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21. 发明申请

US20090227609A1 AMIDINE DERIVATIVES OF 2-HETEROARYL-QUINAZOLINES AND QUINOLINES; POTENT ANALGESICS AND ANTI-INFLAMMATORY AGENTS 有权
标题翻译： 2-异喹啉和喹啉的氨基衍生物; POTENT ANALGESICS和抗炎药物
公开(公告)号：US20090227609A1
公开(公告)日：2009-09-10
申请号：US12376066
申请日：2006-07-31
申请人： Antonio Giordani , Stefano Mandelli , Simona Zanzola , Francesca Tarchino , Gianfranco Caselli , Teresa Simonetta Fiorentino , Silvio Mazzari , Francesco Makovec , Lucio Claudio Rovati
发明人： Antonio Giordani , Stefano Mandelli , Simona Zanzola , Francesca Tarchino , Gianfranco Caselli , Teresa Simonetta Fiorentino , Silvio Mazzari , Francesco Makovec , Lucio Claudio Rovati
IPC分类号： A61K31/517 , C07D239/72 , C07D215/38 , A61K31/4709 , A61P37/06 , A61P29/00
CPC分类号： C07D405/04
摘要： The present invention concerns novel amidines derivatives of 2-heteroaryl-quinazoline and quinolines of general formula (I), to a process for their preparation, to their pharmaceutical compositions and to the use of these compounds, salts and solvates thereof, along with the corresponding pharmaceutical compositions, for the treatment of pain and inflammatory disorders. Compounds of this invention are extremely potent analgesics, suitable for the treatment of both inflammatory and neuropathic pain. Particularly for the treatment of neuropathic pain the compounds of the invention have been proved largely superior to the standards currently in the clinical use. These compounds are not acting through inhibition of COX or NOS enzymes but are effective in inhibiting inflammatory cytokine production induced by inflammatory stimuli.
摘要翻译：本发明涉及通式（I）的2-杂芳基 - 喹唑啉和喹啉的新型脒衍生物，其制备方法，其药物组合物以及这些化合物，其盐和溶剂合物的用途以及相应的药物组合物，用于治疗疼痛和炎症性疾病。本发明的化合物是非常有效的止痛剂，适用于治疗炎性和神经性疼痛。特别是对于神经性疼痛的治疗，本发明的化合物已被证明在很大程度上优于目前在临床应用中的标准。这些化合物不是通过抑制COX或NOS酶而起作用，而是有效抑制由炎症刺激引起的炎性细胞因子产生。

22. 发明申请

US20050197331A1 Novel anti-inflammatory and analgesic heterocyclic amidines that inhibit nitrogen oxide (NO) production 有权
标题翻译：抑制氮氧化物（NO）生产的新型抗炎和止痛杂环脒
公开(公告)号：US20050197331A1
公开(公告)日：2005-09-08
申请号：US11068347
申请日：2005-03-01
申请人： Francesco Makovec , Antonio Giordani , Roberto Artusi , Stefano Mandelli , Ilario Verpilio , Simona Zanzola , Lucio Rovati
发明人： Francesco Makovec , Antonio Giordani , Roberto Artusi , Stefano Mandelli , Ilario Verpilio , Simona Zanzola , Lucio Rovati
IPC分类号： A61K31/343 , A61K31/4045 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/47 , A61K31/517 , A61P1/04 , A61P19/02 , A61P29/00 , A61P37/06 , A61P43/00 , C07D209/08 , C07D215/38 , C07D217/02 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/18 , C07D237/28 , C07D239/74 , C07D263/56 , C07D263/57 , C07D277/64 , C07D277/66 , C07D307/79 , C07D333/54 , C07D403/04 , C07D405/04 , C07D409/04 , C07D417/04 , C07D498/02
CPC分类号： C07D215/06 , C07D209/08 , C07D217/04 , C07D235/08 , C07D235/18 , C07D239/74 , C07D263/57 , C07D277/64 , C07D277/66 , C07D307/79 , C07D333/54 , C07D403/04 , C07D405/04 , C07D409/04 , C07D417/04
摘要： Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which: G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; and Z is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.
摘要翻译：具有抑制氮氧化物生成的抗炎和止痛活性的式（I）的杂环脒：其中：G 1和G 2是氢，卤素，羟基， C 1 -C 4烷氧基，C 1 -C 4烷基和式Q的脒基取代基，条件是对于式（I）的每种化合物，两个取代基G 1或G 2中只有一个是式Q的脒基取代基，并且其中取代基 W，Y和X组合形成在相同环中含有至多2个杂原子的9元或10元双环杂芳族衍生物; Z是芳基或杂芳基，直链或支链C 1 -C 6烷基或烯基链，C 1 -C 3烷基或链烯基，烷基 - 芳基或C 1 -C 4烷基 - 杂芳基。

