HRP20170555T1 - Metilfenidatni prolijekovi, postupci za njihovo dobivanje i njihova primjena - Google Patents

Metilfenidatni prolijekovi, postupci za njihovo dobivanje i njihova primjena Download PDF

Info

Publication number
HRP20170555T1
HRP20170555T1 HRP20170555TT HRP20170555T HRP20170555T1 HR P20170555 T1 HRP20170555 T1 HR P20170555T1 HR P20170555T T HRP20170555T T HR P20170555TT HR P20170555 T HRP20170555 T HR P20170555T HR P20170555 T1 HRP20170555 T1 HR P20170555T1
Authority
HR
Croatia
Prior art keywords
disorder
group
composition according
amino acid
image
Prior art date
Application number
HRP20170555TT
Other languages
English (en)
Inventor
Sven Guenther
Guochen Chi
Bindu Bera
Travis Mickle
Sanjib Bera
Original Assignee
Kempharm, Inc.
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 Kempharm, Inc. filed Critical Kempharm, Inc.
Publication of HRP20170555T1 publication Critical patent/HRP20170555T1/hr

Links

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
    • A61K31/4458—Non condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/548—Phosphates or phosphonates, e.g. bone-seeking
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/59—Hydrogenated pyridine rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Genetics & Genomics (AREA)
  • Psychiatry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Nutrition Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Physiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Toxicology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Addiction (AREA)
  • Anesthesiology (AREA)

Claims (9)

1. Kompozicija koja sadrži najmanje jedan konjugat metilfenidata koji ima strukturu: [image] pri tome X je O; Y je odabrano iz skupine koja se sastoji od O i N; L je odabrano iz skupine koja se sastoji od: [image] pri tome je q = 1-6, [image] i G je derivat karboksipiridina koji je vezan preko amidne veze za G2, pri tome je G kovalentno vezan za L preko njegovog tercijarnog dušika i pri čemu je G2 aminokiselina odabrana iz skupine koja se sastoji od standardne aminokiseline, nestandardne aminokiseline i sintetske aminokiseline.
2. Kompozicija sukladno zahtjevu 1, pri tome je karboksipiridin odabran iz skupine koja se sastoji od nikotinske kiseline, izonikotinske kiseline, i pikolinske kiseline.
3. Kompozicija sukladno zahtjevu 1 ili 2, pri tome je aminokiselina odabrana iz skupine koja se sastoji od alanina, arginina, asparagina, asparaginske kiseline, cisteina, glutaminske kiseline, glutamina, glicina, histidina, izoleucina, leucina, lizina, metionina, fenilalanina, prolina, pirolizina, selenocisteina, serina, treonina, triptofana, tirozina i valina.
4. Kompozicija sukladan bilo kojem od zahtjeva 1-3, pri tome je konjugat u obliku farmaceutski prihvatljive anionskih, amfoterni, cviterionski ili kationski oblik soli ili smjese njihovih soli.
5. Kompozicija sukladno zahtjevu 4, pri tome je oblik anionske soli odabran iz skupine koja se sastoji od acetata, l-aspartata, bezilata, bikarbonata, karbonata, d-kamzilata, l-kamzilata, citrata, edizilata, formata, fumarata, glukonata, hidro-bromida/bromida, hidroklorida/klorida, d-laktata, l-laktata, d,l-laktata, d,l-malata, l-malata, mezilata, pamoata, fosfata, sukcinata, sulfata, bisulfata, d-tartrata, l-tartrata, d,l-tartrata, mezo-tartrata, benzoata, gluceptata, d-glukuronata, hibenzata, izetionata, malonata, metilsulfata, 2-napzilata, nikotinata, nitrata, orotata, stearata, tozilata, tiocijanata, acefilinata, aceturata, aminosalicilata, askorbata, borata, butirata, kamforata, kamfokarbonata, dekanoata, heksanoata, holata, cipionata, dihloroacetata, edentata, etil sulfata, furata, fuzidata, galaktarata, galakturonata, galata, gentizata, glutamata, glutarata, glicerofosfata, heptanoata, hidroksibenzoata, hipurata, fenilpropionata, jodida, ksinafoata, laktobionata, laurata, maleata, mandelata, metansufonata, miristata, napadizilata, oleata, oksalata, palmitata, pikrata, pivalata, propionata, pirofosfata, salicilata, salicilsulfata, sulfosalicilata, tanata, tereftalata, tiosalicilata, tribrofenata, valerata, valproata, adipata, 4-acetamidobenzoata, kamzilata, oktanoata, estolata, ezilata, glikolata, tiocijanata, i undecilenata.
6. Kompozicija sukladno zahtjevu 4, pri tome je oblik kationske soli odabran iz skupine koja se sastoji od natrija, kalija, kalcija, magnezija, cinka, aluminija, litija, kolinata, lizinija, amonija i trometamina.
7. Kompozicija sukladno bilo kojem od zahtjeva 1-6, pri tome je kompozicija u obliku koji obuhvaća tabletu, kapsulu, pilule, dražeje, pastile, oralni prašak, otopina, tanke trake, oralni tanki film (OTF), oralnu traku, rektalni film, transdermalni flaster, sirup, suspenziju, spoj za inhalaciju ili čepići.
8. Kompozicija sukladno zahtjevu 1, pri tome je konjugat odabran iz skupine koja se sastoji od: [image] [image]
9. Kompozicija sukladno bilo kojem od zahtjeva 1-8 za primjenu u metodi liječenja pacijenta koji boluje od bolesti, poremećaja ili stanja koje se bira iz skupine koju čine hiperaktivnosti s poremećajima pažnje, poremećaja pomankanja pažnje, autističnog spektra poremećaja, autizma, Aspergerovog poremećaja, pervazivnog razvojnog poremećaja, poremećaja spavanja, pretilosti, depresije, bipolarnog poremećaja, poremećaja hranjenja, sindroma kroničnog umora, shizofrenije, velikog depresivnog poremećaja, narkolepsije, sindroma posturalne ortostatske tahikardije, letargije, i neuralnog inzulta, obuhvaća oralno davanje pacijentu farmaceutski učinkovite količine pripravka.
HRP20170555TT 2011-07-28 2017-04-05 Metilfenidatni prolijekovi, postupci za njihovo dobivanje i njihova primjena HRP20170555T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161512658P 2011-07-28 2011-07-28
EP12817423.2A EP2736510B1 (en) 2011-07-28 2012-07-27 Methylphenidate-prodrugs, processes of making and using the same
PCT/US2012/048641 WO2013016668A2 (en) 2011-07-28 2012-07-27 Methylphenidate-prodrugs, processes of making and using the same

