发明名称 6,7,8,9-tetrahydro-5H-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
摘要 The present invention relates to compounds defined by formula I; wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.
申请公布号 US9346816(B2) 申请公布日期 2016.05.24
申请号 US201314072324 申请日期 2013.11.05
申请人 Boehringer Ingelheim International GmbH 发明人 Mueller Stephan-Georg;Brown Christopher John;Heifetz Alexander;Nosse Bernd;Prestle Juergen;Prevost Natacha;Rudolf Klaus;Scheuerer Stefan;Schindler Marcus;Stenkamp Dirk;Thomas Leo;Tye Heather
分类号 A61K31/55;C07D487/14 主分类号 A61K31/55
代理机构 代理人 Morris Michael P.;Patel Usha R.
主权项 1. A compound of formula (I) wherein: X denotes a divalent 4- to 10-membered monocylic, 7- to 12-membered spirocyclic or 6- to 12-membered bicyclic saturated, partially or fully unsaturated group selected from a carbocycle, a monoaza-heterocycle and a diaza-heterocycle, which is linked to the adjacent groups via carbon atoms or, if present, via nitrogen atoms, via one carbon and one nitrogen atom or via two nitrogen atoms, wherein 1 or 2 —CH2— groups optionally are replaced independently of each other by O, S, carbonyl, or sulfonyl, with the proviso that two heteroatoms are not directly linked together, and/or1 —CH2— group optionally is replaced by the divalent group >C═C(Rx)2, wherein Rx independently denotes H or C1-3-alkyl, and/orwherein in an unsaturated group 1 double bond optionally is condensed with an aryl or a 5- or 6-membered hetaryl group, and/orwherein in any of the resulting groups one or two carbon atoms optionally and independently are substituted by halogen atoms, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, cyclo C3-7-alkyl, cyclo-C3-7-alkenyl, phenyl, cyano, hydroxy, hydroxy-C1-6-alkyl, hydroxy-C3-6-alkenyl, hydroxy-C3-6-alkynyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, C1-6-alkoxy-C3-6-alkenyl, C1-6-alkoxy-C3-6-alkynyl, C3-6-alkenoxy-C1-6-alkyl, thiohydroxy, C1-6-alkylthio, C3-6-alkenylthio, C3-6-alkynylthio, amino, C1-6-alkyl-amino, C3-6-alkenyl-amino, C3-6-alkynyl-amino, di-(C1-6-alkyl)-amino, di-(C3-6-alkenyl)-amino, di-(C3-6-alkynyl)-amino, amino-C1-6-alkyl, C1-3-alkyl-amino-C1-6-alkyl, di-(C1-3-alkyl)-amino-C1-6-alkyl, amino-C3-6-alkenyl, C1-3-alkyl-amino-C3-6-alkenyl, di-(C1-3-alkyl)-amino-C3-6-alkenyl, amino-C3-6-alkynyl, C1-3-alkyl-amino-C3-6-alkynyl, di-(C1-3-alkyl)-amino-C3-6-alkynyl, hydroxycarbonyl, C1-6-alkyl-carbonyl, C2-6-alkenyl-carbonyl, C2-6-alkynyl-carbonyl, formyl, C1-6-alkoxy-carbonyl, C3-6-alkenoxy-carbonyl, C3-6-alkynoxy-carbonyl, aminocarbonyl, C1-6-alkyl-aminocarbonyl, C3-6-alkenyl-amino-carbonyl, C3-6-alkynyl-aminocarbonyl, di-(C1-6-alkyl)-aminocarbonyl, di-(C3-6-alkenyl)-aminocarbonyl, di-(C3-6-alkynyl)-aminocarbonyl, formylamino, C1-6-alkyl-carbonylamino, C1-6-alkyl-carbonyl-(C1-3-alkyl)-amino, C2-6-alkenyl-carbonylamino,C2-6-alkynyl-carbonylamino, C1-6-alkyl-sulphonyl, C2-6-alkenyl-sulphonyl, C2-6-alkynyl-sulphonyl, C1-6-alkyl-sulphinyl, C2-6-alkenyl-sulphinyl, C2-6-alkynyl-sulphinyl, C1-6-alkyl-sulphonylamino, C2-6-alkenyl-sulphonylamino, C2-6-alkynyl-sulphonylamino, aminosulphonyl, C1-6-alkylaminosulphonyl, di-(C1-6-alkyl)-aminosulphonyl, C3-6-alkenylaminosulphonyl, di-(C3-6-alkenyl)-aminosulphonyl, C3-6-alkynylaminosulphonyl, or