公开(公告)号：US20060281685A1

公开(公告)日：2006-12-14

申请号：US11459583

申请日：2006-07-24

申请人： Michael Bernd ,  Bernhard Kutscher ,  Eckhard Gunther ,  Peter Romeis ,  Thomas Reissmann ,  Thomas Beckers

发明人： Michael Bernd ,  Bernhard Kutscher ,  Eckhard Gunther ,  Peter Romeis ,  Thomas Reissmann ,  Thomas Beckers

IPC分类号： A61K38/10

CPC分类号： A61K38/10 ,  C07K7/06 ,  C07K7/23

摘要： The invention relates to peptides which contain N-methylated amino acid units and have improved water solubility. The invention also relates methods for treating a hormone-dependent tumor or a non-malignant indication that is treatable by LH-RH suppression, the method comprising administering to a patient in need of the treatment a therapeutically effective amount of a compound of the invention. Hormone-dependent cancers that can be treated with the methods of the invention include prostate cancer, breast cancer, ovarian cancer, endometrial cancer, and pancreatic cancer. Non-malignant indications which can be treated by the methods of the invention include benign prostate hyperplasia (BPH), endometriosis, acne, polycystic ovarian disease, dysmenorrhea, precocious puberty, and uterine fibroids and other leiomyomas.

摘要翻译： 本发明涉及含有N-甲基化氨基酸单元并具有改善的水溶性的肽。 本发明还涉及用于治疗激素依赖性肿瘤或可通过LH-RH抑制治疗的非恶性指征的方法，所述方法包括向需要治疗的患者施用治疗有效量的本发明化合物。 可用本发明方法治疗的依赖于激素的癌症包括前列腺癌，乳腺癌，卵巢癌，子宫内膜癌和胰腺癌。 可以通过本发明的方法治疗的非恶性适应症包括良性前列腺增生（BPH），子宫内膜异位症，痤疮，多囊卵巢疾病，痛经，早熟性青春期和子宫肌瘤和其他平滑肌瘤。

公开(公告)号：US5837462A

公开(公告)日：1998-11-17

申请号：US746383

申请日：1996-11-08

申请人： Thomas Beckers ,  Thomas Klenner ,  Silke Baasner

发明人： Thomas Beckers ,  Thomas Klenner ,  Silke Baasner

IPC分类号： C12N15/09 ,  A61P35/00 ,  C07H21/04 ,  C07K14/71 ,  C12N5/10 ,  C12N9/12 ,  C12N9/16 ,  C12Q1/18 ,  C12Q1/42 ,  C12R1/91 ,  C12Q1/68

CPC分类号： C12N9/16 ,  C07K14/71 ,  C12Q1/42 ,  C07K2319/02

摘要： The invention describes a novel method for determining the mass of vital tumor cells of xenotransplants in animal models. Cells altered by genetic engineering which form a tumor after transplantation synthesize an excreted reporter gene. This is shown by way of example for a secreted form of human placenta-specific, alkaline phosphate (SEAP). The latter can be demonstrated in the serum of test animals or in culture supernatants. The activity of SEAP in the serum correlates with the number of vital tumor cells in the animal and can be measured prior to the formation of a palpable tumor. The invention shows the use of cell lines altered by genetic engineering in such a manner in subcutaneous and orthotopic tumor models. Dicistronic, eukaryotic expression vectors are used for the stable transfection of the mammalian cell lines or tumor cells used. These vectors contain, under the control of a constitutive or inducible promotor element, the gene coding for SEAP, coupled with a second gene. This latter gene codes e.g. for a receptor tyrosine kinase such as erbB2/HER2 which transforms during overexpression.

摘要翻译： 本发明描述了用于确定动物模型中异种移植物的重要肿瘤细胞的质量的新方法。 通过基因工程改变的细胞在移植后形成肿瘤合成排泄的报道基因。 这通过例如人胎盘特异性碱性磷酸盐（SEAP）的分泌形式的方式示出。 后者可以在测试动物的血清或培养物上清液中证实。 血清中SEAP的活性与动物中重要的肿瘤细胞的数量相关，并且可以在形成可触及的肿瘤之前测量。 本发明显示了通过基因工程改变的细胞系在皮下和原位肿瘤模型中的使用。 双顺反子，真核表达载体用于稳定转染所用的哺乳动物细胞系或肿瘤细胞。 这些载体在组成型或诱导型启动子元件的控制下含有编码SEAP的基因，加上第二个基因。 后一种基因编码例如 用于在过表达期间转化的受体酪氨酸激酶如erbB2 / HER2。