EA200501426A1 - Производные эстрогена в качестве ингибиторов стероидной сульфатазы - Google Patents
Производные эстрогена в качестве ингибиторов стероидной сульфатазыInfo
- Publication number
- EA200501426A1 EA200501426A1 EA200501426A EA200501426A EA200501426A1 EA 200501426 A1 EA200501426 A1 EA 200501426A1 EA 200501426 A EA200501426 A EA 200501426A EA 200501426 A EA200501426 A EA 200501426A EA 200501426 A1 EA200501426 A1 EA 200501426A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- group
- steroid
- estrogen
- derivatives
- ryavlyaetsya
- Prior art date
Links
- 229940123142 Steroid sulfatase inhibitor Drugs 0.000 title 1
- 229940011871 estrogen Drugs 0.000 title 1
- 239000000262 estrogen Substances 0.000 title 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 abstract 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 2
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical group OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 abstract 1
- 150000001336 alkenes Chemical class 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002560 nitrile group Chemical group 0.000 abstract 1
- 150000003431 steroids Chemical group 0.000 abstract 1
- IIACRCGMVDHOTQ-UHFFFAOYSA-N sulfamic acid Chemical group NS(O)(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-N 0.000 abstract 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 abstract 1
- 125000000565 sulfonamide group Chemical group 0.000 abstract 1
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
Abstract
Объектом настоящего изобретения является соединение, включающее стероидную циклическую систему и необязательную группу R, выбранную среди гидроксигруппы, сульфаматной группы, фосфонатной группы, тиофосфонатной группы, сульфогруппы или сульфонамидной группы, в котором цикл D, входящий в стероидную циклическую систему, замещен группой Rформулы -L-R, где L является необязательной мостиковой группой, а Rвыбрана среди групп, являющихся нитрильной группой, спиртом, сложным эфиром, простым эфиром, амином и алкеном или включающих одну из перечисленных групп, при том условии, что когда Rявляется спиртом или включает его, L наличествует, и в котором цикл А, принадлежащий к стероидной циклической системе, замещен по положению 2 или 4 группой R, где Rявляется гидрокарбильной группой.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0306717A GB0306717D0 (en) | 2003-03-24 | 2003-03-24 | Compound |
| 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 (2)
| Publication Number | Publication Date |
|---|---|
| EA200501426A1 true EA200501426A1 (ru) | 2006-06-30 |
| EA011123B1 EA011123B1 (ru) | 2008-12-30 |
Family
ID=33099976
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200501426A EA011123B1 (ru) | 2003-03-24 | 2004-02-20 | Производные эстрогена в качестве ингибиторов стероидной сульфатазы |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7893284B2 (ru) |
| EP (1) | EP1608671B1 (ru) |
| JP (1) | JP4719144B2 (ru) |
| AT (1) | ATE454395T1 (ru) |
| AU (1) | AU2004224053B2 (ru) |
| BR (1) | BRPI0408703A (ru) |
| CA (1) | CA2520142C (ru) |
| DE (1) | DE602004024966D1 (ru) |
| DK (1) | DK1608671T3 (ru) |
| EA (1) | EA011123B1 (ru) |
| ES (1) | ES2339450T3 (ru) |
| HK (1) | HK1082258A1 (ru) |
| MX (1) | MXPA05010339A (ru) |
| PL (1) | PL378577A1 (ru) |
| WO (1) | WO2004085459A1 (ru) |
Families Citing this family (31)
| 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 |
| WO2010024930A2 (en) * | 2008-08-28 | 2010-03-04 | President And Fellows Of Harvard College | Cortistatin analogues and syntheses therof |
| JP2012524778A (ja) * | 2009-04-22 | 2012-10-18 | プレジデント アンド フェロウズ オブ ハーバード カレッジ | 血管新生阻害剤 |
| 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 |
| ES2738526T3 (es) | 2011-10-14 | 2020-01-23 | Sage Therapeutics Inc | Compuestos 19-norpregnano 3,3-disustituidos, composiciones y usos de los mismos |
| BR112015014397B1 (pt) | 2012-12-18 | 2021-02-02 | Washington University | composto, composição farmacêutica e uso de um composto |
| 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 |
| CA2909546C (en) | 2013-04-17 | 2019-01-22 | Sage Therapeutics, Inc. | 19-nor neuroactive steroids and methods of use thereof |
| US9725481B2 (en) | 2013-04-17 | 2017-08-08 | Sage Therapeutics, Inc. | 19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof |
| EP3498725B1 (en) | 2013-04-17 | 2021-06-09 | Sage Therapeutics, Inc. | 19-nor c3,3-disubstituted c21-n-pyrazolyl steroid for use in therapy |
| CN105555277B (zh) | 2013-07-19 | 2022-01-11 | 萨奇治疗股份有限公司 | 神经活性类固醇化合物、组合物及其用途 |
