JP2019526589A5 - - Google Patents
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- JP2019526589A5 JP2019526589A5 JP2019512639A JP2019512639A JP2019526589A5 JP 2019526589 A5 JP2019526589 A5 JP 2019526589A5 JP 2019512639 A JP2019512639 A JP 2019512639A JP 2019512639 A JP2019512639 A JP 2019512639A JP 2019526589 A5 JP2019526589 A5 JP 2019526589A5
- Authority
- JP
- Japan
- Prior art keywords
- acid
- small molecule
- disease
- loxl2 inhibitor
- inhibitor according
- 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.)
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- 101001043352 Homo sapiens Lysyl oxidase homolog 2 Proteins 0.000 claims 57
- 102100021948 Lysyl oxidase homolog 2 Human genes 0.000 claims 57
- 239000003112 inhibitor Substances 0.000 claims 53
- 150000003384 small molecules Chemical class 0.000 claims 53
- 239000002253 acid Substances 0.000 claims 31
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 16
- 201000010099 disease Diseases 0.000 claims 14
- 208000019423 liver disease Diseases 0.000 claims 14
- 206010016654 Fibrosis Diseases 0.000 claims 11
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 10
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 10
- 208000019693 Lung disease Diseases 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 8
- 241000124008 Mammalia Species 0.000 claims 8
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 8
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 8
- 201000010063 epididymitis Diseases 0.000 claims 8
- 230000004761 fibrosis Effects 0.000 claims 8
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 8
- 208000019425 cirrhosis of liver Diseases 0.000 claims 7
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 6
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 6
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 6
- FUZZWVXGSFPDMH-UHFFFAOYSA-N hexanoic acid Chemical compound CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 claims 6
- 208000017169 kidney disease Diseases 0.000 claims 6
- WSFSSNUMVMOOMR-BJUDXGSMSA-N methanone Chemical compound O=[11CH2] WSFSSNUMVMOOMR-BJUDXGSMSA-N 0.000 claims 6
- 206010028537 myelofibrosis Diseases 0.000 claims 6
- 206010061218 Inflammation Diseases 0.000 claims 5
- 230000004054 inflammatory process Effects 0.000 claims 5
- 239000012453 solvate Substances 0.000 claims 5
- QBYIENPQHBMVBV-HFEGYEGKSA-N (2R)-2-hydroxy-2-phenylacetic acid Chemical compound O[C@@H](C(O)=O)c1ccccc1.O[C@@H](C(O)=O)c1ccccc1 QBYIENPQHBMVBV-HFEGYEGKSA-N 0.000 claims 4
- LBLYYCQCTBFVLH-UHFFFAOYSA-N 2-Methylbenzenesulfonic acid Chemical compound CC1=CC=CC=C1S(O)(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-N 0.000 claims 4
- 208000007082 Alcoholic Fatty Liver Diseases 0.000 claims 4
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 4
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 claims 4
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims 4
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 4
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 claims 4
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 claims 4
- 208000026594 alcoholic fatty liver disease Diseases 0.000 claims 4
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 4
- JXTHNDFMNIQAHM-UHFFFAOYSA-N dichloroacetic acid Chemical compound OC(=O)C(Cl)Cl JXTHNDFMNIQAHM-UHFFFAOYSA-N 0.000 claims 4
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 4
