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1. 发明授权

US08003693B2 Modulation of anxiety through blockade of anandamide hydrolysis 有权
标题翻译：通过封闭anandamide水解调节焦虑
公开(公告)号：US08003693B2
公开(公告)日：2011-08-23
申请号：US11496051
申请日：2006-07-28
申请人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
发明人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
IPC分类号： A61K31/27
CPC分类号： C07C311/29 , C07C271/56 , C07C275/54 , C07C2601/14 , C07D209/08 , C07D211/06 , C07D215/06 , C07D307/79 , C07D487/04
摘要： Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.
摘要翻译：提供了下式的脂肪酸酰胺水解酶抑制剂：其中X是NH，CH 2，O或S; Q是O或S; Z是O或N; R是选自取代或未取代的芳基的芳族部分; 取代或未取代的联苯基，取代或未取代的萘基和取代或未取代的苯基; 取代或未取代的三联苯基; 取代或未取代的环烷基，杂芳基或烷基; 并且R 1和R 2独立地选自H，取代或未取代的烷基，取代或未取代的杂烷基和取代或未取代的苯基，取代或未取代的联苯基，取代或未取代的芳基和取代或未取代的杂芳基; 条件是如果Z是O，则不存在R 1和R 2之一，并且如果Z是N，则任选地R 1和R 2可以任选地一起形成取代或未取代的N-杂环或具有取代或未取代的杂芳基，其中N 它们各自附着的原子。提供了包含式I化合物的药物组合物及其用于抑制FAAH和/或治疗食欲障碍，青光眼，疼痛，失眠以及包括焦虑障碍，癫痫和抑郁症在内的神经和心理障碍的方法。

2. 发明申请

US20090082435A1 Methods, Compositions, And Compounds For Modulation Of Monoacylglycerol Lipase, Pain, And Stress-Related Disorders 审中-公开
标题翻译：用于调节单酰甘油脂肪酶，疼痛和应激相关疾病的方法，组合物和化合物
公开(公告)号：US20090082435A1
公开(公告)日：2009-03-26
申请号：US11912386
申请日：2006-04-26
申请人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia , Andrea Hohmann
发明人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia , Andrea Hohmann
IPC分类号： A61K31/27 , C12Q1/44 , C07C271/02 , C12N9/18 , A61P29/00
CPC分类号： A61K31/17
摘要： Methods, compositions, and compounds for inhibiting monoacyglycerol lipase, and for treating pain, for modulating stress-induced analgesia or for treating stress-induced disorders in mammals are provided.
摘要翻译：提供了用于抑制单甘油脂肪酶和用于治疗疼痛，调节应激诱导的镇痛或用于治疗哺乳动物中的应激诱导的疾病的方法，组合物和化合物。

3. 发明授权

US5580895A 1,5-benzodiazepine derivatives 失效
标题翻译： 1,5-苯并二氮杂衍生物
公开(公告)号：US5580895A
公开(公告)日：1996-12-03
申请号：US256359
申请日：1994-07-20
申请人： Harry Finch , David G. Trist , Giorgio Tarzia , Aldo Feriani
发明人： Harry Finch , David G. Trist , Giorgio Tarzia , Aldo Feriani
IPC分类号： A61K31/55 , A61K31/551 , A61P1/00 , A61P1/04 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07D243/12 , A61K38/00 , C07D403/12
CPC分类号： C07D243/12
摘要： The present invention relates to compounds of formula (I) which are antagonists of gastrin and CCK-B receptors. The compounds of formula (I) are 1,5-benzodiazepine derivatives. ##STR1##
摘要翻译： PCT No.PCT / EP93 / 00098 Sec。 371日期：1994年7月20日 102（e）日期1994年7月20日PCT 1993年1月15日PCT公布。公开号WO93 / 14074 日期：1993年7月22日本发明涉及作为胃泌素和CCK-B受体拮抗剂的式（I）化合物。式（I）化合物是1,5-苯并二氮杂衍生物。（一）

