Patents by Inventor Theodros Asberom

Theodros Asberom 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: 20060009467
    Abstract: Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula: wherein Ar1 and Ar2 independently represent aryl or heteroaryl and Y represents a bond or a —(C(R3)2)1-3 group. Also disclosed is a method of inhibiting gamma secretase, and a method of treating Alzheimer's disease using the compounds of formula I.
    Type: Application
    Filed: September 9, 2005
    Publication date: January 12, 2006
    Inventors: Hubert Josien, John Clader, Theodros Asberom, Dmitri Pissarnitski
  • Publication number: 20060004004
    Abstract: Gamma-secretase inhibitors of the formula: are useful in treating various neurodegenerative diseases, wherein, for example: R1 includes unsubstituted or substituted aryl or heteroaryl groups; R2 includes —C(O)—Y, -alkylene-C(O)—Y, -alkylene-cycloalkylene-C(O)—Y, -cycloalkylene-alkylene-C(O)—Y, -alkylene-cycloalkylene-alkylene-C(O)—Y, -cycloalkylene-C(O)—Y, —S(O)—Y, -alkylene-S(O)—Y, -alkylene-cycloalkylene-S(O)—Y, -cycloalkylene-alkylene-S(O)—Y, -alkylene-cycloalkylene-alkylene-S(O)—Y, -cycloalkylene-S(O)—Y, —S(O2)—Y, -alkylene-S(O2)—Y, -alkylene-cycloalkylene-S(O2)—Y, -cycloalkylene-alkylene-S(O2)—Y, -alkylene-cycloalkylene-alkylene-S(O2)—Y, and -cycloalkylene-S(O2)—Y, wherein Y is as defined herein, and each of said alkylene or cycloalkylene may be unsubstituted or substituted as provided herein; each R3 is independently includes H, alkyl, —O-alkyl, —OH, —N(R9)2, acyl, and aroyl; or the moiety (R3)2, together with the ring carbon atom to which it is shown attached in formula I, defines a carbonyl
    Type: Application
    Filed: April 4, 2005
    Publication date: January 5, 2006
    Inventors: Theodros Asberom, John Clader, Hubert Josien, Mark McBriar, Dmitri Pissarnitski, Zhiqiang Zhao
  • Patent number: 6969719
    Abstract: A polycyclic guanine phosphodiesterase V inhibitor having the formula (I.1) or (II.
    Type: Grant
    Filed: August 26, 2002
    Date of Patent: November 29, 2005
    Assignee: Schering Corporation
    Inventors: Theodros Asberom, Yueqing Hu, Dmitri Pissarnitski, Ruo Xu, Yuguang Wang, Samuel Chackalamannil, John W. Clader, Andrew William Stamford
  • Patent number: 6943171
    Abstract: A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases:
    Type: Grant
    Filed: November 7, 2002
    Date of Patent: September 13, 2005
    Assignee: Schering Corporation
    Inventors: Theodros Asberom, John W. Clader, Yueqing Hu, Dmitri A. Pissarnitski, Andrew W. Stamford, Ruo Xu
  • Publication number: 20050171129
    Abstract: A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases:
    Type: Application
    Filed: December 23, 2004
    Publication date: August 4, 2005
    Inventors: Theodros Asberom, John Clader, Yueqing Hu, Dmitri Pissarnitski, Andrew Stamford, Ruo Xu
  • Publication number: 20050085506
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
    Type: Application
    Filed: September 15, 2004
    Publication date: April 21, 2005
    Inventors: Dmitri Pissarnitski, Hubert Josien, Elizabeth Smith, John Clader, Theodros Asberom, Tao Guo, Douglas Hobbs
  • Publication number: 20040171614
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 1
    Type: Application
    Filed: September 16, 2003
    Publication date: September 2, 2004
    Applicants: Schering-Plough Corporation, Pharmacopeia, Inc.
    Inventors: Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
  • Publication number: 20040048848
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 1
    Type: Application
    Filed: February 5, 2003
    Publication date: March 11, 2004
    Applicant: Schering-Plough Corporation and Pharmacopeia, Inc.
    Inventors: Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
  • Publication number: 20030216380
    Abstract: Novel aryl and heteroaryl sulfonamides are disclosed.
    Type: Application
    Filed: August 1, 2002
    Publication date: November 20, 2003
    Applicant: Schering Corporation
    Inventors: Hubert B. Josien, John W. Clader, Theodros Asberom, Dmitri A. Pissarnitski
  • Publication number: 20030176413
    Abstract: A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases: 1
    Type: Application
    Filed: November 7, 2002
    Publication date: September 18, 2003
    Applicant: Schering Corporation
    Inventors: Theodros Asberom, John W. Clader, Yuequing Hu, Dmitri A. Pissarnitski, Andrew W. Stamford, Ruo Xu
  • Publication number: 20030153587
    Abstract: A polycyclic guanine phosphodiesterase V inhibitor having the formula (I.1) or (II.
