CHROMA THERAPEUTICS LTD. Patent applications |
Patent application number | Title | Published |
20150368210 | 2-AMINOPYRAZINE DERIVATIVES AS CSF-1 R KINASE INHIBITORS - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein: ring A, R | 12-24-2015 |
20150246883 | TERT-BUTYL N-[2-ETHYL]-L-ALANINATE OR A SALT, HYDRATE OR SOLVATE THEREOF - The present invention provides a compound which is: tert-butyl N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alaninate or a salt, hydrate or solvate thereof. The present invention also provides a pharmaceutical composition comprising the compound together with one or more pharmaceutically acceptable carriers and/or excipients. The compound and composition are useful for inhibiting the activity of a p38 MAP kinase enzyme. As such they may be used in the treatment of a autoimmune or inflammatory disease, or a cell proliferative disease. In addition, the invention provides an acid produced by hydrolysis of the ester group of the compound of the invention. The acid is N-[2-{4-[6-amino-5-(2,4-difluorobenzoyl)-2-oxopyridin-1(2H)-yl]-3,5-difluorophenyl}ethyl)-L-alanine. | 09-03-2015 |
20140163042 | ENZYME INHIBITORS - Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R | 06-12-2014 |
20140155439 | ENZYME INHIBITORS - Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH | 06-05-2014 |
20140088159 | ENZYME AND RECEPTOR MODULATION - Covalent conjugates of an α,α-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the α,α-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells. | 03-27-2014 |
20140010762 | IMAGING AGENTS - An imaging agent for cells which produces an intracellular imaging signal proportional to the amount of hCE-1 in the cells independently of the amount of hCE-2 and/or hCE-3 in the cells, said imaging agent being a covalent conjugate of (a) an imaging agent and (b) an alpha mono- or di-substituted amino acid ester, wherein (a) is directly linked to (b), or (a) is indirectly linked to (b) by a linker radical, and wherein said direct or indirect linkage is via the amino group of (b), and wherein the amino group is not directly linked to a carbonyl group, and wherein the said alpha mono- or di-substituted amino acid ester part is selectively hydrolysable to the corresponding carboxylic acid part by the intracellular carboxylesterase enzyme hCE-1 relative to the intracellular enzymes hCE-2 or hCE-3. | 01-09-2014 |
20130116318 | Enzyme Inhibitors - Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: | 05-09-2013 |
20120149736 | ENZYME INHIBITORS - Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH | 06-14-2012 |
20110190306 | Inhibitors of PLK - Compounds of formula (I) are PLK inhibitors, useful for the treatment of cell proliferative diseases: wherein R | 08-04-2011 |
20110046210 | SUBSTITUTED THIOPENECARBOXAMIDES AS IKK-BETA SERINE-, THREONINE-PROTEIN KINASE INHIBITORS - Compounds of formula (IA) or (IB) are IKK inhibitors useful in the treatment of autoimmune and inflammatory diseases: wherein R | 02-24-2011 |
20110039920 | INHIBITORS OF IKK-BETA SERINE-THERONINE PROTEIN KINASE - Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5(carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl(25,4E)-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-2-methylphenyl}pent-4-enoate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate; and tert-Butyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKKβ activity. | 02-17-2011 |
20100317678 | HYDROXAMATES AS INHIBITORS OF HISTONE DEACETYLASE - Compounds of formula (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: | 12-16-2010 |
20100267774 | P38 MAP KINASE INHIBITORS - Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: formula (I) wherein: G is —N═ or —CH═; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R | 10-21-2010 |
20100216802 | PTERIDINE DERIVATIVES AS POLO-LIKE KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER - Compound of formula (I) are inhibitors of Polo-like kinases (PLKs), and are useful in treatment of cell proliferative diseases: | 08-26-2010 |
20100152155 | Histone Deacetylase Inhibitors - Compounds of formula: (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: (I) wherein Q, V and W independently represent —N═ or —C═; B is a divalent radical selected from: (IIA), (IIB), (IIC), (IID), and (IIE). Wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; and -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical. | 06-17-2010 |
20100069473 | Inhibitors Of IKK-Beta Serine-Threonine Protein Kinase - Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: | 03-18-2010 |
20100010057 | THIAZOLE DERIVATIVES AS INHIBITORS OF P13 KINASE - Compounds of formula (I) are inhibitors of P13 kinase activity, and useful in treatment of, inter alia, autoimmune, inflammatory and proliferative diseases: wherein: s is 0 or 1; U is hydrogen or halogen; X is —(C═O), an optionally substituted divalent phenylene, pyridinylene, pyrimidinylene, or pyrazinylene radical, or a bond; P is optionally substituted C | 01-14-2010 |
20100010010 | HDAC INHIBITORS - Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent ═C— or ═N—; W is a divalent radical —CH═CH— or CH | 01-14-2010 |
20100004250 | PTERIDINE DERIVATIVES AS POLO-LIKE KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER - Compounds of formula (I) are inhibitors of Polo-like kinases (PLKs), and are useful, inter alia, in the treatment of proliferative diseases: | 01-07-2010 |
20090298924 | HYDROXAMIC ACID DERIVATIVES AS INHIBITORS OF HDAC ENZYMATIC ACTIVITY - Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: | 12-03-2009 |
20090291978 | Enzyme Inhibitors - Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R | 11-26-2009 |
20090215800 | Enzyme and Receptor Modulation - Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator. | 08-27-2009 |
20090203711 | Inhibitors of P38 Map Kinase - Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: | 08-13-2009 |
20090131461 | Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity - Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y | 05-21-2009 |
20090099185 | P38 Map Kinase Inhibitors - Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: | 04-16-2009 |