ME02765B - (z)-2-cijan0-3-hidroksi-but-2-enske kiseline (4'-trifluormetilfenil) -amid formulacije tableta sa poboljšanom stabilnošću - Google Patents

(z)-2-cijan0-3-hidroksi-but-2-enske kiseline (4'-trifluormetilfenil) -amid formulacije tableta sa poboljšanom stabilnošću

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Publication number
ME02765B
ME02765B MEP-2017-134A MEP13417A ME02765B ME 02765 B ME02765 B ME 02765B ME P13417 A MEP13417 A ME P13417A ME 02765 B ME02765 B ME 02765B
Authority
ME
Montenegro
Prior art keywords
pharmaceutical composition
solid pharmaceutical
weight
composition according
sodium
Prior art date
Application number
MEP-2017-134A
Other languages
German (de)
English (en)
French (fr)
Inventor
Gerrit Hauck
Original Assignee
Sanofi Sa
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41510564&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME02765(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of ME02765B publication Critical patent/ME02765B/me

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/01Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/32Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
    • C07C255/42Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
    • C07C255/44Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms at least one of the singly-bound nitrogen atoms being acylated
    • 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
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/275Nitriles; Isonitriles
    • A61K31/277Nitriles; Isonitriles having a ring, e.g. verapamil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • 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
    • 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
    • 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
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Otolaryngology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Inorganic Chemistry (AREA)
  • Nutrition Science (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (13)

1. Čvrsta farmaceutska kompozicija koja se u osnovi sastoji od a) 1 % do 30 % težina: težine Teriflunomida, ili farmaceutski prihvatljive bazne adicione soli, b) 5 % do 20 % težina: težine rastvarača, c) 0 % do 40 % težina: težine veziva, d) 0.1 % do 2 % težina: težine lubrikanta i e) ostalog procenta razblaživača, omogućava takvu farmaceutsku kompoziciju koja ne sadrži silicijum dioksid.
2.Čvrsta farmaceutska kompozicija prema patentnom zahtevu 1 gde se navedeni rastvarač bira iz grupe koja se sastoji od karboksimetilceluloze, nisko suspstituisane hidroksipropil celuloze, microkristalinske celuloze, celuloze u prahu, natrijum kroskarmelze, metil celuloze, polakrilin kalijuma, natrijum alginata, natrijum skrob glikolata ili mešavine jednog ili više pomenutih rastvarača.
3.Čvrsta farmaceutska kompozicija prema patentnom zahtevu 2 gde se navedeni rastvarač bira iz grupe koja se sastoji od nisko suspstituisane hidroksipropil celuloze, mikrokristalinske celuloze, celuloze u prahu, natrijum kroskarmelze, natrijum skrob glikolata ili mešavine jednog ili više pomeutih rastvarača.
4.Čvrsta farmaceutska kompozicija prema patentnom zahtevu 1 gde se navedeno vezivo bira iz grupe koja se sastoji od akacije, carboksimetilceluloze, hidroksiethilceluloze, hidroksipropilceluloze, dekstrina, želatina, guar gume, hidroksipropil metilceluloze, maltodekstrina, metilceluloze, natrijum alginata, preželatiniziranog skroba, skroba krompira, skroba kukuruza ili skroba žitarica i zejna ili mešavine jednog ili više pomenutih veziva.
5.Čvrsta farmaceutska kompozicija prema patentnom zahtevu 4 gde se vezivo bira iz grupe koja se sastoji od hidroksipropilceluloze, hidroksipropil metilceluloze, preželatiniziranog skroba, skroba krompira, skroba kukuruza ili skroba žitarica ili mešavine jednog ili više pomenutih veziva.
6.Čvrsta farmaceutska kompozicija prema patentnom zahtevu 1 gde se navedeni lubrikant bira iz grupe koja se sastoji od kalcijum stearata, gliceril palmitostearata, natrijum benzoata, natrijum lauril sulfata, natrijum stearil fumarata, stearinske kiseline, talka, zink stearata i magnezijum stearata ili mešavine jednog ili više pomenutih lubrikanata.
7.Čvrsta farmaceutska kompozicija prema patentnom zahtevu 6 gde se navedeni lubrikant bira iz grupe koja se sastoji od natrijum stearil fumarata i magnezijum stearata ili mešavine jednog ili više pomenutih lubrikanata.
8.Čvrsta farmaceutska kompozicija prema patentnom zahtevu 1 gde se navedeni razblaživači biraju iz grupe koja se sastoji od celuloze, celuloza acetata, dekstrata, dekstrina, dekstroze, fruktoze, 1-O-α-D-Glucopiranozil-D-manitola, gliceril palmitostearata, hidrogenizovanog ulja povrća, kaolina, laktitola, laktoze, lactoza mono-hidrata, maltitola, manitola, maltodekstrina, maltoze, preželatiniziranog skroba, natrijum hlorida, sorbitola, skroba, saharoze, talka and ksilitola ili mešavine jednog ili više navedenig razblaživača.
9.Čvrsta farmaceutska kompozicija prema patentnom zahtevu 8 gde se navedeni razblaživači biraju iz grupe koja se sastoji od laktoze, lactoza mono-hidrata, manitola i skrobova ili mešavine jednog ili više navedenog razblaživača.
10.Čvrsta farmaceutska kompozicija prema bilo kom od prethodnih patentnih zahteva u kom je kompozicija obložena.
11.Čvrsta farmaceutska kompozicija prema patentnom zahtevu 10, koja je tableta ili pilula sa omotačem na bazi hidromeloze. .
12.Čvrsta farmaceutska kompozicija prema bilo kom od prethodnih patentnih zahteva koja se u osnovi sastoji od: (a) 2 % do 15 % težina: težine Teriflunomida (b) 7 % do 15 % težina: težine rastvarača selektovanog od jednog ili vise od mikrokristalinske celuloze ili natrijum skrob glikolata, (c) 15 % do 35 % težina: težine veziva selektovanog od jednog ili vise od hidroksipropilceluloze ili skroba kukuruza, (d) 0.1 % do 1.0 % težina: težine lubrikanta selektovanog od magnezijum stearata i, (e) ostalog procenta razblaživača selektovanih od mono-hidrata.
13.Čvrsta farmaceutska kompozicija prema patentnim zahtevima 1 do 12 za korišćenje u tretmanu sepse, alergija, reakcija graft protiv domaćina, rekacija domaćin protiv grafta, reumatoidnog artritisa, sistemskog lupusa eritematodusa, multiple skleroze, psorijaze, astme, urtikarija, ritinisa, uveitisa, karcinoma pluća, leukemija, kacinoma jajnika, sarkoma, Karpošijevog sarkoma, meningeoma, karcinoma creva, karcinoma limfnih čvorova, tumora mozga, karcinoma dojke, karcinoma pankreasa, karcinoma prostate i karcinoma kože.   3
MEP-2017-134A 2009-09-18 2010-09-14 (z)-2-cijan0-3-hidroksi-but-2-enske kiseline (4'-trifluormetilfenil) -amid formulacije tableta sa poboljšanom stabilnošću ME02765B (me)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP09290716 2009-09-18
US36338210P 2010-07-12 2010-07-12
EP10752585.9A EP2477611B1 (en) 2009-09-18 2010-09-14 (z)-2-cyano-3-hydroxy-but-2-enoic acid-(4'-trifluormethylphenyl)-amide tablet formulations with improved stability
PCT/EP2010/063439 WO2011032929A1 (en) 2009-09-18 2010-09-14 (z)-2-cyano-3-hydroxy-but-2-enoic acid-(4'-trifluormethylphenyl)-amide tablet formulations with improved stability

