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1. 发明申请

US20090281094A1 Derivatives of 1--4-methylpiperazine, synthesis process and uses thereof 失效
标题翻译： 1--4甲基哌嗪的衍生物，其合成方法及用途
公开(公告)号：US20090281094A1
公开(公告)日：2009-11-12
申请号：US11817678
申请日：2006-03-03
申请人： Mariangela Biava , Fabrizio Manetti , Delia Deidda , Raffaello Pompei , Maurizio Botta , Giulio Cesare Porretta
发明人： Mariangela Biava , Fabrizio Manetti , Delia Deidda , Raffaello Pompei , Maurizio Botta , Giulio Cesare Porretta
IPC分类号： A61K31/541 , C07D403/02 , C07D417/02 , A61K31/496 , C07C49/105 , C07D207/30 , A61P31/06
CPC分类号： C07D207/335
摘要： The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low toxicity and process to obtain intermediates and final compounds.
摘要翻译：本发明涉及吡咯化合物，1 - {[1,5-双（4-氯苯基）-2-甲基-1H-吡咯-3-基]甲基} -4-甲基哌嗪（BM212）的衍生物。本发明涉及所述化合物作为具有高活性和低毒性的抗结核剂以及获得中间体和最终化合物的方法的用途。

2. 发明授权

US07910581B2 Derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl] methyl}-4-methylpiperazine, synthesis process and uses thereof 失效
标题翻译： 1 - {[1,5-双（4-氯苯基）-2-甲基-1H-吡咯-3-基]甲基} -4-甲基哌嗪的衍生物，其合成方法和用途
公开(公告)号：US07910581B2
公开(公告)日：2011-03-22
申请号：US11817678
申请日：2006-03-03
申请人： Mariangela Biava , Fabrizio Manetti , Delia Deidda , Raffaello Pompei , Maurizio Botta , Giulio Cesare Porretta
发明人： Mariangela Biava , Fabrizio Manetti , Delia Deidda , Raffaello Pompei , Maurizio Botta , Giulio Cesare Porretta
IPC分类号： A61K31/541 , C07D417/06
CPC分类号： C07D207/335
摘要： The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low toxicity and process to obtain intermediates and final compounds.
摘要翻译：本发明涉及吡咯化合物，1 - {[1,5-双（4-氯苯基）-2-甲基-1H-吡咯-3-基]甲基} -4-甲基哌嗪（BM212）的衍生物。本发明涉及所述化合物作为具有高活性和低毒性的抗结核剂以及获得中间体和最终化合物的方法的用途。

3. 发明授权

US08012970B2 Derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine, synthesis process and uses thereof 失效
标题翻译： 1 - {[1,5-双（4-氯苯基）-2-甲基-1H-吡咯-3-基]甲基} -4-甲基哌嗪的衍生物，其合成方法和用途
公开(公告)号：US08012970B2
公开(公告)日：2011-09-06
申请号：US13033117
申请日：2011-02-23
申请人： Mariangela Biava , Fabrizio Manetti , Delia Deidda , Raffaello Pompei , Maurizio Botta , Giulio Cesare Porretta
发明人： Mariangela Biava , Fabrizio Manetti , Delia Deidda , Raffaello Pompei , Maurizio Botta , Giulio Cesare Porretta
IPC分类号： A61K31/5377 , C07D413/06
CPC分类号： C07D207/335
摘要： The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low toxicity and process to obtain intermediates and final compounds.
摘要翻译：本发明涉及吡咯化合物，1 - {[1,5-双（4-氯苯基）-2-甲基-1H-吡咯-3-基]甲基} -4-甲基哌嗪（BM212）的衍生物。本发明涉及所述化合物作为具有高活性和低毒性的抗结核剂以及获得中间体和最终化合物的方法的用途。

4. 发明授权

US08304410B2 Pyrrole compounds as inhibitors of mycobacteria, synthesis thereof and intermediates thereto 失效
标题翻译：吡咯化合物作为分枝杆菌的抑制剂，其合成及其中间体
公开(公告)号：US08304410B2
公开(公告)日：2012-11-06
申请号：US12679848
申请日：2008-09-25
申请人： Mariangela Biava , Giulio Cesare Porretta , Raffaello Pompei , Maurizio Botta , Fabrizio Manetti , Alessandro De Logu
发明人： Mariangela Biava , Giulio Cesare Porretta , Raffaello Pompei , Maurizio Botta , Fabrizio Manetti , Alessandro De Logu
IPC分类号： C07D207/33 , C07D417/06 , A61K31/402
CPC分类号： C07D207/335
摘要： The present invention relates to compounds having formula 3 as well as the synthesis, intermediates and methods of using the same.
摘要翻译：本发明涉及具有式3的化合物及其合成，中间体和使用方法。

