MX2008011553A - Formulacion de polialcohol de ciclohexano para el tratamiento de transtornos de agregacion de proteinas. - Google Patents

Info

Publication number

MX2008011553A

MX2008011553A MX2008011553A MX2008011553A MX2008011553A MX 2008011553 A MX2008011553 A MX 2008011553A MX 2008011553 A MX2008011553 A MX 2008011553A MX 2008011553 A MX2008011553 A MX 2008011553A MX 2008011553 A MX2008011553 A MX 2008011553A

Authority

MX

Mexico

Prior art keywords

compound

dosage form

cyclohexane

alkyl

administration

Prior art date

2006-03-09

Links

• Espacenet
• Global Dossier
• Discuss

• 150000005846 sugar alcohols Polymers 0.000 title claims abstract description 155
• XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 title claims abstract description 149
• 239000000203 mixture Substances 0.000 title claims abstract description 147
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims abstract description 119
• 238000009472 formulation Methods 0.000 title claims abstract description 110
• 238000011282 treatment Methods 0.000 title claims abstract description 48
• 230000004845 protein aggregation Effects 0.000 title claims abstract description 6
• 208000035475 disorder Diseases 0.000 title description 42
• 150000001875 compounds Chemical class 0.000 claims abstract description 471
• 239000002552 dosage form Substances 0.000 claims abstract description 246
• 210000004556 brain Anatomy 0.000 claims abstract description 78
• 201000010099 disease Diseases 0.000 claims abstract description 72
• 210000001175 cerebrospinal fluid Anatomy 0.000 claims abstract description 70
• 230000009286 beneficial effect Effects 0.000 claims abstract description 30
• 230000036470 plasma concentration Effects 0.000 claims abstract description 29
• 238000009825 accumulation Methods 0.000 claims abstract description 24
• 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 24
• 230000003941 amyloidogenesis Effects 0.000 claims abstract description 19
• 230000002688 persistence Effects 0.000 claims abstract description 16
• 238000004220 aggregation Methods 0.000 claims abstract description 14
• 239000003085 diluting agent Substances 0.000 claims abstract description 9
• 230000007082 Aβ accumulation Effects 0.000 claims abstract description 8
• 239000003937 drug carrier Substances 0.000 claims abstract description 7
• -1 cyclohexane polyol compound Chemical class 0.000 claims description 482
• 229920005862 polyol Polymers 0.000 claims description 142
• 210000002381 plasma Anatomy 0.000 claims description 62
• 238000000034 method Methods 0.000 claims description 55
• 239000012730 sustained-release form Substances 0.000 claims description 47
• 238000013268 sustained release Methods 0.000 claims description 46
• 108090000765 processed proteins & peptides Proteins 0.000 claims description 43
• 239000003814 drug Substances 0.000 claims description 41
• 230000001225 therapeutic effect Effects 0.000 claims description 26
• 208000024891 symptom Diseases 0.000 claims description 23
• 108090000623 proteins and genes Proteins 0.000 claims description 20
• 102000004169 proteins and genes Human genes 0.000 claims description 19
• 238000004090 dissolution Methods 0.000 claims description 18
• 230000002265 prevention Effects 0.000 claims description 17
• 230000002776 aggregation Effects 0.000 claims description 11
• 238000010521 absorption reaction Methods 0.000 claims description 9
• 230000001976 improved effect Effects 0.000 claims description 8
• 238000002360 preparation method Methods 0.000 claims description 6
• 238000002156 mixing Methods 0.000 claims description 3
• 230000002349 favourable effect Effects 0.000 claims description 2
• 230000012846 protein folding Effects 0.000 abstract description 4
• 125000002887 hydroxy group Chemical group [H]O* 0.000 description 164
• 125000000217 alkyl group Chemical group 0.000 description 156
• 125000003545 alkoxy group Chemical group 0.000 description 135
• 125000005843 halogen group Chemical group 0.000 description 129
• 125000000753 cycloalkyl group Chemical group 0.000 description 105
• 125000003118 aryl group Chemical group 0.000 description 96
• 125000000623 heterocyclic group Chemical group 0.000 description 80
• 125000003342 alkenyl group Chemical group 0.000 description 73
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 72
• 125000000392 cycloalkenyl group Chemical group 0.000 description 69
• 125000002252 acyl group Chemical group 0.000 description 65
• 125000001072 heteroaryl group Chemical group 0.000 description 63
• 125000005309 thioalkoxy group Chemical group 0.000 description 62
• 229960000367 inositol Drugs 0.000 description 60
• 125000003396 thiol group Chemical class [H]S* 0.000 description 60
• 125000004432 carbon atom Chemical group C* 0.000 description 59
• 125000000304 alkynyl group Chemical group 0.000 description 57
• 125000004001 thioalkyl group Chemical group 0.000 description 56
• 150000001733 carboxylic acid esters Chemical class 0.000 description 55
• 125000000000 cycloalkoxy group Chemical group 0.000 description 52
• 125000004423 acyloxy group Chemical group 0.000 description 49
• 239000001257 hydrogen Substances 0.000 description 49
• 229910052739 hydrogen Inorganic materials 0.000 description 49
• 125000004104 aryloxy group Chemical group 0.000 description 46
• 208000024827 Alzheimer disease Diseases 0.000 description 45
• 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 44
• 125000005000 thioaryl group Chemical group 0.000 description 44
• 125000002102 aryl alkyloxo group Chemical group 0.000 description 43
• 150000002431 hydrogen Chemical class 0.000 description 43
• 125000004450 alkenylene group Chemical group 0.000 description 42
• 125000002947 alkylene group Chemical group 0.000 description 40
• 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 description 40
• 125000003435 aroyl group Chemical group 0.000 description 39
• 150000003839 salts Chemical class 0.000 description 39
• 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 38
• 230000009467 reduction Effects 0.000 description 38
• 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 description 38
• 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 37
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 37
• 125000004646 sulfenyl group Chemical group S(*)* 0.000 description 36
• QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 35
• 229940079593 drug Drugs 0.000 description 34
• CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 description 34
• 150000003462 sulfoxides Chemical class 0.000 description 34
• 125000003302 alkenyloxy group Chemical group 0.000 description 33
• 150000003857 carboxamides Chemical class 0.000 description 33
• 125000001181 organosilyl group Chemical group [SiH3]* 0.000 description 33
• 150000003254 radicals Chemical class 0.000 description 33
• 206010002022 amyloidosis Diseases 0.000 description 32
• 125000001309 chloro group Chemical group Cl* 0.000 description 31
• 125000001153 fluoro group Chemical group F* 0.000 description 31
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 30
• 125000004093 cyano group Chemical group *C#N 0.000 description 30
• BWOVZCWSJFYBRM-UHFFFAOYSA-N carbononitridic isocyanate Chemical compound O=C=NC#N BWOVZCWSJFYBRM-UHFFFAOYSA-N 0.000 description 29
• 230000002459 sustained effect Effects 0.000 description 29
• 125000003601 C2-C6 alkynyl group Chemical group 0.000 description 27
• 239000013078 crystal Substances 0.000 description 27
• 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 27
• BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 26
• 239000000460 chlorine Substances 0.000 description 25
• 229910052801 chlorine Inorganic materials 0.000 description 25
• 239000000126 substance Substances 0.000 description 25
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 25
• 125000001424 substituent group Chemical group 0.000 description 24
• 150000001720 carbohydrates Chemical class 0.000 description 22
• 235000014633 carbohydrates Nutrition 0.000 description 22
• 239000012729 immediate-release (IR) formulation Substances 0.000 description 22
• 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 21
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 21
• 239000004480 active ingredient Substances 0.000 description 20
• 239000002245 particle Substances 0.000 description 20
• 238000000151 deposition Methods 0.000 description 19
• COLOHWPRNRVWPI-UHFFFAOYSA-N 1,1,1-trifluoroethane Chemical compound [CH2]C(F)(F)F COLOHWPRNRVWPI-UHFFFAOYSA-N 0.000 description 18
• XXJGBENTLXFVFI-UHFFFAOYSA-N 1-amino-methylene Chemical compound N[CH2] XXJGBENTLXFVFI-UHFFFAOYSA-N 0.000 description 18
• 125000003320 C2-C6 alkenyloxy group Chemical group 0.000 description 18
• 239000011159 matrix material Substances 0.000 description 18
• 235000018102 proteins Nutrition 0.000 description 18
• 125000000547 substituted alkyl group Chemical group 0.000 description 18
• 206010012289 Dementia Diseases 0.000 description 17
• 239000002253 acid Substances 0.000 description 17
• 230000000694 effects Effects 0.000 description 17
• 239000003826 tablet Substances 0.000 description 17
• QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 16
• 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 16
• 230000035508 accumulation Effects 0.000 description 16
• 125000003282 alkyl amino group Chemical group 0.000 description 16
• 229910052740 iodine Inorganic materials 0.000 description 16
• 125000004438 haloalkoxy group Chemical group 0.000 description 15
• CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 description 15
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 15
• 239000012453 solvate Substances 0.000 description 15
• 229910052794 bromium Inorganic materials 0.000 description 14
• 125000001246 bromo group Chemical group Br* 0.000 description 14
• 238000005259 measurement Methods 0.000 description 14
• 101100516568 Caenorhabditis elegans nhr-7 gene Proteins 0.000 description 13
• 241000124008 Mammalia Species 0.000 description 13
• 230000008021 deposition Effects 0.000 description 13
• 239000002904 solvent Substances 0.000 description 13
• 241001465754 Metazoa Species 0.000 description 12
• 241000699670 Mus sp. Species 0.000 description 12
• 150000001413 amino acids Chemical group 0.000 description 12
• 230000015572 biosynthetic process Effects 0.000 description 12
• 239000002775 capsule Substances 0.000 description 12
• 125000001188 haloalkyl group Chemical group 0.000 description 12
• 125000004433 nitrogen atom Chemical group N* 0.000 description 12
• 208000037259 Amyloid Plaque Diseases 0.000 description 11
• 235000001014 amino acid Nutrition 0.000 description 11
• 229940024606 amino acid Drugs 0.000 description 11
• 125000000113 cyclohexyl group Chemical class [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 11
• 238000005755 formation reaction Methods 0.000 description 11
• 125000002768 hydroxyalkyl group Chemical group 0.000 description 11
• 229920000642 polymer Polymers 0.000 description 11
• 239000000651 prodrug Substances 0.000 description 11
• 229940002612 prodrug Drugs 0.000 description 11
• 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 description 10
• ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 10
• 239000008186 active pharmaceutical agent Substances 0.000 description 10
• 230000003993 interaction Effects 0.000 description 10
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 10
• 230000002490 cerebral effect Effects 0.000 description 9
• KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 9
• 238000000576 coating method Methods 0.000 description 9
• 238000000338 in vitro Methods 0.000 description 9
• 150000002772 monosaccharides Chemical class 0.000 description 9
• 230000008569 process Effects 0.000 description 9
• 229920006395 saturated elastomer Polymers 0.000 description 9
• 239000000243 solution Substances 0.000 description 9
• 235000000346 sugar Nutrition 0.000 description 9
• FIARMZDBEGVMLV-UHFFFAOYSA-N 1,1,2,2,2-pentafluoroethanolate Chemical group [O-]C(F)(F)C(F)(F)F FIARMZDBEGVMLV-UHFFFAOYSA-N 0.000 description 8
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 8
• 102000036770 Islet Amyloid Polypeptide Human genes 0.000 description 8
• 108010041872 Islet Amyloid Polypeptide Proteins 0.000 description 8
• 229910018830 PO3H Inorganic materials 0.000 description 8
• 230000009102 absorption Effects 0.000 description 8
• 125000003710 aryl alkyl group Chemical group 0.000 description 8
• 150000005840 aryl radicals Chemical class 0.000 description 8
• 125000004429 atom Chemical group 0.000 description 8
• 239000002585 base Substances 0.000 description 8
• 229910052799 carbon Inorganic materials 0.000 description 8
• 239000011248 coating agent Substances 0.000 description 8
• 239000007884 disintegrant Substances 0.000 description 8
• 125000004785 fluoromethoxy group Chemical group [H]C([H])(F)O* 0.000 description 8
• 125000000524 functional group Chemical group 0.000 description 8
• 229910052736 halogen Inorganic materials 0.000 description 8
• 150000002367 halogens Chemical class 0.000 description 8
• 102000004196 processed proteins & peptides Human genes 0.000 description 8
• CDAISMWEOUEBRE-CDRYSYESSA-N scyllo-inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O CDAISMWEOUEBRE-CDRYSYESSA-N 0.000 description 8
