JP2016502540A5 - - Google Patents
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- JP2016502540A5 JP2016502540A5 JP2015545447A JP2015545447A JP2016502540A5 JP 2016502540 A5 JP2016502540 A5 JP 2016502540A5 JP 2015545447 A JP2015545447 A JP 2015545447A JP 2015545447 A JP2015545447 A JP 2015545447A JP 2016502540 A5 JP2016502540 A5 JP 2016502540A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- composition according
- pharmaceutical composition
- disease
- alkyl
- 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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- 150000001875 compounds Chemical class 0.000 claims description 40
- 201000010099 disease Diseases 0.000 claims description 32
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 32
- 239000000203 mixture Substances 0.000 claims description 30
- 206010028980 Neoplasm Diseases 0.000 claims description 18
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 239000001257 hydrogen Substances 0.000 claims description 14
- 208000024891 symptom Diseases 0.000 claims description 13
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 12
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims description 12
- 201000011510 cancer Diseases 0.000 claims description 12
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 11
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims description 10
- 229910052736 halogen Inorganic materials 0.000 claims description 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 206010062804 Basal cell naevus syndrome Diseases 0.000 claims description 6
- 208000031995 Gorlin syndrome Diseases 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 201000005734 nevoid basal cell carcinoma syndrome Diseases 0.000 claims description 6
- 230000002265 prevention Effects 0.000 claims description 6
- 239000012453 solvate Substances 0.000 claims description 6
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 5
- 125000003545 alkoxy group Chemical group 0.000 claims description 5
- 150000002367 halogens Chemical class 0.000 claims description 5
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 5
- 201000002528 pancreatic cancer Diseases 0.000 claims description 5
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 5
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims description 4
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 4
- 125000003302 alkenyloxy group Chemical group 0.000 claims description 4
- 125000005133 alkynyloxy group Chemical group 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 3
- 201000003076 Angiosarcoma Diseases 0.000 claims description 3
- 206010004146 Basal cell carcinoma Diseases 0.000 claims description 3
- 206010005003 Bladder cancer Diseases 0.000 claims description 3
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 3
- 206010006187 Breast cancer Diseases 0.000 claims description 3
- 208000026310 Breast neoplasm Diseases 0.000 claims description 3
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 3
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 3
- 208000001258 Hemangiosarcoma Diseases 0.000 claims description 3
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 3
- 206010025323 Lymphomas Diseases 0.000 claims description 3
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims description 3
- 208000000172 Medulloblastoma Diseases 0.000 claims description 3
- 206010033128 Ovarian cancer Diseases 0.000 claims description 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 3
- 206010060862 Prostate cancer Diseases 0.000 claims description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 3
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 3
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims description 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 3
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 3
- 201000001256 adenosarcoma Diseases 0.000 claims description 3
- 125000000217 alkyl group Chemical group 0.000 claims description 3
- 125000000304 alkynyl group Chemical group 0.000 claims description 3
- 201000010881 cervical cancer Diseases 0.000 claims description 3
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims description 3
- 201000007280 estrogen-receptor negative breast cancer Diseases 0.000 claims description 3
- 201000007281 estrogen-receptor positive breast cancer Diseases 0.000 claims description 3
- 206010017758 gastric cancer Diseases 0.000 claims description 3
- 208000005017 glioblastoma Diseases 0.000 claims description 3
- 201000010536 head and neck cancer Diseases 0.000 claims description 3
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 3
- 208000032839 leukemia Diseases 0.000 claims description 3
