HRP20211938T1 - Sol dimetilaminoetanola od modulatora receptora glp-1 - Google Patents
Sol dimetilaminoetanola od modulatora receptora glp-1 Download PDFInfo
- Publication number
- HRP20211938T1 HRP20211938T1 HRP20211938TT HRP20211938T HRP20211938T1 HR P20211938 T1 HRP20211938 T1 HR P20211938T1 HR P20211938T T HRP20211938T T HR P20211938TT HR P20211938 T HRP20211938 T HR P20211938T HR P20211938 T1 HRP20211938 T1 HR P20211938T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound according
- compound
- xrpd
- spacing
- diffraction pattern
- Prior art date
Links
- MDLKWDQMIZRIBY-UHFFFAOYSA-N 1-(dimethylamino)ethanol Chemical class CC(O)N(C)C MDLKWDQMIZRIBY-UHFFFAOYSA-N 0.000 title 1
- 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 title 1
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 title 1
- 229940075993 receptor modulator Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 19
- 238000000634 powder X-ray diffraction Methods 0.000 claims 12
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 230000002159 abnormal effect Effects 0.000 claims 3
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- OBMZMSLWNNWEJA-XNCRXQDQSA-N C1=CC=2C(C[C@@H]3NC(=O)[C@@H](NC(=O)[C@H](NC(=O)N(CC#CCN(CCCC[C@H](NC(=O)[C@@H](CC4=CC=CC=C4)NC3=O)C(=O)N)CC=C)NC(=O)[C@@H](N)C)CC3=CNC4=C3C=CC=C4)C)=CNC=2C=C1 Chemical compound C1=CC=2C(C[C@@H]3NC(=O)[C@@H](NC(=O)[C@H](NC(=O)N(CC#CCN(CCCC[C@H](NC(=O)[C@@H](CC4=CC=CC=C4)NC3=O)C(=O)N)CC=C)NC(=O)[C@@H](N)C)CC3=CNC4=C3C=CC=C4)C)=CNC=2C=C1 OBMZMSLWNNWEJA-XNCRXQDQSA-N 0.000 claims 1
- 102000006419 Glucagon-Like Peptide Receptors Human genes 0.000 claims 1
- 108010083749 Glucagon-Like Peptide Receptors Proteins 0.000 claims 1
- UEEJHVSXFDXPFK-UHFFFAOYSA-N N-dimethylaminoethanol Chemical compound CN(C)CCO UEEJHVSXFDXPFK-UHFFFAOYSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 101710176384 Peptide 1 Proteins 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 230000008484 agonism Effects 0.000 claims 1
- 230000001476 alcoholic effect Effects 0.000 claims 1
- 235000019789 appetite Nutrition 0.000 claims 1
- 230000036528 appetite Effects 0.000 claims 1
- 239000012752 auxiliary agent Substances 0.000 claims 1
- 230000009286 beneficial effect Effects 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000004104 gestational diabetes Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000036186 satiety Effects 0.000 claims 1
- 235000019627 satiety Nutrition 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Endocrinology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Peptides Or Proteins (AREA)
Claims (15)
1. Spoj, naznačen time, da posjeduje sljedeću strukturu:
[image]
2. Spoj prema patentnom zahtjevu 1, naznačen time, da posjeduje sljedeću strukturu:
[image]
3. Spoj prema patentnom zahtjevu 1, naznačen time, da posjeduje sljedeću strukturu:
[image]
4. Spoj prema patentnom zahtjevu 1, naznačen time, da posjeduje sljedeću strukturu:
[image]
5. Racemična smjesa, naznačena time, da je od spojeva prema patentnim zahtjevima 3 i 4.
6. Spoj prema patentnom zahtjevu 1, naznačen time, da se nalazi u obliku kristala 2-hidroksi-N,N-dimetiletanaminij 1-(2-(5-(terc-butil)-tiofen-2-karboksamido)-3-(4-(5-(4'-etil-[1,1-bi(cikloheksan)]-3-en-4-il)pirimidin-2-il)fenil)propanoil)azetidin-3-karboksilatne soli.
7. Spoj prema patentnom zahtjevu 6, naznačen time, da ima (i) uzorak XRPD rendgenske difrakcije na prahu kao što je prikazan na Slici 1A, (ii) uzorak XRPD rendgenske difrakcije na prahu kao što je prikazan na Slici 2A, ili (iii) uzorak XRPD rendgenske difrakcije na prahu kao što je prikazan na Slici 3A.
8. Spoj prema patentnom zahtjevu 6, naznačen time, da spomenuti spoj izlaže uzorak XRPD rendgenske difrakcije na prahu koji ima karakteristične maksimume izražene u udaljenostima (d-razmak) u stupnjevima 2θ (+/- 0,2°θ) kao što je popisano u Tablici 1A u nastavku:
Poz. [°2Teta] d-razmak [Å]
6,51 13,57
16,04 5,53
16,92 5,24
17,22 5,15
19,05 4,66
20,12 4,41
20,84 4,26
22,60 3,93
9. Spoj prema patentnom zahtjevu 6, naznačen time, da spomenuti spoj izlaže uzorak XRPD rendgenske difrakcije na prahu koji ima karakteristične maksimume izražene u udaljenostima (d-razmak) u stupnjevima 2θ (+/- 0,2°θ) kao što je popisano u Tablici 1B u nastavku:
Poz. [°2Teta] d-razmak [Å]
6,53 13,54
13,70 6,47
16,05 5,52
16,91 5,24
17,22 5,15
19,03 4,66
20,11 4,42
20,80 4,27
22,55 3,94
23,06 3,86
25,41 3,51
10. Spoj prema patentnom zahtjevu 6, naznačen time, da spomenuti spoj izlaže uzorak XRPD rendgenske difrakcije na prahu koji ima karakteristične maksimume izražene u udaljenostima (d-razmak) u stupnjevima 2θ (+/- 0,2°θ) kao što je popisano u Tablici 1C u nastavku:
Poz. [°2Teta] d-razmak [Å]
3,58 24,72
6,51 13,57
7,18 12,31
16,04 5,53
16,92 5,24
17,22 5,15
19,05 4,66
20,12 4,41
20,84 4,26
22,60 3,93
11. Spoj prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time, da posjeduje čistoću više od 95% po masi, poželjno više od 98% po masi.
