公开(公告)号：US20080167308A1

公开(公告)日：2008-07-10

申请号：US11932945

申请日：2007-10-31

申请人： Valentina Molteni ,  Xiaolin Li ,  Donatella Chianelli ,  Juliet Nabakka ,  Jon Loren ,  Xiaodong Liu ,  Shifeng Pan ,  Yi Liu ,  Donald S. Karanewsky ,  Pascal Furet ,  Vito Guagnano ,  Shuli You

发明人： Valentina Molteni ,  Xiaolin Li ,  Donatella Chianelli ,  Juliet Nabakka ,  Jon Loren ,  Xiaodong Liu ,  Shifeng Pan ,  Yi Liu ,  Donald S. Karanewsky ,  Pascal Furet ,  Vito Guagnano ,  Shuli You

IPC分类号： A61K31/5377 ,  C07D239/42 ,  A61K31/505 ,  A61K31/506 ,  C12N9/12 ,  C07D403/12 ,  C07D413/12

CPC分类号： C07D403/04 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D491/10

摘要： Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.

公开(公告)号：US20080096868A1

公开(公告)日：2008-04-24

申请号：US11718730

申请日：2005-11-10

申请人： Niko Schmiedeberg ,  Pascal Furet ,  Patricia Imbach ,  Philipp Holzer

发明人： Niko Schmiedeberg ,  Pascal Furet ,  Patricia Imbach ,  Philipp Holzer

IPC分类号： A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  A61P35/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The invention relates to 1,4-substituted pyrazolopyrimidine compounds of the formula I, pharmaceuticals comprising a 1,4-substituted pyrazolopyrimidine compound, the use of a 1,4-substituted pyrazolopyrimidine compound in the treatment or the use thereof in the manufacture of a pharmaceutical formulation for the treatment of a disease that depends on inadequate activity of a protein kinase, methods of treatment comprising administering a 1,4-substituted pyrazolopyrimidine compound, methods for the manufacture of a novel compound of that class, and novel intermediates and partial steps for their synthesis.

摘要翻译： 本发明涉及式I的1,4-取代吡唑并嘧啶化合物，包含1,4-取代的吡唑并嘧啶化合物的药物，1,4-取代的吡唑并嘧啶化合物在其制备中的用途和用途 用于治疗依赖于蛋白激酶活性不足的疾病的药物制剂，包括施用1,4-取代的吡唑并嘧啶化合物的方法，制备该类新化合物的方法，以及新的中间体和部分步骤 为他们的合成。

公开(公告)号：US20070213355A1

公开(公告)日：2007-09-13

申请号：US10579876

申请日：2004-11-19

申请人： Hans-Georg Capraro ,  Pascal Furet ,  Carlos Garcia-Cheverria ,  Frederic Stauffer

发明人： Hans-Georg Capraro ,  Pascal Furet ,  Carlos Garcia-Cheverria ,  Frederic Stauffer

IPC分类号： A61K31/437 ,  C07D471/04

CPC分类号： C07D471/04 ,  A61K31/41

摘要： The invention relates to the use of imidazoquinolines and salts thereof in the treatment of protein kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, imidazoquinolines for use in the treatment of protein kinase dependent diseases, a method of treatment against said diseases, comprising administering the imidazoquinolines to a warm-blooded animal, especially a human, 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： 本发明涉及咪唑并喹啉及其盐在治疗蛋白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，用于治疗蛋白激酶依赖性疾病的咪唑并喹啉， 所述疾病包括向包含咪唑并喹啉的温血动物，特别是用于治疗蛋白激酶依赖性疾病的新型咪唑并喹啉的温血动物，特别是人的药物制剂，以及制备新的咪唑并喹啉的方法施用咪唑并喹啉。

公开(公告)号：US20070093506A1

公开(公告)日：2007-04-26

申请号：US11607542

申请日：2006-12-01

申请人： Werner Breitenstein ,  Pascal Furet ,  Sandra Jacob ,  Paul Manley

发明人： Werner Breitenstein ,  Pascal Furet ,  Sandra Jacob ,  Paul Manley

IPC分类号： A61K31/506 ,  C07D403/14

CPC分类号： C07D401/14 ,  C07D405/14

摘要： The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.

