JP2012528170A5 - - Google Patents
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- Publication number
- JP2012528170A5 JP2012528170A5 JP2012513184A JP2012513184A JP2012528170A5 JP 2012528170 A5 JP2012528170 A5 JP 2012528170A5 JP 2012513184 A JP2012513184 A JP 2012513184A JP 2012513184 A JP2012513184 A JP 2012513184A JP 2012528170 A5 JP2012528170 A5 JP 2012528170A5
- Authority
- JP
- Japan
- Prior art keywords
- inhibitor
- agent
- dapagliflozin
- insulin
- per day
- 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- Withdrawn
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- 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 32
- HYAFETHFCAUJAY-UHFFFAOYSA-N pioglitazone Chemical compound N1=CC(CC)=CC=C1CCOC(C=C1)=CC=C1CC1C(=O)NC(=O)S1 HYAFETHFCAUJAY-UHFFFAOYSA-N 0.000 claims 20
- YASAKCUCGLMORW-UHFFFAOYSA-N Rosiglitazone Chemical compound C=1C=CC=NC=1N(C)CCOC(C=C1)=CC=C1CC1SC(=O)NC1=O YASAKCUCGLMORW-UHFFFAOYSA-N 0.000 claims 18
- 239000003795 chemical substances by application Substances 0.000 claims 17
- 102000004877 Insulin Human genes 0.000 claims 16
- 108090001061 Insulin Proteins 0.000 claims 16
- 229940125396 insulin Drugs 0.000 claims 16
- 239000003814 drug Substances 0.000 claims 15
- 239000003112 inhibitor Substances 0.000 claims 12
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 12
- 229960003105 metformin Drugs 0.000 claims 12
- 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 10
- 229940123518 Sodium/glucose cotransporter 2 inhibitor Drugs 0.000 claims 10
- 229960003834 dapagliflozin Drugs 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- 229960005095 pioglitazone Drugs 0.000 claims 9
- 229960004586 rosiglitazone Drugs 0.000 claims 9
- 229940124597 therapeutic agent Drugs 0.000 claims 8
- 239000003472 antidiabetic agent Substances 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 239000000556 agonist Substances 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 239000005557 antagonist Substances 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 4
- ZOBPZXTWZATXDG-UHFFFAOYSA-N 1,3-thiazolidine-2,4-dione Chemical compound O=C1CSC(=O)N1 ZOBPZXTWZATXDG-UHFFFAOYSA-N 0.000 claims 3
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims 3
- 102000023984 PPAR alpha Human genes 0.000 claims 3
- 229940123464 Thiazolidinedione Drugs 0.000 claims 3
- 229960001138 acetylsalicylic acid Drugs 0.000 claims 3
- 230000003178 anti-diabetic effect Effects 0.000 claims 3
- 239000000883 anti-obesity agent Substances 0.000 claims 3
- 229940125708 antidiabetic agent Drugs 0.000 claims 3
- 229940125710 antiobesity agent Drugs 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
- 108091008725 peroxisome proliferator-activated receptors alpha Proteins 0.000 claims 3
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 2
- 239000005541 ACE inhibitor Substances 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 239000005552 B01AC04 - Clopidogrel Substances 0.000 claims 2
- 239000005528 B01AC05 - Ticlopidine Substances 0.000 claims 2
- 239000005465 B01AC22 - Prasugrel Substances 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 102000012336 Cholesterol Ester Transfer Proteins Human genes 0.000 claims 2
- 108010061846 Cholesterol Ester Transfer Proteins Proteins 0.000 claims 2
- 229940122502 Cholesterol absorption inhibitor Drugs 0.000 claims 2
- 101000783577 Dendroaspis angusticeps Thrombostatin Proteins 0.000 claims 2
- 101000783578 Dendroaspis jamesoni kaimosae Dendroaspin Proteins 0.000 claims 2
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims 2
- HTQBXNHDCUEHJF-XWLPCZSASA-N Exenatide Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=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](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)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)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 HTQBXNHDCUEHJF-XWLPCZSASA-N 0.000 claims 2
- 108010011459 Exenatide Proteins 0.000 claims 2
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 2
- 102000000853 LDL receptors Human genes 0.000 claims 2
- 108010001831 LDL receptors Proteins 0.000 claims 2
- 102000003729 Neprilysin Human genes 0.000 claims 2
- 108090000028 Neprilysin Proteins 0.000 claims 2
- 102000008078 Sterol Regulatory Element Binding Protein 1 Human genes 0.000 claims 2
- 108010074436 Sterol Regulatory Element Binding Protein 1 Proteins 0.000 claims 2
- 229940062328 actos Drugs 0.000 claims 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 2
- 239000002220 antihypertensive agent Substances 0.000 claims 2
- 229940127218 antiplatelet drug Drugs 0.000 claims 2
- 229940062310 avandia Drugs 0.000 claims 2
- -1 axoquin Chemical compound 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 229960003009 clopidogrel Drugs 0.000 claims 2
- GKTWGGQPFAXNFI-HNNXBMFYSA-N clopidogrel Chemical compound C1([C@H](N2CC=3C=CSC=3CC2)C(=O)OC)=CC=CC=C1Cl GKTWGGQPFAXNFI-HNNXBMFYSA-N 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims 2
- 230000009977 dual effect Effects 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 239000003538 oral antidiabetic agent Substances 0.000 claims 2
- DHHVAGZRUROJKS-UHFFFAOYSA-N phentermine Chemical compound CC(C)(N)CC1=CC=CC=C1 DHHVAGZRUROJKS-UHFFFAOYSA-N 0.000 claims 2
- 239000000106 platelet aggregation inhibitor Substances 0.000 claims 2
- 229960004197 prasugrel Drugs 0.000 claims 2
- DTGLZDAWLRGWQN-UHFFFAOYSA-N prasugrel Chemical compound C1CC=2SC(OC(=O)C)=CC=2CN1C(C=1C(=CC=CC=1)F)C(=O)C1CC1 DTGLZDAWLRGWQN-UHFFFAOYSA-N 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 239000003801 protein tyrosine phosphatase 1B inhibitor Substances 0.000 claims 2
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 229940044551 receptor antagonist Drugs 0.000 claims 2
- SUFUKZSWUHZXAV-BTJKTKAUSA-N rosiglitazone maleate Chemical compound [H+].[H+].[O-]C(=O)\C=C/C([O-])=O.C=1C=CC=NC=1N(C)CCOC(C=C1)=CC=C1CC1SC(=O)NC1=O SUFUKZSWUHZXAV-BTJKTKAUSA-N 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229960005001 ticlopidine Drugs 0.000 claims 2
- PHWBOXQYWZNQIN-UHFFFAOYSA-N ticlopidine Chemical compound ClC1=CC=CC=C1CN1CC(C=CS2)=C2CC1 PHWBOXQYWZNQIN-UHFFFAOYSA-N 0.000 claims 2
- BQPPJGMMIYJVBR-UHFFFAOYSA-N (10S)-3c-Acetoxy-4.4.10r.13c.14t-pentamethyl-17c-((R)-1.5-dimethyl-hexen-(4)-yl)-(5tH)-Delta8-tetradecahydro-1H-cyclopenta[a]phenanthren Natural products CC12CCC(OC(C)=O)C(C)(C)C1CCC1=C2CCC2(C)C(C(CCC=C(C)C)C)CCC21C BQPPJGMMIYJVBR-UHFFFAOYSA-N 0.000 claims 1
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims 1
- ZGGHKIMDNBDHJB-NRFPMOEYSA-M (3R,5S)-fluvastatin sodium Chemical compound [Na+].C12=CC=CC=C2N(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC([O-])=O)=C1C1=CC=C(F)C=C1 ZGGHKIMDNBDHJB-NRFPMOEYSA-M 0.000 claims 1
- CHGIKSSZNBCNDW-UHFFFAOYSA-N (3beta,5alpha)-4,4-Dimethylcholesta-8,24-dien-3-ol Natural products CC12CCC(O)C(C)(C)C1CCC1=C2CCC2(C)C(C(CCC=C(C)C)C)CCC21 CHGIKSSZNBCNDW-UHFFFAOYSA-N 0.000 claims 1
- KWTSXDURSIMDCE-QMMMGPOBSA-N (S)-amphetamine Chemical compound C[C@H](N)CC1=CC=CC=C1 KWTSXDURSIMDCE-QMMMGPOBSA-N 0.000 claims 1
- 229940126558 11β-HSD1 inhibitor Drugs 0.000 claims 1
- XYTLYKGXLMKYMV-UHFFFAOYSA-N 14alpha-methylzymosterol Natural products CC12CCC(O)CC1CCC1=C2CCC2(C)C(C(CCC=C(C)C)C)CCC21C XYTLYKGXLMKYMV-UHFFFAOYSA-N 0.000 claims 1
- ROJNYKZWTOHRNU-UHFFFAOYSA-N 2-chloro-4,5-difluoro-n-[[2-methoxy-5-(methylcarbamoylamino)phenyl]carbamoyl]benzamide Chemical compound CNC(=O)NC1=CC=C(OC)C(NC(=O)NC(=O)C=2C(=CC(F)=C(F)C=2)Cl)=C1 ROJNYKZWTOHRNU-UHFFFAOYSA-N 0.000 claims 1
- ILPUOPPYSQEBNJ-UHFFFAOYSA-N 2-methyl-2-phenoxypropanoic acid Chemical class OC(=O)C(C)(C)OC1=CC=CC=C1 ILPUOPPYSQEBNJ-UHFFFAOYSA-N 0.000 claims 1
- SXKBTDJJEQQEGE-UHFFFAOYSA-N 3-(3,5-dibromo-4-hydroxy-benzoyl)-2-ethyl-benzofuran-6-sulfonic acid [4-(thiazol-2-ylsulfamoyl)-phenyl]-amide Chemical compound CCC=1OC2=CC(S(=O)(=O)NC=3C=CC(=CC=3)S(=O)(=O)NC=3SC=CN=3)=CC=C2C=1C(=O)C1=CC(Br)=C(O)C(Br)=C1 SXKBTDJJEQQEGE-UHFFFAOYSA-N 0.000 claims 1
- FPTJELQXIUUCEY-UHFFFAOYSA-N 3beta-Hydroxy-lanostan Natural products C1CC2C(C)(C)C(O)CCC2(C)C2C1C1(C)CCC(C(C)CCCC(C)C)C1(C)CC2 FPTJELQXIUUCEY-UHFFFAOYSA-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
- 125000001054 5 membered carbocyclic group Chemical group 0.000 claims 1
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 1
- 229940118148 Aldose reductase inhibitor Drugs 0.000 claims 1
- XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 claims 1
- XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 claims 1
- 229940123208 Biguanide Drugs 0.000 claims 1
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
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- 102000034534 Cotransporters Human genes 0.000 claims 1
- 108020003264 Cotransporters Proteins 0.000 claims 1
- 101100393023 Crocus sativus GLT2 gene Proteins 0.000 claims 1
- 229940122680 Demethylase inhibitor Drugs 0.000 claims 1
- 102100036869 Diacylglycerol O-acyltransferase 1 Human genes 0.000 claims 1
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- BKLIAINBCQPSOV-UHFFFAOYSA-N Gluanol Natural products CC(C)CC=CC(C)C1CCC2(C)C3=C(CCC12C)C4(C)CCC(O)C(C)(C)C4CC3 BKLIAINBCQPSOV-UHFFFAOYSA-N 0.000 claims 1
- 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 claims 1
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- 102000004366 Glucosidases Human genes 0.000 claims 1
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- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 101000581402 Homo sapiens Melanin-concentrating hormone receptor 1 Proteins 0.000 claims 1
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- 102000007330 LDL Lipoproteins Human genes 0.000 claims 1
