JP2017512769A5 - - Google Patents
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- Publication number
- JP2017512769A5 JP2017512769A5 JP2016556841A JP2016556841A JP2017512769A5 JP 2017512769 A5 JP2017512769 A5 JP 2017512769A5 JP 2016556841 A JP2016556841 A JP 2016556841A JP 2016556841 A JP2016556841 A JP 2016556841A JP 2017512769 A5 JP2017512769 A5 JP 2017512769A5
- 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.)
- Pending
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 21
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 11
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 8
- 125000001475 halogen functional group Chemical group 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 208000024827 Alzheimer disease Diseases 0.000 claims 5
- 108010024284 Apolipoprotein C-II Proteins 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 230000005714 functional activity Effects 0.000 claims 5
- 229940124597 therapeutic agent Drugs 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
- 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
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 3
- 230000000069 prophylactic effect Effects 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
- 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 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 229930182480 glucuronide Natural products 0.000 claims 2
- 150000008134 glucuronides Chemical class 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 125000000468 ketone group Chemical group 0.000 claims 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 2
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 2
- ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical group [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 claims 2
- 230000003449 preventive effect Effects 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 150000002159 estradiols Chemical class 0.000 claims 1
- 230000003827 upregulation Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461955578P | 2014-03-19 | 2014-03-19 | |
| US61/955,578 | 2014-03-19 | ||
| PCT/US2015/021538 WO2015143201A2 (en) | 2014-03-19 | 2015-03-19 | 6-substituted estradiol derivatives for the treatment of alzheimer's disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017512769A JP2017512769A (ja) | 2017-05-25 |
| JP2017512769A5 true JP2017512769A5 (https=) | 2018-04-26 |
Family
ID=54141046
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016556841A Pending JP2017512769A (ja) | 2014-03-19 | 2015-03-19 | 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 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20150265630A1 (https=) |
| EP (1) | EP3119402A4 (https=) |
| JP (1) | JP2017512769A (https=) |
| KR (1) | KR20160136363A (https=) |
| CN (1) | CN106255501A (https=) |
| AU (2) | AU2015231172A1 (https=) |
| BR (1) | BR112016021408A2 (https=) |
| CA (1) | CA2940536A1 (https=) |
| MX (1) | MX2016012045A (https=) |
| SG (1) | SG11201607693WA (https=) |
| WO (1) | WO2015143201A2 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020247407A1 (en) * | 2019-06-03 | 2020-12-10 | Aihol Corporation | Hyaluronan conjugates and uses thereof |
| 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 (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10174070B2 (en) * | 2005-09-30 | 2019-01-08 | Endece Llc | 6-substituted estradiol derivatives and methods of use |
| US20080200441A1 (en) * | 2007-02-14 | 2008-08-21 | University Of Southern California | Estrogen receptor modulators associated pharmaceutical compositions and methods of use |
| 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 |
-
2015
- 2015-03-19 SG SG11201607693WA patent/SG11201607693WA/en unknown
- 2015-03-19 EP EP15765290.0A patent/EP3119402A4/en not_active Withdrawn
- 2015-03-19 MX MX2016012045A patent/MX2016012045A/es unknown
- 2015-03-19 AU AU2015231172A patent/AU2015231172A1/en not_active Abandoned
- 2015-03-19 JP JP2016556841A patent/JP2017512769A/ja active Pending
- 2015-03-19 KR KR1020167028986A patent/KR20160136363A/ko not_active Withdrawn
- 2015-03-19 BR BR112016021408A patent/BR112016021408A2/pt not_active IP Right Cessation
- 2015-03-19 CA CA2940536A patent/CA2940536A1/en not_active Abandoned
- 2015-03-19 CN CN201580014623.7A patent/CN106255501A/zh active Pending
- 2015-03-19 WO PCT/US2015/021538 patent/WO2015143201A2/en not_active Ceased
- 2015-03-19 US US14/663,043 patent/US20150265630A1/en not_active Abandoned
-
2018
- 2018-02-12 AU AU2018201003A patent/AU2018201003A1/en not_active Abandoned
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