JP2017533963A5 - - Google Patents
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- Publication number
- 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 (OSRAM) | 2018-12-13 |
| JP6716585B2 JP6716585B2 (ja) | 2020-07-01 |
Family
ID=54548301
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
| 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 |
Family Applications After (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) | US20190209576A1 (OSRAM) |
| EP (3) | EP3215157B8 (OSRAM) |
| JP (2) | JP6716585B2 (OSRAM) |
| KR (2) | KR20170101907A (OSRAM) |
| CN (2) | CN107206090A (OSRAM) |
| AU (2) | AU2015342863B2 (OSRAM) |
| BR (2) | BR112017009000A2 (OSRAM) |
| CA (2) | CA2966334A1 (OSRAM) |
| ES (1) | ES2734081T3 (OSRAM) |
| HU (1) | HUE044153T2 (OSRAM) |
| IL (2) | IL251903B (OSRAM) |
| MX (2) | MX374385B (OSRAM) |
| PL (1) | PL3215157T3 (OSRAM) |
| PT (1) | PT3215157T (OSRAM) |
| RU (2) | RU2731908C2 (OSRAM) |
| WO (2) | WO2016073871A1 (OSRAM) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6855243B2 (ja) | 2014-01-24 | 2021-04-07 | エイアイ・セラピューティクス・インコーポレーテッド | 癌治療のためのアピリモド（ａｐｉｌｉｍｏｄ）組成物 |
| GB201408100D0 (en) * | 2014-05-07 | 2014-06-18 | Sec Dep For Health The | Detection method |
| KR20170098812A (ko) | 2014-11-07 | 2017-08-30 | 램 테라퓨틱스, 인코포레이티드 | 신장암의 치료에 사용하기 위한 아필리모드 |
| AU2017210324A1 (en) * | 2016-01-21 | 2018-08-16 | AI Therapeutics, Inc. | Biomarkers for treating cancer with apilimod |
| US20190365771A1 (en) * | 2016-10-12 | 2019-12-05 | AI Therapeutics, Inc. | Apilimod compositions and methods for using same in the treatment of alzheimer's disease |
| WO2018134254A1 (en) | 2017-01-17 | 2018-07-26 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| JP7354123B2 (ja) | 2018-02-21 | 2023-10-02 | エイアイ・セラピューティクス・インコーポレーテッド | アピリモドとグルタミン酸作動薬を用いた併用療法 |
| MX2022008627A (es) | 2020-01-13 | 2022-11-08 | Verge Analytics Inc | Pirazolo-pirimidinas sustituidas y usos de las mismas. |
| KR20240075774A (ko) * | 2021-06-11 | 2024-05-29 | 오르파이 테라퓨틱스 인코포레이티드 | 안정화된 아필리모드 조성물 및 이의 용도 |
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 |
| NZ584288A (en) | 2004-02-06 | 2011-10-28 | Elan Pharm Inc | Methods and compositions for treating tumors and metastatic disease |
| WO2005112938A2 (en) * | 2004-04-13 | 2005-12-01 | Synta Pharmaceuticals Corp. | Disalt inhibitors of il-12 production |
| AU2005282241B2 (en) | 2004-09-08 | 2011-03-03 | Chelsea Therapeutics, Inc. | Quinazoline derivatives as metabolically inert antifolate compounds. |
| US7923557B2 (en) | 2004-11-10 | 2011-04-12 | Synta Pharmaceuticals Corporation | Process for preparing trisubstituted pyrimidine compounds |
| US7863270B2 (en) * | 2005-05-13 | 2011-01-04 | Synta Pharmaceuticals Corp. | IL-12 modulatory compounds |
| WO2006128129A2 (en) * | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating cancer |
| PT2385053E (pt) | 2005-11-17 | 2013-12-17 | Osi Pharm Inc | Intermediários para a preparação de compostos bicíclicos condensados como inibidores mtor |
| CA2658394C (en) | 2006-07-12 | 2016-08-16 | University Of Tennessee Research Foundation | Substituted acylanilides and methods of use thereof |
| 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 |
| WO2011146727A1 (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 |
| JP6855243B2 (ja) * | 2014-01-24 | 2021-04-07 | エイアイ・セラピューティクス・インコーポレーテッド | 癌治療のためのアピリモド（ａｐｉｌｉｍｏｄ）組成物 |
| KR20170098812A (ko) * | 2014-11-07 | 2017-08-30 | 램 테라퓨틱스, 인코포레이티드 | 신장암의 치료에 사용하기 위한 아필리모드 |
| US20180015098A1 (en) * | 2015-02-03 | 2018-01-18 | Lam Therapeutics, Inc. | Apilimod compositions and methods for using same |
| US20180078561A1 (en) * | 2015-03-31 | 2018-03-22 | 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 US US15/524,846 patent/US20190209576A1/en not_active Abandoned
- 2015-11-06 EP EP15795317.5A patent/EP3215157B8/en not_active Not-in-force
- 2015-11-06 PL PL15795317T patent/PL3215157T3/pl unknown
- 2015-11-06 KR KR1020177015387A patent/KR20170101907A/ko not_active Ceased
- 2015-11-06 PT PT15795317T patent/PT3215157T/pt unknown
- 2015-11-06 HU HUE15795317A patent/HUE044153T2/hu unknown
- 2015-11-06 US US15/524,841 patent/US10765682B2/en active Active
- 2015-11-06 JP JP2017543330A patent/JP6716585B2/ja not_active Expired - Fee Related
- 2015-11-06 MX MX2017006019A patent/MX374385B/es active IP Right Grant
- 2015-11-06 EP EP15795319.1A patent/EP3215159B1/en active Active
- 2015-11-06 RU RU2017119064A patent/RU2731908C2/ru active
- 2015-11-06 RU RU2017119066A patent/RU2739992C2/ru active
- 2015-11-06 MX MX2017006026A patent/MX2017006026A/es unknown
- 2015-11-06 CN CN201580072610.5A patent/CN107206090A/zh active Pending
- 2015-11-06 CN CN201580072613.9A patent/CN107427522B/zh not_active Expired - Fee Related
- 2015-11-06 JP JP2017543327A patent/JP6768682B2/ja not_active Expired - Fee Related
- 2015-11-06 CA CA2966334A patent/CA2966334A1/en not_active Abandoned
- 2015-11-06 AU AU2015342863A patent/AU2015342863B2/en not_active Ceased
- 2015-11-06 BR BR112017009000A patent/BR112017009000A2/pt not_active Application Discontinuation
- 2015-11-06 AU AU2015342876A patent/AU2015342876B2/en not_active Ceased
- 2015-11-06 CA CA2966356A patent/CA2966356A1/en not_active Abandoned
- 2015-11-06 ES ES15795317T patent/ES2734081T3/es active Active
- 2015-11-06 WO PCT/US2015/059502 patent/WO2016073871A1/en not_active Ceased
- 2015-11-06 KR KR1020177015389A patent/KR20170098813A/ko not_active Ceased
- 2015-11-06 EP EP21186071.3A patent/EP3954375A1/en not_active Withdrawn
- 2015-11-06 WO PCT/US2015/059526 patent/WO2016073884A1/en not_active Ceased
- 2015-11-06 BR BR112017009265A patent/BR112017009265A2/pt not_active Application Discontinuation
-
2017
- 2017-04-24 IL IL251903A patent/IL251903B/en active IP Right Grant
- 2017-04-24 IL IL251904A patent/IL251904B/en active IP Right Grant
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