专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2009071483A1 1- (INDAZ0L-5-YL) -UREAS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS 审中-公开
标题翻译： 1-（INDAZ0L-5-YL） - 作为二乙酰胆碱酯酶抑制剂
公开(公告)号：WO2009071483A1
公开(公告)日：2009-06-11
申请号：PCT/EP2008/066288
申请日：2008-11-27
申请人： VIA PHARMACEUTICALS, INC. , BOLIN, David Robert , CAI, Jianping , GOODNOW, Robert, Alan Jr.
发明人： BOLIN, David Robert , CAI, Jianping , GOODNOW, Robert, Alan Jr.
IPC分类号： C07D231/56 , C07D401/12 , A61P3/06 , A61K31/416
CPC分类号： C07D231/56 , C07D401/12
摘要： Provided herein are compounds of the Formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
摘要翻译：本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。这些化合物和含有它们的药物组合物可用于治疗疾病，例如肥胖症，II型糖尿病和代谢综合征。

2. 发明申请

WO2012130887A1 USE OF PHOSPHO-AKT AS A BIOMARKER OF DRUG RESPONSE 审中-公开
标题翻译：作为药物生物标记物的磷酸化AKT的应用
公开(公告)号：WO2012130887A1
公开(公告)日：2012-10-04
申请号：PCT/EP2012/055522
申请日：2012-03-28
申请人： BASILEA PHARMACEUTICA AG , BACHMANN, Felix , LANE, Heidi, Alexandra
发明人： BACHMANN, Felix , LANE, Heidi, Alexandra
IPC分类号： C12Q1/48 , G01N33/68 , G01N33/574
CPC分类号： C12Q1/485 , C07D413/04 , C07D413/14 , G01N33/57407 , G01N2440/14 , G01N2800/52
摘要： Use of phospho-Akt as a biomarker for predicting the response, such as resistance, to a compound, wherein phospho-Akt is Akt that has been phosphorylated on one or more residues, with the proviso that for Akt1, Akt2, and Akt3 the designation phospho-Akt is used to indicate phosphorylation at a site other than T308, T309 or T305 respectively, wherein the compound is a compound of general formula (I) wherein R represents phenyl, thienyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents a group C=Y, wherein Y stands for oxygen or nitrogen substituted by hydroxy or lower alkoxy; R 1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; R 2 , R 3 and R 6 represent hydrogen; R 4 and R 5 , independently of each other, represent hydrogen, lower alkyi or lower alkoxy; or R 4 and R 5 together represent methylenedioxy; and pharmaceutically acceptable derivatives thereof; or wherein R represents phenyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyi, halo-lower alkyi, hydroxy-lower alkyi, lower alkoxy-lower alkyi, acyloxy-lower alkyi, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, formyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents oxygen; R 1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyi or cyano-lower alkyi; R 2 , R 3 and R 6 represent hydrogen; R 4 and R 5 , independently of each other, represent hydrogen, lower alkyi or lower alkoxy; or R 4 and R 5 together represent methylenedioxy; and pharmaceutically acceptable derivatives thereof. Methods of treatment of neoplastic and autoimmune diseases with these compounds are also disclosed.
摘要翻译：使用磷酸-Akt作为生物标志物来预测对一种或多种残基已经被磷酸化的磷酸化Akt的化合物的反应（例如抗性），条件是Akt1，Akt2和Akt3的指定为磷酸化Akt用于分别指示除了T308，T309或T305以外的位点的磷酸化，其中该化合物是通式（I）的化合物，其中R表示苯基，噻吩基或吡啶基，其中苯基任选被一个或两个取代基取代烷基，卤代低级烷基，羟基 - 低级烷基，低级烷氧基 - 低级烷基，酰氧基 - 低级烷基，苯基，羟基，低级烷氧基，羟基 - 低级烷氧基，低级烷氧基 - 低级烷氧基，苯基 - 低级烷氧基，低级烷基羰基氧基，氨基，单烷基氨基，二烷基氨基，低级烷氧基羰基氨基，低级烷基羰基氨基，取代的氨基，其中氮上的两个取代基与氮杂环基一起形成，低级烷基羰基，羧基，低级烷基氧羰基，氰基，卤素和硝基; 并且其中两个相邻的取代基是亚甲二氧基; 并且其中吡啶基任选被低级烷氧基，氨基或卤素取代; X表示基团C = Y，其中Y表示被羟基或低级烷氧基取代的氧或氮; R 1表示氢，低级烷基羰基，羟基 - 低级烷基或氰基 - 低级烷基; R2，R3和R6表示氢; R4和R5彼此独立地表示氢，低级烷基或低级烷氧基; 或R4和R5一起表示亚甲二氧基; 及其药学上可接受的衍生物; 或其中R表示苯基或吡啶基，其中苯基任选被一个或两个独立地选自烷基，卤代低级烷基，羟基 - 低级烷基，低级烷氧基 - 低级烷基，酰氧基 - 低级烷基，苯基，羟基，低级烷氧基，羟基 - 低级烷氧基，低级烷氧基 - 低级烷氧基，苯基 - 低级烷氧基，低级烷基羰基氧基，氨基，单烷基氨基，二烷基氨基，低级烷氧基羰基氨基，低级烷基羰基氨基，取代氨基，其中氮上的两个取代基与氮杂环基一起形成低级烷基羰基，羧基，低级烷氧基羰基，甲酰基，氰基，卤素和硝基; 并且其中两个相邻的取代基是亚甲二氧基; 并且其中吡啶基任选被低级烷氧基，氨基或卤素取代; X表示氧; R1代表氢，低级烷基羰基，羟基 - 低级烷基或氰基 - 低级烷基; R2，R3和R6表示氢; R4和R5彼此独立地表示氢，低级烷基或低级烷氧基; 或R4和R5一起表示亚甲二氧基; 及其药学上可接受的衍生物。还公开了用这些化合物治疗肿瘤和自身免疫疾病的方法。