4. 发明授权

US4211709A Aminopyrrole derivatives 失效
标题翻译：氨基吡咯衍生物
公开(公告)号：US4211709A
公开(公告)日：1980-07-08
申请号：US960386
申请日：1978-11-13
申请人： Giorgio Tarzia , Gianbattista Panzone
发明人： Giorgio Tarzia , Gianbattista Panzone
IPC分类号： C07D207/34 , C07D207/36 , C07D209/40 , C07D207/44
CPC分类号： C07D209/40 , C07D207/34 , C07D207/36
摘要： Pharmacologically-active aminopyrrole derivatives of the formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, benzyl and chlorobenzyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, phenyl and phenyl substituted by a radical selected from methyl, ethyl, methoxy, ethoxy, benzyloxy, fluoro, chloro and bromo;R.sub.2 and R.sub.3 individually represent hydrogen or (C.sub.1-4)alkyl or, taken together, represent an isopropylidene, a benzylidene or a chlorobenzylidene radical;R.sub.4 is selected from (C.sub.2-4)alkanoyl; carbo(C.sub.1-3)alkoxy; benzoyl, benzoyl substituted by a radical selected from chloro, methoxy or ethoxy; carbamoyl, methylcarbamoyl and phenyl carbamoyl;R.sub.5 is selected from hydrogen, (C.sub.1-4)alkyl, carbo(C.sub.1-3)alkoxy, carbomethoxymethyl, carbethoxymethyl, trifluoromethyl and carbamoyl, with the proviso that when R is hydrogen, R.sub.1 and R.sub.5 are methyl and R.sub.4 is carbethoxy, and R.sub.2 and R.sub.3 cannot simultaneously represent hydrogen;and a salt thereof with a pharmaceutically-acceptable acid.The compounds have anti-inflammatory and CNS-depressant utility. They are also useful as analgesics and antipyretics and display a very low degree of anti-ulcerogenic activity.
摘要翻译：式（Ia）的药理学活性氨基吡咯衍生物，其中：R选自氢，（C 1-4）烷基，苄基和氯苄基; R 1选自氢，（C 1-4）烷基，苯基和被选自甲基，乙基，甲氧基，乙氧基，苄氧基，氟，氯和溴的基团取代的苯基; R2和R3分别表示氢或（C1-4）烷基，或者一起表示异亚丙基，亚苄基或氯亚苄基; R4选自（C2-4）烷酰基; 碳（C 1-3）烷氧基; 苯甲酰基，被选自氯，甲氧基或乙氧基的基团取代的苯甲酰基; 氨基甲酰基，甲基氨基甲酰基和苯基氨基甲酰基; R 5选自氢，（C 1-4）烷基，碳（C 1-3）烷氧基，甲酯基甲基，乙氧羰基甲基，三氟甲基和氨基甲酰基，条件是当R为氢时，R 1和R 5为甲基，R 4为乙氧羰基，而R3不能同时代表氢; 及其与药学上可接受的酸的盐。该化合物具有抗炎和CNS抑制作用。它们也可用作镇痛药和解热药，并显示非常低程度的抗溃疡活性。

