JP2011509922A5 - - Google Patents
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- JP2011509922A5 JP2011509922A5 JP2010528230A JP2010528230A JP2011509922A5 JP 2011509922 A5 JP2011509922 A5 JP 2011509922A5 JP 2010528230 A JP2010528230 A JP 2010528230A JP 2010528230 A JP2010528230 A JP 2010528230A JP 2011509922 A5 JP2011509922 A5 JP 2011509922A5
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- JP
- Japan
- Prior art keywords
- group
- ring
- alkyl
- heteroaryl
- acceptable salt
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims description 195
- 125000000623 heterocyclic group Chemical group 0.000 claims description 93
- 125000003118 aryl group Chemical group 0.000 claims description 82
- 125000001072 heteroaryl group Chemical group 0.000 claims description 73
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 70
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 66
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 66
- 150000003839 salts Chemical class 0.000 claims description 58
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 56
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 56
- 125000003545 alkoxy group Chemical group 0.000 claims description 39
- 125000001424 substituent group Chemical group 0.000 claims description 36
- 229940090124 dipeptidyl peptidase 4 (dpp-4) inhibitors for blood glucose lowering Drugs 0.000 claims description 31
- 125000005843 halogen group Chemical group 0.000 claims description 30
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 23
- 125000005018 aryl alkenyl group Chemical group 0.000 claims description 22
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 22
- 229910052731 fluorine Inorganic materials 0.000 claims description 19
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 18
- 150000001875 compounds Chemical class 0.000 claims description 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 17
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 125000002252 acyl group Chemical group 0.000 claims description 13
- 239000001257 hydrogen Substances 0.000 claims description 13
- 125000003282 alkyl amino group Chemical group 0.000 claims description 12
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims description 12
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 11
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims description 11
- 125000003003 spiro group Chemical group 0.000 claims description 11
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 10
- 229910052801 chlorine Inorganic materials 0.000 claims description 10
- 239000011737 fluorine Substances 0.000 claims description 10
- 229910052757 nitrogen Chemical group 0.000 claims description 10
- -1 methylenedioxy group Chemical group 0.000 claims description 9
- 239000000651 prodrug Substances 0.000 claims description 7
- 229940002612 prodrug Drugs 0.000 claims description 7
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- 125000004432 carbon atom Chemical group C* 0.000 claims description 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- 239000005977 Ethylene Substances 0.000 claims description 4
- 229940049964 oleate Drugs 0.000 claims description 4
- 125000002619 bicyclic group Chemical group 0.000 claims 34
- 229940121377 sodium-glucose co-transporter inhibitor Drugs 0.000 claims 24
- 125000002950 monocyclic group Chemical group 0.000 claims 19
- 125000004122 cyclic group Chemical group 0.000 claims 16
- 206010012601 diabetes mellitus Diseases 0.000 claims 13
- 239000008280 blood Substances 0.000 claims 12
- 210000004369 blood Anatomy 0.000 claims 12
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 claims 10
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims 10
- 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 10
- 229960004034 sitagliptin Drugs 0.000 claims 10
- MFFMDFFZMYYVKS-SECBINFHSA-N sitagliptin Chemical compound 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 10
- 125000003277 amino group Chemical group 0.000 claims 8
- 150000002430 hydrocarbons Chemical group 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 150000001555 benzenes Chemical group 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 208000024891 symptom Diseases 0.000 claims 5
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- UTFVDMCHZXTLTA-PFKOEMKTSA-N (2r,3r,4s,5s,6r)-2-[3-[(4-cyclopropylphenyl)methyl]-4,6-difluoroindol-1-yl]-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1N1C2=CC(F)=CC(F)=C2C(CC=2C=CC(=CC=2)C2CC2)=C1 UTFVDMCHZXTLTA-PFKOEMKTSA-N 0.000 claims 2
- PXRGAWZIQZMHTH-PFKOEMKTSA-N (2r,3r,4s,5s,6r)-2-[3-[(4-cyclopropylphenyl)methyl]-4-fluoroindol-1-yl]-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1N1C2=CC=CC(F)=C2C(CC=2C=CC(=CC=2)C2CC2)=C1 PXRGAWZIQZMHTH-PFKOEMKTSA-N 0.000 claims 2
- OWXVLYMIZSXRHK-OSKXVONFSA-N (2s,3r,4r,5s,6r)-2-[4-chloro-3-[[5-(6-fluoropyridin-2-yl)thiophen-2-yl]methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(Cl)C(CC=2SC(=CC=2)C=2N=C(F)C=CC=2)=C1 OWXVLYMIZSXRHK-OSKXVONFSA-N 0.000 claims 2
