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1. 发明申请

WO2005070926A1 THIAZOLE DERIVATIVES AS A2B ANTAGONISTS 审中-公开
标题翻译：噻唑衍生物作为A2B拮抗剂
公开(公告)号：WO2005070926A1
公开(公告)日：2005-08-04
申请号：PCT/EP2005/000542
申请日：2005-01-20
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , PRESS, Neil, John , TAYLOR, Roger, John
发明人： PRESS, Neil, John , TAYLOR, Roger, John
IPC分类号： C07D417/04
CPC分类号： C07D417/04 , C07D417/14
摘要： Compounds of formula (I) in free or salt form, where Ar is phenyl substituted by one or more substituents selected from halogen, cyano and C 1- C 8 -haloalkyl, or naphthyl, R 1 is hydrogen, phenyl optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkoxy-C l -C 8 alkyl, carboxy, C 1 -C 8 -alkoxycarbonyl and acyloxy, or R 1 is a 5- or 6- membered monovalent heterocyclic group, R 2 is hydrogen, C l -C 8 -alkyl, acyl or -CON(R 3 )R 4 , R 3 and R 4 are each independently hydrogen or C 1 -C s -alkyl, or together with the nitrogen atom to which they are attached denote a 5- or 6- membered heterocyclic group, and Y is a pyrimidinyl or pyridazinyl group, optionally substituted by at least one C 1 -C s -alkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkylthio, C 1 -C 8 -alkyl amino, di(C l -C 8 -alkyl) amino or acylamino group. The compounds are useful as pharmaceuticals.
摘要翻译：式（I）化合物为游离或盐形式，其中Ar为被一个或多个选自卤素，氰基和C 1 -C 8 - 卤代烷基或萘基的取代基取代的苯基，R 1为氢，任选被一个或多个更多选自卤素，氰基，羟基，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷氧基-C 1 -C 8烷基，羧基，C 1 -C 8 - 烷氧基羰基和酰氧基的取代基或 R 1是5-或6-元一价杂环基，R 2是氢，C 1 -C 8 - 烷基，酰基或-CON（R 3）R 4，R 3和R 4独立地为氢或C 1 -C 8 - 烷基，或与它们所连接的氮原子一起表示5-或6-元杂环基，Y为嘧啶基或哒嗪基，任选被至少一个C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷硫基，C 1 -C 8烷基氨基，二（C 1 -C 8 - 烷基）氨基或酰氨基。这些化合物可用作药物。

2. 发明申请

WO2005067976A2 DIRECT COMPRESSION FORMULATION AND PROCESS 审中-公开
标题翻译：直接压缩配方和工艺
公开(公告)号：WO2005067976A2
公开(公告)日：2005-07-28
申请号：PCT/EP2005/000400
申请日：2005-01-17
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , KOWALSKI, James , PARTHIBAN, Lakshman, Jayanth , PATEL, Arun, P.
发明人： KOWALSKI, James , PARTHIBAN, Lakshman, Jayanth , PATEL, Arun, P.
IPC分类号： A61K47/00
CPC分类号： A61K9/2077 , A61K9/2013 , A61K9/2054 , A61K9/2059 , A61K9/2095 , A61K31/40 , C07D207/16 , Y10T428/268
摘要： Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of being directly compressed with specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus presents formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.
摘要翻译：可以为98.5-100％纯度的二肽基肽酶IV抑制剂（本文称为DPP-IV）是能够用特定赋形剂直接压制成销售形式剂型的高剂量药物，例如具有所需硬度，分解能力和可接受的溶解特性。 DPP-IV不是固有的可压缩性，因此呈现配方问题。制剂中使用的赋形剂增强了药物和压片混合物的流动和压实性能。最佳流量有助于均匀的模头填充和重量控制。使用的粘合剂确保足够的内聚性质，使得DPP-IV能够使用直接压制方法进行压缩。所制备的片剂提供可接受的体外溶出曲线。

