HRP20230645T1 - Farmaceutski spoj, njegove soli, njegove formulacije i postupci izrade i upotrebe istih - Google Patents

Farmaceutski spoj, njegove soli, njegove formulacije i postupci izrade i upotrebe istih Download PDF

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HRP20230645T1
HRP20230645T1 HRP20230645TT HRP20230645T HRP20230645T1 HR P20230645 T1 HRP20230645 T1 HR P20230645T1 HR P20230645T T HRP20230645T T HR P20230645TT HR P20230645 T HRP20230645 T HR P20230645T HR P20230645 T1 HRP20230645 T1 HR P20230645T1
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compound
mono
methyl
tosylate
mixture
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Karthik Nagapudi
Yuan Liu
Shuai WANG
Wei Zhang
Fritz Blatter
Srikonda Sastry
Manshiu Leung
Ramachandran Radhakrishnan
Rajendra S. Tandale
Ludwig Pilsl
Roland Muller
Markus Frieser
Christine CZAUDERNA
Lawrence Emerson Fisher
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Genentech, Inc.
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
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    • A61K9/1605—Excipients; Inactive ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
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    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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Claims (18)

1. Spoj koji je sol 1-metil-7-(1-metil-1H-pirazol-4-il)-5-(4-(trifluormetoksi)fenil)-1,5-dihidro-4H-imidazo[4,5-c]piridin-4-ona (Spoj I): [image] pri čemu je sol odabrana iz skupine koju čine bezilatne, hemi-edisilatne, hemi-napadisilatne, mono-hidrobromidne, mono-nitratne, mono-sulfatne i mono-tozilatne soli spoja I, poželjno mono-tozilatna sol Spoja I.
2. Spoj prema zahtjevu 1, pri čemu je sol mono-tozilat i naznačen time što ima uzorak rendgenske difrakcije (XRPD) kada se ozrači s Cu-Kα izvorom svjetlosti koji je uglavnom sličan onom prikazanom na SLICI 8.
3. Spoj prema zahtjevu 1 ili 2, pri čemu je spoj mono-tozilatna sol naznačen time što ima uzorak rendgenske difrakcije (XRPD) kada se ozrači s Cu-Kα izvorom svjetlosti koji ima tri ili više vrhova odabranih od onih pod vrijednostima kuta difrakcije 2θ od (i) 10,92°± 0,2°, 13,28°± 0,2°, 15,36°± 0,2°, 16,94°± 0,2°, 17,74°± 0,2°, 18,20°± 0,2°, 20,51°± 0,2°, 23,21°± 0,2°, 23,86°± 0,2°, 24,73°± 0,2°, 25,69°± 0,2°, 26,68°± 0,2°, 27,63°± 0,2°, 29,12°± 0,2°, i 30,532°± 0,2°; ili (ii) 10,92°± 0,2°, 15,36°± 0,2°, 16,94°± 0,2°, 17,74°± 0,2°, 23,21°± 0,2°, 23,86°± 0,2°, 24,73°± 0,2°, 25,69°± 0,2°, 27,63°± 0,2°, i 29,12°± 0,2°; ili (iii) 15,36°± 0,2°, 17,74°± 0,2°, 23,21°± 0,2°, 23,86°± 0,2°, i 24,73°± 0,2°.
4. Spoj prema bilo kojem od zahtjeva 1 do 3, pri čemu je spoj mono-tozilatna sol i nadalje je naznačen time što ima početak taljenja u rasponu od oko 204 °C do oko 207 °C.
5. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time što je spoj amorfan ili kristaliničan.
6. Postupak za pripremanje mono-tozilata 1-metil-7-(1-metil-1H-pirazol-4-il)-5-(4-(trifluormetoksi)fenil)-1,5-dihidro-4H-imidazo[4,5-c]piridin-4-ona (mono-tozilat Spoja I) naznačen time što sadrži korak: spajanje 7-bromo-1-metil-5-(4-(trifluormetoksi)fenil)-1,5-dihidro-4H-imidazo[4,5-c]piridin-4-ona s 1-metil-4-(4,4,5,5-tetrametil-1,3,2-dioksaborolan-2-il)-1H-pirazolom da se dobije Spoj I; dovođenje u kontakt Spoja I s p-toluensulfonskom kiselinom da se dobije mono-tozilat Spoja I.
7. Postupak prema zahtjevu 6, naznačen time što sadrži korak bromiranja 1-metil-5-(4-(trifluormetoksi)fenil)-1,5-dihidro-4H-imidazo[4,5-c]piridin-4-ona da se dobije 7-bromo-1-metil-5-(4-(trifluormetoksi)fenil)-1,5-dihidro-4H-imidazo[4, 5-c]piridin-4-on.
8. Postupak prema zahtjevu 7, naznačen time što sadrži korak spajanja 1-metil-1,5-dihidro-4H-imidazo[4,5-c]piridin-4-ona s 1-bromo-4-(trifluormetoksi)benzenom da se dobije 1-metil-5-(4-(trifluormetoksi)fenil)-1,5-dihidro-4H-imidazo[4,5-c]piridin-4-on.
9. Postupak prema zahtjevu 8, naznačen time što sadrži korak kondenzacije 2-klor-N4-metilpiridin-3,4-diamina s mravljom kiselinom da se dobije 1-metil-1,5-dihidro-4H-imidazo[4,5-c]piridin-4-on.
