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    • 3. 发明申请
    • METHOD FOR PREPARING 2H-NAPHTHO[1,8-cd]ISOTHIAZOLE-1,1-DIOXIDE
    • 制备2H-萘并[1,8-cd]异噻唑-1,1-二氧化物的方法
    • WO1997036884A1
    • 1997-10-09
    • PCT/FR1997000533
    • 1997-03-26
    • RHONE-POULENC RORER S.A.GRONDARD, LucHENRIET, Daniel
    • RHONE-POULENC RORER S.A.
    • C07D275/06
    • C07D275/06
    • A method for preparing colourless 2H-naphtho[1,8-cd]isothiazole-1,1-dioxide or 1,8-naphthosultam with a purity of more than 99 % by 8-amino-1-naphthalenesulphonic acid cyclisation using phosphoryl chloride in the presence of pyridine, wherein (a) 1.5-2 mol of phosphoryl chloride and 0.05-0.3 mol of pyridine are used per mole of 8-amino-1-naphthalenesulphonic acid in a backflow of toluene, (b) the reaction medium is poured onto an aqueous potash or soda solution and the aqueous and toluene phases are separated, (c) the aqueous phase from b is maintained at a pH of 6-8 and a temperature of 55-80 DEG C, then acidified, and the precipitate is separated, and (d) the raw product is treated with activated carbon in an organic solvent then separated.
    • 通过使用磷酰氯在8-氨基-1-萘磺酸环化中制备纯度大于99%的无色2H-萘并[1,8-cd]异噻唑-1,1-二氧化物或1,8-萘磺酸钠的方法 吡啶的存在,其中(a)在甲苯回流中每摩尔8-氨基-1-萘磺酸使用1.5-2摩尔磷酰氯和0.05-0.3摩尔吡啶,(b)将反应介质倒入 分离到水溶液或苏打溶液中,并分离水相和甲苯相,(c)b的水相保持在6-8的温度和55-80℃的温度,然后酸化,沉淀物为 分离,(d)将原料在有机溶剂中用活性炭处理然后分离。
    • 5. 发明申请
    • 5H,10H-IMIDAZO[1,2-a]INDENO[1,2-e]PYRAZINE-4-ONE DERIVATIVES, PREPARATION THEREOF AND DRUGS CONTAINING SAME
    • 5H,10H-咪唑并[1,2-a]茚并[1,2-e]吡嗪-4-酮衍生物,其制备方法和含有其的药物
    • WO1997025327A1
    • 1997-07-17
    • PCT/FR1997000018
    • 1997-01-06
    • RHONE-POULENC RORER S.A.DAMOUR, DominiqueHARDY, Jean-ClaudeMIGNANI, Serge
    • RHONE-POULENC RORER S.A.
    • C07D487/04
    • C07D487/04
    • Compounds of formula (I), wherein R is a hydrogen atom or a -COOH or CH2OH radical, R1 is a -CH-R2 radical, R2 is a 3-dimethyl-1H-pyrazole-4-yl, 4-chloro-1-methylimidazole-5-yl or 3-hydroxy-isoxazole-5-yl radical, except for 10-(1,3-dimethyl-1H-pyrazole-4-methylene)-5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, isomers thereof, salts thereof, the preparation thereof and drugs containing said compounds, are disclosed. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the alpha -amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor, and specifically ligands for NMDA receptor glycine modulator sites.
    • 式(I)化合物,其中R是氢原子或-COOH或CH 2 OH基团,R 1是-CH-R 2基团,R 2是3-二甲基-1H-吡唑-4-基,4-氯-1 - 甲基咪唑-5-基或3-羟基 - 异恶唑-5-基,除了10-(1,3-二甲基-1H-吡唑-4-亚甲基)-5H,10H-咪唑并[1,2-a] 茚并[1,2-e]吡嗪-4-酮,其异构体,其盐,其制备方法和含有所述化合物的药物。 式(I)化合物具有有价值的药理学性质,也是也称为quisqualate受体的α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体的拮抗剂。 此外,式(I)化合物是N-甲基-D-天冬氨酸(NMDA)受体的非竞争性拮抗剂,特别是NMDA受体甘氨酸调节剂位点的配体。
    • 7. 发明申请
    • NOVEL TAXOIDS, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    • 新型紫杉醇,其制备方法及含有其的药物组合物
    • WO1997023472A1
    • 1997-07-03
    • PCT/FR1996002030
    • 1996-12-19
    • RHONE-POULENC RORER S.A.BOUCHARD, HervéCOMMERÇON, Alain
    • RHONE-POULENC RORER S.A.
