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    Diaminopyridine-containing thiourea inhibitors of herpes viruses
    2.
    发明授权
    Diaminopyridine-containing thiourea inhibitors of herpes viruses 失效
    含二氨基吡啶的疱疹病毒的硫脲抑制剂

    公开(公告)号：US06407123B1

    公开(公告)日：2002-06-18

    申请号：US09670180

    申请日：2000-09-26

    申请人： Jonathan Bloom ,  Martin DiGrandi ,  Russell Dushin ,  Stanley Lang ,  Bryan O'Hara

    发明人： Jonathan Bloom ,  Martin DiGrandi ,  Russell Dushin ,  Stanley Lang ,  Bryan O'Hara

    IPC分类号： A61K31443

    CPC分类号： C07D213/75 ,  C07D213/81 ,  C07D405/12 ,  C07D417/12

    摘要： Compounds of the formula wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W—Y—(CH2)n—Z ; or R2 and R3 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 membered heterocycloalkyl; A is heteroaryl.

    摘要翻译： 式R 1 -R 5的化合物独立地选自氢，1至6个碳原子的烷基，2至6个碳原子的链烯基，2至6个碳原子的炔基，1至6个碳原子的全卤代烷基，3至10个碳原子的环烷基 原子，3至10个碳成员的杂环烷基，芳基，杂芳基，卤素，-CN，-NO 2，-CO 2 R 6，-COR 6，-OR 6，-SR 6，-SOR 6，-SO 2 R 6，-CONR 7 R 8，-NR 6 N（R 7 R 8） N（R 7 R 8）或WY-（CH 2）n Z; 或R2和R3或R3和R4一起形成3至7元杂环烷基或3至7元杂芳基; R6和R7独立地为氢，1至6个碳原子的烷基，1至6个碳原子的全卤代烷基或芳基 ; R 8为氢，1至6个碳原子的烷基，1至6个碳原子的全卤烷基，3至10个碳原子的环烷基，3至10个成员的杂环烷基，芳基或杂芳基，或R 7和R 8一起可以形成3 至7元杂环烷基; A为杂芳基。

    Benzimidazole cyclooxygenase-2 inhibitors
    4.
    发明授权
    Benzimidazole cyclooxygenase-2 inhibitors 失效
    苯并咪唑环加氧酶-2抑制剂

    公开(公告)号：US06310079B1

    公开(公告)日：2001-10-30

    申请号：US09244875

    申请日：1999-02-05

    申请人： Yoshiyuki Okumura ,  Yoshinori Murata ,  Takashi Mano

    发明人： Yoshiyuki Okumura ,  Yoshinori Murata ,  Takashi Mano

    IPC分类号： A61K31443

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14

    摘要： This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof, wherein Ar is heteroaryl; X1 and X2 are independently selected from halo, C1-C4 alkyl, hydroxy, C1-C4 alkoxy, amino, C1-C4 alkanoyl, carboxy, carbamoyl, cyano, nitro, mercapto, (C1-C4 alkyl)thio, (C1-C4 alkyl)sulfinyl, (C1-C4 alkyl)sulfonyl, aminosulfonyl, or the like; R1 is selected from hydrogen, straight or branched C1-C4 alkyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, phenyl , heteroaryl and the like; R2 and R3 are independently selected from hydrogen, halo, C1-C4 alkyl, phenyl and the like; or R1 and R2 can form, together with the carbon atom to which they are attached, a C5-C7 cycloalkyl ring; and m and n are independently 0, 1, 2 or 3. These compounds and pharmaceutical compositions containing such compounds are useful as analgesics and anti-inflammatory agents.

    摘要翻译： 本发明提供下式的化合物或其药学上可接受的盐，其中Ar是杂芳基; X1和X2独立地选自卤素，C1-C4烷基，羟基，C1-C4烷氧基，氨基，C1-C4烷酰基，羧基，氨基甲酰基，氰基，硝基，巯基，（C1-C4烷基）硫基，（C1-C4 烷基）亚磺酰基，（C 1 -C 4烷基）磺酰基，氨基磺酰基等; R 1选自氢，直链或支链C 1 -C 4烷基，C 3 -C 8环烷基，C 4 -C 8环烯基，苯基，杂芳基等; R2和R3独立地选自氢，卤素，C1-C4烷基，苯基等; 或者R 1和R 2可以与它们所连接的碳原子一起形成C 5 -C 7环烷基环; 并且m和n独立地为0,1,2或3.这些化合物和含有这些化合物的药物组合物可用作止痛剂和抗炎剂。

    Benzofuran-4-carboxamides
    7.
    发明授权
    Benzofuran-4-carboxamides 有权
    苯并呋喃-4-甲酰胺

    公开(公告)号：US06211203B1

    公开(公告)日：2001-04-03

    申请号：US09147640

    申请日：1999-02-05

    申请人： Hermann Amschler

    发明人： Hermann Amschler

    IPC分类号： A61K31443

    CPC分类号： C07D307/79 ,  C07D405/12

    摘要： Compounds of formula I wherein R1 is 1-2C-alkoxy optionally substituted by flourine, R2 is methyl, 1-methylethyl, 3-7C-cycloalkyl or 3-7Ccycloalkylmethyl and Ar is a pyridyl which is optionally di-halo substituted.

