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Gao Zhongli, Davis Larry, Levell Julian, Czekaj Mark, Sledeski Adam W, Haddad El Bdaoui: [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone hydrochloride as an inhibitor of mast cell tryptase. Aventis Pharmaceuticals, Gao Zhongli, Davis Larry, Levell Julian, Czekaj Mark, Sledeski Adam W, Haddad El Bdaoui, KNIGHT Julie Anne, October 20, 2005: WO/2005/097780 (5 worldwide citation)

The present invention extends to the compound of formula I, or a prodrug, pharmaceutically acceptable salt, or solvate of said compound. Furthermore, the present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a p ...


2
Gelormini Ann Marie, Sledeski Adam W, Shay John Joseph Jr: Use of 4-bromo-3-methyl-5-propoxythiophene-2-carboxylic acid 2,5-dioxo-pyrrolidin-1-yl ester for preparing the tryptase inhibitor [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone. Sanofi Aventis, Gelormini Ann Marie, Sledeski Adam W, Shay John Joseph Jr, PARKER Raymond S III, October 9, 2008: WO/2008/121666 (4 worldwide citation)

This invention is directed to a five step regio-specific synthesis of 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylic acid compound of formula 16 comprising the steps of acetalating 3-methyl-thiophene-2-carbaldehyde in an alcohol solvent; iodinating the acetalated 3-methyl-thiophene-2-carbaldehyde ...


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Pauls Heinz W, Aldous Suzanne C, Merriman Gregory H, Farr Robert A, Sledeski Adam W: [4-(3-aminomethylphenyl) piperidin-1-yl]- [5-(2-fluorophenylethynyl)furan-2-yl]-methanone as an inhibitor of mast cell tryptase. Aventis Pharmaceuticals, Pauls Heinz W, Aldous Suzanne C, Merriman Gregory H, Farr Robert A, Sledeski Adam W, KNIGHT Julie Anne, July 22, 2004: WO/2004/060884 (2 worldwide citation)

The present invention extends to the compund of formula (I): (I) or a prodrug, pharmaceutically acceptable salt, or solvate of said compound; to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of forumula (I), and a pharmaceutically acceptable carrier; the ...


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Graf Claus Dieter, Tappertzhofen Christoph, Sledeski Adam W: Process for the preparation of tryptase inhibitors. Aventis Pharmaceuticals, Graf Claus Dieter, Tappertzhofen Christoph, Sledeski Adam W, October 13, 2005: WO/2005/095385 (2 worldwide citation)

This invention is directed to processes for the preparation of compounds of the formula (I) and their salts, formula (I) which are useful as tryptase inhibitors, to intermediates useful in the preparation of such compounds, to processes for the preparation of such intermediates, and to the use of su ...


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Mencel James J, Stammler Robert, Daubie Christophe, Lavigne Michel, Vanasse Benoit J, Liu Robert C, Leon Patrick, D Netto Geoffrey A, Sledeski Adam W: Process for the preparation of azacycloalkylalkanoyl pseudotetrapeptides. Aventis Pharm Prod, August 30, 2000: EP1030831-A1

"This invention is directed to a process for preparing a pseudotetrapeptide of formula I or a salt or prodrug thereof wherein is optionally nitrogen protected azaheterocyclyl; ?? is a single or double bond; q is 1-5; B is alkyl, cycloalkyl, cycloalkyl"


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Chrzan Zofia J, Mencel James J, Toledo Velasquez David, Windisch Vincent, Woodward Rick G, Salazar Diane C, Vemuri Narasimha M, Gardetto Anthony J, Powers Matthew R, Kubiak Gregory G, Liu Robert C, Vanasse Benoit J, Sherbine James P, Rodriguez Walter, Sledeski Adam W: Stable non-hygroscopic crystalline form of n- n-n-(4-(piperidin-4-yl)butanoyl)-n-ethylglycyl compounds. Rhone Poulenc Rorer Pharma, June 23, 1999: EP0923553-A1

The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-[N-[N-(4-piperidin-4-yl)butanoyl)-N-ethylglycyl]-(L)-aspartyl]-(L)- beta -cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof ...


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Graf Claus Dieter, Tappertzhofen Christoph, Sledeski Adam W: Process for the preparation of tryptase inhibitors. Aventis Pharma, September 7, 2005: EP1571150-A1

This invention is directed to processes for the preparation of compounds of the formula I and their salts, which are useful as tryptase inhibitors, to intermediates useful in the preparation of such compounds, to processes for the preparation of such intermediates, and to the use of such intermediat ...


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Sledeski Adam W, Mencel James J: Process for the preparation of resin-bound cyclic peptides. Aventis Pharm Prod, April 25, 2001: EP1093458-A1

This invention is directed to a process for the solid phase, fragment-based synthesis of resin-bound cyclic peptide analogs of parathyroid hormones and analogs of parathyroid hormone-related proteins, which analogs contain at least one bridge between the side chains of two non-adjacent amino acid re ...


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