MX2022000747A - 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. - Google Patents
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.Info
- Publication number
- MX2022000747A MX2022000747A MX2022000747A MX2022000747A MX2022000747A MX 2022000747 A MX2022000747 A MX 2022000747A MX 2022000747 A MX2022000747 A MX 2022000747A MX 2022000747 A MX2022000747 A MX 2022000747A MX 2022000747 A MX2022000747 A MX 2022000747A
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- beta
- oximes
- inhibition
- propanamido
- Prior art date
Links
Classifications
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- 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
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
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- 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
- 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
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
- C07J41/0016—Oximes
-
- 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
- C07J41/0044—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an estrane or gonane skeleton, including 18-substituted derivatives and derivatives where position 17-beta is substituted by a carbon atom not directly bonded to another carbon atom and not being part of an amide group
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
La invención se relaciona con compuestos de fórmula (I) y sales farmacéuticamente aceptables de los mismos: (ver Fórmula) en donde R1 a R4 corresponden a la definición de las reivindicaciones. La invención se relaciona además con su uso como inhibidores de 17ß-HSD1 y en el tratamiento o la prevención de enfermedades o trastornos dependientes de hormonas esteroideas, como enfermedades o trastornos dependientes de hormonas esteroideas que requieran la inhibición de la enzima 17ß-HSD1 y/o la reducción de la concentración de estradiol endógeno. La presente invención se relaciona además con los compuestos de formula (II) los cuales se definen a partir de los compuestos de carbonilo C-17 que corresponden a las 17-oximas de fórmula (I). La presente invención además se relaciona a la preparación de los compuestos antes mencionados y a las composiciones farmacéuticas que comprenden como ingredientes activos uno o más de los compuestos mencionados de sales farmacéuticamente aceptables del mismo.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FI20175530 | 2017-06-08 | ||
PCT/FI2018/050427 WO2018224736A2 (en) | 2017-06-08 | 2018-06-07 | Therapeutically active steroidal derivatives |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2022000747A true MX2022000747A (es) | 2023-01-24 |
Family
ID=62716091
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2019014677A MX2019014677A (es) | 2017-06-08 | 2018-06-07 | 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. |
MX2022000747A MX2022000747A (es) | 2017-06-08 | 2018-06-07 | 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. |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2019014677A MX2019014677A (es) | 2017-06-08 | 2018-06-07 | 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. |
Country Status (19)
Country | Link |
---|---|
US (3) | US10717761B2 (es) |
EP (1) | EP3634975B1 (es) |
JP (3) | JP7064515B2 (es) |
KR (1) | KR102420512B1 (es) |
CN (2) | CN110945007B (es) |
AU (1) | AU2018279205B2 (es) |
BR (1) | BR112019025782A2 (es) |
CA (1) | CA3066196C (es) |
CL (1) | CL2019003562A1 (es) |
DK (1) | DK3634975T3 (es) |
