JP2006521335A5 - - Google Patents
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- Publication number
- JP2006521335A5 JP2006521335A5 JP2006505892A JP2006505892A JP2006521335A5 JP 2006521335 A5 JP2006521335 A5 JP 2006521335A5 JP 2006505892 A JP2006505892 A JP 2006505892A JP 2006505892 A JP2006505892 A JP 2006505892A JP 2006521335 A5 JP2006521335 A5 JP 2006521335A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- compound
- compound according
- hydrocarbyl
- composition
- 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
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- 150000001875 compounds Chemical class 0.000 claims 73
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 27
- 239000000203 mixture Substances 0.000 claims 19
- 108010087999 Steryl-Sulfatase Proteins 0.000 claims 15
- 102100038021 Steryl-sulfatase Human genes 0.000 claims 15
- 230000006907 apoptotic process Effects 0.000 claims 11
- IIACRCGMVDHOTQ-UHFFFAOYSA-N sulfamic acid Chemical group NS(O)(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-N 0.000 claims 11
- 102000005262 Sulfatase Human genes 0.000 claims 9
- 230000000694 effects Effects 0.000 claims 9
- 230000005764 inhibitory process Effects 0.000 claims 9
- 108060007951 sulfatase Proteins 0.000 claims 9
- -1 hydrocarbyl compound Chemical class 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 230000022131 cell cycle Effects 0.000 claims 7
- 230000004190 glucose uptake Effects 0.000 claims 7
- 230000005747 tumor angiogenesis Effects 0.000 claims 7
- 230000004663 cell proliferation Effects 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 6
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical group OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 125000000565 sulfonamide group Chemical group 0.000 claims 5
- 125000001273 sulfonato group Chemical group [O-]S(*)(=O)=O 0.000 claims 5
- 102000029749 Microtubule Human genes 0.000 claims 4
- 108091022875 Microtubule Proteins 0.000 claims 4
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims 4
- 230000015572 biosynthetic process Effects 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 210000004688 microtubule Anatomy 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 102000003390 tumor necrosis factor Human genes 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000002560 nitrile group Chemical group 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 150000003431 steroids Chemical group 0.000 claims 3
- QAOWNCQODCNURD-UHFFFAOYSA-L sulfate group Chemical group S(=O)(=O)([O-])[O-] QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 3
- 102000004127 Cytokines Human genes 0.000 claims 2
- 108090000695 Cytokines Proteins 0.000 claims 2
- DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical compound OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 230000033228 biological regulation Effects 0.000 claims 2
- 230000008512 biological response Effects 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 230000006698 induction Effects 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 239000003607 modifier Substances 0.000 claims 2
- 230000025915 regulation of apoptotic process Effects 0.000 claims 2
- 230000025053 regulation of cell proliferation Effects 0.000 claims 2
- 230000004614 tumor growth Effects 0.000 claims 2
- DNXHEGUUPJUMQT-UHFFFAOYSA-N (+)-estrone Natural products OC1=CC=C2C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 DNXHEGUUPJUMQT-UHFFFAOYSA-N 0.000 claims 1
- 125000006833 (C1-C5) alkylene group Chemical group 0.000 claims 1
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 1
- 101150065749 Churc1 gene Proteins 0.000 claims 1
- 102100038239 Protein Churchill Human genes 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000002411 adverse Effects 0.000 claims 1
- 125000003158 alcohol group Chemical group 0.000 claims 1
- 125000002009 alkene group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 230000002939 deleterious effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004185 ester group Chemical group 0.000 claims 1
- 229960003399 estrone Drugs 0.000 claims 1
- 125000001033 ether group Chemical group 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000006882 induction of apoptosis Effects 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 0 C*(CCC1CC2)CC1C(CC1)C2C2C1C*CCC2 Chemical compound C*(CCC1CC2)CC1C(CC1)C2C2C1C*CCC2 0.000 description 5
