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1. (WO2001005756) 3-ARYLSULFONYL-2-(SUBSTITUTED METHYL)PROPANOIC ACID DERIVATES AS MATRIX METALLOPROTEINASE INHIBITORS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2001/005756 International Application No.: PCT/EP2000/006429
Publication Date: 25.01.2001 International Filing Date: 07.07.2000
Chapter 2 Demand Filed: 12.02.2001
IPC:
C07C 317/46 (2006.01) ,C07C 323/65 (2006.01) ,C07D 213/70 (2006.01) ,C07D 233/72 (2006.01) ,C07D 233/84 (2006.01) ,C07D 235/28 (2006.01) ,C07D 239/38 (2006.01) ,C07D 239/56 (2006.01) ,C07D 249/12 (2006.01) ,C07D 257/04 (2006.01) ,C07D 277/36 (2006.01) ,C07D 285/125 (2006.01) ,C07D 285/135 (2006.01) ,C07D 333/34 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
317
Sulfones; Sulfoxides
44
having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
46
the carbon skeleton being further substituted by singly-bound oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
323
Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
64
containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
65
containing sulfur atoms of sulfone or sulfoxide groups bound to the carbon skeleton
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
233
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54
having two double bonds between ring members or between ring members and non-ring members
66
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
72
Two oxygen atoms, e.g. hydantoin
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
233
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54
having two double bonds between ring members or between ring members and non-ring members
66
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
84
Sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
24
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 in position 2
28
Sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
32
One oxygen, sulfur or nitrogen atom
38
One sulfur atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02
not condensed with other rings
24
having three or more double bonds between ring members or between ring members and non-ring members
28
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46
Two or more oxygen, sulfur or nitrogen atoms
56
One oxygen atom and one sulfur atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
249
Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
02
not condensed with other rings
08
1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
10
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
12
Oxygen or sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
257
Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
02
not condensed with other rings
04
Five-membered rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02
not condensed with other rings
20
having two or three double bonds between ring members or between ring members and non-ring members
32
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
36
Sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
285
Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/-C07D283/183
01
Five-membered rings
02
Thiadiazoles; Hydrogenated thiadiazoles
04
not condensed with other rings
12
1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
125
with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
285
Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/-C07D283/183
01
Five-membered rings
02
Thiadiazoles; Hydrogenated thiadiazoles
04
not condensed with other rings
12
1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
125
with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
135
Nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
333
Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02
not condensed with other rings
04
not substituted on the ring sulfur atom
26
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
30
Hetero atoms other than halogen
34
Sulfur atoms
Applicants: MANTEGANI, Sergio[IT/IT]; IT (UsOnly)
ABRATE, Francesca[IT/IT]; IT (UsOnly)
BISSOLINO, Pierluigi[IT/IT]; IT (UsOnly)
CREMONESI, Paolo[IT/IT]; IT (UsOnly)
PERRONE, Ettore[IT/IT]; IT (UsOnly)
JABES, Daniela[IT/IT]; IT (UsOnly)
PHARMACIA & UPJOHN SpA[IT/IT]; Via Robert Koch, 1.2 I-20152 Milan, IT (AllExceptUS)
Inventors: MANTEGANI, Sergio; IT
ABRATE, Francesca; IT
BISSOLINO, Pierluigi; IT
CREMONESI, Paolo; IT
PERRONE, Ettore; IT
JABES, Daniela; IT
Priority Data:
9916562.314.07.1999GB
Title (EN) 3-ARYLSULFONYL-2-(SUBSTITUTED METHYL)PROPANOIC ACID DERIVATES AS MATRIX METALLOPROTEINASE INHIBITORS
(FR) DERIVES D'ACIDE 3-ARYLSULFONYL-2-(A SUBSTITUTION METHYL)PROPANOIQUE UTILISES COMME INHIBITEURS DE LA METALLOPROTEINASE A MATRICE
Abstract:
(EN) Compounds which are 3-arylsulfonyl-2-methyl propanoic acid derivatives of formula (I): wherein X is HO-NH- or HO-, R1 is selected from phenyl, 4-chlorophenyl, 4-fluorophenyl, 4-cyanophenyl, benzamido (i.e., -NH-CO-Ph) and benzamido substituted on the terminal phenyl ring by C1-C4 alkyl, fluoro, chloro, cyano or C1-4 alkoxy; R2 is selected from (a) -S-Ar or -S-CH2-Ar wherein Ar is an aromatic moiety; (b) -O-Ar wherein Ar is as defined above; (c) -S-Het or -S-CH2-Het wherein Het is a heterocyclic ring; and (d) 2,5-dioxo-1-imidazolidinyl or 2,4-dioxo-1-imidazolinyl; and the pharmaceutically acceptable salts thereof; have potent and selective inhibitory activity against matrix metalloproteinases (MMPs) and can thus be used in the treatment and prevention of diseases mediated by MMPs.
(FR) Cette invention a trait à des composés, en l'occurrence, des dérivés d'acide 3-arylsulfonyl-2-methyl propanoïque correspondant à la formule (I) ainsi qu'à leurs sels acceptables du point de vue pharmaceutique. Dans cette formule, X représente HO-NH- ou HO-, R1 est choisi dans le groupe constitué par du phényle, du 4-chlorophényle, du 4-fluorophényle, du 4-cyanophényle, un benzamido (par exemple, -NH-CO-Ph) et un benzamido substitué à la hauteur du noyau phényle par un alkyle porteur de 1 à 4 atomes de carbone, un fluoro, un chloro, un cyano ou un alcoxy porteur de 1 à 4 atomes de carbone, R2 est choisi dans le groupe constitué, (a), par -S-Ar ou -S-CH2-Ar, Ar représentant une fraction aromatique, (b), par -O-Ar, Ar étant tel que défini ci-dessus, (c), par -S-Het ou -S-CH2-Het, Het représentant un noyau hétérocyclique et, (d), par 2,5-dioxo-1-imidazolidinyle ou par 2,4-dioxo-1-imidazolinyle. Ces composés, qui comme leurs sels, témoignent d'une action sélective et vigoureuse d'inhibition des métalloprotéinases à matrice (MMP), peuvent être utilisés pour le traitement et la prophylaxie d'états pathologiques induits par les MMP.
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Designated States: AE, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CR, CU, CZ, DE, DK, DM, 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, NO, NZ, 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)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)