000 claims 5
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 5
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000002877 alkyl aryl group Chemical group 0.000 claims 5
- 150000001408 amides Chemical class 0.000 claims 5
- 125000004103 aminoalkyl group Chemical group 0.000 claims 5
- 125000004404 heteroalkyl group Chemical group 0.000 claims 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 5
- 239000000314 lubricant Substances 0.000 claims 5
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 4
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 4
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 4
- 125000004104 aryloxy group Chemical group 0.000 claims 4
- 239000011248 coating agent Substances 0.000 claims 4
- 238000000576 coating method Methods 0.000 claims 4
- 230000003111 delayed effect Effects 0.000 claims 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 239000012943 hotmelt Substances 0.000 claims 4
- 235000019359 magnesium stearate Nutrition 0.000 claims 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 3
- 125000002723 alicyclic group Chemical group 0.000 claims 3
- 239000011230 binding agent Substances 0.000 claims 3
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 3
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 3
- 230000002354 daily effect Effects 0.000 claims 3
- 239000003085 diluting agent Substances 0.000 claims 3
- 239000000945 filler Substances 0.000 claims 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 3
- 125000005647 linker group Chemical group 0.000 claims 3
- 239000008185 minitablet Substances 0.000 claims 3
- 125000000168 pyrrolyl group Chemical group 0.000 claims 3
- 229920006395 saturated elastomer Chemical group 0.000 claims 3
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 3
- 125000004001 thioalkyl group Chemical group 0.000 claims 3
- 125000004951 trihalomethoxy group Chemical group 0.000 claims 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 claims 2
- 101001016865 Homo sapiens Heat shock protein HSP 90-alpha Proteins 0.000 claims 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 2
- 229930195725 Mannitol Natural products 0.000 claims 2
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical compound O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 claims 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 2
- 125000003302 alkenyloxy group Chemical group 0.000 claims 2
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 2
- 125000004422 alkyl sulphonamide group Chemical group 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 230000000181 anti-adherent effect Effects 0.000 claims 2
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 2
- 229940125904 compound 1 Drugs 0.000 claims 2
- 229960001681 croscarmellose sodium Drugs 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 239000003480 eluent Substances 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 239000012530 fluid Substances 0.000 claims 2
- 229910021485 fumed silica Inorganic materials 0.000 claims 2
- 239000008101 lactose Substances 0.000 claims 2
- 229960001375 lactose Drugs 0.000 claims 2
- 239000000594 mannitol Substances 0.000 claims 2
- 235000010355 mannitol Nutrition 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 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 2
- 208000037244 polycythemia vera Diseases 0.000 claims 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 2
- 238000010922 spray-dried dispersion Methods 0.000 claims 2
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 2
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 2
- 229940124530 sulfonamide Drugs 0.000 claims 2
- 150000003456 sulfonamides Chemical class 0.000 claims 2
- QTTFSPIZCUFHGX-UHFFFAOYSA-N 2,3-dihydroxypropanoic acid;octadecanoic acid Chemical compound OCC(O)C(O)=O.CCCCCCCCCCCCCCCCCC(O)=O QTTFSPIZCUFHGX-UHFFFAOYSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-UHFFFAOYSA-N 2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol Chemical compound OCC1OC(OC2C(O)C(O)C(O)OC2CO)C(O)C(O)C1O GUBGYTABKSRVRQ-UHFFFAOYSA-N 0.000 claims 1
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000004051 Chronic Traumatic Encephalopathy Diseases 0.000 claims 1
- 229920002261 Corn starch Polymers 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 101000614095 Homo sapiens Proton-activated chloride channel Proteins 0.000 claims 1
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 1
