AR096728A1 - Derivados de estratrieno-tiazol terapéuticamente activos - Google Patents
Derivados de estratrieno-tiazol terapéuticamente activosInfo
- Publication number
- AR096728A1 AR096728A1 ARP140102398A ARP140102398A AR096728A1 AR 096728 A1 AR096728 A1 AR 096728A1 AR P140102398 A ARP140102398 A AR P140102398A AR P140102398 A ARP140102398 A AR P140102398A AR 096728 A1 AR096728 A1 AR 096728A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- perhaloalkyl
- independently selected
- halogen
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 230000001419 dependent effect Effects 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 239000003270 steroid hormone Substances 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 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
- 101100451537 Caenorhabditis elegans hsd-1 gene Proteins 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
- 125000001931 aliphatic group Chemical group 0.000 abstract 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 229960005309 estradiol Drugs 0.000 abstract 1
- 229930182833 estradiol Natural products 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000002730 succinyl group Chemical group C(CCC(=O)*)(=O)* 0.000 abstract 1
- 125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0036—Nitrogen-containing hetero ring
- C07J71/0057—Nitrogen and oxygen
- C07J71/0063—Nitrogen and oxygen at position 2(3)
-
- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- 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
- A61P19/00—Drugs for skeletal disorders
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/12—Ophthalmic agents for cataracts
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P5/28—Antiandrogens
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0036—Nitrogen-containing hetero ring
- C07J71/0057—Nitrogen and oxygen
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Ophthalmology & Optometry (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
La presente se refiere a los compuestos de la fórmula (1) y sus sales farmacéuticamente aceptables. La presente se refiere asimismo a su utilización como inhibidores de 17b-HSD1 y en el tratamiento o la prevención de enfermedades o trastornos dependientes de las hormonas esteroides, tales como enfermedades o trastornos dependientes de las hormonas esteroides que requieren la inhibición de la enzima 17b-HSD1 y/o que requieren la disminución de la concentración de estradiol endógeno. La presente también se refiere a la preparación de los compuestos antes mencionados y a composiciones farmacéuticas que comprenden como ingrediente(s) activo(s) uno o más de los compuestos antes mencionados o sales farmacéuticamente aceptables de los mismos. Reivindicación 1: Un compuesto de fórmula (1) en donde (i) R¹ se selecciona del grupo integrado por H, NO₂, OH y N(R)₂; (ii-a) R² y R⁴ se seleccionan cada uno independientemente del grupo integrado por H, halógeno, alquilo-C₁₋₆, haloalquilo-C₁₋₃, perhaloalquilo-C₁₋₃, CN, NO₂, N₃, N(R)₂, (-CH₂)ₙN(R)₂, OR, (CH₂)ₙOR, CO₂R, CONHR, NHCOR, C(=NH)R, C(=N-OH)R y COR; y R³ se selecciona del grupo integrado por H, alquilo-C₁₋₆, haloalquilo-C₁₋₃, perhaloalquilo-C₁₋₆, N(R)₂, N₃ y OR³, en donde R³ se selecciona del grupo integrado por R, bencilo, succinilo, glucuronilo opcionalmente acilado, (CH₂)ₙOH, SO₂OH, SO₂R, tosilo, SO₂N(R)₂, PO(OR)₂, COOR, C(O)N(R)₂, C(O)(CH₂)ₙN(R)₂, C(O)CH₂NHC(O)R, C(O)CH₂NHC(O)OR y C(O)R; o (ii-b) R² y R³ o R³ y R⁴, junto con los átomos de carbono del anillo a los cuales están unidos, forman un anillo heterocíclico insaturado o aromático de 5 miembros que comprende 1 ó 2 heteroátomos, cada uno seleccionado independientemente de N y O, opcionalmente sustituido con metilo u oxo; y R⁴ o R², respectivamente, es H y halógeno; (iii) R⁵ y R⁶ se seleccionan cada uno independientemente del grupo integrado por H, halógeno,-OH, alcoxi-C₁₋₃ y CHO, o R⁵ y R⁶ forman juntos =CH-OH; R es H o alquilo-C₁₋₆, haloalquilo-C₁₋₃, o perhaloalquilo-C₁₋₃, o cuando es parte de