JP2006063074A5 - - Google Patents
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- JP2006063074A5 JP2006063074A5 JP2005219763A JP2005219763A JP2006063074A5 JP 2006063074 A5 JP2006063074 A5 JP 2006063074A5 JP 2005219763 A JP2005219763 A JP 2005219763A JP 2005219763 A JP2005219763 A JP 2005219763A JP 2006063074 A5 JP2006063074 A5 JP 2006063074A5
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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 62
- 239000008194 pharmaceutical composition Substances 0.000 claims 46
- 108090001061 Insulin Proteins 0.000 claims 31
- 102000004877 Insulin Human genes 0.000 claims 31
- 101700032406 IAA Proteins 0.000 claims 24
- 239000003392 amylase inhibitor Substances 0.000 claims 24
- 101700007658 leg3 Proteins 0.000 claims 24
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 12
- 239000003623 enhancer Substances 0.000 claims 12
- 230000002708 enhancing Effects 0.000 claims 12
- 230000035945 sensitivity Effects 0.000 claims 12
- WLDBVPWSCOUGQI-ZMMVPWHFSA-N (2S,3R,4S,5S,6R)-2-[(2R,3S,4R,5R,6S)-4,5-dihydroxy-6-[(2R,3R,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-3-yl]oxy-2-(hydroxymethyl)oxan-3-yl]oxy-6-methyloxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](C)O[C@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H](O[C@@H]2[C@H](NC[C@H]2O)CO)O[C@@H]1CO WLDBVPWSCOUGQI-ZMMVPWHFSA-N 0.000 claims 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 10
- 230000000580 secretagogue Effects 0.000 claims 10
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N diguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 9
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 8
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 8
- 101700062901 DPP Proteins 0.000 claims 7
- 102100012353 DPP4 Human genes 0.000 claims 7
- 101700039720 DPP4 Proteins 0.000 claims 7
- 239000003112 inhibitor Substances 0.000 claims 7
- 230000002401 inhibitory effect Effects 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 239000011780 sodium chloride Substances 0.000 claims 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 6
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 6
- 125000003277 amino group Chemical group 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 150000002148 esters Chemical class 0.000 claims 6
- 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 4
- 229960005095 Pioglitazone Drugs 0.000 claims 4
- 125000004849 alkoxymethyl group Chemical group 0.000 claims 4
- 229940079593 drugs Drugs 0.000 claims 4
- WLDBVPWSCOUGQI-WPCAJUIMSA-N (2R,3R,4S,5S,6R)-2-[(2R,3S,4R,5R,6S)-4,5-dihydroxy-6-[(2R,3R,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-3-yl]oxy-2-(hydroxymethyl)oxan-3-yl]oxy-6-methyloxane-3,4,5-triol Chemical group O[C@@H]1[C@@H](O)[C@H](O)[C@@H](C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H](O[C@@H]2[C@H](NC[C@H]2O)CO)O[C@@H]1CO WLDBVPWSCOUGQI-WPCAJUIMSA-N 0.000 claims 3
- 229960003105 Metformin Drugs 0.000 claims 3
- OELFLUMRDSZNSF-BRWVUGGUSA-N Nateglinide Chemical compound C1C[C@@H](C(C)C)CC[C@@H]1C(=O)N[C@@H](C(O)=O)CC1=CC=CC=C1 OELFLUMRDSZNSF-BRWVUGGUSA-N 0.000 claims 3
- 229960000698 Nateglinide Drugs 0.000 claims 3
- MFFMDFFZMYYVKS-SECBINFHSA-N Sitagliptin Chemical group C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical group CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 3
