UA61898C2 - Pharmaceutical composition based on 9-hydroxyrisperidone esters, method for its production and method for treatment - Google Patents

Pharmaceutical composition based on 9-hydroxyrisperidone esters, method for its production and method for treatment Download PDF

Info

Publication number: UA61898C2
Authority: UA; Ukraine
Prior art keywords: fact; composition according; active ingredient; mixture; agent
Prior art date: 1996-05-20

Application number

UA98052747A

Other languages

English (en)

Ukrainian (uk)

Original Assignee

Janssen Pharmaceutica Nv

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1996-05-20

Filing date

1997-12-05

Publication date

2003-12-15

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=8224016&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=UA61898(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

1997-12-05 Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv

2003-12-15 Publication of UA61898C2 publication Critical patent/UA61898C2/uk

Links

238000000034 method Methods 0.000 title claims abstract description 14
239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 8
PMXMIIMHBWHSKN-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one Chemical class FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCC(O)C4=NC=3C)=NOC2=C1 PMXMIIMHBWHSKN-UHFFFAOYSA-N 0.000 title claims description 18
238000004519 manufacturing process Methods 0.000 title description 2
239000000203 mixture Substances 0.000 claims abstract description 48
239000003814 drug Substances 0.000 claims abstract description 41
239000004480 active ingredient Substances 0.000 claims abstract description 24
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WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical group OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 claims description 18
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
239000003755 preservative agent Substances 0.000 claims description 10
239000000375 suspending agent Substances 0.000 claims description 10
VOMKSBFLAZZBOW-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-9-yl hexadecanoate Chemical group FC1=CC=C2C(C3CCN(CC3)CCC3=C(C)N=C4N(C3=O)CCCC4OC(=O)CCCCCCCCCCCCCCC)=NOC2=C1 VOMKSBFLAZZBOW-UHFFFAOYSA-N 0.000 claims description 9
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DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical group [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 7
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239000004615 ingredient Substances 0.000 claims description 4
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125000002958 pentadecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
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239000008240 homogeneous mixture Substances 0.000 claims 1
239000008363 phosphate buffer Substances 0.000 claims 1
238000012876 topography Methods 0.000 claims 1
-1 9-hydroxyrisperidone fatty acid ester Chemical class 0.000 abstract description 8
238000009472 formulation Methods 0.000 abstract 1
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239000007927 intramuscular injection Substances 0.000 abstract 1
238000010254 subcutaneous injection Methods 0.000 abstract 1
239000007929 subcutaneous injection Substances 0.000 abstract 1
RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 description 23
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IPCSVZSSVZVIGE-UHFFFAOYSA-N palmitic acid group Chemical group C(CCCCCCCCCCCCCCC)(=O)O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 3
AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical group [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 description 3
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CFKMVGJGLGKFKI-UHFFFAOYSA-N 4-chloro-m-cresol Chemical compound CC1=CC(O)=CC=C1Cl CFKMVGJGLGKFKI-UHFFFAOYSA-N 0.000 description 2
HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
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KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
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239000003792 electrolyte Substances 0.000 description 2
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LNEPOXFFQSENCJ-UHFFFAOYSA-N haloperidol Chemical compound C1CC(O)(C=2C=CC(Cl)=CC=2)CCN1CCCC(=O)C1=CC=C(F)C=C1 LNEPOXFFQSENCJ-UHFFFAOYSA-N 0.000 description 2
IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 description 2
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JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 1
RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical compound O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 description 1
IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
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FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 description 1
GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
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IPBVNPXQWQGGJP-UHFFFAOYSA-N acetic acid phenyl ester Natural products CC(=O)OC1=CC=CC=C1 IPBVNPXQWQGGJP-UHFFFAOYSA-N 0.000 description 1
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WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
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Classifications

- 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
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
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- A61K31/495—Heterocyclic 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
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- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- 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
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof

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Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Chemical & Material Sciences (AREA)
Veterinary Medicine (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Chemical Kinetics & Catalysis (AREA)
Epidemiology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Psychiatry (AREA)
Dermatology (AREA)
Hospice & Palliative Care (AREA)
Pain & Pain Management (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Agricultural Chemicals And Associated Chemicals (AREA)

UA98052747A 1996-05-20 1997-12-05 Pharmaceutical composition based on 9-hydroxyrisperidone esters, method for its production and method for treatment UA61898C2 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
EP96201429		1996-05-20
PCT/EP1997/002504 WO1997044039A1 (en)	1996-05-20	1997-05-12	Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters

Publications (1)

Publication Number	Publication Date
UA61898C2 true UA61898C2 (en)	2003-12-15

Family

ID=8224016

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
UA98052747A UA61898C2 (en)	1996-05-20	1997-12-05	Pharmaceutical composition based on 9-hydroxyrisperidone esters, method for its production and method for treatment

Country Status (38)

Country	Link
US (1)	US6077843A (es)
EP (1)	EP0904081B1 (es)
JP (1)	JP3274687B2 (es)
KR (1)	KR100358373B1 (es)
CN (1)	CN1093762C (es)
AR (1)	AR007194A1 (es)
AT (1)	ATE208619T1 (es)
AU (1)	AU715572B2 (es)
BG (1)	BG62684B1 (es)
BR (1)	BR9706824B8 (es)
CA (1)	CA2236691C (es)
CY (2)	CY2270B1 (es)
CZ (1)	CZ291284B6 (es)
DE (2)	DE122011100027I1 (es)
DK (1)	DK0904081T3 (es)
EA (1)	EA000536B1 (es)
EE (1)	EE03594B1 (es)
ES (1)	ES2167745T3 (es)
FR (1)	FR11C0035I2 (es)
HK (1)	HK1017852A1 (es)
HR (1)	HRP970276B1 (es)
HU (2)	HU224025B1 (es)
ID (1)	ID16927A (es)
IL (1)	IL124551A (es)
LU (1)	LU91842I2 (es)
MX (1)	MX9804816A (es)
MY (1)	MY126302A (es)
NO (2)	NO315931B1 (es)
NZ (1)	NZ330369A (es)
PL (1)	PL188309B1 (es)
PT (1)	PT904081E (es)
SI (1)	SI0904081T1 (es)
SK (1)	SK284013B6 (es)
TR (1)	TR199800923T2 (es)
TW (1)	TW487572B (es)
UA (1)	UA61898C2 (es)
WO (1)	WO1997044039A1 (es)
ZA (1)	ZA974331B (es)

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1997
- 1997-05-01 TW TW086105768A patent/TW487572B/zh not_active IP Right Cessation
- 1997-05-12 EE EE9800136A patent/EE03594B1/xx active Protection Beyond IP Right Term
- 1997-05-12 PT PT97923912T patent/PT904081E/pt unknown
- 1997-05-12 IL IL12455197A patent/IL124551A/xx not_active IP Right Cessation
- 1997-05-12 PL PL97327995A patent/PL188309B1/pl unknown
- 1997-05-12 CZ CZ19981401A patent/CZ291284B6/cs not_active IP Right Cessation
- 1997-05-12 CA CA002236691A patent/CA2236691C/en not_active Expired - Lifetime
- 1997-05-12 AU AU29559/97A patent/AU715572B2/en not_active Expired
- 1997-05-12 DE DE201112100027 patent/DE122011100027I1/de active Pending
- 1997-05-12 US US09/180,659 patent/US6077843A/en not_active Expired - Lifetime
- 1997-05-12 NZ NZ330369A patent/NZ330369A/xx not_active IP Right Cessation
- 1997-05-12 SI SI9730272T patent/SI0904081T1/xx unknown
- 1997-05-12 JP JP54150097A patent/JP3274687B2/ja not_active Expired - Lifetime
- 1997-05-12 TR TR1998/00923T patent/TR199800923T2/xx unknown
- 1997-05-12 CN CN97191494A patent/CN1093762C/zh not_active Expired - Lifetime
- 1997-05-12 SK SK620-98A patent/SK284013B6/sk not_active IP Right Cessation
- 1997-05-12 ES ES97923912T patent/ES2167745T3/es not_active Expired - Lifetime
- 1997-05-12 DE DE69708284T patent/DE69708284T2/de not_active Expired - Lifetime
- 1997-05-12 WO PCT/EP1997/002504 patent/WO1997044039A1/en active IP Right Grant
- 1997-05-12 AT AT97923912T patent/ATE208619T1/de active
- 1997-05-12 BR BRPI9706824-1B8A patent/BR9706824B8/pt not_active IP Right Cessation
- 1997-05-12 KR KR10-1998-0703629A patent/KR100358373B1/ko active IP Right Review Request
- 1997-05-12 EA EA199800531A patent/EA000536B1/ru not_active IP Right Cessation
- 1997-05-12 HU HU9901319A patent/HU224025B1/hu active Protection Beyond IP Right Term
- 1997-05-12 DK DK97923912T patent/DK0904081T3/da active
- 1997-05-12 EP EP97923912A patent/EP0904081B1/en not_active Expired - Lifetime
- 1997-05-19 ZA ZA974331A patent/ZA974331B/xx unknown
- 1997-05-19 MY MYPI97002172A patent/MY126302A/en unknown
- 1997-05-19 ID IDP971649A patent/ID16927A/id unknown
- 1997-05-19 AR ARP970102112A patent/AR007194A1/es active IP Right Grant
- 1997-05-20 HR HR970276A patent/HRP970276B1/xx not_active IP Right Cessation
- 1997-12-05 UA UA98052747A patent/UA61898C2/uk unknown
1998
- 1998-04-30 NO NO19981984A patent/NO315931B1/no not_active IP Right Cessation
- 1998-05-12 BG BG102443A patent/BG62684B1/bg unknown
- 1998-06-15 MX MX9804816A patent/MX9804816A/es unknown
1999
- 1999-07-10 HK HK99102949A patent/HK1017852A1/xx not_active IP Right Cessation
2002
- 2002-04-25 CY CY0200021A patent/CY2270B1/xx unknown
2011
- 2011-07-20 LU LU91842C patent/LU91842I2/fr unknown
- 2011-08-18 CY CY2011011C patent/CY2011011I1/el unknown
- 2011-08-18 HU HUS1100013C patent/HUS1100013I1/hu unknown
- 2011-08-29 NO NO2011015C patent/NO2011015I2/no unknown
- 2011-09-02 FR FR11C0035C patent/FR11C0035I2/fr active Active

