1260403-53-9

Upstream product

• 610-22-0 dimethyl 4-nitrophthalate 
• 610-27-5 4-nitrophthalic acid 
• 51832-31-6 4-amino-phthalic acid dimethyl ester 
• 100-44-7 benzyl chloride 

Downstream Products

• 957130-49-3 (R)-5-amino-1,3-dihydrospiro[indene-2,3’-pyrrolo[2,3-b]pyridin]-2’(1’H)-one 
• 957118-49-9 [3H]-MK 3207 
• 1260403-54-0 [4-(dibenzylamino)-2-(hydroxymethyl)phenyl]methanol 
• 1260403-57-3 (R)-1’-(tert-butyl)-5-(dibenzylamino)-1,3-dihydrospiro[indene-2,3’-pyrrolo[2,3-b]pyridin]-2’(1’H)-one 
• 1260403-55-1 [2-(chloromethyl)-4-(dibenzylamino)phenyl]methanol hydro chloride 

Relevant academic research and scientific papers

HETEROCYCLIC SPIRO-COMPOUNDS AS AM2 RECEPTOR INHIBITORS

Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein HET, R1, R2, R3, R4, R5, L, L1, X1, X2, X3 and q are as defined herein. The compounds are inhibitors of adrenomedullin receptor subtype 2 (AM2). Also disclosed are the compounds for use in the treatment of diseases modulated AM2, including proliferative diseases such as cancer; pharmaceutical compositions comprising the compounds; methods for preparing the compounds; and intermediates useful in the preparation of the compounds.

HETEROCYCLIC SPIRO-COMPOUNDS AS AM2 RECEPTOR INHIBITORS

Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1, R2, R4, R5, R6, R7, R8, R9, R10,Z, X1, X2, X3, L2, HET, n and q are as defined herein. The compounds are inhibitors of adrenomedullin receptor subtype 2 (AM2). Also disclosed are the compounds for use in the treatment of diseases modulated AM2, including proliferative diseases such as cancer; pharmaceutical compositions comprising the compounds; methods for preparing the compounds; and intermediates useful in the preparation of the compounds.

Piperidinone carboxamide indane CGRP receptor antagonists

The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

PYRIDINE CGRP RECEPTOR ANTAGONISTS

The present invention is directed to pyridine derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

ALIPHATIC SPIROLACTAM CGRP RECEPTOR ANTAGONISTS

The present invention is directed to aliphatic spirolactam derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical\compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

PROCESS FOR MAKING CGRP RECEPTOR ANTAGONIST

The invention encompasses a novel process for making 2-[(8R)-8-(3,5-Difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]dec-9-yl]-N-[(2R)-2'-oxo-1,1',2',3-tetrahydrospiro[indene-2,3'-pyrrolo[2,3-b]pyridin]-5-yl]acetamide, which is a CGRP receptor antagonist useful for the treatment of migraine, using an asymmetric phase-transfer catalysis route. The invention also encompasses an efficient and practical synthesis of the (R)-acid intermediate, and generates the benzylic stereocenter in an enantioselective manner.