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1. (WO2001005746) AMINOBENZOPHENONES AS INHIBITORS OF IL-1$g(b) AND TNF-$g(a)
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2001/005746 International Application No.: PCT/DK2000/000385
Publication Date: 25.01.2001 International Filing Date: 11.07.2000
Chapter 2 Demand Filed: 03.02.2001
IPC:
C07C 225/22 (2006.01) ,C07C 229/18 (2006.01) ,C07C 233/43 (2006.01) ,C07C 235/10 (2006.01) ,C07C 235/72 (2006.01) ,C07C 235/74 (2006.01) ,C07C 237/20 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
225
Compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly-bound oxygen atoms not being part of a -CHO group, e.g. amino ketones
22
having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
229
Compounds containing amino and carboxyl groups bound to the same carbon skeleton
02
having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
04
the carbon skeleton being acyclic and saturated
06
having only one amino and one carboxyl group bound to the carbon skeleton
18
the nitrogen atom of the amino group being further bound to carbon atoms of six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
233
Carboxylic acid amides
01
having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
34
having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
42
with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
43
having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
235
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
02
having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
04
the carbon skeleton being acyclic and saturated
10
having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
235
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
70
having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
72
with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
235
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
70
having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
72
with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
74
of a saturated carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
237
Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
02
having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
20
the carbon skeleton containing six-membered aromatic rings
Applicants: OTTOSEN, Erik, Rytter[DK/DK]; DK (UsOnly)
LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LØVENS KEMISKE FABRIK PRODUKTIONSAKTIESELSKAB)[DK/DK]; Industriparken 55 DK-2750 Ballerup, DK (AllExceptUS)
Inventors: OTTOSEN, Erik, Rytter; DK
Agent: THALSØ-MADSEN, Birgit; Patent Department Leo Pharmaceutical Products Ltd. A/S Industriparken 55 DK-2750 Ballerup, DK
Priority Data:
60/144,16616.07.1999US
Title (EN) AMINOBENZOPHENONES AS INHIBITORS OF IL-1$g(b) AND TNF-$g(a)
(FR) AMINOBENZOPHENONES EN TANT QU'INHIBITEURS DE IL-1$g(b) ET TNF-$g(a)
Abstract:
(EN) The present invention relates to a compound of general formula (I) wherein R1, R2, and R3 represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, -CONH2, phenyl, or nitro; further R2 can be hydrogen, and R3 can be carboxy and carbamoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulphur; Q represents -(CO)-, -(CS)-, or a bond; Y represents (C5-C15)alkyl; (C2-C15)olefinic group; (C3-C10)monocyclic hydrocarbon group; or phenyl; any of which may be optionally substituted by one or more, same or different substituents selected from the group consisting of the formula R5 defined below; (C1-C4)alkyl substituted by one or more substituents selected for the group R5; or a group of the formula -(Z-O)n-Z, wherein Z is a (C1-C3)alkyl, n is an integer > 1; and no continuous linear sequence of atoms in the group Y exceeds 15; R5 represents halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, azido, nitro, -COOH, -CONH2, -CONHR', or COONR'R' wherein R' represents (C1-C3)alkyl; or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof. The compounds are valuable in the human and veterinary therapy.
(FR) La présente invention concerne un composé correspondant à la formule générale (I) dans laquelle R1, R2, et R3 représentent un ou plusieurs substituants, identiques ou différents, choisis dans le groupe constitué d'un groupe halogène, hydroxy, mercapto, trifluorométhyle, amino, alkyle en C1-C3, groupe oléfinique en C2-C3, alcoxy en C1-C3, alkylthio en C1-C3, alkylamino en C1-C6, alcoxycarbonyle en C1-C3, cyano, -CONH2, phényle, ou nitro; R2 peut également représenter un groupe carboxy ou carbamoyle; R4 représente un atome d'hydrogène, un groupe alkyle en C1-C3, ou allyle; X représente un atome d'oxygène ou de soufre; Q représente un groupe -(CO)-, -(CS)-, ou une liaison; Y représente un groupe alkyle en C5-C15; un groupe oléfinique en C2-C15; un groupe d'hydrocarbure monocyclique en C3-C10; ou un groupe phényle; chacun desquels pouvant être facultativement substitués par un ou plusieurs substituants, identiques ou différents, choisis dans le groupe correspondant à la formule R5 définie ci-dessous; un groupe alkyle en C1-C4 substitué par un ou plusieurs substituants choisis dans le groupe R5; ou un groupe correspondant à la formule -(Z-O)n-Z, dans laquelle Z représente un groupe alkyle en C1-C3, n prend la valeur d'un entier > 1 ; et il n'existe aucune séquence linéaire continue d'atomes dans le groupe Y supérieure à 15; R5 représente un groupe halogène, hydroxy, mercapto, trifluorométhyle, amino, un groupe alcoxy en C1-C3, alkylthio en C1-C3, alkylamino en C1-C6, alcoxycarbonyle en C1-C3, cyano, azido, nitro, -COOH, -CONH2, -CONHR', ou COONR'R', R' représentant un groupe alkyle en C1-C3. L'invention concerne aussi tous les sels de ces composés acceptables sur le plan pharmaceutique, ou un de leurs hydrates ou solvates. Ces composés présentent un grand intérêt pour la thérapie humaine et vétérinaire.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CR, CU, CZ, DE, DK, DM, DZ, 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, 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)