AR092025A1 - Derivados de estra-1,3,5(10),16-tetraeno 3-sustituidos, procedimientos para su preparacion, preparaciones farmaceuticas que los contienen, asi como su uso para la preparacion de medicamentos - Google Patents

Derivados de estra-1,3,5(10),16-tetraeno 3-sustituidos, procedimientos para su preparacion, preparaciones farmaceuticas que los contienen, asi como su uso para la preparacion de medicamentos

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Publication number
AR092025A1
AR092025A1 ARP130102438A ARP130102438A AR092025A1 AR 092025 A1 AR092025 A1 AR 092025A1 AR P130102438 A ARP130102438 A AR P130102438A AR P130102438 A ARP130102438 A AR P130102438A AR 092025 A1 AR092025 A1 AR 092025A1
Authority
AR
Argentina
Prior art keywords
ch2ch2
hydrogen
methyl
ethyl
trifluoromethyl
Prior art date
Application number
ARP130102438A
Other languages
English (en)
Inventor
Dr Bothe Ulrich
Dr Busemann Matthias
Martin Dr Fischer Oliver
Dra Barak Naomi
Dra Rogeri Andrea
Dr Marquardt Tobias
Dr Stegmann Christian
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48748225&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR092025(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of AR092025A1 publication Critical patent/AR092025A1/es

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Classifications

    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Son inhibidores de AKR1C3 que es una enzima multifuncional, útiles en especial en trastornos hemorrágicos y endometriosis. Reivindicación 1: Compuestos de la fórmula (1) en donde A es piridin-3-ilo, pirimidin-5-ilo, pirimidin-4-ilo, pirazin-2-ilo, piridazin-4-ilo, piridazin-3-ilo, opcionalmente mono- o disustituido con flúor, cloro, nitrilo, hidroxilo, carboxilo, trifluorometilo, pentafluoroetilo, metoxi, etoxi, trifluorometoxi, -OCH₂CF₃, -SO₂CH₃, -SO₂CH₂CH₃, -(C=O)CH₃, alquilo C₁₋₄, -CH₂OH, -C(CH₃)₂OH, -CONH₂, -(C=O)NHCH₃, -(C=O)NHCH₂CH₃, -(C=O)N(CH₃)₂, -SO₂NH₂, -SO₂NHCH₃, -SO₂N(CH₃)₂; R¹ es -O-CRᵃRᵇ-Y, Rᵃ y Rᵇ son, de modo independiente entre sí, hidrógeno, metilo, etilo, propilo, isopropilo, fenilo, 4-fluorofenilo, 3-fluorofenilo, 2-fluorofenilo, CH₃-O-CH₂-, -CH₂CF₃ o Rᵃ y Rᵇ son juntos -(CH₂)ₙ- con n = 2, 3, 4 ó 5, o Rᵃ y Rᵇ son juntos -CH₂-O-CH₂-, -CH₂-NH-CH₂-, -CH₂-N(CH₃)-CH₂-, -CH₂CH₂-O-CH₂CH₂-, -CH₂CH₂-NH-CH₂CH₂-, -CH₂CH₂-N(CH₃)-CH₂CH₂-; -O-CRᶜRᵈ-CRᵉRᶠ-Y, Rᶜ, Rᵈ, Rᵉ, Rᶠ son hidrógeno o Rᵉ, Rᶠ son hidrógeno y Rᶜ, Rᵈ son, de modo independiente entre sí, metilo, etilo o juntos son -(CH₂)ₙ- con n = 2, 3, 4, 5 o son juntos -CH₂-O-CH₂- o -CH₂CH₂-O-CH₂CH₂-, o Rᶜ, Rᵈ son hidrógeno y Rᵉ, Rᶠ son, de modo independiente entre sí, metilo, etilo, CF₃CH₂- o son juntos -(CH₂)ₙ- con n = 2, 3, 4, 5, -CH₂CH₂-O-CH₂CH₂-, -CH₂CH₂-NH-CH₂CH₂-, -CH₂CH₂-N(CH₃)-CH₂CH₂-, -CH₂-O-CH₂-, -CH₂-NH-CH₂-, -CH₂-N(CH₃)-CH₂-, o Rᵈ, Rᵉ, Rᶠ son hidrógeno y Rᶜ es metilo, etilo, trifluorometilo, o Rᶜ, Rᵈ, Rᶠ son hidrógeno y Rᵉ es metilo, etilo, trifluorometilo, hidroxilo, metoxi, trifluorometoxi, o Rᵈ, Rᶠ son hidrógeno y Rᶜ, Rᵉ son, de modo independiente entre sí, metilo, etilo, trifluorometilo; -O-CH₂CH₂CH₂-Y; -O-CH₂C(CH₃)₂CH₂-Y; -O-CH₂CH₂C(CH₃)₂-Y; -O-CH₂CH₂CH(CH₃)-Y; -O-CH₂-CH(OH)-CH₂-Y; -OCH₂CH₂CH₂CH₂-Y; -CH₂-Y; -CRᵍRʰ-CRⁱRʲ-Y, con Rᵍ, Rʰ, Rⁱ, Rʲ son hidrógeno, o Rᵍ, Rʰ, Rⁱ son hidrógeno y Rʲ es metilo, etilo, trifluorometilo, o Rⁱ, Rʲ son hidrógeno y Rᵍ, Rʰ son metilo o juntos son -CH₂-, -CH₂CH₂-, -CH₂CH₂CH₂-, o Rᵍ es metilo y Rʰ, Rⁱ, Rʲ son hidrógeno; -CH₂CH₂CH₂-Y; -CH₂CH₂C(CH₃)₂-Y; o -CH₂CH₂CH₂CH₂-Y; e Y es -CO₂H, -OH, -(C=O)NH₂, -(C=O)NH-alquilo C₁₋₄, -S(=O)CH₃; y sus sales, solvatos y solvatos de las sales.
ARP130102438A 2012-07-10 2013-07-10 Derivados de estra-1,3,5(10),16-tetraeno 3-sustituidos, procedimientos para su preparacion, preparaciones farmaceuticas que los contienen, asi como su uso para la preparacion de medicamentos AR092025A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102012211970 2012-07-10

