HRP20170093T1 - Kombinacije koje sadrže derivate 6-benzilfenil-2-sumporterahidropiran-3,4,5-triola kao inhibitore kotransportera natrijeve-glukoze 1 i 2 za uporabu kod pacijenata s dijabetesom - Google Patents
Kombinacije koje sadrže derivate 6-benzilfenil-2-sumporterahidropiran-3,4,5-triola kao inhibitore kotransportera natrijeve-glukoze 1 i 2 za uporabu kod pacijenata s dijabetesom Download PDFInfo
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- HRP20170093T1 HRP20170093T1 HRP20170093TT HRP20170093T HRP20170093T1 HR P20170093 T1 HRP20170093 T1 HR P20170093T1 HR P20170093T T HRP20170093T T HR P20170093TT HR P20170093 T HRP20170093 T HR P20170093T HR P20170093 T1 HRP20170093 T1 HR P20170093T1
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- aryl
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- 239000003112 inhibitor Substances 0.000 title claims 6
- 206010012601 diabetes mellitus Diseases 0.000 title claims 2
- 102000000070 Sodium-Glucose Transport Proteins Human genes 0.000 title 1
- 108010080361 Sodium-Glucose Transport Proteins Proteins 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 108091006277 SLC5A1 Proteins 0.000 claims 5
- 102000058090 Sodium-Glucose Transporter 1 Human genes 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000004404 heteroalkyl group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 229940090124 dipeptidyl peptidase 4 (dpp-4) inhibitors for blood glucose lowering Drugs 0.000 claims 2
- 230000009977 dual effect Effects 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 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 group 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
- 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 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000036772 blood pressure Effects 0.000 claims 1
- 230000036996 cardiovascular health Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- IXZISFNWUWKBOM-ARQDHWQXSA-N fructosamine Chemical compound NC[C@@]1(O)OC[C@@H](O)[C@@H](O)[C@@H]1O IXZISFNWUWKBOM-ARQDHWQXSA-N 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 230000010034 metabolic health Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229960004034 sitagliptin Drugs 0.000 claims 1
- 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 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/32—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Animal Behavior & Ethology (AREA)
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- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Molecular Biology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Saccharide Compounds (AREA)
- Pyrane Compounds (AREA)
Claims (12)
1. Doza od 300 mg/dan ili manje (npr., 250, 200, 150, 100, ili 50 mg/dan ili manje) dvostrukog inhibitora SGLT1/2 prema formuli:
[image]
ili njegova farmaceutski prihvatljiva sol, naznačena time da je namijenjena upotrebi za poboljšanje kardiovaskularnog ili metaboličkog zdravlja dijabetičara ili pred-dijabetičkog pacijenta koji trenutno uzima DPP-4 inhibitor, pri čemu:
svaki R1A je neovisno vodik, alkil, aril ili heterocikal;
svaki R6 je neovisno vodik, hidroksil, amino, alkil, aril, cijano, halogen, heteroalkil, heterocikal, nitro, C≡CR6A, OR6A, SR6A, SOR6A, SO2R6A, C(O)R6A, CO2R6A, CO2H, CON(R6A)(R6A), CONH(R6A), CONH2, NHC(O)R6A, ili NHSO2R6A;
svaki R6A je neovisno alkil, aril ili heterocikal;
svaki R7 je neovisno vodik, hidroksil, amino, alkil, aril, cijano, halogen, heteroalkil, heterocikal, nitro, C≡CR7A, OR7A, SR7A, SOR7A, SO2R7A, C(O)R7A, CO2R7A, CO2H, CON(R7A)(R7A), CONH(R7A), CONH2, NHC(O)R7A, ili NHSO2R7A;
svaki R7A je neovisno alkil, aril ili heterocikal;
m je 1-4;
n je 1-3;
p je 0-2; i
pri čemu svaki alkil, aril, heteroalkil ili heterocikal je proizvoljno supstituiran s jednim ili više od alkoksi, amino, cijano, halo, hidroksil, ili nitro, te pri čemu inhibitor DPP-4 je sitagliptin.
2. Doza za uporabu prema zahtjevu 1, naznačena time da poboljšanje je snižavanje razine glukoze u plazmi natašte kod pacijenta za više od oko 50, 55, ili 60 mg/dl.
3. Doza za uporabu prema zahtjevu 1, naznačena time da poboljšanje je snižavanje razine HbA1c kod pacijenta za više od oko 1.0, 1.1, ili 1.2 posto.
4. Doza za uporabu prema zahtjevu 1, naznačena time da poboljšanje je snižavanje razine fruktozamina u plazmi kod pacijenta za više od oko 30, 40, ili 50 µmol/l.
