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    • 7. 发明授权
    • Piperidinylmethyloxazolidinones
    • 哌啶基甲基恶唑烷酮
    • US5714502A
    • 1998-02-03
    • US701852
    • 1996-08-23
    • Helmut PrucherGerd Bartoszyk
    • Helmut PrucherGerd Bartoszyk
    • A61K31/422A61K31/435A61K31/445A61K31/4523A61P9/12A61P25/00A61P25/04A61P25/18A61P25/20A61P25/24A61P25/26C07D263/18C07D295/00C07D413/06
    • C07D413/06
    • The invention relates to novel piperidinylmethyloxazolidin-2-one derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 in each case independently of one another are unsubstituted or mono- to disubstituted phenyl radicals whose substituents can be A, OA, aryloxy having 6-10 C atoms, aralkyloxy having 7-11 C atoms, --O--(CH.sub.2).sub.n --O-- (bonded in directly adjacent positions or in the meta- or para-position to one another on the phenyl ring), --O--(CH.sub.2).sub.n --OH, Hal, CF.sub.3, OH, NO.sub.2, NH.sub.2, NHA, NA.sub.2, NHR.sup.3, NAR.sup.3, SO.sub.2 NH.sub.2, SO.sub.2 NHA, SO.sub.2 NA.sub.2, SO.sub.2 NHR.sup.3 (excluding R.sup.3 =SO.sub.2 A) , SO.sub.2 N (R.sup.3).sub.2 (excluding R.sup.3 =SO.sub.2 A) or R.sup.3, R.sup.3 is COH, CO-alkyl having 1-7 C atoms in the alkyl, CO-alkyl-Ar having 8-12 C atoms, CO-Ar having 7-13 C atoms, SO.sub.2 A A is an alkyl radical having 1-6 C atoms n is 1 or 2 Hal is F, Cl, Br or I and their physiologically acceptable salts.
    • 本发明涉及式I(I)的新颖的哌啶基甲基恶唑烷-2-酮衍生物,其中R 1和R 2各自独立地是未取代的或被单取代或被取代的苯基,其取代基可以是A,OA, 具有6-10个碳原子的芳氧基,具有7-11个碳原子的芳烷氧基,-O-(CH 2)n O-(在苯环的直接相邻位置或彼此间位置或对位键合),-O - (CH2)n-OH,Hal,CF3,OH,NO2,NH2,NHA,NA2,NHR3,NAR3,SO2NH2,SO2NHA,SO2NA2,SO2NHR3(不包括R3 = SO2A),SO2N(R3)2(不包括R3 = )或R3,R3是COH,在烷基中具有1-7个C原子的CO-烷基,具有8-12个C原子的CO-烷基-Ar,具有7-13个C原子的CO-Ar,SO2A A是具有 1-6个碳原子,n为1或2个Hal为F,Cl,Br或I及其生理上可接受的盐。
    • 9. 发明授权
    • Benzylpiperidine derivatives
    • 苄基哌啶衍生物
    • US5698553A
    • 1997-12-16
    • US550105
    • 1995-10-30
    • Helmut PrucherRudolf GottschlichJoachim LeibrockHarry Schwartz
    • Helmut PrucherRudolf GottschlichJoachim LeibrockHarry Schwartz
    • C07D413/12A61K31/4427A61K31/445A61K31/454A61K31/4545A61K31/47A61P9/10A61P25/00A61P25/04A61P25/18A61P25/28A61P43/00C07D401/06C07D401/12C07D403/12C07D413/06C07D417/06
    • C07D401/06C07D413/06C07D417/06
    • A benzylpiperidine compound of formula I ##STR1## in which R.sup.1 is H, Hal or nitro, R.sup.2 is a benzyl group, which is unsubstituted or substituted by Hal on the aromatic portion, in the 2-, 3- or 4-position of the piperidine ring, with the proviso that R.sup.2 is not in the 4-position if X is --CO--, Y and Z are --CH.sub.2 and R.sup.1 is H, R.sup.3 is H or A, X is --O--, --S--, --NH--, --CO-- or --SO.sub.2 --, Y is --CH.sub.2 --, --NH--, --O--, --S--, --NH-- or alternatively --CO-- if X is --CO-- and Z is --NH-- or --NA--, Z is --CH.sub.2 --, --C(A).sub.2-, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CO--, --NH--, --NA--, --O--, --S-- or a bond, wherein X--Y or Y--Z is not --O--, --S--S--, --NH--O--, --O--NH--, --NH--NH--, --O--S-- or --S--O, A is alkyl having 1-6 C atoms, B is O or both H and OH, i.e., ##STR2## together with the carbon atom to which B is bonded, Hal is F, Cl, Br or I and n is 0, 1 or 2 or a physiologically acceptable salt thereof, and their salts show a high affinity for binding sites of amino acid receptors and are suitable for the treatment of neurodegenerative disorders.
    • 式I的苄基哌啶化合物其中R 1是H,Hal或硝基,R 2是未取代的或被芳族部分上的Hal取代的苄基,在2-,3-或4- 哌啶环的位置,条件是如果X是-CO-,则R2不在4-位,Y和Z是-CH2,R1是H,R3是H或A,X是-O - , - S - ,-NH-,-CO-或-SO 2 - ,Y是-CH 2 - , - NH - , - O - , - S - , - NH-或者-CO-,如果X是-CO-,Z是 - NH-或-NH-,Z是-CH 2 - , - C(A)2 - , - CH 2 CH 2 - , - CH = CH-,-CO-,-NH-,-NA-,-O-,-S- 或键,其中XY或YZ不是-O-,-SS-,-NH-O-,-O-NH-,-NH-NH-,-OS-或-SO,A是具有1-6个 C原子,B为O或H和OH两者,即,与IMA键合的碳原子一起,Hal为F,Cl,Br或I,n为0,1或2,或生理上可接受的盐 并且其盐对氨基酸受体的结合位点显示出高亲和力,并且适用于治疗神经变性疾病。