Abstract:
PROBLEM TO BE SOLVED: To provide new semi-synthesized macrolides having antibacterial activity, a pharmaceutical composition including these compounds, and a medical treatment method of remedy.SOLUTION: There is provided a 6-O-substituted erythromycin ketolide derivative expressed by formula (IV-A), where in formula, Rc is hydrogen or a hydroxy-protective group; R is a substituted methyl group; A, B, D and E are each selected from hydrogen, a 1-6C alkyl which may be substituted by a substituent, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, hydroxy, 1-6C alkoxy, and halogen of Br, Cl, F or I, or the like, under conditions that at least two of A, B, D and E are both hydrogen.
Abstract:
PROBLEM TO BE SOLVED: To provide new polymorphic and other crystalline forms of FTC, to provide a new method for preparing and isolating polymorphic and other crystalline forms of FTC and to provide a use of FTC polymorphic body, FTC of other phases and treatment purpose.SOLUTION: A solid phase of (-)-cis-FTC, which can be distinguished from form (I) (-)-cis-FTC by means of X-ray power diffraction pattern, thermal properties and methods of manufacture and is designated herein as amorphous (-)-FTC and (form II (-)-cis-FTC) and (form III (-)-cis FTC), is provided. Likewise, hydrated crystalline form of (±)-cis-FTC (that is, cis-FTC of racemic body) which can be distinguished from other forms of FTC by means of X-ray power diffraction pattern, thermal properties and methods of manufacture, and a dehydrated form of the hydrate are provided. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. These forms are particularly desirably used for treating HIV or hepatitis B.
Abstract:
PROBLEM TO BE SOLVED: To provide small particles of lipid-regulating drugs, more preferably fenofibrate, having comparable dissolution and absorption characteristics to the particles of such drugs prepared by the prior art techniques without the need of micronizing the lipid-regulating drug or utilizing surfactants.SOLUTION: A process for preparing a formulation of a lipid-regulating drug comprises dissolving the lipid-regulating drug such as fenofibrate in a solvent free of surfactant, premixing an excipient such as lactose, starch, polyvinyl pyrrolidone, and magnesium stearate, wet granulating the drug solution/excipient mixture, drying the mixture and forming a final dosage form.
Abstract:
PROBLEM TO BE SOLVED: To provide a new antigen construct useful as a reagent in immunoassay for detection and identification of antibodies to human immunodeficiency virus type 1 (HIV-1) group M, HIV-1 group O and human immunodeficiency virus type 2 (HIV-2), polynucleotides useful for the preparation of antigens, DNA clone, expression vectors, and transformed host cells.SOLUTION: There are provided isolated HIV-1 group O env polypeptides obtained from the HIV-1 isolate HAM112, as well as (a) antigen constructs comprising fusions of one or more of each of HIV-1 group O env polypeptides and HIV-1 group M env polypeptide and (b) additional antigen constructs containing additional group O sequences.
Abstract:
PROBLEM TO BE SOLVED: To provide a novel VR1 antagonist useful for treatment of pain, inflammatory thermalgesia, urorrhea and bladder hyperactivity.SOLUTION: The compound is represented by formula (I) (wherein Xto Xare each a nitrogen atom or the like; R, Rand Rare each a hydrogen atom or the like; Zand Zare each an oxygen atom or the like; and L is an alkenylene or the like).
Abstract:
PROBLEM TO BE SOLVED: To improve calibration accuracy to seasonal and psychological variation of tissue property.SOLUTION: A noninvasive measurement instrument has a measurement probe 1 supposed to get into touch with a trial subject, a light source 6 and a photodetector 7 to be connected to the measurement probe, and a computer section 5 for controlling the light source and photodetector to optically and noninvasively measure information relating to glucose in the trial subject and predict the value of glucose by a calibration model from an output of the photodetector. The computer section updates the calibration model by executing regression estimation based on the acquired data by noninvasive measurement on a different day and the corresponding reference measurement value and predicts glucose density from the acquired data by noninvasive measurement by using the updated calibration model.
Abstract:
PROBLEM TO BE SOLVED: To provide an improved HIV protease inhibitor that is very potent, that has reduced side-effects and that is effective against resistant strains of HIV.SOLUTION: This invention relates to: a compound of formula (I) as the HIV protease inhibitor; or a pharmaceutically acceptable salt form, stereoisomer, ester, salt of the ester, prodrug, salt of the prodrug, or combination thereof.
Abstract:
PROBLEM TO BE SOLVED: To provide a solid pharmaceutical dosage form that gives improved oral bioavailability for inhibitors of HIV protease.SOLUTION: The solid pharmaceutical dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant. The pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50°C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.
Abstract:
PROBLEM TO BE SOLVED: To identify four genes involved in an elongation of polyunsaturated acid (i.e., "elongase"); and to provide a use thereof. SOLUTION: Two of four genes involved in an elongation of polyunsaturated acid (i.e., "elongase") are also involved in the elongation of monounsaturated fatty acids. In particular, elongase is utilized in the conversion of gamma linolenic acid (GLA) to dihomogama linolenic acid (DGLA) and in the conversion of DGLA or 20:4n-3 to eicosapentaenoic acid (EPA). DGLA may be utilized in the production of polyunsaturated fatty acids, such as arachidonic acid (AA), docosahexaenoic acid (DHA), EPA, adrenic acid, ω6-docosapentaenoic acid or ω3-docosapentaenoic acid, added to pharmaceutical compositions, nutritional compositions, animal feeds, as well as other products such as cosmetics. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide an antibody which binds to human interleukin-18 (hIL-18), to provide a method for producing the same; and to provide a method for using the same. SOLUTION: There are provided a neutrally binding protein which is an antibody comprising immune globulin heavy chain and light chain having specific amino acid sequences and specifically binding to human IL-18, and has an ability to neutralize IL-18; a method for producing the antibody; and a use for detecting hIL-18 or treating a human testee suffering from a disease wherein the activity of hIL-18 is harmful. COPYRIGHT: (C)2011,JPO&INPIT