- 230000001629 suppression Effects 0.000 claims 3
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 2
- 206010012601 Diabetes mellitus Diseases 0.000 claims 2
- 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 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 230000003449 preventive Effects 0.000 claims 2
- 229960004586 rosiglitazone Drugs 0.000 claims 2
- 230000004584 weight gain Effects 0.000 claims 2
- 235000019786 weight gain Nutrition 0.000 claims 2
- QGJUIPDUBHWZPV-VFGQHSGRSA-N (1R,3S,5R)-2-[(2S)-2-amino-2-[(5S,7R)-3-hydroxy-1-adamantyl]acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile Chemical compound C([C@@H](C1)C2)[C@@H](C3)CC1(O)CC23[C@H](N)C(=O)N1[C@H](C#N)C[C@H]2C[C@H]21 QGJUIPDUBHWZPV-VFGQHSGRSA-N 0.000 claims 1
- SYOKIDBDQMKNDQ-HHUWHTLVSA-N (2S)-1-[2-[[(5S,7R)-3-hydroxy-1-adamantyl]amino]acetyl]pyrrolidine-2-carbonitrile Chemical compound C([C@@H]1C[C@H](C2)CC(C1)(C1)O)C21NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-HHUWHTLVSA-N 0.000 claims 1
- HBBJLDPBYHSWOK-ZMMVPWHFSA-N (2S,3R,4S,5S,6R)-2-[(2R,3S,4R,5R,6S)-4,5-dihydroxy-6-[(2R,3R,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-3-yl]oxy-2-(hydroxymethyl)oxan-3-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound OC[C@H]1NC[C@@H](O)[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)[C@@H](CO)O1 HBBJLDPBYHSWOK-ZMMVPWHFSA-N 0.000 claims 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- -1 6-fluoro-6-deoxy-β-D-glucopyranosyl Chemical group 0.000 claims 1
- 210000004369 Blood Anatomy 0.000 claims 1
- XSEUMFJMFFMCIU-UHFFFAOYSA-N Buformin Chemical compound CCCC\N=C(/N)N=C(N)N XSEUMFJMFFMCIU-UHFFFAOYSA-N 0.000 claims 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N D-Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 229960004580 GLIBENCLAMIDE Drugs 0.000 claims 1
- ZNNLBTZKUZBEKO-UHFFFAOYSA-N Glibenclamide Chemical group 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
- WIGIZIANZCJQQY-RUCARUNLSA-N Glimepiride Chemical compound O=C1C(CC)=C(C)CN1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)N[C@@H]2CC[C@@H](C)CC2)C=C1 WIGIZIANZCJQQY-RUCARUNLSA-N 0.000 claims 1
- 206010020993 Hypoglycaemia Diseases 0.000 claims 1
- 108010016731 PPAR gamma Proteins 0.000 claims 1
- 102000012132 Peroxisome proliferator-activated receptor gamma Human genes 0.000 claims 1
- 229960003243 Phenformin Drugs 0.000 claims 1
- ICFJFFQQTFMIBG-UHFFFAOYSA-N Phenformin Chemical compound NC(=N)NC(=N)NCCC1=CC=CC=C1 ICFJFFQQTFMIBG-UHFFFAOYSA-N 0.000 claims 1
- XMSXOLDPMGMWTH-UHFFFAOYSA-N Rivoglitazone Chemical compound CN1C2=CC(OC)=CC=C2N=C1COC(C=C1)=CC=C1CC1SC(=O)NC1=O XMSXOLDPMGMWTH-UHFFFAOYSA-N 0.000 claims 1
- 229960004937 Saxagliptin Drugs 0.000 claims 1
- 108010026951 Short-Acting Insulin Proteins 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 229960004111 buformin Drugs 0.000 claims 1
- 229960004346 glimepiride Drugs 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000002218 hypoglycaemic Effects 0.000 claims 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 1
- 235000014655 lactic acid Nutrition 0.000 claims 1
- 239000004310 lactic acid Substances 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000000291 postprandial Effects 0.000 claims 1
- 230000000069 prophylaxis Effects 0.000 claims 1
- 230000002829 reduced Effects 0.000 claims 1
