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) | GEP20196940B (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 |
|---|---|---|---|---|
| EP2430026A1 (en) | 2009-05-14 | 2012-03-21 | Millennium Pharmaceuticals, 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 |
| JP6038150B2 (ja) * | 2011-08-24 | 2016-12-07 | ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | Ｎｅｄｄ８活性化酵素阻害剤 |
| 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 |
| JP2016525531A (ja) * | 2013-07-26 | 2016-08-25 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 急性骨髄性白血病及び骨髄異形成症候群の処置のためのアザシチジンと組み合わせたボラセルチブ |
| KR102359214B1 (ko) | 2014-04-04 | 2022-02-07 | 델 마 파마슈티컬스 | 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체 |
| 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 |
| WO2018218119A1 (en) * | 2017-05-25 | 2018-11-29 | 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 |
| EP3684363A4 (en) * | 2017-09-21 | 2021-05-12 | Millennium Pharmaceuticals, Inc. | CO-CRYSTALLINE FORMS OF ((1S, 2S, 4R) -4- {4 - [(1S) -2,3-DIHYDRO-1H-INDÉN-1-YLAMINO] -7H-PYRROLO [2,3-D] PYRIMIDIN -7-YL} -2-HYDROXYCYCLOPENTYL) METHYLSULFAMATE, THEIR FORMULATIONS AND USES |
| US20220017908A1 (en) * | 2018-11-20 | 2022-01-20 | Fulcrum Therapeutics, Inc. | Compositions and methods for increasing fetal hemoglobin and treating sickle cell disease |
| CA3133751A1 (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 |
| EP4554608A1 (en) * | 2022-07-11 | 2025-05-21 | 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 |
|---|---|---|---|---|
| US6887855B2 (en) | 2003-03-17 | 2005-05-03 | Pharmion Corporation | Forms of 5-azacytidine |
| US6943249B2 (en) | 2003-03-17 | 2005-09-13 | Ash Stevens, Inc. | Methods for isolating crystalline Form I 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 |
| RS52458B (sr) | 2005-02-04 | 2013-02-28 | Millennium Pharmaceuticals Inc. | Inhibitori e1 aktivirajućih enzima |
| EA024006B1 (ru) | 2006-02-02 | 2016-08-31 | Миллениум Фармасьютикалз, Инк. | Ингибиторы е1 активирующих ферментов |
| ZA200900670B (en) * | 2006-08-08 | 2010-04-28 | Millennium Pharm Inc | Heteroaryl compounds useful as inhititors of E1 activating enzymes |
| 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 |
| EP2257310A2 (en) * | 2008-02-26 | 2010-12-08 | Nerviano Medical Sciences S.r.l. | Antitumor combination comprising a morpholinyl anthracycline derivative and demethylating agents |
| EP3782612B1 (en) | 2008-05-15 | 2023-11-08 | Celgene Corporation | Oral formulations of cytidine analogs and methods of use thereof |
| NZ589719A (en) * | 2008-06-09 | 2012-08-31 | Cyclacel Ltd | Combinations of sapacitabine or cndac with dna methyltransferase inhibitors such as decitabine and procaine |
| CN102438588B (zh) * | 2009-03-23 | 2015-04-01 | 埃姆比特生物科学公司 | 使用联合治疗法治疗疾病的方法 |
| EP2430026A1 (en) | 2009-05-14 | 2012-03-21 | Millennium Pharmaceuticals, 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 |
| WO2012106299A1 (en) | 2011-01-31 | 2012-08-09 | Celgene Corporation | Pharmaceutical compositions of cytidine analogs and methods of use thereof |
| US9125884B2 (en) | 2011-11-01 | 2015-09-08 | Celgene Corporation | Methods for treating cancers using oral formulations of cytidine analogs |
-
2012
- 2012-11-02 MY MYPI2014001239A patent/MY176125A/en unknown
- 2012-11-02 GE GEAP201213483A patent/GEP20196940B/en unknown
- 2012-11-02 EA EA201400539A patent/EA028380B1/ru not_active IP Right Cessation
- 2012-11-02 GE GEAP201813483A patent/GEP20186940B/en unknown
- 2012-11-02 JP JP2014540146A patent/JP6231988B2/ja active Active
- 2012-11-02 HK HK15102294.2A patent/HK1201733A1/xx unknown
- 2012-11-02 ES ES12844799.2T patent/ES2668272T3/es active Active
- 2012-11-02 MX MX2014005323A patent/MX357835B/es active IP Right Grant
- 2012-11-02 TR TR2018/07342T patent/TR201807342T4/tr unknown
- 2012-11-02 WO PCT/US2012/063382 patent/WO2013067396A2/en not_active Ceased
- 2012-11-02 CN CN201280062112.9A patent/CN104245699B/zh active Active
- 2012-11-02 PH PH1/2014/501001A patent/PH12014501001B1/en unknown
- 2012-11-02 EP EP12844799.2A patent/EP2773360B1/en active Active
- 2012-11-02 AU AU2012321106A patent/AU2012321106C1/en not_active Ceased
- 2012-11-02 US US13/667,641 patent/US8980850B2/en active Active
- 2012-11-02 SG SG11201401895WA patent/SG11201401895WA/en unknown
- 2012-11-02 UA UAA201405842A patent/UA114414C2/uk unknown
- 2012-11-02 CA CA2854461A patent/CA2854461C/en not_active Expired - Fee Related
- 2012-11-02 KR KR1020147014236A patent/KR101987861B1/ko not_active Expired - Fee Related
- 2012-11-02 BR BR112014010699-1A patent/BR112014010699B1/pt not_active IP Right Cessation
- 2012-11-02 PL PL12844799T patent/PL2773360T3/pl unknown
-
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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