Ruxolitinib patented technology retrieval search results - Eureka

Q: How to Ruxolitinib?

Sustained-release dosage forms of ruxolitinib,Sustained-release dosage forms of ruxolitinib,Synthesis method of ruxolitinib intermediate,Synthetic method of 4-chloro-7H-pyrrolo[2,3-d] pyrimidine,Deuterated Derivatives of Ruxolitinib

Sustained-release dosage forms of ruxolitinib

ActiveUS20140135350A1Lower the volumeBiocideSenses disorderDiseaseSustained release drug

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.

Sustained-release dosage forms of ruxolitinib

View all

Owner:INCYTE HLDG & INCYTE

Sustained-release dosage forms of ruxolitinib

ActiveUS10166191B2Lower the volumeOrganic active ingredientsSenses disorderDiseaseSustained release drug

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.

View all

Owner:INCYTE HLDG & INCYTE

Synthesis method of ruxolitinib intermediate

ActiveCN104496904AMild conditionsFew reaction stepsOrganic chemistrySynthesis methodsRuxolitinib

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.

Synthesis method of ruxolitinib intermediate

View all

Owner:BIOCOMPOUNDS PHARMACEUTICAL INC +1

Synthetic method of 4-chloro-7H-pyrrolo[2,3-d] pyrimidine

ActiveCN107011347AShort synthetic routeHigh yieldOrganic chemistryRuxolitinibAlkyl substitution

The invention discloses a synthetic method of 4-chloro-7H-pyrrolo[2,3-d] pyrimidine. The compound is an important intermediate for synthesizing rheumatoid arthritis JAK inhibitors: ruxolitinib and tofacitinib. The synthetic method comprises the following steps: by taking a compound I (4,6-dichloro-5-allyl pyrimidine) as an initial raw material, performing a nucleophilic substitution reaction with ammonia water to generate a compound II; then performing a reaction on the compound II and ozone and performing a reduction reaction to generate a compound III; and finally, performing self ring-closing reaction in an acidic environment to generate a compound IV, that is, the 4-chloro-7H-pyrrolo[2,3-d] pyrimidine. The synthetic route is as shown in the formula in the description. According to the synthetic process provided by the invention, the raw material is cheap and easily available, the synthetic route is simple, the cost is low, the yield is high, and the synthetic method is easy for industrial production.

View all

Owner:EAST CHINA NORMAL UNIV +1

Deuterated Derivatives of Ruxolitinib

ActiveUS20150239896A1Organic active ingredientsBiocideRuxolitinibCombinatorial chemistry

The present invention in one embodiment provides a compound of Formula A:or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising the compound; and methods of treating the indications disclosed herein.

View all

Owner:SUN PHARMA IND INC

Deuterated derivatives of ruxolitinib

InactiveUS20150197525A1BiocideOrganic active ingredientsMedicineRuxolitinib

The present invention in one embodiment provides a compound of Formula A:or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising the compound; and methods of treating the indications disclosed herein.

View all

Owner:CONCERT PHARMA INC

4-chloro-7H-pyrrolo[2,3-d]pyrimidine synthetic method

InactiveCN108409745AShort synthetic routeHigh yieldOrganic chemistryRuxolitinibAlkyl substitution

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.

View all

Owner:EAST CHINA NORMAL UNIVERSITY +1

Preparation method of ruxolitinib intermediate (3R)-3-(4-Br-1H-pyrazole-1-yl)-cyclopentyl propanenitrile

ActiveCN107674026AHigh stereoselectivityLow costOrganic chemistryRuxolitinibPropionitrile

The present invention relates to a preparation method of ruxolitinib intermediate (3R)-3-(4-Br-1H-pyrazole-1-yl)-cyclopentyl propanenitrile, and the method comprises the following steps: (1) synthesisof 3-oxo-3-cyclopentyl propionitrile (II); (2) synthesis of (S)-3-cyclopentyl-3-hydroxypropionitrile (III); (3) synthesis of (3R)-3-(4-nitro-1H-pyrazole-1-yl)-cyclopentyl propionitrile (IV); (4) synthesis of (3R)-3-(4-amino-1H-pyrazole-1-yl)-cyclopentyl propionitrile (V); and (5) (3R)-3-(4-Br-1H-pyrazole-1-yl)-cyclopentyl propanenitrile (VI). The method has the advantages of good stereoselectivity, low cost, mild reaction conditions, no requirement on harsh reaction such as high temperature, high pressure and ultra-low temperature.

