ZA200410323B - Injectable depot formulation comprising crystals of iloperidone - Google Patents

Injectable depot formulation comprising crystals of iloperidone Download PDF

Info

Publication number: ZA200410323B
Authority: ZA; South Africa
Prior art keywords: crystals; depot formulation; formulation according; iloperidone; microns
Prior art date: 2002-07-15

Application number

ZA200410323A

Other languages

English (en)

Inventor

Dierk Wieckhusen

Alexandra Glausch

Markus Ahlheim

Original Assignee

Novartis Ag

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.)

2002-07-15

Filing date

2004-12-22

Publication date

2006-06-28

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=9940486&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ZA200410323(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2004-12-22 Application filed by Novartis Ag filed Critical Novartis Ag

2006-06-28 Publication of ZA200410323B publication Critical patent/ZA200410323B/en

Links

239000013078 crystal Substances 0.000 title claims abstract description 96
239000000203 mixture Substances 0.000 title claims abstract description 70
238000009472 formulation Methods 0.000 title claims abstract description 65
XMXHEBAFVSFQEX-UHFFFAOYSA-N iloperidone Chemical compound COC1=CC(C(C)=O)=CC=C1OCCCN1CCC(C=2C3=CC=C(F)C=C3ON=2)CC1 XMXHEBAFVSFQEX-UHFFFAOYSA-N 0.000 title claims abstract description 49
229960003162 iloperidone Drugs 0.000 title claims abstract description 45
239000002207 metabolite Substances 0.000 claims abstract description 18
239000000725 suspension Substances 0.000 claims description 14
239000004615 ingredient Substances 0.000 claims description 9
150000003839 salts Chemical class 0.000 claims description 9
239000004094 surface-active agent Substances 0.000 claims description 9
239000002562 thickening agent Substances 0.000 claims description 9
239000003795 chemical substances by application Substances 0.000 claims description 8
FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 7
229930195725 Mannitol Natural products 0.000 claims description 7
239000000594 mannitol Substances 0.000 claims description 7
235000010355 mannitol Nutrition 0.000 claims description 7
239000012453 solvate Substances 0.000 claims description 7
235000014113 dietary fatty acids Nutrition 0.000 claims description 6
239000000194 fatty acid Substances 0.000 claims description 6
229930195729 fatty acid Natural products 0.000 claims description 6
-1 sorbitan fatty acid ester Chemical class 0.000 claims description 6
238000002347 injection Methods 0.000 claims description 5
239000007924 injection Substances 0.000 claims description 5
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 5
DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical class CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 4
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 4
DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 4
239000002904 solvent Substances 0.000 claims description 4
WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 3
239000001768 carboxy methyl cellulose Substances 0.000 claims description 3
235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 3
229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 3
239000003981 vehicle Substances 0.000 claims description 3
ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Polymers FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 claims description 2
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 claims description 2
229920002785 Croscarmellose sodium Polymers 0.000 claims description 2
229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 2
DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical group C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 2
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 2
229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 2
239000000872 buffer Substances 0.000 claims description 2
239000007859 condensation product Substances 0.000 claims description 2
RKTYLMNFRDHKIL-UHFFFAOYSA-N copper;5,10,15,20-tetraphenylporphyrin-22,24-diide Chemical group [Cu+2].C1=CC(C(=C2C=CC([N-]2)=C(C=2C=CC=CC=2)C=2C=CC(N=2)=C(C=2C=CC=CC=2)C2=CC=C3[N-]2)C=2C=CC=CC=2)=NC1=C3C1=CC=CC=C1 RKTYLMNFRDHKIL-UHFFFAOYSA-N 0.000 claims description 2
239000008121 dextrose Substances 0.000 claims description 2
239000002270 dispersing agent Substances 0.000 claims description 2
239000003995 emulsifying agent Substances 0.000 claims description 2
150000002191 fatty alcohols Chemical class 0.000 claims description 2
239000000945 filler Substances 0.000 claims description 2
239000001863 hydroxypropyl cellulose Substances 0.000 claims description 2
235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 2
239000008101 lactose Substances 0.000 claims description 2
239000000314 lubricant Substances 0.000 claims description 2
239000003755 preservative agent Substances 0.000 claims description 2
230000002335 preservative effect Effects 0.000 claims description 2
239000011734 sodium Substances 0.000 claims description 2
229910052708 sodium Inorganic materials 0.000 claims description 2
239000011780 sodium chloride Substances 0.000 claims description 2
239000003381 stabilizer Substances 0.000 claims description 2
235000000346 sugar Nutrition 0.000 claims description 2
