ES2658064T3 - Moduladores de isoquinolina de transportadores de casete de unión a ATP - Google Patents
Moduladores de isoquinolina de transportadores de casete de unión a ATP Download PDFInfo
- Publication number
- ES2658064T3 ES2658064T3 ES15180766.6T ES15180766T ES2658064T3 ES 2658064 T3 ES2658064 T3 ES 2658064T3 ES 15180766 T ES15180766 T ES 15180766T ES 2658064 T3 ES2658064 T3 ES 2658064T3
- Authority
- ES
- Spain
- Prior art keywords
- aliphatic
- carbonyl
- cycloaliphatic
- heterocycloaliphatic
- aryl
- 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.)
- Active
Links
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 title 2
- 108010006533 ATP-Binding Cassette Transporters Proteins 0.000 title 1
- 102000005416 ATP-Binding Cassette Transporters Human genes 0.000 title 1
- 125000001931 aliphatic group Chemical group 0.000 abstract description 96
- 125000001072 heteroaryl group Chemical group 0.000 abstract description 86
- 125000003118 aryl group Chemical group 0.000 abstract description 84
- -1 sulfoxy Chemical group 0.000 abstract description 81
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract description 65
- 125000000217 alkyl group Chemical group 0.000 abstract description 60
- 125000001424 substituent group Chemical group 0.000 abstract description 56
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract description 46
- 125000003545 alkoxy group Chemical group 0.000 abstract description 36
- 229910052739 hydrogen Inorganic materials 0.000 abstract description 36
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract description 33
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 abstract description 29
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract description 26
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 abstract description 25
- 125000003368 amide group Chemical group 0.000 abstract description 25
- 125000004093 cyano group Chemical group *C#N 0.000 abstract description 23
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract description 22
- 125000002252 acyl group Chemical group 0.000 abstract description 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract description 20
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 abstract description 20
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract description 20
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract description 19
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 abstract description 19
- 125000003396 thiol group Chemical group [H]S* 0.000 abstract description 19
- 125000003342 alkenyl group Chemical group 0.000 abstract description 18
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract description 18
- 125000000304 alkynyl group Chemical group 0.000 abstract description 18
- 125000000753 cycloalkyl group Chemical group 0.000 abstract description 18
- 125000004043 oxo group Chemical group O=* 0.000 abstract description 18
- 125000003435 aroyl group Chemical group 0.000 abstract description 17
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract description 17
- 125000004104 aryloxy group Chemical group 0.000 abstract description 15
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract description 15
- 239000001257 hydrogen Substances 0.000 abstract description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract description 14
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract description 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract description 13
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 abstract description 12
- 125000002619 bicyclic group Chemical group 0.000 abstract description 12
- 150000001875 compounds Chemical class 0.000 abstract description 11
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 abstract description 10
- NWGPLYYBECWONP-UHFFFAOYSA-N (carbamoylamino) hydrogen sulfate Chemical compound NC(=O)NOS(O)(=O)=O NWGPLYYBECWONP-UHFFFAOYSA-N 0.000 abstract description 9
- 125000004414 alkyl thio group Chemical group 0.000 abstract description 9
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract description 9
- NVBFHJWHLNUMCV-UHFFFAOYSA-N sulfamide Chemical compound NS(N)(=O)=O NVBFHJWHLNUMCV-UHFFFAOYSA-N 0.000 abstract description 9
- 125000004432 carbon atom Chemical group C* 0.000 abstract description 8
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract description 7
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract description 7
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 abstract description 6
- 125000003107 substituted aryl group Chemical group 0.000 abstract description 6
- 229940124530 sulfonamide Drugs 0.000 abstract description 6
- 150000003456 sulfonamides Chemical class 0.000 abstract description 6
- 125000004658 aryl carbonyl amino group Chemical group 0.000 abstract description 5
- 125000004391 aryl sulfonyl group Chemical group 0.000 abstract description 5
- 239000004202 carbamide Substances 0.000 abstract description 5
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract description 5
- 238000000034 method Methods 0.000 abstract description 5
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract description 4
- 125000005129 aryl carbonyl group Chemical group 0.000 abstract description 4
- 125000004644 alkyl sulfinyl group Chemical group 0.000 abstract description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract description 3
