105 results about "PTK Inhibitors" patented technology

The present invention relates to compounds of formula (I) below, or any one of its pharmaceutically acceptable salts: [Formula 1] JPEG2023523788000127.jpg41170 where R 1 is (C1-C6) alkyl group, spiro (C5-C 11 ) bicyclic rings, fused phenyl groups, substituted phenyl groups, R'-L- groups, where L is either a single bond or a (C1-C3) alkanediyl group, and R' is a (C3-C8) cycloalkyl group, a bridged (C6-C 10 ) cycloalkyl group, (C3-C8) heterocycloalkyl group, or (C3-C8) heteroaryl group, or R'-L- group, where L is a (C1-C3) alkanediyl group and R' is an optionally substituted phenyl group, and R 2 represents a hydrogen atom or a (C1-C3) alkyl group. The present invention further relates to compositions comprising the compound of formula (I), as well as methods for preparing the compound and synthetic intermediates thereof. The present invention also relates to the compound for use as a pharmaceutical, in particular for treating and / or preventing cognitive impairment associated with Down's syndrome; Alzheimer's disease; dementia; tauopathies; Parkinson's disease; CDKL5 deficiency disorders; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; folate and methionine metabolism disorders; osteoarthritis; Duchenne muscular dystrophy; some cancers; neuroinflammation, anemia, and viral and unicellular infections, and for regulating body temperature.

Disclosed are a series of isoquinolone derivatives as ROCK protein kinase inhibitors and uses thereof in preparing medicaments for ROCK protein kinase inhibitor-related glaucoma or ocular hypertension diseases. Specially, disclosed are a compound of formula (I), an isomer thereof or a pharmaceutically acceptable salt thereof.

The invention provides a cyclic compound with a structure as shown in a formula (I) or a pharmaceutically acceptable salt or a stereoisomer or a prodrug molecule of the cyclic compound, and a pharmaceutical composition and application of the cyclic compound or the pharmaceutically acceptable salt or the stereoisomer or the prodrug molecule of the cyclic compound. The compound can be used as a protein kinase inhibitor, has very strong inhibitory activity on FLT3 mutant kinase, has very strong proliferation inhibitory activity on Ba / F3-FLT3-ITD and stable strain cells containing drug-resistant point mutation, can inhibit proliferation, migration and invasion of various tumor cells, and especially can overcome the drug resistance of existing clinical drugs. The cyclic compound provided by the invention can be used for preparing medicines for preventing or treating FLT3 tyrosine kinase mediated diseases (such as hematological malignancies), and can be used for treating various hematological malignancies of human beings and other mammals. # imgabs0 #

To provide IRAK degraders and uses thereof.SOLUTION: The present invention provides compounds, compositions thereof, and methods of using the same. The compounds include an IRAK binding moiety capable of binding to IRAK4 and a degradation inducing moiety (DIM). The DIM could be DTM, a ligase binding moiety (LBM) or lysine mimetic. The compounds could be useful as IRAK protein kinase inhibitors and applied to IRAK mediated disorders. Compounds of the present invention, and compositions thereof, are useful as degraders and / or inhibitors of one or more IRAK protein kinases. In some embodiments, a provided compound degrades and / or inhibits IRAK-1 / 2 / 3 / 4.SELECTED DRAWING: None

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

The invention relates to a preparation method and application of a novel CDK12 / 13 covalent inhibitor substituted by a fused ring structure or a pharmaceutical composition of the novel CDK12 / 13 covalent inhibitor. The novel CDK12 / 13 covalent inhibitor with the substituted ring-fused structure has a structure as shown in a formula (I), can be used as a protein kinase inhibitor, can effectively and highly selectively inhibit the activity of CDK12 / 13 protein kinase, and can inhibit proliferation, migration and invasion of various tumor cells. # imgabs0 #

The present invention relates to a preparation method for a novel CDK12 / 13 covalent inhibitor having a fused ring structure substituent or a pharmaceutical composition thereof and the use thereof. The novel CDK12 / 13 covalent inhibitor having a fused ring structure substituent has a structure shown as formula (I), and the compound can be used as a protein kinase inhibitor, can effectively and highly selectively inhibit the activity of CDK12 / 13 protein kinase, and can inhibit the proliferation, migration and invasion of a plurality of tumor cells.

