http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-057976-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_12a9e9ce63eb0bbf3658453fb50a6d9b |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 |
| filingDate | 2006-08-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_523f4a07260a50d472dc1c0670d75cf9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_070c548f2509c9ab0f98e4cc6c1313d5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_49b65f0b283407d8c9ce49db5554257d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c9f2b43b9904d60c6060d563a54cfafb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5cc1c1f495068d5d04f326d1e2de71bc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ff9d614067e2b34a0a0ac0ebf55a78a0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_64c382bbd23338942d7703bf7ff885be |
| publicationDate | 2008-01-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-057976-A1 |
| titleOfInvention | SUBSTITUTED BIARILOS AND ITS USE AS MEDICINES. |
| abstract | Substituted biaryls and pharmaceutical compositions comprising them. Claim 1: Compounds of the general formula (1), wherein A is a radical of the group of formulas (2); X1 is a carbonyl, thiocarbonyl, -C (N-R4c) -, -C (NOR4c) -, -C (N-NO2) -, -C (NCN) - or sulfonyl group; X2 is an oxygen atom or a group -N (R4b) -; X3 is an oxygen or sulfur atom or a group -N (R4c) -; m is the number 1 or 2; L is a 5-membered monocyclic heteroarylene group optionally substituted in the carbon structure with an R5a group and the two bonds shown in formula (1) can be produced through two carbon atoms or an imino group and a carbon atom of the heterocycle, where an optionally -NH- group may be replaced by a group -N (R5b) -; B is a radical of the general formula -G-T; G is a remainder selected from the group of formulas (3); T is a 5 or 6 membered monocyclic heteroaryl or phenyl group, which is optionally substituted on one or two carbon atoms independently of each other with R6; R1 is a hydrogen, fluorine, chlorine, bromine or iodine atom, a C1-3 alkyl or C1-3 alkoxy group, wherein the hydrogen atoms of the C1-3 alkyl or C1-3 alkoxy group may eventually be wholly or partially replaced by fluorine atoms, a C2-3 alkenyl group, C2-3 alkynyl, nitrile, nitro or amino; R2 is a hydrogen or halogen atom or a C1-3alkyl or C1-3alkoxy group, wherein the hydrogen atoms of the C1-3alkyl or C1-3alkoxy group may optionally or partially be replaced by fluorine atoms ; R3a and R3b are each, independently of each other, a hydrogen atom, a C2-5 alkenyl or C2-5 alkynyl group, a straight or branched C1-5 alkyl group, wherein the hydrogen atoms of the group C1-5 straight or branched chain alkyl may be replaced, in whole or in part, by fluorine atoms, and which may eventually be substituted with a group R7a, R7b, R7c or a C1-4 alkyloxy group which is substituted with an R7b group, a mercapto, a C1-5 alkylsulfanyl group, C1-5 alkylsulfonyl group, an R7b or R7c group, a 3 to 7 membered cycloalkyl group, cycloalkyl-C1-5 alkyl or cycloalkyleneimino-C1-3 alkyl, wherein in the case of the 4 to 7 member cycles in the cyclic part, a methyl group may eventually be replaced by a group -N (R4c) -, an oxygen or sulfur atom or a carbonyl group, -S (O) - or - S (O) 2-, or where in the case of cycles of 4 to 7 members in the cyclic part, two adjacent methylene groups together pu They may eventually be replaced by a group -C (O) N (R4b) - or -S (O) 2N (R4b) -, where a 3- to 7-membered cycloalkyl group, cycloalkyleneimino, cycloalkyl-C1-5 alkyl or cycloalkyleneimino -C1-3 alkyl in one or two groups -CH2- may be substituted with one or two R4a groups, with the proviso that a cycloalkyl, cycloalkyleneimino, cycloalkyl-C1-5 alkyl or cycloalkyleneimino-C1-3 alkyl group is excluded 3 to 7 members, defined as above, in which two heteroatoms of the oxygen and nitrogen group are separated from each other by exactly one optionally substituted -CH2- group, or R3a and R3b form together with the carbon atom to which they are attached, a C3-8 cycloalkyl or C3-8 cycloalkenyl group, wherein a C3-8 cycloalkyl group in a single carbon atom may be substituted with a C2-5 alkylene group or at the same time in two different carbon atoms with a C1 alkylene group -4 with the formation of a corresponding spirocycle or a bicycle in bridge, wherein one of the methylene groups of a C4-8 cycloalkyl or C5-8 cycloalkenyl group or one of the corresponding spirocycles or bridge bicycles as described above may be replaced by an oxygen or sulfur atom or a group -B (R4c) -, or a carbonyl, sulfinyl or sulfonyl group, and / or two directly adjacent methylene groups of a C4-8 cycloalkyl group may be replaced by a group -C (O) N (R4b) -, -C (O) O- or -S (O) 2N (R4b) -, and / or three directly adjacent methylene groups of a C6-8 cycloalkyl group together may be replaced by a group - OC (O) N (R4b) -, -N (R4b) C (O) N (R4b) - or -N (R4b) S (O) 2N (R4b) -, wherein 1 to 3 carbon atoms of a C3-8 cycloalkyl group or one of the corresponding spirocycles or bridge bicycles as described above may eventually be substituted, independently of one another, with one or two fluorine atoms or