- 229910052799 carbon Inorganic materials 0.000 abstract description 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract description 2
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract description 2
- TXKMVPPZCYKFAC-UHFFFAOYSA-N disulfur monoxide Chemical compound O=S=S TXKMVPPZCYKFAC-UHFFFAOYSA-N 0.000 abstract 8
- 125000001475 halogen functional group Chemical group 0.000 abstract 7
- 201000010099 disease Diseases 0.000 abstract 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 5
- 230000007812 deficiency Effects 0.000 abstract 3
- 206010012601 diabetes mellitus Diseases 0.000 abstract 3
- 206010006474 Bronchopulmonary aspergillosis allergic Diseases 0.000 abstract 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 2
- 206010033645 Pancreatitis Diseases 0.000 abstract 2
- 208000006778 allergic bronchopulmonary aspergillosis Diseases 0.000 abstract 2
- 102100034452 Alternative prion protein Human genes 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 206010003591 Ataxia Diseases 0.000 abstract 1
- 206010003694 Atrophy Diseases 0.000 abstract 1
- 206010006458 Bronchitis chronic Diseases 0.000 abstract 1
- 201000004807 Char syndrome Diseases 0.000 abstract 1
- 206010010356 Congenital anomaly Diseases 0.000 abstract 1
- 201000002200 Congenital disorder of glycosylation Diseases 0.000 abstract 1
- 206010062264 Congenital hyperthyroidism Diseases 0.000 abstract 1
- 206010010774 Constipation Diseases 0.000 abstract 1
- 208000020406 Creutzfeldt Jacob disease Diseases 0.000 abstract 1
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 abstract 1
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 abstract 1
- 201000003883 Cystic fibrosis Diseases 0.000 abstract 1
- 206010013883 Dwarfism Diseases 0.000 abstract 1
- 206010014561 Emphysema Diseases 0.000 abstract 1
- 208000024720 Fabry Disease Diseases 0.000 abstract 1
- 201000011240 Frontotemporal dementia Diseases 0.000 abstract 1
- 208000033981 Hereditary haemochromatosis Diseases 0.000 abstract 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 abstract 1
- 208000000563 Hyperlipoproteinemia Type II Diseases 0.000 abstract 1
- 206010051125 Hypofibrinogenaemia Diseases 0.000 abstract 1
- 208000000038 Hypoparathyroidism Diseases 0.000 abstract 1
- 102100024640 Low-density lipoprotein receptor Human genes 0.000 abstract 1
- 208000019693 Lung disease Diseases 0.000 abstract 1
- 208000015439 Lysosomal storage disease Diseases 0.000 abstract 1
- 208000007466 Male Infertility Diseases 0.000 abstract 1
- 208000002678 Mucopolysaccharidoses Diseases 0.000 abstract 1
- 206010068871 Myotonic dystrophy Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 241000208125 Nicotiana Species 0.000 abstract 1
- 235000002637 Nicotiana tabacum Nutrition 0.000 abstract 1
- 206010031243 Osteogenesis imperfecta Diseases 0.000 abstract 1
- 208000035467 Pancreatic insufficiency Diseases 0.000 abstract 1
- 206010033799 Paralysis Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 abstract 1
- 108091000054 Prion Proteins 0.000 abstract 1
- 208000024777 Prion disease Diseases 0.000 abstract 1
- 201000005660 Protein C Deficiency Diseases 0.000 abstract 1
- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 abstract 1
- 208000004622 abetalipoproteinemia Diseases 0.000 abstract 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 230000037444 atrophy Effects 0.000 abstract 1
- 230000002146 bilateral effect Effects 0.000 abstract 1
- 206010006451 bronchitis Diseases 0.000 abstract 1
- 208000007451 chronic bronchitis Diseases 0.000 abstract 1
- 230000007547 defect Effects 0.000 abstract 1
- 208000030533 eye disease Diseases 0.000 abstract 1
- 201000001386 familial hypercholesterolemia Diseases 0.000 abstract 1
- 208000030409 hereditary angioedema with C1Inh deficiency Diseases 0.000 abstract 1
- 208000013746 hereditary thrombophilia due to congenital protein C deficiency Diseases 0.000 abstract 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 abstract 1
- 201000008980 hyperinsulinism Diseases 0.000 abstract 1
- 150000002632 lipids Chemical class 0.000 abstract 1
- 208000019423 liver disease Diseases 0.000 abstract 1
- 201000001441 melanoma Diseases 0.000 abstract 1
- 206010028093 mucopolysaccharidosis Diseases 0.000 abstract 1
- 210000003205 muscle Anatomy 0.000 abstract 1
- 208000000638 myeloperoxidase deficiency Diseases 0.000 abstract 1
- 230000002988 nephrogenic effect Effects 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 108010040003 polyglutamine Proteins 0.000 abstract 1
- 229920000155 polyglutamine Polymers 0.000 abstract 1
- 230000000750 progressive effect Effects 0.000 abstract 1
- 230000020978 protein processing Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000009890 sinusitis Diseases 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
- 210000001177 vas deferen Anatomy 0.000 abstract 1
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 39
- 125000005843 halogen group Chemical group 0.000 description 21
- 125000003282 alkyl amino group Chemical group 0.000 description 16
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 14
- 125000005169 cycloalkylcarbonylamino group Chemical group 0.000 description 12
- 125000004122 cyclic group Chemical group 0.000 description 11
- 125000001188 haloalkyl group Chemical group 0.000 description 9
- 150000002431 hydrogen Chemical class 0.000 description 9
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 9
