The present invention relates to N-acyl derivatives of amino acids and pharmaceutically acceptable salts thereof ##STR00001## wherein n is 2 or 3; and R.sub.1 represents ##STR00002## or pharmaceutically acceptable salts thereof, to novel processes for preparing the same, to use thereof as anti-allergic, anti-anaphylactic, anti-inflammatory and hypolipidemic agents as well as to a pharmaceutical composition comprising the indicated compounds in an efficient amount and to a method for treating allergic and inflammatory diseases and lipid metabolism disorders: bronchial asthma, allergic rhinitis, pollinoses, seasonal and year-round rhinitis, allergic pneumonitis, atopic dermatitis, psoriasis, urticaria, allergic (including anaphylactic) reactions to insect stings and medicaments, cold allergy, allergic conjunctivitis, atherosclerosis, obesity, ischemic heart and cerebral disease, myocardial infarction and stroke.

Otkrytoe Aktsionernoe Obschestvo-Otechestvennye Lekarstva

N-acyl amino acid derivatives, a method for the preparation thereof, a pharmaceutical composition and use thereof as anti-allergic, anti-inflammatory and hypolipidemic agents

Nebolsin; Vladimir Evgenievich

Kromova; Tatyana Alexandrovna

Zheltukhina; Galina Alexandrovna

Kovaleva; Violetta Leonidovna

Otkrytoe Aktsionernoe Obschestvo Otechestvennye Lekarstva

Vladimir Evgenievich Nebolsin

N-acylic aminoacid derivatives, method for the production thereof, pharmacological composition and the use in the form anti-allergic, anti-inflammatory and hypolipidemic agents

The present application relates to internally cyclized naphthamide compounds of the formula Ia (wherein R.sup.1a, R.sup.1b, R.sup.1c, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, X.sup.1, X.sup.2, Y, Z, and n are as defined herein), which are useful, for example, for antagonizing the pharmacological actions of the neurokinin 1 (NK.sub.1) receptor. In particular, these compounds are useful in the treatment of diseases in which Substance P is involved such as, for example, major depressive disorder, severe anxiety disorders, stress disorders, major depressive disorder with anxiety, eating disorders, bipolar disorder, substance use disorder, schizophrenic disorders, psychotic disorders, movement disorders, cognitive disorders, depression and/or anxiety, mania or hypomania, aggressive behaviour, obesity, rheumatoid arthritis, Alzheimer's disease, cancer, oedema, allergic rhinitis, inflammation, pain, gastrointestinal-hypermotility, Huntington's disease, chronic obstructive pulmonary disorder (COPD), hypertension, migraine, bladder hypermotility, and urticaria.

urticaria/fetma

N-acyl amino acid derivatives, a method for the preparation thereof, a pharmaceutical composition and use thereof as anti-allergic, anti-inflammatory and hypolipidemic agents

N-acylic aminoacid derivatives, method for the production thereof, pharmacological composition and the use in the form anti-allergic, anti-inflammatory and hypolipidemic agents

Neurokinin antagonists for use as medicaments

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