Abstract: Provided are uses for a substance capable of operating an aberrant gene product, which is prepared by a new drug creation technology that focuses on the cause of disease using information obtained from analysis of structural genes associated with diseases. Thus, the present invention includes (1) a pharmaceutical composition containing a substance capable of operating an aberrant gene product, (2) a method of using said substance for treatment of a disease caused by said product, (3) a screening method for said substance, and (4) a method of preparing a drug for treatment of a disease caused by said product.

Abstract: The present invention is to provide a multiple-agents-binding compound comprising a compound having anti-HIV activity and having no affinity for cell surface protein bound together with a same or different kind of at least one compound having anti-HIV activity and having no affinity for cell surface protein, or a salt thereof, and a pharmaceutical composition for the prevention or treatment of infectious diseases of HIV or AIDS comprising said multiple-agents-binding compound.

Abstract: A peptide represented by the formula: ##STR1## wherein R.sub.1 represents an oil-soluble group; R.sub.2 and R.sub.5 represent a hydrogen atom or a lower alkyl group; R.sub.3 represents an aliphatic group which may have O or S; R.sub.4 represents a heterocyclic-substituted lower alkyl group; R.sub.6 represents a hydrogen atom, a lower alkyl group or an aromatic cyclic group; X represents a group having an aromatic ring; n represents an integer of 0 or more and m represents an integer of 2 or more, or a salt thereof exhibits a marked endothelin receptor-antagonistic action, and the peptide [I] is pharmaceutically useful as a therapeutic agent for hypertension, cardiovascular disease and renal disease, for instance.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is an amino group which may be protected, R.sup.3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S.fwdarw.O, O or CH.sub.2, R.sup.4 is a hydrogen atom, methoxy group or formamido group, R.sup.13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A.sup..sym. is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.

Abstract: A peptide derivative of the formula ##STR1## wherein A is hydrogen or a hydrocarbon acyl having 2 to 18 carbon atoms which is substituted by an amino group at the .alpha.-position; B is F-Gly wherein F is a neutral .alpha.-amino acid residue, or NH-(CH.sub.2)nCO wherein n is an integer of 1 to 4; C is a neutral .alpha.-amino acid residue; and E is L-Arg or D-Arg; when A, B and C are hydrogen, Gly-Gly, and Met or Ile, respectively, E is D-Arg, or its pharmacologically acceptable salt has strong hypotensive and natriuretic activity; therefore it is useful as a therapeutic drug for hypertension, a diuretic, and a therapeutic drug for cardiac and cerebral circulatory diseases.

Abstract: The invention provides chemically modified proteins having a group of the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl, m represents an optional positive integer and n represents an integer 1 to 4, the group being bonded to at least one primary amino group of the protein, and a method of producing the same. The chemically modified proteins according to the invention can be produced by reacting a protein with an imidoester of the formula: ##STR2## wherein R, n and m are as defined above, R' represents a group constituting an imidoester with an adjacent imidoyl group. The chemically modified proteins according to the invention are useful as drugs, among others.

Abstract: The invention provides a compound of the formula (I): R--O--CH.sub.2 CH.sub.2 O.sub.m CH.sub.2).sub.n --Z wherein R is a glycosyl group, m is an optional positive integer, n is an integer from 1 to 3 and Z is --CHO, --CH.sub.2 OH or --COOH.The compound of the formula (I'): R--O--CH.sub.2 CH.sub.2 O.sub.m CH.sub.2).sub.n --CHO wherein R, m and n are as defined above and the formula (I"'): R--OCH.sub.2 CH.sub.2 O.sub.m CH.sub.2).sub.n --COOH wherein R, m and n are as defined above is useful as a chemically modifying agent for protein.The compound of the formula (I"): R--O--CH.sub.2 CH.sub.2 O.sub.m CH.sub.2).sub.n --CH.sub.2 OH wherein R, m and n are as defined above is useful as a protein fractionating agent.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is an amino group which may be protected, R.sup.3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S.fwdarw.O, O or CH.sub.2, R.sup.4 is a hydrogen atom, methoxy group or formamido group, R.sup.13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A.sup..sym. is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.

Abstract: A compound of the formula; ##STR1## wherein R.sup.0 stands for nitrogen-containing heterocyclic group, acyl group or amino-protecting group, Z stands for S, S.fwdarw.O, O or CH.sub.2, R.sup.4 stands for hydrogen atom, methoxy group or formamido group, R.sup.13 stands for hydrogen atom, methyl group, hydroxyl group or halogen atom and A stands for an optionally substituted thiazol-3-yl group forming a fused ring at the 4,5-position or a physiologically or pharmaceutically acceptable salt or ester thereof.This compound is novel and has excellent antibacterial activity.

Abstract: A compound of the formula; ##STR1## wherein R.sup.1 is an amino group which may be protected, R.sup.3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S.fwdarw.O, O or CH.sub.2, R.sup.4 is a hydrogen atom, methoxy group or formamido group, R.sup.13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A.sym. is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.