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 8
- 125000003710 aryl alkyl group Chemical group 0.000 description 8
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 7
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 7
- 125000004429 atom Chemical group 0.000 description 7
- 125000004966 cyanoalkyl group Chemical group 0.000 description 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 6
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 6
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 description 5
- 125000004181 carboxyalkyl group Chemical group 0.000 description 5
- 125000005224 heteroarylcarbonylamino group Chemical group 0.000 description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 5
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 4
- 125000005126 aryl alkyl carbonyl amino group Chemical group 0.000 description 4
- 125000004475 heteroaralkyl group Chemical group 0.000 description 4
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 description 3
- 125000006325 2-propenyl amino group Chemical group [H]C([H])=C([H])C([H])([H])N([H])* 0.000 description 3
- 125000004103 aminoalkyl group Chemical group 0.000 description 3
- 125000001769 aryl amino group Chemical group 0.000 description 3
- 125000005605 benzo group Chemical group 0.000 description 3
- 229910052801 chlorine Inorganic materials 0.000 description 3
- 239000000460 chlorine Substances 0.000 description 3
- 229910052731 fluorine Inorganic materials 0.000 description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 2
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 description 2
- 125000005001 aminoaryl group Chemical group 0.000 description 2
- 125000005100 aryl amino carbonyl group Chemical group 0.000 description 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 2
- 229910052794 bromium Inorganic materials 0.000 description 2
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 description 2
- 125000005167 cycloalkylaminocarbonyl group Chemical group 0.000 description 2
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 description 2
- 125000004663 dialkyl amino group Chemical group 0.000 description 2
- 229910052736 halogen Inorganic materials 0.000 description 2
- 150000002367 halogens Chemical class 0.000 description 2
- 125000005114 heteroarylalkoxy group Chemical group 0.000 description 2
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 description 2
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 description 2
- 125000004971 nitroalkyl group Chemical group 0.000 description 2
- 229910052757 nitrogen Inorganic materials 0.000 description 2
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 description 1
- YQTCQNIPQMJNTI-UHFFFAOYSA-N 2,2-dimethylpropan-1-one Chemical group CC(C)(C)[C]=O YQTCQNIPQMJNTI-UHFFFAOYSA-N 0.000 description 1
- 125000004974 2-butenyl group Chemical group C(C=CC)* 0.000 description 1
- 125000006040 2-hexenyl group Chemical group 0.000 description 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 description 1
- 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 description 1
- UTBULQCHEUWJNV-UHFFFAOYSA-N 4-phenylpiperidine Chemical compound C1CNCCC1C1=CC=CC=C1 UTBULQCHEUWJNV-UHFFFAOYSA-N 0.000 description 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- OWYWGLHRNBIFJP-UHFFFAOYSA-N Ipazine Chemical compound CCN(CC)C1=NC(Cl)=NC(NC(C)C)=N1 OWYWGLHRNBIFJP-UHFFFAOYSA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 229910006069 SO3H Inorganic materials 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 1
- 125000005354 acylalkyl group Chemical group 0.000 description 1
- 125000004171 alkoxy aryl group Chemical group 0.000 description 1
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 description 1
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 description 1
- 125000002877 alkyl aryl group Chemical group 0.000 description 1
- 125000005197 alkyl carbonyloxy alkyl group Chemical group 0.000 description 1
- 125000005157 alkyl carboxy group Chemical group 0.000 description 1
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 125000005214 aminoheteroaryl group Chemical group 0.000 description 1
- 125000002178 anthracenyl group Chemical group C1(=CC=CC2=CC3=CC=CC=C3C=C12)* 0.000 description 1
- 125000005160 aryl oxy alkyl group Chemical group 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 150000001602 bicycloalkyls Chemical group 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 125000000480 butynyl group Chemical group [*]C#CC([H])([H])C([H])([H])[H] 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 125000002837 carbocyclic group Chemical group 0.000 description 1
- 150000001721 carbon Chemical group 0.000 description 1
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 description 1
- 125000005145 cycloalkylaminosulfonyl group Chemical group 0.000 description 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000001162 cycloheptenyl group Chemical group C1(=CCCCCC1)* 0.000 description 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000000522 cyclooctenyl group Chemical group C1(=CCCCCCC1)* 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 1
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 description 1
- 125000003106 haloaryl group Chemical group 0.000 description 1
- 125000005222 heteroarylaminocarbonyl group Chemical group 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 125000002757 morpholinyl group Chemical group 0.000 description 1
