JP2013533291A5 - - Google Patents
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- JP2013533291A5 JP2013533291A5 JP2013523477A JP2013523477A JP2013533291A5 JP 2013533291 A5 JP2013533291 A5 JP 2013533291A5 JP 2013523477 A JP2013523477 A JP 2013523477A JP 2013523477 A JP2013523477 A JP 2013523477A JP 2013533291 A5 JP2013533291 A5 JP 2013533291A5
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- JP
- Japan
- Prior art keywords
- alkyl
- group
- heteroaryl
- aryl
- formula
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 25
- 150000003839 salts Chemical class 0.000 claims description 21
- 125000000217 alkyl group Chemical group 0.000 claims 29
- 125000001072 heteroaryl group Chemical group 0.000 claims 22
- 125000003118 aryl group Chemical group 0.000 claims 21
- 125000000753 cycloalkyl group Chemical group 0.000 claims 21
- 125000000623 heterocyclic group Chemical group 0.000 claims 20
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 11
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 9
- 229910052805 deuterium Inorganic materials 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 7
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 125000000304 alkynyl group Chemical group 0.000 claims 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 150000001733 carboxylic acid esters Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 201000001320 Atherosclerosis Diseases 0.000 claims 3
- 208000002249 Diabetes Complications Diseases 0.000 claims 3
- 206010012655 Diabetic complications Diseases 0.000 claims 3
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 3
- 206010020772 Hypertension Diseases 0.000 claims 3
- 206010022489 Insulin Resistance Diseases 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 208000017442 Retinal disease Diseases 0.000 claims 3
- 206010038923 Retinopathy Diseases 0.000 claims 3
- 206010012601 diabetes mellitus Diseases 0.000 claims 3
- 235000014113 dietary fatty acids Nutrition 0.000 claims 3
- 229930195729 fatty acid Natural products 0.000 claims 3
- 239000000194 fatty acid Substances 0.000 claims 3
- 150000004665 fatty acids Chemical class 0.000 claims 3
- 201000001421 hyperglycemia Diseases 0.000 claims 3
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 3
- 201000008980 hyperinsulinism Diseases 0.000 claims 3
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 3
- 210000001596 intra-abdominal fat Anatomy 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 201000001119 neuropathy Diseases 0.000 claims 3
