ME02573B - Farmaceutska kompozicija koja sadrži glukopiranozilom supstituisani derivat benzena - Google Patents
Farmaceutska kompozicija koja sadrži glukopiranozilom supstituisani derivat benzenaInfo
- Publication number
- ME02573B ME02573B MEP-2016-255A MEP25516A ME02573B ME 02573 B ME02573 B ME 02573B ME P25516 A MEP25516 A ME P25516A ME 02573 B ME02573 B ME 02573B
- Authority
- ME
- Montenegro
- Prior art keywords
- pharmaceutical composition
- inhibitor
- glucopyranosyl
- dpp
- substituted benzene
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims 21
- 125000001997 phenyl group Chemical class [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 title 1
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 10
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 10
- 239000003112 inhibitor Substances 0.000 claims 10
- 150000001555 benzenes Chemical class 0.000 claims 9
- 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 8
- 239000008103 glucose Substances 0.000 claims 8
- 239000008280 blood Substances 0.000 claims 6
- 210000004369 blood Anatomy 0.000 claims 6
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 5
- 208000004611 Abdominal Obesity Diseases 0.000 claims 4
- 125000005640 glucopyranosyl group Chemical group 0.000 claims 4
- 230000002641 glycemic effect Effects 0.000 claims 4
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 claims 3
- 206010022489 Insulin Resistance Diseases 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 238000009097 single-agent therapy Methods 0.000 claims 3
- 206010065941 Central obesity Diseases 0.000 claims 2
- 208000002705 Glucose Intolerance Diseases 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 206010033307 Overweight Diseases 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 201000001421 hyperglycemia Diseases 0.000 claims 2
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 2
- 229960003105 metformin Drugs 0.000 claims 2
- 230000000291 postprandial effect Effects 0.000 claims 2
- 201000009104 prediabetes syndrome Diseases 0.000 claims 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 102000017011 Glycated Hemoglobin A Human genes 0.000 claims 1
- 108010014663 Glycated Hemoglobin A Proteins 0.000 claims 1
- 108010023302 HDL Cholesterol Proteins 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 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
- 206010054805 Macroangiopathy Diseases 0.000 claims 1
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 229940123518 Sodium/glucose cotransporter 2 inhibitor Drugs 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 238000009825 accumulation Methods 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- UHOVQNZJYSORNB-UHFFFAOYSA-N benzene Substances C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 230000037396 body weight Effects 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 230000035487 diastolic blood pressure Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 230000003914 insulin secretion Effects 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 230000000979 retarding effect Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 210000002966 serum Anatomy 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 208000023516 stroke disease Diseases 0.000 claims 1
- 230000035488 systolic blood pressure Effects 0.000 claims 1
- 238000011287 therapeutic dose Methods 0.000 claims 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 1
- 230000004584 weight gain Effects 0.000 claims 1
- 235000019786 weight gain Nutrition 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
Classifications
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- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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Claims (19)
1.Farmaceutska kompozicija koja sadrži glukopiranozilom supstituisani derivat benzola 1-hloro-4-((3-D-glukopiranoz-1-il)-2-[4-((S)-tetrahidrofuran-3-iloksi)-benzil]-benzol u kombinaciji sa DPP IV inhibitorom 1-[(4-metil-hinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(R)-amino-piperidin-1-il)-ksantinom ili njegovu farmaceutski prihvatljivu so.
2.Farmaceutska kompozicija prema zahtjevu 1, naznačena time što je kompozicija podesna za kombinovanu ili simultanu ili sukcesivnu primjenu glukopiranozilom supstituisanog derivata benzola i DPP IV inhibitora.
3.Farmaceutska kompozicija prema jednom od prethodnih zahtjeva, naznačena time što su glukopiranozilom supstituisani derivat benzola i DPP IV inhibitor prisutni u samo jednom farmaceutskom obliku.
4.Farmaceutska kompozicija prema jednom od prethodnih zahtjeva, naznačena time što su glukopiranozilom supstituisani derivat benzola i DPP IV inhibitor prisutni u posebnim farmaceutskim oblicima.
5.Farmaceutska kompozicija prema jednom od prethodnih zahtjeva, koja sadrži količinu od 5 do 50 mg glukopiranozilom supstituisanog derivata benzola.
6.Farmaceutska kompozicija prema zahtjevu 5, koja sadrži količinu od 5 mg, 10 mg, 15 mg, 20 mg, 25 mg ili 50 mg glukopiranozilom supstituisanog derivata benzola.
7.Farmaceutska kompozicija prema jednom od prethodnih zahtjeva koja sadrži količinu od 0.5 do 10 mg DPP IV inhibitora.
8.Farmaceutska kompozicija prema zahtjevu 7, koja sadrži količinu od 1 mg, 2.5 mg ili 5 mg DPP IV inhibitora.
9.Farmaceutska kompozicija prema zahtjevu 1, 2, 3 ili 4, koja sadrži količinu od 5 do 50 mg glukopiranozilom supstituisanog derivata benzola i količinu od 0.5 do 10 mg DPP IV inhibitora.
10.Farmaceutska kompozicija prema bilo kom od prethodnih zahtjeva, naznačena time što je farmaceutska kompozicija formulisana za oralnu primjenu u čvrstom obliku.
11.Farmaceutska kompozicija prema jednom od zahtjeva 1 do 10 za primjenu u -sprečavanju, usporavanju napredovanja, odlaganju ili liječenju metaboličkog poremećaja izabranog iz grupe koja se sastoji od tipa 1 dijabetes melitusa, tipa 2 dijabetes melitusa, poremećene tolerancije glukoze, povišenog nivoa glukoze u krvi našte, hiperglikemije, postprandijalne hiperglikemije, prekomjerne težine, gojaznosti i metaboličkog sindroma; ili -poboljšanju glikemijske kontrole i/ili smanjenju povišenog nivoa glukoze u plazmi našte, postprandijalnog nivoa glukoze u plazmi i/ili glikozilovanog hemoglobina HbA1c; ili -sprečavanju, usporavanju, odlaganju ili preokretanju napredovanja od poremećene tolerancije glukoze, povišenog nivoa glukoze u krvi našte, insulinske rezistencije i/ili od metaboličkog sindroma do tipa 2 dijabetesa melitusa; ili -sprečavanju, usporavanju napredovanja, odlaganju ili liječenju stanja ili poremećaja izabranog iz grupe koja se sastoji od komplikacija dijabetes melitusa, kao što su katarakte, i mikro- i makrovaskularnih bolesti, kao što su nefropatija, retinopatija, neuropatija, ishemija tkiva, arterioskleroza, infarkt miokarda, moždani udar i periferna arterijska okluzivna bolest; ili -smanjenju tjelesne težine ili sprečavanju povećanja tjelesne težine ili olakšanju smanjenja tjelesne težine; ili -sprečavanju, usporavanju, odlaganju ili liječenju degeneracije pankreasnih beta ćelija i/ili opadanju funkcionalnosti pankreasnih beta ćelija i/ili poboljšanju i/ili ponovnom uspostavljanju funkcionalnosti pankreasnih beta ćelija i/ili ponovnom uspostavljanju funkcionalnosti pankreasnog lučenja insulina; ili -sprečavanju, usporavanju, odlaganju ili liječenju bolesti ili stanja koja se pripisuju abnormalnoj akumulaciji masti u jetri; ili - održavanju i/ili poboljšanju osjetljivosti na insulin i/ili liječenju ili sprečavanju hiperinsulinemije i/ili insulinske rezistencije; kod pacijenta kome je to potrebno.
12.Farmaceutska kompozicija prema zahtjevu 11 za primjenu u poboljšanju glikemijske kontrole kod pacijenata sa tipom 2 dijabetes melitusa.
13.Farmaceutska kompozicija za primjenu prema zahtjevu 11 ili 12, naznačena time što se glukopiranozilom supstituisani derivat benzola primjenjuje u kombinaciji ili naizmjenično sa DPP IV inhibitorom.
14. Farmaceutska kompozicija za primjenu prema zahtjevu 11, 12 ili 13, pri čemu je pacijent pojedinac kome je dijagnostikovano jedno ili više stanja koja su izabrana iz grupe koja se sastoji od prekomjerne težine, gojaznosti, visceralne gojaznosti i abdominalne gojaznosti.
15. Farmaceutska kompozicija za primjenu prema zahtjevu 11, 12 ili 13, pri čemu je pacijent pojedinac kod koga se ispoljava jedno, dva, tri ili više od slijedećih stanja: (a)nivo glukoze u krvi našte ili koncentracija glukoze u serumu veći od 110 mg/dL, a naročito veći od 125 mg/dL; (b)postprandijalni nivo glukoze u plazmi jednak ili veći od 140 mg/dL; (c)HbA1c vrednost jednaka ili veća od 6.5 %, a naročito jednaka ili veća od 8.0 %.
16. Farmaceutska kompozicija za primjenu prema zahtjevu 11, 12 ili 13, pri čemu je pacijent pojedinac kod koga su prisutni jedno, dva, tri ili više od slijedećih stanja: (a)gojaznost, visceralna gojaznost i/ili abdominalna gojaznost, (b)nivo triglicerida u krvi ≥ 150 mg/dL, (c)nivo HDL-holesterola u krvi < 40 mg/dL kod pacijentkinja, i < 50 mg/dL kod pacijenata, (d)sistolni krvni pritisak ≥ 130 mm Hg i dijastolni krvni pritisak ≥ 85 mm Hg, (e)nivo glukoze u krvi našte ≥ 110 mg/dL.
17. Farmaceutska kompozicija za primjenu prema zahtjevu 11, 12 ili 13, pri čemu je pacijent pojedinac kome je monoterapija sa metforminom kontraindikovana i/ili koji ima netoleranciju na metformin u terapeutskim dozama.
18. Farmaceutska kompozicija za primjenu prema zahtjevu 11, 12 ili 13, pri čemu je pacijent pojedinac sa nedovoljnom glikemijskom kontrolom uprskos monoterapiji sa SGLT2 inhibitorom, a naročito sa glukopiranozilom supstituisanim derivatom benzola prema zahtevu 1.
19. Farmaceutska kompozicija za primjenu prema zahtjevu 11, 12 ili 13, pri čemu je pacijent pojedinac sa nedovoljnom glikemijskom kontrolom uprkos monoterapiji sa DPP IV inhibitorom, a naročito DPP IV inhibitorom prema zahtjevu 1. 4
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| PCT/EP2008/060736 WO2009022007A1 (en) | 2007-08-16 | 2008-08-15 | Pharmaceutical composition comprising a glucopyranosyl-substituted benzene derivative |
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| MEP-2016-255A ME02573B (me) | 2007-08-16 | 2008-08-15 | Farmaceutska kompozicija koja sadrži glukopiranozilom supstituisani derivat benzena |
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