3. 发明申请

WO2011141415A1 OXIDATION PROCESS FOR PREPARING 3-FORMYL-CEPHEM DERIVATIVES 审中-公开
标题翻译：用于制备3-甲基孕酮衍生物的氧化方法
公开(公告)号：WO2011141415A1
公开(公告)日：2011-11-17
申请号：PCT/EP2011/057404
申请日：2011-05-09
申请人： BASILEA PHARMACEUTICA INTERNATIONAL LTD. , VERVEST, Ivan, Joseph, Maria
发明人： VERVEST, Ivan, Joseph, Maria
IPC分类号： C07D501/34
CPC分类号： C07D501/04 , C07D501/34
摘要： The present invention relates to an improved process for oxidizing 3-hydroxy-methyl-cephem derivatives to the corresponding 3-formyl-cephem derivatives. In particular this oxidation process is for the preparation of 7-[2-(5-amino-[1,2,4]thia-diazol-3-yl)-2-hydroxyimino-acetylamino]-3-formyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid derivatives of formula (I) using a combination of a hypervalent iodine oxidizing agent of the type 10-I-3 such as bis(acetoxy)iodo-benzene (BAIB) and a catalyst such as 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). These compounds of formula (I) are intermediates in the synthesis of ceftobiprole.
摘要翻译：本发明涉及将3-羟基甲基头孢烯衍生物氧化为相应的3-甲酰基头孢烯衍生物的改进方法。特别地，该氧化方法用于制备7- [2-（5-氨基 - [1,2,4]噻二唑-3-基）-2-羟基亚氨基 - 乙酰基氨基] -3-甲酰基-8-氧代 -5-硫杂-1-氮杂 - 双环[4.2.0]辛-2-烯-2-羧酸衍生物，其使用10-I-3型的高价碘氧化剂的组合，例如双（乙酰氧基）碘 - 苯（BAIB）和催化剂如2,2,6,6-四甲基-1-哌啶氧基（TEMPO）。这些式（I）化合物是合成头孢匹罗的中间体。

