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1. 发明申请

WO2007084319A3 DIARYL PIPERIDINES AS CB1 MODULATORS 审中-公开
标题翻译： DIARYL PIPERIDINES作为CB1调节器
公开(公告)号：WO2007084319A3
公开(公告)日：2007-09-20
申请号：PCT/US2007000705
申请日：2007-01-11
申请人： SCHERING CORP , SCOTT JACK D , WEINSTEIN JAY , MILLER MICHAEL W , STAMFORD ANDREW W , GILBERT ERIC J , XIA YAN , GREENLEE WILLIAM J , LI WEI
发明人： SCOTT JACK D , WEINSTEIN JAY , MILLER MICHAEL W , STAMFORD ANDREW W , GILBERT ERIC J , XIA YAN , GREENLEE WILLIAM J , LI WEI
IPC分类号： C07D211/18 , C07D211/26 , C07D211/28 , C07D211/32 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06
CPC分类号： C07D211/18 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/30 , C07D211/32 , C07D211/58 , C07D211/60 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D471/10
摘要： A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome (e.g., obesity, waist circumference, lipid profile, and insulin sensitivity), neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：具有式（I）的通式结构的化合物或其药学上可接受的盐，溶剂化物或酯可用于治疗疾病，病症或病症如代谢综合征（例如，肥胖，腰围，脂质分布和胰岛素敏感性），神经炎症性疾病，认知障碍，精神病，成瘾行为，胃肠道疾病和心血管疾病。

2. 发明授权

US3915955A Amino glycoside antibiotics having antiprotozoal and anthelmintic activity 失效
标题翻译：具有抗原虫和驱虫活性的氨基糖苷抗生素
公开(公告)号：US3915955A
公开(公告)日：1975-10-28
申请号：US38977473
申请日：1973-08-20
申请人： SCHERING CORP
发明人： COOPER DAVID J , WAITZ JAY ALLAN , COUNELIS MAE , WEINSTEIN JAY
IPC分类号： C07H15/22 , C07C47/18
CPC分类号： C07H15/22 , Y10S514/96 , Y10S514/962 , Y10S514/969
摘要： In the fermentation production of gentamicin C a plurality of additional antibiotic compounds are obtained. Four of these compounds, gentamicin A, gentamicin B, gentamicin B1 and gentamicin X exhibit significant anti-protozoal and anthelmintic activity while gentamicin B and B1 have significant antibacterial properties with markedly reduced side effects.
摘要翻译：在庆大霉素C的发酵生产中，获得了多种另外的抗生素化合物。这些化合物中的四种，庆大霉素A，庆大霉素B，庆大霉素B1和庆大霉素X表现出显着的抗原生动物和驱虫活性，而庆大霉素B和B1具有显着的抗菌性质并显着降低副作用。

3. 发明授权

US3868360A Process for preparing 2-deroxy-3-desamino-2,3-epimino-aminoglycosides and intermediates useful therein 失效
标题翻译：制备2-脱氧-3-脱甲酰氨基-2,3-苯二胺 - 氨基糖苷的方法及其有用的中间体
公开(公告)号：US3868360A
公开(公告)日：1975-02-25
申请号：US29998372
申请日：1972-10-24
申请人： SCHERING CORP
发明人： DANIELS PETER J L , WEINSTEIN JAY
IPC分类号： C07H15/226 , C07C47/18
CPC分类号： C07H15/226
摘要： 2''''-Deoxy-3''''-desamino-2'''',3''''-epimino-aminoglycosides useful as intermediates in preparing antibacterially active 2''''deoxyaminoglycosides, are prepared from antibacterially active aminoglycosides having a 2''''-hydroxyl group and a 3''''-primary or secondary amino function, by a process which comprises protecting primary amino groups and secondary amino groups capable of oxazolidine formation with an aldehyde and a neighboring hydroxyl group, by conversion thereof to Schiff base-oxazolidine condensation products with aldehydes (preferably benzaldehyde), converting any protectable primary and secondary hydroxyl groups to a trityl ether or to a cyclic ketal or acetal, treating said N-protected-O-protected-aminoglycoside with a hydrocarbonsulfonyl halide in a tertiary amine, treating the resulting N-protected-Oprotected-2''''-O-hydrocarbonsulfonylaminoglycoside (novel intermediates) with dilute aqueous acid to a pH in the range of from about 1 to about 5, and converting the resulting 2''''-Ohydrocarbonsulfonylaminoglycoside to a 2''''-deoxy-3''''-desamino2'''',3''''-epimino-aminoglycoside either by spontaneous transformation or heating in a lower alkanol alone or together with an alkali metal salt of said alkanol. The 2''''-deoxy-3''''desamino-2'''',3''''-epiminoaminoglycosides upon hydrogenation followed by acid hydrolysis of any ketal or acetal functions are converted to a product mixture comprising an antibacterially active 2''''-deoxyaminoglycoside isolatable via chromatographic techniques.
摘要翻译：用作制备抗菌活性2'-脱氧氨基糖苷类的中间体的“脱氧-3” - 脱氨基-2“，3” - 亚氨基 - 氨基糖苷类，由具有2“ - 羟基的抗菌活性氨基糖苷和3“ - 伯或仲氨基功能，通过一种方法，该方法包括用醛和相邻的羟基保护伯氨基和能够形成恶唑烷的仲氨基，通过将其转化成与醛的席夫碱 - 恶唑烷缩合产物（优选苯甲醛），将任何可保护的伯和仲羟基转化成三苯甲醚或环状缩酮或缩醛，在叔胺中用烃磺酰卤处理所述N-保护的O-保护的氨基糖苷，受保护的O保护的2'-O-烃磺酰氨基糖苷（新型中间体）与pH为约1至约5的酸性水溶液，并转化所得的2“ 通过在低级烷醇中单独或与所述链烷醇的碱金属盐一起自发转化或加热，将二烃基磺酰氨基糖苷转化为2“ - 脱氧-3” - 脱氨基-2“，3” - 异氨基 - 氨基糖苷。 2'-脱氧-3'-脱氨基-2“，3” - 异亚氨基氨基糖苷在氢化之后，任何缩酮或缩醛功能的酸水解转化为包含抗菌活性2'-脱氧氨基糖苷可分离的产物混合物通过色谱技术。

