ZA200602755B - Modulators of ATP-binding cassette transporters - Google Patents
Modulators of ATP-binding cassette transporters Download PDFInfo
- Publication number
- ZA200602755B ZA200602755B ZA200602755A ZA200602755A ZA200602755B ZA 200602755 B ZA200602755 B ZA 200602755B ZA 200602755 A ZA200602755 A ZA 200602755A ZA 200602755 A ZA200602755 A ZA 200602755A ZA 200602755 B ZA200602755 B ZA 200602755B
- Authority
- ZA
- South Africa
- Prior art keywords
- aliphatic
- optionally substituted
- ors
- phenyl
- ring
- Prior art date
Links
- 102000005416 ATP-Binding Cassette Transporters Human genes 0.000 title claims description 30
- 108010006533 ATP-Binding Cassette Transporters Proteins 0.000 title claims description 30
- 125000001424 substituent group Chemical group 0.000 claims description 229
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 221
- -1 1,2-methylenedioxy Chemical group 0.000 claims description 211
- 150000001875 compounds Chemical class 0.000 claims description 189
- 125000001931 aliphatic group Chemical group 0.000 claims description 181
- 238000000034 method Methods 0.000 claims description 127
- 125000003118 aryl group Chemical group 0.000 claims description 116
- 125000001072 heteroaryl group Chemical group 0.000 claims description 98
- 125000000623 heterocyclic group Chemical group 0.000 claims description 94
- 125000005843 halogen group Chemical group 0.000 claims description 90
- 125000000217 alkyl group Chemical group 0.000 claims description 88
- 125000005842 heteroatom Chemical group 0.000 claims description 85
- 229910052757 nitrogen Inorganic materials 0.000 claims description 85
- 229910052717 sulfur Inorganic materials 0.000 claims description 76
- 229920006395 saturated elastomer Polymers 0.000 claims description 62
- 229910052739 hydrogen Inorganic materials 0.000 claims description 61
- 125000002950 monocyclic group Chemical group 0.000 claims description 61
- 229910052760 oxygen Inorganic materials 0.000 claims description 61
- 239000001257 hydrogen Substances 0.000 claims description 58
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims description 54
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 53
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 39
- 229910052799 carbon Inorganic materials 0.000 claims description 36
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 32
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 31
- 125000000304 alkynyl group Chemical group 0.000 claims description 29
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 29
- 125000002619 bicyclic group Chemical group 0.000 claims description 27
- 125000003342 alkenyl group Chemical group 0.000 claims description 24
- 201000010099 disease Diseases 0.000 claims description 24
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 24
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims description 23
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims description 23
- 230000000694 effects Effects 0.000 claims description 21
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 20
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 20
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 19
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 19
- 125000006413 ring segment Chemical group 0.000 claims description 19
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 19
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 17
- 125000001624 naphthyl group Chemical group 0.000 claims description 17
- 150000002431 hydrogen Chemical class 0.000 claims description 16
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 16
- 125000001118 alkylidene group Chemical group 0.000 claims description 15
- 150000003839 salts Chemical class 0.000 claims description 15
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 14
- 206010012735 Diarrhoea Diseases 0.000 claims description 14
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 13
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 13
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 13
- 125000002837 carbocyclic group Chemical group 0.000 claims description 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 12
- 125000002757 morpholinyl group Chemical group 0.000 claims description 12
- 125000001544 thienyl group Chemical group 0.000 claims description 12
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims description 12
- 125000003386 piperidinyl group Chemical group 0.000 claims description 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 10
- 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 claims description 10
- 125000004193 piperazinyl group Chemical group 0.000 claims description 10
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims description 9
- 230000001404 mediated effect Effects 0.000 claims description 9
- 125000005936 piperidyl group Chemical group 0.000 claims description 9
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 8
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 8
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 8
- 241000124008 Mammalia Species 0.000 claims description 8
- 102100026383 Vasopressin-neurophysin 2-copeptin Human genes 0.000 claims description 8
- 125000005605 benzo group Chemical group 0.000 claims description 8
- 230000007812 deficiency Effects 0.000 claims description 8
- 201000010064 diabetes insipidus Diseases 0.000 claims description 8
- 125000002883 imidazolyl group Chemical group 0.000 claims description 8
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 8
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 7
- HKDFRDIIELOLTJ-UHFFFAOYSA-N 1,4-dithianyl Chemical group [CH]1CSCCS1 HKDFRDIIELOLTJ-UHFFFAOYSA-N 0.000 claims description 7
- 125000005955 1H-indazolyl group Chemical group 0.000 claims description 7
- JECYNCQXXKQDJN-UHFFFAOYSA-N 2-(2-methylhexan-2-yloxymethyl)oxirane Chemical compound CCCCC(C)(C)OCC1CO1 JECYNCQXXKQDJN-UHFFFAOYSA-N 0.000 claims description 7
- 108091006146 Channels Proteins 0.000 claims description 7
- 125000000641 acridinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3C=C12)* 0.000 claims description 7
- 150000001541 aziridines Chemical class 0.000 claims description 7
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 7
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 7
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 7
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 7
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 7
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 7
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims description 7
- 125000005879 dioxolanyl group Chemical group 0.000 claims description 7
- 239000012634 fragment Substances 0.000 claims description 7
- 125000002541 furyl group Chemical group 0.000 claims description 7
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 7
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims description 7
- 125000001041 indolyl group Chemical group 0.000 claims description 7
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 claims description 7
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 7
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 7
- 239000000203 mixture Substances 0.000 claims description 7
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 7
- 125000002971 oxazolyl group Chemical group 0.000 claims description 7
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims description 7
- 125000001791 phenazinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3N=C12)* 0.000 claims description 7