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 229920003081 Povidone K 30 Polymers 0.000 claims 1
- 102100040631 Proton-activated chloride channel Human genes 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- AOBORMOPSGHCAX-UHFFFAOYSA-N Tocophersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-UHFFFAOYSA-N 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- YLEIFZAVNWDOBM-ZTNXSLBXSA-N ac1l9hc7 Chemical compound C([C@H]12)C[C@@H](C([C@@H](O)CC3)(C)C)[C@@]43C[C@@]14CC[C@@]1(C)[C@@]2(C)C[C@@H]2O[C@]3(O)[C@H](O)C(C)(C)O[C@@H]3[C@@H](C)[C@H]12 YLEIFZAVNWDOBM-ZTNXSLBXSA-N 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 150000001345 alkine derivatives Chemical class 0.000 claims 1
- 150000003973 alkyl amines Chemical group 0.000 claims 1
- 125000005094 alkyl carbonyl amino alkyl group Chemical group 0.000 claims 1
- 125000005197 alkyl carbonyloxy alkyl group Chemical group 0.000 claims 1
- 150000001350 alkyl halides Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 239000004067 bulking agent Substances 0.000 claims 1
- 239000000378 calcium silicate Substances 0.000 claims 1
- 229910052918 calcium silicate Inorganic materials 0.000 claims 1
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000007963 capsule composition Substances 0.000 claims 1
- 229940125782 compound 2 Drugs 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000008120 corn starch Substances 0.000 claims 1
- 229940099112 cornstarch Drugs 0.000 claims 1
- 229960000913 crospovidone Drugs 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 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 1
- 208000017004 dementia pugilistica Diseases 0.000 claims 1
- 239000002270 dispersing agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 1
- 230000003203 everyday effect Effects 0.000 claims 1
- 239000008273 gelatin Substances 0.000 claims 1
- 229920000159 gelatin Polymers 0.000 claims 1
- 239000007903 gelatin capsule Substances 0.000 claims 1
- 235000019322 gelatine Nutrition 0.000 claims 1
- 235000011852 gelatine desserts Nutrition 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 229960001021 lactose monohydrate Drugs 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 229960001855 mannitol Drugs 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 238000007909 melt granulation Methods 0.000 claims 1
- 229940117841 methacrylic acid copolymer Drugs 0.000 claims 1
- 229920003145 methacrylic acid copolymer Polymers 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- GVOISEJVFFIGQE-YCZSINBZSA-N n-[(1r,2s,5r)-5-[methyl(propan-2-yl)amino]-2-[(3s)-2-oxo-3-[[6-(trifluoromethyl)quinazolin-4-yl]amino]pyrrolidin-1-yl]cyclohexyl]acetamide Chemical compound CC(=O)N[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1C(=O)[C@@H](NC=2C3=CC(=CC=C3N=CN=2)C(F)(F)F)CC1 GVOISEJVFFIGQE-YCZSINBZSA-N 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 239000006191 orally-disintegrating tablet Substances 0.000 claims 1
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 239000004014 plasticizer Substances 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 1
- 229940068968 polysorbate 80 Drugs 0.000 claims 1
- 229920000053 polysorbate 80 Polymers 0.000 claims 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 1
- 229940069328 povidone Drugs 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 230000004043 responsiveness Effects 0.000 claims 1
- 239000000377 silicon dioxide Substances 0.000 claims 1
- 235000012239 silicon dioxide Nutrition 0.000 claims 1
- 229940079832 sodium starch glycolate Drugs 0.000 claims 1
- 239000008109 sodium starch glycolate Substances 0.000 claims 1
- 229920003109 sodium starch glycolate Polymers 0.000 claims 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 1
- STFSJTPVIIDAQX-LTRPLHCISA-M sodium;(e)-4-octadecoxy-4-oxobut-2-enoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCCOC(=O)\C=C\C([O-])=O STFSJTPVIIDAQX-LTRPLHCISA-M 0.000 claims 1
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- 239000000454 talc Substances 0.000 claims 1
- 229910052623 talc Inorganic materials 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
- 229930192474 thiophene Natural products 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 239000001069 triethyl citrate Substances 0.000 claims 1
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 claims 1
- 235000013769 triethyl citrate Nutrition 0.000 claims 1
- 125000004953 trihalomethyl group Chemical group 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 238000005550 wet granulation Methods 0.000 claims 1
