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1. (WO2010142934) INDOLE DERIVATIVES AS LIGANDS OF CRTH2 RECEPTORS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2010/142934 International Application No.: PCT/GB2009/050671
Publication Date: 16.12.2010 International Filing Date: 12.06.2009
IPC:
C07D 209/10 (2006.01) ,C07D 401/06 (2006.01) ,C07D 401/12 (2006.01) ,C07D 401/14 (2006.01) ,C07D 403/06 (2006.01) ,A61P 37/00 (2006.01) ,A61K 31/4439 (2006.01) ,C07D 409/06 (2006.01) ,C07D 409/14 (2006.01) ,C07D 413/06 (2006.01) ,C07D 417/06 (2006.01) ,C07D 417/14 (2006.01) ,A61K 31/4178 (2006.01) ,A61K 31/422 (2006.01) ,A61K 31/404 (2006.01)
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
10
with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
4439
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14
containing three or more hetero 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
4164
1,3-Diazoles
4178
not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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
42
Oxazoles
422
not condensed and containing further heterocyclic 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
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403
condensed with carbocyclic rings, e.g. carbazole
404
Indoles, e.g. pindolol
Applicants:
HYND, George [GB/GB]; GB (UsOnly)
MONTANA, John Gary [GB/GB]; GB (UsOnly)
FINCH, Harry [GB/GB]; GB (UsOnly)
ARIENZO, Rosa [IT/GB]; GB (UsOnly)
AHMED, Shahadat [IN/GB]; GB (UsOnly)
PULMAGEN THERAPEUTICS (ASTHMA) LIMITED [GB/GB]; Fulmer Hall Windmill Road Fulmer Slough SL3 6HD, GB (AllExceptUS)
Inventors:
HYND, George; GB
MONTANA, John Gary; GB
FINCH, Harry; GB
ARIENZO, Rosa; GB
AHMED, Shahadat; GB
Agent:
PERRY, Robert, Edward; Gill Jennings & Every LLP The Broadgate Tower 20 Primrose Street London EC2A 2ES, GB
Priority Data:
Title (EN) INDOLE DERIVATIVES AS LIGANDS OF CRTH2 RECEPTORS
(FR) DÉRIVÉS D'INDOLE EN TANT QUE LIGANDS DES RÉCEPTEURS CRTH2
Abstract:
(EN) The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: {3-[3-chloro-4-(pyridine-2-sulfonyl)isothiazol-5-ylmethyl]-5-fluoro-2- methylindol-1-yl}acetic acid, [3-(5-benzenesulfonyl-3-methyl-3H-imidazol-4-ylmethyl)-5-fluoro-2- methylindol-1-yl]acetic acid, [3-(5-benzenesulfonyloxazol-4-ylmethyl)-5-fluoro-2-methylindol-1-yl]acetic acid, [3-(3-benzenesulfonyl-4-met ylthiophen-2-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, {5-fluoro-2-methyl-3-[2-(pyridin-2-ylsulfamoyl)benzyl]indol-1-yl}acetic acid, {5-fluoro-2-methyl-3-[4-methyl-3-(pyridine-2-sulfonyl)thiophen-2- ylmethyl]indol-1-yl}acetic acid, {5-fluoro-2-methyl-3-[3-methyl-5-(pyridine-2-sulfonyl)-3H-imidazol-4- ylmethyl]indol-1-yl}acetic acid, {5-fluoro-3-[2-(3-fluorophenylsulfamoyl)pyridin-3-ylmethyl]-2-methylindol-1- yl}acetic acid, [3-(4-benzenesulfonyloxazol-5-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, {3-[2-(3-cyanophenylsulfamoyl)benzyl]-5-fluoro-2-methylindol-1-yl}acetic acid, [3-(4-benzenesulfonylthiazol-5-ylmethyl)-5-chloro-2-methyl-indol-1-yl]acetic acid, [3-(4-benzenesulfonyl-2-methylthiazol-5-ylmethyl)-5-fluoro-2-methylindol-1- yl]acetic acid, and [3-(4-benzenesulfonyl-3-methylisothiazol-5-ylmethyl)-5-fluoro-2- methylindol-1-yl]acetic acid.
(FR) La présente invention a pour objet les composés suivants qui sont des antagonistes du CRTH2, utiles dans le traitement des maladies respiratoires : l'acide {3-[3-chloro-4-(pyridine-2-sulfonyle) isothiazol-5-ylméthyle]-5-fluoro-2-méthylindol-1-yle} acétique, l'acide [3-(5-benzène sulfonyl-3-méthyl-3H-imidazol-4-ylméthyle)-5-fluoro-2- méthylindol-1-yle] acétique, l'acide [3-(5-benzène sulfonyloxazol-4-ylméthyle)-5-fluoro-2-méthylindol-1-yle] acétique, l'acide [3-(3-benzène sulfonyl-4-méthylthiophèn-2-ylméthyle)-5-fluoro-2-méthylindol-1- yle] acétique, l'acide {5-fluoro-2-méthyl-3-[2-(pyridine-2-ylsulfamoyle) benzyle] indol-1-yle} acétique, l'acide {5-fluoro-2-méthyl-3-[4-méthyl-3-(pyridine-2-sulfonyle) thiophène-2- ylméthyle] indol-1-yle} acétique, l'acide {5-fluoro-2-méthyl-3-[3-méthyl-5-(pyridine-2-sulfonyle)-3H-imidazol-4-ylméthyle] indol-1-yle} acétique, l'acide {5-fluoro-3-[2-(3-fluorophénylsulfamoyle) pyridine-3-ylméthyle]-2-méthylindol-1-yle} acétique, l'acide [3-(4-benzène sulfonyloxazol-5-ylméthyle)-5-fluoro-2-méthylindol-1-yle] acétique, l'acide {3-[2-(3-cyanophénylsulfamoyle) benzyle]-5-fluoro-2-méthylindol-1-yle} acétique, l'acide [3-(4-benzène sulfonylthiazol-5-ylméthyle)-5-chloro-2-méthyl-indol-1-yle] acétique, l'acide [3-(4-benzène sulfonyl-2-méthylthiazol-5-ylméthyle)-5-fluoro-2-méthylindol-1- yle] acétique, et l'acide [3-(4-benzène sulfonyl-3-méthylisothiazol-5-ylméthyle)-5-fluoro-2- méthylindol-1-yle] acétique.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, 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, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, 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)