- 201000007270 liver cancer Diseases 0.000 claims description 3
- 208000014018 liver neoplasm Diseases 0.000 claims description 3
- 201000005202 lung cancer Diseases 0.000 claims description 3
- 208000020816 lung neoplasm Diseases 0.000 claims description 3
- 208000037843 metastatic solid tumor Diseases 0.000 claims description 3
- 201000000849 skin cancer Diseases 0.000 claims description 3
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 3
- 201000011549 stomach cancer Diseases 0.000 claims description 3
- 238000001356 surgical procedure Methods 0.000 claims description 3
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims description 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 3
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 29
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 230000036571 hydration Effects 0.000 claims 4
- 238000006703 hydration reaction Methods 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims 3
- 229930012538 Paclitaxel Natural products 0.000 claims 3
- 239000013543 active substance Substances 0.000 claims 3
- 230000003176 fibrotic effect Effects 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 229960001592 paclitaxel Drugs 0.000 claims 3
- 239000000126 substance Substances 0.000 claims 3
- -1 3,5-dimethylphenyl Chemical group 0.000 claims 2
- 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 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 208000037844 advanced solid tumor Diseases 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 229960003668 docetaxel Drugs 0.000 claims 2
- 210000003236 esophagogastric junction Anatomy 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 230000004761 fibrosis Effects 0.000 claims 2
- 230000000977 initiatory effect Effects 0.000 claims 2
- 208000037819 metastatic cancer Diseases 0.000 claims 2
- 208000011575 metastatic malignant neoplasm Diseases 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 210000000496 pancreas Anatomy 0.000 claims 2
- 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 2
- 230000014616 translation Effects 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000006625 (C3-C8) cycloalkyloxy group Chemical group 0.000 claims 1
- VTCJJHNDFUBYRW-UHFFFAOYSA-N 2-(fluoromethyl)benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC=C1CF VTCJJHNDFUBYRW-UHFFFAOYSA-N 0.000 claims 1
- 101001082110 Acanthamoeba polyphaga mimivirus Eukaryotic translation initiation factor 4E homolog Proteins 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- ODDDGBHORBBPQL-UHFFFAOYSA-N CCC1=CC=CC(C)=C1NS(=O)(=O)C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 Chemical compound CCC1=CC=CC(C)=C1NS(=O)(=O)C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 ODDDGBHORBBPQL-UHFFFAOYSA-N 0.000 claims 1
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical group 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 1
- 101001082109 Danio rerio Eukaryotic translation initiation factor 4E-1B Proteins 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 230000009787 cardiac fibrosis Effects 0.000 claims 1
- 238000011443 conventional therapy Methods 0.000 claims 1
- 229960000684 cytarabine Drugs 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- ANYMTDGFEKYJRL-UHFFFAOYSA-N n-(2,6-dimethylphenyl)-3,5-bis(trifluoromethyl)benzenesulfonamide Chemical compound CC1=CC=CC(C)=C1NS(=O)(=O)C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 ANYMTDGFEKYJRL-UHFFFAOYSA-N 0.000 claims 1
- VHVZXUPCKQNRBU-UHFFFAOYSA-N n-(2-methyl-6-propan-2-ylphenyl)-3,5-bis(trifluoromethyl)benzenesulfonamide Chemical compound CC(C)C1=CC=CC(C)=C1NS(=O)(=O)C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 VHVZXUPCKQNRBU-UHFFFAOYSA-N 0.000 claims 1
- SCZMFQTXQDNCNX-UHFFFAOYSA-N n-[3,5-bis(trifluoromethyl)phenyl]-2,3,5,6-tetramethylbenzenesulfonamide Chemical compound CC1=CC(C)=C(C)C(S(=O)(=O)NC=2C=C(C=C(C=2)C(F)(F)F)C(F)(F)F)=C1C SCZMFQTXQDNCNX-UHFFFAOYSA-N 0.000 claims 1
- QVFWYKSUDLYTTA-UHFFFAOYSA-N n-[3,5-bis(trifluoromethyl)phenyl]-2,4,6-trimethylbenzenesulfonamide Chemical compound CC1=CC(C)=CC(C)=C1S(=O)(=O)NC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 QVFWYKSUDLYTTA-UHFFFAOYSA-N 0.000 claims 1
- JAGPNGDKNSBBSM-UHFFFAOYSA-N n-[3,5-bis(trifluoromethyl)phenyl]-2,4-dimethylbenzenesulfonamide Chemical compound CC1=CC(C)=CC=C1S(=O)(=O)NC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 JAGPNGDKNSBBSM-UHFFFAOYSA-N 0.000 claims 1
- GTRKZGOSBOQYEL-UHFFFAOYSA-N n-[3,5-bis(trifluoromethyl)phenyl]-2,5-dimethylbenzenesulfonamide Chemical compound CC1=CC=C(C)C(S(=O)(=O)NC=2C=C(C=C(C=2)C(F)(F)F)C(F)(F)F)=C1 GTRKZGOSBOQYEL-UHFFFAOYSA-N 0.000 claims 1