3. 发明申请

WO2005067895A1 CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：控制释放药物组合物
公开(公告)号：WO2005067895A1
公开(公告)日：2005-07-28
申请号：PCT/EP2005/000322
申请日：2005-01-14
申请人： SANDOZ AG , SRITHARAN, Seetharaman , DABHADE, Harsha, M. , ROY, Sunilendu, Bhushan
发明人： SRITHARAN, Seetharaman , DABHADE, Harsha, M. , ROY, Sunilendu, Bhushan
IPC分类号： A61K9/22
CPC分类号： A61K9/2009 , A61K9/2013 , A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K31/546
摘要： This invention relates to pharmaceutical compositions of the I-acetoxyethyl ester of the antibiotic compound cefuroxime, known as cefuroxime axetil. The invention more prticularly relates to controlled release formulations of cefuroxime axetil, containing one or more water soluble hydrophilic agents.
摘要翻译：本发明涉及抗生素化合物头孢呋辛的I-乙酰氧基乙酯的药物组合物，称为头孢呋辛酯。本发明更具体地涉及含有一种或多种水溶性亲水剂的头孢呋辛酯的控释制剂。

4. 发明申请

WO2005059132A1 RNAI POTENCY PREDICTION METHOD 审中-公开
标题翻译： RNAI POTENCY预测方法
公开(公告)号：WO2005059132A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/014037
申请日：2004-12-09
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , HALL, Jonathan , HUESKEN, Dieter , LANGE, Jörg, Bernd , NATT, Francois, Jean-Charles , REINHARDT, Mischa, Werner, Henri, Marie
发明人： HALL, Jonathan , HUESKEN, Dieter , LANGE, Jörg, Bernd , NATT, Francois, Jean-Charles , REINHARDT, Mischa, Werner, Henri, Marie
IPC分类号： C12N15/11
CPC分类号： G06F19/24 , C12N15/111 , C12N2310/14 , C12N2320/11
摘要： Methods for making an algorithm for the prediction of the RNAi potency of a RNAi reagent are provided. Also provided are methods for predicting the RNAi potency of a RNAi reagent and methods for inhibiting the expression of a given target gene using such an algorithm.
摘要翻译：提供了用于制备用于预测RNAi试剂的RNAi效力的算法的方法。还提供了用于预测RNAi试剂的RNAi效力的方法和使用这种算法抑制给定靶基因表达的方法。

5. 发明申请

WO2005059122A1 PATHOGENIC BOVINE ENTEROVIRUS, VACCINES, AND DIAGNOSTIC METHODS 审中-公开
标题翻译：病原体肠毒素，疫苗和诊断方法
公开(公告)号：WO2005059122A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/014117
申请日：2004-12-10
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , ANDERSON, Gary, A. , KEIL, Daniel, J. , FLAKUS, Robert, J.
发明人： ANDERSON, Gary, A. , KEIL, Daniel, J. , FLAKUS, Robert, J.
IPC分类号： C12N7/00
CPC分类号： C12N7/00 , A61K39/12 , A61K39/125 , A61K2039/5252 , A61K2039/5254 , A61K2039/552 , C12N2770/32334 , C12N2770/32351
摘要： The isolation of a novel pathogenic bovine enterovirus is described. The novel pathogenic bovine enterovirus is used to develop antibodies and immunogenic compositions against the novel pathogenic bovine enterovirus. Diagnostic assays are described.
摘要翻译：描述了新型致病性牛肠道病毒的分离。新型致病性牛肠道病毒用于开发针对新型致病性牛肠道病毒的抗体和免疫原性组合物。描述诊断测定。

