JP2014524476A5 - - Google Patents
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- JP2014524476A5 JP2014524476A5 JP2014527287A JP2014527287A JP2014524476A5 JP 2014524476 A5 JP2014524476 A5 JP 2014524476A5 JP 2014527287 A JP2014527287 A JP 2014527287A JP 2014527287 A JP2014527287 A JP 2014527287A JP 2014524476 A5 JP2014524476 A5 JP 2014524476A5
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- Japan
- Prior art keywords
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- cancer
- Prior art date
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- 239000000126 substance Substances 0.000 claims description 76
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 55
- 238000000034 method Methods 0.000 claims description 15
- 239000000203 mixture Substances 0.000 claims description 14
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 7
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 6
- 238000001757 thermogravimetry curve Methods 0.000 claims description 6
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 4
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 4
- 238000002411 thermogravimetry Methods 0.000 claims description 4
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims description 3
- 239000012453 solvate Substances 0.000 claims description 3
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims description 2
- -1 Compound {(1S, 2S, 4R) -4 - [(6 - {[(1R, 2S) -5- chloro-2-methoxy-2,3-dihydro -1H- inden-1-yl] amino} pyrimidine -4-yl) oxy] -2-hydroxycyclopentyl} methylsulfamate Chemical class 0.000 claims description 2
- 150000001408 amides Chemical class 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims description 2
- 230000004580 weight loss Effects 0.000 claims description 2
- 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 3
- FDIXENDMLKAZSA-FHXVVSRQSA-N CNS(O[C@@H]1[C@H](C[C@H](C1)OC1=NC=NC(=C1)N[C@H]1[C@H](CC2=CC(=CC=C12)Cl)OC)O)(=O)=O Chemical compound CNS(O[C@@H]1[C@H](C[C@H](C1)OC1=NC=NC(=C1)N[C@H]1[C@H](CC2=CC(=CC=C12)Cl)OC)O)(=O)=O FDIXENDMLKAZSA-FHXVVSRQSA-N 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- FDDDEECHVMSUSB-UHFFFAOYSA-N sulfanilamide Chemical compound NC1=CC=C(S(N)(=O)=O)C=C1 FDDDEECHVMSUSB-UHFFFAOYSA-N 0.000 claims 2
- 229940124530 sulfonamide Drugs 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000019838 Blood disease Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 239000012296 anti-solvent Substances 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 150000005829 chemical entities Chemical class 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000018706 hematopoietic system disease Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000002071 myeloproliferative effect Effects 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 150000003138 primary alcohols Chemical class 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 208000016261 weight loss Diseases 0.000 claims 1
- 239000000651 prodrug Substances 0.000 description 6
- 229940002612 prodrug Drugs 0.000 description 6
- 150000001875 compounds Chemical class 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161526830P | 2011-08-24 | 2011-08-24 | |
| US61/526,830 | 2011-08-24 | ||
| PCT/US2012/052007 WO2013028832A2 (en) | 2011-08-24 | 2012-08-23 | Inhibitors of nedd8-activating enzyme |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014524476A JP2014524476A (ja) | 2014-09-22 |
