BR112015016889A8 - derivados de catecolamina enriquecidos com deutério em posição específica - Google Patents

derivados de catecolamina enriquecidos com deutério em posição específica

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Publication number
BR112015016889A8
BR112015016889A8 BR112015016889A BR112015016889A BR112015016889A8 BR 112015016889 A8 BR112015016889 A8 BR 112015016889A8 BR 112015016889 A BR112015016889 A BR 112015016889A BR 112015016889 A BR112015016889 A BR 112015016889A BR 112015016889 A8 BR112015016889 A8 BR 112015016889A8
Authority
BR
Brazil
Prior art keywords
deuterium
compounds
deuterated
enrichment
catecholamine derivatives
Prior art date
Application number
BR112015016889A
Other languages
English (en)
Other versions
BR112015016889A2 (pt
Inventor
Schneider Frank
Alken Rudolf-Giesbert
Original Assignee
Imphar 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.)
Filing date
Publication date
Application filed by Imphar Ag filed Critical Imphar Ag
Publication of BR112015016889A2 publication Critical patent/BR112015016889A2/pt
Publication of BR112015016889A8 publication Critical patent/BR112015016889A8/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C229/36—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2813—Inorganic compounds
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/2853—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/16—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

resumo patente de invenção: "derivados de catecolamina enriquecidos com deutério em posição específica assimétrica e medicamentos compreendendo os referidos compostos". a presente invenção refere-se a derivados de catecolamina deuterados da fórmula geral (i), em que r1 é deutério, r2 e r3 são selecionados independentemente a partir de hidrogênio e deutério e em que pelo menos um de r2 e r3 tem um enriquecimento de deutério na gama de 0,02% em mol a 100% em mol de deutério, e em que o enriquecimento de deutério de r2 e r3 é diferente um do outro e em que a diferença entre o enriquecimento de deutério de r2 e r3 é de pelo menos 5 pontos percentuais, r4 é hidrogênio, deutério, c1 a c6-alquila ou c5 a c6-cicloalquila, c1 a c6-alquila ou c5 a c6-cicloalquila deuterado, ou um grupo que é facilmente hidroliticamente ou enzimaticamente clivável sob condições fisiológicas, bem como seus sais fisiologicamente aceitáveis e os seus estereoisômeros, enantiômeros ou diastereômeros sob forma opticamente pura. os compostos podem ser facilmente preparados por mistura de compostos deuterados e não deuterados em uma razão predefinida. os compostos apresentam efeito anti-parkinson em doses mais baixas e apresentam efeitos colaterais mais baixos.
BR112015016889A 2013-02-05 2014-02-05 derivados de catecolamina enriquecidos com deutério em posição específica BR112015016889A8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361760738P 2013-02-05 2013-02-05
EP13182708 2013-09-02
PCT/EP2014/052267 WO2014122184A1 (en) 2013-02-05 2014-02-05 Position-specific asymmetric deuterium enriched catecholamine derivatives and medicaments comprising said compounds

Publications (2)

Publication Number Publication Date
BR112015016889A2 BR112015016889A2 (pt) 2017-07-11
BR112015016889A8 true BR112015016889A8 (pt) 2018-01-23

Family

ID=49084847

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015016889A BR112015016889A8 (pt) 2013-02-05 2014-02-05 derivados de catecolamina enriquecidos com deutério em posição específica

Country Status (14)

Country Link
US (2) US9567289B2 (pt)
EP (1) EP2953926B1 (pt)
JP (1) JP6704252B2 (pt)
KR (1) KR20150115807A (pt)
CN (1) CN104968643B (pt)
AU (2) AU2014214055A1 (pt)
BR (1) BR112015016889A8 (pt)
CA (1) CA2897132C (pt)
EA (1) EA028931B1 (pt)
ES (1) ES2901752T3 (pt)
HK (2) HK1214241A1 (pt)
IL (2) IL239733A0 (pt)
MX (1) MX370884B (pt)
WO (1) WO2014122184A1 (pt)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2918266A1 (en) 2014-03-11 2015-09-16 CDRD Berolina AB Composition comprising a dopamine agonist and an L-DOPA derivative for treating Parkinson's disease
MX2018004339A (es) * 2015-10-09 2019-04-15 Teva Pharmaceuticals Int Gmbh Combinación de levodopa deuterado con carbidopa y opicapona para el tratamiento del mal de parkinson.
ES2942468T3 (es) * 2018-10-18 2023-06-01 Oncopeptides Ab Compuestos que contienen deuterio
JP7471298B2 (ja) * 2018-12-06 2024-04-19 イントラビオ エルティーディー アセチル－ロイシンの重水素化類似体

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2049115C3 (de) 1970-10-06 1981-07-30 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai, Tokyo Verwendung von Calcium-5-butylpicolinat und/oder Calcium-5-pentylpicolinat bei der Bekämpfung des Parkinsonismus mit 3-(3,4-Dihydroxyphenyl)-L-alanin (L-Dopa)
DE10261807A1 (de) 2002-12-19 2004-07-01 Turicum Drug Development Ag Deuterierte Catecholaminderivate sowie diese Verbindungen enthaltende Arzneimittel
AU2007214622B2 (en) 2006-02-17 2012-02-23 Teva Pharmaceuticals International Gmbh Deuterated catecholamine derivatives and medicaments comprising said compounds
GB0904300D0 (en) * 2009-03-12 2009-04-22 Amarin Neuroscience Ltd Essential fatty acid compounds

Also Published As

Publication number Publication date
AU2014214055A1 (en) 2015-07-16
ES2901752T3 (es) 2022-03-23
MX370884B (es) 2020-01-09
US9567289B2 (en) 2017-02-14
EA201500739A1 (ru) 2015-11-30
IL239733A0 (en) 2015-08-31
EP2953926A1 (en) 2015-12-16
MX2015010087A (es) 2016-04-21
US20150376117A1 (en) 2015-12-31
BR112015016889A2 (pt) 2017-07-11
HK1214810A1 (zh) 2016-08-05
CN104968643B (zh) 2020-03-03
CA2897132A1 (en) 2014-08-14
KR20150115807A (ko) 2015-10-14
IL260018A (en) 2018-07-31
CN104968643A (zh) 2015-10-07
JP2016513084A (ja) 2016-05-12
WO2014122184A1 (en) 2014-08-14
AU2018247203A1 (en) 2018-11-01
CA2897132C (en) 2021-05-25
US20200163918A1 (en) 2020-05-28
HK1214241A1 (zh) 2016-07-22
JP6704252B2 (ja) 2020-06-03
EP2953926B1 (en) 2021-10-20
EA028931B1 (ru) 2018-01-31
IL260018B (en) 2020-01-30

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B25A Requested transfer of rights approved

Owner name: RATIOPHARM GMBH (DE)

B25A Requested transfer of rights approved

Owner name: TEVA PHARMACEUTICALS INTERNATIONAL GMBH (CH)

B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements