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1. 发明专利

JPH07500184A 失效
公开(公告)号：JPH07500184A
公开(公告)日：1995-01-05
申请号：JP50684393
申请日：1992-10-06
申请人： KAROBIO AB
IPC分类号： G01N33/566 , G01N33/50 , G01N33/68 , G01N33/74 , G01N33/78

2. 发明专利

JP2002010788A ORPHAN RECEPTOR 失效
公开(公告)号：JP2002010788A
公开(公告)日：2002-01-15
申请号：JP2000240120
申请日：2000-08-08
申请人： KAROBIO AB
发明人： KUIPER GEORGE G J M , ENMARK EVA , GUSTAFSSON JAN-AKE
IPC分类号： G01N33/50 , A61K38/00 , A61K45/00 , A61P9/00 , A61P13/08 , A61P19/10 , A61P25/28 , A61P35/00 , C07K14/705 , C07K14/72 , C12N15/09 , C12N15/12 , C12P21/02 , C12Q1/68 , G01N33/15 , G01N33/53
摘要： PROBLEM TO BE SOLVED: To obtain an orphan receptor useful for isolating a molecule for treating diseases such as prostatic cancer, benign prostatic hyperplasia, osteoporosis or cardiovascular disease, etc., and for testing a substance in terms of influences of estrogen and other hormones. SOLUTION: This orphan receptor is concerned with a new estrogen/receptor- related nuclear receptor termed 'ERβ' containing substantially the same amino acid sequence as that of a specific amino acid sequence derived from a rat or an amino acid sequence functionally similar to the amino acid sequence. The DNA sequence encoding the receptor is obtained.

3. 发明申请

WO2007006561A3 IMPROVED CRYSTALLINE FORM OF THE COMPOUND A-348441 审中-公开
标题翻译：化合物A-348441的改进的结晶形式
公开(公告)号：WO2007006561A3
公开(公告)日：2007-04-12
申请号：PCT/EP2006006811
申请日：2006-07-12
申请人： KAROBIO AB , CINK RUSSELL DREW , ZOU DAOZHONG , LEANNA MARVIN ROBERT , TOMA PASCAL H , LONG MICHELLE ANDREE
发明人： CINK RUSSELL DREW , ZOU DAOZHONG , LEANNA MARVIN ROBERT , TOMA PASCAL H , LONG MICHELLE ANDREE
IPC分类号： C07J41/00 , A61K31/575 , A61P3/10
CPC分类号： C07J41/0083
摘要： There is provided a hemihydrate of (3ß, 5ß, 7a, 12a) -7 , 12- dihydroxy-3-{2- [ {4- [17ß-hydroxy-3-oxo-17a-prop-l-ynylestra- 4 , 9-dien-llß-yl] phenyl } (methyl) amino] ethoxy} cholan-24-oic acid in a crystalline form which is characterised by an X-ray diffraction pattern having major peaks at 2? = 6.58±0.2, 8.54+0.2, 12.28±0.2, and 19.68±0.2. This crystalline material is useful in the treatment of conditions associated with an excess of hepatic glucocorticoid response.
摘要翻译：提供了一种半水合物（3β，5β，7a，12a）-7,12-二羟基-3- {2 - [{4- [17β-羟基-3-氧代-17α-丙-1-炔基] 9-二烯-11β-基]苯基}（甲基）氨基]乙氧基}哒嗪-4-酸的结晶形式，其特征在于具有2θ的主峰的X射线衍射图 = 6.58±0.2,8.54±0.2,12.28±0.2和19.68±0.2。该结晶材料可用于治疗与过量肝糖皮质激素反应相关的病症。

4. 发明申请

WO9963976A3 LIVER-SELECTIVE GLUCOCORTICOID ANTAGONIST FOR TREATING DIABETES 审中-公开
标题翻译：用于治疗糖尿病的肝脏选择性GLUCOCORTICOID ANTAGONIST
公开(公告)号：WO9963976A3
公开(公告)日：2001-12-20
申请号：PCT/IB9901175
申请日：1999-06-07
申请人： KAROBIO AB , APELQVIST THERESA , EFENDIC SUAD
发明人： APELQVIST THERESA , EFENDIC SUAD
IPC分类号： A61K45/00 , A61K31/00 , A61K31/155 , A61K31/192 , A61K31/426 , A61K31/64 , A61K38/28 , A61K45/06 , A61P3/10 , A61P43/00 , C07C57/58 , A61K31/19
CPC分类号： A61K31/00
摘要： Use of a liver-selective glucocorticoid antagonist, preferably the compound having formula (I) in the preparation of a pharmaceutical composition for the treatment of diabetes. A composition for the treatment of diabetes containing such a glucocorticoid antagonist, and a method of treating diabetes using the composition.
摘要翻译：使用肝选择性糖皮质激素拮抗剂，优选具有式（I）的化合物在制备用于治疗糖尿病的药物组合物中。用于治疗含有这种糖皮质激素拮抗剂的糖尿病的组合物，以及使用该组合物治疗糖尿病的方法。

5. 发明申请

WO9832863A3 MAMMALIAN THIOREDOXIN 审中-公开
公开(公告)号：WO9832863A3
公开(公告)日：1998-11-05
申请号：PCT/GB9800263
申请日：1998-01-28
申请人： KAROBIO AB , DEAN JOHN PAUL , SPYROU GIANNIS
发明人： SPYROU GIANNIS
IPC分类号： G01N33/53 , A61K38/00 , A61P9/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P39/00 , A61P43/00 , C07K14/47 , C07K16/18 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/02 , C12N15/09 , C12N15/53 , C12P21/02 , C12Q1/68 , A01K67/027 , A61K38/44 , C07K16/40 , C12N15/70 , C12N15/85 , G01N33/68
CPC分类号： C12N9/0036 , A01K2217/05 , A61K38/00
摘要： This invention relates to a thioredoxin and to methods for its use.

6. 发明申请

WO2004058819A3 CRYSTALLINE LIVER X RECEPTOR BETA PROTEIN 审中-公开
标题翻译：水晶蛋白X受体蛋白质
公开(公告)号：WO2004058819A3
公开(公告)日：2004-12-02
申请号：PCT/IB0306412
申请日：2003-12-24
申请人： KAROBIO AB , FARNEGARDH MATHIAS , BONN TOMAS , SUN SHERRY , LJUNGGREN JAN , AHOLA HARRI , CARLQUIST MATS
发明人： FARNEGARDH MATHIAS , BONN TOMAS , SUN SHERRY , LJUNGGREN JAN , AHOLA HARRI , CARLQUIST MATS
IPC分类号： C07K14/705 , C07K14/72 , G06T17/00
CPC分类号： C07K14/70567 , C07K2299/00 , Y02A90/26
摘要： The present invention is in the fields of biotechnology, protein purification and crystallization, x-ray diffraction analysis, three-dimensional computer molecular modelling and rational drug design. The invention is directed to the Liver X receptor and ligands for this receptor, and in particular to crystalline Liver X receptor beta (LXRbeta) and to methods of identifying ligands utilizing LXRbeta, as well as to compounds, compositions and methods for selecting, making, and using therapeutic or diagnostic agents having LXRbeta modulating or binding activity.
摘要翻译：本发明涉及生物技术，蛋白质纯化和结晶，X射线衍射分析，三维计算机分子建模和合理药物设计领域。本发明涉及用于该受体的肝X受体和配体，特别是结晶肝X受体β（LXRbeta）以及利用LXRβ鉴定配体的方法，以及用于选择，制备，并使用具有LXRbeta调节或结合活性的治疗或诊断剂。

7. 发明申请

WO2004037792A3 BENZO (F) QUINOLINONE VARIANTS AS NUCLEAR HORMONE RECEPTOR LIGANDS 审中-公开
标题翻译：苯醌（F）喹诺酮类变体作为核激素受体配体
公开(公告)号：WO2004037792A3
公开(公告)日：2004-09-02
申请号：PCT/EP0310108
申请日：2003-09-10
申请人： KAROBIO AB , RUDA MARCUS , WENSBO DAVID
发明人： RUDA MARCUS , WENSBO DAVID
IPC分类号： C07D221/10 , A61K31/435 , A61K31/4375 , A61K31/47 , C07D215/00 , C07D221/16
CPC分类号： C07D221/10
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as nuclear hormone receptor modulators. The compounds of the instant invention are ligands for nuclear hormone receptors and as such may be useful for treatment or prevention of a variety of conditions related to nuclear hormone functioning including proliferative diseases, cancers, benign prostate hyperplasia, adenomas and neoplasisms of the prostate, benign or malignant tumor cells containing the androgen receptor, cardiovascular diseases, angiogenic conditions or disorders, hirsutism, acne, hyperpilosity, inflammation, immune modulation, seborrhea, endometriosis, polycycstic ovary syndrome, androgen alopecia, hypogonadism, osteoporosis, suppressing spermatogenesis, libido, cachexia, anorexia, cancers expressing the estrogen receptor, prostate cancer, breast cancer, endometrial cancer, incontinence, hot flashes, vaginal dryness, menopause, contraception, pregnancy termination, cancers containing the progesterone e receptor, endometriosis, cachexia, menopause fibrosis, labor induction, autoimmune diseases, impairment of cognitive functioning, cerebral degenerative disorders, Alzheimer's disease, psychotic disorders, type-II diabetes, congestive heart failure, disregulation of cholesterol or lipid homeostasis, and/or obesity. A compound having the general formula I or II:
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其作为核激素受体调节剂的用途。本发明的化合物是核激素受体的配体，因此可用于治疗或预防与核激素功能相关的各种病症，包括增殖性疾病，癌症，良性前列腺增生，前列腺腺瘤和肿瘤，良性或含有雄激素受体的恶性肿瘤细胞，心血管疾病，血管生成病症或病症，多毛症，痤疮，高通气，炎症，免疫调节，脂溢性皮脂血症，子宫内膜异位症，多环性卵巢综合征，雄激素性脱发，性腺机能减退，骨质疏松症，抑制精子发生，性欲，恶病质，厌食症，表达雌激素受体的癌症，前列腺癌，乳腺癌，子宫内膜癌，失禁，潮热，阴道干燥，绝经，避孕，妊娠终止，含有孕酮e受体的癌症，子宫内膜异位症，恶病质，绝经纤维化，劳动诱导，自身免疫疾病，齿轮损伤硝基功能，脑退行性疾病，阿尔茨海默病，精神病，II型糖尿病，充血性心力衰竭，胆固醇或脂质体内平衡失调和/或肥胖。具有通式I或II的化合物：

8. 发明申请

WO0162792A3 CANCER TREATMENT AND PROGNOSIS INVOLVING HES-1 PROTEIN 审中-公开
标题翻译：涉及HES-1蛋白的癌症治疗和预防
公开(公告)号：WO0162792A3
公开(公告)日：2002-04-04
申请号：PCT/EP0102171
申请日：2001-02-26
申请人： KAROBIO AB , STROM ANDERS , GUSTAFSSON JAN AAKE
发明人： STROM ANDERS , GUSTAFSSON JAN AAKE
IPC分类号： A61K31/138 , A61K31/165 , A61K31/4436 , A61K38/00 , A61K45/06 , A61K48/00 , C07K14/47 , C07K16/18 , G01N33/574 , A61K38/17 , A61K31/4535 , A61K31/565 , A61P35/00 , G01N33/50
CPC分类号： G01N33/57484 , A61K31/138 , A61K31/165 , A61K31/4436 , A61K38/00 , A61K45/06 , A61K48/00 , C07K14/4702 , C07K16/18 , G01N2500/00 , G01N2800/52
摘要： This invention relates to methods of cancer treatment and prognosis and in particular to such methods involving the HES-1 protein.
摘要翻译：本发明涉及癌症治疗和预后的方法，特别涉及涉及HES-1蛋白质的方法。

9. 发明申请

WO0076529A3 USE OF ESTROGEN RECEPTOR AGONISTS OR ANTAGONISTS FOR TREATING GROWTH, BONE DISORDERS 审中-公开
标题翻译：使用雌激素受体激动剂或拮抗剂治疗生长，骨质疏松症
公开(公告)号：WO0076529A3
公开(公告)日：2001-07-12
申请号：PCT/GB0002283
申请日：2000-06-12
申请人： KAROBIO AB , DEAN JOHN PAUL , OHLSSON CLAES , GUSTAFSSON JAN AKE
发明人： OHLSSON CLAES , GUSTAFSSON JAN AKE
IPC分类号： A61K31/00 , A61K31/138 , A61K31/4535 , A61P19/00
CPC分类号： A61K31/00 , A61K31/138 , A61K31/4535
摘要： Androgens regulate the male skeleton directly via a stimulation of androgen receptors and indirectly via aromatization of androgens into estrogen and thereafter stimulation of estrogen receptors (ER). In order to investigate the relative importance of estrogen receptor subtypes in the regulation of the male skeleton, the skeletal phenotypes of wild type (WT), ER alpha , Knockout (ERKO), ER beta Knockout (BERKO) and ER alpha / beta Double Knockout (DERKO) mice were compared. ERKO and DERKO had reduced body weight as well as longitudinal bone growth. Furthermore, ERKO and DERKO but not BERKO demonstrated a pronounced decrease in bone mineral content in the long bones and in the axial skeleton. This decrease in BMC was due to cortical ostopenia as a result of decreased radial growth of the bones. Mechanical testing demonstrated that femora from ERKO were weaker as a result of the altered cortical bone dimensions. No significant change in trabecular BMD was seen in any group. ERKO demonstrated decreased serum levels of osteocalcin and IGF-I. Furthermore, serum levels of IGF-I were correlated to most of the skeletal changes seen in DERKO and ERKO. In conclusion , the skeletal phenotypes of DERKO and ERKO are similar and clearly distinguishable from WT and BERKO. Therefore, ER alpha , but not ER beta , mediates the effect of estrogen in the skeleton of male mice.
摘要翻译：雄激素通过雄激素受体的刺激直接调节雄性骨骼，间接通过雄激素的芳构化进入雌激素，此后刺激雌激素受体（ER）。为了研究雌激素受体亚型在雄性骨骼调控中的相对重要性，野生型（WT），ERα，Knockout（ERKO），ERβ敲除（BERKO）和ERα/β双重敲除的骨骼表型（DERKO）小鼠进行比较。 ERKO和DERKO具有减轻体重以及纵向骨骼生长。此外，ERKO和DERKO，但不是BERKO，证明长骨骼和轴向骨骼中骨矿物质含量明显下降。 BMC的这种减少是由于骨骼的径向生长减少导致的皮质骨质减少。机械测试表明，ERKO的股骨由于皮质骨尺寸的变化而较弱。任何组中均未观察到小梁骨BMD发生明显变化。 ERKO表现出骨钙素和IGF-I的血清水平降低。此外，IGF-I的血清水平与DERKO和ERKO中观察到的大多数骨骼变化相关。总之，DERKO和ERKO的骨骼表型与WT和BERKO相似且明显区别。因此，ERα，而不是ERβ介导雌激素在雄性小鼠骨骼中的作用。

10. 发明申请

WO0052050A3 HOMOLOGY MODELS OF THE GLUCOCORTICOID RECEPTOR 审中-公开
标题翻译： GLUCOCORTICOID受体的同源模型
公开(公告)号：WO0052050A3
公开(公告)日：2000-12-28
申请号：PCT/GB0000727
申请日：2000-03-01
申请人： KAROBIO AB , GILLNER MIKAEL , GREENIDGE PAULETTE
发明人： GILLNER MIKAEL , GREENIDGE PAULETTE
IPC分类号： C07K14/72 , G06F19/16 , G06F19/18 , C07K14/705
CPC分类号： C07K14/721 , G06F19/16 , G06F19/18
摘要： A method of designing a homology model of the ligand binding domain of a glucocorticoid receptor wherein the homology model may be displayed as a three-dimensional image, the method comprising: (i) providing an amino acid sequence and an x-ray crystallographic structure of the ligand binding domain of a thyroid, estrogen or progesterone receptor; (ii) modifying said x-ray crystallographic structure to take account of differences between the amino acid configuration of the ligand binding domains of the glucocorticoid receptor on the one hand and the thyroid, estrogen, or progesterone receptor on the other hand; (iii) verifying the accuracy of the homology model by comparing it with experimentally-determined binding properties of a number of ligands for the glucocorticoid receptor; and (iv) if required modifying the homology model for greater consistency with those binding properties.
摘要翻译：设计糖皮质激素受体的配体结合结构域的同源性模型的方法，其中所述同源性模型可以显示为三维图像，所述方法包括：（i）提供氨基酸序列和x射线晶体结构甲状腺配体结合域，雌激素或孕激素受体; （ii）修改所述x射线晶体结构以考虑到糖皮质激素受体的配体结合结构域与甲状腺，雌激素或孕酮受体之间的氨基酸构型之间的差异; （iii）通过将其与糖皮质激素受体的许多配体的实验确定的结合特性进行比较来验证同源性模型的准确性; 和（iv）如果需要修改同源性模型以与这些结合性质更一致。

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