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1. 发明申请

US20090275555A1 Substituted indole ligands for the ORL-1 receptor 审中-公开
标题翻译：用于ORL-1受体的取代的吲哚配体
公开(公告)号：US20090275555A1
公开(公告)日：2009-11-05
申请号：US11794654
申请日：2005-12-28
申请人： Silvano Ronzoni , Stefania Gagliardi
发明人： Silvano Ronzoni , Stefania Gagliardi
IPC分类号： A61K31/454 , C07D401/06 , A61K31/55 , C07D401/14 , A61K31/497
CPC分类号： C07D405/14 , C07D401/06 , C07D401/14
摘要： New ligands for the ORL-1 receptor are described, useful for antagonising the activity of said receptors in a patient in need thereof, and for preventing and treating illnesses dependent on the activation of this receptor. The new compounds conform to structural formula (I) wherein R1, R2, R3, R4 are further defined in the description.
摘要翻译：描述了ORL-1受体的新配体，其可用于拮抗有需要的患者中所述受体的活性，以及用于预防和治疗依赖于该受体活化的疾病。新化合物符合结构式（I），其中R1，R2，R3，R4在描述中进一步定义。

2. 发明申请

US20070197603A1 Substituted indole ligands for the orl-1 receptor 审中-公开
标题翻译：用于orl-1受体的取代的吲哚配体
公开(公告)号：US20070197603A1
公开(公告)日：2007-08-23
申请号：US10561282
申请日：2004-07-01
申请人： Alessandra Consonni , Simone Del Sordo , Carlo Farina , Stefania Gagliardi , Silvano Ronzoni , Stefania Vallese
发明人： Alessandra Consonni , Simone Del Sordo , Carlo Farina , Stefania Gagliardi , Silvano Ronzoni , Stefania Vallese
IPC分类号： A61K31/44 , C07D401/06
CPC分类号： C07D409/14 , C07D401/06 , C07D401/14 , C07D405/14
摘要： New ligands for the ORL-1 receptor are described, useful for modulating the activity of said receptors in a patient in need thereof, and for preventing and treating illnesses dependent on the stimulation of this receptor. The new compounds conform to structural formula (I), wherein Q is a moiety of formula: and R, R0, R1, R2, R3, R4, R5, R6 are further defined in the description.
摘要翻译：描述了ORL-1受体的新配体，可用于调节有需要的患者中所述受体的活性，以及用于预防和治疗依赖于该受体刺激的疾病。新化合物符合结构式（I），其中Q是下式的部分：R 1，R 0，R 1，R 2， >，R 3，R 4，R 5，R 6，6在说明书中进一步定义。

3. 发明授权

US06365594B1 Heterocycle-condensed morphinoid derivatives (II) 失效
标题翻译：杂环稠合吗啉衍生物（II）
公开(公告)号：US06365594B1
公开(公告)日：2002-04-02
申请号：US09101213
申请日：1999-02-22
申请人： Giulio Dondio , Silvano Ronzoni , Pier Andrea Gatti , Davide Graziani
发明人： Giulio Dondio , Silvano Ronzoni , Pier Andrea Gatti , Davide Graziani
IPC分类号： A61K31445
CPC分类号： C07D471/10 , C07F7/0838 , C07F7/0896 , C08G77/12 , C08G77/14 , C08G77/16 , C08G77/18 , C08G77/20 , C08G77/24 , C08G77/26 , C08G77/28 , C08G77/50 , C08G77/70 , C08K5/5419 , C08L83/04 , H05K3/285 , C08L83/00 , C08L2666/44
摘要： Heterocycle-condensed morphinoid derivatives of formula (I), or solvates or salts thereof, are potent and selective delta opioid agonists and antagonists and are useful as i.a. analgesics. Pharmaceutical compositions containing such compounds, the use of such compounds as therapeutic agents, a method of treatment comprising the administration of such compounds, and a process for the preparation of such compounds are also described.
摘要翻译：式（I）的杂环稠合吗啉衍生物或其溶剂合物或其盐是有效和选择性的阿片样物质激动剂和拮抗剂，并且可用于如下。止痛药还描述了含有这些化合物的药物组合物，这些化合物作为治疗剂的用途，包括施用这些化合物的治疗方法和制备这些化合物的方法。