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical compound OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 1
Claims (49)
[式中、Aは下記一般式(A1)、(A2)又は(A3)
を示し、R1及びR2はそれぞれ同一若しくは異なって、C1-6アルキル基、ヒドロキシメチル基、C1-6アルコキシメチル基又はC1-6ハロアルキル基を示し、R3、R4、R5及びR6はそれぞれ同一若しくは異なって、C1-6アルキル基、C1-6アルコキシ基、C1-6ヒドロキシアルキル基、C1-6ハロアルキル基、アミノ基(該アミノ基はC1-6アルキル基又はC1-6ヒドロキシアルキル基で1又は2個置換されていてもよい) 、水酸基、水素原子又はハロゲン原子を示し、R7はC1-6アルキル基、C1-6アルコキシ基、C1-6ヒドロキシアルキル基、C1-6ハロアルキル基、水酸基又は水素原子を示し、nは1又は2の整数を示す。] で表わされる化合物又はその薬理上許容される塩若しくはエステルから選ばれるα‐アミラーゼ阻害剤と、インスリン感受性増強剤、インスリン分泌促進剤、ビグアナイド剤、インスリン製剤及びDPP-IV阻害剤から選ばれる少なくとも一種の薬剤とを組み合わせてなる医薬組成物。 The following general formula (I)
[Wherein A represents the following general formula (A1), (A2) or (A3)
R 1 and R 2 are the same or different and each represents a C 1-6 alkyl group, a hydroxymethyl group, a C 1-6 alkoxymethyl group or a C 1-6 haloalkyl group, and R 3 , R 4 , R 5 and R 6 are the same or different and each represents a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 hydroxyalkyl group, a C1-6 haloalkyl group, an amino group (the amino group is a C1-6 alkyl group or a C1-6 hydroxy group). 1 or 2 may be substituted with an alkyl group), a hydroxyl group, a hydrogen atom or a halogen atom, R 7 is a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 hydroxyalkyl group, C1-6 A haloalkyl group, a hydroxyl group or a hydrogen atom; n represents an integer of 1 or 2; An α-amylase inhibitor selected from the compounds represented by the formula (I) or a pharmacologically acceptable salt or ester thereof, and at least selected from an insulin sensitivity enhancer, an insulin secretagogue, a biguanide, an insulin preparation, and a DPP-IV inhibitor. A pharmaceutical composition comprising a combination of a kind of drugs.
[式中、Aは下記一般式(A1)、(A2)又は(A3)
を示し、R1及びR2はそれぞれ同一若しくは異なって、C1-6アルキル基、ヒドロキシメチル基、C1-6アルコキシメチル基又はC1-6ハロアルキル基を示し、R3、R4、R5及びR6はそれぞれ同一若しくは異なって、C1-6アルキル基、C1-6アルコキシ基、C1-6ヒドロキシアルキル基、C1-6ハロアルキル基、アミノ基(該アミノ基はC1-6アルキル基又はC1-6ヒドロキシアルキル基で1又は2個置換されていてもよい) 、水酸基、水素原子又はハロゲン原子を示し、R7はC1-6アルキル基、C1-6アルコキシ基、C1-6ヒドロキシアルキル基、C1-6ハロアルキル基、水酸基又は水素原子を示し、nは1又は2の整数を示す。] で表わされる化合物又はその薬理上許容される塩若しくはエステルから選ばれるα‐アミラーゼ阻害剤と、インスリン感受性増強剤、インスリン分泌促進剤、ビグアナイド剤及びインスリン製剤から選ばれる薬剤の少なくとも一種とを組み合わせてなる医薬組成物。 The following general formula (I)
[Wherein A represents the following general formula (A1), (A2) or (A3)
R 1 and R 2 are the same or different and each represents a C 1-6 alkyl group, a hydroxymethyl group, a C 1-6 alkoxymethyl group or a C 1-6 haloalkyl group, and R 3 , R 4 , R 5 and R 6 are the same or different and each represents a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 hydroxyalkyl group, a C1-6 haloalkyl group, an amino group (the amino group is a C1-6 alkyl group or a C1-6 hydroxy group). 1 or 2 may be substituted with an alkyl group), a hydroxyl group, a hydrogen atom or a halogen atom, R 7 is a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 hydroxyalkyl group, C1-6 A haloalkyl group, a hydroxyl group or a hydrogen atom; n represents an integer of 1 or 2; Or a pharmacologically acceptable salt or ester thereof and an at least one drug selected from an insulin sensitivity enhancer, an insulin secretagogue, a biguanide, and an insulin preparation. A pharmaceutical composition.
である請求項1乃至6に記載の医薬組成物。 A is the following general formula (A1)
The pharmaceutical composition according to any one of claims 1 to 6.
