摘要:
An object of the present invention is to provide a novel double-stranded RNA that has high resistance to nuclease and cellular uptake efficiency and that can produce an excellent RNA interference effect. The present invention provides a double-stranded lipid-modified RNA comprising a sense strand having a nucleotide sequence complementary to a target sequence in a target gene, and an antisense strand having a nucleotide sequence complementary to the sense strand, the double-stranded RNA being capable of suppressing the expression of the target gene, and the sense strand having a double-stranded lipid bound directly or via a linker to at least one of the first to sixth nucleotides from the 5' end.
摘要:
The present invention relates to novel amino acid and nucleic acid sequences of cyclic nucleotide-specific phosphodiesterases from the parasite Leishmania major. The invention also relates to nucleic acid constructs, vectors, and host cells comprising the nucleic acid sequences as well as methods for producing and using the amino acid and nucleic acid sequences. The invention further relates to the use of these sequences, and of antibodies directed against these sequences, in the diagnosis and treatment of disorders related to the infection of Leishmania major, including the identification of compounds that form complexes with the polypeptides and nucleic acids of the present invention.
摘要:
The present invention provides a novel benzodiazepine compound that blocks the I Kur current or the Kv1.5 channel or the IKACH current (the GIRK1/4 channel) potently and more selectively than other K + channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R 1 , R 2 , R 3 , and R 4 are each independently hydrogen or lower alkyl; R 2 and R 3 may be linked to form lower alkylene; A 1 is lower alkylene optionally substituted with one or more hydroxy; and R 5 is group represented by wherein R 6 and R 7 are each independently hydrogen or organic group; X A and X B are each independently bond, lower alkylene, etc.
摘要:
The invention provides an amine salt of a carbostyril derivative formed from a carbostyril derivative represented by the formula (1) [wherein R is a halogen atom; the substituted position of the side chain is 3- or 4-position in the carbostyril skeleton; and the bonding between 3- and 4-positions of the carbostyril skeleton is a single bond or a double bond] and an amine; and the invention is useful as drugs for treating various diseases, especially as aqueous formulations due to the superior water solubility and the superior pharmacologic effects.
摘要:
It is intended to provide an antiaging composition by which skin aging can be effectively retarded and, in particular, skin pigmentation can be improved. It is also intended to provide a method of potentiating the antiaging effect of ascorbic acid or its analog. Namely, an antiaging composition characterized by containing (A) at least one member selected from the group consisting of ascorbic acid, its derivatives and salts thereof; and (B) a purine nucleic acid-related substance. A method of using (A) at least one member selected from the group consisting of ascorbic acid, its derivatives and salts thereof together with (B) a purine nucleic acid-related substance to thereby potentiate the antiaging effect of the component A.
摘要:
An object of the present invention is to provide a novel double-stranded RNA that has high nuclease resistance and high cellular uptake efficiency, and that is capable of producing an excellent RNA interference effect. The present invention provides a lipid-modified double-stranded RNA comprising a sense strand having a nucleotide sequence complementary to a target sequence, and an antisense strand having a nucleotide sequence complementary to the sense strand, the double-stranded RNA being capable of inhibiting the expression of the target gene, the sense strand having a lipid linked to at least one of the first to sixth nucleotides from the 5′ end side directly or via a linker.
摘要:
The present invention provides a heterocyclic compound represented by General Formula (1): wherein R1 is a group R5-Z1-, etc., Z1 is a lower alkylene group, etc., and R5 is a group represented by General Formula; wherein R13 is a hydrogen atom, etc., m is an integer from 1 to 5; R2 is a hydrogen atom: Y is CH or N: A1 is a heterocyclic ring selected from the group consisting of indolediyl groups, wherein the heterocyclic ring may have at least one substituent: T is a group -CO-, etc.: R3 is a hydrogen atom, etc.: R4 is a lower alkyl group optionally substituted by one or more hydroxy groups, etc.: R3 and R4, together with the nitrogen atom to which they bind, may bind to each other and form a 5- to 10-membered saturated heterocyclic ring, wherein the heterocyclic ring may have at least one substituent. The heterocyclic compound of the present invention has excellent effects of suppressing the production of collagen and/or treating tumors.
摘要:
The present invention provides a tetomilast crystal that is industrially easily produced in a large volume. (1) a tetomilast hydrate crystal having a powder X-ray diffraction spectrum having characteristic peaks at 2θ = 10.6°, 12.9°, 21.1°, 22.3° and 25.0°; (2) an anhydrous tetomilast type C crystal having a powder X-ray diffraction spectrum having characteristic peaks at 2θ = 4.2°, 8.2°, 12.0°, 16.4°, 24.7° and 25.9°; (3) a tetomilast acetonitrile solvate crystal having a powder X-ray diffraction spectrum having characteristic peaks at 2θ = 3.6°, 7.1°, 10.6°, 14.2° and 24.8°. These crystals are stable towards heat and moisture, and are also excellent in terms of the disintegration property and dissolution property of tablets. Accordingly, these crystals are preferably used as pharmaceutical compositions.
摘要:
The present invention provides an improved metered dose inhaler utilizing the property of the aerosol canister. The metered dose inhaler includes: a housing body (2); an aerosol canister (3) including a canister body (3a), a valve stem (3b), and a spring urging the valve stem, wherein the valve stem (3b) is held at a fixed position inside the housing body (2), and wherein the canister body (3a) is supported inside the housing body (2) to be depressible against a spring force of the spring; a dose counter (10) including display members (12) and (13) rotatably supported inside the housing body (2), and a control lever (14) swingably supported inside the housing body (2) to rotate the display member (13); and a control cap (20) including a junction member rotatably joined to the control lever (14), and a cap portion (20b) which sheaths the canister body (3a) from a bottom side of the canister body (3a), wherein the control cap (20) causes the control lever (14) to swing.