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1. 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。

2. 发明申请

WO02053522A3 NOVEL ESTROGEN RECEPTOR LIGANDS AND METHODS I 审中-公开
标题翻译：新颖的雌激素受体配体和方法I
公开(公告)号：WO02053522A3
公开(公告)日：2004-01-08
申请号：PCT/EP0115230
申请日：2001-12-24
申请人： KAROBIO AB , MERCK & CO INC , KOEHLER KONRAD , HENSSEN CECILIA , NILSSON MARITA , GILLNER MIKAEL , LIU YE , SANIN ANDREI , WILKENING ROBERT R , RATCLIFFE RONALD W , WENSBO DAVID
发明人： KOEHLER KONRAD , HENSSEN CECILIA , NILSSON MARITA , GILLNER MIKAEL , LIU YE , SANIN ANDREI , WILKENING ROBERT R , RATCLIFFE RONALD W , WENSBO DAVID
IPC分类号： A61K31/343 , A61K31/05 , A61K31/10 , A61K31/122 , A61K31/15 , A61K31/352 , A61K31/357 , A61K31/385 , A61P3/02 , A61P3/04 , A61P3/06 , A61P5/30 , A61P9/00 , A61P9/10 , A61P15/08 , A61P19/00 , A61P19/08 , A61P19/10 , A61P25/28 , A61P35/00 , A61P37/02 , A61P43/00 , C07C35/37 , C07C35/44 , C07C39/17 , C07C39/42 , C07C49/727 , C07C49/737 , C07C49/747 , C07C251/44 , C07C323/17 , C07D307/94 , C07D311/96 , C07D317/72 , C07D339/06 , C07D339/08 , A61K31/045 , A61K31/39 , A61K31/557 , C07C43/315
CPC分类号： C07D317/72 , C07C39/17 , C07C39/42 , C07C49/747 , C07C251/44 , C07C323/17 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2601/16 , C07C2603/26 , C07C2603/96 , C07D307/94 , C07D311/96 , C07D339/06 , C07D339/08
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant inventive are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynecomastia, autoimmune disease, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer of the lung, colon, breast, uterus, and prostate.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括骨丢失，骨折，骨质疏松症，软骨退化，子宫内膜异位症，子宫肌瘤病，潮热，低密度脂蛋白胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子女性生殖症，自身免疫性疾病，血管平滑肌细胞增殖，肥胖症，失禁和肺癌，结肠癌，乳腺癌，子宫癌和前列腺癌。

3. 发明专利

AT301629T 未知
公开(公告)号：AT301629T
公开(公告)日：2005-08-15
申请号：AT01272663
申请日：2001-12-24
申请人： KAROBIO AB , MERCK & CO INC
发明人： KOEHLER KONRAD , HENSSEN CECILIA , NILSSON MARITA , GILLNER MIKAEL , LIU YE , SANIN ANDREI , WILKENING ROBERT R , RATCLIFFE RONALD W , WENSBO DAVID
IPC分类号： A61K31/343 , A61K31/05 , A61K31/10 , A61K31/122 , A61K31/15 , A61K31/352 , A61K31/357 , A61K31/385 , A61P3/02 , A61P3/04 , A61P3/06 , A61P5/30 , A61P9/00 , A61P9/10 , A61P15/08 , A61P19/00 , A61P19/08 , A61P19/10 , A61P25/28 , A61P35/00 , A61P37/02 , A61P43/00 , C07C35/37 , C07C35/44 , C07C39/17 , C07C39/42 , C07C49/727 , C07C49/737 , C07C49/747 , C07C251/44 , C07C323/17 , C07D307/94 , C07D311/96 , C07D317/72 , C07D339/06 , C07D339/08 , C07C43/315
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant inventive are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynecomastia, autoimmune disease, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer of the lung, colon, breast, uterus, and prrostate.

4. 发明专利

AU2004285744A1 Androgen receptor modulators 未知
公开(公告)号：AU2004285744A1
公开(公告)日：2005-05-12
申请号：AU2004285744
申请日：2004-10-21
申请人： KAROBIO AB
发明人： JERNSTEDT HENRIK , COLLAZO ANA MARIA GARCIA , GUSTAVSSON ANNIKA , GARG NEERAJ , GILLNER MIKAEL , KOCH EVA
IPC分类号： C07C205/11 , A61K31/04 , A61K31/10 , A61K31/277 , A61K31/435 , C07C215/16 , C07C215/28 , C07C215/44 , C07C215/52 , C07C215/60 , C07C255/42 , C07C255/50 , C07C255/58 , C07C317/36 , C07C323/25 , C07D213/70 , C07D213/74 , C07D213/85 , C07D295/13 , C07D307/52 , C07D401/12 , C07D405/12
摘要： Treatment of Diseases caused by Disturbances of the Activity of the Androgen Receptor uses of compounds of Formula (I): (as defined herein), for the treatment of diseases caused by disturbances of the activity of androgen receptor are provided: Formula (I). Isolated compounds of Formula (I) are also provided.

5. 发明专利

PE10972001A1 COMPUESTOS FENOXI FENIL ACTIVOS EN EL RECEPTOR GLUCOCORTICOIDE 未知
公开(公告)号：PE10972001A1
公开(公告)日：2001-10-27
申请号：PE0013192000
申请日：2000-12-07
申请人： ABBOTT LAB , KAROBIO AB
发明人： PELCMAN BENJAMIN , GILLNER MIKAEL , HAGBERG LARS , LINDBERG MARITA , KYM PHILIP R , WU JINCHANG , KOCH EVA , GUSTAVSSON ANNIKA , APELQVIST THERESA
IPC分类号： C07D295/12 , A61K31/166 , A61K31/192 , A61K31/195 , A61K31/341 , A61K31/40 , A61K31/404 , A61K31/4453 , A61K31/495 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/46 , A61P7/00 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/02 , A61P11/06 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/02 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P27/02 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C59/68 , C07C59/72 , C07C69/736 , C07C69/92 , C07C205/37 , C07C215/50 , C07C217/58 , C07C217/80 , C07C217/86 , C07C229/60 , C07C233/25 , C07C233/75 , C07C235/48 , C07C311/17 , C07C317/18 , C07C323/16 , C07C323/52 , C07D209/12 , C07D295/096 , C07D295/13 , C07D307/28 , C07D307/38
CPC分类号： C07D295/096 , C07C59/68 , C07C59/72 , C07C69/736 , C07C215/50 , C07C217/58 , C07C217/86 , C07C229/60 , C07C233/25 , C07C233/75 , C07C235/48 , C07C311/17 , C07C317/18 , C07C323/16 , C07C323/52 , C07C2601/02 , C07D209/12 , C07D295/13 , C07D307/38
摘要： SE REFIERE A COMPUESTOS 5-ISOPROPIL-FENOXI FENILACETICO DE FORMULA I DONDE R1 ES COOH, CONHOH, SO3H, P(O)(OH)(OR8), HETEROARILO; R2 Y R3 SON H, HALOGENO, ALQUILO C1-C6, ENTRE OTROS; R4, R5, R6 Y R7 SON ALQUILO C1-C12, PERFLUOROALQUILO C1-C6, ALQUILO C3-C8, ALQUENILO C2-C5, ENTRE OTROS; O R4 Y R5 SON HETEROCICLOALQUILO C3-C8, ARILO, HETEROARILO; O R4 ES HALOGENO, R80, R8S, R9S(O), ENTRE OTROS; R6 Y R7 SON H, HALOGENO, R8O, R9R10N, ENTRE OTROS; R8, R9, R10 SON H, ALQUILO C1-C12, CICLOALQUILO C3-C8, ARILO, HETEROARILO, ENTRE OTROS; Y ES H, HALOGENO, OH, ALCOXI C1-C6; ENTRE OTROS; n ES 0-3. SON COMPUESTOS PREFERIDOS ACIDO 3,5-DIBROMO-4-[2-(1-HIDROXIETIL)-5-ISOPROPIL-4-METOXIFENOXI]FENILACETICO, ACIDO 3,5-DIBROMO-4-[2(1-(3-INDOLIL)ETIL)-5-ISOPROPIL-4-METOXIFENOXI]FENILACETICO, ENTRE OTROS; EL COMPUESTO I MODULA RECEPTOR GLUCOCORTICOIDE SELECTIVO PARA HIGADO Y PUEDE SER UTIL PARA EL TRATAMIENTO DE DISFUNCION METABOLICA COMO DIABETES, ENFERMEDAD DE CUSHING, INFLAMACION, ENFERMEDADES AUTOINMUNES, RECHAZO DE TRASPLANTES, NEOPLASMA, LEUCEMIA

6. 发明专利

AU5787201A Compounds active at the glucocorticoid receptor 未知
公开(公告)号：AU5787201A
公开(公告)日：2001-07-09
申请号：AU5787201
申请日：2000-12-06
申请人： KAROBIO AB , ABBOTT LAB
发明人： APELQVIST THERESA , GILLNER MIKAEL , GUSTAVSSON ANNIKA , HAGBERG LARS , KOCH EVA , LINDBERG MARITA , PELCMAN BENJAMIN , WU JINCHANG , KYM PHILIP R
IPC分类号： C07D295/12 , A61K31/166 , A61K31/192 , A61K31/195 , A61K31/341 , A61K31/40 , A61K31/404 , A61K31/4453 , A61K31/495 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/46 , A61P7/00 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/02 , A61P11/06 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/02 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P27/02 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C59/68 , C07C59/72 , C07C69/736 , C07C69/92 , C07C205/37 , C07C215/50 , C07C217/58 , C07C217/80 , C07C217/86 , C07C229/60 , C07C233/25 , C07C233/75 , C07C235/48 , C07C311/17 , C07C317/18 , C07C323/16 , C07C323/52 , C07D209/12 , C07D295/096 , C07D295/13 , C07D307/28 , C07D307/38 , C07C69/88 , C07C217/56
摘要： This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula (I).

7. 发明专利

ES2247010T3 NUEVOS LIGANDOS DEL RECEPTOR DE ESTROGENOS Y PROCEDIMIENTOS I. 未知
公开(公告)号：ES2247010T3
公开(公告)日：2006-03-01
申请号：ES01272663
申请日：2001-12-24
申请人： KAROBIO AB , MERCK & CO INC
发明人： KOEHLER KONRAD , HENSSEN CECILIA , NILSSON MARITA , GILLNER MIKAEL , LIU YE , SANIN ANDREI
IPC分类号： A61K31/343 , A61K31/05 , A61K31/10 , A61K31/122 , A61K31/15 , A61K31/352 , A61K31/357 , A61K31/385 , A61P3/02 , A61P3/04 , A61P3/06 , A61P5/30 , A61P9/00 , A61P9/10 , A61P15/08 , A61P19/00 , A61P19/08 , A61P19/10 , A61P25/28 , A61P35/00 , A61P37/02 , A61P43/00 , C07C35/37 , C07C35/44 , C07C39/17 , C07C39/42 , C07C49/727 , C07C49/737 , C07C49/747 , C07C251/44 , C07C323/17 , C07D307/94 , C07D311/96 , C07D317/72 , C07D339/06 , C07D339/08 , C07C43/315 , A61K31/045 , A61K31/557 , A61K31/39
摘要： Un compuesto que tiene la **fórmula**, en las que el enlace entre los átomos de carbono C1 y C2 (de los compuestos de fórmula general I) o el enlace entre C2 y C3 (de los compuestos de fórmula general II) o el enlace entre C1 y C10 (de los compuestos de fórmula general III) es un enlace sencillo o doble; R1 (de los compuestos de fórmula general I o III) es un grupo RA distinto de un grupo fenilo; RA se selecciona del grupo de hidrógeno, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, cicloalquilalquilo, arilo o aralquilo; R1 y R1 (de los compuestos de fórmula general II) son iguales o son diferentes y cada uno es un grupo RA; R2 (de los compuestos de fórmula general I o II) es un grupo hidroxilo o RA o es un grupo hidroxialquilo o aminoalquilo de 1 a 2 átomos de carbono; R3 y R3 juntos pueden ser un solo átomo de oxígeno o azufre; o R3 y R3 juntos pueden ser un solo átomo de nitrógeno que a su vez está unido a un grupo seleccionado de RA o ORA; o R3 y R3 juntos pueden ser un solo átomo de carbono que a su vez está unido a dos grupos RA que pueden ser iguales o diferentes; o R3 y R3 pueden ser iguales o son diferentes, y cada uno se puede seleccionar de RA, ORA, SRA, o N(RA)2 en los que los grupos RA individuales pueden ser iguales o son diferentes y opcionalmente se pueden considerar juntos con cualesquiera átomos unidos e intermedios para formar un anillo de 3-8 miembros.

8. 发明专利

CA2543345A1 ANDROGEN RECEPTOR MODULATORS 未知
公开(公告)号：CA2543345A1
公开(公告)日：2005-05-12
申请号：CA2543345
申请日：2004-10-21
申请人： KAROBIO AB
发明人： KOCH EVA , GARG NEERAJ , JERNSTEDT HENRIK , GUSTAVSSON ANNIKA , GILLNER MIKAEL , GARCIA COLLAZO ANA MARIA
IPC分类号： C07C205/11 , A61K31/04 , A61K31/10 , A61K31/277 , A61K31/435 , A61P5/28 , C07C215/16 , C07C215/28 , C07C215/44 , C07C215/52 , C07C215/60 , C07C255/42 , C07C255/50 , C07C255/58 , C07C317/36 , C07C323/25 , C07D213/70 , C07D213/74 , C07D213/85 , C07D295/13 , C07D307/52 , C07D401/12 , C07D405/12
摘要： Treatment of Diseases caused by Disturbances of the Activity of the Androgen Receptor uses of compounds of Formula (I): (as defined herein), for the treatment of diseases caused by disturbances of the activity of androgen receptor are provided: Formula (I). Isolated compounds of Formula (I) are also provided.

9. 发明专利

CA2393583A1 COMPOUNDS ACTIVE AT THE GLUCOCORTICOID RECEPTOR 未知
公开(公告)号：CA2393583A1
公开(公告)日：2001-07-05
申请号：CA2393583
申请日：2000-12-06
申请人： ABBOTT LAB , KAROBIO AB
发明人： KOCH EVA , GUSTAVSSON ANNIKA , PELCMAN BENJAMIN , KYM PHILIP R , WU JINCHANG , HAGBERG LARS , GILLNER MIKAEL , APELQVIST THERESA , NILLSON MARITA
IPC分类号： C07D295/12 , A61K31/166 , A61K31/192 , A61K31/195 , A61K31/341 , A61K31/40 , A61K31/404 , A61K31/4453 , A61K31/495 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P3/14 , A61P5/46 , A61P7/00 , A61P7/02 , A61P9/10 , A61P9/12 , A61P11/02 , A61P11/06 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/02 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P27/02 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C59/68 , C07C59/72 , C07C69/736 , C07C69/92 , C07C205/37 , C07C215/50 , C07C217/58 , C07C217/80 , C07C217/86 , C07C229/60 , C07C233/25 , C07C233/75 , C07C235/48 , C07C311/17 , C07C317/18 , C07C323/16 , C07C323/52 , C07D209/12 , C07D295/096 , C07D295/13 , C07D307/28 , C07D307/38 , A61K31/10 , A61K31/136 , C07C323/18 , A61K31/18 , A61K31/235 , A61K31/435 , C07C217/56 , C07C69/88
摘要： This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in therapy and in the regulation of metabolism, especially lowering blood glucose levels. The compounds referred to are compounds according to the formula (I).

10. 发明专利

AU2007201347A1 Novel estrogen receptor ligands and methods I 未知
公开(公告)号：AU2007201347A1
公开(公告)日：2007-04-19
申请号：AU2007201347
申请日：2007-03-28
申请人： MERCK & CO INC , KAROBIO AB
发明人： WENSBO DAVID , KOEHLER KONRAD , GILLNER MIKAEL , RATCLIFFE RONALD W , LIU YE , WILKENING ROBERT R , NILSSON MARITA , HENSSEN CECILIA , SANIN ANDREI
IPC分类号： A61K31/343 , A61K31/05 , A61K31/10 , A61K31/122 , A61K31/15 , A61K31/352 , A61K31/357 , A61K31/385 , A61P3/02 , A61P3/04 , A61P3/06 , A61P5/30 , A61P9/00 , A61P9/10 , A61P15/08 , A61P19/00 , A61P19/08 , A61P19/10 , A61P25/28 , A61P35/00 , A61P37/02 , A61P43/00 , C07C35/37 , C07C35/44 , C07C39/17 , C07C39/42 , C07C49/727 , C07C49/737 , C07C49/747 , C07C251/44 , C07C323/17 , C07D307/94 , C07D311/96 , C07D317/72 , C07D339/06 , C07D339/08
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant inventive are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynecomastia, autoimmune disease, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer of the lung, colon, breast, uterus, and prrostate.

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