JP2011522825A5 - - Google Patents
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- Publication number
- JP2011522825A5 JP2011522825A5 JP2011512613A JP2011512613A JP2011522825A5 JP 2011522825 A5 JP2011522825 A5 JP 2011522825A5 JP 2011512613 A JP2011512613 A JP 2011512613A JP 2011512613 A JP2011512613 A JP 2011512613A JP 2011522825 A5 JP2011522825 A5 JP 2011522825A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- compound
- substituted alkyl
- halogen
- 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
- 150000001875 compounds Chemical class 0.000 claims 29
- 229910052739 hydrogen Inorganic materials 0.000 claims 25
- 125000000547 substituted alkyl group Chemical group 0.000 claims 22
- 206010028980 Neoplasm Diseases 0.000 claims 19
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 229910052736 halogen Inorganic materials 0.000 claims 15
- 150000002367 halogens Chemical class 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 13
- 201000011510 cancer Diseases 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 239000007787 solid Substances 0.000 claims 8
- 229930182480 glucuronide Natural products 0.000 claims 7
- 150000008134 glucuronides Chemical class 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 229940011871 estrogen Drugs 0.000 claims 6
- 239000000262 estrogen Substances 0.000 claims 6
- 125000000468 ketone group Chemical group 0.000 claims 6
- 150000001350 alkyl halides Chemical class 0.000 claims 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 210000004027 cell Anatomy 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 4
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 208000014829 head and neck neoplasm Diseases 0.000 claims 4
- 210000001672 ovary Anatomy 0.000 claims 4
- 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 3
- ACVYVLVWPXVTIT-UHFFFAOYSA-N phosphinic acid Chemical group O[PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-N 0.000 claims 3
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- 210000000601 blood cell Anatomy 0.000 claims 2
- 210000000988 bone and bone Anatomy 0.000 claims 2
- 201000006491 bone marrow cancer Diseases 0.000 claims 2
- 210000004556 brain Anatomy 0.000 claims 2
- 210000000481 breast Anatomy 0.000 claims 2
- 210000001072 colon Anatomy 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 210000004696 endometrium Anatomy 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 210000003238 esophagus Anatomy 0.000 claims 2
- -1 glucoronide Chemical group 0.000 claims 2
- 210000003128 head Anatomy 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 210000003734 kidney Anatomy 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 210000004072 lung Anatomy 0.000 claims 2
- 210000001165 lymph node Anatomy 0.000 claims 2
- 208000026037 malignant tumor of neck Diseases 0.000 claims 2
- 210000003739 neck Anatomy 0.000 claims 2
- 210000005036 nerve Anatomy 0.000 claims 2
- 210000000496 pancreas Anatomy 0.000 claims 2
- 210000002307 prostate Anatomy 0.000 claims 2
- 210000000813 small intestine Anatomy 0.000 claims 2
- 210000000952 spleen Anatomy 0.000 claims 2
- 210000002784 stomach Anatomy 0.000 claims 2
- 210000001550 testis Anatomy 0.000 claims 2
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical group OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 230000005907 cancer growth Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12/132,857 | 2008-06-04 | ||
| US12/132,857 US8168621B2 (en) | 2005-09-30 | 2008-06-04 | 6-substituted estradiol derivatives and methods of use |
| PCT/US2009/046120 WO2009149176A1 (en) | 2008-06-04 | 2009-06-03 | 6-substituted estradiol derivatives and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011522825A JP2011522825A (ja) | 2011-08-04 |
| JP2011522825A5 true JP2011522825A5 (enExample) | 2012-07-19 |
| JP5727370B2 JP5727370B2 (ja) | 2015-06-03 |
Family
ID=41398499
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011512613A Active JP5727370B2 (ja) | 2008-06-04 | 2009-06-03 | ６−置換エストラジオール誘導体および使用方法 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US8168621B2 (enExample) |
| EP (1) | EP2300016B1 (enExample) |
| JP (1) | JP5727370B2 (enExample) |
| KR (1) | KR101769152B1 (enExample) |
| CN (1) | CN102076343B (enExample) |
| AU (1) | AU2009256237B2 (enExample) |
| BR (1) | BRPI0913632A2 (enExample) |
| CA (1) | CA2726364C (enExample) |
| DK (1) | DK2300016T3 (enExample) |
| ES (1) | ES2641779T3 (enExample) |
| MX (1) | MX2010013288A (enExample) |
| NO (1) | NO2300016T3 (enExample) |
