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1. 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。

2. 发明申请

WO2017021716A1 ANTIVIRAL 4-(2-AMINO-6-HETEROCYLYL-9H-PURIN-9-YL)-2-CYCLOPENTENE-1 -METHANOL COMPOUNDS 审中-公开
标题翻译：抗坏血酸4-（2-氨基-6-杂环基-9H-嘌呤-9-基）-2-环戊烯-1-甲醇化合物
公开(公告)号：WO2017021716A1
公开(公告)日：2017-02-09
申请号：PCT/GB2016/052356
申请日：2016-07-29
申请人： THE UNIVERSITY OF LIVERPOOL
发明人： O'NEILL, Paul , BERRY, Neil
IPC分类号： C07D473/16 , A61K31/52 , A61P31/18
CPC分类号： C07D473/16
摘要： The present invention relates to certain antiviral compounds of formula I as defined herein that function as nucleoside reverse transcriptase inhibitors. The present invention also relates to processes for the preparation of these compounds, pharmaceutical compositions comprising them and to their use for the treatment of retroviral infections, and in particular their use in the treatment of HIV-1 virus.
摘要翻译：本发明涉及用作核苷逆转录酶抑制剂的某些本文所定义的式I的抗病毒化合物。本发明还涉及制备这些化合物的方法，包含它们的药物组合物及其用于治疗逆转录病毒感染的用途，特别是其用于治疗HIV-1病毒。

3. 发明申请

WO2016160617A2 INHIBITORS OF CYCLIN-DEPENDENT KINASES 审中-公开
标题翻译：循环依赖激素的抑制剂
公开(公告)号：WO2016160617A2
公开(公告)日：2016-10-06
申请号：PCT/US2016/024345
申请日：2016-03-25
申请人： DANA-FARBER CANCER INSTITUTE, INC.
发明人： GRAY, Nathanael, S. , ZHANG, Tinghu , KWIATKOWSKI, Nicholas, Paul
IPC分类号： A61K31/52 , A61K31/519
CPC分类号： A61K45/06 , C07D473/16 , C07D473/34 , C07D487/04 , C07K14/4738
摘要： The present invention provides novel compounds of Formula (I), (II), or (III), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., CDK7, CDK12, or CDK13), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
摘要翻译：本发明提供新的式（I），（II）或（III）化合物及其药学上可接受的盐，溶剂合物，水合物，多晶型物，共晶体，互变异构体，立体异构体，同位素标记的衍生物，前药及其组合物。还提供了涉及用于治疗和/或预防增殖性疾病（例如，癌症（例如白血病，急性淋巴细胞白血病，淋巴瘤，伯基特淋巴瘤，黑素瘤，多发性骨髓瘤，乳腺癌，尤因氏肉瘤，骨肉瘤）的本发明化合物或组合物的方法和试剂盒，脑癌，卵巢癌，神经母细胞瘤，肺癌，结肠直肠癌），良性肿瘤，与血管生成相关的疾病，炎性疾病，自身炎性疾病和自身免疫性疾病）。使用本发明的化合物或组合物治疗具有增殖性疾病的受试者可以抑制激酶例如细胞周期蛋白依赖性激酶（CDK）（例如CDK7，CDK12或CDK13）的异常活性，因此诱导细胞凋亡和/或抑制受试者的转录。

