480 results about "Cytidine" patented technology

The present invention provides an oral formulation of a cytidine analog, including, 5-azacytidine, for delivery to the lower gastrointestinal tract, including, the large intestine; methods to treat diseases associated with abnormal cell proliferation by treatment with the oral formulations of the present invention; and methods to increase the bioavailability of a cytidine analog upon administration to a patient by providing an oral formulation of the present invention.

The present invention provides methods for generating CMP-sialic acid in a non-human host which lacks endogenous CMP-Sialic by providing the host with enzymes involved in CMP-sialic acid synthesis from a bacterial, mammalian or hybrid CMP-sialic acid biosynthetic pathway. Novel fungal hosts expressing a CMP-sialic acid biosynthetic pathway for the production of sialylated glycoproteins are also provided.

Oral formulations of pharmaceuticals are provided with enhanced bioavailability by targeting specific regions of the gastrointestinal tract. Particularly, water soluble and acid-labile drugs such as cytidine analogs (e.g., decitabine) and 2'-deoxyadenosine analogs (e.g., pentostatin) are formulated with pH-sensitive polymers so that these drugs are preferably absorbed in the upper regions of the small intestine, such as the jejunum. In addition, drugs with poor oral bioavailability such as camptothecin compounds (e.g., 9-nitro-camptothecin) can also be formulated using similar strategies in order to significantly improve their oral bioavailability. These formulations can be used to treat a wide variety of diseases or conditions, such hematological disorders, benign tumors, cancer, restenosis, inflammatory diseases, and autoimmune diseases.

The invention provides a method for continuous production of polyformaldehyde dimethyl ether. The method is characterized by comprising the following steps: a) feeding dimethoxymethane and hot-melted paraformaldehyde into a fixed bed reactor and adopting an acidic resin catalyst, so as to prepare polyformaldehyde dimethyl ether (DMM3-8), wherein the reaction temperature is 120-180 DEG C and the pressure is 0.1-10 MPa; b) cooling the reaction product, and then performing adsorptive separation through a dehydrating tower, so as to obtain polyformaldehyde dimethyl ether of which most water, cytidine glycol and hemiacetal are desorbed; c) feeding the polyformaldehyde dimethyl ether subjected to desorption into a distillation tower for separation, wherein most of a low-boiling component (dimethoxymethane (DMM)), poly-di-formaldehyde dimethyl ether (DMM2), a by-product (methanol) and triformol are extracted first, and then the materials in a tower kettle are fed into a rectifying tower in the next step, so as to extract the rest of the DMM2 and the triformol; and d) returning the low-boiling component (dimethoxymethane (DMM)), the methanol, the DMM2 and the triformol, which are evaporated out by the distillation tower and the rectifying tower in the last step, into the fixed bed reactor to continue to react to prepare polyformaldehyde dimethyl ether.

Methods of treating certain neurological diseases using exogenous uridine or a uridine source alone as a precursor of endogenous cytidine, particularly in the human brain, are disclosed. Methods are also disclosed wherein exogenous uridine or a uridine source is combined either with drugs increasing uridine availability or with compounds that serve as a source of choline in phospholipid synthesis.

A method for preparing a nucleic acid probe is provided. The method comprises forming an activated cytosine or cytidine by a bisulfite catalyzed reaction; and covalently linking a reporter molecule to the activated cytosine or cytidine, wherein said activating step, said covalently linking step, or both are conducted in the presence of microwave energy. Also provided by the invention are nucleic acid probes.

The present invention provides pharmaceutical formulations of cytidine analogs and derivatives, such as 5-azacytidine, 5-aza-2′-deoxy-2′,2′-difluorocytidine, 5-aza-2′-deoxy-2′-fluorocytidine, 2′-deoxy-2′,2′-difluorocytidine, and cytosine 1-β-D-arabinofuranoside, as well as methods of manufacturing the formulations. In particular, the cytidine analog or derivative is formulated with a cyclodextrin compound to stabilize and/or enhance solubility of the drug. Kits and methods for using the pharmaceutical formulations are also provided, including methods of administering the cytidine analog or derivative to treat conditions or diseases, such as cancer and hematological disorders.

The invention provides a method of regulating water and mucin secretions and fluid transport in the gastrointestinal tract. The invention also provides a method for treating a gastrointestinal disease in which the mucosal barrier of the gastrointestinal system is impaired. The invention additionally provides a method for correcting disorders of fluid secretion or absorption in the gastrointestinal system. The method comprises administering to a patient a pharmaceutical composition comprising a purinergic P2Y receptor agonist, in an amount effective to regulate water and mucin secretions or to correct abnormal fluid transport in the gastrointestinal tract. The pharmaceutical composition used in this invention comprises a P2Y purinergic receptor agonist such as uridine 5'-diphosphate (UDP), uridine 5'-triphosphate (UTP), cytidine 5'-diphosphate (CDP), cytidine 5'-triphosphate (CTP), adenosine 5'-diphosphate (ADP), adenosine 5'-triphosphate (ATP), and their analogs; and dinucleotide polyphosphate compounds of general Formula (IV). Said compound is prepared in an oral form, an injectable form, or a suppository form, and administered to a patient.