- 230000007823 neuropathy Effects 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 208000033808 peripheral neuropathy Diseases 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- -1 cyano, hydroxyl Chemical group 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 102000018711 Facilitative Glucose Transport Proteins Human genes 0.000 claims 1
- 108091052347 Glucose transporter family Proteins 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 150000001502 aryl halides Chemical class 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 150000001975 deuterium Chemical group 0.000 claims 1
- 125000004431 deuterium atom Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 0 *C(*)(*)C(*)(*)Oc(ccc(Cc1cc([C@@](C2)OC(CO)C(COO)C2O)ccc1Cl)c1)c1F Chemical compound *C(*)(*)C(*)(*)Oc(ccc(Cc1cc([C@@](C2)OC(CO)C(COO)C2O)ccc1Cl)c1)c1F 0.000 description 8
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 3
- 239000011541 reaction mixture Substances 0.000 description 3
- ARHSAZVNLCYXIR-KNJMJIDISA-N (1s,2s,3s,4r,5s)-5-[4-chloro-3-[[4-(trifluoromethoxy)phenyl]methyl]phenyl]-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol Chemical compound C=1C([C@]23OC[C@](O2)([C@H]([C@H](O)[C@H]3O)O)CO)=CC=C(Cl)C=1CC1=CC=C(OC(F)(F)F)C=C1 ARHSAZVNLCYXIR-KNJMJIDISA-N 0.000 description 1
- VUXHGIZYRNNOSE-UHFFFAOYSA-N 5-bromo-2-chloro-n-methoxy-n-methylbenzamide Chemical compound CON(C)C(=O)C1=CC(Br)=CC=C1Cl VUXHGIZYRNNOSE-UHFFFAOYSA-N 0.000 description 1
- FGERXQWKKIVFQG-UHFFFAOYSA-N 5-bromo-2-chlorobenzoic acid Chemical compound OC(=O)C1=CC(Br)=CC=C1Cl FGERXQWKKIVFQG-UHFFFAOYSA-N 0.000 description 1
- DBEGWSNCIZPWJB-XCJLJZCSSA-N CC(C)([C@@H](CO)O[C@]([C@@H]1O)(c(cc2Cc(cc3)cc(F)c3O)ccc2Cl)O)[C@@H]1O Chemical compound CC(C)([C@@H](CO)O[C@]([C@@H]1O)(c(cc2Cc(cc3)cc(F)c3O)ccc2Cl)O)[C@@H]1O DBEGWSNCIZPWJB-XCJLJZCSSA-N 0.000 description 1
- ANZZPAKNZCWSHZ-VKQJQLINSA-N CCOc1ccc(Cc2cc([C@@H]([C@@H]([C@H]3O)O)OC(CO)[C@H]3O)ccc2Cl)cc1F Chemical compound CCOc1ccc(Cc2cc([C@@H]([C@@H]([C@H]3O)O)OC(CO)[C@H]3O)ccc2Cl)cc1F ANZZPAKNZCWSHZ-VKQJQLINSA-N 0.000 description 1
- USGYFMGQEXGTQY-JRSUCEMESA-N CCOc1ccc(Cc2cc([C@]3([C@@H]([C@H]([C@@H]4O)O)O)O[C@]4(CO)O3)ccc2Cl)c(F)c1F Chemical compound CCOc1ccc(Cc2cc([C@]3([C@@H]([C@H]([C@@H]4O)O)O)O[C@]4(CO)O3)ccc2Cl)c(F)c1F USGYFMGQEXGTQY-JRSUCEMESA-N 0.000 description 1
- MICDRAMXONRKDN-JRSUCEMESA-N CCOc1ccc(Cc2cc([C@]3([C@@H]([C@H]([C@@H]4O)O)O)O[C@]4(CO)O3)ccc2Cl)cc1F Chemical compound CCOc1ccc(Cc2cc([C@]3([C@@H]([C@H]([C@@H]4O)O)O)O[C@]4(CO)O3)ccc2Cl)cc1F MICDRAMXONRKDN-JRSUCEMESA-N 0.000 description 1
- OWCMXVKRWYFOKK-JLVOSQQTSA-N CC[C@](CO)([C@H]([C@@H]([C@H](/C(/C)=C(\C=C/CC)/Cl)O)O)O)O Chemical compound CC[C@](CO)([C@H]([C@@H]([C@H](/C(/C)=C(\C=C/CC)/Cl)O)O)O)O OWCMXVKRWYFOKK-JLVOSQQTSA-N 0.000 description 1
- ZBDLJUKKESWZQT-SVPZFONSSA-N COc1ccc(Cc(cc([C@@H]([C@@H]([C@H]2O)O)OC(CO)[C@H]2O)cc2)c2Cl)c(F)c1F Chemical compound COc1ccc(Cc(cc([C@@H]([C@@H]([C@H]2O)O)OC(CO)[C@H]2O)cc2)c2Cl)c(F)c1F ZBDLJUKKESWZQT-SVPZFONSSA-N 0.000 description 1
- KKGHYRTVONXIRE-ONUIULTDSA-N C[C@@](CO)([C@@](C)([C@@H]([C@H]1O)O)O)O[C@]1(c(cc1Cc(cc2)ccc2OC(F)(F)F)ccc1Cl)O Chemical compound C[C@@](CO)([C@@](C)([C@@H]([C@H]1O)O)O)O[C@]1(c(cc1Cc(cc2)ccc2OC(F)(F)F)ccc1Cl)O KKGHYRTVONXIRE-ONUIULTDSA-N 0.000 description 1
- FVDICEDDSRDDLA-URYYLNOGSA-N Cc1ccc([C@@H]([C@@H]([C@H]([C@@H]2O)O)O)O[C@@]2(CO)O)cc1C/C(/[S-2])=C/C=C/c(cc1)ccc1F Chemical compound Cc1ccc([C@@H]([C@@H]([C@H]([C@@H]2O)O)O)O[C@@]2(CO)O)cc1C/C(/[S-2])=C/C=C/c(cc1)ccc1F FVDICEDDSRDDLA-URYYLNOGSA-N 0.000 description 1
- YXFVVABEGXRONW-UHFFFAOYSA-N Cc1ccccc1 Chemical compound Cc1ccccc1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 1
- BOOQJYYVKDXEEZ-UHFFFAOYSA-N Cl.CNOC.BrC=1C=CC(=C(C(=O)N(C)OC)C1)Cl Chemical compound Cl.CNOC.BrC=1C=CC(=C(C(=O)N(C)OC)C1)Cl BOOQJYYVKDXEEZ-UHFFFAOYSA-N 0.000 description 1
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 1
- IERDPZTZIONHSM-UHFFFAOYSA-N O=C1OCCN1[ClH]P(=O)[ClH]N1C(OCC1)=O Chemical compound O=C1OCCN1[ClH]P(=O)[ClH]N1C(OCC1)=O IERDPZTZIONHSM-UHFFFAOYSA-N 0.000 description 1
- XFTPNAQQCNPMJB-UHFFFAOYSA-N OCC(CC(C1)O)OC1=O Chemical compound OCC(CC(C1)O)OC1=O XFTPNAQQCNPMJB-UHFFFAOYSA-N 0.000 description 1
- SVARVAJYXWDDFZ-SOAISFHBSA-N OCC([C@H]([C@@H](C1)O)O)(OO)OC1c(cc1Cc(cc2)ccc2OCC(F)(F)F)ccc1Cl Chemical compound OCC([C@H]([C@@H](C1)O)O)(OO)OC1c(cc1Cc(cc2)ccc2OCC(F)(F)F)ccc1Cl SVARVAJYXWDDFZ-SOAISFHBSA-N 0.000 description 1
- VAZZALKXFYPXLX-DOIVMEMASA-N OCC1([C@H]([C@@H]([C@H]2O)O)O)OC2(c(cc2Cc(cc3)ccc3OCC(F)F)ccc2Cl)O1 Chemical compound OCC1([C@H]([C@@H]([C@H]2O)O)O)OC2(c(cc2Cc(cc3)ccc3OCC(F)F)ccc2Cl)O1 VAZZALKXFYPXLX-DOIVMEMASA-N 0.000 description 1
- YUNVXSRXOXQDAQ-JNBCYNBSSA-N OC[C@@](C[C@@H](C1)O)(O)OC1c(cc1Cc(cc2)ccc2OC(F)(F)F)ccc1Cl Chemical compound OC[C@@](C[C@@H](C1)O)(O)OC1c(cc1Cc(cc2)ccc2OC(F)(F)F)ccc1Cl YUNVXSRXOXQDAQ-JNBCYNBSSA-N 0.000 description 1
- YXDBYBANFNHJPX-LYSZKAAZSA-N OC[C@@]([C@@H]1[C@@H]([C@H]2O)O)([C@@H]1O)O[C@]2(c(cc1Cc2ccc3OCCc3c2)ccc1Cl)O Chemical compound OC[C@@]([C@@H]1[C@@H]([C@H]2O)O)([C@@H]1O)O[C@]2(c(cc1Cc2ccc3OCCc3c2)ccc1Cl)O YXDBYBANFNHJPX-LYSZKAAZSA-N 0.000 description 1
- WVDDGKGOMKODPV-UHFFFAOYSA-N OCc1ccccc1 Chemical compound OCc1ccccc1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 1
