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1. 发明申请

WO2016118825A1 HETEROCYCLIC INHIBITORS OF MONOCARBOXYLATE TRANSPORTERS 审中-公开
标题翻译：单羟基苯甲酸酯运输商的杂环抑制剂
公开(公告)号：WO2016118825A1
公开(公告)日：2016-07-28
申请号：PCT/US2016/014461
申请日：2016-01-22
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： BANNISTER, Thomas, D. , ROUSH, William, R. , CHOI, Jun, Yong , NAIR, Reji , TSAI, Andy, S. , MISHRA, Jitendra, K. , CLEVELAND, John, L.
IPC分类号： A61K31/519 , A61P35/00 , C07D495/04
CPC分类号： C07D495/04 , A61K31/155 , A61K31/5025 , A61K31/519 , C07D487/04 , A61K2300/00
摘要： The invention provides compounds that inhibit monocarboxylate transporters, such as MCT1 and MCT4. Compounds of the invention can be used for treatment of a condition in a patient, wherein the condition is characterized by the heightened activity or by the high prevalence of MCT1 and/or MCT4, such as cancer or type II diabetes.
摘要翻译：本发明提供抑制单羧酸转运体如MCT1和MCT4的化合物。本发明的化合物可用于治疗患者的病症，其中所述病症的特征在于活动增高或由高表达的MCT1和/或MCT4，如癌症或II型糖尿病。

2. 发明申请

WO2019217421A1 SMALL MOLECULE INHIBITORS OF CDK12/CDK13 审中-公开
公开(公告)号：WO2019217421A1
公开(公告)日：2019-11-14
申请号：PCT/US2019/031116
申请日：2019-05-07
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： ROUSH, William, R. , DUCKETT, Derek , MONASTYRSKYI, Andrii
IPC分类号： C07D401/14 , C07D471/04 , C07D487/04
摘要： The invention provides compounds and methods of inhibiting a cyclin-dependent kinase, comprising contacting the cyclin-dependent kinase and an effective amount or concentration of a compound of formula (I) wherein variables are as defined herein. Compounds of formula (I) can be highly selective inhibitors of cyclin-dependent kinases such as CDK12/13, relative to other kinases such as casein kinases, such as CK1δ/ε. Compounds can be used in treatment of cancers, such as breast cancer, brain cancer and ovarian cancer.

3. 发明申请

WO2017066055A1 THERAPEUTIC TARGETING OF CASEIN KINASE 1δ IN BREAST CANCER 审中-公开
标题翻译：酪蛋白激酶1δ在乳腺癌治疗中的应用
公开(公告)号：WO2017066055A1
公开(公告)日：2017-04-20
申请号：PCT/US2016/055436
申请日：2016-10-05
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： ROUSH, William, R. , DUCKETT, Derek, R. , CLEVELAND, John, L. , ROSENBERG, Laura, H.
IPC分类号： C07D473/32 , C07D473/16
CPC分类号： C07D473/16
摘要： The invention provides a method of inhibiting casein kinase 1δ (CK1δ), comprising contacting the CK1δ with a compound of formula (I), as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that CK1δ can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1δ and β-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.
摘要翻译：本发明提供了抑制酪蛋白激酶1δ（CK1δ）的方法，包括使CK1δ与本文定义的式（I）化合物接触; 如复合SR-3029。我们证明CSNK1D在人乳腺肿瘤中被扩增和/或过表达，并且CK1δ可以在过度表达该激酶的人乳腺癌亚型中医学靶向。本发明进一步提供了治疗癌症例如乳腺癌，黑素瘤，成胶质细胞瘤，成神经管细胞瘤，肾，膀胱或结肠癌或转移至脑，肺或骨的癌症的方法，前提是CK1δ和β- 连环蛋白依赖性参与了这些转移性疾病。癌症可以是乳腺癌三阴性亚型（TNBC）的乳腺癌，或者可以是HER +乳腺癌。

