Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formula IIIB have the structure:
wherein
R1, R2, R, Ar
and n are as described in the specification.
Type:
Grant
Filed:
May 15, 2002
Date of Patent:
June 15, 2004
Assignee:
Adolor Corporation
Inventors:
Virendra Kumar, Deqi Guo, Michael Anthony Marella, Alan L. Maycock
Abstract: Compositions and methods using the compositions for treatment of peripheral hyperalgesia are provided. The compositions contain an anti-hyperalgesia effective amount of one or more compounds that directly or indirectly interact with peripheral opiate receptors, but that do not, upon topical or local administration, elicit substantial central nervous system effects. The anti-diarrheal compound 4-(p-chlorophenyl)-4-hydroxy-N-N-dimethyl-&agr;,&agr;-diphenyl-1-piperidinebutyramide hydrochloride is preferred for use in the compositions and methods.
Type:
Grant
Filed:
August 16, 1999
Date of Patent:
June 3, 2003
Assignees:
Adolor Corporation, The Regents of the University of California
Abstract: Novel methods for the treatment and/or prevention of ileus. The methods may comprise administering to a patient an effective amount of a peripheral mu opioid antagonist compound. Preferred compounds for use in the methods include piperidine-N-alkylcarboxylates, quaternary morphinans, opium alkaloid derivatives and quaternary benzomorphans. The methods are particularly suitable for treating and/or preventing postsurgical ileus and postpartum ileus.
Type:
Application
Filed:
June 13, 2002
Publication date:
December 12, 2002
Applicant:
Adolor Corporation
Inventors:
John J. Farrar, Peter J. Schied, William K. Schmidt, Randall L. Carpenter
Abstract: Method for the prevention or treatment of pruritus with anti-pruritic compounds is provided.
The compounds of formulae I, II, IIA, III, IIIA, IV and IVA have the structure:
wherein
R1, R2, R3, R4; and
X, X4, X5, X7, X9;
Y, Z and n are as described in the specification.
Type:
Grant
Filed:
March 13, 2001
Date of Patent:
November 5, 2002
Assignee:
Adolor Corporation
Inventors:
Wei Yuan Zhang, Alan L. Maycock, Anthony Michael Marella, Virendra Kumar, Forrest Gaul, Deqi Guo
Abstract: Methods for the treatment and/or prevention of ileus are disclosed. The methods comprise administering to a patient an effective amount of a peripheral mu opioid antagonist compound. Preferred compounds for use in the methods include piperidine-N-alkylcarboxylates.
Type:
Grant
Filed:
November 29, 2000
Date of Patent:
October 22, 2002
Assignee:
Adolor Corporation
Inventors:
John J. Farrar, Peter J. Schied, William K. Schmidt, Randall L. Carpenter
Abstract: Novel methods and compositions comprising opioids and opioid antagonists. In preferred embodiments, the methods and compositions comprise opioids and peripheral mu opioid antagonist compounds. The methods and compositions are particularly suitable for treating and/or preventing side effects associated with opioids including, for example, constipation, vomiting and/or nausea.
Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided.
The compounds of formulae I, II, IIA, III, IIIA, IV and IVA have the structure:
wherein
R1, R2, R3, R4; and
X, X4, X5, X7, X9;
Y, Z and n are as described in the specification.
Type:
Grant
Filed:
January 6, 2000
Date of Patent:
May 21, 2002
Assignee:
Adolor Corporation
Inventors:
Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, An-Chih Chang, Deqi Guo
Abstract: Compounds having kappa opioid agonist activity, compositions containing them and 5 method of using them as analgesics and pruritic agents are provided.
Type:
Application
Filed:
January 26, 2001
Publication date:
April 11, 2002
Applicant:
Adolor Corporation
Inventors:
Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang
Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided.
The compounds of formula having the structure:
wherein
R1, R2, and X Y, Z, Ar and n are as described in the specification.
Type:
Grant
Filed:
September 9, 1998
Date of Patent:
October 16, 2001
Assignee:
Adolor Corporation
Inventors:
Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, An-Chih Chang, Deqi Guo
Abstract: Method for the prevention or treatment of pruritis by administering to a patient an antipruritic compound, or pharmaceutically acceptable salt thereof, of the class arylacetamide, which is exemplified by compounds of the formulae I, II, IIA, III, IV and IVA having the structures:
and in which R1-4, X, X4, X5, X7, X9, Y and Z are as described in the specification.
Type:
Grant
Filed:
August 11, 1999
Date of Patent:
May 29, 2001
Assignee:
Adolor Corporation
Inventors:
Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, Deqi Guo
Abstract: The present invention provides a number of screening methods for evaluating compounds capable of suppressing cytokine production either in vitro or in vivo. The methods generally involve stimulating the production of a cytokine in a cell, exposing a portion of the cells to a putative cytokine modulating agent and determining subsequent levels of cytokine production in the cells. Additionally, the present invention provides certain compounds identified by this method.
Abstract: Compounds having kappa opioid agonist activity, compositions containing them and methods of using them as analgesics and anti-pruritic agents are provided.
The compounds of formula IV have the structure:
wherein
X9;
R1, R2, R3, R4; and
n are as described in the specification.
Type:
Grant
Filed:
November 8, 1999
Date of Patent:
January 30, 2001
Assignee:
Adolor Corporation
Inventors:
Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang
Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided.The compound of formula I, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;X; and ArY, Z and n are as described in the specification.
Type:
Grant
Filed:
October 30, 1998
Date of Patent:
May 2, 2000
Assignee:
Adolor Corporation
Inventors:
Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, An-Chih Chang, Deqi Guo
Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compound of formulae IIA, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;X.sub.4, X.sub.5 ; andAr and n are as described in the specification.
Type:
Grant
Filed:
May 7, 1999
Date of Patent:
April 25, 2000
Assignee:
Adolor Corporation
Inventors:
Wei Yuan Zhang, Alan L. Maycock, Michael Anthony Marella, Virendra Kumar, Forrest Gaul, An-Chih Chang, Deqi Guo
Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.
Type:
Grant
Filed:
October 4, 1999
Date of Patent:
April 11, 2000
Assignee:
Adolor Corporation
Inventors:
John J. Farrar, An-Chih Chang, Virendra Kumar, Wei Yuan Zhang, Alan Cowan
Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided.The compounds of formula III having the structure: ##STR1## wherein Ar and X.sup.7 ;R.sub.1 and R.sub.2 ; andn are as described in the specification.
Type:
Grant
Filed:
May 7, 1999
Date of Patent:
February 22, 2000
Assignee:
Adolor Corporation
Inventors:
Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang
Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided.
The compounds of formulae I, II, III and IV have the structure:
wherein:
X, X4, X5, X7, X9;
R1, R2, R3, R4; and
Y, Z and n are as described in the specification.
Type:
Grant
Filed:
February 4, 2002
Date of Patent:
June 3, 2003
Assignee:
Adolor Corporation
Inventors:
Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang