71 results about "Ruxolitinib" patented technology

By constructing an age-related macular degeneration animal model, experimental results in multiple aspects of clinical examination (FFA and ERG), pathological detection (RPE-choroidal patch IB4 fluorescent staining) and the like prove that the rucotinib can be used for effectively treating age-related macular degeneration, especially wet age-related macular degeneration.

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.

The present invention discloses an externally applied rapid-dissolving film containing ruxolitinib, a preparation method thereof and applications. The raw materials of the externally applied rapid-dissolving film include ruxolitinib phosphate or a pharmaceutically acceptable salt thereof and a film-forming agent in a weight ratio of 1:5 to 20, and the film-forming agent is polyethylene oxide or polyvinyl alcohol. The externally applied rapid-dissolving film of the present invention has the advantages of high drug loading, fast dissolution rate, high cumulative drug release amount, and high penetration rate. It has good adhesion to the skin and is not easy to stain clothes. Compared with cream agents or other external dosage forms, it has better compliance.

The main objective of the present invention is to improve the process for the preparation of ruxolitinib using protected (E)-N-(3-(Dimethylamino)-2-(7H-pyrrolo [2,3-d]pyrimidin-4-yl) allylidene)-N-methylmethanaminium chloride hydrochloride and (R)-5-cyclopentylpyrazolidin-3-one D-tartrate with higher yields on commercial scale. Formula (I):

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.

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

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.

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

The present disclosure relates to a polymorph Form 1 of ([beta] R)-[beta]-(cyclopentyl-2, 2, 3, 3, 4, 4, 5, 5-d8)-4-(7H-pyrrolo [2, 3-d] pyrimidin-4-yl)-1H-pyrazol-1-propionitrile phosphate (1: 1) (deuterated ruxolitinib phosphate), in particular, to a polymorph Form 1 of ([beta] R)-[beta]-(cyclopentyl-2, 2, 3, 3, 4, 4, 5, 5-d8)-4-(7H-pyrrolo [2, 3-d] pyrimidin-4-yl)-1H-pyrazol-1-propionitrile phosphate (1: 1). Also disclosed are methods of treatment using the polymorph Form 1 of deuterated rusotinib phosphate and methods of producing the polymorph Form 1 of deuterated rusotinib phosphate.

The present invention relates to a solid oral pharmaceutical composition comprising rusotinib or a pharmaceutically acceptable salt thereof as an active pharmaceutical ingredient wherein the composition comprises less than 2.0% by weight of povidone. In addition, the present invention relates to a process for the preparation of the pharmaceutical composition according to the present invention.

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.

The invention discloses an application of a CaMKII-gamma inhibitor serving as a bortezomib-resistant multiple myeloma treatment medicine. On the basis of si-RNA, cell proliferation activity can be inhibited by down-regulating expression of CaMKII-gamma in bortezomib-resistant multiple myeloma U266.BR cells and KMS11. BR cells, a small molecule compound rucotinib capable of effectively inhibiting activity of CaMKII-gamma kinase is obtained through high-throughput screening, growth of multiple myeloma U266 cells and KMS11 cells can be obviously inhibited, and the activity of the rucotinib can be effectively inhibited. The compound has an obvious inhibition effect on the growth of bortezomib-resistant multiple myeloma U266.BR cells and KMS11. BR cells, also has an obvious inhibition effect on the growth of U266.BR transplantation tumors, and shows a good tumor inhibition effect as a potential medicine for treating multiple myeloma and bortezomib-resistant multiple myeloma.

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.

Disclosed are methods of accelerating development of new hair follicles in pluripotent stem cell-derived skin organoids. In particular, disclosed are methods of accelerating development of new hair follicles in skin organoids by adding one or more growth factors, such as FGF10, FGF20, BIO, ruxolitinib, tofacitinib, LDN193189, vitamin E, GDNF, retinoic acid, or IGF2. The growth factors are added to a culture of skin organoid at critical windows of time of the skin organoid development, such as after (or upon) the formation of epidermis and dermis in the skin organoid.

Improved processes and intermediates for preparing ruxolitinib and deuterated analogs of ruxolitinib are disclosed.

