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1. 发明申请

WO1998015532A1 SOLID PHASE SYNTHESIS OF HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：固相化合物的固相合成
公开(公告)号：WO1998015532A1
公开(公告)日：1998-04-16
申请号：PCT/EP1997005547
申请日：1997-10-08
申请人： NOVARTIS AG , MARZINZIK, Andreas , FELDER, Eduard
发明人： NOVARTIS AG
IPC分类号： C07D239/42
CPC分类号： C07D231/12 , C07D211/86 , C07D211/90 , C07D213/56 , C07D213/85 , C07D215/14 , C07D239/22 , C07D239/26 , C07D239/42 , C07D243/12 , C07D401/04 , C07D403/04 , C07D409/04 , C07D417/04 , C40B40/00
摘要： Here we report a study on a reaction sequence on solid phase, suitable for the generation of molecular diversity on small heterocycles. For each reaction, suitable conditions on solid phase were worked out and a variety of reactive agents (building blocks) was utilized in an effort to grasp the system's breadth of applicability. The inventive reaction sequence can be applied, for example, to exploit by the combinatorial approaches of the split and mix concept. The reaction sequence comprises the following steps: a) a solid carrier having reactive surface groups is loaded directly or via a spacer group with a compound bearing an aldehyde or a methylketon function, b) said function is modified using the Witting reaction or the aldol condensation, c) the heterocyclic ring is closed using a compound comprising two nucleophiles, wherein at least one of the said nucleophiles is NH2.
摘要翻译：在这里，我们报告了关于固相反应序列的研究，适用于在小杂环上产生分子多样性。对于每个反应，制备了固相上的合适条件，并利用各种反应剂（构件）来努力掌握系统的适用范围。本发明的反应序列可以应用于例如通过分组和混合概念的组合方法的利用。反应顺序包括以下步骤：a）具有反应性表面基团的固体载体直接或通过间隔基团与具有醛或甲基酮官能团的化合物一起加载，b）使用Witting反应或醛醇缩合 c）使用包含两个亲核试剂的化合物封闭杂环，其中所述亲核试剂中的至少一个是NH 2。

2. 发明申请

WO2002062804A1 OXAZOLYL-PYRAZOLE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：氧化吡唑衍生物作为激酶抑制剂
公开(公告)号：WO2002062804A1
公开(公告)日：2002-08-15
申请号：PCT/EP2002/000995
申请日：2002-01-28
申请人： PHARMACIA ITALIA S.P.A. , BERTA, Daniela , FELDER, Eduard , VULPETTI, Anna , VILLA, Marzia
发明人： BERTA, Daniela , FELDER, Eduard , VULPETTI, Anna , VILLA, Marzia
IPC分类号： C07D498/04
CPC分类号： C07D413/04 , A61K31/4155 , A61K31/437 , C07D413/14
摘要： Compounds which are oxazolyl-pyrazole derivatives, as defined in the specification, and pharmaceutically acceptable salts thereof; are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.
摘要翻译：化合物，如说明书中所定义的恶唑基 - 吡唑衍生物及其药学上可接受的盐; 可用于治疗由改变的蛋白激酶活性如癌症，细胞增殖性病症，病毒感染，自身免疫性疾病和神经变性疾病引起的和/或与其相关的疾病。

