JP2013523746A - Ｄｇａｔ１阻害剤の使用 - Google Patents
Ｄｇａｔ１阻害剤の使用 Download PDFInfo
- Publication number
- JP2013523746A JP2013523746A JP2013502706A JP2013502706A JP2013523746A JP 2013523746 A JP2013523746 A JP 2013523746A JP 2013502706 A JP2013502706 A JP 2013502706A JP 2013502706 A JP2013502706 A JP 2013502706A JP 2013523746 A JP2013523746 A JP 2013523746A
- Authority
- JP
- Japan
- Prior art keywords
- group
- phenyl
- dgat1 inhibitor
- pharmaceutically acceptable
- acceptable salt
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 229940127193 DGAT1 inhibitor Drugs 0.000 title claims abstract description 95
- 238000011282 treatment Methods 0.000 claims abstract description 58
- 150000003839 salts Chemical class 0.000 claims abstract description 51
- 208000011580 syndromic disease Diseases 0.000 claims abstract description 49
- 150000002148 esters Chemical class 0.000 claims abstract description 41
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 37
- 206010060755 Type V hyperlipidaemia Diseases 0.000 claims abstract description 35
- 201000010099 disease Diseases 0.000 claims abstract description 32
- 230000002265 prevention Effects 0.000 claims abstract description 25
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 19
- -1 N-methylpiperidinyl group Chemical group 0.000 claims description 52
- 150000003626 triacylglycerols Chemical group 0.000 claims description 52
- 150000001875 compounds Chemical class 0.000 claims description 44
- 125000000217 alkyl group Chemical group 0.000 claims description 43
- 238000000034 method Methods 0.000 claims description 41
- 208000016667 Familial chylomicronemia syndrome Diseases 0.000 claims description 40
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims description 33
- 125000000623 heterocyclic group Chemical group 0.000 claims description 29
- 125000003118 aryl group Chemical group 0.000 claims description 27
- 206010033645 Pancreatitis Diseases 0.000 claims description 26
- 125000005842 heteroatom Chemical group 0.000 claims description 23
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 21
- 125000004432 carbon atom Chemical group C* 0.000 claims description 19
- 229910052799 carbon Inorganic materials 0.000 claims description 14
- 125000001072 heteroaryl group Chemical group 0.000 claims description 14
- 230000000291 postprandial effect Effects 0.000 claims description 14
- 208000010201 Exanthema Diseases 0.000 claims description 12
- 230000008021 deposition Effects 0.000 claims description 12
- 201000005884 exanthem Diseases 0.000 claims description 12
- 206010019847 hepatosplenomegaly Diseases 0.000 claims description 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 12
- 206010037844 rash Diseases 0.000 claims description 12
- 230000000306 recurrent effect Effects 0.000 claims description 12
- 206010048214 Xanthoma Diseases 0.000 claims description 11
- 206010048215 Xanthomatosis Diseases 0.000 claims description 11
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 11
- 125000002950 monocyclic group Chemical group 0.000 claims description 11
- 208000024891 symptom Diseases 0.000 claims description 11
- 230000006735 deficit Effects 0.000 claims description 10
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Substances CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims description 8
- 229920006395 saturated elastomer Polymers 0.000 claims description 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 7
- ABLZXFCXXLZCGV-UHFFFAOYSA-N phosphonic acid group Chemical group P(O)(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims description 7
- 125000003368 amide group Chemical group 0.000 claims description 6
- 125000003277 amino group Chemical group 0.000 claims description 6
- VILAVOFMIJHSJA-UHFFFAOYSA-N dicarbon monoxide Chemical group [C]=C=O VILAVOFMIJHSJA-UHFFFAOYSA-N 0.000 claims description 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
- 125000003342 alkenyl group Chemical group 0.000 claims description 5
- 125000002947 alkylene group Chemical group 0.000 claims description 5
- 125000000304 alkynyl group Chemical group 0.000 claims description 5
- MUZRGKSNUTWRAF-BHQIMSFRSA-M chembl2364625 Chemical group [Na+].C1C[C@@H](CC(=O)[O-])CC[C@@H]1C1=CC=C(C=2N=CC(NC=3C=NC(=CC=3)C(F)(F)F)=CC=2)C=C1 MUZRGKSNUTWRAF-BHQIMSFRSA-M 0.000 claims description 5
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 5
- 229910052757 nitrogen Inorganic materials 0.000 claims description 5
- 230000009467 reduction Effects 0.000 claims description 5
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 4
- 125000003003 spiro group Chemical group 0.000 claims description 4
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims description 4
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims description 3
- SSCBDEUAEZBUIJ-UHFFFAOYSA-N 2-[4-[6-[5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl]-1h-benzimidazol-2-yl]-3,5-dimethylphenoxy]acetic acid Chemical compound CC1=CC(OCC(O)=O)=CC(C)=C1C1=NC2=CC=C(C=3OC(=NN=3)C=3C=CC(Cl)=CC=3)C=C2N1 SSCBDEUAEZBUIJ-UHFFFAOYSA-N 0.000 claims description 3
- DZTVXQZHWYUNLE-UHFFFAOYSA-N 3-[4-[6-[5-(4-methoxyanilino)-1,3,4-oxadiazol-2-yl]-1h-benzimidazol-2-yl]-3,5-dimethylphenyl]propanoic acid Chemical compound C1=CC(OC)=CC=C1NC1=NN=C(C=2C=C3NC(=NC3=CC=2)C=2C(=CC(CCC(O)=O)=CC=2C)C)O1 DZTVXQZHWYUNLE-UHFFFAOYSA-N 0.000 claims description 3
- 125000006267 biphenyl group Chemical group 0.000 claims description 3
- 125000005392 carboxamide group Chemical group NC(=O)* 0.000 claims description 3
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims description 3
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 3
- BDHFUVZGWQCTTF-UHFFFAOYSA-N sulfonic acid Chemical group OS(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-N 0.000 claims description 3
- XSQUKJJJFZCRTK-UHFFFAOYSA-N urea group Chemical group NC(=O)N XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 3
