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1. (WO2010075869) TOLUIDINE SULFONAMIDES AND THEIR USE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/075869 International Application No.: PCT/EP2008/011147
Publication Date: 08.07.2010 International Filing Date: 30.12.2008
IPC:
C07C 311/21 (2006.01) ,C07D 213/76 (2006.01) ,C07D 231/42 (2006.01) ,C07D 249/14 (2006.01) ,C07D 257/04 (2006.01) ,C07D 261/16 (2006.01) ,C07D 277/52 (2006.01) ,C07D 307/66 (2006.01) ,C07D 333/36 (2006.01) ,C07D 207/416 (2006.01) ,A61P 35/00 (2006.01) ,A61K 31/18 (2006.01) ,A61K 31/41 (2006.01) ,A61K 31/341 (2006.01) ,A61K 31/381 (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
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
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
76
to which a second hetero atom is attached
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02
not condensed with other rings
10
having two or 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
38
Nitrogen atoms
42
Benzene-sulfonamido pyrazoles
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
14
Nitrogen 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
261
Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
02
not condensed with other rings
06
having two or more double bonds between ring members or between ring members and non-ring members
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
14
Nitrogen atoms
16
Benzene-sulfonamido isoxazoles
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
38
Nitrogen atoms
50
Nitrogen atoms bound to hetero atoms
52
to sulfur atoms, e.g. sulfonamides
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
56
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
66
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
36
Nitrogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
30
having two double bonds between ring members or between ring members and non-ring members
34
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
Oxygen or sulfur atoms
40
2,5-Pyrrolidine-diones
416
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 other ring carbon atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
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
18
Sulfonamides
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
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
335
having oxygen as the only ring hetero atom, e.g. fungichromin
34
having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
341
not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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
Applicants:
EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL) [DE/DE]; Meyerhofstrasse 1 69117 Heidelberg, DE (AllExceptUS)
ELARA PHARMACEUTICALS GMBH [DE/DE]; Boxbergring 107 69126 Heidelberg, DE (AllExceptUS)
ALONSO, Jorge [ES/DE]; DE (UsOnly)
ENCINAS LOPEZ, Arantxa [DE/DE]; DE (UsOnly)
MUELBAIER, Marcel [DE/DE]; DE (UsOnly)
AMMENN, Jochen [DE/DE]; DE (UsOnly)
WENDT, Bernd [DE/DE]; DE (UsOnly)
LEWIS, Joe [GB/DE]; DE (UsOnly)
SCHULTES, Christoph [DE/DE]; DE (UsOnly)
JANSSEN, Bernd [DE/US]; US (UsOnly)
Inventors:
ALONSO, Jorge; DE
ENCINAS LOPEZ, Arantxa; DE
MUELBAIER, Marcel; DE
AMMENN, Jochen; DE
WENDT, Bernd; DE
LEWIS, Joe; DE
SCHULTES, Christoph; DE
JANSSEN, Bernd; US
Agent:
VOSSIUS, Volker; Geibelstr. 6 81679 München, DE
Priority Data:
Title (EN) TOLUIDINE SULFONAMIDES AND THEIR USE
(FR) TOLUIDINE SULFONAMIDES ET LEUR UTILISATION
Abstract:
(EN) The present invention provides novel compounds that inhibit cell proliferation and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)- mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition comprising a compound of the invention and a second therapeutic agent or radiation useful for the treatment or prevention of the mentioned diseases or disorders. In a first aspect the present invention relates to a compound having a structure according to formula (I).
(FR) La présente invention concerne des nouveaux composés qui inhibent la prolifération cellulaire et la division cellulaire et qui inhibent l'activation de la transcription médiée par le facteur inductible par l'hypoxie (HIF) et la signalisation dans des conditions hypoxiques. Selon un aspect de l'invention, les composés de la présente invention sont utiles pour la préparation d'un médicament destiné au traitement ou à la prévention d'une maladie ou d'un trouble sélectionné dans le groupe constitué d'une maladie inflammatoire, d'une maladie ou d'un trouble hyperprolifératif, d'une pathologie liée à l'hypoxie et d'une maladie caractérisée par une vascularisation excessive. L'invention décrit également une composition pharmaceutique, comprenant un composé de l'invention et un second agent thérapeutique ou un rayonnement thérapeutique, utile pour le traitement ou la prévention des maladies ou troubles susmentionnés. Selon un premier aspect, la présente invention concerne un composé possédant une structure représentée par la formule (I).
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, 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, 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 Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, 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)