- FFBHFFJDDLITSX-UHFFFAOYSA-N benzyl N-[2-hydroxy-4-(3-oxomorpholin-4-yl)phenyl]carbamate Chemical compound OC1=C(NC(=O)OCC2=CC=CC=C2)C=CC(=C1)N1CCOCC1=O FFBHFFJDDLITSX-UHFFFAOYSA-N 0.000 description 1
- 238000010828 elution Methods 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 238000010898 silica gel chromatography Methods 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical class O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201010249618 | 2010-08-10 | ||
| CN201010249618.3 | 2010-08-10 | ||
| CN2010105896065A CN102372722A (zh) | 2010-08-10 | 2010-12-06 | C-芳基葡萄糖苷衍生物、其制备方法及其在医药上的应用 |
| CN201010589606.5 | 2010-12-06 | ||
| PCT/CN2011/076680 WO2012019496A1 (zh) | 2010-08-10 | 2011-06-30 | C-芳基葡萄糖苷衍生物、其制备方法及其在医药上的应用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013533291A JP2013533291A (ja) | 2013-08-22 |
| JP2013533291A5 true JP2013533291A5 (enExample) | 2014-07-31 |
| JP5984808B2 JP5984808B2 (ja) | 2016-09-06 |
Family
ID=45567352
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013523477A Expired - Fee Related JP5984808B2 (ja) | 2010-08-10 | 2011-06-30 | Ｃ−アリールグルコシド誘導体、製造法およびその医薬用途 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8609622B2 (enExample) |
| EP (1) | EP2604612B1 (enExample) |
| JP (1) | JP5984808B2 (enExample) |
| KR (1) | KR101862891B1 (enExample) |
| CN (2) | CN102372722A (enExample) |
| BR (1) | BR112013002125A2 (enExample) |
| CA (1) | CA2807034C (enExample) |
| ES (1) | ES2581728T3 (enExample) |
| MX (1) | MX2013001098A (enExample) |
| RU (1) | RU2606501C2 (enExample) |
| WO (1) | WO2012019496A1 (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102757415B (zh) * | 2011-04-25 | 2015-07-29 | 北京普禄德医药科技有限公司 | 一种钠依赖性葡萄糖转运蛋白抑制剂及其制备方法和用途 |
| EP2755722B1 (en) | 2011-09-13 | 2017-05-24 | Panacea Biotec Ltd. | Novel sglt inhibitors |
| CN102627535A (zh) * | 2012-03-31 | 2012-08-08 | 天津药物研究院 | 含1,1-二苯基环丙基结构的化合物的制备方法 |
| WO2013178064A1 (zh) * | 2012-05-29 | 2013-12-05 | 广东东阳光药业有限公司 | 吡喃葡萄糖基衍生物、其制备方法及其在医药上的应用 |
| WO2014159151A1 (en) * | 2013-03-14 | 2014-10-02 | Msd International Gmbh | Methods for preparing sglt2 inhibitors |
| CN104151306A (zh) * | 2013-05-13 | 2014-11-19 | 北京新天宇科技开发有限公司 | 一种坎格列净的新的制备方法 |
| CN104619713B (zh) * | 2013-05-24 | 2017-06-16 | 四川海思科制药有限公司 | 氧杂双环衍生物、制备方法及其应用 |
| WO2014206349A1 (zh) * | 2013-06-28 | 2014-12-31 | 四川海思科制药有限公司 | 氧杂-硫杂-双环[3.2.1]辛烷衍生物、制备方法及其用途 |
| WO2015032272A1 (zh) * | 2013-09-09 | 2015-03-12 | 江苏豪森药业股份有限公司 | C-芳基葡糖苷衍生物、其制备方法及其在医药上的应用 |
| CN104447893B (zh) * | 2013-09-25 | 2018-01-23 | 广东东阳光药业有限公司 | 吡喃葡萄糖基衍生物及其在医药上的应用 |
