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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
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
185
Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19
Carboxylic acids, e.g. valproic acid
195
having an amino group
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
185
Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19
Carboxylic acids, e.g. valproic acid
195
having an amino group
197
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, pantothenic acid
198
Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
275
Nitriles; Isonitriles
277
having a ring, e.g. verapamil
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
38
having sulfur as a ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
38
having sulfur as a ring hetero atom
381
having five-membered rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
426
1,3-Thiazoles
A61K 31/16 (2006.01)
A61K 31/195 (2006.01)
A61K 31/198 (2006.01)
A61K 31/277 (2006.01)
A61K 31/38 (2006.01)
A61K 31/381 (2006.01)
CPC
A61K 31/16
A61K 31/195
A61K 31/198
A61K 31/277
A61K 31/38
A61K 31/381
Applicants
  • PROLIFIX LIMITED [GB/GB]; 91 Milton Park Abingdon, Oxfordshire OX14 4RY, GB (AllExceptUS)
  • WATKINS, Clare, J. [GB/GB]; GB (UsOnly)
  • ROMERO-MARTIN, Maria-Rosario [ES/GB]; GB (UsOnly)
  • MOORE, Kathryn, G. [GB/GB]; GB (UsOnly)
  • RITCHIE, James [GB/GB]; GB (UsOnly)
  • FINN, Paul, W. [GB/GB]; GB (UsOnly)
  • KALVINSH, Ivars [LV/LV]; LV (UsOnly)
  • LOZA, Einars [LV/LV]; LV (UsOnly)
  • STARCHENKOV, Igor; LV (UsOnly)
  • DIKOVSKA, Klara [LV/LV]; LV (UsOnly)
  • BOKALDERE, Rasma, Melita [LV/LV]; LV (UsOnly)
  • GAILITE, Vija [LV/LV]; LV (UsOnly)
  • VORONA, Maxim [LV/LV]; LV (UsOnly)
  • ANDRIANOV, Victor [--/LV]; LV (UsOnly)
  • LOLYA, Daina [LV/LV]; LV (UsOnly)
  • SEMENIKHINA, Valentina; LV (UsOnly)
  • AMOLINS, Andris [LV/LV]; LV (UsOnly)
  • HARRIS, C., John, [GB/GB]; GB (UsOnly)
  • DUFFY, James, E., S. [GB/GB]; GB (UsOnly)
Inventors
  • WATKINS, Clare, J.; GB
  • ROMERO-MARTIN, Maria-Rosario; GB
  • MOORE, Kathryn, G.; GB
  • RITCHIE, James; GB
  • FINN, Paul, W.; GB
  • KALVINSH, Ivars; LV
  • LOZA, Einars; LV
  • STARCHENKOV, Igor; LV
  • DIKOVSKA, Klara; LV
  • BOKALDERE, Rasma, Melita; LV
  • GAILITE, Vija; LV
  • VORONA, Maxim; LV
  • ANDRIANOV, Victor; LV
  • LOLYA, Daina; LV
  • SEMENIKHINA, Valentina; LV
  • AMOLINS, Andris; LV
  • HARRIS, C., John,; GB
  • DUFFY, James, E., S.; GB
Agents
  • ARMITAGE, Ian, M. ; Mewburn Ellis York House 23 Kingsway London WC2B 6HP, GB
  • ADRIAN H. BRASNETT and others Mewburn Ellis; York House 23 Kingsway London WC2B 6HP, GB
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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