JP2015536986A5 - - Google Patents

Info

Publication number

JP2015536986A5

JP2015536986A5 JP2015541875A JP2015541875A JP2015536986A5 JP 2015536986 A5 JP2015536986 A5 JP 2015536986A5 JP 2015541875 A JP2015541875 A JP 2015541875A JP 2015541875 A JP2015541875 A JP 2015541875A JP 2015536986 A5 JP2015536986 A5 JP 2015536986A5

Authority

JP

Japan

Prior art keywords

pharmaceutically acceptable

independently

acceptable salt

phenyl

formula

Prior art date

2013-11-06

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.)

Pending

Links

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• PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims description 24
• 150000003839 salts Chemical class 0.000 claims description 24
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
• 239000003814 drug Substances 0.000 claims description 16
• AYUNIORJHRXIBJ-TXHRRWQRSA-N tanespimycin Chemical compound N1C(=O)\C(C)=C\C=C/[C@H](OC)[C@@H](OC(N)=O)\C(C)=C\[C@H](C)[C@@H](O)[C@@H](OC)C[C@H](C)CC2=C(NCC=C)C(=O)C=C1C2=O AYUNIORJHRXIBJ-TXHRRWQRSA-N 0.000 claims description 16
• 201000010099 disease Diseases 0.000 claims description 15
• 230000002062 proliferating effect Effects 0.000 claims description 15
• 239000003481 heat shock protein 90 inhibitor Substances 0.000 claims description 14
• 125000000217 alkyl group Chemical group 0.000 claims description 12
• 229910052799 carbon Inorganic materials 0.000 claims description 12
• 150000001875 compounds Chemical class 0.000 claims description 12
• 125000001072 heteroaryl group Chemical group 0.000 claims description 10
• 239000008194 pharmaceutical composition Substances 0.000 claims description 9
• SWDZPNJZKUGIIH-QQTULTPQSA-N (5z)-n-ethyl-5-(4-hydroxy-6-oxo-3-propan-2-ylcyclohexa-2,4-dien-1-ylidene)-4-[4-(morpholin-4-ylmethyl)phenyl]-2h-1,2-oxazole-3-carboxamide Chemical compound O1NC(C(=O)NCC)=C(C=2C=CC(CN3CCOCC3)=CC=2)\C1=C1/C=C(C(C)C)C(O)=CC1=O SWDZPNJZKUGIIH-QQTULTPQSA-N 0.000 claims description 8
• 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 8
• 206010035226 Plasma cell myeloma Diseases 0.000 claims description 8
• 125000003118 aryl group Chemical group 0.000 claims description 8
• 229940079593 drug Drugs 0.000 claims description 8
• 125000000623 heterocyclic group Chemical group 0.000 claims description 8
• 210000000244 kidney pelvis Anatomy 0.000 claims description 8
• 229950005069 luminespib Drugs 0.000 claims description 8
• 229950007866 tanespimycin Drugs 0.000 claims description 8
• -1 6-methoxy-pyridin-2-yl Chemical group 0.000 claims description 6
• 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 6
• 125000002837 carbocyclic group Chemical group 0.000 claims description 6
• 125000001475 halogen functional group Chemical group 0.000 claims description 6
• 229910052739 hydrogen Inorganic materials 0.000 claims description 6
• WSMQUUGTQYPVPD-OAHLLOKOSA-N (7r)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydro-6h-pyrido[4,3-d]pyrimidin-5-one Chemical compound COC1=CC=CC(C=2C(=CC=C(F)C=2)[C@@H]2NC(=O)C3=C(C)N=C(N)N=C3C2)=N1 WSMQUUGTQYPVPD-OAHLLOKOSA-N 0.000 claims description 4
• QQYUAUPJJLOCHU-UHFFFAOYSA-N 6-chloro-9-[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]purin-2-amine;methanesulfonic acid Chemical compound CS(O)(=O)=O.COC1=C(C)C=NC(CN2C3=NC(N)=NC(Cl)=C3N=C2)=C1C QQYUAUPJJLOCHU-UHFFFAOYSA-N 0.000 claims description 4
• 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 4
• 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims description 4
• 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 4
• QULDDKSCVCJTPV-UHFFFAOYSA-N BIIB021 Chemical compound COC1=C(C)C=NC(CN2C3=NC(N)=NC(Cl)=C3N=C2)=C1C QULDDKSCVCJTPV-UHFFFAOYSA-N 0.000 claims description 4
• 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 4
• 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims description 4
• 206010025323 Lymphomas Diseases 0.000 claims description 4
• 208000034578 Multiple myelomas Diseases 0.000 claims description 4
• 208000007727 Muscle Tissue Neoplasms Diseases 0.000 claims description 4
• 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 4
• 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 4
• 206010028980 Neoplasm Diseases 0.000 claims description 4
• 206010029260 Neuroblastoma Diseases 0.000 claims description 4
• 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 4
