摘要:
The invention provides a polypeptide of calcitonin analogue and use thereof. The polypeptide has such an amino acid sequence that proline-amide residue (Pro-NH.sub.2) at C-terminal of native eel calcitonin is substituted to a homoserine amide residue (Hse.multidot.NH.sub.2).
摘要:
The modified polypeptide compound of the present invention is represented by the following general formula ((SEQ ID NO: 2)-X):His-Ser-Asp-Ala-Val-Phe-Thr-Gly-Asn-Tyr-Thr-Lys-Leu-Arg-Lys-Gln-Leu-Ala-Ala-Lys-Lys-Tyr-Leu-R.sup.1 -Lys-Ala-Leu-R.sup.2 -Hse-Xwherein R.sup.1 represents an Asn, Lys or Gln residue, R.sup.2 represents a Lys or Arg residue, Hse represents a homoserine residue, and X represents NHR.sup.3 or NR.sup.4 R.sup.5, wherein R.sup.3 represents a hydrocarbon residue having 18 or less carbon atoms or a polyalkylamine having 2 or more amino groups in its molecule, or R.sup.4 and R.sup.5 represent hydrocarbon residues, provided that the total carbon number of R.sup.4 and R.sup.5 is 18 or less. This modified polypeptide compound has a strong activity as a smooth muscle relaxant, and has excellent stability and prolonged duration of action. These characteristics make it suitable as an active ingredient in a drug for preventing and treating bronchial asthma and impotence.
摘要翻译:本发明的修饰多肽化合物由以下通式((SEQ ID NO:2)-X)表示:His-Ser-Asp-Ala-Val-Phe-Thr-Gly-Asn-Tyr-Thr-Lys -Leu-Arg-Lys-Gln-Leu-Ala-Ala-Lys-Lys-Tyr-Leu-R1-Lys-Ala-Leu-R2-Hse-X其中R1表示Asn,Lys或Gln残基,R2表示 Lys或Arg残基,Hse表示高丝氨酸残基,X表示NHR3或NR4R5,其中R3表示碳原子数为18以下的烃残基或其分子中具有2个以上氨基的多烷基胺,或者R4和R5表示烃残基 条件是R4和R5的总碳数为18以下。 这种修饰的多肽化合物作为平滑肌松弛剂具有强烈的活性,并且具有优异的稳定性和延长的作用持续时间。 这些特征使其适合作为预防和治疗支气管哮喘和阳a药物的有效成分。
摘要:
The invention relates to a hydantoin derivative, salt thereof, process for the preparation thereof, and medicine containing the derivative. The derivative is represented by the formula ##STR1## wherein M is --CONH--NHR.sup.1 group, --CONH--OR.sup.2 group, ##STR2## in which R.sup.1 is hydrogen atom, an alkyl group, an alkenyl group, a phenyl radical, a substituted phenyl group, a naphthyl radical, a substituted naphthyl group, a pyridyl radical, a furyl radical or a thienyl radical, R.sup.2 is a hydrogen atom, an alkyl group, a phenyl radical or a substituted phenyl group, R.sup.3 and R.sup.4 are the same or different independently, each being a phenyl radical, or an aralkyl group, or R.sup.3 may form a substituted or non-substituted C.sub.5-6 saturated heterocyclic ring together with R.sup.4 and a possible nitrogen or oxygen atom, R.sup.5 forms a substituted or non-substituted saturated heterocyclic ring together with R.sup.6 and a possible nitrogen or oxygen atom, R.sup.7 is a nitroxy radical or a heteroaryl group, .sub.m and .sub.n are an integer of 2 to 5, Q is a hydrogen atom or ##STR3## in which R.sup.8 and R.sup.9 are the same or different independently, each being a substituted or non-substituted alkyl group, or R.sup.8 may form a substituted or non-substituted C.sub.5-6 saturated heterocyclic ring together with R.sup.9 and a possible nitrogen or oxygen atom, .sub.r is an integer of 2 to 5, T and X are the same or different independently, each being a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or an alkylmercapto group, and Z is an oxygen or sulfur atom.The derivatives and salts thereof are useful for the treatment of complications of diabetes and circulatory diseases.
摘要:
A multi-layered film preparation is disclosed having a drug-containing layer which contains at least one water-soluble high molecular weight compound as a main base material, a layer which is made difficult to dissolve in water and positioned at one side of the drug-containing layer and a powdery adhesive compound positioned at the other side of the drug-containing layer.