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21. 发明申请

WO2011047432A1 FUSED RING ANALOGUES OF ANTI-FIBROTIC AGENTS 审中-公开
标题翻译：抗纤维剂的熔融环形成
公开(公告)号：WO2011047432A1
公开(公告)日：2011-04-28
申请号：PCT/AU2010/001398
申请日：2010-10-21
申请人： FIBROTECH THERAPEUTICS PTY LTD , WILLIAMS, Spencer John , ZAMMIT, Steven , KELLY, Darren James
发明人： WILLIAMS, Spencer John , ZAMMIT, Steven , KELLY, Darren James
IPC分类号： C07D413/04 , C07D333/64 , C07D209/46 , C07D209/34 , C07D211/18 , C07D215/233 , C07D241/42 , C07D265/24 , C07D239/88 , C07D241/44 , C07D215/58 , C07D235/26 , C07D209/12 , C07D235/28 , C07D235/12 , C07D335/06 , C07D311/08 , C07D317/70 , C07D403/12 , C07D311/76 , C07D307/87 , C07D235/16 , C07D333/62 , C07D405/12 , C07D401/04 , C07D409/12 , C07D311/04 , C07D401/12 , C07D261/20 , C07D275/04 , C07D277/70 , C07D263/56 , C07D277/62 , C07D263/58 , C07D277/68 , C07D417/04 , C07D235/06 , C07D277/64 , C07D265/22 , C07D239/91 , C07D403/04 , C07D291/08 , C07D265/36 , C07D279/16 , C07C233/81 , A61K31/517 , A61K31/4184 , A61K31/498 , A61K31/343 , A61K31/424 , A61K31/506 , A61K31/352 , A61K31/428 , A61K31/536 , A61K31/381 , A61K31/5365 , A61K31/382 , A61K31/429 , A61K31/538 , A61K31/403 , A61K31/435 , A61K31/5383 , A61K31/4035 , A61K31/4355 , A61K31/5415 , A61K31/404 , A61K31/4365 , A61K31/416 , A61K31/437 , A61P35/00 , A61P11/00 , A61P17/02 , A61P9/00 , A61P13/12 , A61P29/00
CPC分类号： C07D498/04 , C07C235/40 , C07C235/56 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D233/64 , C07D235/12 , C07D235/24 , C07D235/26 , C07D239/91 , C07D241/44 , C07D263/56 , C07D265/22 , C07D265/36 , C07D277/64 , C07D285/24 , C07D307/85 , C07D311/16 , C07D333/62 , C07D333/70 , C07D335/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
摘要翻译：本发明涉及可用作抗纤维化剂的芳基羰基和杂芳基羰基邻氨基苯甲酸酯化合物。本发明还涉及其制备方法，含有这些化合物的药物组合物和这些化合物在治疗障碍中的用途。

22. 发明申请

WO2010023685A3 CRYSTALLINE FORM OF 2-(2-HYDROXY PHENYL)BENZ[E][1,3]OXAZIN-4-ONE, PROCESS FOR THE SAME AND USE FOR PRODUCING 4-(3,5-BIS(2-HYDROXYPHENYL)-1H-1,2,4-TRIAZOL-1-YL)BENZOIC ACID 审中-公开
标题翻译： 2-（2-羟基苯基）苯并[E] [1,3]氧杂-4-酮的结晶形式及其制备方法及用于制备4-（3,5-双（2-羟基苯基） 1,2,4-TRIAZOL-1-YL）苯甲酸
公开(公告)号：WO2010023685A3
公开(公告)日：2010-08-19
申请号：PCT/IN2009000461
申请日：2009-08-20
申请人： MATRIX LAB LTD , KARUSALA NAGESWARA RAO , CHAVHAN BHAUSAHEB SHRIRANG , GOSULA VEERA VENKATA SATYA SURYA APPALA NARASIMHA , DATTA DEBASHISH
发明人： KARUSALA NAGESWARA RAO , CHAVHAN BHAUSAHEB SHRIRANG , GOSULA VEERA VENKATA SATYA SURYA APPALA NARASIMHA , DATTA DEBASHISH
IPC分类号： C07D265/22 , C07D249/08
CPC分类号： C07D265/22
摘要： The present invention relates to a crystalline form of 2-(2-hydroxyphenyl) benz [e] [1, 3] oxazin-4-one, a process for production thereof and its use in the preparation of 4- (3, 5-bis (2-hydroxyphenyl)-1H-1, 2, 4-triazol-1-yl) benzoic acid. The improved process for the preparation 4-(3,5-bis (2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl) benzoic acid (Deferasirox), wherein salicylic chloride is reacted with salicylamide in presence of a solvent to give acyl compound, which is heated to higher temperature in-situ to undergo cyclization to obtain crystalline form of 2-(2-hydroxyphenyl) benz [e] [1, 3] oxazin-4-on and further reaction with hydrazino benzoic acid to give 4-(3,5- bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl)benzoic acid.
摘要翻译：本发明涉及2-（2-羟基苯基）苯并[e] [1,3]恶嗪-4-酮的结晶形式，其制备方法及其在制备4-（3,5- 双（2-羟基苯基）-1H-1,2,4-三唑-1-基）苯甲酸。制备4-（3,5-双（2-羟基苯基）-1H-1,2,4-三唑-1-基）苯甲酸（Deferasirox）的改进方法，其中水杨酰氯与水杨酰胺在得到酰基化合物的溶剂，将其原位加热至更高温度进行环化，得到2-（2-羟基苯基）苯并[e] [1,3]恶嗪-4-酮的结晶形式，并进一步与肼基反应苯甲酸，得到4-（3,5-双（2-羟基苯基）-1H-1,2,4-三唑-1-基）苯甲酸。

