Cycloheptene compounds
    3.
    发明授权
    Cycloheptene compounds 失效
    环庚烯化合物

    公开(公告)号:US06638962B2

    公开(公告)日:2003-10-28

    申请号:US10050666

    申请日:2002-01-16

    IPC分类号: A61K314174

    摘要: Compound of formula (I): wherein: X represents a bond or alkylene, CO, S(O)n, —S(O)n—A1—, —CO—A1—, —A—S(O)n—A′1— or —A1—CO—A′1—, Y represents aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, R1, R2, R3 and R4 each independently of the others represent hydrogen or aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each unsubstituted or substituted, or R1, R2, R3 and R4, taken in pairs, together form a bond, or form a fused benzene ring or a fused aromatic or partially unsaturated heterocycle, T represents —CH(R5)—, —N(R5)— or —N(R5)CO—, V represents hydrogen or unsubstituted or substituted aryl or heteroaryl, A2 represents [C(R6)(R′6)]p, R7 and R8 are as defined in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as farnesyl transferase inhibitors.

    摘要翻译: 式(I)的化合物:其中:X表示键或亚烷基,CO,S(O)n,-S(O)n -A1,-CO-A1-,-AS(O)n-A'1 - 或-A1-CO-A'1-,Y表示芳基,杂芳基,环烷基或杂环烷基,每个未取代或取代的,R 1,R 2,R 3和R 4各自独立地表示氢或芳基,杂芳基,环烷基或杂环烷基, 每个未取代或取代的或R 1,R 2,R 3和R 4成对取代,一起形成键,或形成稠合苯环或稠合芳族或部分不饱和杂环,T表示-CH(R 5) - , - N( R5) - 或-N(R5)CO-,V表示氢或未取代或取代的芳基或杂芳基,A2表示[C(R6)(R'6)] p,R7和R8如说明书中所定义, 并且其与药学上可接受的酸或碱的加成盐和含有它们的药物可用作法呢基转移酶抑制剂。

    Carboxylic and hydroxamic acid compounds inhibiting metalloproteases, method for preparing same and pharmaceutical compositions containing them
    4.
    发明授权
    Carboxylic and hydroxamic acid compounds inhibiting metalloproteases, method for preparing same and pharmaceutical compositions containing them 失效
    抑制金属蛋白酶的羧酸和异羟肟酸化合物,其制备方法和含有它们的药物组合物

    公开(公告)号:US06605604B1

    公开(公告)日:2003-08-12

    申请号:US09720850

    申请日:2000-12-26

    IPC分类号: C07D20948

    摘要: The invention concerns a compound of formula (I) wherein: n is equal to 0 or 1; R1, R2, R3, R4 represent a hydrogen or an alkyl group, or R1 and R3 together form a cycloalkyl group; R5 represents a hydrogen, an alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl, hetereoalkylalkyl, hetereocycloalkyl, hetereocycloalkylalkyl group (all optionally substituted), or a —CO—R6 group; and R6 represents R7 or OR7 or NR7R8, with R7 representing an aryl, arylalkyl, heteroaryl or heteroarylalkyl, heterocycloalkyl, heterocycloalkylalkyl group (all optionally substituted), and R8 representing an alkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl (all optionally substituted); or R5 and R6 form with the nitrogen atom and the Z group bearing them a saturated monocyclic, bicyclic or tricyclic group, partially unsaturated or unsaturated, with 5 to 16 chain links containing 1 to 7 heteroatoms and optionally substituted; R10 represents a hydrogen atom or a hydroxy group, and in the latter case R1, R2, R3, R4 are independently selected among hydrogen and alkyl; Z represents a hydroxy, alkoxy, alkenyloxy, benzyloxy group or a NH—OR group; X represents a sulphur, a SO, SO2 group (in those cases where R3 and R4 are different from an alkyl) or a group —CO—O— (in which case R1 and R3 form a cycloalkyl group), or X represents an oxygen atom; W represents a W1—(A)p or W1—B—W2—(A)p group wherein W1 and W2 represent an aryl or heteroaryl group, A is a standard substituent of aromatic cycles, B a bond, an oxygen or an alkylene, alkenylene, alkynylene group, and p is an integer ranging between 0 and 5; T1 and T2 represent a bond or an alkylene, alkenylene, or alkynylene group. The invention is useful for preparing medicines.

