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1. 发明授权

US5468758A Crystalline forms of endo-2,3-dihydro-N-(8-methyl)-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-1H-benz imidazole-1-carboxamides 失效
标题翻译：结晶形式的内-2,3-二氢-N-（8-甲基）-8-氮杂双环[3.2.1]辛-3-基）-2-氧代-1H-苯并咪唑-1-甲酰胺
公开(公告)号：US5468758A
公开(公告)日：1995-11-21
申请号：US264104
申请日：1994-06-22
申请人： Enzo Cereda , Antoine Ezhaya , Marco Turconi , Enrica Dubini , Grazia Maffione
发明人： Enzo Cereda , Antoine Ezhaya , Marco Turconi , Enrica Dubini , Grazia Maffione
IPC分类号： A61K31/46 , A61K31/415 , A61K31/4184 , A61K31/495 , A61P1/00 , A61P1/08 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , C07D235/32 , C07D401/00 , C07D403/12 , C07D451/04 , C07D451/12
CPC分类号： C07D451/04
摘要： Crystalline and pharmacologically active monohydrates of endo-2,3-dihydro-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-1H-benzimidazole-1-carboxamide hydrochloride and of endo-3-ethyl-2,3-dihydro-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-1H-benzimidazole-1-carboxamide hydrochloride.
摘要翻译：内-2,3-二氢-N-（8-甲基-8-氮杂双环[3.2.1]辛-3-基）-2-氧代-1H-苯并咪唑-1-甲酰胺盐酸盐的结晶和药理活性一水合物和内-3-乙基-2,3-二氢-N-（8-甲基-8-氮杂双环[3.2.1]辛-3-基）-2-氧代-1H-苯并咪唑-1-甲酰胺盐酸盐。

2. 发明授权

US4973592A 1,3-diazocycloalkenes as muscarinic receptor blocking agents 失效
标题翻译： 1,3-二氮杂环烯烃作为毒蕈碱受体阻断剂
公开(公告)号：US4973592A
公开(公告)日：1990-11-27
申请号：US243942
申请日：1988-09-13
申请人： Massimo Nicola , Arturo Donetti , Enzo Cereda , Marco Turconi , Giovanni B. Schiavi , Rosamaria Micheletti
发明人： Massimo Nicola , Arturo Donetti , Enzo Cereda , Marco Turconi , Giovanni B. Schiavi , Rosamaria Micheletti
IPC分类号： C07D233/14 , A61K31/415 , A61K31/4166 , A61K31/505 , A61P1/00 , A61P1/04 , A61P1/10 , A61P1/12 , A61P35/00 , A61P43/00 , C07D233/06 , C07D233/10 , C07D233/18 , C07D233/22 , C07D233/26 , C07D233/32 , C07D233/46 , C07D233/48 , C07D233/52 , C07D239/06 , C07D239/08 , C07D239/24 , C07D243/04
CPC分类号： C07D239/06 , C07D233/48 , C07D239/24
摘要： New pharmacologically active heterocyclic derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders, of the following formula ##STR1## wherein the substituents are defined hereinbelow.

3. 发明授权

US06521623B1 N,N'-disubstituted benzimidazolone derivatives with affinity at the serotonin and dopamine receptors 有权
公开(公告)号：US06521623B1
公开(公告)日：2003-02-18
申请号：US09933598
申请日：2001-08-21
申请人： Enzo Cereda , Luciano Maiocchi , Alessandro Brambilla , Ettore Giraldo , Eugenia Monferini , Giovanni Battista Schiavi
发明人： Enzo Cereda , Luciano Maiocchi , Alessandro Brambilla , Ettore Giraldo , Eugenia Monferini , Giovanni Battista Schiavi
IPC分类号： C07D23526
CPC分类号： C07D401/06 , C07D235/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D471/04 , C07D471/10
摘要： A compound of formula (I) wherein: R1 is C1-C6-alkyl substituted by a group selected from OH, C1-C6-alkoxy, —OCONHC1-C6-alkyl, —OCONHC1-C6-alkyl, —NHSO2C1-C6-alkyl, and —NHCOC1-C6-alkyl, or R1 is C1-C6-alkyl substituted by a saturated or unsaturated 5- or 6-membered heterocycle containing one or two heteroatoms selected from the group consisting of nitrogen and oxygen, the heterocycle optionally substituted by a group selected from C1-C4-alkyl, halogen, and benzyl; R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring thereof substituted by a group selected from phenyl, benzyl, and diphenylmethyl, each of these groups optionally mono- or di-substituted by one or two groups selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, and OH, or R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring thereof linked via a single bond, a methylene-bridge, or spiro-connected to a saturated or unsaturated heterocyclic group containing one or two heteroatoms selected from oxygen and nitrogen, the heterocyclic group optionally mono- or di-substituted by a group selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, ═O, and OH, or R2 and R3 together with the nitrogen form a saturated or unsaturated bi- or tricyclic heterocyclic ring-system optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring-system being optionally substituted by a group selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, ═O, and OH; and A is C1-C6-alkylene, C2-C6-alkenylene, or C2-C6-alkynylene, their pharmaceutically acceptable salts, their preparation, and their use for therapeutic purposes.

