HRP20150196T1 - Farmaceutske formulacije s ligandima receptora dopamina - Google Patents

Farmaceutske formulacije s ligandima receptora dopamina Download PDF

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HRP20150196T1
HRP20150196T1 HRP20150196TT HRP20150196T HRP20150196T1 HR P20150196 T1 HRP20150196 T1 HR P20150196T1 HR P20150196T T HRP20150196T T HR P20150196TT HR P20150196 T HRP20150196 T HR P20150196T HR P20150196 T1 HRP20150196 T1 HR P20150196T1
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mean
piperazin
dichlorophenyl
trans
ethyl
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HRP20150196TT
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Ranajoy Sarkar
Mahendra G. Dedhiya
Anil Chhettry
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Richter Gedeon Nyrt.
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Publication of HRP20150196T1 publication Critical patent/HRP20150196T1/hr

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    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
    • H04NPICTORIAL COMMUNICATION, e.g. TELEVISION
    • H04N25/00Circuitry of solid-state image sensors [SSIS]; Control thereof
    • H04N25/70SSIS architectures; Circuits associated therewith
    • H04N25/71Charge-coupled device [CCD] sensors; Charge-transfer registers specially adapted for CCD sensors
    • H04N25/75Circuitry for providing, modifying or processing image signals from the pixel array
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
    • H04NPICTORIAL COMMUNICATION, e.g. TELEVISION
    • H04N25/00Circuitry of solid-state image sensors [SSIS]; Control thereof
    • H04N25/70SSIS architectures; Circuits associated therewith
    • H04N25/76Addressed sensors, e.g. MOS or CMOS sensors

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Claims (15)

