JP2015505816A5 - - Google Patents
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- Publication number
- JP2015505816A5 JP2015505816A5 JP2014540146A JP2014540146A JP2015505816A5 JP 2015505816 A5 JP2015505816 A5 JP 2015505816A5 JP 2014540146 A JP2014540146 A JP 2014540146A JP 2014540146 A JP2014540146 A JP 2014540146A JP 2015505816 A5 JP2015505816 A5 JP 2015505816A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- hydroxycyclopentyl
- inden
- dihydro
- 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
- 150000003839 salts Chemical class 0.000 claims description 73
- 206010028980 Neoplasm Diseases 0.000 claims description 38
- 201000011510 cancer Diseases 0.000 claims description 38
- 102000038427 NEDD8-activating enzyme E1 Human genes 0.000 claims description 27
- 108091007790 NEDD8-activating enzyme E1 Proteins 0.000 claims description 27
- 239000003112 inhibitor Substances 0.000 claims description 27
- BDAGIHXWWSANSR-UHFFFAOYSA-M Formate Chemical compound [O-]C=O BDAGIHXWWSANSR-UHFFFAOYSA-M 0.000 claims description 25
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 24
- 229940075628 hypomethylating agent Drugs 0.000 claims description 22
- NMUSYJAQQFHJEW-KVTDHHQDSA-N 5-azacytidine Chemical group O=C1N=C(N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 NMUSYJAQQFHJEW-KVTDHHQDSA-N 0.000 claims description 15
- 229960002756 azacitidine Drugs 0.000 claims description 15
- MPUQHZXIXSTTDU-QXGSTGNESA-N sulfamic acid [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]-7-pyrrolo[2,3-d]pyrimidinyl]-2-hydroxycyclopentyl]methyl ester Chemical group C1[C@H](O)[C@H](COS(=O)(=O)N)C[C@H]1N1C2=NC=NC(N[C@@H]3C4=CC=CC=C4CC3)=C2C=C1 MPUQHZXIXSTTDU-QXGSTGNESA-N 0.000 claims description 11
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 10
- 229940079593 drug Drugs 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 10
- -1 {(1S, 2S, 4R) -4- [ (6-{[(1R, 2S) -5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl] amino} pyrimidin-4-yl) oxy] -2-hydroxycyclopentyl} methyl Chemical group 0.000 claims description 10
- 208000009527 Refractory anemia Diseases 0.000 claims description 8
- 206010072684 Refractory cytopenia with unilineage dysplasia Diseases 0.000 claims description 8
- 238000003745 diagnosis Methods 0.000 claims description 8
- XAUDJQYHKZQPEU-KVQBGUIXSA-N 5-aza-2'-deoxycytidine Chemical compound O=C1N=C(N)N=CN1[C@@H]1O[C@H](CO)[C@@H](O)C1 XAUDJQYHKZQPEU-KVQBGUIXSA-N 0.000 claims description 7
- 229960003603 decitabine Drugs 0.000 claims description 7
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 6
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 6
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 6
- 230000002071 myeloproliferative effect Effects 0.000 claims description 6
- 208000011580 syndromic disease Diseases 0.000 claims description 6
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 4
- 239000002552 dosage form Substances 0.000 claims description 4
- UVNSDOGOYDQGLY-ZDUSSCGKSA-N n-[(1s)-2,3-dihydro-1h-inden-1-yl]-7h-pyrrolo[2,3-d]pyrimidin-4-amine Chemical compound N([C@@H]1C2=CC=CC=C2CC1)C1=NC=NC2=C1C=CN2 UVNSDOGOYDQGLY-ZDUSSCGKSA-N 0.000 claims description 3
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims description 2
- 229910052742 iron Inorganic materials 0.000 claims description 2
