HRP20130868T1 - Hidrokloridi i hidrati od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-amino-piperidin-1-il)-ksantina, njihova proizvodnja i njihova uporaba kao lijekova - Google Patents
Hidrokloridi i hidrati od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-amino-piperidin-1-il)-ksantina, njihova proizvodnja i njihova uporaba kao lijekova Download PDFInfo
- Publication number
- HRP20130868T1 HRP20130868T1 HRP20130868TT HRP20130868T HRP20130868T1 HR P20130868 T1 HRP20130868 T1 HR P20130868T1 HR P20130868T T HRP20130868T T HR P20130868TT HR P20130868 T HRP20130868 T HR P20130868T HR P20130868 T1 HRP20130868 T1 HR P20130868T1
- Authority
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- Croatia
- Prior art keywords
- methyl
- butyn
- xanthine
- pyridin
- cyano
- Prior art date
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- 239000003814 drug Substances 0.000 title claims 3
- ISVBJQYIQQKSGK-UHFFFAOYSA-N 2-[[8-(3-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-2,6-dioxopurin-1-yl]methyl]pyridine-3-carbonitrile Chemical compound O=C1C=2N(CC#CC)C(N3CC(N)CCC3)=NC=2N(C)C(=O)N1CC1=NC=CC=C1C#N ISVBJQYIQQKSGK-UHFFFAOYSA-N 0.000 title claims 2
- 150000004677 hydrates Chemical class 0.000 title 1
- 150000003840 hydrochlorides Chemical class 0.000 title 1
- -1 3-cyano-pyridin-2-yl Chemical group 0.000 claims 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 11
- 229940075420 xanthine Drugs 0.000 claims 11
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- PEUGKEHLRUVPAN-RXMQYKEDSA-N (3r)-piperidin-3-amine Chemical compound N[C@@H]1CCCNC1 PEUGKEHLRUVPAN-RXMQYKEDSA-N 0.000 claims 4
- 239000000969 carrier Substances 0.000 claims 4
- 239000003085 diluting agent Substances 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000008589 Obesity Diseases 0.000 claims 2
- 230000008018 melting Effects 0.000 claims 2
- 238000002844 melting Methods 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000000843 powder Substances 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- 102000055006 Calcitonin Human genes 0.000 claims 1
- 108060001064 Calcitonin Proteins 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- BBBFJLBPOGFECG-VJVYQDLKSA-N calcitonin Chemical compound N([C@H](C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N1[C@@H](CCC1)C(N)=O)C(C)C)C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 BBBFJLBPOGFECG-VJVYQDLKSA-N 0.000 claims 1
- 229960004015 calcitonin Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
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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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
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Claims (15)
1. Spoj, naznačen time, da je to hidrokloridna sol od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-amino-piperidin-1-il)-ksantina.
2. Spoj, naznačen time, da je to monohidrokloridna sol ili dihidrokloridna sol od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(R)-3-amino-piperidin-1-il)]-ksantina.
3. Monohidrokloridna sol ili dihidrokloridna sol od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(R)-3-amino-piperidin-1-il)]-ksantina, naznačena time, da je u kristalnom ne-hidratnom obliku.
4. Spoj, naznačen time, da je to 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(R)-3-amino-piperidin-1-il)]-ksantin monohidroklorid.
5. Spoj, naznačen time, da je to 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(R)-3-amino-piperidin-1-il)]-ksantin dihidroklorid.
6. Monohidrokloridna sol od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(R)-3-amino-piperidin-1-il)]-ksantina, naznačena time, da ima talište na 265°C ± 5°C.
7. Dihidrokloridna sol od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(R)-3-amino-piperidin-1-il)]-ksantina, naznačena time, da ima talište na 205°C ± 5°C.
8. Monohidrokloridna sol od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(R)-3-amino-piperidin-1-il)]-ksantina, naznačena time, da dijagram praha X-zraka od toga monohidroklorida uključuje karakteristične d-vrijednosti na 10,38 Å, 8,99 Å, 6,80 Å, 5,19 Å, 4,44 Å, 4,31 Å, 3,98 Å, 3,93 Å, 3,57 Å, 3,50 Å.
9. Dihidrokloridna sol od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(R)-3-amino-piperidin-1-il)]-ksantina, naznačena time, da dijagram praha X-zraka od toga dihidroklorida uključuje karakteristične d-vrijednosti na 11,24 Å, 8,81 Å, 7,67 Å, 7,25 Å, 5,61 Å, 4,79 Å, 4,10 Å, 3,32 Å, 3,03 Å, 2,96 Å.
10. Uporaba spoja prema jednom od zahtjeva 1 do 9, naznačena time, da je za proizvodnju lijeka koji je prikladan za liječenje mellitus dijabetesa tipa I i tipa II, artritisa, pretilosti, allograft transplantacije i osteoporoze uzrokovane kalcitoninom.
11. Uporaba spoja prema jednom od zahtjeva 1 do 9, naznačena time, da je za proizvodnju lijeka koji je prikladan za liječenje mellitus dijabetesa tipa II ili pretilosti.
12. Farmaceutski sastav, naznačen time, da obuhvaća sol prema jednom od zahtjeva 1 do 9 opcijski zajedno s jednim ili više inertnih nosača i/ili razrjeđivača.
13. Farmaceutski sastav, naznačen time, da sadrži monohidrokloridnu sol od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(R)-3-amino-piperidin-1-il)]-ksantina, opcijski zajedno s jednim ili više inertnih nosača i/ili razrjeđivača.
14. Farmaceutski sastav, naznačen time, da sadrži dihidrokloridnu sol od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(R)-3-amino-piperidin-1-il)]-ksantina, opcijski zajedno s jednim ili više inertnih nosača i/ili razrjeđivača.
15. Farmaceutski sastav, naznačen time, da sadrži monohidrokloridnu sol od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-[(R)-3-amino-piperidin-1-il)]-ksantina prema zahtjevu 4, 6 ili 8, opcijski zajedno s jednim ili više inertnih nosača i/ili razrjeđivača.
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DE102005035891A DE102005035891A1 (de) | 2005-07-30 | 2005-07-30 | 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
PCT/EP2006/064657 WO2007014886A1 (de) | 2005-07-30 | 2006-07-26 | Hydrochloride und hydrate von 1-[(3-cyano-pyridin-2-yl) methyl]-3-methyl-7-(2-butin-1-yl)-8-(3-amino-piperidin-1-yl)-xanthin, deren herstellung und deren verwendung als arzneimittel |
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HRP20130868TT HRP20130868T1 (hr) | 2005-07-30 | 2013-09-16 | Hidrokloridi i hidrati od 1-[(3-cijano-piridin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-amino-piperidin-1-il)-ksantina, njihova proizvodnja i njihova uporaba kao lijekova |
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