68 results about "Janus kinase" patented technology

The invention belongs to the technical field of biological medicine, and particularly relates to a novel deuterated JAK2 inhibitor or pharmaceutically acceptable salt thereof. Compared with the prior art, the compound or the pharmaceutically acceptable salt thereof provided by the invention has better JAK2 inhibition activity, and the JAK2 inhibition target selectivity of the compound or the pharmaceutically acceptable salt thereof is obviously superior to that of the existing compound, so that the compound or the pharmaceutically acceptable salt thereof has better druggability.

Described herein is a method of treating an autoimmune and / or inflammatory condition in an individual in need thereof, the method comprising (a) systemic administration of a first inhibitor to the individual in need thereof, wherein the first inhibitor comprises an inhibitor of interleukin-23 (IL-23), an inhibitor of tumor necrosis factor alpha (TNF-alpha), or combinations thereof; and (b) local administration of a second inhibitor to the individual in need thereof, wherein the second inhibitor comprises an inhibitor of interleukin-23 (IL-23), an inhibitor of tumornecrosis factor alpha (TNF-alpha), a Janus kinase (JAK) inhibitor, a sphingosine- 1 phosphate (SIP) modulator, an inhibitor of TNF-like ligand 1 A (TL1 A), or combinations thereof, thereby treating the autoimmune and / or inflammatory condition in the individual in need thereof.

The invention relates to inhibitors of JAK proteins for use in the treatment of cancer. In vitro methods for screening of candidate agents as JAK inhibitors, and methods for the selection of a subject suffering from cancer as candidate for a cancer therapy comprising in particular JAK inhibitors are also disclosed.

A personalized medical method for treating amyotrophic lateral sclerosis (ALS), comprising screening out a subpopulation of ALS patients having highly immunologically active causes, and administering a therapeutically effective amount of a Janus kinase (JAK) inhibitor to the patients screened out thereby. Also provided are the use of a corresponding JAK inhibitor, an in vitro diagnostic method for screening patients, a kit, and a computer-implemented method. After patients screened out by means of the method are treated with a JAK inhibitor (such as tofacitinib), the level of a nerve damage marker is significantly reduced, and clinical functions are stabilized or improved, and therefore the present invention shows a good therapeutic prospect.

Provided herein are methods of treating or preventing a T-cell mediated inflammatory disease or cancer in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an antibody that specifically binds to human PSGL-1 in combination with a Janus kinase (JAK) inhibitor. In some embodiments, the T-cell mediated inflammatory disease is GVHD, e.g., acute GVHD or chronic GVHD.

The present invention describes novel boron containing pyrazole compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the invention have activity as Janus kinase (JAK) inhibitors and are useful in the in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described are methods of treating inflammation, auto-immune diseases, cancer, and other conditions that are susceptible to the inhibition of a Janus kinase by administering a compound herein described.

The present invention relates to the use and methods of a Janus kinase (JAK) inhibitor or a Janus kinase protein degrading agent for the treatment of fibrosis. Specifically, the present invention relates to a method of treating fibrosis using a JAK inhibitor or a Janus kinase protein degrading agent, comprising administering to the subject a therapeutically effective amount of a JAK inhibitor or a Janus kinase protein degrading agent; the invention relates to a pharmaceutical composition composed of a JAK inhibitor or a Janus kinase protein degradation agent or a therapeutically effective amount of the JAK inhibitor or the Janus kinase protein degradation agent and other medicines for treating fibrosis, a medicine box containing the pharmaceutical composition and a use method of the pharmaceutical composition.

In some embodiments, the invention provides a method for identifying an agent beneficial to treat a patient with inflammatory bowel disease comprising: a) determining a status of an intestinal barrier in the patient; and b) categorizing the status as severe dysfunction or moderate dysfunction, wherein a patient categorized as having severe dysfunction is identified as a patient who will benefit from treatment with an agent selected from the group consisting of an anti-TNF agent and / or an anti-IL-12 / 23 agent, and a patient categorized as having moderate dysfunction is identified as a patient who will benefit from treatment with an anti-integrin agent, an anti-janus kinase agent, and / or and a sphingosine-1-phosphate receptor agonist agent.