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 claims 4
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 claims 4
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 4
- SUMDYPCJJOFFON-UHFFFAOYSA-N isethionic acid Chemical compound OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 0.000 claims 4
- KQNPFQTWMSNSAP-UHFFFAOYSA-N isobutyric acid Chemical compound CC(C)C(O)=O KQNPFQTWMSNSAP-UHFFFAOYSA-N 0.000 claims 4
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 4
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims 4
- 208000011580 syndromic disease Diseases 0.000 claims 4
- -1 3-((4- (aminomethyl) -6- (trifluoromethyl) pyridin-2-yl) oxy) phenyl Chemical group 0.000 claims 3
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 3
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 3
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 3
- 208000003167 cholangitis Diseases 0.000 claims 3
- 230000007882 cirrhosis Effects 0.000 claims 3
- 210000001508 eye Anatomy 0.000 claims 3
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 3
- 201000004595 synovitis Diseases 0.000 claims 3
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims 2
- MIOPJNTWMNEORI-GMSGAONNSA-N (S)-camphorsulfonic acid Chemical compound C1C[C@@]2(CS(O)(=O)=O)C(=O)C[C@@H]1C2(C)C MIOPJNTWMNEORI-GMSGAONNSA-N 0.000 claims 2
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims 2
- SJJCQDRGABAVBB-UHFFFAOYSA-N 1-hydroxy-2-naphthoic acid Chemical compound C1=CC=CC2=C(O)C(C(=O)O)=CC=C21 SJJCQDRGABAVBB-UHFFFAOYSA-N 0.000 claims 2
- RTBFRGCFXZNCOE-UHFFFAOYSA-N 1-methylsulfonylpiperidin-4-one Chemical compound CS(=O)(=O)N1CCC(=O)CC1 RTBFRGCFXZNCOE-UHFFFAOYSA-N 0.000 claims 2
- KPGXRSRHYNQIFN-UHFFFAOYSA-N 2-oxoglutaric acid Chemical compound OC(=O)CCC(=O)C(O)=O KPGXRSRHYNQIFN-UHFFFAOYSA-N 0.000 claims 2
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims 2
- AEMOLEFTQBMNLQ-UHFFFAOYSA-N 3,4,5,6-tetrahydroxyoxane-2-carboxylic acid Chemical compound OC1OC(C(O)=O)C(O)C(O)C1O AEMOLEFTQBMNLQ-UHFFFAOYSA-N 0.000 claims 2
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 claims 2
- UOQHWNPVNXSDDO-UHFFFAOYSA-N 3-bromoimidazo[1,2-a]pyridine-6-carbonitrile Chemical compound C1=CC(C#N)=CN2C(Br)=CN=C21 UOQHWNPVNXSDDO-UHFFFAOYSA-N 0.000 claims 2
- WUBBRNOQWQTFEX-UHFFFAOYSA-N 4-aminosalicylic acid Chemical compound NC1=CC=C(C(O)=O)C(O)=C1 WUBBRNOQWQTFEX-UHFFFAOYSA-N 0.000 claims 2
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 2
- 208000009304 Acute Kidney Injury Diseases 0.000 claims 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 2
- WWZKQHOCKIZLMA-UHFFFAOYSA-N Caprylic acid Natural products CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 claims 2
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 2
- 241000723347 Cinnamomum Species 0.000 claims 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- YVECGMZCTULTIS-HSUXUTPPSA-N D-galactal Chemical compound OC[C@H]1OC=C[C@@H](O)[C@H]1O YVECGMZCTULTIS-HSUXUTPPSA-N 0.000 claims 2
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 claims 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 2
- 208000004145 Endometritis Diseases 0.000 claims 2
- 208000004232 Enteritis Diseases 0.000 claims 2
- RGHNJXZEOKUKBD-SQOUGZDYSA-N Gluconic acid Natural products OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 claims 2
- 208000031071 Hamman-Rich Syndrome Diseases 0.000 claims 2
- 241000711549 Hepacivirus C Species 0.000 claims 2
