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1. 发明申请

WO1995011895A1 N-BENZOYL-4-OXY/THIO-2-SUBSTITUTED PIPERIDINES AS SUBSTANCE-P RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为物质受体拮抗剂的N-苯甲酰基-4-氧代/噻二唑替代的哌啶
公开(公告)号：WO1995011895A1
公开(公告)日：1995-05-04
申请号：PCT/EP1994003394
申请日：1994-10-14
申请人： CIBA-GEIGY AG , OFNER, Silvio , ROGGO, Silvio , SCHILLING, Walter , VEENSTRA, Siem, J.
发明人： CIBA-GEIGY AG
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D211/46 , C07D211/54
摘要： 1,2,4-Trisubstituted piperidine compounds of fomula (I), wherein R1 is an unsubstituted or substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical, or is the acyl radical of an alpha -amino acid that is unsubstituted or N-substituted by lower alkanoyl or by carbamoyl-lower alkanoyl; R2 is cycloalkyl or an unsubstituted or substituted aryl or heteroaryl radical; R3 is an unsubstituted or substituted, optionally hydrogenated aryl or heteroaryl radical or, when n is 1, X2 is imino that is unsubstituted or substituted by lower alkyl or by cycloalkyl and X3 is lower alkylene, R3 is lower alkyl or free or esterified or amidated carboxy, R4 is hydrogen or alkyl; X1 is methylene, ethylene, a direct bond, a free or ketalised carbonyl group or a free or etherified hydroxymethylene group; X2 is lower alkylene, imino that is unsubstituted or substituted by lower alkyl or by cycloalkyl, or a direct bond; X3 is lower alkylene or a direct bond; X4 is oxo or thioxo; and n is 1 or, when X2 is lower alkylene and X3 is a direct bond, n is 0; and the salts thereof, have compound-P-antagonistic properties and can be used as active ingredients of medicaments.
摘要翻译：式（I）的1,2,4-三取代哌啶化合物，其中R 1是未取代或取代的芳烷基，芳氧基烷基，杂芳烷基，芳酰基，杂芳酰基，环烷基羰基，芳烷酰基，杂芳基烷酰基，芳烷氧基羰基或芳基氨基甲酰基，或是未被取代或被低级烷酰基或氨基甲酰基 - 低级烷酰基取代的α-氨基酸; R2是环烷基或未取代或取代的芳基或杂芳基; R3是未取代或取代的，任选氢化的芳基或杂芳基，或当n为1时，X 2为未被取代或被低级烷基或环烷基取代的亚氨基，X3为低级亚烷基，R3为低级烷基或游离或酯化或酰胺化羧基，R 4是氢或烷基; X1是亚甲基，亚乙基，直接键，游离的或缩酮化的羰基或游离的或醚化的羟基亚甲基; X2是低级亚烷基，未被取代或被低级烷基或环烷基取代的亚氨基或直接键; X3是低级亚烷基或直接键; X4是氧代或硫代; n为1或X2为低级亚烷基且X3为直接键时，n为0; 及其盐具有化合物P-拮抗性质，可用作药物的有效成分。

2. 发明申请

WO1997045422A1 ANTI-NEURODEGENERATIVELY EFFECTIVE 10-AMINOALIPHATYL-DIBENZ[b,f]OXEPINE SALTS 审中-公开
标题翻译：抗神经营养因子有效的10-氨基尿嘧啶[b，f] OXEPINE SALTS
公开(公告)号：WO1997045422A1
公开(公告)日：1997-12-04
申请号：PCT/EP1997002794
申请日：1997-05-28
申请人： NOVARTIS AG , ZIMMERMANN, Kaspar , ROGGO, Silvio , BETSCHART, Claudia
发明人： NOVARTIS AG
IPC分类号： C07D313/14
CPC分类号： C07D405/06 , C07D313/14 , C07D405/12
摘要： Acid addition salts of 10-aminoaliphatyl-dibenz[b,f]oxepines of formula (I), wherein alk signifies a divalent, aliphatic radical, R represents an amino group, either unsubstituted or mono- or di-substituted by monovalent aliphatic and/or araliphatic radicals, or disubstituted by divalent aliphatic or araliphatic radicals, and R1, R2, R3 and R4, independently of one another, denote hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, with organic carboxylic acids, may be employed as anti-neurodegenerative active ingredients for medicaments. The invention also relates to new compounds of formula (I) in free form.
摘要翻译：式（I）的10-氨基联苯二基[b，f]氧杂七环素的酸加成盐，其中alk表示二价脂族基团，R表示氨基，未取代的或被一价脂族和/ 或芳脂族基团，或被二价脂族或芳脂族基团二取代，并且R 1，R 2，R 3和R 4彼此独立地表示氢，低级烷基，低级烷氧基，卤素或三氟甲基与有机羧酸反应用于药物的神经变性活性成分。本发明还涉及游离形式的新的式（I）化合物。