• 125000005415 substituted alkoxy group Chemical group 0.000 description 8
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 8
• 102000009091 Amyloidogenic Proteins Human genes 0.000 description 7
• 108010048112 Amyloidogenic Proteins Proteins 0.000 description 7
• WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 7
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 7
• WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 7
• 229920000168 Microcrystalline cellulose Polymers 0.000 description 7
• 208000001089 Multiple system atrophy Diseases 0.000 description 7
• 206010035226 Plasma cell myeloma Diseases 0.000 description 7
• WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 7
• GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 7
• ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 description 7
• 229910052731 fluorine Inorganic materials 0.000 description 7
• 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 7
• 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 7
• 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 7
• 235000019813 microcrystalline cellulose Nutrition 0.000 description 7
• 230000004048 modification Effects 0.000 description 7
• 238000012986 modification Methods 0.000 description 7
• 125000002911 monocyclic heterocycle group Chemical group 0.000 description 7
• 229910052757 nitrogen Inorganic materials 0.000 description 7
• 239000006187 pill Substances 0.000 description 7
• 229920001223 polyethylene glycol Polymers 0.000 description 7
• 229910052717 sulfur Inorganic materials 0.000 description 7
• 125000004434 sulfur atom Chemical group 0.000 description 7
• 238000012360 testing method Methods 0.000 description 7
• 208000001072 type 2 diabetes mellitus Diseases 0.000 description 7
• 125000004191 (C1-C6) alkoxy group Chemical group 0.000 description 6
• 206010059245 Angiopathy Diseases 0.000 description 6
• 125000000041 C6-C10 aryl group Chemical group 0.000 description 6
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 6
• 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 description 6
• 239000002202 Polyethylene glycol Substances 0.000 description 6
• 208000024777 Prion disease Diseases 0.000 description 6
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 6
• 102100029290 Transthyretin Human genes 0.000 description 6
• 230000008901 benefit Effects 0.000 description 6
• MSWZFWKMSRAUBD-UHFFFAOYSA-N beta-D-galactosamine Natural products NC1C(O)OC(CO)C(O)C1O MSWZFWKMSRAUBD-UHFFFAOYSA-N 0.000 description 6
• 229920002678 cellulose Polymers 0.000 description 6
• 208000010877 cognitive disease Diseases 0.000 description 6
• CDAISMWEOUEBRE-NIPYSYMMSA-N epi-inositol Chemical group O[C@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](O)[C@H]1O CDAISMWEOUEBRE-NIPYSYMMSA-N 0.000 description 6
• 150000002148 esters Chemical class 0.000 description 6
• 239000008103 glucose Substances 0.000 description 6
• 230000004054 inflammatory process Effects 0.000 description 6
• 239000008108 microcrystalline cellulose Substances 0.000 description 6
• 229940016286 microcrystalline cellulose Drugs 0.000 description 6
• 210000000056 organ Anatomy 0.000 description 6
• 125000004430 oxygen atom Chemical group O* 0.000 description 6
• 239000007787 solid Substances 0.000 description 6
• 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 5
• 102000013455 Amyloid beta-Peptides Human genes 0.000 description 5
• 108010090849 Amyloid beta-Peptides Proteins 0.000 description 5
• 241000282472 Canis lupus familiaris Species 0.000 description 5
• 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 description 5
• 201000010374 Down Syndrome Diseases 0.000 description 5
• PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 5
• 108010071690 Prealbumin Proteins 0.000 description 5
• 102000029797 Prion Human genes 0.000 description 5
• 108091000054 Prion Proteins 0.000 description 5
• 229910006069 SO3H Inorganic materials 0.000 description 5
• 229920002472 Starch Polymers 0.000 description 5
• CTQJAETYIVEEFX-UHFFFAOYSA-N [N-]=[N+]=NN(N)N=[N+]=[N-] Chemical compound [N-]=[N+]=NN(N)N=[N+]=[N-] CTQJAETYIVEEFX-UHFFFAOYSA-N 0.000 description 5
• 230000002159 abnormal effect Effects 0.000 description 5
• 150000001408 amides Chemical class 0.000 description 5
• 239000011230 binding agent Substances 0.000 description 5
• 230000004071 biological effect Effects 0.000 description 5
• 210000004369 blood Anatomy 0.000 description 5
• 239000008280 blood Substances 0.000 description 5
• 125000004181 carboxyalkyl group Chemical group 0.000 description 5
• 238000006243 chemical reaction Methods 0.000 description 5
• 239000003153 chemical reaction reagent Substances 0.000 description 5
• 239000003795 chemical substances by application Substances 0.000 description 5
• 208000037976 chronic inflammation Diseases 0.000 description 5
• 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 5
• 230000018109 developmental process Effects 0.000 description 5
• 238000009792 diffusion process Methods 0.000 description 5
• 230000008030 elimination Effects 0.000 description 5
• 238000003379 elimination reaction Methods 0.000 description 5
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 5
• 239000011737 fluorine Substances 0.000 description 5
• 230000006870 function Effects 0.000 description 5
• 230000001771 impaired effect Effects 0.000 description 5
• 125000000468 ketone group Chemical group 0.000 description 5
• 239000000314 lubricant Substances 0.000 description 5
• 238000004519 manufacturing process Methods 0.000 description 5
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 5
• 239000002243 precursor Substances 0.000 description 5
• 230000003381 solubilizing effect Effects 0.000 description 5
• 235000019698 starch Nutrition 0.000 description 5
• 229940032147 starch Drugs 0.000 description 5
• 239000008107 starch Substances 0.000 description 5
• 239000005720 sucrose Substances 0.000 description 5
• 150000008163 sugars Chemical class 0.000 description 5
• 230000003977 synaptic function Effects 0.000 description 5
• 125000000335 thiazolyl group Chemical group 0.000 description 5
• 230000001988 toxicity Effects 0.000 description 5
• 231100000419 toxicity Toxicity 0.000 description 5
• 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 5
• 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 description 4
• GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 4
• 208000003808 Amyloid Neuropathies Diseases 0.000 description 4
• 208000020406 Creutzfeldt Jacob disease Diseases 0.000 description 4
• 150000008574 D-amino acids Chemical class 0.000 description 4
• VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 4
• DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 4
• SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 description 4
• 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 4
• XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 4
• 229930194542 Keto Natural products 0.000 description 4
• GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 4
• 102100025818 Major prion protein Human genes 0.000 description 4
• AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 4
• OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical class OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 4
• HSHXDCVZWHOWCS-UHFFFAOYSA-N N'-hexadecylthiophene-2-carbohydrazide Chemical compound CCCCCCCCCCCCCCCCNNC(=O)c1cccs1 HSHXDCVZWHOWCS-UHFFFAOYSA-N 0.000 description 4
• 208000018737 Parkinson disease Diseases 0.000 description 4
• 241001494479 Pecora Species 0.000 description 4
• OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 4
• 206010037660 Pyrexia Diseases 0.000 description 4
• CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 4
• 229930006000 Sucrose Natural products 0.000 description 4
• 102000004874 Synaptophysin Human genes 0.000 description 4
• 108090001076 Synaptophysin Proteins 0.000 description 4
• 229960000583 acetic acid Drugs 0.000 description 4
• 235000011054 acetic acid Nutrition 0.000 description 4
• DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 4
• 230000009471 action Effects 0.000 description 4
• 125000004442 acylamino group Chemical group 0.000 description 4
• DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 description 4
• 125000001769 aryl amino group Chemical group 0.000 description 4
• JXLHNMVSKXFWAO-UHFFFAOYSA-N azane;7-fluoro-2,1,3-benzoxadiazole-4-sulfonic acid Chemical compound N.OS(=O)(=O)C1=CC=C(F)C2=NON=C12 JXLHNMVSKXFWAO-UHFFFAOYSA-N 0.000 description 4
• 239000004305 biphenyl Substances 0.000 description 4
• 235000010290 biphenyl Nutrition 0.000 description 4
• OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 4
• 235000010980 cellulose Nutrition 0.000 description 4
• 230000001684 chronic effect Effects 0.000 description 4
• 230000007423 decrease Effects 0.000 description 4
• 230000003247 decreasing effect Effects 0.000 description 4
• 238000011161 development Methods 0.000 description 4
• 150000002016 disaccharides Chemical class 0.000 description 4
• 238000007922 dissolution test Methods 0.000 description 4
• 238000009510 drug design Methods 0.000 description 4
• 238000005516 engineering process Methods 0.000 description 4
• 238000011156 evaluation Methods 0.000 description 4
• 230000037406 food intake Effects 0.000 description 4
• 239000012458 free base Substances 0.000 description 4
• 230000002518 glial effect Effects 0.000 description 4
• 125000005456 glyceride group Chemical group 0.000 description 4
• 125000004994 halo alkoxy alkyl group Chemical group 0.000 description 4
• 125000005842 heteroatom Chemical group 0.000 description 4
• 150000002402 hexoses Chemical class 0.000 description 4
• 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 4
• 239000001863 hydroxypropyl cellulose Substances 0.000 description 4
• 230000002401 inhibitory effect Effects 0.000 description 4
• 239000008101 lactose Substances 0.000 description 4
• 230000003902 lesion Effects 0.000 description 4
• 239000000463 material Substances 0.000 description 4
• 230000003278 mimic effect Effects 0.000 description 4
• 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 4
• 230000004770 neurodegeneration Effects 0.000 description 4
• 238000003786 synthesis reaction Methods 0.000 description 4
• 230000009885 systemic effect Effects 0.000 description 4
• VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 4
• 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 4
• 239000003981 vehicle Substances 0.000 description 4
• 229920002554 vinyl polymer Polymers 0.000 description 4
• 125000006273 (C1-C3) alkyl group Chemical group 0.000 description 3
• CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 3
• 206010003591 Ataxia Diseases 0.000 description 3
• 102000014461 Ataxins Human genes 0.000 description 3
• 108010078286 Ataxins Proteins 0.000 description 3
• 229910014585 C2-Ce Inorganic materials 0.000 description 3
• 206010008025 Cerebellar ataxia Diseases 0.000 description 3
• 208000005145 Cerebral amyloid angiopathy Diseases 0.000 description 3
• 208000028698 Cognitive impairment Diseases 0.000 description 3
• XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
• ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 3
• 239000001856 Ethyl cellulose Substances 0.000 description 3
• 102000003886 Glycoproteins Human genes 0.000 description 3
• 108090000288 Glycoproteins Proteins 0.000 description 3
• 229920002683 Glycosaminoglycan Polymers 0.000 description 3
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
• 206010061218 Inflammation Diseases 0.000 description 3
• 150000008575 L-amino acids Chemical class 0.000 description 3
• 101710138751 Major prion protein Proteins 0.000 description 3
• 208000034578 Multiple myelomas Diseases 0.000 description 3
• 239000004372 Polyvinyl alcohol Substances 0.000 description 3
• 241000700159 Rattus Species 0.000 description 3
• 229910018165 SeH Inorganic materials 0.000 description 3
• MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 description 3
• 208000009415 Spinocerebellar Ataxias Diseases 0.000 description 3
• NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 3
• 150000007513 acids Chemical class 0.000 description 3
• 125000005236 alkanoylamino group Chemical group 0.000 description 3
• 125000004183 alkoxy alkyl group Chemical group 0.000 description 3
• 125000004453 alkoxycarbonyl group Chemical group 0.000 description 3
• 125000005055 alkyl alkoxy group Chemical group 0.000 description 3
• 125000004390 alkyl sulfonyl group Chemical group 0.000 description 3
• 125000004414 alkyl thio group Chemical group 0.000 description 3
• 125000000266 alpha-aminoacyl group Chemical group 0.000 description 3
• 125000002178 anthracenyl group Chemical group C1(=CC=CC2=CC3=CC=CC=C3C=C12)* 0.000 description 3
• PYMYPHUHKUWMLA-UHFFFAOYSA-N arabinose Natural products OCC(O)C(O)C(O)C=O PYMYPHUHKUWMLA-UHFFFAOYSA-N 0.000 description 3
• 125000001204 arachidyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 3
• 125000001691 aryl alkyl amino group Chemical group 0.000 description 3
• QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 3
• 201000004562 autosomal dominant cerebellar ataxia Diseases 0.000 description 3
• WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 3
• 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 3
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 3