4. 发明申请

WO2017053510A1 SMALL MOLECULE MODULATORS OF CELLULAR LIPOLYSIS 审中-公开
标题翻译：小分子细胞调节因子
公开(公告)号：WO2017053510A1
公开(公告)日：2017-03-30
申请号：PCT/US2016/053005
申请日：2016-09-22
申请人： THE SCRIPPS RESEARCH INSTITUTE , WAYNE STATE UNIVERSITY
发明人： ROUSH, William, R. , GRANNEMAN, James, G. , HALVORSEN, Geoff, T.
IPC分类号： A61K36/82 , A61P3/04
CPC分类号： A61K31/554 , A61K31/496
摘要： The invention provides a compound which binds ABHD5, disrupts complexes of ABHD5 and PLJN1 or PLIN5, and stimulates cellular lipolysis. The compound can be used, in an effective dose, to promote fat catabolism. Consequently, the invention also provides a method of treatment of obesity, diabetes, cardiovascular disease, or cancer when an effective amount of the compound is administered to a patient. The invention further provides a method of treatment of icthyosis and a method of increasing the content in skin of skin barrier lipids, comprising applying an effective amount or concentration of the compound topically.
摘要翻译：本发明提供了结合ABHD5的化合物，破坏ABHD5和PLJN1或PLIN5的复合物，并刺激细胞脂肪分解。该化合物可以以有效剂量用于促进脂肪分解代谢。因此，本发明还提供了当向患者施用有效量的化合物时，治疗肥胖症，糖尿病，心血管疾病或癌症的方法。本发明还提供了一种治疗荨麻疹的方法和增加皮肤屏障脂质含量的方法，包括局部施用有效量或浓度的化合物。

5. 发明申请

WO2013130461A1 WEE1 DEGRADATION INHIBITORS 审中-公开
标题翻译： WEE1降解抑制剂
公开(公告)号：WO2013130461A1
公开(公告)日：2013-09-06
申请号：PCT/US2013/027784
申请日：2013-02-26
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： ROUSH, William, R. , AYAD, Nagi , RAHAIM, Ronald , SIMANSKI, Scott, P. , BIBIAN, Mathieu
IPC分类号： A01N43/90 , A61K31/52
CPC分类号： C07D473/32 , C07D473/16 , C07D473/34 , C07D519/00
摘要： The invention provides compounds that inhibit the degradation of Weel. The compounds of the present invention are generally N-((1H -benzo [d ]imidazol-2- yl)methyl)- 9H -purin-6-amines. Compounds of the invention can be used for treatment of malconditions in patients for which inhibition of Weel is medically indicated, for example cancer, Alzheimer's, neurological disorders, psychiatric disorders, or inflammation-related disorders.
摘要翻译：本发明提供抑制Weel降解的化合物。本发明的化合物通常是N - （（1H-苯并[d]咪唑-2-基）甲基）-9H-嘌呤-6-胺。本发明的化合物可用于治疗在医学上指示Weel的抑制的患者中的病情，例如癌症，阿尔茨海默氏症，神经障碍，精神病学障碍或炎症相关疾病。

6. 发明申请

WO2008134432A1 PROTEINASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译：蛋白酶抑制剂及其用途
公开(公告)号：WO2008134432A1
公开(公告)日：2008-11-06
申请号：PCT/US2008/061427
申请日：2008-04-24
申请人： THE SCRIPPS RESEARCH INSTITUTE , ROUSH, William, R. , CHEN, Yen, Ting , MCKERROW, James, H.
发明人： ROUSH, William, R. , CHEN, Yen, Ting , MCKERROW, James, H.
IPC分类号： A61K38/00 , C07D295/00
CPC分类号： C07D295/215 , A61K38/00 , Y02A50/414
摘要： Compositions of inhibitors of proteases are identified. Methods of preventing and treating diseases associated with proteases comprise administering one or more inhibitors to a subject.
摘要翻译：鉴定蛋白酶抑制剂的组成。预防和治疗与蛋白酶相关疾病的方法包括向受试者施用一种或多种抑制剂。

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