Provided is a 1H-imidazo[4,5-h]quinazoline compound of formula (I). The compound is a broad spectrum inhibitor having strong activity for cyclin-dependent kinase (CDK) and is applicable in treating cell proliferative disorder

The invention relates to a compound used as a CDK2 / 4 protein kinase inhibitor and application thereof. Specifically, the invention discloses a compound shown as a formula I, or pharmaceutically acceptable salt, stereoisomer, tautomer, hydrate, solvate, isotope compound or prodrug thereof, and the definitions of all groups and substituent groups are described in the specification. The compound provided by the invention can be used as an inhibitor of cyclin dependent kinase (CDK), and is used for preventing or treating cell proliferative diseases and symptoms including various cancers, in particular for regulating and / or treating related diseases caused by overexpression and / or abnormal activity of the cyclin dependent kinase CDK2 / 4. # imgabs0 #

The present invention provides methods for treating patients with ccRCC and other VHL(−) cancers, the method comprising administering to the patient a therapeutically effective amount of a protein kinase inhibitor and a therapeutically effective amount of at least a second agent comprising bisantrene or a derivative thereof, or a pharmaceutically acceptable salt of bisantrene or derivative thereof. Also provided by the present invention are pharmaceutical compositions and kits for the treatment of ccRCC and other VHL(−) cancers as well as the use of such compositions for the manufacture of medicaments for the treatment of ccRCC and other VHL(−) cancers.

The present application relates to a kind of polymorphs of FGFR4 protein kinase inhibitor and its preparation method.N-(2-(4-cyclopropylpiperazine-1-yl)-5-(4-(2,6-dichloro-3,5-dimethoxyphenyl)imidazo [1,2-a][1,6] naphthyridin-8-yl)-4-methoxyphenyl) acrylamide is a kind of FGFR4 protein kinase inhibitor, it can high selectivity inhibit FGFR4 tyrosine kinase, and the inhibitory effect of FGFR1-3 is weak, so it can safely, effectively treat the liver cancer patient of FGFR4 high expression.

The invention provides compounds of formula (I), or pharmaceutically acceptable salts and pharmaceutical compositions thereof, (I) which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit, CSF1R and PDGFR (PDGFRα, PDGFRβ) kinases.

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

The present invention provides a culture medium for primary ovarian cancer cells, an in vitro culture method, and applications thereof. The culture medium comprises an MST1 / 2 kinase inhibitor; at least one Rho protein kinase inhibitor selected from Y27632, fasudil, and H-1152; an insulin-transferrin-selenium supplement; insulin; prostaglandin E2; epidermal growth factor; gastrin; insulin-like growth factor-1; cholera toxin; amphiregulin; N2; and B27. Compared to existing culture methods, in vitro culture using the culture medium of the present invention has higher expansion efficiency. Culturing primary ovarian cancer cells using this culture medium can maintain the morphological structure and pathological characteristics of the primary tissue, thereby improving the success rate and survival rate of primary ovarian cancer cell culture.

Disclosed is an application of a protein kinase inhibitor in preparation of a medicine for inhibiting uterine leiomyosarcoma, wherein the protein kinase inhibitor can effectively inhibit tumor growth in vitro and in vivo, and has better efficacy and safety compared with traditional chemotherapy. The protein kinase is one of the following: Wee1-like protein kinase, cyclin-dependent kinase 1, serine / threonine protein kinase 1 and serine / threonine protein kinase ATR.

The present invention provides a new group of protein kinase inhibitors, aminopyrimidine derivatives, and pharmaceutically acceptable salts thereof that are useful for treating cell proliferative disease and disorder such as cancer and immune disease. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefore. The invention also provides useful intermediates generated during the syntheses of the aminopyrimidine derivatives.

Substituted naphthyl p38a mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and the use of the substituted naphthyl p38a mitogen-activated protein kinase inhibitors and pharmaceutical compositions thereof for treating diseases are disclosed.

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection. The compositions may be administered intact, or may be crushed prior to administration.

Disclosed are a compound selected from novel pyrimido[4,5-d]pyrimidin-2-one derivatives exhibiting excellent antiproliferative activity against cancer cells, its pharmaceutically acceptable salts, its hydrates, and its stereoisomers; a method for preparing said compound; a pharmaceutical composition comprising said compound as an active ingredient for the prevention, mitigation, or treatment of cancer metastasis and proliferative diseases; and an anticancer composition containing said compound as an active ingredient targeting cancer cells. The compound of the present invention exhibits superior selective inhibitory activity against LCK and antiproliferative activity against cancer cells, and is therefore suitable for inhibiting cancer cells and for the prevention or treatment of cancer metastasis and proliferative diseases.