公开(公告)号：US07189729B2

公开(公告)日：2007-03-13

申请号：US10956412

申请日：2004-09-30

申请人： Greg Chopiuk ,  Pascal Furet ,  Nathanael Schiander Gray ,  Patricia Imbach ,  Yi Liu ,  Joseph Schoepfer ,  Ruo Steensma

发明人： Greg Chopiuk ,  Pascal Furet ,  Nathanael Schiander Gray ,  Patricia Imbach ,  Yi Liu ,  Joseph Schoepfer ,  Ruo Steensma

IPC分类号： C07D239/42 ,  C07D403/12 ,  A61K31/506 ,  A61P19/02 ,  A61P35/00

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。

公开(公告)号：US07169791B2

公开(公告)日：2007-01-30

申请号：US10520359

申请日：2003-07-04

申请人： Werner Breitenstein ,  Pascal Furet ,  Sandra Jacob ,  Paul William Manley

发明人： Werner Breitenstein ,  Pascal Furet ,  Sandra Jacob ,  Paul William Manley

IPC分类号： C07D401/14 ,  A06K31/506 ,  C07D213/38

CPC分类号： C07D401/14 ,  C07D405/14

摘要： The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.

摘要翻译： 本发明涉及下式的化合物，其中取代基R 1，R 2和R 4具有本发明说明书中阐述和解释的含义，制备这些化合物的方法，含有它们的药物组合物，其任选组合的用途 与一种或多种用于治疗对蛋白激酶活性，特别是肿瘤性疾病，特别是白血病的抑制作出反应的疾病的其它药学活性化合物，以及治疗这种疾病的方法。

公开(公告)号：US07091224B2

公开(公告)日：2006-08-15

申请号：US10494591

申请日：2002-11-07

申请人： Guido Bold ,  Pascal Furet ,  Paul W Manley

发明人： Guido Bold ,  Pascal Furet ,  Paul W Manley

IPC分类号： A61K31/44 ,  C07D211/72

CPC分类号： C07D213/64 ,  C07D213/70

摘要： The invention relates to anthranilic acid amide derivatives of formula (I), wherein R1 represents H or lower alkyl, R2 represents H or lower alkyl, R3 represents perfluoro lower alkyl, and X is O or S, or an N-oxide or a tautomer thereof, to salts of such anthranilic acid amides, their N-oxides and their tautomers; processes for the preparation thereof, the application thereof for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age—related macular degeneration; a method for the treatment of such a disease in animals, especially in humans, and the use of such a compound—alone or in combination with one or more other pharmaceutically active compounds—for the manufacture of a pharmaceutical preparation for the treatment of a neoplastic disease, of retinopathy or age-related macular degeneration.

摘要翻译： 本发明涉及式（I）的邻氨基苯甲酰胺衍生物，其中R 1代表H或低级烷基，R 2代表H或低级烷基，R 3 表示全氟低级烷基，X是O或S，或其N-氧化物或互变异构体，与邻氨基苯甲酸酰胺的盐，它们的N-氧化物及其互变异构体; 其制备方法，其用于治疗人或动物体的应用，其单独使用或与一种或多种其它药学活性化合物组合用于特别是肿瘤性疾病如肿瘤疾病的治疗 ，视网膜病变或年龄相关性黄斑变性; 用于治疗动物，特别是人类中的这种疾病的方法，以及使用这样的化合物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗肿瘤的药物制剂 视网膜病变或年龄相关性黄斑变性疾病。

