JPWO2020194046A5 - - Google Patents
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- Publication number
- JPWO2020194046A5 JPWO2020194046A5 JP2021556883A JP2021556883A JPWO2020194046A5 JP WO2020194046 A5 JPWO2020194046 A5 JP WO2020194046A5 JP 2021556883 A JP2021556883 A JP 2021556883A JP 2021556883 A JP2021556883 A JP 2021556883A JP WO2020194046 A5 JPWO2020194046 A5 JP WO2020194046A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- dose
- metformin
- sitagliptin
- glimepiride
- 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.)
- Pending
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 59
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical group CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 25
- 206010012601 diabetes mellitus Diseases 0.000 claims 23
- 229960004034 sitagliptin Drugs 0.000 claims 21
- 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 21
- 229960003105 metformin Drugs 0.000 claims 20
- 229940100389 Sulfonylurea Drugs 0.000 claims 19
- 229960004346 glimepiride Drugs 0.000 claims 19
- WIGIZIANZCJQQY-RUCARUNLSA-N glimepiride Chemical compound O=C1C(CC)=C(C)CN1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)N[C@@H]2CC[C@@H](C)CC2)C=C1 WIGIZIANZCJQQY-RUCARUNLSA-N 0.000 claims 19
- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 17
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 16
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 16
- 239000003112 inhibitor Substances 0.000 claims 16
- 238000011287 therapeutic dose Methods 0.000 claims 15
- 229940123208 Biguanide Drugs 0.000 claims 14
- XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 14
- 239000003472 antidiabetic agent Substances 0.000 claims 13
- 230000000291 postprandial effect Effects 0.000 claims 8
- 229940127003 anti-diabetic drug Drugs 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 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 5
- 239000008103 glucose Substances 0.000 claims 5
- 230000010030 glucose lowering effect Effects 0.000 claims 5
- 229960004329 metformin hydrochloride Drugs 0.000 claims 5
- OETHQSJEHLVLGH-UHFFFAOYSA-N metformin hydrochloride Chemical group Cl.CN(C)C(=N)N=C(N)N OETHQSJEHLVLGH-UHFFFAOYSA-N 0.000 claims 5
- 230000003178 anti-diabetic effect Effects 0.000 claims 4
- 201000001421 hyperglycemia Diseases 0.000 claims 4
- 208000030159 metabolic disease Diseases 0.000 claims 4
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 3
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 3
- 239000008280 blood Substances 0.000 claims 3
- 210000004369 blood Anatomy 0.000 claims 3
- 230000002195 synergetic effect Effects 0.000 claims 3
- 238000002054 transplantation Methods 0.000 claims 3
- 208000002705 Glucose Intolerance Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 206010033307 Overweight Diseases 0.000 claims 2
- 230000002058 anti-hyperglycaemic effect Effects 0.000 claims 2
- 229940000425 combination drug Drugs 0.000 claims 2
- 208000004104 gestational diabetes Diseases 0.000 claims 2
- 229960004580 glibenclamide Drugs 0.000 claims 2