- 230000035755 proliferation Effects 0.000 claims description 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 8
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 8
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 4
- 230000001684 chronic effect Effects 0.000 claims 4
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 4
- 208000032839 leukemia Diseases 0.000 claims 4
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 210000001185 bone marrow Anatomy 0.000 claims 1
- FIYXUOWXHWJDAM-UHFFFAOYSA-N methyl sulfamate Chemical compound COS(N)(=O)=O FIYXUOWXHWJDAM-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 description 31
- 208000017604 Hodgkin disease Diseases 0.000 description 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 description 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 206010066476 Haematological malignancy Diseases 0.000 description 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 description 1
- 208000034578 Multiple myelomas Diseases 0.000 description 1
- 206010035226 Plasma cell myeloma Diseases 0.000 description 1
- 206010042971 T-cell lymphoma Diseases 0.000 description 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 description 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 description 1
- HJKDNNXKYODZJI-BVMPOVDASA-N [(1s,2s,4r)-4-[4-[[(1s)-2,3-dihydro-1h-inden-1-yl]amino]pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl sulfamate;hydrochloride Chemical compound Cl.C1[C@H](O)[C@H](COS(=O)(=O)N)C[C@H]1N1C2=NC=NC(N[C@@H]3C4=CC=CC=C4CC3)=C2C=C1 HJKDNNXKYODZJI-BVMPOVDASA-N 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161555049P | 2011-11-03 | 2011-11-03 | |
| US61/555,049 | 2011-11-03 | ||
| PCT/US2012/063382 WO2013067396A2 (en) | 2011-11-03 | 2012-11-02 | Administration of nedd8-activating enzyme inhibitor and hypomethylating agent |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017203560A Division JP2018009035A (ja) | 2011-11-03 | 2017-10-20 | Ｎｅｄｄ８活性化酵素阻害剤および低メチル化剤の投与 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015505816A JP2015505816A (ja) | 2015-02-26 |
| JP2015505816A5 true JP2015505816A5 (https=) | 2017-10-26 |
| JP6231988B2 JP6231988B2 (ja) | 2017-11-15 |
Family
ID=48193039
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014540146A Active JP6231988B2 (ja) | 2011-11-03 | 2012-11-02 | Ｎｅｄｄ８活性化酵素阻害剤および低メチル化剤の投与 |
| JP2017203560A Pending JP2018009035A (ja) | 2011-11-03 | 2017-10-20 | Ｎｅｄｄ８活性化酵素阻害剤および低メチル化剤の投与 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017203560A Pending JP2018009035A (ja) | 2011-11-03 | 2017-10-20 | Ｎｅｄｄ８活性化酵素阻害剤および低メチル化剤の投与 |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US8980850B2 (https=) |
| EP (1) | EP2773360B1 (https=) |
| JP (2) | JP6231988B2 (https=) |
| KR (1) | KR101987861B1 (https=) |
| CN (1) | CN104245699B (https=) |
| AU (1) | AU2012321106C1 (https=) |
| BR (1) | BR112014010699B1 (https=) |
| CA (1) | CA2854461C (https=) |
| EA (1) | EA028380B1 (https=) |
| ES (1) | ES2668272T3 (https=) |
| GE (2) | GEP20186940B (https=) |
| HK (1) | HK1201733A1 (https=) |
| IL (1) | IL232353B (https=) |
| MA (1) | MA35662B1 (https=) |
| MX (1) | MX357835B (https=) |
| MY (1) | MY176125A (https=) |
| PH (1) | PH12014501001B1 (https=) |
| PL (1) | PL2773360T3 (https=) |
| SG (1) | SG11201401895WA (https=) |
| TN (1) | TN2014000194A1 (https=) |
| TR (1) | TR201807342T4 (https=) |
| UA (1) | UA114414C2 (https=) |
