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.)
- Granted
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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 |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| SG174054A1 (en) | 2006-05-04 | 2011-09-29 | Boehringer Ingelheim Int | Polymorphs |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20090938A1 (es) | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo |
| 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 |
| AR071175A1 (es) | 2008-04-03 | 2010-06-02 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un inhibidor de la dipeptidil-peptidasa-4 (dpp4) y un farmaco acompanante |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| ATE540040T1 (de) | 2008-08-28 | 2012-01-15 | Pfizer | Dioxabicycloä3.2.1üoctan-2,3,4-triolderivate |
| 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 |
| SG173619A1 (en) * | 2009-02-13 | 2011-09-29 | Boehringer Ingelheim Int | 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 |
| WO2011003976A1 (en) | 2009-07-10 | 2011-01-13 | Janssen Pharmaceutica Nv | CRYSTALLISATION PROCESS FOR 1-(ß-D-GLUCOPYRANOSYL)-4-METHYL-3-[5-(4-FLUOROPHENYL)-2-THIENYLMETHYL] BENZENE |
| MX2012002942A (es) | 2009-09-30 | 2012-04-11 | Boehringer Ingelheim Int | Metodo para la preparacion de una forma cristalina de 1-cloro-4-(beta-d-glucopiranos-1-il)-2-(4-((s)-teteahidrofuran-3- iloxi)bencil)-benceno. |
| CN102574829B (zh) | 2009-09-30 | 2015-07-01 | 贝林格尔.英格海姆国际有限公司 | 吡喃葡萄糖基取代的苄基-苯衍生物的制备方法 |
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-
2008
- 2008-12-09 CL CL2008003653A patent/CL2008003653A1/es unknown
-
2009
- 2009-01-16 ES ES09701670T patent/ES2763239T3/es active Active
- 2009-01-16 WO PCT/JP2009/051023 patent/WO2009091082A1/en not_active Ceased
- 2009-01-16 EP EP09701670.3A patent/EP2252289B1/en not_active Revoked
- 2009-01-16 US US12/863,429 patent/US8853385B2/en not_active Expired - Fee Related
- 2009-01-16 CN CN200980102300.8A patent/CN101932321B/zh active Active
- 2009-01-16 BR BRPI0906735-3A patent/BRPI0906735A2/pt not_active Application Discontinuation
- 2009-01-16 CN CN201310475934.6A patent/CN103599539A/zh active Pending
- 2009-01-16 JP JP2010528230A patent/JP5204849B2/ja active Active
- 2009-01-16 AU AU2009205060A patent/AU2009205060C1/en not_active Ceased
- 2009-01-16 KR KR1020107018132A patent/KR101257554B1/ko active Active
- 2009-01-16 MX MX2010007818A patent/MX2010007818A/es active IP Right Grant
- 2009-01-16 AR ARP090100146A patent/AR070193A1/es not_active Application Discontinuation
- 2009-01-16 CA CA2712614A patent/CA2712614C/en not_active Expired - Fee Related
- 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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