- 206010019799 Hepatitis viral Diseases 0.000 claims 2
- 208000002972 Hepatolenticular Degeneration Diseases 0.000 claims 2
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 2
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 2
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 2
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-L L-tartrate(2-) Chemical compound [O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O FEWJPZIEWOKRBE-JCYAYHJZSA-L 0.000 claims 2
- 239000005639 Lauric acid Substances 0.000 claims 2
- 208000009525 Myocarditis Diseases 0.000 claims 2
- 229910002651 NO3 Inorganic materials 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims 2
- 239000005642 Oleic acid Substances 0.000 claims 2
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims 2
- 229910019142 PO4 Inorganic materials 0.000 claims 2
- 235000021314 Palmitic acid Nutrition 0.000 claims 2
- 206010035664 Pneumonia Diseases 0.000 claims 2
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 2
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 2
- IWYDHOAUDWTVEP-UHFFFAOYSA-N R-2-phenyl-2-hydroxyacetic acid Natural products OC(=O)C(O)C1=CC=CC=C1 IWYDHOAUDWTVEP-UHFFFAOYSA-N 0.000 claims 2
- 208000033626 Renal failure acute Diseases 0.000 claims 2
- 206010038933 Retinopathy of prematurity Diseases 0.000 claims 2
- 206010039710 Scleroderma Diseases 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 2
- 206010042953 Systemic sclerosis Diseases 0.000 claims 2
- 208000018839 Wilson disease Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 201000004073 acute interstitial pneumonia Diseases 0.000 claims 2
- 201000011040 acute kidney failure Diseases 0.000 claims 2
- 239000001361 adipic acid Substances 0.000 claims 2
- 235000011037 adipic acid Nutrition 0.000 claims 2
- 206010064930 age-related macular degeneration Diseases 0.000 claims 2
- 230000001476 alcoholic effect Effects 0.000 claims 2
- AWUCVROLDVIAJX-UHFFFAOYSA-N alpha-glycerophosphate Natural products OCC(O)COP(O)(O)=O AWUCVROLDVIAJX-UHFFFAOYSA-N 0.000 claims 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 2
- 229960004909 aminosalicylic acid Drugs 0.000 claims 2
- JFCQEDHGNNZCLN-UHFFFAOYSA-N anhydrous glutaric acid Natural products OC(=O)CCCC(O)=O JFCQEDHGNNZCLN-UHFFFAOYSA-N 0.000 claims 2
- 235000010323 ascorbic acid Nutrition 0.000 claims 2
- 229960005070 ascorbic acid Drugs 0.000 claims 2
- 239000011668 ascorbic acid Substances 0.000 claims 2
- 235000003704 aspartic acid Nutrition 0.000 claims 2
- YINMBLWEHNCLFF-UHFFFAOYSA-N benzenesulfonic acid;benzoic acid Chemical compound OC(=O)C1=CC=CC=C1.OS(=O)(=O)C1=CC=CC=C1 YINMBLWEHNCLFF-UHFFFAOYSA-N 0.000 claims 2
- GONOPSZTUGRENK-UHFFFAOYSA-N benzyl(trichloro)silane Chemical compound Cl[Si](Cl)(Cl)CC1=CC=CC=C1 GONOPSZTUGRENK-UHFFFAOYSA-N 0.000 claims 2
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 2
- RLDQYSHDFVSAPL-UHFFFAOYSA-L calcium;dithiocyanate Chemical compound [Ca+2].[S-]C#N.[S-]C#N RLDQYSHDFVSAPL-UHFFFAOYSA-L 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000001569 carbon dioxide Substances 0.000 claims 2
- 229910002092 carbon dioxide Inorganic materials 0.000 claims 2
- 235000017803 cinnamon Nutrition 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 201000009805 cryptogenic organizing pneumonia Diseases 0.000 claims 2
- 239000000625 cyclamic acid and its Na and Ca salt Substances 0.000 claims 2
