JP2010077163A5 - - Google Patents
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- Publication number
- JP2010077163A5 JP2010077163A5 JP2010006181A JP2010006181A JP2010077163A5 JP 2010077163 A5 JP2010077163 A5 JP 2010077163A5 JP 2010006181 A JP2010006181 A JP 2010006181A JP 2010006181 A JP2010006181 A JP 2010006181A JP 2010077163 A5 JP2010077163 A5 JP 2010077163A5
- Authority
- JP
- Japan
- Prior art keywords
- cycloalkyl
- cycloheteroalkyl
- alkyl
- amino
- hydrogen atom
- 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.)
- Granted
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- -1 tricycloalkyl Chemical group 0.000 claims 38
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 28
- 125000000753 cycloalkyl group Chemical group 0.000 claims 25
- 125000000217 alkyl group Chemical group 0.000 claims 24
- 125000003342 alkenyl group Chemical group 0.000 claims 20
- 125000000304 alkynyl group Chemical group 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 20
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000003710 aryl alkyl group Chemical group 0.000 claims 18
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 15
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 15
- 125000004949 alkyl amino carbonyl amino group Chemical group 0.000 claims 15
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 15
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 15
- 125000005843 halogen group Chemical group 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 15
- 125000003545 alkoxy group Chemical group 0.000 claims 14
- 125000004658 aryl carbonyl amino group Chemical group 0.000 claims 14
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims 12
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 12
- 239000003112 inhibitor Substances 0.000 claims 11
- 125000005162 aryl oxy carbonyl amino group Chemical group 0.000 claims 10
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 10
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 8
- 150000001602 bicycloalkyls Chemical group 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 125000005350 hydroxycycloalkyl group Chemical group 0.000 claims 8
- 229940124597 therapeutic agent Drugs 0.000 claims 7
- 102100038129 Transcription factor Dp family member 3 Human genes 0.000 claims 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 5
- 125000002252 acyl group Chemical group 0.000 claims 5
- 125000005089 alkenylaminocarbonyl group Chemical group 0.000 claims 5
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 5
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 5
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 5
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 5
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 5
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims 5
- 125000006350 alkyl thio alkyl group Chemical group 0.000 claims 5
- 125000004414 alkyl thio group Chemical group 0.000 claims 5
- 125000005095 alkynylaminocarbonyl group Chemical group 0.000 claims 5
- 125000001091 aminosulfinyl group Chemical group [H]N([H])S(*)=O 0.000 claims 5
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 5
- 239000003472 antidiabetic agent Substances 0.000 claims 5
- 125000001769 aryl amino group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 238000010276 construction Methods 0.000 claims 5
- 125000004663 dialkyl amino group Chemical group 0.000 claims 5
- 150000002148 esters Chemical class 0.000 claims 5
- 125000004438 haloalkoxy group Chemical group 0.000 claims 5
- 125000005241 heteroarylamino group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 125000004430 oxygen atom Chemical group O* 0.000 claims 5
- 125000005592 polycycloalkyl group Polymers 0.000 claims 5
- 125000006684 polyhaloalkyl group Polymers 0.000 claims 5
- 229940002612 prodrug Drugs 0.000 claims 5
- 239000000651 prodrug Substances 0.000 claims 5
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 5
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000004434 sulfur atom Chemical group 0.000 claims 5
- 208000011580 syndromic disease Diseases 0.000 claims 5
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 5
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 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 4
- 150000002632 lipids Chemical class 0.000 claims 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 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
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- QGJUIPDUBHWZPV-SGTAVMJGSA-N saxagliptin Chemical compound 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
- 229960004937 saxagliptin Drugs 0.000 claims 3
- 108010033693 saxagliptin Proteins 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 2
- 102000004877 Insulin Human genes 0.000 claims 2
- 108090001061 Insulin Proteins 0.000 claims 2
- 208000008589 Obesity 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
- 239000000556 agonist Substances 0.000 claims 2
- 229940127003 anti-diabetic drug Drugs 0.000 claims 2
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims 2
- 208000037824 growth disorder Diseases 0.000 claims 2
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 2
- 201000008980 hyperinsulinism Diseases 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 229940125396 insulin Drugs 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000008194 pharmaceutical composition 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
- 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 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical compound O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-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
- DDYAPMZTJAYBOF-ZMYDTDHYSA-N (3S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(2S,3S)-1-[[(1S)-1-carboxyethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-4-oxobutanoic acid Chemical class [H]N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)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)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O DDYAPMZTJAYBOF-ZMYDTDHYSA-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
- BOVGTQGAOIONJV-BETUJISGSA-N 1-[(3ar,6as)-3,3a,4,5,6,6a-hexahydro-1h-cyclopenta[c]pyrrol-2-yl]-3-(4-methylphenyl)sulfonylurea Chemical compound C1=CC(C)=CC=C1S(=O)(=O)NC(=O)NN1C[C@H]2CCC[C@H]2C1 BOVGTQGAOIONJV-BETUJISGSA-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
- 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
- QBQLYIISSRXYKL-UHFFFAOYSA-N 4-[[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]phenyl]methyl]-1,2-oxazolidine-3,5-dione Chemical compound CC=1OC(C=2C=CC=CC=2)=NC=1CCOC(C=C1)=CC=C1CC1C(=O)NOC1=O QBQLYIISSRXYKL-UHFFFAOYSA-N 0.000 claims 1
- NFFXEUUOMTXWCX-UHFFFAOYSA-N 5-[(2,4-dioxo-1,3-thiazolidin-5-yl)methyl]-2-methoxy-n-[[4-(trifluoromethyl)phenyl]methyl]benzamide Chemical compound C1=C(C(=O)NCC=2C=CC(=CC=2)C(F)(F)F)C(OC)=CC=C1CC1SC(=O)NC1=O NFFXEUUOMTXWCX-UHFFFAOYSA-N 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 claims 1
- 208000000103 Anorexia Nervosa Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 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
