HRP20201000T1 - POLIMORF I MONOFOSFATNE SOLI 6-FLUORO-2-[4-(PIRIDIN-2-IL)BUT-3-IN-1-IL] IMIDAZO [1,2A]PIRIDINA I NJEGOVI POLIMORFI KAO NEGATIVNI ALOSTERIČNI MODULATORI mGlu5 RECEPTORA - Google Patents

POLIMORF I MONOFOSFATNE SOLI 6-FLUORO-2-[4-(PIRIDIN-2-IL)BUT-3-IN-1-IL] IMIDAZO [1,2A]PIRIDINA I NJEGOVI POLIMORFI KAO NEGATIVNI ALOSTERIČNI MODULATORI mGlu5 RECEPTORA Download PDF

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HRP20201000T1
HRP20201000T1 HRP20201000TT HRP20201000T HRP20201000T1 HR P20201000 T1 HRP20201000 T1 HR P20201000T1 HR P20201000T T HRP20201000T T HR P20201000TT HR P20201000 T HRP20201000 T HR P20201000T HR P20201000 T1 HRP20201000 T1 HR P20201000T1
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Croatia
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disorders
imidazo
pyridin
fluoro
pyridine
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HRP20201000TT
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Béatrice BONNET
Sonia Maria Poli
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Addex Pharma S.A
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
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    • A61P25/00Drugs for disorders of the nervous system
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
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    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Organic Chemistry (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (8)

1. Kristalni oblik monofosfatne soli 6-fluoro-2-[4-(piridin-2-il)but-3-in-1-il]imidazo[1,2-a]piridina naznačen time da su najmanje 3 vrha odabrana iz vrhova X-Röntgenske difrakcije dobivene pomoću CuKα zračenja pri 2 ϴ (2 Theta (deg)) = 8.4, 10.2, 12.5, 15.7, 16.8, 18.6, 20.5, 21.3, 28.1, 29.4.
2. Kristalni oblik monofosfatne soli 6-fluoro-2-[4-(piridin-2-il)but-3-in-1-il]imidazo[1,2-a]piridina naznačen time da je praškasti uzorak X-Röntgenske difrakcije prikazan na Slici 1.
3. Kristalni oblik monofosfatne soli 6-fluoro-2-[4-(piridin-2-il)but-3-in-1-il]imidazo[1,2-a]piridina naznačen time da infracrveni spektar ima oštre vrpce pri 3059, 2937, 2233, 1592, 1564, 1537, 1515, 1477, 1429, 1317, 1262, 1168, 1162, 1117, 863, 819, 772, 691.
4. Kristalni oblik monofosfatne soli 6-fluoro-2-[4-(piridin-2-il)but-3-in-1-il]imidazo[1,2-a]piridina naznačen time da je infracrveni spektar prikazan na Slici 2.
5. Postupak za pripremu spoja prema zahtjevima 1 do 4, naznačen time da sadrži korake a) nastajanje soli 6-fluoro-2-[4-(piridin-2-il)but-3-in-1-il]imidazo[1,2-a]piridina sa fosfornom kiselinom sa naknadnim spontanim taloženjem, i rekristalizacijom produkta iz koraka a) u smjesi etanol:voda (80:20).
6. Farmaceutski pripravak, naznačen time da sadrži terapeutski aktivnu količinu spoja prema zahtjevima 1 do 4, i najmanje jedan farmaceutski prihvatljivi nosač, otapalo ili ekscipijens.
7. Spoj/pripravak prema zahtjevima 1 do 4 i 6 naznačen time da je za upotrebu u liječenju ili prevenciji poremećaja u kojima mGlu5 receptor igra ulogu, pri čemu su poremećaji izabrani iz skupine koju čini: epilepsija, ishemija, neuropatska ili upalna bol, fizijatrijski poremećaji kao što su psihotični poremećaji, poremećaji centralnog živčanog sustava izabrani iz adikcije, tolerancije ili ovisnosti, afektivni poremećaji, kao što su depresija i anksioznosti, poremećaji pomanjkanja pažnje/hiperaktivnosti, bipolarnog poremećaja, poremećaja kretanja, neuroprotekcije, migrene, neurološki poremećaja kao što su neurodegeneracija, neurotoksičnost, Parkinson-ova bolest, PD-LID, distonija, poremećaj pamćenja, Alzheimer-ove bolesti, demencije, delirija tremensa, poremećaja pažnje, poremećaja ishrane, poremećaja kretanja, kognitivnih poremećaja, poremećaja osobnosti, poremećaja ponašanja, poremećaja sličnih zlostavljanja predmeta, uključivo alkohol, nikotin, kokain, amfetamin, benzodiazepin, analgetici, opijati ili ostale tolerantne tvari ili ovisnosti, bulimija nervoza, anoreksija nervoza, ovisnost o kockanju, ovisnost o seksu, opsesivni kompulzivni poremećaji, poremećaji panike, fobije, poremećaji posttraumatskog stresa, opći poremećaji anksioznosti, sezonski afektivni poremećaji, poremećaji akutnog stresa, naslijeđeni poremećaji kao što je Fragile X sindrom, autizam, debljina i gastroenterološki poremećaj, na primjer, poremećaj gastro-esofegalnog refulska (GERD), poremećaj nižeg ezofagealnog sfinktera ili poremećaji, bolesti gastroentološke pokretljivosti, kolitis, Chron-ova bolest ili sindrom iritabilnog crijeva (IBS).
8. Spoj/pripravak prema zahtjevima 1 d o4 i 6, naznačen time da je za upotrebu u liječenju ili prevenciji: dostojine, Parkinson-ove bolesti, L-DOPA diskinezije, poremećaja kretanja, autizma, Fraglie X, anksioznosti, depresije, ili bolova.
HRP20201000TT 2013-09-25 2020-06-25 POLIMORF I MONOFOSFATNE SOLI 6-FLUORO-2-[4-(PIRIDIN-2-IL)BUT-3-IN-1-IL] IMIDAZO [1,2A]PIRIDINA I NJEGOVI POLIMORFI KAO NEGATIVNI ALOSTERIČNI MODULATORI mGlu5 RECEPTORA HRP20201000T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1317022.0A GB201317022D0 (en) 2013-09-25 2013-09-25 Polymorphs
EP14777052.3A EP3049413B1 (en) 2013-09-25 2014-09-25 Polymorph i of the mono-phosphate salt of 6-fluoro-2-[4-(pyridin-2-yl)but-3-yn-1-yl] imidazo[1,2a]pyridine and polymorphs thereof as negative allosteric modulator of mglu5 receptor
PCT/EP2014/070492 WO2015044270A1 (en) 2013-09-25 2014-09-25 Mono-phosphate salt of 6-fluoro-2-[4-(pyridin-2-yl)but-3-yn-1-yl]imidazo[1,2a]pyridine and polymorphs thereof as negative allosteric modulator of mglu5 receptor

