公开(公告)号：US06686347B2

公开(公告)日：2004-02-03

申请号：US09964025

申请日：2001-09-26

申请人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

发明人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

IPC分类号： A61K3133

CPC分类号： C07D401/06 ,  A61K31/501 ,  A61K31/502 ,  C07D401/14

摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof; the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.

摘要翻译： 本发明涉及治疗炎症性疾病，特别是炎性类风湿病或风湿性疾病，和/或具有式I的VEGF受体酪氨酸激酶的活性抑制剂的疼痛，所述取代基在本说明书中定义;以及 新的酞嗪衍生物; 制备方法; 其用于治疗人或动物体的过程中的应用; 其用于治疗疾病，特别是由眼睛新生血管形成引起的疾病，例如年龄相关性黄斑变性或糖尿病性视网膜病，或其它对酪氨酸激酶（例如增殖性疾病）的抑制作用的疾病; 哺乳动物治疗这种疾病的方法; 以及这种化合物用于制造特别是上述疾病的药物制剂的用途。

公开(公告)号：US06911440B2

公开(公告)日：2005-06-28

申请号：US10723238

申请日：2003-11-26

申请人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

发明人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

IPC分类号： A61K31/502 ,  A61K31/506 ,  A61P1/16 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/12 ,  A61P17/06 ,  A61P19/02 ,  A61P25/04 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  A61K31/33 ,  A61K31/44 ,  C07D237/00 ,  C07D401/00 ,  C07D487/00

CPC分类号： C07D401/06 ,  A61K31/501 ,  A61K31/502 ,  C07D401/14

摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.

摘要翻译： 本发明涉及治疗炎症性疾病，特别是炎性类风湿病或风湿性疾病，和/或具有式I的VEGF受体酪氨酸激酶的活性抑制剂的疼痛，该说明书中定义的取代基; 以及新的酞嗪衍生物; 其制备方法，其用于治疗人或动物体的方法中的应用; 其用于治疗疾病，特别是由眼睛新生血管形成引起的疾病，例如年龄相关性黄斑变性或糖尿病性视网膜病，或其它对酪氨酸激酶（例如增殖性疾病）的抑制作用的疾病的用途; 哺乳动物治疗这种疾病的方法; 以及这种化合物用于制造特别是上述疾病的药物制剂的用途。

公开(公告)号：US20100144835A1

公开(公告)日：2010-06-10

申请号：US12518709

申请日：2007-12-13

申请人： Klaus Seuwen ,  Eric Billy ,  Thomas Suply ,  Lorenza Wyder ,  Janet Dawson King ,  Marie-Gabrielle Ludwig ,  Matthias Mueller ,  Puneeta Nath ,  Carol Elizabeth Jones

发明人： Klaus Seuwen ,  Eric Billy ,  Thomas Suply ,  Lorenza Wyder ,  Janet Dawson King ,  Marie-Gabrielle Ludwig ,  Matthias Mueller ,  Puneeta Nath ,  Carol Elizabeth Jones

IPC分类号： A61K31/7052 ,  C07H21/02 ,  A01K67/033 ,  A61P9/00 ,  C12Q1/02

CPC分类号： C12N15/1138 ,  A01K67/0275 ,  A01K2217/075 ,  A01K2227/105 ,  A01K2267/03 ,  C07K14/723 ,  C12N15/8509 ,  C12N2310/14 ,  G01N2333/726

摘要： The present invention relates to the use of a GPR4 inhibitor for the manufacture of a medicament for the inhibition of angiogenesis, for instance for the inhibition of tumour growth in the treatment of cancer. In a preferred embodiment, said inhibitor is a siRNA, preferably double-stranded.In addition, the present invention further encompasses non-human animals wherein the GPR4 has been inactivated, for instance a knock-out mouse lacking GPR4, and the use of said animals as an experimental model for angiogenesis and for screening for compounds modulating angiogenesis.

