Patents by Inventor Mark A. Schwindt
Mark A. Schwindt has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 7439222Abstract: The invention provides methods of synthesizing peptides, involving the steps of providing a composition including a peptide fragment, wherein the peptide fragment has at least one amino acid residue and includes a base-sensitive, N-terminal protecting group; removing the base-sensitive, N-terminal protecting group from the peptide fragment using a deprotection reagent that includes a base, whereby an N-terminal functionality on the peptide fragment is deprotected; removing the base from the composition to provide a residual base content of more than 100 ppm; causing a reactive peptide fragment having a reactive C-terminus and a base-sensitive N-terminal protecting group to react with the deprotected N-terminal functionality of the peptide fragment under conditions such that the reactive peptide fragment is added to the peptide fragment; and optionally repeating the deprotection and coupling steps until a desired peptide is obtained.Type: GrantFiled: December 23, 2004Date of Patent: October 21, 2008Assignee: Roche Palo Alto LLCInventors: Martin R. Guinn, Lewis M. Hodges, David A. Johnston, Hendrick Moorlag, Mark A. Schwindt
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Publication number: 20080161564Abstract: The present invention advantageously provides ketal functional compounds that can be strong electrophiles under conditions compatible with ketal groups, are stable, crystalline solids at room temperature, and are much safer to handle than ketal iodides. The present invention accomplishes by incorporating aromatic sulfonyl moieties into ketal functional materials. The compounds are useful starting materials or intermediates in the synthesis of more complex organic molecules.Type: ApplicationFiled: December 20, 2007Publication date: July 3, 2008Inventors: Mark A. Schwindt, Robert J. Topping, Charles E. Tucker
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Publication number: 20060167220Abstract: The formation of inactive, insoluble forms of peptide can be minimized or, alternatively, inactive, insoluble forms of peptide compounds, if present, can be converted into more physiologically active, soluble forms by dissolving peptide samples in aqueous base and then acidifying the aqueous mixture to precipitate the peptide in the presence of at least one of a salt and a co-solvent. Preferably, both a salt and co-solvent are present. By carrying out the precipitation relatively rapidly (at least in a first stage of acidifying in which the pH of the alkaline medium is reduced to a pH in the range of 6 to 7.5, after which acidification to a final desired pH, e.g., 3 to 6, can occur more slowly) at relatively low temperature, the dissolution characteristics of the resultant precipitated peptide are even further improved. The process is robust, consistent, and suitable for commercial scale manufacture of peptides.Type: ApplicationFiled: December 28, 2005Publication date: July 27, 2006Inventors: Richard Dauer, Christina Evanson, Paul Friedrich, Hafez Hafezzadeh, Ramakrishna Nalitham, Stephen Schneider, Mark Schwindt, Roger Snyder, Joseph White, Gregory Withers
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Publication number: 20050165215Abstract: The invention provides methods for synthesizing peptides, which include taking an organic solvent having non-resin bound protected peptide and performing a deprotection reaction on the non-resin bound protected peptide. In these methods it is not required that the peptide is dried immediately before providing to the deprotection reaction. Also provided are methods of synthesizing peptides, wherein a protected peptide is formed in a solution phase reaction, dissolved into an organic solvent, and then introduced into a deprotection reaction. Also provided are methods of synthesizing peptides, wherein a non-resin bound protected peptide is concentrated in an organic solvent prior to being subject to a deprotection reaction.Type: ApplicationFiled: December 23, 2004Publication date: July 28, 2005Inventors: Roger Bigelow, Mark Schwindt, Gregory Withers
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Publication number: 20050165217Abstract: The invention provides methods of synthesizing peptides, involving the steps of providing a composition including a peptide fragment, wherein the peptide fragment has at least one amino acid residue and includes a base-sensitive, N-terminal protecting group; removing the base-sensitive, N-terminal protecting group from the peptide fragment using a deprotection reagent that includes a base, whereby an N-terminal functionality on the peptide fragment is deprotected; removing the base from the composition to provide a residual base content of more than 100 ppm; causing a reactive peptide fragment having a reactive C-terminus and a base-sensitive N-terminal protecting group to react with the deprotected N-terminal functionality of the peptide fragment under conditions such that the reactive peptide fragment is added to the peptide fragment; and optionally repeating the deprotection and coupling steps until a desired peptide is obtained.Type: ApplicationFiled: December 23, 2004Publication date: July 28, 2005Inventors: Martin Guinn, Lewis Hodges, David Johnston, Hendrik Moorlag, Mark Schwindt
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Publication number: 20050143568Abstract: The invention provides methods for synthesizing peptides, which include a step of filter decanting. Filter decanting involves removing supernatant from a mixture containing a precipitated peptide. A filter decanting apparatus can be used to remove the supernatant. The invention also provides methods, such as deprotection methods, that can be performed prior to the filter decanting method.Type: ApplicationFiled: December 23, 2004Publication date: June 30, 2005Inventor: Mark Schwindt
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Patent number: 6858749Abstract: The present invention relates to a novel process for producing a ?-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-?-lactone.Type: GrantFiled: February 10, 2003Date of Patent: February 22, 2005Assignee: Roche Colorado CorporationInventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
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Patent number: 6818789Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.Type: GrantFiled: February 10, 2003Date of Patent: November 16, 2004Assignee: Roche Colorado CorporationInventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
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Patent number: 6743927Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.Type: GrantFiled: February 10, 2003Date of Patent: June 1, 2004Assignee: Roche Colorado CorporationInventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
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Publication number: 20030171602Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1Type: ApplicationFiled: February 10, 2003Publication date: September 11, 2003Applicant: Roche Colorado CorporationInventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Rober J. Topping
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Publication number: 20030158423Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1Type: ApplicationFiled: February 10, 2003Publication date: August 21, 2003Applicant: Roche Colorado CorporationInventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
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Publication number: 20030158422Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1Type: ApplicationFiled: February 10, 2003Publication date: August 21, 2003Applicant: Roche Colorado CorporationInventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Mitcheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
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Patent number: 6545165Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.Type: GrantFiled: September 22, 2000Date of Patent: April 8, 2003Assignee: Roche Colorado CorporationInventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
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Patent number: 5608090Abstract: A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.Type: GrantFiled: April 12, 1995Date of Patent: March 4, 1997Assignees: Northwestern University, Warner-Lambert CompanyInventors: Richard B. Silverman, Ryszard Andruszkiewicz, Po-Wai Yuen, Denis M. Sobieray, Lloyd C. Franklin, Mark A. Schwindt
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Patent number: 5599973Abstract: A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.Type: GrantFiled: April 12, 1995Date of Patent: February 4, 1997Assignees: Northwestern University, Warner-Lambert CompanyInventors: Richard B. Silverman, Ryszard Andruszkiewicz, Po-Wai Yuen, Denis M. Sobieray, Lloyd C. Franklin, Mark A. Schwindt
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Patent number: 5563175Abstract: A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.Type: GrantFiled: April 12, 1995Date of Patent: October 8, 1996Assignees: Northwestern University, Warner-Lambert CompanyInventors: Richard B. Silverman, Ryszard Andruszkiewicz, Po-Wai Yuen, Denis M. Sobieray, Lloyd C. Franklin, Mark A. Schwindt