4. 发明申请

WO2008025758A1 MANUFACTURE OF SUBSTANTIALLY PURE MONOCHLOROACETIC ACID 审中-公开
标题翻译：主要单稳态酸的制备
公开(公告)号：WO2008025758A1
公开(公告)日：2008-03-06
申请号：PCT/EP2007/058908
申请日：2007-08-28
申请人： BUSS CHEMTECH AG , STOENESCU TIMMERMANS, Roxana , KETTENBACH, Gerhard
发明人： STOENESCU TIMMERMANS, Roxana , KETTENBACH, Gerhard
IPC分类号： C07C51/377 , C07C53/16
CPC分类号： C07C51/377 , C07C53/16
摘要： A process for the manufacture of substantially pure monochloroacetic acid from a liquid chloroacetic acid mixture comprising monochloroacetic acid and dichloroacetic acid, in particular in an amount of 2 to 40 percent by weight, wherein said mixture, further mixed with a suspended hydrogenation catalyst, is mixed with hydrogen gas and the resulting mixture is brought to reaction in a reactor, which is characterized in that the reactor is a loop reactor comprising a gas and liquid recirculation system coupled via an ejector mixing nozzle, in which reactor the gas and liquid are circulated in co-current flow, and the mixing intensity introduced to the liquid phase is at least 50 W/l of liquid phase.
摘要翻译：一种从包含一氯乙酸和二氯乙酸的液体氯乙酸混合物制备基本上纯的一氯乙酸的方法，特别是2-40重量％，其中进一步与悬浮氢化催化剂混合的混合物混合用氢气将所得混合物在反应器中进行反应，其特征在于反应器是环流反应器，其包括通过喷射器混合喷嘴耦合的气体和液体再循环系统，其中气体和液体在其中循环并流流动，引入液相的混合强度至少为50W / l液相。

