60630-68-4

Upstream product

• 3161-52-2 N-(3-chloropropyl)-N-methylbenzylamine 
• 74-89-5 methylamine 
• 103-67-3 benzyl-methyl-amine 
• 100-44-7 benzyl chloride 
• 111-33-1 1,3-bis(methylamino)propane 

Downstream Products

• 98902-04-6 Tetrahydro-furan-2-carboxylic acid [3-(benzyl-methyl-amino)-propyl]-methyl-amide 
• 65189-24-4 N¹,N²-dimethyl-N²-(phenylmethyl)-N¹-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1,3-propanediamine 
• 98902-39-7 N-{3-[(4-amino-6,7-dimethoxy-quinazolin-2-yl)-methyl-amino]-propyl}-N-methyl-benzamide 
• 98902-42-2 N-{3-[(4-Amino-6,7-dimethoxy-quinazolin-2-yl)-methyl-amino]-propyl}-3,4,5-trimethoxy-N-methyl-benzamide 
• 98902-41-1 N-{3-[(4-Amino-6,7-dimethoxy-quinazolin-2-yl)-methyl-amino]-propyl}-3,5-dimethoxy-N-methyl-benzamide 
• 98902-40-0 N-methyl-N-<3-<(4-amino-6,7-dimethoxy-2-quinazolinyl)methylamino>propyl>-3-methoxybenzenecarboxamide 
• 72766-65-5 N-{3-[(4-Amino-6,7-dimethoxy-quinazolin-2-yl)-methyl-amino]-propyl}-3,N-dimethyl-benzamide 

Relevant academic research and scientific papers

Carbachol dimers with primary carbamate groups as homobivalent modulators of muscarinic receptors

Although agonists and antagonists of muscarinic receptors have been known for long time, there is renewed interest in compounds (such as allosteric or bitopic ligands, or biased agonists) able to differently and selectively modulate these receptors. As a continuation of our previous research, we designed a new series of dimers of the well-known cholinergic agonist carbachol. The new compounds were tested on the five cloned human muscarinic receptors (hM1–5) expressed in CHO cells by means of equilibrium binding experiments, showing a dependence of the binding affinity on the length and position of the linker connecting the two monomers. Kinetic binding studies revealed that some of the tested compounds were able to slow the rate of NMS dissociation, suggesting allosteric behavior, also supported by docking simulations. Assessment of ERK1/2 phosphorylation on hM1, hM2 and hM3 activation showed that the new compounds are endowed with muscarinic antagonist properties. At hM2 receptors, some compounds were able to stimulate GTPγS binding but not cAMP accumulation, suggesting a biased behavior. Classification, Molecular and cellular pharmacology.

CGAS IN SYSTEMIC LUPUS ERYTHEMATOSUS (SLE)

The present invention provides therapeutic strategies for treatment of severe debilitating diseases associated with IFN-I due to cGAS activation. In one aspect, the invention provides compounds of Formula (I): [Formula should be inserted here] and pharmaceutical uses thereof. In another aspect, the invention provides methods for treating an autoimmune disease or a monogenic disorder by administering an effective amount of a compound of Formula (I).

COMPOUNDS, PHARMACEUTICAL COMPOSITION AND THEIR USE IN TREATING NEURODEGENERATIVE DISEASES

The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.

Synthesis and antihypertensive activity of a series of 4-amino-6,7-dimethoxyquinazoline derivatives

A series of N2-[(acylamino)alkyl]-6,7-dimethoxy-2,4-quinazolinediamines was synthesized as potential α1-adrenoceptor antagonists. When administered to spontaneously hypertensive rats at 10 mg/kg po, a number of propanediamine derivatives showed good antihypertensive activity, whereas the ethanediamine derivatives, albeit being structurally more closely related to prazosin, were devoid of this property. The most active derivative, N-[3-[(4-amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro- 2-furancarboxamide hydrochloride, alfuzosin, showed high selectivity for peripheral α1-postjunctional adrenoceptors. At equiactive antihypertensive doses, its effect on the pressor response to postural changes in conscious dog was less marked than that shown by prazosin. In the light of these results, alfuzosin was selected for clinical evaluation.