3. 发明申请

WO2006005620A1 USE OF MANZAMINES IN TRANSPLANTATION AND AUTOIMMUNE DISEASES 审中-公开
标题翻译：在移植和自发性疾病中使用曼扎米霉素
公开(公告)号：WO2006005620A1
公开(公告)日：2006-01-19
申请号：PCT/EP2005/007678
申请日：2005-07-14
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , THE UNIVERSITY OF MISSISSIPPI , HIESTAND, Peter, C. , PETERSEN, Frank , ROGGO, Silvio , HAMANN, Mark, T.
发明人： HIESTAND, Peter, C. , PETERSEN, Frank , ROGGO, Silvio , HAMANN, Mark, T.
IPC分类号： A61K31/437
CPC分类号： A61K31/4748 , A61K31/437
摘要： The use of a manzamine for preventing, treating or inhibiting (a) acute or chronic graft rejection in a recipient of cell, tissue or organ allotransplant, (b) vein graft stenosis, restenosis and/or vascular occlusion following vascular injury or (c) an autoimmune disease is described.
摘要翻译：（a）在细胞，组织或器官移植物的接受者中预防，治疗或抑制（a）急性或慢性移植物排斥，（b）静脉移植物狭窄，血管损伤后的再狭窄和/或血管闭塞的用途，或（c）描述了自身免疫性疾病。

4. 发明申请

WO2010066689A3 MODULATORS OF THE INTERACTION BETWEEN CHOLESTEROL MOLECULES AND THE EPSTEIN-BARR VIRUS INDUCED RECEPTOR 2 审中-公开
标题翻译：胆固醇分子与EPSTEIN-BARR病毒感染受体2之间的相互作用的调节剂
公开(公告)号：WO2010066689A3
公开(公告)日：2010-08-05
申请号：PCT/EP2009066550
申请日：2009-12-07
申请人： NOVARTIS AG , SCRIPPS RESEARCH INST , IRM LLC , BAUMGARTEN BIRGIT , GESSIER FRANCOIS , KATOPODIS ANDREAS , KNOCHENMUSS RICHARD , FALCHETTO ROCCO , ROGGO SILVIO , SAILER ANDREAS , SEUWEN KLAUS , SPANKA CARSTEN , ZHANG JUAN , HANNEDOUCHE SEBASTIEN , NOEL SOPHIE , ROY MARIE-ODILE , CHEN YU , CHO CHARLES Y , LI WEI , SHEN WEIJUN
发明人： BAUMGARTEN BIRGIT , GESSIER FRANCOIS , KATOPODIS ANDREAS , KNOCHENMUSS RICHARD , FALCHETTO ROCCO , ROGGO SILVIO , SAILER ANDREAS , SEUWEN KLAUS , SPANKA CARSTEN , ZHANG JUAN , HANNEDOUCHE SEBASTIEN , NOEL SOPHIE , ROY MARIE-ODILE , CHEN YU , CHO CHARLES Y , LI WEI , SHEN WEIJUN
IPC分类号： C07K14/705 , A61K31/7105 , A61K39/395 , C07K16/28 , C12N15/113 , C12N15/12 , G01N33/566
CPC分类号： C07K14/705 , C12N15/1138 , C12N2310/14 , G01N33/56994 , G01N33/92 , G01N2800/044 , G01N2800/2871 , G01N2800/321
摘要： The present invention relates to modulators of the interaction between Epstein-Barr Virus induced receptor-2 (EBI2) and cholest-5-ene-3b,7b,25-triol(7, 25- dihydroxycholesterol)(''7,25DHC'') and/orcholest-5-ene-3b, 7b-diol(7- hydroxycholesterol)(''7HC'') 25-diol (25-hydroxycholesterol)(''25HC''), especially the cholest-5-ene-3b,7a,25-triol(7a, 25-dihydroxycholesterol)(''7a,25DHC'')and/or cholest-5-ene-3b,7b,25-triol(7b, 25-dihydroxycholesterol)(''7b,25DHC'') stereoisomers. The modulator maybe a small chemical molecule, antibody or other therapeutic protein. Methods of medical treatment and methods of identifying modulators are also described.
摘要翻译：本发明涉及爱泼斯坦 - 巴尔病毒诱导的受体-2（EBI2）和胆甾烯-5-烯-3b，7b，25-三醇（7,25-二羟基胆固醇）（“7,25DHC”）之间相互作用的调节剂）和/或胆甾-5-烯-3b，7b-二醇（7-羟基胆固醇）（“7HC”）25-二醇（25-羟基胆固醇）（“25HC”），特别是胆甾-5-烯 - （7a，25-二羟基胆固醇）（“7a，25DHC”）和/或胆甾烯-5-烯-3b，7b，25-三醇（7b，25-二羟基胆固醇）（“7b” ，25DHC“）立体异构体。调节剂可能是一种小的化学分子，抗体或其他治疗性蛋白质。还描述了治疗方法和识别调节剂的方法。