4. 发明专利

JP2011251994A Substituted piperazine as cb1 antagonist 审中-公开
标题翻译：取代的哌嗪作为CB1拮抗剂
公开(公告)号：JP2011251994A
公开(公告)日：2011-12-15
申请号：JP2011170530
申请日：2011-08-03
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： GILBERT ERIC J , MILLER MICHAEL W , SCOTT JACK D , STAMFORD ANDREW W , GREENLEE WILLIAM J , WEINSTEIN JAY
IPC分类号： C07D241/04 , A61K31/397 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K45/00 , A61P1/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P25/00 , A61P25/28 , A61P25/30 , A61P43/00 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06
CPC分类号： C07D241/04 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/08 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/10
摘要： PROBLEM TO BE SOLVED: To provide a novel class of substituted piperazine compounds as CBreceptor antagonists for treating various conditions.SOLUTION: Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CBreceptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions. The selective CBreceptors are piperazine derivatives having the structure of formula (I), or a pharmaceutically acceptable salt, solvate or ester thereof.
摘要翻译：待解决的问题：提供一类新颖的取代的哌嗪化合物作为治疗各种病症的CB 1“/ 1> 1受体拮抗剂。解决方案：式（I）化合物或其药学上可接受的盐，溶剂化物或酯可用于治疗由CB 1 受体介导的疾病或病症，例如代谢综合征和肥胖症，神经炎症性疾病，认知障碍和精神病，成瘾（例如戒烟），胃肠道疾病和心血管疾病。选择性CB 1 受体是具有式（I）结构的哌嗪衍生物或其药学上可接受的盐，溶剂合物或酯。版权所有（C）2012，JPO＆INPIT

5. 发明专利

ZA200104233B Tricyclic farnesyl protein transferase inhibitors. 未知
公开(公告)号：ZA200104233B
公开(公告)日：2002-08-22
申请号：ZA200104233
申请日：2001-05-23
申请人： SCHERING CORP
发明人： TAVERAS ARTHUR G , COOPER ALAN B , GUZI TIMOTHY , RANE DINANATH F , AFONSO ANDRIANO , CHAO JIANPING , KELLY JOSEPH M , DESAI JAGDISH A , WEINSTEIN JAY , DOLL RONALD J , FERREIRA JOHAN A , MALLAMS ALAN K , GIRJIAVALLABHAN VIYYOOR M , AKI CYNTHIA J , ALVAREZ CARMEN , LALWANI TARIK , WANG JAMES J S
IPC分类号： A61K31/496 , A61P35/00 , A61P35/02 , A61P43/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D521/00 , C07D , A61K , A61P
摘要： Disclosed are compounds of formula (1.0) wherein R represents an imidazole ring; R represents a carbamate, urea, amide or sulfonamide group; R represents H when the alkyl chain between the amide group and the R imidazole group is substituted, or R represents a substituent such aa arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R is H, and the alkyl chain between the amide group and the R imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

