JP2017533963A5 - - Google Patents
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- JP2017533963A5 JP2017533963A5 JP2017543330A JP2017543330A JP2017533963A5 JP 2017533963 A5 JP2017533963 A5 JP 2017533963A5 JP 2017543330 A JP2017543330 A JP 2017543330A JP 2017543330 A JP2017543330 A JP 2017543330A JP 2017533963 A5 JP2017533963 A5 JP 2017533963A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- colorectal cancer
- apilimod
- vemurafenib
- composition according
- 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
- 239000000203 mixture Substances 0.000 claims description 59
- 206010009944 Colon cancer Diseases 0.000 claims description 23
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 23
- 239000003814 drug Substances 0.000 claims description 18
- 229940124597 therapeutic agent Drugs 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 16
- 229950002889 apilimod Drugs 0.000 claims description 14
- HSKAZIJJKRAJAV-KOEQRZSOSA-N n-[(e)-(3-methylphenyl)methylideneamino]-6-morpholin-4-yl-2-(2-pyridin-2-ylethoxy)pyrimidin-4-amine Chemical compound CC1=CC=CC(\C=N\NC=2N=C(OCCC=3N=CC=CC=3)N=C(C=2)N2CCOCC2)=C1 HSKAZIJJKRAJAV-KOEQRZSOSA-N 0.000 claims description 14
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 claims description 14
- 229960003862 vemurafenib Drugs 0.000 claims description 14
- GAJWNIKZLYZYSY-OKUPSQOASA-N methanesulfonic acid;n-[(e)-(3-methylphenyl)methylideneamino]-6-morpholin-4-yl-2-(2-pyridin-2-ylethoxy)pyrimidin-4-amine Chemical compound CS(O)(=O)=O.CS(O)(=O)=O.CC1=CC=CC(\C=N\NC=2N=C(OCCC=3N=CC=CC=3)N=C(C=2)N2CCOCC2)=C1 GAJWNIKZLYZYSY-OKUPSQOASA-N 0.000 claims description 13
- 239000002138 L01XE21 - Regorafenib Substances 0.000 claims description 8
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims description 8
- 229960004836 regorafenib Drugs 0.000 claims description 8
- FNHKPVJBJVTLMP-UHFFFAOYSA-N regorafenib Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=C(F)C(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 FNHKPVJBJVTLMP-UHFFFAOYSA-N 0.000 claims description 7
- FELGMEQIXOGIFQ-CYBMUJFWSA-N (3r)-9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1h-carbazol-4-one Chemical compound CC1=NC=CN1C[C@@H]1C(=O)C(C=2C(=CC=CC=2)N2C)=C2CC1 FELGMEQIXOGIFQ-CYBMUJFWSA-N 0.000 claims description 6
- 239000013543 active substance Substances 0.000 claims description 6
- UKTAZPQNNNJVKR-KJGYPYNMSA-N chembl2368925 Chemical compound C1=CC=C2C(C(O[C@@H]3C[C@@H]4C[C@H]5C[C@@H](N4CC5=O)C3)=O)=CNC2=C1 UKTAZPQNNNJVKR-KJGYPYNMSA-N 0.000 claims description 6
- 229960003413 dolasetron Drugs 0.000 claims description 6
- 229960003727 granisetron Drugs 0.000 claims description 6
- MFWNKCLOYSRHCJ-BTTYYORXSA-N granisetron Chemical compound C1=CC=C2C(C(=O)N[C@H]3C[C@H]4CCC[C@@H](C3)N4C)=NN(C)C2=C1 MFWNKCLOYSRHCJ-BTTYYORXSA-N 0.000 claims description 6
- 239000003112 inhibitor Substances 0.000 claims description 6
- 230000035772 mutation Effects 0.000 claims description 6
- 229960005343 ondansetron Drugs 0.000 claims description 6
- 229960002131 palonosetron Drugs 0.000 claims description 6
- CPZBLNMUGSZIPR-NVXWUHKLSA-N palonosetron Chemical compound C1N(CC2)CCC2[C@@H]1N1C(=O)C(C=CC=C2CCC3)=C2[C@H]3C1 CPZBLNMUGSZIPR-NVXWUHKLSA-N 0.000 claims description 6
- 229960002621 pembrolizumab Drugs 0.000 claims description 6
- PHUTUTUABXHXLW-UHFFFAOYSA-N pindolol Chemical compound CC(C)NCC(O)COC1=CC=CC2=NC=C[C]12 PHUTUTUABXHXLW-UHFFFAOYSA-N 0.000 claims description 6
- 229960002508 pindolol Drugs 0.000 claims description 6
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 claims description 6
- 229960001534 risperidone Drugs 0.000 claims description 6
- 206010070308 Refractory cancer Diseases 0.000 claims description 5
- 208000016691 refractory malignant neoplasm Diseases 0.000 claims description 5
