RU2001125673A - Способ контроля продуцирования эстрогена - Google Patents
Способ контроля продуцирования эстрогенаInfo
- Publication number
- RU2001125673A RU2001125673A RU2001125673/14A RU2001125673A RU2001125673A RU 2001125673 A RU2001125673 A RU 2001125673A RU 2001125673/14 A RU2001125673/14 A RU 2001125673/14A RU 2001125673 A RU2001125673 A RU 2001125673A RU 2001125673 A RU2001125673 A RU 2001125673A
- Authority
- RU
- Russia
- Prior art keywords
- compound
- group
- sub
- sulfate
- enzyme
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- 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
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/36—Antigestagens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Enzymes And Modification Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Surgical Instruments (AREA)
- Mechanical Treatment Of Semiconductor (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Claims (13)
1. Способ контроля продуцирования эстрогена, заключающийся в введении субъекту соединения, содержащего циклическую систему, включающей сложноэфирную группу сульфаминовой кислоты, при том, что данное соединение является ингибитором фермента, обладающего стероидсульфатазной активностью (ЕС 3.1.6.2) и при том, что данное соединение в условиях замещения сложноэфирной группы сульфаминовой кислоты на сульфатную группу с образованием соответствующего сульфатного соединения и инкубированной со стероидсульфатазным ферментом (ЕС 3.1.6.2) при рН 7,4 и 37°С, обеспечивает его ингибирование со значением Кm менее чем 50 μm.
2. Способ целевого определения метаболического пути эстрогена, включающий введение субъекту соединения циклической системы, содержащего сложноэфирную группу сульфаминовой кислоты, при том, что данное соединение является ингибитором фермента, обладающего стероидсульфатазной активностью (ЕС 3.1.6.2) и при том, что данное соединение в условиях замещения сложноэфирной группы сульфаминовой кислоты на сульфатную группу с образованием соответствующего сульфатного соединения и инкубированной со стероидсульфатазным ферментом (ЕС 3.1.6.2) при рН 7,4 и 37°С, обеспечивает его ингибирование со значением Кm менее чем 50 μm.
3. Способ по п.1 или 2, где соединение, содержащее циклическую систему, включает кольцо и сульфаматную группу формулы
где каждый из R1 и R2 независимо выбран из Н, алкила, алкенила, циклоалкила и арила, или оба вместе представляют собой алкилен, не обязательно содержащий один или более гетероатомов или групп в алкиленовой цепи.
5. Способ по п.4, где группа Полицикл является остатком полициклического спирта.
6. Способ по п.4 или 5, где группа Полицикл является остатком стерола.
7. Способ по п.6, где стеролом является 3-стерол.
8. Способ по п.6 или 7, где стерол выбирают из группы, состоящей из эстрона, дегидроэпиандростеронов, замещенных эстронов и замещенных дегидроэпиандростеронов.
9. Способ по любому из пп.3-8, где R1 и R2 независимо друг от друга выбирают из водорода или С1-С10алкила.
10. Способ по любому из пп.3-9, где R1 и R2 независимо друг от друга выбирают из водорода или С1-С5алкила.
11. Способ по любому из пп.3-10, где R1 и R2 независимо друг от друга выбирают из водорода или метила.
12. Способ по любому из предыдущих пунктов, где соединение выбирают из группы, включающей 3-сульфамат эстрона, 3-N,N-диметилсульфамат эстрона, 3-N-монометилсульфамат эстрона.
