JP2017515908A5 - - Google Patents

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Publication number: JP2017515908A5
Authority: JP; Japan
Prior art keywords: inhibitor; pharmaceutical composition; composition according; sglt2; dpp
Prior art date: 2015-05-14
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

Application number

JP2017512456A

Other languages

English (en)

Japanese (ja)

Other versions

JP2017515908A (ja

Filing date

2015-05-14

Publication date

2018-04-19

2015-05-14 Application filed filed Critical

2015-05-14 Priority claimed from PCT/GB2015/051437 external-priority patent/WO2015173584A1/en

2017-06-15 Publication of JP2017515908A publication Critical patent/JP2017515908A/ja

2018-04-19 Publication of JP2017515908A5 publication Critical patent/JP2017515908A5/ja

Status Pending legal-status Critical Current

Links

239000003112 inhibitor Substances 0.000 claims 18
239000008194 pharmaceutical composition Substances 0.000 claims 17
102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 13
108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 8
241000124008 Mammalia Species 0.000 claims 7
101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 claims 5
150000002148 esters Chemical class 0.000 claims 5
229940002612 prodrug Drugs 0.000 claims 5
239000000651 prodrug Substances 0.000 claims 5
150000003839 salts Chemical class 0.000 claims 5
102000051325 Glucagon Human genes 0.000 claims 4
108060003199 Glucagon Proteins 0.000 claims 4
102100020888 Sodium/glucose cotransporter 2 Human genes 0.000 claims 4
101710103228 Sodium/glucose cotransporter 2 Proteins 0.000 claims 4
239000000556 agonist Substances 0.000 claims 4
MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)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(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 4
229960004666 glucagon Drugs 0.000 claims 4
230000028327 secretion Effects 0.000 claims 4
239000003472 antidiabetic agent Substances 0.000 claims 3
229960004937 saxagliptin Drugs 0.000 claims 3
QGJUIPDUBHWZPV-SGTAVMJGSA-N saxagliptin Chemical group C1C(C2)CC(C3)CC2(O)CC13[C@H](N)C(=O)N1[C@H](C#N)C[C@@H]2C[C@@H]21 QGJUIPDUBHWZPV-SGTAVMJGSA-N 0.000 claims 3
108010033693 saxagliptin Proteins 0.000 claims 3
229940123208 Biguanide Drugs 0.000 claims 2
JVHXJTBJCFBINQ-ADAARDCZSA-N Dapagliflozin Chemical group 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 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
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 2
108010016731 PPAR gamma Proteins 0.000 claims 2
229940123518 Sodium/glucose cotransporter 2 inhibitor Drugs 0.000 claims 2
229940125708 antidiabetic agent Drugs 0.000 claims 2
229960003834 dapagliflozin Drugs 0.000 claims 2
206010012601 diabetes mellitus Diseases 0.000 claims 2
239000008103 glucose Substances 0.000 claims 2
NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
229960002397 linagliptin Drugs 0.000 claims 2
229960001254 vildagliptin Drugs 0.000 claims 2
SYOKIDBDQMKNDQ-XWTIBIIYSA-N vildagliptin Chemical compound C1C(O)(C2)CC(C3)CC1CC32NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-XWTIBIIYSA-N 0.000 claims 2
QKDRXGFQVGOQKS-CRSSMBPESA-N (2s,3r,4r,5s,6r)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-methylsulfanyloxane-3,4,5-triol Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](SC)O2)O)=CC=C1Cl QKDRXGFQVGOQKS-CRSSMBPESA-N 0.000 claims 1
AOBLNYCSGWSIPG-YRIDSSQKSA-N (2s,3r,4s,5s,6r)-2-[4-[(2-fluoro-4-methoxyphenyl)methyl]-5-methyl-1-propan-2-ylpyrazol-3-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound FC1=CC(OC)=CC=C1CC1=C(C)N(C(C)C)N=C1O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 AOBLNYCSGWSIPG-YRIDSSQKSA-N 0.000 claims 1
SWLAMJPTOQZTAE-UHFFFAOYSA-N 4-[2-[(5-chloro-2-methoxybenzoyl)amino]ethyl]benzoic acid Chemical compound COC1=CC=C(Cl)C=C1C(=O)NCCC1=CC=C(C(O)=O)C=C1 SWLAMJPTOQZTAE-UHFFFAOYSA-N 0.000 claims 1
XNCOSPRUTUOJCJ-UHFFFAOYSA-N Biguanide Chemical compound NC(N)=NC(N)=N XNCOSPRUTUOJCJ-UHFFFAOYSA-N 0.000 claims 1
102000030914 Fatty Acid-Binding Human genes 0.000 claims 1
102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 claims 1
