Patents by Inventor Roger Nosal
Roger Nosal 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).
-
Publication number: 20050032793Abstract: A class of compounds for the treatment of viral infections. Compounds of particular interest are defined by Formula I wherein R-R4 are as defined herein, or a pharmaceutically-acceptable salt thereof.Type: ApplicationFiled: December 8, 2003Publication date: February 10, 2005Applicant: G.D. Searle & Co.Inventors: Norman Abood, Daniel Flynn, Daniel Becker, Brian Bax, Hui Li, Roger Nosal, Lori Schretzman, Clara Villamil
-
Patent number: 6683077Abstract: A class of compounds for the treatment of viral infections. Compounds of particular interest are defined by Formula I wherein R-R4 are as defined herein, or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: January 4, 2002Date of Patent: January 27, 2004Assignee: G.D. Searle & Co.Inventors: Norman Abood, Daniel L. Flynn, Daniel P. Becker, Brian M. Bax, Hui Li, Roger A. Nosal, Lori A. Schretzman, Clara I. Villamil
-
Publication number: 20030022895Abstract: A class of compounds for the treatment of viral infections.Type: ApplicationFiled: January 4, 2002Publication date: January 30, 2003Applicant: G.D. Searle & Co.Inventors: Norman Abood, Daniel L. Flynn, Daniel P. Becker, Brian M. Bax, Hui Li, Roger A. Nosal, Lori A. Schretzman, Clara I. Villamil
-
Patent number: 6380189Abstract: A class of compounds for the treatment of viral infections. Compounds of particular interest are defined by Formula I wherein R-R4 are as defined herein, or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 11, 2000Date of Patent: April 30, 2002Assignee: G.D. Searle & Co.Inventors: Norman Abood, Daniel L. Flynn, Daniel P. Becker, Brian M. Bax, Hui Li, Roger A. Nosal, Lori A. Schretzman, Clara I. Villamil
-
Patent number: 5985872Abstract: A class of compounds for the treatment of viral infections. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.28 is selected from (a) amino substituted with one or two radicals selected from alkyl, aralkyl, heterocycoalkyl, heterocyclo, and aryl, and (b) amino acid residues and derivatives thereof; wherein R.sup.29 is selected from hydrido, alkyl, halo, ##STR2## wherein R.sup.30 is selected from alkyl, alkoxy, alkylamino, carboxyalkyl, alkoxyalkyl, alkylaminoalkyl, cycloalkyl, heterocyclo, heterocycloalkyl, heterocycloalkoxy, alkylaminoalkoxy, alkylaminoalkylamino, heterocycloalkylamino, and N-aralkylamino; wherein R.sup.31 is alkyl; wherein R.sup.32 is alkyl and aryl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: May 24, 1995Date of Patent: November 16, 1999Assignee: G.D. Searle & Co.Inventors: Norman Anthony Abood, Daniel L. Flynn, Daniel P. Becker, Brian M. Bax, Hui Li, Roger A. Nosal, Lori A Schretzman, Clara I Villamil
-
Patent number: 5665598Abstract: A method is described for synthesis of N-Boc-L-propargylglycine, a key intermediate used in the preparation of high-potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc-2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc-propargylglycine with .alpha.-chymotrypsin provides N-Boc-L-propargylglycine in high yield.Type: GrantFiled: January 29, 1996Date of Patent: September 9, 1997Assignee: G. D. Searle & Co.Inventors: Norman A. Abood, Roger A. Nosal
-
Patent number: 5659063Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.Type: GrantFiled: June 6, 1995Date of Patent: August 19, 1997Assignee: G. D. Searle & Co.Inventors: Norman Anthony Abood, Daniel Lee Flynn, Scott Anthony Laneman, Roger Nosal, Lori Ann Schretzman
-
Patent number: 5612366Abstract: The meso-azacyclic aromatic acid amides and esters of the present invention are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrome, and the like. Additionally, the compounds of the present invention find utility as antagonists of serotonin 5-HT.sub.3 receptors. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.Type: GrantFiled: April 28, 1994Date of Patent: March 18, 1997Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moorman, Roger Nosal, Clara I. Villamil
-
Patent number: 5610296Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.Type: GrantFiled: December 5, 1994Date of Patent: March 11, 1997Assignee: G. D. Searle & Co.Inventors: Norman A. Abood, Daniel L. Flynn, Scott A. Laneman, Roger Nosal, Lori A. Schretzman
-