4. 发明授权

US5441956A Hydroisoquinoline derivatives 失效
标题翻译：氢异喹啉衍生物
公开(公告)号：US5441956A
公开(公告)日：1995-08-15
申请号：US175371
申请日：1994-01-05
申请人： Vittorio Vecchietti , Giulio Dondio , Silvano Ronzoni , Roberto Colle
发明人： Vittorio Vecchietti , Giulio Dondio , Silvano Ronzoni , Roberto Colle
IPC分类号： A61K31/47 , A61K31/475 , A61P25/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , A61K31/495
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： ##STR1## Compounds of formula (I) in which, R is linear or branched alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, aryl, aralkyl or furan-2-yl alkyl; R
1 and R
2 , which may be the same or different, are each hydrogen, hydroxy, alkoxy, or halogen; R
3 is hydrogen, hydroxy or alkoxy; "Het" is optionally substituted single or fused heteroxyclic ring, containing from 5 to 10 ring atoms and comprising up to four heteratoms in the or each ring, selected from oxygen, nitrogen and sulphur; R
4 and R
5 , which may be the same or different, are each hydrogen alkyl, halogen, nitro; CF, cyano, alkoxy carbonyl, NH, alkylcarbonylamino, hydroxy, alkoxy, or benzyl, are selective delta receptor agonists and are useful in the treatment of pain.
摘要翻译： PCT No.PCT / EP92 / 01483第 371日期1994年1月5日 102（e）日期1994年1月5日PCT提交1992年7月1日PCT公布。公开号WO93 / 01186 （I）其中R为直链或支链烷基，环烷基，环烷基烷基，烯基，芳基，芳烷基或呋喃-2-基烷基的式（I）化合物; R 1和R 2可以相同或不同，分别为氢，羟基，烷氧基或卤素; R3是氢，羟基或烷氧基; “Het”是任选取代的单或稠环氧环，其含有5至10个环原子，并且在该环或每个环中包含至多四个杂原子，选自氧，氮和硫; R 4和R 5可以相同或不同，分别为氢烷基，卤素，硝基; CF，氰基，烷氧基羰基，NH，烷基羰基氨基，羟基，烷氧基或苄基是选择性δ受体激动剂，可用于治疗疼痛。

5. 发明授权

US06262104B1 Diarylalkenylamine derivatives 失效
标题翻译：二芳基烯基胺衍生物
公开(公告)号：US06262104B1
公开(公告)日：2001-07-17
申请号：US09029892
申请日：1998-06-05
申请人： Giulio Dondio , Silvano Ronzoni
发明人： Giulio Dondio , Silvano Ronzoni
IPC分类号： A61K207401
CPC分类号： C07D295/192 , C07C237/30 , C07D295/155
摘要： Compounds, or solvates or salts thereof, of formula (I): selective delta opioid agonists and antagonists and may be of therapeutic utility as analgesics, immunosuppressants to prevent rejection in organ transplant and skin graft, anti-allergic and anti-inflammatory agents, brain cell protectants, agents for treating drug and alcohol abuse, gastritis, diarrhoea, cardiovascular and respiratory diseases, cough, mental illness, epilepsy and, in general, agents for the treatment of those pathological conditions which, customarily, can be treated with agonists and antagonists of the delta opioid receptor.
摘要翻译：式（I）的化合物或溶剂合物或其盐：选择性δ阿片样物质激动剂和拮抗剂，可用作止痛剂，用于防止器官移植和皮肤移植物中的排斥的免疫抑制剂，抗过敏和抗炎剂，脑细胞保护剂，用于治疗药物和酒精滥用的药物，胃炎，腹泻，心血管和呼吸系统疾病，咳嗽，精神疾病，癫痫以及通常用于治疗通常可用激动剂和拮抗剂治疗的病理状况的药剂的阿片样物质受体。

6. 发明授权

US07223867B2 Preparation of benzosuberonylpiperidine compounds 失效
公开(公告)号：US07223867B2
公开(公告)日：2007-05-29
申请号：US10494838
申请日：2002-11-05
申请人： Giovanni Palombi , Silvano Ronzoni
发明人： Giovanni Palombi , Silvano Ronzoni
IPC分类号： C07D211/06
CPC分类号： C07D211/22
摘要： Diastereoselective and enantioselective synthetic routes for the preparation of compounds of formula (I): or derivatives thereof, wherein: R is C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, hydroxy, halo, C1-6alkenyl, C1-6alkynyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, arylC1-6alkoxy, heteroarylC1-6alkoxy, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, arylC1-6alkylamino, heteroarylC1-6alkyamino; R1 is hydrogen or R; R2 is hydroxy, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R3 and R4 are each independently selected from the list consisting of perhaloC1-6alkyl, hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl,(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl, and COX wherein X may be hydroxy, C1-6 alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6alkyl)amino; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by halo.

