Amino acid derivatives, pharmaceutical compositions containing these compounds and processes for preparing them

US6114390A · kind A · utility

Assignee

• Karl Thomae GmbH · DE

Inventors

• Wolfhard Engel
• Wolfgang Eberlein · Biberach, DE
• Klaus Rudolf · Warthausen, DE
• Henri Doods · Warthausen, DE
• Heike-Andrea Wieland · Biberach, DE
• Klaus-Dieter Willim · Biberach an der Riß, DE
• Michael Entzeroth · Warthausen, DE
• Wolfgang Wienen · Äpfingen, DE

Key dates

• Filing date: Oct 14, 1997
• Grant date: Sep 5, 2000
• Expiry date: Oct 14, 2017

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

NPY-antagonistic compounds of the formula ##STR1## Exemplary are: (A) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -bis(4-hydroxyphenyl)acetyl]-argininamide-trifluoracetate; PA1 (B) (R)-N-[[4-(Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -[bis(4-chlorphenyl)acetyl]-argininamide-trifluoracetate; PA1 (C) (R)-N-[[4-Aminocarbonylaminomethyl)phenyl]methyl]-N.sup.2 -(diphenylacetyl)-argininamide-trifluoracetate; PA1 (D) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethoxycarbonylmethylamino-carbonylaminomethyl)phe nyl]methyl]-argininamide-trifluoroacetate; PA1 (E) (R,S)-N.sup.5 -(Aminoiminomethyl)-N.sup.2 -(diphenylacetyl)-N-[(4-hy-droxyphenyl)methyl]-N.sup.5 -methyl-ornithinamide-hydrochloride; PA1 (F) (R)-N-[[4-(Aminocarbonylmethyl)phenyl]methyl]-N.sup.2 -(diphenyl-acetyl)-argininamide-diacetate; PA1 (G) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethylaminocarbonylamino-methyl)-phenyl]methyl]-ar gininamide-bis-(trifluoroacetate); and, PA1 (H) (R)-N.sup.2 -(Diphenylacetyl)-N-[[4-(ethoxycarbonylamino-carbonylaminomethyl)phenyl]me thyl]-argininamide-trifluoroacetate.