17 results about "Ruxolitinib" patented technology

There is provided inhalable formulations of ruxolitinib, manufacture, and uses thereof.

Improved processes and intermediates for preparing ruxolitinib, deuterated analogs of ruxolitinib, and other JAK inhibitors are disclosed.

The present invention relates to an improved process for the preparation of ruxolitinib or its salts and intermediates thereof. The present invention also relates to a novel crystalline form G of ruxolitinib, a process for its preparation, use of it in the preparation of ruxolitinib salts, a pharmaceutical composition comprising it, and method of use thereof. The present invention also relates to an improved process for preparation of crystal modification 3 of ruxolitinib hydrochloride salt.

This invention relates to a novel method for preparing ruxolitinib phosphate. Methyl 4-(1-(2-cyano-1-cyclopentylethyl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-D]pyrimidin-7-yl)terpentanoate (compound X) is deprotected under alkaline conditions, then directly resolved without separation, alkalized to release the free ruxolitinib, and salted to obtain the ruxolitinib phosphate. The obtained ruxolitinib phosphate has an HPLC purity >99.90%, and the ruxolitinib phosphate isomer has a purity >99.50%. The preparation method of this invention has the advantages of simple operation, controllable impurities, low cost, and suitability for industrial production.

This disclosure relates to methods of reducing itch in patients with atopic dermatitis and treating patients with atopic dermatitis by administering a topical 0.75% or 1.5% ruxolitinib cream two times per day.

Improved processes for preparing enantiomerically enriched intermediates for the synthesis of ruxolitinib and deuterated forms of ruxolitinib and deuterated analogs of ruxolitinib of Formula I:wherein, Y1 is hydrogen or deuterium; each Y2 is the same and is hydrogen or deuterium; and each Y3 is the same and is hydrogen or deuterium are disclosed. Certain aspects are also directed to deuterated intermediates useful in the synthesis of deuterated forms of ruxolitinib. Certain aspects are also directed to reaction mixtures for preparing enantiomerically enriched intermediates useful in the synthesis of ruxolitinib and deuterated forms of ruxolitinib.

Title of the Invention: Novel process for the preparation of (R)-3-(4-(7H- pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile or a salt thereof The present invention relates to a novel process for the preparation of (R)-3-(4-(7H- pyrrolo[2,3­d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile or a salt thereof, which is referred to as Ruxolitinib and represented by the following structural formulae, Formula-1

There is provided inhalable formulations of ruxolitinib, manufacture, and uses thereof.

This invention relates to topical skin formulations comprising a pharmaceutically acceptable salt of ruxolitinib, and use in the treatment of skin disorders.

The present invention relates to a solid oral pharmaceutical composition containing ruxolitinib or a pharmaceutically acceptable salt thereof as a pharmaceutically active ingredient, wherein the composition contains less than 2.0% by weight of povidone relative to the total weight of the composition. The present invention also relates to a method for producing the pharmaceutical composition.

The present application provides a drug composition of lucotinib or its pharmaceutically acceptable salt which is not easy to precipitate, coalesce and physically stable, the raw material drug is lucotinib or its pharmaceutically acceptable salt, and the stabilizer comprises a non-ionic surfactant and a space structure stabilizer; the non-ionic surfactant comprises a fatty alcohol polyoxyethylene ether, an alkyl phenol polyoxyethylene ether, a polyoxyethylene alkyl acyl alcohol amine, a fatty acid polyoxyethylene, a polyoxyethylene alkyl amine, a polyhydric alcohol, a polysorbate, a glycerol stearate; the space structure stabilizer comprises one or more of polyvinyl alcohol, sodium polyacrylate, gelatin, povidone, polyethylene glycol, poloxamer, hydroxypropyl cellulose, hydroxymethyl cellulose, vinyl pyrrolidone, sorbitol, arabinose, trehalose and the like. In addition, the present application also provides a preparation method of the lucotinib drug composition. The starting raw and auxiliary materials of the present application are easy to obtain, the process is stable, and the stability of the commercially available lucotinib cream is effectively improved.

Immunotherapy leverages the body's immune system to target cancer cells, but some tumors resist this treatment due to low infiltration of T CD8+ cells and high infiltration of regulatory T cells in the tumor microenvironment. The inventors showed that a JAK inhibitor (i.e. ruxolitinib) reshapes the tumor immune microenvironment resulting in T regulatory cells reduction and T CD8+ cells increase. Ruxolitinib-mediated immune microenvironment effects create new therapeutic opportunities by enhancing anti-PD1 treatment efficacy in cSCC and melanoma and other immunotherapy resistant cancer types such as pancreatic cancer and acute myeloid leukemia (AML). Cell-based immunotherapy response is also improved in AML. Accordingly, the present invention relates to the use of JAK inhibitors for enhancing the potency of immunotherapy.

The present application relates to treatment of myeloproliferative neoplasms using the JAK1 / JAK2 inhibitor, ruxolitinib, in combination with a BET protein inhibitor, 2,2,4-trimethyl-8-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-6-(methylsulfonyl)-2H-1,4-benzoxazin-3(4H)-one, wherein the combination is unexpectedly synergistic.

The present disclosure relates to topical formulations and methods of treating skin diseases using topical formulations comprising a JAK 1 / 2 inhibitor, which is ruxolitinib, or a pharmaceutically acceptable salt thereof, and an organic amine pH adjusting agent. The skin diseases for treatment include, but are not limited to, psoriasis, atopic dermatitis, alopecia, vitiligo, Reiter's syndrome, pityriasis rubra pilaris, epidermolysis bullosa simplex, palmoplantar keratoderma, pachyonychia congenita, steatocystoma multiplex, cutaneous lichen planus, cutaneous T-cell lymphoma, hidradenitis suppurativa, contact dermatitis, ichthyosis, and a disorder of keratinization. The organic amine pH adjusting agent is a tertiary amine or an alkanol amine.

This invention relates to topical skin formulations comprising a pharmaceutically acceptable salt of ruxolitinib, and use in the treatment of skin disorders.

This article provides the medical use of CXCR4-enriched regulatory T cells in combination with ruxolitinib for the treatment of myelofibrosis or to improve symptoms of myelofibrosis in subjects who have poor response to ruxolitinib monotherapy.