Publications (1)

Publication Number Publication Date
ME02765B true ME02765B (me) 2018-01-20

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ID=41510564

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2017-134A ME02765B (me) 2009-09-18 2010-09-14 (z)-2-cijan0-3-hidroksi-but-2-enske kiseline (4'-trifluormetilfenil) -amid formulacije tableta sa poboljšanom stabilnošću

Country Status (42)

Country Link
US (5) US20120172427A1 (me)
EP (1) EP2477611B1 (me)
JP (1) JP2013505213A (me)
KR (1) KR101547880B1 (me)
CN (4) CN104666272A (me)
AR (1) AR078383A1 (me)
AU (2) AU2010297357B2 (me)
BR (1) BR112012006184B1 (me)
CA (1) CA2772275A1 (me)
CL (1) CL2015000047A1 (me)
CO (1) CO6511244A2 (me)
CR (2) CR20170078A (me)
CY (1) CY1119364T1 (me)
DK (1) DK2477611T3 (me)
DO (1) DOP2012000070A (me)
ES (1) ES2625731T3 (me)
GT (1) GT201200075A (me)
HK (1) HK1206244A1 (me)
HN (1) HN2012000576A (me)
HR (1) HRP20170904T1 (me)
HU (1) HUE032963T2 (me)
IL (3) IL218492A (me)
JO (1) JO3327B1 (me)
LT (1) LT2477611T (me)
MA (1) MA33585B1 (me)
ME (1) ME02765B (me)
MX (1) MX336663B (me)
MY (1) MY155613A (me)
NZ (2) NZ617025A (me)
PE (2) PE20121478A1 (me)
PL (1) PL2477611T3 (me)
PT (1) PT2477611T (me)
PY (1) PY1038455A (me)
RS (1) RS56074B1 (me)
RU (2) RU2681079C2 (me)
SI (1) SI2477611T1 (me)
SM (1) SMT201700299T1 (me)
TN (1) TN2012000061A1 (me)
TW (2) TWI468190B (me)
UA (2) UA107582C2 (me)
UY (1) UY32889A (me)
WO (1) WO2011032929A1 (me)

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