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    AZOLE COMPOUNDS USED AS TUBERCULOSTATIC AND LEISHMANICIDE AGENTS
    1.
    发明申请
    AZOLE COMPOUNDS USED AS TUBERCULOSTATIC AND LEISHMANICIDE AGENTS 有权
    用作溶液和稀土助剂的AZOLE化合物

    公开(公告)号：US20110269803A1

    公开(公告)日：2011-11-03

    申请号：US12981315

    申请日：2010-12-29

    申请人： Nubia Boechat ,  Marilia dos Santos Costa ,  Maria Cristina da Silva Lourenco ,  Ivan Neves, JR. ,  Marcelo da Silva Genestra ,  Vitor Francisco Ferreira

    发明人： Nubia Boechat ,  Marilia dos Santos Costa ,  Maria Cristina da Silva Lourenco ,  Ivan Neves, JR. ,  Marcelo da Silva Genestra ,  Vitor Francisco Ferreira

    IPC分类号： A61K31/4192 ,  A61P31/06 ,  C07D249/06 ,  C07D233/88 ,  A61K31/4172

    CPC分类号： A61K31/4192 ,  C07D233/90 ,  C07D249/06

    摘要： This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII. where: X is an atom of “C” or “N” where X is “N” the radicals do triazole ring are represented by: R1=COR2, CSR3, CN(R4)R5 or CF2R6; R2=H, NHNH2, alkyl, aryl substituted or not, OH, NR7R8 or OR9 R3=alkyl or aryl substituted or not R4=H, OH, alkyl or aryl substituted or not R5=R6=R7=R8=R9=R10=H, alkyl or aryl substituted or not where X is “C” the radicals do imidazolic ring are represented by: R1=COR2 R2=NHNH2, OH, OR3, or NR4R5 R3=alkyl or aryl substituted or not R4=R5=H, alkyl or aryl substituted or not R10=NHR6 or NR6R7 R6=R7=COR8 R8=aryl substituted or not while radical Rn can be located in any one or in more than one of the carbon atoms of the aromatic ring, and these radicals can be equal or different, represented by hydrogen, alkylic groups with 1 or more carbon atoms in a linear or branched chain alkenes or alkynes, hydroxyl, hydroxyalkyl or oxygenated functions in acyclic or cyclic systems forming an heterocyclic ring, free or substituted amines, thioalkyl, donators and/or removing groupings of electrons or halogens, thus “n” can vary from 1 to 5. This invention also refers to a pharmaceutical composition comprising, as active principle, at least one of the azole compounds represented by the general formula VIII, to the use of such compositions and to method of treatment or inhibition de tuberculosis and leishmaniasis.

    摘要翻译： 本发明涉及由通式VIII表示的化合物族中包括的新的1,2,3-三唑和咪唑化合物。 其中：X为“C”或“N”的原子，其中X为“N”，自由基为三唑环表示为：R1 = COR2，CSR3，CN（R4）R5或CF2R6; R 2 = H，NHNH 2，烷基，被取代或未取代的芳基，OH，NR 7 R 8或OR 9 R 3 =被取代或未取代的烷基或芳基R 4 = H，OH，烷基或芳基被取代或未被取代。R5 = R6 = R7 = R8 = R9 = H，烷基或芳基被取代或不取代，其中X为“C”的基团为咪唑环，其表示为：R1 = COR2 R2 = NHNH2，OH，OR3或NR4R5 R3 =烷基或芳基被取代或未取代R4 = R5 = 烷基或芳基被取代或未取代R 10 = NHR 6或NR 6 R 7 R 6 = R 7 = COR 8 R 8 =芳基被取代或未取代，而基团Rn可以位于芳环的任何一个或多于一个碳原子中，并且这些基团可以是 相同或不同的，由氢代表，直链或支链烯烃或炔烃中具有一个或多个碳原子的烷基，在形成杂环的无环或环状体系中的羟基，羟烷基或氧化官能团，游离或取代的胺，硫代烷基， 和/或去除电子或卤素的分组，因此“n”可以在1至5之间变化。本发明还涉及药物组合物 作为活性成分，本发明包含至少一种由通式VIII表示的唑类化合物，使用这种组合物以及治疗或抑制结核病和利什曼病的方法。

    AZOLE COMPOUNDS USED AS TUBERCULOSTATIC AND LEISHMANICIDE AGENTS
    2.
    发明申请
    AZOLE COMPOUNDS USED AS TUBERCULOSTATIC AND LEISHMANICIDE AGENTS 审中-公开
    用作溶液和稀土助剂的AZOLE化合物

    公开(公告)号：US20090054501A1

    公开(公告)日：2009-02-26

    申请号：US12064241

    申请日：2006-08-21

    申请人： Nubia Boechat ,  Marilia dos Santos Costa ,  Maria Cristina da Silva Lourenco ,  Ivan Neves Jr ,  Marcelo da Silva Genestra ,  Vitor Francisco Ferreira