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0306717.0 | 2003-03-24 | ||
| GB0306717A GB0306717D0 (en) | 2003-03-24 | 2003-03-24 | Compound |
| GB0315885.4 | 2003-07-07 | ||
| GB0315885A GB0315885D0 (en) | 2003-07-07 | 2003-07-07 | Compound |
| PCT/GB2004/000705 WO2004085459A1 (en) | 2003-03-24 | 2004-02-20 | Oestrogen derivatives as inhibitors of steroid sulphatase |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006521335A JP2006521335A (ja) | 2006-09-21 |
| JP2006521335A5 true JP2006521335A5 (https=) | 2007-03-01 |
| JP4719144B2 JP4719144B2 (ja) | 2011-07-06 |
Family
ID=33099976
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006505892A Expired - Fee Related JP4719144B2 (ja) | 2003-03-24 | 2004-02-20 | ステロイドスルファターゼのインヒビターとしてのエストロゲン誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US7893284B2 (https=) |
| EP (1) | EP1608671B1 (https=) |
| JP (1) | JP4719144B2 (https=) |
| AT (1) | ATE454395T1 (https=) |
| AU (1) | AU2004224053B2 (https=) |
| BR (1) | BRPI0408703A (https=) |
| CA (1) | CA2520142C (https=) |
| DE (1) | DE602004024966D1 (https=) |
| DK (1) | DK1608671T3 (https=) |
| EA (1) | EA011123B1 (https=) |
| ES (1) | ES2339450T3 (https=) |
| MX (1) | MXPA05010339A (https=) |
| PL (1) | PL378577A1 (https=) |
| WO (1) | WO2004085459A1 (https=) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0113920D0 (en) | 2001-06-07 | 2001-08-01 | Sterix Ltd | Composition |
| US8030298B2 (en) | 2005-05-26 | 2011-10-04 | Abbott Products Gmbh | 17β-HSD1 and STS inhibitors |
| US8288367B2 (en) | 2006-11-30 | 2012-10-16 | Solvay Pharmaceuticals Gmbh | Substituted estratriene derivatives as 17BETA HSD inhibitors |
| WO2008090517A2 (en) * | 2007-01-26 | 2008-07-31 | Piramal Life Sciences Limited | Enriched plant extract, compound, and methods for the treatment of proliferative disorders |
| EP2149371A1 (en) | 2008-07-28 | 2010-02-03 | PregLem S.A. | Use of steroid sulfatase inhibitors for the treatment of preterm labor |
| EP2334686B1 (en) | 2008-08-28 | 2019-02-27 | President and Fellows of Harvard College | Cortistatin analogues and syntheses therof |
| WO2010123545A2 (en) * | 2009-04-22 | 2010-10-28 | President And Fellows Of Harvard College | Angiogenesis inhibitors |
| WO2012116290A2 (en) * | 2011-02-25 | 2012-08-30 | Washington University | Neuroactive 17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same |
| CN119192266A (zh) | 2011-10-14 | 2024-12-27 | 萨奇治疗股份有限公司 | 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途 |
| MX365644B (es) | 2012-12-18 | 2019-06-10 | Univ Washington | Esteroides neuroactivos sustituidos con 19-alcoxi-17, profarmacos de los mismos, y metodos de tratamiento usando los mismos. |
| US9512170B2 (en) | 2013-03-01 | 2016-12-06 | Washington University | Neuroactive 13, 17-substituted steroids as modulators for GABA type-A receptors |
| US9365502B2 (en) | 2013-03-11 | 2016-06-14 | Washington University | Neuroactive substituted cyclopenta[b]phenanthrenes as modulators for GABA type-A receptors |
| US9562026B2 (en) | 2013-03-14 | 2017-02-07 | Washington University | Neuroactive substituted cyclopent[a]anthracenes as modulators for GABA type-A receptors |
| WO2014169836A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor neuroactive steroids and methods of use thereof |
| WO2014169831A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor c3,3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof |
| ES2807264T3 (es) | 2013-04-17 | 2021-02-22 | Sage Therapeutics Inc | Esteroides neuroactivos 19-nor para métodos de tratamiento |
| JP6470258B2 (ja) | 2013-04-17 | 2019-02-13 | セージ セラピューティクス， インコーポレイテッド | １９−ノルｃ３，３−ジ置換ｃ２１−ｎ−ピラゾリルステロイドおよびその使用方法 |
| WO2015010054A2 (en) | 2013-07-19 | 2015-01-22 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| ES2848823T3 (es) | 2013-08-23 | 2021-08-12 | Sage Therapeutics Inc | Esteroides neuroactivos, composiciones y usos de los mismos |
| SG11201605178WA (en) | 2013-12-24 | 2016-07-28 | Harvard College | Cortistatin analogues and syntheses and uses thereof |
| WO2015195962A1 (en) | 2014-06-18 | 2015-12-23 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| US10577390B2 (en) | 2014-10-16 | 2020-03-03 | Sage Therapeutics, Inc. | Compositions and methods for treating CNS disorders |
