123 results about "Janus kinase" patented technology

The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases are therapeutically useful.

A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R¹, R², R³, R⁴ and R⁵ are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.

The present invention relates to sustained-release formulations and dosage forms of ruxolitinib, or a pharmaceutically acceptable salt thereof, which are useful in the treatment of Janus kinase-associated diseases such as myeloproliferative disorders.

The present invention is directed to compounds of formula (I)-(II) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases.

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as cardiovascular disease, inflammatory disease, autoimmune disease and cell proliferative disorder, thrombosis, allergy, asthma, rheumatoid arthritis, leukemia, or non-Hodgkin's lymphoma. The formula I-II is shown in the description.

The invention provides a baricitinib polymorph A. The baricitinib polymorph A is characterized in that diffraction peaks are arranged on an XRPD (X Ray Powder Diffraction) map when values of 2 theta are equal to 12.46, 13.921, 14.94, 15.359, 16.26, 16.639, 17.36, 19.08, 20.321, 21.961, 22.381, 24.118, 25.42, 27.441, 28.381, 29.321, 29.799, 32.675, 33.14, 33.563, 33.923 and 41.6, wherein an error range of the values of the 2 theta is +/- 0.2. The baricitinib polymorph A provided by the invention has good high-temperature stability, good high-humidity stability and good illumination stability, can be applied to medicine for treating or preventing diseases related to JAK (Janus Kinase) and has better biological availability; meanwhile, provided qualitative and quantitative information has important significance in further studying the therapeutic effect of such solid medicine.

The invention provides a small molecular compound, The small molecular compound is characterized by having a structure as shown in the following molecular general formula, wherein X1 and X2 are selected from carbon or nitrogen, G1 is a carbon ring or a heterocyclic ring with aromaticity, any one or more hydrogen atoms on the G1 ring are substituted by R1, wherein R1 is selected from nitrogen-containing groups. The small molecule compound can be used as an efficient and specific JAK kinase inhibitor, especially a Tyk2 inhibitor, and/or a JAK1 inhibitor, and/or a JAK1/Tyk2 dual inhibitor, or a Tyk2/JAK1 dual inhibitor or a Tyk2/Jak2 dual inhibitor.

In part, the present disclosure relates methods for treating, preventing, or reducing the severity of a myeloproliferative disorder (e.g., polycythemia vera, essential thrombocythemia, and myelofibrosis) or one or more complications of a myeloproliferative disorder. The present disclosure further relates methods for treating, preventing, or reducing the severity of a Janus kinase-associated disorder or one or more complications of a Janus kinase-associated disorder. In certain aspects the disclosure provides TβRII antagonists for treating, preventing, or reducing the severity of a myeloproliferative disorder (e.g., polycythemia vera, essential thrombocythemia, and myelofibrosis) or a Janus kinase-associated disorder or one or more complications of a myeloproliferative disorder or a Janus kinase-associated disorder.

The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

The invention discloses a 5-member and 6-member rings heterocyclic compound shown as a formula I, its pharmaceutically acceptable salt, a metabolite, a metabolism precursor or its medicine precursor, a preparation method, a pharmaceutical composition and an application. The 5-member and 6-member rings heterocyclic compound has activity by being as a Janus kinases (JAK) inhibitor, and be used for treating diseases due to abnormal activity of kinases, such as cell proliferation diseases such as cancer, and can be used for preparing the medicines for treating the disease.

The invention provides a substituted heteroaryl compound and a pharmaceutical composition and application thereof. The compound is a compound as shown in formula (I) or the stereisomer, tautomer, nitric oxide, solvate, metabolite, pharmaceutically acceptable salt or prodrug of the compound as shown in formula (I). The pharmaceutical composition containing the compound can regulate the activity ofprotein kinase and especially the activity of Aurora kinase and JAK kinase and is used for preventing, treating and relieving diseases or disorder mediated by protein kinase and especially JAK kinase.

The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.

New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).

Disclosed are pyrrolopyrimidine compounds of formula (I) capable of inhibiting JAK kinase, wherein R1, R2 and m are defined as in the description. The pharmaceutical compositions containing said pyrrolopyrimidine compounds and uses of said pyrrolopyrimidine compounds in the treatment of disorders or diseases such as inflammatory diseases and cancers are also disclosed.

The invention provides compounds of formula (I):

which contain a 4-membered heterocyclic amide, where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.