Cambridge Enterprise Limited

Centessa Pharmaceuticals (uk) Limited

Tcp Innovations Limited

Z Factor Limited

Centessa Pharmaceuticals Limited

David John Fox

David John Grainger

James Andrew Huntington

Nigel Ramsden

James Michael Tomlinson

David Dept Of Med Cambridge Uni Grainger

The invention relates to specified oxazole compounds of formula (1), and pharmaceutical compositions containing the compounds. The compounds may be inducers of α-antitrypsin (A1AT), and may be used in the treatment of a disease or disorder such as α-antitrypsin deficiency (A1AD or AATD).

Compounds and their use for the treatment of alpha1-antitrypsin deficiency

The invention relates to specified benzamide compounds of formula (1), and pharmaceutical compositions containing the compounds. The compounds may be inducers of α-antitrypsin (A1AT), and may be used in the treatment of a disease or disorder such as α-antitrypsin deficiency (A1AD or AATD).

Compounds and their use for the treatment of ALPHA1-antitrypsin deficiency

The invention relates to oxopyrimidinyl-methyl-benzamide derivatives, for example in a pharmaceutically acceptable salt form or crystal form, pharmaceutical compositions comprising the derivatives, and their medical use, in particular for use in the treatment of α-antitrypsin deficiency (A1AD or AATD).

The invention relates to oxopyrimidinyl-methyl-benzamide derivatives, for example in a pharmaceutically acceptable salt form or crystal form, pharmaceutical compositions comprising the derivatives, and their medical use, in particular for use in the treatment of &#x3b1;-antitrypsin deficiency (A1AD or AATD).

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

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

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. 

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Coventry, United Kingdom

David John Fox