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    3β-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof
    2.
    发明授权
    3β-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof 有权
    3β-氨基偶氮二异辛烷杂芳族衍生物的制备方法及其治疗用途

    公开(公告)号：US07456192B2

    公开(公告)日：2008-11-25

    申请号：US10494639

    申请日：2002-10-30

    申请人： Thierry Imbert ,  Barbara Monse ,  Wouter Koek

    发明人： Thierry Imbert ,  Barbara Monse ,  Wouter Koek

    IPC分类号： A61K31/4353 ,  A61K31/4365 ,  A61K31/46 ,  C07D471/04 ,  C07D419/04

    CPC分类号： C07D491/04 ,  C07D495/04

    摘要： The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a bicyclic fused heteroaromatic, such as thieno[2,3-b]pyridine, furo[2,3-b]pyridine, thieno[3,2-b]pyridine, furo[3,2-b]pyridine, thieno[2,3-b]pyrazine, furo[2,3-b]pyrazine, thieno[2,3-c]pyridine, furo[2,3-c]pyridine, thieno[3,2-c]pyridine and furo[3,2-c]pyridine; R1 represents a linear or branched C1-C6 alkoxy group, a linear or branched C1-C6 alkylthio group; R2 represents a linear, branched, cyclic C2-C8 group, a 2- or 3-thienylmethyl group, or a benzyl group optionally substituted by one or several halogens, F, Cl, Br, I, C1-C4alkyl, C1-C4 alkoxy, CF3, CN, NO2, OH; and their pharmaceutically acceptable salts. Said compounds are anti-dopaminergic agents.

    摘要翻译： 本发明涉及通式1的化合物，其中：A，B，D和E代表一个或两个氮原子，其余是碳原子; X表示S或O，由此形成双环稠合杂芳族化合物，例如噻吩并[2,3-b]吡啶，呋喃并[2,3-b]吡啶，噻吩并[3,2-b]吡啶，呋喃并[ 3,2-b]吡啶，噻吩并[2,3-b]吡嗪，呋喃并[2,3-b]吡嗪，噻吩并[2,3-c]吡啶，呋喃并[2,3-c]吡啶，噻吩并[ 3,2-c]吡啶和呋喃并[3,2-c]吡啶; R 1表示直链或支链C 1 -C 6烷氧基，直链或支链C 1 -C 6烷氧基，直链或支链C 1 -C 6 - 烷硫基 R 2表示直链，支链，环状C 2 -C 8亚烷基，2-或3-噻吩基甲基或任选被一个或多个卤素取代的苄基， F，Cl，Br，I，C 1 -C 4烷基，C 1 -C 4烷氧基， CF 3，CN，NO 2，OH; 及其药学上可接受的盐。 所述化合物是抗多巴胺能药。

    Heterocyclo-substituted imidazoles for the treatment of inflammation
    4.
    发明申请
    Heterocyclo-substituted imidazoles for the treatment of inflammation 审中-公开
    杂环取代的咪唑用于治疗炎症

    公开(公告)号：US20050096368A1

    公开(公告)日：2005-05-05

    申请号：US10653399

    申请日：2003-09-02

    申请人： Ish Khanna ,  Richard Weier ,  Paul Collins ,  Yi Yu ,  Xiangdong Xu ,  Richard Partis ,  Francis Koszyk ,  Renee Huff

    发明人： Ish Khanna ,  Richard Weier ,  Paul Collins ,  Yi Yu ,  Xiangdong Xu ,  Richard Partis ,  Francis Koszyk ,  Renee Huff

    IPC分类号： A61K31/4178 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/5377 ,  C07D233/32 ,  C07D233/54 ,  C07D233/90 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/02 ,  C07D419/04

    CPC分类号： C07D233/64 ,  C07D233/32 ,  C07D233/90 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D419/04