    发明人： Nubia Boechat ,  Marilia dos Santos Costa ,  Maria Cristina da Silva Lourenco ,  Ivan Neves Jr ,  Marcelo da Silva Genestra ,  Vitor Francisco Ferreira

    IPC分类号： A61K31/4192 ,  C07D249/04 ,  A61K31/4164 ,  A61P33/02 ,  A61P31/06 ,  C07D233/44

    CPC分类号： A61K31/4192 ,  C07D233/90 ,  C07D249/06

    摘要： This invention refers to new 1,2,3-triazole and imidazole compounds included in the families of compounds represented by general formula VIII. where: X is an atom of “C” or “N;” where X is “N” the radicals do triazole ring are represented by: R1=COR2, CSR3, CN(R4)R5 or CF2R6; R2=H, NHNH2, alkyl, aryl substituted or not, OH, NR7R8 or OR9; R3=alkyl or aryl substituted or not; R4=H, OH, alkyl or aryl substituted or not; R5=R6=R7=R8=R9=R10=H, alkyl or aryl substituted or not; where X is “C” the radicals do imidazolic ring are represented by: R1=COR2; R2=NHNH2, OH, OR3, or NR4R5; R3=alkyl or aryl substituted or not; =R5H, alkyl or aryl substituted or not; R10=NHR6 or NR6R7; R6=R7=COR8; R8=aryl substituted or not; while radical Rn can be located in any one or in more than one of the carbon atoms of the aromatic ring, and these radicals can be equal or different, represented by hydrogen, alkylic groups with 1 or more carbon atoms in a linear or branched chain alkenes or alkynes, hydroxyl, hydroxyalkyl or oxygenated functions in acyclic or cyclic systems forming an heterocyclic ring, free or substituted amines, thioalkyl, donators and/or removing groupings of electrons or halogens, thus “n” can vary from 1 to 5. This invention also refers to a pharmaceutical composition comprising, as active principle, at least one of the azole compounds represented by the general formula VIII, to the use of such compositions and to method of treatment or inhibition de tuberculosis and leishmaniasis.

    摘要翻译： 本发明涉及由通式VIII表示的化合物族中包括的新的1,2,3-三唑和咪唑化合物。 其中：X是“C”或“N”的原子 其中X为“N”，自由基为三唑环表示为：R1 = COR2，CSR3，CN（R4）R5或CF2R6; R2 = H，NHNH2，烷基，取代或未取代的芳基，OH，NR7R8或OR9; R3 =烷基或芳基被取代或未取代; R4 = H，OH，烷基或芳基取代或未取代; R5 = R6 = R7 = R8 = R9 = R10 = H，烷基或芳基被取代或未取代; 其中X为“C”，自由基为咪唑环由下式表示：R1 = COR2; R2 = NHNH2，OH，OR3或NR4R5; R3 =烷基或芳基被取代或未取代; = R5H，烷基或芳基被取代或未取代; R10 = NHR6或NR6R7; R6 = R7 = COR8; R8 =芳基取代或未取代; 而基团Rn可以位于芳族环的任何一个或多于一个碳原子中，并且这些基团可以相同或不同，由氢表示，直链或支链中具有一个或多个碳原子的烷基 烯烃或炔烃，在形成杂环的无环或环状体系中的羟基，羟基烷基或氧化官能团，游离或取代的胺，硫代烷基，给体和/或去除电子或卤素的分组，因此“n”可以在1至5之间变化。 本发明还涉及药物组合物，其包含作为活性成分的至少一种由通式VIII表示的唑类化合物，使用这种组合物以及治疗或抑制结核病和利什曼病的方法。

    Compounds Derived From Lidocaine, Pharmaceutical Compositions, Use And Method Of Treatment, Prevention Or Inhibition Of Disease
    5.
    发明申请
    Compounds Derived From Lidocaine, Pharmaceutical Compositions, Use And Method Of Treatment, Prevention Or Inhibition Of Disease 失效
    衍生自利多卡因，药物组合物，使用和治疗方法，预防或抑制疾病的化合物

    公开(公告)号：US20080221206A1

    公开(公告)日：2008-09-11

    申请号：US11570234

    申请日：2005-06-07

    申请人： Marco Aurelio Martins ,  Jorge Carlos Santos Da Costa ,  Nubia Boechat ,  Rodrigo de Azeredo Siqueira

    发明人： Marco Aurelio Martins ,  Jorge Carlos Santos Da Costa ,  Nubia Boechat ,  Rodrigo de Azeredo Siqueira

