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51. 发明申请

WO2020164648A1 HETEROCYCLIC NITROGEN-CONTAINING PURINE DERIVATIVES, PHARMACEUTICAL PREPARATIONS CONTAINING THESE DERIVATIVES AND THEIR USE IN NEUROPROTECTION 审中-公开
公开(公告)号：WO2020164648A1
公开(公告)日：2020-08-20
申请号：PCT/CZ2020/050004
申请日：2020-01-27
申请人： UNIVERZITA PALACKEHO , FAKULTNI NEMOCNICE OLOMOUC
发明人： GONZALES, Gabriel , MIK, Vaclav , BUCHAROVA, Noemi , GRUZ, Jiri , KANOVSKY, Petr , STRNAD, Miroslav
IPC分类号： C07D473/16 , A61P25/16 , A61K31/52
摘要： The invention relates to heterocyclic nitrogen-containing purine derivatives, their use in the medicinal applications and compositions containing these derivatives. New generation of compounds possess selective antineurodegenerative properties on neuronal cells and tissues and can be particularly used in the treatment and prophylaxis of neurodegenerative disease, particularly in the treatment and prophylaxis of Parkinson's disease.

52. 发明申请

WO2019172835A1 CANCER TREATMENT WITH (2,2-BISHYDROXYMETHYL) METHYLENECYCLOPROPANE NUCLEOTIDES 审中-公开
公开(公告)号：WO2019172835A1
公开(公告)日：2019-09-12
申请号：PCT/SE2019/050209
申请日：2019-03-08
申请人： MEDIVIR AKTIEBOLAG
发明人： KLASSON, Björn , ÖBERG, Fredrik
IPC分类号： C07F9/6561 , A61K31/675 , A61P35/00 , C07F9/6512 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/522 , A61K31/685 , C07D239/36 , C07D239/54 , C07D473/16 , C07D473/18 , C07D473/30 , C07D473/34
摘要： The invention provides a compound of formula (I) wherein B is a nucleobase; U is O or S; R x is -OC(=O)R y , -OC(=O)CH(R y )NH 2 , -OCH 2 OC(=O)R y ; R y is optionally substituted alkyl or alkenyl or the side chain of a natural or unnatural amino acid R 1 is H, or optionally substituted phenyl, benzyl, naphthyl, pyridyl or indolyl, or R x and R 1 together define a bond thus forming a cyclic phosphate; R 2 and R 2' together define the side chain of a natural or unnatural amino acid; R 3 is optionally substituted alkyl, cycloalkyl, phenyl or benzyl; and pharmaceutically acceptable salts and compositions thereof which are useful in the treatment of cancer, especially leukemias.

53. 发明申请

WO2018138500A1 PROCESS FOR PREPARING PURINE DERIVATIVES 审中-公开
公开(公告)号：WO2018138500A1
公开(公告)日：2018-08-02
申请号：PCT/GB2018/050208
申请日：2018-01-25
申请人： CYCLACEL LIMITED
发明人： SKEAD, Ben , WESTWOOD, Robert , LONDESBROUGH, Derek , NORTHERN, Julian , ATHERTON, Chris
IPC分类号： C07D473/16 , A61P35/00 , A61K31/52
摘要： The present invention relates to a process for preparing a compound of formula [I], said process comprising the steps of: formula [II]+formula [III]−>formula [I] (i) forming a reaction mixture comprising (a) a compound of formula [II], (b) a compound of formula [III] and (c) 1,2-propanediol or polyethylene glycol, or a mixture thereof, and optionally (d) a base; (ii) heating said reaction mixture to a temperature of at least about 150°C to form a compound of formula [I]; (iii) isolating said compound of formula [I]; and (iv) optionally converting said compound of formula [I] into salt form; wherein: R 1 and R 2 are each independently H, alkyl or haloalkyl; R 3 and R 4 are each independently H, alkyl, haloalkyl or aryl; R 5 is alkyl, alkenyl, cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R 6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and formula (A) where one of X, Y and Z is N and the remainder are CR 9 ; R 7 , R 8 and each R 9 are independently H, alkyl or haloalkyl, wherein at least one of R 7 , R 8 and R 9 is other than H. Further aspects of the invention relate to a highly diastereoselective process for the preparation of compounds of formula [III], a process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I], and to a process for preparing the crystalline tartrate salt and free base of compounds of formula [I].

54. 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。

55. 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。

56. 发明申请

WO2016147185A1 ADENOSINE THIOPHOSPHATE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译：腺嘌呤硫代磷酸酯衍生物及其用途
公开(公告)号：WO2016147185A1
公开(公告)日：2016-09-22
申请号：PCT/IL2016/050288
申请日：2016-03-16
申请人： BAR-ILAN UNIVERSITY , RAMOT AT TEL-AVIV UNIVERSITY LTD.
发明人： FISCHER, Bilha , OFFEN, Daniel
IPC分类号： C07D405/14 , C07D473/24 , C07D473/34 , C07D473/40 , C07D473/16 , A61K31/66 , A61K31/52 , A61P25/28 , A61P39/00 , A61P39/04 , C07H19/167 , C07H19/20 , C07H21/02 , C07F9/02 , A61K31/7076
CPC分类号： C07H19/20 , A61K31/7076 , C07F9/65616
摘要： Novel adenosine 5'-thiophosphate derivatives, represented by Formulae (I) or (I*), and salts thereof, represented by Formulae (Ia) and (I*a), as defined in the specification, and uses thereof as antioxidants and/or P2Y 1 -R agonists, and/or in the treatment of medical conditions associated with oxidative stress and/or neurodegeneration, and in the treatment of Alzheimer's Disease in particular, are disclosed.
摘要翻译：由式（I）或（I *）表示的新型腺苷5'-硫代磷酸酯衍生物及其盐，其如本说明书中所定义的式（Ia）和（I * a）表示，及其用作抗氧化剂和/ 或P2Y1-R激动剂，和/或治疗与氧化应激和/或神经变性相关的医学病症，特别是治疗阿尔茨海默病。

57. 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。

58. 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。

59. 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。

60. 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。

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