BRPI0416551A - inibidores da 17beta-hidróxi-esteróide deshidrogenase de tipo i - Google Patents
inibidores da 17beta-hidróxi-esteróide deshidrogenase de tipo iInfo
- Publication number
- BRPI0416551A BRPI0416551A BRPI0416551-9A BRPI0416551A BRPI0416551A BR PI0416551 A BRPI0416551 A BR PI0416551A BR PI0416551 A BRPI0416551 A BR PI0416551A BR PI0416551 A BRPI0416551 A BR PI0416551A
- Authority
- BR
- Brazil
- Prior art keywords
- type
- hydroxy
- steroid dehydrogenase
- steroid
- disorders
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 108010070743 3(or 17)-beta-hydroxysteroid dehydrogenase Proteins 0.000 title abstract 2
- 102100034067 Dehydrogenase/reductase SDR family member 11 Human genes 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 5
- 101710088194 Dehydrogenase Proteins 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 230000001419 dependent effect Effects 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 150000002167 estrones Chemical class 0.000 abstract 2
- 230000002265 prevention Effects 0.000 abstract 2
- 239000003270 steroid hormone Substances 0.000 abstract 2
- 201000009273 Endometriosis Diseases 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 229960005309 estradiol Drugs 0.000 abstract 1
- 102000015694 estrogen receptors Human genes 0.000 abstract 1
- 108010038795 estrogen receptors Proteins 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
"INIBIDORES DA 17BETA-HIDRóXI-ESTERóIDE DESHIDROGENASE DE TIPO I". A presente invenção refere-se a novos derivados de estrona substituída nas posições 3 e 15, os quais representam compostos inibidores da 17<225>-hidróxi-esteróide deshidrogenase de tipo I (17<225>-HSD1), com os seus sais, a preparações farmacêuticas que contêm estes compostos e com processos para a preparação destes compostos. Além disso, a invenção referese ao uso terapêutica dos referidos novos derivados de estrona substituída nas posições 3 e 15, em particular com o seu uso no tratamento ou prevenção de doenças ou distúrbios dependentes de hormónio esteróide, tais como doenças ou distúrbios dependentes de hormónio esteróide que requerem a inibição de enzimas 17<225>-hidróxi-esteróide deshidrogenase de tipo I e/ou que requerem a diminuição da concentração do 17<225>-estradiol endógeno. Além disso, a presente invenção refere-se ao uso geral de inibidores seletivos da 17<225>-hidróxi-esteróide deshidrogenase de tipo 1 os quais possuem, além disso, nenhuma afinidade ou apenas afinidades de ligação antagonistas puras para o receptor de estrogênio para o tratamento e prevenção de distúrbios ginecológicos benignos, em particular endometriose.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03104169 | 2003-11-12 | ||
| EP04105313 | 2004-10-26 | ||
| PCT/EP2004/052925 WO2005047303A2 (en) | 2003-11-12 | 2004-11-11 | NOVEL 17β HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0416551A true BRPI0416551A (pt) | 2007-02-27 |
Family
ID=34593637
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0416551-9A BRPI0416551A (pt) | 2003-11-12 | 2004-11-11 | inibidores da 17beta-hidróxi-esteróide deshidrogenase de tipo i |
Country Status (21)
| Country | Link |
|---|---|
| EP (1) | EP1685150B1 (pt) |
| JP (1) | JP4778438B2 (pt) |
| KR (1) | KR101070025B1 (pt) |
| AR (1) | AR046580A1 (pt) |
| AT (1) | ATE407139T1 (pt) |
| AU (1) | AU2004289459B2 (pt) |
| BR (1) | BRPI0416551A (pt) |
| CA (1) | CA2545704C (pt) |
| DE (1) | DE602004016373D1 (pt) |
| DK (1) | DK1685150T3 (pt) |
| ES (1) | ES2314478T3 (pt) |
| HR (1) | HRP20080603T3 (pt) |
| IL (1) | IL175220A (pt) |
| NO (1) | NO20062679L (pt) |
| PL (1) | PL1685150T3 (pt) |
| PT (1) | PT1685150E (pt) |
| RU (1) | RU2369614C2 (pt) |
| SA (1) | SA04250373B1 (pt) |
| SI (1) | SI1685150T1 (pt) |
| TW (1) | TWI331154B (pt) |
| WO (1) | WO2005047303A2 (pt) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102004025966A1 (de) * | 2004-05-21 | 2005-12-15 | Schering Ag | Estradiol-Prodrugs |
| DE102004025985A1 (de) * | 2004-05-21 | 2005-12-15 | Schering Ag | Estriol- und Estetrol-Prodrugs |
| ES2388297T3 (es) * | 2005-05-26 | 2012-10-11 | Abbott Products Gmbh | Inhibidores de 17-HSD1 y STS |
| US8030298B2 (en) | 2005-05-26 | 2011-10-04 | Abbott Products Gmbh | 17β-HSD1 and STS inhibitors |
| CA2643670A1 (en) * | 2006-02-27 | 2007-08-30 | Sterix Limited | Diaryl compounds as non-steroidal inhibitors of 17-beta hydroxysteroid dehydrogenase and/or steroid sulphatase for the treatment of oestrogen-related diseases such as hormone dependent breast cancer |
| US8080540B2 (en) | 2006-09-19 | 2011-12-20 | Abbott Products Gmbh | Therapeutically active triazoles and their use |
| JP5268917B2 (ja) * | 2006-09-19 | 2013-08-21 | アボット プロダクツ ゲゼルシャフト ミット ベシュレンクテル ハフツング | 治療学的に有効なトリアゾール類及びそれらの使用 |
| US8314119B2 (en) | 2006-11-06 | 2012-11-20 | Abbvie Inc. | Azaadamantane derivatives and methods of use |
| US8288367B2 (en) | 2006-11-30 | 2012-10-16 | Solvay Pharmaceuticals Gmbh | Substituted estratriene derivatives as 17BETA HSD inhibitors |
| CA2671075A1 (en) * | 2006-11-30 | 2008-06-05 | Solvay Pharmaceuticals Gmbh | Substituted estratrien derivatives as 17beta hsd inhibitors |
| DE102007015169A1 (de) | 2007-03-27 | 2008-10-02 | Universität des Saarlandes Campus Saarbrücken | 17Beta-Hydroxysteroid-Dehydrogenase-Typ1-Inhibitoren zur Behandlung hormonabhängiger Erkrankungen |
| DE102007040243A1 (de) | 2007-08-25 | 2009-02-26 | Universität des Saarlandes | 17Beta-Hydroxysteriod-Dehydrogenase Typ1 Inhibitoren zur Behandlung hormonabhängiger Erkrankungen |
| CN103180321A (zh) | 2010-09-23 | 2013-06-26 | Abbvie公司 | 氮杂金刚烷衍生物的一水合物 |
| CA2830984C (en) | 2011-03-25 | 2020-02-11 | Universite Laval | Inhibitors of 17.beta.-hsd1, 17.beta.-hsd3 and 17.beta.-hsd10. |
| BR112015031846A8 (pt) * | 2013-06-25 | 2018-03-06 | Forendo Pharma Ltd | derivados de estratrientiazol, seus usos, e composição farmacêutica |
| JP6456373B2 (ja) | 2013-06-25 | 2019-01-23 | フォレンド ファーマ リミテッド | １７β−ヒドロキシステロイドデヒドロゲナーゼ タイプ１の阻害剤として治療活性のあるエストラトリエンチアゾール誘導体 |
| WO2014207309A1 (en) | 2013-06-25 | 2014-12-31 | Forendo Pharma Ltd | Therapeutically active estratrienthiazole derivatives as inhibitors of 17 b-hydroxysteroid dehydrogenase, type 1 |
| CN107207562B (zh) | 2014-12-23 | 2020-03-06 | 佛恩多制药有限公司 | 17β-HSD1抑制剂的前药 |
| EP3237431B1 (en) | 2014-12-23 | 2019-03-20 | Forendo Pharma Ltd | Prodrugs of 17.beta.-hsd1 -inhibitors |
| CZ307437B6 (cs) | 2016-06-07 | 2018-08-22 | Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. | 15β-substituované deriváty estronu jako selektivní inhibitory 17β-hydroxysteoiddehydrogenáz |
| MX391234B (es) | 2017-06-08 | 2025-03-21 | Forendo Pharma Ltd | Compuestos de estra-1,3,5(10)-trien-17-ona sustituida con 15.beta.-[3-propanamido] y sus 17-oximas para usarse en la inhibicion de 17.beta.-hidroxiesteroides deshidrogenasas. |
