Claims Analysis
Total Claims: 5
Claim 1
Independent Claim
541 words
A peptide derivative of the formula: wherein A is a group of the formula R"O-CO- (wherein R 11 is a lower alkyl group or a phenyl group), or a group of the formula R 12 R 13 N-C(=O)- (wherein R 12 is a lower alkyl group, a cycloalkyl group, a 1- adamantyl group, a phenyl group wherein one or two optional hydrogen atoms on the benzene ring may independently be replaced by a halogen atom, a trifluoromethyl group, a nitro group, an amino group or a formylamino group, a pyridyl group, or a thienyl group, R 13 is a hydrogen atom, a lower alkyl group or a cycloalkyl group, or R 12 and R 13 form, together with the adjacent nitrogen atom, a 5- to 9- membered nitrogen-containing saturated heterocyclic ring having 4 to 8 carbon atoms, wherein among methylene groups forming the ring, one optional methylene group not adjacent to the above nitrogen atom may be replaced by a thio group, and one to four optional hydrogen atoms on the carbon atoms of the heterocyclic ring may independently be replaced by a lower alkyl group, and further two adjacent carbon atoms in the heterocyclic ring may form a benzo-fused ring); B is an oxygen atom or a group of the formula -NR 2- (wherein R 2 is a hydrogen atom or a lower alkyl group); R 3 is a lower alkyl group, a cycloalkyl group, an aryl group, a heterocyclic group, a cycloalkyl lower alkyl group, an aryl lower alkyl group or a heterocyclic lower alkyl group; X 1 is an oxygen atom or a group of the formula -NR 4- (wherein R 4 is a hydrogen atom or a lower alkyl group); R 5 is a 3-indolylmethyl, 3-benzothienylmethyl, 1-naphthylmethyl or benzyl group wherein one or two optional hydrogen atoms on the ring may be replaced by a hydroxyl group, a halogen atom, a formyl group, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkylsulfinyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a nitro group or a group of the formula R 51 -CO-X 2 {wherein R 51 is a lower alkyl group, a lower alkoxy group, or an amino group which may be substituted by a lower alkyl group, and X 2 is an oxygen atom or a group of the formula -NR 52- (wherein R 52 is a hydrogen atom or a lower alkyl group)}; X 3 is an oxygen atom or a sulfur atom; R 6 is a hydrogen atom, or a lower alkyl or lower alkenyl group which may have a substituent selected from the group consisting of a hydroxyl group, a lower alkoxy group, a lower alkylthio group and a heterocyclic group; n is 0 or 1; Y is a hydroxymethyl group, a group of the formula C02 R" (wherein R 71 is a hydrogen atom or a lower alkyl group), a group of the formula CONHR 72 (wherein R 72 is a hydrogen atom or a lower alkyl group which may have a substituent selected from the group consisting of a hydroxyl group, a carboxyl group and a sulfo group), a 1H-tetrazol-5-yl group, a sulfo group and a phosphono group; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
541 words
A peptide derivative of the formula: wherein A is a group of the formula R"O-CO- (wherein R 11 is a lower alkyl group or a phenyl group), or a group of the formula R 12 R 13 N-C(=O)- (wherein R 12 is a lower alkyl group, a cycloalkyl group, a 1- adamantyl group, a phenyl group wherein one or two optional hydrogen atoms on the benzene ring may independently be replaced by a halogen atom, a trifluoromethyl group, a nitro group, an amino group or a formylamino group, a pyridyl group, or a thienyl group, R 13 is a hydrogen atom, a lower alkyl group or a cycloalkyl group, or R 12 and R 13 form, together with the adjacent nitrogen atom, a 5- to 9- membered nitrogen-containing saturated heterocyclic ring having 4 to 8 carbon atoms, wherein among methylene groups forming the ring, one optional methylene group not adjacent to the above nitrogen atom may be replaced by a thio group, and one to four optional hydrogen atoms on the carbon atoms of the heterocyclic ring may independently be replaced by a lower alkyl group, and further two adjacent carbon atoms in the heterocyclic ring may form a benzo-fused ring); B is an oxygen atom or a group of the formula -NR 2- (wherein R 2 is a hydrogen atom or a lower alkyl group); R 3 is a lower alkyl group, a cycloalkyl group, an aryl group, a heterocyclic group, a cycloalkyl lower alkyl group, an aryl lower alkyl group or a heterocyclic lower alkyl group; X 1 is an oxygen atom or a group of the formula -NR 4- (wherein R 4 is a hydrogen atom or a lower alkyl group); R 5 is a 3-indolylmethyl, 3-benzothienylmethyl, 1-naphthylmethyl or benzyl group wherein one or two optional hydrogen atoms on the ring may be replaced by a hydroxyl group, a halogen atom, a formyl group, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkylsulfinyl group, a lower alkylsulfonyl group, a lower alkoxycarbonyl group, a nitro group or a group of the formula R 51 -CO-X 2 {wherein R 51 is a lower alkyl group, a lower alkoxy group, or an amino group which may be substituted by a lower alkyl group, and X 2 is an oxygen atom or a group of the formula -NR 52- (wherein R 52 is a hydrogen atom or a lower alkyl group)}; X 3 is an oxygen atom or a sulfur atom; R 6 is a hydrogen atom, or a lower alkyl or lower alkenyl group which may have a substituent selected from the group consisting of a hydroxyl group, a lower alkoxy group, a lower alkylthio group and a heterocyclic group; n is 0 or 1; Y is a hydroxymethyl group, a group of the formula C02 R" (wherein R 71 is a hydrogen atom or a lower alkyl group), a group of the formula CONHR 72 (wherein R 72 is a hydrogen atom or a lower alkyl group which may have a substituent selected from the group consisting of a hydroxyl group, a carboxyl group and a sulfo group), a 1H-tetrazol-5-yl group, a sulfo group and a phosphono group; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
100 words
The peptide derivative or the pharmaceutically acceptable salt thereof according to Claim 1, wherein R 5 is a 3-indolylmethyl group wherein the indole ring is substituted at the 1-position and/or 2-position by one or two substituents selected from the group consisting of a lower alkoxy group, a lower alkylthio group, a lower alkanoyloxy group, a lower alkoxy carbonyl group, a halogen atom or a lower alkyl group; and R 6 is a lower alkyl group or a lower alkenyl group which may have a substituent selected from the group consisting of a lower alkoxy group and a lower alkylthio group.
Claim 4
Dependent Claim
18 words
An endothelin antagonistic agent comprising a compound as defined in Claim 1 or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim
61 words
A drug for treating hypertension, pulmonary hypertension, Raynaud's disease, acute renal failure, myocardial infarction, angina pectoris, cerebral infarction, cerebral vasospasm, arteriosclerosis, asthma, gastric ulcer, diabetes, endotoxin shock, endotoxin-induced multiple organ failure or disseminated intravascular coagulation, and/or cyclosporin-induced renal failure or hypertension, which contains a peptide derivative of the formula (1) as defined in Claim 1 or a pharmaceutically acceptable salt thereof.