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 claims description 7
- 125000001644 phenoxazinyl group Chemical group C1(=CC=CC=2OC3=CC=CC=C3NC12)* 0.000 claims description 7
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 claims description 7
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims description 7
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims description 7
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 7
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims description 7
- 125000002755 pyrazolinyl group Chemical group 0.000 claims description 7
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 7
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 7
- 125000001422 pyrrolinyl group Chemical group 0.000 claims description 7
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 7
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 7
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 7
- 125000005958 tetrahydrothienyl group Chemical group 0.000 claims description 7
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 7
- 125000000335 thiazolyl group Chemical group 0.000 claims description 7
- VOVUARRWDCVURC-UHFFFAOYSA-N thiirane Chemical compound C1CS1 VOVUARRWDCVURC-UHFFFAOYSA-N 0.000 claims description 7
- 125000004306 triazinyl group Chemical group 0.000 claims description 7
- 125000001425 triazolyl group Chemical group 0.000 claims description 7
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 6
- 125000005940 1,4-dioxanyl group Chemical group 0.000 claims description 6
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims description 6
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 6
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 6
- 125000005982 diphenylmethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 6
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 6
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 6
- 238000012545 processing Methods 0.000 claims description 6
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims description 5
- 206010014561 Emphysema Diseases 0.000 claims description 5
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims description 5
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 5
- 208000011580 syndromic disease Diseases 0.000 claims description 5
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims description 4
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims description 4
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims description 4
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims description 4
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 4
- 125000002178 anthracenyl group Chemical group C1(=CC=CC2=CC3=CC=CC=C3C=C12)* 0.000 claims description 4
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims description 4
- 230000007547 defect Effects 0.000 claims description 4
- 238000000338 in vitro Methods 0.000 claims description 4
- 238000001727 in vivo Methods 0.000 claims description 4
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims description 4
- 125000006239 protecting group Chemical group 0.000 claims description 4
- 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 4
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims description 3
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims description 3
- 102000011045 Chloride Channels Human genes 0.000 claims description 3
- 108010062745 Chloride Channels Proteins 0.000 claims description 3
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims description 3
- 125000003545 alkoxy group Chemical group 0.000 claims description 3
- 150000002632 lipids Chemical class 0.000 claims description 3
- 230000000750 progressive effect Effects 0.000 claims description 3
- 125000003944 tolyl group Chemical group 0.000 claims description 3
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims description 2
- 125000005809 3,4,5-trimethoxyphenyl group Chemical group [H]C1=C(OC([H])([H])[H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 claims description 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 2
- 102100034452 Alternative prion protein Human genes 0.000 claims description 2
- 102100032187 Androgen receptor Human genes 0.000 claims description 2
- 206010003591 Ataxia Diseases 0.000 claims description 2
- 208000010693 Charcot-Marie-Tooth Disease Diseases 0.000 claims description 2
- 206010062264 Congenital hyperthyroidism Diseases 0.000 claims description 2
- 208000020406 Creutzfeldt Jacob disease Diseases 0.000 claims description 2
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 claims description 2
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 claims description 2
- 208000024720 Fabry Disease Diseases 0.000 claims description 2
- 206010019860 Hereditary angioedema Diseases 0.000 claims description 2
- 208000033981 Hereditary haemochromatosis Diseases 0.000 claims description 2
- 101000775732 Homo sapiens Androgen receptor Proteins 0.000 claims description 2
- 208000000563 Hyperlipoproteinemia Type II Diseases 0.000 claims description 2
- 206010051125 Hypofibrinogenaemia Diseases 0.000 claims description 2
- 208000000038 Hypoparathyroidism Diseases 0.000 claims description 2
- 102100024640 Low-density lipoprotein receptor Human genes 0.000 claims description 2
- 208000015439 Lysosomal storage disease Diseases 0.000 claims description 2
- 208000002678 Mucopolysaccharidoses Diseases 0.000 claims description 2
- 206010068871 Myotonic dystrophy Diseases 0.000 claims description 2
- 208000012902 Nervous system disease Diseases 0.000 claims description 2
- 208000025966 Neurological disease Diseases 0.000 claims description 2
- 206010031243 Osteogenesis imperfecta Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 208000025237 Polyendocrinopathy Diseases 0.000 claims description 2
- 108091000054 Prion Proteins 0.000 claims description 2
- 208000024777 Prion disease Diseases 0.000 claims description 2
- 201000005660 Protein C Deficiency Diseases 0.000 claims description 2
- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 claims description 2
- 208000006269 X-Linked Bulbo-Spinal Atrophy Diseases 0.000 claims description 2
- 208000004622 abetalipoproteinemia Diseases 0.000 claims description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 125000004190 benzothiazol-2-yl group Chemical group [H]C1=C([H])C([H])=C2N=C(*)SC2=C1[H] 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims description 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 2
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 201000001386 familial hypercholesterolemia Diseases 0.000 claims description 2
- 208000013746 hereditary thrombophilia due to congenital protein C deficiency Diseases 0.000 claims description 2
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 206010028093 mucopolysaccharidosis Diseases 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims description 2
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 claims description 2
- 108010040003 polyglutamine Proteins 0.000 claims description 2
- 229920000155 polyglutamine Polymers 0.000 claims description 2
- 230000020978 protein processing Effects 0.000 claims description 2
- 125000004159 quinolin-2-yl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C([H])C(*)=NC2=C1[H] 0.000 claims description 2
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 claims description 2
- 108091006515 Anion channels Proteins 0.000 claims 4
