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11. 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。

12. 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。

13. 发明授权

US4508730A 1,7-Dihydro-pyrrolo[3,4-e][1,4]diazepin-2(3H)-one derivatives a process for preparing them and their use as anticonvulsant and anti-anxiety agents 失效
标题翻译： 1,7-二氢 - 吡咯并[3,4-e] [1,4]二氮杂-2（3H） - 酮衍生物的制备方法及其作为抗惊厥和抗焦虑剂
公开(公告)号：US4508730A
公开(公告)日：1985-04-02
申请号：US521774
申请日：1983-08-09
申请人： Luigi Mariani , Giorgio Tarzia
发明人： Luigi Mariani , Giorgio Tarzia
IPC分类号： A61K31/55 , A61P25/08 , A61P25/20 , C07D207/34 , C07D487/04
CPC分类号： C07D487/04 , C07D207/34
摘要： 1,7-Dihydro-pyrrolo[3,4-e][1,4]diazepin-2(3H)-one derivatives of the formula ##STR1## wherein R is (C.sub.1-4)alkyl, R.sub.1 stands for hydrogen, methyl, ethyl, phenyl, bromo, chloro or nitro, R.sub.2 is hydrogen or (C.sub.1-4)alkyl, R.sub.3 represents hydrogen, chloro, fluoro, bromo, trifluoromethyl and methoxy, and X is ##STR2## wherein n is zero or 1, or --NH--R.sub.4 wherein R.sub.4 represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, or phenyl group.The novel compounds are useful as anticonvulsant and anti-anxiety agents.Also encompassed by the present invention are the process for preparing the novel pyrrolodiazepines and the pharmaceutical compositions containing them.
摘要翻译：其中R是（C 1-4）烷基，R 1代表氢，甲基（C 1 -C 4）烷基，，乙基，苯基，溴，氯或硝基，R 2是氢或（C 1-4）烷基，R 3表示氢，氯，氟，溴，三氟甲基和甲氧基，X是其中n是0或1， -NH-R4，其中R4表示取代或未取代的烷基，烯基，环烷基或苯基。新化合物可用作抗惊厥药和抗焦虑剂。本发明还包括制备新型吡咯并二氮杂的方法和含有它们的药物组合物。

14. 发明授权

US4402970A 1,7-Dihydro-pyrrolo[3,4-e][1,4]diazepin-2(1H)-one derivatives 失效
标题翻译： 1,7-二氢 - 吡咯并[3,4-e] [1,4]二氮杂-2（1H） - 酮衍生物
公开(公告)号：US4402970A
公开(公告)日：1983-09-06
申请号：US381272
申请日：1982-05-24
申请人： Luigi Mariani , Giorgio Tarzia
发明人： Luigi Mariani , Giorgio Tarzia
IPC分类号： A61K31/55 , A61P25/08 , A61P25/20 , C07D207/34 , C07D487/04
CPC分类号： C07D487/04 , C07D207/34
摘要： 1,7-Dihydro-pyrrolo[3,4-e][1,4]diazepin-2(1H)-ones of the formula ##STR1## wherein R is lower alkyl, R.sub.1 stands for hydrogen, methyl, ethyl or phenyl, R.sub.2 is hydrogen or lower alkyl and R.sub.3 is hydrogen, chloro, fluoro, bromo, trifluoromethyl or methoxy are described with anticonvulsant and anti-anxiety activity.Also described is the process for preparing the above compounds and pharmaceutical preparations containing them.
摘要翻译：其中R是低级烷基，R1代表氢，甲基，乙基或苯基的1,7-二氢 - 吡咯并[3,4-e] [1,4]二氮杂-2（1H） R2是氢或低级烷基，R3是氢，氯，氟，溴，三氟甲基或甲氧基被描述为抗惊厥和抗焦虑活性。还描述了制备上述化合物的方法和含有它们的药物制剂。

