EA201500851A1 - ЭСТРА-1,3,5(10),16-ТЕТРАЕН-3-КАРБОКСАМИДЫ ДЛЯ ИНГИБИРОВАНИЯ 17β-ГИДРОКСИСТЕРОИД-ДЕГИДРОГЕНАЗЫ (AKR1C3) - Google Patents

ЭСТРА-1,3,5(10),16-ТЕТРАЕН-3-КАРБОКСАМИДЫ ДЛЯ ИНГИБИРОВАНИЯ 17β-ГИДРОКСИСТЕРОИД-ДЕГИДРОГЕНАЗЫ (AKR1C3)

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Publication number
EA201500851A1
EA201500851A1 EA201500851A EA201500851A EA201500851A1 EA 201500851 A1 EA201500851 A1 EA 201500851A1 EA 201500851 A EA201500851 A EA 201500851A EA 201500851 A EA201500851 A EA 201500851A EA 201500851 A1 EA201500851 A1 EA 201500851A1
Authority
EA
Eurasian Patent Office
Prior art keywords
akr1c3
degydrogenase
tetraen
estra
hydroxysteroid
Prior art date
Application number
EA201500851A
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English (en)
Inventor
Ульрих Боте
Маттиас Буземанн
Наоми Барак
Андреа Ротгери
Оливер Мартин Фишер
Тобиас Марквардт
Original Assignee
Байер Фарма Акциенгезельшафт
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Publication date
Application filed by Байер Фарма Акциенгезельшафт filed Critical Байер Фарма Акциенгезельшафт
Publication of EA201500851A1 publication Critical patent/EA201500851A1/ru

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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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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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
    • A—HUMAN NECESSITIES
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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
    • A—HUMAN NECESSITIES
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    • 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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • 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

Abstract

Изобретение относится к ингибиторам AKR1C3 формулы (I) и к способу их получения, к их применению для лечения и/или профилактики заболеваний, а также к их применению для изготовления лекарственных средств для лечения и/или профилактики заболеваний, в особенности маточных кровотечений и эндометриоза.
EA201500851A 2013-02-21 2014-02-18 ЭСТРА-1,3,5(10),16-ТЕТРАЕН-3-КАРБОКСАМИДЫ ДЛЯ ИНГИБИРОВАНИЯ 17β-ГИДРОКСИСТЕРОИД-ДЕГИДРОГЕНАЗЫ (AKR1C3) EA201500851A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13156125 2013-02-21
PCT/EP2014/053094 WO2014128108A1 (de) 2013-02-21 2014-02-18 Estra-1,3,5(10),16-tetraen-3-carboxamide zur inhibierung von 17.beta.-hydroxysteroid dehdrogenase (akr1 c3)

Publications (1)

Publication Number Publication Date
EA201500851A1 true EA201500851A1 (ru) 2016-02-29

Family

ID=47748503

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201500851A EA201500851A1 (ru) 2013-02-21 2014-02-18 ЭСТРА-1,3,5(10),16-ТЕТРАЕН-3-КАРБОКСАМИДЫ ДЛЯ ИНГИБИРОВАНИЯ 17β-ГИДРОКСИСТЕРОИД-ДЕГИДРОГЕНАЗЫ (AKR1C3)

Country Status (28)

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

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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
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EP3269373A1 (en) 2016-07-11 2018-01-17 Bayer Pharma Aktiengesellschaft Low-dosed oral dosage form of an akr1c3 inhibitor for treatment of diseases
WO2018114677A2 (en) 2016-12-19 2018-06-28 Bayer Pharma Aktiengesellschaft [(phenylsulfonyl)octahydro-epiminoisoindol-yl](1h-1,2,3-triazol-5-yl)methanones
CA3047191A1 (en) 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－***－４-基）甲酮
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
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