- LOPKHWOTGJIQLC-UHFFFAOYSA-N Lanosterol Natural products CC(CCC=C(C)C)C1CCC2(C)C3=C(CCC12C)C4(C)CCC(C)(O)C(C)(C)C4CC3 LOPKHWOTGJIQLC-UHFFFAOYSA-N 0.000 claims 1
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- 241000124008 Mammalia Species 0.000 claims 1
- ZPXSCAKFGYXMGA-UHFFFAOYSA-N Mazindol Chemical compound N12CCN=C2C2=CC=CC=C2C1(O)C1=CC=C(Cl)C=C1 ZPXSCAKFGYXMGA-UHFFFAOYSA-N 0.000 claims 1
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- YXKTVDFXDRQTKV-HNNXBMFYSA-N benzphetamine Chemical compound C([C@H](C)N(C)CC=1C=CC=CC=1)C1=CC=CC=C1 YXKTVDFXDRQTKV-HNNXBMFYSA-N 0.000 claims 1
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- 230000031200 bile acid secretion Effects 0.000 claims 1
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- 239000003536 cannabinoid receptor antagonist Substances 0.000 claims 1
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- 239000002604 chemokine receptor CCR2 antagonist Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 229960004890 diethylpropion Drugs 0.000 claims 1
- XXEPPPIWZFICOJ-UHFFFAOYSA-N diethylpropion Chemical compound CCN(CC)C(C)C(=O)C1=CC=CC=C1 XXEPPPIWZFICOJ-UHFFFAOYSA-N 0.000 claims 1
- QBSJHOGDIUQWTH-UHFFFAOYSA-N dihydrolanosterol Natural products CC(C)CCCC(C)C1CCC2(C)C3=C(CCC12C)C4(C)CCC(C)(O)C(C)(C)C4CC3 QBSJHOGDIUQWTH-UHFFFAOYSA-N 0.000 claims 1
- 239000002934 diuretic Substances 0.000 claims 1
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- 239000000706 filtrate Substances 0.000 claims 1
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- ZJJXGWJIGJFDTL-UHFFFAOYSA-N glipizide Chemical compound C1=NC(C)=CN=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZJJXGWJIGJFDTL-UHFFFAOYSA-N 0.000 claims 1
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| JP2017074526A Pending JP2017160212A (ja) | 2009-05-27 | 2017-04-04 | 別の抗糖尿病薬を用いた先の治療に抵抗性を有する２型糖尿病患者をｓｇｌｔ２阻害剤およびその組成物を用いて治療する方法 |
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| US7772191B2 (en) | 2005-05-10 | 2010-08-10 | Boehringer Ingelheim International Gmbh | Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein |
| PE20080697A1 (es) | 2006-05-03 | 2008-08-05 | Boehringer Ingelheim Int | Derivados de benzonitrilo sustituidos con glucopiranosilo, composiciones farmaceuticas que contienen compuestos de este tipo, su uso y procedimiento para su fabricacion |
| PE20090938A1 (es) | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo |
| PL2395983T3 (pl) | 2009-02-13 | 2020-09-07 | Boehringer Ingelheim International Gmbh | Kompozycja farmaceutyczna zawierająca inhibitor sglt2, inhibitor dpp-iv i ewentualnie dalszy środek przeciwcukrzycowy oraz jej zastosowania |
| MY161472A (en) | 2009-02-13 | 2017-04-14 | Boehringer Ingelheim Int | Sglt-2 inhibitor for treating type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance or hyperglycemia |
| BR112012007085B8 (pt) | 2009-09-30 | 2021-05-25 | Boehringer Ingelheim Int | processos para a preparação de derivados de benzil-benzeno substituídos com glicopiranosila |
| HUE029381T2 (en) * | 2009-09-30 | 2017-02-28 | Boehringer Ingelheim Int | Method for the preparation of a crystalline form of 1-chloro-4-(beta-d-glucopyranos-1-yl)-2-(4-((s)-tetrahydrofuran-3-yloxy)benzyl)benzene |
| US10610489B2 (en) * | 2009-10-02 | 2020-04-07 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, pharmaceutical dosage form, process for their preparation, methods for treating and uses thereof |
| CN104825417A (zh) | 2009-11-13 | 2015-08-12 | 阿斯利康(瑞典)有限公司 | 立即释放片剂 |
| ES2689107T3 (es) | 2009-11-13 | 2018-11-08 | Astrazeneca Ab | Formulaciones de tabletas bicapa |
| US20140088027A1 (en) * | 2010-03-30 | 2014-03-27 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition comprising an sglt2 inhibitor and a ppar- gamma agonist and uses thereof |
| US20120283169A1 (en) * | 2010-11-08 | 2012-11-08 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| IL295438B2 (en) * | 2011-01-05 | 2026-05-01 | Lexicon Pharmaceuticals Inc | Compositions containing and methods for using inhibitors of sodium-glucose cotransporters 1 and 2 |
| US20130035281A1 (en) * | 2011-02-09 | 2013-02-07 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| UY33937A (es) | 2011-03-07 | 2012-09-28 | Boehringer Ingelheim Int | Composiciones farmacéuticas que contienen inhibidores de dpp-4 y/o sglt-2 y metformina |
| WO2013095316A1 (en) * | 2011-12-19 | 2013-06-27 | Mahmut Bilgic | Synergic combination comprising anti-diabetic agent |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| US9192617B2 (en) | 2012-03-20 | 2015-11-24 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| JP6198013B2 (ja) * | 2012-08-30 | 2017-09-20 | 大正製薬株式会社 | Ｓｇｌｔ２阻害薬と抗高血圧薬との組み合わせ |
| PT3466431T (pt) | 2013-03-14 | 2024-01-26 | Msd Int Gmbh | Formas cristalinas e métodos para preparação de inibidores de sglt2 |
| HRP20190101T1 (hr) | 2013-04-05 | 2019-03-08 | Boehringer Ingelheim International Gmbh | Terapeutske uporabe empagliflozina |
| CA2812519A1 (en) | 2013-04-05 | 2014-10-05 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| US11813275B2 (en) | 2013-04-05 | 2023-11-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| US20140303097A1 (en) | 2013-04-05 | 2014-10-09 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| KR102309654B1 (ko) | 2013-04-18 | 2021-10-08 | 베링거 인겔하임 인터내셔날 게엠베하 | 약제학적 조성물, 치료 방법 및 이의 용도 |
| EP2991999B1 (en) | 2013-04-29 | 2019-05-08 | Mapi Pharma Limited | Dapagliflozin lactose co-crystal |
| CN104496952B (zh) * | 2014-11-28 | 2017-04-19 | 深圳翰宇药业股份有限公司 | 一种达格列净的合成方法 |
| US10894054B2 (en) * | 2015-04-07 | 2021-01-19 | Intercept Pharmaceuticals, Inc. | FXR agonist compositions for combination therapy |
| WO2017134615A1 (en) * | 2016-02-03 | 2017-08-10 | Dr. Reddy's Laboratories Limited | Solid state forms of dasatinib and processes for their preparation |
| BR112018073688A2 (pt) * | 2016-05-20 | 2019-02-26 | Center Laboratories, Inc. | método de tratamento de hiperglicemia |
| CA3039745A1 (en) | 2016-11-10 | 2018-05-17 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| WO2018167589A1 (en) | 2017-03-16 | 2018-09-20 | Inventia Healthcare Private Limited | Pharmaceutical composition comprising dapagliflozin |
| AR112015A1 (es) | 2017-06-09 | 2019-09-11 | Novo Nordisk As | Composiciones sólidas para administración oral |
