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)

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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
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PE
Peru
Prior art keywords
akr1
estra
tetraene
carboxamides
inhibition
Prior art date
Application number
PE2015001794A
Other languages
English (en)
Inventor
Ulrich Bothe
Matthias Busemann
Naomi Barak
Andrea Rotgeri
Oliver Martin Fischer
Tobias Marquardt
Original Assignee
Bayer Pharma AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of PE20151754A1 publication Critical patent/PE20151754A1/es

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    • 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
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    • 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
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    • 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)
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  • Cardiology (AREA)
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  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (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
PE2015001794A 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) PE20151754A1 (es)

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

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ID=47748503

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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)

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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
WO2017119340A1 (ja) * 2016-01-05 2017-07-13 浜松ホトニクス株式会社 生体観察方法及び生体観察装置
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
CA3047196A1 (en) 2016-12-19 2018-06-28 Bayer Pharma Aktiengesellschaft [(phenylsulfonyl)octahydro-epiminoisoindol-yl](1h-1,2,3-triazol-5-yl)methanones
US20200087284A1 (en) 2016-12-19 2020-03-19 Bayer Pharma Aktiengesellschaft [4-(phenylsulfonyl)piperazin-1-yl](1h-1, 2, 3-triazol-4-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

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