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21. 发明授权

US07091346B1 Purine derivatives and processes for their preparation 失效
标题翻译：嘌呤衍生物及其制备方法
公开(公告)号：US07091346B1
公开(公告)日：2006-08-15
申请号：US09051827
申请日：1996-10-22
申请人： Jürg Zimmermann , Hans-Georg Capraro , Patricia Imbach , Pascal Furet
发明人： Jürg Zimmermann , Hans-Georg Capraro , Patricia Imbach , Pascal Furet
IPC分类号： C07D473/40 , C07D473/16 , A61K31/52 , A61P35/00 , A61P17/06
CPC分类号： C07D473/16
摘要： 2-Amino-6-anilino-purine derivatives of the formula 1 in which the symbols are as defined in claim 1 are described. These compounds inhibit p34cdc2/cyclin Bcdc13 kinase and can be used for treatment of hyperproliferative diseases, for example tumour diseases.
摘要翻译：描述了其中符号如权利要求1中所定义的式1的2-氨基-6-苯胺基 - 嘌呤衍生物。这些化合物抑制p34cd2细胞周期蛋白Bclc13激酶，并可用于治疗过度增殖性疾病，例如肿瘤疾病。

22. 发明申请

US20050222171A1 Organic compounds 审中-公开
标题翻译：有机化合物
公开(公告)号：US20050222171A1
公开(公告)日：2005-10-06
申请号：US11039445
申请日：2005-01-20
申请人： Guido Bold , Andreas Floersheimer , Pascal Furet , Patricia Imbach , Keiichi Masuya , Joseph Schoepfer
发明人： Guido Bold , Andreas Floersheimer , Pascal Furet , Patricia Imbach , Keiichi Masuya , Joseph Schoepfer
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to the use of pyrazolo[1,5a]pyrimidin-7-yl amine compounds and salts thereof in the treatment of kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds, and a process for the preparation of the novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds.
摘要翻译：本发明涉及吡唑并[1,5a]嘧啶-7-基胺化合物及其盐在治疗激酶依赖性疾病中的用途以及用于制备用于治疗所述疾病的药物制剂，新颖的吡唑并[1,5a ]嘧啶-7-基胺化合物，以及制备新的吡唑并[1,5a]嘧啶-7-基胺化合物的方法。

23. 发明授权

US06933290B2 2-{N-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl}-amino}-alkylboronic acid derivatives 失效
标题翻译： 2- {N-（2-氨基-3-（杂芳基或芳基）丙酰基） - 氨基酰基} - 氨基} - 烷基硼酸衍生物
公开(公告)号：US06933290B2
公开(公告)日：2005-08-23
申请号：US10478794
申请日：2002-05-29
申请人： Pascal Furet , Vito Guagnano , Patricia Imbach , Marc Lang
发明人： Pascal Furet , Vito Guagnano , Patricia Imbach , Marc Lang
IPC分类号： A61K38/00 , A61P35/00 , A61P43/00 , C07K5/06 , A61K31/69 , A61K38/05 , C07K5/08
CPC分类号： C07K5/06191 , A61K38/00
摘要： Disclosed are derivatives of 2-{[N-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl]-amino}-alkylboronic acid, processes for the preparation of such compounds, pharmaceutical preparations, and the use of such derivatives in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans
摘要翻译：公开了2 - {[N-（2-氨基-3-（杂芳基或芳基）丙酰基） - 氨基酰基] - 氨基} - 烷基硼酸的衍生物，这些化合物的制备方法，药物制剂及其用途制备用于治疗温血动物（包括人）的药物组合物的衍生物