| WO (1) | WO2009149176A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1392313E (pt) * | 2001-05-16 | 2007-07-17 | Novartis Ag | Combinação que compreende n - ( 5- [ 4- ( metil-piperazinomrtil ) - benxoilamido ] - 2 -metilfenil ) - 4 -( 3 - piridil ) - 2 - pirimidina-amina e um agente quimioterapêutico |
| US10174070B2 (en) | 2005-09-30 | 2019-01-08 | Endece Llc | 6-substituted estradiol derivatives and methods of use |
| US20090028895A1 (en) * | 2007-07-27 | 2009-01-29 | Smith Walter P | Methods and compositions for reducing facial lines and wrinkles |
| 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 |
| US11624095B2 (en) | 2017-09-27 | 2023-04-11 | Case Western Reserve University | Method of quantifying HIV reservoirs by induced transcription based sequencing |
| 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 (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL122154C (enExample) | 1963-10-18 | |||
| GB8517360D0 (en) | 1985-07-09 | 1985-08-14 | Erba Farmitalia | Substituted androsta-1,4-diene-3,17-diones |
| GB8615092D0 (en) * | 1986-06-20 | 1986-07-23 | Erba Farmitalia | Androst-4-ene-317-diones |
| GB8801697D0 (en) | 1988-01-26 | 1988-02-24 | Erba Farmitalia | Improvements in synthesis of 6-methylene derivatives of androsta-1 4-diene-3 17-dione |
| US4904950A (en) | 1988-11-04 | 1990-02-27 | Medical Data Electronics, Inc. | Telemetry digital subcarrier demodulator |
| US5504074A (en) * | 1993-08-06 | 1996-04-02 | Children's Medical Center Corporation | Estrogenic compounds as anti-angiogenic agents |
| JPH07215992A (ja) | 1993-12-07 | 1995-08-15 | Teikoku Hormone Mfg Co Ltd | ６−又は７−置換アンドロスタ−１，４−ジエン誘導体 |
| DE19633349A1 (de) | 1996-08-19 | 1998-02-26 | Sigma Tau Ind Farmaceuti | Neue 6-Hydroxy- und 6-Oxo-androstan-Derivate, die auf das kardiovaskuläre System wirken und pharmazeutische Zusammensetzungen, die diese enthalten |
| AU764266B2 (en) * | 1998-08-11 | 2003-08-14 | Entremed, Inc | Use of estrogenic and anti-estrogenic compounds as anti-fungal compounds |
| WO2001058919A2 (en) * | 2000-02-11 | 2001-08-16 | Sri International | Synthesis of anti-estrogenic and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one |
| IT1317031B1 (it) | 2000-05-17 | 2003-05-26 | Sigma Tau Ind Farmaceuti | Procedimento migliorato per la preparazione di (e,z)3-(2-amminoetossimmino)-androstano-6, 17-dione e di suoi analoghi. |
| WO2002022645A2 (en) | 2000-09-14 | 2002-03-21 | Accelerated Pharmaceuticals, Inc. | Method of making 7alpha-methyl-11beta-methoxy estradiol and related compounds with estrogenic activity |
| AU2004275693A1 (en) | 2003-05-28 | 2005-04-07 | Entremed, Inc. | Antiangiogenic agents |
| US8088758B2 (en) * | 2003-11-12 | 2012-01-03 | Abbott Products Gmbh | 17β-hydroxysteroid dehydrogenase type I inhibitors |
| ATE548375T1 (de) | 2004-01-16 | 2012-03-15 | Cedarburg Pharmaceuticals Inc | Exemestan und zwischenprodukte davon und verfahren zu dessen herstellung |
| US7419972B2 (en) * | 2004-07-02 | 2008-09-02 | Schering Ag | 2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17β-hydroxy steroid dehydrogenase type 1 |
| US20080119447A1 (en) * | 2005-09-30 | 2008-05-22 | James Yarger | 6-alkoxyalkyl estradiol derivatives and methods of use |
| 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 |
| TWI392682B (zh) | 2006-04-13 | 2013-04-11 | Sigma Tau Ind Farmaceuti | 作為心血管疾病的治療藥物之雄甾烷和雄甾烯的胺基衍生物 |
-
2008
- 2008-06-04 US US12/132,857 patent/US8168621B2/en not_active Expired - Fee Related
-
2009
- 2009-06-03 EP EP09759335.4A patent/EP2300016B1/en not_active Not-in-force
- 2009-06-03 CA CA2726364A patent/CA2726364C/en not_active Expired - Fee Related
- 2009-06-03 WO PCT/US2009/046120 patent/WO2009149176A1/en not_active Ceased
- 2009-06-03 ES ES09759335.4T patent/ES2641779T3/es active Active
- 2009-06-03 JP JP2011512613A patent/JP5727370B2/ja active Active
- 2009-06-03 MX MX2010013288A patent/MX2010013288A/es active IP Right Grant
- 2009-06-03 CN CN200980124997.9A patent/CN102076343B/zh not_active Expired - Fee Related
- 2009-06-03 KR KR1020107029911A patent/KR101769152B1/ko not_active Expired - Fee Related
- 2009-06-03 NO NO09759335A patent/NO2300016T3/no unknown
- 2009-06-03 BR BRPI0913632A patent/BRPI0913632A2/pt not_active Application Discontinuation
- 2009-06-03 AU AU2009256237A patent/AU2009256237B2/en not_active Ceased
- 2009-06-03 DK DK09759335.4T patent/DK2300016T3/en active
-
2012
- 2012-04-30 US US13/459,665 patent/US8629130B2/en not_active Expired - Fee Related
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