5. 发明申请

WO2008017696A1 NEW MACROLIDES USEFUL AGAINST INFLAMMATORY AND ALLERGIC DISSEASES 审中-公开
标题翻译：适用于抗炎和过敏症的新型抗体
公开(公告)号：WO2008017696A1
公开(公告)日：2008-02-14
申请号：PCT/EP2007/058247
申请日：2007-08-08
申请人： BASILEA PHARMACEUTICA AG , KELLENBERGER, Johannes Laurenz , DREIER, Jürg , REINELT, Stefan Bernhard
发明人： KELLENBERGER, Johannes Laurenz , DREIER, Jürg , REINELT, Stefan Bernhard
IPC分类号： C07H17/08 , A61K31/7048
CPC分类号： C07H17/08
摘要： Macrolide compounds of formula I: with PDF4 inhibiting activity are described, wherein R1 is a residue -Y-X-Q; Y is S, SO or SO 2 ; X is a bond or a linear group consisting of hydrogen atoms and with up to 9 atoms selected from C, N, O and/or S, of which up to 2 atoms can be N and one atom can be O or S, one carbon atom can appear as a CO group and the sulphur atom can appear as an SO2 group and two adjacent C atoms can be present as - CH=CH- or -C≡C- and which group X is unsubstituted or is substituted with - COO-W or -CONH-W; Q is a residue -V-A1-L- A2-W or, if X does not represent a bond, may also be -NR6R7; V is a divalent aromatic or heterocyclic group; W is aryl or heterocyclyl; or in a group -V-A1-L- A2-W, wherein at least one of the groups A1; L or A2 is present, can also be a monovalent substituted or unsubstituted, saturated or unsaturated linear group with up to 5 atoms consisting of C, N, O and/or S of which one carbon can appear as a CO group one sulphur atom can appear as an SO2 group, A1, A2 are independently of each other either absent or a C 1 -C 4 alkylene group; L is -0-, -S-, -SO2-, -NH-, -CO-, -(CO)O-, -O(OC)-, -(CO)NH-, -NH(CO)-, -(SO 2 )NH-, -HN(SO 2 )-, -HN(CO)NH-, -0(CO)NH-, -NH(CO)O-, or can also be absent if Al and/or A2 are present; R2 is hydrogen and R3 is and 0R4 or R2, R3 taken together form a C=O group; R4 is hydrogen or an saturated or unsaturated aliphatic group with 1 to 6 carbon atoms; R6, R7 are independently selected from aryl; aralkyl; heterocyclyl and heterocyclylalkyl; and one of R6 and R7 can also be a group -L-W; and * indicates a chiral centre which is in the (R) or (S) form.
摘要翻译：描述了式I的大环内酯化合物：具有PDF4抑制活性，其中R1是残基-Y-X-Q; Y是S，SO或SO 2; X是由氢原子和最多9个选自C，N，O和/或S的原子组成的键或线性基团，其中最多2个原子可以是N，一个原子可以是O或S，一个碳原子可以表现为CO基团，硫原子可以表现为SO 2基团，并且两个相邻的C原子可以以CH = CH-或-C = C-存在，并且X基团是未取代的或被-OCO- W或-CONH-W; Q是残基-V-A1-L-A2-W，或者如果X不表示键，也可以是-NR6R7; V是二价芳族或杂环基; W是芳基或杂环基; 或基团-V-A1-L-A2-W，其中组A1中的至少一个; 存在L或A2，也可以是具有至多5个原子组成的C，N，O和/或S的一价取代或未取代的饱和或不饱和的直链基团，其中一个碳可以作为CO基团出现，一个硫原子可以表示为SO 2基团，A1，A2彼此独立地不存在或者是C 1 -C 4亚烷基; L是-O - ， - S - ， - SO 2 - ， - NH - ， - CO-， - （CO）O-， - O（OC） - ， - （CO）NH-， - NH - （SO 2 - ）NH - ， - NH（SO 2 - ） - ， - NH（CO）NH - ， - （CO）NH - ， - NH ）O-，或者如果存在Al和/或A2也可以不存在; R2为氢，R3为0R4或R2，R3一起形成C = O基团; R4是氢或具有1至6个碳原子的饱和或不饱和脂族基; R6，R7独立地选自芳基; 芳; 杂环基和杂环基烷基; R6和R7之一也可以是-L-W基团; 和*表示处于（R）或（S）形式的手性中心。

6. 发明申请

WO2008116813A2 COMBINATION MEDICAMENTS FOR TREATING BACTERIAL INFECTIONS 审中-公开
标题翻译：用于治疗细菌感染的组合药物
公开(公告)号：WO2008116813A2
公开(公告)日：2008-10-02
申请号：PCT/EP2008/053336
申请日：2008-03-19
申请人： BASILEA PHARMACEUTICA AG , DESARBRE, Eric , PAGE, Malcolm G.P.
发明人： DESARBRE, Eric , PAGE, Malcolm G.P.
IPC分类号： A61K31/427 , A61K31/4436 , A61P31/04
CPC分类号： C07D417/14 , A61K31/197 , A61K31/407 , A61K31/4162 , A61K31/427 , A61K31/43 , A61K31/4436 , A61K31/4439 , A61K2300/00
摘要： Use of a monobactam antibiotic of formula (I) wherein the oxyimino group i.e. >C=N-O- has Z-orientation, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a bacterial infection in combination with a carbapenem antibiotic or a pharmaceutically acceptable salt thereof.
摘要翻译：其中氧亚氨基（即> C = NO-具有Z取向）的式（I）的单环内酯抗生素或其药学上可接受的盐在制备药物中的用途，所述药物用于治疗细菌感染与碳青霉烯类抗生素或其药学上可接受的盐组合。