23. 发明申请

WO2008036843A2 PLATELET ADP RECEPTOR INHIBITORS 审中-公开
标题翻译： PLATELET ADP受体抑制剂
公开(公告)号：WO2008036843A2
公开(公告)日：2008-03-27
申请号：PCT/US2007/079076
申请日：2007-09-20
申请人： PORTOLA PHARMACEUTICALS, INC. , SCARBOROUGH, Robert M. , BAUER, Shawn M. , PANDEY, Anjali
发明人： SCARBOROUGH, Robert M. , BAUER, Shawn M. , PANDEY, Anjali
IPC分类号： A61K31/536 , A61K31/517 , A61K31/381 , C07D239/96 , C07D265/22
CPC分类号： C07D409/12 , C07D239/96 , C07D265/22 , C07D403/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Compounds are provided which are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.
摘要翻译：提供了可用作血小板ADP受体抑制剂，用于治疗血栓形成和降低患者的次级缺血事件的可能性和/或严重性的化合物。

24. 发明申请

WO2006128802A2 3-METHANESULFONYLQUINOLINES AS GABA-B ENHANCERS 审中-公开
标题翻译：作为GABA-B增强剂的3-甲磺酰基胆碱
公开(公告)号：WO2006128802A2
公开(公告)日：2006-12-07
申请号：PCT/EP2006/062514
申请日：2006-05-23
申请人： F. HOFFMANN-LA ROCHE AG , MALHERBE, Parichehr , MASCIADRI, Raffaello , NORCROSS, Roger David , PRINSSEN, Eric
发明人： MALHERBE, Parichehr , MASCIADRI, Raffaello , NORCROSS, Roger David , PRINSSEN, Eric
IPC分类号： C07C225/22 , C07D265/22 , C07D215/36 , C07D215/38
CPC分类号： C07D265/22 , C07D215/36 , C07D215/38 , C07D215/42 , C07D401/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 , R 2 and R 3 are as defined hereinabove which are active at the GABA B receptor and which can be used for the preparation of medicaments useful in the control or prevention of CNS disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3和R 3如上所定义，其在 GABA B 受体，其可用于制备可用于控制或预防CNS障碍的药物。

25. 发明申请

WO2006036790A1 ARYL-UREIDO BENZOXAZINONE COMPOUNDS 审中-公开
标题翻译： ARYL-UREIDO BENZOXAZINONE化合物
公开(公告)号：WO2006036790A1
公开(公告)日：2006-04-06
申请号：PCT/US2005/034155
申请日：2005-09-22
申请人： HONEYWELL INTERNATIONAL INC. , POTRAWA, Thomas , SCHULZ, Joachim
发明人： POTRAWA, Thomas , SCHULZ, Joachim
IPC分类号： C07D265/22
CPC分类号： C09K11/06 , C07D265/22 , C09D11/037 , C09K2211/1007 , C09K2211/1033
摘要： Fluorescent pigment compounds comprising aryl-ureido benzoxazinone compounds of the general formula (I): wherein R 1 is an substituted or unsubstituted aryl group, R 2 and R 3 are each independently selected from an H atom, an alkyl group, an alkoxy group, an alkylcarboxy group and a halogen atom, X is a carbon or sulfur atom and n is an integer of I or more. Many of the compounds of this class produce a yellow, generally deep yellow, emission at wavelengths of about 560 to about 585 nm when excited by an appropriate UV source. These compounds produce fluorescence making them useful as fluorescent pigments, those compounds providing emission wavelengths within the range of from about 560 to about 585 or higher when excited by a UV source are particularly useful. Those compounds having this emission spectra for the compounds makes these compounds particularly useful as pigments in security applications, particularly as pigments for use in security inks and fibers.
摘要翻译：包含通式（I）的芳基 - 脲基苯并嗪酮化合物的荧光颜料化合物：其中R