di-(C3-6-alkynyl)-aminosulphonyl groups, while the substituents may be identical or different, and/orwherein one ring member nitrogen atom optionally is substituted by a C1-6-alkyl, C3-6-alkenyl, C3-6-alkynyl, cyclo-C3-7-alkenyl, hydroxy, hydroxy-C1-6-alkyl, hydroxy-C3-6-alkenyl, hydroxy-C3-6-alkynyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, C1-6-alkoxy-C3-6-alkenyl, C1-6-alkoxy-C3-6-alkynyl, C3-6-alkenoxy-C1-6-alkyl, C1-6-alkyl-carbonyl, C2-6-alkenyl-carbonyl, C2-6-alkynyl-carbonyl, formyl, C1-6-alkoxy-carbonyl, C3-6-alkenoxy-carbonyl, C3-6-alkynoxy-carbonyl, C1-6-alkyl-sulphonyl, C2-6-alkenyl-sulphonyl, C2-6-alkynyl-sulphonyl, C1-6-alkyl-sulphinyl, C2-6-alkenyl-sulphinyl, C2-6-alkynyl-sulphinyl, aminosulphonyl, phenyl or phenyl-C1-3-alkyl group, Y is absent or denotes a —(CH2)n— group, wherein n is 1, 2, 3, 4, 5 or 6 and wherein 1 or 2 —CH2— groups optionally are replaced independently by O, S, carbonyl, sulfonyl, or —NH—, with the proviso that two heteroatoms are not directly linked together, or wherein 1 —CH2— group is replaced by O, S, carbonyl, sulfonyl, or —NH—, and additionally a —CH2—CH2— subgroup is replaced by —C(O)—O—, —O—C(O)—, —C(O)—NH—, or —NH—C(O)—, with the proviso that two heteroatoms are not directly linked together, and wherein any hydrogen atom of the —NH— groups mentioned hereinbefore optionally and independently is replaced by a C3-6-cycloalkyl or phenyl group, or by a straight-chained or branched C1-6-alkyl, C3-6-alkenyl, C3-6-alkynyl, phenyl-C1-6-alkyl, C1-6-alkyl-carbonyl, or C1-6-alkyl-sulphonyl group, and/orwherein 1 or 2 hydrogen atoms attached to carbon atoms optionally are replaced by halogen atoms, trifluoromethyl, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, phenyl, phenyl-C1-6-alkyl, cyano, hydroxy, hydroxy-C1-6-alkyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, C1-6-alkyl-carbonyl, C1-6-alkoxy-carbonyl, C1-6-alkyl-carbonylamino, C1-6-alkyl-carbonyl-(C1-3-alkyl)-amino, C1-3-alkyl-aminocarbonyl, di-(C1-3-alkyl)-aminocarbonyl or C1-6-alkyl-sulphonyl groups, while the substituents may be identical or different, or 2 geminal hydrogen atoms are replaced by a —(CH2)m— bridge, wherein m is 2, 3, 4, or 5, W denotes H or an optionally substituted straight-chained or branched C1-6-alkyl, C2-6-alkenyl or C2-6-alkynyl group, wherein 1 or 2 methyl groups optionally are replaced by optionally substituted phenyl groups or an optionally substituted cyclo-C3-9-alkyl group, wherein independently in a cyclo-C4-9-alkyl group 2 hydrogen atoms attached to adjacent carbon atoms optionally are replaced to form a double bond within the ring, which optionally is condensed with an optionally substituted aryl or an optionally substituted 5- or 6-membered hetaryl group, and the resulting group is bound via a saturated or unsaturated carbon atom, orin a cyclo-C4-9-alkyl group 2 hydrogen atoms attached to the same carbon atom (relative 1,1-position) optionally are replaced by a C2-5-alkylenyl bridge or 2 hydrogen atoms attached to carbon atoms in relative 1,2-, 1,3- or 1,4-position optionally are replaced by a C1-5-alkylenyl bridge, wherein any of the resulting polycyclic groups one or two —CH2— groups optionally are replaced