5159-63-7

Upstream product

• 60-29-7 diethyl ether 
• 58556-75-5 2,7-dibromonaphthalene 
• 1210226-26-8 C₁₂H₁₀BrNO₂ 
• 67-56-1 methanol 
• 5043-14-1 7-bromonaphthalene-2-carboxylic acid 

Downstream Products

• 1026807-94-2 7-[3-(Tetrahydro-pyran-2-yloxymethyl)-phenyl]-naphthalene-2-carboxylic acid methyl ester 
• 1613219-66-1 7-(4-phenylthiazol-2-yl)-naphthalene-2-carboxylic acid methyl ester 
• 1613219-39-8 7-(4-phenylthiazol-2-yl)-naphthalene-2-carboxylic acid 
• 1620738-95-5 {[7-(4-phenylthiazol-2-yl)naphthalene-2-carbonyl]amino}acetic acid methyl ester 
• 1620738-76-2 {[7-(4-phenylthiazol-2-yl)naphthalene-2-carbonyl]amino}acetic acid 
• 1620738-96-6 3-methyl-2-{[7-(4-phenylthiazol-2-yl)naphthalene-2-carbonyl]amino}butyric acid methyl ester 
• 1620738-77-3 3-methyl-2-{[7-(4-phenylthiazol-2-yl)naphthalene-2-carbonyl]amino}butyric acid 
• 1620738-85-3 (3,4-dichlorophenyl)-{[7-(4-phenylthiazol-2-yl)naphthalene-2-carbonyl]amino}acetic acid 
• 1620738-97-7 (3,4-dichlorophenyl)-{[7-(4-phenylthiazol-2-yl)naphthalene-2-carbonyl]amino}acetic acid methyl ester 
• 1620738-98-8 (4-chlorophenyl)-{[7-(4-phenylthiazol-2-yl)naphthalene-2-carbonyl]amino}acetic acid methyl ester 
• 1620738-86-4 (4-chlorophenyl)-{[7-(4-phenylthiazol-2-yl)naphthalene-2-carbonyl]amino}acetic acid 
• 1613317-20-6 2-cyclohexyl-N-[7-(4-phenylthiazol-2-yl)naphthalen-2-yl]succinamic acid 
• 1613317-36-4 7-(4-phenylthiazol-2-yl)naphthalen-2-ylamine 
• 1613317-35-3 [7-(4-phenylthiazol-2-yl)naphthalen-2-yl]carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

SUBSTITUTED THIAZOLE COMPOUNDS

The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.

SUBSTITUTED THIAZOLE COMPOUNDS

The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.

SUBSTITUTED THIAZOLE COMPOUNDS

The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.

Modulation on C- and N-terminal moieties of a series of potent and selective linear tachykinin NK2 receptor antagonists

Herein we describe the synthesis of a series of new potent tachykinin NK2 receptor antagonists by the modulation of the Cand N-terminal moieties of ibodutant (MEN 15596, 1). The Nterminal benzo[b]thiophene ring was replaced by different substituted naphthalenes and benzofurans, while further modifications were evaluated at the C-terminal tetrahydropyran moiety. Most compounds demonstrated a high affinity for the human NK2 receptor and high in vitro antagonist potency, indicating that a wide range of substituents at both termini can be incorporated in the molecule without detrimental effects on the interactions with the NK2 receptor. Selected compounds were tested in vivo confirming their activity as NK2 antagonists. In particular, after both iv and id administration to guinea pig, compound 61b was able to antagonize NK2-induced colonic contractions with a potency and duration-of-action fully comparable to the reference compound 1 (MEN 15596, ibodutant).

Cyclic imino derivatives and pharmaceutical compositions containing them

The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.