JP4719144B2 - 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 - Google Patents
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 Download PDFInfo
- Publication number
- JP4719144B2 JP4719144B2 JP2006505892A JP2006505892A JP4719144B2 JP 4719144 B2 JP4719144 B2 JP 4719144B2 JP 2006505892 A JP2006505892 A JP 2006505892A JP 2006505892 A JP2006505892 A JP 2006505892A JP 4719144 B2 JP4719144 B2 JP 4719144B2
- Authority
- JP
- Japan
- Prior art keywords
- group
- compound
- mmol
- ethyl
- alkyl
- 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.)
- Expired - Fee Related
Links
- 0 C*(CCC1CC2)CC1C(CC1)C2C2C1CICCC2 Chemical compound C*(CCC1CC2)CC1C(CC1)C2C2C1CICCC2 0.000 description 12
- KJZGKEBTVBJPGW-LIGHTNSPSA-N CC(CC1)(C(CC2)C(CCc3c4)C1c3cc(C)c4OCc1ccccc1)[C@H]2OCCOC Chemical compound CC(CC1)(C(CC2)C(CCc3c4)C1c3cc(C)c4OCc1ccccc1)[C@H]2OCCOC KJZGKEBTVBJPGW-LIGHTNSPSA-N 0.000 description 1
- NTAAYXYMXREDHO-YLOYLXSZSA-N CCC1=CC(C(CC2)[C@@H](CC3)C(CC4)[C@@]2(C)[C@H]4C(C)C#N)C3C=C1O Chemical compound CCC1=CC(C(CC2)[C@@H](CC3)C(CC4)[C@@]2(C)[C@H]4C(C)C#N)C3C=C1O NTAAYXYMXREDHO-YLOYLXSZSA-N 0.000 description 1
- ULWPFRRVBLSYOS-CXUHLZMHSA-N CCc(cc(C(CC1)C(CC2)C(CC3)C1(C)/C3=C/CO)c2c1)c1O Chemical compound CCc(cc(C(CC1)C(CC2)C(CC3)C1(C)/C3=C/CO)c2c1)c1O ULWPFRRVBLSYOS-CXUHLZMHSA-N 0.000 description 1
- FFUFRNDKVZDNFW-UHFFFAOYSA-N CCc(cc(C(CC1)C(CC2)C(CC3)C1(C)C3O)c2c1)c1OCOC Chemical compound CCc(cc(C(CC1)C(CC2)C(CC3)C1(C)C3O)c2c1)c1OCOC FFUFRNDKVZDNFW-UHFFFAOYSA-N 0.000 description 1
- LEMLOZUONYRJOT-LRUVZNEXSA-N CCc(cc(C(CC1)C(CC2)C(CC3)[C@@]1(C)C3OCCOC)c2c1)c1OCOC Chemical compound CCc(cc(C(CC1)C(CC2)C(CC3)[C@@]1(C)C3OCCOC)c2c1)c1OCOC LEMLOZUONYRJOT-LRUVZNEXSA-N 0.000 description 1
- BDUXUZGPIVJVQH-CEINQSIVSA-N CCc(cc(C(CC1)C(CC2)C(CC3)[C@@]1(C)[C@H]3NCc1ccccn1)c2c1)c1O Chemical compound CCc(cc(C(CC1)C(CC2)C(CC3)[C@@]1(C)[C@H]3NCc1ccccn1)c2c1)c1O BDUXUZGPIVJVQH-CEINQSIVSA-N 0.000 description 1
- XZCUZVXBIAKJOG-QBWMBKMBSA-N CCc(cc(C(CC1)C(CC2)C(CC3)[C@@]1(C)[C@H]3NCc1ccccn1)c2c1)c1OCOC Chemical compound CCc(cc(C(CC1)C(CC2)C(CC3)[C@@]1(C)[C@H]3NCc1ccccn1)c2c1)c1OCOC XZCUZVXBIAKJOG-QBWMBKMBSA-N 0.000 description 1
- MWXFVZDWSYGMDC-XMAZARRUSA-N CCc(cc(C(CC1)C(CC2)C3[C@@]1(C)[C@@H](CC#N)CC3)c2c1)c1O[Si+](C)(C)C(C)(C)C Chemical compound CCc(cc(C(CC1)C(CC2)C3[C@@]1(C)[C@@H](CC#N)CC3)c2c1)c1O[Si+](C)(C)C(C)(C)C MWXFVZDWSYGMDC-XMAZARRUSA-N 0.000 description 1
- UGMPGVLZEISWCJ-CTYSQQGOSA-N CCc(cc(C(CC1)C(CC2)C3[C@@]1(C)[C@@H](CCOS(N)(=O)=O)CC3)c2c1)c1OS(N)(=O)=O Chemical compound CCc(cc(C(CC1)C(CC2)C3[C@@]1(C)[C@@H](CCOS(N)(=O)=O)CC3)c2c1)c1OS(N)(=O)=O UGMPGVLZEISWCJ-CTYSQQGOSA-N 0.000 description 1
- UVSJIJJDJTZBNV-IFWOZUGISA-N C[C@](CC1)(C(CC2)C(CC3)C1c(cc1OC)c3cc1O)[C@H]2OCCO Chemical compound C[C@](CC1)(C(CC2)C(CC3)C1c(cc1OC)c3cc1O)[C@H]2OCCO UVSJIJJDJTZBNV-IFWOZUGISA-N 0.000 description 1
- DZUMTLFRSVBPNW-VYJKVFMHSA-N C[C@](CC1)(C(CC2)C(CCc3c4)C1c3ccc4O)[C@H]2NCCOC Chemical compound C[C@](CC1)(C(CC2)C(CCc3c4)C1c3ccc4O)[C@H]2NCCOC DZUMTLFRSVBPNW-VYJKVFMHSA-N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Virology (AREA)
- Hospice & Palliative Care (AREA)
- Tropical Medicine & Parasitology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Communicable Diseases (AREA)
- Transplantation (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- AIDS & HIV (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
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 JP2006521335A5 (https=) | 2007-03-01 |
| JP4719144B2 true 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
Also Published As
| Publication number | Publication date |
|---|---|
| JP2006521335A (ja) | 2006-09-21 |
| US7893284B2 (en) | 2011-02-22 |
| US20060094696A1 (en) | 2006-05-04 |
| EP1608671A1 (en) | 2005-12-28 |
| ES2339450T3 (es) | 2010-05-20 |
| DE602004024966D1 (de) | 2010-02-25 |
| EA200501426A1 (ru) | 2006-06-30 |
| DK1608671T3 (da) | 2010-05-10 |
| CA2520142C (en) | 2011-01-04 |
| BRPI0408703A (pt) | 2006-03-07 |
| CA2520142A1 (en) | 2004-10-07 |
| EA011123B1 (ru) | 2008-12-30 |
| AU2004224053A1 (en) | 2004-10-07 |
| HK1082258A1 (en) | 2006-06-02 |
| AU2004224053B2 (en) | 2011-06-09 |
| EP1608671B1 (en) | 2010-01-06 |
| PL378577A1 (pl) | 2006-05-02 |
| MXPA05010339A (es) | 2005-12-14 |
| WO2004085459A1 (en) | 2004-10-07 |
| ATE454395T1 (de) | 2010-01-15 |
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