23. 发明授权

US5973006A Fluoro-substituted benzoylpropionic acid derivatives 失效
标题翻译：氟取代的苯甲酰基丙酸衍生物
公开(公告)号：US5973006A
公开(公告)日：1999-10-26
申请号：US51486
申请日：1998-04-20
申请人： Mario Varasi , Antonio Giordani , Carmela Speciale , Massimo Cini , Alberto Bianchetti
发明人： Mario Varasi , Antonio Giordani , Carmela Speciale , Massimo Cini , Alberto Bianchetti
IPC分类号： A61K31/00 , A61K31/165 , A61K31/195 , A61K31/197 , A61K31/22 , A61P5/36 , A61P25/08 , A61P25/16 , A61P25/28 , C07C227/12 , C07C229/36 , C07C237/20 , C07C259/06 , A01N37/12 , A01N37/18 , C07C229/28 , C07C233/05
CPC分类号： C07C259/06 , C07C229/36 , C07C237/20
摘要： A fluoro-substituted benzoylpropionic acid compound of formula (I) either as a single optical isomer or as a mixture of optical isomers ##STR1## wherein R is hydroxy, amino, hydroxylamine, --OR', --NHR', N(R').sub.2 or --NHOR' in which R' is C.sub.1 -C.sub.6 alkyl or benzyl;or a pharmaceutically acceptable salt thereof.
摘要翻译： PCT No.PCT / EP96 / 04321 Sec。 371日期：1998年4月20日 102（e）1998年4月20日PCT PCT 1996年10月4日PCT公布。第WO97 / 15550号公报日期：1997年5月1日一种式（I）的氟取代的苯甲酰基丙酸化合物作为单一光学异构体或作为光学异构体的混合物，其中R是羟基，氨基，羟胺，-OR'，-NHR'，N（R' ）2或-NHOR'，其中R'是C 1 -C 6烷基或苄基; 或其药学上可接受的盐。

24. 发明授权

US4994450A Azacyclic compounds and their use as analgesic agents 失效
标题翻译：氮环化合物及其作为止痛剂的用途
公开(公告)号：US4994450A
公开(公告)日：1991-02-19
申请号：US309687
申请日：1989-02-10
申请人： Vittorio Vecchietti , Antonio Giordani
发明人： Vittorio Vecchietti , Antonio Giordani
IPC分类号： C07D223/04 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/55 , A61P25/04 , C07D211/26 , C07D225/02 , C07D409/06
CPC分类号： C07D409/06 , C07D211/26
摘要： A compound, or a solvate or salt thereof, of formula (I) ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear 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;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;p is 1, 2, 3 or 4, andR is a group of formula (II) ##STR2## in which the group --(CHR.sub.4).sub.n --X-- is in the meta- or para-position with respect to YR.sub.5 or R.sub.6, R.sub.4 is hydrogen or C.sub.1-6 alkyl, preferably hydrogen;n is 0, 1 or 2, preferably 1;X is a direct bond, or O, S or NR.sub.a in which R.sub.a is hydrogen or C.sub.1-6 alkyl, and is preferably a direct bond;Y is >C.dbd.O, >CHOH, --S.dbd.O or --SO.sub.2 ; each of R.sub.5 and R.sub.6 is C.sub.1-6 alkyl, orR.sub.5 and R.sub.6 are linked together and R.sub.5 represents --(Z).sub.m -- where m is 0 or 1 and Z is O, S or NR.sub.7 where R.sub.7 is hydrogen or C.sub.1-6 alkyl, andR.sub.6 represents --(CH.sub.2).sub.9 -- where q is an integer of from 1 to 4, preferably 2 or 3, and in which one or more of the --(CH.sub.2)-- groups is optionally substituted by a C.sub.1-6 alkyl group, is useful for the treatment of pain.

25. 发明授权

US4801585A Cyclic carboxamide derivatives and their use as analgesics 失效
标题翻译：环状羧酰胺衍生物及其用作镇痛药
公开(公告)号：US4801585A
公开(公告)日：1989-01-31
申请号：US945038
申请日：1986-12-22
申请人： Vittorio Vecchietti , Massimo Signorini , Antonio Giordani
发明人： Vittorio Vecchietti , Massimo Signorini , Antonio Giordani
IPC分类号： C07D207/09 , C07D211/26 , C07D223/04 , A61K31/55 , A61K31/455 , C07D401/06
CPC分类号： C07D223/04 , C07D207/09 , C07D211/26
摘要： A compound of formula (I): ##STR1## or a salt or solvate thereof in which R. CO is an acyl group containing a substituted or unsubstituted carbocyclic or heterocyclic aromatic ring, R.sub.1 and R.sub.2 are independently C.sub.1-6 alkyl or together form a C.sub.3-6 polymethylene or alkylene group, and p is 1, 2, 3 or 4, is useful for treating pain.
摘要翻译：式（I）的化合物：其中R CO为含有取代或未取代的碳环或杂环芳环的酰基的盐或其溶剂化物，R 1和R 2独立地为C 1-6烷基或一起形成C3-6聚亚甲基或亚烷基，p为1,2,3或4，可用于治疗疼痛。