- UBGWQKWLRPICHU-UHFFFAOYSA-N 2-[3,5-dichloro-4-[6-[5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl]-1h-benzimidazol-2-yl]phenoxy]acetic acid Chemical compound ClC1=CC(OCC(=O)O)=CC(Cl)=C1C1=NC2=CC=C(C=3OC(=NN=3)C=3C=CC(Cl)=CC=3)C=C2N1 UBGWQKWLRPICHU-UHFFFAOYSA-N 0.000 claims description 2
- TUBPDBIOKLNJTG-UHFFFAOYSA-N 3-[4-[6-(5-methoxy-1,3,4-oxadiazol-2-yl)-1h-indol-2-yl]-3,5-dimethylphenyl]propanoic acid Chemical compound O1C(OC)=NN=C1C1=CC=C(C=C(N2)C=3C(=CC(CCC(O)=O)=CC=3C)C)C2=C1 TUBPDBIOKLNJTG-UHFFFAOYSA-N 0.000 claims description 2
- GXALXAKNHIROPE-UHFFFAOYSA-N 2-[4-[4-[5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl]phenyl]cyclohexyl]acetic acid Chemical group C1CC(CC(=O)O)CCC1C1=CC=C(C=2N=CC(NC=3C=NC(=CC=3)C(F)(F)F)=CC=2)C=C1 GXALXAKNHIROPE-UHFFFAOYSA-N 0.000 claims 2
- YPGCWEMNNLXISK-UHFFFAOYSA-N hydratropic acid Chemical compound OC(=O)C(C)C1=CC=CC=C1 YPGCWEMNNLXISK-UHFFFAOYSA-N 0.000 claims 1
- 239000000203 mixture Substances 0.000 description 37
- 229940125904 compound 1 Drugs 0.000 description 22
- 239000003814 drug Substances 0.000 description 20
- 229940079593 drug Drugs 0.000 description 16
- 125000003545 alkoxy group Chemical group 0.000 description 14
- 208000006575 hypertriglyceridemia Diseases 0.000 description 13
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 12
- 239000008280 blood Substances 0.000 description 12
- 210000004369 blood Anatomy 0.000 description 12
- 238000012360 testing method Methods 0.000 description 12
- 239000003981 vehicle Substances 0.000 description 11
- 108010004103 Chylomicrons Proteins 0.000 description 10
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 10
- 239000004480 active ingredient Substances 0.000 description 9
- 239000001257 hydrogen Substances 0.000 description 9
- 229910052739 hydrogen Inorganic materials 0.000 description 9
- 241001465754 Metazoa Species 0.000 description 8
- 125000002252 acyl group Chemical group 0.000 description 8
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 description 8
- 150000001721 carbon Chemical group 0.000 description 8
- 230000000694 effects Effects 0.000 description 8
- 229940028435 intralipid Drugs 0.000 description 8
- 239000000546 pharmaceutical excipient Substances 0.000 description 8
- 125000001424 substituent group Chemical group 0.000 description 8
- 229940124530 sulfonamide Drugs 0.000 description 8
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 8
- 241000700159 Rattus Species 0.000 description 7
- 125000003710 aryl alkyl group Chemical group 0.000 description 7
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 description 7
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 7
- 229910052736 halogen Inorganic materials 0.000 description 7
- 125000005843 halogen group Chemical group 0.000 description 7
- 150000002367 halogens Chemical class 0.000 description 7
- 235000012054 meals Nutrition 0.000 description 7
- AHLBNYSZXLDEJQ-FWEHEUNISA-N orlistat Chemical compound CCCCCCCCCCC[C@H](OC(=O)[C@H](CC(C)C)NC=O)C[C@@H]1OC(=O)[C@H]1CCCCCC AHLBNYSZXLDEJQ-FWEHEUNISA-N 0.000 description 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 7
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 6
- 208000008589 Obesity Diseases 0.000 description 6
- 125000003282 alkyl amino group Chemical group 0.000 description 6
- 235000020824 obesity Nutrition 0.000 description 6
- 229960001243 orlistat Drugs 0.000 description 6
- 150000003456 sulfonamides Chemical class 0.000 description 6
- 208000001021 Hyperlipoproteinemia Type I Diseases 0.000 description 5
- 108010013563 Lipoprotein Lipase Proteins 0.000 description 5
- 102000043296 Lipoprotein lipases Human genes 0.000 description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 5
- 239000002253 acid Substances 0.000 description 5
- 125000004414 alkyl thio group Chemical group 0.000 description 5
- 239000001913 cellulose Substances 0.000 description 5
- 229920002678 cellulose Polymers 0.000 description 5
- 229960000913 crospovidone Drugs 0.000 description 5
- 125000004663 dialkyl amino group Chemical group 0.000 description 5
- 239000007884 disintegrant Substances 0.000 description 5
- 208000035475 disorder Diseases 0.000 description 5
- 150000002430 hydrocarbons Chemical group 0.000 description 5
- 235000015263 low fat diet Nutrition 0.000 description 5
- 235000019359 magnesium stearate Nutrition 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 229910052760 oxygen Inorganic materials 0.000 description 5
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 5
- 229920000053 polysorbate 80 Polymers 0.000 description 5
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 5
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- 230000004044 response Effects 0.000 description 5
- 239000000725 suspension Substances 0.000 description 5
- 238000002560 therapeutic procedure Methods 0.000 description 5
- MDYZKJNTKZIUSK-UHFFFAOYSA-N tyloxapol Chemical compound O=C.C1CO1.CC(C)(C)CC(C)(C)C1=CC=C(O)C=C1 MDYZKJNTKZIUSK-UHFFFAOYSA-N 0.000 description 5
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical class OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 4
- 125000004423 acyloxy group Chemical group 0.000 description 4
- 125000005236 alkanoylamino group Chemical group 0.000 description 4
- 125000005110 aryl thio group Chemical group 0.000 description 4
- 125000002619 bicyclic group Chemical group 0.000 description 4
- 239000011230 binding agent Substances 0.000 description 4
- 239000004067 bulking agent Substances 0.000 description 4
- 239000002775 capsule Substances 0.000 description 4
- 125000001589 carboacyl group Chemical group 0.000 description 4
- 230000007812 deficiency Effects 0.000 description 4
- 206010012601 diabetes mellitus Diseases 0.000 description 4
- 235000019197 fats Nutrition 0.000 description 4
- 239000008187 granular material Substances 0.000 description 4
- 239000000314 lubricant Substances 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 229920000609 methyl cellulose Polymers 0.000 description 4
