31 results about "Casein kinase 1" patented technology

Methods relating to selective inhibitors of the casein kinase 1 isoforms that are useful for the treatment of inflammatory diseases are presented.

The invention discloses a novel substituted pyrazolopyrimidine compound for inhibiting the activity of casein kinase 1[epsilon] (CK1[epsilon]), a stereoisomer or a stereoisomer mixture of the novel substituted pyrazolopyrimidine compound, a pharmaceutically acceptable salt or solvate of the novel substituted pyrazolopyrimidine compound, and application of the compound to preparation of medicine for treating diseases, disorders or symptoms benefiting from the inhibition of the activity of casein kinase 1[epsilon] (CK1[epsilon]). The compound has inhibitory activity on CK1[epsilon] kinase, OCI-LY10 cells and Karpas299 cells, shows good anti-tumor activity in an OCI-LY10 subcutaneous xenogeneic model, shows excellent synergistic anti-tumor activity when being combined with a BTK inhibitor, has good pharmacokinetic properties, and can be applied to treatment of diseases, disorders or symptoms, including cancers, autoimmune diseases and the like, which benefit from inhibition of casein kinase 1[epsilon] activity, alone or in combination with other drugs.

The invention provides an application of promoting the expression of an I-type interferon by inhibiting the activity of casein kinase 2. Specifically, the invention relates to the applications of casein kinase 2 (CK2) inhibitor: (i) in preparing medicinal compositions for promoting the expression of the I-type interferon (I-IFN) and/or the expression of I-IFN-induced genes or proteins thereof; and/or (ii) in preparing medicinal compositions for treating relevant diseases due to lack of I-IFN. The experiment proves that the inhibition on the CK2 can effectively induce and promote the generation of the I-IFN, and activate the expression of the downstream genes of the I-IFN, thus achieving good treatment effects for the relevant diseases due to lack of the I-IFN.

A transgenic plant transformed by a casein kinase Stress-Related Polypeptide (CKSRP) coding nucleic acid, wherein expression of the nucleic acid sequence in the plant results in increased tolerance to environmental stress as compared to a wild type variety of the plant. Also provided are agricultural products, including seeds, produced by the transgenic plants. Also provided are isolated CKSRPs, and isolated nucleic acid coding CKSRPs, and vectors and host cells containing the latter.

The present invention provides pyrazole derivatives of Formula (I), and in particular N1-(4-(5-(cyclopropylmethyl)-1-methyl-lH-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and relatedcompounds as casein kinase 1 (CK1) and/or interleukin 1 receptor associated kinase 1 (IRAKI) inhibitors for treating cancer, inflammatory and immune related disorders.

This invention relates to a method for inducing or enhancing the differentiation of pluripotent stem cells into cardiomyocyte via casein kinase 1 inhibition said method comprising culturing the stem cells in the presence of a medium comprising a casein kinase 1 inhibitor of the formula (I) or (II) or a stereoisomer, tautomer, or a salt thereof wherein R¹, R² and R³ independently from another represent hydrogen, optionally substituted alkyl, alkenyl, alkynyl, heterocyclyl, heteroaryl or aryl; X represents NR⁴, O or S; and R⁴ represents hydrogen, optionally substituted alkyl, alkenyl, alkynyl, heterocyclyl, heteroaryl or aryl. The method can be used in the late phase of stem cell differentiation and in the compounds of formula (I) or (II) in combination with other small molecules can lead to especially high differentiation of stem cells into cardiomyocytes. The invention further relates to novel compounds which can be used in the method of the invention and kits for stem cell differentiation.

An object of the present invention is to provide a method for preparing osteoblasts that are applicable, without causing risk of canceration, to bone defect repair or to the treatment of bone resorption, fracture, osteoporosis, or the like. To solve this problem, the present invention provides a method for preparing osteoblasts, the method comprising culturing mammal differentiated somatic cells in a medium in the presence of at least one compound selected from the group consisting of (1) statin compounds, (2) casein kinase 1 inhibitors, (3) cAMP inducers, and (4) histone methyltransferase inhibitors, to convert the somatic cells into osteoblasts.

Methods and related compositions are disclosed for treating an array of myeloproliferative disorders and hematological malignancies. In particular, treatment methods and compositions for treating chronic myelogenous leukemia are disclosed. The methods and compositions utilize certain casein kinases, and specifically CK2α agents.

The invention provides an application of a casein kinase PPK related to the growth and development of plants. The casein kinase PPK is PPK1, PPK2, PPK3 or PPK4, and the sequence registration numbers thereof are At3G13670, At5G18190, At3G03940 and At2G25760 respectively. The casein kinase PPK is used for improving the growth and development of the plants, and then is applied to crop production.

The invention provides a method of inhibiting casein kinase 1 DETA (CK1 DETA), comprising contacting the CK1 DETA 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 CK1 delta 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 CK1 DETA and BETA-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.

There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1δ and casein kinase 1ε. In addition, the present inhibitor inhibits casein kinase 1δ and casein kinase 1ε, and thus there is also provided a pharmaceutical agent useful for the treatment and/or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1δ or casein kinase 1ε is associated. There is further provided a pharmaceutical agent useful for the treatment of particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer.

An inhibitor of casein kinase 1δ and casein kinase 1ε comprising, as an act ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof:

wherein X represents a halogen atom (which may be any one of a fluorine atom, a chlorine atom, a bromine atom, and an iodine atom).

The present invention aims to provide a brown adipocyte and a generation method thereof, a transplantation material containing a brown adipocyte, a prophylactic agent or therapeutic agent containing a brown adipocyte for various diseases and conditions, and use thereof. Provided is a method for generating a brown adipocyte, including converting a differentiated somatic cell of a mammal to a brown adipocyte by culturing the somatic cell in a medium in the presence of at least one kind of a compound selected from the group consisting of (1) a TGFβ/SMAD pathway inhibitor, (2) a casein kinase 1 inhibitor, (3) a cAMP inducer and (4) a MEK/ERK pathway inhibitor.

The present invention relates to the use of casein kinase 1 inhibitors for treating vascular diseases, preferably peripheral vascular diseases, and to corresponding treatment methods.