| ME03809B (me) | 2014-10-16 | 2021-04-20 | Sage Therapeutics Inc | KOMPOZICIJE I POSTUPCI ZA LEČENJE POREMEĆAJA CNS-a |
| WO2016082789A1 (en) | 2014-11-27 | 2016-06-02 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| WO2016123056A1 (en) | 2015-01-26 | 2016-08-04 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| EP4155314A1 (en) | 2015-02-20 | 2023-03-29 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| WO2016182932A1 (en) | 2015-05-08 | 2016-11-17 | President And Fellows Of Harvard College | Cortistatin analogues, syntheses, and uses thereof |
| WO2017004411A1 (en) | 2015-07-01 | 2017-01-05 | President And Fellows Of Harvard College | Cortistatin analogues and syntheses and uses thereof |
| AU2017283878A1 (en) * | 2016-06-15 | 2019-01-03 | Sony Corporation | Information processing device, observation system, observation method, and program |
| MA45599A (fr) | 2016-07-11 | 2019-05-15 | Sage Therapeutics Inc | Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation |
| US20190233465A1 (en) | 2016-07-11 | 2019-08-01 | Sage Therapeutics, Inc. | C7, c12, and c16 substituted neuroactive steroids and their methods of use |
| CR20240234A (es) | 2019-05-31 | 2024-07-09 | Sage Therapeutics Inc | ESTEROIDES NEUROACTIVOS Y COMPOSICIONES DE ESTOS (Divisional 2021-629) |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4994439A (en) * | 1989-01-19 | 1991-02-19 | California Biotechnology Inc. | Transmembrane formulations for drug administration |
| DE19723794A1 (de) * | 1997-06-06 | 1998-12-10 | Jenapharm Gmbh | Nichtestrogene Derivate des Estradiols mit antioxidativer Aktivität |
| US6288050B1 (en) * | 1997-07-18 | 2001-09-11 | Duquesne University Of The Holy Ghost | Steroid sulfatase inhibitors and methods for making and using the same |
| GB2331987B (en) * | 1997-12-04 | 2002-11-27 | Imperial College | Polycyclic sulphamate inhibitors of oestrone sulphatase |
| US6046186A (en) * | 1997-12-24 | 2000-04-04 | Sri International | Estrone sulfamate inhibitors of estrone sulfatase, and associated pharmaceutical compositions and methods of use |
| ATE401896T1 (de) * | 1998-06-10 | 2008-08-15 | Sterix Ltd | Pharmazeutische zusammensetzungen mit tumor nekrose faktor und 2-methoxyestron-3-o-sulphamat als estrone sulphatasehemmern |
| AU783910B2 (en) * | 1999-04-30 | 2005-12-22 | Sterix Limited | Use of estrone derivatives as antitumour agents |
| US6953785B2 (en) * | 2000-04-24 | 2005-10-11 | Kyowa Hakko Kogyo Co., Ltd. | Estra-1,3,5(10)-triene derivatives |
| CN100338088C (zh) * | 2000-05-11 | 2007-09-19 | 医学与化学研究所 | 2－取代的孕－1,3,5(10)－三烯和胆－1,3,5(10)－三烯衍生物及其生物活性 |
| GB0020498D0 (en) * | 2000-08-18 | 2000-10-11 | Sterix Ltd | Compound |
| WO2002016395A1 (en) * | 2000-08-18 | 2002-02-28 | The Board Of Trustees Of The University Of Illinois | Prodrugs of betulinic acid derivatives for the treatment of cancer and hiv |
| WO2002062347A1 (en) | 2001-02-05 | 2002-08-15 | Oncology Sciences Corporation | Method and composition of novel compounds for the therapy and targeting of the primary modalities of cancer cell proliferation and homeostasis |
| GB0421106D0 (en) * | 2004-09-22 | 2004-10-27 | Sterix Ltd | Compound |
-
2004
- 2004-02-20 ES ES04713124T patent/ES2339450T3/es not_active Expired - Lifetime
- 2004-02-20 JP JP2006505892A patent/JP4719144B2/ja not_active Expired - Fee Related
- 2004-02-20 BR BRPI0408703-8A patent/BRPI0408703A/pt not_active IP Right Cessation
- 2004-02-20 PL PL378577A patent/PL378577A1/pl not_active Application Discontinuation
- 2004-02-20 MX MXPA05010339A patent/MXPA05010339A/es active IP Right Grant
- 2004-02-20 DK DK04713124.8T patent/DK1608671T3/da active
- 2004-02-20 EA EA200501426A patent/EA011123B1/ru not_active IP Right Cessation
- 2004-02-20 DE DE602004024966T patent/DE602004024966D1/de not_active Expired - Lifetime
- 2004-02-20 AT AT04713124T patent/ATE454395T1/de not_active IP Right Cessation
- 2004-02-20 CA CA2520142A patent/CA2520142C/en not_active Expired - Fee Related
- 2004-02-20 EP EP04713124A patent/EP1608671B1/en not_active Expired - Lifetime
- 2004-02-20 WO PCT/GB2004/000705 patent/WO2004085459A1/en not_active Ceased
- 2004-02-20 AU AU2004224053A patent/AU2004224053B2/en not_active Ceased
-
2005
- 2005-09-23 US US11/233,945 patent/US7893284B2/en not_active Expired - Fee Related
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