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- Withdrawn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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| 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 |
| US20110046076A1 (en) | 2009-02-13 | 2011-02-24 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| DK2486029T3 (en) | 2009-09-30 | 2015-08-24 | Boehringer Ingelheim Int | Methods of making of glucopyranosyl-substituted benzyl-benzene derivatives. |
| CA2775961C (en) * | 2009-09-30 | 2017-11-07 | Boehringer Ingelheim International Gmbh | 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 |
| UY32919A (es) | 2009-10-02 | 2011-04-29 | Boehringer Ingelheim Int | Composición farmacéutica, forma de dosificación farmacéutica, procedimiento para su preparación, mé todos para su tratamiento y sus usos |
| EP2498759B1 (en) | 2009-11-13 | 2018-08-01 | AstraZeneca AB | Immediate release tablet formulations |
| PT2498758T (pt) | 2009-11-13 | 2018-10-23 | Astrazeneca Uk Ltd | Formulações de comprimido bicamada |
| EP2552442A1 (en) * | 2010-03-30 | 2013-02-06 | 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 |
| TWI631963B (zh) * | 2011-01-05 | 2018-08-11 | 雷西肯製藥股份有限公司 | 包含鈉－葡萄糖共同輸送體１與２之抑制劑的組合物與應用方法 |
| 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 |
| TW201414472A (zh) | 2012-08-30 | 2014-04-16 | 大正製藥股份有限公司 | Ｓｇｌｔ２抑制藥與抗高血壓藥之組合 |
| WO2014159151A1 (en) | 2013-03-14 | 2014-10-02 | Msd International Gmbh | Methods for preparing sglt2 inhibitors |
| CA2812519A1 (en) | 2013-04-05 | 2014-10-05 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| TR201901110T4 (tr) | 2013-04-05 | 2019-02-21 | Boehringer Ingelheim Int | Empagliflozinin terapötik kullanımları. |
| US11813275B2 (en) | 2013-04-05 | 2023-11-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| HK1213818A1 (zh) | 2013-04-05 | 2016-07-15 | 勃林格殷格翰国际有限公司 | 依帕列净的治疗用途 |
| DK2986304T3 (da) | 2013-04-18 | 2022-04-04 | Boehringer Ingelheim Int | Farmaceutisk sammensætning, fremgangsmåder til behandling og anvendelser deraf. |
| WO2014178040A1 (en) | 2013-04-29 | 2014-11-06 | Mapi Pharma Ltd. | Co-crystals of dapagliflozin |
| 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 |
| MX2017012893A (es) * | 2015-04-07 | 2018-01-15 | Intercept Pharmaceuticals Inc | Composiciones farmaceuticas para terapias combinadas. |
| US10464933B2 (en) * | 2016-02-03 | 2019-11-05 | Dr. Reddy's Laboratories Limited | Solid state forms of dasatinib and processes for their preparation |
| TWI659738B (zh) * | 2016-05-20 | 2019-05-21 | 晟德大藥廠股份有限公司 | (r)-(+)-維拉帕米用於治療高血糖的用途 |
| AU2017357589B2 (en) | 2016-11-10 | 2023-05-11 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| US11020412B2 (en) | 2017-03-16 | 2021-06-01 | Inventia Healthcare Limited | Pharmaceutical composition comprising dapagliflozin |
| AR112015A1 (es) | 2017-06-09 | 2019-09-11 | Novo Nordisk As | Composiciones sólidas para administración oral |
| US12144811B2 (en) * | 2017-11-30 | 2024-11-19 | 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 |
| EP3811939A4 (en) | 2018-05-31 | 2022-05-25 | Hua Medicine (Shanghai) Ltd. | PHARMACEUTICAL COMBINATION, COMPOSITION AND FORMULATION CONTAINING A GLUCOSIDASE ACTIVATOR AND A &X3B1;-GLUCOSIDASE INHIBITOR, METHODS OF PREPARING THEM AND USES THEREOF |
| CA3103424A1 (en) * | 2018-06-14 | 2019-12-19 | Astrazeneca Uk Limited | Methods for lowering blood sugar with a gliflozin sodium-glucose cotransporter 2 inhibitor pharmaceutical composition |
| JP7523545B2 (ja) * | 2019-12-24 | 2024-07-26 | ハンミ ファーマシューティカルズ カンパニー リミテッド | シタグリプチン及びダパグリフロジンを含む複合製剤及びその製造方法 |
| JP2023521169A (ja) * | 2020-04-10 | 2023-05-23 | チヌーク セラピューティクス，インコーポレイテッド | 糖尿病性腎疾患の処置方法 |
| JP2023523596A (ja) | 2020-04-22 | 2023-06-06 | バイエル アクチェンゲゼルシャフト | 心血管疾患および／または腎疾患を治療および／または予防するためのフィネレノンとｓｇｌｔ２阻害剤の組み合わせ |
| 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 |
| WO2023144722A1 (en) * | 2022-01-26 | 2023-08-03 | Astrazeneca Ab | Dapagliflozin for use in the treatment of prediabetes or reducing the risk of developing type 2 diabetes |
| EP4493272A1 (en) * | 2022-03-14 | 2025-01-22 | 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 |
| PE20090185A1 (es) * | 2007-03-22 | 2009-02-28 | 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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