[式中、Aは下記一般式(A1)、(A2)又は(A3)
を示し、R1及びR2はそれぞれ同一若しくは異なって、C1-6アルキル基、ヒドロキシメチル基、C1-6アルコキシメチル基又はC1-6ハロアルキル基を示し、R3、R4、R5及びR6はそれぞれ同一若しくは異なって、C1-6アルキル基、C1-6アルコキシ基、C1-6ヒドロキシアルキル基、C1-6ハロアルキル基、アミノ基(該アミノ基はC1-6アルキル基又はC1-6ヒドロキシアルキル基で1又は2個置換されていてもよい) 、水酸基、水素原子又はハロゲン原子を示し、R7はC1-6アルキル基、C1-6アルコキシ基、C1-6ヒドロキシアルキル基、C1-6ハロアルキル基、水酸基又は水素原子を示し、nは1又は2の整数を示す。] で表わされる化合物又はその薬理上許容される塩若しくはエステルから選ばれるα‐アミラーゼ阻害剤と、インスリン感受性増強剤、インスリン分泌促進剤、ビグアナイド剤、インスリン製剤及びDPP-IV阻害剤から選ばれる少なくとも一種の薬剤とを組み合わせてなる医薬組成物を製造するための、α‐アミラーゼ阻害剤と、インスリン感受性増強剤、インスリン分泌促進剤、ビグアナイド剤、インスリン製剤及びDPP-IV阻害剤から選ばれる薬剤の使用。 The following general formula (I)
[Wherein A represents the following general formula (A1), (A2) or (A3)
R 1 and R 2 are the same or different and each represents a C 1-6 alkyl group, a hydroxymethyl group, a C 1-6 alkoxymethyl group or a C 1-6 haloalkyl group, and R 3 , R 4 , R 5 and R 6 are the same or different and each represents a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 hydroxyalkyl group, a C1-6 haloalkyl group, an amino group (the amino group is a C1-6 alkyl group or a C1-6 hydroxy group). 1 or 2 may be substituted with an alkyl group), a hydroxyl group, a hydrogen atom or a halogen atom, R 7 is a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 hydroxyalkyl group, C1-6 A haloalkyl group, a hydroxyl group or a hydrogen atom; n represents an integer of 1 or 2; An α-amylase inhibitor selected from the compounds represented by the formula (I) or a pharmacologically acceptable salt or ester thereof, and at least selected from an insulin sensitivity enhancer, an insulin secretagogue, a biguanide, an insulin preparation, and a DPP-IV inhibitor. An α-amylase inhibitor and an agent selected from an insulin sensitivity enhancer, an insulin secretagogue, a biguanide, an insulin preparation and a DPP-IV inhibitor for producing a pharmaceutical composition comprising a combination of one kind of drug use.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2005219763A JP2006063074A (en) | 2004-07-29 | 2005-07-29 | Medicinal composition containing diabetes therapeutic agent |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2004222419 | 2004-07-29 | ||
JP2005219763A JP2006063074A (en) | 2004-07-29 | 2005-07-29 | Medicinal composition containing diabetes therapeutic agent |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2006063074A JP2006063074A (en) | 2006-03-09 |
JP2006063074A5 true JP2006063074A5 (en) | 2008-09-04 |
Family
ID=36109854
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2005219763A Pending JP2006063074A (en) | 2004-07-29 | 2005-07-29 | Medicinal composition containing diabetes therapeutic agent |
Country Status (1)
Country | Link |
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JP (1) | JP2006063074A (en) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR3017536B1 (en) * | 2014-02-18 | 2017-05-26 | Univ La Rochelle | COMPOSITIONS FOR THE PREVENTION AND / OR TREATMENT OF ALPHA GLUCOSIDASE PATHOLOGIES |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH02215394A (en) * | 1989-02-14 | 1990-08-28 | Nippon Shinyaku Co Ltd | Production of moranoline derivative |
JP2000044589A (en) * | 1998-08-03 | 2000-02-15 | Kikkoman Corp | Maltooligosaccharide derivative and its use |
JP3909735B2 (en) * | 1999-02-22 | 2007-04-25 | キッコーマン株式会社 | Maltooligosaccharide derivatives and uses thereof |
JP4373671B2 (en) * | 2000-06-06 | 2009-11-25 | キッコーマン株式会社 | Maltooligosaccharide derivatives and uses thereof |
-
2005
- 2005-07-29 JP JP2005219763A patent/JP2006063074A/en active Pending
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