公开(公告)号：US20060074112A1

公开(公告)日：2006-04-06

申请号：US11254897

申请日：2005-10-20

申请人： Karl-Heinz Altmann ,  Guido Bold ,  Pascal Furet ,  Paul Manley ,  Jeanette Wood ,  Stefano Ferrari ,  Francesco Hofmann ,  Jurgen Mestan ,  Andreas Huth ,  Martin Kruger ,  Dieter Seidelmann ,  Andreas Menrad ,  Martin Haberey ,  Karl-Heinz Thierauch

发明人： Karl-Heinz Altmann ,  Guido Bold ,  Pascal Furet ,  Paul Manley ,  Jeanette Wood ,  Stefano Ferrari ,  Francesco Hofmann ,  Jurgen Mestan ,  Andreas Huth ,  Martin Kruger ,  Dieter Seidelmann ,  Andreas Menrad ,  Martin Haberey ,  Karl-Heinz Thierauch

IPC分类号： C07D213/56 ,  A61K31/44 ,  C07D233/54

CPC分类号： A61K31/415 ,  A61K31/44 ,  A61K31/47 ,  C07D213/38 ,  C07D213/56 ,  C07D213/64 ,  C07D213/89 ,  C07D215/12 ,  C07D233/54 ,  C07D405/12

摘要： Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y═SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each, other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.

摘要翻译： 描述的是式（I）的化合物，其中W是O或S; X是NR 8; Y是CR 9 R 10其中R 9是（CH 2）n - 和R 10彼此独立地为氢或低级烷基，n为0〜3的整数。 或Y为SO 2; R 1是芳基; R 2是包含一个或多个环氮原子的单环或双环杂芳基，除了R 2不能表示2-邻苯二甲酰亚氨基，并且在Y-SO的情况下 2不能表示2,1,3-苯并噻二唑-4-基; R 3，R 4，R 5和R 6中的任何一个独立地是H或 除氢以外的取代基; R 7和R 8分别独立地为H或低级烷基; 或N-氧化物或其药学上可接受的盐在制备用于治疗对VEGF受体酪氨酸激酶活性的抑制作出反应的肿瘤疾病的药物产品中的用途。 式（I）化合物可用于治疗，例如， 的肿瘤疾病，如肿瘤疾病，视网膜病变和年龄相关性黄斑变性。

公开(公告)号：US20050239716A1

公开(公告)日：2005-10-27

申请号：US11172146

申请日：2005-06-30

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 ,  C07F5/02 ,  A61K38/04

CPC分类号： C07K5/06191 ,  A61K38/00

摘要： The present invention relates to compounds of formula I wherein the substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical preparations comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.

摘要翻译： 本发明涉及式I化合物，其中取代基如说明书中所定义，其制备方法，包含那些化合物的药物制剂及其在制备用于治疗温热的药物组合物中的用途 动物，包括人类。

公开(公告)号：US5981533A

公开(公告)日：1999-11-09

申请号：US930904

申请日：1997-10-03

申请人： Peter Traxler ,  Pascal Furet ,  Guido Bold ,  Jorg Frei ,  Marc Lang

发明人： Peter Traxler ,  Pascal Furet ,  Guido Bold ,  Jorg Frei ,  Marc Lang

IPC分类号： C07D231/38 ,  A61K31/505 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： 4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula I ##STR1## wherein the symbols are as defined in claim 1, and intermediates for their manufacture are described.The compounds of formula I inhibit especially the tyrosine kinase activity of the receptor for epidermal growth factor and can be used, for example, in the case of epidermal hyperproliferation (psoriasis) and as anti-tumor agents.

摘要翻译： PCT No.PCT / EP96 / 01263。 371日期1997年10月3日第 102（e）日期1997年10月3日PCT 1996年3月22日PCT公布。 公开号WO96 / 31510PC。 日期：19964年10月10日 - 描述了式I的氨基-1H-吡唑并[3,4-d]嘧啶衍生物，其中符号如权利要求1中所定义，其中描述其制备方法。 式I的化合物特别地抑制表皮生长因子受体的酪氨酸激酶活性，并且可以用于例如表皮过度增生（牛皮癣）和作为抗肿瘤剂的情况。