- HCAJEUSONLESMK-UHFFFAOYSA-N cyclohexylsulfamic acid Chemical compound OS(=O)(=O)NC1CCCCC1 HCAJEUSONLESMK-UHFFFAOYSA-N 0.000 claims 2
- HABLENUWIZGESP-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O.CCCCCCCCCC(O)=O HABLENUWIZGESP-UHFFFAOYSA-N 0.000 claims 2
- NXMUXTAGFPJGTQ-UHFFFAOYSA-N decanoic acid;octanoic acid Chemical compound CCCCCCCC(O)=O.CCCCCCCCCC(O)=O NXMUXTAGFPJGTQ-UHFFFAOYSA-N 0.000 claims 2
- 201000001981 dermatomyositis Diseases 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- MOTZDAYCYVMXPC-UHFFFAOYSA-N dodecyl hydrogen sulfate Chemical compound CCCCCCCCCCCCOS(O)(=O)=O MOTZDAYCYVMXPC-UHFFFAOYSA-N 0.000 claims 2
- 229940043264 dodecyl sulfate Drugs 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- RATDTFKSUHXONC-UHFFFAOYSA-N ethanesulfonic acid;formic acid Chemical compound OC=O.CCS(O)(=O)=O RATDTFKSUHXONC-UHFFFAOYSA-N 0.000 claims 2
- 239000001530 fumaric acid Substances 0.000 claims 2
- NKHAVTQWNUWKEO-UHFFFAOYSA-N fumaric acid monomethyl ester Natural products COC(=O)C=CC(O)=O NKHAVTQWNUWKEO-UHFFFAOYSA-N 0.000 claims 2
- 239000000174 gluconic acid Substances 0.000 claims 2
- 235000012208 gluconic acid Nutrition 0.000 claims 2
- 229930195712 glutamate Natural products 0.000 claims 2
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims 2
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 2
- 229940099563 lactobionic acid Drugs 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 201000003265 lymphadenitis Diseases 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 239000011976 maleic acid Substances 0.000 claims 2
- 239000001630 malic acid Substances 0.000 claims 2
- 235000011090 malic acid Nutrition 0.000 claims 2
- 229960002510 mandelic acid Drugs 0.000 claims 2
- 125000005341 metaphosphate group Chemical group 0.000 claims 2
- 229940098779 methanesulfonic acid Drugs 0.000 claims 2
- NKHAVTQWNUWKEO-NSCUHMNNSA-N monomethyl fumarate Chemical compound COC(=O)\C=C\C(O)=O NKHAVTQWNUWKEO-NSCUHMNNSA-N 0.000 claims 2
- 229940005650 monomethyl fumarate Drugs 0.000 claims 2
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 claims 2
- 201000008383 nephritis Diseases 0.000 claims 2
- 235000001968 nicotinic acid Nutrition 0.000 claims 2
- 229960003512 nicotinic acid Drugs 0.000 claims 2
- 239000011664 nicotinic acid Substances 0.000 claims 2
- 201000004071 non-specific interstitial pneumonia Diseases 0.000 claims 2
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- WLJNZVDCPSBLRP-UHFFFAOYSA-N pamoic acid Chemical compound C1=CC=C2C(CC=3C4=CC=CC=C4C=C(C=3O)C(=O)O)=C(O)C(C(O)=O)=CC2=C1 WLJNZVDCPSBLRP-UHFFFAOYSA-N 0.000 claims 2
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims 2
- 206010034674 peritonitis Diseases 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 2
- 239000010452 phosphate Substances 0.000 claims 2
- WSHYKIAQCMIPTB-UHFFFAOYSA-M potassium;2-oxo-3-(3-oxo-1-phenylbutyl)chromen-4-olate Chemical compound [K+].[O-]C=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 WSHYKIAQCMIPTB-UHFFFAOYSA-M 0.000 claims 2
- 208000003476 primary myelofibrosis Diseases 0.000 claims 2
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- 235000019260 propionic acid Nutrition 0.000 claims 2
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 2
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 229960004889 salicylic acid Drugs 0.000 claims 2