Abstract: A compound of the formula; ##STR1## wherein R.sup.0 stands for hydrogen atom, nitrogen-containing heterocyclic group, acyl group or esterified carboxyl group, Z stands for S, S.fwdarw.O, O or CH.sub.2, R.sup.4 stands for hydrogen atom, methoxy group or formamido group, R.sup.13 stands for hydrogen atom, methyl group, hydroxyl group or halogen atom and A stands for an optionally substituted imidazol-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a physiologically or pharmaceutically acceptable salt or ester thereof.This compound is novel and has excellent antibacterial activity.

Abstract: A compound of the formula; ##STR1## wherein R.sup.0 stands for hydrogen atom, nitrogen-containing heterocyclic group, acyl group or amino-protecting group, Z stands for S, S.fwdarw.O, O or CH.sub.2, R.sup.4 stands for hydrogen atom, methoxy group or formamido group, R.sup.13 stands for hydrogen atom, methyl group, hydroxyl group or halogen atom and A stands for an optionally substituted pyrazol-2-yl group forming a fused ring at the 1,5-position or a physiologically or pharmaceutically acceptable salt or ester thereof.This compound is novel and has excellent antibacterial activity.

Abstract: Novel polypeptide-diesters, inclusive of salts thereof, which have the formula: ##STR1## wherein A.sub.1 is arginine or lysine or a di- or tripeptide residue having arginine or lysine at its N-terminal; A.sub.2 is an aromatic amino acid residue; A.sub.3 is a neutral amino acid or aromatic amino acid residue; each of the amino acid residues mentioned may be optionally L-configured or D-configured; and n is 0, 1 or 2. These compounds are useful as analgesics.

Abstract: The novel nonapeptide amide derivatives of the formula(Pyr)Glu--R.sub.1 --Trp--Ser--R.sub.2 --(D)--Ala--R.sub.3 --Arg--Pro--NH--R.sub.4wherein R.sub.1 is His, Tyr, Trp or p-NH.sub.2 --Phe; R.sub.2 is Tyr or Phe; R.sub.3 is Leu, Ile or Nle and R.sub.4 is alkyl of 1 to 3 carbon atoms which may be substituted with hydroxyl group have a strong ovulation inducing activity.

Abstract: A guanidino group in an amino acid or a peptide can be protected with a specific group, i.e. pentamethylbenzenesulfonyl, 2,4,6-trimethoxybenzenesulfonyl, 4-methoxy-2,3,5,6-tetramethylbenzenesulfonyl, 4-methoxy-2,6-dimethylbenzenesulfonyl or 4-methoxy-2,3,6-trimethylbenzenesulfonyl, and said group may easily be removed without affecting the amino acid or the peptide to be derived from the protected amino acid or peptide. Thus, the present invention is useful in the synthesis of peptides containing the guanidino group.

Abstract: An .omega.-amino group and/or .alpha.-amino group in an amino acid or a peptide can be protected with a 4-methoxy-2,3,6-trimethylbenzenesulfonyl group, and said group may easily be removed without affecting the amino acid or the peptide. Thus, the present invention is useful in the synthesis of peptide containing .omega.-amino group and/or .alpha.-amino group.

Abstract: An indole group in an amino acid or a peptide can be protected with a group shown by the formula: ##STR1## wherein R.sub.1 and R.sub.5 each is hydrogen, methyl or methoxy; R.sub.2 and R.sub.4 each is hydrogen or methyl; and R.sub.3 is methyl or methoxy, and said group may easily be removed without affecting the amino acid or the peptide to be derived from the protected amino acid or peptide. Thus, the present invention is useful in the synthesis of a peptide containing an indole group.

Abstract: Novel tetrapeptide acylhydrazides, inclusive of acid addition salts thereof, which have the formula: ##STR1## wherein R.sub.1 is hydrogen or methyl, R.sub.2 is lower alkyl; are useful as analgesics.

Abstract: A guanidino group in an amino acid or a peptide can be protected with a specific group, i.e. pentamethylbenzensulfonyl, 2,4,6-trimethoxybenzenesulfonyl, 4-methoxy-2,3,5,6-tetramethylbenzenesulfonyl, 4-methoxy-2,6-dimethylbenzenesulfonyl or 4-methoxy-2,3,6-trimethylbenzenesulfonyl, and said group may easily be removed without affecting the amino acid or the peptide to be derived from the protected amino acid or peptide. Thus, the present invention is useful in the synthesis of peptides containing the guanidino group.

Abstract: The invention provides chemically modified lymphokines comprising a lymphokine moiety and at least one polyethylene glycol moiety of the formula: R.paren open-st.O--CH.sub.2 CH.sub.2 .paren close-st..sub.n wherein R is a protective group for the terminal oxygen and n is at least one, bonded directly to at least one primary amino group of the lymphokine moiety, and a method of producing the same.The chemically modified lymphokines according to the invention can be produced by reacting a lymphokine with an aldehyde of the formula R.paren open-st.O--CH.sub.2 CH.sub.2 .paren close-st..sub.n-1 O--CH.sub.2 CHO wherein R and n are as defined above, in the presence of a reducing agent.The chemically modified lymphokines according to the invention are useful as drugs, among others.