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61. 发明申请

WO2010039256A1 2-ACYLAMINOPROPOANOL-TYPE GLUCOSYLCERAMIDE SYNTHASE INHIBITORS 审中-公开
标题翻译： 2-乙酰氨基酚类型葡萄糖苷合成酶抑制剂
公开(公告)号：WO2010039256A1
公开(公告)日：2010-04-08
申请号：PCT/US2009/005435
申请日：2009-10-02
申请人： GENZYME CORPORATION , SIEGEL, Craig , BASTOS, Cecilia, M. , HARRIS, David, J. , DIOS, Angeles , LEE, Edward , SILVA, Richard , CUFF, Lisa, M. , LEVINE, Mikaela , CELATKA, Cassandra, A. , JOZAFIAK, Thomas, H. , VINICK, Frederic , XIANG, Yibin , KANE, John , LIAO, Junkai
发明人： SIEGEL, Craig , BASTOS, Cecilia, M. , HARRIS, David, J. , DIOS, Angeles , LEE, Edward , SILVA, Richard , CUFF, Lisa, M. , LEVINE, Mikaela , CELATKA, Cassandra, A. , JOZAFIAK, Thomas, H. , VINICK, Frederic , XIANG, Yibin , KANE, John , LIAO, Junkai
IPC分类号： A61K31/4025 , C07C271/12 , C07D207/10 , C07D295/04 , C07D295/10 , C07D319/08 , C07D405/06 , C07D405/14 , C07D407/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
CPC分类号： A61K31/4025 , C07C271/12 , C07D207/12 , C07D317/60 , C07D319/18 , C07D319/20 , C07D333/16 , C07D407/06 , C07D407/12 , C07D409/04 , C07D413/04 , C07D417/12
摘要： A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译：用于治疗多囊肾病的化合物由结构式（I）表示：或其药学上可接受的盐。药物组合物包含由结构式（I）表示的化合物或其药学上可接受的盐。在有需要的受试者中治疗多囊肾病的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。分别在有需要的受试者中治疗多囊肾病的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。

62. 发明申请

WO2009138338A1 NOVEL N-(2-AMINO-PHENYL)-ACRYLAMIDES 审中-公开
标题翻译：新型N-（2-氨基 - 苯基） - 丙烯酰胺
公开(公告)号：WO2009138338A1
公开(公告)日：2009-11-19
申请号：PCT/EP2009/055441
申请日：2009-05-06
申请人： F. HOFFMANN-LA ROCHE AG , WONG, Jason Christopher , WU, Xihan
发明人： WONG, Jason Christopher , WU, Xihan
IPC分类号： C07D207/10 , C07D207/12 , C07D207/14 , C07D401/12 , C07D405/12 , C07D491/08 , A61K31/40 , A61K31/4433 , A61K31/444 , A61P35/00
CPC分类号： C07D207/10 , C07D207/12 , C07D207/14 , C07D401/12 , C07D405/12 , C07D491/08
摘要： The present invention is directed to the compounds of formula (I), wherein R 1 to R 4 have the significances given herein, to processes for the manufacture of said compounds as well as medicaments containing said compounds. The compounds according to this invention show anti-proliferative and differentiation-inducing activity and are thus useful for the treatment of diseases such as cancer in humans or animals.
摘要翻译：本发明涉及式（I）化合物，其中R1至R4具有本文给出的意义，涉及制备所述化合物的方法以及含有所述化合物的药物。根据本发明的化合物显示抗增殖和分化诱导活性，因此可用于治疗诸如人或动物中的癌症的疾病。

63. 发明申请

WO2009100095A1 3-(4-FLUOROPHENYL)-3-HYDROXY-2-AMINO-PROPIONIC ACID AMIDES AND RELATED COMPOUNDS HAVING ANALGESIC ACTIVITY 审中-公开
标题翻译： 3-（4-氟苯基）-3-羟基-2-氨基 - 丙酸和相关化合物具有活性
公开(公告)号：WO2009100095A1
公开(公告)日：2009-08-13
申请号：PCT/US2009/033014
申请日：2009-02-04
申请人： ALLERGAN, INC. , LEBLOND, Bertrand , BEAUSOLEIL, Eric , TAVERNE, Thierry , DONELLO, John, E. , YANG, Rong , CHAUVIGNAC, Cedric
发明人： LEBLOND, Bertrand , BEAUSOLEIL, Eric , TAVERNE, Thierry , DONELLO, John, E. , YANG, Rong , CHAUVIGNAC, Cedric
IPC分类号： C07D207/10 , C07D207/20 , C07D277/04 , C07D295/185 , C07C233/00 , C07C311/00 , A61K31/40 , A61P29/00
CPC分类号： C07D277/04 , C07C229/36 , C07C233/11 , C07C259/06 , C07C271/22 , C07C311/06 , C07D207/10 , C07D207/20 , C07D295/185
摘要： Compounds according to the formula below are disclosed herein: Therapeutic methods for the treatment of pain, compositions, and medicaments related thereto are also disclosed.
摘要翻译：本文公开了根据下式的化合物：还公开了治疗与其相关的疼痛，组合物和药物的治疗方法。