- WQWNUPFPUXHKAQ-OSKXVONFSA-N (2s,3r,4r,5s,6r)-2-[4-chloro-3-[[5-(6-fluoropyridin-3-yl)thiophen-2-yl]methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(Cl)C(CC=2SC(=CC=2)C=2C=NC(F)=CC=2)=C1 WQWNUPFPUXHKAQ-OSKXVONFSA-N 0.000 claims 2
- XTNGUQKDFGDXSJ-ZXGKGEBGSA-N Canagliflozin Chemical compound CC1=CC=C([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)O)C=C1CC(S1)=CC=C1C1=CC=C(F)C=C1 XTNGUQKDFGDXSJ-ZXGKGEBGSA-N 0.000 claims 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 2
- 208000026106 cerebrovascular disease Diseases 0.000 claims 2
- 239000008103 glucose Substances 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- WGRQANOPCQRCME-PMACEKPBSA-N teneligliptin Chemical compound O=C([C@H]1NC[C@H](C1)N1CCN(CC1)C1=CC(=NN1C=1C=CC=CC=1)C)N1CCSC1 WGRQANOPCQRCME-PMACEKPBSA-N 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 208000010444 Acidosis Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- JVHXJTBJCFBINQ-ADAARDCZSA-N Dapagliflozin Chemical compound 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 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000013600 Diabetic vascular disease Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000020358 Learning disease Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 206010027417 Metabolic acidosis Diseases 0.000 claims 1
- 208000026072 Motor neurone disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000024777 Prion disease Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 229960001667 alogliptin Drugs 0.000 claims 1
- ZSBOMTDTBDDKMP-OAHLLOKOSA-N alogliptin Chemical compound C=1C=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 ZSBOMTDTBDDKMP-OAHLLOKOSA-N 0.000 claims 1
- 208000029028 brain injury Diseases 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 125000004802 cyanophenyl group Chemical group 0.000 claims 1
- 229960003834 dapagliflozin Drugs 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 125000004852 dihydrofuranyl group Chemical group O1C(CC=C1)* 0.000 claims 1
- 210000003158 enteroendocrine cell Anatomy 0.000 claims 1
- 231100000318 excitotoxic Toxicity 0.000 claims 1
- 230000003492 excitotoxic effect Effects 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005059 halophenyl group Chemical group 0.000 claims 1
- 125000006377 halopyridyl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 201000003723 learning disability Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000005264 motor neuron disease Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 229960004937 saxagliptin Drugs 0.000 claims 1
- 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 1
- 108010033693 saxagliptin Proteins 0.000 claims 1
- 229940126842 sergliflozin Drugs 0.000 claims 1
- HFLCZNNDZKKXCS-OUUBHVDSSA-N sergliflozin Chemical compound C1=CC(OC)=CC=C1CC1=CC=CC=C1O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HFLCZNNDZKKXCS-OUUBHVDSSA-N 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 229960001254 vildagliptin Drugs 0.000 claims 1
- SYOKIDBDQMKNDQ-XWTIBIIYSA-N vildagliptin Chemical compound C1C(O)(C2)CC(C3)CC1CC32NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-XWTIBIIYSA-N 0.000 claims 1
- 0 *C(C1)CN[C@]1C(N1[C@](*)C*C1)=O Chemical compound *C(C1)CN[C@]1C(N1[C@](*)C*C1)=O 0.000 description 10
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 10
- 229910052794 bromium Inorganic materials 0.000 description 6
- 229910052717 sulfur Inorganic materials 0.000 description 6
- 235000019000 fluorine Nutrition 0.000 description 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 description 4
- 125000005842 heteroatom Chemical group 0.000 description 4
- 229910052740 iodine Inorganic materials 0.000 description 4
- 125000000896 monocarboxylic acid group Chemical group 0.000 description 4
- 229920006395 saturated elastomer Polymers 0.000 description 4
- 125000003342 alkenyl group Chemical group 0.000 description 3
- 125000000304 alkynyl group Chemical group 0.000 description 3
- 125000001153 fluoro group Chemical group F* 0.000 description 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 3
- 229910052760 oxygen Inorganic materials 0.000 description 3
- 125000005037 alkyl phenyl group Chemical group 0.000 description 1
- 125000002947 alkylene group Chemical group 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2177708P | 2008-01-17 | 2008-01-17 | |
| US61/021,777 | 2008-01-17 | ||
| PCT/JP2009/051023 WO2009091082A1 (en) | 2008-01-17 | 2009-01-16 | Combination therapy comprising sglt inhibitors and dpp4 inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012284625A Division JP5646588B2 (ja) | 2008-01-17 | 2012-12-27 | Ｓｇｌｔ阻害剤及びｄｐｐ４阻害剤からなる併用療法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011509922A JP2011509922A (ja) | 2011-03-31 |
| JP2011509922A5 true JP2011509922A5 (enExample) | 2012-03-01 |
| JP5204849B2 JP5204849B2 (ja) | 2013-06-05 |
Family
ID=40433628
