Renin inhibitors

• US 5,242,903 A
• Filed: 10/02/1991
• Issued: 09/07/1993
• Est. Priority Date: 08/05/1989
• Status: Expired due to Fees

• Current Assignee: Bayer AG
• Original Assignee: Bayer AG
• Inventors: Kinast, Gunther, Bender, Wolfgang, Stasch, Johannes-Peter, Knorr, Andreas
• Primary Examiner(s): GRIFFIN, RONALD
• Application Number:
  US07/771,077
• Time in Patent Office: 706 Days
• Field of Search: 514/18, 514/19, 530/323, 530/330, 530/331, 548/344, 562/445
• US Class Current: 530/330
• CPC Class Codes: A61K 38/00 Medicinal preparations containing peptides peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00
• CPC Class Codes: C07C 229/34 the carbon skeleton containing six-membered aromatic rings
• CPC Class Codes: C07C 2601/14 The ring being saturated
• CPC Class Codes: C07C 271/22 to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
• CPC Class Codes: C07C 311/19 to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
• CPC Class Codes: C07D 207/08 with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
• CPC Class Codes: C07D 209/48 with oxygen atoms in positions 1 and 3, e.g. phthalimide
• CPC Class Codes: C07D 233/54 having two double bonds between ring members or between ring members and non-ring members
• CPC Class Codes: C07D 233/64 with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
• CPC Class Codes: C07D 263/26 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
• CPC Class Codes: C07K 5/0205 containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
• CPC Class Codes: C07K 5/06147 and His-amino acid; Derivatives thereof

Abstract

Renin-inhibiting peptides of the formula ##STR1## in which X represents a group of the formula ##STR2## represents hydroxyl, alkoxy having up to 8 carbon atoms, benzyloxy or a group of the formula --NR⁴ R⁵,

A, B, D and E are identical or different and in each case

represent a direct bond,

represent a radical of the formula ##STR3## in which Z denotes oxygen, sulphur or the methylene group

represents a grouping of the formula ##STR4## m represents a number 0, 1 or 2, and L represents a group of the formula --CH₂ --NR2R₃

and physiologically acceptable salts thereof.

Claims

1. A compound of the formula ##STR248## in which R¹ represents straight-chain or branched alkyl having up to 4 carbon atoms, cyclohexyl or phenyl,

L represents a group of the formula --CH₂ --NR² R³ in which

R² and R³ are identical or different and in each case represent hydrogen, phenyl or represent straight-chain or branched alkyl having up to 4 carbon atoms, which is optionally substituted by phenyl pr pyridyl, or represent a group of the formula --COR⁹ in which R⁹ denotes straight-chain or branched alkyl having up to 4 carbon atoms, which may be substituted by phenyl or pyridyl, or denotes phenyl which, in turn, may be substituted by carboxyl, alkoxycarbonyl having up to 4 carbon atoms or by a group of the formula --CONR¹⁰ R¹¹ in which R¹⁰ and R¹¹ are identical or different and in each case denote cyclopentyl, hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms, which, in turn, may be substituted by phenyl or pyridyl, or one of the substituents

R² and R³ represents an amino protecting group or

R² and R³ together represent phthalimido or morpholino or represents a group pf the formula ##STR249## in which R^2'"'"' represents hydrogen and

R^3'"'"' represents hydrogen Boc, ethoxycarbonyl or pyridylacetyl, or

R^2'"'"' and R^3'"'"' together represent a morpholino group, or

L represents a group of the formula ##STR250##