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    Pyrrole derivatives with angiotensin II antagonist activity
    23.
    发明授权
    Pyrrole derivatives with angiotensin II antagonist activity 有权
    具有血管紧张素II拮抗剂活性的吡咯衍生物

    公开(公告)号：US07906501B2

    公开(公告)日：2011-03-15

    申请号：US11568362

    申请日：2005-04-27

    申请人： Francesco Makovec ,  Roberto Artusi ,  Antonio Giordani ,  Simona Zanzola ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Roberto Artusi ,  Antonio Giordani ,  Simona Zanzola ,  Lucio Claudio Rovati

    IPC分类号： A61K31/41 ,  C07D293/00 ,  C07D257/04 ,  C07D403/10 ,  C07D295/04

    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的基团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 R4中的卤素基团是直链或支链C 3 -C 5烷基及其药学上可接受的盐，例如钠盐或钾盐。 该化合物显示出有效和选择性的所有拮抗剂活性，并且可用于治疗其中AT1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 与其相关的聚集和紊乱，例如心肌和脑梗死，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。

    1,5-Diary1-2-alkylpyrrole-3-substituted nitro esters, selective COX-2 inhibitors and nitric oxide donors
    28.
    发明授权
    1,5-Diary1-2-alkylpyrrole-3-substituted nitro esters, selective COX-2 inhibitors and nitric oxide donors 有权
    1,5-二辛基-2-烷基吡咯-3-取代的硝基酯，选择性COX-2抑制剂和一氧化氮供体

    公开(公告)号：US09162979B2

    公开(公告)日：2015-10-20

    申请号：US13820533

    申请日：2011-09-07

    申请人： Antonio Giordani ,  Mariangela Biava ,  Maurizio Anzini ,  Vincenzo Calderone ,  Lucio Claudio Rovati

    发明人： Antonio Giordani ,  Mariangela Biava ,  Maurizio Anzini ,  Vincenzo Calderone ,  Lucio Claudio Rovati

    IPC分类号： A61K31/40 ,  A01N43/36 ,  C07D207/337 ,  A61K45/00 ,  C07D207/333 ,  C07D207/335

    CPC分类号： C07D207/337 ,  A61K31/40 ,  A61K45/00 ,  C07D207/333 ,  C07D207/335 ,  Y02A50/473

    摘要： 1,5-diaryl-2-alkylpyrrole-3-substituted nitro esters, of Formula (I) are provided. Such compounds are potent and selective COX-2 inhibitors which are able to release NO in concentrations that make it possible to counteract the side effects due to selective COX-2 inhibition, without giving rise to hypotensive effects. Formula (I) includes compounds wherein the groups R′ and R″ are: —H, —F, —Cl, —Br, —CH3, —CF3, —OCH3, —SCH3, R1 is methyl, ethyl, trifluoromethyl, hydroxymethyl, methoxymethyl and the substituent in position −3 of the pyrrole ring is a chain, where the groups X, Y, Z, W and R2 are: X is a carbonyl or a group —(CHR3)—, Y is an oxygen atom or the group —NR3— and Z is a carbonyl or a group —(CHR3)—, or a [—CH(COOH)—] group, or a group —(NR3)—, W is an aliphatic chain substituted with one or two (—O—NO2) groups, R2 is: —H, —OH, —OCH3, or —NHR3. R3 is: —H, —CH3, —CH2CH3, [—CH2(CH3)2]. R′″ is methylsulphonyl or sulphonamido. Pharmaceutical formulations and methods of making an using such formulations are also provided.

    摘要翻译： 提供式（I）的1,5-二芳基-2-烷基吡咯-3-取代的硝基酯。 这些化合物是能够释放NO的有效和选择性COX-2抑制剂，其浓度可以抵消由于选择性COX-2抑制引起的副作用，而不会引起降血压作用。 式（I）包括其中基团R'和R“为：-H，-F，-Cl，-Br，-CH 3，-CF 3，-OCH 3，-SCH 3，R 1为甲基，乙基，三氟甲基，羟甲基， 甲氧基甲基和吡咯环位置-3的取代基是一个链，其中基团X，Y，Z，W和R 2是：X是羰基或基团 - （CHR 3） - ，Y是氧原子或 基团-NR 3 - 和Z是羰基或 - （CHR 3） - 或[-CH（COOH） - ]基团或 - （NR 3） - 基团，W是被一个或两个 -O-NO 2）基团，R 2是：-H，-OH，-OCH 3或-NHR 3。 R3是：-H，-CH3，-CH2CH3，[-CH2（CH3）2]。 R'“是甲基磺酰基或磺酰胺基。 还提供了制备使用这些制剂的药物制剂和方法。