    摘要翻译： 式Ⅰ的化合物，其中R 1是任选被氟取代的1-2C-烷氧基，R 2是甲基，1-甲基乙基，3-7C-环烷基或3-7C环烷基甲基，Ar是任选被二卤代基取代的吡啶基。

    Substituted bicyclic heteroaryl compounds and their use as integrin antagonists
    8.
    发明授权
    Substituted bicyclic heteroaryl compounds and their use as integrin antagonists 有权
    取代的双环杂芳基化合物及其作为整联蛋白拮抗剂的用途

    公开(公告)号：US06706738B2

    公开(公告)日：2004-03-16

    申请号：US09975721

    申请日：2001-10-11

    申请人： David Edward Clark ,  Paul Robert Eastwood ,  Neil Victor Harris ,  Clive McCarthy ,  Andrew David Morley ,  Stephen Dennis Pickett

    发明人： David Edward Clark ,  Paul Robert Eastwood ,  Neil Victor Harris ,  Clive McCarthy ,  Andrew David Morley ,  Stephen Dennis Pickett

    IPC分类号： A61K31443

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14

    摘要： The invention is directed to physiologically active compounds of general formula (I): R1Z1—Het—L1—Ar1—L2—Y  (I) wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring containing at least one heteroatom selected from O, S or N; R1 is optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; Z1 represents a direct bond, an alkylene chain, NR4, O or S(O)n; L1 is an a —R5—R6— linkage where R5 is alkylene, alkenylene or alkynylene and R6 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, —C(═Z3)—NR4—, —NR4—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR4)—, —NR4—, —NR4—C(═Z3)—NR4—, —SO2—NR4—, —NR4—SO2—, —O—C(═O)—, —C(═O)—O—, —NR4—C(═O)—O— or —O—C(═O)—NR4—; L2 is a direct bond; an optionally substituted alkylene, alkenylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene or arylene linkage; a —[C(═O)—N(R9)—C(R4)(R10)]p— linkage; a —Z4—R11— linkage; a —C(═O)—CH2—C(═O)— linkage; a —R11—Z4—R11— linkage; or a —L3—L4—L5— linkage; and Y is carboxy or an acid bioisostere; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).

    摘要翻译： 本发明涉及通式（I）的生理活性化合物：其中Het是任选取代的，饱和的，部分饱和的或完全不饱和的8至10元双环，其含有至少一个选自O，S或N的杂原子; R 1是任选取代的芳基，杂芳基，烷基，烯基，炔基，环烷基或杂环烷基; Z 1表示直接键，亚烷基链，NR 4，O或S（O）n; L 1是-R 5 -R 6 - 键，其中R 5是亚烷基，亚烯基或亚炔基，R 6是直接键，亚环烷基，亚杂环亚烷基，亚芳基，杂芳基二基，-C （= Z 3）-NR 4 - ， - NR 4 -C（= Z 3） - ， - Z 3 - ， - C（= O） - ， - -NR 4 - ， - NR 4 -C（= Z 3）-NR 4 - ， - SO 2 -NR 4 - ， - NR 4 -SO 2 - ， - OC（= O） - ， - C（= O）-O-，-NR 4 -C（= O）-O-或-OC（= O）-NR 4 - L 2是直接键; 亚烯基，亚炔基，亚环烯基，亚环烷基，杂芳基二基，杂环亚烷基或亚芳基键; a - [C（= O）-N（R 9）-C（R 4）（R 10）] p - 键; a -Z 4 -R 11 - 键; -C（= O）-CH 2 -C（= O） - 键; -R 11 -Z 4 -R 11 - 键; 或-L 3 -L 4 -L 5 - 键; Y为羧基或酸式生物电子等排体; 和相应的N-氧化物及其前药; 和这些化合物的药学上可接受的盐和溶剂合物（例如水合物）及其N-氧化物和前药。 这些化合物具有有价值的药物性质，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1）的相互作用的能力。