3. 发明申请

WO1996040759A1 ANTIVIRAL PEPTOID COMPOUNDS 审中-公开
标题翻译：抗生素PEPTOID化合物
公开(公告)号：WO1996040759A1
公开(公告)日：1996-12-19
申请号：PCT/EP1996002424
申请日：1996-06-04
申请人： CIBA-GEIGY AG , FELDER, Eduard , HAMY, François , HEIZMANN, Gerhard , KLIMKAIT, Thomas , LAZDINS, Janis, Karlis
发明人： CIBA-GEIGY AG
IPC分类号： C07K14/00
CPC分类号： C07K14/005 , A61K38/00 , C07K14/001 , C12N2740/16322
摘要： Described are peptoid compounds of the formula (I): R1-(A)k-(X)m-(B)n-R2 wherein k, n, R1, R2, A and B have the meanings given in the specification, m is 3 to 10, and any X independently of the others being present represents a bivalent radical of partial formula (II), wherein each of R3, R4 and R5, independently of the others, represents hydrogen or a side chain of an alpha -amino acid other than glycine, or R3 and R4 together form an alkylene bridge and R5 is hydrogen, or R4 and R5 together form an alkylene bridge and R3 is hydrogen; with the proviso, that a) at least one of these bivalent radicals has an R3 which is a side chain of an alpha -amino acid other than glycine and proline; b) that at least one R3 other than alkyl or benzyl is present; and c) that the bivalent radicals X together form a TAR-binding, transactivation-deficient oligopeptide analogue of the basic domain of the HIV Tat protein, and any B independently of the others being present represents a bivalent radical of an alpha -amino acid, or salts thereof if a salt-forming group is present. The compounds act, for example, as inhibitors of HIV growth by inhibition of the Tat/TAR-interaction.
摘要翻译：描述了式（I）的拟肽化合物：R1-（A）k-（X）m-（B）n-R2其中k，n，R1，R2，A和B具有说明书中给出的含义，m 是3至10，并且存在的其它任何X独立地表示部分式（II）的二价基团，其中R 3，R 4和R 5各自独立地表示氢或α-氨基的侧链除了甘氨酸以外，还有R3和R4一起形成亚烷基桥，R5是氢，R4和R5一起形成亚烷基桥，R3是氢; 条件是a）这些二价基团中的至少一个具有R3，其是除了甘氨酸和脯氨酸之外的α-氨基酸的侧链; b）存在至少一种不同于烷基或苄基的R 3; 和c）二价基团X一起形成HIV Tat蛋白质的碱性结构域的TAR结合，反式激活缺陷的寡肽类似物，并且与存在的其它B独立的任何B代表α-氨基酸的二价基团，或其盐，如果存在成盐基团。该化合物例如通过抑制Tat / TAR-相互作用而作为HIV生长抑制剂。

4. 发明申请

WO1997019039A1 SOLID PHASE SYNTHESIS OF HETEROCYCLIC COMPOUNDS AND COMBINATORIAL COMPOUND LIBRARY 审中-公开
标题翻译：杂环化合物和组合化合物库的固相合成
公开(公告)号：WO1997019039A1
公开(公告)日：1997-05-29
申请号：PCT/EP1996004808
申请日：1996-11-05
申请人： NOVARTIS AG , MARZINZIK, Andreas , FELDER, Eduard
发明人： NOVARTIS AG
IPC分类号： C07B61/00
CPC分类号： C07D231/12 , C07D261/08 , C07D403/04 , C40B40/04 , C40B50/14
摘要： Here we report a study on a reaction sequence on solid phase, suitable for the generation of molecular diversity on small heterocycles of the pyrazole and isoxazole type. For each reaction, suitable conditions on solid phase were worked out and a variety of reactive agents (building blocks) was utilized in an effort to grasp the system's breadth of applicability. The inventive reaction sequence can be applied, for example, to exploit by the combinatorial approaches of the split and mix concept.
摘要翻译：在这里，我们报告了关于固相反应序列的研究，适用于在吡唑和异恶唑类的小杂环上产生分子多样性。对于每个反应，制备了固相上的合适条件，并利用各种反应剂（构件）来努力掌握系统的适用范围。本发明的反应序列可以应用于例如通过分组和混合概念的组合方法的利用。

