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    • 2. 发明申请
    • TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULAIONT OF THE DOPAMINE D3 RECEPTOR
    • 适用于治疗多巴胺D3受体调节症状的三唑化合物
    • WO2006058753A1
    • 2006-06-08
    • PCT/EP2005/012856
    • 2005-12-01
    • ABBOTT GMBH & CO. KGUNGER, LilianeHAUPT, AndreasBEYERBACH, ArminDRESCHER, KarlaBRAJE, WilfriedDARBYSHIRE, JohnTURNER, Sean, C.BACKFISCH, Gisela
    • UNGER, LilianeHAUPT, AndreasBEYERBACH, ArminDRESCHER, KarlaBRAJE, WilfriedDARBYSHIRE, JohnTURNER, Sean, C.BACKFISCH, Gisela
    • A61K31/506C07D403/12A61P25/18
    • C07D403/12
    • The invention relates to compounds of formula (I), wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R 1 on the remaining carbon atom and a radical R 1a on one of the nitrogen atoms; R 1 is hydrogen, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 1 -C 4 alkoxymethyl, fluorinated C 1 -C 6 alkyl, fluorinated C 3 -C 6 cycloalkyl, fluorinated C 1 -C 4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R 1a is hydrogen or C 1 -C 4 alkyl; and R 2 is C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, fluorinated C 1 -C 6 alkyl or fluorinated C 3 -C 6 cycloalkyl; and to the physiologically tolerated acid addition salts of there compounds. The invention also relates to a pharmaceuticaly composition that comprises at least one triazole compound of the formula (I) and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D 3 receptor antagonists or dopamine D 3 agonists, said method comprising administering an effective amount of at least one traizole compound or physiologically tolerated acid addition salt of the formula (I) to a subject in need thereof.
    • 本发明涉及式(I)化合物,其中n是1或2,Ar是在剩余的碳原子上带有自由基R 1的C结合的1,2,4-三唑基 和其中一个氮原子上的基团R 1a; R 1是氢,C 1 -C 6烷基,C 3 -C 6烷基,C 1 -C 6烷基,C 1 -C 6烷基, 氟化C 1 -C 6烷基,氟化C 1 -C 6烷基,C 1 -C 6烷基,C 1 -C 6烷基, 氟化C 1 -C 4烷氧基甲基或任选取代的苯基或5-或6位的C 1 -C 6烷基, 杂芳基; R 1a是氢或C 1 -C 4烷基; R 2是C 1 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基, 氟化C 1 -C 6烷基或氟化C 3 -C 6环烷基; 以及该化合物的生理耐受酸加成盐。 本发明还涉及包含至少一种式(I)的三唑化合物和/或其至少一种生理上耐受的酸加成盐的药物组合物,还涉及治疗有益于多巴胺D 3受体拮抗剂或多巴胺D 3激动剂,所述方法包括给受试者施用有效量的式(I)化合物或生理学耐受的酸加成盐, 需要。
    • 3. 发明申请
    • N-[(PIPERAZINYL)HETARYL]ARYLSULFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR
    • N - [(PIPERAZINYL)HETARYL]具有多巴胺D3受体亲和性的芳香酰胺化合物
    • WO2004089905A1
    • 2004-10-21
    • PCT/EP2004/003872
    • 2004-04-13
    • ABBOTT GMBH & CO. KGBRAJE, WilfriedHAUPT, AndreasLUBISCH, WilfriedGRANDEL, RolandDRESCHER, KarlaGENESTE, HervéUNGER, LilianeSAUER, Daryl, R.TURNER, Sean, C.
    • BRAJE, WilfriedHAUPT, AndreasLUBISCH, WilfriedGRANDEL, RolandDRESCHER, KarlaGENESTE, HervéUNGER, LilianeSAUER, Daryl, R.TURNER, Sean, C.
