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PE20070334A1 - COMPOSITIONS AND PHARMACEUTICAL DOSAGE FORMS INCLUDED BY LECOZOTAN - Google Patents

COMPOSITIONS AND PHARMACEUTICAL DOSAGE FORMS INCLUDED BY LECOZOTAN

Info

Publication number
PE20070334A1
PE20070334A1 PE2006001076A PE2006001076A PE20070334A1 PE 20070334 A1 PE20070334 A1 PE 20070334A1 PE 2006001076 A PE2006001076 A PE 2006001076A PE 2006001076 A PE2006001076 A PE 2006001076A PE 20070334 A1 PE20070334 A1 PE 20070334A1
Authority
PE
Peru
Prior art keywords
lecozotan
propil
dioxin
piperazin
pyridin
Prior art date
Application number
PE2006001076A
Other languages
Spanish (es)
Inventor
Krishnendu S Ghosh
Arwinder S Nagi
Melissa Lin
Ping Cai
Michel Bernatchez
Sangeeta Raje
Mark Lankau
Eric N C Browne
Leonid Linberg
Xiaohong Pan
Original Assignee
Wyeth Corp
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.)
Filing date
Publication date
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of PE20070334A1 publication Critical patent/PE20070334A1/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • 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
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • 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
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • 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
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

SE REFIERE A UNA COMPOSICION FARMACEUTICA QUE COMPRENDE DERIVADOS DE {(2R)-2-[4-(2,3-DIHIDRO-BENZO[1,4]DIOXIN-5-IL)-PIPERAZIN-1-IL]-PROPIL}-N-PIRIDIN-2-IL Y METABOLITOS, SIENDO PREFERIDO EL COMPUESTO 4-CIANO-N-{(2R)-2-[4-(2,3-DIHIDRO-BENZO[1,4]DIOXIN-5-IL)-PIPERAZIN-1-IL]-PROPIL}-N-PIRIDIN-2-IL-BENZAMIDA O DENOMINADO LECOZOTAN QUE SE ENCUENTRAN BAJO LA FORMA DE PARTICULAS, CON UN DIAMETRO NO MAYOR A 20 MICRONES Y ADEMAS COMPRENDE AL MENOS UN POLIMERO QUE CONTROLA LA VELOCIDAD DE LIBERACION TAL COMO METILCELULOSA; UN ACIDO ORGANICO TAL COMO ACIDO CITRICO O ACIDO ORGANICO POLIFUNCIONAL; UN RELLENADOR TAL COMO CELULOSA MICROCRISTALINA, LACTOSA, CARBONATOS, ENTRE OTROS Y UN LUBRICANTE. TAMBIEN SE REFIERE A UNA FORMA DE DOSIFICACION ORAL QUE LUEGO DE ADMINISTRAR AL PACIENTE ALCANZA UNA CONCENTRACION MAXIMA EN EL PLASMA (Cmax) Y UNA CONCENTRACION EN PLASMA DE 24 HORAS (C24) UNA RELACION MEDIA Cmax/C24 DESDE 5:1 HASTA 1,1:1. ESTOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE ALZHEIMERIT REFERS TO A PHARMACEUTICAL COMPOSITION INCLUDING DERIVATIVES OF {(2R) -2- [4- (2,3-DIHYDRO-BENZO [1,4] DIOXIN-5-IL) -PIPERAZIN-1-IL] -PROPIL} - N-PYRIDIN-2-IL AND METABOLITES, THE COMPOUND 4-CYANE-N - {(2R) -2- [4- (2,3-DIHYDRO-BENZO [1,4] DIOXIN-5-IL) being preferred. PIPERAZIN-1-IL] -PROPIL} -N-PYRIDIN-2-IL-BENZAMIDE OR SO-CALLED LECOZOTAN WHICH ARE FOUND IN THE FORM OF PARTICLES, WITH A DIAMETER NOT GREATER THAN 20 MICRONS AND ALSO INCLUDES AT LEAST ONE POLYMER THAT CONTROLS IT OF RELEASE SUCH AS METILCELLULOSE; AN ORGANIC ACID SUCH AS CITRIC ACID OR POLYFUNCTIONAL ORGANIC ACID; A FILLER SUCH AS MICROCRYSTALLINE CELLULOSE, LACTOSE, CARBONATES, AMONG OTHERS AND A LUBRICANT. IT ALSO REFERS TO AN ORAL DOSAGE FORM THAT AFTER ADMINISTERING THE PATIENT REACHES A MAXIMUM CONCENTRATION IN PLASMA (Cmax) AND A CONCENTRATION IN PLASMA OF 24 HOURS (C24) AN AVERAGE RATIO Cmax / C24 FROM 5: 1 TO 1.1 :one. THESE COMPOUNDS ARE USEFUL IN THE TREATMENT OF ALZHEIMER'S DISEASE