- 102000037829 Anion channels Human genes 0.000 claims 4
- LHJWROKKBRFPLT-UHFFFAOYSA-N 4,5-diphenyl-1,3-thiazole-2-carboxamide Chemical compound S1C(C(=O)N)=NC(C=2C=CC=CC=2)=C1C1=CC=CC=C1 LHJWROKKBRFPLT-UHFFFAOYSA-N 0.000 claims 2
- 101100516563 Caenorhabditis elegans nhr-6 gene Proteins 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 238000004793 spatially offset Raman spectroscopy Methods 0.000 claims 2
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims 1
- 108020004021 3-ketosteroid receptors Proteins 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 108091008717 AR-A Proteins 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 101100412459 Arabidopsis thaliana RER3 gene Proteins 0.000 claims 1
- 101100412461 Arabidopsis thaliana RER5 gene Proteins 0.000 claims 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical compound OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 claims 1
- 206010007134 Candida infections Diseases 0.000 claims 1
- 206010013883 Dwarfism Diseases 0.000 claims 1
- 208000008955 Mucolipidoses Diseases 0.000 claims 1
- 206010072928 Mucolipidosis type II Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 239000008186 active pharmaceutical agent Substances 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 229940088710 antibiotic agent Drugs 0.000 claims 1
- 229960005475 antiinfective agent Drugs 0.000 claims 1
- 239000004599 antimicrobial Substances 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 125000000319 biphenyl-4-yl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000000532 dioxanyl group Chemical group 0.000 claims 1
- 239000003172 expectorant agent Substances 0.000 claims 1
- 125000002249 indol-2-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([*])=C([H])C2=C1[H] 0.000 claims 1
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 208000020460 mucolipidosis II alpha/beta Diseases 0.000 claims 1
- 229940066491 mucolytics Drugs 0.000 claims 1
- 235000016709 nutrition Nutrition 0.000 claims 1
- 208000030761 polycystic kidney disease Diseases 0.000 claims 1
- 102000012605 Cystic Fibrosis Transmembrane Conductance Regulator Human genes 0.000 description 29
- 108010079245 Cystic Fibrosis Transmembrane Conductance Regulator Proteins 0.000 description 29
- 108090000623 proteins and genes Proteins 0.000 description 22
- 230000032258 transport Effects 0.000 description 16
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 14
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 13
- 102000004169 proteins and genes Human genes 0.000 description 13
- 210000000170 cell membrane Anatomy 0.000 description 10
- 210000004027 cell Anatomy 0.000 description 9
- 230000028327 secretion Effects 0.000 description 7
- 125000004432 carbon atom Chemical group C* 0.000 description 6
- 230000002950 deficient Effects 0.000 description 6
- 230000035772 mutation Effects 0.000 description 6
- 239000011734 sodium Substances 0.000 description 6
- 241001465754 Metazoa Species 0.000 description 5
- 230000034994 death Effects 0.000 description 5
- 231100000517 death Toxicity 0.000 description 5
- 150000002430 hydrocarbons Chemical group 0.000 description 5
- 210000003097 mucus Anatomy 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- 150000001450 anions Chemical class 0.000 description 4
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 description 4
- 230000001413 cellular effect Effects 0.000 description 4
- 210000000981 epithelium Anatomy 0.000 description 4
- 239000012530 fluid Substances 0.000 description 4
- 230000007257 malfunction Effects 0.000 description 4
- 230000002829 reductive effect Effects 0.000 description 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 3
- 101150029409 CFTR gene Proteins 0.000 description 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 3
- 230000002159 abnormal effect Effects 0.000 description 3
- 238000009825 accumulation Methods 0.000 description 3
- 230000001684 chronic effect Effects 0.000 description 3
- 125000004122 cyclic group Chemical group 0.000 description 3
- 230000018044 dehydration Effects 0.000 description 3
- 238000006297 dehydration reaction Methods 0.000 description 3
- 238000012217 deletion Methods 0.000 description 3
- 230000037430 deletion Effects 0.000 description 3
- 239000012528 membrane Substances 0.000 description 3
- 239000011593 sulfur Substances 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 208000030507 AIDS Diseases 0.000 description 2
- ZKHQWZAMYRWXGA-KQYNXXCUSA-J ATP(4-) Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](COP([O-])(=O)OP([O-])(=O)OP([O-])([O-])=O)[C@@H](O)[C@H]1O ZKHQWZAMYRWXGA-KQYNXXCUSA-J 0.000 description 2
- ZKHQWZAMYRWXGA-UHFFFAOYSA-N Adenosine triphosphate Natural products C1=NC=2C(N)=NC=NC=2N1C1OC(COP(O)(=O)OP(O)(=O)OP(O)(O)=O)C(O)C1O ZKHQWZAMYRWXGA-UHFFFAOYSA-N 0.000 description 2
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 description 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 description 2
- 108010078791 Carrier Proteins Proteins 0.000 description 2
- 241000711573 Coronaviridae Species 0.000 description 2
- 241000790917 Dioxys <bee> Species 0.000 description 2
- 206010013774 Dry eye Diseases 0.000 description 2
- 208000028782 Hereditary disease Diseases 0.000 description 2
- 101100533874 Hypocrea jecorina (strain QM6a) sor5 gene Proteins 0.000 description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 description 2
- 108010021466 Mutant Proteins Proteins 0.000 description 2
- 102000008300 Mutant Proteins Human genes 0.000 description 2
- 206010039231 Rotaviral infections Diseases 0.000 description 2
- 102000003673 Symporters Human genes 0.000 description 2
- 108090000088 Symporters Proteins 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
- 230000001580 bacterial effect Effects 0.000 description 2
- 230000015556 catabolic process Effects 0.000 description 2
- 125000003636 chemical group Chemical group 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 230000008878 coupling Effects 0.000 description 2
- 238000010168 coupling process Methods 0.000 description 2
- 238000005859 coupling reaction Methods 0.000 description 2
- 230000003247 decreasing effect Effects 0.000 description 2
- 238000006731 degradation reaction Methods 0.000 description 2
- 125000005805 dimethoxy phenyl group Chemical group 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 210000002919 epithelial cell Anatomy 0.000 description 2
- 210000004907 gland Anatomy 0.000 description 2
- 230000001771 impaired effect Effects 0.000 description 2
- 150000002500 ions Chemical class 0.000 description 2
- 230000002132 lysosomal effect Effects 0.000 description 2
- 230000007246 mechanism Effects 0.000 description 2
- 230000000420 mucociliary effect Effects 0.000 description 2
- 239000002773 nucleotide Substances 0.000 description 2
- 125000003729 nucleotide group Chemical group 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- 230000000241 respiratory effect Effects 0.000 description 2
- 230000003248 secreting effect Effects 0.000 description 2
- 201000009881 secretory diarrhea Diseases 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 239000002753 trypsin inhibitor Substances 0.000 description 2
- 210000001215 vagina Anatomy 0.000 description 2
- 230000003612 virological effect Effects 0.000 description 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 description 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- XUSNPFGLKGCWGN-UHFFFAOYSA-N 3-[4-(3-aminopropyl)piperazin-1-yl]propan-1-amine Chemical compound NCCCN1CCN(CCCN)CC1 XUSNPFGLKGCWGN-UHFFFAOYSA-N 0.000 description 1