6. 发明申请

WO2005054325A2 CROSSLINKABLE POLYUREA PREPOLYMERS 审中-公开
标题翻译：可交联的聚脲预聚物
公开(公告)号：WO2005054325A2
公开(公告)日：2005-06-16
申请号：PCT/EP2004/013352
申请日：2004-11-24
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , DEVLIN, Brian, Gerrard , TENA, Mireille
发明人： DEVLIN, Brian, Gerrard , TENA, Mireille
IPC分类号： C08G18/50
CPC分类号： C08G18/5024 , C08G18/6685 , C08G18/792 , C08L75/16
摘要： The present invention provides a water-soluble crosslinkable polyurea prepolymer. The crosslinkable polyurea prepolymer of the invention is prepared by reacting an amine- or isocyanate-capped polyurea with a multifunctional compound having at least one one ethylenically unsaturated group and a functional group coreactive with the capping amine or isocyanate groups of the amine- or isocyanate-capped polyurea. The amine- or isocyanatecapped polyurea is a copolymerization production of: (a) at least one poly(oxyalkylene) diamine, (b) optionally at least one organic dior poly-amine, (c) optionally at least one diisocyanate, and (d) at least one polyisocyanate. The crosslinkable polyurea prepolymer of the invention can find use in economically producing contact lenses which have durable, highly elastic soft contact lenses with desired physical properties. In addition, the present invention provides method for making a medical device, preferably an ophthalmic device, more preferably a contact lens.
摘要翻译：本发明提供了一种水溶性可交联聚脲预聚物。本发明的可交联聚脲预聚物通过胺封端或异氰酸酯封端的聚脲与具有至少一个烯键式不饱和基团和与封端胺共聚的官能团的多官能化合物或胺 - 或异氰酸酯 - 封端的聚脲。（a）至少一种聚（氧化烯）二胺，（b）任选的至少一种有机二酯或聚胺，（c）任选的至少一种二异氰酸酯和（ d）至少一种多异氰酸酯。本发明的可交联聚脲预聚物可用于经济地生产具有所需物理性能的耐用，高弹性软性隐形眼镜的隐形眼镜。此外，本发明提供了用于制造医疗装置，优选眼科装置，更优选为隐形眼镜的方法。

7. 发明申请

WO2005053704A1 METHOD FOR PREDICTING DRUG RESPONSIVENESS IN MYELOID NEOPLASMS 审中-公开
标题翻译：用于预测MYELOID NEOPLASMS中药物应答的方法
公开(公告)号：WO2005053704A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/013588
申请日：2004-11-30
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , CULVER, Kenneth, Wayne
发明人： CULVER, Kenneth, Wayne
IPC分类号： A61K31/553
CPC分类号： A61K31/553
摘要： This invention provides methods to predict from samples of blood or bone marrow which patients with myeloid neoplasms will show a good therapeutic response to therapeutic agents that work, at least in part, by inducing apoptosis in tumour cells. These methods can help determine treatment choices and select patients for drug studies.
摘要翻译：本发明提供从血液或骨髓样品中预测的方法，所述骨髓瘤患者对治疗剂显示良好的治疗反应，所述治疗剂至少部分通过诱导肿瘤细胞凋亡而起作用。这些方法可以帮助确定治疗选择并选择患者进行药物研究。