one or two equal or different alkyl groups or R7a or R7b groups or C1-5 carboxyalkyl, C1-5 alkyl-oxycarbonyl-C1-5 alkyl, C1-5 alkyl sulfanyl or C1-5 alkyl sulfonyl, wherein 1 to 2 carbon atoms of a C3 cycloalkenyl group -8 may optionally be substituted, independently of one another, with a C1-5 alkyl group or an R7b group, and 1 to 2 sp3-hybridized carbon atoms of a C4-8 cycloalkenyl group may eventually be substituted, independently each other, with one or two fluorine atoms or an R7b group, with the proviso that a C3-8 cycloalkyl or C3-8 cycloalkenyl group formed by R3a and R3b together or a corresponding spirocycle described as above or a bicyclo in corresponding bridge, in which two heteroatoms in the oxygen and nitrogen group cycle are separated from each other exactly by an optionally substituted -CH2 group, and / or where one or both methylene groups of the cycle, which are directly linked to the atom of carbon, are linked with radicals R3a and R3b, are replaced by a heteroatom of the oxygen, nitrogen and sulfur group, and / or in which a substituent attached to the cyclic group, which is characterized in that a hetero atom of the oxygen, nitrogen, sulfur and halogen atom group is directly linked to the cyclic group, it is separated, by exactly one methylene group, optionally substituted, from another heteroatom of the oxygen, nitrogen and sulfur group, with the exception of the sulfone group, and / or where two oxygen atoms are directly linked to each other, and / or wherein a heteroatom of the oxygen, nitrogen and sulfur group are directly linked to the carbon atom, which is linked to another carbon atom through a double bond, and / or that contains a cycle with three ring members , of which one or more correspond to the group of oxygen or sulfur atom or -N (R4c) -; R4a are, independently of each other, a hydrogen or fluorine atom or a C1-4 alkyl group optionally substituted with a group R7a, R7b or R7c or representing as a substituent of a sp3-hybridized carbon atom a group R7a, R7b, or R7c, where in the case of the above-mentioned substituted 5- to 7-membered radicals A, the F, O or N heteroatoms possibly introduced with as substituents are not just separated by a sp3-hybridized carbon atom from a heteroatom of group N, O, S; R4b are each, independently of each other, a hydrogen atom or a C1-5 alkyl group; R4c are each, independently of each other, a hydrogen atom, a C1-5 alkyl, C1-5 alkylcarbonyl, C1-5 alkylcarboxylic or C1-5 alkyl sulfonyl group; R5a are each, independently of each other, a hydrogen or halogen atom or a C1-4 alkyl group optionally substituted with a group R7a, R7b, R7c or R7e, where the hydrogen atoms are totally or partially replaced by fluorine atoms, or a group R7a, R7b, R7c or R7e, wherein each group R7c in the carbon structure may be substituted with one or two groups selected from halogen atom, C1-4 alkyl group and groups R7a, R7b and R7e as well as in the case of 5-membered heterocycles in a substitutable nitrogen atom may be substituted with a C1-4 alkyl group optionally substituted with R7a, wherein a heteroatom introduced with R7a as a substituent of the alkyl group is separated from the nitrogen atom of the heterocycle by at least two methylene groups, or with R7a, and the group R7b or R7e in the carbon structure may be substituted with one or two C1-4 alkyl groups, which in turn may be independently substituted ent yes with an R7a group; R5b are each, independently of each other, a hydrogen atom or a C1-5 alkyl group optionally substituted with a group R7a, R7b, R7c or R7e or a group R7a, R7c or R7e, wherein the group R7c in the Carbon structure may be substituted with one or two groups selected from halogen atom, C1-4 alkyl group, and R7a, R7b and R7e groups as well as in the case of 5-membered heterocycles in a substitutable nitrogen atom, with a group C1-4 alkyl optionally substituted with R7a, wherein a heteroatom introduced with R7a as a substituent of the alkyl group is separated from the nitrogen atom of the heterocycle by at least two methylene groups, or with R7a, and the group R7e in the carbon structure can be substituted with one or two C1-4 alkyl groups, which in turn can be independently substituted with each other with a group R7a, wherein the heteroatoms possibly introduced with R7a as a substituent, O or N are not just separated with volume carbon atom substituted with R5b nitrogen in the heterocycle; R6 is a fluorine, chlorine, bromine or iodine atom, a nitro, amino, nitrile, hydroxy, C2-3 alkenyl, C2-3 alkynyl, C1-3 alkyl or a C1-3 alkoxy group group, wherein the atoms of hydrogen of the C1-3 alkyl or C1-3 alkoxy group may optionally be totally or partially replaced by fluorine atoms; R7a are each, independently of each other, a hydroxyl group or an R7d group; R7b are each, independently of each other, a carboxy, C1-3-alkoxycarbonyl, aminocarbonyl, C1-3-aminocarbonyl, di- (C1-3 alkyl) -aminocarbonyl, morpholin-4-i-carbonyl group, (4-C1-3 alkyl-piperazin-1-yl) -carbonyl, (4- [C1-3 alkyl) -carbonyl] -piperazin-1-yl) -carbonyl, a group |
| priorityDate | 2005-08-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 59.