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MA38349A1 - Œstra-1,3,5(10),16-tétraéno-3-carboxamide pour inhiber la 17-bêta-hydroxystéroïde déshydrogénase (akr1c3) - Google Patents

Œstra-1,3,5(10),16-tétraéno-3-carboxamide pour inhiber la 17-bêta-hydroxystéroïde déshydrogénase (akr1c3)

Info

Publication number
MA38349A1
MA38349A1 MA38349A MA38349A MA38349A1 MA 38349 A1 MA38349 A1 MA 38349A1 MA 38349 A MA38349 A MA 38349A MA 38349 A MA38349 A MA 38349A MA 38349 A1 MA38349 A1 MA 38349A1
Authority
MA
Morocco
Prior art keywords
akr1c3
tetraeno
estra
carboxamide
beta
Prior art date
Application number
MA38349A
Other languages
English (en)
Inventor
Ulrich Bothe
Naomi Barak
Matthias Busemann
Oliver Martin Fischer
Andrea Rotgeri
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 MA38349A1 publication Critical patent/MA38349A1/fr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28Antiandrogens
    • AHUMAN NECESSITIES
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    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/18Heterocyclic 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)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)

Abstract

L'invention concerne des inhibiteurs de l'akr1c3 suivant la formule (i) et des procédés pour les préparer, leur utilisation dans le traitement et/ou la prévention de maladies ainsi que leur utilisation pour fabriquer des médicaments destinés au traitement et/ou à la prévention de maladies, en particulier des troubles hémorragiques et de l'endométriose.
MA38349A 2013-02-21 2014-02-18 Œstra-1,3,5(10),16-tétraéno-3-carboxamide pour inhiber la 17-bêta-hydroxystéroïde déshydrogénase (akr1c3) MA38349A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13156125 2013-02-21
PCT/EP2014/053094 WO2014128108A1 (fr) 2013-02-21 2014-02-18 Œstra-1,3,5(10),16-tétraéno-3-carboxamide pour inhiber la 17-bêta-hydroxystéroïde déshydrogénase (akr1c3)

Publications (1)

Publication Number Publication Date
MA38349A1 true MA38349A1 (fr) 2017-02-28

Family

ID=47748503

Family Applications (1)

Application Number Title Priority Date Filing Date
MA38349A MA38349A1 (fr) 2013-02-21 2014-02-18 Œstra-1,3,5(10),16-tétraéno-3-carboxamide pour inhiber la 17-bêta-hydroxystéroïde déshydrogénase (akr1c3)

Country Status (28)

Country Link
US (1) US9714266B2 (fr)
EP (1) EP2958928B1 (fr)
JP (1) JP6254195B2 (fr)
KR (1) KR20150118153A (fr)
CN (1) CN105008382B (fr)
AP (1) AP3826A (fr)
AR (1) AR094852A1 (fr)
AU (1) AU2014220800A1 (fr)
BR (1) BR112015018071A2 (fr)
CA (1) CA2901632C (fr)
CL (1) CL2015002346A1 (fr)
CR (1) CR20150432A (fr)
CU (1) CU20150091A7 (fr)
EA (1) EA201500851A1 (fr)
ES (1) ES2678993T3 (fr)
GT (1) GT201500235A (fr)
HK (1) HK1211592A1 (fr)
IL (1) IL240191A0 (fr)
MA (1) MA38349A1 (fr)
MX (1) MX2015010876A (fr)
NI (1) NI201500115A (fr)
PE (1) PE20151754A1 (fr)
PH (1) PH12015501819A1 (fr)
SG (1) SG11201505875WA (fr)
TN (1) TN2015000362A1 (fr)
TW (1) TWI523862B (fr)
UY (1) UY35344A (fr)
WO (1) WO2014128108A1 (fr)

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US20170260226A1 (en) * 2014-09-11 2017-09-14 Bayer Pharma Aktiengesellschaft 3-nitrogen or sulphur substituted oestra-1,3,5(10),16-tetraene akr1c3 inhibitors
CN108474780A (zh) * 2016-01-05 2018-08-31 浜松光子学株式会社 生物体观察方法和生物体观察装置
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 (fr) 2016-07-11 2018-01-17 Bayer Pharma Aktiengesellschaft Formes posologiques orales à faible dosage d'un inhibiteur de akr1c3 pour le traitement des maladies
CA3047191A1 (fr) 2016-12-19 2018-06-28 Bayer Pharma Aktiengesellschaft [4-(phenylsulfonyl)piperazin-1-yl](1h-1,2,3-triazol-4-yl)methanones
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
US20200085791A1 (en) 2016-12-19 2020-03-19 Bayer Pharma Aktiengesellschaft [(phenylsulfonyl)octahydro-epiminoisoindol-yl](1h-1,2,3-triazol-5-yl)methanones
EP3421483A1 (fr) 2017-06-29 2019-01-02 Bayer Pharma Aktiengesellschaft Nouveaux dérivés 17-beta-hétéroaryle des stéroïdes comme inhibiteurs de 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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ES2678993T3 (es) 2018-08-21
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BR112015018071A2 (pt) 2017-07-18
CN105008382B (zh) 2018-01-30
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US20160024142A1 (en) 2016-01-28
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