JP2017515908A5 - - Google Patents

Info

Publication number

JP2017515908A5

JP2017515908A5 JP2017512456A JP2017512456A JP2017515908A5 JP 2017515908 A5 JP2017515908 A5 JP 2017515908A5 JP 2017512456 A JP2017512456 A JP 2017512456A JP 2017512456 A JP2017512456 A JP 2017512456A JP 2017515908 A5 JP2017515908 A5 JP 2017515908A5

Authority

JP

Japan

Prior art keywords

inhibitor

pharmaceutical composition

composition according

sglt2

dpp

Prior art date

2015-05-14

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.)

Pending

Links

• Espacenet
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• 239000003112 inhibitor Substances 0.000 claims 18
• 239000008194 pharmaceutical composition Substances 0.000 claims 17
• 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 13
• 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 8
• 241000124008 Mammalia Species 0.000 claims 7
• 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 5
• 150000002148 esters Chemical class 0.000 claims 5
• 229940002612 prodrug Drugs 0.000 claims 5
• 239000000651 prodrug Substances 0.000 claims 5
• 150000003839 salts Chemical class 0.000 claims 5
• 102000051325 Glucagon Human genes 0.000 claims 4
• 108060003199 Glucagon Proteins 0.000 claims 4
• 102100020888 Sodium/glucose cotransporter 2 Human genes 0.000 claims 4
• 101710103228 Sodium/glucose cotransporter 2 Proteins 0.000 claims 4
• 239000000556 agonist Substances 0.000 claims 4
• MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 4
• 229960004666 glucagon Drugs 0.000 claims 4
• 230000028327 secretion Effects 0.000 claims 4
• 239000003472 antidiabetic agent Substances 0.000 claims 3
• 229960004937 saxagliptin Drugs 0.000 claims 3
• QGJUIPDUBHWZPV-SGTAVMJGSA-N saxagliptin Chemical group C1C(C2)CC(C3)CC2(O)CC13[C@H](N)C(=O)N1[C@H](C#N)C[C@@H]2C[C@@H]21 QGJUIPDUBHWZPV-SGTAVMJGSA-N 0.000 claims 3
• 108010033693 saxagliptin Proteins 0.000 claims 3
• 229940123208 Biguanide Drugs 0.000 claims 2
• JVHXJTBJCFBINQ-ADAARDCZSA-N Dapagliflozin Chemical group C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)=CC=C1Cl JVHXJTBJCFBINQ-ADAARDCZSA-N 0.000 claims 2
• 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 claims 2
• LTXREWYXXSTFRX-QGZVFWFLSA-N Linagliptin Chemical compound N=1C=2N(C)C(=O)N(CC=3N=C4C=CC=CC4=C(C)N=3)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 LTXREWYXXSTFRX-QGZVFWFLSA-N 0.000 claims 2
• 108010016731 PPAR gamma Proteins 0.000 claims 2
• 229940123518 Sodium/glucose cotransporter 2 inhibitor Drugs 0.000 claims 2
• 229940125708 antidiabetic agent Drugs 0.000 claims 2
• 229960003834 dapagliflozin Drugs 0.000 claims 2
• 206010012601 diabetes mellitus Diseases 0.000 claims 2
• 239000008103 glucose Substances 0.000 claims 2
• NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
• 229960002397 linagliptin Drugs 0.000 claims 2
• 229960001254 vildagliptin Drugs 0.000 claims 2
• SYOKIDBDQMKNDQ-XWTIBIIYSA-N vildagliptin Chemical compound C1C(O)(C2)CC(C3)CC1CC32NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-XWTIBIIYSA-N 0.000 claims 2
• QKDRXGFQVGOQKS-CRSSMBPESA-N (2s,3r,4r,5s,6r)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-methylsulfanyloxane-3,4,5-triol Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](SC)O2)O)=CC=C1Cl QKDRXGFQVGOQKS-CRSSMBPESA-N 0.000 claims 1
• AOBLNYCSGWSIPG-YRIDSSQKSA-N (2s,3r,4s,5s,6r)-2-[4-[(2-fluoro-4-methoxyphenyl)methyl]-5-methyl-1-propan-2-ylpyrazol-3-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound FC1=CC(OC)=CC=C1CC1=C(C)N(C(C)C)N=C1O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 AOBLNYCSGWSIPG-YRIDSSQKSA-N 0.000 claims 1
• SWLAMJPTOQZTAE-UHFFFAOYSA-N 4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]benzoic acid Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(C(O)=O)C=C1 SWLAMJPTOQZTAE-UHFFFAOYSA-N 0.000 claims 1
• XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 1
