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    USE OF DIMIRACETAM IN THE TREATMENT OF CHRONIC PAIN
    1.
    发明申请
    USE OF DIMIRACETAM IN THE TREATMENT OF CHRONIC PAIN 有权
    二甲双胍在治疗慢性疼痛中的应用

    公开(公告)号：US20110251250A1

    公开(公告)日：2011-10-13

    申请号：US13166088

    申请日：2011-06-22

    申请人： Carlo FARINA ,  Carla Ghelardini ,  Paola Petrillo

    发明人： Carlo FARINA ,  Carla Ghelardini ,  Paola Petrillo

    IPC分类号： A61K31/4188 ,  A61P25/04 ,  A61P19/02

    CPC分类号： A61K31/7068 ,  A61K31/4188 ,  A61K31/555 ,  A61K45/06 ,  A61K2300/00

    摘要： The use of dimiracetam in the treatment of chronic pain is disclosed. At doses higher than those previously disclosed in relation with its cognition enhancing activity (i.e. amelioration of learning and memory), dimiracetam was able to completely revert hyperalgesia or allodynia associated with several animal models of chronic pain. Dimiracetam showed high activity in iatrogenic neuropathies associated with antiviral and chemotherapeutic drug treatments and in painful conditions caused by osteoarthritis. In addition, dimiracetam was devoid of toxicity even at doses 10-fold higher than the highest therapeutic dose. The possibility of treating such debilitating pathologies with a highly effective and essentially non-toxic compound is therefore disclosed.

    摘要翻译： 公开了使用二拉西坦治疗慢性疼痛。 在比以前公开的与其认知增强活性（即改善学习和记忆）相比更高的剂量下，双拉西坦能够完全恢复与慢性疼痛的几种动物模型相关的痛觉过敏或异常性疼痛。 二西拉西坦在与抗病毒和化疗药物治疗相关的医源性神经病变以及由骨关节炎引起的疼痛状况下表现出高活性。 此外，即使在比最高治疗剂量高10倍的剂量下，二西拉坦也没有毒性。 因此公开了用高效和基本上无毒化合物治疗这种衰弱病态的可能性。

    Use of dimiracetam in the treatment of chronic pain
    2.
    发明授权
    Use of dimiracetam in the treatment of chronic pain 有权
    使用双拉西坦治疗慢性疼痛

    公开(公告)号：US07989421B2

    公开(公告)日：2011-08-02

    申请号：US12450944

    申请日：2008-04-15

    申请人： Carlo Farina ,  Carla Ghelardini ,  Paola Petrillo

    发明人： Carlo Farina ,  Carla Ghelardini ,  Paola Petrillo

    IPC分类号： A61K31/44 ,  A61K31/40 ,  A61P23/00

    CPC分类号： A61K31/7068 ,  A61K31/4188 ,  A61K31/555 ,  A61K45/06 ,  A61K2300/00

    摘要： The use of dimiracetam in the treatment of chronic pain is disclosed. At doses higher than those previously disclosed in relation with its cognition enhancing activity (i.e. amelioration of learning and memory), dimiracetam was able to completely revert hyperalgesia or allodynia associated with several animal models of chronic pain. Dimiracetam showed high activity in iatrogenic neuropathies associated with antiviral and chemotherapeutic drug treatments and in painful conditions caused by osteoarthritis. In addition, dimiracetam was devoid of toxicity even at doses 10-fold higher than the highest therapeutic dose. The possibility of treating such debilitating pathologies with a highly effective and essentially non-toxic compound is therefore disclosed.

    摘要翻译： 公开了使用二拉西坦治疗慢性疼痛。 在比以前公开的与其认知增强活性（即改善学习和记忆）相比更高的剂量下，二西拉坦能够完全恢复与慢性疼痛的几种动物模型相关的痛觉过敏或异常性疼痛。 二西拉西坦在与抗病毒和化疗药物治疗相关的医源性神经病变以及由骨关节炎引起的疼痛状况下表现出高活性。 此外，即使在比最高治疗剂量高10倍的剂量下，二西拉坦也没有毒性。 因此公开了用高效和基本上无毒化合物治疗这种衰弱病态的可能性。

    Indole derivatives for the treatment of osteoporosis
    8.
    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
    9.
    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。

    Pyridazine derivatives
    10.
    发明授权
    Pyridazine derivatives 失效
    哒嗪衍生物

    公开(公告)号：US5082939A

    公开(公告)日：1992-01-21

    申请号：US384947

    申请日：1989-07-25

    申请人： Carlo Farina ,  Mario Pinza ,  Alberto Cerri ,  Francesco Parravicini

    发明人： Carlo Farina ,  Mario Pinza ,  Alberto Cerri ,  Francesco Parravicini

    IPC分类号： C07D237/22

    CPC分类号： C07D237/22

    摘要： A novel process for preparing alkoxyalkylidenehydrazinopyridazine derivatives which comprises reducing a novel alkoxytriphenylmethylazopyridazine derivative, removing the triphenylmethyl group and reacting with an aldehyde or ketone derivative.A specific compound produced by this process is 3-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-2-hydroxypropoxy]-6-isopropylidenehydrazinopyridazine.

    摘要翻译： 制备烷氧基亚烷基肼哒嗪衍生物的新方法，包括还原新的烷氧基三苯基甲基偶氮哒嗪衍生物，除去三苯基甲基并与醛或酮衍生物反应。 通过该方法制备的具体化合物是3- [3 - [[2-（3,4-二甲氧基苯基）乙基]氨基] -2-羟基丙氧基] -6-异丙基亚肼基哒嗪。