4. 发明申请

WO2016091916A1 PYRAZOLYLAMINOPURINES AS ITK INHIBITORS 审中-公开
标题翻译：作为ITK抑制剂的吡唑啉酰胺
公开(公告)号：WO2016091916A1
公开(公告)日：2016-06-16
申请号：PCT/EP2015/079043
申请日：2015-12-09
申请人： F. HOFFMANN-LA ROCHE AG , GENENTECH, INC.
发明人： BURCH, Jason , ORTWINE, Daniel , PEI, Zhonghua
IPC分类号： C07D473/16 , C07D473/34 , A61K31/52 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P37/00
CPC分类号： C07D473/16 , C07D473/34
摘要： Provided are pyrazolylaminopurine compounds that are inhibitors of ITK kinase, compositions containing these compounds and methods for treating diseases mediated by ITK kinase. In particular, provided are compounds of Formula I or II, stereoisomers, tautomers, solvates, prodrugs or pharmaceutically acceptable salts thereof, where n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are defined herein, pharmaceutical compositions comprising the compound and a pharmaceutically acceptable carrier, methods of using the compound or composition in therapy, for example, for treating a disease or condition mediated by ITK kinase in a patient.
摘要翻译：提供的是作为ITK激酶抑制剂的吡唑基氨基嘌呤化合物，含有这些化合物的组合物和用于治疗由ITK激酶介导的疾病的方法。特别地，提供式I或II的化合物，其立体异构体，互变异构体，溶剂合物，前药或其药学上可接受的盐，其中n，R 1，R 2，R 3，R 4，R 5，R 6和R 7在本文中定义，药物组合物包含化合物和药学上可接受的载体，在治疗中使用该化合物或组合物的方法，例如用于治疗患者中ITK激酶介导的疾病或病症。

5. 发明申请

WO2015175813A1 HETEROCYCLIC HYDROXAMIC ACIDS AS PROTEIN DEACETYLASE INHIBITORS AND DUAL PROTEIN DEACETYLASE-PROTEIN KINASE INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：作为蛋白质脱乙酰酶抑制剂和双蛋白脱乙酰壳多糖酶蛋白激酶抑制剂的杂环羟基酸及其使用方法
公开(公告)号：WO2015175813A1
公开(公告)日：2015-11-19
申请号：PCT/US2015/030842
申请日：2015-05-14
申请人： THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE
发明人： LIU, Xuedong , ZHANG, Gan , CHAN, Daniel, Chuen-Fong , PISCOPIO, Anthony, D.
IPC分类号： A61K31/165
CPC分类号： C07D513/04 , C07D473/16 , C07D473/34 , C07D487/04
摘要： The present invention relates to novel hydroxamic acids which are specific histone deacetylase (HDAC) inhibitors and/or TTK/Mpsl kinase inhibitors, including pharmaceutically acceptable salts thereof, which are useful for modulating HDAC and/or TTK/Mpsl kinase activity, pharmaceutical compositions comprising these compounds, and processes for their preparation.
摘要翻译：本发明涉及可用于调节HDAC和/或TTK / Mps1激酶活性的特异性组蛋白脱乙酰酶（HDAC）抑制剂和/或TTK / Mps1激酶抑制剂（包括其药学上可接受的盐）的新型异羟肟酸，其包含这些化合物及其制备方法。

6. 发明申请

WO2015106624A1 2，4(1H，3H)-嘧啶二酮衍生物及其制备方法审中-公开
公开(公告)号：WO2015106624A1
公开(公告)日：2015-07-23
申请号：PCT/CN2014/095255
申请日：2014-12-29
申请人：四川大学华西医院
发明人：黄文
IPC分类号： C07D473/08 , C07D473/04 , C07D473/10 , C07D473/06 , C07D473/12 , C07D519/00 , C07D473/30 , C07D239/54 , C07D239/553 , C07D239/58 , C07D239/48 , C07D473/16
CPC分类号： C07D239/48 , C07D239/54 , C07D239/553 , C07D239/58 , C07D473/04 , C07D473/06 , C07D473/08 , C07D473/10 , C07D473/12 , C07D473/16 , C07D473/30 , C07D519/00
摘要：本发明涉及3，7-二氢-1，3，7-三甲基-1H-咪唑[4，5-d]嘧啶-2，6-二酮、1，7-二氢-6H-咪唑[4，5-d]嘧啶-6-酮和2，4(1H，3H)-嘧啶二酮衍生物及其制备方法。

