EA026578B1 - Вещества, связывающие ядерные рецепторы - Google Patents
Вещества, связывающие ядерные рецепторы Download PDFInfo
- Publication number
- EA026578B1 EA026578B1 EA201400056A EA201400056A EA026578B1 EA 026578 B1 EA026578 B1 EA 026578B1 EA 201400056 A EA201400056 A EA 201400056A EA 201400056 A EA201400056 A EA 201400056A EA 026578 B1 EA026578 B1 EA 026578B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- hydroxyphenyl
- dihydroxy
- isoquinolin
- hydroxy
- represents hydrogen
- Prior art date
Links
- 108020005497 Nuclear hormone receptor Proteins 0.000 title description 2
- 102000006255 nuclear receptors Human genes 0.000 title description 2
- 108020004017 nuclear receptors Proteins 0.000 title description 2
- 239000011230 binding agent Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 3
- 239000003814 drug Substances 0.000 claims abstract 2
- 238000004519 manufacturing process Methods 0.000 claims abstract 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims abstract 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims abstract 2
- 230000003287 optical effect Effects 0.000 claims abstract 2
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 230000035755 proliferation Effects 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 206010067125 Liver injury Diseases 0.000 claims 2
- -1 OSOR Chemical group 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 231100000234 hepatic damage Toxicity 0.000 claims 2
- 238000011534 incubation Methods 0.000 claims 2
- 230000008818 liver damage Effects 0.000 claims 2
- HIMXYYUQWXTNIB-UHFFFAOYSA-N 2-(3-fluoro-4-hydroxyphenyl)-6,8-dihydroxyisoquinolin-1-one Chemical compound C=1C(O)=CC(O)=C(C2=O)C=1C=CN2C1=CC=C(O)C(F)=C1 HIMXYYUQWXTNIB-UHFFFAOYSA-N 0.000 claims 1
- CYOPMEZSMPDHMG-UHFFFAOYSA-N 2-(3-fluoro-4-hydroxyphenyl)-6-hydroxy-4-iodoisoquinolin-1-one Chemical compound C=1C(O)=CC=C(C2=O)C=1C(I)=CN2C1=CC=C(O)C(F)=C1 CYOPMEZSMPDHMG-UHFFFAOYSA-N 0.000 claims 1
- TYWJUKOBNZCZNP-UHFFFAOYSA-N 4-bromo-2-(3-fluoro-4-hydroxyphenyl)-6,8-dihydroxyisoquinolin-1-one Chemical compound C=1C(O)=CC(O)=C(C2=O)C=1C(Br)=CN2C1=CC=C(O)C(F)=C1 TYWJUKOBNZCZNP-UHFFFAOYSA-N 0.000 claims 1
- CJNRHMOCAFYPNU-UHFFFAOYSA-N 4-bromo-2-(3-fluoro-4-hydroxyphenyl)-6-hydroxyisoquinolin-1-one Chemical compound C=1C(O)=CC=C(C2=O)C=1C(Br)=CN2C1=CC=C(O)C(F)=C1 CJNRHMOCAFYPNU-UHFFFAOYSA-N 0.000 claims 1
- GLVQMSCCFOGRRG-UHFFFAOYSA-N 4-bromo-6,8-dihydroxy-2-(4-hydroxyphenyl)isoquinolin-1-one Chemical compound C1=CC(O)=CC=C1N1C(=O)C2=C(O)C=C(O)C=C2C(Br)=C1 GLVQMSCCFOGRRG-UHFFFAOYSA-N 0.000 claims 1
- IYKXSJBWAQMFEC-UHFFFAOYSA-N 4-bromo-6-hydroxy-2-(4-hydroxyphenyl)-1-oxoisoquinoline-8-carbonitrile Chemical compound C1=CC(O)=CC=C1N1C(=O)C2=C(C#N)C=C(O)C=C2C(Br)=C1 IYKXSJBWAQMFEC-UHFFFAOYSA-N 0.000 claims 1
- QJLDXJQEOCNNNN-UHFFFAOYSA-N 4-bromo-8-hydroxy-2-(4-hydroxyphenyl)-6-methoxyisoquinolin-1-one Chemical compound C=1C(OC)=CC(O)=C(C2=O)C=1C(Br)=CN2C1=CC=C(O)C=C1 QJLDXJQEOCNNNN-UHFFFAOYSA-N 0.000 claims 1
- AZVDUDPENBFRBD-UHFFFAOYSA-N 4-chloro-2-(3-fluoro-4-hydroxyphenyl)-6-hydroxyisoquinolin-1-one Chemical compound C=1C(O)=CC=C(C2=O)C=1C(Cl)=CN2C1=CC=C(O)C(F)=C1 AZVDUDPENBFRBD-UHFFFAOYSA-N 0.000 claims 1