View all

Owner:海化生命(厦门)科技有限公司

Preparation methods of JAK inhibitor and salt thereof

ActiveCN107759601AHigh yieldHigh reaction yieldPreparation by aldehyde oxidation-reductionGroup 3/13 element organic compoundsHalogenRuxolitinib

The present invention relates to preparation methods of a JAK inhibitor and a salt thereof. The preparation method comprises: (1) carrying out a Suzuki coupling reaction on (R)-3-(4-boronic acid-1H-pyrazol-1-yl)-3-cyclopentylpropionitrile and 6-halogen-5-(2-methoxyvinyl)pyrimidin-4-ylamine to generate (3R)-cyclopentyl-3-[4-(5-(2-methoxyvinyl)pyrimidin-4-ylamine)pyrazol-1-yl]propionitrile; and (2)carrying out a protection group removing and ring-closure reaction on the (3R)-cyclopentyl-3-[4-(5-(2-methoxyvinyl)pyrimidin-4-ylamine)pyrazol-1-yl]propionitrile to generate a JAK inhibitor ruxolitinib. According to the present invention, the new ruxolitinib preparation route is provided, wherein each reaction of the route has the high yield, the total yield of the route is high, the purity of theobtained product is good, the post-treatment of the reaction is simple, and column chromatography is not required; by adopting the route, the required raw materials or catalysts and other materials are relatively easy to obtain; and compared to the method in the prior art, the method of the present invention is economical and is suitable for industrial production.

Preparation methods of JAK inhibitor and salt thereof

View all

Owner:SUZHOU VIGONVITA LIFE SCIENCES CO LTD

Intermediate of JAK inhibitor, and preparation method thereof

ActiveCN107759623AHigh yieldHigh reaction yieldGroup 3/13 element organic compoundsState of artRuxolitinib

The present invention relates to a novel key intermediate of a JAK inhibitor ruxolitinib, and a preparation method thereof, wherein the chemical name of the intermediate is (R)-3-(4-boric acid-1H-pyrazole-1-yl)-3-cyclopentylpropionitrile. According to the present invention, the new ruxolitinib preparation route is provided, wherein each reaction of the route has the high yield, the total yield ofthe route is high, the purity of the obtained product is good, the post-treatment of the reaction is simple, and column chromatography is not required; by adopting the route, the required raw materials or catalysts and other materials are relatively easy to obtain; and compared to the method in the prior art, the method of the present invention is economical and is suitable for industrial production.

Intermediate of JAK inhibitor, and preparation method thereof

View all

Owner:SUZHOU VIGONVITA LIFE SCIENCES CO LTD

New application of sorafenib, regorafenib and analogues or derivatives thereof

ActiveCN111870600AExempt from transplantSmall burdenAntineoplastic agentsHeterocyclic compound active ingredientsChemical synthesisRed blood cell

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.

New application of sorafenib, regorafenib and analogues or derivatives thereof

View all

Owner:THE SECOND XIANGYA HOSPITAL OF CENT SOUTH UNIV

Reagent composition for improving cell transfection efficiency

ActiveCN108715865AEasy to operateLow biological toxicityMicroencapsulation basedVector-based foreign material introductionTofacitinibRuxolitinib

The invention relates to a reagent composition for improving the cell transfection efficiency, and belongs to the technical field of biology. The reagent composition comprises two or more of a compound BX975 which is 0.01 to 10 micrometers, a compound Ruxolitinib which is 0.1 to 100 micrometers, a compound Tofacitinib which is 0.1 to 100 micrometers, and a compound Actinomycin D which is 0.1 to 100 nM. Reagent mixed liquor and compounds containing NDA and transfection reagents or lentivirus packaged with destination vector are respectively added into cell culture fluid, so that the cell transfection efficiency is improved. The reagent composition is simple to operate, high in repeatability and large in application range, and is successfully applied to cell lines, such as L929 and BI, and primary cell, such as mice primary lung fibrocyte and T lymphocyte.

Reagent composition for improving cell transfection efficiency

View all

Owner:FUJIAN NORMAL UNIV

Method of enhancing immune-based therapy

PendingUS20220000872A1Good curative effectOrganic active ingredientsMammal material medical ingredientsRuxolitinibOncology

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.

Method of enhancing immune-based therapy

View all

Owner:ONCOTRACKER INC

Synthesis process of ruxolitinib

ActiveUS20190023712A1Mild reaction conditionsShort stepsGroup 4/14 element organic compoundsBlood disorderDrugs synthesisRuxolitinib

The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production.

View all

Owner:CHIA TAI TIANQING PHARMA GRP CO LTD

Use of Ruxolitinib in preparation of drug for treating M2 type acute myeloid leukemia

ActiveCN104398520AOvercoming TRAIL ResistanceIncreased sensitivityOrganic active ingredientsPeptide/protein ingredientsRuxolitinibAPOPTOGENIC PROTEIN

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.