• AVDSOVJPJZVBTC-UHFFFAOYSA-N [4-[2-carbamoyl-5-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-5,7-dihydroindazol-1-yl]anilino]cyclohexyl] 2-aminoacetate Chemical compound O=C1CC(C)(C)CC2=C1C(C(F)(F)F)=NN2C(C=1)=CC=C(C(N)=O)C=1NC1CCC(OC(=O)CN)CC1 AVDSOVJPJZVBTC-UHFFFAOYSA-N 0.000 claims description 4
• 210000000481 breast Anatomy 0.000 claims description 4
• 125000004432 carbon atom Chemical group C* 0.000 claims description 4
• 210000003679 cervix uteri Anatomy 0.000 claims description 4
• 210000001072 colon Anatomy 0.000 claims description 4
• 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
• 210000003238 esophagus Anatomy 0.000 claims description 4
• 210000001035 gastrointestinal tract Anatomy 0.000 claims description 4
• QTQAWLPCGQOSGP-GBTDJJJQSA-N geldanamycin Chemical class N1C(=O)\C(C)=C/C=C\[C@@H](OC)[C@H](OC(N)=O)\C(C)=C/[C@@H](C)[C@@H](O)[C@H](OC)C[C@@H](C)CC2=C(OC)C(=O)C=C1C2=O QTQAWLPCGQOSGP-GBTDJJJQSA-N 0.000 claims description 4
• 210000003128 head Anatomy 0.000 claims description 4
• 230000002757 inflammatory effect Effects 0.000 claims description 4
• 210000003228 intrahepatic bile duct Anatomy 0.000 claims description 4
• 210000000867 larynx Anatomy 0.000 claims description 4
• NDAZATDQFDPQBD-UHFFFAOYSA-N luminespib Chemical compound CCNC(=O)C1=NOC(C=2C(=CC(O)=C(C(C)C)C=2)O)=C1C(C=C1)=CC=C1CN1CCOCC1 NDAZATDQFDPQBD-UHFFFAOYSA-N 0.000 claims description 4
• 210000004072 lung Anatomy 0.000 claims description 4
• 201000001441 melanoma Diseases 0.000 claims description 4
• VYGYNVZNSSTDLJ-HKCOAVLJSA-N monorden Natural products CC1CC2OC2C=C/C=C/C(=O)CC3C(C(=CC(=C3Cl)O)O)C(=O)O1 VYGYNVZNSSTDLJ-HKCOAVLJSA-N 0.000 claims description 4
• 201000000050 myeloid neoplasm Diseases 0.000 claims description 4
• 208000024305 myofibroblastoma Diseases 0.000 claims description 4
• 201000008968 osteosarcoma Diseases 0.000 claims description 4
• 210000001672 ovary Anatomy 0.000 claims description 4
• 229910052760 oxygen Inorganic materials 0.000 claims description 4
• 210000000496 pancreas Anatomy 0.000 claims description 4
• 210000003800 pharynx Anatomy 0.000 claims description 4
• 210000002307 prostate Anatomy 0.000 claims description 4
• AECPBJMOGBFQDN-YMYQVXQQSA-N radicicol Chemical compound C1CCCC(=O)C[C@H]2[C@H](Cl)C(=O)CC(=O)[C@H]2C(=O)O[C@H](C)C[C@H]2O[C@@H]21 AECPBJMOGBFQDN-YMYQVXQQSA-N 0.000 claims description 4
• 229930192524 radicicol Natural products 0.000 claims description 4
• 210000000664 rectum Anatomy 0.000 claims description 4
• OIRUWDYJGMHDHJ-AFXVCOSJSA-N retaspimycin hydrochloride Chemical compound Cl.N1C(=O)\C(C)=C\C=C/[C@H](OC)[C@@H](OC(N)=O)\C(C)=C\[C@H](C)[C@@H](O)[C@@H](OC)C[C@H](C)CC2=C(O)C1=CC(O)=C2NCC=C OIRUWDYJGMHDHJ-AFXVCOSJSA-N 0.000 claims description 4
• 210000000813 small intestine Anatomy 0.000 claims description 4
• 210000002784 stomach Anatomy 0.000 claims description 4
• 210000001685 thyroid gland Anatomy 0.000 claims description 4
• 208000028018 Lymphocytic leukaemia Diseases 0.000 claims description 3
• 208000003747 lymphoid leukemia Diseases 0.000 claims description 3
• 210000000214 mouth Anatomy 0.000 claims description 3
• BDTRIDKONHOQQN-UHFFFAOYSA-N 4h-pyrimidin-5-one Chemical compound O=C1CN=CN=C1 BDTRIDKONHOQQN-UHFFFAOYSA-N 0.000 claims description 2
• JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims description 2
• 239000000203 mixture Substances 0.000 claims description 2
• 229910052757 nitrogen Inorganic materials 0.000 claims description 2
• 229920006395 saturated elastomer Polymers 0.000 claims description 2
• 229910052717 sulfur Inorganic materials 0.000 claims description 2
• 229940000425 combination drug Drugs 0.000 claims 1
• 238000000034 method Methods 0.000 description 5
• 229940126062 Compound A Drugs 0.000 description 3
• NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 description 3
• 230000000259 anti-tumor effect Effects 0.000 description 2
• 206010048832 Colon adenoma Diseases 0.000 description 1
• 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
• 239000003795 chemical substances by application Substances 0.000 description 1
• 208000035475 disorder Diseases 0.000 description 1
• 201000005202 lung cancer Diseases 0.000 description 1
• 208000020816 lung neoplasm Diseases 0.000 description 1
• 238000009097 single-agent therapy Methods 0.000 description 1