| JP2014524476A5 true JP2014524476A5 (enExample) | 2015-10-08 |
| JP6038150B2 JP6038150B2 (ja) | 2016-12-07 |
Family
ID=47747080
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014527287A Expired - Fee Related JP6038150B2 (ja) | 2011-08-24 | 2012-08-23 | Ｎｅｄｄ８活性化酵素阻害剤 |
Country Status (29)
| Country | Link |
|---|---|
| US (3) | US8809356B2 (enExample) |
| EP (2) | EP3323414A1 (enExample) |
| JP (1) | JP6038150B2 (enExample) |
| KR (1) | KR20140054288A (enExample) |
| CN (1) | CN103889988B (enExample) |
| AR (1) | AR087672A1 (enExample) |
| AU (1) | AU2012298813B2 (enExample) |
| BR (1) | BR112014004239A2 (enExample) |
| CA (1) | CA2846231C (enExample) |
| CL (1) | CL2014000441A1 (enExample) |
| CO (1) | CO6900148A2 (enExample) |
| CR (1) | CR20140128A (enExample) |
| DO (1) | DOP2014000037A (enExample) |
| EA (1) | EA031067B1 (enExample) |
| EC (1) | ECSP14013263A (enExample) |
| GE (1) | GEP201606522B (enExample) |
| HK (1) | HK1199252A1 (enExample) |
| IL (1) | IL231069B (enExample) |
| MA (1) | MA35439B1 (enExample) |
| MX (1) | MX2014002015A (enExample) |
| MY (1) | MY166889A (enExample) |
| PE (1) | PE20141146A1 (enExample) |
| PH (1) | PH12014500419A1 (enExample) |
| SG (2) | SG10201601023UA (enExample) |
| TN (1) | TN2014000080A1 (enExample) |
| TW (1) | TWI577667B (enExample) |
| UA (1) | UA114894C2 (enExample) |
| UY (1) | UY34292A (enExample) |
| WO (1) | WO2013028832A2 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8008307B2 (en) | 2006-08-08 | 2011-08-30 | Millennium Pharmaceuticals, Inc. | Heteroaryl compounds useful as inhibitors of E1 activating enzymes |
| 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 |
| GEP201706687B (en) | 2012-02-17 | 2017-06-26 | Millennium Pharmaceuticals Inc (A Delaware Corporation) | Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme |
| CN104684559A (zh) | 2012-08-03 | 2015-06-03 | 米伦纽姆医药公司 | 针对Uba6的吲哚取代的吡咯并嘧啶基抑制剂 |
| EP2764866A1 (en) | 2013-02-07 | 2014-08-13 | IP Gesellschaft für Management mbH | Inhibitors of nedd8-activating enzyme |
| JP6378759B2 (ja) * | 2013-07-02 | 2018-08-22 | 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． | Ｓｕｍｏ活性化酵素阻害剤として有用なヘテロアリール化合物 |
| 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 |
| EP3901159A1 (en) * | 2014-07-01 | 2021-10-27 | Millennium Pharmaceuticals, Inc. | Heteroaryl compounds useful as inhibitors of sumo activating enzyme |
| WO2017183927A1 (ko) * | 2016-04-20 | 2017-10-26 | 한국화학연구원 | 신규한 헤테로고리 화합물, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
| WO2018213258A1 (en) * | 2017-05-15 | 2018-11-22 | Millennium Pharmaceuticals, Inc. | Treatment of merlin-deficient tumors using nae inhibitors |
| AU2019265134B2 (en) | 2018-05-08 | 2024-02-29 | Nippon Shinyaku Co., Ltd. | Azabenzimidazole compounds and pharmaceutical |
| 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 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5194446A (en) | 1989-06-12 | 1993-03-16 | A. H. Robins Company, Incorporated | Compounds having one or more aminosulfaonyloxy radicals useful as pharmaceuticals |
| AU6500696A (en) | 1995-07-28 | 1997-02-26 | Cubist Pharmaceuticals, Inc. | Aminoacyl adenylate mimics as novel antimicrobial and antiparasitic agents |
| WO2004043955A1 (en) | 2002-11-13 | 2004-05-27 | Rigel Pharmaceuticals, Inc. | Rhodanine derivatives and pharmaceutical compositions containing them |
| EP1680431A1 (en) | 2003-10-17 | 2006-07-19 | Rigel Pharmaceuticals, Inc. | Benzothiazole and thiazole'5,5-b!pyridine compositions and their use as ubiquitin ligase inhibitors |
