HRP20170022T1 - Farmaceutski sastav koji obuhvaća derivat benzena supstituiran glukopiranozilom - Google Patents
Farmaceutski sastav koji obuhvaća derivat benzena supstituiran glukopiranozilom Download PDFInfo
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- HRP20170022T1 HRP20170022T1 HRP20170022TT HRP20170022T HRP20170022T1 HR P20170022 T1 HRP20170022 T1 HR P20170022T1 HR P20170022T T HRP20170022T T HR P20170022TT HR P20170022 T HRP20170022 T HR P20170022T HR P20170022 T1 HRP20170022 T1 HR P20170022T1
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- pharmaceutical composition
- glucopyranosyl
- dpp
- inhibitor
- composition according
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- 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
- 239000003112 inhibitor Substances 0.000 claims 10
- 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 9
- 150000001555 benzenes Chemical group 0.000 claims 9
- 239000008103 glucose Substances 0.000 claims 9
- 125000005640 glucopyranosyl group Chemical group 0.000 claims 7
- 230000002265 prevention Effects 0.000 claims 7
- 239000008280 blood Substances 0.000 claims 6
- 210000004369 blood Anatomy 0.000 claims 6
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 5
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 5
- 208000008589 Obesity Diseases 0.000 claims 5
- 235000020824 obesity Nutrition 0.000 claims 5
- 230000002641 glycemic effect Effects 0.000 claims 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 4
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 claims 3
- 206010022489 Insulin Resistance Diseases 0.000 claims 3
- 238000009097 single-agent therapy Methods 0.000 claims 3
- 208000004611 Abdominal Obesity Diseases 0.000 claims 2
- 206010065941 Central obesity 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
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000002552 dosage form Substances 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
- YZGOOQZXQOPQNT-DNNBANOASA-N (2r,3r,4s,5s,6r)-2-[4-chloro-3-[[4-[(3s)-oxolan-3-yl]oxyphenyl]methyl]phenyl]-6-(hydroxymethyl)oxane-2,3,4,5-tetrol Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@]1(O)C1=CC=C(Cl)C(CC=2C=CC(O[C@@H]3COCC3)=CC=2)=C1 YZGOOQZXQOPQNT-DNNBANOASA-N 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance 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
- 230000002159 abnormal effect Effects 0.000 claims 1
- 238000009825 accumulation Methods 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 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
- 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
- 230000001747 exhibiting effect Effects 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
- 238000012423 maintenance Methods 0.000 claims 1
- 201000000083 maturity-onset diabetes of the young type 1 Diseases 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
- 201000009104 prediabetes syndrome Diseases 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
- 239000013585 weight reducing agent Substances 0.000 claims 1
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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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- 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
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- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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Claims (19)
1. Farmaceutski sastav, naznačen time, da obuhvaća derivat benzena supstituiran glukopiranozilom: 1-kloro-4-(β-D-glukopiranoz-1-il)-2-[4-((S)-tetrahidrofuran-3-iloksi)-benzil]-benzen, u kombinaciji s DPP IV-inhibitorom: 1-[(4-metil-kinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(R)-amino-piperidin-1-il)-ksantin, ili njegova farmaceutski prihvatljiva sol.
2. Farmaceutski sastav prema zahtjevu 1, naznačen time, da je sastav prikladan za kombiniranu ili istovremenu ili uzastopnu uporabu derivata benzena supstituiranog glukopiranozilom i DPP IV-inhibitora.
3. Farmaceutski sastav prema jednom od prethodnih zahtjeva, naznačen time, da su derivat benzena supstituiran glukopiranozilom i DPP IV-inhibitor prisutni u jednostrukom doznom obliku.
4. Farmaceutski sastav prema jednom od prethodnih zahtjeva, naznačen time, da su derivat benzena supstituiran glukopiranozilom i DPP IV-inhibitor prisutni u odvojenom doznom obliku.
5. Farmaceutski sastav prema jednom od prethodnih zahtjeva, naznačen time, da sadrži količinu od 5 do 50 mg derivata benzena supstituiranog glukopiranozilom.
6. Farmaceutski sastav prema zahtjevu 5, naznačen time, da sadrži količinu od 5 mg, 10 mg, 15 mg, 20 mg, 25 mg ili 50 mg derivata benzena supstituiranog glukopiranozilom.
