43 results about "Ruxolitinib" patented technology

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 invention relates to a synthesis method of a ruxolitinib intermediate. The method comprises the following steps: firstly, carrying out catalytic reaction on cyclopentane methyl formate and acetonitrile to prepare 3-cyclopentyl-3-oxypropionitrile; carrying out enzymatic asymmetric reduction on 3-cyclopentyl-3-oxypropionitrile to generate chiral alcohol (S)-3-cyclopentyl-3-oxypropionitrile; and carrying out Mitsunobu reaction and 4-bromopyrazole coupling on (S)-3-cyclopentyl-3-oxypropionitrile to obtain ruxolitinib intermediate (3R)-3-(4-bromo-1H-pyrazole-1-yl)-3-cyclopentane propionitrile. The synthesis method has the advantages of short route, low cost, mild condition and good stereoselectivity, and is suitable for industrialized mass production.

The invention discloses a 4-chloro-7H-pyrrolo[2,3-d]pyrimidine synthetic method. A compound is an important intermediate for synthesizing ruxolitinib and tofacitinib as a JAK inhibitor for treating rheumatoid arthritis. The 4-chloro-7H-pyrrolo[2,3-d]pyrimidine synthetic method comprises the following steps of by taking a compound I (4,6-dichloro-5-allyl pyrimidine) as a starting material, performing oxidation reaction on the compound I and ozone to produce a compound II; then performing nucleophilic substitution reaction on the compound II and triethyl orthoformate to produce a compound III; then performing nucleophilic substitution reaction on the compound III and ammonia gas to produce a compound IV; and finally, performing ring closing on the compound IV self in an acid environment to produce a compound V, i.e., 4-chloro-7H-pyrrolo[2,3-d]pyrimidine, wherein a synthetic route is shown as the following formula (described in the description). The synthetic method disclosed by the invention is cheap and available in raw materials, simple and short in synthetic route, low in cost, high in yield and easy in industrial production.

The invention belongs to the technical field of medicines, discloses an new application of sorafenib, and particularly relates to an application of the sorafenib to preparation of medicines for treating myeloproliferative neoplasmas. The myeloproliferative neoplasmas is myeloproliferative neoplasmas with polycythemia vera or drug resistance of ruxolitinib. The sorafenib is used for treating the polycythemia vera, a new treatment way is provided for patients suffering from the polycythemia vera, and more choices are provided for clinicians and patients. For a patient suffering from myeloproliferative neoplasmas with drug resistance of ruxolitinib, the sorafenib can provide continuous oral drug therapy for the patient, and bone marrow transplantation is avoided. The sorafenib can be chemically synthesized, and the cost is lower than that of a biological agent. And the sorafenib is approved by FDA and NMPA to appear on the market and is used for clinical treatment. The side reaction is less and lighter, the tolerance of clinical patients is good, and the burden of the patients is lighter.

The present invention provides methods of treating and/or inhibiting cancer by administering a JAK1/2 inhibitor (e.g., ruxolitinib). The JAK1/2 inhibitor decreases expression of (or inhibits increased expression of) the checkpoint proteins PD-1, PD-L1, PD-L2, or B7 H3, and/or enhances T-cell killing of tumor cells, and/or enhances the anti-tumor effects of checkpoint inhibitors. The disclosed methods improve the efficacy of immune-based therapies used in treatment of cancer.

The invention relates to use of Ruxolitinib in preparation of a drug for treating M2 type acute myeloid leukemia with t (8; 21) chromosome translocation, and the in-vitro effective concentration is 1 * 10<-6>-1 *10<-5>M. Drug Ruxolitinib is not only itself has the effect of inhibiting growth and inducing apoptosis on leukemia cell Kasumi-1, and enhances the drug sensitivity of the leukemia cell Kasumi-1 on rsTRAI by up-regulation of mRNA and protein expression level of DR4, up-regulation of cell apoptosis protein Bax expression, activation of apoptosis protein caspase-3 and inhibition of NF-kappa B protein activity. The drug can be used for treating the M2 type acute myeloid leukemia with t (8; 21) chromosome translocation, the new drug for treating the M2 type acute myeloid leukemia with t (8; 21) chromosome translocation is provided, and a new approach for overcoming TRAIL resistance in leukemia cells can be provided.

The present invention relates to the use of MDM2 inhibitors in the treatment of myelofibrosis (MF). The invention also relates to a pharmaceutical combination comprising a) an MDM2 inhibitor, and b) at least one additional therapeutic agent, preferably rusotinib or a pharmaceutically acceptable salt thereof.

The invention relates to the use of an anti-P-selectin antibody or binding fragment thereof, suitably crizanlizumab or a binding fragment thereof in the treatment of myelofibrosis (MF). The invention also relates to a pharmaceutical combination comprising a) an anti-P-Selectin antibody and b) at least one further therapeutic agent, preferably ruxolitinib or a pharmaceutically acceptable salt thereof.

The invention described herein relates to methods for treating a human subject with myelofibrosis or an MPN-related disorder, comprising administering navitoclax to the subject optionally in combination with ruxolitinib.