5. 发明申请

WO1996030392A1 PROCESS FOR THE PRODUCTION OF COMBINATORIAL COMPOUND LIBRARIES 审中-公开
标题翻译：生产组合复合图书馆的过程
公开(公告)号：WO1996030392A1
公开(公告)日：1996-10-03
申请号：PCT/EP1996001154
申请日：1996-03-18
申请人： CIBA-GEIGY AG , RINK, Hans , VETTER, Dirk , GERCKEN, Bertold , FELDER, Eduard
发明人： CIBA-GEIGY AG
IPC分类号： C07K01/04
CPC分类号： C07K1/047 , A61K38/00 , B01J2219/005 , B01J2219/00572 , B01J2219/00596 , B01J2219/00725 , C40B40/10 , C40B70/00
摘要： Described is a process for the production of a library from a plurality of different units consisting of a solid or semisolid carrier (bead), a synthetic ligand and a binary information structure (tag), by means of which the building blocks of the ligand are coded, and the use of that library for searching for novel classes of active ingredient and individual active ingredients. Also described are compounds found using that process. The process is characterized by the use of element atoms or ions as binary tags which are bound non covalently to the beads. Their unique combination which can be measured by e.g. mass spectrometry codes for the specific ligand.
摘要翻译：描述了从由固体或半固体载体（珠粒），合成配体和二元信息结构（标签）组成的多个不同单元生产文库的方法，通过该文库，配体的结构单元编码，以及使用该库搜索新类别的活性成分和各种活性成分。还描述了使用该方法发现的化合物。该方法的特征在于使用元素原子或离子作为与珠不共价结合的二进制标记。它们独特的组合可以通过例如用于特定配体的质谱法编码。

6. 发明申请

WO2003051358A1 HYDROXYPHENYL-PYRAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
标题翻译：作为激酶抑制剂活性的羟基苯基 - 吡唑衍生物，其制备方法和包含它们的药物组合物
公开(公告)号：WO2003051358A1
公开(公告)日：2003-06-26
申请号：PCT/EP2002/014087
申请日：2002-12-11
申请人： PHARMACIA ITALIA SPA , CASUSCELLI, Francesco , D'ALESSIO, Roberto , FELDER, Eduard , VULPETTI, Anna
发明人： CASUSCELLI, Francesco , D'ALESSIO, Roberto , FELDER, Eduard , VULPETTI, Anna
IPC分类号： A61K31/415
CPC分类号： C07D231/12 , C07D401/04
摘要： The present invention provides a method for treating diseases caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof and effective amount of o-hydroxy phenyl-pyrazol-3-yl derivatives optionally substituted of formula (I). The invention also provides some new compounds, a library comprising at least two of them, a process for their preparation and the pharmaceutical compositions containing them, which are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.
摘要翻译：本发明提供了治疗由变化的蛋白激酶活性引起和/或与其相关的疾病的方法，该方法包括向有需要的哺乳动物施用有效量的任选取代于式（Ⅱ）的邻羟基苯基 - 吡唑-3-基衍生物一世）。本发明还提供了一些新的化合物，其中包含至少两个它们的文库，它们的制备方法和含有它们的药物组合物，其可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如作为癌症，细胞增殖性病症，病毒感染，自身免疫疾病和神经变性疾病。

7. 发明申请

WO1995016209A1 PROCESS FOR THE PRODUCTION OF COMBINATORIAL COMPOUND LIBRARIES 审中-公开
标题翻译：生产组合复合图书馆的过程
公开(公告)号：WO1995016209A1
公开(公告)日：1995-06-15
申请号：PCT/EP1994003936
申请日：1994-11-28
申请人： CIBA-GEIGY AG , FELDER, Eduard , RINK, Hans , MATTHEWS, Ian, Timothy, William
发明人： CIBA-GEIGY AG
IPC分类号： G01N33/68
CPC分类号： C40B30/04 , B01J2219/005 , B01J2219/00572 , C07K1/047 , C07K5/0205 , C12Q1/6811 , C40B70/00 , G01N33/6845
摘要： The present invention relates to a process for the preparation of a plurality of different units consisting of a solid or semisolid carrier (bead), a synthetic oligomer (ligand) and an identification structure (tag) by means of which the monomers of the ligands are coded, and the use of said library for searching for novel classes of compounds and individual compounds. The invention further relates to compounds found with the novel process and the use thereof as thrombin inhibitors.
摘要翻译：本发明涉及一种制备由固体或半固体载体（珠粒），合成低聚物（配体）和识别结构（标签）构成的多个不同单元的方法，借助于此，配体的单体为并且使用所述文库来搜索新类别的化合物和单个化合物。本发明还涉及通过新方法发现的化合物及其作为凝血酶抑制剂的用途。

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