PE20151754A1 - Estra-1,3,5(10),16-tetraeno-3-carboxamidas para la inhibicion de la 17b-hidroxiesteroide deshidrogenasa (akr1 c3) - Google Patents
Estra-1,3,5(10),16-tetraeno-3-carboxamidas para la inhibicion de la 17b-hidroxiesteroide deshidrogenasa (akr1 c3)Info
- Publication number
- PE20151754A1 PE20151754A1 PE2015001794A PE2015001794A PE20151754A1 PE 20151754 A1 PE20151754 A1 PE 20151754A1 PE 2015001794 A PE2015001794 A PE 2015001794A PE 2015001794 A PE2015001794 A PE 2015001794A PE 20151754 A1 PE20151754 A1 PE 20151754A1
- Authority
- PE
- Peru
- Prior art keywords
- akr1
- estra
- tetraene
- carboxamides
- inhibition
- Prior art date
Links
- 101150005096 AKR1 gene Proteins 0.000 title 1
- 101710088194 Dehydrogenase Proteins 0.000 title 1
- 101100215778 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) ptr-1 gene Proteins 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 238000011321 prophylaxis Methods 0.000 abstract 2
- 238000011282 treatment Methods 0.000 abstract 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 abstract 1
- -1 5-methoxypyridin-3-yl Chemical group 0.000 abstract 1
- 102000004602 Aldo-Keto Reductase Family 1 Member C3 Human genes 0.000 abstract 1
- 201000009273 Endometriosis Diseases 0.000 abstract 1
- 108010065942 Prostaglandin-F synthase Proteins 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 229910052736 halogen Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 208000031169 hemorrhagic disease Diseases 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 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
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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- 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
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
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Abstract
Referida a inhibidores de AKR1C3 de formula (I) y procesos para su preparacion, uso de los mismos para el tratamiento y/o profilaxis de enfermedades y uso de los mismos para la produccion de medicamentos para el tratamiento y/o profilaxis de enfermedades, en especial de trastornos de sangrado y endometriosis, donde: X es carbono, etc; Y es carbono, etc; R3 es hidrogeno o halogeno; R4 es hidrogeno, alquilo C1-C6, etc; R5 es hidrogeno, alquilo C1-C6, etc. Compuestos preferidos: 17-(piridin-3-il)oestra-1,3,5(10), 16-tetraen-3-carboxamida; 17-(5-metoxipiridin-3-il)oestra-1,3,5(10), 16-tetraen-3-carboxamida
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13156125 | 2013-02-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20151754A1 true PE20151754A1 (es) | 2015-12-20 |
Family
ID=47748503
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2015001794A PE20151754A1 (es) | 2013-02-21 | 2014-02-18 | Estra-1,3,5(10),16-tetraeno-3-carboxamidas para la inhibicion de la 17b-hidroxiesteroide deshidrogenasa (akr1 c3) |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US9714266B2 (es) |
| EP (1) | EP2958928B1 (es) |
| JP (1) | JP6254195B2 (es) |
| KR (1) | KR20150118153A (es) |
| CN (1) | CN105008382B (es) |
| AP (1) | AP3826A (es) |
| AR (1) | AR094852A1 (es) |
| AU (1) | AU2014220800A1 (es) |
| BR (1) | BR112015018071A2 (es) |
| CA (1) | CA2901632C (es) |
| CL (1) | CL2015002346A1 (es) |
| CR (1) | CR20150432A (es) |
| CU (1) | CU20150091A7 (es) |
| EA (1) | EA201500851A1 (es) |
| ES (1) | ES2678993T3 (es) |
| GT (1) | GT201500235A (es) |
| HK (1) | HK1211592A1 (es) |
| IL (1) | IL240191A0 (es) |
| MA (1) | MA38349A1 (es) |
| MX (1) | MX2015010876A (es) |
| NI (1) | NI201500115A (es) |
| PE (1) | PE20151754A1 (es) |
| PH (1) | PH12015501819A1 (es) |
| SG (1) | SG11201505875WA (es) |
| TN (1) | TN2015000362A1 (es) |
| TW (1) | TWI523862B (es) |
| UY (1) | UY35344A (es) |
