JP2014508807A5 - - Google Patents
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- Publication number
- JP2014508807A5 JP2014508807A5 JP2014501213A JP2014501213A JP2014508807A5 JP 2014508807 A5 JP2014508807 A5 JP 2014508807A5 JP 2014501213 A JP2014501213 A JP 2014501213A JP 2014501213 A JP2014501213 A JP 2014501213A JP 2014508807 A5 JP2014508807 A5 JP 2014508807A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- cyclopenta
- phenanthrene
- decahydro
- diol
- 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
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 28
- -1 -N (CH 2) n Chemical group 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 12
- 239000003814 drug Substances 0.000 claims 9
- 229940124597 therapeutic agent Drugs 0.000 claims 9
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000001475 halogen functional group Chemical group 0.000 claims 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 6
- 229930182480 glucuronide Natural products 0.000 claims 6
- 150000008134 glucuronides Chemical class 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- GBAGOJGTNKBYMI-OCJHARCKSA-N (6r,8r,9s,10r,13s,14s)-6-(methoxymethyl)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound C([C@@]12C)CC(O)CC1[C@H](COC)C[C@@H]1[C@@H]2CC[C@]2(C)C(O)CC[C@H]21 GBAGOJGTNKBYMI-OCJHARCKSA-N 0.000 claims 4
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 4
- CIUICCYYGROKEM-UHFFFAOYSA-N 2h-phenanthren-3-one Chemical compound C1=CC=C2C3=CC(=O)CC=C3C=CC2=C1 CIUICCYYGROKEM-UHFFFAOYSA-N 0.000 claims 4
- DFCZQECVFFVKDE-UHFFFAOYSA-N 3-phenanthryl hydrogen sulfate Chemical compound C1=CC=C2C3=CC(OS(=O)(=O)O)=CC=C3C=CC2=C1 DFCZQECVFFVKDE-UHFFFAOYSA-N 0.000 claims 4
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 4
- ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical compound [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 208000016192 Demyelinating disease Diseases 0.000 claims 3
- NMPCUPPFFBXPKH-LOPRSAABSA-N (6r,8s,9s,14s,17s)-6-(methoxymethyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6h-cyclopenta[a]phenanthrene-3,17-diol Chemical compound C12=CC=C(O)C=C2[C@H](COC)C[C@@H]2[C@@H]1CCC1[C@@H](O)CC[C@H]12 NMPCUPPFFBXPKH-LOPRSAABSA-N 0.000 claims 2
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims 2
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 201000002491 encephalomyelitis Diseases 0.000 claims 2
- 150000002159 estradiols Chemical class 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000000468 ketone group Chemical group 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 210000002569 neuron Anatomy 0.000 claims 2
- QVLTXCYWHPZMCA-UHFFFAOYSA-N po4-po4 Chemical group OP(O)(O)=O.OP(O)(O)=O QVLTXCYWHPZMCA-UHFFFAOYSA-N 0.000 claims 2
- 206010036807 progressive multifocal leukoencephalopathy Diseases 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 208000011403 Alexander disease Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010003591 Ataxia Diseases 0.000 claims 1
- 208000032116 Autoimmune Experimental Encephalomyelitis Diseases 0.000 claims 1
- 208000022526 Canavan disease Diseases 0.000 claims 1
- 208000010200 Cockayne syndrome Diseases 0.000 claims 1
- 206010010252 Concentric sclerosis Diseases 0.000 claims 1
- 206010012305 Demyelination Diseases 0.000 claims 1
- 208000010055 Globoid Cell Leukodystrophy Diseases 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 208000028226 Krabbe disease Diseases 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 206010069350 Osmotic demyelination syndrome Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 201000004525 Zellweger Syndrome Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 230000001919 adrenal effect Effects 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 230000003376 axonal effect Effects 0.000 claims 1
- 208000009885 central pontine myelinolysis Diseases 0.000 claims 1
- 201000005795 chronic inflammatory demyelinating polyneuritis Diseases 0.000 claims 1
- 230000002708 enhancing effect Effects 0.000 claims 1
- 208000012997 experimental autoimmune encephalomyelitis Diseases 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 208000036546 leukodystrophy Diseases 0.000 claims 1