150000008163 sugars Chemical class 0.000 claims description 2
239000000080 wetting agent Substances 0.000 claims description 2
239000011575 calcium Substances 0.000 claims 1
229910052791 calcium Inorganic materials 0.000 claims 1
235000001465 calcium Nutrition 0.000 claims 1
239000001913 cellulose Substances 0.000 claims 1
229920006184 cellulose methylcellulose Polymers 0.000 claims 1
239000002245 particle Substances 0.000 abstract description 10
230000002596 correlated effect Effects 0.000 abstract description 8
238000003801 milling Methods 0.000 abstract description 6
238000010521 absorption reaction Methods 0.000 abstract description 4
238000012414 sterilization procedure Methods 0.000 abstract description 4
241000283973 Oryctolagus cuniculus Species 0.000 description 14
230000036470 plasma concentration Effects 0.000 description 6
DKPFZGUDAPQIHT-UHFFFAOYSA-N Butyl acetate Natural products CCCCOC(C)=O DKPFZGUDAPQIHT-UHFFFAOYSA-N 0.000 description 4
229940043232 butyl acetate Drugs 0.000 description 4
FUZZWVXGSFPDMH-UHFFFAOYSA-N hexanoic acid Chemical compound CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 description 4
229920001983 poloxamer Polymers 0.000 description 4
239000000243 solution Substances 0.000 description 4
238000013270 controlled release Methods 0.000 description 3
150000004665 fatty acids Chemical class 0.000 description 3
239000011521 glass Substances 0.000 description 3
201000000980 schizophrenia Diseases 0.000 description 3
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
239000012065 filter cake Substances 0.000 description 2
150000004677 hydrates Chemical class 0.000 description 2
239000004005 microsphere Substances 0.000 description 2
239000012299 nitrogen atmosphere Substances 0.000 description 2
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
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
241000220479 Acacia Species 0.000 description 1
241000416162 Astragalus gummifer Species 0.000 description 1
AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Polymers OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 1
235000010643 Leucaena leucocephala Nutrition 0.000 description 1
208000028017 Psychotic disease Diseases 0.000 description 1
239000004147 Sorbitan trioleate Substances 0.000 description 1
PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 description 1
229920001615 Tragacanth Polymers 0.000 description 1
VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 description 1
239000013543 active substance Substances 0.000 description 1
239000007900 aqueous suspension Substances 0.000 description 1
239000005415 artificial ingredient Substances 0.000 description 1
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
210000000170 cell membrane Anatomy 0.000 description 1
208000015114 central nervous system disease Diseases 0.000 description 1
229960001681 croscarmellose sodium Drugs 0.000 description 1
235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 1
201000010099 disease Diseases 0.000 description 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
238000004090 dissolution Methods 0.000 description 1
239000003925 fat Substances 0.000 description 1
VIQCGTZFEYDQMR-UHFFFAOYSA-N fluphenazine decanoate Chemical compound C1CN(CCOC(=O)CCCCCCCCC)CCN1CCCN1C2=CC(C(F)(F)F)=CC=C2SC2=CC=CC=C21 VIQCGTZFEYDQMR-UHFFFAOYSA-N 0.000 description 1
239000008103 glucose Substances 0.000 description 1
238000010255 intramuscular injection Methods 0.000 description 1
239000007927 intramuscular injection Substances 0.000 description 1
125000004284 isoxazol-3-yl group Chemical group [H]C1=C([H])C(*)=NO1 0.000 description 1
JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical compound CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 description 1
235000010445 lecithin Nutrition 0.000 description 1
239000000787 lecithin Substances 0.000 description 1
229940067606 lecithin Drugs 0.000 description 1
239000000463 material Substances 0.000 description 1
238000000034 method Methods 0.000 description 1
238000012986 modification Methods 0.000 description 1
230000004048 modification Effects 0.000 description 1
239000012452 mother liquor Substances 0.000 description 1
229910052757 nitrogen Inorganic materials 0.000 description 1
239000008194 pharmaceutical composition Substances 0.000 description 1
229920000747 poly(lactic acid) Polymers 0.000 description 1
229920000642 polymer Polymers 0.000 description 1
238000006116 polymerization reaction Methods 0.000 description 1
238000002360 preparation method Methods 0.000 description 1
239000000047 product Substances 0.000 description 1
125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 description 1
238000010992 reflux Methods 0.000 description 1
239000003488 releasing hormone Substances 0.000 description 1
230000000717 retained effect Effects 0.000 description 1
235000019337 sorbitan trioleate Nutrition 0.000 description 1
229960000391 sorbitan trioleate Drugs 0.000 description 1
238000010254 subcutaneous injection Methods 0.000 description 1
239000007929 subcutaneous injection Substances 0.000 description 1
239000000126 substance Substances 0.000 description 1
239000000196 tragacanth Substances 0.000 description 1
235000010487 tragacanth Nutrition 0.000 description 1
229940116362 tragacanth Drugs 0.000 description 1