- ZNNLBTZKUZBEKO-UHFFFAOYSA-N glyburide Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZNNLBTZKUZBEKO-UHFFFAOYSA-N 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 201000009104 prediabetes syndrome Diseases 0.000 claims 2
- 230000008085 renal dysfunction Effects 0.000 claims 2
- 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
- LLJFMFZYVVLQKT-UHFFFAOYSA-N 1-cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-2-isoquinolinyl)ethyl]phenyl]sulfonylurea Chemical compound C=1C(OC)=CC=C(C(C2=O)(C)C)C=1C(=O)N2CCC(C=C1)=CC=C1S(=O)(=O)NC(=O)NC1CCCCC1 LLJFMFZYVVLQKT-UHFFFAOYSA-N 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
- 102000016622 Dipeptidyl Peptidase 4 Human genes 0.000 claims 1
- DVJAMEIQRSHVKC-BDAKNGLRSA-N Dutogliptin Chemical compound OB(O)[C@@H]1CCCN1C(=O)CN[C@H]1CNCC1 DVJAMEIQRSHVKC-BDAKNGLRSA-N 0.000 claims 1
- LCDDAGSJHKEABN-MLGOLLRUSA-N Evogliptin Chemical compound C1CNC(=O)[C@@H](COC(C)(C)C)N1C(=O)C[C@H](N)CC1=CC(F)=C(F)C=C1F LCDDAGSJHKEABN-MLGOLLRUSA-N 0.000 claims 1
- ZWPRRQZNBDYKLH-VIFPVBQESA-N Gemigliptin Chemical compound C([C@@H](N)CC(=O)N1CC2=C(C(=NC(=N2)C(F)(F)F)C(F)(F)F)CC1)N1CC(F)(F)CCC1=O ZWPRRQZNBDYKLH-VIFPVBQESA-N 0.000 claims 1
- 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 1
- HNSCCNJWTJUGNQ-UHFFFAOYSA-N Glyclopyramide Chemical compound C1=CC(Cl)=CC=C1S(=O)(=O)NC(=O)NN1CCCC1 HNSCCNJWTJUGNQ-UHFFFAOYSA-N 0.000 claims 1
- LTXREWYXXSTFRX-QGZVFWFLSA-N Linagliptin Chemical compound N=1C=2N(C)C(=O)N(CC=3N=C4C=CC=CC4=C(C)N=3)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 LTXREWYXXSTFRX-QGZVFWFLSA-N 0.000 claims 1
- JLRGJRBPOGGCBT-UHFFFAOYSA-N Tolbutamide Chemical compound CCCCNC(=O)NS(=O)(=O)C1=CC=C(C)C=C1 JLRGJRBPOGGCBT-UHFFFAOYSA-N 0.000 claims 1
- 230000005856 abnormality Effects 0.000 claims 1
- 229960001466 acetohexamide Drugs 0.000 claims 1
- VGZSUPCWNCWDAN-UHFFFAOYSA-N acetohexamide Chemical compound C1=CC(C(=O)C)=CC=C1S(=O)(=O)NC(=O)NC1CCCCC1 VGZSUPCWNCWDAN-UHFFFAOYSA-N 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
- 229950009977 anagliptin Drugs 0.000 claims 1
- LDXYBEHACFJIEL-HNNXBMFYSA-N anagliptin Chemical compound C=1N2N=C(C)C=C2N=CC=1C(=O)NCC(C)(C)NCC(=O)N1CCC[C@H]1C#N LDXYBEHACFJIEL-HNNXBMFYSA-N 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 229960003362 carbutamide Drugs 0.000 claims 1
- VDTNNGKXZGSZIP-UHFFFAOYSA-N carbutamide Chemical compound CCCCNC(=O)NS(=O)(=O)C1=CC=C(N)C=C1 VDTNNGKXZGSZIP-UHFFFAOYSA-N 0.000 claims 1
- 229960001761 chlorpropamide Drugs 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 239000003603 dipeptidyl peptidase IV inhibitor Substances 0.000 claims 1
- 229950003693 dutogliptin Drugs 0.000 claims 1
- 229950011259 evogliptin Drugs 0.000 claims 1
- 229960002458 gemigliptin Drugs 0.000 claims 1
- 229960001764 glibornuride Drugs 0.000 claims 1
- RMTYNAPTNBJHQI-LLDVTBCESA-N glibornuride Chemical compound C1=CC(C)=CC=C1S(=O)(=O)NC(=O)N[C@H]1[C@H](C2(C)C)CC[C@@]2(C)[C@H]1O RMTYNAPTNBJHQI-LLDVTBCESA-N 0.000 claims 1
- 229960000346 gliclazide Drugs 0.000 claims 1
- 229960001381 glipizide Drugs 0.000 claims 1