    摘要翻译: 本发明涉及式(I)的化合物,其中:n等于0或1; R1,R2,R3,R4表示氢或烷基,或R1和R3一起形成环烷基; R5代表氢,烷基,环烷基,环烷基烷基,芳基,芳烷基,杂芳基,杂芳烷基烷基,杂三环烷基,杂三环烷基烷基(全部任意取代)或-CO-R 6基团; 并且R 6表示R 7或OR 7或NR 7 R 8,其中R 7表示芳基,芳基烷基,杂芳基或杂芳基烷基,杂环烷基,杂环烷基烷基(全部被取代),R 8表示烷基,芳基,芳基烷基,杂芳基或杂芳基烷基(全部被取代) 或R 5和R 6与氮原子一起形成,Z基团带有饱和的单环,双环或三环基团,部分不饱和或不饱和的,具有5至16个含有1至7个杂原子和任选取代的链节; R 10表示氢原子或羟基,在后一种情况下,R 1,R 2,R 3,R 4独立地选自氢和烷基; Z表示羟基,烷氧基,烯氧基,苄氧基或NH-OR基; X表示硫,SO,SO 2基(在那些R3和R4不同于烷基的情况下)或基团-CO-O-(在这种情况下,R1和R3形成环烷基),或X表示氧 原子; W表示W1-(A)p或W1-B-W2-(A)p基团,其中W1和W2表示芳基或杂芳基,A是芳族环的标准取代基,B a键,氧或亚烷基 亚烯基,亚炔基,p为0〜5的整数。 T1和T2表示键或亚烷基,亚烯基或亚炔基。 本发明可用于制备药物。

    Azabicylic compounds, a process for their preparation and pharmaceutical compositions containing them
    8.
    发明授权
    Azabicylic compounds, a process for their preparation and pharmaceutical compositions containing them 失效
    Azabicylic化合物,其制备方法和含有它们的药物组合物

    公开(公告)号:US07906547B2

    公开(公告)日:2011-03-15

    申请号:US12456165

    申请日:2009-06-12

    IPC分类号: A61K31/403 C07D209/52

    CPC分类号: C07D209/52

    摘要: Compounds of formula (I): wherein: ALK represents an alkylene chain, W represents a group selected from wherein R and R′ are as defined in the description. Medicinal products containing the same which are useful in the treatment of cognitive and psycho-behavioural disorders associated with cerebral ageing, with neurodegenerative diseases or with cranial traumas and also in the treatment of mood disorders, of schizophrenia and of cognitive disorders associated therewith, of sleep disorders, of sleep-waking rhythm disorders, of attention-deficit hyperactivity syndrome or of obesity.

    摘要翻译: 式(I)化合物:其中:ALK表示亚烷基链,W表示选自其中R和R'如说明书中所定义的基团。 含有相同的药用产品,其可用于治疗与脑衰老相关的认知和心理行为障碍,神经变性疾病或颅外伤,以及治疗精神分裂症和与其相关的认知障碍的情绪障碍,睡眠 睡眠障碍,节律障碍,注意力缺陷多动症或肥胖症。

    Unsaturated acetylene phosphonate derivatives of purines
    9.
    发明授权
    Unsaturated acetylene phosphonate derivatives of purines 失效
    嘌呤的不饱和乙炔膦酸酯衍生物

    公开(公告)号:US5817647A

    公开(公告)日:1998-10-06

    申请号:US505168

    申请日:1995-11-17

    IPC分类号: A61K31/675 C07F9/6512

    CPC分类号: A61K31/675 C07F9/6512

    摘要: Disclosed are novel unsaturated acetylene phosphonate derivatives of certain purines or pyrimidines useful as antiviral agents, methods useful for their preparation and use of these compounds as antiviral agents effective against DNA viruses, retroviruses and viruses involved in tumor formation.

    摘要翻译: PCT No.PCT / US94 / 01837 Sec。 371日期:1995年11月17日 102(e)日期1995年11月17日PCT 1994年2月25日PCT PCT。 第WO94 / 22882号公报 日期1994年10月13日公开是用作抗病毒剂的某些嘌呤或嘧啶的新型不饱和乙炔膦酸衍生物,可用于其制备和使用这些化合物作为抗病毒剂的抗病毒剂的方法,所述抗病毒剂有效对抗涉及肿瘤形成的DNA病毒,逆转录病毒和病毒。