15. 发明授权

US09187413B2 Peripherally restricted FAAH inhibitors 有权
标题翻译：外周限制的FAAH抑制剂
公开(公告)号：US09187413B2
公开(公告)日：2015-11-17
申请号：US13812777
申请日：2011-07-22
申请人： Daniele Piomelli , Jason R. Clapper , Guillermo Moreno-Sanz , Andrea Duranti , Giovanna Guiducci , Marco Mor , Giorgio Tarzia
发明人： Daniele Piomelli , Jason R. Clapper , Guillermo Moreno-Sanz , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
IPC分类号： C07C233/00 , A61K31/265 , A61K31/16 , A61K31/165 , C07C271/56
CPC分类号： C07C271/56 , C07C2601/14
摘要： Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof. R2 and R3 are independently selected from the group consisting of hydrogen and substituted or unsubstituted hydrocarbyl; each R4 is independently selected from the group consisting of halogen and substituted or unsubstituted hydrocarbyl and n is an integer from 0 to 4; each R5 is independently selected from the group consisting of halo and substituted or unsubstituted hydrocarbyl and m is an integer from 0 to 3; and R6 is substituted or unsubstituted cyclohexyl; and the pharmaceutically acceptable salts thereof.
摘要翻译：提供脂肪酸酰胺水解酶（FAAH）的外周限制性抑制剂。该化合物可以抑制FAAH活性，并增加中枢神经系统（CNS）外的氨基酰胺水平。尽管它们相对不能进入脑和脊髓，但化合物减弱了指示炎症和周围神经损伤的啮齿动物模型中的持续疼痛的行为反应，并且抑制了与伤害性处理相关的脊髓区域中的有害刺激诱发的神经元激活。 CBi受体阻断防止这些影响。因此，本发明还提供了用于治疗其中外周FAAH的抑制将是有益的病症的方法和药物组合物。本发明的化合物根据式（I）：其中R1是极性基团。在一些实施方案中，R 1选自羟基及其生理上可水解的酯。 R2和R3独立地选自氢和取代或未取代的烃基; 每个R 4独立地选自卤素和取代或未取代的烃基，n是0至4的整数; 每个R 5独立地选自卤素和取代或未取代的烃基，m是0-3的整数; 并且R 6是取代或未取代的环己基; 及其药学上可接受的盐。

16. 发明申请

US20130217764A1 PERIPHERALLY RESTRICTED FAAH INHIBITORS 有权
标题翻译：外用限制性FAAH抑制剂
公开(公告)号：US20130217764A1
公开(公告)日：2013-08-22
申请号：US13812777
申请日：2011-07-22
申请人： Daniele Piomelli , Jason R. Clapper , Guillermo Moreno-Sanz , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia , Todd A. Ostomel
发明人： Daniele Piomelli , Jason R. Clapper , Guillermo Moreno-Sanz , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia , Todd A. Ostomel
IPC分类号： C07C271/56
CPC分类号： C07C271/56 , C07C2601/14
摘要： Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof. R2 and R3 are independently selected from the group consisting of hydrogen and substituted or unsubstituted hydrocarbyl; each R4 is independently selected from the group consisting of halogen and substituted or unsubstituted hydrocarbyl and n is an integer from 0 to 4; each R5 is independently selected from the group consisting of halo and substituted or unsubstituted hydrocarbyl and m is an integer from 0 to 3; and R6 is substituted or unsubstituted cyclohexyl; and the pharmaceutically acceptable salts thereof.
摘要翻译：提供脂肪酸酰胺水解酶（FAAH）的外周限制性抑制剂。该化合物可以抑制FAAH活性，并增加中枢神经系统（CNS）外的氨基酰胺水平。尽管它们相对不能进入脑和脊髓，但化合物减弱了指示炎症和周围神经损伤的啮齿动物模型中的持续疼痛的行为反应，并且抑制了与伤害性处理相关的脊髓区域中的有害刺激诱发的神经元激活。 CBi受体阻断防止这些影响。因此，本发明还提供了用于治疗其中外周FAAH的抑制将是有益的病症的方法和药物组合物。本发明的化合物根据式（I）：其中R1是极性基团。在一些实施方案中，R 1选自羟基及其生理上可水解的酯。 R2和R3独立地选自氢和取代或未取代的烃基; 每个R 4独立地选自卤素和取代或未取代的烃基，n是0至4的整数; 每个R 5独立地选自卤素和取代或未取代的烃基，m是0-3的整数; 并且R 6是取代或未取代的环己基; 及其药学上可接受的盐。

17. 发明授权

US07098233B2 5-halo-tryptamine derivatives used as ligands on the 5-HT6 and/or 5-HT7 serotonin receptors 失效
标题翻译：用作5-HT6和/或5-HT7血清素受体的配体的5-卤素 - 色胺衍生物
公开(公告)号：US07098233B2
公开(公告)日：2006-08-29
申请号：US10481433
申请日：2002-06-17
申请人： Maria Assunta Di Cesare , Patrizia Minetti , Giorgio Tarzia , Gilberto Spadoni
发明人： Maria Assunta Di Cesare , Patrizia Minetti , Giorgio Tarzia , Gilberto Spadoni
IPC分类号： A61K31/405 , C07D209/196
CPC分类号： C07D209/16 , A61K31/405
摘要： Compounds of Formula (I): (I); wherein: R1 and R2 either the same or different, are H or linear or branched C1–C6 alkyl; R3=linear or branched C1–C6 alkyl; R4=halogen, and pharmaceutically acceptable salts thereof are useful as active ingredients in the preparation of medicaments used as ligands of the 5-HT6 and/or 5-HT7 serotoninergic receptors.
摘要翻译：式（I）的化合物：（I）; 其中：R 1和R 2相同或不同，为H或直链或支链C 1 -C 6 - 烷基; R 3 =直链或支链C 1 -C 6烷基; R 4 =卤素及其药学上可接受的盐可用作制备用作5-HT 6和/或5-HT 6配体的药物的活性成分， 5-羟色胺能受体。