- 239000001923 methylcellulose Substances 0.000 description 4
- UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 description 4
- 108090000623 proteins and genes Proteins 0.000 description 4
- 238000012216 screening Methods 0.000 description 4
- ZSJLQEPLLKMAKR-GKHCUFPYSA-N streptozocin Chemical compound O=NN(C)C(=O)N[C@H]1[C@@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O ZSJLQEPLLKMAKR-GKHCUFPYSA-N 0.000 description 4
- 125000000547 substituted alkyl group Chemical group 0.000 description 4
- 125000003396 thiol group Chemical class [H]S* 0.000 description 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 4
- 108010001348 Diacylglycerol O-acyltransferase Proteins 0.000 description 3
- 102100036869 Diacylglycerol O-acyltransferase 1 Human genes 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 208000035150 Hypercholesterolemia Diseases 0.000 description 3
- 208000031226 Hyperlipidaemia Diseases 0.000 description 3
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
- 125000004442 acylamino group Chemical group 0.000 description 3
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 3
- 125000003435 aroyl group Chemical group 0.000 description 3
- 125000005333 aroyloxy group Chemical group 0.000 description 3
- 125000004391 aryl sulfonyl group Chemical group 0.000 description 3
- 125000004104 aryloxy group Chemical group 0.000 description 3
- 239000011203 carbon fibre reinforced carbon Substances 0.000 description 3
- 230000008859 change Effects 0.000 description 3
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 3
- 239000003086 colorant Substances 0.000 description 3
- 125000004093 cyano group Chemical group *C#N 0.000 description 3
- 235000005911 diet Nutrition 0.000 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 235000003599 food sweetener Nutrition 0.000 description 3
- 125000004475 heteroaralkyl group Chemical group 0.000 description 3
- 235000009200 high fat diet Nutrition 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 239000003112 inhibitor Substances 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 3
- 239000000651 prodrug Substances 0.000 description 3
- 229940002612 prodrug Drugs 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 229910052717 sulfur Inorganic materials 0.000 description 3
- 239000003765 sweetening agent Substances 0.000 description 3
- 125000001984 thiazolidinyl group Chemical group 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 208000004998 Abdominal Pain Diseases 0.000 description 2
- 229920002261 Corn starch Polymers 0.000 description 2
- 102000002148 Diacylglycerol O-acyltransferase Human genes 0.000 description 2
- 108050004099 Diacylglycerol O-acyltransferase 1 Proteins 0.000 description 2
- 206010014486 Elevated triglycerides Diseases 0.000 description 2
- 102100026256 Glycosylphosphatidylinositol-anchored high density lipoprotein-binding protein 1 Human genes 0.000 description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 description 2
- 108090001030 Lipoproteins Proteins 0.000 description 2
- 102000004895 Lipoproteins Human genes 0.000 description 2
- ZSJLQEPLLKMAKR-UHFFFAOYSA-N Streptozotocin Natural products O=NN(C)C(=O)NC1C(O)OC(CO)C(O)C1O ZSJLQEPLLKMAKR-UHFFFAOYSA-N 0.000 description 2
- 206010060749 Type I hyperlipidaemia Diseases 0.000 description 2
- 108010062497 VLDL Lipoproteins Proteins 0.000 description 2
- 238000009825 accumulation Methods 0.000 description 2
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 125000005239 aroylamino group Chemical group 0.000 description 2
- 125000004659 aryl alkyl thio group Chemical group 0.000 description 2
- 125000004618 benzofuryl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 description 2
- 125000004619 benzopyranyl group Chemical group O1C(C=CC2=C1C=CC=C2)* 0.000 description 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 description 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 description 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 2
- 210000004204 blood vessel Anatomy 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 235000021152 breakfast Nutrition 0.000 description 2
- 150000003857 carboxamides Chemical class 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- GXALXAKNHIROPE-QAQDUYKDSA-N chembl2364624 Chemical group C1C[C@@H](CC(=O)O)CC[C@@H]1C1=CC=C(C=2N=CC(NC=3C=NC(=CC=3)C(F)(F)F)=CC=2)C=C1 GXALXAKNHIROPE-QAQDUYKDSA-N 0.000 description 2
- 239000008120 corn starch Substances 0.000 description 2
- 125000004122 cyclic group Chemical group 0.000 description 2
- 230000000378 dietary effect Effects 0.000 description 2
- 235000013367 dietary fats Nutrition 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 description 2
- 238000001647 drug administration Methods 0.000 description 2
- 201000011110 familial lipoprotein lipase deficiency Diseases 0.000 description 2
- 229940125753 fibrate Drugs 0.000 description 2
- 125000002541 furyl group Chemical group 0.000 description 2
- 230000002068 genetic effect Effects 0.000 description 2
- 125000005143 heteroarylsulfonyl group Chemical group 0.000 description 2
- 125000004470 heterocyclooxy group Chemical group 0.000 description 2
- 125000002883 imidazolyl group Chemical group 0.000 description 2
- 125000001041 indolyl group Chemical group 0.000 description 2
- 230000003993 interaction Effects 0.000 description 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 description 2
- 125000000842 isoxazolyl group Chemical group 0.000 description 2
- 150000002632 lipids Chemical class 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 229960003512 nicotinic acid Drugs 0.000 description 2
- 235000001968 nicotinic acid Nutrition 0.000 description 2
- 239000011664 nicotinic acid Substances 0.000 description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 2
- 235000020660 omega-3 fatty acid Nutrition 0.000 description 2
- 229940012843 omega-3 fatty acid Drugs 0.000 description 2
- 239000006014 omega-3 oil Substances 0.000 description 2