- GCXNMLMLUZNOKK-UHFFFAOYSA-N n-(1-bromoisoquinolin-3-yl)-1-(4-methoxyphenyl)cyclopropane-1-carboxamide Chemical compound C1=CC(OC)=CC=C1C1(C(=O)NC=2N=C(Br)C3=CC=CC=C3C=2)CC1 GCXNMLMLUZNOKK-UHFFFAOYSA-N 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 125000005593 norbornanyl group Chemical group 0.000 description 1
- 125000002868 norbornyl group Chemical group C12(CCC(CC1)C2)* 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- IWELDVXSEVIIGI-UHFFFAOYSA-N piperazin-2-one Chemical compound O=C1CNCCN1 IWELDVXSEVIIGI-UHFFFAOYSA-N 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 125000005415 substituted alkoxy group Chemical group 0.000 description 1
- 125000000547 substituted alkyl group Chemical group 0.000 description 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 description 1
- 125000006296 sulfonyl amino group Chemical group [H]N(*)S(*)(=O)=O 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000004385 trihaloalkyl group Chemical group 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- 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
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- 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
-
- A—HUMAN NECESSITIES
- 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
- A61K31/495—Heterocyclic 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Gynecology & Obstetrics (AREA)
- Oncology (AREA)
- Psychology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Hospice & Palliative Care (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Nutrition Science (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98855907P | 2007-11-16 | 2007-11-16 | |
| US988559P | 2007-11-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2658064T3 true ES2658064T3 (es) | 2018-03-08 |
Family
ID=40303494
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES15180766.6T Active ES2658064T3 (es) | 2007-11-16 | 2008-11-14 | Moduladores de isoquinolina de transportadores de casete de unión a ATP |
| ES08849242T Active ES2445447T3 (es) | 2007-11-16 | 2008-11-14 | Moduladores de isoquinolina de transportadores de casete de unión a ATP |
| ES12181370.3T Active ES2556080T3 (es) | 2007-11-16 | 2008-11-14 | Moduladores de isoquinolina de transportadores de casete de unión a ATP |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES08849242T Active ES2445447T3 (es) | 2007-11-16 | 2008-11-14 | Moduladores de isoquinolina de transportadores de casete de unión a ATP |
| ES12181370.3T Active ES2556080T3 (es) | 2007-11-16 | 2008-11-14 | Moduladores de isoquinolina de transportadores de casete de unión a ATP |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US8507524B2 (https=) |
| EP (3) | EP2578571B1 (https=) |
| JP (3) | JP5646338B2 (https=) |
| CN (2) | CN101952254B (https=) |
| AU (1) | AU2008322616B2 (https=) |
| CA (1) | CA2705562C (https=) |
| CY (1) | CY1115318T1 (https=) |
| DK (2) | DK2217572T3 (https=) |
| ES (3) | ES2658064T3 (https=) |
| HR (2) | HRP20140103T1 (https=) |
| HU (1) | HUE026334T2 (https=) |
| NZ (2) | NZ585980A (https=) |
| PL (2) | PL2217572T3 (https=) |
| PT (2) | PT2578571E (https=) |
| SI (2) | SI2578571T1 (https=) |
| WO (1) | WO2009064959A1 (https=) |
Families Citing this family (63)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2006111093A (ru) | 2003-09-06 | 2007-10-27 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Модуляторы атр-связывающих кассетных транспортеров |
| CN101675928A (zh) * | 2003-11-14 | 2010-03-24 | 沃泰克斯药物股份有限公司 | 可用作atp-结合弹夹转运蛋白调控剂的噻唑和噁唑 |
| US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| BRPI0507278A (pt) * | 2004-01-30 | 2007-06-26 | Vertex Pharma | moduladores dos transportadores do cassete de ligação ao atp |
| RS56037B1 (sr) | 2004-06-24 | 2017-09-29 | Vertex Pharma | Modulatori atp-vezujućih kasetnih transportera |
| US7999113B2 (en) | 2005-08-11 | 2011-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| CN102775396B (zh) | 2005-11-08 | 2014-10-08 | 沃泰克斯药物股份有限公司 | Atp-结合弹夹转运蛋白的杂环调控剂 |
| CA2856037C (en) | 2005-12-28 | 2017-03-07 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
| EP3219705B1 (en) | 2005-12-28 | 2020-03-11 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of the amorphous form of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| US7671221B2 (en) * | 2005-12-28 | 2010-03-02 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
| EP2674428B1 (en) | 2006-04-07 | 2016-04-06 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| USRE50453E1 (en) | 2006-04-07 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| US10022352B2 (en) | 2006-04-07 | 2018-07-17 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| US7645789B2 (en) | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| US7754739B2 (en) * | 2007-05-09 | 2010-07-13 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
| US8455513B2 (en) | 2007-01-10 | 2013-06-04 | Aerie Pharmaceuticals, Inc. | 6-aminoisoquinoline compounds |
| CN104447716A (zh) | 2007-05-09 | 2015-03-25 | 沃泰克斯药物股份有限公司 | Cftr调节剂 |
| AU2008256937A1 (en) * | 2007-05-25 | 2008-12-04 | Vertex Pharmaceuticals Incorporated | Ion channel modulators and methods of use |
| JP5389030B2 (ja) | 2007-08-24 | 2014-01-15 | バーテックス ファーマシューティカルズ インコーポレイテッド | (特に)嚢胞性線維症の処置に有用なイソチアゾロピリジノン |