Also Published As

Publication number	Publication date
AU2955997A (en)	1997-12-09
SK62098A3 (en)	2000-04-10
EP0904081A1 (en)	1999-03-31
EE03594B1 (et)	2002-02-15
KR100358373B1 (ko)	2003-02-11
CN1093762C (zh)	2002-11-06
ES2167745T3 (es)	2002-05-16
KR19990067603A (ko)	1999-08-25
EA000536B1 (ru)	1999-10-28
JP3274687B2 (ja)	2002-04-15
MY126302A (en)	2006-09-29
NO981984D0 (no)	1998-04-30
HK1017852A1 (en)	1999-12-03
HU224025B1 (hu)	2005-05-30
AU715572B2 (en)	2000-02-03
NZ330369A (en)	2000-04-28
ZA974331B (en)	1998-11-19
DE69708284T2 (de)	2002-07-25
ID16927A (id)	1997-11-20
BR9706824A (pt)	1999-03-23
PL327995A1 (en)	1999-01-04
IL124551A0 (en)	1998-12-06
NO2011015I1 (no)	2011-09-19
CZ291284B6 (cs)	2003-01-15
BR9706824B8 (pt)	2015-02-18
WO1997044039A1 (en)	1997-11-27
TR199800923T2 (xx)	1999-09-21
JP2000513718A (ja)	2000-10-17
ATE208619T1 (de)	2001-11-15
IL124551A (en)	2001-08-26
SK284013B6 (sk)	2004-08-03
FR11C0035I1 (es)	2011-07-10
CZ140198A3 (cs)	1999-04-14
NO981984L (no)	1998-11-19
NO2011015I2 (no)	2013-03-11
EE9800136A (et)	1998-10-15
DE122011100027I1 (de)	2011-11-17
HUP9901319A2 (hu)	1999-08-30
EA199800531A1 (ru)	1998-12-24
HRP970276A2 (en)	1998-04-30
DE69708284D1 (de)	2001-12-20
AR007194A1 (es)	1999-10-13
CA2236691C (en)	2007-01-02
CY2270B1 (en)	2003-07-04
DK0904081T3 (da)	2002-02-25
TW487572B (en)	2002-05-21
SI0904081T1 (en)	2002-04-30
NO315931B1 (no)	2003-11-17
BG102443A (en)	1999-06-30
CY2011011I2 (el)	2016-12-14
LU91842I2 (fr)	2011-09-20
MX9804816A (es)	1998-10-31
PL188309B1 (pl)	2005-01-31
PT904081E (pt)	2002-04-29
CA2236691A1 (en)	1997-11-27
HUP9901319A3 (en)	1999-11-29
EP0904081B1 (en)	2001-11-14
HUS1100013I1 (hu)	2017-03-28
CY2011011I1 (el)	2016-12-14
BG62684B1 (bg)	2000-05-31
FR11C0035I2 (fr)	2013-08-16
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HRP970276B1 (en)	2002-04-30
US6077843A (en)	2000-06-20

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