- RKWGIWYCVPQPMF-UHFFFAOYSA-N Chloropropamide Chemical compound CCCNC(=O)NS(=O)(=O)C1=CC=C(Cl)C=C1 RKWGIWYCVPQPMF-UHFFFAOYSA-N 0.000 claims 1
- 108010036824 Citrate (pro-3S)-lyase Proteins 0.000 claims 1
- 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 1
- 108010011459 Exenatide Proteins 0.000 claims 1
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 1
- GGUVRMBIEPYOKL-WMVCGJOFSA-N GW 409544 Chemical compound C([C@H](NC(/C)=C\C(=O)C=1C=CC=CC=1)C(O)=O)C(C=C1)=CC=C1OCCC(=C(O1)C)N=C1C1=CC=CC=C1 GGUVRMBIEPYOKL-WMVCGJOFSA-N 0.000 claims 1
- HEMJJKBWTPKOJG-UHFFFAOYSA-N Gemfibrozil Chemical compound CC1=CC=C(C)C(OCCCC(C)(C)C(O)=O)=C1 HEMJJKBWTPKOJG-UHFFFAOYSA-N 0.000 claims 1
- 108010088406 Glucagon-Like Peptides Proteins 0.000 claims 1
- 102400000322 Glucagon-like peptide 1 Human genes 0.000 claims 1
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 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(N)=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 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 1
- FAEKWTJYAYMJKF-QHCPKHFHSA-N GlucoNorm Chemical compound C1=C(C(O)=O)C(OCC)=CC(CC(=O)N[C@@H](CC(C)C)C=2C(=CC=CC=2)N2CCCCC2)=C1 FAEKWTJYAYMJKF-QHCPKHFHSA-N 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 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
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 229940122355 Insulin sensitizer Drugs 0.000 claims 1
- 102000000853 LDL receptors Human genes 0.000 claims 1
- 108010001831 LDL receptors Proteins 0.000 claims 1
- 229940086609 Lipase inhibitor Drugs 0.000 claims 1
- 239000000867 Lipoxygenase Inhibitor Substances 0.000 claims 1
- 229940122142 Lipoxygenase inhibitor Drugs 0.000 claims 1
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| JP4504924B2 (ja) * | 2002-12-20 | 2010-07-14 | メルク・シャープ・エンド・ドーム・コーポレイション | 糖尿病の治療および予防のためのジペプチジルペプチダーゼ阻害薬としての３−アミノ−４−フェニルブタン酸誘導体 |
| US20040242566A1 (en) * | 2003-03-25 | 2004-12-02 | Syrrx, Inc. | Dipeptidyl peptidase inhibitors |
| US7371871B2 (en) | 2003-05-05 | 2008-05-13 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| NZ572274A (en) | 2003-05-05 | 2009-06-26 | Probiodrug Ag | Use of effectors of glutaminyl and glutamate cyclases |
| MXPA05011861A (es) | 2003-05-05 | 2006-02-17 | Probiodrug Ag | Uso de efectores de ciclasas de glutamato y glutaminil. |
| JP2007511467A (ja) | 2003-05-14 | 2007-05-10 | タケダ サン ディエゴ インコーポレイテッド | ジペプチジルペプチダーゼインヒビター |
| US7459474B2 (en) | 2003-06-11 | 2008-12-02 | Bristol-Myers Squibb Company | Modulators of the glucocorticoid receptor and method |
| US6995183B2 (en) * | 2003-08-01 | 2006-02-07 | Bristol Myers Squibb Company | Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods |
| MXPA06001601A (es) * | 2003-08-13 | 2006-08-25 | Takeda Pharmaceutical | Derivados de 4-pirimidona y su uso como inhibidores de dipeptidilpeptidasa. |
| US7169926B1 (en) | 2003-08-13 | 2007-01-30 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7678909B1 (en) | 2003-08-13 | 2010-03-16 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7205409B2 (en) * | 2003-09-04 | 2007-04-17 | Abbott Laboratories | Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) |
| US20050065144A1 (en) * | 2003-09-08 | 2005-03-24 | Syrrx, Inc. | Dipeptidyl peptidase inhibitors |
| WO2005026148A1 (en) * | 2003-09-08 | 2005-03-24 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| US7371759B2 (en) * | 2003-09-25 | 2008-05-13 | Bristol-Myers Squibb Company | HMG-CoA reductase inhibitors and method |
| EA010108B1 (ru) | 2003-10-15 | 2008-06-30 | Пробиодруг Аг | Применение эффекторов глутаминил- и глутаматциклаз |
| CA2544573A1 (en) | 2003-11-03 | 2005-06-02 | Probiodrug Ag | Combinations useful for the treatment of neuronal disorders |
| US7576121B2 (en) * | 2003-11-12 | 2009-08-18 | Phenomix Corporation | Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| US7767828B2 (en) * | 2003-11-12 | 2010-08-03 | Phenomix Corporation | Methyl and ethyl substituted pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| DK1689757T3 (en) | 2003-11-12 | 2014-12-08 | Sino Med Internat Alliance Inc | HETEROCYCLIC DRY ACID COMPOUNDS |
| US7317109B2 (en) * | 2003-11-12 | 2008-01-08 | Phenomix Corporation | Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| KR20120008093A (ko) | 2003-11-17 | 2012-01-25 | 노파르티스 아게 | 디펩티딜 펩티다제 ⅳ 억제제의 용도 |
| US20070149451A1 (en) * | 2003-11-17 | 2007-06-28 | Holmes David G | Combination of a dpp IV inhibitor and an antiobesity or appetite regulating agent |
| US7420059B2 (en) * | 2003-11-20 | 2008-09-02 | Bristol-Myers Squibb Company | HMG-CoA reductase inhibitors and method |
| ES2684325T5 (es) | 2004-01-20 | 2024-06-10 | Novartis Ag | Formulación y proceso de compresión directa |
| US7470810B2 (en) | 2004-01-21 | 2008-12-30 | Bristol-Myers Squibb Company | Alkyl and aryl-thiotrifluoroacetates and process |
| WO2005073186A1 (ja) * | 2004-01-29 | 2005-08-11 | Ono Pharmaceutical Co., Ltd. | ピロリジン誘導体 |
| CN101684089A (zh) * | 2004-02-05 | 2010-03-31 | 杏林制药株式会社 | 双环酯类衍生物 |
| KR101099206B1 (ko) | 2004-02-05 | 2011-12-27 | 프로비오드룩 아게 | 신규한 글루타미닐 시클라제 저해제 |
| AU2005212073B2 (en) * | 2004-02-18 | 2010-07-08 | Kyorin Pharmaceutical Co., Ltd. | Bicyclic amide derivatives |
| US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
| US7514571B2 (en) * | 2004-02-27 | 2009-04-07 | Kyorin Pharmaceutical Co., Ltd. | Bicyclo derivative |
| US20070238753A1 (en) * | 2004-02-27 | 2007-10-11 | Madar David J | Pharmaceutical Compositions as Inhibitors of Dipeptidyl Peptidase-IV (DPP-IV) |
| US7732446B1 (en) | 2004-03-11 | 2010-06-08 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| CN102127057A (zh) * | 2004-03-15 | 2011-07-20 | 武田药品工业株式会社 | 二肽基肽酶抑制剂 |
| TW200534879A (en) * | 2004-03-25 | 2005-11-01 | Bristol Myers Squibb Co | Coated tablet formulation and method |
| TW200538122A (en) * | 2004-03-31 | 2005-12-01 | Bristol Myers Squibb Co | Process for preparing a dipeptidyl peptidase Ⅳ inhibitor and intermediates employed therein |
| US7741082B2 (en) | 2004-04-14 | 2010-06-22 | Bristol-Myers Squibb Company | Process for preparing dipeptidyl peptidase IV inhibitors and intermediates therefor |
| US7829720B2 (en) | 2004-05-04 | 2010-11-09 | Bristol-Myers Squibb Company | Process for preparing atazanavir bisulfate and novel forms |
| US20050256314A1 (en) * | 2004-05-04 | 2005-11-17 | Soojin Kim | Process employing controlled crystallization in forming crystals of a pharmaceutical |
| TW200536827A (en) * | 2004-05-04 | 2005-11-16 | Bristol Myers Squibb Co | Enzymatic ammonolysis process for the preparation of intermediates for DPP IV inhibitors |
| US7214702B2 (en) * | 2004-05-25 | 2007-05-08 | Bristol-Myers Squibb Company | Process for producing a dipeptidyl peptidase IV inhibitor |
| TWI415635B (zh) | 2004-05-28 | 2013-11-21 | 必治妥施貴寶公司 | 加衣錠片調製物及製備彼之方法 |
| WO2005118555A1 (en) * | 2004-06-04 | 2005-12-15 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US9889110B2 (en) | 2004-06-07 | 2018-02-13 | University Of Tennessee Research Foundation | Selective androgen receptor modulator for treating hormone-related conditions |