- 102000041092 ABC transporter family Human genes 0.000 description 1
- 108091060858 ABC transporter family Proteins 0.000 description 1
- 208000010444 Acidosis Diseases 0.000 description 1
- 102000010637 Aquaporins Human genes 0.000 description 1
- 108010063290 Aquaporins Proteins 0.000 description 1
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- 206010006448 Bronchiolitis Diseases 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 241000283707 Capra Species 0.000 description 1
- 208000009043 Chemical Burns Diseases 0.000 description 1
- 206010008631 Cholera Diseases 0.000 description 1
- 241000761389 Copa Species 0.000 description 1
- 241000223935 Cryptosporidium Species 0.000 description 1
- 206010061818 Disease progression Diseases 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 241000283086 Equidae Species 0.000 description 1
- 241000282326 Felis catus Species 0.000 description 1
- 108010049003 Fibrinogen Proteins 0.000 description 1
- 102000008946 Fibrinogen Human genes 0.000 description 1
- 201000011240 Frontotemporal dementia Diseases 0.000 description 1
- 102000002464 Galactosidases Human genes 0.000 description 1
- 108010093031 Galactosidases Proteins 0.000 description 1
- 241000224467 Giardia intestinalis Species 0.000 description 1
- 102000003886 Glycoproteins Human genes 0.000 description 1
- 108090000288 Glycoproteins Proteins 0.000 description 1
- 102100020948 Growth hormone receptor Human genes 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 208000026350 Inborn Genetic disease Diseases 0.000 description 1
- 108010001127 Insulin Receptor Proteins 0.000 description 1
- 102100036721 Insulin receptor Human genes 0.000 description 1
- 208000019693 Lung disease Diseases 0.000 description 1
- 208000002720 Malnutrition Diseases 0.000 description 1
- 108010052285 Membrane Proteins Proteins 0.000 description 1
- 102000003939 Membrane transport proteins Human genes 0.000 description 1
- 108090000301 Membrane transport proteins Proteins 0.000 description 1
- 102000014842 Multidrug resistance proteins Human genes 0.000 description 1
- 108050005144 Multidrug resistance proteins Proteins 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 description 1
- 208000035467 Pancreatic insufficiency Diseases 0.000 description 1
- 102100036893 Parathyroid hormone Human genes 0.000 description 1
- 241001494479 Pecora Species 0.000 description 1
- 102100035917 Peripheral myelin protein 22 Human genes 0.000 description 1
- 101710199257 Peripheral myelin protein 22 Proteins 0.000 description 1
- 208000000609 Pick Disease of the Brain Diseases 0.000 description 1
- 108010050254 Presenilins Proteins 0.000 description 1
- 102000015499 Presenilins Human genes 0.000 description 1
- 108010050808 Procollagen Proteins 0.000 description 1
- 241000702670 Rotavirus Species 0.000 description 1
- 241000607142 Salmonella Species 0.000 description 1
- 238000012300 Sequence Analysis Methods 0.000 description 1
- 108010068542 Somatotropin Receptors Proteins 0.000 description 1
- 102000018075 Subfamily B ATP Binding Cassette Transporter Human genes 0.000 description 1
- 108010091105 Subfamily B ATP Binding Cassette Transporter Proteins 0.000 description 1
- 241000282887 Suidae Species 0.000 description 1
- 201000009594 Systemic Scleroderma Diseases 0.000 description 1
- 206010042953 Systemic sclerosis Diseases 0.000 description 1
- 208000037913 T-cell disorder Diseases 0.000 description 1
- 241001122767 Theaceae Species 0.000 description 1
- 206010053615 Thermal burn Diseases 0.000 description 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical group C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 description 1
- 102000004357 Transferases Human genes 0.000 description 1
- 108090000992 Transferases Proteins 0.000 description 1
- 102000003425 Tyrosinase Human genes 0.000 description 1
- 108060008724 Tyrosinase Proteins 0.000 description 1
- GXBMIBRIOWHPDT-UHFFFAOYSA-N Vasopressin Natural products N1C(=O)C(CC=2C=C(O)C=CC=2)NC(=O)C(N)CSSCC(C(=O)N2C(CCC2)C(=O)NC(CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CCC(N)=O)NC(=O)C1CC1=CC=CC=C1 GXBMIBRIOWHPDT-UHFFFAOYSA-N 0.000 description 1
- 108090000643 Vasopressin Receptors Proteins 0.000 description 1
- 102000004136 Vasopressin Receptors Human genes 0.000 description 1
- 102000002852 Vasopressins Human genes 0.000 description 1
- 108010004977 Vasopressins Proteins 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 1
- 230000007950 acidosis Effects 0.000 description 1
- 208000026545 acidosis disease Diseases 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- 230000009056 active transport Effects 0.000 description 1
- 201000009840 acute diarrhea Diseases 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 210000005058 airway cell Anatomy 0.000 description 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 1
- IYABWNGZIDDRAK-UHFFFAOYSA-N allene Chemical group C=C=C IYABWNGZIDDRAK-UHFFFAOYSA-N 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 239000000427 antigen Substances 0.000 description 1
- 108091007433 antigens Proteins 0.000 description 1
- 102000036639 antigens Human genes 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- KBZOIRJILGZLEJ-LGYYRGKSSA-N argipressin Chemical compound C([C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@@H](C(N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N1)=O)N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C1=CC=CC=C1 KBZOIRJILGZLEJ-LGYYRGKSSA-N 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 125000003710 aryl alkyl group Chemical group 0.000 description 1
- 125000005160 aryl oxy alkyl group Chemical group 0.000 description 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 230000005779 cell damage Effects 0.000 description 1
- 208000037887 cell injury Diseases 0.000 description 1
- 150000001805 chlorine compounds Chemical class 0.000 description 1
- 210000000349 chromosome Anatomy 0.000 description 1
- 208000019902 chronic diarrheal disease Diseases 0.000 description 1
- 231100000762 chronic effect Toxicity 0.000 description 1
- 239000003541 chymotrypsin inhibitor Substances 0.000 description 1
- 210000000399 corneal endothelial cell Anatomy 0.000 description 1
- 125000004802 cyanophenyl group Chemical group 0.000 description 1
- 229940127089 cytotoxic agent Drugs 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 230000007123 defense Effects 0.000 description 1
- 230000000741 diarrhetic effect Effects 0.000 description 1
- 230000005750 disease progression Effects 0.000 description 1
- 239000003596 drug target Substances 0.000 description 1
- 239000003792 electrolyte Substances 0.000 description 1
- 210000002472 endoplasmic reticulum Anatomy 0.000 description 1
- 229940088598 enzyme Drugs 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 210000003608 fece Anatomy 0.000 description 1
- 230000035558 fertility Effects 0.000 description 1
- 229940012952 fibrinogen Drugs 0.000 description 1
- 230000020764 fibrinolysis Effects 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 208000016361 genetic disease Diseases 0.000 description 1
- 229940085435 giardia lamblia Drugs 0.000 description 1
- 125000005059 halophenyl group Chemical group 0.000 description 1
- 125000004475 heteroaralkyl group Chemical group 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 108091008039 hormone receptors Proteins 0.000 description 1
- 230000036571 hydration Effects 0.000 description 1