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 101150044014 Snx10 gene Proteins 0.000 claims description 4
- 229940034982 antineoplastic agent Drugs 0.000 claims description 4
- 239000002246 antineoplastic agent Substances 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 238000002648 combination therapy Methods 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 229960002949 fluorouracil Drugs 0.000 claims description 4
- 230000014509 gene expression Effects 0.000 claims description 4
- 229960004768 irinotecan Drugs 0.000 claims description 4
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims description 4
- 229960003301 nivolumab Drugs 0.000 claims description 4
- 239000002777 nucleoside Substances 0.000 claims description 4
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 4
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims description 4
- 229960001756 oxaliplatin Drugs 0.000 claims description 4
- 229910052697 platinum Inorganic materials 0.000 claims description 4
- 239000003909 protein kinase inhibitor Substances 0.000 claims description 4
- 239000000523 sample Substances 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 3
- 229940043355 kinase inhibitor Drugs 0.000 claims description 3
- 230000004060 metabolic process Effects 0.000 claims description 3
- 208000037819 metastatic cancer Diseases 0.000 claims description 3
- 208000011575 metastatic malignant neoplasm Diseases 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims description 3
- 239000012453 solvate Substances 0.000 claims description 3
- 101100463133 Caenorhabditis elegans pdl-1 gene Proteins 0.000 claims description 2
- 206010052358 Colorectal cancer metastatic Diseases 0.000 claims description 2
- 102000004243 Tubulin Human genes 0.000 claims description 2
- 108090000704 Tubulin Proteins 0.000 claims description 2
- 229940100198 alkylating agent Drugs 0.000 claims description 2
- 239000002168 alkylating agent Substances 0.000 claims description 2
- 230000006907 apoptotic process Effects 0.000 claims description 2
- 229960003852 atezolizumab Drugs 0.000 claims description 2
- 230000004900 autophagic degradation Effects 0.000 claims description 2
- 229950002916 avelumab Drugs 0.000 claims description 2
- 239000011230 binding agent Substances 0.000 claims description 2
- 239000012472 biological sample Substances 0.000 claims description 2
- 238000001574 biopsy Methods 0.000 claims description 2
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 229950009791 durvalumab Drugs 0.000 claims description 2
- 230000002708 enhancing effect Effects 0.000 claims description 2
- 230000002068 genetic effect Effects 0.000 claims description 2
- 230000001939 inductive effect Effects 0.000 claims description 2
- 239000000138 intercalating agent Substances 0.000 claims description 2
- 238000001990 intravenous administration Methods 0.000 claims description 2
- 230000001394 metastastic effect Effects 0.000 claims description 2
- 206010061289 metastatic neoplasm Diseases 0.000 claims description 2
- 239000006186 oral dosage form Substances 0.000 claims description 2
- 230000008520 organization Effects 0.000 claims description 2
- 230000037361 pathway Effects 0.000 claims description 2
- 229950010773 pidilizumab Drugs 0.000 claims description 2
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims description 2
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims 1
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims 1
- 230000000340 anti-metabolite Effects 0.000 claims 1
- 229940100197 antimetabolite Drugs 0.000 claims 1
- 239000002256 antimetabolite Substances 0.000 claims 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 description 2
- 239000000651 prodrug Substances 0.000 description 2
- 229940125431 BRAF inhibitor Drugs 0.000 description 1