| SI2578571T1 (sl) | 2007-11-16 | 2016-01-29 | Vertex Pharmaceuticals Incorporated | Izokinolinski modulatorji prenašalcev z atp-vezavno kaseto |
| MX365732B (es) * | 2007-12-07 | 2019-06-12 | Vertex Pharma | Procesos para producir acidos cicloalquilcarboxamido-piridin benzoicos. |
| US20100036130A1 (en) | 2007-12-07 | 2010-02-11 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| CN101998854A (zh) * | 2007-12-07 | 2011-03-30 | 沃泰克斯药物股份有限公司 | 3-(6-(1-(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)环丙烷甲酰氨基)-3-甲基吡啶-2-基)苯甲酸的制剂 |
| EP3683218B1 (en) | 2007-12-07 | 2024-09-18 | Vertex Pharmaceuticals Incorporated | Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid |
| NZ720282A (en) | 2008-02-28 | 2017-12-22 | Vertex Pharma | Heteroaryl derivatives as cftr modulators |
| NZ616097A (en) | 2008-03-31 | 2015-04-24 | Vertex Pharma | Pyridyl derivatives as cftr modulators |
| US8450344B2 (en) | 2008-07-25 | 2013-05-28 | Aerie Pharmaceuticals, Inc. | Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| US12458635B2 (en) | 2008-08-13 | 2025-11-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| AR073709A1 (es) | 2008-09-29 | 2010-11-24 | Vertex Pharma | Unidades de dosis de acido 3-(6-(1-(2,2-difluorobenzeno (d) (1,3) dioxol-5-il) ciclopropancarboxamido)-3-metilpiridin-2-il) benzoico |
| EP2349263B1 (en) * | 2008-10-23 | 2014-04-23 | Vertex Pharmaceuticals Inc. | Modulators of cystic fibrosis transmembrane conductance regulator |
| PL2408750T3 (pl) | 2009-03-20 | 2016-02-29 | Vertex Pharma | Sposób otrzymywania modulatorów błonowego regulatora przewodnictwa swoistego dla mukowiscydozy |
| EP3053913B1 (en) | 2009-05-01 | 2018-03-07 | Aerie Pharmaceuticals, Inc. | Dual mechanism inhibitors for the treatment of disease |
| US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
| MX2012011655A (es) | 2010-04-07 | 2012-11-23 | Vertex Pharma | Formas solidas de acido 3-(6-(1-(2,2-difluorobenzo [d][1-3]dioxol-5-il]ciclopropanocarboxamido)-3-metilpiridin-2-il) benzoico. |
| JP2013523833A (ja) | 2010-04-07 | 2013-06-17 | バーテックス ファーマシューティカルズ インコーポレイテッド | 3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸の医薬組成物およびその投与 |
| MX353408B (es) | 2010-04-22 | 2018-01-11 | Vertex Pharma | Proceso para producir compuestos de cicloalquilcarboxamido-indol. |
| US8563593B2 (en) | 2010-06-08 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Formulations of (R)-1-(2,2-difluorobenzo[D] [1,3] dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide |
| WO2013070961A1 (en) | 2011-11-08 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
| NZ727015A (en) | 2012-01-25 | 2017-12-22 | Vertex Pharma | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| JP2015511583A (ja) | 2012-02-27 | 2015-04-20 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | 薬学的組成物およびその投与 |
| US8674108B2 (en) | 2012-04-20 | 2014-03-18 | Vertex Pharmaceuticals Incorporated | Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| AU2013270681A1 (en) | 2012-06-08 | 2014-12-18 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions for the treatment of CFTR -mediated disorders |
| AR092857A1 (es) | 2012-07-16 | 2015-05-06 | Vertex Pharma | Composiciones farmaceuticas de (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)-n-(1-(2,3-dihidroxipropil)-6-fluoro-2-(1-hidroxi-2-metilpropan-2-il)-1h-indol-5-il)ciclopropancarboxamida y administracion de las mismas |
| DK3811943T3 (da) | 2013-03-15 | 2023-04-03 | Aerie Pharmaceuticals Inc | Forbindelse til anvendelse til behandling af øjenlidelser |
| AU2014349010C1 (en) | 2013-11-12 | 2020-08-06 | Vertex Pharmaceuticals Incorporated | Process of preparing pharmaceutical compositions for the treatment of CFTR mediated diseases |
| RU2744460C2 (ru) | 2014-04-15 | 2021-03-09 | Вертекс Фармасьютикалз Инкорпорейтед | Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости |
| GB201415381D0 (en) | 2014-08-29 | 2014-10-15 | Algipharma As | Inhalable powder formulations of alginate oligomers |
| CN107250113B (zh) | 2014-10-07 | 2019-03-29 | 弗特克斯药品有限公司 | 囊性纤维化跨膜传导调节蛋白的调节剂的共晶 |
| DK3212189T3 (da) | 2014-10-31 | 2020-10-26 | Abbvie Overseas Sarl | Substituerede chromaner og fremgangsmåde til anvendelse deraf |
| RU2691136C2 (ru) | 2014-11-18 | 2019-06-11 | Вертекс Фармасьютикалз Инкорпорейтед | Способ проведения высокопроизводительной тестовой высокоэффективной жидкостной хроматографии |
| GB201504878D0 (en) | 2015-03-23 | 2015-05-06 | Algipharma As | Use of alginate oligomers and CFTR modulators in the treatment of conditions associated with CFTR dysfuntion |
| CN105153013B (zh) * | 2015-09-16 | 2017-12-29 | 苏州昊帆生物科技有限公司 | 6‑溴异吲哚啉‑1‑酮的合成方法 |
| GB201517639D0 (en) | 2015-10-06 | 2015-11-18 | Algipharma As | Use of alginate oligomers to treat or prevent microbial overgrowth in the intestinal tract |
| KR102568079B1 (ko) | 2016-08-31 | 2023-08-17 | 에어리 파마슈티컬즈, 인코포레이티드 | 안과용 조성물 |
| CN110494432B (zh) * | 2016-12-28 | 2022-08-12 | 米尼奥尔克斯治疗有限公司 | 异喹啉化合物,其制备方法及其在与β-半乳糖苷酶活性改变相关的病症中的治疗用途 |
| KR20190135027A (ko) | 2017-03-31 | 2019-12-05 | 에어리 파마슈티컬즈, 인코포레이티드 | 아릴 시클로프로필-아미노-이소퀴놀리닐 아미드 화합물 |
| AU2019337703B2 (en) | 2018-09-14 | 2023-02-02 | Aerie Pharmaceuticals, Inc. | Aryl cyclopropyl-amino-isoquinolinyl amide compounds |
| CN113943229B (zh) * | 2020-07-15 | 2025-02-07 | 天津师范大学 | 生物碱pulmonarin B的合成及在防治植物病毒和病菌病中的应用 |
| CR20230120A (es) | 2020-08-07 | 2023-09-01 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