- AWUCVROLDVIAJX-GSVOUGTGSA-N sn-glycerol 3-phosphate Chemical compound OC[C@@H](O)COP(O)(O)=O AWUCVROLDVIAJX-GSVOUGTGSA-N 0.000 claims 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 2
- 229940095064 tartrate Drugs 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 201000001862 viral hepatitis Diseases 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- WWGCKRAFNGJJGY-UHFFFAOYSA-N 3-fluoro-4-hydroxypyrrolidine-1-carbaldehyde Chemical compound FC1CN(CC1O)C=O WWGCKRAFNGJJGY-UHFFFAOYSA-N 0.000 claims 1
- 208000007122 AIDS-Associated Nephropathy Diseases 0.000 claims 1
- 208000026872 Addison Disease Diseases 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 208000024985 Alport syndrome Diseases 0.000 claims 1
- 206010001881 Alveolar proteinosis Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 208000003343 Antiphospholipid Syndrome Diseases 0.000 claims 1
- 206010003694 Atrophy Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 206010009346 Clonus Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 206010010996 Corneal degeneration Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 201000003066 Diffuse Scleroderma Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 208000007882 Gastritis Diseases 0.000 claims 1
- 208000005577 Gastroenteritis Diseases 0.000 claims 1
- 206010061979 Genital pain Diseases 0.000 claims 1
- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000024869 Goodpasture syndrome Diseases 0.000 claims 1
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Family Cites Families (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4229447A (en) | 1979-06-04 | 1980-10-21 | American Home Products Corporation | Intraoral methods of using benzodiazepines |
| IE56702B1 (en) | 1982-12-01 | 1991-11-06 | Usv Pharma Corp | Antiinflammatory antiallergic compounds |
| US4596795A (en) | 1984-04-25 | 1986-06-24 | The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services | Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives |
| US4755386A (en) | 1986-01-22 | 1988-07-05 | Schering Corporation | Buccal formulation |
| US5021456A (en) | 1988-02-25 | 1991-06-04 | Merrell Dow Pharmaceuticals Inc. | Inhibitors of lysyl oxidase |
| US5739136A (en) | 1989-10-17 | 1998-04-14 | Ellinwood, Jr.; Everett H. | Intraoral dosing method of administering medicaments |
| US5250532A (en) | 1991-04-11 | 1993-10-05 | Dowelanco | 3,4,N-trisubstituted-4,5-dihydro-1H-pyrazole-1-carboxamides and their use as insecticides |
| US5563143A (en) | 1994-09-21 | 1996-10-08 | Pfizer Inc. | Catechol diether compounds as inhibitors of TNF release |
| US5691364A (en) | 1995-03-10 | 1997-11-25 | Berlex Laboratories, Inc. | Benzamidine derivatives and their use as anti-coagulants |
| US7125880B1 (en) | 1995-06-06 | 2006-10-24 | Pfizer Inc. | Corticotropin releasing factor antagonists |
| US6956047B1 (en) | 1995-06-06 | 2005-10-18 | Pfizer Inc. | Corticotropin releasing factor antagonists |
| US6632823B1 (en) | 1997-12-22 | 2003-10-14 | Merck & Co., Inc. | Substituted pyridine compounds useful as modulators of acetylcholine receptors |
| PL357589A1 (en) | 2000-01-18 | 2004-07-26 | Pfizer Products Inc. | Corticotropin releasing factor antagonists |
| US20030134836A1 (en) | 2001-01-12 | 2003-07-17 | Amgen Inc. | Substituted arylamine derivatives and methods of use |
| US7105682B2 (en) | 2001-01-12 | 2006-09-12 | Amgen Inc. | Substituted amine derivatives and methods of use |
| US6878714B2 (en) | 2001-01-12 | 2005-04-12 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