    IPC分类号： A61K31/36 ,  C07C233/00 ,  C07D317/48 ,  A61P11/00 ,  A61P11/06 ,  A61K31/167

    CPC分类号： C07C237/04 ,  C07D317/66 ,  C07D405/12 ,  C07D413/12

    摘要： The present invention relates to lidocaine derived compounds, which present less anesthetic activity than lidocaine itself, but with more anti-inflammatory and spasmolytic activity than said lidocaine as well as pharmaceutical compositions with at least one of these compounds or a salt of those as active principle and to the use of such compositions to treat, prevent or inhibit atopic diseases including asthma, rhinitis, allergic urticaria, chronic lung inflammation associated with eosinophilia, following the example of atopic asthma and chronic intestinal inflammation, as colitis for instance. The pharmaceutical composition may be available in spray form, solution, suspension, emulsion destinated to be applied by nebulization, or in any of the pharmaceutical available forms for oral or injectable use.

    摘要翻译： 本发明涉及利多卡因衍生化合物，其比利多卡因本身具有更少的麻醉活性，但具有比所述利多卡因更多的抗炎和解痉活性，以及​​具有至少一种这些化合物的药物组合物或作为活性成分的那些的盐 以及使用这样的组合物治疗，预防或抑制特应性疾病，包括哮喘，鼻炎，过敏性荨麻疹，伴随嗜酸性粒细胞增多的慢性肺部炎症，以特应性哮喘和慢性肠炎症为例，如结肠炎。 药物组合物可以以喷雾形式，溶液，悬浮液，预定为通过雾化施用的乳液，或任何药物可用形式用于口服或可注射使用。

    Gem-difluoro derivative of phenylacetamide and phenylacetic acid and their pharmaceutical uses
    7.
    发明授权
    Gem-difluoro derivative of phenylacetamide and phenylacetic acid and their pharmaceutical uses 失效
    苯乙酰胺和苯乙酸的双 - 二氟衍生物及其药用

    公开(公告)号：US6034266A

    公开(公告)日：2000-03-07

    申请号：US710399

    申请日：1996-09-17

    申请人： Nubia Boechat ,  Angelo Da Cunha Pinto

    发明人： Nubia Boechat ,  Angelo Da Cunha Pinto

    IPC分类号： C07C233/54 ,  C07C233/81 ,  C07C237/22 ,  C07C229/00 ,  C07C233/00

    CPC分类号： C07C233/54 ,  C07C233/81 ,  C07C237/22

    摘要： The present invention refers to novel gem-difluoro compounds of formula: ##STR1## wherein: R.sub.1 can be hydrogen, acyl or acyl substituted; R.sub.2 is hydrogen, lower alkyl, lower alkyl substituted, nitro, halogen, methylenedioxy, trifluoromethyl or OR';Y is oxygen, sulfur or NR";R.sub.3 is hydrogen, lower alkyl, lower alkyl substituted, phenyl, aryl group substituted or metal selected of the group consisting of sodium, potassium, clcium, magnesium, zinc or aluminum;R' and R" are hydrogen, lower alkyl, lower alkyl substituted, phenyl or aryl substituted; and(a) in the group C.sub.1 -C.sub.4 alkyl substitued, one or more the hydrogen atoms are substituted by lower alkyl, lower alkyl substituted, phenyl or aryl substituted;(b) in the group aryl substituted, one or more of the hydrogen atoms are substituted by lower alkyl, halogen, nitro, trifluoromethyl or OR';(c) in the group acyl substituted, one or more of the hydrogen atoms are substituted by lower alkyl, lower alkyl substituted, phenyl or aryl substituted.The compounds as defined above are useful for the treatment of all pain disorders associated to inflammatory and/or rheumatic diseases. The present invention also provides a new process to obtain the compounds from isatin.

    摘要翻译： 本发明涉及下式的新型偕二氟化合物：其中：R 1可以是氢，酰基或酰基取代的; R2是氢，低级烷基，低级烷基取代的，硝基，卤素，亚甲二氧基，三氟甲基或OR'; Y是氧，硫或NR“; R3是氢，低级烷基，低级烷基取代的苯基，被取代的芳基或选自钠，钾，氯，镁，锌或铝的金属; R'和R“是氢，低级烷基，低级烷基取代的苯基或芳基取代的; 和（a）在取代的C1-C4烷基中，一个或多个氢原子被低级烷基，低级烷基取代，苯基或芳基取代; （b）在取代的芳基中，一个或多个氢原子被低级烷基，卤素，硝基，三氟甲基或OR'取代; （c）在酰基取代基中，一个或多个氢原子被低级烷基，低级烷基取代，苯基或被取代的芳基取代。 如上定义的化合物可用于治疗与炎性和/或风湿性疾病相关的所有疼痛疾病。 本发明还提供了从靛红获得化合物的新方法。