    摘要： A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by formula (V), wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, heteroaralkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclocarbonyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkylaminocarbonylalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, aralkoxy, aralkylthio, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, arylthio, aryloxy. aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl; wherein R4 is a radical selected from hydrido, alkyl and halo; and wherein R13 and R14 are independently selected from aryl and heterocyclo, wherein R13 and R14 are optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfonyl, aminosulfonyl, halo, alkylthio, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino and nitro; provided at least one of R13 and R14 is aryl substituted with alkylsulfonyl or aminosulfonyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类咪唑基化合物用于治疗炎症。 特别感兴趣的化合物由式（V）定义，其中R 3是选自氢，烷基，卤代烷基，芳烷基，杂环烷基，杂芳烷基，酰基，氰基，烷氧基，烷硫基，烷硫基烷基，烷基磺酰基 环烷基硫基，环烷硫基烷基，环烷基磺酰基，环烷基磺酰基烷基，卤代烷基磺酰基，芳基磺酰基，卤素，羟基烷基，烷氧基烷基，烷基羰基，芳基羰基，芳烷基羰基，杂环羰基，氰基烷基，氨基烷基，烷基氨基烷基，N-芳基氨基烷基，N-烷基-N-芳基氨基烷基，羧基烷基，烷氧基羰基烷基， 卤代烷基羰基，羧基，氨基羰基，烷基氨基羰基，烷基氨基羰基烷基，杂芳基烷氧基烷基，杂芳氧基烷基，杂芳硫基烷基，芳烷氧基，芳烷硫基，杂芳烷氧基，杂芳烷硫基，杂芳基烷硫基烷基，杂芳氧基，杂芳硫基，芳硫基烷基，芳氧基烷基，芳硫基，芳氧基。 芳烷硫基烷基，芳烷氧基烷基，芳基和杂芳基; 其中R 4是选自氢，烷基和卤素的基团; 并且其中R 13和R 14独立地选自芳基和杂环，其中R 13和R 14是 任选地在可取代的位置被一个或多个独立地选自烷基磺酰基，氨基磺酰基，卤素，烷硫基，烷基，氰基，羧基，烷氧基羰基，卤代烷基，羟基，烷氧基，羟基烷基，烷氧基烷基，卤代烷氧基，氨基，烷基氨基，芳基氨基和硝基的基团取代。 只要R 13和R 14中的至少一个为被烷基磺酰基或氨基磺酰基取代的芳基; 或其药学上可接受的盐。

    Positive allosteric AMPA receptor modulators
    5.
    发明申请
    Positive allosteric AMPA receptor modulators 有权
    正变构AMPA受体调节剂

    公开(公告)号：US20020013313A1

    公开(公告)日：2002-01-31

    申请号：US09774864

    申请日：2001-01-31

    发明人： Karin Winter ,  Thomas Weiser ,  Stefan M. Blech ,  Angelo Ceci

    IPC分类号： A61K031/542 ,  C07D419/04 ,  C07D419/14

    CPC分类号： C07D513/06

    摘要： The present invention relates to new positive allosteric AMPA receptor modulators of general formula (I) 1 wherein R1, R2 R3, R4, R5 and R6 may have the meanings indicated in the specification and claims, processes for preparing them and their use as pharmaceutical compositions.

    摘要翻译： 本发明涉及通式（I）的新的正变构AMPA受体调节剂，其中R 1，R 2，R 3，R 4，R 5和R 6可以具有说明书和权利要求书中指出的含义，其制备方法及其作为药物组合物的用途。

    Antibacterial and antifouling oxathiazines and their oxides
    6.
    发明授权
    Antibacterial and antifouling oxathiazines and their oxides 失效
    抗菌和防污的恶噻嗪及其氧化物