26. 发明授权

US09174966B2 Crystalline forms of 6-(1H-imidazol-1-yl)-2-phenylquinazoline 有权
标题翻译： 6-（1H-咪唑-1-基）-2-苯基喹唑啉的结晶形式
公开(公告)号：US09174966B2
公开(公告)日：2015-11-03
申请号：US13375816
申请日：2010-06-04
申请人： Antonio Giordani , Stefano Mandelli , Francesca Porta , Matteo Ghirri , Lucio Claudio Rovati
发明人： Antonio Giordani , Stefano Mandelli , Francesca Porta , Matteo Ghirri , Lucio Claudio Rovati
IPC分类号： C07D403/04 , A61K31/517 , A01N43/54
CPC分类号： C07D403/04 , A01N43/54 , A61K31/517
摘要： The present invention relates to the solid state of 6-(1H-imidazol-1-yl)-2-phenylquinazoline (I) and therefore to novel crystalline forms of the base and of pharmaceutically acceptable salts and solvates thereof, and also to methods for preparing them, to the respective pharmaceutical formulations and to their therapeutic use. Compound (I) may be obtained as the free base in five different crystalline forms, three polymorphic forms and two hydrates. Some pharmaceutically acceptable salts of (I) that have physicochemical characteristics acceptable for pharmaceutical development were obtained, and the respective polymorphic forms and/or hydrates were characterized.
摘要翻译：本发明涉及6-（1H-咪唑-1-基）-2-苯基喹唑啉（I）的固态，因此涉及碱的新型结晶形式及其药学上可接受的盐和溶剂合物，以及涉及制备它们，各自的药物制剂及其治疗用途。化合物（I）可以以五种不同的晶型，三种多晶型和两种水合物形式获得为游离碱。获得了具有药物发育可接受的物理化学特性的（I）的一些药学上可接受的盐，并对其各自的多晶型和/或水合物进行了表征。

27. 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。

28. 发明申请

US20110257209A1 6-1H-IMIDAZO-QUINAZOLINE AND QUINOLINES DERIVATIVES, NEW POTENT ANALGESICS AND ANTI-INFLAMMATORY AGENTS 有权
标题翻译： 6-1H-IMIDAZO-喹唑啉和喹啉衍生物，新的药物和抗炎药物
公开(公告)号：US20110257209A1
公开(公告)日：2011-10-20
申请号：US13169350
申请日：2011-06-27
申请人： Antonio GIORDANI , Stefano MANDELLI , Ilario VERPILIO , Simona ZANZOLA , Francesca TARCHINO , Gianfranco CASELLI , Tiziana Piepoli , Silvio MAZZARI , Francesco MAKOVEC , Lucio Claudio ROVATI
发明人： Antonio GIORDANI , Stefano MANDELLI , Ilario VERPILIO , Simona ZANZOLA , Francesca TARCHINO , Gianfranco CASELLI , Tiziana Piepoli , Silvio MAZZARI , Francesco MAKOVEC , Lucio Claudio ROVATI
IPC分类号： A61K31/517 , A61P25/00 , A61K31/4709
CPC分类号： C07D413/14 , C07D401/04 , C07D403/04 , C07D405/14 , C07D409/14
摘要： The present invention is directed to novel 6-1H-imidazo-2-aryl and 2-heteroaryl quinazoline and quinoline of formula I, corresponding salts and solvates thereof, to a process for their preparation and to the use of this compounds and corresponding pharmaceutical composition for the treatment of pain and inflammatory related disorders. Compounds of the invention have been proven highly effective in the pharmacological treatment of both inflammatory and neuropathic pain, in addition to striking anti-inflammatory properties. Their effectiveness in interfering with COX-2 and inflammatory cytokines expressions and production, highlights them as interesting compounds also for the treatment of cancer in addition to several inflammatory diseases.
摘要翻译：本发明涉及式I的新颖的6-1H-咪唑-2-芳基和2-杂芳基喹唑啉和喹啉，其相应的盐和溶剂合物，其制备方法和该化合物及相应的药物组合物的用途用于治疗疼痛和炎症相关疾病。除了具有显着的抗炎特性之外，本发明的化合物已经被证明在炎性和神经性疼痛的药理学治疗中都是非常有效的。它们在干扰COX-2和炎性细胞因子表达和产生方面的有效性，也将它们作为有趣的化合物，也用于治疗癌症以及多种炎性疾病。