- 150000004934 Regorafenib derivatives Chemical group 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462077127P | 2014-11-07 | 2014-11-07 | |
| US62/077,127 | 2014-11-07 | ||
| US201562115228P | 2015-02-12 | 2015-02-12 | |
| US62/115,228 | 2015-02-12 | ||
| US201562119540P | 2015-02-23 | 2015-02-23 | |
| US62/119,540 | 2015-02-23 | ||
| PCT/US2015/059526 WO2016073884A1 (en) | 2014-11-07 | 2015-11-06 | Apilimod for use in the treatment of colorectal cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017533963A JP2017533963A (ja) | 2017-11-16 |
| JP2017533963A5 true JP2017533963A5 (enExample) | 2018-12-13 |
| JP6716585B2 JP6716585B2 (ja) | 2020-07-01 |
Family
ID=54548301
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017543327A Expired - Fee Related JP6768682B2 (ja) | 2014-11-07 | 2015-11-06 | メラノーマの処置に使用するためのアピリモド |
| JP2017543330A Expired - Fee Related JP6716585B2 (ja) | 2014-11-07 | 2015-11-06 | 結腸直腸癌の処置に使用するためのアピリモド |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017543327A Expired - Fee Related JP6768682B2 (ja) | 2014-11-07 | 2015-11-06 | メラノーマの処置に使用するためのアピリモド |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US10765682B2 (enExample) |
| EP (3) | EP3215157B8 (enExample) |
| JP (2) | JP6768682B2 (enExample) |
| KR (2) | KR20170101907A (enExample) |
| CN (2) | CN107427522B (enExample) |
| AU (2) | AU2015342876B2 (enExample) |
| BR (2) | BR112017009265A2 (enExample) |
| CA (2) | CA2966334A1 (enExample) |
| ES (1) | ES2734081T3 (enExample) |
| HU (1) | HUE044153T2 (enExample) |
| IL (2) | IL251904B (enExample) |
| MX (2) | MX2017006026A (enExample) |
| PL (1) | PL3215157T3 (enExample) |
| PT (1) | PT3215157T (enExample) |
| RU (2) | RU2731908C2 (enExample) |
| WO (2) | WO2016073884A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10179135B2 (en) | 2014-01-24 | 2019-01-15 | Lam Therapeutics, Inc. | Apilimod compositions and methods for using same |
| GB201408100D0 (en) * | 2014-05-07 | 2014-06-18 | Sec Dep For Health The | Detection method |
| BR112017008799A2 (pt) | 2014-11-07 | 2017-12-19 | Lam Therapeutics Inc | composições de apilimod e métodos de uso das mesmas no tratamento de câncer renal |
| EP3405199A1 (en) * | 2016-01-21 | 2018-11-28 | LAM Therapeutics, Inc. | Biomarkers for treating cancer with apilimod |
| AU2017342262B2 (en) * | 2016-10-12 | 2023-09-28 | Orphai Therapeutics Inc. | Apilimod compositions and methods for using same in the treatment of alzheimer's disease |
| JP7300394B2 (ja) | 2017-01-17 | 2023-06-29 | ヘパリジェニックス ゲーエムベーハー | 肝再生の促進又は肝細胞死の低減もしくは予防のためのプロテインキナーゼ阻害 |
| RU2020130837A (ru) | 2018-02-21 | 2022-03-21 | ЭйАй ТЕРАПЬЮТИКС, ИНК. | Комбинационная терапия апилимодом и глутаматергическими агентами |
| PH12022551623A1 (en) | 2020-01-13 | 2023-11-29 | Verge Analytics Inc | Substituted pyrazolo-pyrimidines and uses thereof |
| IL309143A (en) * | 2021-06-11 | 2024-02-01 | Orphai Therapeutics Inc | Stabilized apilimod compositions and uses thereof |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6693097B2 (en) * | 2001-11-30 | 2004-02-17 | Synta Pharmaceuticals Corp. | Pyrimidine compounds |
| MXPA06008746A (es) | 2004-02-06 | 2007-01-23 | Elan Pharm Inc | Metodos y composiciones para tratamiento de tumores y enfermedad metastatica. |
| WO2005112938A2 (en) * | 2004-04-13 | 2005-12-01 | Synta Pharmaceuticals Corp. | Disalt inhibitors of il-12 production |
| CA2579096C (en) | 2004-09-08 | 2012-11-13 | Chelsea Therapeutics, Inc. | Quinazoline derivatives as metabolically inert antifolate compounds |
| WO2006053112A1 (en) | 2004-11-10 | 2006-05-18 | Synta Pharmaceuticals Corp. | Process for preparing trisubstituted pyrimidine compounds |
| WO2006124662A1 (en) | 2005-05-13 | 2006-11-23 | Synta Pharmaceuticals Corp. | Il-12 modulatory compounds |
| WO2006128129A2 (en) * | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating cancer |
