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1. (WO2002030879) CARBAMIC ACID COMPOUNDS COMPRISING A SULFONAMIDE LINKAGE AS HDAC INHIBITORS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2002/030879 International Application No.: PCT/GB2001/004326
Publication Date: 18.04.2002 International Filing Date: 27.09.2001
Chapter 2 Demand Filed: 26.04.2002
IPC:
C07C 311/06 (2006.01) ,C07C 311/13 (2006.01) ,C07C 311/16 (2006.01) ,C07C 311/19 (2006.01) ,C07C 311/21 (2006.01) ,C07C 311/29 (2006.01) ,C07D 209/88 (2006.01) ,C07D 213/40 (2006.01) ,C07D 213/42 (2006.01) ,C07D 213/65 (2006.01) ,C07D 213/71 (2006.01) ,C07D 307/52 (2006.01) ,C07D 317/58 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
01
Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
02
of an acyclic saturated carbon skeleton
03
having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
06
to acyclic carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
01
Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
12
of an unsaturated carbon skeleton containing rings
13
the carbon skeleton containing six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
15
Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
16
having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
15
Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
16
having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
19
to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
15
Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
21
having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
311
Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
22
Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
29
having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
56
Ring systems containing three or more rings
80
[b, c]- or [b, d]-condensed
82
Carbazoles; Hydrogenated carbazoles
88
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24
with substituted hydrocarbon radicals attached to ring carbon atoms
36
Radicals substituted by singly-bound nitrogen atoms
40
Acylated substituent nitrogen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24
with substituted hydrocarbon radicals attached to ring carbon atoms
36
Radicals substituted by singly-bound nitrogen atoms
42
having hetero atoms attached to the substituent nitrogen atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
62
Oxygen or sulfur atoms
63
One oxygen atom
65
attached in position 3 or 5
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
62
Oxygen or sulfur atoms
70
Sulfur atoms
71
to which a second hetero atom is attached
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
34
having two or three double bonds between ring members or between ring members and non-ring members
38
with substituted hydrocarbon radicals attached to ring carbon atoms
52
Radicals substituted by nitrogen atoms not forming part of a nitro radical
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
317
Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
08
having the hetero atoms in positions 1 and 3
44
ortho- or peri-condensed with carbocyclic rings or ring systems
46
condensed with one six-membered ring
48
Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
50
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
58
Radicals substituted by nitrogen atoms
Applicants:
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)
DIKOVSKA, Klara [LV/LV]; LV (UsOnly)
GAILITE, Vija [LV/LV]; LV (UsOnly)
VORONA, Maxim [LV/LV]; LV (UsOnly)
PISKUNOVA, Irina [LV/LV]; LV (UsOnly)
STARCHENKOV, Igor; LV (UsOnly)
ADRIANOV, Victor; LV (UsOnly)
HARRIS, C., John [GB/GB]; GB (UsOnly)
DUFFY, James, E., S. [GB/GB]; GB (UsOnly)
PROLIFIX LIMITED [GB/GB]; 91 Milton Park Abingdon Oxfordshire OX14 4RY, GB (AllExceptUS)
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
DIKOVSKA, Klara; LV
GAILITE, Vija; LV
VORONA, Maxim; LV
PISKUNOVA, Irina; LV
STARCHENKOV, Igor; LV
ADRIANOV, Victor; LV
HARRIS, C., John; GB
DUFFY, James, E., S.; GB
Agent:
ARMITAGE, Ian, M.; Mewburn Ellis York House 23 Kingsway London, Greater London WC2B 6HP, GB
ADRIAN H. BRASNETT and others Mewburn Ellis; York House 23 Kingsway London WC2B 6HP, GB
Priority Data:
0023986.329.09.2000GB
60/297,78414.06.2001US
60/308,13630.07.2001US
Title (EN) CARBAMIC ACID COMPOUNDS COMPRISING A SULFONAMIDE LINKAGE AS HDAC INHIBITORS
(FR) COMPOSES D'ACIDE CARBAMIQUE COMPRENANT UNE LIAISON SULFONAMIDE EN TANT QU'INHIBITEURS DE HDAC
Abstract:
(EN) This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: -S(=O)2NR1- and -NR1S(=O)2-; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is -S(=O)2NR1-, then Q1 is an aryl 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) La présente invention concerne certains composés actifs d'acide carbamique inhibiteurs de l'activité histone diacétylase (HDAC) et correspondant à la formule (I), dans laquelle: A est un groupe aryle; Q1 est une liaison covalente ou un groupe aryle de tête; J est une liaison sulfonamide choisie parmi: -S(=O)2NR1- et -NR1S(=O)2-; R1 est une substituant sulfonamide; et Q2 est un groupe acide de tête; et des sels pharmaceutiquement acceptables, des solvates, des amides, des esters, des éthers, des formes chimiquement protégées, et des prodrogues de ceux-ci. La présente invention concerne également des compositions pharmaceutiques comprenant de tels composés, et l'utilisation de tels composés et compositions, in vitro ainsi que in vivo, pour inhiber des pathologies proliférantes, tel que le cancer et le psoriasis.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NO, NZ, PH, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)