Abstract: Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a linked cyclic polyamine derivative.
Abstract:
Compounds of structure (1) are obtained by reduction of compounds of the structures
Compounds of structure (1), especially where Z is a hydrogen atom or a 3,4-methylenedioxyphenyl group, are important intermediates for inter alia paroxetine.
Type:
Grant
Filed:
May 29, 1998
Date of Patent:
December 3, 2002
Assignee:
SmithKline Beecham plc
Inventors:
Victor Withold Jacewicz, Marvin Sungwhan Yu, Evgeny Shapiro
Abstract: Dimeric cell-surface receptors in a subject are agonized by administering a metal chelated dimeric cell-surface receptor ligand formed by chelating a receptor binding moiety with a metal ion such as zinc, or by co-administering the receptor binding moiety and the metal ion. The binding moiety is a small organic molecule having a molecular weight of from about 100 to about 850, and metal chelation may form a symmetrical multimer such as a dimer of the receptor binding moiety. An example is bis{2,5-bis[2-benzimidazolylimino]-3a,6a-bis(2-pyridyl)-1,2,3,3a,4,5,6,6a-octahydroimidazo[4,5-d]imidazole-N,N′}-zinc(II). Dimeric cell surface receptors include granulocyte colony-stimulating factor, erythropoeitin receptor, macrophage-colony-stimulating factor, growth hormone receptor, thrombopoietin receptor, interferon alpha receptor, interferon beta receptor, tyrosine kinase receptor, insulin receptor and leptin receptor.
Abstract: A mixture of beads of uniform size from is deposited in an array by establishing discrete attachment areas each consisting either of a droplet of adhesive or a small area of a continuous adhesive layer exposed through an aperture in a mask. Beads which are trapped by the attachment areas are released either by a solvent on a vacuum manifold, or by evaporation of the adhesive, preferably by means of a vacuum centrifuge. The beads are released into capillaries, in which cleavage of attached compounds, or synthesis of new compounds, can be carried out. Also invented is the apparatus used in carrying out the invention.
Abstract: A method for treating and/or preventing cardiac disorders in human or non-human animals comprises administering an effective, non-toxic amount of an SSRI or a pharmaceutically acceptable salt thereof, to a human or non-human animal in need thereof.
Abstract: A process for preparing controlled release solid dosage forms of lithium carbonate by using a dissolution rate stabilizer and a hydrophobic waxy material.
Type:
Grant
Filed:
May 18, 2000
Date of Patent:
April 2, 2002
Assignee:
SmithKline Beecham Corporation
Inventors:
Gopadi M. Venkatesh, Nageswara R. Palepu
Abstract: Invented are G-CSF mimetics. Also invented are selected octacyclic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds as G-CSF mimetics. Also invented are novel processes used in preparing these compounds.
Abstract: The present invention is directed to a method for promoting somking cessation or reduction or preventing relapse smoking, comprising administering an effective, non-toxic amount of paroxetine or a pharmaceutically acceptable salt or solvate thereof, to a human in need thereof.
Abstract: Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentano[b]pyridine derivatives. The most preferred compounds prepared by this invention are (+)(1S, 2R, 3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S, 2R, 3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.
Type:
Grant
Filed:
March 8, 2000
Date of Patent:
September 11, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
Yemane Woldeselassie Andemichael, Neil Howard Baine, William Morrow Clark, Conrad John Kowalski, Michael Anthony McGuire, Robert John Mills
Abstract: The invention describes zinc chelated dimeric cell-surface receptor ligands, pharmaceutical compositions containing these compounds, methods of using these compounds as agonist of dimeric cell-surface receptors. Novel processes used in preparing the compounds are also described. Further, the invention describes novel receptor binding moieties of the zinc chelated cell-surface receptor ligands.
Abstract: Invented is a method of preparing combinatorial libraries and combinatorial libraries prepared thereby. Also invented is a method for identifying compounds having desired characteristics from a combinatorial library or a set of combinatorial libraries by the use of flow cytometry. Also invented is a method for encoding combinatorial libraries using fluorophore labeled beads.
Type:
Grant
Filed:
November 22, 1996
Date of Patent:
April 3, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
Dennis Shinji Yamashita, Joseph Weinstock
Abstract: Cyclic penta- and hexa-peptide libraries containing one or more known amino acids, one or more randomized amino acids and a conformationally constraining element are disclosed. These peptide libraries may be used for screening for new bioactive peptides and for elucidating structural information pertinent to drug design.
Type:
Grant
Filed:
January 5, 1996
Date of Patent:
February 27, 2001
Assignee:
SmithKline Beecham Corporation
Inventors:
William Francis Huffman, Michael Lee Moore
Abstract: Compounds of structure (2) are prepared by reaction of an arecoline analogue of structure(4) with an organometallic compound containing an X-substituted phenyl group, such as a compound of structure (3).
Suitably the compound of structure (3) is a Grignard reagent, where M is magnesium and Y is a halogen atom, or M may be a Group II metal and Y is a halogen atom or a second X-substituted phenyl group. When structure (3) is a Grignard reagent, the reaction is carried out either in a suitable non-ether solvent, typically a hydrocarbon or a non-reactive chlorinated hydrocarbon, or in a mixture of such a solvent with diethyl ether. Compounds of structure (2) are important intermediates in the preparation of inter alia paroxetine.
Abstract: Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentano[b]pyridine derivatives. The most preferred compounds prepared by this invention are (+)(1S, 2R, 3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphen yl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S, 2R, 3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyphenyl)-5-(p rop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.
Type:
Grant
Filed:
May 8, 1998
Date of Patent:
November 14, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
Yemane Woldeselassie Andemichael, Neil Howard Baine, William Morrow Clark, Conrad John Kowalski, Michael Anthony McGuire, Robert John Mills
Abstract: Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentanopyridine derivatives. The most preferred compounds prepared by this invention are (+)(1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylen edioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S,2R,3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyph eyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.
Type:
Grant
Filed:
February 4, 1997
Date of Patent:
November 7, 2000
Assignee:
SmithKline Beecham Corporation
Inventors:
William Morrow Clark, Ivan Lantos, Robert John Mills, Lendon Norwood Pridgen, Ann Marie Tickner