12. Farmaceutski pripravak, naznačen time, da sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 11, s najmanje jednim farmaceutski prihvatljivim nosačem, razrjeđivačem ili pomoćnim sredstvom.
13. Spoj prema bilo kojem od patentnih zahtjeva 1 do 11, ili farmaceutski pripravak prema patentnom zahtjevu 12, naznačen time, da je za uporabu u postupku liječenja bolesti ili nenormalnog stanja kod pacijenta kod kojega je medicinski indicirana aktivacija, potencijacija, modulacija ili agonizam peptidnog 1 receptora nalik na glukagon, gdje postupak obuhvaća davanje pacijentu učinkovite količine spoja ili farmaceutskog pripravka uz učestalost i u dovoljnom vremenskom trajanju, kako bi se dobio povoljan učinak kod pacijenta.
14. Spoj ili farmaceutski pripravak za uporabu prema patentnom zahtjevu 13, naznačen time, da se kod bolesti ili nenormalnog stanja radi o dijabetesu tipa I, dijabetesu tipa II, gestacijskom dijabetesu, pretilosti, prekomjernom apetitu, nedovoljnoj sitosti, metaboličkom poremećaju, nealkoholnoj bolesti masne jetre ili nealkoholnom steatohepatitisu.
15. Spoj ili farmaceutski pripravak za uporabu prema patentnom zahtjevu 13, naznačen time, da bolest ili nenormalno stanje je (i) dijabetes tipa II, (ii) nealkoholna bolest masne jetre, ili (iii) nealkoholni steatohepatitis.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662402565P | 2016-09-30 | 2016-09-30 | |
| EP17781347.4A EP3519407B1 (en) | 2016-09-30 | 2017-09-29 | Dimethylaminoethanol salt of a glp-1 receptor modulator |
| PCT/US2017/054298 WO2018064476A1 (en) | 2016-09-30 | 2017-09-29 | Dimethylaminoethanol salt of a glp-1 receptor modulator |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20211938T1 true HRP20211938T1 (hr) | 2022-03-18 |
Family
ID=60043396
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20211938TT HRP20211938T1 (hr) | 2016-09-30 | 2017-09-29 | Sol dimetilaminoetanola od modulatora receptora glp-1 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US11066395B2 (hr) |
| EP (1) | EP3519407B1 (hr) |
| CY (1) | CY1124940T1 (hr) |
| ES (1) | ES2901599T3 (hr) |
| HR (1) | HRP20211938T1 (hr) |
| HU (1) | HUE056805T2 (hr) |
| LT (1) | LT3519407T (hr) |
| PL (1) | PL3519407T3 (hr) |
| PT (1) | PT3519407T (hr) |
| RS (1) | RS62814B1 (hr) |
| SI (1) | SI3519407T1 (hr) |
| WO (1) | WO2018064476A1 (hr) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12098127B2 (en) | 2018-11-28 | 2024-09-24 | Luoxin Pharmaceutical (Shanghai) Co., Ltd. | Salt form of estrogen receptor downregulator, crystalline form thereof, and preparation method therefor |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2819534T3 (es) * | 2014-07-25 | 2021-04-16 | Receptos Llc | Derivados de pirimidina como moduladores del receptor GLP-1 |
-
2017
- 2017-09-29 US US16/337,298 patent/US11066395B2/en active Active
- 2017-09-29 ES ES17781347T patent/ES2901599T3/es active Active
- 2017-09-29 PL PL17781347T patent/PL3519407T3/pl unknown
- 2017-09-29 WO PCT/US2017/054298 patent/WO2018064476A1/en unknown
- 2017-09-29 SI SI201731018T patent/SI3519407T1/sl unknown
- 2017-09-29 HR HRP20211938TT patent/HRP20211938T1/hr unknown
- 2017-09-29 LT LTEPPCT/US2017/054298T patent/LT3519407T/lt unknown
- 2017-09-29 EP EP17781347.4A patent/EP3519407B1/en active Active
- 2017-09-29 RS RS20211553A patent/RS62814B1/sr unknown
- 2017-09-29 PT PT177813474T patent/PT3519407T/pt unknown
- 2017-09-29 HU HUE17781347A patent/HUE056805T2/hu unknown
-
2021
- 2021-12-10 CY CY20211101089T patent/CY1124940T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PL3519407T3 (pl) | 2022-02-14 |
| RS62814B1 (sr) | 2022-02-28 |
| PT3519407T (pt) | 2021-12-10 |
| US20200131164A1 (en) | 2020-04-30 |
| ES2901599T3 (es) | 2022-03-23 |
| WO2018064476A1 (en) | 2018-04-05 |
| LT3519407T (lt) | 2022-01-10 |
| CY1124940T1 (el) | 2023-01-05 |
| HUE056805T2 (hu) | 2022-03-28 |
| SI3519407T1 (sl) | 2022-01-31 |
| EP3519407B1 (en) | 2021-09-22 |
| US11066395B2 (en) | 2021-07-20 |
| EP3519407A1 (en) | 2019-08-07 |
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