4. 发明授权

US4643993A Substituted heterocyclyl-phenyl-(sulfonyl-or phosphonyl)-amidines 失效
标题翻译：取代的杂环基 - 苯基 - （磺酰基或膦酰基） - 脒基
公开(公告)号：US4643993A
公开(公告)日：1987-02-17
申请号：US495717
申请日：1983-05-18
申请人： Enzo Cereda , Arturo Donetti , Antonio Giachetti , Piero del Soldato
发明人： Enzo Cereda , Arturo Donetti , Antonio Giachetti , Piero del Soldato
IPC分类号： A61K31/41 , A61P1/04 , C07D231/12 , C07D233/54 , C07D233/64 , C07D249/08 , C07F9/40 , C07F9/6503 , C07F9/6506 , C07F9/6518 , A61K31/675 , C07F9/65
CPC分类号： C07D231/12 , C07D233/64 , C07D249/08 , C07F9/4006 , C07F9/65037 , C07F9/65067 , C07F9/65187
摘要： Compounds of the formula ##STR1## wherein Het is a heterocycle containing 2 to 3 nitrogen atoms;R is hydrogen, lower alkyl, alkoxy of 1 to 3 carbon atoms or halogen;Y is --SO.sub.3 H or ##STR2## R" is alkyl of 1 to 3 carbon atoms; and R' is straight or branched alkyl which may contain a heteroatom such as sulfur, oxygen or nitrogen; straight or branched alkenyl; cycloalkyl; alkyl-cycloalkyl; aryl; or aralkyl optionally substituted by lower alkyl, alkoxy of 1 to 3 carbon atoms or halogen; tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics and gastric acid secretion inhibitors.
摘要翻译：其中Het是含有2至3个氮原子的杂环的式“IMAGE”的化合物; R为氢，低级烷基，1〜3个碳原子的烷氧基或卤素; Y是-SO 3 H或R 3是具有1至3个碳原子的烷基; 并且R'是可以含有杂原子如硫，氧或氮的直链或支链烷基; 直链或支链烯基; 环烷基烷基 - 环烷基芳基; 或任选被低级烷基，1至3个碳原子的烷氧基或卤素取代的芳烷基; 互变异构体及其无毒的药理学上可接受的酸加成盐。化合物及其盐可用作抗溃疡发生剂和胃酸分泌抑制剂。

5. 发明授权

US4301177A (3-Methyl-2-butenyl)propanedioic acid mono (1,2-diphenylhydrazide) and salts thereof 失效
标题翻译：（3-甲基-2-丁烯基）丙二酸单（1,2-二苯基酰肼）及其盐
公开(公告)号：US4301177A
公开(公告)日：1981-11-17
申请号：US135865
申请日：1980-03-31
申请人： Gianfranco Pala , Enzo Cereda
发明人： Gianfranco Pala , Enzo Cereda
IPC分类号： A61K31/19 , A01N37/10 , A61K20060101 , A61K31/15 , A61K31/16 , A61K31/185 , A61K31/195 , A61P29/00 , C06C20060101 , C07C20060101 , C07C67/00 , C07C241/00 , C07C243/30 , C07C109/10
CPC分类号： C07C243/00 , Y10S514/825 , Y10S514/916
摘要： The compound of the formula ##STR1## and non-toxic, pharmacologically acceptable salts thereof, which are useful as analgesics, antipyretics and anti-rheumatics.
摘要翻译：式“IMAGE”的化合物及其无毒的药学上可接受的盐，其可用作镇痛药，解热药和抗风湿药。