EA (1) | EA201992826A1 (es) |
FI (1) | FI3634975T3 (es) |
IL (2) | IL294140B1 (es) |
MX (2) | MX2019014677A (es) |
NZ (1) | NZ760155A (es) |
SG (1) | SG11201911776PA (es) |
UA (1) | UA126342C2 (es) |
WO (1) | WO2018224736A2 (es) |
ZA (1) | ZA201908404B (es) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BR112021010598A2 (pt) * | 2018-12-05 | 2021-08-24 | Forendo Pharma Ltd | Compostos, método para preparação de um composto e composição farmacêutica |
CN114644673B (zh) * | 2020-12-19 | 2023-12-26 | 上海喀露蓝科技有限公司 | 一种雌二醇衍生物、其制备方法及其在医药上的用途 |
Family Cites Families (30)
Publication number | Priority date | Publication date | Assignee | Title |
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BR9908592A (pt) | 1998-03-11 | 2001-04-24 | Endorech Inc | Processo para inibir a atividade de 17ß-hidroxiesteróide desidrogenase tipo 5, composição farmacêutica, inibidor de 17ß-hidroxiesteróide desidrogenase tipo 5, processo para inibir 17ß-hidroxiesteróide desidrogenase tipo 3, inibidor de 17ß-hidroxiesteróide desidrogenase tipo 3, processos para tratar, ou reduzir o risco de desenvolver, câncer da próstata, hiperplasia prostática benigna, acne, seborréia, hirsutismo ou alopécia androgênica, sìndrome de ovário policìstico, câncer de mama, endometriose ou leiomioma, para inibir as secreções hormonais testiculares, para tratar puberdade precoce, e, kit |
GB9929302D0 (en) | 1999-12-11 | 2000-02-02 | Univ Cardiff | Benzyl tetralins compositions and uses thereof |
EP1423381B1 (en) | 2001-09-06 | 2007-01-03 | Schering Corporation | 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases |
JP4309761B2 (ja) | 2001-10-17 | 2009-08-05 | シェーリング コーポレイション | アンドロゲン依存性疾患の治療を目的とする17βヒドロキシステロイドデヒドロゲナーゼ3型の阻害剤としてのピペリジンアセトアミンおよびピペラジンアセトアミン |
AR042046A1 (es) | 2002-11-18 | 2005-06-08 | Schering Corp | Inhibidores de 17 beta-hidroxiesteroide deshidrogenasa de tipo 3 para el tratamiento de enfermedades que dependen de androgenos |
MXPA05006485A (es) | 2002-12-17 | 2005-08-26 | Schering Corp | Inhibidores de la 17 beta-hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades dependientes de androgeno. |
US7015211B2 (en) | 2003-03-21 | 2006-03-21 | Yale University | 15α-substituted estradiol carboxylic acid esters as locally active estrogens |
GB0306718D0 (en) | 2003-03-24 | 2003-04-30 | Sterix Ltd | Compound |
US20040224935A1 (en) | 2003-04-07 | 2004-11-11 | Endorecherche, Inc. | Topical antiandrogenic steroids |
US7465739B2 (en) | 2003-06-10 | 2008-12-16 | Solvay Pharmaceuticals B.V. | Compounds and their use in therapy |
US7754709B2 (en) | 2003-06-10 | 2010-07-13 | Solvay Pharmaceuticals Bv | Tetracyclic thiophenepyrimidinone compounds as inhibitors of 17β hydroxysteroid dehydrogenase compounds |
TWI331154B (en) * | 2003-11-12 | 2010-10-01 | Solvay Pharm Gmbh | Novel 17-hydroxysteroid dehydrogenase type i inhibitors |
US8088758B2 (en) * | 2003-11-12 | 2012-01-03 | Abbott Products Gmbh | 17β-hydroxysteroid dehydrogenase type I inhibitors |
US7378426B2 (en) | 2004-03-01 | 2008-05-27 | Bristol-Myers Squibb Company | Fused heterotricyclic compounds as inhibitors of 17β-hydroxysteroid dehydrogenase 3 |
DE102004032674A1 (de) | 2004-07-02 | 2006-01-26 | Schering Ag | Neue 2-substituierte Estra-1,3,5(10)-trien-17-one als Inhibitoren der 17β-Hydroxysteroiddehydrogenase Typ 1 |
DE102004032673A1 (de) | 2004-07-02 | 2006-01-26 | Schering Ag | Neue 2-substituierte D-Homo-estra-1,3,5(10)-triene als Inhibitoren der 17ß-Hydroxysteroiddehydrogenase Typ 1 |