Disclosed herein are compounds of Formula (I), and pharmaceutically acceptable salts thereof, that are useful as DNA-PK inhibitors. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula (I), and methods of using such compounds or compositions to treat DNA-PK related disorder (e.g., cancer).

The present invention relates to the field of methods for providing pharmaceutical compositions comprising poorly water-soluble drugs. In particular the present invention relates to compositions comprising stable, amorphous hybrid nanoparticles, comprising at least one protein kinase inhibitor and at least one polymeric stabilizing and matrix-forming component, useful in pharmaceutical compositions and in therapy.

The application provides a culture medium and a culture method of a gastric cancer organoid. The culture medium comprises an MST1 / 2 kinase inhibitor, a fibroblast growth factor 7, R-spondin 1, hydrocortisone, a B27 supplement, an N2 supplement, insulin, a dual regulatory protein, at least one Rho protein kinase inhibitor selected from Y27632, fasudil and H-1152, forskolin, gastrin, fetal bovine serum and cholera toxin. Compared with the existing culture method, the in-vitro culture using the culture medium has higher amplification efficiency; the culture of the gastric cancer organoid using the culture medium can maintain the morphological structure and pathological characteristics of the primary tissue, and improve the success rate and survival rate of the gastric cancer organoid culture.

Amorphous solid dispersions of the protein kinase inhibitor cabozantinib. The amorphous solid dispersions exhibit chemical and physical stability under stressed conditions. The amorphous solid dispersions may be suitable for use in pharmaceutical compositions for administration to human subjects or patients.

This invention discloses the use of tumor cell inhibitors to improve the efficiency of genetic transformation in wheat, belonging to the field of mutation or genetic engineering. The technical problem addressed by this invention is how to improve the efficiency of genetic transformation in plants. The tumor cell inhibitor disclosed in this invention is at least one of a histone modification inhibitor and a serine / threonine protein kinase inhibitor. The histone modification inhibitor is the histone deacetylase inhibitor tucidinostat, and the serine / threonine protein kinase inhibitor is Torin2. The present invention discovers that treating plant genetic transformation calli with tumor cell inhibitors promotes callus differentiation into more regenerated buds, thereby improving the efficiency of genetic transformation in plants.

Compounds useful as CDK2 / 4 protein kinase inhibitors and uses thereof are provided. Specifically, provided are compounds of formula I, or pharmaceutically acceptable salts, stereoisomers, tautomers, hydrates, solvates, isotope compounds or prodrugs thereof, in which the definitions of each group and substituent group are as described in the specification, and which are useful as inhibitors of cyclin dependent kinases (CDKs), in particular as inhibitors of Cyclin dependent kinases (CDKs), as well as inhibitors of Cyclin dependent kinases (CDKs), as well as inhibitors of Cyclin dependent kinases (CDKs). The compound is used for preventing or treating cell proliferative diseases and symptoms including various cancers, and is particularly used for regulating and / or treating related diseases caused by overexpression and / or abnormal activity of cyclin-dependent kinase CDK2 / 4.

This specification discloses the use of alternating electric fields and DNA-dependent PK inhibitors for cancer treatment. This specification discloses the use of alternating electric fields and DNA-dependent PK inhibitors for inducing cell death. This specification discloses the use of alternating electric fields and DNA-dependent PK inhibitors to inhibit DNA repair in cancer cells having DNA strand breaks (e.g., double-strand DNA breaks). This specification discloses the use of alternating electric fields and DNA-dependent PK inhibitors to enhance the effectiveness of radiotherapy.

The present disclosure relates to compounds of Formula (I):stereoisomers thereof, prodrugs thereof, and pharmaceutically acceptable salts thereof. The present disclosure also relates to uses of the compounds, e.g., to inhibit AMP-Activated protein kinase (AMPK) and treat cancer in a subject.

The present invention relates to novel salts of heterocyclic compounds as protein kinase inhibitors and their uses, and the novel salts have excellent water solubility and excellent physical and chemical stability, and therefore can be usefully utilized in the formulation of pharmaceuticals. In addition, the heterocyclic compounds or their salts can effectively treat and prevent atopic dermatitis and inflammatory bowel disease, respectively.

The present invention relates to novel compounds as protein kinase inhibitors, in particular RON inhibitors.