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1. WO2011002995 - PHENYLETHANOIC ACID, PHENYLPROPANOIC ACID AND PHENYLPROPENOIC ACID CONJUGATES AND PRODRUGS OF HYDROCODONE, METHODS OF MAKING AND USE THEREOF

Publication Number WO/2011/002995
Publication Date 06.01.2011
International Application No. PCT/US2010/040785
International Filing Date 01.07.2010
IPC
A01N 43/42 2006.01
AHUMAN NECESSITIES
01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
43Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
34having rings with one nitrogen atom as the only ring hetero atom
40six-membered rings
42condensed with carbocyclic rings
A61K 31/44 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
CPC
A61K 31/44
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
A61K 31/485
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
485Morphinan derivatives, e.g. morphine, codeine
A61K 47/542
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
542Carboxylic acids, e.g. a fatty acid or an amino acid
A61P 25/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
04Centrally acting analgesics, e.g. opioids
A61P 25/30
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
30for treating abuse or dependence
A61P 25/36
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
30for treating abuse or dependence
36Opioid-abuse
Applicants
  • KEMPHARM, INC. [US]/[US] (AllExceptUS)
  • MICKLE, Travis [US]/[US] (UsOnly)
  • GUENTHER, Sven [US]/[US] (UsOnly)
  • MICKLE, Christal [US]/[US] (UsOnly)
  • CHI, Guochen [CN]/[US] (UsOnly)
  • KANSKI, Jaroslaw [PL]/[US] (UsOnly)
  • MARTIN, Andrea, K. [US]/[US] (UsOnly)
  • BERA, Bindu [IN]/[US] (UsOnly)
Inventors
  • MICKLE, Travis
  • GUENTHER, Sven
  • MICKLE, Christal
  • CHI, Guochen
  • KANSKI, Jaroslaw
  • MARTIN, Andrea, K.
  • BERA, Bindu
Agents
  • O'CONNOR, Kevin, A.
Priority Data
61/222,73002.07.2009US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PHENYLETHANOIC ACID, PHENYLPROPANOIC ACID AND PHENYLPROPENOIC ACID CONJUGATES AND PRODRUGS OF HYDROCODONE, METHODS OF MAKING AND USE THEREOF
(FR) CONJUGUÉS D'ACIDE PHÉNYLÉTHANOÏQUE, D'ACIDE PHÉNYLPROPANOÏQUE ET D'ACIDE PHÉNYLPROPÉNOÏQUE ET PROMÉDICAMENTS D'HYDROCODONE, LEURS PROCÉDÉS DE FABRICATION ET D'UTILISATION
Abstract
(EN)
The presently described technology provides phenylethanoic acid, phenylpropanoic acid, phenylpropenoic acid, a salt thereof, a derivative thereof or a combination thereof chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs or compositions of hydrocodone which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.
(FR)
La présente invention concerne une technique de production d'acide phényléthanoïque, d'acide phénylpropanoïque, d'acide phénylpropénoïque, d'un sel de ceux-ci, d'un dérivé de ceux-ci ou d'une combinaison de ceux-ci chimiquement conjugués à de l'hydrocodone (morphinane-6-one, 4,5-alpha-époxy-3-méthoxy-17-méthyle) pour former de nouveaux promédicaments ou des compositions d'hydrocodone qui présentent un potentiel réduit d'abus d'hydrocodone. La présente technique comprend également des méthodes de traitement de patients, des trousses pharmaceutiques et des procédés de synthèse de conjugués
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