algún N(R)₂, ambos R junto con el nitrógeno al cual están unidos pueden formar un anillo heterocíclico alifático o aromático de 5 a 6 miembros que comprende 1 ó 2 heteroátomos, cada uno seleccionado independientemente de N y O; R es alquilo-C₁₋₆, haloalquilo-C₁₋₃ o perhaloalquilo-C₁₋₃; R es alquilo-C₁₋₁₈, alquenilo-C₂₋₁₈, -(CH₂)ₙ-cicloalquilo-C₃₋₆, o fenilo opcionalmente sustituido; y n es 1 ó 2; o con la condición deque cuando R¹, R², R⁴, R⁵ y R⁶ son cada uno H, R³ no es OH o metoxi; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FI20135693 | 2013-06-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR096728A1 true AR096728A1 (es) | 2016-01-27 |
Family
ID=51220583
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140102398A AR096728A1 (es) | 2013-06-25 | 2014-06-25 | Derivados de estratrieno-tiazol terapéuticamente activos |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10377791B2 (es) |
| EP (1) | EP3013845B1 (es) |
| JP (1) | JP6461127B2 (es) |
| CN (1) | CN105518016B (es) |
| AR (1) | AR096728A1 (es) |
| TW (1) | TW201512215A (es) |
| WO (1) | WO2014207309A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9320528B2 (en) * | 2013-06-26 | 2016-04-26 | Misonix, Incorporated | Ultrasonic cutting blade with cooling liquid conduction |
| 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 |
| DK3634975T3 (da) | 2017-06-08 | 2024-05-27 | Organon R&D Finland Ltd | 17-oximer af 15.beta.-[3-propanamido]-substituerede estra-1,3,5(10)-trien-17-oner til anvendelse i inhibition af 17.beta.-hydroxysteroid-dehydrogenaser |
| EP3891167B1 (en) * | 2018-12-05 | 2024-11-13 | Organon R&D Finland Oy | Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1 |
| AR133544A1 (es) * | 2023-08-15 | 2025-10-08 | Univ Laval | INHIBIDORES IRREVERSIBLES DE 17b-HSD1 |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2323089A1 (en) | 1998-03-11 | 1999-09-16 | Endorecherche, Inc. | Inhibitors of type 5 and type 3 17.beta.-hydroxysteroid dehydrogenase and methods for their use |
| DE69935335T2 (de) | 1998-08-07 | 2007-11-22 | Novartis Vaccines and Diagnostics, Inc., Emeryville | Pyrazole als modulatoren des östrogenrezeptors |
| GB9929302D0 (en) | 1999-12-11 | 2000-02-02 | Univ Cardiff | Benzyl tetralins compositions and uses thereof |
| AU2001288386B2 (en) | 2000-11-27 | 2006-11-02 | Entremed, Inc. | 2-substituted estrogens as antiangiogenic agents |
| AR036492A1 (es) | 2001-09-06 | 2004-09-15 | Schering Corp | Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos inhibidores para la elaboracion de un medicamento para el tratamiento de enfermedades androgeno dependientes |
| ES2347643T3 (es) | 2001-10-17 | 2010-11-03 | Schering Corporation | Piperin- y piperazinacetamidas como inhibidores de 17beta hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades dependientes de androgenos. |
| US6750248B2 (en) | 2001-11-09 | 2004-06-15 | National University Of Singapore | Methods for preparing an estrogenic preparation and isolated estrogenic compounds from a plant and uses thereof |
| 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 |
| AU2003293555A1 (en) | 2002-12-17 | 2004-07-29 | Schering Corporation | 17 beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases |
| 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 |
| 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 |
| 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 |
| UA89964C2 (ru) | 2004-09-08 | 2010-03-25 | Н.В. Органон | 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ |
| 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 |
| WO2008034796A2 (en) | 2006-09-19 | 2008-03-27 | Solvay Pharmaceuticals Gmbh | Estratriene derivatives and their uses as 17beta-hydr0xyster0id dehydrogenase inhibitors |
| AU2007327653B2 (en) * | 2006-11-30 | 2013-04-18 | Solvay Pharmaceuticals Gmbh | Substituted estratrien derivatives as 17beta HSD inhibitors |
| US8288367B2 (en) | 2006-11-30 | 2012-10-16 | Solvay Pharmaceuticals Gmbh | Substituted estratriene derivatives as 17BETA HSD inhibitors |