• SRBFZHDQGSBBOR-UHFFFAOYSA-N beta-D-Pyranose-Lyxose Natural products OC1COC(O)C(O)C1O SRBFZHDQGSBBOR-UHFFFAOYSA-N 0.000 description 3
• 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 3
• 239000011575 calcium Substances 0.000 description 3
• 210000004027 cell Anatomy 0.000 description 3
• 239000001913 cellulose Substances 0.000 description 3
• 230000008859 change Effects 0.000 description 3
• 230000006020 chronic inflammation Effects 0.000 description 3
• 235000015165 citric acid Nutrition 0.000 description 3
• 230000001149 cognitive effect Effects 0.000 description 3
• 238000013270 controlled release Methods 0.000 description 3
• 238000007796 conventional method Methods 0.000 description 3
• 238000002425 crystallisation Methods 0.000 description 3
• 230000008025 crystallization Effects 0.000 description 3
• 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 3
• FGFCSHCXBYAKOL-UHFFFAOYSA-N cyclohexane-1,1,2,2,3,3-hexol Chemical compound OC1(O)CCCC(O)(O)C1(O)O FGFCSHCXBYAKOL-UHFFFAOYSA-N 0.000 description 3
• 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 description 3
• 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 description 3
• 238000013461 design Methods 0.000 description 3
• 125000004663 dialkyl amino group Chemical group 0.000 description 3
• 235000019325 ethyl cellulose Nutrition 0.000 description 3
• 229920001249 ethyl cellulose Polymers 0.000 description 3
• 238000001704 evaporation Methods 0.000 description 3
• 150000004676 glycans Chemical class 0.000 description 3
• 238000001631 haemodialysis Methods 0.000 description 3
• 230000000322 hemodialysis Effects 0.000 description 3
• 229960003943 hypromellose Drugs 0.000 description 3
• 125000002883 imidazolyl group Chemical group 0.000 description 3
• 238000001727 in vivo Methods 0.000 description 3
• 210000003000 inclusion body Anatomy 0.000 description 3
• 230000005764 inhibitory process Effects 0.000 description 3
• 125000000654 isopropylidene group Chemical group C(C)(C)=* 0.000 description 3
• 210000004558 lewy body Anatomy 0.000 description 3
• 150000002632 lipids Chemical class 0.000 description 3
• 210000002540 macrophage Anatomy 0.000 description 3
• 238000012423 maintenance Methods 0.000 description 3
• 125000002960 margaryl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 3
• 239000002609 medium Substances 0.000 description 3
• 230000008018 melting Effects 0.000 description 3
• 238000002844 melting Methods 0.000 description 3
• 229920000609 methyl cellulose Polymers 0.000 description 3
• CPRRHERYRRXBRZ-SRVKXCTJSA-N methyl n-[(2s)-1-[[(2s)-1-hydroxy-3-[(3s)-2-oxopyrrolidin-3-yl]propan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamate Chemical compound COC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CO)C[C@@H]1CCNC1=O CPRRHERYRRXBRZ-SRVKXCTJSA-N 0.000 description 3
• 235000010981 methylcellulose Nutrition 0.000 description 3
• 239000001923 methylcellulose Substances 0.000 description 3
• 230000000813 microbial effect Effects 0.000 description 3
• 230000004001 molecular interaction Effects 0.000 description 3
• 125000002757 morpholinyl group Chemical group 0.000 description 3
• 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 description 3
• 125000001624 naphthyl group Chemical group 0.000 description 3
• 208000015122 neurodegenerative disease Diseases 0.000 description 3
• 210000002682 neurofibrillary tangle Anatomy 0.000 description 3
• 229920001542 oligosaccharide Polymers 0.000 description 3
• 150000002482 oligosaccharides Chemical class 0.000 description 3
• 150000007524 organic acids Chemical class 0.000 description 3
• 125000004043 oxo group Chemical group O=* 0.000 description 3
• 229910052760 oxygen Inorganic materials 0.000 description 3
• 239000001301 oxygen Substances 0.000 description 3
• 125000002958 pentadecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 3
• 125000001792 phenanthrenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3C=CC12)* 0.000 description 3
• 229940023488 pill Drugs 0.000 description 3
• 125000003386 piperidinyl group Chemical group 0.000 description 3
• 229920001282 polysaccharide Polymers 0.000 description 3
• 239000005017 polysaccharide Substances 0.000 description 3
• 229920002451 polyvinyl alcohol Polymers 0.000 description 3
• 239000000843 powder Substances 0.000 description 3
• 208000022256 primary systemic amyloidosis Diseases 0.000 description 3
• 125000004368 propenyl group Chemical group C(=CC)* 0.000 description 3
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 3
• 125000004076 pyridyl group Chemical group 0.000 description 3
• 230000002829 reductive effect Effects 0.000 description 3
• 238000011160 research Methods 0.000 description 3
• 208000008864 scrapie Diseases 0.000 description 3
• 239000011780 sodium chloride Substances 0.000 description 3
• 239000007909 solid dosage form Substances 0.000 description 3
• 238000006467 substitution reaction Methods 0.000 description 3
• 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 description 3
• 239000011593 sulfur Substances 0.000 description 3
• 239000000725 suspension Substances 0.000 description 3
• 208000011580 syndromic disease Diseases 0.000 description 3
• 210000001519 tissue Anatomy 0.000 description 3
• 230000032258 transport Effects 0.000 description 3
• MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 description 2
• JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical class OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 2
• 125000001831 (C6-C10) heteroaryl group Chemical group 0.000 description 2
• BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 2
• YJTKZCDBKVTVBY-UHFFFAOYSA-N 1,3-Diphenylbenzene Chemical group C1=CC=CC=C1C1=CC=CC(C=2C=CC=CC=2)=C1 YJTKZCDBKVTVBY-UHFFFAOYSA-N 0.000 description 2
• FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 description 2
• VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
• OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 2
• HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 2
• MSWZFWKMSRAUBD-GASJEMHNSA-N 2-amino-2-deoxy-D-galactopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@H](O)[C@@H]1O MSWZFWKMSRAUBD-GASJEMHNSA-N 0.000 description 2
• MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 description 2
• NBDAHKQJXVLAID-UHFFFAOYSA-N 5-nitroisophthalic acid Chemical compound OC(=O)C1=CC(C(O)=O)=CC([N+]([O-])=O)=C1 NBDAHKQJXVLAID-UHFFFAOYSA-N 0.000 description 2
• 208000023769 AA amyloidosis Diseases 0.000 description 2
• QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 2
• 102000001049 Amyloid Human genes 0.000 description 2
• 108010094108 Amyloid Proteins 0.000 description 2
• DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 description 2
• KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 description 2
• FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 2
• OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 2
• 239000004215 Carbon black (E152) Substances 0.000 description 2
• CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
• 201000009030 Carcinoma Diseases 0.000 description 2
• 206010007509 Cardiac amyloidosis Diseases 0.000 description 2
• 206010008111 Cerebral haemorrhage Diseases 0.000 description 2
• 229920002785 Croscarmellose sodium Polymers 0.000 description 2
• 239000004971 Cross linker Substances 0.000 description 2
• FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
• WQZGKKKJIJFFOK-QTVWNMPRSA-N D-mannopyranose Chemical compound OC[C@H]1OC(O)[C@@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-QTVWNMPRSA-N 0.000 description 2
• HMFHBZSHGGEWLO-SOOFDHNKSA-N D-ribofuranose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H]1O HMFHBZSHGGEWLO-SOOFDHNKSA-N 0.000 description 2
• SRBFZHDQGSBBOR-IOVATXLUSA-N D-xylopyranose Chemical compound O[C@@H]1COC(O)[C@H](O)[C@H]1O SRBFZHDQGSBBOR-IOVATXLUSA-N 0.000 description 2
• 201000008163 Dentatorubral pallidoluysian atrophy Diseases 0.000 description 2
• FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
• SNRUBQQJIBEYMU-UHFFFAOYSA-N Dodecane Natural products CCCCCCCCCCCC SNRUBQQJIBEYMU-UHFFFAOYSA-N 0.000 description 2
• 208000001976 Endocrine Gland Neoplasms Diseases 0.000 description 2
• 241000588724 Escherichia coli Species 0.000 description 2
• 208000034846 Familial Amyloid Neuropathies Diseases 0.000 description 2
• ZHNUHDYFZUAESO-UHFFFAOYSA-N Formamide Chemical compound NC=O ZHNUHDYFZUAESO-UHFFFAOYSA-N 0.000 description 2
• 201000011240 Frontotemporal dementia Diseases 0.000 description 2
• 229930091371 Fructose Natural products 0.000 description 2
• 239000005715 Fructose Substances 0.000 description 2
• RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 2
• 208000003736 Gerstmann-Straussler-Scheinker Disease Diseases 0.000 description 2
• PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
• 239000004471 Glycine Substances 0.000 description 2
• AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 2
• 206010019889 Hereditary neuropathic amyloidosis Diseases 0.000 description 2
• CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical class Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 2
• 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 2
• ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 description 2
• QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 2
• DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 description 2
• FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 description 2
• AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 description 2
• GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 description 2
• 229930195725 Mannitol Natural products 0.000 description 2
• 108010006519 Molecular Chaperones Proteins 0.000 description 2
• 208000026072 Motor neurone disease Diseases 0.000 description 2
• PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 2
• 102000012404 Orosomucoid Human genes 0.000 description 2
• 108010061952 Orosomucoid Proteins 0.000 description 2
• 229910018828 PO3H2 Inorganic materials 0.000 description 2
• 206010033892 Paraplegia Diseases 0.000 description 2
• GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 2
• 229920003171 Poly (ethylene oxide) Polymers 0.000 description 2
• ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 2
• 108010048233 Procalcitonin Proteins 0.000 description 2
• ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 description 2
• PYMYPHUHKUWMLA-LMVFSUKVSA-N Ribose Natural products OC[C@@H](O)[C@@H](O)[C@@H](O)C=O PYMYPHUHKUWMLA-LMVFSUKVSA-N 0.000 description 2
• 206010039811 Secondary amyloidosis Diseases 0.000 description 2
• 102000054727 Serum Amyloid A Human genes 0.000 description 2
• 108700028909 Serum Amyloid A Proteins 0.000 description 2
• XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical group [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 description 2
• 208000001077 Spastic ataxia Diseases 0.000 description 2
• 208000032930 Spastic paraplegia Diseases 0.000 description 2
• PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 2
• 102000019355 Synuclein Human genes 0.000 description 2
• 108050006783 Synuclein Proteins 0.000 description 2
• 208000032859 Synucleinopathies Diseases 0.000 description 2
• FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 2
• DGDCHPCRMWEOJR-FQPOAREZSA-N Thr-Ala-Tyr Chemical group C[C@@H](O)[C@H](N)C(=O)N[C@@H](C)C(=O)N[C@H](C(O)=O)CC1=CC=C(O)C=C1 DGDCHPCRMWEOJR-FQPOAREZSA-N 0.000 description 2
• AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 description 2
• 239000004473 Threonine Substances 0.000 description 2
• NOXKHHXSHQFSGJ-FQPOAREZSA-N Tyr-Ala-Thr Chemical group C[C@@H](O)[C@@H](C(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC1=CC=C(O)C=C1 NOXKHHXSHQFSGJ-FQPOAREZSA-N 0.000 description 2
• XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 2
• 208000018756 Variant Creutzfeldt-Jakob disease Diseases 0.000 description 2
• 241000700605 Viruses Species 0.000 description 2
• 230000002378 acidificating effect Effects 0.000 description 2
• WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 description 2
• 235000004279 alanine Nutrition 0.000 description 2
• 150000001299 aldehydes Chemical class 0.000 description 2
• 229910052783 alkali metal Inorganic materials 0.000 description 2
• 125000000033 alkoxyamino group Chemical group 0.000 description 2
• 125000002877 alkyl aryl group Chemical group 0.000 description 2
• 125000004644 alkyl sulfinyl group Chemical group 0.000 description 2
• 208000026935 allergic disease Diseases 0.000 description 2
• HMFHBZSHGGEWLO-UHFFFAOYSA-N alpha-D-Furanose-Ribose Natural products OCC1OC(O)C(O)C1O HMFHBZSHGGEWLO-UHFFFAOYSA-N 0.000 description 2
• WQZGKKKJIJFFOK-PHYPRBDBSA-N alpha-D-galactose Chemical compound OC[C@H]1O[C@H](O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-PHYPRBDBSA-N 0.000 description 2
• BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 2
• 150000001412 amines Chemical class 0.000 description 2
• 150000003862 amino acid derivatives Chemical class 0.000 description 2
• 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 2
• 238000013459 approach Methods 0.000 description 2
• 239000003125 aqueous solvent Substances 0.000 description 2
• PYMYPHUHKUWMLA-WDCZJNDASA-N arabinose Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)C=O PYMYPHUHKUWMLA-WDCZJNDASA-N 0.000 description 2