5. 发明申请

WO1997046549A1 ANTI-NEURODEGENERATIVELY EFFECTIVE XANTHENE DERIVATIVES 审中-公开
标题翻译：抗神经元有效的XANTHENE衍生物
公开(公告)号：WO1997046549A1
公开(公告)日：1997-12-11
申请号：PCT/EP1997002885
申请日：1997-06-04
申请人： NOVARTIS AG , ROGGO, Silvio , ZIMMERMANN, Kaspar , BETSCHART, Claudia
发明人： NOVARTIS AG
IPC分类号： C07D311/84
CPC分类号： C07D405/06 , A61K31/352 , A61K31/4025 , A61K31/4433 , A61K31/453 , A61K31/496 , A61K31/5377 , C07D311/84 , C07D311/90
摘要： Xanthene derivatives of formula (I) wherein A signifies methylene, carbonyl or thiocarbonyl, R represents an amino group, either unsubstituted or mono- or di-substituted by monovalent aliphatic and/or araliphatic radicals, or disubstituted by divalent aliphatic radicals, and R1, R2, R3 and R4, independently of one another, denote hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, and their pharmaceutically employable salts, may be used as anti-neurodegenerative active ingredients for medicaments. The invention also relates to new compounds of formula (I).
摘要翻译：式（I）的呫吨衍生物其中A表示亚甲基，羰基或硫代羰基，R表示氨基，未取代的或被一价脂族和/或芳脂族基团单取代或二取代，或被二价脂族基团二取代， R2，R3和R4彼此独立地表示氢，低级烷基，低级烷氧基，卤素或三氟甲基及其药学上可用的盐，可用作药物的抗神经变性活性成分。本发明还涉及新的式（I）化合物。