| US9884038B2 (en) | 2004-06-07 | 2018-02-06 | University Of Tennessee Research Foundation | Selective androgen receptor modulator and methods of use thereof |
| US7572805B2 (en) | 2004-07-14 | 2009-08-11 | Bristol-Myers Squibb Company | Pyrrolo(oxo)isoquinolines as 5HT ligands |
| WO2006019965A2 (en) | 2004-07-16 | 2006-02-23 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| AU2005267093B2 (en) * | 2004-07-23 | 2009-10-01 | Nuada Llc | Peptidase inhibitors |
| TW200608967A (en) | 2004-07-29 | 2006-03-16 | Sankyo Co | Pharmaceutical compositions containing with diabetic agent |
| US20060035954A1 (en) * | 2004-08-11 | 2006-02-16 | Sharma Padam N | Ammonolysis process for the preparation of intermediates for DPP IV inhibitors |
| AR051446A1 (es) * | 2004-09-23 | 2007-01-17 | Bristol Myers Squibb Co | Glucosidos de c-arilo como inhibidores selectivos de transportadores de glucosa (sglt2) |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| EP1828192B1 (en) * | 2004-12-21 | 2014-12-03 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| US7589088B2 (en) * | 2004-12-29 | 2009-09-15 | Bristol-Myers Squibb Company | Pyrimidine-based inhibitors of dipeptidyl peptidase IV and methods |
| US7635699B2 (en) * | 2004-12-29 | 2009-12-22 | Bristol-Myers Squibb Company | Azolopyrimidine-based inhibitors of dipeptidyl peptidase IV and methods |
| DOP2006000008A (es) | 2005-01-10 | 2006-08-31 | Arena Pharm Inc | Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1 |
| JP2008024592A (ja) * | 2005-01-28 | 2008-02-07 | Taisho Pharmaceut Co Ltd | シアノピロリジン誘導体含有固形製剤用組成物、それを含有する固形製剤及びその製造方法 |
| EP1846410B1 (en) * | 2005-02-10 | 2009-01-21 | Bristol-Myers Squibb Company | Dihydroquinazolinones as 5ht modulators |
| JP2008115080A (ja) * | 2005-04-22 | 2008-05-22 | Taisho Pharmaceutical Co Ltd | 併用医薬 |
| US7521557B2 (en) | 2005-05-20 | 2009-04-21 | Bristol-Myers Squibb Company | Pyrrolopyridine-based inhibitors of dipeptidyl peptidase IV and methods |
| US20060264433A1 (en) * | 2005-05-23 | 2006-11-23 | Backes Bradley J | Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) |
| US7825139B2 (en) * | 2005-05-25 | 2010-11-02 | Forest Laboratories Holdings Limited (BM) | Compounds and methods for selective inhibition of dipeptidyl peptidase-IV |
| MY152185A (en) | 2005-06-10 | 2014-08-29 | Novartis Ag | Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation |
| WO2007016353A2 (en) * | 2005-07-28 | 2007-02-08 | Bristol-Myers Squibb Company | Substituted tetrahydro-1h-pyrido[4,3,b]indoles as serotonin receptor agonists and antagonists |
| DE102005035891A1 (de) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| TW200738245A (en) * | 2005-08-22 | 2007-10-16 | Sankyo Co | Pharmaceutical composition containing FBPase inhibitor |
| US7795436B2 (en) * | 2005-08-24 | 2010-09-14 | Bristol-Myers Squibb Company | Substituted tricyclic heterocycles as serotonin receptor agonists and antagonists |
| EP1931199A4 (en) | 2005-08-31 | 2009-07-29 | Univ Tennessee Res Foundation | COMBATING NURSE DISEASE, BURNS, WOUNDS AND BACKMARK INJURIES WITH SELECTIVE ANDROGEN RECEPTOR MODULATORS |
| US20070060529A1 (en) * | 2005-09-14 | 2007-03-15 | Christopher Ronald J | Administration of dipeptidyl peptidase inhibitors |
| SI1942898T2 (sl) * | 2005-09-14 | 2014-08-29 | Takeda Pharmaceutical Company Limited | Dipeptidil-peptidazni inhibitorji za zdravljenje diabetesa |
| SI1931350T2 (sl) * | 2005-09-14 | 2021-11-30 | Takeda Pharmaceutical Company Limited | Uporaba inhibitorjev dipeptidil peptidaze |
| EP1924567B1 (en) | 2005-09-16 | 2012-08-22 | Takeda Pharmaceutical Company Limited | Process for the preparation of pyrimidinedione derivatives |
| TW200745080A (en) * | 2005-09-16 | 2007-12-16 | Takeda Pharmaceuticals Co | Polymorphs of tartrate salt of 2-[2-(3-(R)-amino-piperidin-1-yl)-5-fluoro-6-oxo-6H-pyrimidin-1-ylmethyl]-benzonitrile and methods of use therefor |
| TW200745079A (en) * | 2005-09-16 | 2007-12-16 | Takeda Pharmaceuticals Co | Polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and methods of use therefor |
| TW200738266A (en) * | 2005-09-29 | 2007-10-16 | Sankyo Co | Pharmaceutical agent containing insulin resistance improving agent |
| WO2007053819A2 (en) | 2005-10-31 | 2007-05-10 | Bristol-Myers Squibb Company | Pyrrolidinyl beta-amino amide-based inhibitors of dipeptidyl peptidase iv and methods |
| EP1971614A1 (en) | 2005-11-14 | 2008-09-24 | Probiodrug AG | Cyclopropyl-fused pyrrolidine derivatives as dipeptidyl peptidase iv inhibitors |
| GB0526291D0 (en) * | 2005-12-23 | 2006-02-01 | Prosidion Ltd | Therapeutic method |
| WO2007102286A1 (ja) * | 2006-03-08 | 2007-09-13 | Kyorin Pharmaceutical Co., Ltd. | アミノアセチルピロリジンカルボニトリル誘導体の製造方法およびその製造中間体 |
| RU2465264C2 (ru) * | 2006-03-16 | 2012-10-27 | Вертекс Фармасьютикалз Инкорпорейтед | Дейтерированные ингибиторы протеазы гепатита с |
| WO2007112347A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| JP2009531456A (ja) * | 2006-03-28 | 2009-09-03 | 武田薬品工業株式会社 | （ｒ）−３−アミノピペリジン二塩酸塩の調製 |
| US20070238770A1 (en) * | 2006-04-05 | 2007-10-11 | Bristol-Myers Squibb Company | Process for preparing novel crystalline forms of peliglitazar, novel stable forms produced therein and formulations |
| PE20071221A1 (es) | 2006-04-11 | 2007-12-14 | Arena Pharm Inc | Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas |
| DE602007010420D1 (de) | 2006-04-11 | 2010-12-23 | Arena Pharm Inc | Verfahren zur verwendung des gpr119-rezeptors zur identifizierung von verbindungen zur erhöhung der knochenmasse bei einer person |
| AU2007235876A1 (en) | 2006-04-12 | 2007-10-18 | Probiodrug Ag | Enzyme inhibitors |
| US20090281331A1 (en) * | 2006-04-17 | 2009-11-12 | Sumitomo Chemical Company, Limited | Method of producing polycyclic proline derivative or acid addition salt thereof |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| BRPI0711558A2 (pt) | 2006-05-04 | 2011-11-08 | Boeringer Ingelheim Internat Gmbh | polimorfos |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| US7919598B2 (en) | 2006-06-28 | 2011-04-05 | Bristol-Myers Squibb Company | Crystal structures of SGLT2 inhibitors and processes for preparing same |
| CA2658394C (en) | 2006-07-12 | 2016-08-16 | University Of Tennessee Research Foundation | Substituted acylanilides and methods of use thereof |
| US9844528B2 (en) | 2006-08-24 | 2017-12-19 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| US9730908B2 (en) | 2006-08-24 | 2017-08-15 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| BRPI0716134A2 (pt) | 2006-09-07 | 2013-09-17 | Nycomed Gmbh | tratamento de combinaÇço para diabetes mellitus |
| JO2945B1 (en) * | 2006-09-13 | 2016-03-15 | سميث كلاين بيتشام كوربوريشن | Methods of giving prolonged hypoglycemic agents |
| RS51965B (sr) * | 2006-09-13 | 2012-02-29 | Takeda Pharmaceutical Company Limited | Upotreba 2-6-(3-amino-piperidin-1-il)-3-metil-2,4-diokso-3,4-dihidro-2h-pirimidin-1-ilmetil-4-fluoro-benzonitrila za lečenje dijabetesa, kancera, autoimunih poremećaja i hiv infekcije |
| US8324383B2 (en) | 2006-09-13 | 2012-12-04 | Takeda Pharmaceutical Company Limited | Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile |
| CN101594878A (zh) | 2006-09-18 | 2009-12-02 | 雷普特药品公司 | 通过给予受体相关蛋白（rap）-缀合物对肝病症的治疗 |
| WO2008055945A1 (en) | 2006-11-09 | 2008-05-15 | Probiodrug Ag | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
| US8217025B2 (en) * | 2006-11-17 | 2012-07-10 | Harbor Therapeutics, Inc. | Drug screening and treatment methods |
| TW200838536A (en) * | 2006-11-29 | 2008-10-01 | Takeda Pharmaceutical | Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor |
| EP2091948B1 (en) | 2006-11-30 | 2012-04-18 | Probiodrug AG | Novel inhibitors of glutaminyl cyclase |
| US9623021B2 (en) | 2007-01-22 | 2017-04-18 | Gtx, Inc. | Nuclear receptor binding agents |
| US9604931B2 (en) | 2007-01-22 | 2017-03-28 | Gtx, Inc. | Nuclear receptor binding agents |
| BRPI0806371A2 (pt) | 2007-01-22 | 2011-09-13 | Gtx Inc | agentes ligação de receptor nuclear |
| CN101230058A (zh) * | 2007-01-23 | 2008-07-30 | 上海恒瑞医药有限公司 | 双环氮杂烷类衍生物、其制备方法及其在医药上的用途 |
| ME01239B (me) | 2007-02-01 | 2013-06-20 | Takeda Pharmaceuticals Co | Čvrsti preparat koji sadrži alogliptin i pioglitazon |
| US20110020797A1 (en) * | 2007-02-09 | 2011-01-27 | Bristol-Myers Squibb Company | Methods For Identifying Patients With An Increased Likelihood Of Responding To DPP-IV Inhibitors |
| US8093236B2 (en) | 2007-03-13 | 2012-01-10 | Takeda Pharmaceuticals Company Limited | Weekly administration of dipeptidyl peptidase inhibitors |
| US20080064701A1 (en) * | 2007-04-24 | 2008-03-13 | Ramesh Sesha | Anti-diabetic combinations |
| EP2123636B1 (en) * | 2007-03-22 | 2012-03-21 | Kyorin Pharmaceutical Co., Ltd. | Method for producing aminoacetylpyrrolidinecarbonitrile derivative |
| TW200904405A (en) | 2007-03-22 | 2009-02-01 | Bristol Myers Squibb Co | Pharmaceutical formulations containing an SGLT2 inhibitor |
| ES2529149T3 (es) | 2007-04-03 | 2015-02-17 | Mitsubishi Tanabe Pharma Corporation | Una combinación de inhibidor de dipeptidil peptidasa IV y edulcorante para uso en el tratamiento de la obesidad |
| US9656991B2 (en) | 2007-04-18 | 2017-05-23 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| PE20090696A1 (es) * | 2007-04-20 | 2009-06-20 | Bristol Myers Squibb Co | Formas cristalinas de saxagliptina y procesos para preparar las mismas |
| US20080287529A1 (en) * | 2007-05-18 | 2008-11-20 | Bristol-Myers Squibb Company | Crystal structures of sglt2 inhibitors and processes for preparing same |
| CN101318925A (zh) * | 2007-06-04 | 2008-12-10 | 上海恒瑞医药有限公司 | 吡咯烷并四元环类衍生物、其制备方法及其在医药上的用途 |
| EA021544B1 (ru) | 2007-06-04 | 2015-07-30 | Бен-Гурион Юниверсити Оф Дзе Негев Рисерч Энд Дивелопмент Оторити | Триарильные соединения и фармацевтические композиции, их содержащие |
| PT2178513E (pt) * | 2007-06-22 | 2011-05-31 | Bristol Myers Squibb Co | Composi??es em comprimido que cont?m atazanavir |
| EP2178512B1 (en) * | 2007-06-22 | 2011-03-09 | Bristol-Myers Squibb Company | Tableted compositions containing atazanavir |
| JP2010530889A (ja) * | 2007-06-22 | 2010-09-16 | ブリストル−マイヤーズ スクイブ カンパニー | アタザナビルを含む錠剤組成物 |
| JP2010530888A (ja) * | 2007-06-22 | 2010-09-16 | ブリストル−マイヤーズ スクイブ カンパニー | アタザナビルを含む錠剤組成物 |
| PE20090938A1 (es) | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo |
| CA2696579C (en) * | 2007-08-17 | 2017-01-24 | Boehringer Ingelheim International Gmbh | Purine derivatives for use in the treatment of fab-related diseases |
| US7968603B2 (en) | 2007-09-11 | 2011-06-28 | University Of Tennessee Research Foundation | Solid forms of selective androgen receptor modulators |
| US20090076118A1 (en) * | 2007-09-13 | 2009-03-19 | Protia, Llc | Deuterium-enriched saxagliptin |
| GB2465132B (en) * | 2007-09-21 | 2012-06-06 | Lupin Ltd | Compounds as dipeptidyl peptidase IV (DPP IV) inhibitors |
| CL2008003653A1 (es) | 2008-01-17 | 2010-03-05 | Mitsubishi Tanabe Pharma Corp | Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica. |
| US8551524B2 (en) * | 2008-03-14 | 2013-10-08 | Iycus, Llc | Anti-diabetic combinations |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| EP2146210A1 (en) | 2008-04-07 | 2010-01-20 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY |
| EP2993239A1 (en) | 2008-05-16 | 2016-03-09 | AstraZeneca AB | Methods for identifying subjects with an increased likelihood of responding to dpp-iv inhibitors |
| PE20100156A1 (es) * | 2008-06-03 | 2010-02-23 | Boehringer Ingelheim Int | Tratamiento de nafld |
| US8003689B2 (en) | 2008-06-20 | 2011-08-23 | Gtx, Inc. | Metabolites of selective androgen receptor modulators and methods of use thereof |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| WO2010016584A1 (ja) * | 2008-08-07 | 2010-02-11 | 杏林製薬株式会社 | ビシクロ[２．２．２]オクチルアミン誘導体の製造方法 |
| CA2733778A1 (en) * | 2008-08-14 | 2010-02-18 | Hiroshi Uchida | Stabilized pharmaceutical composition |
| NZ604091A (en) | 2008-08-15 | 2014-08-29 | Boehringer Ingelheim Int | Purin derivatives for use in the treatment of fab-related diseases |
| BRPI0919288A2 (pt) | 2008-09-10 | 2015-12-15 | Boehring Ingelheim Internat Gmbh | teriapia de combinação para tratamento de diabetes e condições relacionadas. |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| HUE068164T2 (hu) | 2008-10-17 | 2024-12-28 | Sanofi Aventis Deutschland | Egy inzulin és egy GLP-1 agonista kombinációja |
| WO2010054326A2 (en) | 2008-11-07 | 2010-05-14 | The General Hospital Corporation | C-terminal fragments of glucagon-like peptide-1 (glp-1) |
| JP2012509277A (ja) * | 2008-11-19 | 2012-04-19 | オースペックス・ファーマシューティカルズ・インコーポレイテッド | ジペプチジルペプチダーゼｉｖのヒドロキシアダマンチル阻害剤 |
| US20100144140A1 (en) * | 2008-12-10 | 2010-06-10 | Novellus Systems, Inc. | Methods for depositing tungsten films having low resistivity for gapfill applications |
| DE102008062136B4 (de) | 2008-12-16 | 2012-05-03 | Kamamed Ug | Pharmazeutische Zusammensetzung auf Basis von Peptid aus Kamelmilch |
| AU2009331471B2 (en) | 2008-12-23 | 2015-09-03 | Boehringer Ingelheim International Gmbh | Salt forms of organic compound |
| AR074990A1 (es) | 2009-01-07 | 2011-03-02 | Boehringer Ingelheim Int | Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina |
| US8706650B2 (en) * | 2009-01-14 | 2014-04-22 | Integral Analytics, Inc. | Optimization of microgrid energy use and distribution |
| AR075204A1 (es) | 2009-01-29 | 2011-03-16 | Boehringer Ingelheim Int | Inhibidores de dpp-4 y composiciones farmaceuticas que los comprenden, utiles para tratar enfermedades metabolicas en pacientes pediatricos, particularmente diabetes mellitus tipo 2 |
| PE20120017A1 (es) | 2009-02-13 | 2012-02-12 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un inhibidor de sglt2, un inhibidor de dpp-iv, opcionalmente, un agente antidiabetico adicional, y sus usos |
| MX2011008416A (es) | 2009-02-13 | 2011-09-08 | Boehringer Ingelheim Int | Medicaciones antidiabeticas que comprenden un inhibidor de dpp-4 (linagliptina) opcionalmente en combinacion con otros antidiabeticos. |
| KR20110135411A (ko) * | 2009-03-27 | 2011-12-16 | 브리스톨-마이어스 스큅 컴퍼니 | Ｄｐｐ-ｉｖ 억제제로 주요 유해 심장혈관 이벤트를 예방하는 방법 |
| CA2756428A1 (en) | 2009-03-27 | 2010-09-30 | Mamoru Fukuda | Matrix-type sustained release preparation containing basic additive |