7. 发明申请

WO2014121764A3 2-SUBSTITUTED-6-BIARYLMETHYLAMINO-9-CYCLOPENTYL-9H-PURINE DERIVATIVES, USE THEREOF AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译： 2-取代-6-芳基甲基氨基-9-环戊基-9H-嘌呤衍生物，其用作药物和药物组合物
公开(公告)号：WO2014121764A3
公开(公告)日：2014-10-16
申请号：PCT/CZ2014000014
申请日：2014-02-05
申请人： UNIVERZITA PALACKEHO V OLOMOUCI , BIOPATTERNS S R O
发明人： GUCKY TOMAS , JORDA RADEK , ZATLOUKAL MAREK , KRYSTOF VLADIMIR , RAROVA LUCIE , REZNICKOVA EVA , MIKULITS WOLFGANG , STRNAD MIROSLAV
IPC分类号： C07D473/16 , A61K31/52 , A61P35/00
CPC分类号： C07D473/40 , A61K31/44 , A61K31/704 , A61K33/24 , C07D473/16 , A61K2300/00
摘要： This invention relates to novel 2-substituted-6-biarylmethylamino-9-cyclopentyl-9H-purine derivatives, showing activity as specific inhibitors of growth and angiogenesis of hepatocellular carcinoma. The invention further includes pharmaceutical compositions containing the 2-substituted-6-biarylmethylamino-9-cyclopentylpurines.
摘要翻译：本发明涉及新的2-取代-6-联芳基甲基氨基-9-环戊基-9H-嘌呤衍生物，显示出作为肝细胞癌生长和血管生成的特异性抑制剂的活性。本发明还包括含有2-取代-6-联芳基甲基氨基-9-环戊基嘌呤的药物组合物。

8. 发明申请

WO2014135473A1 INHIBITORS OF BRUTON'S TYROSINE KINASE 审中-公开
标题翻译： BRUTON的酪氨酸激酶抑制剂
公开(公告)号：WO2014135473A1
公开(公告)日：2014-09-12
申请号：PCT/EP2014/054017
申请日：2014-03-03
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DE VICENTE FIDALGO, Javier , DOMINIQUE, Romyr , LOPEZ-TAPIA, Francisco Javier , SO, Sung-Sau
IPC分类号： C07D473/16 , C07D473/34 , A61K31/52 , A61P11/06
CPC分类号： C07D473/34 , A61K31/52 , C07D473/16
摘要： This application discloses compounds according to generic Formula (I) wherein all variables are defined as described herein, which inhibit BTK. The compounds disclosed herein are useful to modulate the activity of BTK and treat diseases associated with excessive BTK activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
摘要翻译：本申请公开了根据通式（I）的化合物，其中所有变量如本文所述限定，其抑制BTK。本文公开的化合物可用于调节BTK的活性并治疗与过量BTK活性相关的疾病。该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，例如类风湿性关节炎。还公开了含有式（I）化合物和至少一种载体，稀释剂或赋形剂的组合物。

9. 发明申请

WO2014121764A2 2-SUBSTITUTED-6-BIARYLMETHYLAMINO-9-CYCLOPENTYL-9H-PURINE DERIVATIVES, USE THEREOF AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译： 2-取代的6-二氨基甲酰氨基-9-环丙基-9H-嘌呤衍生物，其作为药物和药物组合物的用途
公开(公告)号：WO2014121764A2
公开(公告)日：2014-08-14
申请号：PCT/CZ2014/000014
申请日：2014-02-05
申请人： UNIVERZITA PALACKEHO V OLOMOUCI , BIOPATTERNS S.R.O.
发明人： GUCKY, Tomas , JORDA, Radek , ZATLOUKAL, Marek , KRYSTOF, Vladimir , RAROVA, Lucie , REZNICKOVA, Eva , MIKULITS, Wolfgang , STRNAD, Miroslav
CPC分类号： C07D473/40 , A61K31/44 , A61K31/704 , A61K33/24 , C07D473/16 , A61K2300/00
摘要： This invention relates to novel 2-substituted-6-biarylmethylamino-9-cyclopentyl-9H-purine derivatives, showing activity as specific inhibitors of growth and angiogenesis of hepatocellular carcinoma. The invention further includes pharmaceutical compositions containing the 2-substituted-6-biarylmethylamino-9-cyclopentylpurines.
摘要翻译：本发明涉及新型2-取代-6-联芳基甲基氨基-9-环戊基-9H-嘌呤衍生物，显示作为肝细胞癌生长和血管发生的特异性抑制剂的活性。本发明还包括含有2-取代-6-联芳基甲基氨基-9-环戊基嘌呤的药物组合物。

10. 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。

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