    Type: Application
    Filed: August 26, 2002
    Publication date: August 14, 2003
    Applicant: Schering Corporation
    Inventors: Theodros Asberom, Yueqing Hu, Dmitri Pissarnitski, Ruo Xu, Yuguang Wang, Samuel Chackalamannil, John W. Clader, Andrew William Stamford
  • Publication number: 20030135044
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 1
    Type: Application
    Filed: August 1, 2002
    Publication date: July 17, 2003
    Applicant: SCHERING CORPORATION
    Inventors: Theodros Asberom, Henry S. Guzik, Hubert B. Josien, Dmitri A. Pissarnitski
  • Patent number: 6498168
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: December 24, 2002
    Assignee: Schering Corporation
    Inventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
  • Publication number: 20020103205
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) 1
    Type: Application
    Filed: July 11, 2001
    Publication date: August 1, 2002
    Inventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
  • Patent number: 6326380
    Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Q is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is —(CH2)n3—, wherein n3 is 0-5, —CH2—O—, —CH2S—, —CH2—NR6—, —C(O)NR6—, —NR6C(O)—,  optionally substituted alkenyl or optionally substituted alkynyl; X is —O— or —NR6— when the double dotted line represents a single bond, or X is —OH or —NHR20 when the bond is absent; Y is ═O, ═S, (H, H), (H, OH) or (H, C1-C6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is ═O, (H, H), (H, OH), (H, SH) or (H, C1-C
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: December 4, 2001
    Assignee: Schering Corporation
    Inventors: Samuel Chackalamannil, Theodros Asberom, Yan Xia, Dario Doller, Martin C. Clasby, Michael F. Czarniecki
  • Patent number: 6288068
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.
    Type: Grant
    Filed: January 12, 2000
    Date of Patent: September 11, 2001
    Assignee: Schering Corporation
    Inventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Javaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
  • Patent number: 6063847
    Abstract: Heterocyclic-substituted tricyclics of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: the single dotted line represents an optional double bond;the double dotted line represents an optional single bond;n is 0-2;Q is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl;Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group;B is --(CH.sub.2).sub.n3 --, wherein n.sub.3 is 0-5, --CH.sub.2 --O--, --CH.sub.2 S--, --CH.sub.2 --NR.sup.6 --, --C(O)NR.sup.6 --. --NR.sup.6 C(O)--, ##STR2## optionally substituted alkenyl or optionally substituted alkynyl; X is --O-- or --NR.sup.6 -- when the double dotted line represents a single bond, or X is --OH or --NHR.sup.20 when the bond is absent;Y is .dbd.O, .dbd.S, (H, H), (H, OH) or (H, C.sub.1 -C.sub.6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is .dbd.O, (H, H), (H, OH), (H, SH) or (H, C.sub.1 -C.sub.6 alkoxy);R.sup.
    Type: Grant
    Filed: November 23, 1998
    Date of Patent: May 16, 2000
    Assignee: Schering Corporation
    Inventors: Samuel Chackalamannil, Theodros Asberom, Yan Xia, Dario Doller, Martin C. Clasby, Michael F. Czarniecki
  • Patent number: 6043255
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: March 28, 2000
    Assignee: Schering Corporation
    Inventors: Derek B. Lowe, Wei K. Chang, Joseph A. Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W Clader, Samuel Chackalamannil, Yuguang Wang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom, Craig D. Boyle
  • Patent number: 6037352
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.
    Type: Grant
    Filed: November 19, 1998
    Date of Patent: March 14, 2000
    Assignee: Schering Corporation
    Inventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
  • Patent number: 5952349
    Abstract: 1,4 Di-substituted piperidine muscarinic antagonists of formula I ##STR1## or a pharmaceutically acceptable salt, ester, or solvate thereof, wherein X is a bond, --O--, --SO.sub.0-2 --, --CO--, --C(OR.sup.7).sub.2 --, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --, --CH(C.sub.1 --C.sub.6 alkyl)--, --C(C.sub.1 --C.sub.6 alkyl).sub.2 --, --CONR.sup.17 --, --NR.sup.17 CO--, --SO.sub.2 NR.sup.17 -- or --NR.sup.17 SO.sub.2 --; R is C.sub.3 --C.sub.6 cycloalkyl, optionally substituted phenyl or optionally substituted pyridyl; R.sup.1 is H, --CN, --CF.sub.3, alkyl, cycloalkyl, cycloalkenyl, alkenyl, --COR.sup.15, --COO(alkyl, aryl, heteroaryl, alkylaryl or alkylheteroaryl), alkylaryl, alkylheteroaryl or --CON(R.sup.13).sub.2 ; R.sup.2 is cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted 4-piperidinyl; and R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.13, R.sup.15 and R.sup.
    Type: Grant
    Filed: July 8, 1997
    Date of Patent: September 14, 1999
    Assignee: Schering Corporation
    Inventors: Theodros Asberom, Derek B. Lowe, Michael J. Green