| US7102009B2 (en) | 2001-01-12 | 2006-09-05 | Amgen Inc. | Substituted amine derivatives and methods of use |
| US20020147198A1 (en) | 2001-01-12 | 2002-10-10 | Guoqing Chen | Substituted arylamine derivatives and methods of use |
| US6995162B2 (en) | 2001-01-12 | 2006-02-07 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
| TWI319387B (en) | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
| US7307088B2 (en) | 2002-07-09 | 2007-12-11 | Amgen Inc. | Substituted anthranilic amide derivatives and methods of use |
| FI20030030A0 (fi) | 2003-01-09 | 2003-01-09 | Orion Corp | Uusia yhdisteitä |
| WO2004103309A2 (en) | 2003-05-19 | 2004-12-02 | Irm Llc | Immunosuppressant compounds and compositions |
| JP2007519705A (ja) | 2004-01-29 | 2007-07-19 | ファイザー・プロダクツ・インク | Ｃｎｓ障害を治療するための非定型抗精神病薬とアミノメチルピリジルオキシメチル／ベンゾイソオキサゾールアザビシクロ誘導体の組合せ |
| CA2558568A1 (en) | 2004-03-12 | 2005-09-29 | Eli Lilly And Company | Opioid receptor antagonists |
| US7378448B2 (en) | 2004-03-15 | 2008-05-27 | Eli Lilly And Company | Diphenylether amide derivatives as opioid receptor antagonists |
| AU2005238386A1 (en) | 2004-04-30 | 2005-11-10 | Takeda Pharmaceutical Company Limited | Heterocyclic amide compound and use thereof as an MMP-13 inhibitor |
| US7507748B2 (en) | 2004-07-22 | 2009-03-24 | Amgen Inc. | Substituted aryl-amine derivatives and methods of use |
| EP1791541A2 (en) | 2004-09-10 | 2007-06-06 | Pfizer Products Inc. | Methods of treating mood disorders using benzisoxazole containing diazabicyclic compounds |
| US20070270430A1 (en) | 2004-09-10 | 2007-11-22 | Pfzer Inc | Methods of Treating Cognitive Disorders Using Pyridyloxymethyl and Benzisoxazole Azabicyclic Derivatives |
| EP1807417A2 (en) | 2004-11-04 | 2007-07-18 | Neurogen Corporation | Pyrazolylmethyl heteroaryl derivatives |
| DE102004056226A1 (de) | 2004-11-22 | 2006-05-24 | Burchardt, Elmar Reinhold, Dr.Dr. | Neuartige Inhibitoren der Lysyloxidase |
| ATE440091T1 (de) | 2005-01-31 | 2009-09-15 | Merck & Co Inc | Antidiabetische bicyclische verbindungen |
| AR055041A1 (es) | 2005-03-23 | 2007-08-01 | Merck Frosst Canada Ltd | Tiadiazoles y oxadiazoles como inhibidores de la sintesis de leucotrienos. composiciones farmaceuticas. |
| AU2006279211A1 (en) | 2005-08-11 | 2007-02-15 | Merck Frosst Canada Ltd | Novel substituted 1,2,3-triazolylmethyl-benzothiophene or -indole and their use as leukotriene biosynthesis inhibitors |
| US7405302B2 (en) | 2005-10-11 | 2008-07-29 | Amira Pharmaceuticals, Inc. | 5-lipoxygenase-activating protein (FLAP) inhibitors |
| ITMI20051943A1 (it) | 2005-10-14 | 2007-04-15 | Procos Spa | Processo di risoluzione anantiomerica di 2-aminometil-pirrolidine 1-sostitute per ammidazione in presenza di lipasi |
| US7977359B2 (en) | 2005-11-04 | 2011-07-12 | Amira Pharmaceuticals, Inc. | 5-lipdxygenase-activating protein (FLAP) inhibitors |
| US20070225285A1 (en) | 2005-11-04 | 2007-09-27 | Amira Pharmaceuticals, Inc. | 5-lipoxygenase-activating protein (flap) inhibitors |
| US20070219206A1 (en) | 2005-11-04 | 2007-09-20 | Amira Pharmaceuticals, Inc. | 5-lipoxygenase-activating protein (flap) inhibitors |
| CA2636043A1 (en) | 2006-01-23 | 2007-08-02 | Amira Pharmaceuticals, Inc. | Tricyclic inhibitors of 5-lipoxygenase |
| GB0614579D0 (en) | 2006-07-21 | 2006-08-30 | Black James Foundation | Pyrimidine derivatives |
