Abstract: This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.
Type:
Grant
Filed:
September 12, 2002
Date of Patent:
November 30, 2004
Assignee:
Anormed, Inc.
Inventors:
Ernest J. McEachern, Gary J. Bridger, Krystyna Skupinska, Renato T. Skerlj
Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.
Type:
Grant
Filed:
May 9, 2002
Date of Patent:
June 29, 2004
Assignee:
AnorMed, Inc.
Inventors:
Gary James Bridger, Eva Maria Boehringer, Zhongren Wang, Dominique Schols, Renato Tony Skerlj, David Earl Bogucki
Abstract: This invention relates to a novel class of heterocyclic compounds that bind chemokine receptors, inhibiting the binding of their natural ligands thereby. These compounds result in protective effects against infection by HIV through binding to chemokine receptors, including CXCR4 and CCR5, thus inhibiting the subsequent binding by these chemokines.
Type:
Grant
Filed:
March 24, 2000
Date of Patent:
June 15, 2004
Assignee:
AnorMED, Inc.
Inventors:
Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols
Abstract: Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole.
Type:
Grant
Filed:
March 28, 2002
Date of Patent:
May 11, 2004
Assignee:
AnorMED, Inc.
Inventors:
Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bern Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis, Rosaria Maria Di Fluri
Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.
Type:
Grant
Filed:
July 8, 1998
Date of Patent:
January 14, 2003
Assignee:
AnorMED, Inc.
Inventors:
Gary James Bridger, Eva Maria Boehringer, Zhongren Wang, Dominique Schols, Renato Tony Skerlj, David Earl Bogucki
Abstract: Cyclic polyamines containing N nitrogens on the ring are protected with high yields in a N-1 manner, e.g. all protected but one amino group, by using certain fluoro-containing agents that offer easy deprotection. Preferably, a new process for preparing 1,1′-[1,4-phenylenebis (methylene)]-bis1,4,8,11-tetraazacyclotetradecane is disclosed.
Abstract: New pharmaceutical compositions and pharmaceutical compositions comprising metal complexes have activity against diseases caused by or related to overproduction or localized high concentration of nitric oxide in the body.
Type:
Grant
Filed:
March 9, 2001
Date of Patent:
July 9, 2002
Assignee:
AnorMED Inc.
Inventors:
Michael J Abrams, Simon P Fricker, Barry A Murrer, Owen J Vaughan
Abstract: New pharmaceutical compositions and pharmaceutical compositions comprising metal complexes have activity against diseases caused by or related to overproduction or localised high concentration of nitric oxide in the body.
Type:
Grant
Filed:
October 19, 1998
Date of Patent:
September 4, 2001
Assignee:
AnorMED Inc.
Inventors:
Michael J Abrams, Simon P Fricker, Barry A Murrer, Owen J Vaughan
Abstract: Bifunctional aromatic compounds which are capable of linking metal ions to biologically useful molecules. The bifunctional compounds are characterized as having a hydrazine or hydrazide group and a protein reactive group. The hydrazine or hydrazide group may be protected as a lower alkyl hydrazone. Conjugates of the bifunctional compounds with macromolecules are also described and labelled macromolecules comprised of the conjugates and metal ions are provided. Additionally, a method is provided for forming a labelled macromolecule by reacting a conjugate with a metal species. The compounds and method of this invention are particularly useful in the fields of biology and medicine for imaging and/or therapy.
Type:
Grant
Filed:
November 6, 1997
Date of Patent:
April 17, 2001
Assignee:
AnorMed, Inc.
Inventors:
David A. Schwartz, Michael J. Abrams, Christen M. Giandomenico, Jon A. Zubieta
Abstract: A pharmaceutical composition containing a non-specific (NS) suppressor cell inducing compound and cyclosporin A and a pharmaceutically acceptable carrier or diluent, and method of inducing an immunosuppressive effect in a mammal, including a hyman, in need thereof which comprises administering an effective dose of a non-specific suppressor cell inducing compound and cyclosporin A to such mammal.
Abstract: Invented is a method of treating asthma, in mammals, including humans, which comprises administering to such human an effective amount of a substituted azaspirane.
Type:
Grant
Filed:
January 15, 1999
Date of Patent:
February 15, 2000
Assignee:
AnorMed, Inc.
Inventors:
Alison Mary Badger, John Gerald Gleason
Abstract: Pharmaceutical compositions containing as active ingredients a linked cyclic compound of the general formula IZ--(A).sub.n --Y (I)in which Z and Y are independently cyclic polyamine moieties having from 9 to 32 ring members and from 3 to 8 amine nitrogen atoms in the ring, A is a linking atom or group, and n is O or an integer from 1 to 6, are indicated for the treatment of viral infections, and preventative administration, especially for retroviral infections.
Abstract: Invented is a method of treatment of psoriasis in a mammal in need thereof which comprises administering to such mammal an effective amount of a substituted azaspirane.
Abstract: Selected lanthanum carbonate hydrates may be administered into the gastrointestinal tract, to treat hyperphosphataemia in patients with renal failure.
Abstract: The present invention is directed to an improved antihyperlipidemic agent, the dimaleate salt of 2-?2-(dimethylamino)ethyl!-8,8-dipropyl-2-azaspiro?4.5!decane.