The present invention relates to a multiple controlled-release tablet composition of ruxolitinib or a pharmaceutically acceptable salt thereof, which is useful for treating Janus kinase-associated diseases such as myeloproliferative disorders, and a method for producing the same. More specifically, the present invention relates to a multiple controlled-release tablet composition and a method for producing the same, which exhibits a maximum drug blood concentration similar to that of commercially available immediate-release formulations, while controlling the drug release rate so as to efficiently maintain the drug at or above the effective blood concentration in the body, thereby enabling once-daily administration, unlike commercially available formulations that are administered twice daily.

The present disclosure provides compositions, systems, devices, and methods for the delivery of therapeutics. Particularly, the disclosure provides composition, systems, and devices of the delivery of Janus kinase (JAK) inhibitors and uses thereof, such as for inhibiting allograft rejection or treating autoimmune diseases.

The present disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be kinase (e.g., Janus kinase (JAK), e.g., Janus kinase 2 (JAK2)) inhibitors. Also provided are pharmaceutical compositions and kits including the provided compounds. Further provided are methods of using the provided compounds, pharmaceutical compositions, and kits (e.g., for treating a disease (e.g., proliferative disease) in a subject in need thereof).

Provided herein are compounds having inhibitory activity toward the Janus Kinase 1 (JAK-1) enzyme, and which are useful as therapeutic and / or prophylactic agents. The compounds may be useful in treating inflammatory disorders in non-human mammals, for example, in treating canine atopic dermatitis. Also provided herein are methods for preparation of such compounds.

This disclosure relates to methods of treating, preventing, or reversing inflammation-associated central nervous system (CNS) disorders or conditions comprising administering an effective amount of a Janus kinases (JAK) inhibitor such as baricitinib to a patient in need thereof. In certain embodiments, the CNS associated inflammatory disorder is depression, treatment resistant depression, fatigue, or cognitive dysfunction.

Described herein are certain quinoline carboxamides for use in the treatment of myeloproliferative tumors (MPNs). Said quinoline carboxamides, optionally in combination with an additional compound selected from the group consisting of Janus kinase (JAK) inhibitors, bromodomains and terminal exo-motif protein (BET) inhibitors, B cell lymphoma 2 (Bcl-2) inhibitors, and combinations thereof, can more specifically be used for the treatment of advanced MPNs, including accelerated MPNs and secondary acute myeloid leukemia, such as acute myeloid leukemia. , acute myelogenous leukemia evolved from a previous myeloproliferative tumor (AML after MPN). Also included are pharmaceutical combinations of the quinoline carboxamide and a second agent, such as a BET inhibitor or a Bcl-2 inhibitor. Also included are certain quinoline carboxamides for use in the treatment of myeloproliferative tumors (MPN) in combination with a BET inhibitor or a Bcl-2 inhibitor.

The present invention describes novel boron containing pyrazole compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the invention have activity as Janus kinase (JAK) inhibitors and are useful in the in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described are methods of treating inflammation, auto-immune diseases, cancer, and other conditions that are susceptible to the inhibition of a Janus kinase by administering a compound herein described.

The present application relates to heterocyclic compounds or pharmaceutically acceptable salts thereof as Janus kinase (JAK) inhibitors. In particular, the present application relates to a compound of general formula (I) or a pharmaceutically acceptable salt thereof. The present application also relates to a preparation method of the compound or the pharmaceutically acceptable salt thereof. The compound of the present application can be used for treating and / or preventing JAK-mediated related diseases, particularly inflammatory diseases, autoimmune diseases and cancers. In the general formula (I), each substituent is the same as defined in the specification.

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 invention provides compounds that modulate the activity of protein kinases that are associated with human diseases, disorders, and conditions. In particular, compounds of the invention inhibitTYK2, a member of the Janus Kinase (JAK) family of non -receptor protein kinases.