The invention relates to compositions comprising acyl derivatives of cytidine and uridine. The invention also relates to methods of treating hepatopathies, diabetes, heart disease, cerebrovascular disorders, Parkinson's disease, infant respiratory distress syndrome and for enhancement of phospholipid biosynthesis comprising administering the acyl derivatives of the invention to an animal.

A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5′-triphosphate [UTP], dinucleotides, cytidine 5′-triphosphate [CTP], adenosine 5′-triphosphate [ATP], or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.

The present disclosure provides methods of treating diseases or disorders with oral cytidine analogs (e.g., 5-azacytidine) in combination with anti-PD1/anti-PDL1 antibodies (e.g., pembrolizumab or durvalumab). The diseases or disorders include, but are not limited to, relapsed or refractory myelodysplastic syndromes, acute myeloid leukemia, ovarian cancer, or non-small cell lung cancer.

The invention provides methods for treating or preventing psychiatric disorders, substance abuse disorders, and other conditions, e.g., cardiovascular disease and cancer, involving administration of a therapeutically-effective amount of a cytosine-containing or cytidine-containing compound, creatine-containing compound, adenosine-containing, adenosine-elevating compound, omega-3 fatty acids, or combinations thereof to a mammal. The invention further provides methods of enhancing neurodevelopment and delaying premature pregnancy by administration of an effective amount of a cytosine-containing or cytidine-containing compound, creatine-containing compound, adenosine-containing, adenosine-elevating compound, omega-3 fatty acids, or combinations thereof to a mammal.

[PROBLEMS] To provide a derivative of a cytidine metabolic antagonist which can exert a high therapeutic effect at a low dose.

[MEANS FOR SOLVING PROBLEMS] A polymeric derivative of a cytidine metabolic antagonist which comprises a polymeric compound having a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a cytidine metabolic antagonist, which has such a structure that the carboxyl group in the side chain of the polymeric compound and an amino group in the cytidine metabolic antagonist are bound together to form an amide bond.

The present invention is directed to a method of altering the amount or composition of synovial fluids secreted from joints in a subject in need of such treatment. The method comprises administering to a subject a pharmaceutical composition comprising a P2Y purinergic receptor agonist in an amount effective to alter the amount or composition of synovial fluids. The P2Y purinergic receptor agonist is administered in an amount effective to stimulate secretion of synovial fluid, lubricin, hyaluronic acid, or surface-active phospholipids; to enhance joint lubrication; or to treat osteoarthritis. The pharmaceutical compositions useful in the present invention comprise a P2Y purinergic receptor agonist of Formula I and include, but are not limited to: uridine-, adenosine-, cytidine-5′-di- or triphosphates, dinucleoside polyphosphates, and analogs thereof. The invention is useful for treating conditions associated with reduced joint lubrication and joint stiffness, such as osteoarthritis.

The invention relates to a method for testing a sequence of a nucleic acid single molecule in the technical field of biology, which comprises the following steps: respectively detecting Raman spectrumsignals of deoxyadenosine 5'-phosphoric acid, deoxyguanosine 5'-phosphoric acid, deoxycytidine 5'-phosphoric acid, deoxythymidine 5'-phosphoric acid, methyldeoxycytidine 5'-phosphoric acid, adenosine5'-phosphoric acid, vernine 5'-phosphoric acid, cytidine 5'-phosphoric acid and uridine 5'-phosphoric acid and establishing a standard curve; cutting a nucleic acid molecule to be detected by exonclease and detecting the Raman spectrum signal transmitted by a cut product when passing through a zero mode waveguide by the trigger of a laser; converting the Raman spectrum signal obtained in the step2 into concrete ribotide according to the standard curve obtained in the step 1 and obtaining the concrete sequence of the nucleic acid molecule to be detected by combining the cutting direction of the exonclease. The method can directly detect a natural nucleic acid sequence without a mark and has high detecting speed and detecting quality and low detecting cost.

The invention provides a recombinant microorganism for producing cytidine and a method for producing the cytidine from the recombinant microorganism. A degradation and use gene of the cytidine is knocked off, and the gene encodes cytidine ammonialyase, ribonucleotide hydrolase, cytidine/uridine kinase and nucleoside transporter. Meanwhile key enzymes in biological synthesis process of the cytidine are over-expressed, including degrading cytidine triphosphoric acid to cytidine triphosphoric acid pyrophosphorylase of the cytidine monohosphoric acid, and catalyzing the cytidine monohosphoric acid to cytidine monohosphoric acid phosphorylase of the cytidine. In addition, pyrimidine nucleoside process is subjected to genetic engineering reform, and feedback inhibition of the synthesis process is relieved. By using a biological fermentation method, the cytidine yield greater than 20g/L can be achieved for a recombinant strain in a fermentation tank of 5L, industrial on-scale production can be achieved, and meanwhile the recombinant microorganism is low in cytidine production cost, small in pollution, green and environmental-friendly and relatively high in popularization and application value.

The invention discloses anextract of Chinese herbs containing alpha-glycoside enzyme inhibitor, which comprises cytidine, 2-(1',2',3',4'-tetrahydroxylbutyl)-5-(2'',3'',4''-trihydroxybutyl)-pyrazine and 1-deoxynojirimycin. The extract can be obtained from leaves, branches and peels of mulberries. The extract can be used for preparing medicament for treating diabetes.