| US12324802B2 (en) | 2020-11-18 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| US12331063B2 (en) | 2021-04-29 | 2025-06-17 | Incyte Corporation | Hetero-bicyclic inhibitors of KRAS |
Family Cites Families (96)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5886026A (en) | 1993-07-19 | 1999-03-23 | Angiotech Pharmaceuticals Inc. | Anti-angiogenic compositions and methods of use |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| TW200307539A (en) * | 2002-02-01 | 2003-12-16 | Bristol Myers Squibb Co | Cycloalkyl inhibitors of potassium channel function |
| BR0314943A (pt) | 2002-09-30 | 2005-08-02 | Univ California | Inibidores da proteìna reguladora da condutância transmembrana da fibrose cìstica e usos destes |
| US20050113423A1 (en) | 2003-03-12 | 2005-05-26 | Vangoor Frederick F. | Modulators of ATP-binding cassette transporters |
| EP4101846B1 (en) | 2003-04-11 | 2023-08-02 | PTC Therapeutics, Inc. | 1,2,4-oxadiazole benzoic acid compounds and their use for nonsense suppression and the treatment of disease |
| US7696244B2 (en) | 2003-05-16 | 2010-04-13 | The Regents Of The University Of California | Compounds having activity in increasing ion transport by mutant-CFTR and uses thereof |
| DE602004022819D1 (de) | 2003-06-06 | 2009-10-08 | Vertex Pharma | Von atp-bindende kassette transportern |
| RU2006111093A (ru) | 2003-09-06 | 2007-10-27 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Модуляторы атр-связывающих кассетных транспортеров |
| EP1680411A2 (en) | 2003-10-08 | 2006-07-19 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters containing cycloalkyl or pyranyl groups |
| CN101675928A (zh) | 2003-11-14 | 2010-03-24 | 沃泰克斯药物股份有限公司 | 可用作atp-结合弹夹转运蛋白调控剂的噻唑和噁唑 |
| BRPI0507278A (pt) * | 2004-01-30 | 2007-06-26 | Vertex Pharma | moduladores dos transportadores do cassete de ligação ao atp |
| US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| US7522995B2 (en) | 2004-02-05 | 2009-04-21 | Nortrup Edward H | Method and system for providing travel time information |
| EP1740532A4 (en) | 2004-03-30 | 2009-06-10 | Univ California | CFTR INHIBITOR COMPOUNDS CONTAINING HYDRAZIDS AND USES THEREOF |
| CA2569402A1 (en) | 2004-06-04 | 2005-12-22 | The Regents Of The University Of California | Compounds having activity in increasing ion transport by mutant-cftr and uses thereof |
| US8354427B2 (en) | 2004-06-24 | 2013-01-15 | Vertex Pharmaceutical Incorporated | Modulators of ATP-binding cassette transporters |
| RS56037B1 (sr) | 2004-06-24 | 2017-09-29 | Vertex Pharma | Modulatori atp-vezujućih kasetnih transportera |
| US20140343098A1 (en) | 2004-06-24 | 2014-11-20 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
| EP1799659A1 (en) | 2004-10-13 | 2007-06-27 | PTC Therapeutics, Inc. | Compounds for nonsense suppression, and methods for their use |
| JP5385605B2 (ja) | 2005-03-11 | 2014-01-08 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atp結合カセットトランスポーターのモジュレーター |
| CA2600869A1 (en) | 2005-03-18 | 2006-09-28 | The Regents Of The University Of California | Compounds having activity in correcting mutant-cftr processing and uses thereof |
| PL2402002T3 (pl) | 2005-04-08 | 2018-11-30 | Ptc Therapeutics, Inc. | Kompozycje zawierające kwas 1,2,4-oksadiazolobenzoesowy i ich zastosowania do leczenia chorób związanych z przedwczesnym kodonem stop |
| JP5426878B2 (ja) | 2005-05-24 | 2014-02-26 | バーテックス ファーマシューティカルズ インコーポレイテッド | Atp−結合カセットトランスポーターのモジュレーター |
| US7999113B2 (en) | 2005-08-11 | 2011-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| KR20080064971A (ko) | 2005-10-06 | 2008-07-10 | 버텍스 파마슈티칼스 인코포레이티드 | Atp-결합 카세트 전달체의 조절자 |
| US20120232059A1 (en) | 2005-11-08 | 2012-09-13 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette Transporters |
| CN102775396B (zh) | 2005-11-08 | 2014-10-08 | 沃泰克斯药物股份有限公司 | Atp-结合弹夹转运蛋白的杂环调控剂 |
| EP1979367A2 (en) | 2005-12-24 | 2008-10-15 | Vertex Pharmaceuticals Incorporated | Quinolin-4-one derivatives as modulators of abc transporters |
| AU2006331565A1 (en) | 2005-12-27 | 2007-07-05 | Vertex Pharmaceuticals Incorporated | Compounds useful in CFTR assays and methods therewith |
| CA2856037C (en) | 2005-12-28 | 2017-03-07 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
| EP3219705B1 (en) | 2005-12-28 | 2020-03-11 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of the amorphous form of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| US7671221B2 (en) | 2005-12-28 | 2010-03-02 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
| US7645789B2 (en) | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| EP2674428B1 (en) | 2006-04-07 | 2016-04-06 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| CN101478964B (zh) | 2006-05-12 | 2012-02-29 | 沃泰克斯药物股份有限公司 | N-[2,4-双(1,1-二甲基乙基)-5-羟苯基]-1,4-二氢-4-氧代喹啉-3-羧酰胺的组合物 |
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| US7754739B2 (en) | 2007-05-09 | 2010-07-13 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
| CN104447716A (zh) | 2007-05-09 | 2015-03-25 | 沃泰克斯药物股份有限公司 | Cftr调节剂 |
| JP5686596B2 (ja) | 2007-05-25 | 2015-03-18 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | 嚢胞性線維症膜貫通コンダクタンス制御因子の調節因子 |
| US20110177999A1 (en) | 2007-08-09 | 2011-07-21 | Vertex Pharmaceuticals Incorporated | Therapeutic Combinations Useful in Treating CFTR Related Diseases |
| JP5389030B2 (ja) | 2007-08-24 | 2014-01-15 | バーテックス ファーマシューティカルズ インコーポレイテッド | (特に)嚢胞性線維症の処置に有用なイソチアゾロピリジノン |