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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- 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
- 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
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- 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

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Epidemiology (AREA)
Engineering & Computer Science (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Oil, Petroleum & Natural Gas (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Neurology (AREA)
Biochemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
Psychiatry (AREA)
Molecular Biology (AREA)
Dermatology (AREA)
Inorganic Chemistry (AREA)
Hospice & Palliative Care (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)
Plural Heterocyclic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

ZA200410323A 2002-07-15 2004-12-22 Injectable depot formulation comprising crystals of iloperidone ZA200410323B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
GBGB0216416.8A GB0216416D0 (en)	2002-07-15	2002-07-15	Organic compounds

Publications (1)

Publication Number	Publication Date
ZA200410323B true ZA200410323B (en)	2006-06-28

Family

ID=9940486

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200410323A ZA200410323B (en)	2002-07-15	2004-12-22	Injectable depot formulation comprising crystals of iloperidone

Country Status (15)

Country	Link
US (5)	US20050250813A1 (de)
EP (1)	EP1523335B1 (de)
JP (2)	JP5392961B2 (de)
AT (1)	ATE348635T1 (de)
AU (1)	AU2003281154B2 (de)
CA (1)	CA2492467C (de)
CY (1)	CY1106305T1 (de)
DE (1)	DE60310564T2 (de)
DK (1)	DK1523335T3 (de)
ES (1)	ES2279153T3 (de)
GB (1)	GB0216416D0 (de)
NZ (1)	NZ537598A (de)
PT (1)	PT1523335E (de)
WO (1)	WO2004006886A2 (de)
ZA (1)	ZA200410323B (de)