7. Farmaceutski sastav prema jednom od prethodnih zahtjeva, naznačen time, da sadrži količinu od 0,5 do 10 mg DPP IV-inhibitora.
8. Farmaceutski sastav prema zahtjevu 7, naznačen time, da sadrži količinu od 1 mg, 2,5 mg ili 5 mg DPP IV-inhibitora.
9. Farmaceutski sastav prema zahtjevu 1, 2, 3 ili 4, naznačen time, da sadrži količinu od 5 do 50 mg derivata benzena supstituiranog glukopiranozilom i količinu od 0,5 do 10 mg DPP IV-inhibitora.
10. Farmaceutski sastav prema bilo kojem od prethodnih zahtjeva, naznačen time, da se farmaceutski sastav formulira za oralnu primjenu u čvrstom obliku.
11. Farmaceutski sastav prema bilo kojem od zahtjeva 1 do 10, naznačen time, da se upotrebljava za sljedeće:
- prevencija, usporavanje njegove progresije, odgađanje ili liječenje metaboličkog poremećaja odabranog iz skupine koju čine: dijabetes melitus tipa 1, dijabetes melitus tipa 2, oslabljena tolerancija na glukozu, pogoršana glukoza u krvi natašte, hiperglikemija, reaktivna hiperglikemija, prekomjerna težina, pretilost i metabolički sindrom; ili
- poboljšanje glikemijske kontrole i/ili za smanjenje glukoze u plazmi natašte, od reaktivne glukoze u plazmi i/ili od glikoziliranog hemoglobina HbA1c; ili
- prevencija, usporavanje, odgađanje ili ukidanje progresije smanjene tolerancije na glukozu, pogoršane glukoze u krvi natašte, otpornosti na inzulin i/ili od metaboličkog sindroma do dijabetesa melitus tipa 2; ili
- prevencija, usporavanje njegove progresije, odgađanje ili liječenje stanja ili poremećaja odabranog iz skupine koju čine: komplikacije kod dijabetesa melitus, kao što su katarakti i mikrovaskularne i makrovaskularne bolesti, kao što je nefropatija, retinopatija, neuropatija, ishemija tkiva, arterioskleroza, infarkt miokarda, moždani udar i okluzivna bolest perifernih arterija; ili
- smanjenje tjelesne težine ili prevencija povećanja tjelesne težine ili olakšavanje smanjenja tjelesne težine; ili
- prevencija, usporavanje, odgađanje ili liječenje degeneracije beta stanica pankreasa i/ili odstranjivanja funkcionalnosti beta stanica pankreasa i/ili za poboljšanje i/ili ponovno uspostavljanje funkcionalnosti beta stanica pankreasa i/ili ponovno uspostavljanje funkcionalnosti sekrecije inzulina pankreasa; ili
- prevencija, usporavanje, odgađanje ili liječenje bolesti ili stanja, koja se pripisuju abnormalnoj akumulaciji masti u jetri; ili
- održavanje i/ili poboljšanje osjetljivosti na inzulin i/ili liječenje ili prevencija hiperinzulinemije i/ili otpornosti na inzulin;
za pacijenta kojemu je to potrebno.
12. Farmaceutski sastav prema zahtjevu 11, naznačen time, da se upotrebljava za poboljšanje glikemijske kontrole kod pacijenata s dijabetesom melitus tipa 2.
13. Farmaceutski sastav za uporabu prema zahtjevu 11 ili 12, naznačen time, da se derivat benzena supstituiran glukopiranozilom, primjenjuje u kombinaciji ili alternativno s DPP IV-inhibitorom.
14. Farmaceutski sastav za uporabu prema zahtjevu 11, 12 ili 13, naznačen time, da je pacijent pojedinac kojemu je dijagnosticirano jedno ili više stanja odabranih iz skupine koju čine prekomjerna težina, pretilost, organska pretilost i abdominalna pretilost.
15. Farmaceutski sastav za uporabu prema zahtjevu 11, 12 ili 13, naznačen time, da je pacijent pojedinac kod kojega se pokazuje jedno, dva ili više sljedećih stanja:
(a) koncentracija glukoze u krvi natašte ili glukoze u serumu, koja je veća od 110 mg/dL, posebno je veća od 125 mg/dL;
(b) reaktivna glukoza u plazmi je jednaka ili veća od 140 mg/dL;
(c) vrijednost HbA1c je jednaka ili veća od 6,5%, posebno jednaka ili veća od 8,0%.
