Abstract: Combinatorial libraries are disclosed which are represented by Formula I:(T'-L).sub.q -S-C(O)-L'-II' Iwherein:S is a solid support; T'-L- is an identifier residue; and -L'-II' is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: ##STR1## which interact (i.e., as agonists or antagonists) with .alpha. adrenergic receptors, dopamine receptors, .sigma.-opiate receptors, and K.sup.+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatment of ocular diseases such as glaucoma.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
November 18, 1997
Assignee:
Pharmacopeia, Inc.
Inventors:
John J. Baldwin, John C. Reader, Lawrence W. Dillard, Ge Li, Jonathan J. Burbaum, Wenguang Zeng
Abstract: Directly dividing the contents of each sub-pool into the sub-pools for the next step in the synthetic scheme for producing a combinatorial library reduces the standard deviation, .sigma., relative to the standard deviation of the split synthesis method for producing such libraries.
Abstract: A system which precisely arrays small objects into a plurality of containers which comprises a vessel containing the objects in a fluid suspension; a tube, the proximal end of which is positioned substantially at the bottom of the vessel and the distal end of which is connected to a member which directs gravitationally-formed fluid drops from the distal end downward into a container positioned below said distal end; a small-objects detector, for detecting the objects in the fluid in the tube, disposed near the distal end; a drop detector connected to the member below the distal end; a device for controlling flow of the suspension through the tube by pressurizing the vessel; or device for discriminating between those signals from the small-objects detector caused by the small objects and those signals caused by other events, i.e.
Type:
Grant
Filed:
February 26, 1996
Date of Patent:
July 22, 1997
Assignee:
Pharmacopeia, Inc.
Inventors:
Gregory L. Kirk, Joseph J. Brzezinski, Jr., Daniel Chelsky, Thirleen G. Nichols, T. C. Ramaraj
Abstract: Combinatorial libraries are disclosed which are represented by Formula I:(T'--L).sub.q -- S--C(O)--L'--II' Iwherein:S is a solid support; T'--L-- is an identifier residue; and --L'--II' is a ligand/linker residue. Compounds which contain aryl sulfonamides, N-acyl derivatives, and N-substituted pyrrolidines and piperidines of the formula :Y--A--CO--R.sup.1are inhibitors of serine proteases and carbonic anhydrase isozymes. They are useful in the treatment of hyper-coagulation disease and ocular diseases such as glaucoma.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
April 8, 1997
Assignee:
Pharmacopeia, Inc.
Inventors:
John J. Baldwin, Michael H. J. Ohlmeyer, Ian Henderson