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 (enExample) | 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 (enExample) |
| EP (1) | EP3342768A4 (enExample) |
| JP (2) | JP2017043614A (enExample) |
| KR (1) | KR20180043329A (enExample) |
| CN (1) | CN107922356A (enExample) |
| CA (1) | CA2996278A1 (enExample) |
| EA (1) | EA201890570A1 (enExample) |
| HK (1) | HK1252159A1 (enExample) |
| WO (1) | WO2017034006A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3342768A4 (en) * | 2015-08-25 | 2019-01-23 | Santen Pharmaceutical Co., Ltd. | [4- (1,3,3-TRIMETHYL-2-OXO-3,4-DIHYDRO-1H-CHINOXALIN-7-YL) PHENOXY] ETHYLOXY COMPOUND OR SALT THEREOF |
| CN110944668A (zh) | 2017-06-16 | 2020-03-31 | 学校法人同志社 | 用于治疗或预防眼部症状、障碍或疾病的包含mTOR抑制剂的药物及其应用 |
| JPWO2018230713A1 (ja) | 2017-06-16 | 2020-04-16 | 学校法人同志社 | カスパーゼ阻害活性を有する化合物、これらの化合物を含む、角膜内皮の症状、障害または疾患を治療または予防するための医薬およびその応用 |
| CN111556867A (zh) | 2017-12-18 | 2020-08-18 | 格吕伦塔尔有限公司 | 经取代的吡咯烷酰胺i |
| 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 |
| AR117951A1 (es) | 2018-07-20 | 2021-09-08 | Gruenenthal Gmbh | Derivados de triazolquinoxalina adicionalmente sustituidos |
| LT3823971T (lt) | 2018-07-20 | 2022-09-12 | Grünenthal GmbH | Pakeisti triazolo chinoksalino dariniai |
| CN113382990B (zh) | 2019-01-11 | 2024-11-19 | 格吕伦塔尔有限公司 | 取代的吡咯烷酰胺iii |
| EP3986886A2 (en) | 2019-06-19 | 2022-04-27 | Grünenthal GmbH | Substituted pyrrolidine amides v |
| EP3986885B1 (en) | 2019-06-19 | 2023-05-03 | Grünenthal GmbH | Substituted pyrrolidine amides iv |
| EP4090660B1 (en) | 2020-01-17 | 2024-01-31 | Grünenthal GmbH | Quinoxaline derivatives |
| EP4090661B1 (en) | 2020-01-17 | 2025-03-12 | Grünenthal GmbH | Quinoxaline derivatives as modulators of the glucocorticoid receptor |
| EP4178954B1 (en) | 2020-07-09 | 2025-11-19 | Grünenthal GmbH | Substituted pyrrolidine amines and amides as mediator of the glucocortoid receptor |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2246292T3 (es) | 2000-10-30 | 2006-02-16 | Pfizer Products Inc. | Moduladores de receptor glucocorticoide. |
| SI1995242T1 (sl) * | 2006-03-14 | 2013-01-31 | Santen Pharmaceutical Co., Ltd. | Nov derivat 1,2,3,4-tetrahidrokinoksalina z aktivnostjo vezanja glukokortikoidnega receptorja |
| 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 |
| CA2687948A1 (en) * | 2007-05-29 | 2008-12-04 | Mamoru Matsuda | Novel 1,2,3,4-tetrahydroquinoxaline derivative which has, as substituent, phenyl group having sulfonic acid ester structure or sulfonic acid amide structure introduced therein andhas glucocorticoid receptor-binding activity |
| 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 |
| JP2009084273A (ja) | 2007-09-13 | 2009-04-23 | Santen Pharmaceut 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 |
| EA018420B1 (ru) | 2008-09-12 | 2013-07-30 | Сантен Фармасьютикал Ко., Лтд. | Агонист глюкокортикоидного рецептора, содержащий новые производные 1,2,3,4-тетрагидрохиноксалина с фенильной группой, имеющей структуру эфира сульфоновой кислоты, введенной в нее в качестве заместителя |
| EP3342768A4 (en) * | 2015-08-25 | 2019-01-23 | Santen Pharmaceutical Co., Ltd. | [4- (1,3,3-TRIMETHYL-2-OXO-3,4-DIHYDRO-1H-CHINOXALIN-7-YL) PHENOXY] ETHYLOXY COMPOUND OR SALT THEREOF |
-
2016
- 2016-08-25 EP EP16839353.6A patent/EP3342768A4/en not_active Withdrawn
- 2016-08-25 CN CN201680049254.XA patent/CN107922356A/zh active Pending
- 2016-08-25 HK HK18111552.7A patent/HK1252159A1/zh unknown
- 2016-08-25 EA EA201890570A patent/EA201890570A1/ru unknown
- 2016-08-25 US US15/753,410 patent/US10189796B2/en active Active
- 2016-08-25 JP JP2016164830A patent/JP2017043614A/ja active Pending
- 2016-08-25 WO PCT/JP2016/074863 patent/WO2017034006A1/ja not_active Ceased
- 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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