Publications (1)

Publication Number Publication Date
HRP20170555T1 true HRP20170555T1 (hr) 2017-06-16

Family

ID=47601775

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20170555TT HRP20170555T1 (hr) 2011-07-28 2017-04-05 Metilfenidatni prolijekovi, postupci za njihovo dobivanje i njihova primjena

Country Status (28)

Country Link
US (4) US9079928B2 (hr)
EP (2) EP3189840B1 (hr)
JP (4) JP5976111B2 (hr)
KR (5) KR101616111B1 (hr)
CN (2) CN107261148B (hr)
AR (1) AR087390A1 (hr)
AU (1) AU2012286683C1 (hr)
BR (1) BR112014002084B1 (hr)
CA (3) CA2984544C (hr)
CL (1) CL2014000210A1 (hr)
CO (1) CO6900135A2 (hr)
DK (1) DK2736510T3 (hr)
ES (2) ES2621306T3 (hr)
HR (1) HRP20170555T1 (hr)
HU (1) HUE032113T2 (hr)
IL (5) IL230650A (hr)
LT (1) LT2736510T (hr)
MX (3) MX362571B (hr)
MY (1) MY162499A (hr)
PL (1) PL2736510T3 (hr)
PT (1) PT2736510T (hr)
RS (1) RS55812B1 (hr)
RU (1) RU2573835C2 (hr)
SG (1) SG10201606225XA (hr)
SI (1) SI2736510T1 (hr)
UA (1) UA112654C2 (hr)
WO (1) WO2013016668A2 (hr)
ZA (1) ZA201308766B (hr)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101616111B1 (ko) 2011-07-28 2016-04-27 켐팜 인코포레이티드 메틸페니데이트 프로드러그, 이의 제조 방법 및 사용 방법
ES2715562T3 (es) * 2011-12-15 2019-06-04 Alkermes Pharma Ireland Ltd Profármacos de compuestos de amina secundaria
US9556156B2 (en) * 2012-10-05 2017-01-31 Sphaera Pharma Pte Ltd. Compounds, their synthesis and their uses
WO2015001499A2 (en) * 2013-07-04 2015-01-08 Mahesh Kandula Compositions and methods for the treatment of irritable bowel syndrome and the associated abdominal cramping
CN104418797B (zh) * 2013-08-26 2019-04-19 上海医药集团股份有限公司 哌甲酯、右哌甲酯的制备方法、其中间体及制备方法
US20170056352A1 (en) 2015-08-25 2017-03-02 Rgenix, Inc. PHARMACEUTICALLY ACCEPTABLE SALTS OF beta-GUANIDINOPROPIONIC ACID WITH IMPROVED PROPERTIES AND USES THEREOF
WO2017048720A1 (en) * 2015-09-15 2017-03-23 Praxis Biosciences, Llc Prodrugs of fencamfamine
CA3041058A1 (en) 2016-10-31 2018-05-03 Biocryst Pharmaceuticals, Inc. Carbamimidoylphenylcarbamoyl derivatives and pharmaceutical compositions thereof useful as kallikrein inhibithors
NZ754751A (en) * 2016-12-11 2022-05-27 Kempharm Inc Compositions comprising methylphenidate-prodrugs, processes of making and using the same
WO2018107131A1 (en) * 2016-12-11 2018-06-14 Kempharm, Inc. Methylphenidate-prodrugs, processes of making and using the same
WO2018160178A1 (en) 2017-03-01 2018-09-07 Rgenix, Inc. Pharmaceutically acceptable salts of b-guanidinopropionic acid with improved properties and uses thereof
US20200114014A1 (en) * 2017-04-11 2020-04-16 John K. Thottathil Novel Alpha-Hydroxy Carboxylic Acid and Derivatives and Other GRAS-Based Amide and Imide Prodrugs of Amphetamine Compounds and Uses Thereof
US11975039B2 (en) 2018-05-10 2024-05-07 Helixmith Co., Ltd. Herbal composition for treatment of attention deficit hyperactivity disorder