    • C07D213/76
    • C07D213/74C07D213/76C07D239/48C07D239/50C07D403/04C07D403/14C07D487/08
    • The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula (I ) in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents R a which is/are selected, independently of each other, from halogen, CN, NO 2 , C0 2 R 4 , COR 5 , C 1 -C 4 -alkyl and C 1 -C 4 -haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents R b , which is/are selected from halogen, NO 2 , CN, C0 2 R 4 , COR 5 , C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 4 -alkyl and C 1 -C 4 -haloalkyl, with it also being possible for two radicals R b which are bonded to adjacent C atoms of Ar to be together C 3 -C 4 -alkylene; R 1 is hydrogen, C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 4 -alkyl, C 1 -C 4 -hydroxyalkyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, C 3 -C 4 -alkenyl or C 3 -C 4 -alkynyl; with the radicals n, R 1 , R 2 , R 3 , R 4 and R 5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropriate together with physiologically acceptable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D 3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.
    • 本发明涉及通式(I)的N - [(哌嗪基)杂芳基]芳基磺酰胺化合物,其中Q是具有1或2个N原子作为环成员的二价,6元杂芳族基团,并且任选地带有一个或两个 取代基R a彼此独立地选自卤素,CN,NO 2,CO 2 R 4,COR 5,C 1 -C 4烷基和C 1 -C 4卤代烷基; Ar是苯基或6元杂芳族基,其具有1或2个N原子作为环成员,并且任选地带有一个或两个选自卤素,NO 2,CN,CO 2 R 4, COR 5,C 1 -C 6 - 烷基,C 2 -C 6 - 烯基,C 2 -C 6 - 炔基,C 3 -C 6 - 环烷基,C 3 -C 6 - 环烷基-C 1 -C 4烷基和C 1 -C 4卤代烷基, 对于与Ar的相邻C原子键合在一起为C 3 -C 4亚烷基的两个基团R b是可能的; R 1是氢,C 1 -C 4烷基,C 1 -C 4卤代烷基,C 3 -C 6环烷基,C 3 -C 6环烷基-C 1 -C 4烷基,C 1 -C 4羟烷基,C 1 -C 4烷氧基-C 1 C 1-4 - 烷基,C 3 -C 4 - 烯基或C 3 -C 4 - 炔基; 具有如专利权利要求中给出的含义的基团n,R 1,R 2,R 3,R 4和R 5与N-氧化物和生理上耐受的酸添加 这些化合物的盐和包含至少一种如权利要求1至10中任一项所述的N - [(哌嗪基)杂芳基]芳基磺酰胺化合物和/或至少一种I和/或N的生理上耐受的酸加成盐的药物组合物 氧化物,其中适当地与生理上可接受的载体和/或辅助物质一起用于治疗对由多巴胺D3受体拮抗剂或激动剂影响的疾病,特别是用于治疗中枢神经系统疾病和肾功能紊乱。
    • 5. 发明申请
    • AMINOMETHYL SUBSTITUTED BICYCLIC AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
    • 适用于治疗多巴胺D3受体调节障碍的氨基甲酸替代双相芳族化合物
    • WO2006040180A1
    • 2006-04-20
    • PCT/EP2005/011093
    • 2005-10-14
    • ABBOTT GMBH & CO. KGDRESCHER, KarlaHAUPT, AndreasUNGER, LilianeTURNER, Sean, C.BRAJE, WilfriedGRANDEL, Roland
    • DRESCHER, KarlaHAUPT, AndreasUNGER, LilianeTURNER, Sean, C.BRAJE, WilfriedGRANDEL, Roland
    • C07C317/34C07D209/14C07D209/62C07D235/14A61K31/136A61P25/00A61K31/145A61K31/403A61K31/407A61K31/4174
    • C07D471/04C07D209/14C07D209/62C07D235/14