6. 发明授权

US08916589B2 Bradykinin B1-antagonists 有权
标题翻译：缓激肽B1拮抗剂
公开(公告)号：US08916589B2
公开(公告)日：2014-12-23
申请号：US12675224
申请日：2008-08-28
申请人： Norbert Hauel , Angelo Ceci , Enzo Cereda , Henri Doods , Ingo Konetzki , Juergen Mack , Henning Priepke , Annette Schuler-Metz , Rainer Walter
发明人： Norbert Hauel , Angelo Ceci , Enzo Cereda , Henri Doods , Ingo Konetzki , Juergen Mack , Henning Priepke , Annette Schuler-Metz , Rainer Walter
IPC分类号： A61K31/44 , A61K31/41 , C07D239/28 , C07C237/24 , C07C317/44 , C07D209/42 , C07D213/64 , C07D213/82 , C07D233/90 , C07D237/24 , C07D239/34 , C07D239/36 , C07D239/42 , C07D261/18 , C07D263/34 , C07D277/56 , C07D307/68 , C07K5/062 , C07K5/078
CPC分类号： C07D239/28 , C07C237/24 , C07C317/44 , C07C2601/02 , C07D209/42 , C07D213/64 , C07D213/82 , C07D233/90 , C07D237/24 , C07D239/34 , C07D239/36 , C07D239/42 , C07D261/18 , C07D263/34 , C07D277/56 , C07D307/68 , C07K5/06026 , C07K5/06139
摘要： The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
摘要翻译：本发明涉及通式I的化合物，其中n，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如下文所定义，对映异构体，非对映体，其混合物及其盐，其有机或无机酸或碱的生理上可接受的盐，其具有有价值的性质，其制备，含有药理学有效化合物的药物组合物，其制备及其用途。

7. 发明申请

US20100099680A1 PTERIDINONE DERIVATIVES AS P13-KINASES INHIBITORS 有权
标题翻译：哌啶酮衍生物作为P13-激酶抑制剂
公开(公告)号：US20100099680A1
公开(公告)日：2010-04-22
申请号：US12524791
申请日：2008-01-28
申请人： Riccardo Giovannini , Sara Frattini , Trixi Brandl , Steffen Breitfelder , Enzo Cereda , Matthias Grauert , Matthias Hoffmann , Anne T. Joergensen , Udo Maier , Alexander Pautsch , Monica Quai , Stefan Scheuerer
发明人： Riccardo Giovannini , Sara Frattini , Trixi Brandl , Steffen Breitfelder , Enzo Cereda , Matthias Grauert , Matthias Hoffmann , Anne T. Joergensen , Udo Maier , Alexander Pautsch , Monica Quai , Stefan Scheuerer
IPC分类号： A61K31/519 , C07D475/00 , A61P29/00 , A61P37/08 , A61P11/00
CPC分类号： C07D487/04
摘要： New compounds of Formula (1) are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.
摘要翻译：提供式（1）的新化合物，其由于其药物活性，因为PI3-激酶调节剂可用于治疗炎症或过敏性疾病的治疗领域。这些实例包括炎性和过敏性呼吸道疾病，胃肠道炎症性疾病和运动器官，炎性和过敏性皮肤疾病，炎症性眼病，鼻粘膜疾病，涉及自身免疫反应或炎症的炎性或过敏性疾病。

8. 发明授权

US07164018B2 Polymers based on N-carbamyl-N'-dimethylsilyl methyl-piperazine traceless linkers for the solid phase synthesis of phenyl based libraries 有权
标题翻译：基于N-氨基甲酰基-N'-二甲基甲硅烷基甲基哌嗪无定形连接剂的聚合物，用于固相合成苯基文库
公开(公告)号：US07164018B2
公开(公告)日：2007-01-16
申请号：US10766981
申请日：2004-01-29
申请人： Enzo Cereda , Carlo Maria Pellegrini , Monica Quai , Walter Barbaglia
发明人： Enzo Cereda , Carlo Maria Pellegrini , Monica Quai , Walter Barbaglia
IPC分类号： C07F7/10
CPC分类号： C40B99/00 , C07B2200/11 , C07F7/0812 , C08F8/42 , C08G65/329 , C08G65/3331 , C08G65/336 , C40B50/18 , C40B80/00
摘要： The present invention relates to polymers characterized by novel silicon linkers based on the carbamyl piperazine moiety, methods of preparing these polymers and their use in the solid phase synthesis of compounds or libraries of compounds embracing a phenyl ring in their structure.
摘要翻译：本发明涉及以基于氨基甲酰哌嗪部分的新型硅接头为特征的聚合物，制备这些聚合物的方法及其在固相合成化合物或其结构中包含苯环的化合物文库的用途。