13. Способ по любому из пп.3-12, где по меньшей мере один из R1 и R2 представляют собой водород.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB919118478A GB9118478D0 (en) | 1991-08-29 | 1991-08-29 | Steroid sulphatase inhibitors |
GB9118478.8 | 1991-08-29 |
Publications (1)
Publication Number | Publication Date |
---|---|
RU2001125673A true RU2001125673A (ru) | 2003-06-27 |
Family
ID=10700604
Family Applications (4)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2000116237/04A RU2210574C2 (ru) | 1991-08-29 | 1992-08-28 | Очищенные стероидсульфаматные соединения, эстрон-сульфаматы |
RU2001125673/14A RU2001125673A (ru) | 1991-08-29 | 1992-08-28 | Способ контроля продуцирования эстрогена |
RU94019334/14A RU2182152C2 (ru) | 1991-08-29 | 1992-08-28 | Ингибиторы стероид-сульфатазы |
RU2000116238/14A RU2207134C2 (ru) | 1991-08-29 | 1992-08-28 | Ингибиторы стероидсульфатазы |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2000116237/04A RU2210574C2 (ru) | 1991-08-29 | 1992-08-28 | Очищенные стероидсульфаматные соединения, эстрон-сульфаматы |
Family Applications After (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU94019334/14A RU2182152C2 (ru) | 1991-08-29 | 1992-08-28 | Ингибиторы стероид-сульфатазы |
RU2000116238/14A RU2207134C2 (ru) | 1991-08-29 | 1992-08-28 | Ингибиторы стероидсульфатазы |
Country Status (26)
Country | Link |
---|---|
US (3) | US5616574A (ru) |
EP (6) | EP0641355B1 (ru) |
JP (6) | JP3219408B2 (ru) |
KR (4) | KR100258396B1 (ru) |
AT (5) | ATE194843T1 (ru) |
AU (2) | AU689043B2 (ru) |
BR (1) | BR9206434A (ru) |
CA (4) | CA2114630C (ru) |
CY (4) | CY2253B1 (ru) |
CZ (1) | CZ295939B6 (ru) |
DE (5) | DE69233149T2 (ru) |
DK (4) | DK0921130T3 (ru) |
ES (4) | ES2196483T3 (ru) |
FI (5) | FI940903A (ru) |
GB (1) | GB9118478D0 (ru) |
GE (6) | GEP20022766B (ru) |
GR (1) | GR3034579T3 (ru) |
HK (3) | HK1020672A1 (ru) |
HU (1) | HUT66097A (ru) |
LV (1) | LV12618B (ru) |
NO (6) | NO307301B1 (ru) |
RU (4) | RU2210574C2 (ru) |
SG (7) | SG103820A1 (ru) |
SK (4) | SK282188B6 (ru) |
UA (4) | UA41875C2 (ru) |
WO (1) | WO1993005064A1 (ru) |
Families Citing this family (72)
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US6476011B1 (en) | 1991-08-28 | 2002-11-05 | Sterix Limited | Methods for introducing an estrogenic compound |
US6011024A (en) | 1991-08-28 | 2000-01-04 | Imperial College Of Science Technology & Medicine | Steroid sulphatase inhibitors |
GB9604709D0 (en) * | 1996-03-05 | 1996-05-01 | Imperial College | A compound |
US6903084B2 (en) * | 1991-08-28 | 2005-06-07 | Sterix Limited | Steroid sulphatase inhibitors |
GB9625334D0 (en) * | 1996-12-05 | 1997-01-22 | Imperial College | Compound |
GB9118478D0 (en) * | 1991-08-29 | 1991-10-16 | Imperial College | Steroid sulphatase inhibitors |
GB9603325D0 (en) * | 1996-02-16 | 1996-04-17 | Imperial College | A compound |
EP0758230B1 (en) * | 1994-04-05 | 2003-06-11 | Celltech Therapeutics Limited | Use of steroid sulphatase inhibitors |
DE4447714C2 (de) * | 1994-08-09 | 1998-02-05 | Jenapharm Gmbh | Verwendung von Estra-1,3,5(10)-trien-Derivaten zur Hormonsubstitutions-Therapie |
DE4429397C2 (de) * | 1994-08-09 | 2003-11-20 | Jenapharm Gmbh | Estra-1,3,5(10)-trien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen |
GB9422777D0 (en) * | 1994-11-11 | 1995-01-04 | Imperial College | Assay |
US5571933A (en) * | 1994-11-17 | 1996-11-05 | Duquesne University Of The Holy Ghost | Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use |
US5705495A (en) * | 1995-10-19 | 1998-01-06 | Jenapharm Gmbh & Co. Kg. | Sulfamate derivatives of 1,3,5(10)-estratriene derivatives, methods for their production and pharmaceuticals containing these compounds |
US6921776B1 (en) | 1996-02-16 | 2005-07-26 | Sterix Limited | Compound |
US6506792B1 (en) | 1997-03-04 | 2003-01-14 | Sterix Limited | Compounds that inhibit oestrone sulphatase and/or aromatase and methods for making and using |
EP0885211B1 (en) * | 1996-03-05 | 2004-12-29 | Sterix Limited | Compounds with a sulfamate group |
WO1998011124A1 (fr) * | 1996-09-12 | 1998-03-19 | Teikoku Hormone Mfg. Co., Ltd. | Derives d'oestrariene a trisubstitution-d-homo-1,3,5,(10) |
US6642220B1 (en) * | 1996-12-05 | 2003-11-04 | Sterix Limited | Compounds that inhibit oestrone sulphatase; compositions thereof; and methods employing the same |
US20040127473A1 (en) * | 1996-12-05 | 2004-07-01 | Reed Michael John | Compound |
US5763432A (en) * | 1997-01-29 | 1998-06-09 | Sri International | Steriod inhibitors of estrone sulfatase and associated pharmaceutical compositions and methods of use |