JPWO2020067507A1 (ja) * 2018-09-28 2021-08-30 生化学工業株式会社 第１級アミン化合物又は第２級アミン化合物−酸性多糖コンジュゲートとその製造方法
US11174229B2 (en) * 2018-10-29 2021-11-16 Kempharm, Inc. D-amphetamine compounds, compositions, and processes for making and using the same
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4428935A (en) * 1982-05-24 1984-01-31 Pfizer Inc. Penicillanic acid dioxide prodrug
US6210705B1 (en) * 1997-12-15 2001-04-03 Noven Pharmaceuticals, Nc. Compositions and methods for treatment of attention deficit disorder and attention deficit/hyperactivity disorder with methylphenidate
WO1999036403A1 (en) * 1998-01-13 1999-07-22 The Trustees Of The University Of Pennsylvania Novel dopamine re-uptake inhibitors and methods of synthesizing and using the same
US7060708B2 (en) * 1999-03-10 2006-06-13 New River Pharmaceuticals Inc. Active agent delivery systems and methods for protecting and administering active agents
WO2001054481A2 (en) * 2000-01-28 2001-08-02 Rohm And Haas Company Enhanced propertied pharmaceuticals
JP2004507503A (ja) * 2000-08-28 2004-03-11 センション，インコーポレイテッド 記憶を増強するためのトレオ−メチルフェニデートの使用
US20020132793A1 (en) * 2000-08-28 2002-09-19 Mel Epstein Use of methylphenidate compounds to enhance memory
US7700561B2 (en) 2002-02-22 2010-04-20 Shire Llc Abuse-resistant amphetamine prodrugs
WO2004080959A2 (en) * 2003-03-07 2004-09-23 Isp Investments Inc. Process for the preparation of dexmethylphenidate hydrochloride
FI120187B (fi) * 2003-03-14 2009-07-31 Outotec Oyj Menetelmä prosessin säätämiseksi
WO2006047330A2 (en) 2004-10-22 2006-05-04 Mark Froimowitz Methylphenidate analogs and methods of use thereof
EP1928881A2 (en) 2005-08-19 2008-06-11 Pharmacofore, Inc. Prodrugs of active agents
KR20090086627A (ko) * 2006-12-05 2009-08-13 노이로제스엑스, 인코포레이티드 프로드러그 및 그것의 제조 및 사용 방법
EP2101571B1 (en) * 2006-12-11 2011-05-18 Kempharm, Inc. Ornithine conjugates of amphetamine and processes for making and using the same
CN101631770A (zh) * 2007-02-02 2010-01-20 科露西德医药品公司 抑制胆碱酯酶的化合物
MX2009008288A (es) * 2007-02-02 2009-12-01 Colucid Pharmaceuticals Inc Compuestos que inhiben la colinesterasa.
AU2008213643A1 (en) * 2007-02-08 2008-08-14 Kempharm, Inc. Polar hydrophilic prodrugs of amphetamine and other stimulants and processes for making and using the same
CN101631768A (zh) * 2007-03-15 2010-01-20 太阳医药高级研究有限公司 新型前药
DK2152690T3 (da) * 2007-05-23 2012-05-07 Merck Sharp & Dohme Pyridylpiperidinorexin-receptorantagonister
EP2182938A2 (en) * 2007-07-18 2010-05-12 Colucid Pharmaceuticals, Inc. Methods for promoting wakefulness
WO2009035473A2 (en) 2007-09-13 2009-03-19 Sanfilippo Louis C Method of treating binge eating disorder, obesity resulting from binge eating behavior and depressive disorders
KR101616111B1 (ko) * 2011-07-28 2016-04-27 켐팜 인코포레이티드 메틸페니데이트 프로드러그, 이의 제조 방법 및 사용 방법
ES2715562T3 (es) 2011-12-15 2019-06-04 Alkermes Pharma Ireland Ltd Profármacos de compuestos de amina secundaria