7. 发明申请

WO2006128730A1 IMPROVED PROCESS FOR TREATING AN AQUEOUS MEDIUM USING REVERSE OSMOSIS AND REVERSE OSMOSIS SYSTEM THEREFOR 审中-公开
标题翻译：使用反向麻醉和反转的OSMOSIS系统治疗水质中毒的改进方法
公开(公告)号：WO2006128730A1
公开(公告)日：2006-12-07
申请号：PCT/EP2006/005318
申请日：2006-06-02
申请人： TORAY MEMBRANE EUROPE AG , JANK, Manfred , MÜLLER, Andrea
发明人： JANK, Manfred , MÜLLER, Andrea
IPC分类号： B01D61/12 , C02F1/44 , B01D65/08
CPC分类号： B01D61/04 , B01D61/022 , B01D61/12 , B01D2311/04 , C02F1/441 , C02F5/08 , C02F2209/005 , B01D2311/12
摘要： Process for treating a feed stream of an aqueous medium of a given composition, which comprises dissolved potentially scale-forming components, in a reverse osmosis (RO) system under given process conditions, providing a permeate stream and a stream of a retentate (concentrate) which comprises potentially scale-forming components at a concentration sufficiently high to cause scale formation in those parts of the RO system being in contact with said retentate in the absence of a scale inhibitor, in which process (a) the retentate is continuously monitored to detect the presence of particles of potentially scale-forming components in said retentate and a reading of one or more physical parameters of the retentate related to the presence of such particles is continuously recorded; (b) said recorded reading is continuously compared to measurement values for said one or more parameters of a retentate obtained from an aqueous medium of the same composition under the same process conditions which values have empirically been predetermined; and (c) an amount of scale inhibitor is added to the RO system upstream of the membrane once the recorded reading for the one or more parameters differs from said predetermined measurement values, said amount of scale inhibitor having been empirically predetermined to prevent scale formation under said conditions.
摘要翻译：在给定的工艺条件下，在反渗透（RO）系统中处理给定组合物的含水介质的进料流，其包含溶解的潜在的结垢成分组分，提供渗透物流和渗余物（浓缩物）流，其包括在足够高的浓度下潜在的水垢形成组分，以在不存在阻垢剂的情况下在RO系统的那些部分与所述滞留物接触的水垢形成，其中过程（a）持续监测渗余物以检测持续记录所述滞留物中潜在的水垢形成成分的颗粒的存在以及与这种颗粒的存在相关的渗余物的一个或多个物理参数的读数; （b）将所记录的读数连续地与在经验上预先确定的相同工艺条件下从相同成分的水性介质获得的所述一个或多个参数的测量值进行比较; 一旦所述一个或多个参数的记录读数与所述预定测量值不同，所述防垢剂的量就被添加到所述膜上游的RO系统中，所述阻垢剂的量已被经验地预定以防止结垢形成说条件

8. 发明申请

WO2006002836A1 BRAUSEZUSAMMENSETZUNGEN VON EINSCHLAFMITTELN 审中-公开
标题翻译： EINSCHLAFMITTELN淋浴房组合物
公开(公告)号：WO2006002836A1
公开(公告)日：2006-01-12
申请号：PCT/EP2005/006847
申请日：2005-06-24
申请人： LOSAN PHARMA GMBH , GRUBER, Peter
发明人： GRUBER, Peter
IPC分类号： A61K9/20
CPC分类号： A61K9/0007
摘要： Eine feste, schnell zerfallende Brauseformulierung, umfassend ein Einschlafmittel und ein Brausesystem, gestattet eine problemlose Einnahme und bewirkt eine rasche Resorption und einen beschleunigten Blutspiegelanstieg, womit ein rasches Einschlafen gewährleistet wird.
摘要翻译：一种固体，快速崩解包括安眠药和泡腾系统，该系统允许容易摄取，并导致迅速吸收和血液水平加速增加泡腾制剂，从而快速睡眠得到保证。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式