108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims 1
102000004366 Glucosidases Human genes 0.000 claims 1
108010056771 Glucosidases Proteins 0.000 claims 1
102000007390 Glycogen Phosphorylase Human genes 0.000 claims 1
108010046163 Glycogen Phosphorylase Proteins 0.000 claims 1
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
102100023915 Insulin Human genes 0.000 claims 1
108090001061 Insulin Proteins 0.000 claims 1
WHSOLWOTCHFFBK-ZQGJOIPISA-N Luseogliflozin Chemical compound C1=CC(OCC)=CC=C1CC1=CC([C@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)S2)O)=C(OC)C=C1C WHSOLWOTCHFFBK-ZQGJOIPISA-N 0.000 claims 1
108010028924 PPAR alpha Proteins 0.000 claims 1
102000023984 PPAR alpha Human genes 0.000 claims 1
102000000536 PPAR gamma Human genes 0.000 claims 1
102100038831 Peroxisome proliferator-activated receptor alpha Human genes 0.000 claims 1
102100038825 Peroxisome proliferator-activated receptor gamma Human genes 0.000 claims 1
229940100389 Sulfonylurea Drugs 0.000 claims 1
102000003673 Symporters Human genes 0.000 claims 1
108090000088 Symporters Proteins 0.000 claims 1
229940123464 Thiazolidinedione Drugs 0.000 claims 1
ZXOCGDDVNPDRIW-NHFZGCSJSA-N Tofogliflozin Chemical compound O.C1=CC(CC)=CC=C1CC1=CC=C(CO[C@@]23[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O3)O)C2=C1 ZXOCGDDVNPDRIW-NHFZGCSJSA-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
229940127003 anti-diabetic drug Drugs 0.000 claims 1
150000004283 biguanides Chemical class 0.000 claims 1
229960001713 canagliflozin Drugs 0.000 claims 1
VHOFTEAWFCUTOS-TUGBYPPCSA-N canagliflozin hydrate Chemical compound O.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.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 VHOFTEAWFCUTOS-TUGBYPPCSA-N 0.000 claims 1
238000011260 co-administration Methods 0.000 claims 1
230000009977 dual effect Effects 0.000 claims 1
229960003345 empagliflozin Drugs 0.000 claims 1
OBWASQILIWPZMG-QZMOQZSNSA-N empagliflozin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(Cl)C(CC=2C=CC(O[C@@H]3COCC3)=CC=2)=C1 OBWASQILIWPZMG-QZMOQZSNSA-N 0.000 claims 1
108091022862 fatty acid binding Proteins 0.000 claims 1
229960004580 glibenclamide Drugs 0.000 claims 1
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 1
230000002641 glycemic effect Effects 0.000 claims 1
230000002440 hepatic effect Effects 0.000 claims 1
229940125396 insulin Drugs 0.000 claims 1
229950000991 ipragliflozin Drugs 0.000 claims 1
AHFWIQIYAXSLBA-RQXATKFSSA-N ipragliflozin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1C1=CC=C(F)C(CC=2SC3=CC=CC=C3C=2)=C1 AHFWIQIYAXSLBA-RQXATKFSSA-N 0.000 claims 1
229950004397 luseogliflozin Drugs 0.000 claims 1
229950004994 meglitinide Drugs 0.000 claims 1
XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 1
229960003105 metformin Drugs 0.000 claims 1
108091008725 peroxisome proliferator-activated receptors alpha Proteins 0.000 claims 1
GCYXWQUSHADNBF-AAEALURTSA-N preproglucagon 78-108 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(=O)NCC(O)=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 GCYXWQUSHADNBF-AAEALURTSA-N 0.000 claims 1
229910052708 sodium Inorganic materials 0.000 claims 1
239000011734 sodium Substances 0.000 claims 1
YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 claims 1
238000002560 therapeutic procedure Methods 0.000 claims 1
150000001467 thiazolidinediones Chemical class 0.000 claims 1
229950006667 tofogliflozin Drugs 0.000 claims 1
208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1

JP2017512456A 2014-05-16 2015-05-14 Ｓｇｌｔ２インヒビター誘発性グルカゴン分泌の抑制方法 Pending JP2017515908A (ja)

Applications Claiming Priority (5)

Application Number	Priority Date	Filing Date	Title
US201461994222P	2014-05-16	2014-05-16
US61/994,222		2014-05-16
US201462011084P	2014-06-12	2014-06-12
US62/011,084		2014-06-12
PCT/GB2015/051437 WO2015173584A1 (en)	2014-05-16	2015-05-14	Method for suppressing glucagon secretion of an sglt2 inhibitor

Publications (2)

Publication Number	Publication Date
JP2017515908A JP2017515908A (ja)	2017-06-15
JP2017515908A5 true JP2017515908A5 (2)	2018-04-19