| US9394329B2 (en) * | 2013-09-27 | 2016-07-19 | Sunshine Lake Pharma Co., Ltd. | Glucopyranosyl derivatives and their uses in medicine |
| BR112016015578A2 (pt) * | 2014-01-03 | 2017-08-08 | Elexopharm Gmbh | Inibidores de 17beta-hidroxiesteroide desidrogenases tipo 1 e tipo 2 |
| BR112016026809A2 (pt) | 2014-05-19 | 2017-12-12 | Pfizer | compostos de 6,8-dioxabiciclo[3.2.1]octano-2,3-diol substituído como agentes de alvejamento de asgpr |
| CN104017031A (zh) * | 2014-06-21 | 2014-09-03 | 李友香 | 降血糖药物和组合物 |
| CN104031098A (zh) * | 2014-06-21 | 2014-09-10 | 李友香 | 降糖药物 |
| CN105294785A (zh) * | 2014-07-02 | 2016-02-03 | 上海阳帆医药科技有限公司 | C-苯并五元杂芳环类芳基葡萄糖苷衍生物及其制备方法与用途 |
| US20160002275A1 (en) * | 2014-07-03 | 2016-01-07 | Cadila Healthcare Limited | Process for preparation and purification of canagliflozin |
| CN104119324B (zh) * | 2014-07-23 | 2016-03-30 | 齐鲁天和惠世制药有限公司 | 一种卡格列净的制备方法 |
| CN105461762B (zh) * | 2014-09-27 | 2018-12-04 | 广东东阳光药业有限公司 | 吡喃葡萄糖基衍生物及其在医药上的应用 |
| PL3202772T3 (pl) | 2014-09-30 | 2021-02-22 | Jiangsu Hengrui Medicine Co. Ltd. | Kryształ kompleksu inhibitora l-proliny/glukozy sodowej 2 |
| US20170342100A1 (en) * | 2014-12-03 | 2017-11-30 | Sun Pharmaceutical Industries Limited | Processes for the preparation of ertugliflozin |
| US10294239B2 (en) | 2015-05-25 | 2019-05-21 | Sun Pharmaceutical Industries Limited | Ertugliflozin co-crystals and process for their preparation |
| CN108699098B (zh) * | 2016-01-04 | 2022-01-25 | 第一药品株式会社 | 具有稠合苯环的c-葡糖苷衍生物或其药物学可接受的盐、其制备方法以及包含其的药物组合物 |
| CN106955273B (zh) * | 2016-01-11 | 2020-10-20 | 江苏恒瑞医药股份有限公司 | 一种含有钠-葡萄糖协同转运蛋白2抑制剂的药物组合物 |
| CN107686496B (zh) * | 2016-08-05 | 2021-01-19 | 江苏恒瑞医药股份有限公司 | 一种钠-葡萄糖协同转运蛋白2抑制剂的制备方法 |
| CN106674245B (zh) * | 2017-01-10 | 2019-07-26 | 北京中海康医药科技发展有限公司 | 吡喃葡萄糖基衍生物的制备及医药上的应用 |
| CN109549939A (zh) * | 2017-09-26 | 2019-04-02 | 江苏恒瑞医药股份有限公司 | Sglt2抑制剂和dpp-4抑制剂联合在制备治疗糖尿病的药物中的用途 |
| CN109806397A (zh) * | 2017-11-20 | 2019-05-28 | 江苏恒瑞医药股份有限公司 | Sglt2抑制剂与arb联合在制备治疗高血压等疾病的药物中的用途 |
| WO2020039394A1 (en) | 2018-08-24 | 2020-02-27 | Novartis Ag | New drug combinations |
| CN113004349A (zh) * | 2019-12-19 | 2021-06-22 | 上海研健新药研发有限公司 | 一种SGLTs抑制剂的制备方法及其关键中间体 |
| WO2021121270A1 (zh) * | 2019-12-19 | 2021-06-24 | 上海研健新药研发有限公司 | 一种SGLTs抑制剂的纯化方法及其应用 |
| WO2021176096A1 (en) | 2020-03-05 | 2021-09-10 | Krka, D.D., Novo Mesto | Pharmaceutical composition comprising sglt2 inhibitor |
| EP4161912A1 (en) | 2020-06-05 | 2023-04-12 | KRKA, d.d., Novo mesto | Preparation of highly pure amorphous dapagliflozin |
| CN114195748B (zh) * | 2020-09-17 | 2023-11-14 | 上海森辉医药有限公司 | 一种钠-葡萄糖协同转运蛋白2抑制剂的制备方法 |