7. 发明授权

US08334286B2 Substituted pyrrolo[1,2-A] pyrazines, compositions containing these, processes of making these, and uses thereof 有权
标题翻译：取代的吡咯并[1,2-A]吡嗪，含有它们的组合物，制备方法及其用途
公开(公告)号：US08334286B2
公开(公告)日：2012-12-18
申请号：US12918718
申请日：2009-02-17
申请人： Carla Ghelardini , Marisa Martinelli , Carlo Parini , Silvano Ronzoni
发明人： Carla Ghelardini , Marisa Martinelli , Carlo Parini , Silvano Ronzoni
IPC分类号： A61K31/495
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention refers to compounds of general formula (I) wherein the R groups are, independently, H, C1-6alkyl, aryl, CF3; Y is CH2, C═O; X is bond, C═O, SO2, or C═N—CN; m is 0, 1; n is 0, 1; A is a heterocycle, or a phenyl group optionally substituted as defined in the specification. The compounds are active on chronic pain conditions of different origin; they can be administered alone or with other drugs. Most of these compounds are new. The invention include a process to prepare said compounds, and pharmaceutical compositions suitable for their administration to a patient.
摘要翻译：本发明涉及通式（I）的化合物，其中R基团独立地为H，C 1-6烷基，芳基，CF 3; Y是CH 2，C = O; X是键，C = O，SO 2或C = N-CN; m为0,1; n为0，1; A是杂环，或者如说明书中所定义的任选取代的苯基。该化合物对不同来源的慢性疼痛病症有活性; 它们可以单独使用或与其他药物一起施用。这些化合物大部分是新的。本发明包括制备所述化合物的方法和适于给予患者的药物组合物。

8. 发明授权

US06969724B2 Compounds 失效
公开(公告)号：US06969724B2
公开(公告)日：2005-11-29
申请号：US10324571
申请日：2002-12-19
申请人： Daniela Barlocco , Giorgio Cignarella , Giuseppe Arnaldo Maria Giardina , Mario Grugni , Silvano Ronzoni
发明人： Daniela Barlocco , Giorgio Cignarella , Giuseppe Arnaldo Maria Giardina , Mario Grugni , Silvano Ronzoni
IPC分类号： A61K31/451 , A61P1/16 , A61P5/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/02 , A61P15/10 , A61P25/00 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28 , A61P43/00 , C07D211/14 , C07D211/18 , C07D211/22 , A61K31/445
CPC分类号： C07D211/18 , C07D211/14 , C07D211/22
摘要： Compounds of formula I, or a salt thereof or a hydrate thereof, as follows: wherein X and Y are selected independently from hydrogen and aryl, which aryl is unsubstituted or substituted one or more times by hydroxy, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aryl, heterocyclyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, arylC1-6alkoxy, C1-6alkyl, C1-6alkoxy or halo, which alkyl or alkoxy groups are unsubstituted or substituted one or more times by halo; m and n are independently 0 to 3, provided that m and n are not both 0; A represents a single bond or is —(CRpa Rpb)p— wherein p is 1-3 and Rpa and Rpb are selected independently from hydrogen, C1-6alkyl, C1-6alkoxy and halo, which alkyl or alkoxy groups are independently substituted one or more times by halo; B represents a C4-8 saturated or unsaturated ring, which ring is unsubstituted or substituted one or more times by C1-6alkyl, C1-6alkoxy, aryl, aryloxy, hydroxy, oxo, halo, amino, C1-6alkylamino, di(C1-6 alkyl)amino, and C1-6alkylamido, which C1-6alkyl or C1-6alkoxy groups are unsubstituted or substituted one or more times by halo, which aryl group is unsubstituted or substituted one or more times by aryl, heterocyclyl, aryloxy, arylC1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, arylC1-6alkyl, hydroxy, C1-6alkenoxy, C1-6alkoxy, halo, or C1-6alkyl, which C1-6alkyl may be substituted one or more times by halo, and which aryl group is linked to said ring by a single bond or is benzo-condensed therewith are ligands of the ORL-1 receptor.

