Abstract: This invention relates to compounds of formula (I) and methods of treatment using the compounds. The invention also relates to processes and methods for producing the compounds of the invention. The compounds of the invention are modulators of Factor XII (e.g. Factor XIIa). In particular, the compounds are inhibitors of Factor XIIa and may be useful as anticoagulants.

Abstract: One aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring B is: a monocyclic aromatic group; or a monocyclic or bicyclic heteroaromatic group, each of which is optionally substituted by halo, CN, OH, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, hydroxycycloalkyl, O-cycloalkyl, alkoxy, haloalkoxy, heterocycloalkyl, O-heterocycloalkyl, aryl, heteroaryl, O-aryl, NHCO-alkenyl, NHCO-aryl, —(CH2)q—O-heteroaryl, CONH-aryl, aryloxy-alkyl, O-aralkyl, and CO2-alkyl, wherein said aryl, heteroaryl, heterocycloalkyl, O-cycloalkyl, NHCO-aryl, —(CH2)q—O-heteroaryl, CONH-aryl, aryloxy-alkyl, O-aralkyl, and O-aryl groups are each optionally further substituted by one or more groups independently selected from halo, alkyl, haloalkyl, alkoxy, NHCO-alkyl, NR13R13?, SO2-alkyl, CN, hydroxyalkyl, CONR14R14?, alkyl-NR15R15?, heterocycloalkyl, alkyl-heterocycloalkyl, alkyl-cycloalkyl, aryl, (CH2)m—NHSO2-alkyl, CO2R16, alkoxy-alkyl, haloalkoxy, O-hete

Abstract: The compounds of the invention are modulators of the Factor XII (e.g. Factor XIIa). In particular, the compounds are inhibitors of Factor XIIa and may be useful as anticoagulants.

Abstract: A drug-polymer conjugate, which is a copolymer of at least one monomer of formula (I): (I) where: X may be the same or different at each occurrence and represents a terminal functional group comprising an alkyne or an azide; Q is independently selected at each occurrence and may be present or absent and when present, represents a linking group; R is selected from the group consisting of linear or branched hydrocarbon, optionally substituted aryl and optionally substituted heteroaryl; D is a releasable drug selected from prostaglandins, ?-blockers and mixtures thereof; L is a linker group group; and at least one co-monomer of Formula III III J represents a linking functional group, n is 2 to 8, preferably 3 to 8; Y comprises a polyether of formula (ORa)m wherein Ra is independently ethylene, propylene and butylene and m is from 1 to 300 (preferably 2 to 300) and the polyether is in chain with one or more groups which are preferably selected from one or more of optionally substituted straight or branched Ci to

Abstract: One aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, (I) ring A is an is optionally substituted 5 or 6 membered aromatic or heteroaromatic ring; Y is selected from CH2, C?N—OH, and CR10R10?; Ra and Rb are each independently selected from H and alkyl; Z is selected from O, S, NR17 and CR18; X is selected from O and NH; p is 0, 1 or 2; q is 0 or 1; and r is 0 or 1; wherein at least one of p, q and r is other than zero, and with the proviso that: (i) when r is 0, p is 1 and q is 1, when X is NH, Z is other than O; (ii) when r and q are both 0, and p is 1, Z is not O; R1, R4, and R5 are each independently selected from H, alkyl, alkoxy, OH, F, Cl, Br, and I; R2 and R3 are each independently selected from H, F, Cl, Br, I, CN, methoxy, haloalkyl, haloalkoxy and CO2-alkyl; R10 and R10? are each independently selected from H, F, alkyl, and haloalkyl; R15 and R16 are each independently selected from H, alkoxy, alkyl and OH; R17 is selected from H,

Abstract: Compounds of the formula (I) and pharmaceutically acceptable salts thereof: (I) wherein the substituents are defined in the specification. The compounds are hyperpolarisation activated cyclic-nucleotide modulated ion channel 2 (HCN2) inhibitors. Also disclosed are pharmaceutical compositions comprising the compounds, and the use of the compounds for the treatment or prevention of medical conditions mediated by HCN2, including neuropathic pain.

Abstract: Compounds of the formula (I) and pharmaceutically acceptable salts thereof: (I) wherein the substituents are defined in the specification. The compounds are hyperpolarisation activated cyclic-nucleotide modulated ion channel 2 (HCN2) inhibitors. Also disclosed are pharmaceutical compositions comprising the compounds, and the use of the compounds for the treatment or prevention of medical conditions mediated by HCN2, including neuropathic pain.

Abstract: Compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are defined in the specification. The compounds are hyperpolarisation activated cyclic-nucleotide modulated ion channel 2 (HCN2) inhibitors. Also disclosed are pharmaceutical compositions comprising the compounds, and the use of the compounds for the treatment or prevention of medical conditions mediated by HCN2, including neuropathic pain.

Abstract: The present invention relates to compounds of formula (I) as GPR65 modulators for the treatment of a proliferative disorder, such as e.g. cancer, an immune disorder, asthma, chronic obstructive pulmonary disease (CORD) or acute respiratory distress syndrome (ARDS). Preferred compounds are e.g. N-(Pyridin-2-yl)-6,7,8,9-tetrahydro-5H-5,8-epiminocyclohepta[c]pyridine-10-carboxamide derivatives and similar compounds, such as e.g.

