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AR124199A1 - Nuevos compuestos como inhibidor dual del receptor de andrógenos y de la fosfodiesterasa - Google Patents

Nuevos compuestos como inhibidor dual del receptor de andrógenos y de la fosfodiesterasa

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Publication number
AR124199A1
AR124199A1 ARP210103440A ARP210103440A AR124199A1 AR 124199 A1 AR124199 A1 AR 124199A1 AR P210103440 A ARP210103440 A AR P210103440A AR P210103440 A ARP210103440 A AR P210103440A AR 124199 A1 AR124199 A1 AR 124199A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
compounds
pde
androgen receptor
independently selected
Prior art date
Application number
ARP210103440A
Other languages
English (en)
Inventor
Yoon Lee
- Kwon Sung Suk
- Kim Kyung Wook
- Kim Jeong Sun
- Kim Jeong Geun
- Moon An Ah
- Park Sun Na
- Ban Jun Young
- Song Dong Su
- Jung Ju Keun
- Lee Soo-Jin Young
Original Assignee
Ildong Pharmaceutical Co Ltd
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 Ildong Pharmaceutical Co Ltd filed Critical Ildong Pharmaceutical Co Ltd
Publication of AR124199A1 publication Critical patent/AR124199A1/es

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    • CCHEMISTRY; METALLURGY
    • 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
    • AHUMAN NECESSITIES
    • 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
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/44Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving esterase
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/502Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects
    • G01N33/5041Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects involving analysis of members of signalling pathways
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • G01N33/743Steroid hormones
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/72Assays involving receptors, cell surface antigens or cell surface determinants for hormones
    • G01N2333/723Steroid/thyroid hormone superfamily, e.g. GR, EcR, androgen receptor, oestrogen receptor

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Food Science & Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pathology (AREA)
  • Cell Biology (AREA)
  • General Physics & Mathematics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Toxicology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Endocrinology (AREA)
  • Genetics & Genomics (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente divulgación proporciona compuestos inhibidores del receptor de andrógenos (AR) y de la fosfodiesterasa 5 (PDE-5) y composiciones que incluyen dichos compuestos. Los compuestos pueden proporcionar una funcionalidad dual para inhibir el AR e inhibir la PDE-5. La presente divulgación también proporciona métodos para utilizar dichos compuestos y composiciones para inhibir el AR y la PDE-5 en un sistema o muestra biológica. También se proporcionan métodos de preparación de dichos compuestos y composiciones, y precursores sintéticos de dichos compuestos. Reivindicación 1: Un compuesto de fórmula (1) o un solvato, un hidrato, un profármaco y/o un estereoisómero de este, o una sal farmacéuticamente aceptable de este, caracterizado porque: L es una porción de enlace; R¹ y R² se seleccionan de manera independiente entre -H, alquilo(C₁-C₆) opcionalmente sustituido, cicloalquilo(C₃-C₆) opcionalmente sustituido, alcoxi(C₁-C₆) opcionalmente sustituido y alquenilo(C₂-C₄) opcionalmente sustituido; cada R¹³ se selecciona entre -H, alquilo(C₁-C₆) opcionalmente sustituido y alcoxi(C₁-C₆) opcionalmente sustituido; cada R¹⁴ se selecciona de forma independiente de -H, -CN, -OH, -NH₂, -NO₂, halógeno, alquilo(C₁-C₅) opcionalmente sustituido, haloalquilo(C₁-C₅) opcionalmente sustituido, alcoxi(C₁-C₅) opcionalmente sustituido, cicloalquilo(C₃-C₆) opcionalmente sustituido y alquenilo(C₂-C₄) opcionalmente sustituido; X¹ es N o CR¹⁴; X² y X³ se seleccionan de manera independiente entre N y CR¹³; Y¹ e Y² se seleccionan de manera independiente entre N y C, donde uno entre Y¹ e Y² es N; m es 0 a 2; y n es 1 a 4. Reivindicación 42: Un método para modular el receptor de andrógenos y/o inhibir PDE-5, el método caracterizado porque comprende poner en contacto un sistema biológico que comprende el receptor de andrógenos y/o PDE-5 con una cantidad de eficaz de un compuesto o un solvato, un hidrato, un profármaco, y/o un estereoisómero de este, o una sal farmacéuticamente aceptable de este según una cualquiera de las reivindicaciones 1 a 40 o una composición farmacéutica según la reivindicación 41.
ARP210103440A 2020-12-11 2021-12-10 Nuevos compuestos como inhibidor dual del receptor de andrógenos y de la fosfodiesterasa AR124199A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US202063124615P 2020-12-11 2020-12-11

Publications (1)

Publication Number Publication Date
AR124199A1 true AR124199A1 (es) 2023-02-22

Family

ID=81974180

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Country Status (17)