| EA015463B1 (ru) | 2005-11-17 | 2011-08-30 | Оси Фармасьютикалз, Инк. | КОНДЕНСИРОВАННОЕ БИЦИКЛИЧЕСКОЕ СОЕДИНЕНИЕ - ИНГИБИТОР mTOR, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ЕГО СОДЕРЖАЩАЯ, И СПОСОБ ЛЕЧЕНИЯ РАКА |
| EA031888B1 (ru) | 2006-07-12 | 2019-03-29 | Юниверсити Оф Теннесси Рисерч Фаундейшн | Способы применения замещенных ациланилидов |
| RU2438664C2 (ru) * | 2007-05-15 | 2012-01-10 | Пирамал Лайф Сайнсиз Лимитед | Синергическая фармацевтическая комбинация для лечения рака |
| US8402515B2 (en) | 2010-05-06 | 2013-03-19 | Jonathan Weizman | Apparatus and method for establishing a peer-to-peer communication session with a client device |
| US20110287018A1 (en) * | 2010-05-19 | 2011-11-24 | Philip Bosch | Methods of Treating Interstitial Cystitis |
| WO2013152342A1 (en) * | 2012-04-06 | 2013-10-10 | OSI Pharmaceuticals, LLC | Anti-cancer mtor inhibitor and anti-androgen combination |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| US9295731B2 (en) * | 2013-04-01 | 2016-03-29 | Mark Quang Nguyen | Cleavable drug conjugates, compositions thereof and methods of use |
| US10179135B2 (en) * | 2014-01-24 | 2019-01-15 | Lam Therapeutics, Inc. | Apilimod compositions and methods for using same |
| BR112017008799A2 (pt) * | 2014-11-07 | 2017-12-19 | Lam Therapeutics Inc | composições de apilimod e métodos de uso das mesmas no tratamento de câncer renal |
| WO2016126707A1 (en) * | 2015-02-03 | 2016-08-11 | Lam Therapeutics, Inc. | Apilimod compositions and methods for using same |
| WO2016160102A1 (en) * | 2015-03-31 | 2016-10-06 | Lam Therapeutics, Inc. | Active metabolites of apilimod and uses thereof |
| TWI746449B (zh) * | 2015-07-20 | 2021-11-21 | 美商Ａｉ治療公司 | 使用阿吡莫德治療癌症之方法 |
-
2015
- 2015-11-06 CN CN201580072613.9A patent/CN107427522B/zh not_active Expired - Fee Related
- 2015-11-06 BR BR112017009265A patent/BR112017009265A2/pt not_active Application Discontinuation
- 2015-11-06 EP EP15795317.5A patent/EP3215157B8/en not_active Not-in-force
- 2015-11-06 JP JP2017543327A patent/JP6768682B2/ja not_active Expired - Fee Related
- 2015-11-06 WO PCT/US2015/059526 patent/WO2016073884A1/en not_active Ceased
- 2015-11-06 CA CA2966334A patent/CA2966334A1/en not_active Abandoned
- 2015-11-06 CA CA2966356A patent/CA2966356A1/en not_active Abandoned
- 2015-11-06 RU RU2017119064A patent/RU2731908C2/ru active
- 2015-11-06 AU AU2015342876A patent/AU2015342876B2/en not_active Ceased
- 2015-11-06 PL PL15795317T patent/PL3215157T3/pl unknown
- 2015-11-06 EP EP15795319.1A patent/EP3215159B1/en active Active
- 2015-11-06 KR KR1020177015387A patent/KR20170101907A/ko not_active Ceased
- 2015-11-06 PT PT15795317T patent/PT3215157T/pt unknown
- 2015-11-06 AU AU2015342863A patent/AU2015342863B2/en not_active Ceased
- 2015-11-06 EP EP21186071.3A patent/EP3954375A1/en not_active Withdrawn
- 2015-11-06 ES ES15795317T patent/ES2734081T3/es active Active
- 2015-11-06 HU HUE15795317A patent/HUE044153T2/hu unknown
- 2015-11-06 WO PCT/US2015/059502 patent/WO2016073871A1/en not_active Ceased
- 2015-11-06 BR BR112017009000A patent/BR112017009000A2/pt not_active Application Discontinuation
- 2015-11-06 CN CN201580072610.5A patent/CN107206090A/zh active Pending
- 2015-11-06 MX MX2017006026A patent/MX2017006026A/es unknown
- 2015-11-06 JP JP2017543330A patent/JP6716585B2/ja not_active Expired - Fee Related
- 2015-11-06 US US15/524,841 patent/US10765682B2/en active Active
- 2015-11-06 KR KR1020177015389A patent/KR20170098813A/ko not_active Ceased
- 2015-11-06 RU RU2017119066A patent/RU2739992C2/ru active
- 2015-11-06 US US15/524,846 patent/US20190209576A1/en not_active Abandoned
- 2015-11-06 MX MX2017006019A patent/MX374385B/es active IP Right Grant
-
2017
- 2017-04-24 IL IL251904A patent/IL251904B/en active IP Right Grant
- 2017-04-24 IL IL251903A patent/IL251903B/en active IP Right Grant
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