| WO (1) | WO2013067396A2 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG175929A1 (en) | 2009-05-14 | 2011-12-29 | Millennium Pharm Inc | Hydrochloride salt of ((1s,2s,4r)-4-{4-[(1s)-2,3-dihydro-1h-inden-1-ylamino]-7h-pyrrolo [2,3-d]pyrimidin-7-yl}-2-hydroxycyclopentyl)methyl sulfamate |
| SG11201400102WA (en) * | 2011-08-24 | 2014-03-28 | Millennium Pharm Inc | Inhibitors of nedd8-activating enzyme |
| EP2764866A1 (en) * | 2013-02-07 | 2014-08-13 | IP Gesellschaft für Management mbH | Inhibitors of nedd8-activating enzyme |
| CA2923752A1 (en) | 2013-05-14 | 2014-11-20 | Millennium Pharmaceuticals, Inc. | Administration of nedd8-activating enzyme inhibitor and chemotherapeutic agents |
| EP3024488A1 (en) * | 2013-07-26 | 2016-06-01 | Boehringer Ingelheim International GmbH | Volasertib in combination with azacitidine for the treatment of acute myeloid leukemia and myelodysplastic syndrome ii |
| SG11201608303QA (en) | 2014-04-04 | 2016-11-29 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
| CN103948590A (zh) * | 2014-05-22 | 2014-07-30 | 中国药科大学 | Nedd8激活酶抑制剂及其医药用途 |
| US10695352B2 (en) * | 2015-10-15 | 2020-06-30 | Celgene Corporation | Combination therapy for treating malignancies |
| US11701406B2 (en) | 2017-05-25 | 2023-07-18 | The Board Of Trustees Of The Leland Stanford Junior University | Combination of low dose IL-2 and an inhibitor of Treg IL-2R desensitization to treat autoimmune and allergic inflammatory diseases |
| WO2019060536A1 (en) * | 2017-09-21 | 2019-03-28 | Millennium Pharmaceuticals, Inc. | CO-CRYSTALLINE FORMS OF ((1S, 2S, 4R) -4- {4 - [(1S) -2,3-DIHYDRO-1H-INDEN-1-YLAMINO] -7H-PYRROLO [2,3-D] PYRIMIDIN -7-YL} -2-HYDROXYCYCLOPENTYL) METHYLSULFAMATE, THEIR FORMULATIONS AND USES |
| WO2020106876A2 (en) * | 2018-11-20 | 2020-05-28 | Fulcrum Therapeutics, Inc. | Compositions and methods for increasing fetal hemoglobin and treating sickle cell disease |
| WO2020190754A1 (en) | 2019-03-15 | 2020-09-24 | Fulcrum Therapeutics, Inc. | Macrocyclic azolopyridine derivatives as eed and prc2 modulators |
| WO2023025668A1 (en) | 2021-08-25 | 2023-03-02 | Asociación Centro De Investigación Cooperativa En Biociencias-Cic Biogune | Methods for the generation of stem cell memory t cells for adoptive t cell therapy |
| WO2023242235A1 (en) * | 2022-06-14 | 2023-12-21 | Scandion Oncology A/S | Abcg2 inhibitor and nae inhibitor for the treatment of cancer |
| CN115007323B (zh) * | 2022-06-17 | 2024-01-23 | 中南大学 | 一种抑制矿物中黄铁矿浮选的方法 |
| US20260023068A1 (en) * | 2022-07-11 | 2026-01-22 | Westlake University | Use of a fbxo42 specific inhibitor in treating notch signaling-dependent disease |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6943249B2 (en) | 2003-03-17 | 2005-09-13 | Ash Stevens, Inc. | Methods for isolating crystalline Form I of 5-azacytidine |
| US6887855B2 (en) | 2003-03-17 | 2005-05-03 | Pharmion Corporation | Forms of 5-azacytidine |
| US20060063735A1 (en) | 2004-09-17 | 2006-03-23 | Supergen, Inc. | Salts of 5-azacytidine |
| US20060128654A1 (en) | 2004-12-10 | 2006-06-15 | Chunlin Tang | Pharmaceutical formulation of cytidine analogs and derivatives |
| PT1848718E (pt) | 2005-02-04 | 2012-10-11 | Millennium Pharm Inc | Inibidores de enzimas de activação e1 |
| KR101450535B1 (ko) | 2006-02-02 | 2014-10-14 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Ｅ１ 활성화 효소의 억제제 |