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010528230A Active JP5204849B2 (ja) | 2008-01-17 | 2009-01-16 | Ｓｇｌｔ阻害剤及びｄｐｐ４阻害剤からなる併用療法 |
| JP2012284625A Active JP5646588B2 (ja) | 2008-01-17 | 2012-12-27 | Ｓｇｌｔ阻害剤及びｄｐｐ４阻害剤からなる併用療法 |
| JP2014225301A Active JP5908563B2 (ja) | 2008-01-17 | 2014-11-05 | Ｓｇｌｔ阻害剤及びｄｐｐ４阻害剤からなる併用療法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012284625A Active JP5646588B2 (ja) | 2008-01-17 | 2012-12-27 | Ｓｇｌｔ阻害剤及びｄｐｐ４阻害剤からなる併用療法 |
| JP2014225301A Active JP5908563B2 (ja) | 2008-01-17 | 2014-11-05 | Ｓｇｌｔ阻害剤及びｄｐｐ４阻害剤からなる併用療法 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US8853385B2 (enExample) |
| EP (1) | EP2252289B1 (enExample) |
| JP (3) | JP5204849B2 (enExample) |
| KR (1) | KR101257554B1 (enExample) |
| CN (2) | CN101932321B (enExample) |
| AR (1) | AR070193A1 (enExample) |
| AU (1) | AU2009205060C1 (enExample) |
| BR (1) | BRPI0906735A2 (enExample) |
| CA (1) | CA2712614C (enExample) |
| CL (1) | CL2008003653A1 (enExample) |
| ES (1) | ES2763239T3 (enExample) |
| MX (1) | MX2010007818A (enExample) |
| TW (1) | TWI437996B (enExample) |
| WO (1) | WO2009091082A1 (enExample) |
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| 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 |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| NZ573360A (en) | 2006-05-04 | 2012-08-31 | Boehringer Ingelheim Int | Polymorphic forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine |
| CL2008002427A1 (es) | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende 1-cloro-4-(b-d-glucopiranos-1-il)-2-[4-((s)-tetrahidrofurano-3-iloxi)bencil]-benceno combinado con 1-[(4-metilquinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(r)-aminopiperidin-1-il)xantina; y su uso para tratar diabetes mellitus tipo 2. |
| HUE035130T2 (en) | 2007-09-10 | 2018-05-02 | Janssen Pharmaceutica Nv | A method for preparing compounds useful as SGLT 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. |
| JP2009196984A (ja) * | 2008-01-25 | 2009-09-03 | Mitsubishi Tanabe Pharma Corp | 医薬組成物 |
| PE20140960A1 (es) | 2008-04-03 | 2014-08-15 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| KR20200118243A (ko) | 2008-08-06 | 2020-10-14 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| SI2334687T1 (sl) | 2008-08-28 | 2012-03-30 | Pfizer | Dioksa biciklo oktan triol derivati |
| 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 |
| US9056850B2 (en) | 2008-10-17 | 2015-06-16 | Janssen Pharmaceutica N.V. | Process for the preparation of compounds useful as inhibitors of SGLT |
| UY32427A (es) | 2009-02-13 | 2010-09-30 | Boheringer Ingelheim Internat Gmbh | Composicion farmaceutica, forma farmaceutica, procedimiento para su preparacion, metodos de tratamiento y usos de la misma |
| CA2751834C (en) * | 2009-02-13 | 2018-07-24 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition comprising a sglt2 inhibitor, a dpp-iv inhibitor and optionally a further antidiabetic agent and uses thereof |
| US20110009347A1 (en) | 2009-07-08 | 2011-01-13 | Yin Liang | Combination therapy for the treatment of diabetes |
| JP5658751B2 (ja) | 2009-07-10 | 2015-01-28 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ | １−（β−Ｄ−グルコピラノシル）−４−メチル−３−［５−（４−フルオロフェニル）−２−チエニルメチル］ベンゼンのための結晶化方法 |
| EA022032B1 (ru) | 2009-09-30 | 2015-10-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Способ получения глюкопиранозилзамещенных производных бензилбензола |
| JP5736377B2 (ja) | 2009-09-30 | 2015-06-17 | 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 | １−クロロ−４−（β−Ｄ−グルコピラノス−１−イル）−２−［４−（（Ｓ）−テトラヒドロフラン−３−イルオキシ）ベンジル］ベンゼンの結晶形の調製方法 |
| US10610489B2 (en) | 2009-10-02 | 2020-04-07 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, pharmaceutical dosage form, process for their preparation, methods for treating and uses thereof |
| SI2488515T1 (sl) | 2009-10-14 | 2017-04-26 | Janssen Pharmaceutica Nv | Postopek za pripravo spojin, ki so uporabne kot inhibitorji SGLT2 |
| US8163704B2 (en) | 2009-10-20 | 2012-04-24 | Novartis Ag | Glycoside derivatives and uses thereof |
| ES2527179T3 (es) | 2009-11-02 | 2015-01-21 | Pfizer Inc. | Derivados de dioxa-biciclo[3.2.1]octano-2,3,4-triol |
| CA2782179C (en) | 2009-11-27 | 2020-06-23 | Boehringer Ingelheim International Gmbh | 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 |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2568988B1 (en) * | 2010-05-11 | 2016-07-13 | Janssen Pharmaceutica, N.V. | Pharmaceutical formulations comprising 1-(beta-d-glucopyranosyl)-2-thienylmethylbenzene derivatives as inhibitors of sglt |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| 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 |
| AR085689A1 (es) | 2011-03-07 | 2013-10-23 | Boehringer Ingelheim Int | Composiciones farmaceuticas de metformina, linagliptina y un inhibidor de sglt-2 |
| DK2697218T3 (en) | 2011-04-13 | 2016-07-25 | Janssen Pharmaceutica Nv | PROCESS FOR THE PREPARATION OF COMPOUNDS useful as inhibitors of SGLT2 |