- 238000006703 hydration reaction Methods 0.000 description 1
- 210000000987 immune system Anatomy 0.000 description 1
- 239000012678 infectious agent Substances 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 208000021267 infertility disease Diseases 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000004807 localization Effects 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 206010025135 lupus erythematosus Diseases 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 230000003211 malignant effect Effects 0.000 description 1
- 230000001071 malnutrition Effects 0.000 description 1
- 235000000824 malnutrition Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000002483 medication Methods 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 230000005012 migration Effects 0.000 description 1
- 238000013508 migration Methods 0.000 description 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 1
- 208000015380 nutritional deficiency disease Diseases 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- 125000004430 oxygen atom Chemical group O* 0.000 description 1
- 239000002831 pharmacologic agent Substances 0.000 description 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 description 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N phenylalanine group Chemical group N[C@@H](CC1=CC=CC=C1)C(=O)O COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 description 1
- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 108010091624 preproparathormone Proteins 0.000 description 1
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 description 1
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 1
- 208000007153 proteostasis deficiencies Diseases 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 230000000580 secretagogue effect Effects 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
- 230000036575 thermal burns Effects 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 229960003726 vasopressin Drugs 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
- 239000002676 xenobiotic agent Substances 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- 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
- A61P11/08—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
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- 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
- 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
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- A61P35/00—Antineoplastic 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
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- 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
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
- C07D263/48—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/44—Acylated amino or imino radicals
- C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/68—Benzothiazoles 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 in position 2
- C07D277/82—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
- G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
- G01N33/5076—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics involving cell organelles, e.g. Golgi complex, endoplasmic reticulum
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Molecular Biology (AREA)
- Psychology (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Food Science & Technology (AREA)
- Physics & Mathematics (AREA)
- Pathology (AREA)
- General Physics & Mathematics (AREA)
- Biochemistry (AREA)
- Toxicology (AREA)
- Analytical Chemistry (AREA)
- Tropical Medicine & Parasitology (AREA)
- Biotechnology (AREA)
- Cell Biology (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US50044403P | 2003-09-06 | 2003-09-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200602755B true ZA200602755B (en) | 2007-06-27 |
Family
ID=34312193
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200602755A ZA200602755B (en) | 2003-09-06 | 2004-09-07 | Modulators of ATP-binding cassette transporters |
Country Status (13)
| Country | Link |
|---|---|
| US (6) | US7973169B2 (enExample) |
| EP (1) | EP1664006A2 (enExample) |
| JP (1) | JP2007504255A (enExample) |
| KR (1) | KR20060088537A (enExample) |
| CN (1) | CN1898221A (enExample) |
| AU (1) | AU2004272599A1 (enExample) |
| CA (1) | CA2537841A1 (enExample) |
| IL (1) | IL174128A0 (enExample) |
| MX (1) | MXPA06002567A (enExample) |
| NO (1) | NO20061543L (enExample) |
| RU (1) | RU2006111093A (enExample) |
| WO (1) | WO2005026137A2 (enExample) |
| ZA (1) | ZA200602755B (enExample) |
Families Citing this family (112)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA80295C2 (en) | 2002-09-06 | 2007-09-10 | Biogen Inc | Pyrazolopyridines and using the same |
| AR044519A1 (es) | 2003-05-02 | 2005-09-14 | Novartis Ag | Derivados de piridin-tiazol amina y de pirimidin-tiazol amina |
| US7973169B2 (en) | 2003-09-06 | 2011-07-05 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
| ATE437640T1 (de) * | 2003-11-14 | 2009-08-15 | Vertex Pharma | Thiazole udn oxazole als modulatoren von atp- bindungs-kassetten-transportern |
| EP3002283B1 (en) * | 2003-12-26 | 2017-06-14 | Kyowa Hakko Kirin Co., Ltd. | Thiazole derivatives |
| US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| US7384968B2 (en) * | 2004-04-01 | 2008-06-10 | Pfizer Inc. | Thiazole-amine compounds for the treatment of neurodegenerative disorders |
| PL2502911T3 (pl) | 2004-06-24 | 2017-09-29 | Vertex Pharma | Modulatory transporterów kasety wiążącej ATP |
| US8148412B2 (en) * | 2004-12-03 | 2012-04-03 | Novo Nordisk A/S | Heteroaromatic glucokinase activators |
| WO2006127588A2 (en) * | 2005-05-24 | 2006-11-30 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
| CA2618057A1 (en) | 2005-08-11 | 2007-02-22 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| DK1945632T3 (da) | 2005-11-08 | 2013-12-16 | Vertex Pharma | Heterocycliske modulatorer af ATP-bindende kassettetransportører |
| US7671221B2 (en) * | 2005-12-28 | 2010-03-02 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
| WO2007079139A2 (en) | 2005-12-28 | 2007-07-12 | Vertex Pharmaceuticals, Inc. | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| CN101395147B (zh) * | 2005-12-28 | 2013-05-29 | 弗特克斯药品有限公司 | 作为atp-结合盒转运蛋白调节剂用于治疗囊性纤维化的1-(苯并[d][1,3]间二氧杂环戊烯-5-基)-n-(苯基)环丙烷-甲酰胺衍生物及相关化合物 |
| WO2007084391A2 (en) * | 2006-01-18 | 2007-07-26 | Amgen Inc. | Thiazole compounds as protein kinase b ( pkb) inhibitors |
| TWI444370B (zh) * | 2006-01-25 | 2014-07-11 | Synta Pharmaceuticals Corp | 用於發炎及免疫相關用途之噻唑及噻二唑化合物 |
| CA2640454A1 (en) * | 2006-01-26 | 2007-08-09 | Foldrx Pharmaceuticals, Inc. | Compounds and methods for modulating protein trafficking |
| USRE50453E1 (en) | 2006-04-07 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| US7645789B2 (en) | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| DK2007756T3 (en) | 2006-04-07 | 2015-10-05 | Vertex Pharma | MODULATORS OF ATP BINDING CASSETTE TRANSPORT |
| US10022352B2 (en) | 2006-04-07 | 2018-07-17 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| US8211925B2 (en) * | 2006-04-28 | 2012-07-03 | Transtech Pharma, Inc. | Benzamide glucokinase activators |
| CN101096363B (zh) * | 2006-06-27 | 2011-05-11 | 中国人民解放军军事医学科学院毒物药物研究所 | 2,4,5-三取代噻唑类化合物、其制备方法、药物组合物及其制药用途 |
| JPWO2008050600A1 (ja) * | 2006-10-25 | 2010-02-25 | 株式会社ニュージェン・ファーマ | 酸化ストレス性細胞死を分子背景とする難治性疾患の治療または予防剤 |
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| GB0701426D0 (en) * | 2007-01-25 | 2007-03-07 | Univ Sheffield | Compounds and their use |
