MX2019014677A - 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
- MX2019014677A MX2019014677A MX2019014677A MX2019014677A MX2019014677A MX 2019014677 A MX2019014677 A MX 2019014677A MX 2019014677 A MX2019014677 A MX 2019014677A MX 2019014677 A MX2019014677 A MX 2019014677A MX 2019014677 A MX2019014677 A MX 2019014677A
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- beta
- oximes
- inhibition
- propanamido
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 230000005764 inhibitory process Effects 0.000 title abstract 2
- LGHBWDKMGOIZKH-CBZIJGRNSA-N 3-Deoxyestrone Chemical group C1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 LGHBWDKMGOIZKH-CBZIJGRNSA-N 0.000 title 1
- 108020005199 Dehydrogenases Proteins 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 230000001419 dependent effect Effects 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000003270 steroid hormone Substances 0.000 abstract 2
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 150000001728 carbonyl compounds Chemical class 0.000 abstract 1
- 229960005309 estradiol Drugs 0.000 abstract 1
- 229930182833 estradiol Natural products 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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: en donde R1 3 R4 corresponden a la definición de las reivindicaciones. La invención se relaciona además con su uso como inhibidores de 176-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 Ia enzima 176-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 (2)
| Publication Number | Publication Date |
|---|---|
| MX2019014677A true MX2019014677A (es) | 2022-04-01 |
| MX391234B MX391234B (es) | 2025-03-21 |
Family
ID=62716091
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2019014677A MX391234B (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 After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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. |
Country Status (26)
| Country | Link |
|---|---|
| US (5) | US10717761B2 (es) |
| EP (1) | EP3634975B1 (es) |
| JP (3) | JP7064515B2 (es) |
| KR (1) | KR102420512B1 (es) |
| CN (2) | CN115716860A (es) |
| AU (1) | AU2018279205B2 (es) |
| CA (1) | CA3066196C (es) |
| CL (1) | CL2019003562A1 (es) |
| DK (1) | DK3634975T3 (es) |
| EA (1) | EA201992826A1 (es) |
| ES (1) | ES2988187T3 (es) |
| FI (1) | FI3634975T3 (es) |
| HR (1) | HRP20240679T1 (es) |
| HU (1) | HUE066375T2 (es) |
| IL (2) | IL294140B2 (es) |
| LT (1) | LT3634975T (es) |
| MX (2) | MX391234B (es) |
| NZ (1) | NZ760155A (es) |
| PL (1) | PL3634975T3 (es) |
| PT (1) | PT3634975T (es) |
| RS (1) | RS65529B1 (es) |
| SG (1) | SG11201911776PA (es) |
| SI (1) | SI3634975T1 (es) |
| UA (1) | UA126342C2 (es) |
| WO (1) | WO2018224736A2 (es) |
| ZA (1) | ZA201908404B (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2021006452A (es) * | 2018-12-05 | 2021-09-28 | Forendo Pharma Ltd | Compuestos estra-1,3,5(10)-trieno condensados en posición 16(17) con un anillo de pirazol como inhibidores de 17-hsd1. |
| 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 |
| CN117264008A (zh) * | 2022-06-15 | 2023-12-22 | 中国科学院大连化学物理研究所 | 一种化合物及应用和抑制剂与药物 |
| WO2025185710A1 (zh) * | 2024-03-08 | 2025-09-12 | 长春金赛药业有限责任公司 | 17β-HSD1抑制剂化合物、药物组合物及其应用 |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999046279A2 (en) | 1998-03-11 | 1999-09-16 | Endorecherche, Inc. | INHIBITORS OF TYPE 5 AND TYPE 3 17β-HYDROXYSTEROID DEHYDROGENASE AND METHODS FOR THEIR USE |
| GB9929302D0 (en) | 1999-12-11 | 2000-02-02 | Univ Cardiff | Benzyl tetralins compositions and uses thereof |
| CA2459311C (en) | 2001-09-06 | 2010-08-03 | Schering Corporation | 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases |
| CA2463626C (en) | 2001-10-17 | 2011-05-24 | Schering Corporation | Piperidine- and piperazineacetamines as 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases |
| JP4614770B2 (ja) | 2002-11-18 | 2011-01-19 | 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を処置するための１７β−ヒドロキシステロイドデヒドロゲナーゼタイプ３インヒビター |
| ATE409065T1 (de) | 2002-12-17 | 2008-10-15 | Schering Corp | Inhibitoren der 17 beta- hydroxysteroiddehydrogenase des typs 3 zur behandlung androgenabhängiger krankheiten |
| WO2004085345A2 (en) | 2003-03-21 | 2004-10-07 | 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 |
| US8088758B2 (en) * | 2003-11-12 | 2012-01-03 | Abbott Products Gmbh | 17β-hydroxysteroid dehydrogenase type I inhibitors |
| TWI331154B (en) | 2003-11-12 | 2010-10-01 | Solvay Pharm Gmbh | Novel 17-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 |
| 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 |
| 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 |
| 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 |
| US8030298B2 (en) * | 2005-05-26 | 2011-10-04 | Abbott Products Gmbh | 17β-HSD1 and STS inhibitors |
| JP5268635B2 (ja) | 2005-05-26 | 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 | １７β−ＨＳＤ１及びＳＴＳインヒビター |
| EP2125859B1 (en) | 2006-09-19 | 2013-05-15 | Abbott Products GmbH | Estratriene derivatives and their uses as 17beta-hydroxysteroid dehydrogenase inhibitors |
| EP2099814A1 (en) | 2006-11-30 | 2009-09-16 | Solvay Pharmaceuticals GmbH | Substituted estratrien derivatives as 17beta hsd inhibitors |
| US9284345B2 (en) | 2007-04-12 | 2016-03-15 | Endorecherche, Inc. | 17alpha-substituted steroids as systemic antiandrogens and selective androgen receptor modulators |
| WO2010059943A2 (en) | 2008-11-20 | 2010-05-27 | President And Fellows Of Harvard College | Fluorination of organic compounds |
| EP2688901B1 (en) * | 2011-03-25 | 2019-05-08 | Université Laval | INHIBITORS OF 17ß-HSD1, 17ß-HSD3 AND 17ß-HSD10 |
| AR096729A1 (es) * | 2013-06-25 | 2016-01-27 | Forendo Pharma Ltd | Derivados terapéuticamente activos de estratien-tiazol |
| WO2014207309A1 (en) | 2013-06-25 | 2014-12-31 | Forendo Pharma Ltd | Therapeutically active estratrienthiazole derivatives as inhibitors of 17 b-hydroxysteroid dehydrogenase, type 1 |
| WO2014207311A1 (en) | 2013-06-25 | 2014-12-31 | Forendo Pharma Ltd | Therapeutically active estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxy-steroid dehydrogenase, type 1 |
| EP3237430B1 (en) | 2014-12-23 | 2019-03-20 | Forendo Pharma Ltd | PRODRUGS OF 17ß -HSD1 -INHIBITORS |
| CN107207561B (zh) | 2014-12-23 | 2020-03-31 | 佛恩多制药有限公司 | 17β-HSD1–抑制剂的前药 |
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2018
- 2018-06-07 UA UAA201912052A patent/UA126342C2/uk unknown
- 2018-06-07 RS RS20240572A patent/RS65529B1/sr unknown
- 2018-06-07 EA EA201992826A patent/EA201992826A1/ru unknown
- 2018-06-07 DK DK18733926.2T patent/DK3634975T3/da active
- 2018-06-07 PT PT187339262T patent/PT3634975T/pt unknown
- 2018-06-07 FI FIEP18733926.2T patent/FI3634975T3/fi active
- 2018-06-07 US US16/002,227 patent/US10717761B2/en active Active
- 2018-06-07 WO PCT/FI2018/050427 patent/WO2018224736A2/en not_active Ceased
- 2018-06-07 IL IL294140A patent/IL294140B2/en unknown
- 2018-06-07 CA CA3066196A patent/CA3066196C/en active Active
- 2018-06-07 EP EP18733926.2A patent/EP3634975B1/en active Active
- 2018-06-07 HU HUE18733926A patent/HUE066375T2/hu unknown
- 2018-06-07 CN CN202211366607.2A patent/CN115716860A/zh active Pending
- 2018-06-07 SI SI201831096T patent/SI3634975T1/sl unknown
- 2018-06-07 KR KR1020207000499A patent/KR102420512B1/ko active Active
- 2018-06-07 JP JP2019567580A patent/JP7064515B2/ja active Active
- 2018-06-07 SG SG11201911776PA patent/SG11201911776PA/en unknown
- 2018-06-07 MX MX2019014677A patent/MX391234B/es unknown
- 2018-06-07 NZ NZ760155A patent/NZ760155A/en unknown
- 2018-06-07 MX MX2022000747A patent/MX2022000747A/es unknown
- 2018-06-07 PL PL18733926.2T patent/PL3634975T3/pl unknown
- 2018-06-07 HR HRP20240679TT patent/HRP20240679T1/hr unknown
- 2018-06-07 AU AU2018279205A patent/AU2018279205B2/en active Active
- 2018-06-07 LT LTEPPCT/FI2018/050427T patent/LT3634975T/lt unknown
- 2018-06-07 ES ES18733926T patent/ES2988187T3/es active Active
- 2018-06-07 CN CN201880048486.2A patent/CN110945007B/zh active Active
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2019
- 2019-12-05 CL CL2019003562A patent/CL2019003562A1/es unknown
- 2019-12-05 IL IL271218A patent/IL271218A/en unknown
- 2019-12-17 ZA ZA2019/08404A patent/ZA201908404B/en unknown
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2020
- 2020-06-05 US US16/893,494 patent/US11254703B2/en active Active
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2022
- 2022-01-11 US US17/573,081 patent/US20220127303A1/en not_active Abandoned
- 2022-02-07 JP JP2022017522A patent/JP7401576B2/ja active Active
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2023
- 2023-12-07 JP JP2023207267A patent/JP7664359B2/ja active Active
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2024
- 2024-04-19 US US18/640,607 patent/US20240309043A1/en not_active Abandoned
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2025
- 2025-05-01 US US19/196,058 patent/US20250263431A1/en active Pending
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