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
BRPI0213564B8 (pt)	2001-10-30	2021-05-25	Novartis Ag	formulação depósito e micropartícula compreendendo iloperidona e polímero poli(d,l-lactídeo-co-glicolídeo), e processo para preparação da referida micropartícula
GB0216416D0 (en)	2002-07-15	2002-08-21	Novartis Ag	Organic compounds
UA82561C2 (uk)	2003-10-23	2008-04-25	Оцука Фармасьютикалз Ко., Лтд.	Стерильна ін'єкційна композиція арипіпразолу з контрольованим вивільненням, спосіб її виготовлення та спосіб лікування шизофренії
US20100063093A1 (en)	2007-03-28	2010-03-11	Curt Wolfgang	Methods for the administration of iloperidone
WO2006039663A2 (en)	2004-09-30	2006-04-13	Vanda Pharmaceuticals, Inc	Methods for the administration of iloperidone
US20090306137A1 (en)	2006-05-22	2009-12-10	Wolfgang Curt D	Treatment for depressive disorders
US8198305B2 (en)	2007-04-13	2012-06-12	Concert Pharmaceuticals Inc.	1,2-benzisoxazol-3-yl compounds
SI2170279T1 (en)	2007-07-31	2018-04-30	Otsuka Pharmaceutical Co., Ltd.	Methods for producing aripiprazole suspension and freeze-dried formulation
CA2698534C (en)	2007-09-10	2018-10-09	Vanda Pharmaceuticals, Inc.	Prediction of qt prolongation based on snp genotype
EP2222301B1 (de)	2007-12-13	2014-10-08	Vanda Pharmaceuticals Inc.	Verfahren und zusammensetzung zur behandlung einer erkrankung, die durch den alpha-adrenozeptor vermittelt wird
WO2009076664A1 (en)	2007-12-13	2009-06-18	Vanda Pharmaceuticals Inc.	Method and composition for treating a serotonin receptor-mediated condition
WO2010031497A1 (en) *	2008-09-19	2010-03-25	Miklos Vertessy	New process for the preparation of iloperidone
CN101822673B (zh) *	2009-03-04	2013-09-18	北京德众万全药物技术开发有限公司	一种含有伊潘立酮的固体药物组合物
US20120136050A1 (en)	2009-07-16	2012-05-31	Vanda Pharmaceuticals Inc.	Use of a melatonin agonist for the treatment of sleep disorders including primary insomnia
WO2011032404A1 (zh)	2009-09-19	2011-03-24	浙江华海药业股份有限公司	伊潘立酮的一种制备方法及结晶方法
CN102030744B (zh) *	2009-09-30	2013-04-17	天津药物研究院	伊潘立酮晶体、其制备方法及药物组合物
WO2011055188A1 (en) *	2009-11-05	2011-05-12	Orchid Chemicals And Pharmaceuticals Limited	An improved process for the preparation of iloperidone
BR112012015084A2 (pt) *	2009-12-23	2017-03-07	Lupin Ltd	composição farmacêutica de liberação lenta de iloperidone
CN102108081A (zh) *	2009-12-25	2011-06-29	重庆医药工业研究院有限责任公司	伊潘立酮的新晶型及其制备方法
SG182285A1 (en)	2010-01-11	2012-08-30	Inotek Pharmaceuticals Corp	Combination, kit and method of reducing intraocular pressure
EA201290958A1 (ru)	2010-03-26	2013-04-30	Инотек Фармасьютикалз Корпорейшн	Способ снижения внутриглазного давления у людей с применением n6-циклопентиладенозина (cpa), производных cpa или их пролекарств
CN101822674B (zh) *	2010-05-27	2015-03-11	北京德众万全医药科技有限公司	一种伊潘立酮药物组合物及其制备方法
EP2629775A4 (de) *	2010-10-18	2014-06-11	Dainippon Sumitomo Pharma Co	Injizierbare formulierung mit verzögerter freisetzung
WO2012063269A2 (en)	2010-11-12	2012-05-18	Cadila Healthcare Limited	Process for preparing iloperidone
WO2012090138A1 (en)	2010-12-27	2012-07-05	Ranbaxy Laboratories Limited	Processes for the preparation of iloperidone
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2002
- 2002-07-15 GB GBGB0216416.8A patent/GB0216416D0/en not_active Ceased
2003
- 2003-07-14 US US10/521,064 patent/US20050250813A1/en not_active Abandoned
- 2003-07-14 WO PCT/EP2003/007619 patent/WO2004006886A2/en not_active Ceased
- 2003-07-14 DE DE60310564T patent/DE60310564T2/de not_active Expired - Lifetime
- 2003-07-14 ES ES03756455T patent/ES2279153T3/es not_active Expired - Lifetime
- 2003-07-14 DK DK03756455T patent/DK1523335T3/da active
- 2003-07-14 AU AU2003281154A patent/AU2003281154B2/en not_active Expired
- 2003-07-14 EP EP03756455A patent/EP1523335B1/de not_active Expired - Lifetime
- 2003-07-14 PT PT03756455T patent/PT1523335E/pt unknown
- 2003-07-14 AT AT03756455T patent/ATE348635T1/de active
- 2003-07-14 JP JP2004520629A patent/JP5392961B2/ja not_active Expired - Lifetime
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- 2008-10-21 US US12/254,925 patent/US20090099232A1/en not_active Abandoned
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Publication number	Publication date
AU2003281154B2 (en)	2006-10-12
US8293765B2 (en)	2012-10-23
GB0216416D0 (en)	2002-08-21
WO2004006886A3 (en)	2004-02-19
DE60310564T2 (de)	2007-10-04
NZ537598A (en)	2006-07-28
JP5392961B2 (ja)	2014-01-22
CY1106305T1 (el)	2011-10-12
PT1523335E (pt)	2007-02-28
DE60310564D1 (de)	2007-02-01
CA2492467A1 (en)	2004-01-22
ES2279153T3 (es)	2007-08-16
CA2492467C (en)	2010-03-16
US8614232B2 (en)	2013-12-24
AU2003281154A1 (en)	2004-02-02
US20110212141A1 (en)	2011-09-01
WO2004006886A2 (en)	2004-01-22
US20120156264A1 (en)	2012-06-21
ATE348635T1 (de)	2007-01-15
JP5670698B2 (ja)	2015-02-18
JP2011016849A (ja)	2011-01-27
EP1523335B1 (de)	2006-12-20
JP2005533093A (ja)	2005-11-04
EP1523335A2 (de)	2005-04-20
US8227488B2 (en)	2012-07-24
US20050250813A1 (en)	2005-11-10
HK1076029A1 (en)	2006-01-06
US20090099232A1 (en)	2009-04-16
US20130012542A1 (en)	2013-01-10
DK1523335T3 (da)	2007-01-29

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