Use of Ruxolitinib in preparation of drug for treating M2 type acute myeloid leukemia

View all

Owner:THE FIFTH PEOPLES HOSPITAL OF SHANGHAI FUDAN UNIV

Method for synthesizing ruxolitinib intermediate (R)-3-(4-bromo-1H-pyrazol-1-yl)-3-cyclopentyl propionitrile

InactiveCN105461630ASimple methodHigh yieldOrganic chemistryRuxolitinibSquaric acid amide

The invention relates to a method for synthesizing a ruxolitinib intermediate (R)-3-(4-bromo-1H-pyrazol-1-yl)-3-cyclopentyl propionitrile. The method includes the steps that 3-cyclopentyl-2-cyanoacrylate (I) serves as a raw material, the 3-cyclopentyl-2-cyanoacrylate (I) and 4-bromo-1H-pyrazol (II) are subjected to Michael addition under the condition of a chiral squaric acid amide catalyst (III), and (R)-3-(4-bromo-1H-pyrazol-1-yl)-2-cyano-3-cyclopentyl propanoic acid alkyl ester (IV) is obtained; the (R)-3-(4-bromo-1H-pyrazol-1-yl)-2-cyano-3-cyclopentyl propanoic acid alkyl ester (IV) is hydrolyzed and decarboxylated to obtain the (R)-3-(4-bromo-1H-pyrazol-1-yl)-3-cyclopentyl propionitrile (V). The synthesis method is simple, the product yield can be 80% or above, the enantioselectivity of the product is 90% or above, conditions are moderate, operation is easy, production cost is low, and the method can be used for industrial production.

Method for synthesizing ruxolitinib intermediate (R)-3-(4-bromo-1H-pyrazol-1-yl)-3-cyclopentyl propionitrile

View all

Owner:滨州市帅博木业有限公司

Intermediate of jak inhibitor and preparation method thereof

ActiveCN107759623BHigh yieldHigh reaction yieldGroup 3/13 element organic compoundsPtru catalystRuxolitinib

The present invention relates to a novel key intermediate of JAK inhibitor ruxolitinib and a preparation method thereof. The chemical name of the intermediate is (R)-3-(4-boric acid-1H-pyrazole-1-yl)-3 ‑Cyclopentapropionitrile. The present invention provides a new route for the preparation of ruxolitinib, each reaction step of the route has relatively high yield, the total reaction yield is high, the obtained product has good purity, the post-treatment of the reaction is simple, and no column chromatography is required; Moreover, by adopting this route, the required raw materials or used catalysts and other substances are relatively easy to obtain. Compared with the prior art, the method of the present invention is more economical and more suitable for industrial production.

View all

Owner:SUZHOU VIGONVITA LIFE SCIENCES CO LTD

Application of jak-1 signal pathway inhibitor in preparation of medicine for treating brain injury

ActiveCN111067904BReduce formationImprovement of neurological impairmentOrganic active ingredientsNervous disorderBone marrow fibrosisInjury brain

The invention relates to the application of JAK-1 signaling pathway inhibitors in the preparation of drugs for treating brain injury and / or protecting brain nerves. Inhibitors of the JAK‑1 signaling pathway (one of which is Ruxolitinib, a clinical drug approved by the FDA for the treatment of myelofibrosis) exert neuroprotective effects by (but not limited to) inhibiting the process of pyroptosis. Injured patients provide new theoretical and technical means.

Application of jak-1 signal pathway inhibitor in preparation of medicine for treating brain injury

View all

Owner:SUZHOU UNIV

A kind of synthetic method of 4-chloro-7h-pyrrolo[2,3-d]pyrimidine

ActiveCN107011347BShort synthetic routeHigh yieldOrganic chemistryRuxolitinibEthyl Chloride

The invention discloses a synthetic method of 4-chloro-7H-pyrrolo[2,3-d] pyrimidine. The compound is an important intermediate for synthesizing rheumatoid arthritis JAK inhibitors: ruxolitinib and tofacitinib. The synthetic method comprises the following steps: by taking a compound I (4,6-dichloro-5-allyl pyrimidine) as an initial raw material, performing a nucleophilic substitution reaction with ammonia water to generate a compound II; then performing a reaction on the compound II and ozone and performing a reduction reaction to generate a compound III; and finally, performing self ring-closing reaction in an acidic environment to generate a compound IV, that is, the 4-chloro-7H-pyrrolo[2,3-d] pyrimidine. The synthetic route is as shown in the formula in the description. According to the synthetic process provided by the invention, the raw material is cheap and easily available, the synthetic route is simple, the cost is low, the yield is high, and the synthetic method is easy for industrial production.

A kind of synthetic method of 4-chloro-7h-pyrrolo[2,3-d]pyrimidine

View all

Owner:EAST CHINA NORMAL UNIV +1

Deuterated derivative of ruxolitinib

ActiveCN110229159AOrganic active ingredientsOrganic chemistryRuxolitinibMedicinal chemistry

The present invention discloses a deuterated derivative of ruxolitinib. One embodiment provides a compound of a formula A, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound, and a method for treating indications disclosed in the specification.

View all

Owner:CONCERT PHARMA INC

Use of MDM2 inhibitors for treatment of myelofibrosis

PendingCN114450008AOrganic active ingredientsAntineoplastic agentsRuxolitinibPharmaceutical drug

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.

Use of MDM2 inhibitors for treatment of myelofibrosis

View all

Owner:NOVARTIS AG

USE OF an anti-P-selectin antibody

InactiveUS20210002374A1Useful in treatmentOrganic active ingredientsImmunoglobulins against cell receptors/antigens/surface-determinantsAntiendomysial antibodiesRuxolitinib

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.