Family

ID=53276183

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2017512456A Pending JP2017515908A (ja)	2014-05-16	2015-05-14	Ｓｇｌｔ２インヒビター誘発性グルカゴン分泌の抑制方法

Country Status (7)

Country	Link
US (1)	US20170135981A1 (2)
EP (1)	EP3142661B1 (2)
JP (1)	JP2017515908A (2)
CN (1)	CN106714796A (2)
ES (1)	ES2900843T3 (2)
TW (1)	TW201607540A (2)
WO (1)	WO2015173584A1 (2)

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US9902751B2 (en)	2013-12-30	2018-02-27	Mylan Laboratories Limited	Process for the preparation of empagliflozin
EP3698801B1 (en) *	2017-10-20	2024-09-04	Novmetapharma Co., Ltd.	Pharmaceutical composition for preventing or treating diabetes, containing zinc salt, cyclo-hispro and antidiabetic drug as active ingredients
KR20260037123A (ko)	2017-11-30	2026-03-17	이도르시아 파마슈티컬스 리미티드	엔도텔린 관련 질병의 치료를 위한 sglt-2 저해제와의 4-피리미딘설파미드 유도체의 병용
US11033544B2 (en) *	2019-03-25	2021-06-15	The George Institute for Global Health	Low-dose triple combination formulation
CN110327355B (zh) *	2019-08-12	2021-06-04	浙江养生堂天然药物研究所有限公司	包含柠檬苦素类化合物和sglt-2抑制剂的组合产品
EP4064854A1 (en)	2019-11-28	2022-10-05	Boehringer Ingelheim Vetmedica GmbH	Use of sglt-2 inhibitors in the drying-off of non-human mammals
CN111588713B (zh) *	2020-06-22	2021-03-09	广州市力鑫药业有限公司	一种治疗糖尿病的药物组合物及其制备方法
CA3224527A1 (en) *	2021-07-26	2023-02-02	Balvir SINGH	A pharmaceutical composition comprising combination of sglt2 inhibitor and dpp-iv inhibitor
WO2023227492A1 (en)	2022-05-25	2023-11-30	Boehringer Ingelheim Vetmedica Gmbh	Aqueous pharmaceutical compositions comprising sglt-2 inhibitors

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US6515117B2 (en) *	1999-10-12	2003-02-04	Bristol-Myers Squibb Company	C-aryl glucoside SGLT2 inhibitors and method
WO2002083066A2 (en) *	2001-04-11	2002-10-24	Bristol-Myers Squibb Company	Amino acid complexes of c-aryl glucosides for treatment of diabetes and method
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.
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
WO2013158939A1 (en) *	2012-04-18	2013-10-24	Hemoshear, Llc	In vitro model for pathological or physiologic conditions
CA2812016A1 (en) *	2013-04-05	2014-10-05	Boehringer Ingelheim International Gmbh	Pharmaceutical composition, methods for treating and uses thereof

2015
- 2015-05-14 EP EP15726257.7A patent/EP3142661B1/en not_active Revoked
- 2015-05-14 US US15/311,203 patent/US20170135981A1/en not_active Abandoned
- 2015-05-14 ES ES15726257T patent/ES2900843T3/es active Active
- 2015-05-14 JP JP2017512456A patent/JP2017515908A/ja active Pending
- 2015-05-14 WO PCT/GB2015/051437 patent/WO2015173584A1/en not_active Ceased
- 2015-05-14 CN CN201580038266.8A patent/CN106714796A/zh active Pending
- 2015-05-15 TW TW104115641A patent/TW201607540A/zh unknown

Publication	Publication Date	Title
JP2017515908A5 (2)	2018-04-19
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FI3716979T3 (fi)	2025-07-08	4-pyrimidiinisulfamidijohdannaisen ja SGLT-2-inhibiittorin yhdistelmä endoteliiniin liittyvien sairauksien hoitamiseksi
CL2011001735A1 (es)	2011-10-28	Composicion farmaceutica que comprende: a) el inhibidor de sglt2 1-cloro-4-(b-d-glucopiranos-1-il)-2-[4-((s)-tetrahidrofurano-3-iloxi)-bencil]-benceno, b) el inhibidor de dppiv linagliptina y c) un tercer agente antidiabetico que es clorhidrato de metformina; y su uso para tratar la diabetes mellitus tipo 2.
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JP2019535791A5 (2)	2020-12-17
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BR112021017315A2 (pt)	2021-11-16	Usos terapêuticos de dulaglutida
CO2022004572A2 (es)	2022-07-08	Tratamiento de la diabetes mellitus tipo 2
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BR112021024099A2 (pt)	2022-01-11	Composição farmacêutica para diabetes mellitus