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    Indole derivatives and their use for the treatment of osteoporosis amongst other applications
    3.
    发明授权
    Indole derivatives and their use for the treatment of osteoporosis amongst other applications 失效
    吲哚衍生物及其在其他应用中用于治疗骨质疏松症的用途

    公开(公告)号：US06787550B1

    公开(公告)日：2004-09-07

    申请号：US10018443

    申请日：2001-12-12

    申请人： Carlo Farina ,  Stefania Gagliardi ,  Pietro A. Novella

    发明人： Carlo Farina ,  Stefania Gagliardi ,  Pietro A. Novella

    IPC分类号： C07D40112

    CPC分类号： C07D209/18 ,  C07D401/12 ,  C07D403/12

    摘要： A compound of formula (1) or a salt thereof, or a solvate thereof, wherein; R1 and R2 each independently represents C1-6alkoxy or halo; R3 and R4 each independently represents hydrogen, C1-6alkoxy, arylC1-6alkoxy, hydroxy, carboxyC1-6alkoxy, hydroxyC1-6alkoxy, dihydroxyC1-6alkoxy, mono- and di-(C1-6alkyl)aminoC1-6alkoxy or aminoC1-6alkoxy, and; R5 represents —NRsRt wherein Rs and Rt each independently represent hydrogen, unsubstituted or substituted C1-6alkyl, or unsubstituted or substituted heterocyclyl, a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of the compound or composition in medicine.

    摘要翻译： 式（1）的化合物或其盐或其溶剂合物，其中：R 1和R 2各自独立地表示C 1-6烷氧基或卤素; R 3和R 4各自独立地表示氢，C 1-6烷氧基，芳基C 1-6烷氧基，羟基，羧基C 1 1-6烷氧基，羟基C 1-6烷氧基，二羟基C 1-6烷氧基，单 - 和二 - （C 1-6烷基）氨基C 1-6烷氧基或氨基C 1-6烷氧基，和R 5表示-NR s R t，其中R 5和R t各自独立地表示氢，未取代或取代的C 1-6烷基 ，或未取代或取代的杂环基，制备这种化合物的方法，含有这种化合物的药物组合物和药物中化合物或组合物的用途。

    Quinoline Derivatives as NK-3 and NK-2 Antagonists
    4.
    发明申请
    Quinoline Derivatives as NK-3 and NK-2 Antagonists 审中-公开
    喹啉衍生物作为NK-3和NK-2拮抗剂

    公开(公告)号：US20070015766A1

    公开(公告)日：2007-01-18

    申请号：US11426414

    申请日：2006-06-26

    申请人： Carlo Farina ,  Stefania Gagliardi ,  Giuseppe Giardina ,  Mario Grugni ,  Marisa Martinelli ,  Guy Marguerite Marie Gerard Nadler

    发明人： Carlo Farina ,  Stefania Gagliardi ,  Giuseppe Giardina ,  Mario Grugni ,  Marisa Martinelli ,  Guy Marguerite Marie Gerard Nadler

    IPC分类号： A61K31/496 ,  C07D403/02

    CPC分类号： C07D401/12 ,  C07D215/52

    摘要： Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: wherein: R1 is H or alkyl; R2 is aryl, cycloalkyl or heteroaryl; R3 is H or C1-3 alkyl, optionally substituted by one or more fluorines; R4 is H, R8NR9R10, R11R13 or R11R12R13; or R5 is branched or linear alkyl, cycloalkyl, aryl, arylalkyl, or a single or fused ring aromatic heterocyclic group; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and the use of such compounds and composition in medicine.

    摘要翻译： 某些下式（I）化合物或其药学上可接受的盐或水合物：其中：R 1是H或烷基; R 2是芳基，环烷基或杂芳基; R 3是H或C 1-3烷基，任选被一个或多个氟取代; R 4是H，R 8 NR 9 R 10，R 11 R 13或13个R 12 R 13 13; 或R 5是支链或直链烷基，环烷基，芳基，芳烷基或单或稠环芳族杂环基; 制备这些化合物的方法，包含这些化合物的药物组合物和这些化合物的用途以及这些化合物和组合物在医药中的用途。

    Indole derivatives for the treatment of osteoporosis
    7.
    发明授权
    Indole derivatives for the treatment of osteoporosis 失效
    吲哚衍生物用于治疗骨质疏松症

    公开(公告)号：US06903117B2

    公开(公告)日：2005-06-07

    申请号：US10300332

    申请日：2002-11-20

    申请人： Carlo Farina ,  Stefania Gagliardi ,  Guy Marguerite Marie Gerard Nadler

    发明人： Carlo Farina ,  Stefania Gagliardi ,  Guy Marguerite Marie Gerard Nadler

    IPC分类号： B82B1/00 ,  C07D209/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D451/02 ,  C07D451/04 ,  C07D455/02 ,  C07D471/04 ,  C07D471/08 ,  C07D471/16 ,  A61K31/454

    CPC分类号： C07D451/02 ,  C07D209/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D451/04 ,  C07D455/02 ,  C07D471/04 ,  C07D471/08

    摘要： A compound of formula (I): or a salt thereof, or a solvate thereof, wherein Ra represents a group R5 which is hydrogen, alkyl or optionally substituted aryl and Rb represents a moiety of formula (a): wherein X represents a hydroxy or an alkoxy group wherein the alkyl group may be substitued or unsubstituted or X represents a group NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclic group; R1 represents an alkyl or a substituted or unsubstituted aryl group; and R2, R3 and R4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R6 and R7 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R6 and R7 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R8 represents hydrogen, hydroxy, alkynoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalky, carbalkoxyalkyl, carbamoyl or aminosulphonyl; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.