• 125000004097 arachidonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])/C([H])=C([H])\C([H])([H])/C([H])=C([H])\C([H])([H])/C([H])=C([H])\C([H])([H])/C([H])=C([H])\C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
• 125000004391 aryl sulfonyl group Chemical group 0.000 description 2
• 230000001174 ascending effect Effects 0.000 description 2
• 235000009582 asparagine Nutrition 0.000 description 2
• 229960001230 asparagine Drugs 0.000 description 2
• 210000003719 b-lymphocyte Anatomy 0.000 description 2
• 125000002511 behenyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
• QMKYBPDZANOJGF-UHFFFAOYSA-N benzene-1,3,5-tricarboxylic acid Chemical compound OC(=O)C1=CC(C(O)=O)=CC(C(O)=O)=C1 QMKYBPDZANOJGF-UHFFFAOYSA-N 0.000 description 2
• 229940049706 benzodiazepine Drugs 0.000 description 2
• 125000003310 benzodiazepinyl group Chemical group N1N=C(C=CC2=C1C=CC=C2)* 0.000 description 2
• GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 2
• 230000027455 binding Effects 0.000 description 2
• 230000033228 biological regulation Effects 0.000 description 2
• 230000037396 body weight Effects 0.000 description 2
• 210000005013 brain tissue Anatomy 0.000 description 2
• 125000004744 butyloxycarbonyl group Chemical group 0.000 description 2
• 229910052791 calcium Inorganic materials 0.000 description 2
• 235000011132 calcium sulphate Nutrition 0.000 description 2
• 150000001723 carbon free-radicals Chemical class 0.000 description 2
• 239000001768 carboxy methyl cellulose Substances 0.000 description 2
• 210000003010 carpal bone Anatomy 0.000 description 2
• 239000000969 carrier Substances 0.000 description 2
• 150000001768 cations Chemical class 0.000 description 2
• 210000005056 cell body Anatomy 0.000 description 2
• 229920003086 cellulose ether Polymers 0.000 description 2
• 210000003169 central nervous system Anatomy 0.000 description 2
• 238000011260 co-administration Methods 0.000 description 2
• 230000003930 cognitive ability Effects 0.000 description 2
• 230000006999 cognitive decline Effects 0.000 description 2
• 229920001577 copolymer Polymers 0.000 description 2
• 230000000875 corresponding effect Effects 0.000 description 2
• 230000001054 cortical effect Effects 0.000 description 2
• 229960001681 croscarmellose sodium Drugs 0.000 description 2
• 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 2
• 230000001186 cumulative effect Effects 0.000 description 2
• 125000004122 cyclic group Chemical group 0.000 description 2
• 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 2
• 125000003678 cyclohexadienyl group Chemical group C1(=CC=CCC1)* 0.000 description 2
• 125000000058 cyclopentadienyl group Chemical group C1(=CC=CC1)* 0.000 description 2
• XVOYSCVBGLVSOL-UHFFFAOYSA-N cysteic acid Chemical compound OC(=O)C(N)CS(O)(=O)=O XVOYSCVBGLVSOL-UHFFFAOYSA-N 0.000 description 2
• 125000003493 decenyl group Chemical group [H]C([*])=C([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
• 125000002704 decyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 2
• 230000007812 deficiency Effects 0.000 description 2
• 230000002950 deficient Effects 0.000 description 2
• 230000007850 degeneration Effects 0.000 description 2
• 238000001514 detection method Methods 0.000 description 2
• 238000003745 diagnosis Methods 0.000 description 2
• 235000014113 dietary fatty acids Nutrition 0.000 description 2
• 238000007907 direct compression Methods 0.000 description 2
• 239000006185 dispersion Substances 0.000 description 2
• 125000005066 dodecenyl group Chemical group C(=CCCCCCCCCCC)* 0.000 description 2
• 125000003438 dodecyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 2
• 231100000673 dose–response relationship Toxicity 0.000 description 2
• 238000001647 drug administration Methods 0.000 description 2
• 238000012377 drug delivery Methods 0.000 description 2
• 238000001035 drying Methods 0.000 description 2
• 230000004064 dysfunction Effects 0.000 description 2
• 239000000839 emulsion Substances 0.000 description 2
• ZSWFCLXCOIISFI-UHFFFAOYSA-N endo-cyclopentadiene Natural products C1C=CC=C1 ZSWFCLXCOIISFI-UHFFFAOYSA-N 0.000 description 2
• 201000011523 endocrine gland cancer Diseases 0.000 description 2
• 230000003628 erosive effect Effects 0.000 description 2
• PAGQVVVNLJPSFU-UHFFFAOYSA-N ethane-1,2-diol;sulfo hydrogen sulfate Chemical compound OCCO.OS(=O)(=O)OS(O)(=O)=O PAGQVVVNLJPSFU-UHFFFAOYSA-N 0.000 description 2
• 230000001747 exhibiting effect Effects 0.000 description 2
• 229930195729 fatty acid Natural products 0.000 description 2
• 239000000194 fatty acid Substances 0.000 description 2
• 125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 2
• 239000001530 fumaric acid Substances 0.000 description 2
• 125000002541 furyl group Chemical group 0.000 description 2
• 229930182830 galactose Natural products 0.000 description 2
• 210000001035 gastrointestinal tract Anatomy 0.000 description 2
• 239000000499 gel Substances 0.000 description 2
• 229920000159 gelatin Polymers 0.000 description 2
• 235000019322 gelatine Nutrition 0.000 description 2
• 229960002442 glucosamine Drugs 0.000 description 2
• 150000002334 glycols Chemical class 0.000 description 2
• 150000002337 glycosamines Chemical class 0.000 description 2
• 229940093915 gynecological organic acid Drugs 0.000 description 2
• 210000002216 heart Anatomy 0.000 description 2
• 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
• 125000005553 heteroaryloxy group Chemical group 0.000 description 2
• 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 description 2
• 150000004677 hydrates Chemical class 0.000 description 2
• 229930195733 hydrocarbon Natural products 0.000 description 2
• 150000002430 hydrocarbons Chemical group 0.000 description 2
• 125000004435 hydrogen atom Chemical group [H]* 0.000 description 2
• 230000001965 increasing effect Effects 0.000 description 2
• 208000015181 infectious disease Diseases 0.000 description 2
• 208000027866 inflammatory disease Diseases 0.000 description 2
• 208000019715 inherited Creutzfeldt-Jakob disease Diseases 0.000 description 2
• 238000001990 intravenous administration Methods 0.000 description 2
• 229910052742 iron Inorganic materials 0.000 description 2
• 230000007794 irritation Effects 0.000 description 2
• 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 2
• 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 description 2
• 125000000555 isopropenyl group Chemical group [H]\C([H])=C(\*)C([H])([H])[H] 0.000 description 2
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 2
• 125000000842 isoxazolyl group Chemical group 0.000 description 2
• 125000005647 linker group Chemical group 0.000 description 2
• 239000007788 liquid Substances 0.000 description 2
• 230000005923 long-lasting effect Effects 0.000 description 2
• 230000007774 longterm Effects 0.000 description 2
• 239000007937 lozenge Substances 0.000 description 2
• HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
• 230000014759 maintenance of location Effects 0.000 description 2
• VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 2
• 239000011976 maleic acid Substances 0.000 description 2
• 239000001630 malic acid Substances 0.000 description 2
• 235000011090 malic acid Nutrition 0.000 description 2
• 230000003211 malignant effect Effects 0.000 description 2
• 235000010355 mannitol Nutrition 0.000 description 2
• 239000000594 mannitol Substances 0.000 description 2
• 230000004060 metabolic process Effects 0.000 description 2
• 229940098779 methanesulfonic acid Drugs 0.000 description 2
• BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 description 2
• 229930182817 methionine Natural products 0.000 description 2
• 239000011859 microparticle Substances 0.000 description 2
• 150000007522 mineralic acids Chemical class 0.000 description 2
• 239000000178 monomer Substances 0.000 description 2
• 208000005264 motor neuron disease Diseases 0.000 description 2
• 125000001421 myristyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
• 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 2
• 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 2
• 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
• 125000005064 octadecenyl group Chemical group C(=CCCCCCCCCCCCCCCCC)* 0.000 description 2
• 125000004365 octenyl group Chemical group C(=CCCCCCC)* 0.000 description 2
• 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
• 208000031237 olivopontocerebellar atrophy Diseases 0.000 description 2
• 239000006186 oral dosage form Substances 0.000 description 2
• 235000005985 organic acids Nutrition 0.000 description 2
• 150000007530 organic bases Chemical class 0.000 description 2
• 239000003960 organic solvent Substances 0.000 description 2
• 230000003204 osmotic effect Effects 0.000 description 2
• 125000000913 palmityl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
• 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 2
• 210000001428 peripheral nervous system Anatomy 0.000 description 2
• 229940068196 placebo Drugs 0.000 description 2
• 239000000902 placebo Substances 0.000 description 2
• 229920001451 polypropylene glycol Polymers 0.000 description 2
• 239000011118 polyvinyl acetate Substances 0.000 description 2
• 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
• 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
• 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
• 239000011591 potassium Substances 0.000 description 2
• 229910052700 potassium Inorganic materials 0.000 description 2
• CWCXERYKLSEGEZ-KDKHKZEGSA-N procalcitonin Chemical compound C([C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)NCC(O)=O)[C@@H](C)O)NC(=O)[C@@H](NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@H]1NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](N)CSSC1)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 CWCXERYKLSEGEZ-KDKHKZEGSA-N 0.000 description 2
• 230000000750 progressive effect Effects 0.000 description 2
• 230000002035 prolonged effect Effects 0.000 description 2
• 125000006239 protecting group Chemical group 0.000 description 2
• 230000006916 protein interaction Effects 0.000 description 2
• 230000000541 pulsatile effect Effects 0.000 description 2
• 239000011541 reaction mixture Substances 0.000 description 2
• 230000004044 response Effects 0.000 description 2
• 230000002441 reversible effect Effects 0.000 description 2
• 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 2
• 235000015424 sodium Nutrition 0.000 description 2
• 239000011734 sodium Substances 0.000 description 2
• 229910052708 sodium Inorganic materials 0.000 description 2
• 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 2
• 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 2
• 239000008109 sodium starch glycolate Substances 0.000 description 2
• 229920003109 sodium starch glycolate Polymers 0.000 description 2
• 229940079832 sodium starch glycolate Drugs 0.000 description 2
• 239000007858 starting material Substances 0.000 description 2
• 125000004079 stearyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
• 238000003756 stirring Methods 0.000 description 2
• 125000005017 substituted alkenyl group Chemical group 0.000 description 2
• 125000004426 substituted alkynyl group Chemical group 0.000 description 2
• 125000003107 substituted aryl group Chemical group 0.000 description 2
• 125000005346 substituted cycloalkyl group Chemical group 0.000 description 2
• 239000006188 syrup Substances 0.000 description 2
• 235000020357 syrup Nutrition 0.000 description 2
• 239000011975 tartaric acid Substances 0.000 description 2
• 235000002906 tartaric acid Nutrition 0.000 description 2
• KUCOHFSKRZZVRO-UHFFFAOYSA-N terephthalaldehyde Chemical compound O=CC1=CC=C(C=O)C=C1 KUCOHFSKRZZVRO-UHFFFAOYSA-N 0.000 description 2
• 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 2
• 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 2
• 125000005063 tetradecenyl group Chemical group C(=CCCCCCCCCCCCC)* 0.000 description 2
• 238000002560 therapeutic procedure Methods 0.000 description 2
• 230000009261 transgenic effect Effects 0.000 description 2
• 201000007905 transthyretin amyloidosis Diseases 0.000 description 2
• 239000001993 wax Substances 0.000 description 2
• 238000005550 wet granulation Methods 0.000 description 2
• QBYIENPQHBMVBV-HFEGYEGKSA-N (2R)-2-hydroxy-2-phenylacetic acid Chemical compound O[C@@H](C(O)=O)c1ccccc1.O[C@@H](C(O)=O)c1ccccc1 QBYIENPQHBMVBV-HFEGYEGKSA-N 0.000 description 1
• JSPNNZKWADNWHI-PNANGNLXSA-N (2r)-2-hydroxy-n-[(2s,3r,4e,8e)-3-hydroxy-9-methyl-1-[(2r,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoctadeca-4,8-dien-2-yl]heptadecanamide Chemical compound CCCCCCCCCCCCCCC[C@@H](O)C(=O)N[C@H]([C@H](O)\C=C\CC\C=C(/C)CCCCCCCCC)CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O JSPNNZKWADNWHI-PNANGNLXSA-N 0.000 description 1
• JWGDJWOYQMYZMW-UAFMIMERSA-N (2r,3s,4s,5r)-2,5-bis(phenylmethoxy)hexane-1,3,4,6-tetrol Chemical compound O([C@H](CO)[C@@H](O)[C@H](O)[C@@H](CO)OCC=1C=CC=CC=1)CC1=CC=CC=C1 JWGDJWOYQMYZMW-UAFMIMERSA-N 0.000 description 1
• LZXHHNKULPHARO-UHFFFAOYSA-M (3,4-dichlorophenyl)methyl-triphenylphosphanium;chloride Chemical compound [Cl-].C1=C(Cl)C(Cl)=CC=C1C[P+](C=1C=CC=CC=1)(C=1C=CC=CC=1)C1=CC=CC=C1 LZXHHNKULPHARO-UHFFFAOYSA-M 0.000 description 1
• IMGXDCAOBSTOQJ-CFTXMQDWSA-N (3R,4R,5R,6R)-3-amino-6-(hydroxymethyl)oxane-2,4,5-triol (2R,3R,4R,5R)-2-amino-3,4,5,6-tetrahydroxyhexanal Chemical compound O=C[C@H](N)[C@@H](O)[C@@H](O)[C@H](O)CO.N[C@H]1C(O)O[C@H](CO)[C@H](O)[C@@H]1O IMGXDCAOBSTOQJ-CFTXMQDWSA-N 0.000 description 1
• NVEGGHPETXMRSV-NIJYPJQDSA-N (4r,5r)-4-[(4r,5r)-5-hydroxy-2-phenyl-1,3-dioxan-4-yl]-2-phenyl-1,3-dioxan-5-ol Chemical compound O([C@H]([C@@H](CO1)O)[C@@H]2OC(OC[C@H]2O)C=2C=CC=CC=2)C1C1=CC=CC=C1 NVEGGHPETXMRSV-NIJYPJQDSA-N 0.000 description 1
• 125000006823 (C1-C6) acyl group Chemical group 0.000 description 1
• 239000001124 (E)-prop-1-ene-1,2,3-tricarboxylic acid Substances 0.000 description 1
• NWUYHJFMYQTDRP-UHFFFAOYSA-N 1,2-bis(ethenyl)benzene;1-ethenyl-2-ethylbenzene;styrene Chemical compound C=CC1=CC=CC=C1.CCC1=CC=CC=C1C=C.C=CC1=CC=CC=C1C=C NWUYHJFMYQTDRP-UHFFFAOYSA-N 0.000 description 1
• JPRPJUMQRZTTED-UHFFFAOYSA-N 1,3-dioxolanyl Chemical group [CH]1OCCO1 JPRPJUMQRZTTED-UHFFFAOYSA-N 0.000 description 1
• AZQWKYJCGOJGHM-UHFFFAOYSA-N 1,4-benzoquinone Chemical compound O=C1C=CC(=O)C=C1 AZQWKYJCGOJGHM-UHFFFAOYSA-N 0.000 description 1
• 125000005940 1,4-dioxanyl group Chemical group 0.000 description 1
• HKDFRDIIELOLTJ-UHFFFAOYSA-N 1,4-dithianyl Chemical group [CH]1CSCCS1 HKDFRDIIELOLTJ-UHFFFAOYSA-N 0.000 description 1
• BDWXGJAPYWYGMT-UHFFFAOYSA-N 1,5-disulfooxyheptan-3-yl hydrogen sulfate Chemical compound OS(=O)(=O)OC(CC)CC(OS(O)(=O)=O)CCOS(O)(=O)=O BDWXGJAPYWYGMT-UHFFFAOYSA-N 0.000 description 1
• 125000004972 1-butynyl group Chemical group [H]C([H])([H])C([H])([H])C#C* 0.000 description 1
• KVGOXGQSTGQXDD-UHFFFAOYSA-N 1-decane-sulfonic-acid Chemical compound CCCCCCCCCCS(O)(=O)=O KVGOXGQSTGQXDD-UHFFFAOYSA-N 0.000 description 1
• IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 1
• CDAISMWEOUEBRE-LKPKBOIGSA-N 1D-chiro-inositol Chemical compound O[C@H]1[C@@H](O)[C@H](O)[C@H](O)[C@@H](O)[C@@H]1O CDAISMWEOUEBRE-LKPKBOIGSA-N 0.000 description 1
• YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 description 1
• GZCGUPFRVQAUEE-UHFFFAOYSA-N 2,3,4,5,6-pentahydroxyhexanal Chemical compound OCC(O)C(O)C(O)C(O)C=O GZCGUPFRVQAUEE-UHFFFAOYSA-N 0.000 description 1
• OXBLVCZKDOZZOJ-UHFFFAOYSA-N 2,3-Dihydrothiophene Chemical compound C1CC=CS1 OXBLVCZKDOZZOJ-UHFFFAOYSA-N 0.000 description 1
• OYJGEOAXBALSMM-UHFFFAOYSA-N 2,3-dihydro-1,3-thiazole Chemical compound C1NC=CS1 OYJGEOAXBALSMM-UHFFFAOYSA-N 0.000 description 1
• JKTCBAGSMQIFNL-UHFFFAOYSA-N 2,3-dihydrofuran Chemical compound C1CC=CO1 JKTCBAGSMQIFNL-UHFFFAOYSA-N 0.000 description 1
• JBZPRXASPJMVEL-UHFFFAOYSA-N 2,5-dimethoxybenzene-1,4-disulfonic acid Chemical compound COC1=CC(S(O)(=O)=O)=C(OC)C=C1S(O)(=O)=O JBZPRXASPJMVEL-UHFFFAOYSA-N 0.000 description 1
• XHZPRMZZQOIPDS-UHFFFAOYSA-N 2-Methyl-2-[(1-oxo-2-propenyl)amino]-1-propanesulfonic acid Chemical compound OS(=O)(=O)CC(C)(C)NC(=O)C=C XHZPRMZZQOIPDS-UHFFFAOYSA-N 0.000 description 1
• IQGWPPQNIZBTBM-UHFFFAOYSA-N 2-aminoethanol;sulfuric acid Chemical compound NCCO.OS(O)(=O)=O IQGWPPQNIZBTBM-UHFFFAOYSA-N 0.000 description 1
• 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 description 1
• 125000006325 2-propenyl amino group Chemical group [H]C([H])=C([H])C([H])([H])N([H])* 0.000 description 1
• 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 description 1
• 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 description 1
• 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 description 1
• 125000001698 2H-pyranyl group Chemical group O1C(C=CC=C1)* 0.000 description 1
• AEMOLEFTQBMNLQ-UHFFFAOYSA-N 3,4,5,6-tetrahydroxyoxane-2-carboxylic acid Chemical compound OC1OC(C(O)=O)C(O)C(O)C1O AEMOLEFTQBMNLQ-UHFFFAOYSA-N 0.000 description 1
• DVLFYONBTKHTER-UHFFFAOYSA-N 3-(N-morpholino)propanesulfonic acid Chemical compound OS(=O)(=O)CCCN1CCOCC1 DVLFYONBTKHTER-UHFFFAOYSA-N 0.000 description 1
• SNKZJIOFVMKAOJ-UHFFFAOYSA-N 3-Amino-1-propanesulfonic acid Natural products NCCCS(O)(=O)=O SNKZJIOFVMKAOJ-UHFFFAOYSA-N 0.000 description 1
• 125000003682 3-furyl group Chemical group O1C([H])=C([*])C([H])=C1[H] 0.000 description 1
• QIKMDZAUHYRRQV-UHFFFAOYSA-N 3-hydroxypropane-1-sulfonic acid;sulfuric acid Chemical compound OS(O)(=O)=O.OCCCS(O)(=O)=O QIKMDZAUHYRRQV-UHFFFAOYSA-N 0.000 description 1
• 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 1
• 125000004364 3-pyrrolinyl group Chemical group [H]C1=C([H])C([H])([H])N(*)C1([H])[H] 0.000 description 1
• 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 description 1
• OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 description 1
• RXCMFQDTWCCLBL-UHFFFAOYSA-N 4-amino-3-hydroxynaphthalene-1-sulfonic acid Chemical compound C1=CC=C2C(N)=C(O)C=C(S(O)(=O)=O)C2=C1 RXCMFQDTWCCLBL-UHFFFAOYSA-N 0.000 description 1
• OMSKWMHSUQZBRS-UHFFFAOYSA-N 4-ethenylbenzenesulfonic acid;sodium Chemical compound [Na].OS(=O)(=O)C1=CC=C(C=C)C=C1 OMSKWMHSUQZBRS-UHFFFAOYSA-N 0.000 description 1
• 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 description 1
• 125000001826 4H-pyranyl group Chemical group O1C(=CCC=C1)* 0.000 description 1
• 208000018282 ACys amyloidosis Diseases 0.000 description 1
• 241000251468 Actinopterygii Species 0.000 description 1
• 108010088751 Albumins Proteins 0.000 description 1
• 102000009027 Albumins Human genes 0.000 description 1
• 208000007848 Alcoholism Diseases 0.000 description 1
• 102000002572 Alpha-Globulins Human genes 0.000 description 1
• 108010068307 Alpha-Globulins Proteins 0.000 description 1
• 239000005995 Aluminium silicate Substances 0.000 description 1
• 101710137189 Amyloid-beta A4 protein Proteins 0.000 description 1
• 102100022704 Amyloid-beta precursor protein Human genes 0.000 description 1
• 101710151993 Amyloid-beta precursor protein Proteins 0.000 description 1
• 206010002556 Ankylosing Spondylitis Diseases 0.000 description 1
• 101710081722 Antitrypsin Proteins 0.000 description 1
• 208000019901 Anxiety disease Diseases 0.000 description 1
• 241000132092 Aster Species 0.000 description 1
• 102000007371 Ataxin-3 Human genes 0.000 description 1
• 241000271566 Aves Species 0.000 description 1
• 241000894006 Bacteria Species 0.000 description 1
• 206010004146 Basal cell carcinoma Diseases 0.000 description 1
• 208000027496 Behcet disease Diseases 0.000 description 1
• 208000009137 Behcet syndrome Diseases 0.000 description 1
• 239000005711 Benzoic acid Substances 0.000 description 1
• 102000006734 Beta-Globulins Human genes 0.000 description 1
• 108010087504 Beta-Globulins Proteins 0.000 description 1
• LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 description 1
• 241000588832 Bordetella pertussis Species 0.000 description 1
• 241000589969 Borreliella burgdorferi Species 0.000 description 1
• 241000283690 Bos taurus Species 0.000 description 1
• 208000014644 Brain disease Diseases 0.000 description 1
• 241000283707 Capra Species 0.000 description 1
• DQEFEBPAPFSJLV-UHFFFAOYSA-N Cellulose propionate Chemical compound CCC(=O)OCC1OC(OC(=O)CC)C(OC(=O)CC)C(OC(=O)CC)C1OC1C(OC(=O)CC)C(OC(=O)CC)C(OC(=O)CC)C(COC(=O)CC)O1 DQEFEBPAPFSJLV-UHFFFAOYSA-N 0.000 description 1
• PTHCMJGKKRQCBF-UHFFFAOYSA-N Cellulose, microcrystalline Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC)C(CO)O1 PTHCMJGKKRQCBF-UHFFFAOYSA-N 0.000 description 1
• 241000606153 Chlamydia trachomatis Species 0.000 description 1
• 241000555825 Clupeidae Species 0.000 description 1
• 208000035473 Communicable disease Diseases 0.000 description 1
• 108010062580 Concanavalin A Proteins 0.000 description 1
• 206010010904 Convulsion Diseases 0.000 description 1
• 208000011990 Corticobasal Degeneration Diseases 0.000 description 1
• 208000011231 Crohn disease Diseases 0.000 description 1
• 208000003311 Cytochrome P-450 Enzyme Inhibitors Diseases 0.000 description 1
• YTBSYETUWUMLBZ-UHFFFAOYSA-N D-Erythrose Natural products OCC(O)C(O)C=O YTBSYETUWUMLBZ-UHFFFAOYSA-N 0.000 description 1
• WQZGKKKJIJFFOK-CBPJZXOFSA-N D-Gulose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@H](O)[C@H]1O WQZGKKKJIJFFOK-CBPJZXOFSA-N 0.000 description 1
• WQZGKKKJIJFFOK-WHZQZERISA-N D-aldose Chemical compound OC[C@H]1OC(O)[C@@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-WHZQZERISA-N 0.000 description 1
• CIWBSHSKHKDKBQ-DUZGATOHSA-N D-araboascorbic acid Natural products OC[C@@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-DUZGATOHSA-N 0.000 description 1
• YTBSYETUWUMLBZ-IUYQGCFVSA-N D-erythrose Chemical compound OC[C@@H](O)[C@@H](O)C=O YTBSYETUWUMLBZ-IUYQGCFVSA-N 0.000 description 1
• SHZGCJCMOBCMKK-UHFFFAOYSA-N D-mannomethylose Natural products CC1OC(O)C(O)C(O)C1O SHZGCJCMOBCMKK-UHFFFAOYSA-N 0.000 description 1
• YTBSYETUWUMLBZ-QWWZWVQMSA-N D-threose Chemical compound OC[C@@H](O)[C@H](O)C=O YTBSYETUWUMLBZ-QWWZWVQMSA-N 0.000 description 1
• 206010011878 Deafness Diseases 0.000 description 1
• 208000009093 Diffuse Neurofibrillary Tangles with Calcification Diseases 0.000 description 1
• BUDQDWGNQVEFAC-UHFFFAOYSA-N Dihydropyran Chemical compound C1COC=CC1 BUDQDWGNQVEFAC-UHFFFAOYSA-N 0.000 description 1
• WJJMNDUMQPNECX-UHFFFAOYSA-N Dipicolinic acid Natural products OC(=O)C1=CC=CC(C(O)=O)=N1 WJJMNDUMQPNECX-UHFFFAOYSA-N 0.000 description 1
• 101100532699 Drosophila melanogaster scyl gene Proteins 0.000 description 1
• 208000032274 Encephalopathy Diseases 0.000 description 1
• 241000283086 Equidae Species 0.000 description 1
• 206010056474 Erythrosis Diseases 0.000 description 1
• KIWBPDUYBMNFTB-UHFFFAOYSA-N Ethyl hydrogen sulfate Chemical group CCOS(O)(=O)=O KIWBPDUYBMNFTB-UHFFFAOYSA-N 0.000 description 1
• IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 description 1
• 108050001049 Extracellular proteins Proteins 0.000 description 1
• 206010016202 Familial Amyloidosis Diseases 0.000 description 1
• 208000007487 Familial Cerebral Amyloid Angiopathy Diseases 0.000 description 1
• 206010016207 Familial Mediterranean fever Diseases 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
• BDAGIHXWWSANSR-UHFFFAOYSA-M Formate Chemical compound [O-]C=O BDAGIHXWWSANSR-UHFFFAOYSA-M 0.000 description 1
• PNNNRSAQSRJVSB-SLPGGIOYSA-N Fucose Natural products C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)C=O PNNNRSAQSRJVSB-SLPGGIOYSA-N 0.000 description 1
• 241000233866 Fungi Species 0.000 description 1
• 108010010803 Gelatin Proteins 0.000 description 1
• 239000001828 Gelatine Substances 0.000 description 1
• 208000034826 Genetic Predisposition to Disease Diseases 0.000 description 1
• 206010072075 Gerstmann-Straussler-Scheinker syndrome Diseases 0.000 description 1
• 206010018341 Gliosis Diseases 0.000 description 1
• WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 1
• 229930186217 Glycolipid Natural products 0.000 description 1
• 241000282575 Gorilla Species 0.000 description 1
• 201000005569 Gout Diseases 0.000 description 1
• 102000015779 HDL Lipoproteins Human genes 0.000 description 1
• 108010010234 HDL Lipoproteins Proteins 0.000 description 1
• 241000606768 Haemophilus influenzae Species 0.000 description 1
• 102000014702 Haptoglobin Human genes 0.000 description 1
• 108050005077 Haptoglobin Proteins 0.000 description 1
• 206010019196 Head injury Diseases 0.000 description 1
• 241000590002 Helicobacter pylori Species 0.000 description 1
• 208000032843 Hemorrhage Diseases 0.000 description 1
• 208000032849 Hereditary cerebral hemorrhage with amyloidosis Diseases 0.000 description 1
• 208000017604 Hodgkin disease Diseases 0.000 description 1
• 208000021519 Hodgkin lymphoma Diseases 0.000 description 1
• 208000010747 Hodgkins lymphoma Diseases 0.000 description 1
• 241001272567 Hominoidea Species 0.000 description 1
• 241000282412 Homo Species 0.000 description 1
• 101000573901 Homo sapiens Major prion protein Proteins 0.000 description 1
• 101000772194 Homo sapiens Transthyretin Proteins 0.000 description 1
• 241000701024 Human betaherpesvirus 5 Species 0.000 description 1
• 241000725303 Human immunodeficiency virus Species 0.000 description 1
• 208000023105 Huntington disease Diseases 0.000 description 1
• OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 description 1
• AVXURJPOCDRRFD-UHFFFAOYSA-N Hydroxylamine Chemical compound ON AVXURJPOCDRRFD-UHFFFAOYSA-N 0.000 description 1
• 206010020772 Hypertension Diseases 0.000 description 1
• 201000000162 ITM2B-related cerebral amyloid angiopathy 1 Diseases 0.000 description 1
• 208000005531 Immunoglobulin Light-chain Amyloidosis Diseases 0.000 description 1
• 208000003456 Juvenile Arthritis Diseases 0.000 description 1
• 206010059176 Juvenile idiopathic arthritis Diseases 0.000 description 1
• 208000007976 Ketosis Diseases 0.000 description 1
• WQZGKKKJIJFFOK-VSOAQEOCSA-N L-altropyranose Chemical compound OC[C@@H]1OC(O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-VSOAQEOCSA-N 0.000 description 1
• CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 1
• SHZGCJCMOBCMKK-DHVFOXMCSA-N L-fucopyranose Chemical compound C[C@@H]1OC(O)[C@@H](O)[C@H](O)[C@@H]1O SHZGCJCMOBCMKK-DHVFOXMCSA-N 0.000 description 1
• WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
• HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 description 1
• 102000007330 LDL Lipoproteins Human genes 0.000 description 1
• 108010007622 LDL Lipoproteins Proteins 0.000 description 1
• 244000147568 Laurus nobilis Species 0.000 description 1
• 235000017858 Laurus nobilis Nutrition 0.000 description 1
• 108090001090 Lectins Proteins 0.000 description 1
• 102000004856 Lectins Human genes 0.000 description 1
• 241000222724 Leishmania amazonensis Species 0.000 description 1
• 206010024229 Leprosy Diseases 0.000 description 1
• 235000010643 Leucaena leucocephala Nutrition 0.000 description 1
• 240000007472 Leucaena leucocephala Species 0.000 description 1
• 208000009829 Lewy Body Disease Diseases 0.000 description 1
• 201000002832 Lewy body dementia Diseases 0.000 description 1
• 241000186779 Listeria monocytogenes Species 0.000 description 1
• 208000002569 Machado-Joseph Disease Diseases 0.000 description 1
• FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
• 229920003091 Methocel™ Polymers 0.000 description 1
• 102000005431 Molecular Chaperones Human genes 0.000 description 1
• 206010060880 Monoclonal gammopathy Diseases 0.000 description 1
• 201000002795 Muckle-Wells syndrome Diseases 0.000 description 1
• 241000187479 Mycobacterium tuberculosis Species 0.000 description 1
• 241000202934 Mycoplasma pneumoniae Species 0.000 description 1
• 201000002481 Myositis Diseases 0.000 description 1
• 206010068871 Myotonic dystrophy Diseases 0.000 description 1
• WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
• MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 description 1
• 241000588652 Neisseria gonorrhoeae Species 0.000 description 1
• 206010028980 Neoplasm Diseases 0.000 description 1
• QITXUNGWNHDLPM-UHFFFAOYSA-N OS(O)(=O)=O.OS(O)(=O)=O.OS(O)(=O)=O.OCC(C)(CO)CO Chemical compound OS(O)(=O)=O.OS(O)(=O)=O.OS(O)(=O)=O.OCC(C)(CO)CO QITXUNGWNHDLPM-UHFFFAOYSA-N 0.000 description 1
• 206010031252 Osteomyelitis Diseases 0.000 description 1
• 241000282579 Pan Species 0.000 description 1
• 206010056332 Panencephalitis Diseases 0.000 description 1
• 208000002774 Paraproteinemias Diseases 0.000 description 1
• 208000027089 Parkinsonian disease Diseases 0.000 description 1
• 206010034010 Parkinsonism Diseases 0.000 description 1
• 108010046016 Peanut Agglutinin Proteins 0.000 description 1
• 102000035195 Peptidases Human genes 0.000 description 1
• 108091005804 Peptidases Proteins 0.000 description 1
• 208000037581 Persistent Infection Diseases 0.000 description 1
• 229940049937 Pgp inhibitor Drugs 0.000 description 1
• 208000000609 Pick Disease of the Brain Diseases 0.000 description 1
• 208000024571 Pick disease Diseases 0.000 description 1
• 241000223960 Plasmodium falciparum Species 0.000 description 1
• 229920002319 Poly(methyl acrylate) Polymers 0.000 description 1
• 239000004698 Polyethylene Substances 0.000 description 1
• 206010036105 Polyneuropathy Diseases 0.000 description 1
• 239000004793 Polystyrene Substances 0.000 description 1
• 208000036757 Postencephalitic parkinsonism Diseases 0.000 description 1
• 206010036631 Presenile dementia Diseases 0.000 description 1
• 208000014675 Prion-associated disease Diseases 0.000 description 1
• 239000004365 Protease Substances 0.000 description 1
• 241000589517 Pseudomonas aeruginosa Species 0.000 description 1
• 201000004681 Psoriasis Diseases 0.000 description 1
• 208000028017 Psychotic disease Diseases 0.000 description 1
• IWYDHOAUDWTVEP-UHFFFAOYSA-N R-2-phenyl-2-hydroxyacetic acid Natural products OC(=O)C(O)C1=CC=CC=C1 IWYDHOAUDWTVEP-UHFFFAOYSA-N 0.000 description 1
• 208000033464 Reiter syndrome Diseases 0.000 description 1
• 206010038389 Renal cancer Diseases 0.000 description 1
• 208000006265 Renal cell carcinoma Diseases 0.000 description 1
• 241000283984 Rodentia Species 0.000 description 1
• 208000009106 Shy-Drager Syndrome Diseases 0.000 description 1
• 241000700584 Simplexvirus Species 0.000 description 1
• 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 1
• DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
• 229920002125 Sokalan® Polymers 0.000 description 1
• 208000036834 Spinocerebellar ataxia type 3 Diseases 0.000 description 1
• 241000191967 Staphylococcus aureus Species 0.000 description 1
• 235000021355 Stearic acid Nutrition 0.000 description 1
• 241000194019 Streptococcus mutans Species 0.000 description 1
• 241000194021 Streptococcus suis Species 0.000 description 1
• KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
• 241000282887 Suidae Species 0.000 description 1
• OUUQCZGPVNCOIJ-UHFFFAOYSA-M Superoxide Chemical compound [O-][O] OUUQCZGPVNCOIJ-UHFFFAOYSA-M 0.000 description 1
• 206010048327 Supranuclear palsy Diseases 0.000 description 1
• 208000034799 Tauopathies Diseases 0.000 description 1
• 235000005212 Terminalia tomentosa Nutrition 0.000 description 1
• 102000004338 Transferrin Human genes 0.000 description 1
• 108090000901 Transferrin Proteins 0.000 description 1
• GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 1
• 206010044688 Trisomy 21 Diseases 0.000 description 1
• 241000223109 Trypanosoma cruzi Species 0.000 description 1
• 208000007930 Type C Niemann-Pick Disease Diseases 0.000 description 1
• 208000024780 Urticaria Diseases 0.000 description 1
• 238000005411 Van der Waals force Methods 0.000 description 1
• 201000004810 Vascular dementia Diseases 0.000 description 1
• XTXRWKRVRITETP-UHFFFAOYSA-N Vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 description 1
• 208000033559 Waldenström macroglobulinemia Diseases 0.000 description 1
• 108010046516 Wheat Germ Agglutinins Proteins 0.000 description 1
• CROCWAYPRBALHB-KVTDHHQDSA-N [(2r,3s,4s,5r)-1,3,4,6-tetrahydroxy-5-sulfooxyhexan-2-yl] hydrogen sulfate Chemical compound OS(=O)(=O)O[C@H](CO)[C@@H](O)[C@H](O)[C@@H](CO)OS(O)(=O)=O CROCWAYPRBALHB-KVTDHHQDSA-N 0.000 description 1
• DDLGCBVIBYNOMF-WLDMJGECSA-N [(3R,4S,5R,6R)-2,5-dihydroxy-6-(hydroxymethyl)-2-methyl-3-sulfooxyoxan-4-yl] hydrogen sulfate Chemical compound S(=O)(=O)(O)O[C@H]1C(O)(O[C@@H]([C@H]([C@@H]1OS(=O)(=O)O)O)CO)C DDLGCBVIBYNOMF-WLDMJGECSA-N 0.000 description 1
• DFPAKSUCGFBDDF-ZQBYOMGUSA-N [14c]-nicotinamide Chemical compound N[14C](=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-ZQBYOMGUSA-N 0.000 description 1
• 230000004849 abnormal protein aggregation Effects 0.000 description 1
• 239000002250 absorbent Substances 0.000 description 1
• 230000002745 absorbent Effects 0.000 description 1
• 230000001133 acceleration Effects 0.000 description 1
• 229940091181 aconitic acid Drugs 0.000 description 1
• 230000004913 activation Effects 0.000 description 1
• 239000013543 active substance Substances 0.000 description 1
• 230000009056 active transport Effects 0.000 description 1
• 230000001154 acute effect Effects 0.000 description 1
• VWAIZPYLEYEEFK-UHFFFAOYSA-N adamantane-1,3,5,7-tetracarboxylic acid Chemical compound C1C(C2)(C(O)=O)CC3(C(O)=O)CC1(C(=O)O)CC2(C(O)=O)C3 VWAIZPYLEYEEFK-UHFFFAOYSA-N 0.000 description 1
• 239000000853 adhesive Substances 0.000 description 1
• 230000001070 adhesive effect Effects 0.000 description 1
• 239000001361 adipic acid Substances 0.000 description 1
• 235000011037 adipic acid Nutrition 0.000 description 1
• 239000000443 aerosol Substances 0.000 description 1
• 230000032683 aging Effects 0.000 description 1
• 201000007930 alcohol dependence Diseases 0.000 description 1
• 150000001320 aldopentoses Chemical class 0.000 description 1
• 235000010443 alginic acid Nutrition 0.000 description 1
• 229920000615 alginic acid Polymers 0.000 description 1
• 150000001335 aliphatic alkanes Chemical class 0.000 description 1
• 150000001340 alkali metals Chemical class 0.000 description 1
• 229910052784 alkaline earth metal Inorganic materials 0.000 description 1
• 125000005024 alkenyl aryl group Chemical group 0.000 description 1
• 125000005452 alkenyloxyalkyl group Chemical group 0.000 description 1
• 125000003806 alkyl carbonyl amino group Chemical group 0.000 description 1
• 125000004448 alkyl carbonyl group Chemical group 0.000 description 1
• 125000005196 alkyl carbonyloxy group Chemical group 0.000 description 1
• 125000004687 alkyl sulfinyl alkyl group Chemical group 0.000 description 1
• 125000004688 alkyl sulfonyl alkyl group Chemical group 0.000 description 1
• 150000001356 alkyl thiols Chemical class 0.000 description 1
• HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 description 1
• 229910052782 aluminium Inorganic materials 0.000 description 1
• XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
• 235000012211 aluminium silicate Nutrition 0.000 description 1
• 125000003277 amino group Chemical group 0.000 description 1
• 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 description 1
• 230000006933 amyloid-beta aggregation Effects 0.000 description 1
• 238000013103 analytical ultracentrifugation Methods 0.000 description 1
• 208000022531 anorexia Diseases 0.000 description 1
• 230000001475 anti-trypsic effect Effects 0.000 description 1
• 230000036506 anxiety Effects 0.000 description 1
• 239000012736 aqueous medium Substances 0.000 description 1
• 239000007864 aqueous solution Substances 0.000 description 1
• 125000004659 aryl alkyl thio group Chemical group 0.000 description 1
• 125000005129 aryl carbonyl group Chemical group 0.000 description 1
• 125000005160 aryl oxy alkyl group Chemical group 0.000 description 1
• 125000005135 aryl sulfinyl group Chemical group 0.000 description 1
• 125000005110 aryl thio group Chemical group 0.000 description 1
• 125000005164 aryl thioalkyl group Chemical group 0.000 description 1
• 235000010323 ascorbic acid Nutrition 0.000 description 1
• 239000011668 ascorbic acid Substances 0.000 description 1
• 229960005070 ascorbic acid Drugs 0.000 description 1
• 235000003704 aspartic acid Nutrition 0.000 description 1
• 238000003556 assay Methods 0.000 description 1
• 230000037424 autonomic function Effects 0.000 description 1
• 125000003828 azulenyl group Chemical group 0.000 description 1
• 239000011324 bead Substances 0.000 description 1
• 235000013871 bee wax Nutrition 0.000 description 1
• 239000012166 beeswax Substances 0.000 description 1
• RFRXIWQYSOIBDI-UHFFFAOYSA-N benzarone Chemical compound CCC=1OC2=CC=CC=C2C=1C(=O)C1=CC=C(O)C=C1 RFRXIWQYSOIBDI-UHFFFAOYSA-N 0.000 description 1
• WRUAHXANJKHFIL-UHFFFAOYSA-N benzene-1,3-disulfonic acid Chemical group OS(=O)(=O)C1=CC=CC(S(O)(=O)=O)=C1 WRUAHXANJKHFIL-UHFFFAOYSA-N 0.000 description 1
• SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 1
• 229940092714 benzenesulfonic acid Drugs 0.000 description 1
• 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
• 235000010233 benzoic acid Nutrition 0.000 description 1
• 125000005874 benzothiadiazolyl group Chemical group 0.000 description 1
• 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 description 1
• 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 description 1
• 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 1
• 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 description 1
• 102000015736 beta 2-Microglobulin Human genes 0.000 description 1
• 108010081355 beta 2-Microglobulin Proteins 0.000 description 1
• MSWZFWKMSRAUBD-QZABAPFNSA-N beta-D-glucosamine Chemical compound N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-QZABAPFNSA-N 0.000 description 1
• OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 1
• 230000002902 bimodal effect Effects 0.000 description 1
• 230000036983 biotransformation Effects 0.000 description 1
• 125000006267 biphenyl group Chemical group 0.000 description 1
• 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 description 1
• 230000000903 blocking effect Effects 0.000 description 1
• 210000004204 blood vessel Anatomy 0.000 description 1
• 210000001124 body fluid Anatomy 0.000 description 1
• 208000005881 bovine spongiform encephalopathy Diseases 0.000 description 1
• 239000000872 buffer Substances 0.000 description 1
• 239000007853 buffer solution Substances 0.000 description 1
• 239000004067 bulking agent Substances 0.000 description 1
• YCRNRLUOZIMHNE-UHFFFAOYSA-N butane-1,4-diol;sulfo hydrogen sulfate Chemical compound OCCCCO.OS(=O)(=O)OS(O)(=O)=O YCRNRLUOZIMHNE-UHFFFAOYSA-N 0.000 description 1
• DFBAXFGODMNLMW-UHFFFAOYSA-N butane-1,4-diol;sulfuric acid Chemical compound OS(O)(=O)=O.OCCCCO DFBAXFGODMNLMW-UHFFFAOYSA-N 0.000 description 1
• QDHFHIQKOVNCNC-UHFFFAOYSA-N butane-1-sulfonic acid Chemical compound CCCCS(O)(=O)=O QDHFHIQKOVNCNC-UHFFFAOYSA-N 0.000 description 1
• KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
• ZTAYJSRSQODHEO-UHFFFAOYSA-N butylsilicon Chemical compound CCCC[Si] ZTAYJSRSQODHEO-UHFFFAOYSA-N 0.000 description 1
• 125000000480 butynyl group Chemical group [*]C#CC([H])([H])C([H])([H])[H] 0.000 description 1
• 210000004899 c-terminal region Anatomy 0.000 description 1
• CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
• 235000013539 calcium stearate Nutrition 0.000 description 1
• 239000008116 calcium stearate Substances 0.000 description 1
• 229940078456 calcium stearate Drugs 0.000 description 1
• 238000004364 calculation method Methods 0.000 description 1
• 201000011510 cancer Diseases 0.000 description 1
• 150000004657 carbamic acid derivatives Chemical class 0.000 description 1
• 239000004202 carbamide Substances 0.000 description 1
• 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 description 1
• 125000002837 carbocyclic group Chemical group 0.000 description 1
• 125000000837 carbohydrate group Chemical group 0.000 description 1
• 150000001722 carbon compounds Chemical class 0.000 description 1
• 239000001569 carbon dioxide Substances 0.000 description 1
• 229910002092 carbon dioxide Inorganic materials 0.000 description 1
• 239000011203 carbon fibre reinforced carbon Substances 0.000 description 1
• 125000001721 carboxyacetyl group Chemical group 0.000 description 1
• 239000004203 carnauba wax Substances 0.000 description 1
• 235000013869 carnauba wax Nutrition 0.000 description 1
• 239000004359 castor oil Substances 0.000 description 1
• 235000019438 castor oil Nutrition 0.000 description 1
• 229920002301 cellulose acetate Polymers 0.000 description 1
• 229920006217 cellulose acetate butyrate Polymers 0.000 description 1
• 229920001727 cellulose butyrate Polymers 0.000 description 1
• 229920006218 cellulose propionate Polymers 0.000 description 1
• 235000013339 cereals Nutrition 0.000 description 1
• 229930183167 cerebroside Natural products 0.000 description 1
• RIZIAUKTHDLMQX-UHFFFAOYSA-N cerebroside D Natural products CCCCCCCCCCCCCCCCC(O)C(=O)NC(C(O)C=CCCC=C(C)CCCCCCCCC)COC1OC(CO)C(O)C(O)C1O RIZIAUKTHDLMQX-UHFFFAOYSA-N 0.000 description 1
• 208000026106 cerebrovascular disease Diseases 0.000 description 1
• 238000001311 chemical methods and process Methods 0.000 description 1
• 239000003638 chemical reducing agent Substances 0.000 description 1
• 229940038705 chlamydia trachomatis Drugs 0.000 description 1
• 125000004803 chlorobenzyl group Chemical group 0.000 description 1
• 238000004587 chromatography analysis Methods 0.000 description 1
• 208000037893 chronic inflammatory disorder Diseases 0.000 description 1
• GTZCVFVGUGFEME-IWQZZHSRSA-N cis-aconitic acid Chemical compound OC(=O)C\C(C(O)=O)=C\C(O)=O GTZCVFVGUGFEME-IWQZZHSRSA-N 0.000 description 1
• 230000019771 cognition Effects 0.000 description 1
• 230000003920 cognitive function Effects 0.000 description 1
• 230000007370 cognitive improvement Effects 0.000 description 1
• 230000003931 cognitive performance Effects 0.000 description 1
• 238000002648 combination therapy Methods 0.000 description 1
• 238000005056 compaction Methods 0.000 description 1
• 239000007891 compressed tablet Substances 0.000 description 1
• 238000007906 compression Methods 0.000 description 1
• 238000012790 confirmation Methods 0.000 description 1
• 239000000039 congener Substances 0.000 description 1
• 239000000470 constituent Substances 0.000 description 1
• 238000010276 construction Methods 0.000 description 1
• 230000001276 controlling effect Effects 0.000 description 1
• 229960000913 crospovidone Drugs 0.000 description 1
• 208000022993 cryopyrin-associated periodic syndrome Diseases 0.000 description 1
• 239000002178 crystalline material Substances 0.000 description 1
• 125000004465 cycloalkenyloxy group Chemical group 0.000 description 1
• 125000001047 cyclobutenyl group Chemical group C1(=CCC1)* 0.000 description 1
• 125000001162 cycloheptenyl group Chemical group C1(=CCCCCC1)* 0.000 description 1
• UXKNXFQFFVTNEO-UHFFFAOYSA-N cyclohexane-1,3-diol;sulfo hydrogen sulfate Chemical group OC1CCCC(O)C1.OS(=O)(=O)OS(O)(=O)=O UXKNXFQFFVTNEO-UHFFFAOYSA-N 0.000 description 1
• 125000006639 cyclohexyl carbonyl group Chemical group 0.000 description 1
• 125000002933 cyclohexyloxy group Chemical group C1(CCCCC1)O* 0.000 description 1
• 125000006547 cyclononyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
• 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
• 125000001887 cyclopentyloxy group Chemical group C1(CCCC1)O* 0.000 description 1
• 231100000895 deafness Toxicity 0.000 description 1
• 206010061428 decreased appetite Diseases 0.000 description 1
• 230000003111 delayed effect Effects 0.000 description 1
• 230000001419 dependent effect Effects 0.000 description 1
• 238000009795 derivation Methods 0.000 description 1
• 239000008121 dextrose Substances 0.000 description 1
• 206010012601 diabetes mellitus Diseases 0.000 description 1
• 238000002405 diagnostic procedure Methods 0.000 description 1
• ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 description 1
• 238000004821 distillation Methods 0.000 description 1
• 238000009826 distribution Methods 0.000 description 1
• 238000009509 drug development Methods 0.000 description 1
• 238000007876 drug discovery Methods 0.000 description 1
• 230000008482 dysregulation Effects 0.000 description 1
• 230000002526 effect on cardiovascular system Effects 0.000 description 1
• 239000003995 emulsifying agent Substances 0.000 description 1
• 230000037149 energy metabolism Effects 0.000 description 1
• 239000003623 enhancer Substances 0.000 description 1
• 230000002708 enhancing effect Effects 0.000 description 1
• 230000000688 enterotoxigenic effect Effects 0.000 description 1
• 206010015037 epilepsy Diseases 0.000 description 1
• 235000010350 erythorbic acid Nutrition 0.000 description 1
• 239000004318 erythorbic acid Substances 0.000 description 1
• CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 description 1
• 150000002170 ethers Chemical class 0.000 description 1
• MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 description 1
• 229920001038 ethylene copolymer Polymers 0.000 description 1
• 230000008020 evaporation Effects 0.000 description 1
• 238000013265 extended release Methods 0.000 description 1
• 150000004665 fatty acids Chemical class 0.000 description 1
• 150000002191 fatty alcohols Chemical class 0.000 description 1
• 229940012952 fibrinogen Drugs 0.000 description 1
• 238000001914 filtration Methods 0.000 description 1
• 239000012530 fluid Substances 0.000 description 1
• 125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 description 1
• 235000013305 food Nutrition 0.000 description 1
• 235000012631 food intake Nutrition 0.000 description 1
• 235000019253 formic acid Nutrition 0.000 description 1
• 229940013688 formic acid Drugs 0.000 description 1
• 239000012634 fragment Substances 0.000 description 1
• 235000011087 fumaric acid Nutrition 0.000 description 1
• 150000002270 gangliosides Chemical class 0.000 description 1
• 238000002290 gas chromatography-mass spectrometry Methods 0.000 description 1
• 239000008273 gelatin Substances 0.000 description 1
• 229940014259 gelatin Drugs 0.000 description 1
• 239000007903 gelatin capsule Substances 0.000 description 1
• 235000011852 gelatine desserts Nutrition 0.000 description 1
• 230000007387 gliosis Effects 0.000 description 1
• 235000013922 glutamic acid Nutrition 0.000 description 1
• 239000004220 glutamic acid Substances 0.000 description 1
• MNQZXJOMYWMBOU-UHFFFAOYSA-N glyceraldehyde Chemical compound OCC(O)C=O MNQZXJOMYWMBOU-UHFFFAOYSA-N 0.000 description 1
• 235000011187 glycerol Nutrition 0.000 description 1
• ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
• 229940075507 glyceryl monostearate Drugs 0.000 description 1
• FETSQPAGYOVAQU-UHFFFAOYSA-N glyceryl palmitostearate Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O FETSQPAGYOVAQU-UHFFFAOYSA-N 0.000 description 1
• 229940046813 glyceryl palmitostearate Drugs 0.000 description 1
• 239000002748 glycoprotein P inhibitor Substances 0.000 description 1
• 239000008187 granular material Substances 0.000 description 1
• 238000000227 grinding Methods 0.000 description 1
• 208000035474 group of disease Diseases 0.000 description 1
• 230000012010 growth Effects 0.000 description 1
• 229940047650 haemophilus influenzae Drugs 0.000 description 1
• 125000000262 haloalkenyl group Chemical group 0.000 description 1
• 125000005291 haloalkenyloxy group Chemical group 0.000 description 1
• 125000001475 halogen functional group Chemical group 0.000 description 1
• 235000015220 hamburgers Nutrition 0.000 description 1
• 210000003128 head Anatomy 0.000 description 1
• 208000016354 hearing loss disease Diseases 0.000 description 1
• 229940037467 helicobacter pylori Drugs 0.000 description 1
• UNDBKFIFRQCZQF-UHFFFAOYSA-N heptane-4-sulfonic acid Chemical compound CCCC(S(O)(=O)=O)CCC UNDBKFIFRQCZQF-UHFFFAOYSA-N 0.000 description 1
• 125000004404 heteroalkyl group Chemical group 0.000 description 1
• 125000004475 heteroaralkyl group Chemical group 0.000 description 1
• 125000004446 heteroarylalkyl group Chemical group 0.000 description 1
• 125000005241 heteroarylamino group Chemical group 0.000 description 1
• 125000005223 heteroarylcarbonyl group Chemical group 0.000 description 1
• 125000005150 heteroarylsulfinyl group Chemical group 0.000 description 1
• 125000005143 heteroarylsulfonyl group Chemical group 0.000 description 1
• 125000005980 hexynyl group Chemical group 0.000 description 1
• HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 1
• 230000003284 homeostatic effect Effects 0.000 description 1
• 230000003054 hormonal effect Effects 0.000 description 1
• 230000036571 hydration Effects 0.000 description 1
• 238000006703 hydration reaction Methods 0.000 description 1
• 239000008172 hydrogenated vegetable oil Substances 0.000 description 1
• 230000007062 hydrolysis Effects 0.000 description 1
• 238000006460 hydrolysis reaction Methods 0.000 description 1
• 230000002209 hydrophobic effect Effects 0.000 description 1
• ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 description 1
• 125000004356 hydroxy functional group Chemical group O* 0.000 description 1
• 125000002349 hydroxyamino group Chemical group [H]ON([H])[*] 0.000 description 1
• 229920003063 hydroxymethyl cellulose Polymers 0.000 description 1
• 229940031574 hydroxymethyl cellulose Drugs 0.000 description 1
• 125000002632 imidazolidinyl group Chemical group 0.000 description 1
• 125000001841 imino group Chemical group [H]N=* 0.000 description 1
• 230000006872 improvement Effects 0.000 description 1
• 239000012535 impurity Substances 0.000 description 1
• 238000010348 incorporation Methods 0.000 description 1
• 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 description 1
• 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 description 1
• 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 description 1
• 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 description 1
• 125000001041 indolyl group Chemical group 0.000 description 1
• 230000002458 infectious effect Effects 0.000 description 1
• 230000028709 inflammatory response Effects 0.000 description 1
• 238000001802 infusion Methods 0.000 description 1
• 229940102223 injectable solution Drugs 0.000 description 1
• 239000000976 ink Substances 0.000 description 1
• 150000007529 inorganic bases Chemical class 0.000 description 1
• 150000004001 inositols Chemical class 0.000 description 1
• 206010022437 insomnia Diseases 0.000 description 1
• 206010022498 insulinoma Diseases 0.000 description 1
• 239000000543 intermediate Substances 0.000 description 1
• 230000003834 intracellular effect Effects 0.000 description 1
• 238000007918 intramuscular administration Methods 0.000 description 1
• 238000007912 intraperitoneal administration Methods 0.000 description 1
• 230000009545 invasion Effects 0.000 description 1
• PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 description 1
• 125000002346 iodo group Chemical group I* 0.000 description 1
• 239000003456 ion exchange resin Substances 0.000 description 1
• 229920003303 ion-exchange polymer Polymers 0.000 description 1
• 150000002500 ions Chemical class 0.000 description 1
• 210000004153 islets of langerhan Anatomy 0.000 description 1
• 229940026239 isoascorbic acid Drugs 0.000 description 1
• IQPQWNKOIGAROB-UHFFFAOYSA-N isocyanate Chemical compound [N-]=C=O IQPQWNKOIGAROB-UHFFFAOYSA-N 0.000 description 1
• 239000012948 isocyanate Substances 0.000 description 1
• 150000002513 isocyanates Chemical class 0.000 description 1
• 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 description 1
• 238000002955 isolation Methods 0.000 description 1
• 125000005956 isoquinolyl group Chemical group 0.000 description 1
• 201000002215 juvenile rheumatoid arthritis Diseases 0.000 description 1
• NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
• 150000002576 ketones Chemical class 0.000 description 1
• 150000002584 ketoses Chemical class 0.000 description 1
• 210000003734 kidney Anatomy 0.000 description 1
• 208000017169 kidney disease Diseases 0.000 description 1
• 238000002372 labelling Methods 0.000 description 1
• 150000003951 lactams Chemical group 0.000 description 1
• 239000002523 lectin Substances 0.000 description 1
• 229940059904 light mineral oil Drugs 0.000 description 1
• 230000027928 long-term synaptic potentiation Effects 0.000 description 1
• 210000004072 lung Anatomy 0.000 description 1
• 201000000564 macroglobulinemia Diseases 0.000 description 1
• 239000011777 magnesium Substances 0.000 description 1
• 229910052749 magnesium Inorganic materials 0.000 description 1
• ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
• 239000001095 magnesium carbonate Substances 0.000 description 1
• 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
• 239000000395 magnesium oxide Substances 0.000 description 1
• CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
• 235000019359 magnesium stearate Nutrition 0.000 description 1
• AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 1
• 229960002510 mandelic acid Drugs 0.000 description 1
• 239000013563 matrix tablet Substances 0.000 description 1
• 230000007246 mechanism Effects 0.000 description 1
• 150000004667 medium chain fatty acids Chemical class 0.000 description 1
• 230000015654 memory Effects 0.000 description 1
• 230000006386 memory function Effects 0.000 description 1
• 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 description 1
• 230000007483 microbial process Effects 0.000 description 1
• 239000002480 mineral oil Substances 0.000 description 1
• 235000010446 mineral oil Nutrition 0.000 description 1
• 230000000116 mitigating effect Effects 0.000 description 1
• 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 1
• 150000004682 monohydrates Chemical class 0.000 description 1
• 230000004973 motor coordination Effects 0.000 description 1
• 201000000050 myeloid neoplasm Diseases 0.000 description 1
• 125000003136 n-heptyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
• 125000005186 naphthyloxy group Chemical group C1(=CC=CC2=CC=CC=C12)O* 0.000 description 1
• 230000001537 neural effect Effects 0.000 description 1
• 210000005044 neurofilament Anatomy 0.000 description 1
• 230000002981 neuropathic effect Effects 0.000 description 1
• 230000007171 neuropathology Effects 0.000 description 1
• 235000001968 nicotinic acid Nutrition 0.000 description 1
• 229960003512 nicotinic acid Drugs 0.000 description 1
• 239000011664 nicotinic acid Substances 0.000 description 1
• 125000001196 nonadecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
• 239000002736 nonionic surfactant Substances 0.000 description 1
• 231100000252 nontoxic Toxicity 0.000 description 1
• 230000003000 nontoxic effect Effects 0.000 description 1
• QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
• OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
• 229940100692 oral suspension Drugs 0.000 description 1
• 238000006053 organic reaction Methods 0.000 description 1
• 125000001715 oxadiazolyl group Chemical group 0.000 description 1
• 125000002971 oxazolyl group Chemical group 0.000 description 1
• 239000006174 pH buffer Substances 0.000 description 1
• 208000021255 pancreatic insulinoma Diseases 0.000 description 1
• 208000002593 pantothenate kinase-associated neurodegeneration Diseases 0.000 description 1
• 239000012188 paraffin wax Substances 0.000 description 1
• 238000007911 parenteral administration Methods 0.000 description 1
• 239000006201 parenteral dosage form Substances 0.000 description 1
• 230000036961 partial effect Effects 0.000 description 1
• 230000009057 passive transport Effects 0.000 description 1
• 230000001717 pathogenic effect Effects 0.000 description 1
• 230000001575 pathological effect Effects 0.000 description 1
• KVLWQGNBEIWRHX-UHFFFAOYSA-N pentane-1,5-diol;sulfuric acid Chemical compound OS(O)(=O)=O.OCCCCCO KVLWQGNBEIWRHX-UHFFFAOYSA-N 0.000 description 1
• WAIFNKJFSAECAT-UHFFFAOYSA-N pentane-1,5-disulfonic acid Chemical compound OS(=O)(=O)CCCCCS(O)(=O)=O WAIFNKJFSAECAT-UHFFFAOYSA-N 0.000 description 1
• RJQRCOMHVBLQIH-UHFFFAOYSA-N pentane-1-sulfonic acid Chemical compound CCCCCS(O)(=O)=O RJQRCOMHVBLQIH-UHFFFAOYSA-N 0.000 description 1
• 150000002972 pentoses Chemical class 0.000 description 1
• 125000005981 pentynyl group Chemical group 0.000 description 1
• 239000000816 peptidomimetic Substances 0.000 description 1
• 239000008194 pharmaceutical composition Substances 0.000 description 1
• 230000000144 pharmacologic effect Effects 0.000 description 1
• 239000012071 phase Substances 0.000 description 1
• 125000001828 phenalenyl group Chemical group C1(C=CC2=CC=CC3=CC=CC1=C23)* 0.000 description 1
• UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 description 1
• 239000008363 phosphate buffer Substances 0.000 description 1
• 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 description 1
• 150000003905 phosphatidylinositols Chemical class 0.000 description 1
• ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical compound [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 description 1
• 150000003904 phospholipids Chemical class 0.000 description 1
• UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 description 1
• 125000000612 phthaloyl group Chemical group C(C=1C(C(=O)*)=CC=CC1)(=O)* 0.000 description 1
• 230000000704 physical effect Effects 0.000 description 1
• 230000035479 physiological effects, processes and functions Effects 0.000 description 1
• 125000004193 piperazinyl group Chemical group 0.000 description 1
• 230000007505 plaque formation Effects 0.000 description 1
• 210000004180 plasmocyte Anatomy 0.000 description 1
• 229960005455 polacrilin Drugs 0.000 description 1
• 229920001983 poloxamer Polymers 0.000 description 1
• 229920003229 poly(methyl methacrylate) Polymers 0.000 description 1
• 108010054442 polyalanine Proteins 0.000 description 1
• 239000004417 polycarbonate Substances 0.000 description 1
• 229920000515 polycarbonate Polymers 0.000 description 1
• 229920000573 polyethylene Polymers 0.000 description 1
• 108010040003 polyglutamine Proteins 0.000 description 1
• 229920000155 polyglutamine Polymers 0.000 description 1
• 239000004926 polymethyl methacrylate Substances 0.000 description 1
• 230000007824 polyneuropathy Effects 0.000 description 1
• 229920000056 polyoxyethylene ether Polymers 0.000 description 1
• 229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 description 1
• 229920006324 polyoxymethylene Polymers 0.000 description 1
• 229920001184 polypeptide Polymers 0.000 description 1
• 229920000136 polysorbate Polymers 0.000 description 1
• 229920002223 polystyrene Polymers 0.000 description 1
• 229920002689 polyvinyl acetate Polymers 0.000 description 1
• 229920000915 polyvinyl chloride Polymers 0.000 description 1
• 239000004800 polyvinyl chloride Substances 0.000 description 1
• 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
• 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
• 208000000170 postencephalitic Parkinson disease Diseases 0.000 description 1
• 238000001556 precipitation Methods 0.000 description 1
• 238000012545 processing Methods 0.000 description 1
• 239000000047 product Substances 0.000 description 1
• 230000001737 promoting effect Effects 0.000 description 1
• 125000006238 prop-1-en-1-yl group Chemical group [H]\C(*)=C(/[H])C([H])([H])[H] 0.000 description 1
• CHOCRVHTVJREPS-UHFFFAOYSA-N propan-1-ol;sulfuric acid Chemical compound CCCO.OS(O)(=O)=O CHOCRVHTVJREPS-UHFFFAOYSA-N 0.000 description 1
• FJEDAOMERWWOGQ-UHFFFAOYSA-N propane-1,3-diol;sulfo hydrogen sulfate Chemical compound OCCCO.OS(=O)(=O)OS(O)(=O)=O FJEDAOMERWWOGQ-UHFFFAOYSA-N 0.000 description 1
• MGNVWUDMMXZUDI-UHFFFAOYSA-N propane-1,3-disulfonic acid Chemical compound OS(=O)(=O)CCCS(O)(=O)=O MGNVWUDMMXZUDI-UHFFFAOYSA-N 0.000 description 1
• KCXFHTAICRTXLI-UHFFFAOYSA-N propane-1-sulfonic acid Chemical compound CCCS(O)(=O)=O KCXFHTAICRTXLI-UHFFFAOYSA-N 0.000 description 1
• HNDXKIMMSFCCFW-UHFFFAOYSA-N propane-2-sulphonic acid Chemical compound CC(C)S(O)(=O)=O HNDXKIMMSFCCFW-UHFFFAOYSA-N 0.000 description 1
• 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 description 1
• 238000000746 purification Methods 0.000 description 1
• 125000003373 pyrazinyl group Chemical group 0.000 description 1
• 125000003226 pyrazolyl group Chemical group 0.000 description 1
• 125000002098 pyridazinyl group Chemical group 0.000 description 1
• 125000000714 pyrimidinyl group Chemical group 0.000 description 1
• HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 description 1
• 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
• 125000001422 pyrrolinyl group Chemical group 0.000 description 1
• 125000000168 pyrrolyl group Chemical group 0.000 description 1
• 125000005493 quinolyl group Chemical group 0.000 description 1
• 208000002574 reactive arthritis Diseases 0.000 description 1
• 201000010174 renal carcinoma Diseases 0.000 description 1
• 230000000979 retarding effect Effects 0.000 description 1
• 206010039073 rheumatoid arthritis Diseases 0.000 description 1
• 238000009666 routine test Methods 0.000 description 1
• CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
• 235000019204 saccharin Nutrition 0.000 description 1
• 229940081974 saccharin Drugs 0.000 description 1
• 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
• 229930195734 saturated hydrocarbon Natural products 0.000 description 1
• 201000000980 schizophrenia Diseases 0.000 description 1
• 230000002784 sclerotic effect Effects 0.000 description 1
• 125000002327 selenol group Chemical group [H][Se]* 0.000 description 1
• 230000001235 sensitizing effect Effects 0.000 description 1
• 210000002966 serum Anatomy 0.000 description 1
• 125000004469 siloxy group Chemical group [SiH3]O* 0.000 description 1
• 238000002603 single-photon emission computed tomography Methods 0.000 description 1
• 235000010413 sodium alginate Nutrition 0.000 description 1
• 239000000661 sodium alginate Substances 0.000 description 1
• 229940005550 sodium alginate Drugs 0.000 description 1
• WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
• 239000004299 sodium benzoate Substances 0.000 description 1
• 235000010234 sodium benzoate Nutrition 0.000 description 1
• 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
• 229940045902 sodium stearyl fumarate Drugs 0.000 description 1
• 239000008279 sol Substances 0.000 description 1
• 239000002195 soluble material Substances 0.000 description 1
• 238000007614 solvation Methods 0.000 description 1
• 230000009870 specific binding Effects 0.000 description 1
• 238000004611 spectroscopical analysis Methods 0.000 description 1
• 238000010561 standard procedure Methods 0.000 description 1
• 238000007619 statistical method Methods 0.000 description 1
• 239000008117 stearic acid Substances 0.000 description 1
• 229960004274 stearic acid Drugs 0.000 description 1
• 239000012058 sterile packaged powder Substances 0.000 description 1
• 208000003755 striatonigral degeneration Diseases 0.000 description 1
• 230000002739 subcortical effect Effects 0.000 description 1
• 238000007920 subcutaneous administration Methods 0.000 description 1
• 229940124530 sulfonamide Drugs 0.000 description 1
• 150000003456 sulfonamides Chemical class 0.000 description 1
• 150000003871 sulfonates Chemical class 0.000 description 1
• 125000001273 sulfonato group Chemical group [O-]S(*)(=O)=O 0.000 description 1
• 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
• 239000000829 suppository Substances 0.000 description 1
• 230000004083 survival effect Effects 0.000 description 1
• 239000007939 sustained release tablet Substances 0.000 description 1
• 230000000946 synaptic effect Effects 0.000 description 1
• 239000000454 talc Substances 0.000 description 1
• 229910052623 talc Inorganic materials 0.000 description 1
• 229940033134 talc Drugs 0.000 description 1
• LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
• 239000012085 test solution Substances 0.000 description 1
• 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
• 125000003831 tetrazolyl group Chemical group 0.000 description 1
• 229940124597 therapeutic agent Drugs 0.000 description 1
• 229920001169 thermoplastic Polymers 0.000 description 1
• 239000004416 thermosoftening plastic Substances 0.000 description 1
• 125000001113 thiadiazolyl group Chemical group 0.000 description 1
• 125000001984 thiazolidinyl group Chemical group 0.000 description 1
• 125000001544 thienyl group Chemical group 0.000 description 1
• 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 description 1
• 125000004014 thioethyl group Chemical group [H]SC([H])([H])C([H])([H])* 0.000 description 1
• 125000005323 thioketone group Chemical group 0.000 description 1
• 150000003573 thiols Chemical group 0.000 description 1
• 125000004055 thiomethyl group Chemical group [H]SC([H])([H])* 0.000 description 1
• 125000004568 thiomorpholinyl group Chemical group 0.000 description 1
• 125000004035 thiopropyl group Chemical group [H]SC([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
• 125000005425 toluyl group Chemical group 0.000 description 1
• 230000000699 topical effect Effects 0.000 description 1
• GTZCVFVGUGFEME-UHFFFAOYSA-N trans-aconitic acid Natural products OC(=O)CC(C(O)=O)=CC(O)=O GTZCVFVGUGFEME-UHFFFAOYSA-N 0.000 description 1
• 239000012581 transferrin Substances 0.000 description 1
• 230000009466 transformation Effects 0.000 description 1
• 238000000844 transformation Methods 0.000 description 1
• 238000011830 transgenic mouse model Methods 0.000 description 1
• 150000003626 triacylglycerols Chemical class 0.000 description 1
• 125000001425 triazolyl group Chemical group 0.000 description 1
• QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
• 235000019731 tricalcium phosphate Nutrition 0.000 description 1
• 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 1
• 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
• LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
• 229960000281 trometamol Drugs 0.000 description 1
• 239000002753 trypsin inhibitor Substances 0.000 description 1
• 201000008827 tuberculosis Diseases 0.000 description 1
• 125000002948 undecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
• 230000002792 vascular Effects 0.000 description 1
• 235000015112 vegetable and seed oil Nutrition 0.000 description 1
• 239000008158 vegetable oil Substances 0.000 description 1
• NLVXSWCKKBEXTG-UHFFFAOYSA-N vinylsulfonic acid Chemical compound OS(=O)(=O)C=C NLVXSWCKKBEXTG-UHFFFAOYSA-N 0.000 description 1
• 229920003169 water-soluble polymer Polymers 0.000 description 1
• 239000013585 weight reducing agent Substances 0.000 description 1
• 239000000080 wetting agent Substances 0.000 description 1
• XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1
• 229940057977 zinc stearate Drugs 0.000 description 1