Derivatives of 4-(2-aminoethyl)phenoxymethyl-phosphonic and -phosphinic
acid and pharmaceutical and veterinary uses therefor
    1.
    发明授权
    Derivatives of 4-(2-aminoethyl)phenoxymethyl-phosphonic and -phosphinic acid and pharmaceutical and veterinary uses therefor 失效
    4-(2-氨基乙基)苯氧基甲基 - 膦酸和次膦酸的衍生物及其药用和兽用用途

    公开(公告)号:US5726165A

    公开(公告)日:1998-03-10

    申请号:US465486

    申请日:1995-06-05

    摘要: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, or solvate thereof, wherein, R.sup.o represents an aryl group, optionally substituted; X represents O or S; R.sup.1 and R.sup.1a each independently represents hydrogen or an alkyl group; R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b): ##STR2## wherein R.sup.4 represent hydrogen, alkyl, hydroxyalkyl, arylalkyl, aralkyloxyalkyl or cycloalkyl and R.sup.5 represent hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, arylalkoxyalkyloxy, cycloalkyloxy, hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, arylalkyloxyalkyl or R.sup.5 together with OR.sup.4 represents O(CH.sub.2).sub.n O wherein n is 2, 3 or 4; and R.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.2 represents a moiety of formula (c): ##STR3## or an ester or amide thereof; a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.

    摘要翻译: 式(I)的化合物:其中,R 1表示任选被取代的芳基;(I)化合物或其药学上可接受的盐或其溶剂合物, X表示O或S; R 1和R 1a各自独立地表示氢或烷基; R 2表示OCH 2 CO 2 H或其酯或酰胺,或R 2表示式(b)的部分:其中R 4表示氢,烷基,羟烷基,芳烷基,芳烷氧基烷基或环烷基,R 5表示羟基,烷氧基,芳基烷氧基 ,羟烷基氧基,烷氧基烷氧基,芳基烷氧基烷氧基,环烷氧基,氢,烷基,取代烷基,环烷基,芳基,芳基烷基,芳基烷氧基烷基或R5与OR4一起表示O(CH2)nO,其中n为2,3或4; 并且R 3表示氢,卤素,烷基或烷氧基,或者R 3与R 2一起表示式(c)的部分:(c)或其酯或酰胺; 含有这种化合物的药物组合物,制备这种化合物的方法以及这种化合物在医药中的用途。

    Heterocyclic ethanolamine derivatives with .beta.-adrenoreceptor
agonistic activity
    2.
    发明授权
    Heterocyclic ethanolamine derivatives with .beta.-adrenoreceptor agonistic activity 失效
    具有β-肾上腺素受体激动活性的杂环乙醇胺衍生物

    公开(公告)号:US5750701A

    公开(公告)日:1998-05-12

    申请号:US704699

    申请日:1996-09-16

    CPC分类号: C07D405/12

    摘要: A compound of the formula (I), or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein, X represents a moiety of formula (a), in which A.sup.1 represents --CH.dbd.CH.dbd., NH, S or O; A.sup.2 represents an oxo or a thioxo group; A.sup.3 represents H or an alkylcarbonyl group; and A.sup.4 represents hydroxy or NR.sup.s R.sup.t wherein R.sup.s and R.sup.t each independently represents H or alkyl; R.sup.0 and R.sup.1 each independently represents hydrogen or an alkyl group; R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b), wherein R.sup.4 and R.sup.5 each independently represent hydrogen, alkyl, hydroxyalkyl, cycloalkyl or R.sup.4 together with R.sup.5 represents (CH.sub.2).sub.n wherein n is 2, 3 or 4; and R.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.2 represents a moiety of formula (c) or an ester or amide thereof, wherein R represents hydrogen, alkyl, hydroxymethyl or a moiety of formula (CH.sub.2).sub.n CO.sub.2 H, wherein n is zero or an integer 1, 2 or 3, or an ester or amide thereof; a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of such a compound and composition in medicine.

    摘要翻译: PCT No.PCT / EP95 / 00794 Sec。 371日期1996年9月16日 102(e)1996年9月16日PCT PCT 1995年3月3日PCT公布。 第WO95 / 25104号公报 日期1995年9月21日一种式(I)化合物或其药学上可接受的盐或其药学上可接受的溶剂化物,其中X表示式(a)的部分,其中A1表示-CH = CH =, NH,S或O; A2表示氧代或硫代基; A3表示H或烷基羰基; 并且A4表示羟基或NRsRt,其中R 5和R 5各自独立地表示H或烷基; R 0和R 1各自独立地表示氢或烷基; R2表示OCH2CO2H,或其酯或酰胺,或R2表示式(b)的部分,其中R4和R5各自独立地表示氢,烷基,羟基烷基,环烷基或R4以及R5表示(CH2)n,其中n为2 ,3或4; 并且R 3表示氢,卤素,烷基或烷氧基或R 3与R 2一起表示式(c)的部分或其酯或酰胺,其中R表示氢,烷基,羟甲基或式(CH2)nCO2H的部分,其中n 为零或整数1,2或3,或其酯或酰胺; 制备这种化合物的方法,含有这种化合物的药物组合物以及这种化合物和组合物在医药中的用途。

    Imidazolidine carboxamide derivatives as P2X7 modulators
    4.
    发明授权
    Imidazolidine carboxamide derivatives as P2X7 modulators 失效
    咪唑烷羧酰胺衍生物作为P2X7调节剂

    公开(公告)号:US07932282B2

    公开(公告)日:2011-04-26

    申请号:US12594381

    申请日:2008-04-02

    IPC分类号: A61K31/4164 C07D233/02

    摘要: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.

    摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐:该化合物或盐调节P2X7受体功能并能够拮抗ATP在P2X7受体(P2X7受体拮抗剂)下的作用。 本发明还提供了这样的化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的病症/疾病中的用途,例如疼痛,炎症或神经变性疾病,特别是疼痛,例如炎性疼痛, 神经性疼痛或内脏痛。

    Pyridine substituted furan derivatives as Raf kinase inhibitors
    6.
    发明授权
    Pyridine substituted furan derivatives as Raf kinase inhibitors 失效
    吡啶取代的呋喃衍生物作为Raf激酶抑制剂

    公开(公告)号:US07375105B2

    公开(公告)日:2008-05-20

    申请号:US10488650

    申请日:2002-09-05

    CPC分类号: C07D405/04 C07D405/14

    摘要: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R1 is hydrogen; Y1 and Y2 independently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of X1 and X2 is selected from O, S or NR11 and the other is CH, wherein R11 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl.

    摘要翻译: 化合物及其作为药物的用途,特别是用作治疗神经创伤性疾病,癌症,慢性神经变性,疼痛,偏头痛和心脏肥大的Raf激酶抑制剂。 其中X是O,CH 2 CO,S或NH,或者X-R 1部分是氢; Y 1和Y 2独立地表示CH或N; Ar是可以任选取代的单或二稠合双环芳族或杂芳族基团; X 1和X 2之一选自O,S或NR 11,另一个是CH,其中R 11, / SUP>是氢,C 1-6烷基,芳基或芳基C 1-6烷基。