6. 发明专利

BR9916314A 未知
公开(公告)号：BR9916314A
公开(公告)日：2001-10-02
申请号：BR9916314
申请日：1999-12-16
申请人： SCHERING CORP
发明人： TAVERAS ARTHUR G , DOLL RONALD J , COOPER ALAN B , FERREIRA JOHAN A , GUZI TIMOTHY , MALLAMS ALAN K , RANE DINANATH F , GIRIJAVALLABHAN VIYYOOR M , AFONSO ADRIANO , AKI CYNTHIA J , CHAO JIANPING , ALVAREZ CARMEN , KELLY JOSEPH M , LALWANI TARIK , DESAI JAGDISH A , WANG JAMES J-S , WEINSTEIN JAY
IPC分类号： A61K31/496 , A61P35/00 , A61P35/02 , A61P43/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D521/00 , C07D413/14 , C07D407/14 , A61K31/445 , A61K31/44 , A61K31/55
摘要： Disclosed are compounds of formula (1.0) wherein R represents an imidazole ring; R represents a carbamate, urea, amide or sulfonamide group; R represents H when the alkyl chain between the amide group and the R imidazole group is substituted, or R represents a substituent such aa arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R is H, and the alkyl chain between the amide group and the R imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

7. 发明专利

NO20012961A 未知
公开(公告)号：NO20012961A
公开(公告)日：2001-08-16
申请号：NO20012961
申请日：2001-06-15
申请人： SCHERING CORP
发明人： TAVERAS ARTHUR G , DOLL RONALD J , COOPER ALAN BRUCE , FERREIRA JOHAN A , GUZI TIMOTHY , MALLAMS ALAN K , RANE DINANATH F , GIRIJAVALLABHAN VIYYOOR MOOPIL , AFONSO ADRIANO , AKI CYNTHIA J , CHAO JIANPING , ALVAREZ CARMEN , KELLY JOSEPH M , LALWANI TARIK , DESAI JAGDISH A , WANG JAMES J S , WEINSTEIN JAY
IPC分类号： A61K31/496 , A61P35/00 , A61P35/02 , A61P43/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D521/00 , C07D
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14

8. 发明专利

CA2354779A1 TRICYCLIC FARNESYL PROTEIN TRANSFERASE INHIBITORS 未知
公开(公告)号：CA2354779A1
公开(公告)日：2000-06-29
申请号：CA2354779
申请日：1999-12-16
申请人： SCHERING CORP
发明人： DOLL RONALD J , AFONSO ADRIANO , GIRIJAVALLABHAN VIYYOOR M , CHAO JIANPING , AKI CYNTHIA J , TAVERAS ARTHUR G , COOPER ALAN B , ALVAREZ CARMEN , RANE DINANATH F , FERREIRA JOHAN A , WEINSTEIN JAY , MALLAMS ALAN K , LALWANI TARIK , KELLY JOSEPH M , WANG JAMES J S , GUZI TIMOTHY , DESAI JAGDISH A
IPC分类号： A61K31/496 , A61P35/00 , A61P35/02 , A61P43/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D521/00 , C07D407/14 , C07D413/14 , A61K31/44 , A61K31/445 , A61K31/55
摘要： Disclosed are compounds of formula (1.0) wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group; R8 represents H when the alkyl chain between the amide group and the R13 imidazole group is substituted, or R8 represents a substituent such aa arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R8 is H, and the alk yl chain between the amide group and the R13 imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

9. 发明专利

AU8253798A Novel phenyl-substituted tricyclic inhibitors of farnesyl-protein transferase 未知
公开(公告)号：AU8253798A
公开(公告)日：1999-01-04
申请号：AU8253798
申请日：1998-06-15
申请人： SCHERING CORP
发明人： AFONSO ADRIANO , KELLY JOSEPH M , WEINSTEIN JAY , WOLIN RONALD L , ROSENBLUM STUART B
IPC分类号： A61K31/4545 , A61K31/496 , A61P35/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D401/04 , C07D221/16 , A61K31/55 , A61K31/435
摘要： Novel phenyl-substituted tricyclic compounds of formula (1.0) and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel halo-N-substituted urea compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.

10. 发明专利

CA2293549A1 NOVEL PHENYL-SUBSTITUTED TRICYCLIC INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE 未知
公开(公告)号：CA2293549A1
公开(公告)日：1998-12-23
申请号：CA2293549
申请日：1998-06-15
申请人： SCHERING CORP
发明人： WOLIN RONALD L , WEINSTEIN JAY , AFONSO ADRIANO , ROSENBLUM STUART B , KELLY JOSEPH M
IPC分类号： A61K31/4545 , A61K31/496 , A61P35/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D401/04 , C07D221/16 , A61K31/435 , A61K31/55
摘要： Novel phenyl-substituted tricyclic compounds of formula (1.0) and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel halo-N-substituted urea compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.

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