| KR101292379B1 (ko) * | 2009-04-08 | 2013-08-09 | 브리스톨-마이어스 스큅 컴퍼니 | Ｐｄｈ 및 ｆｄｈ 효소를 발현하는 유전적으로 안정한 플라스미드 |
| CN102459170B (zh) | 2009-04-09 | 2014-07-23 | 桑多斯股份公司 | 沙格列汀的结晶形式 |
| US8748457B2 (en) | 2009-06-18 | 2014-06-10 | Lupin Limited | 2-amino-2- [8-(dimethyl carbamoyl)- 8-aza- bicyclo [3.2.1] oct-3-yl]-exo- ethanoyl derivatives as potent DPP-IV inhibitors |
| AR077642A1 (es) | 2009-07-09 | 2011-09-14 | Arena Pharm Inc | Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo |
| ES2548913T3 (es) | 2009-09-11 | 2015-10-21 | Probiodrug Ag | Derivados heterocíclicos como inhibidores de glutaminil ciclasa |
| EP2308847B1 (en) | 2009-10-09 | 2014-04-02 | EMC microcollections GmbH | Substituted pyridines as inhibitors of dipeptidyl peptidase IV and their application for the treatment of diabetes and related diseases |
| CA2780460C (en) | 2009-11-13 | 2018-09-04 | Sanofi-Aventis Deutschland Gmbh | Pharmaceutical composition comprising a glp-1 agonist, an insulin and methionine |
| ES2693686T3 (es) | 2009-11-13 | 2018-12-13 | Astrazeneca Ab | Formulaciones de comprimidos de liberación inmediata |
| SG10201500871TA (en) | 2009-11-13 | 2015-04-29 | Sanofi Aventis Deutschland | Pharmaceutical composition comprising a glp-1 agonist and methionine |
| JP5775522B2 (ja) | 2009-11-13 | 2015-09-09 | アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ | 二層錠製剤 |
| PH12012501037A1 (en) | 2009-11-27 | 2013-01-14 | Boehringer Ingelheim Int | Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin |
| TWI562775B (en) | 2010-03-02 | 2016-12-21 | Lexicon Pharmaceuticals Inc | Methods of using inhibitors of sodium-glucose cotransporters 1 and 2 |
| WO2011107530A2 (en) | 2010-03-03 | 2011-09-09 | Probiodrug Ag | Novel inhibitors |
| CA2789440C (en) | 2010-03-10 | 2020-03-24 | Probiodrug Ag | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
| JP2013522279A (ja) | 2010-03-18 | 2013-06-13 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 糖尿病及び関連状態の治療で用いるｇｐｒ１１９作動薬とｄｄｐ−ｉｖ阻害薬リナグリプチンの組合せ |
| EP2368874A1 (en) | 2010-03-26 | 2011-09-28 | Sandoz AG | Racemisation of (R)-N-Boc-3-hydroxyadamant-1-yl glycine |
| WO2011125011A1 (en) * | 2010-04-05 | 2011-10-13 | Cadila Pharmaceuticals Limited | Novel hypoglycemic compounds |
| WO2011127051A1 (en) | 2010-04-06 | 2011-10-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| JP5945532B2 (ja) | 2010-04-21 | 2016-07-05 | プロビオドルグ エージー | グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体 |
| CA2797310C (en) | 2010-05-05 | 2020-03-31 | Boehringer Ingelheim International Gmbh | Glp-1 receptor agonist and dpp-4 inhibitor combination therapy |
| WO2011140328A1 (en) | 2010-05-05 | 2011-11-10 | Teva Pharmaceutical Industries Ltd. | Saxagliptin intermediates, saxagliptin polymorphs, and processes for preparation thereof |
| KR20230051307A (ko) | 2010-06-24 | 2023-04-17 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 요법 |
| WO2012017029A1 (en) | 2010-08-06 | 2012-02-09 | Sandoz Ag | Novel salts of saxagrliptin with organic di-acids |
| EP2601175A1 (en) | 2010-08-06 | 2013-06-12 | Sandoz AG | A novel crystalline compound comprising saxagliptin and phosphoric acid |
| RS55378B1 (sr) | 2010-08-30 | 2017-03-31 | Sanofi Aventis Deutschland | Upotreba ave0010 za proizvodnju leka za tretman diabetes mellitus tipa 2 |
| EP2611442B1 (en) | 2010-09-03 | 2018-07-04 | Bristol-Myers Squibb Company | Drug formulations using water soluble antioxidants |
| WO2012028721A1 (en) | 2010-09-03 | 2012-03-08 | Sandoz Ag | PROCESS FOR THE REDUCTIVE AMINATION OF α-KETO CARBOXYLIC ACIDS |
| US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
| MX2013003184A (es) | 2010-09-22 | 2013-06-07 | Arena Pharm Inc | Moduladores del receptor gpr119 y el tratamiento de transtornos relacionados con el mismo. |
| US20120077778A1 (en) | 2010-09-29 | 2012-03-29 | Andrea Bourdelais | Ladder-Frame Polyether Conjugates |
| EP2608788A1 (en) | 2010-10-04 | 2013-07-03 | Assia Chemical Industries Ltd. | Polymorphs of saxagliptin hydrochloride and processes for preparing them |
| US9040481B2 (en) | 2010-11-02 | 2015-05-26 | The General Hospital Corporation | Methods for treating steatotic disease |
| US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
| 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 |
| RS54735B1 (sr) | 2011-01-31 | 2016-10-31 | Cadila Healthcare Ltd | Tretman za lipodistrofiju |
| BR112013019026A2 (pt) | 2011-02-01 | 2016-10-04 | Astrazeneca Uk Ltd | formulações farmacêuticas incluindo um composto amina |
| US8530670B2 (en) | 2011-03-16 | 2013-09-10 | Probiodrug Ag | Inhibitors |
| WO2012135570A1 (en) | 2011-04-01 | 2012-10-04 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2012145361A1 (en) | 2011-04-19 | 2012-10-26 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| WO2012145603A1 (en) | 2011-04-22 | 2012-10-26 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| US20140051714A1 (en) | 2011-04-22 | 2014-02-20 | Arena Pharmaceuticals, Inc. | Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto |
| US9821032B2 (en) | 2011-05-13 | 2017-11-21 | Sanofi-Aventis Deutschland Gmbh | Pharmaceutical combination for improving glycemic control as add-on therapy to basal insulin |
| WO2012170702A1 (en) | 2011-06-08 | 2012-12-13 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| EP2729157B1 (en) | 2011-07-06 | 2019-01-16 | The General Hospital Corporation | A pentapeptide derived from the c-terminus of glucagon-like peptide 1 (glp-1) for use in treatment |
| ES2713566T3 (es) | 2011-07-15 | 2019-05-22 | Boehringer Ingelheim Int | Derivado de quinazolina dimérico sustituido, su preparación y su uso en composiciones farmacéuticas para el tratamiento de la diabetes de tipo I y II |
| BR112014004726A2 (pt) | 2011-08-29 | 2017-04-04 | Sanofi Aventis Deutschland | combinação farmacêutica para uso no controle glicêmico em pacientes de diabetes tipo 2 |
| TWI559929B (en) | 2011-09-01 | 2016-12-01 | Sanofi Aventis Deutschland | Pharmaceutical composition for use in the treatment of a neurodegenerative disease |
| WO2013036213A1 (en) | 2011-09-07 | 2013-03-14 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Dpp-iv inhibitor formulations |
| PL2578208T3 (pl) | 2011-10-06 | 2014-10-31 | Sanovel Ilac Sanayi Ve Ticaret As | Stałe formulacje dawkowane inhibitora DPP-IV |
| WO2013055910A1 (en) | 2011-10-12 | 2013-04-18 | Arena Pharmaceuticals, Inc. | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| JPWO2013081100A1 (ja) * | 2011-11-30 | 2015-04-27 | 積水メディカル株式会社 | アダマンチルヒダントイン化合物 |
| US9115082B2 (en) | 2012-01-18 | 2015-08-25 | Catherine Yang | Dipeptidyl-peptidase-IV inhibitors for treatment of type 2 diabetes complex with hypertension |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| WO2013160354A1 (en) | 2012-04-25 | 2013-10-31 | Enantia, S.L. | Crystalline forms of saxagliptin |
| EP4151218A1 (en) | 2012-05-14 | 2023-03-22 | Boehringer Ingelheim International GmbH | Linagliptin, a xanthine derivative as dpp-4 inhibitor, for use in the treatment of sirs and/or sepsis |
| US20130303462A1 (en) | 2012-05-14 | 2013-11-14 | Boehringer Ingelheim International Gmbh | Use of a dpp-4 inhibitor in podocytes related disorders and/or nephrotic syndrome |