64. 发明申请

WO2008089485A3 CARBOXYETHYLPYRROLE COMPOUNDS AND METHODS OF THEIR PRODUCTION 审中-公开
标题翻译：羧乙基吡咯化合物及其生产方法
公开(公告)号：WO2008089485A3
公开(公告)日：2008-09-04
申请号：PCT/US2008051685
申请日：2008-01-22
申请人： CLEVELAND CLINIC FOUNDATION , SALOMON ROBERT G , CRABB JOHN W , LU LIANG , GU XIAORONG , CHOI JAEWOO
发明人： SALOMON ROBERT G , CRABB JOHN W , LU LIANG , GU XIAORONG , CHOI JAEWOO
IPC分类号： G01N33/53 , C07D207/10 , C07D207/50
CPC分类号： G01N33/531 , C07C67/313 , C07C69/716 , C07C2603/18 , C07D207/337 , C07D495/04
摘要： Provided herein are a 9-fluorenylmethyl (Fm) ester of 4,7-dioxoheptanoic acid (DOHA) (DOHA-Fm) compound that is useful for the preparation of 2-(?-carboxyethyl)pyrrole (CEP)-carrier derivatives, as well as methods of preparing same. Also provided are isolated CEP-protein derivatives, isolated phosphatidylethanolamine (PE)-CEP derivatives, isolated biotinylated CEP derivative, as well as methods of preparing same. Also included is a CEP- Fm modified lysine and a method of preparing a CEP-carrier derivatives using the CEP-Fm modified lysine.
摘要翻译：本文提供可用于制备2-（α-羧乙基）吡咯（CEP） - 载体衍生物的4,7-二氧代庚酸（DOHA）（DOHA-Fm）化合物的9-芴基甲基（Fm）以及制备它的方法。还提供了分离的CEP-蛋白质衍生物，分离的磷脂酰乙醇胺（PE）-CEP衍生物，分离的生物素化的CEP衍生物，以及制备它们的方法。还包括CEP-Fm修饰的赖氨酸和使用CEP-Fm修饰的赖氨酸制备CEP-载体衍生物的方法。

65. 发明申请

WO2008006702A1 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ACTIVE COMPOUNDS 审中-公开
标题翻译： 11BETA-羟基脱氢酶脱氢酶1型活性化合物
公开(公告)号：WO2008006702A1
公开(公告)日：2008-01-17
申请号：PCT/EP2007/056467
申请日：2007-06-28
申请人： NOVO NORDISK A/S , EBDRUP, Søren , ANDERSEN, Henrik, Sune
发明人： EBDRUP, Søren , ANDERSEN, Henrik, Sune
IPC分类号： C07D487/08 , C07D401/10 , C07D401/14 , C07D207/16 , C07D405/14 , C07D491/08 , C07D471/08 , C07D207/14 , C07D207/10 , A61K31/4025 , A61P3/04 , A61P9/12 , C07D401/12 , C07D207/12
CPC分类号： C07D487/08 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/14 , C07D471/08 , C07D491/08
摘要： The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1 ) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. Their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
摘要翻译：描述了使用取代的酰胺调节11β-羟基类固醇脱氢酶1型（11βHSD1）的活性以及这些化合物作为药物组合物的用途。还有一类新颖的通式I的取代酰胺。它们在治疗中的用途，包含该化合物的药物组合物及其在制备药物中的用途被描述。本发明化合物是11βHSDI的调节剂，更具体地说是抑制剂的活性，可用于治疗一系列需要活性糖皮质激素的细胞内浓度降低的医学疾病。

