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1. WO2002026696 - CARBAMIC ACID COMPOUNDS COMPRISING AN AMIDE LINKAGE AS HDAC INHIBITORS

Publication Number WO/2002/026696
Publication Date 04.04.2002
International Application No. PCT/GB2001/004329
International Filing Date 27.09.2001
Chapter 2 Demand Filed 26.04.2002
IPC
A61K 31/16 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
A61K 31/195 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
A61K 31/198 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
197the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid (GABA), beta-alanine, epsilon-aminocaproic acid, pantothenic acid
198Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
A61K 31/277 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
275Nitriles; Isonitriles
277having a ring, e.g. verapamil
A61K 31/38 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
38having sulfur as a ring hetero atom
A61K 31/381 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
38having sulfur as a ring hetero atom
381having five-membered rings
CPC
A61K 31/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
A61K 31/195
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
A61K 31/198
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
197the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
198Alpha-aminoacids, e.g. alanine, edetic acids [EDTA],
A61K 31/277
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
275Nitriles; Isonitriles
277having a ring, e.g. verapamil
A61K 31/38
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
38having sulfur as a ring hetero atom
A61K 31/381
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
38having sulfur as a ring hetero atom
381having five-membered rings
Applicants
  • PROLIFIX LIMITED [GB]/[GB] (AllExceptUS)
  • WATKINS, Clare, J. [GB]/[GB] (UsOnly)
  • ROMERO-MARTIN, Maria-Rosario [ES]/[GB] (UsOnly)
  • MOORE, Kathryn, G. [GB]/[GB] (UsOnly)
  • RITCHIE, James [GB]/[GB] (UsOnly)
  • FINN, Paul, W. [GB]/[GB] (UsOnly)
  • KALVINSH, Ivars [LV]/[LV] (UsOnly)
  • LOZA, Einars [LV]/[LV] (UsOnly)
  • STARCHENKOV, Igor (UsOnly)
  • DIKOVSKA, Klara [LV]/[LV] (UsOnly)
  • BOKALDERE, Rasma, Melita [LV]/[LV] (UsOnly)
  • GAILITE, Vija [LV]/[LV] (UsOnly)
  • VORONA, Maxim [LV]/[LV] (UsOnly)
  • ANDRIANOV, Victor [--]/[LV] (UsOnly)
  • LOLYA, Daina [LV]/[LV] (UsOnly)
  • SEMENIKHINA, Valentina (UsOnly)
  • AMOLINS, Andris [LV]/[LV] (UsOnly)
  • HARRIS, C., John, [GB]/[GB] (UsOnly)
  • DUFFY, James, E., S. [GB]/[GB] (UsOnly)
Inventors
  • WATKINS, Clare, J.
  • ROMERO-MARTIN, Maria-Rosario
  • MOORE, Kathryn, G.
  • RITCHIE, James
  • FINN, Paul, W.
  • KALVINSH, Ivars
  • LOZA, Einars
  • STARCHENKOV, Igor
  • DIKOVSKA, Klara
  • BOKALDERE, Rasma, Melita
  • GAILITE, Vija
  • VORONA, Maxim
  • ANDRIANOV, Victor
  • LOLYA, Daina
  • SEMENIKHINA, Valentina
  • AMOLINS, Andris
  • HARRIS, C., John,
  • DUFFY, James, E., S.
Agents
  • ARMITAGE, Ian, M.
  • ADRIAN H. BRASNETT and others Mewburn Ellis
Priority Data
0023985.529.09.2000GB
60/297,78514.06.2001US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) CARBAMIC ACID COMPOUNDS COMPRISING AN AMIDE LINKAGE AS HDAC INHIBITORS
(FR) COMPOSES D'ACIDE CARBAMIQUE COMPRENANT UN ENCHAINEMENT AMIDE COMME INHIBITEURS HDAC
Abstract
(EN) This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: -NR1C(=O)- and -C(=O)NR1-; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.
(FR) L'invention concerne certains composés d'acide carbamique actifs inhibant l'activité HDAC et correspondant à la formule (1), dans laquelle A désigne un groupe aryle ; Q1 désigne un groupe leader aryle ayant un squelette d'au moins 2 atomes de carbone; J désigne un enchaînement amide choisi à partir de: -NR1C(=O)- et-C(=O)NR1-; R1 désigne un substituant amido; et Q2 désigne un groupe leader acide ; ainsi que les sels, solvates, amides, esters, éthers pharmaceutiquement acceptables, les formes protégés chimiquement et les promédicaments de ces composés. L'invention concerne en outre des compositions pharmaceutiques comprenant de tels composés, ainsi que l'utilisation de ces composés et de ces compositions, à la fois in vitro et in vivo, en vue d'inhiber HDAC et d'inhiber, par exemple, des états de proliférations tels que cancers et psoriasis.
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