| JP7417608B2 (ja) | 2018-12-05 | 2024-01-18 | フォレンド ファーマ リミテッド | １７－ｈｓｄ１阻害剤としての１６（１７）位でピラゾール環と縮合しているエストラ－１，３，５（１０）－トリエン化合物 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9118478D0 (en) * | 1991-08-29 | 1991-10-16 | Imperial College | Steroid sulphatase inhibitors |
| GB0306718D0 (en) * | 2003-03-24 | 2003-04-30 | Sterix Ltd | Compound |
-
2004
- 2004-11-09 TW TW093134102A patent/TWI331154B/zh not_active IP Right Cessation
- 2004-11-11 RU RU2006120488/04A patent/RU2369614C2/ru not_active IP Right Cessation
- 2004-11-11 CA CA2545704A patent/CA2545704C/en not_active Expired - Fee Related
- 2004-11-11 AT AT04804529T patent/ATE407139T1/de active
- 2004-11-11 AR ARP040104159A patent/AR046580A1/es not_active Application Discontinuation
- 2004-11-11 PL PL04804529T patent/PL1685150T3/pl unknown
- 2004-11-11 WO PCT/EP2004/052925 patent/WO2005047303A2/en not_active Ceased
- 2004-11-11 BR BRPI0416551-9A patent/BRPI0416551A/pt not_active IP Right Cessation
- 2004-11-11 ES ES04804529T patent/ES2314478T3/es not_active Expired - Lifetime
- 2004-11-11 EP EP04804529A patent/EP1685150B1/en not_active Expired - Lifetime
- 2004-11-11 SI SI200430862T patent/SI1685150T1/sl unknown
- 2004-11-11 HR HR20080603T patent/HRP20080603T3/xx unknown
- 2004-11-11 AU AU2004289459A patent/AU2004289459B2/en not_active Ceased
- 2004-11-11 PT PT04804529T patent/PT1685150E/pt unknown
- 2004-11-11 JP JP2006538862A patent/JP4778438B2/ja not_active Expired - Fee Related
- 2004-11-11 DE DE602004016373T patent/DE602004016373D1/de not_active Expired - Lifetime
- 2004-11-11 DK DK04804529T patent/DK1685150T3/da active
- 2004-11-20 SA SA4250373A patent/SA04250373B1/ar unknown
-
2006
- 2006-04-26 IL IL175220A patent/IL175220A/en not_active IP Right Cessation
- 2006-06-09 NO NO20062679A patent/NO20062679L/no not_active Application Discontinuation
- 2006-06-09 KR KR1020067011469A patent/KR101070025B1/ko not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JP4778438B2 (ja) | 2011-09-21 |
| DE602004016373D1 (de) | 2008-10-16 |
| HRP20080603T3 (en) | 2009-03-31 |
| KR101070025B1 (ko) | 2011-10-04 |
| SA04250373B1 (ar) | 2009-12-22 |
| CA2545704C (en) | 2012-06-26 |
| RU2369614C2 (ru) | 2009-10-10 |
| AU2004289459A1 (en) | 2005-05-26 |
| CA2545704A1 (en) | 2005-05-26 |
| IL175220A (en) | 2010-12-30 |
| KR20060121171A (ko) | 2006-11-28 |
| JP2007510697A (ja) | 2007-04-26 |
| EP1685150B1 (en) | 2008-09-03 |
| SA04250373A (ar) | 2005-12-03 |
| HK1099309A1 (en) | 2007-08-10 |
| AU2004289459B2 (en) | 2010-08-19 |
| SI1685150T1 (sl) | 2008-12-31 |
| WO2005047303A2 (en) | 2005-05-26 |
| WO2005047303A3 (en) | 2005-08-25 |
| IL175220A0 (en) | 2006-09-05 |
| PL1685150T3 (pl) | 2009-02-27 |
| TW200521133A (en) | 2005-07-01 |
| RU2006120488A (ru) | 2008-01-10 |
| AR046580A1 (es) | 2005-12-14 |
| DK1685150T3 (da) | 2008-12-01 |
| ATE407139T1 (de) | 2008-09-15 |
| NO20062679L (no) | 2006-08-10 |
| ES2314478T3 (es) | 2009-03-16 |
| TWI331154B (en) | 2010-10-01 |
| PT1685150E (pt) | 2008-11-12 |
| EP1685150A2 (en) | 2006-08-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| BRPI0416551A (pt) | inibidores da 17beta-hidróxi-esteróide deshidrogenase de tipo i | |
| Hunzicker-Dunn | Selective activation of rabbit ovarian protein kinase isozymes in rabbit ovarian follicles and corpora lutea. | |