    1,5-Diaryl-2-alkylpyrrole-3-Substituted Nitro Esters, Selective COX-2 Inhibitors and Nitric Oxide Donors
    29.
    发明申请
    1,5-Diaryl-2-alkylpyrrole-3-Substituted Nitro Esters, Selective COX-2 Inhibitors and Nitric Oxide Donors 有权
    1,5-二芳基-2-烷基吡咯-3-取代的硝基酯，选择性COX-2抑制剂和一氧化氮供体

    公开(公告)号：US20130165494A1

    公开(公告)日：2013-06-27

    申请号：US13820533

    申请日：2011-09-07

    申请人： Antonio Giordani ,  Mariangela Biava ,  Maurizio Anzini ,  Vicenzo Calderone ,  Lucio Claudio Rovati

    发明人： Antonio Giordani ,  Mariangela Biava ,  Maurizio Anzini ,  Vicenzo Calderone ,  Lucio Claudio Rovati

    IPC分类号： C07D207/337 ,  A61K45/00 ,  A61K31/40

    CPC分类号： C07D207/337 ,  A61K31/40 ,  A61K45/00 ,  C07D207/333 ,  C07D207/335 ,  Y02A50/473

    摘要： 1,5-diaryl-2-alkylpyrrole-3-substituted nitro esters, of Formula (I) are provided. Such compounds are potent and selective COX-2 inhibitors which are able to release NO in concentrations that make it possible to counteract the side effects due to selective COX-2 inhibition, without giving rise to hypotensive effects. Formula (I) includes compounds wherein the groups R′ and R″ are: —H, —F, —Cl, —Br, —CH3, —CF3, —OCH3, —SCH3, R1 is methyl, ethyl, trifluoromethyl, hydroxymethyl, methoxymethyl and the substituent in position −3 of the pyrrole ring is a chain, where the groups X, Y, Z, W and R2 are: X is a carbonyl or a group —(CHR3)—, Y is an oxygen atom or the group —NR3— and Z is a carbonyl or a group —(CHR3)—, or a [—CH(COOH)—] group, or a group —(NR3)—, W is an aliphatic chain substituted with one or two (—O—NO2) groups, R2 is: —H, —OH, —OCH3, or —NHR3. R3 is: —H, —CH3, —CH2CH3, [—CH2(CH3)2]. R′″ is methylsulphonyl or sulphonamido. Pharmaceutical formulations and methods of making an using such formulations are also provided.

    摘要翻译： 提供式（I）的1,5-二芳基-2-烷基吡咯-3-取代的硝基酯。 这些化合物是能够释放NO的有效和选择性COX-2抑制剂，其浓度可以抵消由于选择性COX-2抑制引起的副作用，而不会引起降血压作用。 式（I）包括其中基团R'和R“为：-H，-F，-Cl，-Br，-CH 3，-CF 3，-OCH 3，-SCH 3，R 1为甲基，乙基，三氟甲基，羟甲基 ，甲氧基甲基和吡咯环位置-3的取代基是一个链，其中基团X，Y，Z，W和R 2是：X是羰基或基团 - （CHR 3） - ，Y是氧原子或 基团-NR 3 - 和Z是羰基或 - （CHR 3） - 或[-CH（COOH） - ]基团或 - （NR 3） - 基团，W是被一个或两个 （-O-NO 2）基团，R 2是：-H，-OH，-OCH 3或-NHR 3。 R3是：-H，-CH3，-CH2CH3，[-CH2（CH3）2]。 R“'是甲基磺酰基或磺酰胺基。 还提供了制备使用这些制剂的药物制剂和方法。

    N-phenylbenzamide derivatives as drugs for the treatment of COPD
    30.
    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

    申请人： Lucio Claudio Rovati ,  Antonio Giordani ,  Gianfranco Caselli

    发明人： Lucio Claudio Rovati ,  Antonio Giordani ,  Gianfranco Caselli

    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。