N-phenylbenzamide derivatives as drugs for the treatment of COPD
    31.
    发明授权
    N-phenylbenzamide derivatives as drugs for the treatment of COPD 有权
    N-苯基苯甲酰胺衍生物作为治疗COPD的药物

    公开(公告)号:US07482371B2

    公开(公告)日:2009-01-27

    申请号:US11206803

    申请日:2005-08-19

    IPC分类号: C11D3/00

    CPC分类号: A61K31/41

    摘要: The invention relates to the use of a pharmaceutically active derivative of N-phenylbenzamide of Formula (I) or of a pharmaceutically acceptable salt thereof, for preparing a medicament for the therapeutic treatment of Chronic Obstructive Pulmonary Disease (COPD).Compounds of Formula (I): wherein R1 is cyano, nitro, halogen, hydroxy, C1-C4 alkyl, methoxy or tetrazol-5-yl group, R2 is hydrogen, hydroxy or methoxy, R3 is a tetrazol-5-yl group or hydrogen, R4 and R5 are hydrogen if R3 is tetrazol-5-yl group, or R4 and R5 are independently selected from the group consisting of carboxy, methoxycarbonyl, ethoxycarbonyl and carbamoyl if R3 is hydrogen, and R6 is hydrogen or methyl.

    摘要翻译: 本发明涉及式(I)的N-苯基苯甲酰胺或其药学上可接受的盐的药学活性衍生物在制备用于治疗慢性阻塞性肺疾病(COPD)的药物中的用途。 式(I)化合物:其中R 1是氰基,硝基,卤素,羟基,C 1 -C 4烷基,甲氧基或四唑-5-基,R 2是氢,羟基或甲氧基,R 3是四唑-5-基或 如果R 3是氢或甲基,则R 3和R 4各自独立地选自羧基,甲氧基羰基,乙氧基羰基和氨基甲酰基,如果R 3是四唑-5-基,则R 4和R 5是氢。

    Novel Pyrrole Derivatives with Angiotensin II Antagonist Activity
    32.
    发明申请
    Novel Pyrrole Derivatives with Angiotensin II Antagonist Activity 有权
    新型吡咯衍生物与血管紧张素II拮抗剂活性

    公开(公告)号:US20070244170A1

    公开(公告)日:2007-10-18

    申请号:US11568362

    申请日:2005-04-27

    CPC分类号: C07D403/10

    摘要: Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, —COOH, —CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.

    摘要翻译: 可以由下述通式(I)表示的化合物,其中:R 1是独立地选自:CHO,-COOH,-CH 2, OH R 2是氢或直链或支链C 1 -C 6烷基R 3是氢或 选自Cl和Br R 4的卤素基团是直链或支链C 3 -C 5烷基和其药学上可接受的盐 例如钠盐或钾盐。 所述化合物表现出有效和选择性的所有拮抗剂活性,并且可用于治疗其中AT 1受体的全部或过表达的合成升高可能起主要病理学作用的任何障碍,如在 动脉高血压,充血性心功能不全,血小板聚集和与之相关的病症,例如心肌和脑梗塞,肾缺血,静脉和动脉血栓形成,外周血管病变,肺动脉高压,糖尿病,糖尿病性神经病,青光眼和糖尿病性视网膜病变。

    Novel piperidine derivatives
    36.
    发明授权
    Novel piperidine derivatives 失效
    新型哌啶衍生物

    公开(公告)号:US4879300A

    公开(公告)日:1989-11-07

    申请号:US135839

    申请日:1987-12-21

    CPC分类号: C07D401/04 C07D211/26

    摘要: A compound, or a solvate or salt thereof, of formula I: ##STR1## in which: R.CO-- is an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkenyl, C.sub.1-6 cycloalkyl or C.sub.1-12 cycloalkylalkyl or together form a C.sub.2-6 polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom, provided that R.sub.1 and R.sub.2 are not simultaneously hydrogen;Rx is C.sub.1-6 alkyl or phenyl, or Rx together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group, is useful for the treatment of pain.