| BRPI0518281A2 (pt) | inibidores de 11-beta hidroxilesteràide desidrogenase do tipo i e mÉtodos uso dos mesmos | |
| Krajka-Kuźniak et al. | Combination of xanthohumol and phenethyl isothiocyanate inhibits NF-κB and activates Nrf2 in pancreatic cancer cells | |
| Mostafa et al. | Rutin hydrate inhibits apoptosis in the brains of cadmium chloride-treated rats via preserving the mitochondrial integrity and inhibiting endoplasmic reticulum stress | |
| UA92348C2 (en) | 17b-HSD1 AND STS INHIBITORS | |
| ATE128362T1 (de) | Kombinationstherapie zur behandlung von estrogenempfindlichen erkrankungen. | |
| Govind et al. | Membrane associated estrogen receptors and related proteins: localization at the plasma membrane and the endoplasmic reticulum | |
| BR0212586A (pt) | Composição, uso de uma combinação de ipratrópio ou um sal deste e de xilometazolina ou um sal desta, e, métodos para o tratamento de uma condição selecionada ao grupo que consiste de sintomas associados com o resfriado comum e sintomas associaods com a rinite e para estabilizar uma solução aquosa de ipratrópio ou um sal deste e xilometazolina ou um sal desta | |
| BR0104831A (pt) | Moduladores de receptor de glucocorticóide | |
| BR0015821A (pt) | Derivados de pirimidina | |
| BR0013009A (pt) | Uso de antagonistas de cgrp e de inibidores de liberação de cgrp para combate a jatos quentes menopáusicos | |
| BRPI0617683A2 (pt) | processo para a contracepção hormonal preventiva segundo a necessidade e uso de um emplastro transdérmico | |
| BRPI0409884A (pt) | compostos, composições farmacêuticas, método para o tratamento ou porfilaxia de doenças, e, usos de compostos e de um ou mais compostos em combinação com outros compostos farmacologicamente ativos | |
| BR0009476A (pt) | Esteróides imunomoduladores, em particular hemidrato de 16 alfa-bromoepiandrosterona | |
| BR0008437A (pt) | Inibidores esteróides de sulfatase e métodos parafabricação e uso dos mesmos | |
| BRPI0409818A (pt) | compostos, composições farmacêuticas, método para o tratamento ou profilaxia de doenças, e, usos de compostos e de um ou mais compostos em combinação com outros compostos farmacologicamente ativos | |
| ZA201908404B (en) | 15.beta.-[3-propanamido]-substituted estra-1,3,5(10)-trien-17-one compounds and their 17-oximes for use in inhibition of 17.beta.-hydroxysteroid dehydrogenases | |
| NO20072704L (no) | Orale faste doseformer som inneholder en lav ostradioldose | |
| Redlak et al. | Prevention of deoxycholate-induced gastric apoptosis by aspirin: roles of NF-κB and PKC signaling | |
| Chen et al. | Effects of estradiol and progestogens on human breast cells: regulation of sex steroid receptors | |
| NO20080441L (no) | Benzofuranonderivater som ikke-steroide progesteronreseptormodulatorer | |
| Chander et al. | The role of steroid sulphatase in regulating the oestrogenicity of oestrogen sulphamates | |
| EPSTEIN JR et al. | Glucocorticoid receptors of mouse epidermis and dermis | |
| Wang et al. | Calcitriol inhibits NaAsO2 triggered hepatic stellate cells activation and extracellular matrix oversecretion by activating Nrf2 signaling pathway through vitamin D receptor |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 12A ANUIDADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2384 DE 13-09-2016 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |