公开(公告)号：US20090170095A1

公开(公告)日：2009-07-02

申请号：US12174301

申请日：2008-07-16

申请人： Arnd Steuernagel ,  Karsten Eulenberg ,  Gunter Broenner ,  Thomas Clossek ,  Bettina Rudoplh ,  Dorothea Rudolph ,  Funmi Belgore ,  Stefan Jakel ,  Christoph Meyer

发明人： Arnd Steuernagel ,  Karsten Eulenberg ,  Gunter Broenner ,  Thomas Clossek ,  Bettina Rudoplh ,  Dorothea Rudolph ,  Funmi Belgore ,  Stefan Jakel ,  Christoph Meyer

IPC分类号： C12Q1/68 ,  G01N33/53 ,  C12Q1/48

CPC分类号： C12N9/1205 ,  A61K38/45 ,  Y10S514/909

摘要： The present invention discloses Mnk homologous proteins regulating the energy homeostasis, the metabolism of triglycerides, and/or is contributing to membrane stability and/or function of organelles, and polynucleotides, which identify and encode the proteins disclosed in this invention. The invention also relates to the use of these sequences in the diagnosis, study, prevention, and treatment of diseases and disorders related to body-weight regulation and thermogenesis, for example, but not limited to, metabolic diseases such as obesity, as well as related disorders such as eating disorder, cachexia, diabetes mellitus, hypertension, coronary heart disease, hypercholesterolemia, dyslipidemia, osteoarthritis, gallstones, and sleep apnea, and disorders related to ROS defence, such as diabetes mellitus, neurodegenerative disorders, and cancer, e.g. cancers of the reproductive organs, and others.

摘要翻译： 本发明公开了调节能量稳态的Mnk同源蛋白质，甘油三酸酯的代谢和/或有助于细胞器的膜稳定性和/或功能，以及鉴定和编码本发明公开的蛋白质的多核苷酸。 本发明还涉及这些序列用于诊断，研究，预防和治疗与体重调节和产热有关的疾病和病症的用途，例如但不限于代谢性疾病如肥胖症，以及 相关疾病如进食障碍，恶病质，糖尿病，高血压，冠心病，高胆固醇血症，血脂异常，骨关节炎，胆结石和睡眠呼吸暂停，以及与ROS防御相关的疾病，如糖尿病，神经变性疾病和癌症，例如 生殖器官的癌症等。

公开(公告)号：US20110065734A1

公开(公告)日：2011-03-17

申请号：US12743044

申请日：2008-11-14

申请人： Thomas Bar ,  Thomas Maier ,  Thomas Beckers ,  Thomas Clossek ,  Siavosh Mahboobi ,  Andreas Sellmer

发明人： Thomas Bar ,  Thomas Maier ,  Thomas Beckers ,  Thomas Clossek ,  Siavosh Mahboobi ,  Andreas Sellmer

IPC分类号： A61K31/517 ,  C07D213/68 ,  A61K31/44 ,  C07D403/10 ,  A61K31/505 ,  C07D401/10 ,  A61K31/4439 ,  C07D403/12 ,  A61P35/00 ,  A61P19/02 ,  A61P37/06 ,  A61P11/06

CPC分类号： C07D213/68 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14

摘要： The present invention relates to a bifunctional compound of formula I or its pharmaceutically acceptable salts or solvates A-L-B (I) wherein A is a histone deacetylase (HDAC) inhibitory moiety, L is a single bond or a linker group and B is a protein kinase inhibitory moiety. The bifunctional compound according to formula (I) is useful for the treatment of malignant and non-malignant neoplasia and diseases related to abnormal cell growth.

摘要翻译： 本发明涉及式I的双功能化合物或其药学上可接受的盐或溶剂合物ALB（I）其中A是组蛋白脱乙酰酶（HDAC）抑制部分，L是单键或连接基团，B是蛋白激酶抑制 部分。 根据式（I）的双功能化合物可用于治疗恶性和非恶性肿瘤以及与异常细胞生长相关的疾病。