| EA201501088A1 (ru) * | 2006-08-08 | 2017-01-30 | Миллениум Фармасьютикалз, Инк. | Гетероарильные соединения, применяемые в качестве ингибиторов e1 активирующих ферментов |
| US20080057086A1 (en) | 2006-09-01 | 2008-03-06 | Pharmion Corporation | Colon-targeted oral formulations of cytidine analogs |
| EP2211870A1 (en) | 2007-11-01 | 2010-08-04 | Celgene Corporation | Cytidine analogs for treatment of myelodysplastic syndromes |
| US20110021517A1 (en) * | 2008-02-26 | 2011-01-27 | Nerviano Medical Sciences S.R.L. | Antitumor combination comprising a morpholinyl anthracycline derivative and demethylating agents |
| PL3692983T3 (pl) | 2008-05-15 | 2021-12-27 | Celgene Corporation | Doustne formulacje analogów cytydyny i sposoby ich zastosowania |
| AU2009259136B2 (en) * | 2008-06-09 | 2014-09-25 | Cyclacel Limited | Combinations of sapacitabine or CNDAC with DNA methyltransferase inhibitors such as decitabine and procaine |
| CA2755976C (en) * | 2009-03-23 | 2020-04-07 | Ambit Biosciences Corporation | Methods of treatment using combination therapy |
| SG175929A1 (en) | 2009-05-14 | 2011-12-29 | Millennium Pharm Inc | Hydrochloride salt of ((1s,2s,4r)-4-{4-[(1s)-2,3-dihydro-1h-inden-1-ylamino]-7h-pyrrolo [2,3-d]pyrimidin-7-yl}-2-hydroxycyclopentyl)methyl sulfamate |
| JP2014503597A (ja) | 2011-01-31 | 2014-02-13 | セルジーン コーポレイション | シチジンアナログの医薬組成物及びその使用方法 |
| TW201700103A (zh) | 2011-11-01 | 2017-01-01 | 西建公司 | 利用胞嘧啶核苷類似物之口服配方治療癌症的方法 |
-
2012
- 2012-11-02 KR KR1020147014236A patent/KR101987861B1/ko not_active Expired - Fee Related
- 2012-11-02 JP JP2014540146A patent/JP6231988B2/ja active Active
- 2012-11-02 UA UAA201405842A patent/UA114414C2/uk unknown
- 2012-11-02 BR BR112014010699-1A patent/BR112014010699B1/pt not_active IP Right Cessation
- 2012-11-02 AU AU2012321106A patent/AU2012321106C1/en not_active Ceased
- 2012-11-02 GE GEAP201813483A patent/GEP20186940B/en unknown
- 2012-11-02 WO PCT/US2012/063382 patent/WO2013067396A2/en not_active Ceased
- 2012-11-02 TR TR2018/07342T patent/TR201807342T4/tr unknown
- 2012-11-02 US US13/667,641 patent/US8980850B2/en active Active
- 2012-11-02 PH PH1/2014/501001A patent/PH12014501001B1/en unknown
- 2012-11-02 HK HK15102294.2A patent/HK1201733A1/xx unknown
- 2012-11-02 SG SG11201401895WA patent/SG11201401895WA/en unknown
- 2012-11-02 GE GEAP201213483A patent/GEP20196940B/en unknown
- 2012-11-02 EP EP12844799.2A patent/EP2773360B1/en active Active
- 2012-11-02 CN CN201280062112.9A patent/CN104245699B/zh active Active
- 2012-11-02 CA CA2854461A patent/CA2854461C/en not_active Expired - Fee Related
- 2012-11-02 PL PL12844799T patent/PL2773360T3/pl unknown
- 2012-11-02 EA EA201400539A patent/EA028380B1/ru not_active IP Right Cessation
- 2012-11-02 MY MYPI2014001239A patent/MY176125A/en unknown
- 2012-11-02 ES ES12844799.2T patent/ES2668272T3/es active Active
- 2012-11-02 MX MX2014005323A patent/MX357835B/es active IP Right Grant
-
2014
- 2014-04-29 IL IL232353A patent/IL232353B/en active IP Right Grant
- 2014-04-30 TN TNP2014000194A patent/TN2014000194A1/en unknown
- 2014-05-26 MA MA37066A patent/MA35662B1/fr unknown
-
2015
- 2015-01-23 US US14/603,717 patent/US20150366886A1/en not_active Abandoned
-
2017
- 2017-10-20 JP JP2017203560A patent/JP2018009035A/ja active Pending
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