| US8664443B2 (en) | 2012-05-23 | 2014-03-04 | Divi's Laboratories Ltd. | Process for the preparation of (1S, 3S, 5S)-2-[2(S)-2-amino-2-(3-hydroxy-1-adamantan-1-yl) acetyl]-2-azabicyclo [3.1.0] hexane-3-carbonitrile |
| ES2690321T3 (es) | 2012-05-24 | 2018-11-20 | Apotex Inc. | Sales de saxagliptina con ácidos orgánicos |
| WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
| EP2867206A2 (en) | 2012-07-02 | 2015-05-06 | Ranbaxy Laboratories Limited | Saxagliptin salts |
| CN103539724B (zh) * | 2012-07-12 | 2017-09-26 | 博瑞生物医药（苏州）股份有限公司 | 沙格列汀单一立体异构体的新晶型和纯化方法 |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| US9969683B2 (en) | 2012-07-13 | 2018-05-15 | Gtx, Inc. | Method of treating estrogen receptor (ER)-positive breast cancers with selective androgen receptor modulator (SARMS) |
| US10987334B2 (en) | 2012-07-13 | 2021-04-27 | University Of Tennessee Research Foundation | Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs) |
| US9744149B2 (en) | 2012-07-13 | 2017-08-29 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| US10258596B2 (en) | 2012-07-13 | 2019-04-16 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| IN2015DN01046A (enExample) | 2012-07-13 | 2015-06-26 | Gtx Inc | |
| US9622992B2 (en) | 2012-07-13 | 2017-04-18 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| WO2014030051A1 (en) | 2012-08-23 | 2014-02-27 | Aurobindo Pharma Limited | Stable pharmaceutical compositions comprising saxagliptin |
| WO2014057495A1 (en) | 2012-10-11 | 2014-04-17 | Lee Pharma Limited | A process for industrial preparation of [(s)-n-tert butoxycarbonyl-3-hydroxy]adamantylglycine |
| TWI500613B (zh) | 2012-10-17 | 2015-09-21 | Cadila Healthcare Ltd | 新穎之雜環化合物 |
| WO2014074668A1 (en) | 2012-11-08 | 2014-05-15 | Arena Pharmaceuticals, Inc. | Modulators of gpr119 and the treatment of disorders related thereto |
| UA117574C2 (uk) | 2012-11-20 | 2018-08-27 | Лексікон Фармасьютікалз, Інк. | Інгібітори котранспортера натрій-глюкози 1 |
| WO2014096983A1 (en) | 2012-12-21 | 2014-06-26 | Wockhardt Limited | Stable pharmaceutical compositions of saxagliptin or salts thereof |
| US20150250734A1 (en) | 2012-12-21 | 2015-09-10 | Wockhardt Limited | Stable pharmaceutical compositions of saxagliptin or salts thereof |
| WO2014108830A1 (en) | 2013-01-10 | 2014-07-17 | Wockhardt Limited | A process for preparing pharmaceutically acceptable salt of saxagliptin |
| ITMI20130132A1 (it) | 2013-01-30 | 2014-07-31 | Laboratorio Chimico Int Spa | Procedimento per la preparazione di intermedi di sintesi di saxagliptina e nuovi composti |
| TWI641381B (zh) | 2013-02-04 | 2018-11-21 | 法商賽諾菲公司 | 胰島素類似物及／或胰島素衍生物之穩定化醫藥調配物 |
| US8652527B1 (en) | 2013-03-13 | 2014-02-18 | Upsher-Smith Laboratories, Inc | Extended-release topiramate capsules |
| US9101545B2 (en) | 2013-03-15 | 2015-08-11 | Upsher-Smith Laboratories, Inc. | Extended-release topiramate capsules |
| CN104059068B (zh) * | 2013-03-20 | 2017-02-08 | 中国科学院上海药物研究所 | β‑氨基羰基类化合物、其制备方法、药物组合物及其用途 |
| CN104098481B (zh) * | 2013-04-10 | 2016-05-11 | 浙江九洲药物科技有限公司 | 一种沙格列汀中间体的制备方法 |
| EA201592020A1 (ru) | 2013-04-22 | 2016-05-31 | Кадила Хелзкэр Лимитед | Новая композиция для неалкогольной жировой болезни печени (нажбп) |
| WO2014193528A1 (en) * | 2013-04-29 | 2014-12-04 | Anovel Pharmaceuticals, Llc | Amorphous dosage forms and methods |
| ES2889916T3 (es) | 2013-05-30 | 2022-01-14 | Cadila Healthcare Ltd | Un procedimiento para la preparación de pirroles con actividades hipolipidémicas e hipocolesterémicas |
| EP4424697A3 (en) | 2013-06-05 | 2024-12-25 | Bausch Health Ireland Limited | Ultra-pure agonists of guanylate cyclase c, method of making and using same |
| TW201513857A (zh) | 2013-07-05 | 2015-04-16 | Cadila Healthcare Ltd | 協同性組成物 |
| IN2013MU02470A (enExample) | 2013-07-25 | 2015-06-26 | Cadila Healthcare Ltd | |
| EP2832723B1 (en) | 2013-07-29 | 2017-02-15 | Zentiva, a.s. | Stabilised amorphous forms of Saxagliptin |
| IN2013MU02813A (enExample) | 2013-08-28 | 2015-07-03 | Amneal Pharmaceuticals Llc | |
| WO2015033357A2 (en) | 2013-09-06 | 2015-03-12 | Cadila Healthcare Limited | An improved process for the preparation of pyrrole derivatives |
| ITMI20131677A1 (it) * | 2013-10-10 | 2015-04-11 | Olon Spa | Procedimento per la preparazione di saxagliptina |
| AU2014347668A1 (en) | 2013-11-05 | 2016-05-19 | Ben-Gurion University Of The Negev Research And Development Authority | Compounds for the treatment of diabetes and disease complications arising from same |
| WO2015067223A1 (en) | 2013-11-06 | 2015-05-14 | Zentiva, K., S. | L-tartrate salt of (1s,3s,5s)-2-[(2s)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl) acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile and process for preparation thereof |
| WO2015071887A1 (en) | 2013-11-18 | 2015-05-21 | Ranbaxy Laboratories Limited | Oral pharmaceutical compositions of saxagliptin |
| WO2015071889A1 (en) | 2013-11-18 | 2015-05-21 | Ranbaxy Laboratories Limited | Oral compositions of saxagliptin |
| WO2015087262A1 (en) | 2013-12-11 | 2015-06-18 | Ranbaxy Laboratories Limited | Process for the preparation of saxagliptin and its intermediates |
| EP3091995B1 (en) | 2014-01-09 | 2024-03-20 | Sanofi | Stabilized pharmaceutical formulations of insulin aspart |
| WO2015104311A1 (en) | 2014-01-09 | 2015-07-16 | Sanofi | Stabilized glycerol free pharmaceutical formulations of insulin analogues and/or insulin derivatives |
| SG11201604706TA (en) | 2014-01-09 | 2016-07-28 | Sanofi Sa | Stabilized pharmaceutical formulations of insulin aspart |
| EP3110449B1 (en) | 2014-02-28 | 2023-06-28 | Boehringer Ingelheim International GmbH | Medical use of a dpp-4 inhibitor |
| CZ2014177A3 (cs) * | 2014-03-24 | 2015-10-07 | Zentiva, K.S. | Způsob výroby saxagliptinu |
| JP6649902B2 (ja) | 2014-05-30 | 2020-02-19 | ファイザー・インク | 選択的アンドロゲン受容体モジュレーターとしてのカルボニトリル誘導体 |
| WO2016016770A1 (en) | 2014-07-26 | 2016-02-04 | Wockhardt Limited | A novel modified release pharmaceutical composition of sitagliptin or pharmaceutically acceptable salt thereof |
| GB201415598D0 (en) | 2014-09-03 | 2014-10-15 | Univ Birmingham | Elavated Itercranial Pressure Treatment |
| TWI758239B (zh) | 2014-12-12 | 2022-03-21 | 德商賽諾菲阿凡提斯德意志有限公司 | 甘精胰島素/利司那肽固定比率配製劑 |
| CN104557667A (zh) * | 2014-12-12 | 2015-04-29 | 山东省药学科学院 | 2-氰基吡咯烷类化合物、制备方法及其应用 |
| CA2979033A1 (en) | 2015-03-09 | 2016-09-15 | Intekrin Therapeutics, Inc. | Methods for the treatment of nonalcoholic fatty liver disease and/or lipodystrophy |
| TWI748945B (zh) | 2015-03-13 | 2021-12-11 | 德商賽諾菲阿凡提斯德意志有限公司 | 第２型糖尿病病患治療 |
| TW201705975A (zh) | 2015-03-18 | 2017-02-16 | 賽諾菲阿凡提斯德意志有限公司 | 第２型糖尿病病患之治療 |
| CN105037245B (zh) * | 2015-08-03 | 2017-04-12 | 沧州那瑞化学科技有限公司 | 一种沙格列汀中间体的制备方法 |
| WO2017064635A2 (en) | 2015-10-14 | 2017-04-20 | Cadila Healthcare Limited | Pyrrole compound, compositions and process for preparation thereof |
| KR101715682B1 (ko) | 2015-10-29 | 2017-03-13 | 경동제약 주식회사 | 삭사글립틴의 제조를 위한 신규 중간체, 이의 제조방법 및 이를 이용한 삭사글립틴의 제조방법 |
| WO2017211979A1 (en) | 2016-06-10 | 2017-12-14 | Boehringer Ingelheim International Gmbh | Combinations of linagliptin and metformin |