摘要翻译： 本发明涉及GPR4抑制剂在制备用于抑制血管生成的药物中的用途，例如用于抑制癌症治疗中的肿瘤生长。 在优选的实施方案中，所述抑制剂是siRNA，优选双链。 此外，本发明还包括其中GPR4已被灭活的非人动物，例如缺乏GPR4的敲除小鼠，以及所述动物用作血管发生的实验模型并用于筛选调节血管生成的化合物。

公开(公告)号：US20090131408A1

公开(公告)日：2009-05-21

申请号：US12224734

申请日：2007-02-21

申请人： Pietro Bollinger ,  Mahavir Prashad ,  Bernhard Riss ,  Janet Dawson King ,  Peter C. Hiestand ,  Yugang Liu ,  Jonathan King ,  Vincent Schmid ,  Friedrich Schuerch

发明人： Pietro Bollinger ,  Mahavir Prashad ,  Bernhard Riss ,  Janet Dawson King ,  Peter C. Hiestand ,  Yugang Liu ,  Jonathan King ,  Vincent Schmid ,  Friedrich Schuerch

IPC分类号： A61K31/55 ,  C07D495/04 ,  A61P19/02 ,  A61P29/00

CPC分类号： C07D495/04

摘要： The present invention relates to novel aza-thia-benzoazulene derivatives of formula I as defined in the claims, their preparation, the use of these novel compounds for the preparation of pharmaceutical compositions, the use of these novel compounds and compositions for managing arthritis and arthritis-related conditions as well as in the treatment of pain in animals and humans. More particularly, the present invention relates to pharmaceutical, preferably veterinary compositions and methods for reducing inflammation and pain associated with acute inflammation of body parts, particularly joints, due to injury or due to arthritic conditions or other disease conditions.

摘要翻译： 本发明涉及权利要求中定义的式I的新型氮杂 - 硫杂 - 苯并薁衍生物，其制备方法，这些新化合物在制备药物组合物中的用途，这些新化合物的使用和用于治疗关节炎和关节炎的组合物 相关条件以及治疗动物和人类的疼痛。 更具体地，本发明涉及用于减少由于损伤或由于关节炎病症或其他疾病状况而引起的身体部位，特别是关节的急性炎症的炎症和疼痛的药物，优选兽医组合物和方法。

公开(公告)号：US08258128B2

公开(公告)日：2012-09-04

申请号：US12224734

申请日：2007-02-21

申请人： Pietro Bollinger ,  Mahavir Prashad ,  Bernhard Riss ,  Janet Dawson King ,  Peter C. Hiestand ,  Yugang Liu ,  Jonathan King ,  Vincent Schmid ,  Friedrich Schuerch

发明人： Pietro Bollinger ,  Mahavir Prashad ,  Bernhard Riss ,  Janet Dawson King ,  Peter C. Hiestand ,  Yugang Liu ,  Jonathan King ,  Vincent Schmid ,  Friedrich Schuerch

IPC分类号： A61K31/33 ,  A61K31/55 ,  A61K31/38 ,  A01N43/00 ,  A01N43/12

CPC分类号： C07D495/04

摘要： The present invention relates to novel aza-thia-benzoazulene derivatives of formula I as defined in the claims, their preparation, the use of these novel compounds for the preparation of pharmaceutical compositions, the use of these novel compounds and compositions for managing arthritis and arthritis-related conditions as well as in the treatment of pain in animals and humans. More particularly, the present invention relates to pharmaceutical, preferably veterinary compositions and methods for reducing inflammation and pain associated with acute inflammation of body parts, particularly joints, due to injury or due to arthritic conditions or other disease conditions.

摘要翻译： 本发明涉及权利要求中定义的式I的新型氮杂 - 硫杂 - 苯并薁衍生物，其制备方法，这些新化合物在制备药物组合物中的用途，这些新化合物的使用和用于治疗关节炎和关节炎的组合物 相关条件以及治疗动物和人类的疼痛。 更具体地，本发明涉及用于减少由于损伤或由于关节炎病症或其他疾病状况而引起的身体部位，特别是关节的急性炎症的炎症和疼痛的药物，优选兽医组合物和方法。