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1. 发明申请

WO9633724A3 SELECTIVE MODULATORS OF PEROXISOME PROLIFERATOR ACSELECTIVE MODULATORS OF PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR-GAMMA, AND METHODS FOR THE USE THTIVATED RECEPTOR-GAMMA, AND METHODS FOR THE USE THEREOF EREOF 审中-公开
标题翻译：过氧化物酶体增殖物激活受体 - 游离体的过氧化物酶增效剂选择性调节剂的选择性调节剂及其使用的受体 - 游离体的方法及其使用方法
公开(公告)号：WO9633724A3
公开(公告)日：1997-01-30
申请号：PCT/US9605465
申请日：1996-04-18
申请人： SALK INST FOR BIOLOGICAL STUDI , EVANS ROLAND M , FORMAN BARRY M
发明人： EVANS RONALD M , FORMAN BARRY M
IPC分类号： G01N33/15 , A61K31/557 , A61K31/5575 , A61K45/00 , A61P3/04 , A61P3/06 , A61P3/08 , C12Q1/68
CPC分类号： A61K31/5575 , C12Q1/6897
摘要： In accordance with the present invention, there are provided a class of compounds which are capable of selectively modulating processes mediated by peroxisome proliferator activated receptor-gamma (PPAR-η). The identification of such compounds makes possible the selective intervention in PPAR-η mediated pathways, without exerting inadvertent effects on pathways mediated by other PPAR isoforms.

2. 发明申请

WO1996033724A2 SELECTIVE MODULATORS OF PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR-GAMMA, AND METHODS FOR THE USE THEREOF 审中-公开
标题翻译：过氧化物酶体增殖物激活受体 - 游离体选择性调节剂及其使用方法
公开(公告)号：WO1996033724A2
公开(公告)日：1996-10-31
申请号：PCT/US1996005465
申请日：1996-04-18
申请人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES , EVANS, Ronald, M. , FORMAN, Barry, M.
发明人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES
IPC分类号： A61K31/557
CPC分类号： A61K31/5575 , C12Q1/6897
摘要： In accordance with the present invention, there are provided a class of compounds which are capable of selectively modulating processes mediated by peroxisome proliferator activated receptor-gamma (PPAR- gamma ). The identification of such compounds makes possible the selective intervention in PPAR- gamma mediated pathways, without exerting inadvertent effects on pathways mediated by other PPAR isoforms.
摘要翻译：根据本发明，提供了一类能够选择性调节由过氧化物酶体增殖物激活受体-γ（PPAR-γ）介导的过程的化合物。这种化合物的鉴定使得可以选择性干预PPAR-γ介导的途径，而不会对由其他PPAR同种型介导的途径产生无意的影响。

3. 发明申请

WO1997035195A1 IN VITRO METHODS FOR IDENTIFYING MODULATORS OF MEMBERS OF THE STEROID/THYROID SUPERFAMILY OF RECEPTORS 审中-公开
标题翻译：用于鉴定受体的STEROID / THYROID SUPERFAMILY的成员的调节剂的体外方法
公开(公告)号：WO1997035195A1
公开(公告)日：1997-09-25
申请号：PCT/US1997004315
申请日：1997-03-19
申请人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES , EVANS, Ronald, M. , FORMAN, Barry, M.
发明人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES
IPC分类号： G01N33/53
CPC分类号： G01N33/743 , G01N2333/723
摘要： In accordance with the present invention, there are provided in vitro methods for the large scale identification of modulators of members of the steroid/thyroid superfamily of receptors. Invention methods can be rapidly carried out employing large numbers of compounds per screen, thereby facilitating evaluation of large libraries of compounds in a relatively short time. Modulators identified employing invention methods are capable of activating a receptor species in the optional presence of one or more of: a heterodimerizing partner therefor, a co-activator (or co-suppressor), and/or a hormone response element; or of disrupting the activity of a receptor species in the presence or absence of one or more of: a heterodimerizing partner therefor, a co-activator (or co-suppressor), and/or a hormone response element.
摘要翻译：根据本发明，提供了用于大规模鉴定受体类固醇/甲状腺超家族成员调节剂的体外方法。本发明的方法可以在每个筛选中使用大量化合物进行快速进行，从而有助于在较短的时间内评估大型化合物文库。使用本发明方法鉴定的调节剂能够在任选存在一种或多种：异二聚体伴侣，共活化剂（或共抑制剂）和/或激素反应元件的情况下活化受体物质; 或者在存在或不存在以下的一种或多种的异二聚体伴侣，共活化剂（或共抑制剂）和/或激素反应元件的情况下破坏受体物质的活性。

