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1. (WO2003004458) NEW COMPOUNDS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2003/004458 International Application No.: PCT/SE2002/001323
Publication Date: 16.01.2003 International Filing Date: 03.07.2002
Chapter 2 Demand Filed: 28.01.2003
IPC:
A61K 31/00 (2006.01) ,A61K 31/33 (2006.01) ,C07C 233/81 (2006.01) ,C07C 275/30 (2006.01) ,C07C 311/17 (2006.01) ,C07C 323/12 (2006.01) ,C07C 323/20 (2006.01) ,C07D 209/08 (2006.01) ,C07D 213/30 (2006.01) ,C07D 213/643 (2006.01) ,C07D 213/65 (2006.01) ,C07D 213/70 (2006.01) ,C07D 213/71 (2006.01) ,C07D 213/74 (2006.01) ,C07D 215/14 (2006.01) ,C07D 233/84 (2006.01) ,C07D 233/91 (2006.01) ,C07D 239/34 (2006.01) ,C07D 239/52 (2006.01) ,C07D 241/18 (2006.01) ,C07D 241/44 (2006.01) ,C07D 263/32 (2006.01) ,C07D 277/24 (2006.01) ,C07D 307/42 (2006.01) ,C07D 307/54 (2006.01) ,C07D 307/81 (2006.01) ,C07D 317/60 (2006.01) ,C07D 333/16 (2006.01) ,C07D 333/18 (2006.01) ,C07D 333/24 (2006.01) ,C07D 333/28 (2006.01) ,C07D 333/60 (2006.01) ,G01N 33/566 (2006.01) ,G01N 33/68 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
233
Carboxylic acid amides
64
having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
81
having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
275
Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
28
having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
30
being further substituted by halogen atoms, or by nitro or nitroso 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
16
having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
17
to an acyclic carbon atom of a hydrocarbon radical 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
10
containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton
11
having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
12
the carbon skeleton being acyclic and saturated
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
10
containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton
18
having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
20
with singly-bound oxygen atoms bound to carbon atoms of the same non-condensed 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
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
08
with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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
28
Radicals substituted by singly-bound oxygen or sulfur atoms
30
Oxygen atoms
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
64
attached in position 2 or 6
643
2-Phenoxypyridines; Derivatives thereof
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
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
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
72
Nitrogen atoms
74
Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
12
with substituted hydrocarbon radicals attached to ring carbon atoms
14
Radicals substituted by oxygen 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
84
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
91
Nitro radicals
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
34
One oxygen 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
52
Two oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
241
Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
02
not condensed with other rings
10
having three double bonds between ring members or between ring members and non-ring members
14
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
18
Oxygen or sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
241
Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
36
condensed with carbocyclic rings or ring systems
38
with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
40
Benzopyrazines
44
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 hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
263
Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02
not condensed with other rings
30
having two or three double bonds between ring members or between ring members and non-ring members
32
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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
22
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
24
Radicals substituted by oxygen atoms
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
40
Radicals substituted by oxygen atoms
42
Singly bound oxygen atoms
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
54
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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
77
ortho- or peri-condensed with carbocyclic rings or ring systems
78
Benzo [b] furans; Hydrogenated benzo [b] furans
79
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
81
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
60
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
14
Radicals substituted by singly bound hetero atoms other than halogen
16
by oxygen 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
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
14
Radicals substituted by singly bound hetero atoms other than halogen
18
by sulfur 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
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
24
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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
28
Halogen 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
50
condensed with carbocyclic rings or ring systems
52
Benzo [b] thiophenes; Hydrogenated benzo [b] thiophenes
54
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
60
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
G PHYSICS
01
MEASURING; TESTING
N
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33
Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48
Biological material, e.g. blood, urine; Haemocytometers
50
Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
53
Immunoassay; Biospecific binding assay; Materials therefor
566
using specific carrier or receptor proteins as ligand binding reagent
G PHYSICS
01
MEASURING; TESTING
N
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33
Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48
Biological material, e.g. blood, urine; Haemocytometers
50
Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
68
involving proteins, peptides or amino acids
Applicants:
GUSTAVSSON, Anna-Lena [SE/SE]; SE (UsOnly)
JENDEBERG, Lena [SE/SE]; SE (UsOnly)
ROUSSEL, Patrick [FR/IT]; IT (UsOnly)
SLATER, Martin [GB/GB]; GB (UsOnly)
THOR, Markus [SE/SE]; SE (UsOnly)
BIOVITRUM AB [SE/SE]; S-112 76 Stockholm, SE (AE, AG, AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BY, BZ, CA, CF, CG, CH, CI, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GW, HR, HU, ID, IE, IL, IN, IS, IT, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MC, MD, MG, MK, ML, MN, MR, MW, MX, MZ, NE, NL, NO, NZ, OM, PH, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, SN, SZ, TD, TG, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VN, YU, ZA, ZM, ZW)
Inventors:
GUSTAVSSON, Anna-Lena; SE
JENDEBERG, Lena; SE
ROUSSEL, Patrick; IT
SLATER, Martin; GB
THOR, Markus; SE
Agent:
DANIELSSON, Helena; Biovitrum AB S-112 76 Stockholm, SE
Priority Data:
0102384-503.07.2001SE
60/304,70611.07.2001US
Title (EN) NEW COMPOUNDS
(FR) COMPOSES NOUVEAUX
Abstract:
(EN) The present invention relates to 2-(benzoylamino)benzoic acid derivatives of the formula (I), wherein the variants Ar, X and R are described in the specification. The said compounds modulate the activity of peroxisome proliferator-activated receptors (PPAR) α and/or γ, and are predicted to be useful in the treatment of metabolic diseases, e.g. type II diabetes.
(FR) La présente invention a trait à des dérivés de l'acide 2-(benzoylamino)benzoïque de formule (1), dans laquelle les variants Ar, X et R sont tels que définis dans la description. Lesdits composés modulent l'activité des récepteurs activés de la prolifération des (PPAR) peroxysomes $g(a) et/ou $g(g), et sont utiles dans le traitement de maladies métaboliques, par exemple, le diabète de type II.
front page image
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, OM, PH, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE, SK, 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)