DE19712488A1 (de) | 1997-03-25 | 1998-10-01 | Knoell Hans Forschung Ev | Steroidsulfamate, Verfahren zu ihrer Herstellung und Anwendung derselben |
GB9708716D0 (en) * | 1997-04-29 | 1997-06-18 | Imperial College | Chronic heart failure |
US6376687B1 (en) | 1997-07-18 | 2002-04-23 | Duquesne University Of The Holy Ghost | Steroid sulfatase inhibitors and methods for making and using the same |
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 |
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US6046186A (en) * | 1997-12-24 | 2000-04-04 | Sri International | Estrone sulfamate inhibitors of estrone sulfatase, and associated pharmaceutical compositions and methods of use |
GB9807779D0 (en) | 1998-04-09 | 1998-06-10 | Ciba Geigy Ag | Organic compounds |
ES2347027T3 (es) | 1998-05-22 | 2010-10-22 | The Board Of Trustees Of The Leland Stanford Junior University | Moleculas bifuncionales y terapias basadas en las mismas. |
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US6248780B1 (en) | 1998-10-01 | 2001-06-19 | Duquesne University Of The Holy Ghost | Compounds for the treatment of estrogen-dependent illnesses and methods for making and using the same |
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JP2000309599A (ja) | 1999-04-13 | 2000-11-07 | Kyowa Hakko Kogyo Co Ltd | エストラ−1,3,5(10),16−テトラエン誘導体 |
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DE10307104A1 (de) | 2003-02-19 | 2004-09-23 | Schering Ag | Antitumor wirksame 2-substituierte Estra-1,3,5(10)-trien-3-yl sulfamate |
DE10307103A1 (de) | 2003-02-19 | 2004-09-09 | Schering Ag | Antitumor wirksame 2-substituierte D-Homostra-1,3,5(10)-trien-3-yl sulfamate |
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WO2004101545A1 (en) * | 2003-05-16 | 2004-11-25 | Laboratoire Theramex | Sulfamate benzothiophene derivatives as steroid sulfatase inhibitors |
WO2004103971A1 (ja) | 2003-05-21 | 2004-12-02 | Aska Pharmaceutical Co., Ltd. | 環状アミノフェニルスルファメート誘導体 |
US7534780B2 (en) | 2004-05-21 | 2009-05-19 | Bayer Schering Pharma Aktiengesellschaft | Estradiol prodrugs |
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US8030298B2 (en) | 2005-05-26 | 2011-10-04 | Abbott Products Gmbh | 17β-HSD1 and STS inhibitors |
GB0511190D0 (en) * | 2005-06-01 | 2005-07-06 | Sterix Ltd | Use |
JP2009508494A (ja) | 2005-09-16 | 2009-03-05 | ラプトール ファーマシューティカル インコーポレイテッド | Crを含むタンパク質に対して特異的な受容体−結合タンパク質(rap)変異体を含む組成物およびその使用 |
GB0624105D0 (en) * | 2006-12-01 | 2007-01-10 | Sterix Ltd | Use |
GB0706072D0 (en) | 2007-03-28 | 2007-05-09 | Sterix Ltd | Compound |
EP2207544A2 (en) | 2007-09-17 | 2010-07-21 | PregLem S.A. | Treatment of oestrogen dependant conditions in pre-menopausal women |
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KR20180114970A (ko) | 2009-05-06 | 2018-10-19 | 라보라토리 스킨 케어, 인크. | 활성제-칼슘 포스페이트 입자 복합체를 포함하는 피부 전달 조성물 및 이들을 이용하는 방법 |
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- 1991-08-29 GB GB919118478A patent/GB9118478D0/en active Pending
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1992
- 1992-08-28 BR BR9206434A patent/BR9206434A/pt not_active Application Discontinuation
- 1992-08-28 US US08/196,192 patent/US5616574A/en not_active Expired - Lifetime
- 1992-08-28 SG SG200003816A patent/SG103820A1/en unknown
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- 1992-08-28 CA CA002305767A patent/CA2305767A1/en not_active Abandoned
- 1992-08-28 UA UA94005380A patent/UA41875C2/ru unknown
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- 1992-08-28 EP EP04077164A patent/EP1522543A1/en not_active Withdrawn
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- 1992-08-28 DK DK98204340T patent/DK0921130T3/da active
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- 1992-08-28 DK DK99203449T patent/DK0982032T3/da active
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- 1992-08-28 DK DK98204337T patent/DK0928609T3/da active
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- 1992-08-28 DK DK92918285T patent/DK0641355T3/da active
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1994
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1995
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1996
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1998
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1999
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2000
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2001
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2002
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2003
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2004
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2005
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