26. 发明申请

WO2004014880A1 CHROMONE DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译： CHROMONE衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：WO2004014880A1
公开(公告)日：2004-02-19
申请号：PCT/IB2003/003541
申请日：2003-08-04
申请人： WARNER-LAMBERT COMPANY LLC , ORTWINE, Daniel, Fred
发明人： ORTWINE, Daniel, Fred
IPC分类号： C07D265/22
CPC分类号： C07D311/22 , C07D265/22
摘要： This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R 1 , Q, y 2 , y 3 , Y 4 , U 5 , U 6 , U 8 , and R2 are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically 10 acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MW-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MNIP 13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides methods of treating diseases such as heart disease, multiple sclerosis, osteo- and rheumatoid arthritis, arthritis other than osteo- or rheumatoid arthritis, cardiac insufficiency, inflammatory bowel disease, heart failure, age-related macular degeneration, chronic obstructive pulmonary disease, asthma, periodontal diseases, psoriasis, atherosclerosis, and osteoporosis in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition. The invention also provides combinations, comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, together with another pharmaceutically active component as described in the specification.
摘要翻译：本发明提供由式I定义的化合物或其药学上可接受的盐，其中R 1，Q，y 2，y 3，Y 4，U 5，U 6， 8>和R2如说明书中所定义。本发明还提供药物组合物，其包含本说明书中定义的式I化合物或其药学上可接受的盐以及药学上可接受的载体，稀释剂或赋形剂。本发明还提供了在动物中抑制MW-13酶的方法，包括向动物施用式I化合物或其药学上可接受的盐。本发明还提供了治疗由患者中的MNIP13酶介导的疾病的方法，包括单独或在药物组合物中向患者施用式I化合物或其药学上可接受的盐。本发明还提供了治疗诸如心脏病，多发性硬化，骨关节炎和类风湿性关节炎，除了骨关节炎或类风湿性关节炎之外的关节炎，心功能不全，炎性肠病，心力衰竭，年龄相关性黄斑变性，慢性阻塞性肺疾病，哮喘，牙周疾病，牛皮癣，动脉粥样硬化和骨质疏松症，包括单独或在药物组合物中向患者施用式I化合物或其药学上可接受的盐。本发明还提供了包含式I化合物或其药学上可接受的盐以及说明书中描述的另一种药物活性成分的组合。

27. 发明申请

WO0228841B1 REAGENTS FOR LABELING BIOMOLECULES HAVING ALDEHYDE OR KETONE MOIETIES 审中-公开
标题翻译：用于标记含有二醛或酮酮生物分子的试剂
公开(公告)号：WO0228841B1
公开(公告)日：2002-11-21
申请号：PCT/US0130851
申请日：2001-10-02
申请人： MOLECULAR PROBES INC
发明人： HAUGLAND RICHARD P , STEINBERG THOMAS H , PATTON WAYNE P , ZHENJUN DIWU
IPC分类号： G01N33/532 , C07D239/91 , C07D239/94 , C07D249/08 , C07D263/60 , C07D265/22 , C07D277/66 , C07D401/04 , G01N33/58
CPC分类号： C07D265/22 , C07D239/91 , Y10T436/143333 , Y10T436/200833
摘要： Novel fluorescent derivitization reagents are described that are suitable for coupling to biomolecules that contain aldehyde or ketone functional groups. The method of treating a sample with the derivativization reagents is described. The reagents are particularly useful for labeling glycoproteins or glycopeptides, nucleic acids, and lipopolysaccharides in electrophoresis gels.
摘要翻译：描述了适用于与含有醛或酮官能团的生物分子偶联的新型荧光衍生试剂。描述了用衍生化试剂处理样品的方法。这些试剂特别可用于在电泳凝胶中标记糖蛋白或糖肽，核酸和脂多糖。