- 238000001543 one-way ANOVA Methods 0.000 description 2
- 238000003305 oral gavage Methods 0.000 description 2
- 125000002971 oxazolyl group Chemical group 0.000 description 2
- 125000004043 oxo group Chemical group O=* 0.000 description 2
- 239000001301 oxygen Chemical group 0.000 description 2
- 230000003285 pharmacodynamic effect Effects 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 230000000069 prophylactic effect Effects 0.000 description 2
- 125000003373 pyrazinyl group Chemical group 0.000 description 2
- 125000003226 pyrazolyl group Chemical group 0.000 description 2
- 125000002098 pyridazinyl group Chemical group 0.000 description 2
- 125000004076 pyridyl group Chemical group 0.000 description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 description 2
- 125000000168 pyrrolyl group Chemical group 0.000 description 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 2
- 238000007619 statistical method Methods 0.000 description 2
- 229960001052 streptozocin Drugs 0.000 description 2
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 2
- 238000002411 thermogravimetry Methods 0.000 description 2
- 125000000335 thiazolyl group Chemical group 0.000 description 2
- 125000001544 thienyl group Chemical group 0.000 description 2
- 125000001425 triazolyl group Chemical group 0.000 description 2
- 238000007492 two-way ANOVA Methods 0.000 description 2
- 150000003672 ureas Chemical class 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- DTGKSKDOIYIVQL-WEDXCCLWSA-N (+)-borneol Chemical group C1C[C@@]2(C)[C@@H](O)C[C@@H]1C2(C)C DTGKSKDOIYIVQL-WEDXCCLWSA-N 0.000 description 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 1
- 125000006088 2-oxoazepinyl group Chemical group 0.000 description 1
- 125000004638 2-oxopiperazinyl group Chemical group O=C1N(CCNC1)* 0.000 description 1
- 125000004637 2-oxopiperidinyl group Chemical group O=C1N(CCCC1)* 0.000 description 1
- 125000004610 3,4-dihydro-4-oxo-quinazolinyl group Chemical group O=C1NC(=NC2=CC=CC=C12)* 0.000 description 1
- 125000005986 4-piperidonyl group Chemical group 0.000 description 1
- HXFLZWAZSSPLCO-UHFFFAOYSA-N 6,6-dimethylbicyclo[3.1.1]heptyl Chemical group C1[C-]2C([CH2+])([CH2-])[C+]1CCC2 HXFLZWAZSSPLCO-UHFFFAOYSA-N 0.000 description 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 1
- 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 1
- 108010024284 Apolipoprotein C-II Proteins 0.000 description 1
- 108010011485 Aspartame Proteins 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical class OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 description 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 1
- QYOVMAREBTZLBT-KTKRTIGZSA-N CCCCCCCC\C=C/CCCCCCCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO Chemical compound CCCCCCCC\C=C/CCCCCCCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO QYOVMAREBTZLBT-KTKRTIGZSA-N 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 102000014914 Carrier Proteins Human genes 0.000 description 1
- 108010078791 Carrier Proteins Proteins 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 description 1
- 108010036949 Cyclosporine Proteins 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- 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 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 101100055841 Danio rerio apoa1 gene Proteins 0.000 description 1
- 241000702421 Dependoparvovirus Species 0.000 description 1
- 208000034599 Dysbetalipoproteinemia Diseases 0.000 description 1
- 208000032928 Dyslipidaemia Diseases 0.000 description 1
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 description 1
- 206010014476 Elevated cholesterol Diseases 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 206010059183 Familial hypertriglyceridaemia Diseases 0.000 description 1
- 102000030914 Fatty Acid-Binding Human genes 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- 101710161659 Glycosylphosphatidylinositol-anchored high density lipoprotein-binding protein 1 Proteins 0.000 description 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 1
- 101000927974 Homo sapiens Diacylglycerol O-acyltransferase 1 Proteins 0.000 description 1
- 101001003882 Homo sapiens Glycosylphosphatidylinositol-anchored high density lipoprotein-binding protein 1 Proteins 0.000 description 1
- 101000619884 Homo sapiens Lipoprotein lipase Proteins 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 206010020606 Hyperchylomicronaemia Diseases 0.000 description 1
- 201000010252 Hyperlipoproteinemia Type III Diseases 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 206010062016 Immunosuppression Diseases 0.000 description 1
- 206010022489 Insulin Resistance Diseases 0.000 description 1
- 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 1
- 206010049287 Lipodystrophy acquired Diseases 0.000 description 1
- 102100030817 Liver carboxylesterase 1 Human genes 0.000 description 1
- 101710181187 Liver carboxylesterase 1 Proteins 0.000 description 1
- 239000005913 Maltodextrin Substances 0.000 description 1
- 229920002774 Maltodextrin Polymers 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- HSHXDCVZWHOWCS-UHFFFAOYSA-N N'-hexadecylthiophene-2-carbohydrazide Chemical compound CCCCCCCCCCCCCCCCNNC(=O)c1cccs1 HSHXDCVZWHOWCS-UHFFFAOYSA-N 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 238000000692 Student's t-test Methods 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 1
- 206010060751 Type III hyperlipidaemia Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 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 1
- 150000007513 acids Chemical class 0.000 description 1
- 125000000641 acridinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3C=C12)* 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 description 1
- UCTWMZQNUQWSLP-UHFFFAOYSA-N adrenaline Chemical compound CNCC(O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-UHFFFAOYSA-N 0.000 description 1
- 229950006993 alipogene tiparvovec Drugs 0.000 description 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 1
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 description 1
- 238000000540 analysis of variance Methods 0.000 description 1
- 239000000883 anti-obesity agent Substances 0.000 description 1
- 239000003472 antidiabetic agent Substances 0.000 description 1
- 229940125708 antidiabetic agent Drugs 0.000 description 1
- 239000002220 antihypertensive agent Substances 0.000 description 1
- 229940030600 antihypertensive agent Drugs 0.000 description 1
- 239000003524 antilipemic agent Substances 0.000 description 1
- 229940125710 antiobesity agent Drugs 0.000 description 1
- 239000012736 aqueous medium Substances 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 125000005140 aralkylsulfonyl group Chemical group 0.000 description 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 description 1
- 125000002029 aromatic hydrocarbon group Chemical group 0.000 description 1
- 239000000605 aspartame Substances 0.000 description 1
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 1
- 235000010357 aspartame Nutrition 0.000 description 1
- 229960003438 aspartame Drugs 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 125000002785 azepinyl group Chemical group 0.000 description 1
- 125000005870 benzindolyl group Chemical group 0.000 description 1
- 125000004622 benzoxazinyl group Chemical group O1NC(=CC2=C1C=CC=C2)* 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 239000002876 beta blocker Substances 0.000 description 1
- 229940097320 beta blocking agent Drugs 0.000 description 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000004305 biphenyl Substances 0.000 description 1
- 235000010290 biphenyl Nutrition 0.000 description 1
- 238000010241 blood sampling Methods 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- 229910000389 calcium phosphate Inorganic materials 0.000 description 1
- 235000011010 calcium phosphates Nutrition 0.000 description 1
- 238000004364 calculation method Methods 0.000 description 1
- 235000013877 carbamide Nutrition 0.000 description 1
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 description 1
- 230000023852 carbohydrate metabolic process Effects 0.000 description 1
- 235000021256 carbohydrate metabolism Nutrition 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 235000014633 carbohydrates Nutrition 0.000 description 1
- 125000004623 carbolinyl group Chemical group 0.000 description 1
- 150000004649 carbonic acid derivatives Chemical class 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 239000000460 chlorine Substances 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 125000004617 chromonyl group Chemical group O1C(=CC(C2=CC=CC=C12)=O)* 0.000 description 1
- 229960001265 ciclosporin Drugs 0.000 description 1
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 description 1
- 230000003081 coactivator Effects 0.000 description 1
- 238000002648 combination therapy Methods 0.000 description 1
- 229940125773 compound 10 Drugs 0.000 description 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
- 229930182912 cyclosporin Natural products 0.000 description 1
- 125000004652 decahydroisoquinolinyl group Chemical group C1(NCCC2CCCCC12)* 0.000 description 1
- 125000004856 decahydroquinolinyl group Chemical group N1(CCCC2CCCCC12)* 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 238000000280 densification Methods 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 125000004611 dihydroisoindolyl group Chemical group C1(NCC2=CC=CC=C12)* 0.000 description 1
- 125000004609 dihydroquinazolinyl group Chemical group N1(CN=CC2=CC=CC=C12)* 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 239000000262 estrogen Substances 0.000 description 1
- 229940011871 estrogen Drugs 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 108091022862 fatty acid binding Proteins 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 1
- 125000004615 furo[2,3-b]pyridinyl group Chemical group O1C(=CC=2C1=NC=CC2)* 0.000 description 1
- 125000004613 furo[2,3-c]pyridinyl group Chemical group O1C(=CC=2C1=CN=CC2)* 0.000 description 1
- 125000006086 furo[3,2-b]pyridinyl] group Chemical group 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 239000003862 glucocorticoid Substances 0.000 description 1
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 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 1
- 125000005226 heteroaryloxycarbonyl group Chemical group 0.000 description 1
- 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 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 208000020346 hyperlipoproteinemia Diseases 0.000 description 1
- 208000000522 hyperlipoproteinemia type IV Diseases 0.000 description 1
- 208000003532 hypothyroidism Diseases 0.000 description 1
- 230000002989 hypothyroidism Effects 0.000 description 1
- 125000002632 imidazolidinyl group Chemical group 0.000 description 1
- 125000002636 imidazolinyl group Chemical group 0.000 description 1
- 230000001506 immunosuppresive effect Effects 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 description 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 description 1
- 230000000977 initiatory effect Effects 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000004491 isohexyl group Chemical group C(CCC(C)C)* 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 125000004628 isothiazolidinyl group Chemical group S1N(CCC1)* 0.000 description 1
- 125000001786 isothiazolyl group Chemical group 0.000 description 1
- 125000003971 isoxazolinyl group Chemical group 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 208000006132 lipodystrophy Diseases 0.000 description 1
- 235000020888 liquid diet Nutrition 0.000 description 1
- 229940035034 maltodextrin Drugs 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000002483 medication Methods 0.000 description 1
- 239000002609 medium Substances 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- HPNSFSBZBAHARI-UHFFFAOYSA-N micophenolic acid Natural products OC1=C(CC=C(C)CCC(O)=O)C(OC)=C(C)C2=C1C(=O)OC2 HPNSFSBZBAHARI-UHFFFAOYSA-N 0.000 description 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 description 1
- 125000002757 morpholinyl group Chemical group 0.000 description 1
- 229940014456 mycophenolate Drugs 0.000 description 1
- HPNSFSBZBAHARI-RUDMXATFSA-N mycophenolic acid Chemical compound OC1=C(C\C=C(/C)CCC(O)=O)C(OC)=C(C)C2=C1C(=O)OC2 HPNSFSBZBAHARI-RUDMXATFSA-N 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 230000007106 neurocognition Effects 0.000 description 1
- 230000007107 neurocognitive deficit Effects 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 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
- 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 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 150000004866 oxadiazoles Chemical class 0.000 description 1
- 125000001715 oxadiazolyl group Chemical group 0.000 description 1
- 125000000160 oxazolidinyl group Chemical group 0.000 description 1
- 125000003566 oxetanyl group Chemical group 0.000 description 1
- 125000005476 oxopyrrolidinyl group Chemical group 0.000 description 1
- 230000036961 partial effect Effects 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 210000002824 peroxisome Anatomy 0.000 description 1
- 239000002831 pharmacologic agent Substances 0.000 description 1
- 238000001050 pharmacotherapy Methods 0.000 description 1
- 125000004934 phenanthridinyl group Chemical group C1(=CC=CC2=NC=C3C=CC=CC3=C12)* 0.000 description 1
- 125000004625 phenanthrolinyl group Chemical group N1=C(C=CC2=CC=C3C=CC=NC3=C12)* 0.000 description 1
- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 description 1
- 125000001644 phenoxazinyl group Chemical group C1(=CC=CC=2OC3=CC=CC=C3NC12)* 0.000 description 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 102000054765 polymorphisms of proteins Human genes 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 229940068984 polyvinyl alcohol Drugs 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 238000010149 post-hoc-test Methods 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000002755 pyrazolinyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- NISJKLIMPQPAQS-UHFFFAOYSA-N pyrrolo[1,2-b]pyridazine Chemical class C1=CC=NN2C=CC=C21 NISJKLIMPQPAQS-UHFFFAOYSA-N 0.000 description 1
- 125000006085 pyrrolopyridyl group Chemical group 0.000 description 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 1
- 125000004621 quinuclidinyl group Chemical group N12C(CC(CC1)CC2)* 0.000 description 1
- 239000000018 receptor agonist Substances 0.000 description 1
- 229940044601 receptor agonist Drugs 0.000 description 1
- 230000002207 retinal effect Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 238000009490 roller compaction Methods 0.000 description 1
- 125000000467 secondary amino group Chemical group [H]N([*:1])[*:2] 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000008109 sodium starch glycolate Substances 0.000 description 1
- 229940079832 sodium starch glycolate Drugs 0.000 description 1
- 229920003109 sodium starch glycolate Polymers 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000013222 sprague-dawley male rat Methods 0.000 description 1
- 238000012453 sprague-dawley rat model Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000005846 sugar alcohols Chemical class 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L sulfate group Chemical group S(=O)(=O)([O-])[O-] QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 229940037128 systemic glucocorticoids Drugs 0.000 description 1
- 238000012353 t test Methods 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000004797 therapeutic response Effects 0.000 description 1
- 125000006090 thiamorpholinyl sulfone group Chemical group 0.000 description 1
- 239000003451 thiazide diuretic agent Substances 0.000 description 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 1
- 230000036962 time dependent Effects 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
- GPRLSGONYQIRFK-MNYXATJNSA-N triton Chemical compound [3H+] GPRLSGONYQIRFK-MNYXATJNSA-N 0.000 description 1
- 238000005199 ultracentrifugation Methods 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 235000019195 vitamin supplement Nutrition 0.000 description 1
- 125000001834 xanthenyl group Chemical group C1=CC=CC=2OC3=CC=CC=C3C(C12)* 0.000 description 1
- OENHQHLEOONYIE-JLTXGRSLSA-N β-Carotene Chemical compound CC=1CCCC(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C OENHQHLEOONYIE-JLTXGRSLSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31881410P | 2010-03-30 | 2010-03-30 | |
| US61/318,814 | 2010-03-30 | ||
| PCT/US2011/030234 WO2011123401A1 (en) | 2010-03-30 | 2011-03-29 | Uses of dgat1 inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016114803A Division JP6251321B2 (ja) | 2010-03-30 | 2016-06-08 | Ｄｇａｔ１阻害剤の使用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013523746A true JP2013523746A (ja) | 2013-06-17 |
| JP2013523746A5 JP2013523746A5 (https=) | 2014-05-15 |
Family
ID=44170024
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013502706A Withdrawn JP2013523746A (ja) | 2010-03-30 | 2011-03-29 | Ｄｇａｔ１阻害剤の使用 |
| JP2016114803A Active JP6251321B2 (ja) | 2010-03-30 | 2016-06-08 | Ｄｇａｔ１阻害剤の使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016114803A Active JP6251321B2 (ja) | 2010-03-30 | 2016-06-08 | Ｄｇａｔ１阻害剤の使用 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US9061012B2 (https=) |
| EP (1) | EP2552441B1 (https=) |
| JP (2) | JP2013523746A (https=) |
| KR (1) | KR20130073884A (https=) |
| CN (1) | CN102834099B (https=) |
| AU (1) | AU2011235301B2 (https=) |
| BR (1) | BR112012024618A2 (https=) |
| CA (1) | CA2792269A1 (https=) |
| CL (1) | CL2012002716A1 (https=) |
| ES (1) | ES2586127T3 (https=) |
| MA (1) | MA34097B1 (https=) |
| MX (1) | MX2012011333A (https=) |
| NZ (1) | NZ602125A (https=) |
| PH (1) | PH12012501859A1 (https=) |
| RU (1) | RU2012145950A (https=) |
| SG (1) | SG183529A1 (https=) |
| TN (1) | TN2012000458A1 (https=) |
| TW (1) | TW201136916A (https=) |
| WO (1) | WO2011123401A1 (https=) |
| ZA (1) | ZA201206456B (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021001143A (ja) * | 2019-06-21 | 2021-01-07 | 小林製薬株式会社 | 乳び血漿改善剤 |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR083417A1 (es) | 2010-10-14 | 2013-02-21 | Novartis Ag | Composiciones farmaceuticas que contienen un dgat1 inhibidor |
| BR112014026910A8 (pt) * | 2012-04-25 | 2018-01-09 | Handok Pharmaceuticals Co Ltd | novo derivado de beta-alanina, seus sais farmaceuticamente aceitáveis, e composições farmacêuticas compreendendo o mesmo como ingrediente ativo. |
| WO2013169648A1 (en) | 2012-05-07 | 2013-11-14 | Novartis Ag | Pharmaceutical combinations comprising a dgat1 inhibtor and a triglyceride lowering drug |
| AU2014216137B2 (en) | 2013-02-14 | 2018-05-10 | Ionis Pharmaceuticals, Inc. | Modulation of Apolipoprotein C-III (ApoCIII) expression in lipoprotein lipase deficient (LPLD) populations |
| DK2991656T3 (da) | 2013-05-01 | 2020-03-23 | Ionis Pharmaceuticals Inc | Sammensætninger og fremgangsmåder til modulering af apolipoprotein c-iii-ekspression |
| PT3119384T (pt) | 2014-03-20 | 2018-12-12 | Cymabay Therapeutics Inc | Tratamento de doenças colestáticas intra-hepáticas |
| US10272058B2 (en) | 2014-03-20 | 2019-04-30 | Cymabay Therapeutics, Inc. | Treatment of intrahepatic cholestatic diseases |
| EA201790091A1 (ru) * | 2014-06-26 | 2017-07-31 | Саймабэй Терапьютикс, Инк. | Лечение тяжелой гипертриглицеридемии |
| WO2016181409A1 (en) | 2015-05-11 | 2016-11-17 | Cadila Healthcare Limited | Saroglitazar magnesium for the treatment of chylomicronemia syndrome - |
| WO2017064635A2 (en) | 2015-10-14 | 2017-04-20 | Cadila Healthcare Limited | Pyrrole compound, compositions and process for preparation thereof |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| TWI707849B (zh) | 2018-02-13 | 2020-10-21 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
| IL277332B2 (en) | 2018-03-16 | 2025-01-01 | Anji Pharmaceuticals Inc | Preparations and methods for treating severe constipation |
| KR102591947B1 (ko) | 2018-04-19 | 2023-10-25 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| EP3820572B1 (en) | 2018-07-13 | 2023-08-16 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| US11236085B2 (en) | 2018-10-24 | 2022-02-01 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
| CN113365643A (zh) * | 2018-11-30 | 2021-09-07 | Hdl治疗公司 | 用于治疗包括黄色瘤、颈动脉狭窄和脑动脉粥样硬化的脂质相关疾病的方法 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006166742A (ja) * | 2004-12-14 | 2006-06-29 | Japan Health Science Foundation | 高トリグリセリド血症の成因となる２種類のリポタンパクリパーゼ（ｌｐｌ）遺伝子変異及びそれを利用した高トリグリセリド血症を診断するためのｌｐｌ変異検出キット |
| WO2009040410A1 (en) * | 2007-09-28 | 2009-04-02 | Novartis Ag | Oxadiazole- and oxazole-substituted benzimidazole- and indole-derivatives as dgat1 inhibitors |
| JP2009514780A (ja) * | 2003-07-10 | 2009-04-09 | “エス．ウー．カー．”ベタイリグングス・ゲーエムベーハー | メタボリックシンドロームの処置のためのホエーパーミエートの使用 |
| JP2009532355A (ja) * | 2006-03-31 | 2009-09-10 | ノバルティス アクチエンゲゼルシャフト | 新規化合物 |
| WO2009119534A1 (ja) * | 2008-03-26 | 2009-10-01 | 第一三共株式会社 | 新規テトラヒドロイソキノリン誘導体 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU3225997A (en) | 1996-05-30 | 1998-01-05 | Trustees Of Columbia University In The City Of New York, The | Dna encoding acylcoenzyme a: cholesterol acyltransferase and uses thereof |
| US6344548B1 (en) | 1998-06-24 | 2002-02-05 | The Regents Of The University Of California | Diacylglycerol o-acyltransferase |
| US20030167483A1 (en) | 1998-06-24 | 2003-09-04 | Farese Robert V. | Diacylglycerol O-acyltransferase |
| US20030154504A1 (en) | 1998-06-24 | 2003-08-14 | Farese Robert V. | Methods and compositions for modulating carbohydrate metabolism |
| WO1999067268A1 (en) | 1998-06-24 | 1999-12-29 | The Regents Of The University Of California | Diacylglycerol o-acyltransferase |
| US6100077A (en) | 1998-10-01 | 2000-08-08 | The Trustees Of Columbia University In The City Of New York | Isolation of a gene encoding diacylglycerol acyltransferase |
| US6444427B1 (en) | 2000-07-11 | 2002-09-03 | The Regents Of The University Of California | Polymorphisms in a diacylglycerol acyltransferase gene, and methods of use thereof |
| JP4164645B2 (ja) | 2002-08-09 | 2008-10-15 | 株式会社大塚製薬工場 | Ｄｇａｔ阻害剤 |
| KR100772297B1 (ko) | 2002-11-22 | 2007-11-02 | 니뽄 다바코 산교 가부시키가이샤 | 융합 비시클릭 질소-함유 헤테로사이클 |
| US20040185559A1 (en) | 2003-03-21 | 2004-09-23 | Isis Pharmaceuticals Inc. | Modulation of diacylglycerol acyltransferase 1 expression |
| AR044152A1 (es) | 2003-05-09 | 2005-08-24 | Bayer Corp | Derivados de alquilarilo, metodo de preparacion y uso para el tratamiento de la obesidad |
| EP1653969A4 (en) | 2003-08-07 | 2006-12-20 | Japan Tobacco Inc | PYRROLO 1,2-B PYRIDAZINE DERIVATIVES |
| GB0325192D0 (en) | 2003-10-29 | 2003-12-03 | Astrazeneca Ab | Method of use |
| JP2005206492A (ja) | 2004-01-21 | 2005-08-04 | Sankyo Co Ltd | スルホンアミド化合物 |
| EP1718309A2 (en) | 2004-01-30 | 2006-11-08 | Japan Tobacco, Inc. | Anorectic compounds |
| WO2006004200A1 (ja) | 2004-07-02 | 2006-01-12 | Sankyo Company, Limited | ウレア誘導体 |
| JP2006045209A (ja) | 2004-07-02 | 2006-02-16 | Sankyo Co Ltd | ウレア誘導体 |
| WO2006019020A1 (ja) | 2004-08-16 | 2006-02-23 | Sankyo Company, Limited | 置換されたウレア化合物 |
| JP2008516978A (ja) | 2004-10-15 | 2008-05-22 | バイエル・フアーマシユーチカルズ・コーポレーシヨン | 肥満症の処置のためのビフェニル−４−イル−カルボニルアミノ酸誘導体の製造および使用 |
| US7795283B2 (en) | 2004-12-14 | 2010-09-14 | Astrazeneca Ab | Oxadiazole derivative as DGAT inhibitors |
-
2011
- 2011-03-29 MA MA35264A patent/MA34097B1/fr unknown
- 2011-03-29 TW TW100110831A patent/TW201136916A/zh unknown
- 2011-03-29 EP EP11715329.6A patent/EP2552441B1/en active Active
- 2011-03-29 WO PCT/US2011/030234 patent/WO2011123401A1/en not_active Ceased
- 2011-03-29 AU AU2011235301A patent/AU2011235301B2/en not_active Ceased
- 2011-03-29 MX MX2012011333A patent/MX2012011333A/es active IP Right Grant