PE2006001076A 2005-09-09 2006-09-06 COMPOSITIONS AND PHARMACEUTICAL DOSAGE FORMS INCLUDED BY LECOZOTAN PE20070334A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US71541705P 2005-09-09 2005-09-09

Publications (1)

Publication Number Publication Date
PE20070334A1 true PE20070334A1 (en) 2007-05-08

Family

ID=37836444

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006001076A PE20070334A1 (en) 2005-09-09 2006-09-06 COMPOSITIONS AND PHARMACEUTICAL DOSAGE FORMS INCLUDED BY LECOZOTAN

Country Status (17)

Country Link
EP (1) EP1928863A2 (en)
JP (1) JP2009507850A (en)
KR (1) KR20080043855A (en)
CN (1) CN101258146A (en)
AR (1) AR058033A1 (en)
AU (1) AU2006287543A1 (en)
BR (1) BRPI0615771A2 (en)
CA (1) CA2620491A1 (en)
CR (1) CR9800A (en)
EC (1) ECSP088236A (en)
GT (1) GT200600403A (en)
IL (1) IL189827A0 (en)
NO (1) NO20081100L (en)
PE (1) PE20070334A1 (en)
RU (1) RU2008108216A (en)
TW (1) TW200800198A (en)
WO (1) WO2007030589A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8134029B2 (en) 2002-09-16 2012-03-13 Sunovion Pharmaceuticals Inc. Treatment of CNS disorders with trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine
EP1904066B1 (en) 2005-07-06 2018-05-23 Sunovion Pharmaceuticals Inc. COMBINATIONS OF ESZOPICLONE AND TRANS 4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-N-METHYL-1-NAPTHALENAMINE OR TRANS 4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-1-NAPTHALENAMINE, for treating MENOPAUSE, perimenopause AND COGNITIVE DISORDERS
JP2012526832A (en) * 2009-05-13 2012-11-01 スノビオン プハルマセウトイカルス インコーポレイテッド Composition comprising transnorsertraline and serotonin receptor 1A agonist / antagonist and use thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1466451B (en) * 2000-09-29 2010-05-12 索尔瓦药物有限公司 Ion-strength independent sustained release pharmacetuical formulation
GB2407498B (en) * 2003-10-30 2008-06-11 Cipla Ltd Oral formulations for 5-HT receptor agonists with reduced degradation of active ingredient
US20050215561A1 (en) * 2004-03-19 2005-09-29 Krishnendu Ghosh Pharmaceutical dosage forms and compositions
AU2006218845A1 (en) * 2005-03-01 2006-09-08 Wyeth Crystalline and amorphous 4-cyano-N{(2R)-2-(4-(2,3-dihydro-benzo(1,4)dioxin-5-yl)-piperazin-1-yl)-propyl}-N-pyridin-2-yl-benzamide hydrochloride

Also Published As

Publication number Publication date
IL189827A0 (en) 2008-11-03
EP1928863A2 (en) 2008-06-11
CR9800A (en) 2008-04-28
AR058033A1 (en) 2008-01-23
WO2007030589A3 (en) 2007-11-01
KR20080043855A (en) 2008-05-19
NO20081100L (en) 2008-06-03
ECSP088236A (en) 2008-04-28
JP2009507850A (en) 2009-02-26
GT200600403A (en) 2007-09-19
AU2006287543A1 (en) 2007-03-15
TW200800198A (en) 2008-01-01
CA2620491A1 (en) 2007-03-15
RU2008108216A (en) 2009-10-20
CN101258146A (en) 2008-09-03
BRPI0615771A2 (en) 2011-05-24
WO2007030589A2 (en) 2007-03-15

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