US7575828B2 (en) | 2004-07-23 | 2009-08-18 | Kim Manufacturing Co. | Modular rack assemblies for sealed lead acid batteries |
UA89964C2 (ru) | 2004-09-08 | 2010-03-25 | Н.В. Органон | 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ |
MX2007014736A (es) | 2005-05-26 | 2008-02-15 | Solvay Pharm Gmbh | 17beta-hsd1 e inhibidores sts. |
US8030298B2 (en) * | 2005-05-26 | 2011-10-04 | Abbott Products Gmbh | 17β-HSD1 and STS inhibitors |
RU2469042C2 (ru) | 2006-09-19 | 2012-12-10 | Зольвай Фармасьютиклз Гмбх | Терапевтически активные триазолы и их использование |
RU2453554C2 (ru) | 2006-11-30 | 2012-06-20 | Зольвай Фармасьютиклз Гмбх | Замещенные производные эстратриена как ингибиторы 17бета hsd |
US9284345B2 (en) | 2007-04-12 | 2016-03-15 | Endorecherche, Inc. | 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators |
KR20110095898A (ko) | 2008-11-20 | 2011-08-25 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 유기 화합물의 플루오르화 |
EP2688901B1 (en) * | 2011-03-25 | 2019-05-08 | Université Laval | INHIBITORS OF 17ß-HSD1, 17ß-HSD3 AND 17ß-HSD10 |
CN105518017B (zh) * | 2013-06-25 | 2020-07-14 | 佛恩多制药有限公司 | 治疗活性的作为1型17β-羟基类固醇脱氢酶抑制剂的雌三烯噻唑衍生物 |
WO2014207310A1 (en) * | 2013-06-25 | 2014-12-31 | Forendo Pharma Ltd | Therapeutically active 17-nitrogen substituted estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxysteroid dehydrogenase |
AR096728A1 (es) * | 2013-06-25 | 2016-01-27 | Forendo Pharma Ltd | Derivados de estratrieno-tiazol terapéuticamente activos |
JP6523461B2 (ja) * | 2014-12-23 | 2019-06-05 | フォレンド ファーマ リミテッド | 17β−HSD1−阻害剤のプロドラッグ |
EP3237430B1 (en) | 2014-12-23 | 2019-03-20 | Forendo Pharma Ltd | PRODRUGS OF 17ß -HSD1 -INHIBITORS |
-
2018
- 2018-06-07 JP JP2019567580A patent/JP7064515B2/ja active Active
- 2018-06-07 WO PCT/FI2018/050427 patent/WO2018224736A2/en active Application Filing
- 2018-06-07 FI FIEP18733926.2T patent/FI3634975T3/fi active
- 2018-06-07 NZ NZ760155A patent/NZ760155A/en unknown
- 2018-06-07 UA UAA201912052A patent/UA126342C2/uk unknown
- 2018-06-07 BR BR112019025782-9A patent/BR112019025782A2/pt active IP Right Grant
- 2018-06-07 CA CA3066196A patent/CA3066196C/en active Active
- 2018-06-07 MX MX2019014677A patent/MX2019014677A/es unknown
- 2018-06-07 DK DK18733926.2T patent/DK3634975T3/da active
- 2018-06-07 US US16/002,227 patent/US10717761B2/en active Active
- 2018-06-07 SG SG11201911776PA patent/SG11201911776PA/en unknown
- 2018-06-07 CN CN201880048486.2A patent/CN110945007B/zh active Active
- 2018-06-07 AU AU2018279205A patent/AU2018279205B2/en active Active
- 2018-06-07 EP EP18733926.2A patent/EP3634975B1/en active Active
- 2018-06-07 CN CN202211366607.2A patent/CN115716860A/zh active Pending
- 2018-06-07 IL IL294140A patent/IL294140B1/en unknown
- 2018-06-07 EA EA201992826A patent/EA201992826A1/ru unknown
- 2018-06-07 MX MX2022000747A patent/MX2022000747A/es unknown
- 2018-06-07 KR KR1020207000499A patent/KR102420512B1/ko active IP Right Grant
-
2019
- 2019-12-05 IL IL271218A patent/IL271218A/en unknown
- 2019-12-05 CL CL2019003562A patent/CL2019003562A1/es unknown
- 2019-12-17 ZA ZA2019/08404A patent/ZA201908404B/en unknown
-
2020
- 2020-06-05 US US16/893,494 patent/US11254703B2/en active Active
-
2022
- 2022-01-11 US US17/573,081 patent/US20220127303A1/en not_active Abandoned
- 2022-02-07 JP JP2022017522A patent/JP7401576B2/ja active Active
-
2023
- 2023-12-07 JP JP2023207267A patent/JP2024028916A/ja active Pending
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