5. 发明申请

US20100197672A1 PYRROLE COMPOUNDS AS INHIBITORS OF MYCOBACTERIA, SYNTHESIS THEREOF AND INTERMEDIATES THERETO 失效
标题翻译：作为MYCOBACTERIA的抑制剂的PYROROLE化合物，其合成及其中间体
公开(公告)号：US20100197672A1
公开(公告)日：2010-08-05
申请号：US12679848
申请日：2008-09-25
申请人： Mariangela Biava , Giulio Cesare Porretta , Raffaello Pompei , Maurizio Botta , Fabrizio Manetti , Alessandro De Logu
发明人： Mariangela Biava , Giulio Cesare Porretta , Raffaello Pompei , Maurizio Botta , Fabrizio Manetti , Alessandro De Logu
IPC分类号： A61K31/541 , C07D417/12 , A61P31/06 , C07D403/06 , A61K31/496 , C07D413/06 , A61K31/5355 , C07D401/06 , A61K31/454
CPC分类号： C07D207/335
摘要： The present invention relates to a compound having the general formula (3): synthesis, intermediates and uses thereof.
摘要翻译：本发明涉及具有通式（3）的化合物：其合成，中间体和用途。

6. 发明授权

US09162979B2 1,5-Diary1-2-alkylpyrrole-3-substituted nitro esters, selective COX-2 inhibitors and nitric oxide donors 有权
标题翻译： 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。

7. 发明授权

US07906551B2 3-substituted-1,5-diarly-2-alkyl-pyrroles highly selective and orally effective COX-2 inhibitors 有权
标题翻译： 3-取代-1,5-二烯-2-烷基吡咯高选择性和口服有效的COX-2抑制剂
公开(公告)号：US07906551B2
公开(公告)日：2011-03-15
申请号：US12375650
申请日：2006-08-03
申请人： Andrea Cappelli , Maurizio Anzini , Mariangela Biava , Francesco Makovec , Antonio Giordani , Gianfranco Caselli , Lucio Claudio Rovati
发明人： Andrea Cappelli , Maurizio Anzini , Mariangela Biava , Francesco Makovec , Antonio Giordani , Gianfranco Caselli , Lucio Claudio Rovati
IPC分类号： A61K31/40 , C07D207/30
CPC分类号： C07D207/333 , C07D207/337
摘要： This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position -3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position -1 and -5 are variously substituted, but compounds of particular interest are those substituted in position -5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups.
摘要翻译：本发明涉及式I的3-取代-1,5-二芳基-2-烷基吡咯，含有它们的药物组合物及其用于药理学治疗疼痛和COX-2过激活相关病症的用途。本发明的化合物是具有吡咯环位置-3的新的吡咯衍生物，几种各种功能化的，非脂肪族的侧链，赋予化合物相关的COX-2效力和选择性以及显着的口服功效。位置-1和-5的苯环被不同地取代，但特别感兴趣的化合物是在位置-5与4-甲基磺酰基 - 苯基或与4-氨基磺酰基 - 苯基取代的那些。

8. 发明申请

US20130165494A1 1,5-Diaryl-2-alkylpyrrole-3-Substituted Nitro Esters, Selective COX-2 Inhibitors and Nitric Oxide Donors 有权
标题翻译： 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。

9. 发明申请

US20090264500A1 3-SUBSTITUTED-1,5-DIARLY-2-ALKYL-PYRROLES HIGHLY SELECTIVE AND ORALLY EFFECTIVE COX-2 INHIBITORS 有权
标题翻译： 3-取代的-1,5-二-2-甲基-2-吡咯烷酮高选择性和有效的COX-2抑制剂
公开(公告)号：US20090264500A1
公开(公告)日：2009-10-22
申请号：US12375650
申请日：2006-08-03
申请人： Andrea Cappelli , Maurizio Anzini , Mariangela Biava , Francesco Makovec , Antonio Giordani , Gianfranco Caselli , Lucio Claudio Rovati
发明人： Andrea Cappelli , Maurizio Anzini , Mariangela Biava , Francesco Makovec , Antonio Giordani , Gianfranco Caselli , Lucio Claudio Rovati
IPC分类号： A61K31/40 , C07D207/30
CPC分类号： C07D207/333 , C07D207/337
摘要： This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position-3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position-1 and -5 are variously substituted, but compounds of particular interest are those substituted in position-5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups.
摘要翻译：本发明涉及式I的3-取代-1,5-二芳基-2-烷基吡咯，含有它们的药物组合物及其用于药理学治疗疼痛和COX-2过激活相关病症的用途。本发明化合物是具有吡咯环位置3的新型吡咯衍生物，几种不同官能化的非脂族侧链，赋予化合物相关COX-2效能和选择性以及显着的口服功效。位置-1和-5中的苯环被不同地取代，但特别感兴趣的化合物是在位置-5与4-甲基磺酰基 - 苯基或与4-氨基磺酰基 - 苯基取代的那些。

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