24. 发明申请

US20050171105A1 Methods and compositions as protein kinase inhibitors 有权
标题翻译：方法和组合物作为蛋白激酶抑制剂
公开(公告)号：US20050171105A1
公开(公告)日：2005-08-04
申请号：US10956412
申请日：2004-09-30
申请人： Greg Chopiuk , Pascal Furet , Nathanael Gray , Patricia Imbach , Yi Liu , Joseph Schoepfer , Ruo Steensma
发明人： Greg Chopiuk , Pascal Furet , Nathanael Gray , Patricia Imbach , Yi Liu , Joseph Schoepfer , Ruo Steensma
IPC分类号： A61K31/53 , A61P35/00 , C07D239/26 , C07D239/42 , C07D403/12 , C07D43/02
CPC分类号： C07D239/26 , A61K31/5377 , C07D239/42 , C07D403/12
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, EGF-R, c-erbB2 kinase (HER-2), CHK2, FGFR3, p70S6K, PKC, PDGF-R, p38, TGFβ, KDR, c-Kit, b-RAF, c-RAF, FLT1 and/or FLT4 kinases.
摘要翻译：本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Abl，BCR-Abl异常活化的疾病或病症，EGF-R，c-erbB2激酶（HER-2），CHK2，FGFR3，p70S6K，PKC，PDGF-R，p38，TGFbeta，KDR，c-Kit，b-RAF，c-RAF，FLT1和/或FLT4 激酶。

25. 发明申请

US20100305113A1 Substituted Imidazopyridazines as Lipid Kinase Inhibitors 审中-公开
标题翻译：取代的咪唑并哒嗪作为脂质激酶抑制剂
公开(公告)号：US20100305113A1
公开(公告)日：2010-12-02
申请号：US12599131
申请日：2008-05-07
申请人： Hans-Georg Capraro , Patricia Imbach , Giorgio Caravatti , Pascal Furet
发明人： Hans-Georg Capraro , Patricia Imbach , Giorgio Caravatti , Pascal Furet
IPC分类号： A61K31/542 , C07D487/04 , A61K31/5025 , A61K31/5377 , A61P35/00 , A61P29/00 , A61P37/08 , A61P9/00
CPC分类号： C07D487/04
摘要： The invention relates to novel compounds of the formula I, as well as other invention embodiments related to these compounds. The compounds are e.g. useful in the treatment of the animal or human body in view of their ability to inhibit protein kinases such as especially PI3 kinase.
摘要翻译：本发明涉及式I的新化合物以及与这些化合物有关的其它发明实施方案。化合物是例如鉴于其抑制蛋白激酶（例如PI3激酶）的能力，可用于动物或人体的治疗。

26. 发明授权

US07691855B2 Phenyl-[4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yl)-amine derivatives 失效
标题翻译：苯基 - [4-（3-苯基-1H-吡唑-4-基） - 嘧啶-2-基） - 胺衍生物
公开(公告)号：US07691855B2
公开(公告)日：2010-04-06
申请号：US10520567
申请日：2003-07-08
申请人： Pascal Furet , Patricia Imbach , Timothy Michael Ramsey , Achim Schlapbach , Dieter Scholz , Giorgio Caravatti
发明人： Pascal Furet , Patricia Imbach , Timothy Michael Ramsey , Achim Schlapbach , Dieter Scholz , Giorgio Caravatti
IPC分类号： C07D403/04 , A61K31/505
CPC分类号： C07D403/04 , A61K31/505
摘要： The invention relates to phenyl-[4-(3-phenyl-1H-pyrazol-4-yl)-pyrimidin-2-yl]-amine derivatives and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives—alone or in combination with one or more other pharmaceutically active compounds—for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumor.
摘要翻译：本发明涉及苯基 - [4-（3-苯基-1H-吡唑-4-基） - 嘧啶-2-基] - 胺衍生物及其制备方法，涉及包含这些衍生物的药物组合物及其用途的这样的衍生物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗特别是增殖性疾病例如肿瘤的药物组合物。

