Back to results
US 6,319,902 B1Granted
Peptide derivatives having thiazolyl-alanine residue
AssigneeShionogi & Co., Ltd.
InventorsTamio Sugawara, Takayoshi Yoshikawa, Yukio Tada
Life of this patent
Estimating the term…
Abstract
A peptide derivation of the formula (I) or its pharmaceutically acceptable salt or hydrate thereof is disclosed. These compounds have superior ability over thyroid stimulating hormone (TRH) and its derivatives to activate the central nervous system, such as, for example, sustained acetylcholine releasing action, anti-reserpine action and locomotor increment.
Claims14
A peptide derivative of the formula (I):
- wherein
- A is 4-thiazolyl or 5-thiazolyl wherein the nitrogen in the thiazolyl ring may be a quarternary nitrogen which is formed with an optionally substituted alkyl or alkenyl group,
- X is a bond, oxygen, or sulfur,
- m is an integer of 0 to 4,
- Y is an optionally substituted alkyl, an optionally substituted carboxy, a cyano, or a substituent represented by the formula:
- wherein R1 and R2 are independently a hydrogen or an optionally substituted alkyl group, or R1 and R2 taken together with may form a non-aromatic heterocyclic ring with the adjacent nitrogen, which may contain oxygen, nitrogen, or sulfur and may be substituted,
- Z is the substituent represented by the formula:
- wherein R3 is a hydrogen, an optionally substituted alkyl group, an optionally substituted carboxy group, or an optionally substituted acyl group, R4 and R5 are each independently a hydrogen or an optionally substituted alkyl group, and W is an oxygen, a sulfur, an optionally substituted imino, —(CH2)n- wherein n is 0, 1, 2, or 3, or the substituent represented by the formula:
- or an acceptable salt or hydrate thereof.
6 more elements
Dependencies are inferred from the claim text.