by —NH— (or N-atoms for replacement of —CH< members), >N—(C1-6-alkyl), O, S, carbonyl, or sulfonyl, and/or two —CH2— groups in relative 1,3-position within a C4-5-alkylenyl bridge optionally are replaced by O atoms, and/or 2 hydrogen atoms attached to adjacent carbon atoms within a C4-5-alkylenyl bridge optionally are replaced to form a double bond, which optionally is condensed with an optionally substituted aryl or an optionally substituted 5- or 6-membered hetaryl group, and/orin a cyclo-C4-8-alkyl group one, two or three ring members optionally are replaced independently of each other by —NH—, >N—(C1-6-alkyl) (or N-atoms for replacement of —CH< members), O, S, carbonyl, or sulfonyl, with the proviso that two heteroatoms are not directly linked together, and additionally but optionally 2 or 4 hydrogen atoms attached to adjacent ring carbon atoms are replaced to form a double bond or two conjugated double bonds within the ring, either of the double bonds optionally being condensed with an optionally substituted aryl or an optionally substituted 5- or 6-membered hetaryl group,and any of the resulting groups is bound via a saturated or unsaturated carbon atom or a nitrogen atom,and wherein any of the resulting open-chained or cyclic groups independently 1 to 4 hydrogen atoms optionally are replaced by C1-6-alkyl or C1-6-alkoxy groups, and/orany 1 to 6 hydrogen atoms attached to carbon atoms optionally are replaced by fluorine atoms, or W denotes an optionally substituted aryl or hetaryl group, an optionally substituted cyclo-C3-8-alkyl-aryl or cyclo-C3-8-alkyl-hetaryl group, wherein the cyclo-C5-8-alkyl-submoieties one or two ring members optionally are replaced independently of each other by —NH— (or N-atoms for replacement of —CH< members), >N(C1-3-alkyl), O, S, carbonyl, or sulfonyl, with the proviso that two heteroatoms are not directly linked together, or if Y is absent W additionally denotes a divalent —(CH2)p— group, wherein p is 2, 3, 4, 5, 6 or 7, attached via the dotted line in formula I, and via the bond connecting W to X, when Y is absent, in relative 1,1-position (geminal) to a carbon atom of group X, including the options: if p is 3, 4, 5, 6 or 7 it follows that 1 —CH2— group optionally is replaced by O, S, carbonyl, sulfonyl, —NH— or —N(C1-6-alkyl)-, orif p is 4, 5, 6 or 7 it follows that a —CH2—CH2— group optionally is replaced by —C(O)—O—, —O—C(O)—, —C(O)—NH—, —NH—C(O)—, —C(O)—N(C1-6-alkyl)-, —N(C1-6-alkyl)-C(O)—, or —CH═CH—, wherein the double bond optionally is condensed with an aryl or a 5- or 6-membered hetaryl group,a divalent —(CH2)q— group, wherein q is 3, 4, or 5, attached via the dotted line in formula I, and via the bond connecting W to X, when Y is absent, in relative 1,2-position (vicinal) to carbon atoms of group X, including the options: that 1 —CH2— group optionally is replaced by O, S, carbonyl, sulfonyl, —NH— or —N(C1-6-alkyl)-, ora —CH2—CH2— group optionally is replaced by —C(O)—O—, —O—C(O)—, —C(O)—NH—, —NH—C(O)—, —C(O)—N(C1-6-alkyl)-, —N(C1-6-alkyl)-C(O)—, orthat in the resulting 5-, 6- and 7-membered carbocyclic ring 2, 4 or 6 hydrogen atoms optionally are replaced by 1, 2 or 3 bonds to form a partially or fully unsaturated ring with