- OBMYVDPMHJENSJ-UHFFFAOYSA-N 4-chloro-6,8-dihydroxy-2-(4-hydroxyphenyl)isoquinolin-1-one Chemical compound C1=CC(O)=CC=C1N1C(=O)C2=C(O)C=C(O)C=C2C(Cl)=C1 OBMYVDPMHJENSJ-UHFFFAOYSA-N 0.000 claims 1
- OPZIIRQRKPWJSM-UHFFFAOYSA-N 4-chloro-6-hydroxy-2-(4-hydroxyphenyl)isoquinolin-1-one Chemical compound C1=CC(O)=CC=C1N1C(=O)C2=CC=C(O)C=C2C(Cl)=C1 OPZIIRQRKPWJSM-UHFFFAOYSA-N 0.000 claims 1
- UZCGSEMPWJYIKG-UHFFFAOYSA-N 4-ethenyl-2-(3-fluoro-4-hydroxyphenyl)-6,8-dihydroxyisoquinolin-1-one Chemical compound C=1C(O)=CC(O)=C(C2=O)C=1C(C=C)=CN2C1=CC=C(O)C(F)=C1 UZCGSEMPWJYIKG-UHFFFAOYSA-N 0.000 claims 1
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- IWXWZDBKLIOSJS-UHFFFAOYSA-N 5-bromo-6,8-dihydroxy-2-(4-hydroxyphenyl)isoquinolin-1-one Chemical compound C1=CC(O)=CC=C1N1C(=O)C2=C(O)C=C(O)C(Br)=C2C=C1 IWXWZDBKLIOSJS-UHFFFAOYSA-N 0.000 claims 1
- QAGWYKCFYYZWRQ-NSCUHMNNSA-N 6,8-dihydroxy-2-(4-hydroxyphenyl)-4-[(e)-prop-1-enyl]isoquinolin-1-one Chemical compound O=C1C2=C(O)C=C(O)C=C2C(/C=C/C)=CN1C1=CC=C(O)C=C1 QAGWYKCFYYZWRQ-NSCUHMNNSA-N 0.000 claims 1
- BVCSBABZBDLYNM-UHFFFAOYSA-N 6-hydroxy-2-(4-hydroxyphenyl)-4-(4-methoxyphenyl)isoquinolin-1-one Chemical compound C1=CC(OC)=CC=C1C(C1=CC(O)=CC=C1C1=O)=CN1C1=CC=C(O)C=C1 BVCSBABZBDLYNM-UHFFFAOYSA-N 0.000 claims 1
- DWJWQCHKPAXAQA-UHFFFAOYSA-N 6-hydroxy-2-(4-hydroxyphenyl)-4-iodoisoquinolin-1-one Chemical compound C1=CC(O)=CC=C1N1C(=O)C2=CC=C(O)C=C2C(I)=C1 DWJWQCHKPAXAQA-UHFFFAOYSA-N 0.000 claims 1
- YECTYKMUECXIIC-UHFFFAOYSA-N 6-hydroxy-2-(4-hydroxyphenyl)-4-phenylisoquinolin-1-one Chemical compound C1=CC(O)=CC=C1N1C(=O)C2=CC=C(O)C=C2C(C=2C=CC=CC=2)=C1 YECTYKMUECXIIC-UHFFFAOYSA-N 0.000 claims 1
- UKTXTSFJQVTSDF-UHFFFAOYSA-N 8-hydroxy-2-(4-hydroxyphenyl)-6-methoxy-1-oxoisoquinoline-5-carbonitrile Chemical compound N#CC=1C(OC)=CC(O)=C(C2=O)C=1C=CN2C1=CC=C(O)C=C1 UKTXTSFJQVTSDF-UHFFFAOYSA-N 0.000 claims 1
- 241000700159 Rattus Species 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 239000013256 coordination polymer Substances 0.000 claims 1
- 230000001186 cumulative effect Effects 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000004982 dihaloalkyl group Chemical group 0.000 claims 1
- 210000002889 endothelial cell Anatomy 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 210000002540 macrophage Anatomy 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000001629 suppression Effects 0.000 claims 1
- 125000004385 trihaloalkyl group Chemical group 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 abstract 2
- 206010019708 Hepatic steatosis Diseases 0.000 abstract 2
- 208000010706 fatty liver disease Diseases 0.000 abstract 2
- 231100000240 steatosis hepatitis Toxicity 0.000 abstract 2
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 4
- 235000013547 stew Nutrition 0.000 description 3
- 101100510326 Caenorhabditis elegans tpa-1 gene Proteins 0.000 description 1
- 235000002020 sage Nutrition 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
-
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
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