- 0 CC(C)NCCC[n]1c(Sc(cc2OC*c2c2)c2F)nc2c1ncnc2N Chemical compound CC(C)NCCC[n]1c(Sc(cc2OC*c2c2)c2F)nc2c1ncnc2N 0.000 description 1
Applications Claiming Priority (17)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762489434P | 2017-04-24 | 2017-04-24 | |
| US201762489438P | 2017-04-24 | 2017-04-24 | |
| US62/489,438 | 2017-04-24 | ||
| US62/489,434 | 2017-04-24 | ||
| US201762532985P | 2017-07-14 | 2017-07-14 | |
| US201762532987P | 2017-07-14 | 2017-07-14 | |
| US62/532,987 | 2017-07-14 | ||
| US62/532,985 | 2017-07-14 | ||
| US201762588893P | 2017-11-20 | 2017-11-20 | |
| US201762588897P | 2017-11-20 | 2017-11-20 | |
| US62/588,893 | 2017-11-20 | ||
| US62/588,897 | 2017-11-20 | ||
| US201862627229P | 2018-02-07 | 2018-02-07 | |
| US201862627237P | 2018-02-07 | 2018-02-07 | |
| US62/627,237 | 2018-02-07 | ||
| US62/627,229 | 2018-02-07 | ||
| PCT/US2018/029157 WO2018200534A1 (en) | 2017-04-24 | 2018-04-24 | Hsp90 inhibitor oral formulations and related methods |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020517732A JP2020517732A (ja) | 2020-06-18 |
| JP2020517732A5 true JP2020517732A5 (https=) | 2021-06-10 |
Family
ID=63918615
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019559089A Pending JP2020517732A (ja) | 2017-04-24 | 2018-04-24 | Ｈｓｐ９０阻害剤の経口製剤及び関連する方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20200069592A1 (https=) |
| EP (1) | EP3615008A4 (https=) |
| JP (1) | JP2020517732A (https=) |
| KR (1) | KR20190138871A (https=) |
| CN (1) | CN110996918A (https=) |
| AU (2) | AU2018257901A1 (https=) |
| CA (1) | CA3061185A1 (https=) |
| IL (1) | IL296355A (https=) |
| SG (2) | SG11201909825VA (https=) |
| TW (1) | TWI782982B (https=) |
| WO (1) | WO2018200534A1 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111683658A (zh) * | 2017-06-23 | 2020-09-18 | 萨缪斯治疗股份有限公司 | 用于创伤性脑损伤及其后遗症的多蛋白复合物抑制剂疗法 |
| WO2020243393A1 (en) * | 2019-05-30 | 2020-12-03 | Vta Labs, Llc | Design of a single oral delivery system containing a monoclonal antibody for the simultaneous treatment of chron's disease and ulcerative colitis |
| CN114259564B (zh) * | 2021-11-30 | 2023-03-14 | 清华大学 | Hsp90抑制剂阻碍stat3线粒体转运和治疗哮喘的新应用 |
| US12042491B1 (en) * | 2022-12-30 | 2024-07-23 | Tap Pharmaceuticals Ag | Pharmaceutical formulations of quinolines |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
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| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
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| WO2006130469A1 (en) * | 2005-05-27 | 2006-12-07 | Oregon Health & Science University | Stimulation of neurite outgrowth by small molecules |
| WO2008005937A2 (en) * | 2006-06-30 | 2008-01-10 | Sloan-Kettering Institute For Cancer Research | Treatment of neurodegenerative diseases through inhibiton of hsp90 |
| PE20081506A1 (es) * | 2006-12-12 | 2008-12-09 | Infinity Discovery Inc | Formulaciones de ansamicina |
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| JP5941407B2 (ja) * | 2009-10-07 | 2016-06-29 | スローン − ケッタリング インスティチュート フォー キャンサー リサーチ | Ｈｓｐ９０阻害剤 |
| EP2498759B1 (en) * | 2009-11-13 | 2018-08-01 | AstraZeneca AB | Immediate release tablet formulations |
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| CN104173283B (zh) * | 2014-08-27 | 2016-09-07 | 广州暨南生物医药研究开发基地有限公司 | 一种以苯甲酰胺为基本骨架的Hsp90抑制剂的纳米混悬剂及其制备方法 |
| CN111683658A (zh) * | 2017-06-23 | 2020-09-18 | 萨缪斯治疗股份有限公司 | 用于创伤性脑损伤及其后遗症的多蛋白复合物抑制剂疗法 |
-
2018
- 2018-04-24 KR KR1020197034522A patent/KR20190138871A/ko not_active Withdrawn
- 2018-04-24 SG SG11201909825V patent/SG11201909825VA/en unknown
- 2018-04-24 JP JP2019559089A patent/JP2020517732A/ja active Pending
- 2018-04-24 EP EP18790960.1A patent/EP3615008A4/en not_active Withdrawn
- 2018-04-24 IL IL296355A patent/IL296355A/en unknown
- 2018-04-24 CA CA3061185A patent/CA3061185A1/en active Pending
- 2018-04-24 WO PCT/US2018/029157 patent/WO2018200534A1/en not_active Ceased
- 2018-04-24 TW TW107113882A patent/TWI782982B/zh not_active IP Right Cessation
- 2018-04-24 AU AU2018257901A patent/AU2018257901A1/en not_active Abandoned
- 2018-04-24 US US16/607,610 patent/US20200069592A1/en not_active Abandoned
- 2018-04-24 SG SG10201913562VA patent/SG10201913562VA/en unknown
- 2018-04-24 CN CN201880040143.1A patent/CN110996918A/zh active Pending
-
2022
- 2022-10-18 AU AU2022256110A patent/AU2022256110A1/en not_active Abandoned
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