- ZJJXGWJIGJFDTL-UHFFFAOYSA-N glipizide Chemical compound C1=NC(C)=CN=C1C(=O)NCCC1=CC=C(S(=O)(=O)NC(=O)NC2CCCCC2)C=C1 ZJJXGWJIGJFDTL-UHFFFAOYSA-N 0.000 claims 1
- 229960003468 gliquidone Drugs 0.000 claims 1
- 229960003236 glisoxepide Drugs 0.000 claims 1
- ZKUDBRCEOBOWLF-UHFFFAOYSA-N glisoxepide Chemical compound O1C(C)=CC(C(=O)NCCC=2C=CC(=CC=2)S(=O)(=O)NC(=O)NN2CCCCCC2)=N1 ZKUDBRCEOBOWLF-UHFFFAOYSA-N 0.000 claims 1
- BEBCJVAWIBVWNZ-UHFFFAOYSA-N glycinamide Chemical compound NCC(N)=O BEBCJVAWIBVWNZ-UHFFFAOYSA-N 0.000 claims 1
- 229950002888 glyclopyramide Drugs 0.000 claims 1
- 229950005754 gosogliptin Drugs 0.000 claims 1
- QWEWGXUTRTXFRF-KBPBESRZSA-N gosogliptin Chemical compound C1C(F)(F)CCN1C(=O)[C@H]1NC[C@@H](N2CCN(CC2)C=2N=CC=CN=2)C1 QWEWGXUTRTXFRF-KBPBESRZSA-N 0.000 claims 1
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims 1
- 229960002397 linagliptin Drugs 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 230000004060 metabolic process Effects 0.000 claims 1
- 229960005125 metahexamide Drugs 0.000 claims 1
- XXYTXQGCRQLRHA-UHFFFAOYSA-N metahexamide Chemical compound C1=C(N)C(C)=CC=C1S(=O)(=O)NC(=O)NC1CCCCC1 XXYTXQGCRQLRHA-UHFFFAOYSA-N 0.000 claims 1
- 229950000074 omarigliptin Drugs 0.000 claims 1
- MKMPWKUAHLTIBJ-ISTRZQFTSA-N omarigliptin Chemical compound C1([C@H]2OC[C@@H](C[C@@H]2N)N2CC3=CN(N=C3C2)S(=O)(=O)C)=CC(F)=CC=C1F MKMPWKUAHLTIBJ-ISTRZQFTSA-N 0.000 claims 1
- 239000006187 pill Substances 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
- 229960004115 sitagliptin phosphate Drugs 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 229950000034 teneligliptin Drugs 0.000 claims 1
- 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 1
- RTZRUVMEWWPNRR-UHFFFAOYSA-N tert-butyl n-(3-iodo-1h-pyrrolo[2,3-b]pyridin-5-yl)carbamate Chemical group CC(C)(C)OC(=O)NC1=CN=C2NC=C(I)C2=C1 RTZRUVMEWWPNRR-UHFFFAOYSA-N 0.000 claims 1
- 229960002277 tolazamide Drugs 0.000 claims 1
- OUDSBRTVNLOZBN-UHFFFAOYSA-N tolazamide Chemical compound C1=CC(C)=CC=C1S(=O)(=O)NC(=O)NN1CCCCCC1 OUDSBRTVNLOZBN-UHFFFAOYSA-N 0.000 claims 1
- 229960005371 tolbutamide Drugs 0.000 claims 1
- 229950010728 trelagliptin Drugs 0.000 claims 1
- IWYJYHUNXVAVAA-OAHLLOKOSA-N trelagliptin Chemical compound C=1C(F)=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 IWYJYHUNXVAVAA-OAHLLOKOSA-N 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
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962823575P | 2019-03-25 | 2019-03-25 | |
| US62/823,575 | 2019-03-25 | ||
| PCT/IB2020/000141 WO2020194046A1 (en) | 2019-03-25 | 2020-03-25 | Low-dose triple combination formulation |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022529312A JP2022529312A (ja) | 2022-06-21 |
| JP2022529312A5 JP2022529312A5 (https=) | 2023-04-05 |
| JPWO2020194046A5 true JPWO2020194046A5 (https=) | 2023-04-05 |
Family
ID=72611638
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021556883A Pending JP2022529312A (ja) | 2019-03-25 | 2020-03-25 | 低用量の三重複合製剤 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20220184070A1 (https=) |