    公开(公告)号：US5922113A

    公开(公告)日：1999-07-13

    申请号：US951278

    申请日：1997-10-16

    申请人： Jozef Frans Elizabetha Van Gestel

    发明人： Jozef Frans Elizabetha Van Gestel

    IPC分类号： A01N43/88 ,  A01P1/00 ,  C07D291/06 ,  C07D419/04 ,  C09D5/14 ,  C09D5/16 ,  A61K31/54 ,  A01N43/34 ,  A01N43/36

    CPC分类号： C07D419/04 ,  A01N43/88 ,  C07D291/06 ,  C09D5/1625

    摘要： Use of 3-aryl-5,6-dihydro-1,4,2-oxathiazines and their oxides having the formula ##STR1## wherein n is 0, 1 or 2; R.sup.1 is hydrogen, C.sub.1-4 alkyl or benzyl; and R represents (a) phenyl; phenyl substituted with 1 to 3 substituents independently selected from hydroxyl, halo, C.sub.1-12 alkyl, C.sub.5-6 cycloalkyl, trihalomethyl, phenyl, C.sub.1-5 alkoxy, C.sub.1-5 alkylthio, tetrahydropyranyloxy, phenoxy, C.sub.1-4 alkylcarbonyl, phenylcarbonyl, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, carboxy or its alkali metal salt, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkylaminocarbonyl, phenylaminocarbonyl, tolylaminocarbonyl, morpholinocarbonyl, amino, nitro, cyano, dioxolanyl or C.sub.1-4 alkyloxyiminomethyl; naphthyl; pyridinyl; thienyl, preferably when n is not 2; furanyl; or thienyl or furanyl substituted with one to three substituents independently selected from C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, C.sub.1-4 alkylthio, halo, cyano, formyl, acetyl, benzoyl, nitro, C.sub.1-4 alkyloxycarbonyl, phenyl, phenylaminocarbonyl and C.sub.1-4 alkyloxyiminomethyl; or R represents a radical of formula ##STR2## wherein X is oxygen or sulfur, Y is nitrogen, CH or C(C.sub.1-4 alkyloxy); and R" is hydrogen or C.sub.1-4 alkyl, as an antibacterial, anti-yeast, antifungal, algicidal, anticrustacean, molluscicidal and general antifouling agent and compositions containing the same.

    摘要翻译： 3-芳基-5,6-二氢-1,4,2-氧噻嗪及其具有下式的氧化物的用途其中n为0,1或2; R1是氢，C1-4烷基或苄基; 并且R表示（a）苯基; 被1至3个独立地选自羟基，卤素，C 1-12烷基，C 5-6环烷基，三卤甲基，苯基，C 1-5烷氧基，C 1-5烷硫基，四氢吡喃氧基，苯氧基，C 1-4烷基羰基，苯基羰基，C 1-4烷基亚磺酰基， 羧基或其碱金属盐，C 1-4烷氧基羰基，C 1-4烷基氨基羰基，苯基氨基羰基，甲苯基氨基羰基，吗啉代羰基，氨基，硝基，氰基，二氧戊环基或C 1-4烷氧基亚氨基甲基; 萘基; 吡啶基 噻吩基，优选当n不为2时; 呋喃基 或被一至三个独立地选自C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，卤素，氰基，甲酰基，乙酰基，苯甲酰基，硝基，C 1-4烷氧基羰基，苯基，苯氨基羰基和C 1-4烷氧基亚氨基甲基的取代基取代的噻吩基或呋喃基。 或R表示下式的基团其中X是氧或硫，Y是氮，CH或C（C 1-4烷氧基）; 和R“是氢或C 1-4烷基，作为抗菌，抗酵母，抗真菌，杀藻剂，防腐素，杀软体动物和一般的防污剂及含有它们的组合物。

    Wood preservative oxathiazines
    7.
    发明授权
    Wood preservative oxathiazines 失效
    木材防腐剂oxathiazines

    公开(公告)号：US5777110A

    公开(公告)日：1998-07-07

    申请号：US295117

    申请日：1994-08-24

    申请人： Robert Allan Davis ,  Alex R. A. Valcke ,  Walter Gerhard Brouwer

    发明人： Robert Allan Davis ,  Alex R. A. Valcke ,  Walter Gerhard Brouwer

    IPC分类号： A01N43/84 ,  B27K3/34 ,  B27K3/38 ,  C07D291/06 ,  C07D419/02 ,  C07D419/04 ,  C09D5/14 ,  C07D291/00

    CPC分类号： C07D419/04 ,  A01N43/88 ,  C07D291/06 ,  B27K3/343

    摘要： The present invention provides certain 3-aryl-5,6-dihydro-1,4,2-ocathiazines and their oxides, useful for the long-term preservation of wood and composite wood materials against wood damaging and wood destroying materials. The present invention also provides compositions containing these 3-aryl-5,6-dihydro-1,4,2-oxathiazines and their oxides, and a suitable vehicle therefor. A method of preserving wood is also disclosed in which a fungicidally or bactericidally effective amount of the present 3-aryl-5,6-dihydro-1,4,2-oxathiazines and their oxides, are applied to the wood substrate to be protected.

    摘要翻译： 本发明提供某些3-芳基-5,6-二氢-1,4,2-噻嗪及其氧化物，其可用于长期保存木材和复合木材以防止木材损坏和破坏木材的材料。 本发明还提供含有这些3-芳基-5,6-二氢-1,4,2-氧噻嗪及其氧化物的组合物及其合适的载体。 还公开了一种保护木材的方法，其中将杀真菌或杀菌有效量的本发明3-芳基-5,6-二氢-1,4,2-氧噻嗪及其氧化物施加到待保护的木质基材上。