6. 发明申请

WO2010066689A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2010066689A2
公开(公告)日：2010-06-17
申请号：PCT/EP2009/066550
申请日：2009-12-07
申请人： NOVARTIS AG , THE SCRIPPS RESEARCH INSTITUTE , IRM LLC , BAUMGARTEN, Birgit , GESSIER, François , KATOPODIS, Andreas , KNOCHENMUSS, Richard , FALCHETTO, Rocco , ROGGO, Silvio , SAILER, Andreas , SEUWEN, Klaus , SPANKA, Carsten , ZHANG, Juan , HANNEDOUCHE, Sébastien , NOËL, Sophie , ROY, Marie-Odile , CHEN, Yu , CHO, Charles Y. , LI, Wei , SHEN, Weijun
发明人： BAUMGARTEN, Birgit , GESSIER, François , KATOPODIS, Andreas , KNOCHENMUSS, Richard , FALCHETTO, Rocco , ROGGO, Silvio , SAILER, Andreas , SEUWEN, Klaus , SPANKA, Carsten , ZHANG, Juan , HANNEDOUCHE, Sébastien , NOËL, Sophie , ROY, Marie-Odile , CHEN, Yu , CHO, Charles Y. , LI, Wei , SHEN, Weijun
IPC分类号： C07K14/705 , C07K16/28 , C12N15/113 , A61K31/7105 , A61K39/395 , G01N33/566
CPC分类号： C07K14/705 , C12N15/1138 , C12N2310/14 , G01N33/56994 , G01N33/92 , G01N2800/044 , G01N2800/2871 , G01N2800/321
摘要： The present invention relates to modulators of the interaction between Epstein-Barr Virus induced receptor-2 (EBI2) and cholest-5-ene-3b,7b,25-triol(7, 25- dihydroxycholesterol)(''7,25DHC'') and/orcholest-5-ene-3b, 7b-diol(7- hydroxycholesterol)(''7HC'') 25-diol (25-hydroxycholesterol)(''25HC''), especially the cholest-5-ene-3b,7a,25-triol(7a, 25-dihydroxycholesterol)(''7a,25DHC'')and/or cholest-5-ene-3b,7b,25-triol(7b, 25-dihydroxycholesterol)(''7b,25DHC'') stereoisomers. The modulator maybe a small chemical molecule, antibody or other therapeutic protein. Methods of medical treatment and methods of identifying modulators are also described.
摘要翻译：本发明涉及爱泼斯坦 - 巴尔病毒诱导的受体-2（EBI2）和胆甾烯-5-烯-3b，7b，25-三醇（7,25-二羟基胆固醇）（“7,25DHC”）之间相互作用的调节剂）和/或胆甾-5-烯-3b，7b-二醇（7-羟基胆固醇）（“7HC”）25-二醇（25-羟基胆固醇）（“25HC”），特别是胆甾-5-烯 - （7a，25-二羟基胆固醇）（“7a，25DHC”）和/或胆甾烯-5-烯-3b，7b，25-三醇（7b，25-二羟基胆固醇）（“7b” ，25DHC“）立体异构体。调节剂可能是一种小的化学分子，抗体或其他治疗性蛋白质。还描述了治疗方法和识别调节剂的方法。

7. 发明申请

WO2002076968A1 MALONATES AS INHIBITORS OF THE ICE/CED-6 FAMILY OF CYSTEINE PROTEASES 审中-公开
标题翻译：作为ICE / CED-6家族蛋白家族的抑制剂的雄激素
公开(公告)号：WO2002076968A1
公开(公告)日：2002-10-03
申请号：PCT/EP2002/003194
申请日：2002-03-21
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , ROGGO, Silvio , HINTERMANN, Samuel , RASETTI, Vittorio , VON KROSIGK, Ulrike
发明人： ROGGO, Silvio , HINTERMANN, Samuel , RASETTI, Vittorio , VON KROSIGK, Ulrike
IPC分类号： C07D307/20
CPC分类号： C07D295/185 , C07C237/22 , C07C311/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2603/74 , C07D295/32 , C07F9/46
摘要： The invention provides compounds of formula I, wherein Q, R, S, T, U, V, X and Y are as defined in the description, and the preparation thereof. The compounds of formula I are useful as pharmaceuticals.
摘要翻译：本发明提供式I化合物，其中Q，R，S，T，U，V，X和Y如说明书中所定义，及其制备。式I的化合物可用作药物。