| US11096924B2 (en) | 2016-09-07 | 2021-08-24 | Trustees Of Tufts College | Combination therapies using immuno-dash inhibitors and PGE2 antagonists |
| BR112019011740A2 (pt) | 2016-12-09 | 2019-10-29 | Cadila Healthcare Limited | composição farmacêutica e método para o tratamento de colangite biliar primária |
| WO2018162722A1 (en) | 2017-03-09 | 2018-09-13 | Deutsches Institut Für Ernährungsforschung Potsdam-Rehbrücke | Dpp-4 inhibitors for use in treating bone fractures |
| CN110996951A (zh) | 2017-04-03 | 2020-04-10 | 科赫罗斯生物科学股份有限公司 | 治疗进行性核上性麻痹的PPARγ激动剂 |
| EP3461819B1 (en) | 2017-09-29 | 2020-05-27 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
| CN109970620B (zh) * | 2017-12-27 | 2022-07-12 | 江苏威凯尔医药科技有限公司 | 一种制备沙格列汀中间体的方法 |
| CA3103425A1 (en) | 2018-06-14 | 2019-12-19 | Robert Peter PRYBOLSKY | Methods for lowering blood sugar with a dipeptidyl peptidase-4 inhibitor pharmaceutical composition |
| BR112021000139A2 (pt) | 2018-07-19 | 2021-04-06 | Astrazeneca Ab | Métodos de tratamento da hfpef empregando dapagliflozina e composições compreendendo a mesma |
| SG11202102498UA (en) | 2018-09-26 | 2021-04-29 | Lexicon Pharmaceuticals Inc | Crystalline forms of n-(1 -((2-(dimethylamino)ethyl)amino)-2-m ethyl-1 -oopropan-2-yl)-4-(4-(2-methyl-5- (2s,3r,4r,5s,6r)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2h-pyran-2-yl)benzyl) phenl)butanamide and methods of their synthesis |
| RU2712097C1 (ru) * | 2018-09-28 | 2020-01-24 | Общество с ограниченной ответственностью "Необиотек" | Ингибитор дипептидилпептидазы-4 для лечения сахарного диабета 2-го типа, соединения (варианты) |
| RU2727898C1 (ru) * | 2020-02-25 | 2020-07-24 | Общество с ограниченной ответственностью «Необиотек» | Фармацевтическая композиция на основе действующего вещества, ингибитора дипептидилпептидазы-4, для предупреждения развития и лечения сахарного диабета 2 типа |
| US12409186B2 (en) | 2020-07-27 | 2025-09-09 | Astrazeneca Ab | Methods of treating chronic kidney disease with dapagliflozin |
| WO2023275715A1 (en) | 2021-06-30 | 2023-01-05 | Pfizer Inc. | Metabolites of selective androgen receptor modulators |
| CN113666846B (zh) * | 2021-08-31 | 2023-06-27 | 济南立德医药技术有限公司 | 沙格列汀中间体的合成方法 |
| 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 |
| WO2025090919A1 (en) * | 2023-10-25 | 2025-05-01 | Piton Therapeutics, Inc. | Compositions and methods for treating inflammatory bowel disease |
Family Cites Families (90)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3325478A (en) * | 1964-11-17 | 1967-06-13 | Du Pont | alpha-amino-1-adamantylmethyl penicillins |
| US3674836A (en) | 1968-05-21 | 1972-07-04 | Parke Davis & Co | 2,2-dimethyl-{11 -aryloxy-alkanoic acids and salts and esters thereof |
| US4027009A (en) | 1973-06-11 | 1977-05-31 | Merck & Co., Inc. | Compositions and methods for depressing blood serum cholesterol |
| JPS5246949B2 (enExample) | 1973-10-19 | 1977-11-29 | ||
| YU36151B (en) * | 1974-05-16 | 1982-02-25 | Pliva Zagreb | Process for preparing alpha-amino-2-adamantyl acetic acid |
| JPS5612114B2 (enExample) | 1974-06-07 | 1981-03-18 | ||
| US4183857A (en) | 1978-07-06 | 1980-01-15 | Shell Oil Company | 3-Benzyl-3-azabicyclo(3.1.0)hexane-2,4-dione |
| NO154918C (no) | 1977-08-27 | 1987-01-14 | Bayer Ag | Analogifremgangsmaate til fremstilling av terapeutisk aktive derivater av 3,4,5-trihydroksypiperidin. |
| CA1117127A (en) | 1978-06-27 | 1982-01-26 | Janet A. Day | Derivatives of 3-azabicyclo(3.1.0)hexane and a process for their preparation |
| US4231938A (en) | 1979-06-15 | 1980-11-04 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
| DE2951135A1 (de) | 1979-12-19 | 1981-06-25 | Hoechst Ag, 6230 Frankfurt | Sulfonylharnstoffe, verfahren zu ihrer herstellung, pharmazeutische praeparate auf basis dieser verbindungen und ihre verwendung |
| DK149080C (da) | 1980-06-06 | 1986-07-28 | Sankyo Co | Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre |
| US4450171A (en) | 1980-08-05 | 1984-05-22 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
| US4448784A (en) | 1982-04-12 | 1984-05-15 | Hoechst-Roussel Pharmaceuticals, Inc. | 1-(Aminoalkylphenyl and aminoalkylbenzyl)-indoles and indolines and analgesic method of use thereof |
| US5354772A (en) | 1982-11-22 | 1994-10-11 | Sandoz Pharm. Corp. | Indole analogs of mevalonolactone and derivatives thereof |
| DE3324263A1 (de) | 1983-07-06 | 1985-01-17 | Hoechst Ag, 6230 Frankfurt | Derivate der 2-azabicyclo(3.1.0)hexan-3-carbonsaeure, verfahren zu ihrer herstellung, diese enthaltende mittel und deren verwendung sowie 2-azabicyclo(3.1.0)hexan-derivate als zwischenprodukte und verfahren zu deren herstellung |
| JPS6051189A (ja) | 1983-08-30 | 1985-03-22 | Sankyo Co Ltd | チアゾリジン誘導体およびその製造法 |
| DE3536687A1 (de) | 1985-10-15 | 1987-04-16 | Hoechst Ag | Verfahren zur behandlung von atherosklerose, thrombose und der peripheren gefaesskrankheit |
| DE3543999A1 (de) | 1985-12-13 | 1987-06-19 | Bayer Ag | Hochreine acarbose |
| US5614492A (en) | 1986-05-05 | 1997-03-25 | The General Hospital Corporation | Insulinotropic hormone GLP-1 (7-36) and uses thereof |
| US4681893A (en) | 1986-05-30 | 1987-07-21 | Warner-Lambert Company | Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis |
| US4759923A (en) | 1987-06-25 | 1988-07-26 | Hercules Incorporated | Process for lowering serum cholesterol using poly(diallylmethylamine) derivatives |
| JP2569746B2 (ja) | 1987-08-20 | 1997-01-08 | 日産化学工業株式会社 | キノリン系メバロノラクトン類 |
| US4924024A (en) | 1988-01-11 | 1990-05-08 | E. R. Squibb & Sons, Inc. | Phosphorus-containing squalene synthetase inhibitors, new intermediates and method |
| US4871721A (en) | 1988-01-11 | 1989-10-03 | E. R. Squibb & Sons, Inc. | Phosphorus-containing squalene synthetase inhibitors |
| NO177005C (no) | 1988-01-20 | 1995-07-05 | Bayer Ag | Analogifremgangsmåte for fremstilling av substituerte pyridiner, samt mellomprodukter til bruk ved fremstillingen |
| FI94339C (fi) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
| DE3926606A1 (de) | 1989-08-11 | 1991-02-14 | Hoechst Ag | Verfahren zur behandlung der cardialen sowie der vasculaeren hypertrophie und hyperplasie |
| US5462928A (en) | 1990-04-14 | 1995-10-31 | New England Medical Center Hospitals, Inc. | Inhibitors of dipeptidyl-aminopeptidase type IV |
| US5177080A (en) | 1990-12-14 | 1993-01-05 | Bayer Aktiengesellschaft | Substituted pyridyl-dihydroxy-heptenoic acid and its salts |
| JP2648897B2 (ja) | 1991-07-01 | 1997-09-03 | 塩野義製薬株式会社 | ピリミジン誘導体 |
| ES2153831T3 (es) | 1991-10-22 | 2001-03-16 | New England Medical Center Inc | Inhibidores de dipeptidil-aminopeptidasa de tipo iv. |
| US5595872A (en) | 1992-03-06 | 1997-01-21 | Bristol-Myers Squibb Company | Nucleic acids encoding microsomal trigyceride transfer protein |
| DK36392D0 (da) | 1992-03-19 | 1992-03-19 | Novo Nordisk As | Anvendelse af kemisk forbindelse |
| US5447954A (en) | 1992-05-05 | 1995-09-05 | Smithkline Beecham P.L.C. | Phenylderivate as inhibitors of ATP citrate lyase |
| US5712396A (en) | 1992-10-28 | 1998-01-27 | Magnin; David R. | α-phosphonosulfonate squalene synthetase inhibitors |