    • C07D305/14
    • C07D305/14
    • Novel taxoids of general formula (I), the preparation thereof and pharmaceutical compositions containing same, are disclosed. In general formula (I), Z is a hydrogen atom or a radical of general formula (II), wherein R1 is an optionally substituted benzoyl, furoyl or thenoyl radical or a radical R2-O-CO- where R2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted phenyl or heterocyclyl radical; R3 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, naphthyl or aromatic heterocyclic radical; and R4 is a hydrogen atom or a hydroxy radical or an alkoxy, alkenyloxy, optionally substituted alkynyloxy, alkanoyloxy, alkenoyloxy, alkynoyloxy, cycloalkanoyloxy, aroyloxy, alkoxyacetyl, alkylthioacetyl, alkyloxycarbonyloxy radical, or a cycloalkyloxy, cycloalkenyloxy, carbamoyloxy, alkylcarbamoyloxy or dialkylcarbamoyloxy radical. The novel products of general formula (I), wherein Z is a radical of general formula (II), have remarkable antitumoral and antileukemic properties.
    • 公开了通式(I)的新型紫杉烷,其制备方法和含有其的药物组合物。 在通式(I)中,Z是氢原子或通式(II)的基团,其中R 1是任选取代的苯甲酰基,糠基或过氧基或基团R 2 -O-CO-,其中R 2是烷基,烯基 ,炔基,环烷基,环烯基,双环烷基,任选取代的苯基或杂环基; R3是烷基,烯基,炔基,环烷基,环烯基,苯基,萘基或芳族杂环基; 烷氧基乙酰基,烷基硫代乙酰基,烷氧基羰基氧基或环烷氧基,环烯基氧基,氨基甲酰氧基,烷基氨基甲酰氧基或二烷基氨基甲酰氧基,其中R 4为氢原子或羟基或烷氧基,链烯氧基,任选取代的炔氧基,烷酰氧基,烯酰氧基,炔酰氧基,环烷酰氧基。 通式(I)的新产物,其中Z为通式(II)的基团,具有显着的抗肿瘤和抗白血病性质。
    • 9. 发明申请
    • NOVEL INDANE DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    • 新型衍生物,其制备方法和含有其的药物组合物
    • WO1997021657A1
    • 1997-06-19
    • PCT/FR1996001910
    • 1996-12-02
    • RHONE-POULENC RORER S.A.BOUCHARD, HervéCOMMERÇON, Alain
    • RHONE-POULENC RORER S.A.
    • C07C49/753
    • C07C323/16C07C43/23C07C45/62C07C45/78C07C49/753C07C69/013C07C69/017C07C2602/08
    • Novel indane derivatives of general formula (I), the preparation thereof, and pharmaceutical compositions containing same, are disclosed. In general formula (I), R1 is ethyl or vinyl, R1a is H, R3a is H, R3b is H ( alpha or beta ), R4 is OH or alkanoyloxy, R4a is H, or R4 and R4a together form a ketone function, R5 and R5a are H, R6 is H or OH, R6a is H, R7 is optionally substituted methyl, R7a is H or R7 and R7a together form a methylene radical, R7b is H (with relative configuration beta ) and R8 is OH, alkoxy or alkanoyloxy, with the proviso that when R4 is OH and R4a is H, or R4 and R4a together form a ketone function, R7 and R7a together form a methylene radical, R7 is optionally substituted methyl and R7a is H, then R5a and R6a may together form a bond, and when R7 is optionally substituted methyl, R6 is OH and R4 is OH or alkanoyloxy, then R3b-R4a, R5a-R6a and R7a-R7b each form a bond. Said novel derivatives have remarkable antitumoral and antileleucémiques properties.
    • 公开了通式(I)的新型二氢化茚衍生物,其制备方法和含有其的药物组合物。 在通式(Ⅰ)中,R1是乙基或乙烯基,R1a是H,R3a是H,R3b是H(α或β),R4是OH或烷酰氧基,R4a是H或R4和R4a一起形成酮官能团, R5和R5a是H,R6是H或OH,R6a是H,R7是任选取代的甲基,R7a是H或R7,R7a一起形成亚甲基,R7b是H(具有相对构型β),R8是OH,烷氧基 或烷酰氧基,条件是当R4为OH且R4a为H时,或R4和R4a一起形成酮官能团时,R7和R7a一起形成亚甲基,R7为任选取代的甲基,R7a为H,则R5a和R6a可以 一起形成键,当R 7为任选取代的甲基时,R 6为OH,R 4为OH或烷酰氧基,则R 3b,R 4a,R 5a,R 6a和R 7aa-R 7b各自形成键。 所述新型衍生物具有显着的抗肿瘤和抗粘液性。