Patent US2664912A successfully refreshed from Google Patents.
Patent EP0181110A2 successfully refreshed from Google Patents.
EP0181110A2
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Histidine derivatives as renin inhibitors
Assignee: Kissei Pharmaceutical Co Ltd
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Filing: 1985-10-18
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Granted: —
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Expires: 2005-10-18
Abstract
Abstract @ Dipeptides are described which are represented by the formula wherein His represents an L-histidyl group, Ar, represents a phenyl group, a naphthyl group or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -O- or -(CH=CH) P -wherein p is 1 or 2, Z represents an oxygen atom or in which R 2 represents a hydrogen atom or combines with R, to form a chemical bond, m and n, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6 and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond when X is not a chemical bond, or, when X is a chemical bond, an alkylene group having 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobutyl group or a benzyl group, and C represents an L-configurational carbon atom; or the pharmaceutically acceptable salt thereof. These compounds have a strong inhibitory effect on human renin, and are useful as a therapeutically active agent for the treatment of hypertension, especially renin - associated hypertension.
Inventors
- 👤 Kinji Iizuka
- 👤 Tetsuhide Kamijo
- 👤 Tetsuhiro Kubota
- 👤 Kenji Akahane
- 👤 Hideaki Umeyama
- 👤 Yoshiaki Kiso
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-08 14:28
CPC Classifications
C; C07; C07D; C07D233/00; C07D233/54; C07D233/64; C07C; C07C51/00; C07C51/42; C07C51/487; C07C57/00; C07C57/30; C07C57/38; C07C57/40; C07C59/00; C07C59/40; C07C59/58; C07C59/64; C07C59/66; C07C59/68; C07C65/00; C07C65/32; C07C65/34; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06139; C07K5/06147; Y; Y10; Y10S; Y10S530/00; Y10S530/86
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
216 words
A peptide represented by formula (I) wherein His represents an L-histidyl group, Ar 1 represents a phenyl group, a naphthyl group or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -O- or -(CH=CH)p- wherein p is 1 or 2, Z represents an oxygen atom or in which R 2 represents a hydrogen atom or combines with R 1 to form a chemical bond, m and n, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6, and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond when X is not a chemical bond, or, when X is a chemical bond, an alkylene group having from 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents * an isobutyl group or a benzyl group, and C represents an L-configurational carbon atom; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
216 words
A peptide represented by formula (I) wherein His represents an L-histidyl group, Ar 1 represents a phenyl group, a naphthyl group or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -O- or -(CH=CH)p- wherein p is 1 or 2, Z represents an oxygen atom or in which R 2 represents a hydrogen atom or combines with R 1 to form a chemical bond, m and n, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6, and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond when X is not a chemical bond, or, when X is a chemical bond, an alkylene group having from 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents * an isobutyl group or a benzyl group, and C represents an L-configurational carbon atom; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
31 words
A dipeptide as in claim 1 represented by formula wherein Ar l , m, X, n, Ar 2 , His and C have the same meanings as defined in claim 1.
Claim 4
Dependent Claim
28 words
A dipeptide as in claim 1 represented by the formula wherein Ar 2 , m, Y, His and C have the same meanings as defined in claim 1.
Claim 5
Dependent Claim
23 words
A dipeptide as in claim 2 represented by the formula wherein His and C have the same meanings as defined in claim 2.
Claim 6
Dependent Claim
23 words
A dipeptide as in claim 2 represented by the formula wherein His and C have the same meanings as defined in claim 2.
Claim 7
Dependent Claim
23 words
A dipeptide as in claim 2 represented by the formula wherein His and C have the same meanings as defined in claim 2.
Claim 8
Dependent Claim
23 words
A dipeptide as in claim 2 represented by the formula wherein His and C have the same meanings as defined in claim 2.
Claim 9
Dependent Claim
23 words
A dipeptide as in claim 2 represented by the formula wherein His and C have the same meanings as defined in claim 2.
Claim 10
Dependent Claim
23 words
A dipeptide as in claim 2 represented by the formula wherein His and C have the same meanings as defined in claim 2.
Claim 11
Dependent Claim
23 words
A dipeptide as in claim 2 represented by the formula wherein His and C have the same meanings as defined in claim 2.
Claim 12
Dependent Claim
23 words
A dipeptide as in claim 2 represented by the formula wherein His and C have the same meanings as defined in claim 2.
Claim 13
Dependent Claim
23 words
A dipeptide as in claim 3 represented by the formula wherein His and C have the same meanings as defined in claim 3.
Claim 14
Dependent Claim
23 words
A dipeptide as in claim 3 represented by the formula wherein His and C have the same meanings as defined in claim 3.