5. Doza za uporabu prema zahtjevu 1, naznačena time da poboljšanje je snižavanje krvnog tlaka kod pacijenta.
6. Doza za uporabu prema zahtjevu 1, naznačena time da poboljšanje je snižavanje razina triglicerida kod pacijenta.
7. Doza za uporabu prema zahtjevu 1, naznačena time da je dvostruki inhibitor SGLT1/2 prema formuli:
[image]
8. Doza za uporabu prema zahtjevu 7, naznačena time da je dvostruki inhibitor SGLT1/2 prema formuli:
[image]
9. Doza za uporabu prema zahtjevu 8, naznačena time da je dvostruki inhibitor SGLT1/2 prema formuli:
[image]
10. Doza za uporabu prema zahtjevu 9, naznačena time da R7A je metil ili etil.
11. Doza za uporabu prema zahtjevu 9, naznačena time da R1A je metil.
12. Doza za uporabu prema zahtjevu 11, naznačena time da dvostruki inhibitor SGLT1/2 je (2S,3R,4R,5S,6R)-2-(4-klor-3-(4-etoksibenzil)fenil)-6-(metiltio)tetrahidro-2H-piran-3,4,5-triol.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30959210P | 2010-03-02 | 2010-03-02 | |
| EP11707324.7A EP2542236B1 (en) | 2010-03-02 | 2011-03-01 | Combinations comprising 6-benzylphenyl-2- sulfurterahydropyran-3,4,5-triol derivatives as inhibitors of sodium -glucose cotransporters 1 and 2 for use in diabetic patients |
| PCT/US2011/026591 WO2011109333A1 (en) | 2010-03-02 | 2011-03-01 | 6 -benzylphenyl- 2 - sulfurterahydropyran-3, 4, 5 -triol derivatives as inhibitors of sodium -glucose cotrans porters 1 and 2 for use in diabetic patients |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20170093T1 true HRP20170093T1 (hr) | 2017-03-24 |
Family
ID=43795398
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20170093TT HRP20170093T1 (hr) | 2010-03-02 | 2017-01-20 | Kombinacije koje sadrže derivate 6-benzilfenil-2-sumporterahidropiran-3,4,5-triola kao inhibitore kotransportera natrijeve-glukoze 1 i 2 za uporabu kod pacijenata s dijabetesom |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US20110218159A1 (hr) |
| EP (1) | EP2542236B1 (hr) |
| JP (2) | JP6126383B2 (hr) |
| KR (2) | KR20130026422A (hr) |
| CN (1) | CN102821764A (hr) |
| AR (1) | AR080444A1 (hr) |
| AU (1) | AU2011223861B2 (hr) |
| BR (1) | BR112012021771B1 (hr) |
| CA (1) | CA2791300C (hr) |
| CY (1) | CY1118611T1 (hr) |
| DK (1) | DK2542236T3 (hr) |
| ES (1) | ES2609104T3 (hr) |
| HR (1) | HRP20170093T1 (hr) |
| HU (1) | HUE031441T2 (hr) |
| IL (1) | IL221372A0 (hr) |
| LT (1) | LT2542236T (hr) |
| MX (1) | MX342423B (hr) |
| PL (1) | PL2542236T3 (hr) |
| PT (1) | PT2542236T (hr) |
| RS (1) | RS55620B1 (hr) |
| RU (1) | RU2012141893A (hr) |
| SI (1) | SI2542236T1 (hr) |
| TW (1) | TWI562775B (hr) |
| WO (1) | WO2011109333A1 (hr) |
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| 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 |
| PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| NZ619413A (en) | 2006-05-04 | 2015-08-28 | Boehringer Ingelheim Int | Polymorphs of a dpp-iv enzyme inhibitor |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| 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 |
| BRPI0916997A2 (pt) | 2008-08-06 | 2020-12-15 | Boehringer Ingelheim International Gmbh | Inibidor de dpp-4 e seu uso |
| 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 |
| KR20210033559A (ko) | 2009-11-27 | 2021-03-26 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| 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 |
| EP2849755A1 (en) | 2012-05-14 | 2015-03-25 | Boehringer Ingelheim International GmbH | A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome |
| KR102165224B1 (ko) * | 2012-11-20 | 2020-10-13 | 렉시컨 파마슈티컬스 인코퍼레이티드 | 나트륨 글루코스 공동수송체 1의 억제제 |
| KR102238860B1 (ko) * | 2013-06-14 | 2021-04-12 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 및 이의 합병증의 치료를 위한 dpp-4 억제제 |
| 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 |
| US10166246B2 (en) | 2014-05-27 | 2019-01-01 | City Of Hope | TGR5 agonist complexes for treating diabetes and cancer |
| WO2017202351A1 (zh) * | 2016-05-25 | 2017-11-30 | 苏州科睿思制药有限公司 | 一种钠-葡萄糖协同转运蛋白抑制剂药物的新晶型及其制备方法和用途 |
| WO2017211979A1 (en) | 2016-06-10 | 2017-12-14 | Boehringer Ingelheim International Gmbh | Combinations of linagliptin and metformin |
| CN110066302B (zh) | 2018-01-23 | 2022-12-27 | 广东东阳光药业有限公司 | 吡喃葡萄糖基衍生物及其用途 |
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- 2011-03-01 JP JP2012556154A patent/JP6126383B2/ja active Active
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