66. 发明申请

WO2007140197A1 THERAPEUTIC PYRROLIDINE COMPOUNDS 审中-公开
标题翻译：治疗吡咯啉化合物
公开(公告)号：WO2007140197A1
公开(公告)日：2007-12-06
申请号：PCT/US2007/069516
申请日：2007-05-23
申请人： ALLERGAN, INC. , OLD, David, W. , DINH, Danny, T.
发明人： OLD, David, W. , DINH, Danny, T.
IPC分类号： C07D207/10 , C07D207/12 , C07D207/16 , C07D207/24 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , A61K31/4025 , A61P27/06
CPC分类号： C07D207/10 , C07D207/12 , C07D207/16 , C07D207/24 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12
摘要： Disclosed herein is a compound having a structure (I), or a pharmaceutically acceptable salt thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
摘要翻译：本文公开了具有结构（I）的化合物或其药学上可接受的盐。还公开了与之相关的治疗方法，组合物和药物。

67. 发明申请

WO2007102567A1 3,4-ジ置換ピロリジン誘導体の製造方法及び製造中間体审中-公开
标题翻译：生产3,4-取代的吡咯烷衍生物和中间体的方法
公开(公告)号：WO2007102567A1
公开(公告)日：2007-09-13
申请号：PCT/JP2007/054501
申请日：2007-03-08
申请人：杏林製薬株式会社 , 後藤崇之 , 荒谷一郎
发明人：後藤崇之 , 荒谷一郎
IPC分类号： C07D207/10 , C07D207/16 , C07B61/00
CPC分类号： C07D207/10 , C07D207/16
摘要： [PROBLEMS] To provide an industrially advantageous process for production of (3R,4S)-3-cyclopropylaminomethyl-4- fluoropyridine or an enantiomer thereof, which is a useful intermediate for the production of a 10-(3-cyclopropylaminomethyl-4-fluoropyrrolidinyl)- pyridobenzoxazinecarboxylic acid derivative which is a novel antibacterial agent. [MEANS FOR SOLVING PROBLEMS] A novel substance (3R,4S)-1-protected-3-cyclopropylcarbamoyl-4-hydroxy- pyrrolidine or an enantiomer thereof having a high optical purity can be produced by performing the highly stereoselective asymmetric hydrogenation of a 1-protected-4-alkoxycarbonyl-3-oxopyrrolidine, performing the ester hydrolysis, and then performing the amidation with cyclopropylamine to produce a crude crystal, and recrystallizing the crude crystal. By using this compound as an intermediate, it becomes possible to establish an industrial production process for producing (3R,4S)-3-cyclopropylaminomethyl-4- fluoropyrrolidine having a high quality or an enantiomer thereof by means of simple procedures at a high purity and in a steady yield.
摘要翻译：本发明提供工业上有利的（3R，4S）-3-环丙基氨基甲基-4-氟吡啶或其对映异构体的制备方法，其是制备10-（3-环丙基氨基甲基-4-氟吡咯烷基） - 吡啶并苯并恶嗪甲酸衍生物，它是一种新的抗菌剂。解决问题的手段具有高光学纯度的新型物质（3R，4S）-1-保护-3-环丙基氨基甲酰基-4-羟基吡咯烷或其对映异构体可以通过进行高度立体选择性的不对称氢化1 保护的4-烷氧基羰基-3-氧代吡咯烷，进行酯水解，然后用环丙胺进行酰胺化，得到粗结晶，再结晶粗结晶。通过使用该化合物作为中间体，可以通过简单的方法以高纯度制备具有高质量的（3R，4S）-3-环丙基氨基甲基-4-氟吡咯烷的工业生产方法和稳定收益。

68. 发明申请

WO2007058971A3 SOFT ANTICHOLINERGIC ESTERS 审中-公开
标题翻译：软抗胆碱能酯
公开(公告)号：WO2007058971A3
公开(公告)日：2007-07-26
申请号：PCT/US2006043858
申请日：2006-11-13
申请人： BODOR NICHOLAS S
发明人： BODOR NICHOLAS S
IPC分类号： C07D207/10 , A61K31/40 , A61K31/439 , A61P11/00 , A61P11/06 , A61P13/10 , A61P27/08 , C07D451/10
CPC分类号： C07D207/10 , A61K9/0048 , A61K9/0075 , A61K9/008 , A61K9/2059 , A61K31/167 , A61K31/40 , A61K31/439 , A61K31/56 , A61K31/58 , A61K45/06 , C07D451/10 , A61K2300/00
摘要： Soft anticholinergic esters of the formulas (Ia) or (Ib): wherein R 1 and R 2 are both phenyl or one of R 1 and R 2 is phenyl and the other is cyclopentyl; R is C 1 -C 8 alkyl, straight or branched chain; and X" is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
摘要翻译：式（Ia）或（Ib）的软抗胆碱能酯：其中R 1和R 2都是苯基或R 1 SUB和 R 2是苯基，另一个是环戊基; R为C 1 -C 8烷基，直链或支链; 并且X“是具有单一负电荷的阴离子;并且其中每个星号表示手性中心;除非另外指明，否则所述化合物在每个手性中心具有R，S或RS立体异构构型，或者是其混合物。

