808768-95-8Relevant academic research and scientific papers
Development of a potential manufacturing route to PF-00610355: A novel inhaled β2-adrenoreceptor agonist
De Koning, Pieter D.,Castro, Nieves,Gladwell, Iain R.,Morrison, Natalie A.,Moses, Ian B.,Panesar, Maninder S.,Pettman, Alan J.,Thomson, Nicholas M.
scheme or table, p. 1256 - 1265 (2012/02/05)
The development of a practical, scalable route to PF-00610355 (8) is described. In this convergent approach, amine 9 is coupled to protected bromohydrin 1 to give the doubly protected intermediate 26. TBS-Deprotection of 26 affords the benzyl protected pe
Enzymatic desymmetrization route to ethyl [3-(2-amino-2-methylpropyl) phenyl]acetate
De Koning, Pieter D.,Gladwell, Iain R.,Morrison, Natalie A.,Moses, Ian B.,Panesar, Maninder S.,Pettman, Alan J.,Thomson, Nicholas M.,Yazbeck, Daniel R.
experimental part, p. 871 - 875 (2012/06/18)
An efficient process to ethyl [3-(2-amino-2-methylpropyl)phenyl]acetate 6 has been developed. Key steps include a novel enzymatic desymmetrization of diester 2 and a Ritter reaction between alcohol 4 and chloroacetonitrile, followed by chemoselective deprotection with thiourea.
Inhalation by design: Novel ultra-long-acting β2- adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup
Glossop, Paul A.,Lane, Charlotte A. L.,Price, David A.,Bunnage, Mark E.,Lewthwaite, Russell A.,James, Kim,Brown, Alan D.,Yeadon, Michael,Perros-Huguet, Christelle,Trevethick, Michael A.,Clarke, Nicholas P.,Webster, Robert,Jones, Rhys M.,Burrows, Jane L.,Feeder, Neil,Taylor, Stefan C. J.,Spence, Fiona J.
experimental part, p. 6640 - 6652 (2010/11/19)
A novel series of potent and selective sulfonamide derived β2-adrenoreceptor agonists are described that exhibit potential as inhaled ultra-long-acting bronchodilators for the treatment of asthma and chronic obstructive pulmonary disease. Analogues from this series mediate very long-lasting smooth muscle relaxation in guinea pig tracheal strips. The sulfonamide agonist headgroup confers high levels of intrinsic crystallinity that could relate to the acidic sulfonamide motif supporting a zwitterionic form in the solid state. Optimization of pharmacokinetic properties was achieved through targeted introduction of a phenolic moiety to support rapid phase II clearance, thereby minimizing systemic exposure following inhalation and reducing systemically mediated adverse events. Compound 38 (PF-610355) is identified as a clinical candidate from this series, with in vivo duration of action studies confirming its potential for once-daily use in humans. Compound 38 is currently in advanced phase II clinical studies.
PROCESS FOR THE PREPARATION OF SULFONAMIDE DERIVATIVES
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Page/Page column 24, (2010/11/25)
The invention relates to a process for the preparation of compounds of formula (I) wherein Q1 is a group selected from formulae (II and (III) and a group *-NR6 -Q2-A or, if appropriate, their pharmaceutically acceptable sa
COMPOUNDS FOR THE TREATMENT OF DISEASES
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Page/Page column 50, (2008/06/13)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
FORMAMIDE DERIVATIVES USEFUL AS ADRENOCEPTOR
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Page/Page column 49; 83-84, (2008/06/13)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Sulfonamide derivatives for the treatment of diseases
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Page/Page column 17, (2008/06/13)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
Quinolinone derivatives, pharmaceutical compositions containing them and their use
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Page/Page column 27, (2008/06/13)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
Phenylethanolamine derivatives as beta-2 agonists
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Page/Page column 75-76, (2008/06/13)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
Compounds for the treatment of diseases
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Page/Page column 22, (2008/06/13)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