    摘要翻译： 式（I）化合物或其盐或其溶剂合物，其中R a表示R 5基团，其为氢，烷基或任选取代的芳基，R b表示式（a ）：其中X表示羟基或烷氧基，其中烷基可以被取代或未被取代，或X表示基团NR 1 R t R 3和R 3各自独立地表示氢，烷基，取代的烷基，任选取代的烯基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环基或任选取代的杂环基烷基， 和它们所连接的氮一起形成杂环基; R 1表示烷基或取代或未取代的芳基; 和R 2，R 3和R 4各自独立地表示氢，烷基，芳基或取代的芳基; R 6和R 7各自独立地表示氢，羟基，氨基，烷氧基，任选取代的芳氧基，任选取代的苄氧基，烷基氨基，二烷基氨基，卤素，三氟甲基，三氟甲氧基，硝基， 烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基或R 6和R 7一起代表亚甲二氧基，羰基二氧基或羰基二氨基; R 8表示氢，羟基，炔酰基，烷基，氨基烷基，羟基烷基，羧基，烷氧基烷基，氨基甲酰基或氨基磺酰基; 制备这种化合物的方法，含有这种化合物的药物组合物和这种化合物在医药中的用途。

    Heteroaromatic pentadienoic acid derivatives useful as inhibitors of bone resorption
    8.
    发明授权
    Heteroaromatic pentadienoic acid derivatives useful as inhibitors of bone resorption 失效
    可用作骨吸收抑制剂的杂芳族戊二烯酸衍生物

    公开(公告)号：US6025390A

    公开(公告)日：2000-02-15

    申请号：US214689

    申请日：1999-06-23

    申请人： Carlo Farina ,  Stefania Gagliardi ,  Guy Marguerite Marie Gerard Nadler ,  Michel Jean Roger Martin

    发明人： Carlo Farina ,  Stefania Gagliardi ,  Guy Marguerite Marie Gerard Nadler ,  Michel Jean Roger Martin

    IPC分类号： A61K31/343 ,  A61K31/381 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/47 ,  A61P19/10 ,  C07D215/12 ,  C07D307/80 ,  C07D333/60 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  A61K31/34 ,  A61K31/38 ,  A61K31/445 ,  C07D215/00 ,  C07D401/00

    CPC分类号： C07D405/06 ,  C07D215/12 ,  C07D307/80 ,  C07D333/60 ,  C07D409/06

    摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, ##STR1## wherein: R.sub.1 represents an alkyl group or a substituted or unsubstituted aryl group; R.sub.2, R.sub.3 and R.sub.4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R.sub.5 and R.sub.6 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R.sub.5 and R.sub.6 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; X represents a hydroxy or an alkoxy group wherein the alkyl group may be substituted or unsubstituted or X represents a group NR.sub.S R.sub.t wherein R.sub.S and R.sub.t each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or R.sub.S and R.sub.t together with the nitrogen to which they are attached form a heterocyclic group; and Y represents O or S and Z represents CH, CH.dbd.CH or N; or Y represents NR.sub.7 wherein R.sub.7 represents hydrogen, hydroxy, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or aminosulphonyl and Z represents CH.dbd.CH or N; a pharmaceutical composition containing such a compound, a process for preparing such a compound and the use of such a compound in medicine.

    摘要翻译： PCT No.PCT / EP97 / 03709 Sec。 371日期1999年6月23日第 102（e）1999年6月23日PCT 1997年7月7日PCT公布。 出版物WO98 / 01436 日期1998年1月15日A式（I）化合物或其盐或其溶剂化物，其中：R1表示烷基或取代或未取代的芳基; R2，R3和R4各自独立地表示氢，烷基，芳基或取代的芳基; R5和R6各自独立地表示氢，羟基，氨基，烷氧基，任选取代的芳氧基，任选取代的苄氧基，烷基氨基，二烷基氨基，卤素，三氟甲基，三氟甲氧基，硝基，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基或R5和R6一起代表 亚甲二氧基，羰基二氧基或羰基二氨基; X表示羟基或烷氧基，其中烷基可以是取代或未取代的或X表示NRSRt基团，其中RS和Rt各自独立地表示氢，烷基，取代的烷基，任选取代的烯基，任选取代的芳基，任选取代的芳基烷基， 任选取代的杂环基或任选取代的杂环基烷基，或RS和R R与它们所连接的氮一起形成杂环基; Y表示O或S，Z表示CH，CH = CH或N; 或Y表示NR 7，其中R 7表示氢，羟基，烷酰基，烷基，氨基烷基，羟基烷基，羧基烷基，烷氧基烷基，氨基甲酰基或氨基磺酰基，Z表示CH = CH或N; 含有这种化合物的药物组合物，这种化合物的制备方法和这种化合物在医药中的应用。