46 results about "Cladribine" patented technology

Provided are compositions of cladribine and cyclodextrin which are especially suited for the oral and buccal administration of cladribine.

Medical devices, and in particular implantable structures, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic drugs, agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and / or compounds may be utilized to promote healing, including the formation of blood clots. Also, the devices may be modified to promote endothelialization.

The present disclosure relates to a method of treatment of a human patient suffering from a B-cell lymphoproliferative disorders such as B-cell chronic lymphocytic leukemia (B-CLL), splenic marginal zone lymphoma (SMZL), mantle cell lymphoma (MCL), follicular lymphoma (FL), lymphoplasmacytic lymphoma (LPL), and Waldenström syndrome (WS), by the administration of a therapeutically effective amount of 5-aminoimidazole-4-carboxamide riboside (acadesine) or its precursors (eg. its mono-, di- and tri-5′-phosphates). This makes acadesine and its bioprecursors (eg. its mono-, di- and tri-5′-phosphates) useful as therapeutic agents for B-cell lymphoproliferative disorders in humans. The surprising feature that T cells are virtually not affected means that the side effect (immunosuppression) is minor, what represents a therapeutical advantage of acadesine over cladribine, fludarabine and other nucleosides known in the art.

2-Chloro-2′-deoxyadenosine, hereinafter referred to as cladribine, or a pharmaceutically acceptable salt thereof may be used in the treatment or amelioration of neuromyelitis optica, hereinafter referred to as NMO e.g. in patients known to have NMO-IgG seropositivity or in patients optic neuritis, myelitis and at least two of MRI evidence of contiguous spinal cord lesion 3 or more segments in length, onset brain MRI nondiagnostic for multiple sclerosis or NMO-IgG seropositivity.

Provided are compositions of cladribine and cyclodextrin which are especially suited for the oral administration of cladribine.

The present invention is related to the use of Cladribine for the preparation of a pharmaceutical formulation for the treatment of multiple sclerosis, especially relapsing-remitting multiple sclerosis or early secondary progressive multiple sclerosis, wherein the preparation is to be orally administered and wherein re-treatments are possible.

A pharmaceutical composition for induction therapy which has a hypomethylating agent and a histone deacetylase inhibitor (“HDAC inhibitor”); wherein the hypomethylating agent is a DNA and histone methylation inhibitor such as cladribine and the HDAC inhibitor is, for example, entinostat, panobinostat, vorinostat, and / or romedepsin; further wherein the hypomethylating agent and the HDAC inhibitor are combined in formulations for various administrations including e.g., a continuous delivery system such as a transdermal patch of at least one reservoir or a plurality of reservoirs, oral, a fixed-dose oral combination, intravenous, and combinations thereof. This pharmaceutical composition for induction therapy is used with a monoclonal antibody in the treatment of various cancers, sarcomas, and other malignancies.

The invention relates to a cladribine preparation administrated by injection and a preparation method thereof. The preparation is characterized by consisting of cladribine, a water-soluble filler, a pH regulator, water for injection and an osmotic pressure regulator, wherein the preparation contains 0.01 to 50 weight percent of cladribine and the balance of pharmaceutical adjuvant or water. The cladribine preparation administrated by the injection of the invention has the advantages of good stability and high bioavailability and satisfies need for injection medicaments required by the treatment of clinical acute and chronic granulocytic leukemia.

The invention relates to cancer therapy drug sustained-release injection containing gemcitabine. The injection comprises sustained-release microspheres and dissolvent, wherein, the sustained-release microspheres comprise active ingredients for cancer therapy and sustained-release auxiliary materials, and the dissolvent is special dissolvent containing suspending agent. The active ingredients for cancer therapy comprise antimetabolite of gemcitabine or antimetabolite selected from zalcitabine, emtritabine, galocitabine, ibacitabine, ancitabine, decitabine, flurocitabine, enocitabine, imidazoletabine, capecitabine, gemcitabine, fludarabine or cladribine, and / or antimetabolite synergist selected from phosphoinositide 3-kinase inhibitor, pyrimidine analogs and / or DNA repair enzyme inhibitor; the sustained-release auxiliary materials comprise polifeprosan, bi-fatty acid, decanedioic copolymer, polylactic copolymer and EVAc; the viscocity of the suspending agent is 100cp to 3000cp (at 20 to 30 DEG C) and the suspending agent is selected from sodium carboxymethyl cellulose. The sustained-release microspheres can also be produced into sustained-release implant, and by injecting or positioning the sustained release agent in tumor or tumor margin, the efficacy of non-operative treatment such as radiation treatment and chemical treatment can be enhanced.