: The present invention provides a topical pharmaceutical composition comprising Janus kinase (JAK) inhibitors like Tofacitinib, Immunosuppressive agent like Tacrolimus, Fingolimod and statins like atorvastatin, Simvastatin, Fluvastatin, Lovastatin, Pitavastatin, Pravastatin and Rosuvastatin dissolved or dispersed in a pharmaceutically acceptable base together with other pharmaceutically acceptable excipients or in a dermatologically acceptable carrier, useful in the treatment of vitiligo. The inventive concept provided herein are methods and pharmaceutical compositions by preparing oral dosage forms like Topical liquid spray or Topical cream or Topical gel dosage form for the management of vitiligo and its associated disorders and accordingly performing preclinical study to prove the efficacy of the selected drug substances from the class of JAK inhibitors, statins and immunosuppressants.

The present invention provides compounds of Formula I:or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit 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.

The invention discloses a drug delivery microneedle system driven by a miniature ultrasonic patch. The drug delivery microneedle system comprises an excitation circuit, the miniature piezoelectric ultrasonic patch, a drug carrying microneedle array, a coupling structure and a packaging structure. The system has a modulatable sound field characteristic, the excitation circuit drives the piezoelectric ultrasonic patch to generate ultrasonic vibration by applying an electric signal with specific frequency and amplitude, and release of a Janus kinase (JAK) inhibitor loaded by the microneedle array is promoted. The miniature ultrasonic patch adopts a sheet-shaped design, the size is 5-50mm, the thickness is 0.5-5mm, the working frequency is 0.1-4MHz, and the driving voltage is 40-100V. The main body material of the drug-loaded microneedle array is hydrogel capable of loading a JAK inhibitor, the microneedle substrate and the ultrasonic patch are tightly fixed through a coupling structure, and the ultrasonic patch is coated with a packaging structure. The controllability of the drug delivery microneedle is optimized by introducing the modulatable sound field, accurate regulation and control and synergism of drug release can be achieved, and the drug delivery microneedle has important application prospects in targeted therapy of immune skin diseases.

The invention relates to therapeutic and prognostic use based on the findings obtained as a result of investigating the effectiveness of different miRNAs on the expression levels of some genes involved in the Janus Kinase-Signal Transducer Transcription Activator (JAK-STAT) pathway in the treatment of respiratory form distemper.

The present invention provides processes for preparing 7H-pyrrolo[2,3-d]pyrimidine derivatives, which are useful as a Janus kinase (JAK) inhibitor, intermediates thereof, and processes for preparing the intermediates. The present invention provides processes for preparing 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile using salts of (3S,4R)-1-benzyl-3-methyl-1,6-diazaspiro[3.4]octane with organic acids.

A 7-azaindole derivative having the structure of formula (I), a pharmaceutical composition containing the compound of formula (I), and uses of the compound in preparing a medicament for preventing or treating Janus kinase (JAK) family-related diseases, specifically, uses in preventing or treating inflammatory diseases related to protein tyrosine kinase.

The present disclosure describes boron-containing pyrimidine compounds or pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, and medical uses thereof. The compounds of the present disclosure have activity as Janus kinase (JAK) inhibitors and are useful for the treatment or management of inflammation, autoimmune diseases, cancer, and other disorders and indications in which modulation of JAK is desired. Also described are methods of treating inflammation, autoimmune diseases, cancer, and other conditions that are sensitive to inhibition of Janus kinase by administering the compounds described herein.

The present invention provides compounds that modulate the activity of protein kinases associated with human diseases, disorders and conditions. In particular, the compounds of the invention inhibit TYK2 which is a member of the Janus kinase (JAK) family of non-receptor protein kinases.

Provided herein are compounds of formula (I) useful as Janus kinase (JAK) inhibitors. Also provided herein are pharmaceutical compositions comprising such compounds and methods of using such compounds to treat, e.g., inflammatory and fibrotic diseases, including respiratory diseases, autoimmune diseases, and cancers.

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.

There are methods for treating hidradenitis suppurtiva using compounds and analogues that inhibit certain kinases, including Janus Kinase (JAK).

There are methods for treating hidradenitis suppurtiva using compounds and analogues that inhibit certain kinases, including Janus Kinase (JAK).