| EP (1) | EP3946343A4 (https=) |
| JP (1) | JP2022529312A (https=) |
| KR (1) | KR20220004026A (https=) |
| CN (1) | CN113905738A (https=) |
| AU (1) | AU2020245801A1 (https=) |
| BR (1) | BR112021018973A2 (https=) |
| CA (1) | CA3134799A1 (https=) |
| MX (1) | MX2021011745A (https=) |
| TW (1) | TW202102208A (https=) |
| WO (1) | WO2020194046A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102019112190A1 (de) | 2019-05-09 | 2020-11-12 | Mack Rides Gmbh & Co. Kg | Sperrvorrichtung eines Sicherheitsbügels, Fahrgastaufnahme sowie Vergnügungsfahrgeschäft mit einer solchen Sperrvorrichtung |
| JP7830433B2 (ja) * | 2020-09-02 | 2026-03-16 | ラボラトリオス シラネス、エセ．ア．デ セ．べ． | ２型真性糖尿病の制御及び管理のための配合薬剤 |
| CN113559088A (zh) * | 2021-01-21 | 2021-10-29 | 江苏宇锐医药科技有限公司 | 一种含二甲双胍和西格列汀的复方降糖药物制剂 |
| WO2024043358A1 (ko) * | 2022-08-24 | 2024-02-29 | 동아에스티 주식회사 | 에보글립틴 및 메트포르민을 포함하는 경구용 복합제제 및 그의 제조방법 |
| WO2025090920A1 (en) * | 2023-10-25 | 2025-05-01 | Piton Therapeutics, Inc. | Compositions and methods for treating dysfunction of glucose metabolism and/or regulation |
| CN117599008A (zh) * | 2023-11-14 | 2024-02-27 | 华中药业股份有限公司 | 一种西格列汀二甲双胍缓释片及其制作方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0616694B8 (pt) * | 2005-09-29 | 2021-05-25 | Novartis Ag | processo para preparar comprimido farmacêutico com 80 e 96% em peso com base no peso seco de vildagliptina e metformina ou seus sais farmaceuticamente aceitáveis |
| EP2395988A2 (en) * | 2009-02-13 | 2011-12-21 | Boehringer Ingelheim International GmbH | Antidiabetic medications comprising a dpp-4 inhibitor (linagliptin) optionally in combination with other antidiabetics |
| BRPI1008560B1 (pt) * | 2009-02-13 | 2021-08-31 | Boehringer Ingelheim International Gmbh | Composição farmacêutica compreendendo um inibidor de sglt2, um inibidor de dpp-iv e opcionalmente um outro agente antidiabético e usos dos mesmos |
| US20160151382A1 (en) * | 2013-10-08 | 2016-06-02 | Kevin Ray Pickering | Cooperative Medication Combination Systems |
| US20160067217A1 (en) * | 2014-09-09 | 2016-03-10 | ARKAY Therapeutics, LLC | Metabolic syndrome treatment |
| KR20180002460A (ko) * | 2016-06-29 | 2018-01-08 | 주식회사 엘지화학 | 제2형 당뇨병 및 당뇨성 이상지질혈증 치료용 조성물, 키트 및 병용 요법 |
-
2020
- 2020-03-25 WO PCT/IB2020/000141 patent/WO2020194046A1/en not_active Ceased
- 2020-03-25 AU AU2020245801A patent/AU2020245801A1/en not_active Abandoned
- 2020-03-25 BR BR112021018973A patent/BR112021018973A2/pt not_active IP Right Cessation
- 2020-03-25 KR KR1020217033516A patent/KR20220004026A/ko not_active Ceased
- 2020-03-25 TW TW109110097A patent/TW202102208A/zh unknown
- 2020-03-25 JP JP2021556883A patent/JP2022529312A/ja active Pending
- 2020-03-25 CA CA3134799A patent/CA3134799A1/en active Pending
- 2020-03-25 EP EP20777507.3A patent/EP3946343A4/en not_active Withdrawn
- 2020-03-25 CN CN202080039014.8A patent/CN113905738A/zh active Pending
- 2020-03-25 US US17/598,122 patent/US20220184070A1/en not_active Abandoned
- 2020-03-25 MX MX2021011745A patent/MX2021011745A/es unknown
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