isolated or conjugated double bonds, wherein 1 —CH2— group optionally is replaced by O, S, carbonyl, sulfonyl, —NH— or —N(C1-6-alkyl)-, and/or one —CH═ unit is replaced by —N═,a divalent —(CH2)r— group, wherein r is 5, 6 or 7, attached via the dotted line in formula I, and via the bond connecting W to X, when Y is absent, in relative 1,3-position to carbon atoms as binding sites of group X, including the options: that in the resulting 8-, 9- or 10-membered carbocyclic ring 2, 4, 6, 8 or 10 hydrogen atoms optionally are replaced by 1, 2, 3, 4 or 5 bonds to form a partially or fully unsaturated ring with isolated or conjugated double bonds, and/orthat in the resulting 8-, 9- or 10-membered carbocyclic ring 1 hydrogen atom attached to the carbon atom in position 2 relative to the binding sites of group X and 1 hydrogen atom attached to a carbon atom of the —(CH2)r— group in position 6 or 7 relative to the binding sites of group X optionally are replaced by a bond (C0-bridge) to form a bicyclic ring system condensed with the group X,ora divalent —(CH2)r— group, wherein r is 7, attached via the dotted line in formula I and the bond connecting W to X, when Y is absent, in relative 1,3-position to carbon atoms as binding sites of group X, including the option:that in the resulting 10-membered carbocyclic ring 8 hydrogen atoms are replaced by 4 bonds to form fully unsaturated ring conjugated double bonds, andthat in the resulting 10-membered carbocyclic ring 1 hydrogen atom attached to the carbon atom in position 2 relative to the binding sites of group X and 1 hydrogen atom attached to a carbon atom of the —(CH2)r— group in position 7 relative to the binding sites of group X are replaced by a bond (C0-bridge) to form a bicyclic ring system condensed with the group X, resulting in the trivalent group attached in relative 1,2,3-position to carbon atoms * as binding sites of group X, R1 denotes H, C3-6-alkenyl or C3-6-alkynyl, any of those groups being optionally substituted by 1 to 3 fluorine, chlorine or bromine atoms, or by a cyano, hydroxy, C1-3-alkoxy or cyclo-C3-7-alkyl-group, R2 and R3 independently denote H, halogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, hydroxy or C1-6-alkoxy, any of those C1-6-alkyl, C2-6-alkenyl or C3-6-alkynyl groups being optionally substituted by 1 to 3 fluorine, chlorine or bromine atoms, or by a cyano or cyclo-C3-7-alkyl-group, R4 and R5 independently denote H, halogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, cyclo-C3-7-alkyl, hydroxy or C1-3-alkoxy, any of those C1-6-alkyl, C2-6-alkenyl or C3-6-alkynyl groups being optionally substituted by 1 to 3 fluorine, chlorine or bromine atoms, by a cyano, hydroxy, C1-3-alkoxy, or cyclo-C3-5-alkyl-group, or by a phenyl or pyridyl group both optionally substituted independently by 1, 2 or 3 substituents selected from halogen atoms, C1-6-alkyl, cyano, hydroxy, C1-6-alkoxy, amino, C1-6-alkyl-amino, or di-(C1-6-alkyl)-amino groups, wherein, if not specified otherwise, any alkyl groups or subgroups mentioned hereinbefore are straight-chained or branched, the term “aryl” as used hereinbefore, either alone or as a sub-moiety within another substituent, if not otherwise specified means either an