Abstract: One aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring A is a 5 or 6 membered aromatic or heteroaromatic ring, wherein said aromatic or heteroaromatic ring is optionally substituted with one or more substituents selected from F, Cl, Br, I, CN, alkoxy, NR11R11?, OH, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from F, Cl, Br, I, CN, alkoxy, NR11R11?, OH, alkyl, haloalkyl, and aralkyl; Y is selected from C?N—OH and CR10R10?, wherein R10 and R10?, are each independently selected from H, F, alkyl, and haloalkyl; R1, R4, and R5 are each independently selected from H, F, Cl, Br, and I; R2 and R3 are each independently selected from H, F, Cl, Br, I, CN, methoxy, and haloalkyl; and R11 and R11? wherein R12 and R13 are both alkyl; for use as a medicament.

Abstract: A drug-polymer conjugate, which is a copolymer of at least one monomer of formula (I): (I) where: X may be the same or different at each occurrence and represents a terminal functional group comprising an alkyne or an azide; Q is independently selected at each occurrence and may be present or absent and when present, represents a linking group; R is selected from the group consisting of linear or branched hydrocarbon, optionally substituted aryl and optionally substituted heteroaryl; D is a releasable drug selected from prostaglandins, ?-blockers and mixtures thereof; L is a linker group group; and at least one co-monomer of Formula III III J represents a linking functional group, n is 2 to 8, preferably 3 to 8; Y comprises a polyether of formula (ORa)m wherein Ra is independently ethylene, propylene and butylene and m is from 1 to 300 (preferably 2 to 300) and the polyether is in chain with one or more groups which are preferably selected from one or more of optionally substituted straight or branched C1 to

Abstract: A polymer-prostaglandin conjugate comprising: a polymer backbone comprising a plurality of moieties of formula (I): where: T represents a triazole moiety; Q is independently selected at each occurrence and may be present or absent and when present represents a linking group; R is selected from the group consisting of linear or branched hydrocarbon; D is selected from prostaglandins; and L is a group of formula (II) wherein R5 is selected from hydrogen and C1 to C6 alkyl; (R) indicates the end of the group bonded to the R group; and (D) indicates the end of the group attached to the group D.

Abstract: The present invention relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring A is a 5- or 6-membered monocyclic aromatic or heteroaromatic ring, or a 9- or 10-membered bicyclic aromatic or heteroaromatic ring, each of which is optionally substituted with one or more substituents selected from F, Cl, Br, I, CN, alkoxy, NR11R11?, OH, SO2-alkyl, CO2-alkyl, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from F, Cl, Br, I, CN, alkoxy, NR11R11?, OH, alkyl, haloalkyl, and aralkyl; Y and Z are each independently CR10R10?, wherein R10 and R10? are each independently selected from H, F, alkyl, and haloalkyl; R1, R4, and R5 are each independently selected from H, F, Cl, Br, I and haloalkyl; R2 and R3 are each independently selected from H, F, Cl, Br, I, CN, and haloalkyl; wherein at least two of R2, R3 and R4 are other

Abstract: A drug-polymer conjugate, which is a copolymer of at least one monomer of formula (I) where: X may be the same or different at each occurrence and represents a terminal functional group comprising an alkyne or an azide; Q is independently selected at each occurrence and may be present or absent and when present, represents a linking group; R is selected from the group consisting of linear or branched hydrocarbon, optionally substituted aryl and optionally substituted heteroaryl; D is a releasable bicyclic prostaglandin; L is a linker group; and at least one co-monomer of Formula III J-(Y1-A)n, J represents a linking functional group, n is 2 to 8 preferably 3 to 8; Y1 comprises a polyether of formula (ORa)m wherein Ra is independently ethylene, propylene and butylene and m is from 1 to 300 (preferably 2 to 300) and the polyether is in chain with one or more groups which are preferably selected from one or more of optionally substituted straight or branched C1 to C10 alkylene, amino, ether, ester, amide, carbon

Abstract: This invention relates to compounds of formula (I) and methods of treatment using the compounds. The invention also relates to processes and methods for producing the compounds of the invention. The compounds of the invention are modulators of Factor XII (e.g. Factor XIIa). In particular, the compounds are inhibitors of Factor XIIa and may be useful as anticoagulants.

Abstract: A polymer-prostaglandin conjugate comprising: a polymer backbone comprising a plurality of moieties of formula (I): where: T represents a triazole moiety; Q is independently selected at each occurrence and may be present or absent and when present represents a linking group; R is selected from the group consisting of linear or branched hydrocarbon; D is selected from prostaglandins; and L is a group of formula (II) wherein R5 is selected from hydrogen and C1 to C6 alkyl; (R) indicates the end of the group bonded to the R group; and (D) indicates the end of the group attached to the group D.

Abstract: A polymer-prostaglandin conjugate comprising: a polymer backbone comprising a plurality of moieties of formula (I): where: T represents a triazole moiety; Q is independently selected at each occurrence and may be present or absent and when present represents a linking group; R is selected from the group consisting of linear or branched hydrocarbon; D is selected from prostaglandins; and L is a group of formula (II) wherein R5 is selected from hydrogen and C1 to C6 alkyl; (R) indicates the end of the group bonded to the R group; and (D) indicates the end of the group attached to the group D.

Abstract: This invention relates to compounds of formula (I). The compounds of formula (I) are modulators of Factor XII, specifically Factor XIIa. The compounds are inhibitors of Factor XIIa and may be useful as anticoagulants. The compounds of formula (I) may be used in methods of treatment (or prevention) of blood disorders related to bleeding or coagulation.

Abstract: The invention is directed to compounds of general formula (I) and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.

Abstract: The invention is directed to compounds of general formula (I) and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.