Abstract: The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.

Abstract: The invention relates to methods for treating chronic lung disease, in particular, alpha-1 antitrypsin deficiency or emphysema resulting from alpha-1 antitrypsin deficiency, with a neutrophil elastase inhibitor. The invention further relates to pharmaceutical compositions comprising a neutrophil elastase inhibitor.

Abstract: The invention relates to 4-(4-Cyano-2-thioaryl)dihydropyrimidinones of the formula (I) known from WO 2009/080199(A1) for use in a method for the treatment and/or recurrence rate reduction of a chronic wound selected from different types of ulcers and a chronic wound associated with Behçet's disease wherein the compound of the formula (I) is administered orally and wherein the treatment and/or reduction of recurrence rate of the chronic wound causes one or more of the effects selected from an increased wound closure rate, a reduced wound size, a shorter time to wound closure, an increase of the reepithelialisation of the chronic wound, an increase of the deposition of extracellular matrix such as collagen in the chronic wound, and a reduction of pain related to the chronic wound. The invention further relates to compounds of the formula (I) for use in a method for the treatment of neutrophilic dermatoses or for use in a method for the treatment of autoimmune blistering dermatoses.

Abstract: The invention relates to methods for treating chronic liver disease, in particular nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH), with neutrophil elastase inhibitors. The invention further relates to pharmaceutical compositions comprising neutrophil elastase inhibitors.

Abstract: The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.

Abstract: The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.

Abstract: The invention relates to methods for treating chronic liver disease, in particular nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH), with neutrophil elastase inhibitors. The invention further relates to pharmaceutical compositions comprising neutrophil elastase inhibitors.

Abstract: The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.

Abstract: The invention relates to a new and improved method for preparation of (4S)-4-[4-cyano-2-(methyl sulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I), as well as the preparation and use of the crystal form (A) of (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I).

Abstract: The invention relates to methods for treating chronic liver disease, in particular nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH), with neutrophil elastase inhibitors. The invention further relates to pharmaceutical compositions comprising neutrophil elastase inhibitors.

Abstract: The invention relates to a new and improved method for preparation of (4S)-4-[4-cyano-2-(methyl sulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I), as well as the preparation and use of the crystal form (A) of (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I).

Abstract: The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.

Abstract: The present invention concerns a new and improved method for preparation of (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluormethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I), as well as the preparation and use of the crystal form (A) of (4S)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluormethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile of formula (I).

Abstract: The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.

Abstract: The invention relates to 4-(4-Cyano-2-thioaryl)dihydropyrimidinones of the formula (I) known from WO 2009/080199(A1) for use in a method for the treatment and/or recurrence rate reduction of a chronic wound selected from different types of ulcers and a chronic wound associated with Behçet's disease wherein the compound of the formula (I) is administered orally and wherein the treatment and/or reduction of recurrence rate of the chronic wound causes one or more of the effects selected from an increased wound closure rate, a reduced wound size, a shorter time to wound closure, an increase of the reepithelialisation of the chronic wound, an increase of the deposition of extracellular matrix such as collagen in the chronic wound, and a reduction of pain related to the chronic wound. The invention further relates to compounds of the formula (I) for use in a method for the treatment of neutrophilic dermatoses or for use in a method for the treatment of autoimmune blistering dermatoses.