| TWI542596B (zh) | 2011-05-09 | 2016-07-21 | 健生藥品公司 | （２ｓ,３ｒ,４ｒ,５ｓ,６ｒ）－２－（３－（（５－（４－氟苯基）噻吩－２－基）甲基）－４－甲基苯基）－６－（羥甲基）四氫－２ｈ－哌喃－３,４,５－三醇之ｌ－脯胺酸及檸檬酸共晶體 |
| EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| 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 |
| WO2013171167A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome |
| JP6218811B2 (ja) | 2012-05-14 | 2017-10-25 | 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 | Ｓｉｒｓ及び／又は敗血症の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体 |
| 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 |
| TR201901110T4 (tr) | 2013-04-05 | 2019-02-21 | Boehringer Ingelheim Int | Empagliflozinin terapötik kullanımları. |
| CA2812519A1 (en) | 2013-04-05 | 2014-10-05 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| US11813275B2 (en) | 2013-04-05 | 2023-11-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| ES2906115T3 (es) | 2013-04-18 | 2022-04-13 | Boehringer Ingelheim Int | Composición farmacéutica, métodos de tratamiento y usos de la misma |
| WO2014198906A1 (en) * | 2013-06-14 | 2014-12-18 | Boehringer Ingelheim International Gmbh | Dpp-4 inhibitors for treating diabetes and its complications |
| CN104739835A (zh) * | 2013-12-30 | 2015-07-01 | 中美华世通生物医药科技（武汉）有限公司 | 一种治疗糖尿病的新型药物组合物 |
| CN106714796A (zh) * | 2014-05-16 | 2017-05-24 | 阿斯利康(瑞典)有限公司 | 用于抑制sglt2抑制剂的胰高血糖素分泌的方法 |
| JP6027710B1 (ja) * | 2014-12-25 | 2016-11-16 | 田辺三菱製薬株式会社 | 糖尿病治療用固形製剤 |
| US20170071970A1 (en) | 2015-09-15 | 2017-03-16 | Janssen Pharmaceutica Nv | Co-therapy comprising canagliflozin and phentermine for the treatment of obesity and obesity related disorders |
| MX390363B (es) | 2016-06-10 | 2025-03-20 | Boehringer Ingelheim Int | Combinacion de linagliptina y metformina |
| MX2019005435A (es) | 2016-11-10 | 2019-07-10 | Boehringer Ingelheim Int | Composicion farmaceutica, metodos para tratamiento y sus usos. |
| US11020412B2 (en) | 2017-03-16 | 2021-06-01 | Inventia Healthcare Limited | Pharmaceutical composition comprising dapagliflozin |
| KR101943382B1 (ko) * | 2017-09-19 | 2019-01-29 | 오토텔릭바이오 주식회사 | Sglt-2 저해제 및 안지오텐신 수용체 차단제를 포함하는 의약 조성물 |
| KR102204439B1 (ko) * | 2018-05-14 | 2021-01-18 | 에이치케이이노엔 주식회사 | Sglt-2 억제제 및 dpp-iv 억제제를 포함하는 약제학적 조성물 |
| CN109021074B (zh) * | 2018-08-31 | 2021-08-10 | 华南理工大学 | 一种改善糖尿病和老年性痴呆症症状的七肽 |
| CN108976291B (zh) * | 2018-08-31 | 2021-06-08 | 华南理工大学 | 一种改善糖尿病和老年性痴呆的十六肽 |
| WO2021176096A1 (en) | 2020-03-05 | 2021-09-10 | Krka, D.D., Novo Mesto | Pharmaceutical composition comprising sglt2 inhibitor |
| CN115867538A (zh) | 2020-06-05 | 2023-03-28 | 新梅斯托克公司 | 高纯的无定形达格列净的制备 |
| CN111494358B (zh) * | 2020-06-22 | 2021-06-22 | 广州市力鑫药业有限公司 | 用于治疗和预防糖尿病肾病的药物 |
| EP4599828A1 (en) * | 2022-10-05 | 2025-08-13 | Daewoong Pharmaceutical Co., Ltd. | Pharmaceutical composition for prevention or treatment of nephropathy and/or diabetes mellitus, comprising enavogliflozin |
Family Cites Families (155)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4160861A (en) | 1977-10-03 | 1979-07-10 | Merck & Co., Inc. | Method for the separation of antibiotic macrolides |
| US4584369A (en) | 1981-07-31 | 1986-04-22 | Sloan-Kettering Institute For Cancer Research | Anti-leukemic beta-glycosyl C-nucleosides |
| JP2544609B2 (ja) | 1986-10-07 | 1996-10-16 | 和光純薬工業株式会社 | Ｔｃｎｑ錯体 |
| EP0355750B1 (en) | 1988-08-19 | 1995-01-25 | Warner-Lambert Company | Substituted dihydroisoquinolinones and related compounds as potentiators of the lethal effects of radiation and certain chemotherapeutic agents; selected compounds, analogs and process |
| CN1020944C (zh) | 1990-01-30 | 1993-05-26 | 阿图尔-费希尔股份公司费希尔厂 | 紧固件 |
| JPH04253974A (ja) | 1991-02-05 | 1992-09-09 | Ishihara Sangyo Kaisha Ltd | スルホニル尿素系化合物、それらの製造方法及びそれらを含有する除草剤 |
| US5149838A (en) | 1991-09-20 | 1992-09-22 | Merck & Co., Inc. | Intermediates for substituted azetidinones useful as anti-inflammatory and antidegenerative agents |
| GB9208161D0 (en) | 1992-04-14 | 1992-05-27 | Pfizer Ltd | Indoles |
| US5334225A (en) | 1992-07-15 | 1994-08-02 | Kao Corporation | Keratinous fiber dye composition containing a 2-substituted amino-5-alkylphenol derivative coupler |
| US5731292A (en) | 1992-11-12 | 1998-03-24 | Tanabe Seiyaku Co., Ltd. | Dihydrochalcone derivatives which are hypoglycemic agents |
| CA2102591C (en) | 1992-11-12 | 2000-12-26 | Kenji Tsujihara | Hypoglycemic agent |
| US6297363B1 (en) | 1993-02-12 | 2001-10-02 | Nomura Co., Ltd. | Glycoside indoles |
| IL111785A0 (en) | 1993-12-03 | 1995-01-24 | Ferring Bv | Dp-iv inhibitors and pharmaceutical compositions containing them |
| US5830873A (en) | 1994-05-11 | 1998-11-03 | Tanabe Seiyaku Co., Ltd. | Propiophenone derivative and a process for preparing the same |
| US5780483A (en) | 1995-02-17 | 1998-07-14 | Smithkline Beecham Corporation | IL-8 receptor antagonists |
| DE69634045T2 (de) | 1995-10-31 | 2005-05-19 | Eli Lilly And Co., Indianapolis | Antithrombotische diamine |
| JP3059088B2 (ja) | 1995-11-07 | 2000-07-04 | 田辺製薬株式会社 | プロピオフェノン誘導体およびその製法 |