8. 发明申请

WO1998007694A1 ACYLAMINOALKENYLENE-AMIDE DERIVATIVES AS NK1 AND NK2 ANTAGONISTS 审中-公开
标题翻译：作为NK1和NK2拮抗剂的亚氨基亚氨基酰胺衍生物
公开(公告)号：WO1998007694A1
公开(公告)日：1998-02-26
申请号：PCT/EP1997004436
申请日：1997-08-13
申请人： NOVARTIS AG , GERSPACHER, Marc , VON SPRECHER, Andreas , MAH, Robert , ROGGO, Silvio , STUTZ, Stefan
发明人： NOVARTIS AG
IPC分类号： C07D209/20
CPC分类号： C07D403/12 , C07C237/22 , C07D209/20 , C07D209/24 , C07D223/12
摘要： Compounds of formula (I) wherein R is phenyl that is unsubstituted or is substituted by 1, 2 or 3 substituents selected from the group halogen, lower alkyl, trifluoromethyl, hydroxy and lower alkoxy; R1 is hydrogen or lower alkyl, R2 is hydrogen, lower alkyl or phenyl that is unsubstituted or is substituted by 1, 2 or 3 substituents selected from the group halogen, lower alkyl, trifluoromethyl, hydroxy and lower alkoxy, R3 is phenyl that is unsubstituted or is substituted by 1, 2 or 3 substituents selected from the group halogen, lower alkyl, trifluoromethyl, hydroxy and lower alkoxy; or is naphthyl, 1H-indol-3-yl or 1-lower alkyl-indol-3-yl, R4' and R4'' are each independently of the other hydrogen or lower alkyl, at least one of the radicals R4' and R4'' being hydrogen, and R5 is C3-C8cycloalkyl, D-azacycloheptan-2-on-3-yl or L-azacycloheptan-2-on-3-yl; or a salt thereof, have valuable pharmaceutical properties and are effective especially as NK1 and NK2 antagonists.
摘要翻译：式（I）的化合物，其中R是未被取代或被1,2或3个选自卤素，低级烷基，三氟甲基，羟基和低级烷氧基的取代基取代的苯基; R 1是氢或低级烷基，R 2是氢，未被取代的或被1,2或3个选自卤素，低级烷基，三氟甲基，羟基和低级烷氧基的取代基取代的低级烷基或苯基，R 3是未取代的或被1,2或3个选自卤素，低级烷基，三氟甲基，羟基和低级烷氧基的取代基取代; 或是萘基，1H-吲哚-3-基或1-低级烷基 - 吲哚-3-基，R 4'和R 4“各自独立地为另一个氢或低级烷基，基团R 4'和R 4中的至少一个 “为氢，R5为C3-C8环烷基，D-氮杂环庚烷-2-基-3-基或L-氮杂环庚烷-2-基-3-基; 或其盐具有有价值的药物性质，特别是作为NK1和NK2拮抗剂是有效的。

9. 发明申请

WO1996026183A1 1-ARYL-2-ACYLAMINO-ETHANE COMPOUNDS AND THEIR USE AS NEUROKININ ESPECIALLY NEUROKININ 1 ANTAGONISTS 审中-公开
标题翻译： 1-ARYL-2-ACYLAMINO-ETHANE化合物及其作为神经元素特异性神经营养因子1拮抗剂
公开(公告)号：WO1996026183A1
公开(公告)日：1996-08-29
申请号：PCT/EP1996000555
申请日：1996-02-09
申请人： CIBA-GEIGY AG , GERSPACHER, Marc , VON SPRECHER, Andreas , ROGGO, Silvio , MAH, Robert , OFNER, Silvio , VEENSTRA, Siem, Jacob , BETSCHART, Claudia , AUBERSON, Yves , SCHILLING, Walter
发明人： CIBA-GEIGY AG
IPC分类号： C07C237/22
CPC分类号： C07D213/40 , C07C237/22 , C07C255/29 , C07C311/51 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/22 , C07D211/44 , C07D211/48 , C07D211/58 , C07D213/70 , C07D215/46 , C07D223/12 , C07D231/12 , C07D231/38 , C07D233/56 , C07D235/16 , C07D235/28 , C07D239/42 , C07D241/20 , C07D249/08 , C07D295/13 , C07D295/135 , C07D295/185 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/10
摘要： 1-Aryl-2-acylamino-ethane compounds of formula (I), wherein R1 is aryl or heteroaryl; R2 is hydrogen, lower alkyl or aryl-lower alkyl; R3 is hydrogen, lower alkyl, aryl or heteroaryl; R4 is aryl or heteroaryl; X is C1-C7alkylene, C2-C7 alkenyline or C4-C7 alkanedienylene, and Am is an unsubstituted or mono- or di-substituted amino group, a disubstituted amino group being understood as including also an amino group in which the amino nitrogen is bonded into a ring, or a salt thereof, have valuable pharmaceutical properties and are especially effective as NK1 antagonists. They are prepared in a manner known per se.
摘要翻译：式（I）的1-芳基-2-酰基氨基 - 乙烷化合物，其中R 1是芳基或杂芳基; R2是氢，低级烷基或芳基 - 低级烷基; R3是氢，低级烷基，芳基或杂芳基; R4是芳基或杂芳基; X是C 1 -C 7亚烷基，C 2 -C 7链烯基或C 4 -C 7链烷二烯基，并且Am是未取代或单取代或二取代的氨基，二取代的氨基也被理解为也包括其中氨基氮键合的氨基成环或其盐具有有价值的药物性质，并且作为NK1拮抗剂是特别有效的。它们是以本身已知的方式准备的。

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