| AU2014308621C1 (en) | 2013-08-23 | 2022-01-06 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| EA201891279A1 (ru) | 2013-12-24 | 2019-01-31 | Президент Энд Феллоус Оф Гарвард Колледж | Аналоги кортистатина, их синтез и применения |
| US10246482B2 (en) | 2014-06-18 | 2019-04-02 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| CN117024502A (zh) | 2014-10-16 | 2023-11-10 | 萨奇治疗股份有限公司 | 靶向cns障碍的组合物和方法 |
| ES2808855T3 (es) | 2014-10-16 | 2021-03-02 | Sage Therapeutics Inc | Composiciones y métodos para tratar trastornos del SNC |
| SI3224269T1 (sl) | 2014-11-27 | 2020-10-30 | Sage Therapeutics, Inc. | Sestavki in metode za zdravljenje CNS motenj |
| PL3250210T3 (pl) | 2015-01-26 | 2021-07-26 | Sage Therapeutics, Inc. | Kompozycje i sposoby leczenia zaburzeń OUN |
| JP6875996B2 (ja) | 2015-02-20 | 2021-05-26 | セージ セラピューティクス， インコーポレイテッド | 神経刺激性ステロイド、組成物、およびその使用 |
| EP3294298A4 (en) | 2015-05-08 | 2018-10-17 | President and Fellows of Harvard College | Cortistatin analogues, syntheses, and uses thereof |
| EP3316889A4 (en) | 2015-07-01 | 2018-11-14 | President and Fellows of Harvard College | Cortistatin analogues and syntheses and uses thereof |
| EP3473998A4 (en) * | 2016-06-15 | 2019-07-03 | Sony Corporation | INFORMATION PROCESSING DEVICE, OBSERVATION SYSTEM, OBSERVATION PROCEDURE AND PROGRAM |
| JP7049313B2 (ja) | 2016-07-11 | 2022-04-06 | セージ セラピューティクス， インコーポレイテッド | Ｃ１７、ｃ２０、およびｃ２１置換神経刺激性ステロイドおよびそれらの使用方法 |
| JOP20210293A1 (ar) | 2019-05-31 | 2023-01-30 | Sage Therapeutics Inc | ستيرويدات ذات فعالية عصبية وتركيبات منها |
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 |
| AU765386B2 (en) * | 1998-06-10 | 2003-09-18 | Sterix Limited | Pharmaceutical composition with tumor necrosis factor a and 2-methoxyestrone-3-(o)-sulphamate for inhibition of estrone sulphatase |
| WO2000066095A2 (en) * | 1999-04-30 | 2000-11-09 | Sterix Limited | Use of estrone derivatives as antitumour agents |
| EP1284272A4 (en) * | 2000-04-24 | 2003-09-10 | Kyowa Hakko Kogyo Kk | Estra-1,3,5 (10) -triene |
| JP2003532737A (ja) * | 2000-05-11 | 2003-11-05 | リサーチ・インスティテュート・フォア・メディスン・アンド・ケミストリー・インコーポレイテッド | ２位置換プレグナ−１，３，５（１０）−トリエン誘導体およびコラン−１，３，５（１０）−トリエン誘導体およびそれらの生物活性 |
| GB0020498D0 (en) * | 2000-08-18 | 2000-10-11 | Sterix Ltd | Compound |
| CA2418479C (en) * | 2000-08-18 | 2007-12-18 | The Board Of Trustees Of The University Of Illinois | Prodrugs of betulinic acid derivatives for the treatment of cancer |
| 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 BR BRPI0408703-8A patent/BRPI0408703A/pt not_active IP Right Cessation
- 2004-02-20 AT AT04713124T patent/ATE454395T1/de not_active IP Right Cessation
- 2004-02-20 EA EA200501426A patent/EA011123B1/ru not_active IP Right Cessation
- 2004-02-20 CA CA2520142A patent/CA2520142C/en not_active Expired - Fee Related
- 2004-02-20 PL PL378577A patent/PL378577A1/pl not_active Application Discontinuation
- 2004-02-20 JP JP2006505892A patent/JP4719144B2/ja not_active Expired - Fee Related
- 2004-02-20 DK DK04713124.8T patent/DK1608671T3/da active
- 2004-02-20 AU AU2004224053A patent/AU2004224053B2/en not_active Ceased
- 2004-02-20 MX MXPA05010339A patent/MXPA05010339A/es active IP Right Grant
- 2004-02-20 ES ES04713124T patent/ES2339450T3/es not_active Expired - Lifetime
- 2004-02-20 WO PCT/GB2004/000705 patent/WO2004085459A1/en active Application Filing
- 2004-02-20 DE DE602004024966T patent/DE602004024966D1/de not_active Expired - Lifetime
- 2004-02-20 EP EP04713124A patent/EP1608671B1/en not_active Expired - Lifetime
-
2005
- 2005-09-23 US US11/233,945 patent/US7893284B2/en not_active Expired - Fee Related
-
2006
- 2006-03-29 HK HK06103924.9A patent/HK1082258A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| ATE454395T1 (de) | 2010-01-15 |
| JP4719144B2 (ja) | 2011-07-06 |
| US20060094696A1 (en) | 2006-05-04 |
| EP1608671B1 (en) | 2010-01-06 |
| DK1608671T3 (da) | 2010-05-10 |
| JP2006521335A (ja) | 2006-09-21 |
| PL378577A1 (pl) | 2006-05-02 |
| ES2339450T3 (es) | 2010-05-20 |
| AU2004224053A1 (en) | 2004-10-07 |
| EP1608671A1 (en) | 2005-12-28 |
| US7893284B2 (en) | 2011-02-22 |
| AU2004224053B2 (en) | 2011-06-09 |
| CA2520142C (en) | 2011-01-04 |
| EA011123B1 (ru) | 2008-12-30 |
| DE602004024966D1 (de) | 2010-02-25 |
| BRPI0408703A (pt) | 2006-03-07 |
| CA2520142A1 (en) | 2004-10-07 |
| WO2004085459A1 (en) | 2004-10-07 |
| MXPA05010339A (es) | 2005-12-14 |
| HK1082258A1 (en) | 2006-06-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM |
|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |