99057-90-6

Upstream product

• 32337-86-3 1-bromo-5,6,7,8-tetrahydronaphthalen-2-ol 
• 1125-78-6 5,6,7,8-Tetrahydro-2-naphthol 
• 7664-93-9 sulfuric acid 
• 854912-52-0 4-bromo-3-hydroxy-5,6,7,8-tetrahydro-naphthalene-2-sulfonic acid 
• 7697-37-2 nitric acid 
• 6240-79-5 5,6,7,8-Tetrahydro-3-nitro-2-naphthol 

Downstream Products

• 28094-04-4 3-amino-5,6,7,8-tetrahydro-2-naphthalenol 
• 112249-44-2 2-{3-[4-(2-Methoxy-phenyl)-piperazin-1-yl]-propyl}-6,7,8,9-tetrahydro-4H-naphtho[2,3-b][1,4]oxazin-3-one 
• 112249-69-1 (S)-(-)-2-<3-<4-(4-fluorophenyl)-1-piperazinyl>propyl>-6,7,8,9-tetrahydro-2H-naphtho<2,3-b><1,4>oxazin-3(4H)-one 
• 112249-70-4 (R)-(+)-2-<3-<4-(4-fluorophenyl)-1-piperazinyl>propyl>-6,7,8,9-tetrahydro-2H-naphtho<2,3-b><1,4>oxazin-3(4H)-one 
• 112249-42-0 2-<3-<4-(4-fluorophenyl)-1-piperazinyl>propyl>-6,7,8,9-tetrahydro-2H-naphtho<2,3-b><1,4>oxazin-3(4H)-one 
• 139516-37-3 4-(2-Dimethylamino-ethyl)-2-{3-[4-(4-fluoro-phenyl)-piperazin-1-yl]-propyl}-6,7,8,9-tetrahydro-4H-naphtho[2,3-b][1,4]oxazin-3-one; hydrochloride 
• 139516-48-6 2-{3-[4-(4-Fluoro-benzyl)-piperazin-1-yl]-propyl}-6,7,8,9-tetrahydro-4H-naphtho[2,3-b][1,4]oxazin-3-one; hydrochloride 
• 139516-38-4 (2-{3-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-propyl}-3-oxo-2,3,6,7,8,9-hexahydro-naphtho[2,3-b][1,4]oxazin-4-yl)-acetic acid ethyl ester 
• 139516-46-4 2-[3-(4-Benzhydryl-piperazin-1-yl)-propyl]-6,7,8,9-tetrahydro-4H-naphtho[2,3-b][1,4]oxazin-3-one 
• 112249-58-8 2-{3-[4-(3-Trifluoromethyl-phenyl)-piperazin-1-yl]-propyl}-6,7,8,9-tetrahydro-4H-naphtho[2,3-b][1,4]oxazin-3-one 
• 139516-42-0 2-{3-[4-(2-Fluoro-benzoyl)-piperazin-1-yl]-propyl}-6,7,8,9-tetrahydro-4H-naphtho[2,3-b][1,4]oxazin-3-one 
• 112249-61-3 2-{3-[4-(3-Chloro-4-methyl-phenyl)-piperazin-1-yl]-propyl}-6,7,8,9-tetrahydro-4H-naphtho[2,3-b][1,4]oxazin-3-one 
• 112249-64-6 2-<3-<4-(4-fluorophenyl)-1-piperazinyl>propyl>-6,7,8,9-tetrahydro-4-methyl-2H-naphtho<2,3-b><1,4>oxazin-3(4H)-one 
• 112249-62-4 2-{3-[4-(4-Hydroxy-phenyl)-piperazin-1-yl]-propyl}-6,7,8,9-tetrahydro-4H-naphtho[2,3-b][1,4]oxazin-3-one 

Relevant academic research and scientific papers

ORGANIC COMPOUNDS

Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer (such as prostate or breast cancer), osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives

2-(4,5-Dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives and tricyclic analogues with a fused additional ring on the nitrogen atom of the benzoxazine moiety have been prepared and evaluated for their cardiovascular effects as potential antihypertensive agents. The imidazoline ring was generated by reaction of the corresponding ethyl ester with ethylenediamine. Affinities for imidazoline binding sites (IBS) I1 and I2 and α1 and α2 adrenergic receptors were evaluated as well as the effects on mean arterial blood pressure (MAP) and heart rate (HR) of spontaneously hypertensive rats. With few exceptions the most active compounds on MAP were those with high affinities for IBS and α2 receptor. Among these, compound 4h was the most interesting and is now, together with its enantiomers, under complementary pharmacological evaluation.

Synthesis and biological activities of new 2-substituted 1,4-benzoxazine derivatives

A series of new 1,4-benzoxazine derivatives (XI, XII) possessing (4-phenyl-1-piperazinyl)alkyl moieties at the 2-position and related compounds (XIII) were synthesized and tested for calcium antagonistic, calmodulin antagonistic and antihypertensive activ