HRP20161291T1 - Soli fenotiazin-diamina i njihova uporaba - Google Patents

Soli fenotiazin-diamina i njihova uporaba Download PDF

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HRP20161291T1
HRP20161291T1 HRP20161291TT HRP20161291T HRP20161291T1 HR P20161291 T1 HRP20161291 T1 HR P20161291T1 HR P20161291T T HRP20161291T T HR P20161291TT HR P20161291 T HRP20161291 T HR P20161291T HR P20161291 T1 HRP20161291 T1 HR P20161291T1
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Croatia
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compound
use according
prophylaxis
treatment
disease
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HRP20161291TT
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Colin Marshall
Scott Clunas
John Mervyn David Storey
James Peter Sinclair
Thomas Craven Baddeley
Ahtsham ISHAQ
Michael Simpson
Craig Williamson
Barry Alan Wood
Claude Michel Wischik
Charles Robert Harrington
Janet Rickard
David Horsley
Yin Sze Loh
Karrar Ahmad Khan
Christoper Paul Larch
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Wista Laboratories Ltd.
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Publication of HRP20161291T1 publication Critical patent/HRP20161291T1/hr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/12—Antivirals
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
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    • A61P31/18—Antivirals for RNA viruses for HIV
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    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
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    • A61P33/06—Antimalarials
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/18—[b, e]-condensed with two six-membered rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/18—[b, e]-condensed with two six-membered rings
    • C07D279/20—[b, e]-condensed with two six-membered rings with hydrogen atoms directly attached to the ring nitrogen atom
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2893—Tablet coating processes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2/00—Methods or apparatus for disinfecting or sterilising materials or objects other than foodstuffs or contact lenses; Accessories therefor
    • A61L2/0005—Methods or apparatus for disinfecting or sterilising materials or objects other than foodstuffs or contact lenses; Accessories therefor for pharmaceuticals, biologicals or living parts
    • A61L2/0011—Methods or apparatus for disinfecting or sterilising materials or objects other than foodstuffs or contact lenses; Accessories therefor for pharmaceuticals, biologicals or living parts using physical methods
    • A61L2/0029—Radiation
    • A61L2/0052—Visible light
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/32—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/05—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/33—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems
    • C07C309/34—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems formed by two rings
    • C07C309/35—Naphthalene sulfonic acids
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Claims (26)