    • The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula (I) wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR 8 , where R 8 is H, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl, C 1 -C 4 -alkylcarbonyl or fluorinated C 1 -C 4 -alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents R a , wherein the variable R a has the meanings given in the claims and in the description; X is a covalent bond or N-R 2 , CHR 2 , CHR 2 CH 2 , N or C-R 2 ; Y is N-R 2a , CHR 2a , CHR 2a CH 2 or CHR 2a CH 2 CH 2 ; is a single bond or a double bond; E is CH 2 or NR 3 ; R 1 is H, C 1 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -cycloalkylmethyl, C 3 -C 4 -alkenyl, fluorinated C 1 ­-C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -cycloalkylmethyl, fluorinated C 3 ­-C 4 -alkenyl, formyl or C 1 -C 3 -alkylcarbonyl; R 1a is H, C 1 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 ­-C 4 -cycloalkyl, fluorinated C 3 -C 4 -alkenyl, R 2 and R 2a each independently are H, CH 3 , CH 2 F, CHF 2 or CF 3 or R 1a and R 2 or R 1a and R 2a together are (CH 2 ) n with n being 1, 2 or 3; R 3 is H or C 1 -C 4 -alkyl; R 4 and R 5 independently of each other are H, C 1 -C 4 -alkyl, fluorinated C 1 -C 4 -alkyl or C 1 -C 4 ­-alkoxy or may form, together with N, a 4-, 5- or 6-membered saturated or unsaturated ring; R 6 and R 7 independently of each other are H or halogen; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
    • 本发明涉及式(I)的氨基甲基取代的双环芳族化合物,其中Ar是选自苯基,5-或6-元C-结合的杂芳族基团的环状基团,其包含作为环成员1,2 或3个彼此独立地选自O,S和N的杂原子和稠合于饱和或不饱和的5-或6-元碳环或杂环的苯环,其中杂环包含作为环成员1, 2或3个选自N,O和S的杂原子和/或1,2或3个含杂原子的基团,各自独立地选自NR 8,其中R 8是H, C 1 -C 4 - 亚烷基,氟化C 1 -C 4 - 烷基,C 1 -C 1-4烷基,C 1 -C 4烷基,C 1 -C 4 - 其中环状基团Ar可以带有1个碳原子的烷基羰基或氟化C 1 -C 4 - 烷基羰基, 2或3个取代基R a a,其中变量R a a具有在 声明和说明书; X是共价键或NR 2,CHR 2,CHR 2 CH 2,N或CR 2 ; Y是NR 2a,CHR 2,H 2,CH 2,CH 2或CHR 2 O 2, CH 2 CH 2 ; 是单键或双键; E是CH 2或NR 3; R 1是H,C 1 -C 4 - 烷基,C 3 -C 4 - C 3 -C 4 - 环烷基甲基,C 3 -C 4 - 亚烷基,C 3 -C 4 - 环烷基,C 3 -C 4 - 氟化C 1 -C 4 - 亚烷基,氟化C 3 -C 4 - 环烷基,氟化C -C 3 - 烷基羰基; R 1a是H,C 1 -C 4 - 烷基,C 3 -C 4烷基, C 3 -C 4 - 亚烷基,氟化C 1 -C 4 - 亚烷基,C 3 -C 4 - 氟化C 3 -C 4 - 环烷基,氟化C 3 -C 4 - 亚烯基,R SUP > 2和R 2a各自独立地为H,CH 3,CH 2,F,CHF 2, >或CF 3或R 1a和R 2或R 1a和R 2a和R 2b 一起是n为1,2或3的(CH 2)2 n。 R 3是H或C 1 -C 4 - 烷基; R 4和R 5彼此独立地为H,C 1 -C 4 - 烷基,氟化C C 1 -C 4 - 烷基或C 1 -C 4 - 烷氧基,或者可以与N, 4-,5-或6-元饱和或不饱和环; R 6和R 7彼此独立地为H或卤素; 及其生理上耐受的酸加成盐。 本发明还涉及式(I)化合物或其药学上可接受的盐在制备用于治疗易受多巴胺D3受体配体治疗的医学疾病的药物组合物中的用途。