27. 发明申请

US20080300245A1 Pyrazolo[1,5-A]Pyridine-3-Carboxylic Acids as Ephb and Vegfr2 Kinase Inhibitors 失效
标题翻译：吡唑并[1,5-A]吡啶-3-羧酸为Ephb和Vegfr2激酶抑制剂
公开(公告)号：US20080300245A1
公开(公告)日：2008-12-04
申请号：US12096260
申请日：2006-12-06
申请人： Patricia Imbach , Philipp Holzer , Pascal Furet
发明人： Patricia Imbach , Philipp Holzer , Pascal Furet
IPC分类号： A61K31/437 , C07D471/04 , A61K31/5377 , A61P35/00 , A61K31/496
CPC分类号： C07D471/04
摘要： The invention relates to novel pyrazolo[1,5a]pyridine-3-carboxylic acid compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及下式的新型吡唑并[1,5a]吡啶-3-羧酸化合物，其中所有变量如本说明书中所定义，以游离形式或盐形式，其制备方法与其作为药物及其组成的药物。

28. 发明申请

US20080262021A1 1H-Imidazoquinoline Derivatives as Prote In Kinase Inhibitors 审中-公开
标题翻译： 1H-咪唑并喹啉衍生物作为激酶抑制剂中的蛋白质
公开(公告)号：US20080262021A1
公开(公告)日：2008-10-23
申请号：US10579587
申请日：2004-11-19
申请人： Hans-Georg Capraro , Giorgio Caravatti , Pascal Furet , Carlos Garcia-Echeverria , Patricia Imbach , Frederic Stauffer
发明人： Hans-Georg Capraro , Giorgio Caravatti , Pascal Furet , Carlos Garcia-Echeverria , Patricia Imbach , Frederic Stauffer
IPC分类号： A61K31/4745 , C07D471/04 , A61P35/04
CPC分类号： C07D471/04
摘要： The invention relates to imidazoquinolines of formula (I) for use in the treatment of protein kinase dependent diseases; pharmaceutical preparations comprising an imidazoquinoline, especially for the treatment of a protein kinase dependent disease; novel imidazoquinolines; and a process for the preparation of the novel imidazoquinolines.
摘要翻译：本发明涉及用于治疗蛋白激酶依赖性疾病的式（I）的咪唑并喹啉; 包含咪唑并喹啉的药物制剂，特别是用于治疗蛋白激酶依赖性疾病; 新型咪唑并喹啉; 以及制备新的咪唑并喹啉的方法。