| MY210547A (en) * | 2017-11-30 | 2025-09-30 | Idorsia Pharmaceuticals Ltd | Combination of a 4-pyrimidinesulfamide derivative with an sglt-2 inhibitor for the treatment of endothelin related diseases |
| US10639292B2 (en) | 2018-04-20 | 2020-05-05 | Center Laboratories, Inc. | Method of treating hyperglycemia |
| LT3804714T (lt) * | 2018-05-31 | 2025-03-10 | Hua Medicine (Shanghai) Ltd. | Farmacinis derinys ir kompozicija, ir derinio preparatas, kurio sudėtyje yra gliukokinazės aktyvatorius ir biguanido hipoglikeminis vaistas, taip pat jų gamybos būdas ir panaudojimas |
| US11495339B2 (en) * | 2018-06-14 | 2022-11-08 | Astrazeneca Uk Limited | Methods for lowering blood sugar with a gliflozin sodium-glucose cotransport 2 inhibitor pharmaceutical composition |
| TWI867086B (zh) | 2019-11-05 | 2024-12-21 | 加拿大商瑞斯弗洛吉克斯公司 | 以rvx-208及sglt2抑制劑治療及/或預防主要不良心血管事件(mace)的方法 |
| MX2022007945A (es) * | 2019-12-24 | 2022-10-03 | Hanmi Pharm Ind Co Ltd | Formulacion compleja que comprende sitagliptina y dapagliflozina, y metodo de preparacion de la misma. |
| US20230270718A1 (en) * | 2020-04-10 | 2023-08-31 | Chinook Therapeutics, Inc. | Methods of treating diabetic kidney disease |
| WO2021214023A1 (en) | 2020-04-22 | 2021-10-28 | Bayer Aktiengesellschaft | Combination of finerenone and a sglt2 inhibitor for the treatment and/or prevention of cardiovascular and/or renal diseases |
| KR102838283B1 (ko) * | 2020-07-10 | 2025-07-25 | 한미약품 주식회사 | 시타글립틴 및 다파글리플로진을 포함하는 복합제제 및 그 제조방법 |
| PT4188389T (pt) | 2020-07-27 | 2025-10-07 | Astrazeneca Ab | Dapagliflozina para utilização em métodos de tratamento de doença renal crónica |
| WO2022091029A1 (en) * | 2020-10-30 | 2022-05-05 | Resverlogix Corp. | Methods for lowering hba1c level with a combination of a bet bromodomain inhibitor and a sodium dependent glucose transport 2 inhibitor |
| CN114671839B (zh) * | 2020-12-25 | 2024-01-09 | 天地恒一制药股份有限公司 | 达格列净的固体形式复合物及其制备方法与应用 |
| CN118510504A (zh) * | 2022-01-26 | 2024-08-16 | 阿斯利康(瑞典)有限公司 | 用于在治疗糖尿病前期或降低发展2型糖尿病的风险中使用的达格列净 |
| US20250345512A1 (en) * | 2022-03-14 | 2025-11-13 | University Of Virginia Patent Foundation | Combination sodium-glucose cotransporter inhibitor (sglti) insulin therapy for glycemic control in type 1 diabetes |
| EP4385502A1 (en) * | 2022-12-15 | 2024-06-19 | Sanovel Ilac Sanayi Ve Ticaret A.S. | A pharmaceutical formulation comprising metformin, pioglitazone and a sglt-2 inhibitor |
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| US6515117B2 (en) * | 1999-10-12 | 2003-02-04 | Bristol-Myers Squibb Company | C-aryl glucoside SGLT2 inhibitors and method |
| PH12000002657B1 (en) * | 1999-10-12 | 2006-02-21 | Bristol Myers Squibb Co | C-aryl glucoside SGLT2 inhibitors |
| US6936590B2 (en) * | 2001-03-13 | 2005-08-30 | Bristol Myers Squibb Company | C-aryl glucoside SGLT2 inhibitors and method |
| IL149851A0 (en) | 2002-05-26 | 2002-11-10 | Yeda Res & Dev | Resistin binding proteins, their preparation and use |
| AR065809A1 (es) * | 2007-03-22 | 2009-07-01 | Bristol Myers Squibb Co | Formulaciones farmaceuticas que contienen un inhibidor sglt2 |
| WO2010045656A2 (en) * | 2008-10-17 | 2010-04-22 | Nectid, Inc. | Novel sglt2 inhibitor dosage forms |
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