10. Granulat koji sadrži farmaceutski pripravak koji sadrži mono-tozilatnu sol Spoja I prema bilo kojem od zahtjeva 1 do 5 ili njegov pripravak, te navedeni farmaceutski pripravak nadalje sadrži farmaceutski prihvatljivu pomoćnu tvar pri čemu farmaceutski prihvatljiva pomoćna tvar sadrži vezivo, navedena pomoćna tvar izborno sadrži polimerni inhibitor taloženja i navedeni granulat izborno sadrži punilo, sredstvo za raspadanje, sredstvo za povećanje skliskosti i polimerni inhibitor taloženja, pri čemu: (i) vezivo sadrži mikrokristalnu celulozu, karboksimetil celulozu ili kroskarmelozu natrij ili bilo koju njihovu kombinaciju; (ii) punilo sadrži laktozu, manitol ili njihovu kombinaciju; (iii) sredstvo za raspadanje sadrži kroskarmelozu, polivinilpovidon ili njihovu kombinaciju; (iv) sredstvo za povećanje skliskosti je odabrano iz skupine koju čine stearinska kiselina, magnezijev stearat, kalcijev stearat, hidrogenirano biljno ulje, mineralno ulje, polietilen glikol, natrijev lauril sulfat, gliceril palmitostearat, gliceril behenat, natrijev benzoat, natrijev stearil fumarat, talk, i pirogeni silicijev dioksid, poželjno magnezijev stearat; i (v) polimerni inhibitor taloženja inhibitor sadrži jedan ili više celuloznih materijala, poželjno hidroksipropil metil celulozu.
11. Farmaceutski pripravak koji sadrži granulat prema zahtjevu 10, koji nadalje sadrži ekstragranularnu pomoćnu tvar koja sadrži ekstragranularno sredstvo za raspadanje, ekstragranularno sredstvo za povećanje skliskosti, ekstragranularno vezivo ili bilo koju njihovu kombinaciju, i pri čemu (i) ekstragranularno sredstvo za raspadanje sadrži šećer, umreženi polimer, modificirani škrob ili bilo koju njihovu kombinaciju; ili (ii) ekstragranularno vezivo sadrži šećer, škrob, šećerni alkohol, protein, polimer ili bilo koju njihovu kombinaciju; i pri čemu pripravak izborno nadalje sadrži polimerni inhibitor taloženja koji sadrži jedan ili više celuloznih materijala, poželjno hidroksipropil metilcelulozu.
12. Farmaceutski pripravak koji sadrži oko 30 tež.% do oko 40 tež.% mono-tozilata Spoja I, oko 40 tež.% do oko 45 tež.% veziva, oko 10 tež.% do oko 20 tež.% punila i oko 0,5 tež.% do oko 5 tež.% sredstva za raspadanje.
13. Farmaceutski pripravak koji sadrži čestice mono-tozilatne soli Spoja I, pri čemu čestice imaju distribuciju veličine naznačene time što ima D50 u rasponu od 10 µm do 60 µm, izborno pri čemu je D50 u rasponu od 25 µm do 30 µm.
14. Farmaceutski pripravak koji sadrži čestice mono-tozilatne soli Spoja I, pri čemu čestice imaju distribuciju veličine naznačen time što ima volumenski srednji promjer D[4,3] u rasponu od 25 µm do 45 µm, izborno pri čemu je D[4,3] u rasponu od 30 µm do 40 µm.
15. Farmaceutski pripravak prema bilo kojem od zahtjeva 13 i 14, pri čemu su čestice dodatno naznačene time što imaju D10 u rasponu od 1 µm do 20 µm.
16. Farmaceutski pripravak prema bilo kojem od zahtjeva 13 i 14 , pri čemu su čestice dodatno naznačene time što imaju D90 u rasponu od 50 µm do 100 µm.
17. Farmaceutski pripravak koji sadrži: [image]
18. Postupak za proizvodnju farmaceutskog pripravka koji sadrži sol Spoja I prema zahtjevu 1, naznačen time što postupak obuhvaća korake: (a) prosijavanje soli Spoja I prema zahtjevu 1, veziva, punila i sredstva za raspadanje; (b) miješanje prosijanih komponenata da se dobije prva smjesa; (c) daljnje miješanje navedene prve smjese sa sredstvom za povećanje skliskosti da se dobije druga smjesa; (d) komprimiranje druge smjese; (e) mljevenje komprimirane druge smjese; (e) miješanje mljevene druge smjese s ekstragranularnim sredstvom za raspadanje i ekstragranularnim vezivom da se dobije treća smjesa; (f) miješanje navedene treće smjese s ekstragranularnim sredstvom za povećanje skliskosti da se dobije četvrta smjesa; i (g) komprimiranje navedene četvrte smjese da nastane tableta.
HRP20230645TT 2018-02-02 2019-02-01 Farmaceutski spoj, njegove soli, njegove formulacije i postupci izrade i upotrebe istih HRP20230645T1 (hr)

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