Also Published As

Publication number Publication date
CA2837732C (en) 2018-03-20
KR20180069934A (ko) 2018-06-25
AU2012286683B2 (en) 2015-12-17
ES2621306T3 (es) 2017-07-03
MX2013015088A (es) 2014-02-11
CA2984544C (en) 2021-08-31
CA2984544A1 (en) 2013-01-31
AR087390A1 (es) 2014-03-19
CN103826633B (zh) 2017-05-24
EP2736510B1 (en) 2017-03-01
JP6272403B2 (ja) 2018-01-31
EP2736510A4 (en) 2015-02-25
JP6731090B2 (ja) 2020-07-29
IL269322A (en) 2019-11-28
JP5976111B2 (ja) 2016-08-23
JP2018076359A (ja) 2018-05-17
IL230650A0 (en) 2014-03-31
UA112654C2 (uk) 2016-10-10
RU2573835C2 (ru) 2016-01-27
US9079928B2 (en) 2015-07-14
JP6505822B2 (ja) 2019-04-24
KR101616111B1 (ko) 2016-04-27
US20150266911A1 (en) 2015-09-24
SG10201606225XA (en) 2016-09-29
KR101869885B1 (ko) 2018-06-25
IL254143A0 (en) 2017-10-31
KR20190085183A (ko) 2019-07-17
JP2014521656A (ja) 2014-08-28
US9453037B2 (en) 2016-09-27
US20140243291A1 (en) 2014-08-28
MX341416B (es) 2016-08-19
IL269322B (en) 2020-05-31
CN107261148B (zh) 2021-07-13
ES2883259T3 (es) 2021-12-07
CL2014000210A1 (es) 2014-09-26
PL2736510T3 (pl) 2017-07-31
CN107261148A (zh) 2017-10-20
KR20140081761A (ko) 2014-07-01
US10231960B2 (en) 2019-03-19
EP3189840A1 (en) 2017-07-12
CA2837732A1 (en) 2013-01-31
RU2014107678A (ru) 2015-09-10
KR20190085184A (ko) 2019-07-17
US20190142815A1 (en) 2019-05-16
BR112014002084A2 (pt) 2017-06-13
WO2013016668A3 (en) 2013-03-21
AU2012286683C1 (en) 2016-04-21
WO2013016668A2 (en) 2013-01-31
RS55812B1 (sr) 2017-08-31
CO6900135A2 (es) 2014-03-20
PT2736510T (pt) 2017-04-05
CN103826633A (zh) 2014-05-28
NZ618113A (en) 2015-06-26
MX2019001093A (es) 2019-07-04
ZA201308766B (en) 2015-02-25
KR20160047599A (ko) 2016-05-02
IL262493B (en) 2019-10-31
SI2736510T1 (sl) 2017-05-31
JP2016222692A (ja) 2016-12-28
DK2736510T3 (en) 2017-04-24
IL254143B (en) 2018-11-29
BR112014002084B1 (pt) 2022-03-29
US20170049765A1 (en) 2017-02-23
IL246503A (en) 2017-09-28
IL262493A (en) 2018-12-31
MY162499A (en) 2017-06-15
LT2736510T (lt) 2017-04-25
MX362571B (es) 2019-01-25
IL230650A (en) 2016-12-29
CA3123900A1 (en) 2013-01-31
HUE032113T2 (en) 2017-09-28
EP3189840B1 (en) 2021-05-19
EP2736510A2 (en) 2014-06-04
JP2019112462A (ja) 2019-07-11