1. Spoj, naznačen time, da je to spoj sljedeće formule: [image] [image] ili njegova farmaceutski prihvatljiva sol, njegov solvat ili hidrat, te time, da se upotrebljava u postupku liječenja ili profilakse ljudskog ili životinjskog tijela putem terapije.
2. Spoj za uporabu prema zahtjevu 1, naznačen time, da je u kristalnom obliku.
3. Spoj za uporabu prema zahtjevu 1 ili zahtjevu 2, naznačen time, da je u temeljno pročišćenom obliku.
4. Spoj za uporabu prema zahtjevu 1 ili zahtjevu 2, naznačen time, da je prisutan u sastavu koji obuhvaća ovaj spoj i farmaceutski prihvatljiv nosač ili razrjeđivač.
5. Spoj za uporabu prema zahtjevu 4, naznačen time, da spomenuti sastav je farmaceutski sastav koji ju u čvrstom doznom obliku koji obuhvaća ovaj spoj i najmanje jedan razrjeđivač prikladan za suho stlačivanje.
6. Spoj za uporabu prema zahtjevu 5, naznačen time, da se čvrsti dozni oblik proizvodi pomoću izravnog stlačivanja ili pomoću suhe granulacije.
7. Spoj za uporabu prema zahtjevu 5 ili zahtjevu 6, naznačen time, da je spomenuti najmanje jedan razrjeđivač odabran od sljedećih: mikrokristalna celuloza, laktoza, manitol, kalcijeve soli kao što su dibazični kalcijev fosfat, kalcijev sulfat i kalcijev karbonat, te šećeri kao što su laktoza, sukroza, dekstroza i maltodekstrin.
8. Spoj za uporabu prema bilo kojem od zahtjeva 5 do 7, naznačen time, da spomenuti sastav nadalje obuhvaća najmanje jedan dezintegrator.
9. Spoj za uporabu prema zahtjevu 8, naznačen time, da je dezintegrator odabran od sljedećih: križno povezani polivinil pirolidon, natrijev škrobni glikolat, križno povezana natrijeva karboksimetilceluloza ili predželatinizirani škrob.
10. Spoj za uporabu prema bilo kojem od zahtjeva 5 do 9, naznačen time, da je čvrsti dozirni oblik obložen filmom.
11. Spoj za uporabu prema bilo kojem od zahtjeva 5 do 10, naznačen time, da spomenuti sastav nadalje obuhvaća kiselinu koja ima pK1 veći od 1,5.
12. Spoj za uporabu prema zahtjevu 11, naznačen time, da je kiselina odabrana od sljedećih: maleična kiselina, fosforna kiselina, askorbinska kiselina, sorbinska kiselina, aspartna kiselina i sialinska kiselina.
13. Spoj za uporabu prema zahtjevu 11 ili zahtjevu 12, naznačen time, da spomenuti sastav nadalje obuhvaća nosač odabran od sljedećih: manitol, celulozni materijal, škrob ili njihove mješavine.
14. Spoj za uporabu prema bilo kojem od zahtjeva 5 do 13, naznačen time, da spomenuti sastav sadrži čestice od kojih više od 10% ima veličinu koja iznosi više od 10 mikrona.
15. Spoj za uporabu prema bilo kojem od zahtjeva 1 do 14, naznačen time, da se upotrebljava u postupku liječenja ili profilakse proteinopatije TDP-43.
16. Spoj za uporabu prema bilo kojem od zahtjeva 1 do 14, naznačen time, da se upotrebljava u postupku liječenja ili profilakse tautopatije.
17. Spoj za uporabu prema bilo kojem od zahtjeva 1 do 14, naznačen time, da se upotrebljava u postupku liječenja ili profilakse sljedećih stanja: Alzheimerova bolest, Pickova bolest, progresivna supranuklearna palsija (PSP), frontotemporalna demencija (FTD), FTD s parkinsonizmom povezanim s kromosomom 17, sindromi frontotemporalne lobarne degeneracije (FTLD-sindromi), kompleksi disinhibicije, demencije, parkinsonizma i amiotrofije, palido-ponto-nigralna degeneracija, sindrom Guam-ALS, palido-nigro-luizijanska degeneracija, kortiko-bazalna degeneracija, demencija s argirofilijskim zrnima, demencija pugilistika ili kronična traumatska encefalopatija, Downov sindrom, demencija s Lewyjevim tijelima, subakutni sklerozni panencefalitis, blago kognitivno oštećenje, Niemann-Pickova bolest, tip C, Sanfilippo-sindrom tipa B, mijotonijske distrofije DM1 ili DM2, ili amiotrofna lateralna skleroza (ALS).
18. Spoj za uporabu prema bilo kojem od zahtjeva 1 do 14, naznačen time, da se upotrebljava u postupku liječenja ili profilakse Alzheimerove bolesti.
19. Spoj za uporabu prema bilo kojem od zahtjeva 1 do 14, naznačen time, da se upotrebljava u postupku liječenja ili profilakse Parkinsonove bolesti.
20. Spoj za uporabu prema bilo kojem od zahtjeva 1 do 14, naznačen time, da se upotrebljava u postupku liječenja ili profilakse PSP, ALS ili FTLD.
21. Spoj za uporabu prema bilo kojem od zahtjeva 1 do 14, naznačen time, da se upotrebljava u postupku liječenja ili profilakse poliglutaminskog poremećaja.
22. Spoj za uporabu prema zahtjevu 21, naznačen time, da se upotrebljava u postupku liječenja ili profilakse Huntingtonove bolesti, mišićne atrofije kičmenih korijena, dentatorubro-palidoluizijanske atrofije ili spinocereberalnih ataksija.
23. Spoj za uporabu prema bilo kojem od zahtjeva 1 do 14, naznačen time, da se upotrebljava u postupku liječenja ili profilakse raka kože ili melanoma; ili stanja kod virusne, bakterijske ili protozoalne bolesti.
24. Spoj za uporabu prema zahtjevu 23, naznačen time, da je virusna, bakterijska i protozoalna bolest odabrana od sljedećih: hepatitis C, HIV, virus Zapadnog Nila (WNV) i malarija.
25. Spoj za uporabu prema bilo kojem od zahtjeva 1 do 24, naznačen time, da se spoj primjenjuje oralno kod navedenog liječenja ili profilakse.
26. Spoj za uporabu prema bilo kojem od zahtjeva 4 do 14, naznačen time, da je sastav u obliku tablete ili kapsule.
HRP20161291TT 2011-02-11 2016-10-06 Soli fenotiazin-diamina i njihova uporaba HRP20161291T1 (hr)

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Application Number Priority Date Filing Date Title
SG2011010600 2011-02-11
US201161485880P 2011-05-13 2011-05-13
EP11749476.5A EP2673266B1 (en) 2011-02-11 2011-08-15 Phenothiazine diaminium salts and their use
PCT/GB2011/001221 WO2012107706A1 (en) 2011-02-11 2011-08-15 Phenothiazine diaminium salts and their use

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ES2529714T3 (es) 2006-07-11 2015-02-24 Wista Laboratories Ltd. Procedimientos de síntesis y/o de purificación de compuestos de diaminofenotiazinio
US9925282B2 (en) 2009-01-29 2018-03-27 The General Hospital Corporation Cromolyn derivatives and related methods of imaging and treatment
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