The present invention provides a method for preparing ruxolitinib and its intermediates. The method has high synthesis efficiency, simple process, low synthesis cost, and is suitable for large-scale industrial production.

The present invention relates to a direct compressed pharmaceutical tablet comprising a) about 1 wt.% to 10 wt.% ruxolitinib phosphate, b) about 35 wt.% to 55 wt.% of silicified microcrystalline cellulose, c) about 0.1 wt.% to 3 wt.% of one or more binder; and d) at least one more pharmaceutically acceptable excipient, wherein wt.% is based on the total weight of the tablet. The said tablet has a desirable pharmacokinetic characteristic, favorable storage stability and comparative dissolution properties. The invention further relates to a process for the preparation of said pharmaceutical composition and use thereof as medicament in the treatment of myelofibrosis, polycythemia vera, graft versus host disease.

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.

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.

Sulfonate salts of ruxolitinib and crystalline forms thereof, pharmaceutical compositions comprising these salts and crystalline forms thereof, and the use of these salts in the treatment of acute graft versus host disease, polycythemia vera, myelofibrosis, and atopic dermatitis are described. The solubility of individual salt and crystalline forms of a drug substance in an aqueous environment is an important aspect of their relative bioavailability. The specific counter anions of the present invention include mesylate, edisylate, napadisylate, and acesulfamate.

The present invention provides a process for the preparation of ruxolitinib or a pharmaceutically acceptable salt thereof. In particular, the present invention provides a process for the preparation of crystalline (R)-ruxolitinib phosphate. The present invention also provides pharmaceutical composition comprising crystalline (R)-ruxolitinib phosphate which is obtained by the process of the present invention. The present invention provides a compound of formula IV.

The oral solid dosage form of the present invention comprises ruxolitinib or its pharmaceutically acceptable salts thereof, and at least one excipient. Specifically, it involves an immediate-release tablet containing the ruxolitinib salt, as well as a method for preparing this dosage form via direct compression. This method is designed to offer simplified manufacturing processes and ensure long-term stability of the product.

According to the rukotinib phosphate cream and the preparation method thereof provided by the invention, in the preparation process, more sufficient emulsification is carried out by adopting a high-shearing and high-pressure homogenizing mode, so that the prepared cream is fine and smooth in texture, stable in physical property and free of toxic and side effects; the characteristics, the droplet particle size, the dynamic viscosity and the in-vitro release rate of the emulsifiable paste are stable under the accelerated or long-term placement condition, the unstable phenomena of layering, water bleeding and the like of the emulsifiable paste in a short time are avoided, the continuous safety and the curative effect stability of the emulsifiable paste in the using process are ensured, and the preparation method is simple, high in operability and suitable for industrial production. The method is suitable for large-scale industrial production.

Disclosed is a pharmaceutical composition for preventing or treating skin diseases, comprising a Janus kinase inhibitor. A pharmaceutical composition for preventing or treating psoriasis and atopic dermatitis, according to one embodiment, comprises: a Janus kinase inhibitor including at least one of a Janus kinase inhibitory component or a pharmaceutically acceptable salt thereof; and an active ingredient including at least one of octenidine or an octenidine salt, wherein the Janus kinase inhibitory component may include at least one of delgocitinib, ruxolitinib, or tofacitinib.

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

The invention belongs to the technical field of tobaccos, and particularly relates to a method for blocking generation of ash hanging tobaccos through a PPO activity inhibitor. According to the method, a PPO activity inhibitor is adopted for spraying or fumigating treatment before tobacco leaves are cured, so that the activity of PPO is inhibited, and ash-coated tobacco is prevented from being generated; the PPO active inhibitor is any one of Prothionamide (isopropylthioamide), Ruxolitinib (rucotinib) and isoliquiritigenin (isoliquiritigenin), and the PPO active inhibitor is any one of the following raw materials: isopropylthioicotinamide, ruxolitinib (rucotinib) and isoliquiritigenin (isoliquiritigenin). The method provided by the invention is applied to the production link of tobacco processing, the generation of ash-coated tobacco is reduced, and the product appearance and combustion quality are improved.

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

The present disclosure is related to solid forms of ruxolitinib di-hydrate and ruxolitinib free base, process of preparing the same, and compositions comprising the same.