| JPH09263549A (ja) | 1996-01-25 | 1997-10-07 | Fujisawa Pharmaceut Co Ltd | ベンゼン誘導体の製造法 |
| DE122010000020I1 (de) | 1996-04-25 | 2010-07-08 | Prosidion Ltd | Verfahren zur Senkung des Blutglukosespiegels in Säugern |
| US20020006899A1 (en) | 1998-10-06 | 2002-01-17 | Pospisilik Andrew J. | Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals |
| TW492957B (en) | 1996-11-07 | 2002-07-01 | Novartis Ag | N-substituted 2-cyanopyrrolidnes |
| TW406086B (en) | 1996-12-26 | 2000-09-21 | Tanabe Seiyaku Co | Propiophenone derivatives and process for preparing the same |
| AU743591B2 (en) | 1997-01-31 | 2002-01-31 | Seydel Research, Inc. | Water dispersible/redispersible hydrophobic polyester resins and their application in coatings |
| US6153632A (en) | 1997-02-24 | 2000-11-28 | Rieveley; Robert B. | Method and composition for the treatment of diabetes |
| JPH10324632A (ja) | 1997-03-25 | 1998-12-08 | Takeda Chem Ind Ltd | 医薬組成物 |
| DE19823831A1 (de) | 1998-05-28 | 1999-12-02 | Probiodrug Ges Fuer Arzneim | Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen |
| US6274725B1 (en) * | 1998-06-02 | 2001-08-14 | Isis Pharmaceuticals, Inc. | Activators for oligonucleotide synthesis |
| JP2000034239A (ja) | 1998-07-16 | 2000-02-02 | Asahi Glass Co Ltd | トリフルオロメチル化芳香族化合物の製造方法 |
| JP3857429B2 (ja) | 1998-07-17 | 2006-12-13 | ポーラ化成工業株式会社 | 含硫黄抗真菌剤 |
| 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 |
| US20020032164A1 (en) | 1998-12-30 | 2002-03-14 | Dale Roderic M. K. | Antimicrobial compounds and methods for their use |
| GB9912961D0 (en) | 1999-06-03 | 1999-08-04 | Pfizer Ltd | Metalloprotease inhibitors |
| US6107317A (en) * | 1999-06-24 | 2000-08-22 | Novartis Ag | N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| 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 |
| US6172081B1 (en) * | 1999-06-24 | 2001-01-09 | Novartis Ag | Tetrahydroisoquinoline 3-carboxamide derivatives |
| UA71994C2 (en) * | 1999-08-31 | 2005-01-17 | Kissei Pharmaceutical | Glucopyranosyloxypyrazole derivatives, a pharmaceutical composition containing these derivatives and intermediate compounds for the preparation thereof |
| PH12000002657B1 (en) | 1999-10-12 | 2006-02-21 | Bristol Myers Squibb Co | C-aryl glucoside SGLT2 inhibitors |
| US6515117B2 (en) | 1999-10-12 | 2003-02-04 | Bristol-Myers Squibb Company | C-aryl glucoside SGLT2 inhibitors and method |
| GB9928330D0 (en) | 1999-11-30 | 2000-01-26 | Ferring Bv | Novel antidiabetic agents |
| DK1741447T3 (da) | 2000-01-21 | 2013-12-09 | Novartis Ag | Kombinationer omfattende dipeptidylpeptidase-IV-inhibitorer og antidiabetiske midler |
| US6627611B2 (en) | 2000-02-02 | 2003-09-30 | Kotobuki Pharmaceutical Co Ltd | C-glycosides and preparation of thereof as antidiabetic agents |
| JP4456768B2 (ja) | 2000-02-02 | 2010-04-28 | 壽製薬株式会社 | Ｃ−配糖体を含有する薬剤 |
| AU3217501A (en) | 2000-03-03 | 2001-09-12 | Pfizer Prod Inc | Pyrazole ether derivatives as anti-inflammatory/analgesic agents |
| US6395767B2 (en) | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
| IL151757A0 (en) | 2000-03-17 | 2003-04-10 | Kissei Pharmaceutical | Glucopyranosyloxy benzylbenzene derivatives, medicinal compounds containing the same and intermediates for the preparation of the derivatives |
| US6555519B2 (en) | 2000-03-30 | 2003-04-29 | Bristol-Myers Squibb Company | O-glucosylated benzamide SGLT2 inhibitors and method |
| US6683056B2 (en) | 2000-03-30 | 2004-01-27 | Bristol-Myers Squibb Company | O-aryl glucoside SGLT2 inhibitors and method |
| GB0010188D0 (en) | 2000-04-26 | 2000-06-14 | Ferring Bv | Inhibitors of dipeptidyl peptidase IV |
| GB0010183D0 (en) | 2000-04-26 | 2000-06-14 | Ferring Bv | Inhibitors of dipeptidyl peptidase IV |
| TW583185B (en) | 2000-06-13 | 2004-04-11 | Novartis Ag | N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same |
| DE10029014A1 (de) * | 2000-06-15 | 2001-12-20 | Univ Schiller Jena | Urokinase-Hemmstoffe |
| US7078397B2 (en) * | 2000-06-19 | 2006-07-18 | Smithkline Beecham Corporation | Combinations of dipeptidyl peptidase IV inhibitors and other antidiabetic agents for the treatment of diabetes mellitus |
| GB0014969D0 (en) | 2000-06-19 | 2000-08-09 | Smithkline Beecham Plc | Novel method of treatment |
| ES2311534T3 (es) * | 2000-08-10 | 2009-02-16 | Mitsubishi Tanabe Pharma Corporation | Derivados de prolina y su uso como farmacos. |
| WO2002028872A1 (fr) * | 2000-09-29 | 2002-04-11 | Kissei Pharmaceutical Co., Ltd. | Derives de glucopyranosiloxybenzylbenzene et compositions therapeutiques contenant ces composes |
| NZ525630A (en) * | 2000-10-06 | 2004-10-29 | Tanabe Seiyaku Co | Nitrogen-containing 5-membered ring compound used as dipeptidylpeptidase IV (DPPIV) inhibitor |
| DE60141156D1 (de) | 2000-11-02 | 2010-03-11 | Ajinomoto Kk | Neue pyrazolderivate und diese enthaltende mittel gegen diabetes |
| US6476352B2 (en) | 2000-12-18 | 2002-11-05 | General Electric Company | Laser beam stop sensor and method for automatically detecting the presence of laser beam stop material using a laser beam stop sensor |