5. 发明授权

US4072689A Monoamino 2,4,5-trisubstituted oxazoles 失效
标题翻译：单氨基2,4,5-三取代的恶唑
公开(公告)号：US4072689A
公开(公告)日：1978-02-07
申请号：US641410
申请日：1975-12-17
申请人： Giorgio Tarzia
发明人： Giorgio Tarzia
IPC分类号： C07D263/34
CPC分类号： C07D263/34
摘要： Pharmacologically active 2,4,5-trisubstituted oxazoles of the general formula ##STR1## wherein A is cyclohexyl, thienyl or a group of the formula ##STR2## in which R represents one to three substituents each independently selected from the group consisting of hydrogen, lower alkyl, halo, halo-lower alkyl, lower alkoxy, nitro, cyano, amino, carbamoyl, acetamino or carboxy; one of the R.sub.1 and R.sub.2 groups is a lower alkyl group and the other is an amido group, ##STR3## wherein R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, cycloalkyl, phenyl, substituted phenyl, phenyl-lower alkyl, hydroxy-lower alkyl, lower acyloxy-lower alkyl, hydroxy, amino, lower alkylideneamino, cycloalkylideneamino, benzylideneamino and R.sub.4 is selected from hydrogen, lower alkyl, lower alkenyl, cycloalkyl, phenyl, substituted phenyl, phenyl-lower alkyl, hydroxy-lower alkyl, lower acyloxy-lower alkyl, or R.sub.3 and R.sub.4 taken together with the nitrogen atom may also form a 5- to 7-membered hetero ring which may contain one other hetero atom selected from N, O and S. The compounds have antiinflammatory activity.
摘要翻译：其中A是环己基，噻吩基或式“IMAGE”的基团，其中R表示一至三个独立地选自以下的取代基的药学活性的2,4,5-三取代的恶唑：氢，低级烷基，卤素，卤代低级烷基，低级烷氧基，硝基，氰基，氨基，氨基甲酰基，乙酰氨基或羧基; R1和R2之一是低级烷基，另一个是酰胺基，其中R 3选自氢，低级烷基，低级烯基，环烷基，苯基，取代的苯基，苯基 - 低级烷基，羟基 - 低级烷基，低级酰氧基 - 低级烷基，羟基，氨基，低级亚烷基氨基，亚环烷基氨基，亚苄基氨基和R4选自氢，低级烷基，低级烯基，环烷基，苯基，取代的苯基，苯基 - 低级烷基，低级烷基，低级酰氧基 - 低级烷基或R3和R4与氮原子一起也可以形成5-7元杂环，其可以含有选自N，O和S的另一个杂原子。该化合物具有抗炎作用活动。

6. 发明授权

US09133197B2 Oxidated derivatives of triazolylpurines useful as ligands of the adenosine A2A receptor and their use as medicaments 有权
标题翻译：可用作腺苷A2A受体的配体的三唑基嘌呤的氧化衍生物及其作为药物的用途
公开(公告)号：US09133197B2
公开(公告)日：2015-09-15
申请号：US13257750
申请日：2010-03-18
申请人： Walter Cabri , Patrizia Minetti , Giovanni Piersanti , Giorgio Tarzia
发明人： Walter Cabri , Patrizia Minetti , Giovanni Piersanti , Giorgio Tarzia
IPC分类号： C07D473/34
CPC分类号： C07D473/34 , A61K31/198 , A61K31/52
摘要： The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient.
摘要翻译：本发明涉及式（I）的新的三唑基嘌呤衍生物，其制备方法和含有它们的药物组合物，用于治疗神经障碍或脑缺血，其中腺苷A2A受体的抑制将导致改善健康状态病人。

7. 发明申请

US20120053191A1 OXIDATED DERIVATIVES OF TRIAZOLYLPURINES USEFUL AS LIGANDS OF THE ADENOSINE A2A RECEPTOR AND THEIR USE AS MEDICAMENTS 有权
标题翻译：作为腺苷A2A受体的配体及其作为药物使用的三唑来膦的氧化衍生物有用
公开(公告)号：US20120053191A1
公开(公告)日：2012-03-01
申请号：US13257750
申请日：2010-03-18
申请人： Walter Cabri , Patrizia Minetti , Giovanni Piersanti , Giorgio Tarzia
发明人： Walter Cabri , Patrizia Minetti , Giovanni Piersanti , Giorgio Tarzia
IPC分类号： A61K31/52 , A61P3/00 , A61P25/28 , A61P25/14 , C07D473/34 , A61P25/16
CPC分类号： C07D473/34 , A61K31/198 , A61K31/52
摘要： The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient.
摘要翻译：本发明涉及式（I）的新的三唑基嘌呤衍生物，其制备方法和含有它们的药物组合物，用于治疗神经障碍或脑缺血，其中腺苷A2A受体的抑制将导致改善健康状态病人。

