Neorx Corporation

Cambridge Enterprise Limited

Cambridge University Technical Services Limited

Tcp Innovations Limited

Other

Poniard Pharmaceuticals, Inc.

Noerx Corporation

David John Grainger

James C Metcalfe

Peter L Weissberg

David John Fox

Lawrence L Kunz

Lauren Marie Tatalick

Sudhakar Kasina

John M Reno

Richard A Klein

Robert W Schroff

Peter G Anderson

Paul R Kemp

Suzanne T Kanaly

Jeremy Kirk Nicholson

Elaine Holmes

Timothy David Spector

John Christopher Lindon

Kirsten Heathcote

Joanne Tracey Brindle

The invention relates to 3-(2',2&#x2032;-dimethylpropanoylamino)-tetrahydropyridin-2-one, and its pharmaceutical compositions and its use for preparing a medicament intended to prevent or treat inflammatory disorders.

Treatment of rheumatoid arthritis with 3-amino lactam compounds

The invention provides compounds of general formulae (I)-(IV) or pharmaceutically acceptable salts thereof:  The invention also provides methods of preparing the compounds, pharmaceutical compositions comprising the compounds and use of the compounds for the preparation of medicaments intended to modulate the activity of one or more members of the G-protein coupled receptor (GPCR) class. Compounds of the invention may be used to create a compound library for use in screening for agents which modulate signalling through GPCRs.

Ligand libraries for screening GPCRs

The invention provides compounds, compositions and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder: wherein

3-aminocaprolactam compounds for treating inflammatory disorders

Isolated and purified chemokine peptides, variants, and derivatives thereof, as well as chemokine peptide analogs, are provided.

Compounds to inhibit or augment an inflammatory response

The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (I) wherein

&#x3b1;-aminocyclolactam ligands for G-protein coupled receptors, and methods of using same

The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(1'-methylcyclohexylcarbonylamino)-caprolactam: wherein

Anti-inflammatory agents

The invention provides low molecular weight apoE mimetic agents suitable for preparing a medicament to treat autoimmune, inflammatory or neurodegenerative disease, (X)-L-(X)(Formula (I)) wherein each X is a (potentially different) chemical moiety bearing a positive charge at physiological pH a and b are, independently, numbers between 3 and 6; and L is a linker. 

ApoE mimetic agents

The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (I) wherein y is any integer from 1 to 8; z is one integer from 0 to 8 with the proviso that y and z cannot simultaneously be 1; X is &#x2014;CO&#x2014;(Y)&#x2014;(R)or SO&#x2014;(Y)&#x2014;(R); k is 0 or 1; y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or y is a cycloalkenyl or polycycloalkenyl group; each Ris independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl, alkylamino, alkylaminoalkyl, alkylaminodialkyl, charged alkylaminotrialkyl or charged alkylcarboxylate radical of 1 to 20 carbon atoms; or each Ris independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl, aminodialkyl, charged aminotrialkyl, or carboxylate radical; and n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y; or alternatively Rmay be selected from a peptido radical, for example having from 1 to 4 peptidic moieties linked together by peptide bonds (for example a peptido radical of 1 to 4 amino acid residues). 

&#x3b1;-aminocyclolactam ligands for G-protein coupled receptors

The invention provides compounds, compositions, and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, for the preparation of a medicament intended to treat an inflammatory disorder wherein y is any integer from 1 to 8; z is any integer from 1 to 8; with the proviso that y and z cannot both equal 1; X is &#x2014;C &#x2014;(Y)&#x2014;(R)or SO&#x2014;(Y)&#x2014;(R); k is 0 or 1; Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or Y is a cycloalkenyl or polycycloalkenyl group. 

Anti-inflammatory A-aminocyclolactam compounds

Methods to inhibit or augment an inflammatory response

This invention pertains to chemometric methods for the analysis of chemical, biochemical, and biological data, for example, spectral data, for example, nuclear magnetic resonance (NMR) spectra, and their applications, including, e.g., classification, diagnosis, prognosis, etc., especially in the context of bone disorders, e.g., conditions associated with low bone mineral density, e.g., osteoporosis.

Methods for the diagnosis and treatment of bone disorders

The invention relates to the use of 3-(2',2&#x2032;-dimethylpropanoylamino)-tetrahydropyridin-2-one for preparing a medicament intended to prevent or treat inflammatory disorders.

Methods of using anti-inflammatory compounds

The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(r-methylcyclohexyl-carbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is &#x2014;CO&#x2014; or &#x2014;SO2-; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, haloalkyl, aryl or substituted aryl; Tand Ttogether constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by Tand Tmay be independently be substituted by a group R, where Ris independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each Ris independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radical. 

Isolated and purified chemokine peptides, variants, and derivatives thereof, as well as chemokine peptide analogs, are provided. For example, the invention provides peptides of no more than 15 amino acid residues which include chemokine peptide sequences and variants thereof, as well as cyclic reverse derivatives thereof, which inhibit the activity of at least one chemokine.

Compounds and methods to inhibit or augment an inflammatory response

The invention provides compounds, compositions and uses of compounds of general formula (I) or (I'), or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder.

Growing community of inventors

Cambridge, United Kingdom

David John Grainger