1. Farmaceutska formulacija, u čvrstom obliku, za oralno doziranje, koja obuhvaća trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil ureu ili farmaceutski primjenjivu sol te tvari, pufersko sredstvo ili pomoćnu tvar, odabranu iz prethodno želatiniranog škroba i suhog kalcij-hidrogenfosfata, naznačena time da formulacija sadrži manje od 1% G/G trans-4-[2-[4-(2,3-dichlorphenyl)-piperazin-1-yl]-ethyl]-cyclohexylamina ili jednu farmaceutski primjenjivu sol tog spoja.
2. Formulacija, prema zahtjevu 1, koja obuhvaća od oko 0,5 do oko 15 mg trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil uree ili farmaceutski primjenjivu sol tog spoja, naznačena time da formulacija daje jedan in vivo-plazmaprofil, obuhvaćajući: (i) jedan srednji Cmax. od manje nego 26,3 ng/ml, (ii) jednu srednju AUC 0-∞ od više nego 10 ng/h/ml i (iii) jednu srednju Tmax od oko 3 ili više sati.
3. Formulacija prema zahtjevu 2, naznačena time da formulacija obuhvaća od oko 0,5 mg trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil uree ili farmaceutski primjenjivu sol tog spoja, i daje jedan in vivo-plazmaprofil, obuhvaćajući: (i) jedan srednji Cmax. od manje nego 0,9 ng/ml, (ii) jednu srednju AUC 0-∞ od više nego 10 ng/h/ml i (iii) jednu srednju Tmax od oko 3 ili više sati.
4. Formulacija prema zahtjevu 2, naznačena time da formulacija obuhvaća oko 1 mg trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil uree ili farmaceutski primjenjivu sol tog spoja, i daje jedan in vivo-plazmaprofil, obuhvaćajući: (i) jedan srednji Cmax. od manje nego 1,8 ng/ml, (ii) jednu srednju AUC 0-∞ od više nego 20 ng/h/ml i (iii) jednu srednju Tmax od oko 3 ili više sati.
5. Formulacija prema zahtjevu 2, naznačena time da formulacija obuhvaća oko 1,5 mg trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil uree ili farmaceutski primjenjivu sol tog spoja, i daje jedan in vivo-plazmaprofil, obuhvaćajući: (i) jedan srednji Cmax. od manje nego 2,7 ng/ml, (ii) jednu srednju AUC 0-∞ od više nego 30 ng/h/ml i (iii) jednu srednju Tmax od oko 3 ili više sati.
6. Formulacija prema zahtjevu 2, naznačena time da formulacija obuhvaća oko 2 mg trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil uree ili farmaceutski primjenjivu sol tog spoja, i daje jedan in vivo-plazmaprofil, obuhvaćajući: (i) jedan srednji Cmax. od manje nego 3,5 ng/ml, (ii) jednu srednju AUC 0-∞ od više nego oko 40 ng/h/ml i (iii) jednu srednju Tmax od oko 3 ili više sati.
7. Formulacija prema zahtjevu 2, naznačena time da formulacija obuhvaća oko 2,5 mg trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil uree ili farmaceutski primjenjivu sol tog spoja, i daje jedan in vivo-plazmaprofil, obuhvaćajući: (i) jedan srednji Cmax. od manje nego 4,4 ng/ml, (ii) jednu srednju AUC 0-∞ od više nego 50 ng/h/ml i (iii) jednu srednju Tmax od oko 3 ili više sati.
8. Formulacija prema zahtjevu 2, naznačena time da formulacija obuhvaća oko 3 mg trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil uree ili farmaceutski primjenjivu sol tog spoja, i daje jedan in vivo-plazmaprofil, obuhvaćajući: (i) jedan srednji Cmax. od manje nego 5,3 ng/ml, (ii) jednu srednju AUC 0-∞ od više nego 60 ng/h/ml i (iii) jednu srednju Tmax od oko 3 ili više sati.
9. Formulacija prema zahtjevu 2, naznačena time da formulacija obuhvaća oko 6 mg trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil uree ili jednu farmaceutski primjenjivu sol tog spoja, i daje jedan in vivo-plazmaprofil, obuhvaćajući: (i) jedan srednji Cmax. od manje nego 10,5 ng/ml, (ii) jednu srednju AUC 0-∞ od više nego 120 ng/h/ml i (iii) jednu srednju Tmax od oko 3 ili više sati.
10. Formulacija prema zahtjevu 2, naznačena time da formulacija obuhvaća oko 9 mg trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil uree ili farmaceutski primjenjivu sol tog spoja, i daje jedan in vivo-plazmaprofil, obuhvaćajući: (i) jedan srednji Cmax. od manje nego 15,8 ng/ml, (ii) jednu srednju AUC 0-∞ od više nego 180 ng/h/ml i (iii) jednu srednju Tmax od oko 3 ili više sati.
11. Formulacija prema zahtjevu 2, naznačena time da formulacija obuhvaća oko 12,5 mg trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil uree ili jednu farmaceutski primjenjivu sol tog spoja, i daje jedan in vivo-plazmaprofil, obuhvaćajući: (i) jedan srednji Cmax. od manje nego 21,9 ng/ml, (ii) jednu srednju AUC 0-∞ od više nego 250 ng/h/ml i (iii) jednu srednju Tmax od oko 3 ili više sati.
12. Formulacija prema zahtjevu 1 ili zahtjevu 2, naznačena time da formulacija obuhvaća trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil urea-hidroklorid.
13. Formulacija prema zahtjevu 1 ili zahtjevu 2, naznačena time da obuhvaća: (a) Između oko 0,5% i oko 15 % trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil urea-hidroklorida, (b) Između oko 0,1% i oko 20% natrij karbonata, (c) Između 0% i oko 10% talka, (d) Između 0% i oko 5% koloidalnog silicij dioksida, (e) Između 0% i oko 15% natrij-glikolata škroba, (f) Između oko 5% i oko 95% mikrokristalne celuloze i (g) Između oko 0,1% i oko 3% magnezij-stearata.
14. Formulacija prema zahtjevu 1 ili zahtjevu 2, naznačena time da formulacija obuhvaća trans-1{4-[2-[4-(2,3-diklorfenil)-piperazin-1-il]-etil]-cikloheksil}-3,3-dimetil ureu ili farmaceutski primjenjivu sol tog spoja s količinom od više od oko 80%, koja bude oslobođena unutar prvih 60 minuta, nakon aplikacije formulacije, kod potrebitih pacijenata.
15. Formulacija prema zahtjevu 1 ili zahtjevu 2 naznačena time da se primjenjuje u postupku liječenja šizofrenije, biplolarnog poremećaja ili akutne manije.
HRP20150196TT 2008-07-16 2015-02-19 Farmaceutske formulacije s ligandima receptora dopamina HRP20150196T1 (hr)