| EP2332933A1 (en) | 2007-05-07 | 2011-06-15 | Novartis AG | Epithelial sodium channel (ENaC) inhibitors |
| EP2789606B1 (en) | 2007-05-09 | 2017-11-15 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
| US7919504B2 (en) * | 2007-07-17 | 2011-04-05 | Amgen Inc. | Thiadiazole modulators of PKB |
| CA2692713A1 (en) | 2007-07-17 | 2009-01-22 | Amgen Inc. | Heterocyclic modulators of pkb |
| RU2476429C2 (ru) * | 2007-07-31 | 2013-02-27 | Сионоги Энд Ко., Лтд. | Фармацевтическая композиция, содержащая оптически активное соединение, обладающее активностью агониста рецептора тромбопоэтина, и промежуточное соединение для этого |
| 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 |
| PL2578571T3 (pl) | 2007-11-16 | 2016-03-31 | Vertex Pharma | Modulatory izochinolinowe transporterów zawierających kasetę wiążącą ATP |
| US20090176839A1 (en) * | 2007-12-07 | 2009-07-09 | Ali Keshavarz-Shokri | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| ES2604555T3 (es) * | 2007-12-07 | 2017-03-07 | Vertex Pharmaceuticals Incorporated | Procedimiento para producir ácidos cicloalquilcarboxiamido-piridinabenzoicos |
| KR20160040745A (ko) | 2007-12-07 | 2016-04-14 | 버텍스 파마슈티칼스 인코포레이티드 | 3-(6-(1-(2,2-디플루오로벤조[d][1,3]디옥솔-5-일)사이클로프로판카복스아미도)-3-메틸피리딘-2-일)벤조산의 고체 형태 |
| US20100036130A1 (en) | 2007-12-07 | 2010-02-11 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| AR069637A1 (es) | 2007-12-10 | 2010-02-10 | Novartis Ag | Derivados de pirazinas |
| AR069798A1 (es) | 2007-12-20 | 2010-02-17 | Novartis Ag | Derivados de 1, 3-tiazol, metodos para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la manufactura de medicamentos para el tratamiento de enfermedades mediadas por la fosfatidilinositol 3-cinasa. |
| NZ720282A (en) | 2008-02-28 | 2017-12-22 | Vertex Pharma | Heteroaryl derivatives as cftr modulators |
| CN103951614A (zh) | 2008-03-31 | 2014-07-30 | 沃泰克斯药物股份有限公司 | 作为cftr调节剂的吡啶基衍生物 |
| CN102088973A (zh) * | 2008-05-15 | 2011-06-08 | 杜克大学 | 与热休克转录因子激活化合物及其靶标有关的组合物和方法 |
| US9315449B2 (en) | 2008-05-15 | 2016-04-19 | Duke University | Substituted pyrazoles as heat shock transcription factor activators |
| BRPI0915018A2 (pt) | 2008-06-10 | 2015-10-27 | Novartis Ag | compostos orgânicos |
| 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 |
| UA104147C2 (uk) | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| 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 |
| DK2349263T3 (da) * | 2008-10-23 | 2014-07-21 | Vertex Pharma | Modulatorer af transmembranledningsevneregulatoren for cystisk fibrose |
| UA104876C2 (uk) * | 2008-11-06 | 2014-03-25 | Вертекс Фармасьютікалз Інкорпорейтед | Модулятори atф-зв'язувальних касетних транспортерів |
| SG173884A1 (en) | 2009-02-27 | 2011-10-28 | Teijin Pharma Ltd | Process for producing phenyl-substituted heterocyclic derivative through coupling using transition metal catalyst |
| CA3071058C (en) | 2009-03-20 | 2023-01-24 | Vertex Pharmaceuticals Incorporated | Process for making modulators of cystic fibrosis transmembrane conductance regulator |
| GB0905525D0 (en) * | 2009-03-31 | 2009-05-13 | Univ Leiden | Compounds and uses |
| JP5624130B2 (ja) * | 2009-06-12 | 2014-11-12 | アクテリオンファーマシューティカルズ リミテッドActelion Pharmaceuticals Ltd | Alx受容体アゴニストとしてのオキサゾール及びチアゾール誘導体 |
| US8293753B2 (en) | 2009-07-02 | 2012-10-23 | Novartis Ag | Substituted 2-carboxamide cycloamino ureas |
| UY32748A (es) | 2009-07-02 | 2011-01-31 | Novartis Ag | 2-carboxamida-cicloamino-ureas |
| JP2013508414A (ja) | 2009-10-22 | 2013-03-07 | 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 | 嚢胞性線維症および他の慢性疾患の治療のための組成物 |
| WO2011076732A1 (en) * | 2009-12-21 | 2011-06-30 | Euroscreen S.A. | Compounds, pharmaceutical composition and methods for use in treating gastrointestinal disorders |
| WO2011076734A1 (en) * | 2009-12-21 | 2011-06-30 | Euroscreen S.A. | Compounds, pharmaceutical composition and methods for use in treating inflammatory diseases |
| CA2793311C (en) * | 2010-03-17 | 2019-01-15 | Taivex Therapeutics Inc. | Modulators of hec1 activity and methods therefor |
| 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 |
| CN102933206A (zh) | 2010-04-07 | 2013-02-13 | 弗特克斯药品有限公司 | 3-(6-(1-(2,2-二氟苯并[d][1,3]二氧杂环戊烯-5-基)环丙烷甲酰胺基)-3-甲基吡啶-2-基)苯甲酸的固体形式 |
| NZ602838A (en) | 2010-04-07 | 2015-06-26 | Vertex Pharma | Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid and administration thereof |
| KR20130056244A (ko) | 2010-04-22 | 2013-05-29 | 버텍스 파마슈티칼스 인코포레이티드 | 시클로알킬카르복스아미도-인돌 화합물의 제조 방법 |
| 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 |
| US8975411B2 (en) | 2010-07-28 | 2015-03-10 | Neugen Pharma Inc. | Therapeutic agent for neurological diseases |
| EP2610248B1 (en) | 2010-08-27 | 2016-06-08 | Teijin Pharma Limited | Method for producing phenyl-substituted heterocyclic derivative by means of coupling method using a palladium compound |
| US8372845B2 (en) | 2010-09-17 | 2013-02-12 | Novartis Ag | Pyrazine derivatives as enac blockers |
| KR101367568B1 (ko) * | 2011-05-31 | 2014-02-27 | 임우석 | Abc 수송체 조절을 통한 퇴행성신경질환에서 이상단백질 조절 |
| WO2013019621A1 (en) * | 2011-07-29 | 2013-02-07 | Tempero Pharmaceuticals, Inc. | Compounds and methods |
| WO2013033037A2 (en) * | 2011-08-26 | 2013-03-07 | The Regents Of The University Of California | Novel antiprion compounds |
| DE102011083283A1 (de) * | 2011-09-23 | 2013-03-28 | Beiersdorf Ag | Heteroalkylamidothiazole, deren kosmetische oder dermatologische Verwendung sowie kosmetische oder dermatologische Zubereitungen mit einem Gehalt an solchen Heteroalkylamidothiazolen |
| DE102011083271A1 (de) * | 2011-09-23 | 2013-03-28 | Beiersdorf Ag | Aromatische Amidothiazole, deren kosmetische oder dermatologische Verwendung sowie kosmetische oder dermatologische Zubereitungen mit einem Gehalt an solchen Aromatischen Amidothiazolen |
| KR101985044B1 (ko) | 2011-11-08 | 2019-05-31 | 버텍스 파마슈티칼스 인코포레이티드 | Atp-결합 카세트 수송체의 조절제 |
| US11071736B2 (en) | 2011-11-21 | 2021-07-27 | Taivex Therapeutics Corporation | Modulators of HEC1 activity and methods therefor |
| SG10201506881PA (en) | 2011-11-21 | 2015-10-29 | Taivex Therapeutics Corp | Biomarkers for cancers responsive to modulators of hec1 activity |
| TWI640519B (zh) | 2011-11-29 | 2018-11-11 | 泰緯生命科技股份有限公司 | Hec1活性調控因子及其調節方法 |
| PT2806859T (pt) | 2012-01-25 | 2019-09-04 | Vertex Pharma | Formulações de ácido 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)ciclopropanocarboxamido)-3-metilpiridin-2-il)benzoico |
| MX389751B (es) | 2012-02-27 | 2025-03-20 | Vertex Pharma | Composición farmacéutica y administraciones de la misma. |
| US8809340B2 (en) | 2012-03-19 | 2014-08-19 | Novartis Ag | Crystalline form |
| 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 |
| AU2013290444B2 (en) | 2012-07-16 | 2018-04-26 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[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 and administration thereof |
| ES2489297B1 (es) | 2013-01-22 | 2015-06-10 | Consejo Superior De Investigaciones Científicas (Csic) | Benzotiazoles sustituidos y sus aplicaciones terapeuticas para el tratamiento de enfermedades humanas |
| TW201506024A (zh) | 2013-07-02 | 2015-02-16 | 必治妥美雅史谷比公司 | 作為有效rock抑制劑的三環甲醯胺衍生物 |
| CN105518005B (zh) | 2013-07-02 | 2018-07-20 | 百时美施贵宝公司 | 作为rock抑制剂的三环吡啶-甲酰胺衍生物 |
| WO2015073231A1 (en) | 2013-11-12 | 2015-05-21 | Vertex Pharmaceuticals Incorporated | Process of preparing pharmaceutical compositions for the treatment of cftr mediated diseases |
| GB201401886D0 (en) | 2014-02-04 | 2014-03-19 | Lytix Biopharma As | Neurodegenerative therapies |
| KR102447581B1 (ko) | 2014-04-15 | 2022-09-28 | 버텍스 파마슈티칼스 인코포레이티드 | 낭포성 섬유증 막전도 조절자 매개 질환 치료용 약제학적 조성물 |
| RU2749213C2 (ru) | 2014-10-07 | 2021-06-07 | Вертекс Фармасьютикалз Инкорпорейтед | Сокристаллы модуляторов регулятора трансмембранной проводимости при кистозном фиброзе |
| SG11201703963QA (en) | 2014-11-18 | 2017-06-29 | Vertex Pharma | Process of conducting high throughput testing high performance liquid chromatography |
| AU2016233568A1 (en) | 2015-03-13 | 2017-10-05 | Forma Therapeutics, Inc. | Alpha-cinnamide compounds and compositions as HDAC8 inhibitors |
| AU2017249602B2 (en) | 2016-04-11 | 2022-06-16 | Genfit | Methods of treatment for cholestatic and fibrotic diseases |
| US20170290814A1 (en) * | 2016-04-11 | 2017-10-12 | Genfit | Methods of treatment of cholestasis and fibrosis |
| WO2018027193A1 (en) * | 2016-08-05 | 2018-02-08 | The Regents Of The University Of California | Gp130 modulators |
| MA46589A (fr) | 2016-10-24 | 2019-08-28 | Yumanity Therapeutics Inc | Composés et utilisations de ces derniers |
| AU2017358901B2 (en) * | 2016-11-03 | 2023-01-05 | Corvus Pharmaceuticals, Inc. | Compounds and methods for modulating interleukin-2-inducible T-cell kinase |
| AU2018205275B2 (en) | 2017-01-06 | 2024-05-02 | Janssen Pharmaceutica Nv | Methods for the treatment of neurological disorders |
| EA202092225A1 (ru) | 2018-03-23 | 2021-02-09 | Юманити Терапьютикс, Инк. | Соединения и их применение |
| WO2019241376A1 (en) * | 2018-06-14 | 2019-12-19 | The Trustees Of Columbia University In The City Of New York | Treatment of cognitive disorders using nitazoxanide (ntz), nitazoxanide (ntz) analogs, and metabolites thereof |
| US12098146B2 (en) | 2019-01-24 | 2024-09-24 | Janssen Pharmaceutica Nv | Compounds and uses thereof |
| US20230029266A1 (en) * | 2019-11-05 | 2023-01-26 | Dermira, Inc. | MrgprX2 Antagonists for the Treatment of Inflammatory Disorders |
| CA3158057A1 (en) * | 2019-11-12 | 2021-05-20 | Genzyme Corporation | 5-membered heteroarylaminosulfonamides for treating conditions mediated by deficient cftr activity |
| EA202192047A1 (ru) | 2019-11-13 | 2021-12-08 | Юманити Терапьютикс, Инк. | Соединения и их применение |
| 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 |
| US12404242B2 (en) | 2021-12-17 | 2025-09-02 | Reglagene, Inc. | Compositions and methods for making and using small molecules in the treatment of cancer |
| GB2615307A (en) * | 2022-01-28 | 2023-08-09 | Adorx Therapeutics Ltd | Antagonist compounds |
| CN114874155B (zh) * | 2022-05-10 | 2024-02-06 | 华南理工大学 | 一类苄基噻唑胺类化合物及其制备方法与抗肿瘤应用 |
| EP4342467A1 (en) * | 2022-09-20 | 2024-03-27 | Masarykova Univerzita | Ku inhibitors for use in tumor therapy |
| EP4673130A1 (en) | 2023-02-28 | 2026-01-07 | Reglagene, Inc. | Compositions and methods for making and using small molecules for the treatment of health conditions |
| CN116621794B (zh) * | 2023-05-22 | 2025-03-11 | 上海大学 | 一种5-苄基-2-氨基-1,3-噻唑类衍生物及其合成方法与应用 |
Family Cites Families (84)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4129742A1 (de) * | 1991-09-06 | 1993-03-11 | Bayer Ag | Heterocyclisch substituierte chinolylmethoxy-phenylacetamide |
| DE69425882T2 (de) * | 1993-03-29 | 2001-01-11 | Basf Ag | 1-amino-3-phenoxy-propan-derivate als modulatoren bei multi-drug resistenz |
| WO1994022846A1 (en) | 1993-03-30 | 1994-10-13 | Pfizer Inc. | Compounds enhancing antitumor activity of other cytotoxic agents |
| GB9823871D0 (en) * | 1998-10-30 | 1998-12-23 | Pharmacia & Upjohn Spa | 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents |
| TW593241B (en) * | 1999-04-20 | 2004-06-21 | Hoffmann La Roche | Carbamic acid derivatives |
| CA2395513A1 (en) | 1999-12-22 | 2001-06-28 | Rosanne Bonjouklian | Methods and compounds for inhibiting mrp1 |
| MXPA05004689A (es) * | 2002-10-30 | 2005-12-05 | Vertex Pharma | Composiciones utiles como inhibidores de rock y otras proteinas cinasas. |
| US20050113423A1 (en) | 2003-03-12 | 2005-05-26 | Vangoor Frederick F. | Modulators of ATP-binding cassette transporters |
| DE602004022819D1 (de) | 2003-06-06 | 2009-10-08 | Vertex Pharma | Von atp-bindende kassette transportern |
| US7973169B2 (en) | 2003-09-06 | 2011-07-05 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
| CN1886393A (zh) | 2003-10-08 | 2006-12-27 | 沃泰克斯药物股份有限公司 | 含有环烷基或吡喃基基团的atp-结合弹夹转运蛋白的调控剂 |
| ATE437640T1 (de) | 2003-11-14 | 2009-08-15 | Vertex Pharma | Thiazole udn oxazole als modulatoren von atp- bindungs-kassetten-transportern |
| EP3219709B1 (en) | 2004-01-30 | 2020-03-18 | Vertex Pharmaceuticals Incorporated | Intermediate compound of modulators of atp-binding cassette transporters |
| US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| PL2502911T3 (pl) | 2004-06-24 | 2017-09-29 | Vertex Pharma | Modulatory transporterów kasety wiążącej ATP |
| US8354427B2 (en) | 2004-06-24 | 2013-01-15 | Vertex Pharmaceutical Incorporated | Modulators of ATP-binding cassette transporters |
| EP1865949B1 (en) | 2005-03-11 | 2012-11-14 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| WO2006127588A2 (en) | 2005-05-24 | 2006-11-30 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
| CA2618057A1 (en) | 2005-08-11 | 2007-02-22 | 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 |
| DK1945632T3 (da) | 2005-11-08 | 2013-12-16 | Vertex Pharma | Heterocycliske modulatorer af ATP-bindende kassettetransportører |
| WO2007075901A2 (en) | 2005-12-24 | 2007-07-05 | Vertex Pharmaceuticals Incorporated | Quinolin- 4 - one derivatives as modulators of abc transporters |
| CA2635214A1 (en) | 2005-12-27 | 2007-07-05 | Vertex Pharmaceuticals Incorporated | Compounds useful in cftr assays and methods therewith |
| WO2007079139A2 (en) | 2005-12-28 | 2007-07-12 | Vertex Pharmaceuticals, Inc. | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| CN101395147B (zh) | 2005-12-28 | 2013-05-29 | 弗特克斯药品有限公司 | 作为atp-结合盒转运蛋白调节剂用于治疗囊性纤维化的1-(苯并[d][1,3]间二氧杂环戊烯-5-基)-n-(苯基)环丙烷-甲酰胺衍生物及相关化合物 |
| 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 |
| DK2007756T3 (en) | 2006-04-07 | 2015-10-05 | Vertex Pharma | MODULATORS OF ATP BINDING CASSETTE TRANSPORT |
| CA2652072A1 (en) | 2006-05-12 | 2007-11-22 | Vertex Pharmaceuticals Incorporated | Compositions of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| 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 |
| CA2688004C (en) | 2007-05-25 | 2016-07-05 | Vertex Pharmaceuticals Incorporated | Thienopyridone compounds for use as modulators of cystic fibrosis transmembrane conductance regulator |
| WO2009023509A2 (en) | 2007-08-09 | 2009-02-19 | 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 |
| CN101918366A (zh) | 2007-09-14 | 2010-12-15 | 弗特克斯药品有限公司 | N-[2,4-双(1,1-二甲基乙基)-5-羟基苯基]-1,4-二氢-4-氧代喹啉-3-甲酰胺的固体形式 |
| PL2578571T3 (pl) | 2007-11-16 | 2016-03-31 | Vertex Pharma | Modulatory izochinolinowe transporterów zawierających kasetę wiążącą ATP |
| KR20160040745A (ko) | 2007-12-07 | 2016-04-14 | 버텍스 파마슈티칼스 인코포레이티드 | 3-(6-(1-(2,2-디플루오로벤조[d][1,3]디옥솔-5-일)사이클로프로판카복스아미도)-3-메틸피리딘-2-일)벤조산의 고체 형태 |
| US20090176839A1 (en) | 2007-12-07 | 2009-07-09 | Ali Keshavarz-Shokri | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| US20100036130A1 (en) | 2007-12-07 | 2010-02-11 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| ES2604555T3 (es) | 2007-12-07 | 2017-03-07 | Vertex Pharmaceuticals Incorporated | Procedimiento para producir ácidos cicloalquilcarboxiamido-piridinabenzoicos |
| 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 |
| US8216666B2 (en) | 2008-02-29 | 2012-07-10 | The Procter & Gamble Company | Substrates having improved crockfastness |
