Urea compounds, process for producing the same and use thereof
    3.
    发明授权
    Urea compounds, process for producing the same and use thereof 失效
    尿素化合物,其制造方法及其用途

    公开(公告)号:US06787650B1

    公开(公告)日:2004-09-07

    申请号:US10089961

    申请日:2002-04-05

    IPC分类号: C07D41700

    CPC分类号: C07D211/14

    摘要: A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.

    摘要翻译: 下式的化合物:其中R 1为可被取代的烃基; R 2为可被取代的环状烃基或可被取代的杂环基; R 3为卤素原子 ,可以被取代的氨基甲酰基,可以被取代的氨磺酰基,可以被取代的酰基,可以被取代的C1-4烷基,可被取代的C1-4烷氧基,氨基 其可以被取代,硝基或氰基; R 4是氢原子或羟基; n是0或1; 和p为0或1至4];或其盐具有有效的CCR5拮抗活性,并且可有利地用作抑制人外周血单核细胞的HIV感染的药物,特别是用于治疗或预防AIDS。

    Cyclic amine compounds as CCR5 antagonists
    5.
    发明授权
    Cyclic amine compounds as CCR5 antagonists 有权
    环胺化合物作为CCR5拮抗剂

    公开(公告)号:US07348324B2

    公开(公告)日:2008-03-25

    申请号:US10273111

    申请日:2002-10-18

    摘要: A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Y− (R5 is a hydrocarbon group; Y− is a counter anion); R3 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4 is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1 is a bond, CO or SO2; G2 is CO, SO2, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3 aliphatic hydrocarbon which may be substituted; provided that J is methine when G2 is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G1 is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).

    摘要翻译: 式(I)化合物(其中R 1为氢原子,可被取代的烃基,可被取代的非芳香族杂环基,R 2 O 2 >可以被取代的烃基,可以被取代的非芳族杂环基,或者R 1和R 2可以彼此结合形成A至 形成可以被取代的杂环基; A是N或N + - - - - - - - (R 5) SUP>为烃基; Y为 - 抗衡阴离子); R 3为可被取代的环状烃基或可被取代的杂环基; n 为0或1; R 4为氢原子,可被取代的烃基,可被取代的杂环基,可被取代的烷氧基,可被取代的芳氧基 ,或可以被取代的氨基,E是可以是二价脂族烃基 被除氧基以外的基团取代; G 1是一个键,CO或SO 2; G 2是CO,SO 2,NHCO,CONH或OCO; J为次甲基或氮原子; 并且Q和R中的每一个是可被取代的键或二价C 1-3烷基脂族烃; 条件是当G 2 O是OCO时J为次甲基,当另一个为键并且Q和R各自不被氧代基取代时,Q和R中的一个不为键, 当G 1是一个键时)或其盐具有强的CCR5拮抗活性,并且可以有利地用于治疗或预防人类各种HIV感染性疾病(如艾滋病)。

    Substituted thiazole derivatives bearing 3-pyridyl groups, process for preparing the same and use thereof
    6.
    发明授权
    Substituted thiazole derivatives bearing 3-pyridyl groups, process for preparing the same and use thereof 失效
    带有3-吡啶基的取代噻唑衍生物,其制备方法及其应用

    公开(公告)号:US07067537B2

    公开(公告)日:2006-06-27

    申请号:US10433910

    申请日:2001-12-07

    IPC分类号: A01N43/40 A61K31/44

    摘要: The present invention provides a pharmaceutical composition having a steroid C17,20-lyase inhibitory activity, which is useful as a prophylactic or therapeutic agent of prostatism, tumor such as breast cancer and the like, more particularly, a steroid C17,20-lyase inhibitor containing a compound represented by the formula: wherein A1 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, one of A2 and A3 is a hydrogen atom, a halogen atom, a C1-4 aliphatic hydrocarbon group optionally having substituents or an optionally esterified carboxyl group, the other of A2 and A3 is an aromatic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, and at least one of A1, A2 and A3 is a 3-pyridyl group optionally having substituents, or a salt thereof or a prodrug thereof.

    摘要翻译: 本发明提供了具有类固醇C 17-20半胱氨酸酶抑制活性的药物组合物,其可用作前列腺症的预防或治疗剂,诸如乳腺癌等肿瘤,更具体地, 含有由下式表示的化合物的类固醇C 17-20重量酶抑制剂:其中A 1是任选具有取代基的芳族烃基或任选具有取代基的杂环基, A 2和A 3之一是氢原子,卤素原子,任选具有取代基的C 1-4烷基脂族烃基或 任选地酯化的羧基,A 2和A 3中的另一个是任选具有取代基的芳族烃基或任选具有取代基的杂环基,并且A < SUP> 1,A 2和A 3是任选具有取代基的3-吡啶基,或其盐或前药 其中。

    Optical information system focal point displacement detecting means
having Fresnel zone plates with rectilinear grating
    9.
    发明授权
    Optical information system focal point displacement detecting means having Fresnel zone plates with rectilinear grating 失效
    光信息系统焦点位移检测装置,具有带有直线光栅的菲涅耳带片

    公开(公告)号:US5351230A

    公开(公告)日:1994-09-27

    申请号:US964964

    申请日:1992-10-22

    IPC分类号: G11B7/09 G11B7/135 G11B7/00

    CPC分类号: G11B7/1353 G11B7/0909

    摘要: This invention pertains to a displacement detecting device for an optical head for detecting focal point displacement of irradiation light. The displacement detecting device has optical means for converting reflected rays from an irradiated face into an astigmatic bundle of rays and a photodetector for detecting a change in the the focused shape. The displacement detecting device thus detects focal point displacement of irradiation light. The optical means is obtained by integrally forming a plurality of Fresnel zone plates having rectilinear gratings, focusing reflected rays from the irradiated face, and having different focal lengths.

    摘要翻译: 本发明涉及用于检测照射光的焦点位移的光学头的位移检测装置。 位移检测装置具有用于将来自照射面的反射光线转换成散光束的光学装置和用于检测聚焦形状的变化的光电检测器。 因此,位移检测装置检测照射光的焦点位移。 光学装置是通过一体地形成多个具有直线光栅的菲涅耳带板,聚焦来自照射面的反射光线并具有不同的焦距而获得的。

    Phosphonocephem compound
    10.
    发明授权
    Phosphonocephem compound 有权
    膦酰基化合物

    公开(公告)号:US07419973B2

    公开(公告)日:2008-09-02

    申请号:US11063715

    申请日:2005-02-23

    CPC分类号: A61K31/675 C07F9/65613

    摘要: A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like.

    摘要翻译: 由式[I]表示的头孢烯化合物(特别是其结晶),其中X是CH 3 COOH,CH 3 CH 2 COOH或 CH 3 CN,n为0〜5,可用作抗菌剂(特别是抗MRSA剂),并且具有优异的质量,例如高固体稳定性,可能的长期稳定保存等 。