28. 发明申请

WO0204444A3 HETEROCYCLE CARBOXAMIDES AS ANTIVIRAL AGENTS 审中-公开
标题翻译：杂环羧酰胺类作为抗病毒剂
公开(公告)号：WO0204444A3
公开(公告)日：2002-05-30
申请号：PCT/US0116495
申请日：2001-06-25
申请人： UPJOHN CO , BUNDY GORDON L , CISKE FRED L , GENIN MICHAEL J , HEASLEY STEVEN E , LARSEN SCOTT D , LEE BYUNG HYUN , MAY PAUL D , PALMER JOHN R , SCHNUTE MARK E , VAILLANCOURT VALERIE A , THORARENSEN ATLI , WOLF ALLISON J , WICNIENSKI NANCY ANNE , WILHITE DAVID
发明人： BUNDY GORDON L , CISKE FRED L , GENIN MICHAEL J , HEASLEY STEVEN E , LARSEN SCOTT D , LEE BYUNG HYUN , MAY PAUL D , PALMER JOHN R , SCHNUTE MARK E , VAILLANCOURT VALERIE A , THORARENSEN ATLI , WOLF ALLISON J , WICNIENSKI NANCY ANNE , WILHITE DAVID
IPC分类号： A61K31/353 , A61K31/4025 , A61K31/4375 , A61K31/5025 , A61K31/519 , A61K31/536 , A61K31/5377 , A61K31/5415 , A61K31/542 , A61K31/549 , A61P31/22 , C07D265/02 , C07D265/22 , C07D279/02 , C07D285/16 , C07D311/22 , C07D333/58 , C07D405/06 , C07D471/04 , C07D495/04 , C07D513/04 , A61K31/352 , A61K31/381 , A61K31/4365 , A61K31/4985 , C07D333/68
CPC分类号： C07D285/16 , C07D265/22 , C07D279/02 , C07D311/22 , C07D333/58 , C07D471/04 , C07D495/04 , C07D513/04
摘要： The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
摘要翻译：本发明提供可用作抗病毒剂的式I化合物，特别是用作针对疱疹家族病毒的药剂。

29. 发明申请

WO02028841A2 REAGENTS FOR LABELING BIOMOLECULES HAVING ALDEHYDE OR KETONE MOIETIES 审中-公开
标题翻译：用醛或酮馏分标记生物分子的试剂
公开(公告)号：WO02028841A2
公开(公告)日：2002-04-11
申请号：PCT/US2001/030851
申请日：2001-10-02
IPC分类号： G01N33/532 , C07D239/91 , C07D239/94 , C07D249/08 , C07D263/60 , C07D265/22 , C07D277/66 , C07D401/04 , G01N33/58
CPC分类号： C07D265/22 , C07D239/91 , Y10T436/143333 , Y10T436/200833
摘要： Novel fluorescent derivitization reagents are described that are suitable for coupling to biomolecules that contain aldehyde or ketone functional groups. The method of treating a sample with the derivativization reagents is described. The reagents are particularly useful for labeling glycoproteins or glycopeptides, nucleic acids, and lipopolysaccharides in electrophoresis gels.
摘要翻译：本发明涉及用于形成衍生物的荧光试剂，其适于与含有醛或酮官能团的生物分子偶联。本发明还涉及涉及通过所考虑的试剂处理样品的方法。所讨论的试剂特别适用于标记电泳凝胶中的糖蛋白或糖肽，核酸和脂多糖。

30. 发明申请

WO01068619A1 5-AMIDE SUBSTITUTED DIARYLAMINES AS MEX INHIBITORS 审中-公开
标题翻译： 5-酰胺取代的二元胺作为MEX抑制剂
公开(公告)号：WO01068619A1
公开(公告)日：2001-09-20
申请号：PCT/US2001/007816
申请日：2001-03-12
IPC分类号： C07D249/18 , A61K31/166 , A61K31/196 , A61K31/337 , A61K31/357 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/4045 , A61K31/415 , A61K31/416 , A61K31/417 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/4453 , A61K31/4741 , A61K31/475 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/501 , A61K31/5375 , A61K31/538 , A61K31/54 , A61K31/662 , A61P3/02 , A61P5/14 , A61P9/04 , A61P9/10 , A61P13/12 , A61P17/06 , A61P19/02 , A61P25/04 , A61P25/32 , A61P29/00 , A61P29/02 , A61P35/00 , A61P37/02 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/38 , C07C237/40 , C07C259/10 , C07C311/46 , C07C323/42 , C07D207/12 , C07D207/27 , C07D209/16 , C07D211/20 , C07D211/26 , C07D211/32 , C07D211/42 , C07D213/40 , C07D213/74 , C07D213/75 , C07D231/40 , C07D231/56 , C07D233/64 , C07D237/08 , C07D241/04 , C07D241/44 , C07D263/58 , C07D265/22 , C07D277/04 , C07D285/12 , C07D285/135 , C07D295/10 , C07D295/13 , C07D295/192 , C07D307/68 , C07D319/18 , C07D333/36 , C07D333/38 , C07D333/48 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D487/04 , C07D491/048 , C07D521/00 , C07F9/6509 , A61K31/536 , C07D295/12 , C07D295/18
CPC分类号： C07D265/22 , C07C237/30 , C07C237/32 , C07C259/10 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/13 , C07D295/192 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12
摘要： Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.
摘要翻译：二芳基胺，例如式（I）或式（II）的5-酰胺取代的二芳基胺，其中A是羟基，C 1-6烷氧基或NR 6 OR 7; X是OR 12，NR 13 R 12或NR 14; MEK抑制剂可用于治疗各种增生性疾病状态，例如与MEK的多动症有关的病症以及由MEK级联调节的疾病。

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