29. 发明申请

US20050026994A1 Use of 2, 4diamino-3-hydroxycarboxylic acid derivatives as proteasome inhibitors 审中-公开
标题翻译：使用2,4-二氨基-3-羟基羧酸衍生物作为蛋白酶体抑制剂
公开(公告)号：US20050026994A1
公开(公告)日：2005-02-03
申请号：US10035301
申请日：2001-10-25
申请人： Dennis France , Peter Furst , Johann Zimmermann , Carlos Garcia-Echeverria , Dieter Scholz , Pascal Furet , Patricia Imbach
发明人： Dennis France , Peter Furst , Johann Zimmermann , Carlos Garcia-Echeverria , Dieter Scholz , Pascal Furet , Patricia Imbach
IPC分类号： A61K38/00 , A61P17/06 , A61P35/00 , A61P43/00 , C07C237/12 , C07C271/22 , C07K5/00 , A61K31/381 , A61K31/165
CPC分类号： C07C271/22 , Y02P20/55
摘要： The present invention relates to the new use of 2,4-diamino-3-hydroxycarboxylic acids of formula (I), in which A and B independently represent a bond or an unsubstituted or substituted amino acyl moiety; R1 represents hydrogen; an amino protecting group; or a group of formula R5Y— wherein R5 represents hydrogen or an unsubstituted or substituted alkyl, alkenyl, alkinyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl group; and Y represents —CO—; —NH—CO—; —NH—CS—; —SO2—; —O—CO—; or —O—CS—; R2 represents the side chain of a natural amino acid; an alkyl, arylalkyl, heteroarylalkyl or cycloalkylalkyl group; or trimethylsilylmethyl, 2-thienylmethyl or styrylmethyl; R3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; and R4 represents 2(R)-hydroxyindan-1(S)-yl; (S)-2-hydroxy-1-phenylethyl; or 2-hydroxy-benzyl unsubstituted or substituted in 4-position by methoxy; in the manufacture of a pharmaceutical composition for the treatment of a proliferative disease, e.g., of a solid tumor; to a method of treatment of warm-blooded animals; and to 2,4-diamino-3-hydroxycarboxylic acids of formula (I*), wherein A and B independently represent an unsubstituted or substituted amino acyl moiety; R2 represents arylalkyl; R3 represents halogen, alkyl, alkoxy or hydroxyalkoxy; R4 represents 2-hydroxy-benzyl unsubstituted or substituted in 4 position by methoxy; and R5 represents arylalkyl and Y represents —CO—; or R5 represents alkyl substituted by cycloalkyl, naphthyl, pyridyl or phenyl in which phenyl is substituted by alkyl or amino; and Y represents —O—CO; pharmaceutically acceptable salts thereof; and the use of such compounds of formula (I*) for the therapeutic treatment of the human or animal body, especially the treatment of proliferative diseases.
摘要翻译：本发明涉及式（I）的2,4-二氨基-3-羟基羧酸的新用途，其中A和B独立地表示键或未取代或取代的氨基酰基部分; R1表示氢; 氨基保护基; 烯基，炔基，芳基，芳基烷基，杂芳基，杂芳基烷基，杂环基或杂环基烷基;或其中R 5表示氢或未取代或取代的烷基，烯基，炔基，芳基， Y表示-CO-; -NH-CO-; -NH-CS-; -SO2-; -O-CO-; 或-O-CS-; R2表示天然氨基酸的侧链; 烷基，芳基烷基，杂芳基烷基或环烷基烷基; 或三甲基甲硅烷基甲基，2-噻吩基甲基或苯乙烯基甲基; R3表示卤素，烷基，烷氧基或羟基烷氧基; 并且R 4表示2（R） - 羟基茚满-1（S） - 基; （S）-2-羟基-1-苯基乙基; 或2-羟基苄基未被取代或在4-位上被甲氧基取代; 在制备用于治疗增殖性疾病例如实体瘤的药物组合物中; 涉及一种治疗温血动物的方法; 和式（I *）的2,4-二氨基-3-羟基羧酸，其中A和B独立地表示未取代或取代的氨基酰基部分; R2代表芳基烷基; R3表示卤素，烷基，烷氧基或羟基烷氧基; R4代表未取代的或在4位被甲氧基取代的2-羟基 - 苄基; R5表示芳基烷基，Y表示-CO-; 或R 5表示被环烷基，萘基，吡啶基或苯基取代的烷基，其中苯基被烷基或氨基取代; Y表示-O-CO; 其药学上可接受的盐; 以及使用这些式（I *）化合物来治疗人或动物体，特别是治疗增殖性疾病。

30. 发明授权

US08940771B2 Organic compounds 有权
标题翻译：有机化合物
公开(公告)号：US08940771B2
公开(公告)日：2015-01-27
申请号：US12338432
申请日：2008-12-18
申请人： Giorgio Caravatti , Robin Alec Fairhurst , Pascal Furet , Vito Guagnano , Patricia Imbach
发明人： Giorgio Caravatti , Robin Alec Fairhurst , Pascal Furet , Vito Guagnano , Patricia Imbach
IPC分类号： A61K31/4439 , A61K31/427 , C07D417/14 , C07D417/12
CPC分类号： C07D417/14 , A61K31/427 , A61K31/4439 , C07D417/12
摘要： The present invention relates to compounds of formula I and its salts, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
摘要翻译：本发明涉及式I化合物及其盐，其中取代基如说明书中所定义，化合物在治疗通过抑制磷脂酰肌醇3-激酶而变性的疾病中的组合物和用途。

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