18. 发明授权

US5587374A 10(1-hydroxyethyl)-11-oxo-1-azatricyclo/7.2.0.0..sup.3.8/ undec-2-ene-2-carboxylic acid esters and a process for preparing thereof 失效
标题翻译： 10（1-羟乙基）-11-氧代-1-氮杂三环/ 7.2.0.0.3.8 /十一碳-2-烯-2-羧酸酯及其制备方法
公开(公告)号：US5587374A
公开(公告)日：1996-12-24
申请号：US388515
申请日：1995-02-14
申请人： Alcide Perboni , Tino Rossi , Giovanni Gaviraghi , Giorgio Tarzia , Antonella Ursini
发明人： Alcide Perboni , Tino Rossi , Giovanni Gaviraghi , Giorgio Tarzia , Antonella Ursini
IPC分类号： A61K31/40 , A61K31/397 , A61K31/407 , A61P31/04 , C07D477/00 , C07D487/04 , C07D487/00 , A61K31/395
CPC分类号： C07D477/00
摘要： A compound of the formula 1-cyclohexyloxycarbonyloxethyl (4S, 8S, 9R 10S, 12R)-4-methoxy-10-(1-hydroxyethyl)-11-oxo-1-azatricyclo[7.2.0.0..sup.3,8 ]undec-2-ene-2-carboxylate which is useful as a pharmaceutical composition to treat bacterial infection.
摘要翻译：式1-环己基氧基羰基氧基乙基（4S，8S，9R 10S，12R）-4-甲氧基-10-（1-羟乙基）-11-氧代-1-氮杂环[7.2.0.0.3,8]十一烷-2 烯-2-羧酸盐，其可用作治疗细菌感染的药物组合物。

19. 发明授权

US4783461A 3,6-disubstituted triazolo [3,4-A]phthalazine derivatives 失效
标题翻译： 3,6-二取代三唑并[3,4-A]酞嗪衍生物
公开(公告)号：US4783461A
公开(公告)日：1988-11-08
申请号：US629658
申请日：1984-07-11
申请人： Emilio Occelli , Giorgio Tarzia
发明人： Emilio Occelli , Giorgio Tarzia
IPC分类号： A61K31/50 , A61K31/535 , A61P25/20 , C07D237/32 , C07D237/34 , C07D487/04 , A61K31/55
CPC分类号： C07D487/04 , C07D237/32 , C07D237/34
摘要： The present invention is directed to new 3,6-disubstituted-1,2,4-triazolo[3,4-a]phthalazine derivatives of formula I ##STR1## wherein R represents phenyl or substituted phenyl, n is 1 or 2, R.sup.1 is an amino group of formula NR.sup.4 R.sup.5, or an alkoxy of cycloalkoxy group of formula OR.sup.6, and R.sup.2 and R.sup.3 represent hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, to the process for their preparation and to the pharmaceutical compositions containing them. The compounds of the present invention are as active as anti-anxiety substances.
摘要翻译：本发明涉及式I的新的3,6-二取代-1,2,4-三唑并[3,4-a]酞嗪衍生物其中R表示苯基或取代的苯基，n为1或2，R 1 是式NR4R5的氨基或式OR6的环烷氧基的烷氧基，R2和R3表示氢，卤素，（C1-C4）烷基或（C1-C4）烷氧基，其制备方法和含有它们的药物组合物。本发明的化合物与抗焦虑物质一样有活性。

20. 发明授权

US4140696A Aminopyrrole derivatives 失效
标题翻译：氨基吡咯衍生物
公开(公告)号：US4140696A
公开(公告)日：1979-02-20
申请号：US750759
申请日：1976-12-15
申请人： Giorgio Tarzia , Gianbattista Panzone
发明人： Giorgio Tarzia , Gianbattista Panzone
IPC分类号： C07D207/34 , C07D207/36 , C07D209/40 , C07D207/14 , C07D207/44
CPC分类号： C07D207/36 , C07D207/34 , C07D209/40 , Y10S514/916
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, 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：具有下式的药理学活性氨基吡咯衍生物其中：

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