4. 发明申请

WO1996036230A1 MODULATORS FOR NEW MEMBERS OF THE STEROID/THYROID SUPERFAMILY OF RECEPTORS 审中-公开
标题翻译： STEROID / THYROID SUPERFAMILY受体的新成员的调节剂
公开(公告)号：WO1996036230A1
公开(公告)日：1996-11-21
申请号：PCT/US1996003865
申请日：1996-04-17
申请人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES , EVANS, Ronald, M. , FORMAN, Barry, M.
发明人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES
IPC分类号： A16K31/56
CPC分类号： A61K31/568
摘要： In accordance with the present invention, there are provided modulators for orphan member(s) of the steroid/thyroid superfamily of receptors which is related to the previously described CAR- alpha . Thus, compounds of the general class of androstans have been identified as modulators for a newly discovered isoform of CAR. Compounds discovered in accordance with the present invention can be employed in a variety of applications, e.g., for the modulation of processes mediated by an isoform of CAR or CAR-like species, to increase the libido of a subject (especially a subject undergoing therapy using a 5 alpha -reductase inhibitor), in a screening assay for the presence of receptors involved in the modulation of libido, and the like. Also provided in accordance with the present invention are methods for the identification of compounds which modulate processes mediated by an isoform of CAR or CAR-like species, as well as novel compositions derived therefrom.
摘要翻译：根据本发明，提供了与先前描述的CAR-α相关的受体类固醇/甲状腺超家族的孤儿成分的调节剂。因此，一般类型的雄激素类化合物已被鉴定为新发现的CAR同种型的调节剂。根据本发明发现的化合物可以用于各种应用，例如用于调节由CAR或CAR样物质的同种型介导的过程，以增加受试者的性欲（特别是接受治疗的受试者使用 5α-还原酶抑制剂），在涉及调节性欲的受体的存在的筛选测定中等。根据本发明还提供了用于鉴定调节由CAR或CAR样物质的同种型介导的过程的化合物的方法，以及由其衍生的新型组合物。

5. 发明申请

WO1998029120A1 TREATMENT OF LIPOSARCOMAS USING A COMBINATION OF THIAZOLIDINEDIONES AND RETINOID X RECEPTOR SELECTIVE AGONISTS 审中-公开
标题翻译：使用噻唑烷二酮和赖氨酸X受体选择性激素的组合治疗脂蛋白
公开(公告)号：WO1998029120A1
公开(公告)日：1998-07-09
申请号：PCT/US1997024187
申请日：1997-12-29
申请人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES , EVANS, Ronald, M. , TOTONOZ, Peter , SPIEGELMAN, Bruce, M. , FORMAN, Barry, M.
发明人： THE SALK INSTITUTE FOR BIOLOGICAL STUDIES
IPC分类号： A61K31/44
CPC分类号： A61K45/06 , A61K31/426 , A61K31/4406 , A61K2300/00
摘要： In accordance with the present invention, it has been discovered that PPAR gamma is expressed consistently in each of the major histologic types of human liposarcoma. It has further been discovered that maximal activation of PPAR gamma with exogenous ligand (a thiazolidinedione or derivative thereof) promotes terminal differentiation of primary human liposarcoma cells. It has still further been discovered that RXR-specific ligands are also potent adipogenic agents in cells expressing the PPAR gamma /RXR alpha heterodimer, and that simultaneous treatment of liposarcoma cells with a thiazolidinedionyl moiety (a PPAR gamma -selective class of compounds) and an RXR-specific ligand results in an additive stimulation of differentiation. Accordingly, according to the invention, there have been identified compositions which are useful for the treatment of liposarcomas.
摘要翻译：根据本发明，已经发现PPARγ在人脂肪肉瘤的主要组织学类型中均一致地表达。进一步发现外源配体（噻唑烷二酮或其衍生物）对PPARγ的最大活化促进原代人脂肪肉瘤细胞的终末分化。还进一步发现RXR特异性配体在表达PPARγ/RXRα异源二聚体的细胞中也是有效的成脂剂，并且用噻唑烷二酰基部分（PPARγ选择类化合物）同时治疗脂肪肉瘤细胞和 RXR特异性配体导致分化的加性刺激。因此，根据本发明，已经鉴定了可用于治疗脂肪肉瘤的组合物。

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