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HRP20201000T1 true HRP20201000T1 (hr) 2020-10-16

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HRP20201000TT HRP20201000T1 (hr) 2013-09-25 2020-06-25 POLIMORF I MONOFOSFATNE SOLI 6-FLUORO-2-[4-(PIRIDIN-2-IL)BUT-3-IN-1-IL] IMIDAZO [1,2A]PIRIDINA I NJEGOVI POLIMORFI KAO NEGATIVNI ALOSTERIČNI MODULATORI mGlu5 RECEPTORA

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US (1) US9938270B2 (hr)
EP (2) EP3693370A1 (hr)
JP (2) JP6768504B2 (hr)
KR (2) KR102412602B1 (hr)
CN (2) CN105873926A (hr)
AU (1) AU2014327236B2 (hr)
CA (1) CA2925040C (hr)
CY (1) CY1123020T1 (hr)
DK (1) DK3049413T3 (hr)
EA (1) EA028037B1 (hr)
ES (1) ES2794022T3 (hr)
GB (1) GB201317022D0 (hr)
HR (1) HRP20201000T1 (hr)
HU (1) HUE049917T2 (hr)
IL (2) IL244673B (hr)
LT (1) LT3049413T (hr)
MX (1) MX363289B (hr)
NZ (1) NZ719081A (hr)
PH (1) PH12016500546B1 (hr)
PL (1) PL3049413T3 (hr)
PT (1) PT3049413T (hr)
RS (1) RS60478B1 (hr)
SG (1) SG11201602271UA (hr)
SI (1) SI3049413T1 (hr)
UA (1) UA119651C2 (hr)
WO (1) WO2015044270A1 (hr)

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GB201317022D0 (en) * 2013-09-25 2013-11-06 Addex Pharmaceuticals Sa Polymorphs

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* Cited by examiner, † Cited by third party
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GB0413605D0 (en) * 2004-06-17 2004-07-21 Addex Pharmaceuticals Sa Novel compounds
AU2007336369B2 (en) * 2006-12-21 2013-01-17 F. Hoffmann-La Roche Ag Polymorphs of a mGluR5 receptor antagonist
GB201204962D0 (en) 2012-03-21 2012-05-02 Addex Pharmaceuticals Sa Pharmaceutical combination products for parkinsons disease
GB201210530D0 (en) 2012-06-13 2012-07-25 Addex Pharmaceuticals Sa Extended release formulations
GB201317022D0 (en) * 2013-09-25 2013-11-06 Addex Pharmaceuticals Sa Polymorphs

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CY1123020T1 (el) 2021-10-29
UA119651C2 (uk) 2019-07-25
RS60478B1 (sr) 2020-08-31
MX363289B (es) 2019-03-19
PL3049413T3 (pl) 2020-10-19
JP2020172512A (ja) 2020-10-22
CA2925040A1 (en) 2015-04-02
IL244673B (en) 2022-07-01
PH12016500546A1 (en) 2016-06-13
SG11201602271UA (en) 2016-04-28
AU2014327236B2 (en) 2018-03-22
JP6768504B2 (ja) 2020-10-14
EP3693370A1 (en) 2020-08-12
BR112016006513A2 (pt) 2017-08-01
KR102412602B1 (ko) 2022-06-23
CA2925040C (en) 2022-03-22
SI3049413T1 (sl) 2020-08-31
DK3049413T3 (da) 2020-06-15
WO2015044270A1 (en) 2015-04-02
CN105873926A (zh) 2016-08-17
KR20220088960A (ko) 2022-06-28
LT3049413T (lt) 2020-06-25
NZ719081A (en) 2018-08-31
IL293356A (en) 2022-07-01
PT3049413T (pt) 2020-05-27
HUE049917T2 (hu) 2020-11-30
EA201690616A1 (ru) 2016-07-29
EA028037B1 (ru) 2017-09-29
ES2794022T3 (es) 2020-11-17
KR20160092989A (ko) 2016-08-05
MX2016003816A (es) 2016-08-04
US20160214979A1 (en) 2016-07-28
US9938270B2 (en) 2018-04-10
EP3049413A1 (en) 2016-08-03
IL244673A0 (en) 2016-04-21
JP2016531860A (ja) 2016-10-13
GB201317022D0 (en) 2013-11-06
EP3049413B1 (en) 2020-04-29
PH12016500546B1 (en) 2016-06-13
AU2014327236A1 (en) 2016-05-12
CN111574516A (zh) 2020-08-25

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