| CN103951614A (zh) | 2008-03-31 | 2014-07-30 | 沃泰克斯药物股份有限公司 | 作为cftr调节剂的吡啶基衍生物 |
| US20100256184A1 (en) | 2008-08-13 | 2010-10-07 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| NZ591535A (en) | 2008-08-13 | 2012-12-21 | Vertex Pharma | Pharmaceutcial composition comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| 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 |
| US8436014B2 (en) | 2008-10-23 | 2013-05-07 | Vertex Pharmaceutical Incorporated | Solid forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluorormethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihyroquinoline-3-carboxamide |
| EP2358721B1 (en) | 2008-10-23 | 2014-12-10 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| DK2349263T3 (da) | 2008-10-23 | 2014-07-21 | Vertex Pharma | Modulatorer af transmembranledningsevneregulatoren for cystisk fibrose |
| JP5699090B2 (ja) | 2008-12-30 | 2015-04-08 | 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Vertex Pharmaceuticals Incorporated | 嚢胞性線維症膜コンダクタンス調節因子のモジュレーター |
| CA3071058C (en) | 2009-03-20 | 2023-01-24 | Vertex Pharmaceuticals Incorporated | Process for making modulators of cystic fibrosis transmembrane conductance regulator |
| MX2011009868A (es) | 2009-03-20 | 2012-01-12 | Vertex Pharma | Moduladores del regulador de conductancia transmembrana de fibrosis quistica. |
| KR20120083416A (ko) | 2009-09-17 | 2012-07-25 | 버텍스 파마슈티칼스 인코포레이티드 | 아자비시클릭 화합물의 제조 방법 |
| JP2013508414A (ja) | 2009-10-22 | 2013-03-07 | 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 | 嚢胞性線維症および他の慢性疾患の治療のための組成物 |
| CN102648182A (zh) | 2009-10-23 | 2012-08-22 | 沃泰克斯药物股份有限公司 | 用于制备囊性纤维化跨膜传导调节因子的调节剂的方法 |
| JP5877157B2 (ja) | 2009-10-23 | 2016-03-02 | 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 | N−(4−(7−アザビシクロ[2.2.1]ヘプタン−7−イル)−2−(トリフルオロメチル)フェニル)−4−オキソ−5−(トリフルオロメチル)−1,4−ジヒドロキノリン−3−カルボキサミドの固体形態 |
| WO2011116397A1 (en) | 2010-03-19 | 2011-09-22 | Vertex Pharmaceuticals Incorporated | Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| 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 |
| EP4253381A3 (en) | 2010-03-25 | 2023-11-01 | Vertex Pharmaceuticals Incorporated | Solid forms of (r)-1-(2,2-difluorobenzo[d][1,3]d ioxol-5-yl)-n-(1-(2,3-dihydroxyp ropyl)-6-fluoro-2-(1-hydroxy- 2-methylpropan-2-yl)-1h-indol- 5-yl) cyclopropanecarboxamide |
| CN102933206A (zh) | 2010-04-07 | 2013-02-13 | 弗特克斯药品有限公司 | 3-(6-(1-(2,2-二氟苯并[d][1,3]二氧杂环戊烯-5-基)环丙烷甲酰胺基)-3-甲基吡啶-2-基)苯甲酸的固体形式 |
| NZ602838A (en) | 2010-04-07 | 2015-06-26 | Vertex Pharma | Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid and administration thereof |
| KR20130056244A (ko) | 2010-04-22 | 2013-05-29 | 버텍스 파마슈티칼스 인코포레이티드 | 시클로알킬카르복스아미도-인돌 화합물의 제조 방법 |
| CA2796642A1 (en) | 2010-04-22 | 2011-10-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| AU2011242454A1 (en) | 2010-04-22 | 2012-11-08 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| EP2560651A1 (en) | 2010-04-22 | 2013-02-27 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
| TW201202250A (en) | 2010-05-20 | 2012-01-16 | Vertex Pharma | Processes for producing modulators of cystic fibrosis transmembrane conductance regulator |
| NZ603386A (en) | 2010-05-20 | 2015-02-27 | Vertex Pharma | 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 |
| CA2808501A1 (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 |
| RU2013113627A (ru) | 2010-08-27 | 2014-10-10 | Вертекс Фармасьютикалз Инкорпорейтед | Фармацевтическая композиция и ее введения |
| US8802700B2 (en) | 2010-12-10 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
| KR101985044B1 (ko) | 2011-11-08 | 2019-05-31 | 버텍스 파마슈티칼스 인코포레이티드 | Atp-결합 카세트 수송체의 조절제 |
| PT2806859T (pt) | 2012-01-25 | 2019-09-04 | Vertex Pharma | Formulações de ácido 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)ciclopropanocarboxamido)-3-metilpiridin-2-il)benzoico |
| MX389751B (es) | 2012-02-27 | 2025-03-20 | Vertex Pharma | Composición farmacéutica y administraciones de la misma. |
| 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 |
| CA2874851A1 (en) | 2012-06-08 | 2013-12-12 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions for the treatment of cftr-mediated disorders |
| AU2013290444B2 (en) | 2012-07-16 | 2018-04-26 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[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 and administration thereof |
| EP4556008A3 (en) | 2012-11-02 | 2025-08-27 | 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 |
-
2004
- 2004-09-07 US US10/936,448 patent/US7973169B2/en active Active
- 2004-09-07 CN CNA200480031503XA patent/CN1898221A/zh active Pending
- 2004-09-07 KR KR1020067004627A patent/KR20060088537A/ko not_active Withdrawn
- 2004-09-07 ZA ZA200602755A patent/ZA200602755B/en unknown
- 2004-09-07 CA CA002537841A patent/CA2537841A1/en not_active Abandoned
- 2004-09-07 JP JP2006525534A patent/JP2007504255A/ja active Pending
- 2004-09-07 RU RU2006111093/04A patent/RU2006111093A/ru not_active Application Discontinuation
- 2004-09-07 WO PCT/US2004/029206 patent/WO2005026137A2/en not_active Ceased
- 2004-09-07 EP EP04783449A patent/EP1664006A2/en not_active Withdrawn
- 2004-09-07 AU AU2004272599A patent/AU2004272599A1/en not_active Abandoned
- 2004-09-07 MX MXPA06002567A patent/MXPA06002567A/es unknown
-
2006
- 2006-03-06 IL IL174128A patent/IL174128A0/en unknown
- 2006-04-05 NO NO20061543A patent/NO20061543L/no not_active Application Discontinuation
-
2011
- 2011-07-01 US US13/174,844 patent/US8431605B2/en not_active Expired - Fee Related
-
2013
- 2013-03-22 US US13/848,970 patent/US8741939B2/en not_active Expired - Lifetime
- 2013-11-14 US US14/079,664 patent/US8853415B2/en not_active Expired - Fee Related
-
2014
- 2014-10-06 US US14/506,856 patent/US9249131B2/en not_active Expired - Lifetime
-
2016
- 2016-01-29 US US15/010,542 patent/US20160228414A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| IL174128A0 (en) | 2006-08-01 |
| US7973169B2 (en) | 2011-07-05 |
| CA2537841A1 (en) | 2005-03-24 |
| NO20061543L (no) | 2006-06-06 |
| US20130252333A1 (en) | 2013-09-26 |
| WO2005026137A2 (en) | 2005-03-24 |
| KR20060088537A (ko) | 2006-08-04 |
| US8431605B2 (en) | 2013-04-30 |
| US8853415B2 (en) | 2014-10-07 |
| WO2005026137A3 (en) | 2005-07-21 |
| CN1898221A (zh) | 2007-01-17 |
| US8741939B2 (en) | 2014-06-03 |
| US20150025076A1 (en) | 2015-01-22 |
| US9249131B2 (en) | 2016-02-02 |
| JP2007504255A (ja) | 2007-03-01 |
| MXPA06002567A (es) | 2006-09-04 |
| US20160228414A1 (en) | 2016-08-11 |
| US20140072995A1 (en) | 2014-03-13 |
| AU2004272599A1 (en) | 2005-03-24 |
| EP1664006A2 (en) | 2006-06-07 |
| US20120004216A1 (en) | 2012-01-05 |
| US20050176789A1 (en) | 2005-08-11 |
| RU2006111093A (ru) | 2007-10-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ZA200602755B (en) | Modulators of ATP-binding cassette transporters | |
| ES2328824T3 (es) | Tiazoles y oxazoles utiles como moduladores de transportadores de tipo casete de union a atp. | |
| AU2008302598B2 (en) | Isothiazolopyridinones useful for the treatment of (inter alia) Cystic Fibrosis | |
| ES2631362T3 (es) | Moduladores de transportadores de casete de unión a ATP | |
| ZA200603515B (en) | Modulators of ATP-binding cassette transporters | |
| AU2008256717B2 (en) | Modulators of cystic fibrosis transmembrane conductance regulator | |
| US8609703B2 (en) | Modulators of ATP-binding cassette transporters | |
| ES2377840T3 (es) | Composiciones de N-[2,4-bis(1,1-dimetiletil)-5-hidroxifenil]-1,4-dihidro-4-oxoquinolina-3-carboxamida | |
| US20090105272A1 (en) | Prodrugs of modulators of ABC transporters |