Patent number: 5604239Abstract: The imidazopyridines compounds of the present invention are serotonergic 5-HT.sub.3 antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.Type: GrantFiled: April 18, 1995Date of Patent: February 18, 1997Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Roger Nosal, Clara I. Villamil
-
Patent number: 5591749Abstract: The imidazopyridines compounds of the present invention are serotonergic 5-HT.sub.3 antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbances (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.Type: GrantFiled: April 19, 1995Date of Patent: January 7, 1997Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Roger Nosal, Clara I. Villamil
-
Patent number: 5576447Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.Type: GrantFiled: June 5, 1995Date of Patent: November 19, 1996Assignee: G. D. Searle & Co.Inventors: Norman A. Abood, Daniel L. Flynn, Scott A. Laneman, Roger Nosal, Lori A. Schretzman
-
Patent number: 5534521Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof; pharmaceutical compositions containing the compounds and a method for treating serotonin mediated condition with the compositionswhich act as 5-HT.sub.4 agonists or antagonists and/or 5-HT.sub.3 antagonists.Type: GrantFiled: November 8, 1994Date of Patent: July 9, 1996Assignee: G. D. Searle & Co.Inventors: Daniel L. Flynn, Alan E. Moormann, Daniel P. Becker, Michael S. Dappen, Roger Nosal, Robert L. Shone, Clara I. Villamil
-
Patent number: 5521193Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated, conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 19, 1995Date of Patent: May 28, 1996Assignee: G. D. Searle & Co.Inventors: Daniel L. Flynn, Alan E. Moormann, Daniel P. Becker, Michael S. Dappen, Roger Nosal, Robert L. Shone, Clara I. Villamil
-
Patent number: 5516782Abstract: The meso-azacyclic aromatic acid amides and esters of the present invention are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrome, and the like. Additionally, the compounds of the present invention find utility as antagonists of serotonin 5-HT.sub.3 receptors. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.Type: GrantFiled: May 18, 1995Date of Patent: May 14, 1996Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moorman, Roger Nosal, Clara I. Villamil
-
Patent number: 5508466Abstract: A method is described for synthesis of N-Boc-L-propargylglycine, a key intermediate used in the preparation of high-potency, orally-active renin inhibitors. This method involves reaction of an organic halide with a glycine cation equivalent, such as methyl N-Boc-2-acetoxyglycine, in the presence of zinc dust to give Boc-protected amino acid derivatives in high yield. Typically useful organic halides are allylic, benzylic and propargylic halides. Resolution of methyl N-Boc-propargylglycine with .alpha.-chymotrypsin provides N-Boc-L-propargylglycine in high yield.Type: GrantFiled: April 13, 1994Date of Patent: April 16, 1996Assignee: G.D. Searle & Co.Inventors: Norman A. Abood, Roger A. Nosal
-
Patent number: 5484946Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.Type: GrantFiled: June 5, 1995Date of Patent: January 16, 1996Assignee: G. D. Searle & Co.Inventors: Norman A. Abood, Daniel L. Flynn, Scott A. Laneman, Roger Nosal, Lori A. Schretzman
-
Patent number: 5434161Abstract: The imidazopyridines compounds of the present invention are serotonergic 5-HT.sub.3 antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.Type: GrantFiled: November 6, 1992Date of Patent: July 18, 1995Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Roger Nosal, Clara I. Villamil
-
Patent number: 5318977Abstract: The meso-azacyclic aromatic acid amides and esters of the present invention are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrome, and the like. Additionally, the compounds of the present invention find utility as antagonists of serotonin 5-HT.sub.3 receptors. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.Type: GrantFiled: November 6, 1992Date of Patent: June 7, 1994Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moorman, Roger Nosal, Clara I. Villamil
-
Patent number: RE35218Abstract: An azatetracycle compound useful as 5HT.sub.3 antagonists of the general formula ##STR1## wherein D is a tetracycle of the structure ##STR2## wherein Ar is an aromatic moiety and B is either NH or O.Type: GrantFiled: August 18, 1994Date of Patent: April 23, 1996Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Roger Nosal, Dale P. Spangler, Daniel L. Zabrowski