179 results about "PTK Inhibitors" patented technology

The present invention discloses substituted 2-amino-9-(3,3-difluoropiperidin-4-yl)-7,9-dihydro-8H-purin-8-one compounds compounds having the structural formula represented by formula (I)： The substituted 2-amino-9-(3,3-difluoropiperidin-4-yl)-7,9-dihydro-8H-purin-8-one compounds, derivatives and pharmaceutically acceptable salts thereof of the present invention are capable of acting as a drug characteristic of a protein kinase inhibitor, in particular for the expression of a protein through a DNA-dependent protein kinase (DNA-PK) and can be used to treat or prevent disorders associated with abnormal protein kinase activity, such as cancer, cancer with brain metastases, cancer with meningeal metastases, glioma, glioblastoma, DIPG, and the like either as monotherapy or combination with other treatments, such as radiation therapy or chemotherapy.

The invention provides compounds of formulae (I), or pharmaceutically acceptable salts and pharmaceutical compositions thereof, 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.

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.

The invention discloses a pharmaceutical preparation of a protein kinase inhibitor citrate as well as a preparation method and application of the pharmaceutical preparation. The pharmaceutical preparation comprises citrate of a protein kinase CDK4 / 6 inhibitor and auxiliary materials including a filler, a disintegrating agent, an adhesive, a wetting agent, a glidant and a lubricant. The protein kinase inhibitor citrate pharmaceutical preparation has the advantages of being good in quality, high in stability, high in dissolution rate, simple in preparation method, controllable in quality and the like.

The invention provides compounds of formulae (I), or pharmaceutically acceptable salts and pharmaceutical compositions thereof, 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.

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 #

The invention provides compounds of formula (I), or pharmaceutically acceptable salts and pharmaceutical compositions thereof,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.

Described is a combination of a prophylactic or therapeutic agent for glaucoma or ocular hypertension, which is useful as a prophylactic or therapeutic agent for glaucoma or ocular hypertension. By combining sepetaprost and a Rho-associated coiled-coil containing protein kinase inhibitor(s), an intraocular pressure lowering action is enhanced as compared with the case where each drug is used alone. As the form of administration, they may be administered concomitantly or may be administered as a combination drug.

The present invention relates to pharmaceutical compositions comprising Akt protein kinase inhibitors with therapeutic activity against diseases such as cancer as well as processes for their preparation and their use as medicament.

Novel compounds inhibiting ATR protein kinase include compounds of formula (I) disclosed herein, as well as liposome formulations comprising ATR protein kinase inhibitor compounds. The compositions are useful for the treatment of cancer.

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 disclosure relates to a method of treating or delaying the progression of fibrosis in a subject comprising administering the compound of formula (I) or a pharmaceutically acceptable salt thereof. The present disclosure also relates to a method for administering the compound of formula (I) or a pharmaceutically acceptable salt thereof to a lung.

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 present invention relates to compounds that modulate protein kinase activity, in particular compounds that inhibit PLK1 kinase activity. The present invention further provides pharmaceutical compositions containing said compounds and the use of said compounds and pharmaceutical compositions thereof in the manufacture of medicaments for the prevention or treatment of diseases caused by and / or associated with dysregulation of PLK1 kinase activity. [Formula 1] TIFF2024546115000197.tif18160

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.

Identified compounds demonstrate protein kinase inhibitory activity. More specifically, the compounds are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and / or Activin-like kinase 2 (ALK2) and / or receptor interacting kinase 3 (RIPK3). Compounds that are either dual RIPK2 / ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 or RIPK3 could provide therapeutic benefit. Compounds that function as RIPK3 inhibitors provide therapeutic benefit in the treatment of inflammatory and degenerative conditions.

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.

The present invention discloses aminothiazole compounds of the following formula (I) and pharmaceutical compositions containing one of these compounds. The present invention also discloses methods for inhibiting tyrosine kinase and treating cancers associated with tyrosine kinase using one of the aminothiazole compounds.