The invention discloses a novel method for synthesizing cladribine through a nitration-chlorination method. According to the method, cheap 6-chloropurine and 1-chloro-2,3,5-tris-O-p-chlorobenzoyl-D-ribose are taken as raw materials, sodium hydride is taken as alkali, acetonitrile is taken as reaction solvent, and a beta isomer is obtained through a high-selectivity reaction; the obtained beta isomer does not need to remove protecting groups, the beta isomer reacts with trifluoromethanesulfonic anhydride after being separated, and nitryl is introduced at the second position; the nitryl is transformed into chlorine atoms in an ethanol solution of NH4Cl; two steps of reactions of protecting group removal and chlorine atom ammonolysis are completed in a methanol solution saturated by ammonia gas, and then the cladribine is obtained through four steps at the total yield of 78%. The method has the advantages that the raw materials are low in cost and easy to obtain, the technology is simple and convenient, the total yield is higher, the cost is low, amplification is easy, expensive reagents and poisonous and harmful heavy metal catalysts are prevented from being used, and when the reaction scale is expanded to the 100-g scale, the yield is not decreased obviously. A novel synthesizing path is supplied to synthesizing of the cladribine, and the potential application prospect is achieved.

This invention relates to derivatives of cladribine of Formula (I). The compounds are phosphoramidate derivatives in which the phosphoramidate moiety is situated on the 3′-hydroxyl group of cladribine. The invention also relates to pharmaceutical formulations of the cladribine derivatives and their use in methods of treatment. The compounds are useful in the treatment of cancer.

The invention relates to a slow-release injection containing nolatrexed and a synergistic agent of the nolatrexed, which consists of a slow-release microballoon sphere and a solution medium, wherein, the slow-release microballoon sphere comprises active anti-cancer ingredients and slow-release accessories; and the solution medium is a special solution medium containing a suspending agent. The active anti-cancer ingredients are antimetabolites, such as pemetrexed, rumitrexed, raltitrexed, nolatrexed, carmofur, dexrazoxane, tegafur, zalcitabine, emtricitabine, ibatabine, ancitabine, decitabine, flurocitabine, enocitabine, imidazoletabine, capecitabine, gemcitabine, fludarabine or cladribine, and the like, and synergistic agents of the antimetabolites selected from topoisomerase inhibitors and / or tetrazine compounds; the slow-release accessories are selected from one of polifeprosan, di-fatty acid and decanedioic acid copolymer, polylactic acid copolymer and EVAC or the combination thereof; the viscosity of the suspending agent is 100cp to 3000cp (at the temperature of 20 DEG C to 30 DEG C) and the suspending agent is selected from carboxymethylcellulose sodium and the like. The slow-release microballoon sphere can also be prepared into a slow-release implant used for being injected or put in tumors or the surrounding of the tumors so as to enhance the effects of radiotherapy and chemotherapy.

Disclosed is an anticancer slow release agent which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow releaseauxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer antibiotics are selected from Idarubicin, Valtaxin, Pirarubicin and Mitoxantrone, The anti-metabolite drugs are selected from Pemetrexed, Carmustine, Tegafur, Zalcitabine, Emtritabine, Galocitabine, Ibacitabine, Ancitabine, Decitabine, Flurocitabine, Enocitabine, Imidazoletabine, Capecittabine, Gemcitabine, Fludrarbine, Raltitrexed, Dexrazoxane, Cladribine, Nolatrexed and folic acid, The slow release auxiliary materials are selected from EVAc, Polifeprosan, sebacylic acid copolymer, lactic acid, the viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C), and is selected from sodium carboxymethylcellulose. The slow release microspheres can also be prepared into slow release implanting agent for injection or placement in or around tumor.

The present invention relates to the new application of known compounds, especially the application of six small molecular drugs in inhibiting canine parvovirus. The invention provides the purposes of Closantel, Closantel Sodium, Gemcitabine HCl, Trifluridine, Gemcitabine and Cladribine in the preparation of the medicine for inhibiting the replication of canine parvovirus, the active ingredient of the medicine comprises Closantel, Closantel Sodium, Gemcitabine HCl, Trifluridine, Gemcitabine and / or Cladribine. The data prove that these 6 small molecule drugs all have excellent inhibitory effects on CPV replication, and can inhibit the expression of VP2 protein of different genotypes of CPV virus.