16. Farmaceutski sastav za uporabu prema zahtjevu 11, 12 ili 13, naznačen time, da je pacijent pojedinac kod kojega su prisutna jedno, dva ili više sljedećih stanja:
(a) pretilost, organska pretilost i/ili abdominalna pretilost;
(b) razina triglicerida u krvi ≥ 150 mg/dL;
(c) razina HDL-kolesterola u krvi < 40 mg/dL kod ženskih pacijenata i < 50 mg/dL kod muških pacijenata;
(d) sistolički krvni tlak ≥ 130 mm Hg i dijastolički krvni tlak ≥ 85 mm Hg;
(e) razina glukoze u krvi natašte ≥ 110 mg/dL.
17. Farmaceutski sastav za uporabu prema zahtjevu 11, 12 ili 13, naznačen time, da je pacijent pojedinac kod kojega je kontraindicirana monoterapija s metforminom i/ili koji nema toleranciju protiv metformina u terapeutskim dozama.
18. Farmaceutski sastav za uporabu prema zahtjevu 11, 12 ili 13, naznačen time, da je pacijent pojedinac s nedovoljnom glikemijskom kontrolom usprkos monoterapiji sa SGLT2-inhibitorom, posebno s derivatom benzena supstituiranim glukopiranozilom prema zahtjevu 1.
19. Farmaceutski sastav za uporabu prema zahtjevu 11, 12 ili 13, naznačen time, da je pacijent pojedinac s nedovoljnom glikemijskom kontrolom usprkos monoterapiji s DPP IV-inhibitorom, posebno s DPP IV-inhibitorom prema zahtjevu 1.
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EP07114459 | 2007-08-16 | ||
EP08787264.4A EP2187879B1 (en) | 2007-08-16 | 2008-08-15 | Pharmaceutical composition comprising a glucopyranosyl-substituted benzene derivative |
PCT/EP2008/060736 WO2009022007A1 (en) | 2007-08-16 | 2008-08-15 | Pharmaceutical composition comprising a glucopyranosyl-substituted benzene derivative |
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HRP20170022T1 true HRP20170022T1 (hr) | 2017-03-10 |
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HRP20170022TT HRP20170022T1 (hr) | 2007-08-16 | 2017-01-09 | Farmaceutski sastav koji obuhvaća derivat benzena supstituiran glukopiranozilom |
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US (1) | US8551957B2 (hr) |
EP (4) | EP3939577A1 (hr) |
JP (1) | JP5595914B2 (hr) |
KR (1) | KR101491554B1 (hr) |
CN (3) | CN101784270A (hr) |
AR (2) | AR067970A1 (hr) |
AU (1) | AU2008288407B2 (hr) |
BR (1) | BRPI0815331B8 (hr) |
CA (1) | CA2696558C (hr) |
CL (1) | CL2008002427A1 (hr) |
CO (1) | CO6251239A2 (hr) |
CY (2) | CY1118308T1 (hr) |
DK (1) | DK2187879T3 (hr) |
EA (1) | EA018608B1 (hr) |
EC (1) | ECSP109977A (hr) |
ES (1) | ES2602748T3 (hr) |
HK (2) | HK1203351A1 (hr) |
HR (1) | HRP20170022T1 (hr) |
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LT (2) | LT2187879T (hr) |
MA (1) | MA31612B1 (hr) |
ME (1) | ME02573B (hr) |
MX (1) | MX2010001696A (hr) |
MY (1) | MY152037A (hr) |
NL (1) | NL300872I2 (hr) |
NO (1) | NO2017020I2 (hr) |
NZ (1) | NZ583242A (hr) |
PE (1) | PE20090938A1 (hr) |
PL (1) | PL2187879T3 (hr) |
PT (1) | PT2187879T (hr) |
RS (1) | RS55205B1 (hr) |
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TN (1) | TN2010000073A1 (hr) |
TW (2) | TWI472325B (hr) |
UA (1) | UA100384C2 (hr) |
UY (1) | UY31296A1 (hr) |
WO (1) | WO2009022007A1 (hr) |
ZA (1) | ZA200909105B (hr) |
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