Similar Documents

Publication Publication Date Title
HRP20170555T1 (hr) Metilfenidatni prolijekovi, postupci za njihovo dobivanje i njihova primjena
HRP20210928T1 (hr) Soli ili ko-kristali 3- (3-dimetilamino-1-etil-2-metil-propil)-fenola
AU2021201705A1 (en) Ezh2 inhibitors for treating lymphoma
TW201538155A (zh) 活性成份輔助組成物及將活性成份化合物遞送給對象之方法
JP2013537195A5 (ja) 疾患を治療するための医薬品及び同医薬品を含むキット
US20140170086A1 (en) Method for Indicating Time for Washing or Indicating Delivery of Antibacterial Agent
PE20080937A1 (es) Sales de n-hidroxi-3-[4-[[[2-(2-metil-1h-indol-3-il)etil)amino]metil]fenil]-2e-2-propenamida
JP2013545745A5 (hr)
RU2015123740A (ru) Способ индикации времени для мытья или индикации высвобождения антибактериального средства
AR070357A1 (es) Producto para cuidado oral y metodos de uso y manufactura del mismo
JP2013503862A5 (hr)
RU2016135952A (ru) Композиции ингибитора дофа-декарбоксилазы
JP2011527333A5 (hr)
AR061295A1 (es) Procedimiento para hacer sales de n-hidroxi-3- [4-[ [ [ 2- ( 2-metil-1h-indol-3-il) etil] amino] metil] fenil] -2e-2-propenamida
JP2013506004A5 (hr)
US20220000814A1 (en) Methods for treatment of prader-willi syndrome
ES2536402T3 (es) Sales estables de S-adenosilmetionina y procedimiento para la preparación de las mismas
JP2009515953A5 (hr)
CN102796046A (zh) 2–(4-羟基)苯甲酰氨基酸-4,4,5,5-四甲基-1,3-二氧基咪唑啉及其制备方法和应用
JP2007501817A5 (hr)
JPWO2006001251A1 (ja) アトルバスタチン外用剤組成物
AU2017279760A1 (en) Drug substance preparations, pharmaceutical compositions and dosage forms comprising S-(+)-flurbiprofen
JPWO2019150341A5 (hr)
RU2014118122A (ru) Производное бутилфталида, способ его получения и применение
BR112015000107B1 (pt) Método e preparação absorvível por via transdérmica contendo rotigotina, prevenção da cristalização de rotigotina e sistema terapêutico transdérmico