- 206010065579 multifocal motor neuropathy Diseases 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 208000009174 transverse myelitis Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161454873P | 2011-03-21 | 2011-03-21 | |
| US61/454,873 | 2011-03-21 | ||
| PCT/US2012/029973 WO2012129324A2 (en) | 2011-03-21 | 2012-03-21 | 6-substituted estradiol derivatives for use in remyelination of nerve axons |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014508807A JP2014508807A (ja) | 2014-04-10 |
| JP2014508807A5 true JP2014508807A5 (enExample) | 2015-05-07 |
| JP6174563B2 JP6174563B2 (ja) | 2017-08-02 |
Family
ID=46877849
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014501213A Expired - Fee Related JP6174563B2 (ja) | 2011-03-21 | 2012-03-21 | 神経軸索の再ミエリン化における使用のための６−置換エストラジオール誘導体 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US9364486B2 (enExample) |
| EP (1) | EP2688570B1 (enExample) |
| JP (1) | JP6174563B2 (enExample) |
| KR (1) | KR102080151B1 (enExample) |
| CN (2) | CN103501790B (enExample) |
| AU (1) | AU2012230974B2 (enExample) |
| BR (1) | BR112013024168A2 (enExample) |
| CA (1) | CA2830515C (enExample) |
| DK (1) | DK2688570T3 (enExample) |
| ES (1) | ES2561536T3 (enExample) |
| MX (1) | MX354409B (enExample) |
| SG (1) | SG193380A1 (enExample) |
| WO (1) | WO2012129324A2 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG193380A1 (en) * | 2011-03-21 | 2013-10-30 | Endece Llc | 6-substituted estradiol derivatives for use in remyelination of nerve axons |
| WO2014064712A2 (en) * | 2012-10-22 | 2014-05-01 | Intas Pharmaceuticals Limited | An improved process for the preparation of fulvestrant |
| JP2017512769A (ja) * | 2014-03-19 | 2017-05-25 | エンディース エルエルシーＥｎｄｅｃｅ，Ｌｌｃ | アルツハイマー病の治療のための６−置換エストラジオール誘導体 |
| US20210024568A1 (en) * | 2019-07-23 | 2021-01-28 | Endece Llc | Methods for modulation of lipoprotein lipase and apolipoprotein c2 expression and/or activity in the treatment of peripheral and central nervous system tissue disease states |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4136160A (en) * | 1977-08-17 | 1979-01-23 | Cohen Steven R | Specific assay for active demyelinization |
| JPH0193529A (ja) * | 1987-10-05 | 1989-04-12 | Mect Corp | シアロシルコレステロールの脱髄性疾患治療剤 |
| JPH01193529A (ja) | 1988-01-27 | 1989-08-03 | Yoshitsugu Takano | 液体循環装置 |
| JP5255444B2 (ja) * | 2005-09-30 | 2013-08-07 | エンディース エルエルシー | （ｓ）−６−メチルオキサアルキルエキセメスタン化合物および関連する使用方法 |
| US8168621B2 (en) * | 2005-09-30 | 2012-05-01 | Endece, Llc | 6-substituted estradiol derivatives and methods of use |
| US10174070B2 (en) * | 2005-09-30 | 2019-01-08 | Endece Llc | 6-substituted estradiol derivatives and methods of use |
| JP5290189B2 (ja) * | 2006-11-30 | 2013-09-18 | エンディース エルエルシー | ６−アルコキシアルキルエストラジオール誘導体およびその使用 |
| ES2605960T3 (es) | 2010-09-14 | 2017-03-17 | Endece, Llc | Derivados de desmetil-estradiol 6-sustituido como agonistas del RE-beta |
| SG193380A1 (en) * | 2011-03-21 | 2013-10-30 | Endece Llc | 6-substituted estradiol derivatives for use in remyelination of nerve axons |
-
2012
- 2012-03-21 SG SG2013067962A patent/SG193380A1/en unknown
- 2012-03-21 EP EP12761491.5A patent/EP2688570B1/en not_active Not-in-force
- 2012-03-21 US US13/426,364 patent/US9364486B2/en active Active
- 2012-03-21 KR KR1020137027657A patent/KR102080151B1/ko not_active Expired - Fee Related
- 2012-03-21 MX MX2013010650A patent/MX354409B/es active IP Right Grant
- 2012-03-21 ES ES12761491.5T patent/ES2561536T3/es active Active
- 2012-03-21 JP JP2014501213A patent/JP6174563B2/ja not_active Expired - Fee Related
- 2012-03-21 DK DK12761491.5T patent/DK2688570T3/en active
- 2012-03-21 AU AU2012230974A patent/AU2012230974B2/en not_active Ceased
- 2012-03-21 CA CA2830515A patent/CA2830515C/en not_active Expired - Fee Related
- 2012-03-21 CN CN201280014512.2A patent/CN103501790B/zh not_active Expired - Fee Related
- 2012-03-21 CN CN201610455383.0A patent/CN106420767A/zh active Pending
- 2012-03-21 WO PCT/US2012/029973 patent/WO2012129324A2/en not_active Ceased
- 2012-03-21 BR BR112013024168A patent/BR112013024168A2/pt not_active IP Right Cessation
-
2016
- 2016-06-10 US US15/179,349 patent/US9636348B2/en active Active