| EP1354882A1 (en) | 2000-12-27 | 2003-10-22 | Kyowa Hakko Kogyo Co., Ltd. | Dipeptidyl peptidase iv inhibitor |
| NZ526715A (en) | 2000-12-28 | 2005-02-25 | Kissei Pharmaceutical | Glucopyranosyloxypyrazole derivatives and use thereof in medicines |
| ES2319263T3 (es) | 2001-02-26 | 2009-05-06 | Kissei Pharmaceutical Co., Ltd. | Derivados de glucopiranosilooxipirazol y su utilizacion como medicamentos. |
| WO2002068440A1 (en) | 2001-02-27 | 2002-09-06 | Kissei Pharmaceutical Co., Ltd. | Glycopyranosyloxypyrazole derivatives and medicinal use thereof |
| CA2710031A1 (en) | 2001-03-02 | 2002-09-12 | University Of Western Ontario | Polymer precursors of radiolabeled compounds, and methods of making and using the same |
| JP2002265439A (ja) | 2001-03-08 | 2002-09-18 | Mitsubishi Pharma Corp | シアノピロリジン誘導体およびその医薬用途 |
| US6936590B2 (en) | 2001-03-13 | 2005-08-30 | Bristol Myers Squibb Company | C-aryl glucoside SGLT2 inhibitors and method |
| MXPA03008614A (es) | 2001-03-28 | 2003-12-08 | Hercules Inc | Metodos para usar acidos de lupulo para controlar organismos. |
| HUP0600232A2 (en) | 2001-04-11 | 2006-08-28 | Bristol Myers Squibb Co | Amino acid complexes of c-aryl glucosides for treatment of diabetes and method |
| US6573287B2 (en) | 2001-04-12 | 2003-06-03 | Bristo-Myers Squibb Company | 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method |
| EP1389621A4 (en) | 2001-04-27 | 2005-05-11 | Ajinomoto Kk | N-SUBSTITUTED PYRAZOLYL-O-GLYCOSIDE DERIVATIVES AND DIABETES CONTAINING THEREOF |
| GB0112122D0 (en) | 2001-05-18 | 2001-07-11 | Lilly Co Eli | Heteroaryloxy 3-substituted propanamines |
| CA2455300A1 (en) | 2001-06-20 | 2003-01-03 | Kissei Pharmaceutical Co., Ltd. | Nitrogen-containing heterocyclic derivative, medicinal composition containing the same, medicinal use thereof, and intermediate therefor |
| GB0115517D0 (en) | 2001-06-25 | 2001-08-15 | Ferring Bv | Novel antidiabetic agents |
| US7196201B2 (en) | 2001-06-27 | 2007-03-27 | Smithkline Beecham Corporation | Pyrrolidines as dipeptidyl peptidase inhibitors |
| WO2003002553A2 (en) | 2001-06-27 | 2003-01-09 | Smithkline Beecham Corporation | Fluoropyrrolidines as dipeptidyl peptidase inhibitors |
| DE60235212D1 (de) | 2001-06-27 | 2010-03-11 | Smithkline Beecham Corp | Fluoropyrrolidine als Dipeptidylpeptidasehemmer |
| JP4115105B2 (ja) | 2001-07-02 | 2008-07-09 | 協和醗酵工業株式会社 | ピラゾール誘導体 |
| UA74912C2 (en) | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
| WO2003011880A1 (fr) | 2001-07-31 | 2003-02-13 | Kissei Pharmaceutical Co., Ltd. | Derive de glucopyranosyloxybenzylbenzene, composition medicinale contenant ce derive, usage medicinal de cette composition et produit intermediaire pour produire cette composition |
| US20030087843A1 (en) | 2001-09-05 | 2003-05-08 | Washburn William N. | O-pyrazole glucoside SGLT2 inhibitors and method of use |
| TWI246510B (en) * | 2001-09-14 | 2006-01-01 | Mitsubishi Pharma Corp | Thiazolidine derivatives and pharmaceutical uses thereof |
| GB0125445D0 (en) | 2001-10-23 | 2001-12-12 | Ferring Bv | Protease Inhibitors |
| EP1438424B1 (en) | 2001-10-24 | 2006-01-18 | Michael Burton | Enzyme substrates for detecting beta-d-ribofuranosidase activity |
| MXPA04004673A (es) | 2001-11-16 | 2005-05-17 | Cutanix Corp | Composiciones farmaceuticas y cosmeticas que contienen aldehidos aromaticos qeue portan un grupo oxi. |
| US6617313B1 (en) | 2002-03-13 | 2003-09-09 | Council Of Scientific And Industrial Research | Glucopyranoside and process of isolation thereof from pterocarpus marsupium pharmaceutical composition containing the same and use thereof |
| US6562791B1 (en) | 2002-03-29 | 2003-05-13 | Council Of Scientific And Industrial Research | Glucopyranoside, process for isolation thereof, pharmaceutical composition containing same and use thereof |
| ATE433981T1 (de) | 2002-04-18 | 2009-07-15 | Astrazeneca Ab | Heterocyclische verbindungen |
| US6710040B1 (en) * | 2002-06-04 | 2004-03-23 | Pfizer Inc. | Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors |
| DE10231370B4 (de) | 2002-07-11 | 2006-04-06 | Sanofi-Aventis Deutschland Gmbh | Thiophenglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel |
| TW200401635A (en) * | 2002-07-23 | 2004-02-01 | Yamanouchi Pharma Co Ltd | 2-Cyano-4-fluoropyrrolidine derivative or salt thereof |
| TWI254635B (en) | 2002-08-05 | 2006-05-11 | Yamanouchi Pharma Co Ltd | Azulene derivative and salt thereof |
| CA2478889A1 (en) | 2002-08-09 | 2004-02-19 | Taisho Pharmaceutical Co., Ltd. | Aryl 5-thio-.beta.-d-glucopyranoside derivatives and therapeutic agents for diabetes containing the same |
| US20040102477A1 (en) | 2002-08-23 | 2004-05-27 | Dr. Reddy's Laboratories Limited | Polymorphic forms of (S)-Repaglinide and the processes for preparation thereof |
| JP4606876B2 (ja) | 2002-08-27 | 2011-01-05 | キッセイ薬品工業株式会社 | ピラゾール誘導体、それを含有する医薬組成物及びその医薬用途 |