8. 发明申请

WO2005049040A1 COMBINATIONS COMPRISING AMPA RECEPTOR ANTAGONISTS FOR THE TREATMENT OF SCHIZOPHRENIA 审中-公开
标题翻译：包含AMPA受体拮抗剂用于治疗精神病药物的组合
公开(公告)号：WO2005049040A1
公开(公告)日：2005-06-02
申请号：PCT/EP2004/012150
申请日：2004-10-27
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , LINGENHÖHL, Kurt , MARTENYI, Ferenc , OFNER, Silvio , KAROLCHYK, Mary, Ann , O. KALKMAN, Hans
发明人： LINGENHÖHL, Kurt , MARTENYI, Ferenc , OFNER, Silvio , KAROLCHYK, Mary, Ann , O. KALKMAN, Hans
IPC分类号： A61K31/675
CPC分类号： A61K45/06 , A61K31/675 , A61K2300/00
摘要： The present invention relates to combinations suitable for the treatment of psychiatric/neurological disorders, in particular schizophrenia. The combinations comprise at least one AMPA receptor antagonist and at least one compound selected from the group consisting of (a) anti-epileptic drugs selected from barbiturates and derivatives thereof, benzodiazepines, carboxamides, hydantoins, succinimides, valproic acid and other fatty acid derivates and other anti-epileptic drugs, (b) conventional antipsychotics and (c) atypical antipsychotics.
摘要翻译：本发明涉及适用于治疗精神病/神经障碍，特别是精神分裂症的组合。所述组合包含至少一种AMPA受体拮抗剂和至少一种选自（a）选自巴比妥类及其衍生物，苯并二氮杂，甲酰胺，乙内酰脲，琥珀酰亚胺，丙戊酸和其它脂肪酸衍生物的抗癫痫药物的化合物和其他抗癫痫药，（b）常规抗精神病药和（c）非典型抗精神病药。

9. 发明申请

WO2005047273A1 THIAZOLE AND PYRAZOLE DERIVATIVES AS FLT-3 KINASE INHIBITORS 审中-公开
标题翻译：作为FLT-3激酶抑制剂的噻唑和吡唑衍生物
公开(公告)号：WO2005047273A1
公开(公告)日：2005-05-26
申请号：PCT/EP2004/012892
申请日：2004-11-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BOLD, Guido , FLOERSHEIMER, Andreas , FURET, Pascal , GUAGNANO, Vito , MASUYA, Keiichi , VAUPEL, Andrea , SCHOEPFER, Joseph
发明人： BOLD, Guido , FLOERSHEIMER, Andreas , FURET, Pascal , GUAGNANO, Vito , MASUYA, Keiichi , VAUPEL, Andrea , SCHOEPFER, Joseph
IPC分类号： C07D277/42
CPC分类号： C07D277/42 , C07D231/38 , C07D409/04 , C07D417/04 , C07D417/10
摘要： The invention relates to thiazole and pyrazole derivatives of formula (I) wherein Q is S and X is C, or Q is CH and X is N; R 1 is unsubtituted or substituted phenyl; and R 2 is unsubstituted or substituted aryl or heteroaryl; oa a salt of the said compounds, and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour disease, in particular such diseases which respond to an inhibition of the FIt-3 kinase.
摘要翻译：本发明涉及式（I）的噻唑和吡唑衍生物，其中Q为S且X为C，或Q为CH且X为N; R1是未取代的或取代的苯基; 并且R 2是未取代或取代的芳基或杂芳基; 所述化合物的盐，及其制备方法，包含该衍生物的药物组合物，以及该衍生物用于制备用于治疗特别是增殖性疾病如肿瘤疾病的药物组合物的用途，特别是对抑制FIT-3激酶的这些疾病。

10. 发明申请

WO2005045025A2 CLONING AND CHARACTERIZATION OF 5’ FLANKING REGIONS OF A HUMAN AGGRECANASE-1 GENE 审中-公开
标题翻译：人类AGGRECANASE-1基因5'区域的克隆和表征
公开(公告)号：WO2005045025A2
公开(公告)日：2005-05-19
申请号：PCT/EP2004/012567
申请日：2004-11-05
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , KUMAR, Chandrika, Saidapet
发明人： KUMAR, Chandrika, Saidapet
IPC分类号： C12N15/09
CPC分类号： C12N9/50 , A61K48/00 , C12N9/6421 , C12N15/85
摘要： Disclosed is a nucleic acid comprising Agg promoters and methods of using the same. The invention also provides methods for identifying and treating disease based on the activity of Agg promoters.
摘要翻译：公开了包含Agg启动子的核酸及其使用方法。本发明还提供了基于Agg启动子的活性鉴定和治疗疾病的方法。

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