8. 发明申请

US20120010283A1 MODULATION OF ANXIETY THROUGH BLOCKADE OF ANANDAMIDE HYDROLYSIS 审中-公开
标题翻译：通过水杨苷水解的片段调节
公开(公告)号：US20120010283A1
公开(公告)日：2012-01-12
申请号：US13211219
申请日：2011-08-16
申请人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
发明人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
IPC分类号： A61K31/27 , C07C255/60 , A61P27/06 , A61P25/04 , A61P25/22 , A61P25/08 , A61P25/18 , C07C271/56 , A61P25/24
CPC分类号： C07C311/29 , C07C271/56 , C07C275/54 , C07C2601/14 , C07D209/08 , C07D211/06 , C07D215/06 , C07D307/79 , C07D487/04
摘要： Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.
摘要翻译：提供了下式的脂肪酸酰胺水解酶抑制剂：其中X是NH，CH 2，O或S; Q是O或S; Z是O或N; R是选自取代或未取代的芳基的芳族部分; 取代或未取代的联苯基，取代或未取代的萘基和取代或未取代的苯基; 取代或未取代的三联苯基; 取代或未取代的环烷基，杂芳基或烷基; 并且R 1和R 2独立地选自H，取代或未取代的烷基，取代或未取代的杂烷基和取代或未取代的苯基，取代或未取代的联苯基，取代或未取代的芳基和取代或未取代的杂芳基; 条件是如果Z是O，则不存在R 1和R 2之一，并且如果Z是N，则任选地R 1和R 2可以任选地一起形成取代或未取代的N-杂环或具有取代或未取代的杂芳基，其中N 它们各自附着的原子。提供了包含式I化合物的药物组合物及其用于抑制FAAH和/或治疗食欲障碍，青光眼，疼痛，失眠以及包括焦虑障碍，癫痫和抑郁症在内的神经和心理障碍的方法。

9. 发明授权

US5198418A Substituted alkylamides of teicoplanin compounds 失效
标题翻译：替考拉宁化合物的取代烷基酰胺
公开(公告)号：US5198418A
公开(公告)日：1993-03-30
申请号：US826198
申请日：1992-01-21
申请人： Adriano Malabarba , Giorgio Tarzia
发明人： Adriano Malabarba , Giorgio Tarzia
IPC分类号： C07K9/00
CPC分类号： C07K9/008
摘要： The present invention is directed to teicoplanin derivatives in which position 63 of the glycopeptide core is substituted with a substituted alkylamide.
摘要翻译：本发明涉及替考拉宁衍生物，其中糖肽核心的位置63被取代的烷基酰胺取代。

10. 发明授权

US4789661A De-(acetylglucosaminyl)-di(dehydro)-deoxy teicoplanin derivatives 失效
标题翻译：去乙酰葡糖胺基 - 二（脱氢）脱氧替考拉宁衍生物
公开(公告)号：US4789661A
公开(公告)日：1988-12-06
申请号：US102198
申请日：1987-07-17
申请人： Adriano Malabarba , Aldo Trani , Pietro Ferrari , Giorgio Tarzia
发明人： Adriano Malabarba , Aldo Trani , Pietro Ferrari , Giorgio Tarzia
IPC分类号： C07K1/113 , A61K38/00 , C07K1/02 , C07K7/06 , C07K7/64 , C07K9/00 , A61K37/02 , C07K7/50
CPC分类号： C07K9/008 , Y10S930/19 , Y10S930/27
摘要： The present invention is directed to new de-(acetylglucosaminyl-di(dehydro)deoxy teicoplanin derivatives which possess antibiotic activity mainly against gram positive bacteria.The new compounds are obtained by chemical modification of a teicoplanin antibiotic substance.
摘要翻译：本发明涉及具有主要抗革兰氏阳性菌的抗生素活性的新的脱（乙酰葡糖胺基 - 二（脱氢）脱氧替考拉宁衍生物），新化合物是通过化学改性替考拉宁抗生素物质获得的。

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