| ZA200501418B (en) * | 2002-08-29 | 2006-10-25 | Taisho Pharmaceutical Co Ltd | Benzenesulfonate salts of 4-fluoro-2-cyanopyrrolidine derivatives |
| DE10258007B4 (de) | 2002-12-12 | 2006-02-09 | Sanofi-Aventis Deutschland Gmbh | Aromatische Fluorglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel |
| DE10258008B4 (de) | 2002-12-12 | 2006-02-02 | Sanofi-Aventis Deutschland Gmbh | Heterocyclische Fluorglycosidderivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zur Herstellung dieser Arzneimittel |
| JP2006516257A (ja) | 2003-01-03 | 2006-06-29 | ブリストル−マイヤーズ スクイブ カンパニー | Ｃ−アリールグルコシドｓｇｌｔ２阻害剤の製造法 |
| DE10303270A1 (de) | 2003-01-28 | 2004-08-05 | Technische Universität Darmstadt | Medizintechnische Vorrichtung mit einer langgestreckten Einrichtung |
| CA2514191C (en) * | 2003-01-31 | 2011-10-11 | Sanwa Kagaku Kenkyusho Co., Ltd. | Compound inhibiting dipeptidyl peptidase iv |
| KR101001850B1 (ko) | 2003-03-14 | 2010-12-17 | 고토부키 세이야쿠 가부시키가이샤 | Ｃ-글리코시드 유도체 또는 이의 염, 및 이를 포함하는의약 조성물 |
| JP2004300102A (ja) | 2003-03-31 | 2004-10-28 | Kissei Pharmaceut Co Ltd | 縮合複素環誘導体、それを含有する医薬組成物およびその医薬用途 |
| AU2003902263A0 (en) | 2003-05-12 | 2003-05-29 | Fujisawa Pharmaceutical Co., Ltd. | Monosaccharide compounds |
| 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 |
| ES2377741T3 (es) | 2003-06-20 | 2012-03-30 | Kissei Pharmaceutical Co., Ltd. | Derivados de pirazol, composición farmacológica que los contiene e intermedios de producción de los mismos |
| CA2549025A1 (en) | 2003-08-01 | 2005-02-10 | Janssen Pharmaceutica N.V. | Substituted indole-o-glucosides |
| US8785403B2 (en) * | 2003-08-01 | 2014-07-22 | Mitsubishi Tanabe Pharma Corporation | Glucopyranoside compound |
| US6995183B2 (en) | 2003-08-01 | 2006-02-07 | Bristol Myers Squibb Company | Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods |
| CN103819465A (zh) * | 2003-08-01 | 2014-05-28 | 田边三菱制药株式会社 | 新颖化合物 |
| UA86042C2 (en) | 2003-08-01 | 2009-03-25 | Янссен Фармацевтика Н.В. | Substituted indazole-o-glucosides |
| US7094764B2 (en) | 2003-08-01 | 2006-08-22 | Janssen Pharmaceutica N.V. | Substituted benzimidazole-, Benztriazole-, and benzimidazolone-O-glucosides |
| AU2004261660A1 (en) | 2003-08-01 | 2005-02-10 | Janssen Pharmaceutica N.V. | Substituted fused heterocyclic C-glycosides |
| WO2005011592A2 (en) | 2003-08-01 | 2005-02-10 | Janssen Pharmaceutica N.V. | Substituted indazole-o-glucosides |
| JP2007505121A (ja) | 2003-09-08 | 2007-03-08 | 武田薬品工業株式会社 | ジペプチジルぺプチダーゼ阻害剤 |
| JP2007513058A (ja) | 2003-09-08 | 2007-05-24 | 武田薬品工業株式会社 | ジペプチジルぺプチダーゼ阻害剤 |
| US20070021430A1 (en) | 2003-09-23 | 2007-01-25 | Chen Alex M | Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor |
| TW200519105A (en) | 2003-10-20 | 2005-06-16 | Lg Life Science Ltd | Novel inhibitors of DPP-IV, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent |
| US7214735B2 (en) | 2004-02-02 | 2007-05-08 | 3M Innovative Properties Company | Microsphere-filled sealant materials |
| PL1712547T3 (pl) * | 2004-02-05 | 2012-04-30 | Kyorin Seiyaku Kk | Pochodna bicykloestrowa |
| CN1922139B (zh) | 2004-02-18 | 2010-12-29 | 杏林制药株式会社 | 双环酰胺衍生物 |
| US7514571B2 (en) * | 2004-02-27 | 2009-04-07 | Kyorin Pharmaceutical Co., Ltd. | Bicyclo derivative |
| CN1934122B (zh) | 2004-03-04 | 2010-08-04 | 橘生药品工业株式会社 | 稠合杂环衍生物、包含该稠合杂环衍生物的药物组合物、及其药学应用 |
| JP4902348B2 (ja) * | 2004-03-04 | 2012-03-21 | キッセイ薬品工業株式会社 | 含窒素縮合環誘導体、それを含有する医薬組成物およびその医薬用途 |
| 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 |
| SG151271A1 (en) * | 2004-03-16 | 2009-04-30 | Boehringer Ingelheim Int | Glucopyranosyl-substituted benzol derivatives, drugs containing said compounds, the use thereof and method for the production thereof |
| WO2006018150A1 (de) * | 2004-08-11 | 2006-02-23 | Boehringer Ingelheim International Gmbh | D-xylopyranosyl-phenyl-substituierte cyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung |
| AR051446A1 (es) | 2004-09-23 | 2007-01-17 | Bristol Myers Squibb Co | Glucosidos de c-arilo como inhibidores selectivos de transportadores de glucosa (sglt2) |
| WO2006035796A1 (ja) | 2004-09-29 | 2006-04-06 | Kissei Pharmaceutical Co., Ltd. | １－（β－Ｄ－グリコピラノシル）－３－置換含窒素ヘテロ環化合物、それを含有する医薬組成物及びその医薬用途 |
| WO2006073167A1 (ja) | 2005-01-07 | 2006-07-13 | Ono Pharmaceutical Co., Ltd. | ピロリジン誘導体 |
| AR053329A1 (es) * | 2005-01-31 | 2007-05-02 | Tanabe Seiyaku Co | Derivados de indol utiles como inhibidores de los transportadores de glucosa dependientes del sodio (sglt) |
| EP1854795B1 (en) | 2005-02-18 | 2016-06-01 | Mitsubishi Tanabe Pharma Corporation | Salt of a proline derivative, solvate thereof, and production method thereof |
| WO2006090244A1 (en) | 2005-02-22 | 2006-08-31 | Glenmark Pharmaceuticals S.A. | New adamantane derivatives as dipeptidyl, peptidase iv inhibitors, processes for their preparation, and pharmaceutical compositions containing them |
| EP1741790A1 (en) | 2005-03-24 | 2007-01-10 | DIGILAB BioVisioN GmbH | Methods to identify and characterize prolyl oligopeptidases by using substrates and products thereof |