Country Link
US (1) US11787812B2 (es)
EP (1) EP4259634A4 (es)
JP (1) JP2023552632A (es)
KR (1) KR20230118137A (es)
CN (1) CN116848116A (es)
AR (1) AR124199A1 (es)
AU (1) AU2021396593A1 (es)
CA (1) CA3201054A1 (es)
CL (1) CL2023001673A1 (es)
CO (1) CO2023009145A2 (es)
CR (1) CR20230306A (es)
EC (1) ECSP23051657A (es)
IL (1) IL303407A (es)
MX (1) MX2023006911A (es)
PE (1) PE20240248A1 (es)
TW (1) TW202237615A (es)
WO (1) WO2022123310A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3201054A1 (en) * 2020-12-11 2022-06-16 Yoon-Suk Lee Novel compounds as androgen receptor and phosphodiesterase dual inhibitor
WO2023244059A1 (en) * 2022-06-15 2023-12-21 Ildong Pharmaceutical Co., Ltd. Methods of treating cancer using dual androgen receptor and pde5 inhibitor compounds
CN115819303B (zh) * 2022-11-15 2024-10-01 江苏睿实生物科技有限公司 一种化合物3-氟-4-异硫氰基-2-三氟甲基苄腈的制备方法
US20250136578A1 (en) * 2023-10-12 2025-05-01 Kolm Therapeutics Inc. Bifunctional androgen receptor compounds

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2309332C (en) * 1997-11-12 2002-12-03 Bayer Aktiengesellschaft 2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors
DE19827640A1 (de) 1998-06-20 1999-12-23 Bayer Ag 7-Alkyl- und Cycloalkyl-substituierte Imidazotriazinone
KR100353014B1 (ko) * 1998-11-11 2002-09-18 동아제약 주식회사 발기부전 치료에 효과를 갖는 피라졸로피리미디논 화합물
DE10010067A1 (de) * 2000-03-02 2001-09-06 Bayer Ag Neue Imidazotriazinone und ihre Verwendung
KR100377782B1 (ko) 2000-06-23 2003-03-29 동아제약 주식회사 발기부전 치료에 효과를 갖는 피라졸로피리미디논화합물의 제조방법
GB0222833D0 (en) 2002-10-02 2002-11-06 Syngenta Ltd Chemical process
JP2004170323A (ja) 2002-11-22 2004-06-17 Sumitomo Pharmaceut Co Ltd 皮膚疾患治療剤のスクリーニング方法
CA2520124A1 (en) 2003-03-28 2004-10-14 Chiron Corporation Use of benzazole compounds for immunopotentiation
KR101782236B1 (ko) 2005-05-13 2017-09-26 더 리전트 오브 더 유니버시티 오브 캘리포니아 디아릴히단토인 화합물
CN1966506A (zh) 2005-11-17 2007-05-23 上海特化医药科技有限公司 吡唑并嘧啶酮衍生物及其制备方法和用途
WO2008045664A2 (en) 2006-10-06 2008-04-17 Kalypsys, Inc. Heterocyclic pde4 inhibitors as antiinflammatory agents
KR20090087795A (ko) 2008-02-13 2009-08-18 한양대학교 산학협력단 혈관 재협착 예방 및 치료를 위한 약학 조성물 및 이를포함하는 스텐트
JP5578490B2 (ja) 2008-12-26 2014-08-27 味の素株式会社 ピラゾロピリミジン化合物
US8524755B2 (en) 2009-02-24 2013-09-03 Medivation Prostate Therapeutics, Inc. Specific diarylhydantoin and diarylthiohydantoin compounds
WO2010118367A2 (en) 2009-04-10 2010-10-14 Progenics Pharmaceuticals, Inc. Antiviral pyrimidines
CN101691373B (zh) 2009-10-21 2011-12-07 段波 一种治疗勃起功能障碍和早泄的药物及其制备
CN102970965A (zh) 2010-04-05 2013-03-13 Sk化学公司 含有pde5抑制剂的减少皮肤皱纹的合成物
CN102134242B (zh) 2011-01-21 2013-08-28 浙江大德药业集团有限公司 一种用于治疗阳痿的快速长效的化合物
DK2961741T3 (en) 2013-03-01 2017-07-03 Fund Para La Investig Medica Aplicada Novel compounds as dual inhibitors of phosphodiesterases and histone deacetylases
US9969744B2 (en) * 2014-08-04 2018-05-15 Fundación La Investigación Médica Aplicada Compounds for use in cognition improvement
WO2016120432A1 (en) 2015-01-30 2016-08-04 Fundación Para La Investigación Médica Aplicada Compounds and methods for anticoagulation therapy
JP2018076234A (ja) 2015-03-16 2018-05-17 大正製薬株式会社 ピラゾロ[1,5−a]ピリミジン化合物
CA3201054A1 (en) * 2020-12-11 2022-06-16 Yoon-Suk Lee Novel compounds as androgen receptor and phosphodiesterase dual inhibitor

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US11787812B2 (en) 2023-10-17
EP4259634A1 (en) 2023-10-18
JP2023552632A (ja) 2023-12-18
PE20240248A1 (es) 2024-02-19
ECSP23051657A (es) 2023-08-31
CA3201054A1 (en) 2022-06-16
CR20230306A (es) 2023-09-01
AU2021396593A1 (en) 2023-07-20
CL2023001673A1 (es) 2023-12-01
TW202237615A (zh) 2022-10-01
US20220194948A1 (en) 2022-06-23
CO2023009145A2 (es) 2023-07-21
IL303407A (en) 2023-08-01
KR20230118137A (ko) 2023-08-10
CN116848116A (zh) 2023-10-03
MX2023006911A (es) 2023-06-26
EP4259634A4 (en) 2024-11-20
WO2022123310A1 (en) 2022-06-16

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