29. 发明授权

US07994181B2 6-1H-imidazo-quinazoline and quinolines derivatives, new potent analgesics and anti-inflammatory agents 有权
标题翻译： 6-1H-咪唑并喹唑啉和喹啉衍生物，新型强效止痛剂和抗炎剂
公开(公告)号：US07994181B2
公开(公告)日：2011-08-09
申请号：US12376080
申请日：2006-08-03
申请人： Antonio Giordani , Stefano Mandelli , Ilario Verpilio , Simona Zanzola , Francesca Tarchino , Gianfranco Caselli , Tiziana Piepoli , Silvio Mazzari , Francesco Makovec , Lucio Claudio Rovati
发明人： Antonio Giordani , Stefano Mandelli , Ilario Verpilio , Simona Zanzola , Francesca Tarchino , Gianfranco Caselli , Tiziana Piepoli , Silvio Mazzari , Francesco Makovec , Lucio Claudio Rovati
IPC分类号： A61K31/517
CPC分类号： C07D413/14 , C07D401/04 , C07D403/04 , C07D405/14 , C07D409/14
摘要： The present invention is directed to novel 6-1H-imidazo-2-aryl and 2-heteroaryl quinazoline and quinoline of formula I, corresponding salts and solvates thereof, to a process for their preparation and to the use of this compounds and corresponding pharmaceutical composition for the treatment of pain and inflammatory related disorders. Compounds of the invention have been proven highly effective in the pharmacological treatment of both inflammatory and neuropathic pain, in addition to striking anti-inflammatory properties. Their effectiveness in interfering with COX-2 and inflammatory cytokines expressions and production, highlights them as interesting compounds also for the treatment of cancer in addition to several inflammatory diseases.Formula I:
摘要翻译：本发明涉及式I的新颖的6-1H-咪唑-2-芳基和2-杂芳基喹唑啉和喹啉，其相应的盐和溶剂合物，其制备方法和该化合物及相应的药物组合物的用途用于治疗疼痛和炎症相关疾病。除了具有显着的抗炎特性之外，本发明的化合物已经被证明在炎性和神经性疼痛的药理学治疗中都是非常有效的。它们在干扰COX-2和炎性细胞因子表达和产生方面的有效性，也将它们作为有趣的化合物，也用于治疗癌症以及多种炎性疾病。公式I：

30. 发明授权

US07968558B2 Amidine derivatives of 2-heteroaryl-quinazolines and quinolines; potent analgesics and anti-inflammatory agents 有权
标题翻译： 2-杂芳基 - 喹唑啉和喹啉的脒衍生物; 强效止痛剂和抗炎剂
公开(公告)号：US07968558B2
公开(公告)日：2011-06-28
申请号：US12376066
申请日：2006-07-31
申请人： Antonio Giordani , Stefano Mandelli , Simona Zanzola , Francesca Tarchino , Gianfranco Caselli , Teresa Simonetta Fiorentino , Silvio Mazzari , Francesco Makovec , Lucio Claudio Rovati
发明人： Antonio Giordani , Stefano Mandelli , Simona Zanzola , Francesca Tarchino , Gianfranco Caselli , Teresa Simonetta Fiorentino , Silvio Mazzari , Francesco Makovec , Lucio Claudio Rovati
IPC分类号： A61K31/517
CPC分类号： C07D405/04
摘要： The present invention concerns novel amidines derivatives of 2-heteroaryl-quinazoline and quinolines of general formula (I), to a process for their preparation, to their pharmaceutical compositions and to the use of these compounds, salts and solvates thereof, along with the corresponding pharmaceutical compositions, for the treatment of pain and inflammatory disorders. Compounds of this invention are extremely potent analgesics, suitable for the treatment of both inflammatory and neuropathic pain. Particularly for the treatment of neuropathic pain the compounds of the invention have been proved largely superior to the standards currently in the clinical use. These compounds are not acting through inhibition of COX or NOS enzymes but are effective in inhibiting inflammatory cytokine production induced by inflammatory stimuli.
摘要翻译：本发明涉及通式（I）的2-杂芳基 - 喹唑啉和喹啉的新型脒衍生物，其制备方法，其药物组合物以及这些化合物，其盐和溶剂合物的用途以及相应的药物组合物，用于治疗疼痛和炎症性疾病。本发明的化合物是非常有效的止痛剂，适用于治疗炎性和神经性疼痛。特别是对于神经性疼痛的治疗，本发明的化合物已被证明在很大程度上优于目前在临床应用中的标准。这些化合物不是通过抑制COX或NOS酶而起作用，而是有效抑制由炎症刺激引起的炎性细胞因子产生。

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