69. 发明申请

WO2006109075A3 HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90 审中-公开
标题翻译：羟基苯甲酸衍生物及其作为HSP90的抑制剂
公开(公告)号：WO2006109075A3
公开(公告)日：2006-11-30
申请号：PCT/GB2006001358
申请日：2006-04-13
申请人： ASTEX THERAPEUTICS LTD , CHESSARI GIANNI , CONGREVE MILES STUART , NAVARRO EVA FIGUEROA , FREDERICKSON MARTYN , MURRAY CHRISTOPHER , WOOLFORD ALISON JO-ANNE , CARR MARIA GRAZIA , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES
发明人： CHESSARI GIANNI , CONGREVE MILES STUART , NAVARRO EVA FIGUEROA , FREDERICKSON MARTYN , MURRAY CHRISTOPHER , WOOLFORD ALISON JO-ANNE , CARR MARIA GRAZIA , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES
IPC分类号： A61K31/401 , A61K31/166 , A61K31/445 , A61K31/5375 , C07C233/65 , C07C233/66 , C07D207/10 , C07D211/22 , C07D211/34 , C07D211/42 , C07D211/56 , C07D265/30 , C07D295/02 , C07D295/18 , C07D309/14
CPC分类号： C07D401/12 , C07C65/21 , C07D209/08 , C07D209/44 , C07D215/08 , C07D217/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10
摘要： The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R 1 is hydroxy or hydrogen; R 2 is hydroxy; methoxy or hydrogen; provided that at least one of R 1 and R 2 is hydroxy; R 3 is selected from hydrogen; halogen; cyano; C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy; wherein the C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy moieties are each optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; R 4 is selected from hydrogen; a group -(O) n -R 7 where n is 0 or 1 and R 7 is an acyclic C 1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and mono- or di-C 1-5 hydrocarbyl-amino, wherein the acyclic Ci-5 hydrocarbyl group and the mono and di-C 1-5 hydrocarbylamino moieties in each instance are optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; or R 3 and R 4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and R 5 and R 6 are as defined in the claims.
摘要翻译：本发明提供用作Hsp90抑制剂的化合物，具有式（I）的化合物：或其盐，互变异构体，溶剂化物和N-氧化物; 其中R 1是羟基或氢; R 2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R 3选自氢; 卤素; 氰基; C 1-5烃基和C 1-5氢烃氧基; 其中C 1-5烷基和C 1-5 - 烃基氧基部分各自任选被一个或多个选自羟基，卤素，C 1-2 烷氧基，氨基，单和二-C 1-12烷基氨基，以及5至12个环成员的芳基和杂芳基; R 4选自氢; 其中n为0或1且R 7为无环C 1-5的基团 - （O）N - ， - R 7 具有3〜7个环成员的单环碳环或杂环基; 卤素; 氰基; 羟基; 氨基; 和单 - 或二-C 1-5烃基 - 氨基，其中每个中的非环式C 1-5烃基和单和二-C 1-5烃基氨基部分实例任选被一个或多个选自羟基，卤素，C 1-12烷氧基，氨基，单和二-C 1-2烷基氨基的取代基取代，和芳基和5-12个环成员的杂芳基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; R 5和R 6如权利要求中所定义。

70. 发明申请

WO2006014549A3 SYNTHESIS OF AZO BONDED IMMUNOREGULATORY COMPOUNDS 审中-公开
公开(公告)号：WO2006014549A3
公开(公告)日：2006-02-09
申请号：PCT/US2005/024109
申请日：2005-07-07
申请人： NOBEX CORPORATION , SAUTHIER, Jennifer, A., Riggs , EKWURIBE, Nnochiri, N.
发明人： SAUTHIER, Jennifer, A., Riggs , EKWURIBE, Nnochiri, N.
IPC分类号： C07D207/09 , C07D207/10 , A61K31/4025
摘要： Methods are disclosed for preparing compounds of Formula I: where R 1 , R 3 , and R 4 are independently hydrogen or C 1 to C 4 alkyl, and R 2 is: where R 5 is selected from the group consisting of hydrogen and C 1 to C 4 alkyl, or where R 6 , R 7 and R 8 are independently hydrogen or C 1 to C 4 alkyl; or the esters or pharmacologically acceptable salts thereof.. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes. The compounds and or their metabolites can be used to treat or prevent various diseases, particularly inflammatory conditions of the GI tract.

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