Publications (1)

Publication Number Publication Date
AR092025A1 true AR092025A1 (es) 2015-03-18

Family

ID=48748225

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130102438A AR092025A1 (es) 2012-07-10 2013-07-10 Derivados de estra-1,3,5(10),16-tetraeno 3-sustituidos, procedimientos para su preparacion, preparaciones farmaceuticas que los contienen, asi como su uso para la preparacion de medicamentos

Country Status (28)

Country Link
US (1) US9512169B2 (es)
EP (1) EP2872524B1 (es)
JP (1) JP6196302B2 (es)
KR (1) KR20150036319A (es)
CN (1) CN104428309B (es)
AP (1) AP2014008179A0 (es)
AR (1) AR092025A1 (es)
AU (1) AU2013289344A1 (es)
BR (1) BR112015000443A2 (es)
CA (1) CA2878485A1 (es)
CL (1) CL2015000039A1 (es)
CO (1) CO7160008A2 (es)
CR (1) CR20150007A (es)
DO (1) DOP2015000005A (es)
EA (1) EA201500112A1 (es)
EC (1) ECSP15000868A (es)
ES (1) ES2603258T3 (es)
HK (1) HK1205743A1 (es)
IL (1) IL236581A0 (es)
MA (1) MA37742B1 (es)
MX (1) MX2015000347A (es)
PE (1) PE20150353A1 (es)
PH (1) PH12015500062A1 (es)
TN (1) TN2015000007A1 (es)
TW (1) TW201402596A (es)
UY (1) UY34899A (es)
WO (1) WO2014009274A1 (es)
ZA (1) ZA201500920B (es)

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Publication number Priority date Publication date Assignee Title
CN105008382B (zh) * 2013-02-21 2018-01-30 拜耳医药股份公司 用于抑制17β‑羟类固醇脱氢酶(AKR1 C3)的雌甾‑1,3,5(10),16‑四烯‑3‑羧酰胺
WO2016037956A1 (en) * 2014-09-11 2016-03-17 Bayer Pharma Aktiengesellschaft 3-nitrogen or sulphur substituted oestra-1,3,5(10),16-tetraene akr1c3 inhibitors
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
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
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
EP3421483A1 (en) 2017-06-29 2019-01-02 Bayer Pharma Aktiengesellschaft Novel steroidal 17-beta heteroaryl compounds as inhibitors of akr1c3
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
CN110272465A (zh) * 2019-07-15 2019-09-24 成都贝诺科成生物科技有限公司 阿比特龙衍生物、其制备方法与应用

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ES2603258T3 (es) 2017-02-24
MX2015000347A (es) 2015-04-14
US9512169B2 (en) 2016-12-06
IL236581A0 (en) 2015-02-26
AU2013289344A1 (en) 2015-02-05
TN2015000007A1 (en) 2016-06-29
CN104428309A (zh) 2015-03-18
TW201402596A (zh) 2014-01-16
UY34899A (es) 2014-02-28
HK1205743A1 (en) 2015-12-24
KR20150036319A (ko) 2015-04-07
PE20150353A1 (es) 2015-03-28
ECSP15000868A (es) 2016-01-29
CL2015000039A1 (es) 2015-03-27
EP2872524B1 (de) 2016-08-24
JP6196302B2 (ja) 2017-09-13
MA37742A1 (fr) 2016-05-31
AP2014008179A0 (en) 2014-12-31
JP2015522050A (ja) 2015-08-03
CO7160008A2 (es) 2015-01-15
EP2872524A1 (de) 2015-05-20
DOP2015000005A (es) 2015-02-15
PH12015500062A1 (en) 2015-03-02
CA2878485A1 (en) 2014-01-16
CR20150007A (es) 2015-03-13
EA201500112A1 (ru) 2015-07-30
WO2014009274A1 (de) 2014-01-16
BR112015000443A2 (pt) 2017-06-27
MA37742B1 (fr) 2016-12-30
ZA201500920B (en) 2017-01-25
US20150210734A1 (en) 2015-07-30
CN104428309B (zh) 2016-09-14

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