| EP1758873A1 (en) | 2004-06-22 | 2007-03-07 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
| HRP20120847T1 (hr) | 2005-02-04 | 2012-11-30 | Millennium Pharmaceuticals, Inc. | Inhibitori e1 aktivirajuä†ih enzima |
| CA2639924C (en) | 2006-02-02 | 2017-01-10 | Millennium Pharmaceuticals, Inc. | Purinyl-and pyrrolo[2,3-d]pyrimidinyl cyclopentyl compounds and their use as inhibitors of e1 activating enzymes |
| US8008307B2 (en) * | 2006-08-08 | 2011-08-30 | Millennium Pharmaceuticals, Inc. | Heteroaryl compounds useful as inhibitors of E1 activating enzymes |
| DE602007009998D1 (de) * | 2006-08-08 | 2010-12-02 | Millennium Pharm Inc | Heteroarylverbindungen als hemmer der e1-aktivierenden enzyme |
| SG10201402148SA (en) | 2009-05-14 | 2014-07-30 | 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 |
| 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 |
| CN104245699B (zh) * | 2011-11-03 | 2017-06-27 | 米伦纽姆医药公司 | Nedd8‑活化酶抑制剂和低甲基化剂的投与 |
-
2012
- 2012-08-23 JP JP2014527287A patent/JP6038150B2/ja not_active Expired - Fee Related
- 2012-08-23 CA CA2846231A patent/CA2846231C/en not_active Expired - Fee Related
- 2012-08-23 EP EP17193006.8A patent/EP3323414A1/en not_active Withdrawn
- 2012-08-23 EP EP12825411.7A patent/EP2748168A4/en not_active Withdrawn
- 2012-08-23 UA UAA201402893A patent/UA114894C2/uk unknown
- 2012-08-23 WO PCT/US2012/052007 patent/WO2013028832A2/en not_active Ceased
- 2012-08-23 KR KR1020147007200A patent/KR20140054288A/ko not_active Abandoned
- 2012-08-23 BR BR112014004239A patent/BR112014004239A2/pt not_active Application Discontinuation
- 2012-08-23 AU AU2012298813A patent/AU2012298813B2/en not_active Ceased
- 2012-08-23 MY MYPI2014000482A patent/MY166889A/en unknown
- 2012-08-23 GE GEAP201213424A patent/GEP201606522B/en unknown
- 2012-08-23 SG SG10201601023UA patent/SG10201601023UA/en unknown
- 2012-08-23 PE PE2014000250A patent/PE20141146A1/es active IP Right Grant
- 2012-08-23 SG SG11201400102WA patent/SG11201400102WA/en unknown
- 2012-08-23 MX MX2014002015A patent/MX2014002015A/es unknown
- 2012-08-23 PH PH1/2014/500419A patent/PH12014500419A1/en unknown
- 2012-08-23 HK HK14112794.7A patent/HK1199252A1/xx unknown
- 2012-08-23 US US13/592,389 patent/US8809356B2/en active Active
- 2012-08-23 CN CN201280052013.2A patent/CN103889988B/zh not_active Expired - Fee Related
- 2012-08-23 EA EA201400249A patent/EA031067B1/ru not_active IP Right Cessation
- 2012-08-24 AR ARP120103134A patent/AR087672A1/es unknown
- 2012-08-24 UY UY0001034292A patent/UY34292A/es not_active Application Discontinuation
- 2012-08-24 TW TW101130884A patent/TWI577667B/zh not_active IP Right Cessation
-
2014
- 2014-02-20 IL IL231069A patent/IL231069B/en active IP Right Grant
- 2014-02-21 TN TNP2014000080A patent/TN2014000080A1/en unknown
- 2014-02-24 CL CL2014000441A patent/CL2014000441A1/es unknown
- 2014-02-24 DO DO2014000037A patent/DOP2014000037A/es unknown
- 2014-03-12 CO CO14052377A patent/CO6900148A2/es unknown
- 2014-03-13 MA MA36826A patent/MA35439B1/fr unknown
- 2014-03-17 CR CR20140128A patent/CR20140128A/es unknown
- 2014-03-21 EC ECSP14013263 patent/ECSP14013263A/es unknown
- 2014-07-08 US US14/326,051 patent/US9850214B2/en active Active
-
2017
- 2017-11-09 US US15/808,491 patent/US20180290983A1/en not_active Abandoned
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