| EP2201010B1 (en) | 2007-09-14 | 2013-11-06 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| NZ620027A (en) | 2007-09-14 | 2015-05-29 | Vertex Pharma | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| SI2578571T1 (sl) | 2007-11-16 | 2016-01-29 | Vertex Pharmaceuticals Incorporated | Izokinolinski modulatorji prenašalcev z atp-vezavno kaseto |
| EP3683218B1 (en) | 2007-12-07 | 2024-09-18 | Vertex Pharmaceuticals Incorporated | Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid |
| MX365732B (es) | 2007-12-07 | 2019-06-12 | Vertex Pharma | Procesos para producir acidos cicloalquilcarboxamido-piridin benzoicos. |
| US20100036130A1 (en) | 2007-12-07 | 2010-02-11 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| CN101998854A (zh) | 2007-12-07 | 2011-03-30 | 沃泰克斯药物股份有限公司 | 3-(6-(1-(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)环丙烷甲酰氨基)-3-甲基吡啶-2-基)苯甲酸的制剂 |
| JP5637859B2 (ja) | 2007-12-13 | 2014-12-10 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | 嚢胞性線維症膜コンダクタンスレギュレーターのモジュレーター |
| NZ720282A (en) | 2008-02-28 | 2017-12-22 | Vertex Pharma | Heteroaryl derivatives as cftr modulators |
| NZ616097A (en) | 2008-03-31 | 2015-04-24 | Vertex Pharma | Pyridyl derivatives as cftr modulators |
| MX2011001782A (es) | 2008-08-13 | 2012-02-08 | Vertex Pharma | Composicion farmaceutica y su administracion. |
| US20100256184A1 (en) | 2008-08-13 | 2010-10-07 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| AR073709A1 (es) | 2008-09-29 | 2010-11-24 | Vertex Pharma | Unidades de dosis de acido 3-(6-(1-(2,2-difluorobenzeno (d) (1,3) dioxol-5-il) ciclopropancarboxamido)-3-metilpiridin-2-il) benzoico |
| US20110257223A1 (en) | 2008-10-23 | 2011-10-20 | Vertex Pharmaceuticals Incorporated | Modulators of Cystic Fibrosis Transmembrane Conductance Regulator |
| CN102224141B (zh) | 2008-10-23 | 2014-10-08 | 沃泰克斯药物股份有限公司 | N-(4-(7-氮杂双环[2.2.1]庚-7-基)-2-(三氟甲基)苯基)-4-氧代-5-(三氟甲基)-1,4-二氢喹啉-3-甲酰胺的固体形式 |
| WO2010048564A1 (en) | 2008-10-23 | 2010-04-29 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP2349263B1 (en) | 2008-10-23 | 2014-04-23 | Vertex Pharmaceuticals Inc. | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP2382197B1 (en) | 2008-12-30 | 2016-10-05 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| HRP20181261T1 (hr) | 2009-03-20 | 2018-12-14 | Vertex Pharmaceuticals Incorporated | Modulatori regulatora transmembranske provodljivosti cistične fibroze |
| PL2408750T3 (pl) | 2009-03-20 | 2016-02-29 | Vertex Pharma | Sposób otrzymywania modulatorów błonowego regulatora przewodnictwa swoistego dla mukowiscydozy |
| BR112012006031A2 (pt) | 2009-09-17 | 2019-09-24 | Vertex Pharma | processo para preparação de compostos azabicíclicos. |
| MX2012004792A (es) | 2009-10-22 | 2013-02-01 | Vertex Pharma | Composiciones para el tratamiento de fibrosis quistica y otras enfermedades cronicas. |
| US8344147B2 (en) | 2009-10-23 | 2013-01-01 | Vertex Pharmaceutical Incorporated | Process for preparing modulators of cystic fibrosis transmembrane conductance regulator |
| CN102666546B (zh) | 2009-10-23 | 2015-09-09 | 沃泰克斯药物股份有限公司 | N-(4-(7-氮杂双环[2.2.1]庚-7-基)-2-(三氟甲基)苯基)-4-氧代-5-(三氟甲基)-1,4-二氢喹啉-3-甲酰胺的固体形式 |
| EP3037415A1 (en) | 2010-03-19 | 2016-06-29 | Vertex Pharmaceuticals Inc. | Solid form of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| SI2826776T1 (sl) | 2010-03-25 | 2021-02-26 | Vertex Pharmaceuticals Incorporated | Trdna disperzija amorfne oblike (R)-1(2,2-difluorobenzo(D)(1,3)dioksol-5-il)-N-(1-(2,3-dihidroksipropil) -6-fluoro-2-(1-hidroksi-2-metilpropan-2-il)-1H-indol-5-il)- ciklopropankarboksamida |
| US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
| JP2013523833A (ja) | 2010-04-07 | 2013-06-17 | バーテックス ファーマシューティカルズ インコーポレイテッド | 3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸の医薬組成物およびその投与 |
| MX2012011655A (es) | 2010-04-07 | 2012-11-23 | Vertex Pharma | Formas solidas de acido 3-(6-(1-(2,2-difluorobenzo [d][1-3]dioxol-5-il]ciclopropanocarboxamido)-3-metilpiridin-2-il) benzoico. |
| CA2796602A1 (en) | 2010-04-22 | 2011-10-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| EP2560649A1 (en) | 2010-04-22 | 2013-02-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| EP2560651A1 (en) | 2010-04-22 | 2013-02-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| MX353408B (es) | 2010-04-22 | 2018-01-11 | Vertex Pharma | Proceso para producir compuestos de cicloalquilcarboxamido-indol. |
| AR081920A1 (es) | 2010-05-20 | 2012-10-31 | Vertex Pharma | Procesos de produccion de moduladores del regulador de conductancia transmembrana de fibrosis quistica |
| AU2011255237A1 (en) | 2010-05-20 | 2012-11-29 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| US8563593B2 (en) | 2010-06-08 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Formulations of (R)-1-(2,2-difluorobenzo[D] [1,3] dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide |
| WO2012027247A2 (en) | 2010-08-23 | 2012-03-01 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition of (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxy propyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide and administration therof |
| CA2809263A1 (en) | 2010-08-27 | 2012-03-01 | Eleni Dokou | Pharmaceutical composition and administrations thereof |
| US8802700B2 (en) | 2010-12-10 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
| EP2773349A1 (en) | 2011-11-02 | 2014-09-10 | Vertex Pharmaceuticals Incorporated | Use of (n- [2, 4 -bis (1, 1 -dimethylethyl) - 5 - hydroxyphenyl]- 1, 4 - dihydro - 4 - oxoquinoline - 3 - carboxamide) for treating cftr mediated diseases |