| TWI357902B (en) | 2005-04-01 | 2012-02-11 | Lg Life Science Ltd | Dipeptidyl peptidase-iv inhibiting compounds, meth |
| JP5238492B2 (ja) | 2005-04-15 | 2013-07-17 | 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 | Ｓｇｌｔインヒビターとしてのグルコピラノシル置換（ヘテロアリールオキシ−ベンジル）−ベンゼン誘導体 |
| KR20080000665A (ko) * | 2005-04-22 | 2008-01-02 | 알란토스 파마슈티컬즈 홀딩, 인코포레이티드 | 디펩티딜 펩티다아제-ⅳ 억제제 |
| US7723309B2 (en) | 2005-05-03 | 2010-05-25 | Boehringer Ingelheim International Gmbh | Crystalline forms of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((R)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments |
| UA91546C2 (uk) | 2005-05-03 | 2010-08-10 | Бьорінгер Інгельхайм Інтернаціональ Гмбх | КРИСТАЛІЧНА ФОРМА 1-ХЛОР-4-(β-D-ГЛЮКОПІРАНОЗ-1-ИЛ)-2-[4-((S)-ТЕТРАГІДРОФУРАН-3-ІЛОКСИ)-БЕНЗИЛ]-БЕНЗОЛУ, СПОСІБ ЇЇ ОДЕРЖАННЯ ТА ЇЇ ЗАСТОСУВАННЯ ПРИ ПРИГОТУВАННІ ЛІКАРСЬКИХ ЗАСОБІВ |
| US7772191B2 (en) | 2005-05-10 | 2010-08-10 | Boehringer Ingelheim International Gmbh | Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein |
| US8754032B2 (en) * | 2005-06-03 | 2014-06-17 | Mitsubishi Tanabe Pharma Corporation | Concomitant pharmaceutical agents and use thereof |
| US20090221592A1 (en) | 2005-07-25 | 2009-09-03 | Ellison Martha E | Dodecylsulfate Salt Of A Dipeptidyl Peptidase-Iv Inhibitor |
| WO2007054978A2 (en) | 2005-11-10 | 2007-05-18 | Jubilant Organosys Limited | Process for preparing paroxetine hydrochloride hemihydrate |
| WO2007063928A1 (ja) * | 2005-11-30 | 2007-06-07 | Toray Industries, Inc. | 新規な非環状アミンカルボキシアミド誘導体及びその塩 |
| EP1842850A1 (en) | 2006-03-23 | 2007-10-10 | Sandoz AG | Rosiglitazone hydrochloride hemihydrate |
| PE20080251A1 (es) * | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| JP5528699B2 (ja) * | 2006-05-16 | 2014-06-25 | 武田薬品工業株式会社 | 縮合複素環化合物およびその用途 |
| WO2007140191A2 (en) * | 2006-05-23 | 2007-12-06 | Theracos, Inc. | Glucose transport inhibitors and methods of use |
| TWI418556B (zh) | 2006-07-27 | 2013-12-11 | Mitsubishi Tanabe Pharma Corp | 吲哚衍生物 |
| US20080027014A1 (en) | 2006-07-28 | 2008-01-31 | Tanabe Seiyaku Co., Ltd. | Novel SGLT inhibitors |
| US20070172525A1 (en) * | 2007-03-15 | 2007-07-26 | Ramesh Sesha | Anti-diabetic combinations |
| PE20090696A1 (es) * | 2007-04-20 | 2009-06-20 | Bristol Myers Squibb Co | Formas cristalinas de saxagliptina y procesos para preparar las mismas |
| CL2008002425A1 (es) | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Composición farmacéutica que comprende un inhibidor de sglt2 y 1-(4-metil-quinazolin-2-il)metil-3metil-7-(-2-butin-1-il)-8-(3-(r)-amino-piperidin-1il)-xantina, un inhibidor de dpp iv y su uso para el tratamiento de la obesidad y de la diabetes tipo 1 y 2 y complicaciones de esta. |
| CL2008002424A1 (es) * | 2007-08-16 | 2009-09-11 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un compuesto derivado de pirazol-o-glucosido; y uso de la composicion farmaceutica para el tratamiento de la diabetes mellitus, tolerancia anormal a la glucosa e hiperglucemia, trastornos metabolicos, entre otras. |
| 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. |
| UY32427A (es) | 2009-02-13 | 2010-09-30 | Boheringer Ingelheim Internat Gmbh | Composicion farmaceutica, forma farmaceutica, procedimiento para su preparacion, metodos de tratamiento y usos de la misma |
| CA2751834C (en) | 2009-02-13 | 2018-07-24 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition comprising a sglt2 inhibitor, a dpp-iv inhibitor and optionally a further antidiabetic agent and uses thereof |
-
2008
- 2008-12-09 CL CL2008003653A patent/CL2008003653A1/es unknown
-
2009
- 2009-01-16 KR KR1020107018132A patent/KR101257554B1/ko active Active
- 2009-01-16 EP EP09701670.3A patent/EP2252289B1/en not_active Revoked
- 2009-01-16 JP JP2010528230A patent/JP5204849B2/ja active Active
- 2009-01-16 MX MX2010007818A patent/MX2010007818A/es active IP Right Grant
- 2009-01-16 ES ES09701670T patent/ES2763239T3/es active Active
- 2009-01-16 AR ARP090100146A patent/AR070193A1/es not_active Application Discontinuation
- 2009-01-16 CN CN200980102300.8A patent/CN101932321B/zh active Active
- 2009-01-16 AU AU2009205060A patent/AU2009205060C1/en not_active Ceased
- 2009-01-16 US US12/863,429 patent/US8853385B2/en not_active Expired - Fee Related
- 2009-01-16 CA CA2712614A patent/CA2712614C/en not_active Expired - Fee Related
- 2009-01-16 CN CN201310475934.6A patent/CN103599539A/zh active Pending
- 2009-01-16 WO PCT/JP2009/051023 patent/WO2009091082A1/en not_active Ceased
- 2009-01-16 BR BRPI0906735-3A patent/BRPI0906735A2/pt not_active Application Discontinuation
- 2009-01-17 TW TW098101763A patent/TWI437996B/zh not_active IP Right Cessation
-
2012
- 2012-12-27 JP JP2012284625A patent/JP5646588B2/ja active Active
-
2014
- 2014-08-28 US US14/472,037 patent/US20140371162A1/en not_active Abandoned
- 2014-11-05 JP JP2014225301A patent/JP5908563B2/ja active Active
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