| US5594016A (en) | 1992-12-28 | 1997-01-14 | Mitsubishi Chemical Corporation | Naphthalene derivatives |
| SG45369A1 (en) | 1993-01-19 | 1998-10-16 | Warner Lambert Co | Stable oral ci-981 formulation and process of preparing same |
| US5346701A (en) | 1993-02-22 | 1994-09-13 | Theratech, Inc. | Transmucosal delivery of macromolecular drugs |
| US5739135A (en) | 1993-09-03 | 1998-04-14 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| US5484944A (en) * | 1993-10-27 | 1996-01-16 | Neurogen Corporation | Certain fused pyrrolecarboxanilides and their use as GABA brain receptor ligands |
| IL111785A0 (en) | 1993-12-03 | 1995-01-24 | Ferring Bv | Dp-iv inhibitors and pharmaceutical compositions containing them |
| US5776983A (en) | 1993-12-21 | 1998-07-07 | Bristol-Myers Squibb Company | Catecholamine surrogates useful as β3 agonists |
| US5488064A (en) | 1994-05-02 | 1996-01-30 | Bristol-Myers Squibb Company | Benzo 1,3 dioxole derivatives |
| US5385929A (en) | 1994-05-04 | 1995-01-31 | Warner-Lambert Company | [(Hydroxyphenylamino) carbonyl] pyrroles |
| US5561146A (en) | 1994-06-10 | 1996-10-01 | Bristol-Myers Squibb Company | Modified guanidino and amidino thrombin inhibitors |
| US5491134A (en) | 1994-09-16 | 1996-02-13 | Bristol-Myers Squibb Company | Sulfonic, phosphonic or phosphiniic acid β3 agonist derivatives |
| US5541204A (en) | 1994-12-02 | 1996-07-30 | Bristol-Myers Squibb Company | Aryloxypropanolamine β 3 adrenergic agonists |
| US5620997A (en) | 1995-05-31 | 1997-04-15 | Warner-Lambert Company | Isothiazolones |
| MX9709874A (es) | 1995-06-06 | 1998-03-31 | Pfizer | N-(INDOL-2-CARBONIL) beta-ALANILAMIDAS SUSTITUIDAS Y DERIVADOS COMO INHIBIDORES DE GLUCOGENO FOSFORILASA, USO DE LOS MISMOS Y COMPOSICIONES QUE LOS CONTIENEN. |
| JP3314938B2 (ja) | 1995-06-06 | 2002-08-19 | ファイザー・インコーポレーテッド | グリコーゲンホスホリラーゼ抑制剤としての置換されたｎ−（インドール−２−カルボニル）−グリシンアミド類および誘導体 |
| WO1997012613A1 (en) | 1995-10-05 | 1997-04-10 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| CZ121298A3 (cs) | 1995-10-25 | 1998-07-15 | E. I. Du Pont De Nemours And Company | Herbicidní sulfonamidy |
| EP0873361B1 (en) | 1995-12-13 | 2006-11-02 | The Regents Of The University Of California | Crystals of the ligand-binding domain of the thyroid hormone receptor complexed to a ligand |
| US5770615A (en) | 1996-04-04 | 1998-06-23 | Bristol-Myers Squibb Company | Catecholamine surrogates useful as β3 agonists |
| DE19616486C5 (de) | 1996-04-25 | 2016-06-30 | Royalty Pharma Collection Trust | Verfahren zur Senkung des Blutglukosespiegels in Säugern |
| US5962440A (en) | 1996-05-09 | 1999-10-05 | Bristol-Myers Squibb Company | Cyclic phosphonate ester inhibitors of microsomal triglyceride transfer protein and method |
| US5885983A (en) | 1996-05-10 | 1999-03-23 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| US5827875A (en) | 1996-05-10 | 1998-10-27 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| HRP970330B1 (en) | 1996-07-08 | 2004-06-30 | Bayer Ag | Cycloalkano pyridines |
| TW492957B (en) * | 1996-11-07 | 2002-07-01 | Novartis Ag | N-substituted 2-cyanopyrrolidnes |
| US6011155A (en) | 1996-11-07 | 2000-01-04 | Novartis Ag | N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| US5952322A (en) | 1996-12-05 | 1999-09-14 | Pfizer Inc. | Method of reducing tissue damage associated with non-cardiac ischemia using glycogen phosphorylase inhibitors |
| US5760246A (en) | 1996-12-17 | 1998-06-02 | Biller; Scott A. | Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method |
| GB9713739D0 (en) | 1997-06-27 | 1997-09-03 | Karobio Ab | Thyroid receptor ligands |
| DE19742601A1 (de) * | 1997-09-26 | 1999-04-29 | Siemens Ag | Verfahren und Vorrichtung zur Erzeugung von Rahmen um Videobilder |
| UA57811C2 (uk) | 1997-11-21 | 2003-07-15 | Пфайзер Продактс Інк. | Фармацевтична композиція, що містить інгібітор альдозоредуктази та інгібітор глікогенфосфорилази (варіанти), комплект, який її включає, та способи лікування ссавців зі станом інсулінорезистентності |
| US6803357B1 (en) | 1998-02-02 | 2004-10-12 | New England Medical Center Hospitals, Inc. | Method of regulating glucose metabolism, and reagents related thereto |
| TR200002480T2 (tr) | 1998-02-27 | 2000-12-21 | Pfizer Products Inc. | İzaşemi tedavisi için guanidin türevleri |
| US5998463A (en) | 1998-02-27 | 1999-12-07 | Pfizer Inc | Glycogen phosphorylase inhibitors |
| RU2274642C2 (ru) * | 1998-03-19 | 2006-04-20 | Вертекс Фармасьютикалз Инкорпорейтед | Ингибиторы каспаз |
| DE19828114A1 (de) | 1998-06-24 | 2000-01-27 | Probiodrug Ges Fuer Arzneim | Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV |
| EP0978279A1 (en) | 1998-08-07 | 2000-02-09 | Pfizer Products Inc. | Inhibitors of human glycogen phosphorylase |
| IL141471A0 (en) | 1998-08-21 | 2002-03-10 | Point Therapeutics Inc | Regulation of substrate activity |
| CO5150173A1 (es) | 1998-12-10 | 2002-04-29 | Novartis Ag | Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv |
| WO2000038722A1 (en) | 1998-12-23 | 2000-07-06 | G.D. Searle & Co. | COMBINATIONS OF CHOLESTERYL ESTER TRANSFER PROTEIN INHIBITORS AND HMG CoA REDUCTASE INHIBITORS FOR CARDIOVASCULAR INDICATIONS |
| AU760174B2 (en) | 1999-02-09 | 2003-05-08 | Bristol-Myers Squibb Company | Lactam inhibitors of FXa and method |
| AU2535700A (en) | 1999-02-12 | 2000-08-29 | Novo Nordisk A/S | Use of pyrrolidine derivatives for the manufacture of a pharmaceutical composition for the treatment or prophylaxis of obesity or appetite regulation |
| AU3960400A (en) | 1999-03-05 | 2000-09-28 | Molteni L. E C. Dei Fratelli Alitti Societa' Di Esercizio S.P.A. | Use of metformin in the preparation of pharmaceutical compositions capable of inhibiting the enzyme dipeptidyl peptidase iv |
| GB9906714D0 (en) | 1999-03-23 | 1999-05-19 | Ferring Bv | Compositions for improving fertility |
| GB9906715D0 (en) | 1999-03-23 | 1999-05-19 | Ferring Bv | Compositions for promoting growth |
| ES2215570T3 (es) | 1999-04-01 | 2004-10-16 | Pfizer Products Inc. | Compuestos para tratar y prevenir complicaciones diabeticas. |
| JP4121215B2 (ja) | 1999-05-17 | 2008-07-23 | 財団法人微生物化学研究会 | スルフォスチン類縁体、並びにスルフォスチン及びその類縁体の製造方法 |
| US6110949A (en) | 1999-06-24 | 2000-08-29 | Novartis Ag | N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| US6395767B2 (en) * | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
| JP2004518688A (ja) | 2001-01-30 | 2004-06-24 | ブリストル−マイヤーズ スクイブ カンパニー | ファクターＸａ阻害剤のスルホンアミドラクタムおよびその方法 |
| DE10132375A1 (de) | 2001-07-07 | 2003-01-16 | Trench Germany Gmbh | Verfahren und Vorrichtung zur Herstellung eines elektrischen Kunststoffisolators |
| WO2006034175A1 (en) | 2004-09-17 | 2006-03-30 | Albemarle Corporation | Synthesis process for 2-(3-hydroxy-1-adamantyl)-2-oxoacetic acid |
| US7205432B2 (en) | 2005-05-31 | 2007-04-17 | Kemfine Oy | Process for the preparation of adamantane derivatives |
| CA2612338C (en) | 2005-06-17 | 2015-02-03 | Apogee Biotechnology Corporation | Sphingosine kinase inhibitors |
-
2001
- 2001-02-16 US US09/788,173 patent/US6395767B2/en not_active Ceased
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