9. 发明授权

US06586435B2 Benzimidazolone derivatives displaying affinity at the serotonin and dopamine receptors 有权
标题翻译：对5-羟色胺和多巴胺受体显示亲和力的苯并咪唑酮衍生物
公开(公告)号：US06586435B2
公开(公告)日：2003-07-01
申请号：US09933609
申请日：2001-08-21
申请人： Enzo Cereda , Luciano Maiocchi , Alessandro Brambilla , Ettore Giraldo , Giovanni Battista Schiavi
发明人： Enzo Cereda , Luciano Maiocchi , Alessandro Brambilla , Ettore Giraldo , Giovanni Battista Schiavi
IPC分类号： A61K31496
CPC分类号： C07D401/12 , C07D235/26 , C07D401/14 , C07D403/12 , C07D405/12 , C07D471/04 , C07D471/10
摘要： Compound of formula (I) wherein: R1 is hydrogen or C1-C6-alkyl optionally substituted by C3-C6-cycloylalkyl; R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, wherein the heterocyclic ring thereof is substituted by a group selected from phenyl, benzyl, and diphenylmethyl, each optionally mono- or di-substituted by one or two groups selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, and OH, or R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring thereof linked via a single bond, a methylene-bridge, or spiro-connected to another saturated or unsaturated heterocyclic group containing one or two heteroatoms selected from oxygen and nitrogen, the heterocyclic group being optionally mono- or di-substituted by a group selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, ═O, and OH, or R2 and R3 together with the nitrogen form a saturated or unsaturated bi- or tricyclic heterocyclic ring system optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring system is optionally substituted by a group selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, ═O, and OH; and A is C2-C6-alkenylene, their pharmaceutically acceptable salts, their preparation, and their use for therapeutic purposes.
摘要翻译：式（I）的化合物其中：R 1是氢或任选地被C 3 -C 6 - 环烷基取代的C 1 -C 6烷基; R 2和R 3与氮一起形成饱和或不饱和的5-或6-元杂环，任选地含有氮或氧作为另外的杂原子，其中其杂环被选自苯基，苄基和二苯基甲基的基团取代，各自任选被一个或两个选自CF 3，C 1 -C 4 - 烷基，C 1 -C 4烷基的基团单取代或二取代， C 4 - 烷氧基，苯基，苄基，卤素和OH，或R 2和R 3与氮一起形成饱和或不饱和的5-或6-元杂环，任选地含有氮或氧作为另外的杂原子，其杂环通过单键，亚甲基桥，或与另一个含有一个或两个选自氧和氮的杂原子的饱和或不饱和杂环基螺旋连接，杂环基团任选被一个或二个被gr取代的二取代基选自CF 3，C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，苯基，苄基，卤素，= O和OH，或R 2和R 3与氮一起形成饱和或不饱和的双环或三环杂环体系，氮或氧作为另外的杂原子，杂环体系任选被选自CF 3，C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，苯基，苄基，卤素，= O和OH中的基团取代; 且A为C 2 -C 6亚烯基，其药学上可接受的盐，其制备及其用于治疗目的的用途。

10. 发明授权

US06235738B1 Diphenyl-substituted heterocycles with 6-membered ring, processes for the preparation thereof and the use thereof as medicaments 有权
标题翻译：具有6元环的二苯基取代的杂环，其制备方法及其作为药物的用途
公开(公告)号：US06235738B1
公开(公告)日：2001-05-22
申请号：US09290335
申请日：1999-04-12
申请人： Michael Brenner , Rainer Palluk , Marion Wienrich , Thomas Weiser , Enzo Cereda , Maura Bignotti , Carlo Maria Pellegrini , Giovanni Battista Schiavi , Raffaele Cesana
发明人： Michael Brenner , Rainer Palluk , Marion Wienrich , Thomas Weiser , Enzo Cereda , Maura Bignotti , Carlo Maria Pellegrini , Giovanni Battista Schiavi , Raffaele Cesana
IPC分类号： A61K3153
CPC分类号： C07D239/26 , C07D239/36 , C07D251/16 , C07D253/065
摘要： The invention relates to novel diphenyl-substituted heterocycles with 6-membered ring of general formula (I) in which A, X and the residues R1, R2, R3, R4 and R5 are as defined in the claims, processes for the preparation thereof and the use thereof as medicaments.
摘要翻译：本发明涉及具有通式（I）的6-元环的新型二苯基取代的杂环，其中A，X和残基R1，R2，R3，R4和R5如权利要求中所定义，其制备方法和其作为药物的用途。

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