9. 发明申请

US20050059700A1 Preparation of benzosuberonylpiperidine compounds 失效
标题翻译：苯并环己基哌啶化合物的制备
公开(公告)号：US20050059700A1
公开(公告)日：2005-03-17
申请号：US10494838
申请日：2002-11-05
申请人： Giovanni Palombi , Silvano Ronzoni
发明人： Giovanni Palombi , Silvano Ronzoni
IPC分类号： C07D211/18 , A61K31/451 , A61P1/14 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/10 , A61P3/12 , A61P7/10 , A61P9/00 , A61P9/04 , A61P9/12 , A61P11/00 , A61P11/06 , A61P15/00 , A61P15/10 , A61P19/02 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P29/00 , A61P29/02 , A61P31/18 , A61P37/02 , A61P43/00 , C07D211/22 , C07D211/06 , A61K31/445 , C07D41/02
CPC分类号： C07D211/22
摘要： Diastereoselective and enantioselective synthetic routes for the preparation of compounds of formula (I): or derivatives thereof, wherein: R is C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, hydroxy, halo, C1-6alkenyl, C1-6alkynyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, arylC1-6alkoxy, heteroarylC1-6alkoxy, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, arylC1-6alkylamino, heteroarylC1-6alkylamino; R1 is hydrogen or R; R2 is hydroxy, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R3 and R4 are each independently selected from the list consisting of perhaloC1-6alkyl, hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl, and COX wherein X may be hydroxy, C1-6alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6alkyl)amino; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by halo.
摘要翻译：用于制备式（I）化合物或其衍生物的非对映选择性和对映选择性合成路线，其中：R为C 1-6烷基，C 3-7环烷基，C 1-6烷氧基，羟基，卤素，C 1-6烯基，C 1-6炔基，氨基， C 1-6烷基氨基，二（C 1-6烷基）氨基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，芳基C 1-6烷氧基，杂芳基C 1-6烷氧基，氨基C 1-6烷基，（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基） 1-6烷基，芳基C 1-6烷基氨基，杂芳基C 1-6烷基氨基; R 1是氢或R; R 2是羟基，C 1-6烷氧基，氨基，C 1-6烷基氨基，二（C 1-6烷基）氨基; R 3和R 4各自独立地选自全卤代C 1-6烷基，氢，卤素，C 1-6烷基，C 1-6烷氧基，羟基，氨基，C 1-6烷基氨基，二（C 1-6烷基）氨基，羟基C 1-6烷基，C 1-6烷氧基C 1-6烷基，氨基C 1-6烷基，（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基C 1-6烷基，芳基和COX，其中X可以是羟基，C 1-6烷氧基，C 1-6烷基，氨基，C 1-6烷基氨基或二（C 1-6烷基）氨基; 并且其中任何烷基或含有这种部分的任何基团的烷基部分可以被卤素取代一次或多次。

10. 发明授权

US06696457B1 Morphinoid compounds 失效
标题翻译：吗啉化合物
公开(公告)号：US06696457B1
公开(公告)日：2004-02-24
申请号：US09959020
申请日：2002-04-02
申请人： Stephen Edward Clarke , Giulio Dondio , Luca Francesco Raveglia , Silvano Ronzoni
发明人： Stephen Edward Clarke , Giulio Dondio , Luca Francesco Raveglia , Silvano Ronzoni
IPC分类号： A61K3144
CPC分类号： C07D471/08
摘要： Heterocycle condensed morphinoid derivatives of formula (I) have therapeutic utility as analgesics, in collagen disease, as anti-allergic and anti-inflammatory agents, brain cell protectants, in gastritis, diarrhoea, cardiovascular and respiratory diseases, cough, mental illness, epilepsy, for the preservation of organs during transplant operations, and for the treatment of those pathological conditions which customarily can be treated with agonists of the delta opioid receptor.
摘要翻译：式（I）的杂环缩合的吗啉衍生物作为止痛剂，在胶原病中作为抗过敏和抗炎剂，脑细胞保护剂，胃炎，腹泻，心血管和呼吸系统疾病，咳嗽，精神疾病，癫痫，用于在移植手术期间保存器官，以及用于治疗通常可以用Δ阿片受体激动剂治疗的病理状况。

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