| WO (1) | WO2014128108A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6407415B2 (ja) * | 2014-09-11 | 2018-10-17 | バイエル・ファルマ・アクティエンゲゼルシャフト | ３−窒素または硫黄置換エストラ−１，３，５（１０），１６−テトラエンａｋｒ１ｃ３阻害剤 |
| EP3401677A4 (en) * | 2016-01-05 | 2019-06-12 | Hamamatsu Photonics K.K. | LIVING BODY OBSERVATION PROCEDURE LIVING BODY OBSERVATION DEVICE |
| US10167293B2 (en) | 2016-05-26 | 2019-01-01 | Bayer Pharma Aktiengesellschaft | [8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanones |
| 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 |
| EP3269373A1 (en) | 2016-07-11 | 2018-01-17 | Bayer Pharma Aktiengesellschaft | Low-dosed oral dosage form of an akr1c3 inhibitor for treatment of diseases |
| TW201825478A (zh) | 2016-12-19 | 2018-07-16 | 德商拜耳製藥公司 | ［４－（苯基磺醯基）哌嗪－１－-基］（１ｈ－１，２，３－三唑－４-基）甲酮 |
| WO2018114672A1 (en) | 2016-12-19 | 2018-06-28 | Bayer Pharma Aktiengesellschaft | [4-(phenylsulfonyl)piperazin-1-yl](1h-1,2,3-triazol-4-yl)methanones |
| CA3047196A1 (en) | 2016-12-19 | 2018-06-28 | Bayer Pharma Aktiengesellschaft | [(phenylsulfonyl)octahydro-epiminoisoindol-yl](1h-1,2,3-triazol-5-yl)methanones |
| EP3421483A1 (en) | 2017-06-29 | 2019-01-02 | Bayer Pharma Aktiengesellschaft | Novel steroidal 17-beta heteroaryl compounds as inhibitors of akr1c3 |
| CN108159056A (zh) * | 2018-02-09 | 2018-06-15 | 上海礼璞生物医药科技有限公司 | 孕激素在制备组蛋白去乙酰化酶抑制剂和气道周围胶原沉积抑制剂药物中的应用及抑制剂 |
| CN110693892A (zh) * | 2018-07-09 | 2020-01-17 | 深圳艾欣达伟医药科技有限公司 | 化合物用于制备预防、治疗或改善疼痛的药物的用途 |
| 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 |
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| US5604213A (en) | 1992-03-31 | 1997-02-18 | British Technology Group Limited | 17-substituted steroids useful in cancer treatment |
| IL122740A (en) | 1997-01-15 | 2003-09-17 | Akzo Nobel Nv | 16-hydroxy-11-(substituted phenyl)-estra-9,4-diene derivatives, their preparation and pharmaceutical compositions containing them |
| DK0973790T3 (da) | 1997-04-07 | 2003-09-22 | Wyeth Corp | Estra-5(10),7-diener med østrogen aktivitet |
| 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 |
| AU5144999A (en) * | 1998-08-07 | 2000-02-28 | Endorecherche Inc. | Inhibition of type 3 3alpha-hydroxysteroid dehydrogenase |
| JP2007529426A (ja) | 2004-03-12 | 2007-10-25 | エントレメッド インコーポレイテッド | 抗血管新生薬 |
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| AU2007327653B2 (en) | 2006-11-30 | 2013-04-18 | Solvay Pharmaceuticals Gmbh | Substituted estratrien derivatives as 17beta HSD inhibitors |
| WO2008077810A2 (en) | 2006-12-22 | 2008-07-03 | F. Hoffmann-La Roche Ag | Spiro-piperidine derivatives |
| MX2010000918A (es) | 2007-07-24 | 2010-03-15 | Astellas Pharma Inc | Derivado de bencimidazol. |
| WO2009120565A2 (en) | 2008-03-25 | 2009-10-01 | University Of Maryland, Baltimore | Novel prodrugs of c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity |
| AU2010210422A1 (en) | 2009-02-05 | 2011-08-18 | Tokai Pharmaceuticals, Inc. | Novel prodrugs of steroidal CYP17 inhibitors/antiandrogens |
| CA2774015A1 (en) | 2009-09-15 | 2011-03-24 | Cerulean Pharma Inc. | A cdp-camptothecin conjugate, particle or composition and uses thereof |
| EP2729659B1 (en) | 2011-07-08 | 2018-04-04 | FMC Technologies, Inc. | Manifold trailer with multiple articulating arm assemblies |
| DE102011083725A1 (de) * | 2011-09-29 | 2013-04-04 | Bayer Pharma AG | Estra-1,3,5(10),16-tetraen-3-carboxamid-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln |
| US9512169B2 (en) * | 2012-07-10 | 2016-12-06 | Bayer Pharma Aktiengesellschaft | 3-substituted estra-1,3,5(10),16-tetraene derivatives, methods for the production thereof, pharmaceutical preparations containing same, and use thereof for the production of medicaments |
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