| JP2014508784A (ja) * | 2011-03-25 | 2014-04-10 | ユニヴェルシテ ラヴァル | １７β−ＨＳＤ１、１７β−ＨＳＤ３、および１７β−ＨＳＤ１０の阻害剤 |
-
2014
- 2014-06-25 TW TW103121873A patent/TW201512215A/zh unknown
- 2014-06-25 EP EP14742253.9A patent/EP3013845B1/en active Active
- 2014-06-25 CN CN201480046698.9A patent/CN105518016B/zh active Active
- 2014-06-25 JP JP2016522678A patent/JP6461127B2/ja active Active
- 2014-06-25 WO PCT/FI2014/050517 patent/WO2014207309A1/en not_active Ceased
- 2014-06-25 AR ARP140102398A patent/AR096728A1/es unknown
- 2014-06-25 US US14/392,289 patent/US10377791B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP3013845A1 (en) | 2016-05-04 |
| JP6461127B2 (ja) | 2019-01-30 |
| TW201512215A (zh) | 2015-04-01 |
| US20170114090A1 (en) | 2017-04-27 |
| JP2016523885A (ja) | 2016-08-12 |
| EP3013845B1 (en) | 2020-03-18 |
| US10377791B2 (en) | 2019-08-13 |
| CN105518016B (zh) | 2020-10-23 |
| WO2014207309A1 (en) | 2014-12-31 |
| CN105518016A (zh) | 2016-04-20 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR096729A1 (es) | Derivados terapéuticamente activos de estratien-tiazol | |
| AR096728A1 (es) | Derivados de estratrieno-tiazol terapéuticamente activos | |
| CO2022001357A2 (es) | Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina | |
| AR044116A1 (es) | Compuestos derivados de 5,7 diamino pirazolo [4,3-d] pirimidinas, intermediarios para su preparacion, composiciones farmaceuticas que los contienen y su uso para la fabricacion de medicamentos. | |
| CR20220068A (es) | Derivados de 2-morfolinopiridina sustituidos como inhibidores de la cinasa atr | |
| AR119698A2 (es) | Compuesto amida n-urea sustituida derivado de aminoácido | |
| CL2018000666A1 (es) | Nuevos compuestos de espiro[3h-indol-3,2´-pirrolidin]-2(1h)-ona y derivados como inhibidores de mdm2-p53. | |
| AR038823A1 (es) | Composiciones farmaceuticas para inhibidores de proteasa viral de la hepatitis c | |
| MX385158B (es) | Derivados indol para uso en medicina. | |
| AR069510A1 (es) | Arilo y heteroarilo imidazo[1,5-a]pirazinas fusionadas como inhibidores de la fosfodiesterasa 10 | |
| EA201992082A1 (ru) | Ингибитор поверхностного антигена вируса гепатита b | |
| AR067757A1 (es) | Derivados de imidazo[4,5-c]piridin-2-ona, composiciones farmaceuticas que los contienen, procedimiento para su preparacion y uso de los mismos como agentes antivirales. | |
| AR100442A1 (es) | Derivados de pirido[1,2-a]pirimidin-4-ona para tratar atrofia muscular espinal | |
| AR055105A1 (es) | Inhibidores macrociclicos del virus de la hepatitis c | |
| AR078535A1 (es) | Derivados de pirrolo[2,3-b]piridina ligandos de receptores estrogenicos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de la osteoporosis y enfermedades del sistema nervioso central, entre otras | |
| AR106717A1 (es) | Composiciones para tratar atrofia muscular espinal, kits, métodos de tratamiento, usos | |
| AR092288A1 (es) | Ligandos del receptor ep1 | |
| AR038686A1 (es) | Formulaciones de derivados de androstano y agonistas del adrenoreceptor beta 2 antiinflamatorios | |
| AR096727A1 (es) | Derivados terapéuticamente activos de estratrien-tiazol | |
| AR105893A1 (es) | Derivados del anillo (hetero) aromático sustituidos con carboxi como inhibidores de xantina oxidasa y del transportador 1 del anión urato | |
| AR107927A1 (es) | Compuestos de pirrolidina, sal farmacéuticamente aceptable del mismo, composición farmacéutica que lo comprende y su uso para la fabricación de un medicamento | |
| AR078537A1 (es) | Derivados heterociclicos de indol ligandos del receptor de estrogenos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades asociadas al sistema nervioso central, osteoporosis, canceres y otras patologias | |
| AR094412A1 (es) | Carboxamidas basadas en pirazolilo i | |
| AR091534A1 (es) | Derivados de sulfonamida y metodos de uso de los mismos para mejorar la farmacocinetica de un farmaco | |
| AR107937A1 (es) | Compuestos de cinolin-4-amina y su uso en el tratamiento del cáncer |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |