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1. 发明申请

WO2003090737A3 METHODS AND COMPOSITIONS FOR TREATMENT OF CANCER PAIN 审中-公开
公开(公告)号：WO2003090737A3
公开(公告)日：2003-11-06
申请号：PCT/EP2003/004152
申请日：2003-04-22
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FUJIMOTO, Roger, Aki , URBAN, Laszlo , GONZALEZ, Isabel
发明人： FUJIMOTO, Roger, Aki , URBAN, Laszlo , GONZALEZ, Isabel
IPC分类号： A61K31/196
摘要： The invention provides a method of treating cancer pain, e.g. bone cancer pain, in a subject in need of such treatment which comprises administering to the subject an effective amount of a COX-2 inhibitor; advantageously a compound of formula (I); wherein R, R 1 R 2 , R 3 , R 4 , and R 5 are as defined; a pharmaceutically acceptable salts thereof; or a pharmaceutically acceptable prodrug ester thereof.

2. 发明申请

WO2003090737A2 METHODS AND COMPOSITIONS FOR TREATMENT OF CANCER PAIN 审中-公开
标题翻译：治疗癌症的方法和组合物
公开(公告)号：WO2003090737A2
公开(公告)日：2003-11-06
申请号：PCT/EP2003/004152
申请日：2003-04-22
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FUJIMOTO, Roger, Aki , URBAN, Laszlo , GONZALEZ, Isabel
发明人： FUJIMOTO, Roger, Aki , URBAN, Laszlo , GONZALEZ, Isabel
IPC分类号： A61K31/196
CPC分类号： A61K31/196
摘要： The invention provides a method of treating cancer pain, e.g. bone cancer pain, in a subject in need of such treatment which comprises administering to the subject an effective amount of a COX-2 inhibitor; advantageously a compound of formula (I); wherein R, R 1 R 2 , R 3 , R 4 , and R 5 are as defined; a pharmaceutically acceptable salts thereof; or a pharmaceutically acceptable prodrug ester thereof.
摘要翻译：本发明提供了治疗癌症疼痛的方法，例如，在需要这种治疗的受试者中包括对受试者施用有效量的COX-2抑制剂的骨癌疼痛; 有利地是式（I）的化合物; 其中R，R 1，R 2，R 3，R 4和R 5如所定义; 其药学上可接受的盐; 或其药学上可接受的前药酯。

3. 发明申请

WO02072577A2 CERTAIN AZACYCLOALKYL SUBSTITUTED ACETIC ACID DERIVATIVES 审中-公开
标题翻译：某些乙酰胆碱取代的乙酸衍生物
公开(公告)号：WO02072577A2
公开(公告)日：2002-09-19
申请号：PCT/EP0202808
申请日：2002-03-13
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , FUJIMOTO ROGER AKI , MCQUIRE LESLIE WIGHTON , MONOVICH LAUREN G , NANTERMET PHILIPPE , PARKER DAVID THOMAS , ROBINSON LESLIE ANN , SKILES JERRY W , TOMMASI RUBEN ALBERTO
发明人： FUJIMOTO ROGER AKI , MCQUIRE LESLIE WIGHTON , MONOVICH LAUREN G , NANTERMET PHILIPPE , PARKER DAVID THOMAS , ROBINSON LESLIE ANN , SKILES JERRY W , TOMMASI RUBEN ALBERTO
IPC分类号： C12N9/99 , A61K31/40 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K31/55 , A61P1/04 , A61P7/00 , A61P9/10 , A61P11/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P25/00 , A61P25/14 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07D211/32 , C07D211/34 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
CPC分类号： C07D401/12 , C07D211/34 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/12
摘要： Compounds of the formula (I) wherein R represents OH or NHOH; R1 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or acyl derived from a carboxylic acid, from a carbonic acid, from a carbamic acid of from a sulfonic acid; R2 represents biarylsulfonyl or aryloxyarylsufonyl; R3 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl or acyl derived from a carboxylic acid, from a carbonic acid or form a carbamic acid; R4 and R5 represent independently hydrogen, lower alkyl, lower alkoxycarbonyl, aryl-lower alkyl or cycloalkyl-lower alkyl; m is zero, 1, 2 or 3; pharmaceutically acceptable prodrug derivatives thereof; pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; and their use for inhibiting matrix degrading metalloproteinases and preventing or treating matrix metalloproteinase dependent conditions in mammals.
摘要翻译：其中R表示OH或NHOH的式（I）化合物; R 1表示氢，任选取代的低级烷基，芳基 - 低级烷基，环烷基 - 低级烷基或衍生自羧酸的酰基，来自碳酸，来自磺酸的氨基甲酸; R2表示联芳基磺酰基或芳氧基芳基磺酰基; R3表示氢，任选取代的低级烷基，芳基 - 低级烷基，环烷基 - 低级烷基或衍生自羧酸的酰基，由碳酸或形成氨基甲酸; R4和R5独立地表示氢，低级烷基，低级烷氧基羰基，芳基 - 低级烷基或环烷基 - 低级烷基; m为零，1,2或3; 其药学上可接受的前药衍生物; 其药学上可接受的盐; 包含所述化合物的药物组合物; 以及它们用于抑制基质降解金属蛋白酶和预防或治疗哺乳动物中基质金属蛋白酶依赖性条件的用途。

4. 发明申请

WO1998013347A1 ARYL-SUBSTITUTED ACRYLAMIDES WITH LEUKOTRIENE B4 (LTB-4) RECEPTOR ANTAGONIST ACTIVITY 审中-公开
标题翻译： ARYL取代的丙烯酸酯与LEUKOTRIENE B4（LTB-4）受体拮抗剂活性
公开(公告)号：WO1998013347A1
公开(公告)日：1998-04-02
申请号：PCT/EP1997005255
申请日：1997-09-24
申请人： NOVARTIS AG , GREENSPAN, Paul, David , FUJIMOTO, Roger, Aki
发明人： NOVARTIS AG
IPC分类号： C07D213/53
CPC分类号： C07D213/69 , C07C235/34 , C07C317/46 , C07C323/62 , C07D333/16 , C07D333/24
摘要： Disclosed are compounds of formula (I) wherein W is CH or N; R is (mono- or di-carbocyclic or heterocyclic aryl)-lower alkyl; R is hydrogen or lower alkyl; R and R are hydrogen, lower alkyl, lower alkoxy-lower alkyl or aryl-lower alkyl; or R and R joined together represent lower alkylene optionally interrupted by O, NH, N-lower alkyl or S so as to form a ring with the amide nitrogen; X is O, S, SO, SO2 or a direct bond; X is O, S, SO, SO2 or a direct bond; Y is a direct bond, lower alkylene or lower alkylidene; and Z is carboxyl, 5-tetrazolyl, hydroxymethyl or carboxyl derivatized in the form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; which are useful as LTB-4 antagonists.
摘要翻译：公开了式（I）的化合物，其中W是CH或N; R是（单或二碳环或杂环芳基） - 低级烷基; R 1是氢或低级烷基; R 2和R 3是氢，低级烷基，低级烷氧基 - 低级烷基或芳基 - 低级烷基; 或R 2和R 3连接在一起代表被O，NH，N-低级烷基或S间隔的低级亚烷基，以便与酰胺氮形成环; X是O，S，SO，SO 2或直接键; X 1是O，S，SO，SO 2或直接键; Y是直接键，低级亚烷基或低级亚烷基; Z为羧基，5-四唑基，羟甲基或以药学上可接受的酯形式衍生的羧基; 及其药学上可接受的盐; 其作为LTB-4拮抗剂是有用的。

5. 发明申请

WO2008148754A3 MACROCYCLES AND THEIR USES 审中-公开
标题翻译： MACROCYCLES及其用途
公开(公告)号：WO2008148754A3
公开(公告)日：2009-03-05
申请号：PCT/EP2008056838
申请日：2008-06-03
申请人： NOVARTIS AG , FUJIMOTO ROGER AKI , KRASTEL PHILIPP , LAMARCHE MATTHEW J
发明人： FUJIMOTO ROGER AKI , KRASTEL PHILIPP , LAMARCHE MATTHEW J
IPC分类号： C07D513/22 , A61K31/429 , A61K31/4353 , A61P31/04
CPC分类号： C07K7/64 , A61K38/12 , A61K45/06 , C07D513/22
摘要： The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.
摘要翻译：本申请描述了可用于治疗，预防和/或改善疾病的有机化合物。

6. 发明申请

WO9930695A8 SUBSTITUTED AMIDINO COMPOUNDS IN THE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE 审中-公开
标题翻译：取代的氨基酸化合物治疗慢性阻塞性肺疾病
公开(公告)号：WO9930695A8
公开(公告)日：1999-07-29
申请号：PCT/EP9808066
申请日：1998-12-10
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , MARSHALL PAUL JAMES , FUJIMOTO ROGER AKI
发明人： MARSHALL PAUL JAMES , FUJIMOTO ROGER AKI
IPC分类号： A61K31/606 , A61K31/155 , A61K31/166 , A61P11/00 , C07C257/18
CPC分类号： A61K31/166
摘要： Use in medicaments for the treatment of chronic obstructive pulmonary disease of compounds of formula (I) wherein the C(=NH)-NHR3 group may be in tautomeric or isomeric form, or a pharmaceutically acceptable salt thereof, in which: R1 is amino which is mono- or disubstituted by a substitutent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R2 is hydrogen, halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy or is hydroxy which is etherified by an aliphatic, araliphatic or aromatic alcohol or by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy or which is esterified by an aliphatic or araliphatic carboxylic acid; R3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X1 and X3, independently or one another, are oxygen (-O-) or sulphur (-S-); and X2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical; wherein the phenyl rings of formula (I) may be, independently or one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein aryl in the above definitions may be, independently of one another, further substituted by one or more substitutents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is ethereified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein a cycloaliphatic hydrocarbon radical may be substituted by an aliphatic radical.
摘要翻译：用于治疗慢性阻塞性肺疾病的药物，其中C（= NH）-NHR3基团可以是互变异构或异构体形式的式（I）化合物或其药学上可接受的盐，其中：R1是氨基，其中被选自脂族烃基，芳脂族烃基，芳族基和脂环族烃基的取代基单取代或二取代，或者是被二价脂族烃基或所述被氧中断的基团二取代的氨基; R2是氢，卤素，三氟甲基，脂族烃基，羟基或是被脂族，芳脂族或芳族醇或被羧基取代的脂族醇，被酯化的羧基或被酰胺化的羧基醚化的羟基，或被酯化的由脂族或芳脂族羧酸制备; R3是氢或由有机羧酸，有机羧酸，磺酸或氨基甲酸衍生的酰基; X1和X3彼此独立地或彼此是氧（-O-）或硫（-S-）; X2是可以被芳族基团中断的二价脂族烃基; 其中式（I）的苯环可以彼此独立或彼此进一步被一个或多个选自卤素，三氟甲基，脂族烃基，羟基和羟基的取代基取代，所述取代基被脂肪醇醚化或酯化由脂族或芳脂族羧酸制备; 其中上述定义中的芳基可以彼此独立地进一步被一个或多个取代基取代，所述取代基选自卤素，三氟甲基，脂族烃基，羟基和被脂族醇醚化的羟基或被脂族烃酯化的羟基或芳脂族羧酸; 其中脂环族烃基可以被脂族基团取代。

7. 发明申请

WO2008148754A2 MACROCYCLES AND THEIR USES 审中-公开
标题翻译： MACROCYCLES及其用途
公开(公告)号：WO2008148754A2
公开(公告)日：2008-12-11
申请号：PCT/EP2008/056838
申请日：2008-06-03
申请人： NOVARTIS AG , FUJIMOTO, Roger, Aki , KRASTEL, Philipp , LAMARCHE, Matthew, J.
发明人： FUJIMOTO, Roger, Aki , KRASTEL, Philipp , LAMARCHE, Matthew, J.
CPC分类号： C07K7/64 , A61K38/12 , A61K45/06 , C07D513/22
摘要： The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.
摘要翻译：本申请描述了可用于治疗，预防和/或改善疾病的有机化合物。

8. 发明申请

WO2002072577A3 AZACYCLOALKYL SUBSTITUTED ACETIC ACID DERIVATIVES FOR USE AS MMP INHIBITORS. 审中-公开
公开(公告)号：WO2002072577A3
公开(公告)日：2002-09-19
申请号：PCT/EP2002/002808
申请日：2002-03-13
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , FUJIMOTO, Roger, Aki , MCQUIRE, Leslie, Wighton , MONOVICH, Lauren, G. , NANTERMET, Philippe , PARKER, David, Thomas , ROBINSON, Leslie, Ann , SKILES, Jerry, W. , TOMMASI, Ruben, Alberto
发明人： FUJIMOTO, Roger, Aki , MCQUIRE, Leslie, Wighton , MONOVICH, Lauren, G. , NANTERMET, Philippe , PARKER, David, Thomas , ROBINSON, Leslie, Ann , SKILES, Jerry, W. , TOMMASI, Ruben, Alberto
IPC分类号： C07D409/12
摘要： Compounds of the formula (I) wherein R represents OH or NHOH; R 1 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or acyl derived from a carboxylic acid, from a carbonic acid, from a carbamic acid of from a sulfonic acid; R 2 represents biarylsulfonyl or aryloxyarylsufonyl; R 3 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl or acyl derived from a carboxylic acid, from a carbonic acid or form a carbamic acid; R 4 and R 5 represent independently hydrogen, lower alkyl, lower alkoxycarbonyl, aryl-lower alkyl or cycloalkyl-lower alkyl; m is zero, 1, 2 or 3; pharmaceutically acceptable prodrug derivatives thereof; pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; and their use for inhibiting matrix degrading metalloproteinases and preventing or treating matrix metalloproteinase dependent conditions in mammals.

9. 发明申请

WO2004048314A1 SUBSTITUTED AMINO PHENYLACETIC ACIDS, DERIVATIVES THEREOF, THEIR PREPARATION AND THEIR USE AS CYCLOOXYGENASE 2 (COX-2) INHIBITORS 审中-公开
标题翻译：取代的氨基苯乙酸，其衍生物，其制备方法及其作为CYCLOOXYGENASE 2（COX-2）抑制剂的用途
公开(公告)号：WO2004048314A1
公开(公告)日：2004-06-10
申请号：PCT/EP2003/013246
申请日：2003-11-25
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FUJIMOTO, Roger, Aki , MCQUIRE, Leslie, Wighton , MONOVICH, Lauren, G. , MUGRAGE, Benjamin, Biro , PARKER, David, Thomas , VAN DUZER, John, Henry , WATTANASIN, Sompong
发明人： FUJIMOTO, Roger, Aki , MCQUIRE, Leslie, Wighton , MONOVICH, Lauren, G. , MUGRAGE, Benjamin, Biro , PARKER, David, Thomas , VAN DUZER, John, Henry , WATTANASIN, Sompong
IPC分类号： C07C229/42
CPC分类号： C07D215/38 , C07C229/42 , C07D215/40 , C07D215/44 , C07D317/58 , C07D333/20 , C07D333/28
摘要： Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C 3 -C 8 )cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted β-naphthyl, bicyclic heterocyclic aryl, (C 3 -C 6 )cycloalkylmonocyclic carbocyclic aryl, or (C 5 or C 6 )cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof, and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.
摘要翻译：式（I）化合物，其中R是氢，低级烷基，（C 3 -C 8）环烷基，羟基，卤素，低级烷氧基，三氟甲氧基，三氟甲基或氰基; 并且A是联芳基，任选取代的β-萘基，双环杂环芳基，（C 3 -C 6）环烷基单环碳环芳基或（C 5或C 6）环烷烃稠合单环碳环芳基; 其药学上可接受的盐及其药学上可接受的酯; 其可用于治疗COX-2依赖性疾病。

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