optionally substituted aromatic monocyclic or multicyclic system, the term “hetaryl” as used hereinbefore, either alone or as a sub-moiety within another substituent, if not otherwise specified denotes five- or six-membered heterocyclic aromatic groups or 5-10 membered, bicyclic heteroaromatic groups comprising one, two or three heteroatoms selected from oxygen, sulphur and nitrogen, linked through a carbon atom or, if present, through a nitrogen atom, and optionally substituted at carbon atoms and/or a nitrogen atoms, and wherein the expression “substituted” or “optionally substituted” as used hereinbefore if not otherwise specified means substitution with one, two, three, four or more substituents attached to carbon atoms selected from the group consisting of halogen atoms (fluorine, chlorine, bromine or iodine atoms), C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, cyclo-C3-8-alkyl, cyclo-C3-7-alkenyl, cyano, hydroxy, hydroxy-C1-6-alkyl, hydroxy-C3-6-alkenyl, hydroxy-C3-6-alkynyl, C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl, C1-6-alkoxy-C3-6-alkenyl, C1-6-alkoxy-C3-6-alkynyl, C3-6-alkenoxy-C1-6-alkyl, C3-6-alkenoxy-C3-6-alkenyl, C3-6-alkenoxy-C3-6-alkynyl, C3-6-alkynoxy-C1-6-alkyl, C3-6-alkynoxy-C3-6-alkenyl, C3-6-alkynoxy-C3-6-alkynyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, pyrrolidino, piperidino, thiohydroxy, C1-6-alkylthio, C3-6-alkenylthio, C3-6-alkynylthio, amino, C1-6-alkyl-amino, C3-6-alkenyl-amino, C3-6-alkynyl-amino, di-(C1-6-alkyl)-amino, di-(C3-6-alkenyl)-amino, di-(C3-6-alkynyl)-amino, amino-C1-6-alkyl, C1-3-alkyl-amino-C1-6-alkyl, di-(C1-3-alkyl)-amino-C1-6-alkyl, amino-C3-6-alkenyl, C1-3-alkyl-amino-C3-6-alkenyl, di-(C1-3-alkyl)-amino-C3-6-alkenyl, amino-C3-6-alkynyl, C1-3-alkyl-amino-C3-6-alkynyl, di-(C1-3-alkyl)-amino-C3-6-alkynyl, hydroxycarbonyl, phenyl, phenyl-C1-3-alkyl, phenyloxy, phenyl-C1-3-alkoxy, phenyloxy-C1-3-alkyl, phenylcarbonyl, pyridyl, thiazolyl; pyridylcarbonyl, C1-6-alkyl-carbonyl, C2-6-alkenyl-carbonyl, C2-6-alkynyl-carbonyl, formyl, C1-6-alkoxy-carbonyl, C3-6-alkenoxy-carbonyl, C3-6-alkynoxy-carbonyl, aminocarbonyl, C1-6-alkyl-aminocarbonyl, C3-6-alkenyl-amino-carbonyl, C3-6-alkynyl-aminocarbonyl, di-(C1-6-alkyl)-aminocarbonyl, di-(C3-6-alkenyl)-aminocarbonyl, di-(C3-6-alkynyl)-aminocarbonyl, formylamino, C1-6-alkyl-carbonylamino, C2-6-alkenyl-carbonylamino, C2-6-alkynyl-carbonylamino, formyl-C1-6-alkyl-amino, formyl-C3-6-alkenyl-amino, formyl-C3-6-alkynyl-amino, C1-6-alkyl-carbonyl-C1-6-alkyl-amino, C2-6-alkenyl-carbonyl-C1-6-alkyl-amino, C2-6-alkynyl-carbonyl-C1-6-alkyl-amino, C1-6-alkyl-carbonyl-C3-6-alkenyl-amino, C2-6-alkenyl-carbonyl-C3-6-alkenyl-amino, C2-6-alkynyl-carbonyl-C3-6-alkenyl-amino, C1-6-alkyl-carbonyl-C3-6-alkynyl-amino, C2-6-alkenyl-carbonyl-C3-6-alkynyl-amino, C2-6-alkynyl-carbonyl-C3-6-alkynyl-amino, C1-6-alkyl-sulphonyl, C2-6-alkenyl-sulphonyl, C2-6-alkynyl-sulphonyl, C1-6-alkyl-sulphinyl, C2-6-alkenyl-sulphinyl, C2-6-alkynyl-sulphinyl, C1-6-alkyl-sulphonylamino, C2-6-alkenyl-sulphonylamino, C2-6-alkynyl-sulphonylamino, C1-6-alkyl-sulphonyl-C1-6-alkylamino, C1-6-alkyl-sulphonyl-C3-6-alkenylamino, C1-6-alkyl-sulphonyl-C3-6-alkynylamino, C2-6-alkenyl-sulphonyl-C1-6-alkylamino, C2-6-alkenyl-sulphonyl-C3-6-alkenylamino, C2-6-alkenyl-sulphonyl-C3-6-alkynylamino, C2-6-alkynyl-sulphonyl-C1-6-alkylamino, C2-6-alkynyl-sulphonyl-C3-6-alkenylamino, C2-6-alkynyl-sulphonyl-C3-6-alkynylamino, aminosulphonyl, C1-6-alkylaminosulphonyl, di-(C1-6-alkyl)-aminosulphonyl, C3-6-alkenylaminosulphonyl, di-(C3-6-alkenyl)-aminosulphonyl, C3-6-alkynylaminosulphonyl and di-(C3-6-alkynyl)-aminosulphonyl groups, while the substituents may be identical or different and wherein any alkyl groups or alkyl sub-moieties optionally are partially or fully fluorinated, and wherein any phenyl, pyridyl and thiazolyl groups or phenyl-, pyridyl and thiazolyl-submoieties optionally are substituted with 1 or 2 substituents independently of each other selected from fluorine, chlorine, bromine, iodine, C1-3-alkyl, C1-3-alkoxy, amino, C1-3-alkyl-amino, di-(C1-3-alkyl)-amino, C1-3-alkylcarbonyl-amino, C1-3-alkylcarbonyl-C1-3-alkyl-amino, cyano or hydroxy, or with substituents attached to a nitrogen atom selected from the group consisting of C1-6-alkyl, C3-6-alkenyl, C3-6-alkynyl, cyclo-C3-7-alkyl, cyclo-C3-7-alkenyl, cyclo-C3-7-alkyl-C1-6-alkyl, pyrrolidino, piperidino, morpholino, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, cyano, hydroxy, hydroxy-C1-6-alkyl, hydroxy-C3-6-alkenyl, hydroxy-C3-6-alkynyl, C1-6-alkoxy C1-6-alkoxy-C1-6-alkyl, C1-6-alkoxy-C3-6-alkenyl, C1-6-alkoxy-C3-6-alkynyl, C3-6-alkenoxy-C1-6-alkyl, C3-6-alkenoxy-C3-6-alkenyl, C3-6-alkenoxy-C3-6-alkynyl, C3-6-alkynoxy-C1-6-alkyl, C3-6-alkynoxy-C3-6-alkenyl, C3-6-alkynoxy-C3-6-alkynyl, amino-C1-6-alkyl, C1-3-alkyl-amino-C1-6-alkyl, di-(C1-3-alkyl)-amino-C1-6-alkyl, amino-C3-6-alkenyl, C1-3-alkyl-amino-C3-6-alkenyl, di-(C1-3-alkyl)-amino-C3-6-alkenyl, amino-C3-6-alkynyl, C1-3 alkyl-amino-C3-6-alkynyl, di-(C1-3-alkyl)-amino C3-6-alkynyl, hydroxycarbonyl, phenyl, phenyl-C1-6-alkyl, phenylcarbonyl, pyridyl, pyridylcarbonyl, C1-6-alkyl-carbonyl, C2-6-alkenyl-carbonyl, C2-6-alkynyl-carbonyl, C1-6-alkoxy-carbonyl, C3-6-alkenoxy-carbonyl, C3-6-alkynoxy-carbonyl, aminocarbonyl, C1-6-alkyl-aminocarbonyl, C3-6-alkenyl-aminocarbonyl, C3-6-alkynyl-aminocarbonyl, di-(C1-6-alkyl)-aminocarbonyl, di-(C3-6-alkenyl)-aminocarbonyl, di-(C3-6-alkynyl)-aminocarbonyl, C1-6-alkyl-sulphonyl, C2-6-alkenyl-sulphonyl, C2-6-alkynyl-sulphonyl, C1-6-alkyl-sulphinyl, C2-6-alkenyl-sulphinyl, C2-6-alkynyl-sulphinyl, aminosulphonyl, C1-6-alkylaminosulphonyl, di-(C1-6-alkyl)-aminosulphonyl, C3-6-alkenylaminosulphonyl, di-(C3-6-alkenyl)-aminosulphonyl, C3-6-alkynylaminosulphonyl and di-(C3-6-alkynyl)-aminosulphonyl groups, while the substituents may be identical or different and wherein any alkyl groups or alkyl sub-moieties optionally are partially or fully fluorinated, and wherein any of the di-(C1-3-alkyl)-amino or di-(C1-6-alkyl)-amino moieties may form optionally with the nitrogen atom a 4 to 8 membered ring system, and wherein any phenyl and pyridyl groups or phenyl- and pyridyl-submoieties optionally are substituted with 1 or 2 substituents independently of each other selected from fluorine, chlorine, bromine, iodine, C1-3-alkyl, C1-3-alkoxy, amino, C1-3-alkyl-amino, C1-3-alkylcarbonyl-amino, cyano or hydroxy, or a salt thereof.
地址 Ingelheim am Rhein DE