- 2011-03-29 CA CA2792269A patent/CA2792269A1/en not_active Abandoned
- 2011-03-29 CN CN201180016229.9A patent/CN102834099B/zh not_active Expired - Fee Related
- 2011-03-29 ES ES11715329.6T patent/ES2586127T3/es active Active
- 2011-03-29 SG SG2012063848A patent/SG183529A1/en unknown
- 2011-03-29 BR BR112012024618A patent/BR112012024618A2/pt not_active IP Right Cessation
- 2011-03-29 PH PH1/2012/501859A patent/PH12012501859A1/en unknown
- 2011-03-29 JP JP2013502706A patent/JP2013523746A/ja not_active Withdrawn
- 2011-03-29 RU RU2012145950/15A patent/RU2012145950A/ru not_active Application Discontinuation
- 2011-03-29 US US13/637,372 patent/US9061012B2/en active Active
- 2011-03-29 KR KR1020127028214A patent/KR20130073884A/ko not_active Withdrawn
- 2011-03-29 NZ NZ602125A patent/NZ602125A/en not_active IP Right Cessation
-
2012
- 2012-08-28 ZA ZA2012/06456A patent/ZA201206456B/en unknown
- 2012-09-24 TN TNP2012000458A patent/TN2012000458A1/en unknown
- 2012-09-28 CL CL2012002716A patent/CL2012002716A1/es unknown
-
2016
- 2016-06-08 JP JP2016114803A patent/JP6251321B2/ja active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009514780A (ja) * | 2003-07-10 | 2009-04-09 | “エス．ウー．カー．”ベタイリグングス・ゲーエムベーハー | メタボリックシンドロームの処置のためのホエーパーミエートの使用 |
| JP2006166742A (ja) * | 2004-12-14 | 2006-06-29 | Japan Health Science Foundation | 高トリグリセリド血症の成因となる２種類のリポタンパクリパーゼ（ｌｐｌ）遺伝子変異及びそれを利用した高トリグリセリド血症を診断するためのｌｐｌ変異検出キット |
| JP2009532355A (ja) * | 2006-03-31 | 2009-09-10 | ノバルティス アクチエンゲゼルシャフト | 新規化合物 |
| WO2009040410A1 (en) * | 2007-09-28 | 2009-04-02 | Novartis Ag | Oxadiazole- and oxazole-substituted benzimidazole- and indole-derivatives as dgat1 inhibitors |
| WO2009119534A1 (ja) * | 2008-03-26 | 2009-10-01 | 第一三共株式会社 | 新規テトラヒドロイソキノリン誘導体 |
Non-Patent Citations (1)
| Title |
|---|
| JPN5013006252; ＺＨＡＯ: 'ＶＡＬＩＤＡＴＩＯＮ ＯＦ ＤＩＡＣＹＬ ＧＬＹＣＥＲＯＬＡＣＹＬＴＲＡＮＳＦＥＲＡＳＥ Ｉ ＡＳ Ａ ＮＯＶＥＬ ＴＡＲＧＥＴ ＦＯＲ ＴＨＥ ＴＲＥＡＴＭＥＮＴ 以下備考' ＪＯＵＲＮＡＬ ＭＥＤＩＣＡＬ ＣＨＥＭＩＳＴＲＹ Ｖ５１, 20080110, Ｐ３８０-３８３ * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021001143A (ja) * | 2019-06-21 | 2021-01-07 | 小林製薬株式会社 | 乳び血漿改善剤 |
Also Published As
| Publication number | Publication date |
|---|---|
| PH12012501859A1 (en) | 2013-01-07 |
| TN2012000458A1 (en) | 2014-01-30 |
| CN102834099B (zh) | 2015-05-27 |
| CN102834099A (zh) | 2012-12-19 |
| JP6251321B2 (ja) | 2017-12-20 |
| MX2012011333A (es) | 2012-11-16 |
| CA2792269A1 (en) | 2011-10-06 |
| CL2012002716A1 (es) | 2013-01-25 |
| JP2016216466A (ja) | 2016-12-22 |
| NZ602125A (en) | 2014-01-31 |
| ZA201206456B (en) | 2013-05-29 |
| ES2586127T3 (es) | 2016-10-11 |
| AU2011235301A1 (en) | 2012-10-11 |
| EP2552441A1 (en) | 2013-02-06 |
| SG183529A1 (en) | 2012-10-30 |
| US9061012B2 (en) | 2015-06-23 |
| EP2552441B1 (en) | 2016-05-04 |
| KR20130073884A (ko) | 2013-07-03 |
| TW201136916A (en) | 2011-11-01 |
| AU2011235301B2 (en) | 2013-07-18 |
| BR112012024618A2 (pt) | 2019-09-24 |
| WO2011123401A1 (en) | 2011-10-06 |
| MA34097B1 (fr) | 2013-03-05 |
| RU2012145950A (ru) | 2014-05-10 |
| US20130023495A1 (en) | 2013-01-24 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6251321B2 (ja) | Ｄｇａｔ１阻害剤の使用 | |
| ES2433476T3 (es) | Combinaciones que contienen inhibidores de la dipeptidilpeptidasa-IV y agentes 5 antidiabéticos | |
| EP0114886B1 (en) | Improved analgesic and anti-inflammatory compositions comprising caffeine | |
| AU569935B2 (en) | Analgesic & anti-inflammatory compositions containing xanthines | |
| KR20090038908A (ko) | 대사 장애의 조합 치료 | |
| JPH0733331B2 (ja) | ジフェンヒドラミン類を含んで成る鎮痛および抗炎症組成物 | |
| KR20080040643A (ko) | 의약의 병용 및 그 용도 | |
| JP2009526786A (ja) | 炎症性疾患の治療にｇａｂａａ作動性神経伝達を増強する化合物を使用する方法 | |
| JP2012255039A (ja) | ニコチン性アセチルコリンα７受容体アゴニストの組合せ剤 | |
| WO2013120438A1 (zh) | 治疗或缓解疼痛的物质 | |
| JP2016512817A (ja) | 高尿酸血症の治療におけるカナグリフロジンとプロベネシドの組合せ | |
| JP2002053493A (ja) | 全身性エリテマトーデスおよび炎症性腸疾患を治療するための成長ホルモン分泌促進物質の使用 | |
| US7081473B2 (en) | Agent for preventing/ameliorating obesity comprising methylidene hydrizide compound as active ingredient | |
| WO1984000488A1 (en) | Improved analgesic and anti-inflammatory compositions comprising caffeine and methods of using same | |
| TW200843741A (en) | Pharmaceutical composition | |
| Marino et al. | The Drug Update: Recent drug approvals | |
| JP2025160480A (ja) | 不眠症を治療するためのレンボレキサントの使用 | |
| CN117715641A (zh) | 用神经活性类固醇进行治疗的方法 | |
| US12023315B2 (en) | Pharmaceutical compositions and methods utilizing neostigmine and an NK-1 antagonist for treating myasthenia gravis | |
| RU2258506C2 (ru) | Лекарственные средства для предупреждения и лечения нейродегенеративных заболеваний | |
| CN1764457A (zh) | 用于治疗阿尔茨海默病的联合疗法 | |
| US20040102524A1 (en) | Method of treatment | |
| WO2007005763A2 (en) | Combination of a renin inhibitor and an insulin secretion enhancer or an insulin sensitizer | |
| US11752141B2 (en) | Pharmaceutical compositions and methods utilizing neostigmine and an NK-1 antagonist for treating myasthenia gravis | |
| IL292591A (en) | Treatment of diabetic nephropathy by sgc stimulator |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20140328 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20140328 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20150331 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20150630 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20150730 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20150831 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20150929 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20160209 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20160608 |
|
| A911 | Transfer to examiner for re-examination before appeal (zenchi) |
Free format text: JAPANESE INTERMEDIATE CODE: A911 Effective date: 20160616 |
|
| A761 | Written withdrawal of application |
Free format text: JAPANESE INTERMEDIATE CODE: A761 Effective date: 20160708 |
|
| A912 | Re-examination (zenchi) completed and case transferred to appeal board |
Free format text: JAPANESE INTERMEDIATE CODE: A912 Effective date: 20160708 |