• 102000030914 Fatty Acid-Binding Human genes 0.000 claims 1
• 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 claims 1
• 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims 1
• 102000004366 Glucosidases Human genes 0.000 claims 1
• 108010056771 Glucosidases Proteins 0.000 claims 1
• 102000007390 Glycogen Phosphorylase Human genes 0.000 claims 1
• 108010046163 Glycogen Phosphorylase Proteins 0.000 claims 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 claims 1
• 102100023915 Insulin Human genes 0.000 claims 1
• 108090001061 Insulin Proteins 0.000 claims 1
• WHSOLWOTCHFFBK-ZQGJOIPISA-N Luseogliflozin Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)S2)O)=C(OC)C=C1C WHSOLWOTCHFFBK-ZQGJOIPISA-N 0.000 claims 1
• 108010028924 PPAR alpha Proteins 0.000 claims 1
• 102000023984 PPAR alpha Human genes 0.000 claims 1
• 102000000536 PPAR gamma Human genes 0.000 claims 1
• 102100038831 Peroxisome proliferator-activated receptor alpha Human genes 0.000 claims 1
• 102100038825 Peroxisome proliferator-activated receptor gamma Human genes 0.000 claims 1
• 229940100389 Sulfonylurea Drugs 0.000 claims 1
• 102000003673 Symporters Human genes 0.000 claims 1
• 108090000088 Symporters Proteins 0.000 claims 1
• 229940123464 Thiazolidinedione Drugs 0.000 claims 1
• ZXOCGDDVNPDRIW-NHFZGCSJSA-N Tofogliflozin Chemical compound O.C1=CC(CC)=CC=C1CC1=CC=C(CO[C@@]23[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O3)O)C2=C1 ZXOCGDDVNPDRIW-NHFZGCSJSA-N 0.000 claims 1
• 229960001667 alogliptin Drugs 0.000 claims 1
• ZSBOMTDTBDDKMP-OAHLLOKOSA-N alogliptin Chemical compound C=1C=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 ZSBOMTDTBDDKMP-OAHLLOKOSA-N 0.000 claims 1
• 229940127003 anti-diabetic drug Drugs 0.000 claims 1
• 150000004283 biguanides Chemical class 0.000 claims 1
• 229960001713 canagliflozin Drugs 0.000 claims 1
• VHOFTEAWFCUTOS-TUGBYPPCSA-N canagliflozin hydrate Chemical compound O.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1.CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1 VHOFTEAWFCUTOS-TUGBYPPCSA-N 0.000 claims 1
• 238000011260 co-administration Methods 0.000 claims 1
• 230000009977 dual effect Effects 0.000 claims 1
• 229960003345 empagliflozin Drugs 0.000 claims 1
• OBWASQILIWPZMG-QZMOQZSNSA-N empagliflozin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(Cl)C(CC=2C=CC(O[C@@H]3COCC3)=CC=2)=C1 OBWASQILIWPZMG-QZMOQZSNSA-N 0.000 claims 1
• 108091022862 fatty acid binding Proteins 0.000 claims 1
• 229960004580 glibenclamide Drugs 0.000 claims 1
• ZNNLBTZKUZBEKO-UHFFFAOYSA-N glyburide Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZNNLBTZKUZBEKO-UHFFFAOYSA-N 0.000 claims 1
• 230000002641 glycemic effect Effects 0.000 claims 1
• 230000002440 hepatic effect Effects 0.000 claims 1
• 229940125396 insulin Drugs 0.000 claims 1
• 229950000991 ipragliflozin Drugs 0.000 claims 1
• AHFWIQIYAXSLBA-RQXATKFSSA-N ipragliflozin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(F)C(CC=2SC3=CC=CC=C3C=2)=C1 AHFWIQIYAXSLBA-RQXATKFSSA-N 0.000 claims 1
• 229950004397 luseogliflozin Drugs 0.000 claims 1
• 229950004994 meglitinide Drugs 0.000 claims 1
• XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 1
• 229960003105 metformin Drugs 0.000 claims 1
• 108091008725 peroxisome proliferator-activated receptors alpha Proteins 0.000 claims 1
• GCYXWQUSHADNBF-AAEALURTSA-N preproglucagon 78-108 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 GCYXWQUSHADNBF-AAEALURTSA-N 0.000 claims 1
• 229910052708 sodium Inorganic materials 0.000 claims 1
• 239000011734 sodium Substances 0.000 claims 1
• YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 1
• 238000002560 therapeutic procedure Methods 0.000 claims 1
• 150000001467 thiazolidinediones Chemical class 0.000 claims 1
• 229950006667 tofogliflozin Drugs 0.000 claims 1
• 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1