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    • 7. 发明申请
    • BENSOQUINOLIZINE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME
    • 苯并喹啉衍生物及其生产方法
    • WO00006572A1
    • 2000-02-10
    • PCT/JP1999/004035
    • 1999-07-28
    • C07D471/06A61K31/435A61P1/00A61P1/02A61P1/04A61P1/08A61P11/00A61P13/02A61P15/00A61P25/04A61P29/00A61P43/00C07D455/04A61K31/47
    • C07D455/04
    • Benzoquinolizine derivatives having tachykinin antagonism, in particular, substance P receptor antagonism. Namely, benzoquinolizine derivatives represented by general formula (1) and salts thereof and medicinal compositions containing these compounds or pharmaceutically useful salts thereof. In said formula, R , R and R are the same or different and each represents hydrogen or C1-6 alkyl; the ring A is a homocycle or a heterocycle optionally having 1 to 3 substituents selected independently (wherein 2 substituents adjacent to each other may be bonded together to form a ring); the ring B is a benzene ring optionally having 1 to 5 substituents (wherein 2 substituents adjacent to each other may be bonded together to form a ring); and the ring C is a benzene ring optionally having 1 to 3 substituents (wherein 2 substituents adjacent to each other may be bonded together to form a ring).
    • 具有速激肽拮抗作用的苯并喹嗪衍生物,特别是P受体拮抗作用。 即,由通式(1)表示的苯并喹嗪衍生物及其盐和含有这些化合物的药物组合物或其药学上有用的盐。 在所述式中,R 1,R 2和R 3相同或不同,各自表示氢或C 1-6烷基; 环A是任选具有1至3个独立选择的取代基的杂环或杂环(其中彼此相邻的2个取代基可以键合在一起形成环); 环B是任选具有1至5个取代基的苯环(其中彼此相邻的2个取代基可以键合在一起形成环); 并且环C是任选具有1至3个取代基的苯环(其中彼此相邻的2个取代基可以键合在一起形成环)。
    • 9. 发明申请
    • BENZOQUINOLIZINE DERIVATIVES AND MEDICINAL COMPOSITIONS
    • 苯并喹啉衍生物和药物组合物
    • WO1997040046A1
    • 1997-10-30
    • PCT/JP1997001320
    • 1997-04-17
    • NIPPON SHINYAKU CO., LTD.YAMAMOTO, OsamuSHIROUCHI, Yoshiaki
    • NIPPON SHINYAKU CO., LTD.
    • C07D455/04
    • C07D455/06A61K31/473C07D455/04
    • Benzoquinolizine derivatives represented by general formula (1), pharmaceutically acceptable salts thereof and medicinal compositions containing the same as the active ingredients, wherein R represents hydroxy or alkoxy; R represents hydrogen, hydroxy or alkoxy; R represents alkyl optionally substituted by hydroxy, alkoxy, amino, monoalkylamino or dialkylamino; and R represents alkyl optionally substituted by hydroxy or alkoxy, aryl optionally sustituted by alkyl, halogeno, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino, monoalkylamino or dialkylamino. Because of being capable of regulating the gastro-intestinal tract motion, these compounds are efficacious in the treatment of irritable bowel syndrome.
