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 US8168621B2 (en) | 2005-09-30 | 2008-06-04 | 6-substituted estradiol derivatives and methods of use |
| US12/132,857 | 2008-06-04 | ||
| 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 |
|---|---|---|---|---|
| AU2002342335B2 (en) * | 2001-05-16 | 2006-02-02 | Novartis Ag | Combination comprising N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2pyrimidine-amine and a chemotherapeutic agent |
| 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 |
| 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 |
| 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 |
| CA2339835C (en) * | 1998-08-11 | 2008-12-16 | Entremed, Inc. | Use of estrogenic compounds as anti-fungal agents |
| US6784170B2 (en) * | 2000-02-11 | 2004-08-31 | 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 |
| WO2005030120A2 (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 |
| 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 |
| 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 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 ES ES09759335.4T patent/ES2641779T3/es active Active
- 2009-06-03 MX MX2010013288A patent/MX2010013288A/es active IP Right Grant
- 2009-06-03 WO PCT/US2009/046120 patent/WO2009149176A1/en not_active Ceased
- 2009-06-03 DK DK09759335.4T patent/DK2300016T3/en active
- 2009-06-03 JP JP2011512613A patent/JP5727370B2/ja active Active
- 2009-06-03 BR BRPI0913632A patent/BRPI0913632A2/pt not_active Application Discontinuation
- 2009-06-03 EP EP09759335.4A patent/EP2300016B1/en not_active Not-in-force
- 2009-06-03 AU AU2009256237A patent/AU2009256237B2/en not_active Ceased
- 2009-06-03 CA CA2726364A patent/CA2726364C/en not_active Expired - Fee Related
-
2012
- 2012-04-30 US US13/459,665 patent/US8629130B2/en not_active Expired - Fee Related
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