| CN112375087A (zh) * | 2020-11-27 | 2021-02-19 | 浙江天宇药业股份有限公司 | 一种脯氨酸恒格列净的合成方法 |
| CN113880701A (zh) * | 2021-10-10 | 2022-01-04 | 浙江司太立制药股份有限公司 | 一种抗糖尿病药物中间体及其制备方法 |
| CN116785268A (zh) * | 2022-03-14 | 2023-09-22 | 江苏万邦生化医药集团有限责任公司 | 一种sglt-2抑制剂的药物组合物 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| ATE318272T1 (de) * | 2001-04-11 | 2006-03-15 | Bristol Myers Squibb Co | Aminosäurekomplexe von c-arylglycosiden zur behandlung von diabetes und verfahren |
| TWI254635B (en) | 2002-08-05 | 2006-05-11 | Yamanouchi Pharma Co Ltd | Azulene derivative and salt thereof |
| AU2004220222B2 (en) * | 2003-03-14 | 2009-10-01 | Astellas Pharma Inc. | C-glycoside derivatives and salts thereof |
| NZ575711A (en) | 2003-08-01 | 2010-05-28 | Mitsubishi Tanabe Pharma Corp | Novel compounds having inhibitory activity against sodium-dependant transporter |
| EP2074130A1 (en) * | 2006-09-21 | 2009-07-01 | Boehringer Ingelheim International GmbH | Glucopyranosyl-substituted difluorobenzyl-benzene derivatives, medicaments containing such compounds, their use and process for their manufacture |
| ES2654894T3 (es) | 2007-08-23 | 2018-02-15 | Theracos Sub, Llc | Derivados de (2S,3R,4R,5S,6R)-2-(4-cloro-3-bencilfenil)-6-(hidroximetil)tetrahidro-2H-piran-3,4,5-triol para su uso en el tratamiento de diabetes |
| WO2010009243A1 (en) * | 2008-07-15 | 2010-01-21 | Theracos, Inc. | Deuterated benzylbenzene derivatives and methods of use |
| CA2935838C (en) | 2008-08-22 | 2018-04-17 | Theracos Sub, Llc | Processes for the preparation of sglt2 inhibitors |
| PE20110288A1 (es) * | 2008-08-28 | 2011-05-26 | Pfizer | Derivados de dioxa-biciclo[3.2.1]octano-2,3,4-triol |
| US20100167988A1 (en) | 2008-10-22 | 2010-07-01 | Auspex Pharmaceuticals, Inc. | Ethoxyphenylmethyl inhibitors of sglt2 |
| WO2010074219A1 (ja) * | 2008-12-26 | 2010-07-01 | アステラス製薬株式会社 | ベンゾチオフェン化合物 |
| HRP20150107T1 (xx) | 2009-11-02 | 2015-03-13 | Pfizer Inc. | Derivati dioksabiciklo[3.2.1]oktan-2,3,4-triola |
| AR086922A1 (es) * | 2011-06-13 | 2014-01-29 | Panacea Biotec Ltd | Derivados de 3,4,5-trihidroxi-6-(hidroximetil)tetrahidro-2h-pirano utiles para el tratamiento de diabetes y dislipidemias, composiciones farmaceuticas que los contienen y metodo para prepararlos |
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- 2011-06-30 KR KR1020137005058A patent/KR101862891B1/ko not_active Expired - Fee Related
- 2011-06-30 US US13/813,045 patent/US8609622B2/en not_active Expired - Fee Related
- 2011-06-30 RU RU2013107748A patent/RU2606501C2/ru active
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