| EP2121703A4 (en) | 2006-08-18 | 2011-12-28 | Astrazeneca Ab | THIENOPYRIMIDIN-4-ON- AND THIENOPYRIDAZIN-7-ONDERIVATES AS MCH-RL ANTAGONISTS |
| WO2008070616A2 (en) * | 2006-12-01 | 2008-06-12 | University Of Utah Research Foundation | METHODS AND COMPOSITIONS RELATED TO HIF-1α |
| IL184627A0 (en) | 2007-07-15 | 2008-12-29 | Technion Res & Dev Foundation | Agents for diagnosing and modulating metastasis and fibrosis as well as inflammation in a mammalian tissue |
| WO2009035791A1 (en) | 2007-08-02 | 2009-03-19 | Arresto Biosciences | Lox and l0xl2 inhibitors and uses thereof |
| RU2012107163A (ru) | 2009-07-28 | 2013-09-10 | Анакор Фармасьютикалз, Инк. | Тризамещенные борсодержащие молекулы |
| MX2012002271A (es) * | 2009-08-21 | 2012-07-20 | Gilead Biologics Inc | Metodos y composiciones terapeuticas. |
| KR20130008021A (ko) * | 2010-02-04 | 2013-01-21 | 길리아드 바이오로직스, 인크. | 리실 산화효소-유사 2 (ｌｏｘｌ2)에 결합하는 항체, 및 그를 위한 사용 방법 |
| JP2013518909A (ja) | 2010-02-08 | 2013-05-23 | キナゲン，インク． | アロステリックキナーゼ阻害が関係する治療方法および組成物 |
| JP5816635B2 (ja) | 2010-03-05 | 2015-11-18 | カリオファーム セラピューティクス，インコーポレイテッド | 核輸送調節剤およびその使用 |
| WO2011150201A2 (en) | 2010-05-27 | 2011-12-01 | Ambit Biosciences Corporation | Azolyl amide compounds and methods of use thereof |
| EP2441755A1 (en) | 2010-09-30 | 2012-04-18 | Almirall, S.A. | Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors |
| CA2818542A1 (en) * | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| ES2627347T3 (es) | 2011-10-20 | 2017-07-27 | Glaxosmithkline Llc | Aza-heterociclos bicíclicos sustituidos y análogos como moduladores de sirtuina |
| EP2841421B1 (en) | 2012-04-25 | 2019-06-05 | RaQualia Pharma Inc | Amide derivatives as ttx-s blockers |
| JP2016500700A (ja) * | 2012-10-30 | 2016-01-14 | ギリアード サイエンシーズ， インコーポレイテッド | リシルオキシダーゼ様２（ｌｏｘｌ２）に関する治療および診断方法 |
| CN104854086B (zh) | 2012-12-18 | 2017-06-27 | Ea制药株式会社 | 杂环酰胺衍生物和含有其的药物 |
| JP2018522812A (ja) | 2014-08-05 | 2018-08-16 | ザ ユニヴァーシティ オブ ブリティッシュ コロンビア | カスパーゼ−６のモジュレーター |
| US9051320B1 (en) * | 2014-08-18 | 2015-06-09 | Pharmakea, Inc. | Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor |
| PT3256463T (pt) | 2015-02-15 | 2019-12-05 | Hoffmann La Roche | Derivados de 1-(het)arilsulfonil-(pirrolidina ou piperidina)-2-carboxamida e a sua utilização como antagonistas do trpa1 |
| ES2872553T3 (es) | 2015-03-06 | 2021-11-02 | Pharmakea Inc | Inhibidores de lisil oxidasa tipo-2 y usos de los mismos |
| KR102594441B1 (ko) * | 2015-03-06 | 2023-10-25 | 파마케아, 인크. | 플루오르화된 리실 옥시다아제-유사 2 억제제 및 이의 용도 |
| US10774069B2 (en) | 2016-09-07 | 2020-09-15 | Pharmakea, Inc. | Crystalline forms of a lysyl oxidase-like 2 inhibitor and methods of making |
| BR112019004513A2 (pt) | 2016-09-07 | 2019-06-18 | Pharmakea Inc | usos de um inibidor de lisil oxidase-like 2 |
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- 2017-09-06 EP EP17849478.7A patent/EP3509594B1/en active Active
- 2017-09-06 CA CA3036062A patent/CA3036062A1/en active Pending
- 2017-09-06 MX MX2019002612A patent/MX2019002612A/es unknown
- 2017-09-06 CN CN201780068871.9A patent/CN109922803B/zh active Active
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2019
- 2019-03-06 IL IL265232A patent/IL265232A/en unknown
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2021
- 2021-02-03 US US17/166,689 patent/US20210177820A1/en not_active Abandoned
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2024
- 2024-08-27 US US18/816,195 patent/US20240415824A1/en active Pending