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Application Number Priority Date Filing Date Title
US8105208P 2008-07-16 2008-07-16
EP09798745.7A EP2317852B1 (en) 2008-07-16 2009-07-16 Pharmaceutical formulations containing dopamine receptor ligands
PCT/US2009/050835 WO2010009309A1 (en) 2008-07-16 2009-07-16 Pharmaceutical formulations containing dopamine receptor ligands

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HRP20150196T1 true HRP20150196T1 (hr) 2015-06-05

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US (6) US9056845B2 (hr)
EP (1) EP2317852B1 (hr)
JP (1) JP5774988B2 (hr)
KR (1) KR101612146B1 (hr)
CN (2) CN102118970A (hr)
AP (1) AP2975A (hr)
AU (1) AU2009270823B2 (hr)
BR (1) BRPI0916241A2 (hr)
CA (1) CA2730287C (hr)
CL (1) CL2011000091A1 (hr)
CO (1) CO6351689A2 (hr)
CY (1) CY1115994T1 (hr)
DK (1) DK2317852T3 (hr)
EA (1) EA025636B1 (hr)
EC (1) ECSP11010834A (hr)
ES (1) ES2532636T3 (hr)
GE (1) GEP20146052B (hr)
HR (1) HRP20150196T1 (hr)
IL (1) IL210615A (hr)
MA (1) MA32568B1 (hr)
MX (1) MX2011000622A (hr)
MY (1) MY156288A (hr)
NI (1) NI201100016A (hr)
NZ (1) NZ590852A (hr)
PL (1) PL2317852T3 (hr)
PT (1) PT2317852E (hr)
RS (1) RS53866B1 (hr)
SG (1) SG192507A1 (hr)
SI (1) SI2317852T1 (hr)
SM (1) SMT201500063B (hr)
UA (1) UA104869C2 (hr)
WO (1) WO2010009309A1 (hr)
ZA (1) ZA201101134B (hr)

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HUP0700353A2 (en) 2007-05-18 2008-12-29 Richter Gedeon Nyrt Metabolites of (thio)carbamoyl-cyclohexane derivatives
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SG192507A1 (en) 2008-07-16 2013-08-30 Richter Gedeon Nyrt Pharmaceutical formulations containing dopamine receptor ligands
HU230067B1 (hu) 2008-12-17 2015-06-29 Richter Gedeon Nyrt Új piperazin só és eljárás előállítására
HUP0800766A2 (en) 2008-12-18 2010-11-29 Richter Gedeon Vegyeszet Process for the preparation of piperazine derivatives
HUP0800765A2 (en) 2008-12-18 2010-11-29 Richter Gedeon Nyrt A new process for the preparation of piperazine derivatives and their hydrochloric salts
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EP3231418A1 (en) * 2016-04-14 2017-10-18 Richter Gedeon Nyrt. Granule formulation for oral administration
US11274087B2 (en) 2016-07-08 2022-03-15 Richter Gedeon Nyrt. Industrial process for the preparation of cariprazine
CN107970217A (zh) * 2016-10-25 2018-05-01 浙江京新药业股份有限公司 卡利拉嗪口腔崩解片及其制备方法
HUP1700253A1 (hu) * 2017-06-13 2019-01-28 Richter Gedeon Nyrt Szilárd orális gyógyszerkészítmények
CN109589315A (zh) * 2017-10-01 2019-04-09 北京万全德众医药生物技术有限公司 卡利拉嗪-亲水性材料共混物固体制剂的制备方法
HU231500B1 (hu) 2019-04-10 2024-04-28 Richter Gedeon Nyrt Karbamoil-ciklohexán származékok autizmus spektrum betegség kezelésére
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HUP2200312A1 (hu) * 2022-08-05 2024-02-28 Richter Gedeon Nyrt Kariprazin tartalmú szájban diszpergálódó tabletta

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