Claim 15
Dependent Claim
264 words
A pharmaceutical composition for the treatment of hypertension by oral administration, containing, as an active ingredient, a dipeptide represented by formula (I) wherein His represents an L-histidyl group, Ar 1 represents a phenyl group, a naphthyl group, or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -0- or -(CH=CH) p -, wherein R 2 p is 1 or 2, Z represents an oxygen atom or -CH- in which R 2 represents a hydrogen atom or combines with R 1 to form a chemical bond, n and m, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6, and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond when X is not a chemical bond, or, when X is a chemical bond, an alkylene group having from 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobuyl group or a benzyl group, and C represents an L-configurational carbon atom; or a pharmaceutically acceptable salt thereof; in an amount in the range of from about 5 mg to about 5000 mg per day per body in combination with a pharmaceutically acceptable carrier or diluent.
Claim 16
Dependent Claim
264 words
A pharmaceutical composition for the treatment of hypertension by oral administration, containing, as an active ingredient, a dipeptide represented by formula (I) wherein His represents an L-histidyl group, Ar 1 represents a phenyl group, a naphthyl group, or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -0- or -(CH=CH) p -, wherein R 2 p is 1 or 2, Z represents an oxygen atom or -CH- in which R 2 represents a hydrogen atom or combines with R 1 to form a chemical bond, n and m, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6, and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond when X is not a chemical bond, or, when X is a chemical bond, an alkylene group having from 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobuyl group or a benzyl group, and C represents an L-configurational carbon atom; or a pharmaceutically acceptable salt thereof; in an amount in the range of from about 5 mg to about 5000 mg per day per body in combination with a pharmaceutically acceptable carrier or diluent.
Claim 17
Dependent Claim
254 words
A pharmaceutical composition for the treatment of hypertension by parenteral administration, containing, as an active ingredient, a dipeptide represented by formula (I) wherein His represents an L-histidyl group, Ar 1 represents a phenyl group, a naphthyl group, or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, - CONH -, -CO-, -C H2 -, - NH -, -O- or -(CH=CH)p-, wherein p is 1 or 2, Z represents an oxygen atom or in which R 2 represents a hydrogen atom or combines with R 1 to form a chemical bond, m and n, which may be the same or different, each represents an integer of from o to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6, and when X is not a chemical bond, the.sum of n plus m is from 1 to 4, Y represents a chemical bond, or, when X is a chemical bond, an alkylene group having from 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobuyl group or a benzyl group, and C represents an L-configurational carbon atom; or a pharmaceutically acceptable salt thereof; in an amount in the range of from about 1 mg to 1000 mg per day per body in combination with a pharmaceutically acceptable carrier or diluent.
Claim 18
Dependent Claim
254 words
A pharmaceutical composition for the treatment of hypertension by parenteral administration, containing, as an active ingredient, a dipeptide represented by formula (I) wherein His represents an L-histidyl group, Ar 1 represents a phenyl group, a naphthyl group, or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, - CONH -, -CO-, -C H2 -, - NH -, -O- or -(CH=CH)p-, wherein p is 1 or 2, Z represents an oxygen atom or in which R 2 represents a hydrogen atom or combines with R 1 to form a chemical bond, m and n, which may be the same or different, each represents an integer of from o to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6, and when X is not a chemical bond, the.sum of n plus m is from 1 to 4, Y represents a chemical bond, or, when X is a chemical bond, an alkylene group having from 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobuyl group or a benzyl group, and C represents an L-configurational carbon atom; or a pharmaceutically acceptable salt thereof; in an amount in the range of from about 1 mg to 1000 mg per day per body in combination with a pharmaceutically acceptable carrier or diluent.
Claim 19
Dependent Claim
221 words
The use of a compound of formula (I) for the treatment of the human body by therapy. wherein His represents an L-histidyl group, Ar 1 represents a phenyl group, a naphthyl group, or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -O- or -(CH=CH) p -, wherein p is 1 or 2, Z represents an oxygen atom or in which R 2 represents a hydrogen atom or combines with R 1 to form a chemical bond, m and n, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6, and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond, or, when X is a chemical bond, an alkylene group having from 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobuyl group or a benzyl group, and C represents an L-configurational carbon atom; or a pharmaceutically acceptable salt thereof.
Claim 20
Dependent Claim
221 words
The use of a compound of formula (I) for the treatment of the human body by therapy. wherein His represents an L-histidyl group, Ar 1 represents a phenyl group, a naphthyl group, or an indolyl group, Ar 2 represents a phenyl group or a naphthyl group, X represents a chemical bond, -NHCO-, -CONH-, -CO-, -CH 2 -, -NH-, -O- or -(CH=CH) p -, wherein p is 1 or 2, Z represents an oxygen atom or in which R 2 represents a hydrogen atom or combines with R 1 to form a chemical bond, m and n, which may be the same or different, each represents an integer of from 0 to 3, provided that when X is a chemical bond, the sum of n plus m is from 1 to 6, and when X is not a chemical bond, the sum of n plus m is from 1 to 4, Y represents a chemical bond, or, when X is a chemical bond, an alkylene group having from 1 to 3 carbon atoms, R 1 represents a hydrogen atom or combines with R 2 to form a chemical bond, R 3 represents a formyl group or a hydroxymethyl group, R 4 represents an isobuyl group or a benzyl group, and C represents an L-configurational carbon atom; or a pharmaceutically acceptable salt thereof.
References Cited (Backward Citations)
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