| US20140127901A1 (en) | 2012-11-08 | 2014-05-08 | Taiwan Semiconductor Manufacturing Company, Ltd. | Low-k damage free integration scheme for copper interconnects |
| WO2013070961A1 (en) | 2011-11-08 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
| NZ727015A (en) | 2012-01-25 | 2017-12-22 | Vertex Pharma | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| JP2015511583A (ja) | 2012-02-27 | 2015-04-20 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | 薬学的組成物およびその投与 |
| US8674108B2 (en) | 2012-04-20 | 2014-03-18 | Vertex Pharmaceuticals Incorporated | Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| AU2013270681A1 (en) | 2012-06-08 | 2014-12-18 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions for the treatment of CFTR -mediated disorders |
| AR092857A1 (es) | 2012-07-16 | 2015-05-06 | Vertex Pharma | Composiciones farmaceuticas de (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)-n-(1-(2,3-dihidroxipropil)-6-fluoro-2-(1-hidroxi-2-metilpropan-2-il)-1h-indol-5-il)ciclopropancarboxamida y administracion de las mismas |
| EP2914248B2 (en) | 2012-11-02 | 2023-10-18 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions for the treatment of cftr mediated diseases |
| US20140221424A1 (en) | 2013-01-30 | 2014-08-07 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions for use in the treatment of cystic fibrosis |
| RU2744460C2 (ru) | 2014-04-15 | 2021-03-09 | Вертекс Фармасьютикалз Инкорпорейтед | Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости |
| MA41051B1 (fr) | 2014-10-06 | 2020-11-30 | Vertex Pharma | Modulateurs du régulateur de conductance transmembranaire de la mucoviscidose |
| CN107250113B (zh) | 2014-10-07 | 2019-03-29 | 弗特克斯药品有限公司 | 囊性纤维化跨膜传导调节蛋白的调节剂的共晶 |
-
2008
- 2008-11-14 SI SI200831546T patent/SI2578571T1/sl unknown
- 2008-11-14 EP EP12181370.3A patent/EP2578571B1/en active Active
- 2008-11-14 NZ NZ585980A patent/NZ585980A/en unknown
- 2008-11-14 PL PL08849242T patent/PL2217572T3/pl unknown
- 2008-11-14 EP EP15180766.6A patent/EP3012250B1/en active Active
- 2008-11-14 US US12/271,088 patent/US8507524B2/en active Active
- 2008-11-14 CA CA2705562A patent/CA2705562C/en active Active
- 2008-11-14 CN CN2008801235011A patent/CN101952254B/zh active Active
- 2008-11-14 ES ES15180766.6T patent/ES2658064T3/es active Active
- 2008-11-14 JP JP2010534201A patent/JP5646338B2/ja active Active
- 2008-11-14 HR HRP20140103AT patent/HRP20140103T1/hr unknown
- 2008-11-14 EP EP20080849242 patent/EP2217572B1/en active Active
- 2008-11-14 NZ NZ59894108A patent/NZ598941A/xx unknown
- 2008-11-14 ES ES08849242T patent/ES2445447T3/es active Active
- 2008-11-14 PT PT121813703T patent/PT2578571E/pt unknown
- 2008-11-14 AU AU2008322616A patent/AU2008322616B2/en active Active
- 2008-11-14 ES ES12181370.3T patent/ES2556080T3/es active Active
- 2008-11-14 SI SI200831147T patent/SI2217572T1/sl unknown
- 2008-11-14 CN CN201210243185.XA patent/CN102743385B/zh active Active
- 2008-11-14 DK DK08849242T patent/DK2217572T3/da active
- 2008-11-14 DK DK12181370.3T patent/DK2578571T3/en active
- 2008-11-14 PT PT08849242T patent/PT2217572E/pt unknown
- 2008-11-14 PL PL12181370T patent/PL2578571T3/pl unknown
- 2008-11-14 HU HUE12181370A patent/HUE026334T2/en unknown
- 2008-11-14 WO PCT/US2008/083517 patent/WO2009064959A1/en not_active Ceased
-
2013
- 2013-07-08 US US13/936,277 patent/US8722704B2/en active Active
-
2014
- 2014-02-03 JP JP2014018471A patent/JP5885359B2/ja active Active
- 2014-02-03 CY CY20141100083T patent/CY1115318T1/el unknown
- 2014-03-21 US US14/221,537 patent/US9012473B2/en active Active
-
2015
- 2015-03-18 US US14/661,224 patent/US9522145B2/en active Active
- 2015-08-12 JP JP2015159316A patent/JP2015205936A/ja active Pending
- 2015-11-23 HR HRP20151255TT patent/HRP20151255T1/hr unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2658064T3 (es) | Moduladores de isoquinolina de transportadores de casete de unión a ATP | |
| CA2699382C (en) | Modulators of cystic fibrosis transmembrane conductance regulator | |
| DK2774925T3 (en) | Heterocyclic modulators of ATP binding cassette transporters | |
| AU2007227581B2 (en) | Thiazolidinedione analogues for the treatment of metabolic inflammation mediated disease | |
| AU2008363828B2 (en) | Modulators of ATP-binding cassette transporters | |
| CA2609392A1 (en) | Modulators of atp-binding cassette transporters | |
| WO2011133441A2 (en) | Novel synthesis for thiazolidinedione compounds | |
| ES2813363T3 (es) | Compuestos ahorradores de PPAR para el tratamiento de enfermedades metabólicas | |
| CA2646170A1 (en) | Combination therapies of thiazolidinedione analogues and glucocorticoid agonists | |
| ES2588769T3 (es) | Síntesis de compuestos de tiazolidinedionas | |
| AU2013200104B2 (en) | Thiazolidinedione analogues for the treatment of metabolic inflammation mediated disease | |
| HK40033261A (en) | Heterocyclic modulators of atp-binding cassette transporters | |
| HK1222847B (en) | Isoquinoline modulators of atp-binding cassette transporters | |
| HK1240928B (en) | Heterocyclic modulators of atp-binding cassette transporters | |
| HK1177137B (en) | Isoquinoline modulators of atp-binding cassette transporters | |
| NZ624440A (en) | Modulators of atp-binding cassette transporters | |
| NZ624440B2 (en) | Modulators of atp-binding cassette transporters |