- ZMHORLWVBWAGCK-UHFFFAOYSA-N n-[3,5-bis(trifluoromethyl)phenyl]-3,4-dimethylbenzenesulfonamide Chemical compound C1=C(C)C(C)=CC=C1S(=O)(=O)NC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 ZMHORLWVBWAGCK-UHFFFAOYSA-N 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000007614 solvation Methods 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 125000002456 taxol group Chemical group 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical group C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims 1
- 229960004528 vincristine Drugs 0.000 claims 1
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 description 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 description 2
- 239000000651 prodrug Substances 0.000 description 2
- 229940002612 prodrug Drugs 0.000 description 2
- 230000001668 ameliorated effect Effects 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 125000004404 heteroalkyl group Chemical group 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261732218P | 2012-11-30 | 2012-11-30 | |
| US61/732,218 | 2012-11-30 | ||
| PCT/US2013/072303 WO2014085633A1 (en) | 2012-11-30 | 2013-11-27 | Substituted biaryl sulfonamides and the use thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016502540A JP2016502540A (ja) | 2016-01-28 |
| JP2016502540A5 true JP2016502540A5 (enExample) | 2018-03-01 |
| JP6313779B2 JP6313779B2 (ja) | 2018-04-18 |
Family
ID=49765712
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015545447A Active JP6313779B2 (ja) | 2012-11-30 | 2013-11-27 | 置換ビアリールスルホンアミドおよびその利用 |
Country Status (14)
| Country | Link |
|---|---|
| US (6) | US9156781B2 (enExample) |
| EP (2) | EP2925718B1 (enExample) |
| JP (1) | JP6313779B2 (enExample) |
| KR (1) | KR102180342B1 (enExample) |
| CN (2) | CN107698470A (enExample) |
| AU (1) | AU2013352106B2 (enExample) |
| CA (1) | CA2892227C (enExample) |
| DK (1) | DK2925718T3 (enExample) |
| ES (1) | ES2689921T3 (enExample) |
| MX (1) | MX370519B (enExample) |
| NZ (1) | NZ630786A (enExample) |
| SG (1) | SG11201504041WA (enExample) |
| WO (1) | WO2014085633A1 (enExample) |
| ZA (1) | ZA201503797B (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9156781B2 (en) * | 2012-11-30 | 2015-10-13 | Novomedix, Llc | Substituted biaryl sulfonamides and the use thereof |
| WO2015120350A2 (en) | 2014-02-07 | 2015-08-13 | Effector Therapeutics, Inc. | Compositions and methods for treating fibrotic disease |
| BR112020019325A2 (pt) * | 2018-03-28 | 2021-01-05 | Blade Therapeutics, Inc. | Método de tratamento de doença fibrótica |
| WO2021001743A1 (en) * | 2019-07-02 | 2021-01-07 | Effector Therapeutics, Inc. | Translation inhibitors and uses thereof |
| WO2021243319A1 (en) * | 2020-05-29 | 2021-12-02 | Novomedix, Llc | Biarylsulfonamides and pharmaceutical compositions thereof, and their use for treating fibrotic lung disease |
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| NL301745A (enExample) * | 1962-12-17 | |||
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-
2013
- 2013-11-27 US US14/092,425 patent/US9156781B2/en active Active
- 2013-11-27 DK DK13805700.5T patent/DK2925718T3/en active
- 2013-11-27 CN CN201710907127.5A patent/CN107698470A/zh active Pending
- 2013-11-27 EP EP13805700.5A patent/EP2925718B1/en active Active
- 2013-11-27 EP EP18185388.8A patent/EP3447046A1/en not_active Withdrawn
- 2013-11-27 MX MX2015006544A patent/MX370519B/es active IP Right Grant
- 2013-11-27 ES ES13805700.5T patent/ES2689921T3/es active Active
- 2013-11-27 CA CA2892227A patent/CA2892227C/en active Active
- 2013-11-27 KR KR1020157017289A patent/KR102180342B1/ko active Active
- 2013-11-27 AU AU2013352106A patent/AU2013352106B2/en active Active
- 2013-11-27 NZ NZ630786A patent/NZ630786A/en unknown
- 2013-11-27 WO PCT/US2013/072303 patent/WO2014085633A1/en not_active Ceased
- 2013-11-27 SG SG11201504041WA patent/SG11201504041WA/en unknown
- 2013-11-27 CN CN201380071836.4A patent/CN104955801B/zh active Active
- 2013-11-27 JP JP2015545447A patent/JP6313779B2/ja active Active
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2015
- 2015-05-27 ZA ZA2015/03797A patent/ZA201503797B/en unknown
- 2015-09-30 US US14/871,472 patent/US9604924B2/en active Active
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2017
- 2017-02-16 US US15/434,531 patent/US10040757B2/en active Active
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2018
- 2018-07-26 US US16/046,893 patent/US20180327353A1/en not_active Abandoned
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2019
- 2019-11-05 US US16/674,943 patent/US20200062700A1/en not_active Abandoned
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2021
- 2021-06-21 US US17/353,681 patent/US11713293B2/en active Active
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