JP2014508807A5 - - Google Patents
Download PDFInfo
- 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) | CN106420767A (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 |
|---|---|---|---|---|
| CN106420767A (zh) * | 2011-03-21 | 2017-02-22 | 安德斯有限责任公司 | 用于神经轴突的髓鞘再生的6‑取代的雌二醇衍生物 |
| EP2909224B1 (en) * | 2012-10-22 | 2020-03-18 | Intas Pharmaceuticals Limited | An improved process for the preparation of fulvestrant |
| WO2015143201A2 (en) * | 2014-03-19 | 2015-09-24 | Endece Llc | 6-substituted estradiol derivatives for the treatment of alzheimer's disease |
| 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 |
| 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 |
| CN101312743A (zh) * | 2005-09-30 | 2008-11-26 | 安德西有限公司 | (s)-6-甲基氧杂烷基依西美坦化合物及相关使用方法 |
| 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 |
| MX343059B (es) | 2010-09-14 | 2016-10-24 | Endece Llc | Derivados de desmetil-estradiol sustituido en 6 como agonistas de er-beta selectivos. |
| CN106420767A (zh) * | 2011-03-21 | 2017-02-22 | 安德斯有限责任公司 | 用于神经轴突的髓鞘再生的6‑取代的雌二醇衍生物 |
-
2012
- 2012-03-21 CN CN201610455383.0A patent/CN106420767A/zh active Pending
- 2012-03-21 DK DK12761491.5T patent/DK2688570T3/en active
- 2012-03-21 SG SG2013067962A patent/SG193380A1/en unknown
- 2012-03-21 MX MX2013010650A patent/MX354409B/es active IP Right Grant
- 2012-03-21 WO PCT/US2012/029973 patent/WO2012129324A2/en not_active Ceased
- 2012-03-21 EP EP12761491.5A patent/EP2688570B1/en not_active Not-in-force
- 2012-03-21 BR BR112013024168A patent/BR112013024168A2/pt not_active IP Right Cessation
- 2012-03-21 JP JP2014501213A patent/JP6174563B2/ja not_active Expired - Fee Related
- 2012-03-21 CA CA2830515A patent/CA2830515C/en not_active Expired - Fee Related
- 2012-03-21 KR KR1020137027657A patent/KR102080151B1/ko not_active Expired - Fee Related
- 2012-03-21 ES ES12761491.5T patent/ES2561536T3/es active Active
- 2012-03-21 CN CN201280014512.2A patent/CN103501790B/zh not_active Expired - Fee Related
- 2012-03-21 AU AU2012230974A patent/AU2012230974B2/en not_active Ceased
- 2012-03-21 US US13/426,364 patent/US9364486B2/en active Active
-
2016
- 2016-06-10 US US15/179,349 patent/US9636348B2/en active Active