    • 由通式(1)表示的苯并喹嗪衍生物,其药学上可接受的盐和含有与活性成分相同的药物组合物,其中R 1表示羟基或烷氧基; R 2表示氢,羟基或烷氧基; R 3表示任选被羟基,烷氧基,氨基,单烷基氨基或二烷基氨基取代的烷基; 并且R 4表示任选被羟基或烷氧基取代的烷基,任选被烷基,卤代,羟基,烷氧基,氨基,单烷基氨基或二烷基氨基,单烷基氨基或二烷基氨基取代的芳基。 由于能够调节胃肠道运动,这些化合物对肠易激综合征的治疗是有效的。
    • 10. 发明申请
    • QUINOLONES AND THEIR THERAPEUTIC USE
    • 喹诺酮及其治疗用途
    • WO1997031000A1
    • 1997-08-28
    • PCT/GB1997000492
    • 1997-02-21
    • CHIROSCIENCE LIMITED
    • CHIROSCIENCE LIMITEDHAUGHAN, Alan, FindlayBEASLEY, Steven, ColinMONTANA, John, GaryWATSON, Robert, John
    • C07D455/04
    • C07D455/04
    • A compound of formula (I) wherein n is an integer of up to 3; R represents cycloalkyl, aryl, heteroaryl or heterocyclo, any of which rings may be fused to a second ring selected from aryl, heteroaryl, to give a bicyclic structure, and in which the or each ring is optionally substituted by one or more substituents chosen from halo, C1-6 alkoxy, hydroxy, CN, CO2H (or C1-6 alkyl esters or C1-6 alkyl amides thereof), C1-6 alkyl, NR R and SO2NR R ; R , R and R are the same or different and represent H, halo, C1-6 alkoxy, hydroxy, CN, CO2H (or C1-6 alkyl esters or C1-6 alkyl amides thereof), NR R , SO2NR R or C1-6 alkyl in which alkyl is optionally substituted with halo, C1-6 alkoxy, hydroxy, CN, CO2H (or C1-6 alkyl esters or C1-6 alkyl amides thereof), NR R7 or SO2NR R , or any adjacent two substituents R -R are joined to form an optionally substituted carbocyclic aromatic, heteroaromatic, saturated carbocyclic or heterocyclic ring; R and R are the same or different and represent H, C1-6 alkyl, cycloalkyl, C1-6 alkylcarbonyl, arylcarbonyl, C1-6 alkoxycarbonyl, arylsulphonyl or C1-6 alkylsulphonyl, or NR R is a 5- or 6-membered ring such as pyrrolidine, piperidine, morpholine or piperazine; X represents a linking group selected from -(CR R )2-3-, -Y-(CR R )2-, -(CR R )2-Y-, -CR R -Y-CR R - and -Y-CR R -Z-, Y and Z being independently NR , O or S(O)0-2, provided that Y and Z are not both S(O)0-2; Q represents O or S; each R , each R and R are the same or different and are H or C1-6 alkyl; or a pharmaceutically-acceptable salt, solvate or hydrate thereof.
    • 式(I)的化合物,其中n为至多3的整数; R 1表示环烷基,芳基,杂芳基或杂环,其中任一个可以与选自芳基,杂芳基的第二个环稠合,得到双环结构,并且其中该环或每个环任选地被一个或多个 选自卤素,C 1-6烷氧基,羟基,CN,CO 2 H(或其C 1-6烷基酯或其C 1-6烷基酰胺),C 1-6烷基,NR 6 R 7和SO 2 NR 6 R <7>; R 3,R 4和R 5相同或不同,表示H,卤素,C 1-6烷氧基,羟基,CN,CO 2 H(或其中C 1-6烷基酯或C 1-6烷基酰胺) ,NR 6 R 7,SO 2 NR 6 R 7或C 1-6烷基,其中烷基任选被卤素,C 1-6烷氧基,羟基,CN,CO 2 H(或C 1-6烷基酯或 C 6烷基酰胺),NR 6 R 7或SO 2 NR 6 R 7或任何相邻的两个取代基R 3 -R 5连接形成任选取代的碳环芳族杂芳族饱和 碳环或杂环; R 6和R 7相同或不同,表示H,C 1-6烷基,环烷基,C 1-6烷基羰基,芳基羰基,C 1-6烷氧基羰基,芳基磺酰基或C 1-6烷基磺酰基,或NR 6 R 7是5-或6-元环,例如吡咯烷,哌啶,吗啉或哌嗪; 2-(CR 9 R 10)) - (CR 9 R 10)2 - , - (CR 9 R 10) 2-Y-,-CR 9 R 10 -Y-CR 9 R 10和-Y-CR 9 R 10 -Z-,Y和Z独立地是NR 11 >,O或S(O)0-2,条件是Y和Z不同时为S(O)0-2; Q表示O或S; 每个R 9,每个R 10和R 11相同或不同,为H或C 1-6烷基; 或其药学上可接受的盐,溶剂合物或水合物。