JP2017043614A5 - - Google Patents
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- Publication number
- JP2017043614A5 JP2017043614A5 JP2016164830A JP2016164830A JP2017043614A5 JP 2017043614 A5 JP2017043614 A5 JP 2017043614A5 JP 2016164830 A JP2016164830 A JP 2016164830A JP 2016164830 A JP2016164830 A JP 2016164830A JP 2017043614 A5 JP2017043614 A5 JP 2017043614A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- oxy
- fluoro
- methylphenoxymethyl
- quinoxalin
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
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- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 28
- 150000001408 amides Chemical class 0.000 claims 16
- 150000002148 esters Chemical class 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 16
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 14
- -1 alkylamino group Amide Chemical class 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 125000003277 amino group Chemical group 0.000 claims 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 10
- 208000027866 inflammatory disease Diseases 0.000 claims 9
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 8
- 229940124597 therapeutic agent Drugs 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 125000003282 alkyl amino group Chemical group 0.000 claims 6
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 6
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 230000000069 prophylactic effect Effects 0.000 claims 6
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 5
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 5
- 125000001769 aryl amino group Chemical group 0.000 claims 4
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 4
- 102000003676 Glucocorticoid Receptors Human genes 0.000 claims 3
- 108090000079 Glucocorticoid Receptors Proteins 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 3
- 208000020084 Bone disease Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000012659 Joint disease Diseases 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical group OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 2
- 206010046851 Uveitis Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 210000000988 bone and bone Anatomy 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 208000014674 injury Diseases 0.000 claims 2
- 206010023332 keratitis Diseases 0.000 claims 2
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims 2
- 230000003449 preventive effect Effects 0.000 claims 2
- 208000004644 retinal vein occlusion Diseases 0.000 claims 2
- 238000001356 surgical procedure Methods 0.000 claims 2
- 230000008733 trauma Effects 0.000 claims 2
- PRPUCYPOQXAQPA-HXUWFJFHSA-N (3R)-4-[4-[5-[(5-fluoro-2-methylphenoxy)methyl]-2,2,4-trimethyl-3-oxo-1H-quinoxalin-6-yl]-3-methoxyphenoxy]-3-hydroxybutanenitrile Chemical compound C(#N)C[C@H](COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)O PRPUCYPOQXAQPA-HXUWFJFHSA-N 0.000 claims 1
- PRPUCYPOQXAQPA-FQEVSTJZSA-N (3S)-4-[4-[5-[(5-fluoro-2-methylphenoxy)methyl]-2,2,4-trimethyl-3-oxo-1H-quinoxalin-6-yl]-3-methoxyphenoxy]-3-hydroxybutanenitrile Chemical compound C(#N)C[C@@H](COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)O PRPUCYPOQXAQPA-FQEVSTJZSA-N 0.000 claims 1
- NJNXNAWEVLDAOW-UHFFFAOYSA-N 1,3,3-trimethyl-4h-quinoxalin-2-one Chemical compound C1=CC=C2N(C)C(=O)C(C)(C)NC2=C1 NJNXNAWEVLDAOW-UHFFFAOYSA-N 0.000 claims 1
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims 1
- PNTUQGQRALWYMN-FQEVSTJZSA-N 4-[(2S)-1-[4-[5-[(5-fluoro-2-methylphenoxy)methyl]-2,2,4-trimethyl-3-oxo-1H-quinoxalin-6-yl]-3-methoxyphenoxy]propan-2-yl]oxy-4-oxobutanoic acid Chemical compound C(=O)(O)CCC(=O)O[C@H](COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)C PNTUQGQRALWYMN-FQEVSTJZSA-N 0.000 claims 1
- JTJCQMNKJKDYDE-UHFFFAOYSA-N 4-[4-[5-[(5-fluoro-2-methylphenoxy)methyl]-2,2,4-trimethyl-3-oxo-1H-quinoxalin-6-yl]-3-methoxyphenoxy]-3-hydroxybutanoic acid Chemical compound C(=O)(O)CC(COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)O JTJCQMNKJKDYDE-UHFFFAOYSA-N 0.000 claims 1
- JFUAWXPBHXKZGA-IBGZPJMESA-N 4-fluoro-2-[(4r)-5,5,5-trifluoro-4-hydroxy-2-methyl-4-(1h-pyrrolo[2,3-c]pyridin-2-ylmethyl)pentan-2-yl]phenol Chemical compound C([C@@](O)(CC=1NC2=CN=CC=C2C=1)C(F)(F)F)C(C)(C)C1=CC(F)=CC=C1O JFUAWXPBHXKZGA-IBGZPJMESA-N 0.000 claims 1
- CYFHWCSCWBIQHE-UHFFFAOYSA-N 7-[4-(2,3-dihydroxypropoxy)-2-methoxyphenyl]-8-[(5-fluoro-2-methylphenoxy)methyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound OC(COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)CO CYFHWCSCWBIQHE-UHFFFAOYSA-N 0.000 claims 1
- ADLAQYPIAGPPJY-UHFFFAOYSA-N 7-[4-(3-fluoro-2-hydroxypropoxy)-2-methoxyphenyl]-8-[(5-fluoro-2-methylphenoxy)methyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound FCC(COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)O ADLAQYPIAGPPJY-UHFFFAOYSA-N 0.000 claims 1
- CYFHWCSCWBIQHE-LJQANCHMSA-N 7-[4-[(2R)-2,3-dihydroxypropoxy]-2-methoxyphenyl]-8-[(5-fluoro-2-methylphenoxy)methyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound O[C@@H](COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)CO CYFHWCSCWBIQHE-LJQANCHMSA-N 0.000 claims 1
- FQNFVOSZGVJCJD-HXUWFJFHSA-N 7-[4-[(2R)-2,4-dihydroxybutoxy]-2-methoxyphenyl]-8-[(5-fluoro-2-methylphenoxy)methyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound O[C@@H](COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)CCO FQNFVOSZGVJCJD-HXUWFJFHSA-N 0.000 claims 1
- CYFHWCSCWBIQHE-IBGZPJMESA-N 7-[4-[(2S)-2,3-dihydroxypropoxy]-2-methoxyphenyl]-8-[(5-fluoro-2-methylphenoxy)methyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound O[C@H](COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)CO CYFHWCSCWBIQHE-IBGZPJMESA-N 0.000 claims 1
- FQNFVOSZGVJCJD-FQEVSTJZSA-N 7-[4-[(2S)-2,4-dihydroxybutoxy]-2-methoxyphenyl]-8-[(5-fluoro-2-methylphenoxy)methyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound O[C@H](COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)CCO FQNFVOSZGVJCJD-FQEVSTJZSA-N 0.000 claims 1
- FJFREPIFWZMDCP-UHFFFAOYSA-N 8-[(5-fluoro-2-methylphenoxy)methyl]-7-[2-methoxy-4-(3,3,3-trifluoro-2-hydroxypropoxy)phenyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound FC=1C=CC(=C(OCC=2C(=CC=C3NC(C(N(C=23)C)=O)(C)C)C2=C(C=C(C=C2)OCC(C(F)(F)F)O)OC)C=1)C FJFREPIFWZMDCP-UHFFFAOYSA-N 0.000 claims 1
- CKTZGBDBBVXQAA-UHFFFAOYSA-N 8-[(5-fluoro-2-methylphenoxy)methyl]-7-[4-(2-hydroxy-3,3-dimethylbutoxy)-2-methoxyphenyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound CC(C(COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)O)(C)C CKTZGBDBBVXQAA-UHFFFAOYSA-N 0.000 claims 1
- HWUKNAFNKBBHIY-UHFFFAOYSA-N 8-[(5-fluoro-2-methylphenoxy)methyl]-7-[4-(2-hydroxy-4-oxo-4-pyrrolidin-1-ylbutoxy)-2-methoxyphenyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound FC=1C=CC(=C(OCC=2C(=CC=C3NC(C(N(C=23)C)=O)(C)C)C2=C(C=C(C=C2)OCC(CC(=O)N2CCCC2)O)OC)C=1)C HWUKNAFNKBBHIY-UHFFFAOYSA-N 0.000 claims 1
- GOTHEAKPIPZZHI-UHFFFAOYSA-N 8-[(5-fluoro-2-methylphenoxy)methyl]-7-[4-(2-hydroxyethoxy)-2-methoxyphenyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound FC=1C=CC(=C(OCC=2C(=CC=C3NC(C(N(C=23)C)=O)(C)C)C2=C(C=C(C=C2)OCCO)OC)C=1)C GOTHEAKPIPZZHI-UHFFFAOYSA-N 0.000 claims 1
- WBNLLZUROFDWJO-HXUWFJFHSA-N 8-[(5-fluoro-2-methylphenoxy)methyl]-7-[4-[(2R)-2-hydroxybutoxy]-2-methoxyphenyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound FC=1C=CC(=C(OCC=2C(=CC=C3NC(C(N(C=23)C)=O)(C)C)C2=C(C=C(C=C2)OC[C@@H](CC)O)OC)C=1)C WBNLLZUROFDWJO-HXUWFJFHSA-N 0.000 claims 1
- DIJHYLZNFKXKJT-GOSISDBHSA-N 8-[(5-fluoro-2-methylphenoxy)methyl]-7-[4-[(2R)-2-hydroxypropoxy]-2-methoxyphenyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound FC=1C=CC(=C(OCC=2C(=CC=C3NC(C(N(C=23)C)=O)(C)C)C2=C(C=C(C=C2)OC[C@@H](C)O)OC)C=1)C DIJHYLZNFKXKJT-GOSISDBHSA-N 0.000 claims 1
- WBNLLZUROFDWJO-FQEVSTJZSA-N 8-[(5-fluoro-2-methylphenoxy)methyl]-7-[4-[(2S)-2-hydroxybutoxy]-2-methoxyphenyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound FC=1C=CC(=C(OCC=2C(=CC=C3NC(C(N(C=23)C)=O)(C)C)C2=C(C=C(C=C2)OC[C@H](CC)O)OC)C=1)C WBNLLZUROFDWJO-FQEVSTJZSA-N 0.000 claims 1
- DIJHYLZNFKXKJT-SFHVURJKSA-N 8-[(5-fluoro-2-methylphenoxy)methyl]-7-[4-[(2S)-2-hydroxypropoxy]-2-methoxyphenyl]-1,3,3-trimethyl-4H-quinoxalin-2-one Chemical compound FC=1C=CC(=C(OCC=2C(=CC=C3NC(C(N(C=23)C)=O)(C)C)C2=C(C=C(C=C2)OC[C@H](C)O)OC)C=1)C DIJHYLZNFKXKJT-SFHVURJKSA-N 0.000 claims 1
- 208000019838 Blood disease Diseases 0.000 claims 1
- 208000027932 Collagen disease Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 208000017701 Endocrine disease Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000003435 Optic Neuritis Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000002158 Proliferative Vitreoretinopathy Diseases 0.000 claims 1
- 201000007527 Retinal artery occlusion Diseases 0.000 claims 1
- 206010038910 Retinitis Diseases 0.000 claims 1
- 206010038934 Retinopathy proliferative Diseases 0.000 claims 1
- 208000025747 Rheumatic disease Diseases 0.000 claims 1
- 206010039705 Scleritis Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 208000012931 Urologic disease Diseases 0.000 claims 1
- BJRFGKPKUWTKEE-FQEVSTJZSA-N [(2S)-1-[4-[5-[(5-fluoro-2-methylphenoxy)methyl]-2,2,4-trimethyl-3-oxo-1H-quinoxalin-6-yl]-3-methoxyphenoxy]-3-hydroxypropan-2-yl]phosphonic acid Chemical compound FC=1C=CC(=C(OCC=2C(=CC=C3NC(C(N(C=23)C)=O)(C)C)C2=C(C=C(C=C2)OC[C@H](CO)P(=O)(O)O)OC)C=1)C BJRFGKPKUWTKEE-FQEVSTJZSA-N 0.000 claims 1
- VXNDLAALIRRYMJ-NRFANRHFSA-N [(2S)-1-[4-[5-[(5-fluoro-2-methylphenoxy)methyl]-2,2,4-trimethyl-3-oxo-1H-quinoxalin-6-yl]-3-methoxyphenoxy]-4-hydroxybutan-2-yl]phosphonic acid Chemical compound FC=1C=CC(=C(OCC=2C(=CC=C3NC(C(N(C=23)C)=O)(C)C)C2=C(C=C(C=C2)OC[C@H](CCO)P(=O)(O)O)OC)C=1)C VXNDLAALIRRYMJ-NRFANRHFSA-N 0.000 claims 1
- JLGLBZBUYGFFHB-SXMXNQBWSA-N [(2S)-1-[4-[5-[(5-fluoro-2-methylphenoxy)methyl]-2,2,4-trimethyl-3-oxo-1H-quinoxalin-6-yl]-3-methoxyphenoxy]propan-2-yl] 2,3-dihydroxypropanoate Chemical compound OC(C(=O)O[C@H](COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)C)CO JLGLBZBUYGFFHB-SXMXNQBWSA-N 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 229940034982 antineoplastic agent Drugs 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 1
- 208000010217 blepharitis Diseases 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 201000005849 central retinal artery occlusion Diseases 0.000 claims 1
- 201000005667 central retinal vein occlusion Diseases 0.000 claims 1
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 201000011190 diabetic macular edema Diseases 0.000 claims 1
- 208000010643 digestive system disease Diseases 0.000 claims 1
- 208000030172 endocrine system disease Diseases 0.000 claims 1
- SWAFWJVAMSNQLH-RUZDIDTESA-N ethyl (2R)-3-[4-[5-[(5-fluoro-2-methylphenoxy)methyl]-2,2,4-trimethyl-3-oxo-1H-quinoxalin-6-yl]-3-methoxyphenoxy]-2-hydroxypropanoate Chemical compound C(C)OC(=O)[C@@H](COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)O SWAFWJVAMSNQLH-RUZDIDTESA-N 0.000 claims 1
- GNXSSKZHMCHZFG-UHFFFAOYSA-N ethyl 4-[4-[5-[(5-fluoro-2-methylphenoxy)methyl]-2,2,4-trimethyl-3-oxo-1H-quinoxalin-6-yl]-3-methoxyphenoxy]-3-hydroxybutanoate Chemical compound C(C)OC(=O)CC(COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)O GNXSSKZHMCHZFG-UHFFFAOYSA-N 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 229940124750 glucocorticoid receptor agonist Drugs 0.000 claims 1
- 208000019622 heart disease Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000018706 hematopoietic system disease Diseases 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 1
- 201000010666 keratoconjunctivitis Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 208000038015 macular disease Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 208000021971 neovascular inflammatory vitreoretinopathy Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 210000003488 posterior eye segment Anatomy 0.000 claims 1
- 230000006785 proliferative vitreoretinopathy Effects 0.000 claims 1
- 210000001927 retinal artery Anatomy 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 206010039083 rhinitis Diseases 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 201000005671 spondyloarthropathy Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- NNSNQZKFSYVKFX-UHFFFAOYSA-N tert-butyl 4-[4-[5-[(5-fluoro-2-methylphenoxy)methyl]-2,2,4-trimethyl-3-oxo-1H-quinoxalin-6-yl]-3-methoxyphenoxy]-3-hydroxybutanoate Chemical compound C(C)(C)(C)OC(=O)CC(COC1=CC(=C(C=C1)C1=CC=C2NC(C(N(C2=C1COC1=C(C=CC(=C1)F)C)C)=O)(C)C)OC)O NNSNQZKFSYVKFX-UHFFFAOYSA-N 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
- 208000014001 urinary system disease Diseases 0.000 claims 1
- 0 CC1(C)Nc(ccc(-c(ccc(OCC(*)O*)c2)c2OC)c2COc3cc(F)ccc3C)c2N(C)C1=O Chemical compound CC1(C)Nc(ccc(-c(ccc(OCC(*)O*)c2)c2OC)c2COc3cc(F)ccc3C)c2N(C)C1=O 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2015166247 | 2015-08-25 | ||
| JP2015166247 | 2015-08-25 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021089664A Division JP7037687B2 (ja) | 2015-08-25 | 2021-05-28 | ［４－（１，３，３－トリメチル－２－オキソ－３，４－ジヒドロ－１ｈ－キノキサリン－７－イル）フェノキシ］エチルオキシ化合物またはその塩 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017043614A JP2017043614A (ja) | 2017-03-02 |
| JP2017043614A5 true JP2017043614A5 (https=) | 2019-10-03 |
Family
ID=58100493
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016164830A Pending JP2017043614A (ja) | 2015-08-25 | 2016-08-25 | ［４−（１，３，３−トリメチル−２−オキソ−３，４−ジヒドロ−１ｈ−キノキサリン−７−イル）フェノキシ］エチルオキシ化合物またはその塩 |
| JP2021089664A Expired - Fee Related JP7037687B2 (ja) | 2015-08-25 | 2021-05-28 | ［４－（１，３，３－トリメチル－２－オキソ－３，４－ジヒドロ－１ｈ－キノキサリン－７－イル）フェノキシ］エチルオキシ化合物またはその塩 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021089664A Expired - Fee Related JP7037687B2 (ja) | 2015-08-25 | 2021-05-28 | ［４－（１，３，３－トリメチル－２－オキソ－３，４－ジヒドロ－１ｈ－キノキサリン－７－イル）フェノキシ］エチルオキシ化合物またはその塩 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US10189796B2 (https=) |
| EP (1) | EP3342768A4 (https=) |
| JP (2) | JP2017043614A (https=) |
| KR (1) | KR20180043329A (https=) |
| CN (1) | CN107922356A (https=) |
| CA (1) | CA2996278A1 (https=) |
| EA (1) | EA201890570A1 (https=) |
| HK (1) | HK1252159A1 (https=) |
| WO (1) | WO2017034006A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107922356A (zh) * | 2015-08-25 | 2018-04-17 | 参天制药株式会社 | [4‑(1,3,3‑三甲基‑2‑氧代‑3,4‑二氢‑1h‑喹喔啉‑7‑基)苯氧基]乙基氧基化合物或其盐 |
| US20200121652A1 (en) | 2017-06-16 | 2020-04-23 | The Doshisha | Compounds having caspase inhibitory activity, pharmaceutical agent containing said compounds and for treating or preventing corneal endothelial symptoms, disorders, or diseases, and application of said pharmaceutical agent |
| EP3639854B1 (en) | 2017-06-16 | 2026-01-07 | The Doshisha | Mtor-inhibitor-containing medicine for treating or preventing fuchs' endothelial corneal dystrophy |
| AR113967A1 (es) | 2017-12-18 | 2020-07-01 | Gruenenthal Gmbh | Pirrolidinamidas i sustituidas |
| TW201927769A (zh) | 2017-12-18 | 2019-07-16 | 德商歌林達有限公司 | 經取代之吡咯啶醯胺ｉｉ |
| IL280212B2 (en) * | 2018-07-20 | 2023-09-01 | Gruenenthal Chemie | Transmuted triazoloquinoxaline histories |
| TWI811400B (zh) | 2018-07-20 | 2023-08-11 | 德商歌林達有限公司 | 經進一步取代之三唑并喹噁啉衍生物 |
| JP7446316B2 (ja) | 2019-01-11 | 2024-03-08 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 置換ピロリジンアミドｉｉｉ |
| EP3986885B1 (en) | 2019-06-19 | 2023-05-03 | Grünenthal GmbH | Substituted pyrrolidine amides iv |
| EP3986886A2 (en) | 2019-06-19 | 2022-04-27 | Grünenthal GmbH | Substituted pyrrolidine amides v |
| ES3025970T3 (en) * | 2020-01-17 | 2025-06-10 | Gruenenthal Gmbh | Quinoxaline derivatives as modulators of the glucocorticoid receptor |
| WO2021144439A1 (en) * | 2020-01-17 | 2021-07-22 | Grünenthal GmbH | Quinoxaline derivatives |
| WO2022008705A1 (en) | 2020-07-09 | 2022-01-13 | Grünenthal GmbH | Substituted pyrrolidine amines and amides as mediator of the glucocortoid receptor |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60113032T2 (de) | 2000-10-30 | 2006-07-06 | Pfizer Products Inc., Groton | Glukokortikoidrezeptor-Modulatoren |
| EP1995242B1 (en) * | 2006-03-14 | 2012-11-07 | Santen Pharmaceutical Co., Ltd | Novel 1,2,3,4-tetrahydroquinoxaline derivative having glucocorticoid receptor binding activity |
| JP5054996B2 (ja) | 2006-03-14 | 2012-10-24 | 参天製薬株式会社 | グルココルチコイド受容体結合活性を有する新規１，２，３，４−テトラヒドロキノキサリン誘導体 |
| ES2419239T3 (es) * | 2007-05-29 | 2013-08-20 | Santen Pharmaceutical Co., Ltd | Nuevo derivado de 1,2,3,4-tetrahidroquinoxalina que tiene como sustituyente un grupo fenilo con una estructura de éster de ácido sulfónico o una estructura de amida de ácido sulfónico introducida en el mismo y que tienen una actividad de unión al receptor de glucocorticoides |
| JP2009084274A (ja) | 2007-09-13 | 2009-04-23 | Santen Pharmaceut Co Ltd | 新規１，３，３−トリメチル−７−フェニル−３，４−ジヒドロ−１ｈ−キノキサリン−２−オン誘導体 |
| WO2009035067A1 (ja) * | 2007-09-13 | 2009-03-19 | Santen Pharmaceutical Co., Ltd. | １，３，３－トリメチル－７－フェニル－３，４－ジヒドロ－１ｈ－キノキサリン－２－オン誘導体からなるグルココルチコイド受容体アゴニスト |
| KR20110010634A (ko) | 2008-05-12 | 2011-02-01 | 산텐 세이야꾸 가부시키가이샤 | 치환 옥시기를 가지는 2,2,4-트리메틸-6-페닐-1,2-디하이드로퀴놀린 유도체를 포함하는 글루코코르티코이드 수용체 작용제 |
| WO2010029986A1 (ja) * | 2008-09-12 | 2010-03-18 | 参天製薬株式会社 | スルホン酸エステル構造を導入したフェニル基を置換基として有する新規１，２，３，４－テトラヒドロキノキサリン誘導体からなるグルココルチコイド受容体アゴニスト |
| CN107922356A (zh) * | 2015-08-25 | 2018-04-17 | 参天制药株式会社 | [4‑(1,3,3‑三甲基‑2‑氧代‑3,4‑二氢‑1h‑喹喔啉‑7‑基)苯氧基]乙基氧基化合物或其盐 |
-
2016
- 2016-08-25 CN CN201680049254.XA patent/CN107922356A/zh active Pending
- 2016-08-25 HK HK18111552.7A patent/HK1252159A1/zh unknown
- 2016-08-25 US US15/753,410 patent/US10189796B2/en active Active
- 2016-08-25 WO PCT/JP2016/074863 patent/WO2017034006A1/ja not_active Ceased
- 2016-08-25 JP JP2016164830A patent/JP2017043614A/ja active Pending
- 2016-08-25 EP EP16839353.6A patent/EP3342768A4/en not_active Withdrawn
- 2016-08-25 EA EA201890570A patent/EA201890570A1/ru unknown
- 2016-08-25 CA CA2996278A patent/CA2996278A1/en not_active Abandoned
- 2016-08-25 KR KR1020187008105A patent/KR20180043329A/ko not_active Ceased
-
2018
- 2018-12-05 US US16/210,163 patent/US10435379B2/en not_active Expired - Fee Related
-
2019
- 2019-08-06 US US16/532,533 patent/US20190359577A1/en not_active Abandoned
-
2021
- 2021-05-28 JP JP2021089664A patent/JP7037687B2/ja not_active Expired - Fee Related
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